Ofloxacine Ranbaxy

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Ofloxacin

Ofloxacin is reported as an ingredient of Ofloxacine Ranbaxy in the following countries:

• France

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Neoperidol may be available in the countries listed below.

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Haloperidol

Haloperidol decanoate (a derivative of Haloperidol) is reported as an ingredient of Neoperidol in the following countries:

• Japan

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Mono Mack retard

Mono Mack retard may be available in the countries listed below.

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Isosorbide Mononitrate

Isosorbide Mononitrate is reported as an ingredient of Mono Mack retard in the following countries:

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Napromed may be available in the countries listed below.

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Naproxen

Naproxen is reported as an ingredient of Napromed in the following countries:

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Naphazoline Hydrochloride

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Naphazoline

Naphazoline Hydrochloride (BANM, USAN) is known as Naphazoline in the US.

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Glossary

BANM	British Approved Name (Modified)
USAN	United States Adopted Name

Click for further information on drug naming conventions and International Nonproprietary Names.

Ranitidine Biostam

Ranitidine Biostam may be available in the countries listed below.

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Ranitidine

Ranitidine hydrochloride (a derivative of Ranitidine) is reported as an ingredient of Ranitidine Biostam in the following countries:

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Nicotinell Lutschtabletten may be available in the countries listed below.

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Nicotine

Nicotine bitartrate dihydrate (a derivative of Nicotine) is reported as an ingredient of Nicotinell Lutschtabletten in the following countries:

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GRAZAX 75,000 SQ-T oral lyophilisate

GRAZAX 75 000 SQ-T

Phleum pratense

GRAZAX 75 000 SQ-T oral lyophilisate

Standardised allergen extract of grass pollen from Timothy (Phleum pratense)

Read all of this leaflet carefully before you start taking this medicine.

• Keep this leaflet.You may need to read it again


• If you have further questions, ask your doctor or pharmacist


• This medicine has been prescribed for you. Do not pass it on to others. It may harm them, even if their symptoms are the same as yours


• If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist

In this leaflet:

• 1.What GRAZAX is and what it is used for


• 2. Before you take GRAZAX


• 3. How to take GRAZAX


• 4. Possible side effects


• 5. How to store GRAZAX


• 6. Further information

What GRAZAX is and what it is used for

GRAZAX contains an allergen extract of grass pollen.

GRAZAX is used to treat rhinitis and conjunctivitis caused by grass pollen in adults and children (5 years or older). GRAZAX modifies the allergic disease by increasing immunological tolerance towards grass pollen. The effect is sustained after you have completed treatment.

Children are carefully selected for treatment by doctors experienced in the treatment of allergic diseases in children.

The doctor will evaluate your allergic symptoms and perform a skin prick test or take a blood sample in order to decide if GRAZAX should be used for treatment.

You are advised to take the first oral lyophilisate under medical supervision. This is a precaution in order to evaluate each patient's sensitivity to the treatment. This gives you the possibility of discussing possible side effects with the doctor.

GRAZAX is prescribed by doctors with experience in treatment of allergy.

Before you take GRAZAX

Do not take GRAZAX if:

• You are allergic (hypersensitive) to any of the excipients in the oral lyophilisate


• You have an illness which affects the immune system


• You have severe asthma (as assessed by your doctor)


• You have cancer


• You have a mouth inflammation which is severe

Take special care with GRAZAX if:

• You have recently had a tooth taken out or other forms of oral surgery.
  
  Treatment with GRAZAX should in this case be stopped for 7 days to allow your oral cavity to heal


• You have severe allergy to fish


• You previously have had an allergic reaction in connection with injection of allergen extract of grass pollen

Use in children:

• Shedding of a deciduous (milk) tooth
  
  Treatment with GRAZAX should in this case be stopped for 7 days to allow your oral cavity to heal


• In children with asthma experiencing an acute upper respiratory tract infection, GRAZAX treatment should be temporarily discontinued until infection has resolved.

If any of the above applies to you, talk to your doctor before taking GRAZAX.

There is no experience with GRAZAX in the elderly (65 years and older).

Taking other medicines

Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines, including medicines obtained without a prescription. If you are taking other medicines for your allergy symptoms such as antihistamines or corticosteroids your doctor should evaluate the use of such medicines.

Taking GRAZAX with food and drink

Food and drink should not be taken for 5 minutes after taking this oral lyophilisate.

Pregnancy and breast-feeding

At present there is no experience for the use of GRAZAX during pregnancy. Treatment with GRAZAX should not be initiated during pregnancy. If you become pregnant during treatment, speak to your doctor about whether it is appropriate for you to continue the treatment.

At present there is no experience for the use of GRAZAX during breast-feeding. No effects on the breastfed infants are anticipated.

Driving and using machines

You alone are responsible for the judgement of your ability to drive or perform precision work. Effects or side effects from medicine may influence this ability. A description of these effects is available in other sections of this leaflet. Thus, for guidance read all the information in this leaflet.

You should check with your doctor or pharmacist if you are not sure.

Treatment with GRAZAX has no or negligible influence on the ability to drive or use machines.

How to take GRAZAX

Always take GRAZAX exactly as your doctor has told you.You should check with your doctor or pharmacist if you are not sure.

The usual dose is one oral lyophilisate daily. To get the best effect start taking the oral lyophilisates at least 4 months prior to the expected start of the grass pollen season and continue all year round. It is recommended to continue treatment for 3 years.

GRAZAX is an oral lyophilisate. Make sure your hands are dry before handling the oral lyophilisates.Take the oral lyophilisates like this:

• 1. Tear off the strip marked with triangles at the top of the oral lyophilisate pack


• 2. Tear a square off the oral lyophilisate pack along the perforated lines


• 3. Do not force the oral lyophilisate through the foil. It may damage the oral lyophilisate as it easily breaks. Instead, fold back the marked corner of the foil and then pull it off


• 4. Remove the oral lyophilisate carefully from the foil and take the oral lyophilisate immediately


• 5. Place the oral lyophilisate under the tongue. Allow it to remain there for a few seconds until it has dissolved. Do not swallow during the first minute. Do not eat or drink for at least 5 minutes

If you take more GRAZAX than you should

If you have taken too many GRAZAX oral lyophilisates you may experience allergic symptoms including local symptoms from mouth and throat. If you experience severe symptoms, immediately contact a doctor or a hospital.

If you forget to take GRAZAX

If you have forgotten to take an oral lyophilisate, take it later in the day. Do not take a double dose on any one day to make up for a forgotten oral lyophilisate.

If you stop taking GRAZAX

If you do not take this medicine as prescribed, you may not have an effect of the treatment. If you have any further questions on the use of this product, ask your doctor or pharmacist.

Possible side effects

Like all medicines, GRAZAX can cause side effects, although not everybody gets them.

The side effects may be an allergic response to the allergen you are being treated with. In most cases the side effects last from minutes to hours after taking the oral lyophilisate and settles down within one week of starting the treatment.

Very common (affecting more than 1 in 10 people): Itching in the mouth and ears, irritating sensation in the throat, sneezing and swelling in the mouth.

Common (affecting more than 1 in 100 but less than 1 in 10 people): Itchy eyes, inflammation in the eyes, stuffy or runny nose. Swelling, prickling, numbness, blistering, or other discomforts of mouth and tongue. Swollen lips, Tirednesss. Headache. Itching. Nettle rash.A feeling of swelling or tightness in the throat, coughing, asthma. Gastrointestinal problems such as stomach pain, feeling sick and heartburn. Inflammation in the throat.

Uncommon (affecting more than 1 in 1000 but less than 1 in 100 people): Lip blister, mouth ulceration, pain in mouth and gullet, inflammation in the mouth, dryness of mouth and throat, affection of the tongue, salivary gland disorders, difficulty in swallowing, vomiting, diarrhoea. Feeling of swollenness in the throat, discomfort at breathing, short of breath, wheezing breath, hoarseness. Inflammation of the nose and throat. Infection of the upper respiratory tract. Dizziness. Lymph node swelling. Lowered blood pressure.Allergic reaction. Chest discomfort, chest pain, chest tightness. Feeling hot, feeling of discomfort, fever. Sensation of foreign body in the throat. Eye swelling.

Rare (affecting more than 1 in 10000 but less than 1 in 1000 people): Sensation of rapid, forceful or irregular beating of the heart.

Stop the intake of GRAZAX and contact your doctor or hospital immediately if you experience any of the following symptoms:

• Swelling of the face, mouth or throat


• Difficulties in swallowing


• Rash


• Difficulties in breathing


• Voice changes


• Worsening of existing asthma

Upper respiratory tract infection, abdominal pain, and vomiting are reported more frequently in children than in adults.

If you have troublesome side effects you should contact your physician who will determine the anti-allergy medicines you may require, such as antihistamines.

If you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.

How to store GRAZAX

Keep out of the reach and sight of children.

Do not use GRAZAX after the expiry date stated on the blister and the carton after EXP. The expiry date refers to the last day of that month.

This medicinal product does not require any special storage conditions.

Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required.These measures will help to protect the environment.

Further Information

What GRAZAX contains

The active substance is SQ standardised allergen extract of grass pollen from Timothy (Phleum pratense). The activity per oral lyophilisate is expressed using the unit SQ-T*. The activity of one oral lyophilisate is 75,000 SQ-T.

* Standardised Quality units Tablet (SQ-T)

The other ingredients are gelatine (fish source),mannitol and sodium hydroxide.

What GRAZAX looks like and contents of the pack

White to off-white circular oral lyophilisate marked with a debossed image on one side.

Aluminium blister cards with removable aluminium foil in an outer box of carton. Following packages are available: 30, 90 or 100 oral lyophilisates.

Not all pack sizes may be marketed.

Marketing Authorisation Holder and Manufacturer

ALK-Abelló A/S

Bøge Allé 6-8

DK-2970 Hørsholm

Denmark

Distributor

ALK-Abelló Ltd.

1 Tealgate

Hungerford

Berkshire

RG17 0YT

UK

For information in Large Print, tape, CD or Braille, please phone 01488 686 016

This leaflet was last approved on

25 September 2009

1044580

Nifedipin

Nifedipin may be available in the countries listed below.

Ingredient matches for Nifedipin

Nifedipine

Nifedipine is reported as an ingredient of Nifedipin in the following countries:

• Croatia (Hrvatska)


• Georgia


• Romania


• Serbia

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Amoxiclin

Amoxiclin may be available in the countries listed below.

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Amoxicillin

Amoxicillin is reported as an ingredient of Amoxiclin in the following countries:

• Peru

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Antalgin

Antalgin may be available in the countries listed below.

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Indometacin

Indometacin is reported as an ingredient of Antalgin in the following countries:

• Mexico

Naproxen

Naproxen sodium salt (a derivative of Naproxen) is reported as an ingredient of Antalgin in the following countries:

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Nalapril

Nalapril may be available in the countries listed below.

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Enalapril

Enalapril maleate (a derivative of Enalapril) is reported as an ingredient of Nalapril in the following countries:

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Biopoin

Biopoin may be available in the countries listed below.

Ingredient matches for Biopoin

Epoetin Theta

Epoetin Theta is reported as an ingredient of Biopoin in the following countries:

• Germany

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Colestid

Generic Name: Colestipol Hydrochloride
Class: Bile Acid Sequestrants
VA Class: CV350
CAS Number: 37296-80-3

Introduction

Antilipemic agent; bile acid sequestrant.

Uses for Colestid

Dyslipidemias

Adjunct to dietary therapy to decrease elevated serum total and LDL-cholesterol concentrations in the management of primary hypercholesterolemia in patients who do not respond adequately to diet.^{166 167}

Generally has no clinically relevant effect on serum triglyceride concentrations.^{100 167} However, because triglyceride concentrations may be increased in some patients,¹⁶⁷ do not use alone in the management of hypertriglyceridemia.^d

As effective as cholestyramine in lowering serum cholesterol concentrations.^d Select bile acid sequestrant based on patient tolerance, including palatability and taste preference, and cost.^{136 163}

Colestid Dosage and Administration

General

• 
  

  Patients should be placed on a standard lipid-lowering diet before initiation of colestipol therapy and should remain on this diet during treatment with the drug.^{166 167}

  
  


• 
  

  To optimize antilipemic effects while minimizing the risk of adverse GI effects, adjust dosage carefully and titrate slowly.^{135 136 166}

  
  


• 
  

  Instruct patients to take other drugs at least 1 hour before or 4 hours after taking colestipol tablets or suspension to minimize possible interference with absorption.^{166 167} (See Effects on GI Absorption of Drugs under Interactions.)

  
  

Monitoring during Antilipemic Therapy

• 
  

  Monitor lipoprotein concentrations periodically to ensure that target LDL-cholesterol goals are achieved and maintained at <100 mg/dL (optional goal: <70 mg/dL) for patients with CHD or CHD risk equivalents; <130 mg/dL (optional goal: <100 mg/dL) for patients with ≥2 risk factors and 10-year risk of 10–20%; <130 mg/dL for patients with ≥2 risk factors and 10-year risk <10%; or <160 mg/dL for patients with 0–1 risk factor.

  
  

Administration

Oral Administration

Administer tablets one at a time; promptly swallow whole, using plenty of water or other appropriate liquid.¹⁶⁷ The tablets must not be cut, crushed, or chewed.¹⁶⁷

To avoid accidental inhalation or esophageal distress, do not administer colestipol hydrochloride for oral suspension in its dry form.¹⁶⁶

To minimize excessive swallowing of air, advise patients to avoid rapid ingestion of suspensions of the drug.¹³⁶ After the mixture is ingested, rinse the glass with a small amount of additional fluid and ingest the remaining liquid to ensure that the entire dose has been taken.¹⁶⁶

Reconstitution

Add the prescribed amount of colestipol hydrochloride granules to at least 90 mL of a liquid (e.g., fruit juice, water, milk, soft drink) and stir until completely mixed (colestipol will not dissolve in the liquid).¹⁶⁶ Palatability and compliance may be increased if the entire next-day’s dose is mixed in one of these liquids in the evening and then refrigerated.¹²¹ Use of a heavy or pulpy fruit juice may minimize complaints about consistency of suspensions of the drug.^{135 136 166} If a carbonated beverage is used, mix the powder slowly in a large glass to minimize excessive foaming; however, use of a carbonated beverage as a vehicle may be associated with adverse GI effects.¹⁶⁶

Alternatively, mix colestipol powder with milk in hot or regular breakfast cereals, a highly fluid soup, or pulpy fruit (e.g., crushed pineapple, pears, peaches, fruit cocktail).¹⁶⁶

Dosage

Available as colestipol hydrochloride; expressed in terms of the salt.^{166 167}

One dose (1 packet or 1 level teaspoon) of colestipol hydrochloride granules contains 5 g of colestipol hydrochloride.¹⁶⁶ One dose (1 packet or 1 level scoop) of flavored colestipol hydrochloride granules contains 7.5 g of granules, which contains 5 g of colestipol hydrochloride.¹⁶⁶

Pediatric Patients

Dyslipidemias†

Oral

Pediatric dosage has not been established;^{100 166 167} however, dosages of 10–20 g or 500 mg/kg daily in 2–4 divided doses have been used.^{115 116 118 119} Lower dosages (e.g., 125–250 mg/kg daily) have also been used in some children when serum cholesterol concentrations were only 15–20% above normal after dietary management alone.¹¹⁷

Adults

Dyslipidemias

Oral (Tablets)

Initially, 2 g once or twice daily.¹⁶⁷ Increase dosage by 2 g once or twice daily at intervals of 1 or 2 months.¹⁶⁷ Usual daily dosage range is 2–16 g taken once or in divided doses.¹⁶⁷

If the desired therapeutic effect is not achieved with the usual dosage of 2–16 g daily with good compliance and acceptable adverse effects, consider combined therapy or alternative treatment.¹⁶⁷

If triglyceride concentrations increase markedly, consider reducing dosage, discontinuing therapy, or using combined or alternative treatment.¹⁶⁷

Oral (Granules for oral suspension)

Initially, 5 g (1 packet or 1 level scoop) once or twice daily.^{100 166} Titrate dose upward as necessary in 5-g increments at 1- or 2-month intervals.^{135 136 166} Usual daily dosage range is 5–30 g (1–6 packets or level scoops) taken once or in divided doses.^{100 166}

If the desired therapeutic effect is not achieved with the usual dosage of 1–6 doses per day with good compliance and acceptable adverse effects, consider combined therapy or alternative treatment.¹⁶⁶

If triglyceride concentrations increase markedly, consider reducing dosage, discontinuing therapy, or using combined or alternative treatment.¹⁶⁶

Patients with preexisting constipation receiving granules for oral suspension: Initially, 5 g once daily for 5–7 days; then increase dosage to 5 g twice daily and monitor constipation and serum lipoprotein values, at least twice, 4–6 weeks apart.¹⁶⁶ Thereafter, increase dosage as needed by 1 dose per day (at monthly intervals) with periodic monitoring of serum lipoprotein values;¹⁶⁶ adjust dosage accordingly to achieve the desired effect while avoiding excessive dosage.^{135 136} If constipation worsens or the desired effect is not achieved with acceptable adverse effects with the usual dosage of 1–6 doses per day, consider combined therapy or alternative treatment.^{135 136 166}

30 g daily (as granules for oral suspension) has been used in combination with niacin in adults with heterozygous familial hypercholesterolemia.^{111 112 113 114}

Cautions for Colestid

Contraindications

• 
  

  Known hypersensitivity to colestipol or any ingredient in the formulation.¹⁶⁶

  
  

Warnings/Precautions

Warnings

Administration

To avoid accidental inhalation or esophageal distress, do not administer colestipol hydrochloride for oral suspension in its dry form.¹⁶⁶ Always mix colestipol hydrochloride granules with water or other fluids before ingesting.¹⁶⁶ (See Administration under Dosage and Administration.)

Phenylketonuria

Individuals with phenylketonuria (i.e., homozygous genetic deficiency of phenylalanine hydroxylase) and other individuals who must restrict their intake of phenylalanine should be warned that Flavored Colestid granules for oral suspension contain aspartame (NutraSweet), which is metabolized in the GI tract following oral administration to provide 18.2 mg of phenylalanine per 7.5-g packet.¹⁶⁶

General Precautions

GI Effects

Mild and, occasionally, severe constipation has occurred.^{166 167} Exacerbation of preexisting constipation and aggravation of hemorrhoids secondary to constipation may occur.^{166 167} Encourage increased fluid and fiber intake to alleviate constipation;^{111 114 121 136 166 167 173} a stool softener can be added if necessary.^{135 136 166 167} In addition, adjust dosage carefully and titrate slowly to minimize adverse GI effects (e.g., fecal impaction).^{135 166 167} (See Dosage under Dosage and Administration.) Make particular effort to avoid constipation in patients with symptomatic CHD.^{166 167} Discontinuation of colestipol therapy may be required in some patients.^{166 167}

Difficulty swallowing and transient esophageal obstruction have been reported rarely.^{166 167} Patients with a history of swallowing difficulties or choking with food, liquids, or other tablets or capsules should consult a clinician before initiating therapy with colestipol hydrochloride tablets.¹⁶⁷ If abdominal pressure or discomfort (secondary to esophageal obstruction) occurs, advise patients to consult a clinician prior to administering the next dose.¹⁶⁷

Abdominal discomfort (including pain and cramping), belching, flatulence, indigestion, heartburn, nausea, vomiting, and diarrhea or loose stools also have been reported.^{166 167} Bleeding hemorrhoids and blood in the stool have been reported infrequently.^{166 167} Peptic ulceration, cholecystitis, and cholelithiasis have been reported occasionally but are not necessarily drug-related.^{166 167}

Fat-soluble Vitamin Deficiency

May interfere with the absorption of folic acid and fat-soluble vitamins (e.g., vitamins A, D, E, K).^{166 167} Prolonged use may be associated with an increased bleeding tendency as a result of hypoprothrombinemia secondary to vitamin K deficiency.^{166 167} (See Specific Drugs under Interactions.)

Hypothyroidism

Theoretical risk for the development of hypothyroidism, especially in patients with limited thyroid reserve.^{166 167}

Hyperchloremic Acidosis

Because colestipol is the chloride form of an anion-exchange resin, there is a possibility that prolonged use may lead to the development of hyperchloremic acidosis.^{135 166 167}

Specific Populations

Pregnancy

Category B.^c

Interferes with absorption of fat-soluble vitamins, which may be detrimental even in the presence of supplementation.^{166 167}

Lactation

Use with caution; possible lack of proper vitamin absorption associated with colestipol therapy may have an effect on nursing infants.^{166 167}

Pediatric Use

Safety and efficacy not established.^{166 167}

Common Adverse Effects

Constipation.^{166 167}

Interactions for Colestid

Effects on GI Absorption of Drugs

May bind to a number of drugs in the GI tract and may delay or reduce their absorption.^{166 167} Instruct patients to allow as long a time interval as possible between ingestion of other drugs and colestipol.^{166 167} The manufacturer recommends administering other drugs at least 1 hour before or 4 hours after colestipol.^{166 167}

Consider the possibility that discontinuance of colestipol in patients stabilized on potentially toxic drugs that bind to the resin may lead to toxicity and that administration of colestipol to patients stabilized on other drugs may reduce the effect of these drugs.^{166 167}

Specific Drugs

Drug	Interaction	Comments
Antidiabetic agents (sulfonylureas)	Decreased antilipemic effects of colestipold
β-adrenergic blocking agents (propranolol)	Decreases and/or delays GI absorption of propranolol;133 134 135 166 167 effect on absorption of other β-adrenergic blocking agents not fully determined134 135 166 167	Monitor closely whenever colestipol therapy is initiated or discontinued in patients receiving propranolol;133 135 166 167 adjust propranolol dosage as necessary133 134
Digoxin	Colestipol may bind digoxin in the GI tract and impair its absorption166 167
Diuretics, thiazide (e.g., hydrochlorothiazide, chlorothiazide)	Substantially decreased absorption of diuretic166 167	Decreases absorption of chlorothiazide even when administered 1 hour before colestipol hydrochloride166 167
Fat-soluble Vitamins (i.e., vitamins A, D, E, K)	Decreased absorption of fat-soluble vitamins166 167	Consider supplemental administration of vitamins A and D if colestipol is to be given for a prolonged period.d Bleeding secondary to vitamin K deficiency usually responds promptly to parenteral administration of phytonadione; recurrences can be prevented by oral administration of phytonadione166 167
Furosemide	Substantially decreased absorption of furosemide166 167
Gemfibrozil	Substantially decreased absorption of gemfibrozil166 167
Hydrocortisone	Possible interference with absorption of hydrocortisone166 167
Lovastatin	Possible additive antilipemic effects166 167
Niacin	Additive antilipemic effects166 167
Penicillin G	Substantially decreased absorption of penicillin G166 167
Phosphate supplements, oral	Possible interference with absorption of oral phosphate supplements166 167
Tetracycline	Substantially decreased absorption of tetracycline166 167

Colestid Pharmacokinetics

Absorption

Bioavailability

Not absorbed from the GI tract.^{166 167}

Onset

Therapeutic response usually occurs within 1 month.^{166 167}

Elimination

Elimination Route

Binds to bile acids in the intestine and forms a nonabsorbable complex that is excreted in feces.^{166 167}

Stability

Storage

Oral

Tablets

20–25°C.^{166 167}

Granules for Suspension

20–25°C.¹⁰⁰

Actions and SpectrumActions

• 
  

  Binds to bile acids in the intestine and forms a nonabsorbable complex that is excreted in feces.^{166 167} Partial removal of bile acids from the enterohepatic circulation via this mechanism results in increased conversion of cholesterol to bile acids in the liver.^{166 167} This causes an increased demand for cholesterol in liver cells, resulting in a compensatory increase in hepatic uptake (and thus systemic clearance) of circulating LDL-cholesterol.^{166 167}

  
  


• 
  

  Reduces serum total and LDL-cholesterol concentrations.^{166 167} Serum triglyceride concentrations may increase or remain unchanged.^{166 167}

  
  


• 
  

  Antilipemic effects are additive when used with lovastatin or niacin.^{166 167}

  
  

Advice to Patients

• 
  

  Importance of adherence to prescribed directions for use.^{166 167} (See Oral Administration Under Dosage and Administration.)

  
  


• 
  

  Importance of adherence to National Cholesterol Education Program (NCEP)’s dietary recommendations.^{166 167}

  
  


• 
  

  Inform patients that colestipol hydrochloride tablets may be larger than typical tablets or capsules.¹⁶⁷ (See GI Effects under Cautions.)

  
  


• 
  

  Importance of administering other medications at least 1 hour before or 4 hours after colestipol.^{166 167}

  
  


• 
  

  For phenylketonurics, importance to inform them that Flavored Colestid granules for oral suspension contains aspartame.¹⁶⁶

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{166 167}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.^{166 167}

  
  


• 
  

  Importance of informing patients of other important precautionary information. (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Colestipol Hydrochloride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	For suspension	5 g/packet or calibrated scoop*	Colestid Granules	Pfizer
			Colestipol Hydrochloride for Oral Suspension	Global
		5 g/7.5 g packet or calibrated scoop	Colestid Flavored Granules (with aspartame)	Pfizer
	Tablets (micronized)	1 g	Colestid (with povidone)	Pfizer

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Colestid 1GM Tablets (PFIZER U.S.): 120/$106 or 360/$302.98

Colestid 5GM Granules (PFIZER U.S.): 500/$150.99 or 1500/$435.98

Colestid 5GM Packet (PFIZER U.S.): 30/$85.99 or 90/$239.96

Colestid 5GM Packet (PFIZER U.S.): 90/$213.33 or 270/$640

Colestid Flavored 5GM Granules (PFIZER U.S.): 450/$129.99 or 1350/$375.96

Colestid Flavored 5GM/7.5GM Packet (PFIZER U.S.): 60/$165.99 or 180/$496

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions May 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

100. Pfizer. Colestid and Flavored Colestid (colestipol hydrochloride for oral suspension) prescribing information. New York, NY; 2006 Jun.

101. Anon. Addition to labeling of cholestyramine. FDA Drug Bull. 1985; 15:7-8. [PubMed 3858190]

102. National Institutes of Health Offices of Medical Applications of Research. Consensus conference: lowering blood cholesterol to prevent heart disease. JAMA. 1985; 25:2080-6.

103. Rahimtoola SH. Cholesterol and coronary heart disease: a perspective. JAMA. 1985; 253:2094-5. [PubMed 3974101]

104. American Heart Association Committee to Design a Dietary Treatment of Hyperlipoproteinemia. Recommendations for treatment of hyperlipidemia in adults: a joint statement of the Nutrition Committee and the Council on Arteriosclerosis. Circulation. 1984; 69:1065-90A. [PubMed 6713610]

105. American Medical Association Council on Scientific Affairs. Dietary and pharmacologic therapy for the lipid risk factors. JAMA. 1983; 250:1873-9. [IDIS 176576] [PubMed 6620484]

106. Glueck CJ. Nonpharmacologic and pharmacologic alteration of high-density lipoprotein cholesterol: therapeutic approaches to prevention of atherosclerosis. Am Heart J. 1985; 110:1107-15. [IDIS 208439] [PubMed 2865887]

107. National Heart, Lung and Blood Institute Lipid Metabolism-Atherogenesis Branch. The Lipid Research Clinics Coronary Primary Prevention Trial results. Part I: reduction in incidence of coronary heart disease. JAMA. 1984; 251:351-64. [IDIS 180094] [PubMed 6361299]

108. National Heart, Lung and Blood Institute Lipid Metabolism-Atherogenesis Branch. The Lipid Research Clinics Coronary Primary Prevention Trial results. Part II: relationship of reduction in incidence of coronary heart disease to cholesterol lowering. JAMA. 1984; 251:365-74. [IDIS 180095] [PubMed 6361300]

109. Kronmal RA. Commentary on the published results of the lipid research clinics coronary primary prevention trial. JAMA. 1985; 253:2091-3. [PubMed 3883022]

110. Oliver MF. Hypercholesterolaemia and coronary heart disease: an answer. BMJ. 1984; 288:423-4. [IDIS 182823] [PubMed 6419948]

111. Kane JP, Malloy MJ, Tun P et al. Normalization of low density-lipoprotein levels in heterozygous familial hypercholesterolemia with a combined drug regimen. N Engl J Med. 1981; 304:251-8. [IDIS 126648] [PubMed 7003391]

112. Illingworth DR, Phillipson BE, Rapp JH et al. Colestipol plus nicotinic acid in treatment of heterozygous familial hypercholesterolaemia. Lancet. 1981; 1:296-7. [IDIS 127354] [PubMed 6109940]

113. Kuo PT, Kostis JB, Moreyra AE et al. Familial type II hyperlipoproteinemia with coronary heart disease: effect of diet-colestipol-nicotinic acid treatment. Chest. 1981; 79:286-91. [IDIS 149021] [PubMed 7471860]

114. Glueck CJ. Colestipol and probucol: treatment of primary and familial hypercholesterolemia and amelioration of atherosclerosis. Ann Intern Med. 1982; 96:475-82. [IDIS 147431] [PubMed 7039445]

115. Glueck CJ, Fallat RW, Tsang RG. Pediatric familial type II hyperlipoproteinemia: therapy with diet and colestipol resin. Pediatrics. 1976; 57:68-74. [IDIS 68492] [PubMed 174057]

116. Schwarz KB, Goldstein PD, Witztum JL et al. Fat-soluble vitamin concentrations in hypercholesterolemic children treated with colestipol. Pediatrics. 1980; 65:243-50. [IDIS 113975] [PubMed 7354970]

117. Schlierf G, Mrozik K, Heuck CC et al. “Low-dose” colestipol in children, adolescents and young adults with familial hypercholesterolemia. Atherosclerosis. 1982; 41:133-8. [PubMed 7073790]

118. Glueck CJ. Therapy of familial and acquired hyperlipoproteinemia in children and adolescents. Prev Med. 1983; 12:835-47. [PubMed 6676731]

119. Tsang RC, Roginsky MS, Mellies MJ et al. Plasma 25-hydroxy-vitamin D in familial hypercholesterolemic children receiving colestipol resin. Pediatr Res. 1978; 12:980-2. [PubMed 724301]

120. American Health Foundation. Summary and recommendations of the Conference on Blood Lipids in Children: optimal levels for early prevention of coronary artery disease. Prev Med. 1983; 12:728-40. [PubMed 6676727]

121. Hoeg JM, Gregg RE, Brewer HB. An approach to the management of hyperlipoproteinemia. JAMA. 1986; 255:512-21. [IDIS 209539] [PubMed 3510334]

122. National Institutes of Health Office of Medical Applications of Research. Consensus conference: treatment of hypertriglyceridemia. JAMA. 1984; 251:1196-200. [PubMed 6582287]

123. Forman MB, Baker SG, Mieny CJ et al. Treatment of homozygous familial hypercholesterolaemia with portacaval shunt. Atherosclerosis. 1982; 41:349-61. [PubMed 7066082]

124. Thompson GR, Lowenthal R, Myant NB. Plasma exchange in the management of homozygous familial hypercholesterolaemia. Lancet. 1975; 1:1208-11. [PubMed 48833]

125. Postiglione A, Thompson GR. Experience with plasma-exchange in homozygous familial hypercholesterolaemia. Prog Clin Biol Res. 1985; 188:213-20. [PubMed 3903770]

126. Starzl TE, Chase HP, Ahrens EH Jr et al. Portacaval shunt in patients with familial hypercholesterolemia. Ann Surg. 1983; 198:273-83. [PubMed 6615051]

127. King MEE, Breslow JL, Lees RS. Plasma-exchange therapy of homozygous familial hypercholesterolemia. N Engl J Med. 1980; 302:1457-9. [PubMed 7374711]

128. Hoeg JM, Demosky SJ Jr, Schaefer EJ et al. The effect of portacaval shunt on hepatic lipoprotein metabolism in familial hypercholesterolemia. J Surg Res. 1985; 39:369-77. [PubMed 4057999]

129. Schaefer EJ, Levy RI. Pathogenesis and management of lipoprotein disorders. N Engl J Med. 1985; 312:1300-10. [IDIS 199398] [PubMed 3887163]

130. Bilheimer DW, Goldstein JL, Grundy SM et al. Liver transplantation to provide low-density-lipoprotein receptors and lower plasma cholesterol in a child with homozygous familial hypercholesterolemia. N Engl J Med. 1984; 311:1658-64. [PubMed 6390206]

131. Mancini M, Postiglione A, Farinaro E et al. Diet, drugs, and plasma exchange in the treatment of hyperlipidemia in childhood. Prev Med. 1983; 12:848-53. [PubMed 6676732]

132. American Heart Association Committee on Atherosclerosis and Hypertension in Childhood of the Council of Cardiovascular Disease in the Young and the Nutrition Committee. Diagnosis and treatment of primary hyperlipidemia in childhood: a joint statement for physicians by the Committee on Atherosclerosis and Hypertension in Childhood of the Council of Cardiovascular Disease in the Young and the Nutrition Committee. Circulation. 1986: 74:1181-8A.

133. Hibbard DM, Peters JR, Hunninghake DB. Effect of cholestyramine and colestipol on the plasma concentrations of propranolol. Br J Clin Pharmacol. 1984; 18:337-42. [IDIS 191419] [PubMed 6487473]

134. Mangini RJ, ed. Drug interaction facts. St. Louis: JB Lippincott Co; 1985(Jan):110a.

135. The Upjohn Company. Colestid (colestipol hydrochloride) granules prescribing information. Kalamazoo, MI; 1990 Apr.

136. The Expert Panel (coordinated by the National Heart, Lung, and Blood Institute). Report of the National Cholesterol Education Program Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults. Arch Intern Med. 1988; 148:36-69. [IDIS 236890] [PubMed 3422148]

137. Bilheimer DW. Familial hypercholesterolemia: there is a need for early detection and treatment. JAMA. 1987; 257:69-70. [PubMed 3783906]

138. Vega GL, Grundy SM. Treatment of primary moderate hypercholesterolemia with lovastatin (mevinolin) and colestipol. JAMA. 1987; 257:33-8. [IDIS 223496] [PubMed 3537351]

139. Witztum JL. Intensive drug therapy of hypercholesterolemia. Am Heart J. 1987; 113(2 Part 2):603-9. [IDIS 226100] [PubMed 3544777]

140. Blankenhorn DH, Nessim SA, Johnson RL et al. Beneficial effects of colestipol-niacin therapy on coronary atherosclerosis and coronary bypass grafts. JAMA. 1987; 257:3233-40. [IDIS 230814] [PubMed 3295315]

141. Illingworth DR. Mevinolin plus colestipol in therapy for severe heterozygous familial hypercholesterolemia. Ann Intern Med. 1984; 101:598-604. [IDIS 191769] [PubMed 6567462]

142. Mabuchi H, Sakai T, Sakai Y et al. Reduction of serum cholesterol in heterozygous patients with familial hypercholesterolemia: additive effects of compactin and cholestyramine. N Engl J Med. 1983; 308:609-13. [IDIS 166852] [PubMed 6828091]

143. Malloy MJ, Kane JP, Kunitake ST et al. Complementarity of colestipol, niacin, and lovastatin in treatment of severe familial hypercholesterolemia. Ann Intern Med. 1987; 107:616-23. [IDIS 235737] [PubMed 3662275]

144. Tobert JA. New developments in lipid-lowering therapy: the role of inhibitors of hydroxymethylglutaryl-coenzyme A reductase. Circulation. 1987; 76:534-8. [IDIS 252224] [PubMed 3113763]

145. Brown MS, Goldstein JL. The hyperlipoproteinemias and other disorders of lipid metabolism. In: Harrison’s principles of internal medicine. 11th ed. New York: McGraw-Hill Book Co; 1987;1650-61.

146. Goldstein JL, Brown MS. The low-density lipoprotein pathway and its relation to atherosclerosis. Ann Rev Biochem. 1977; 46:897-930. [PubMed 197883]

147. Brown MS, Goldstein JL. Lipoprotein receptors in the liver: control signals for plasma cholesterol traffic. J Clin Invest. 1983; 72:743-7. [PubMed 6309907]

148. Heber D, Koziol BJ, Henson LC. Low density lipoprotein receptor regulation and cellular basis of atherosclerosis: implications for nutritional and pharmacologic treatment of hypercholesterolemia. Am J Cardiol. 1987; 60(Suppl):4-8G.

149. Thompson GR, Ford J, Jenkinson M et al. Efficacy of mevinolin as adjuvant therapy for refractory familial hypercholesterolaemia. Q J Med. 1986; 60:803-11. [IDIS 222246] [PubMed 3640503]

150. East C, Grundy SM, Bilheimer DW. Normal cholesterol levels with lovastatin (mevinolin) therapy in a child with homozygous familial hypercholesterolemia following liver transplantation. JAMA. 1986; 256:2843-8. [IDIS 222763] [PubMed 3534334]

151. Grundy SM. HMG-CoA reductase inhibitors for treatment of hypercholesterolemia. N Engl J Med. 1988; 319:24-33. [IDIS 243240] [PubMed 3288867]

152. Reviewers’ comments on lovastatin (personal observations); 1988 Jul.

153. McNamara DJ, Ahrens EH Jr, Kolb R et al. Treatment of familial hypercholesterolemia by portcaval anastomosis: effect on cholesterol metabolism and pool sizes. Proc Natl Acad Sci USA. 1983; 80:564-8. [PubMed 6572906]

154. Witztum JL, Williams JC, Ostlund R et al. Successful plasmapheresis in a 4-year-old child with homozygous familial hypercholesterolemia. J Pediatr. 1980; 97:615-8. [PubMed 6775065]

155. Graisely B, Cloarec M, Salmon S et al. Extracorporeal plasma therapy for homozygous familial hypercholesterolaemia. Lancet. 1980; 2:1147. [PubMed 6107765]

156. Stoffel W, Borberg H, Greve V. Application of specific extracorporeal removal of low density lipoprotein in familial hypercholesterolaemia. Lancet. 1981; 2:1005-7. [PubMed 6118475]

157. Thompson GR, Miller JP, Breslow JL. Improved survival of patients with homozygous familial hypercholesterolaemia treated with plasma exchange. BMJ. 1985; 291:1671-3. [PubMed 3935235]

158. Illingworth DR, Bacon SP, Larsen KK. Long-term experience with HMG-CoA reductase inhibitors in the therapy of hypercholesterolemia. Atheroscler Rev. 1988; 18:161-87.

159. American Heart Association. AHA conference report on cholesterol. Circulation. 1989; 80:715-48. [PubMed 2670320]

160. Cashin-Hemphill L, Mack WJ, Pogoda JM et al. Beneficial effects of colestipol-niacin on coronary atherosclerosis: a 4-year follow-up. JAMA. 1990; 264:3013-7. [IDIS 275276] [PubMed 2243429]

161. Working Group on Management of Patients with Hypertension and High Blood Cholesterol. National education programs working group report on the management of patients with hypertension and high blood cholesterol. Ann Intern Med. 1991; 114:224-37. [IDIS 276739] [PubMed 1984747]

162. The Upjohn Company. Colestid (colestipol hydrochloride) granules prescribing information. In: Barnhart ER, publisher. Physicians’ desk reference. 45th ed. Oradell, NJ: Medical Economics Company Inc; 1991(Suppl A):A72.

163. The Expert Panel on Blood Cholesterol Levels in Children and Adolescents. Report of the Expert Panel on Blood Cholesterol Levels in Children and Adolescents. Pediatrics. 1992; 89(Suppl):525-84. [PubMed 1538956]

164. American Academy of Pediatrics Committee on Nutrition. Statement on cholesterol. Pediatrics. 1992; 90:469-73. [PubMed 1518712]

165. The Expert Panel. Second Report of the Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel II). Circulation. 1994; 89:1329-1445.

166. Upjohn. Colestid (colestipol hydrochloride for oral suspension) and Flavored Colestid (colestipol hydrochloride for oral suspension) granules for oral suspension prescribing information. Kalamazoo, MI; 1998 Mar.

167. Pfizer. Colestid (micronized colestipol hydrochloride) tablets prescribing information. New York, NY; 2006 Jun.

168. Gibbons RJ, Chatterjee K, Daley J et al. ACC/AHA/ACP-ASIM guidelines for the management of patients with chronic stable angina: a report of the American College of Cardiology, American Heart Association Task Force on Practice Guidelines (Committee on Management of Patients with Chronic Stable Angina). J Am Coll Cardiol. 1999; 33:2092-197. [IDIS 429504] [PubMed 10362225]

169. Scandinavian Simvastatin Survival Study Group. Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease: the Scandinavian Survival Study (4S). Lancet. 1994; 344:1383-9. [IDIS 338582] [PubMed 7968073]

170. Sacks FN, Pfeffer MA, Maye LA et al. The effect of pravastatin on coronary events after myocardial infarction in patients with average cholesterol levels. N Engl J Med. 1996; 335:1001-9. [IDIS 372985] [PubMed 8801446]

171. The Long-term Intervention with Pravastatin in Ischaemic Disease (LIPID) Study Group. Prevention of cardiovascular events and death with pravastatin in patients with coronary heart disease and a broad range of initial cholesterol levels. N Engl J Med. 1998; 339:1349-57. [IDIS 430942] [PubMed 9841303]

172. Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults. Executive summary of the third report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of high Blood Cholesterol in Adults (Adult Treatment Panel III). JAMA. 2001; 285:2486-97. [IDIS 464555] [PubMed 11368702]

173. Anon. Choice of lipid-regulating drugs. Med Lett Drugs Ther. 2001; 43:43-8. [PubMed 11378632]

174. National Cholesterol Education Program Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults: Adult Treatment Panel III Report. From AHA web site.

c. Briggs GG, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation. 6th ed. Baltimore, MD: Williams & Wilkins; 2002:324-5.

d. AHFS Drug Information 2003. McEvoy GK , ed. Colestipol hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists; 2003:1594-6.

More Colestid resources

• Colestid Side Effects (in more detail)
• Colestid Use in Pregnancy & Breastfeeding
• Drug Images
• Colestid Drug Interactions
• Colestid Support Group
• 0 Reviews for Colestid - Add your own review/rating

• Colestid Prescribing Information (FDA)


• Colestid MedFacts Consumer Leaflet (Wolters Kluwer)


• Colestid Concise Consumer Information (Cerner Multum)


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Ocu-Carpine

Generic Name: pilocarpine (Ophthalmic route)

pye-loe-KAR-peen

Commonly used brand name(s)

In the U.S.

• Isopto Carpine


• Ocu-Carpine


• Ocusert Pilo


• Pilocar


• Pilopine-HS

In Canada

• Minims Pilocarpine 2%


• Minims Pilocarpine 4%

Available Dosage Forms:

• Device


• Suspension


• Solution


• Gel/Jelly

Therapeutic Class: Direct Acting Miotic

Pharmacologic Class: Cholinergic

Uses For Ocu-Carpine

Pilocarpine is used to treat glaucoma and other eye conditions.

This medicine is available only with your doctor's prescription.

Before Using Ocu-Carpine

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Although there is no specific information comparing use of this medicine in children with use in other age groups, pilocarpine is not expected to cause different side effects or problems in children than it does in adults.

Geriatric

Many medicines have not been studied specifically in older people. Therefore, it may not be known whether they work exactly the same way they do in younger adults or if they cause different side effects or problems in older people. Although there is no specific information comparing use of pilocarpine in the elderly with use in other age groups, this medicine is not expected to cause different side effects or problems in older people than it does in younger adults.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Asthma or


• Eye disease or problems (other)—Pilocarpine may make the condition worse

Proper Use of pilocarpine

This section provides information on the proper use of a number of products that contain pilocarpine. It may not be specific to Ocu-Carpine. Please read with care.

To use the eye drop form of pilocarpine:

• First, wash your hands. Tilt the head back and, pressing your finger gently on the skin just beneath the lower eyelid, pull the lower eyelid away from the eye to make a space. Drop the medicine into this space. Let go of the eyelid and gently close the eyes. Do not blink. Keep the eyes closed and apply pressure to the inner corner of the eye with your finger for 1 or 2 minutes to allow the medicine to be absorbed by the eye.


• Immediately after using the eye drops, wash your hands to remove any medicine that may be on them.


• To keep the medicine as germ-free as possible, do not touch the applicator tip to any surface (including the eye). Also, keep the container tightly closed.

To use the eye gel form of pilocarpine:

• First, wash your hands. Tilt the head back and, pressing your finger gently on the skin just beneath the lower eyelid, pull the lower eyelid away from the eye to make a space. Squeeze a thin strip of gel into this space. A 1½-cm (approximately ½-inch) strip of gel is usually enough, unless you have been told by your doctor to use a different amount. Let go of the eyelid and gently close the eyes. Keep the eyes closed for 1 or 2 minutes to allow the medicine to be absorbed by the eye.


• Immediately after using the eye gel, wash your hands to remove any medicine that may be on them.


• To keep the medicine as germ-free as possible, do not touch the applicator tip to any surface (including the eye). After using the eye gel, wipe the tip of the gel tube with a clean tissue and keep the tube tightly closed.

To use the eye insert form of pilocarpine:

• This medicine usually comes with patient directions. Read them carefully before using this medicine.


• If you think this medicine unit may be damaged, do not use it. If you have any questions about this, check with your health care professional.


• If the unit seems to be releasing too much medicine into your eye, remove it and replace with a new unit. If you have any questions about this, check with your doctor.

Use this medicine only as directed. Do not use more of it and do not use it more often than your doctor ordered. To do so may increase the chance of too much medicine being absorbed into the body and the chance of side effects.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For eye drop dosage form:
  
  • For chronic glaucoma:
    
    • Adults and children—One drop one to four times a day.
    
    
  
  
  • For acute angle-closure glaucoma:
    
    • Adults and children—One drop every five to ten minutes for three to six doses. Then one drop every one to three hours until eye pressure is reduced.
    
    
  
  


• For eye gel dosage form:
  
  • For glaucoma:
    
    • Adults and teenagers—Use once a day at bedtime.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  


• For eye insert dosage form:
  
  • For glaucoma:
    
    • Adults and children—Insert one ocular system every seven days.
    
    
    • Infants—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Store the eye system form of this medicine in the refrigerator. Keep from freezing. Store the 3.5-gram size (of the gel form) at room temperature.

Precautions While Using Ocu-Carpine

Your doctor should check your eye pressure at regular visits.

For patients using the eye drop or gel form of this medicine:

• For a short time after you use this medicine, your vision may be blurred or there may be a change in your near or far vision, especially at night. Make sure your vision is clear before you drive, use machines, or do anything else that could be dangerous if you are not able to see well.

For patients using the eye insert form of this medicine:

• For the first several hours after you insert this unit in the eye, your vision may be blurred or there may be a change in your near or far vision, especially at night. Therefore, insert this unit in the eye at bedtime, unless otherwise directed by your doctor. If this unit is inserted in the eye at any other time of the day, make sure your vision is clear before you drive, use machines, or do anything else that could be dangerous if you are not able to see well.

Ocu-Carpine Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

Symptoms of too much medicine being absorbed into the body

• Increased sweating


• muscle tremors


• nausea, vomiting, or diarrhea


• troubled breathing or wheezing


• watering of mouth

Less common or rare

• Eye pain

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Blurred vision or change in near or far vision


• decrease in night vision

Less common

• Eye irritation


• headache or browache

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Ocu-Carpine side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Ocu-Carpine resources

• Ocu-Carpine Side Effects (in more detail)
• Ocu-Carpine Use in Pregnancy & Breastfeeding
• Ocu-Carpine Drug Interactions
• Ocu-Carpine Support Group
• 0 Reviews for Ocu-Carpine - Add your own review/rating

• Isopto Carpine Drops MedFacts Consumer Leaflet (Wolters Kluwer)


• Pilocar Concise Consumer Information (Cerner Multum)


• Pilocarpine Monograph (AHFS DI)

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Pentoxifylline

Pentoxifylline is reported as an ingredient of Trentox in the following countries:

• Indonesia

International Drug Name Search

Natriumfluoride PCH

Natriumfluoride PCH may be available in the countries listed below.

Ingredient matches for Natriumfluoride PCH

Sodium Fluoride

Sodium Fluoride is reported as an ingredient of Natriumfluoride PCH in the following countries:

• Netherlands

International Drug Name Search

Naso

Naso may be available in the countries listed below.

Ingredient matches for Naso

Xylometazoline

Xylometazoline hydrochloride (a derivative of Xylometazoline) is reported as an ingredient of Naso in the following countries:

• Norway

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Natecal D

Natecal D may be available in the countries listed below.

Ingredient matches for Natecal D

Calcium Carbonate

Calcium Carbonate is reported as an ingredient of Natecal D in the following countries:

• Greece


• Italy


• Spain


• United Kingdom

Colecalciferol

Colecalciferol is reported as an ingredient of Natecal D in the following countries:

• Greece


• Italy


• Spain


• United Kingdom

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Vasoserc

Vasoserc may be available in the countries listed below.

Ingredient matches for Vasoserc

Betahistine

Betahistine dihydrochloride (a derivative of Betahistine) is reported as an ingredient of Vasoserc in the following countries:

• Georgia


• Turkey

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Meromycin-ratiopharm

Meromycin-ratiopharm may be available in the countries listed below.

Ingredient matches for Meromycin-ratiopharm

Erythromycin

Erythromycin is reported as an ingredient of Meromycin-ratiopharm in the following countries:

• Hungary

Erythromycin stearate (a derivative of Erythromycin) is reported as an ingredient of Meromycin-ratiopharm in the following countries:

• Hungary

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Espironolactona Generis

Espironolactona Generis may be available in the countries listed below.

Ingredient matches for Espironolactona Generis

Spironolactone

Spironolactone is reported as an ingredient of Espironolactona Generis in the following countries:

• Portugal

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Natrium-Bicarbonat B.Braun

Natrium-Bicarbonat B.Braun may be available in the countries listed below.

Ingredient matches for Natrium-Bicarbonat B.Braun

Sodium Bicarbonate

Sodium Bicarbonate is reported as an ingredient of Natrium-Bicarbonat B.Braun in the following countries:

• Switzerland

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Natacin

Natacin may be available in the countries listed below.

Ingredient matches for Natacin

Natamycin

Natamycin is reported as an ingredient of Natacin in the following countries:

• Bangladesh

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nife von ct

nife von ct may be available in the countries listed below.

Ingredient matches for nife von ct

Nifedipine

Nifedipine is reported as an ingredient of nife von ct in the following countries:

• Romania

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Bortezomib

Class: Antineoplastic Agents
VA Class: AN900
Chemical Name: [(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl)amino]propanoyl]amino]butyl]boronic acid
Molecular Formula: C₁₉H₂₅BN₄O₄
CAS Number: 179324-69-7
Brands: Velcade

Introduction

Antineoplastic agent; inhibitor of 26S proteasome.^{1 5}

Uses for Bortezomib

Previously Untreated Multiple Myeloma

Used in combination with melphalan and prednisone for previously untreated multiple myeloma.^{18 20}

Relapsed Multiple Myeloma

Monotherapy for treatment of relapsed multiple myeloma.^{1 3 7}

More effective than high-dose dexamethasone in achieving complete or partial response, prolonging time to disease progression, and improving survival in patients with progressive multiple myeloma who had received 1–3 prior chemotherapy regimens.^{1 8}

Induction Therapy Prior to Stem-cell Transplantation in Newly Diagnosed Multiple Myeloma

Has been studied as a component of various induction regimens in patients newly diagnosed with multiple myeloma who were to undergo autologous stem-cell transplant†.^{10002 10003 10004 10005 10006 10007 10008}

Use with dexamethasone† may be considered a reasonable choice (accepted, with possible conditions) as an induction regimen in patients newly diagnosed with multiple myeloma who are to undergo an autologous stem-cell transplant†.¹⁹ Additional data needed to correlate high posttransplant responses with impact on survival beyond 1 year and to fully establish survival benefit for bortezomib-dexamethasone compared with vincristine-doxorubicin-dexamethasone (VAD) regimen.¹⁹

Use in patients with newly diagnosed multiple myeloma who are to undergo an autologous stem-cell transplant† as a component of other induction regimens (i.e., with thalidomide and dexamethasone [VTD]†; with dexamethasone and either conventional doxorubicin [PAD] or pegylated liposomal doxorubicin [VDD]†; with cyclophosphamide and dexamethasone [CyBorD and BCD regimens]†; as BCD followed by bortezomib with thalidomide and dexamethasone [BTD]†) is not established because of inadequate data, unclear risk/benefit, and/or inadequate experience.^{19 10003 10004 10005 10006 10007 10008}

Mantle Cell Lymphoma

Treatment of mantle cell lymphoma in patients who have received at least 1 prior chemotherapy regimen.^{13 14 18 21}

Bortezomib Dosage and Administration

General

• 
  

  Consult specialized references for procedures for proper handling and disposal of antineoplastics including use of gloves and protective clothing.

  
  


• 
  

  Calculate dose carefully to prevent overdosage; drug quantity contained in one 3.5-mg vial may exceed usual single dose required.

  
  

Administration

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Administer by IV injection over 3–5 seconds.

Reconstitution

To reconstitute, add 3.5 mL of 0.9% sodium chloride injection to vial containing 3.5 mg of bortezomib.

Administer within 8 hours after reconstitution.

Dosage

Consult specialized references and published protocols for dosage (including dosage adjustments in special populations), method of administration, and administration sequence of drugs in combination regimens.¹⁸

Adults

Previously Untreated Multiple Myeloma

Bortezomib, Melphalan, and Prednisone (VMP regimen)

IV

Cycles 1–4 (of the recommended nine 6-week cycles): Bortezomib 1.3 mg/m² IV twice weekly during weeks 1, 2, 4, and 5 (days 1, 4, 8, 11, 22, 25, 29, and 32 of the 6-week cycle) followed by a 10-day rest period (days 33–42).^{18 20}

Cycles 5–9: Bortezomib 1.3 mg/m² IV once weekly during weeks 1, 2, 4, and 5 (days 1, 8, 22, and 29) followed by a 13-day rest period. ^{18 20}

In all 9 cycles: Administer oral melphalan 9 mg/m² and oral prednisone 60 mg/m² once daily on days 1–4.¹⁸

At least 72 hours should elapse between consecutive doses of bortezomib.¹⁸

Dosage Modification for Toxicity for VMP Regimen

IV

Before administering any VMP cycle, platelet counts should be ≥70,000/mm³, ANC should be ≥1000/mm³, and any nonhematologic toxicities should have resolved to grade 1 or baseline.¹⁸

Table 1. Dosage Modification for VMP Regimen in Newly Diagnosed Multiple Myeloma18

Toxicity	Dose Modification or Delay
If prolonged grade 4 neutropenia or thrombocytopenia or thrombocytopenia with bleeding observed in previous VMP cycle	Consider reduction of melphalan dose by 25% in next cycle
Platelet count ≤30,000/mm3 or ANC ≤750/mm3 on a day when bortezomib is to be administered (other than on day 1)	Withhold bortezomib dose
If several doses of bortezomib were withheld in consecutive cycles because of toxicity	Reduce bortezomib dose by one dose level (i.e., a dose of 1.3 mg/m2 reduced to 1 mg/m2 or a dose of 1 mg/m2 reduced to 0.7 mg/m2)
Grade ≥3 nonhematologic toxicity	Withhold bortezomib until toxicity resolves to grade 1 or baseline; may then reinitiate bortezomib with a reduction of one dose level (i.e., 1.3 mg/m2 per dose reduced to 1 mg/m2 per dose; 1 mg/m2 per dose reduced to 0.7 mg/m2 per dose)
Bortezomib-related neuropathic pain and/or peripheral neuropathy	See Table 2 under Dosage Modification for Peripheral Neuropathy in Relapsed Multiple Myeloma

Relapsed Multiple Myeloma

IV

Standard regimen: 1.3 mg/m² twice weekly for 2 weeks (days 1, 4, 8, and 11), followed by a 10-day rest period (days 12–21).^{1 4 5}

For extended therapy of >8 treatment cycles, continue standard 21-day regimen or initiate 35-day maintenance regimen of 1.3 mg/m² once weekly for 4 weeks (days 1, 8, 15, and 22), followed by a 13-day rest period (days 23–35).¹

At least 72 hours should elapse between consecutive doses.¹

In clinical studies, patients expected to benefit from extended therapy received a median of 7 additional treatment cycles, for a total median of 14 treatment cycles.¹

Dosage Modification for Peripheral Neuropathy in Relapsed Multiple Myeloma

IV

Adjust dosage and/or frequency of administration if severe peripheral neuropathy occurs.^{1 6 18}

Table 2. Dosage Modification for Neuropathic Pain and/or Peripheral Sensory or Motor Neuropathy118

Severity of Neuropathy and Manifestations	Comments
Grade 1 (paresthesias, weakness, and/or loss of reflexes) without pain or loss of function	No dosage modification necessary
Grade 1 with pain	Reduce dose to 1 mg/m2
Grade 2 (interfering with function but not with activities of daily living)	Reduce dose to 1 mg/m2
Grade 2 with pain	Temporarily discontinue; after manifestations of toxicity resolve, reinitiate at dosage of 0.7 mg/m2once weekly
Grade 3 (interfering with activities of daily living)	Temporarily discontinue; after manifestations of toxicity resolve, reinitiate at dosage of 0.7 mg/m2once weekly
Grade 4 (disabling sensory neuropathy or motor neuropathy that is life-threatening or leads to paralysis)	Discontinue bortezomib

Dosage Modification for Other Severe Adverse Nonhematologic or Hematologic Effects in Relapsed Multiple Myeloma

IV

Temporarily discontinue therapy if grade 3 nonhematologic (other than peripheral neuropathy) or grade 4 hematologic toxicities (e.g., grade 4 thrombocytopenia [platelet count <25,000/mm³]) occur.^{1 6}

Once manifestations of toxicity resolve, reinitiate but reduce bortezomib dosage by 25% (i.e., reduce from 1.3 mg/m² per dose to 1 mg/m² per dose; reduce from 1 mg/m² per dose to 0.7 mg/m² per dose).¹

Administer the adjusted regimen for 2 weeks, followed by a 10-day rest period.⁶

Induction Therapy Prior to Stem-cell Transplantation in Newly Diagnosed Multiple Myeloma†

Bortezomib and Dexamethasone (VD regimen)†

IV

Bortezomib 1.3 mg/m² twice weekly for 2 weeks (days 1, 4, 8, and 11) followed by a 10-day rest period (days 12–21) has been used.¹⁰⁰⁰²

In cycles 1 and 2, regimen included dexamethasone 40 mg orally on days 1–4 and 9–12; in cycles 3 and 4, dexamethasone 40 mg was administered orally on days 1–4.¹⁰⁰⁰²

Patients in the clinical trial received four 21-day cycles of VD.¹⁰⁰⁰²

Mantle Cell Lymphoma

IV

Standard regimen: 1.3 mg/m² twice weekly for 2 weeks (days 1, 4, 8, and 11), followed by a 10-day rest period (days 12–21).¹⁸

For extended therapy of >8 treatment cycles, continue standard 21-day regimen or initiate 35-day maintenance regimen of 1.3 mg/m² once weekly for 4 weeks (days 1, 8, 15, and 22), followed by a 13-day rest period (days 23–35).¹⁸

At least 72 hours should elapse between consecutive doses.¹⁸

In clinical studies, patients who responded to therapy received a median of 8 treatment cycles.¹⁸

Dosage Modification for Peripheral Neuropathy in Mantle Cell Lymphoma

IV

Adjust dosage and/or frequency of administration if severe peripheral neuropathy occurs.^{1 6 18}

Table 3. Dosage Modification for Neuropathic Pain and/or Peripheral Sensory or Motor Neuropathy118

Severity of Neuropathy and Manifestations	Comments
Grade 1 (paresthesias, weakness, and/or loss of reflexes) without pain or loss of function	No dosage modification necessary
Grade 1 with pain	Reduce dose to 1 mg/m2
Grade 2 (interfering with function but not with activities of daily living)	Reduce dose to 1 mg/m2
Grade 2 with pain	Temporarily discontinue; after manifestations of toxicity resolve, reinitiate at dosage of 0.7 mg/m2once weekly
Grade 3 (interfering with activities of daily living)	Temporarily discontinue; after manifestations of toxicity resolve, reinitiate at dosage of 0.7 mg/m2once weekly
Grade 4 (disabling sensory neuropathy or motor neuropathy that is life-threatening or leads to paralysis)	Discontinue bortezomib

Dosage Modification for Other Severe Adverse Nonhematologic or Hematologic Effects in Mantle Cell Lymphoma

IV

Temporarily discontinue therapy if grade 3 nonhematologic (other than peripheral neuropathy) or grade 4 hematologic toxicities (e.g., grade 4 thrombocytopenia [platelet count <25,000/mm³]) occur.^{1 6}

Once manifestations of toxicity resolve, reinitiate but reduce bortezomib dosage by 25% (i.e., reduce from 1.3 mg/m² per dose to 1 mg/m² per dose; reduce from 1 mg/m² per dose to 0.7 mg/m² per dose).¹

Administer the adjusted regimen for 2 weeks, followed by a 10-day rest period.⁶

Special Populations

Hepatic Impairment

Moderate (i.e., bilirubin concentrations >1.5–3 times ULN with any AST concentrations) or severe (i.e., bilirubin concentrations >3 times ULN with any AST concentrations) hepatic impairment: Reduce bortezomib dose during first cycle to 0.7 mg/m².²² Based on patient tolerance, either increase dosage in subsequent cycles to 1 mg/m² or further reduce to 0.5 mg/m².²²

Mild hepatic impairment (i.e., bilirubin concentrations at or below ULN with AST concentrations exceeding ULN or bilirubin concentrations >1 to 1.5 times ULN with any AST concentrations): Administer usual recommended initial dose.²²

Renal Impairment

Dosage adjustment not required.²²

Dialysis may decrease bortezomib concentrations; administer after a dialysis procedure.¹⁸ (See Special Populations under Pharmacokinetics.)

Geriatric Patients

No specific dosage recommendations at this time.²² (See Geriatric Use under Cautions.)

Cautions for Bortezomib

Contraindications

• 
  

  Known hypersensitivity to bortezomib, boron, or mannitol.¹

  
  

Warnings/Precautions

Experience of Supervising Clinician

Use under supervision of a qualified clinician experienced in therapy with antineoplastic agents.¹

Fetal/Neonatal Morbidity and Mortality

Possible fetal harm; embryolethality and decreased fetal weight demonstrated in animals.¹ Avoid pregnancy during therapy.¹ If used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard.¹

Serious Adverse Effects

Risk of serious adverse events (i.e., fatal, life-threatening, disabling, require or prolong hospitalization, or deemed important medical events).¹ Deaths reported secondary to cardiogenic shock, cardiac arrest, CHF, respiratory failure/insufficiency, renal failure, pneumonia, and sepsis.¹⁸

Peripheral Neuropathy

Risk of severe (≥grade 3) new-onset peripheral neuropathy or exacerbation of preexisting peripheral neuropathy.¹ Occurs predominantly as peripheral sensory neuropathy, but severe peripheral motor neuropathy also reported.¹ Incidence of peripheral neuropathy reportedly higher in patients with mantle cell lymphoma than in patients with relapsed multiple myeloma.¹⁸ Manifestations improved or returned to baseline in some patients with relapsed multiple myeloma following dosage reduction or discontinuance of bortezomib; long-term outcome of peripheral neuropathy not evaluated in patients with mantle cell lymphoma.^{1 18}

Monitor patients for manifestations of neuropathy (e.g., burning sensation, hyperesthesia, hypoesthesia, paresthesia, discomfort, neuropathic pain, weakness).^{1 18} Adjust dosage and/or frequency of administration if new-onset or exacerbation of peripheral neuropathy occurs.¹ (See Dosage under Dosage and Administration.)

Use in patients with preexisting severe neuropathy only after careful assessment of the risks and benefits for the individual patient.¹

Cardiac Effects

Acute development or exacerbation of CHF and/or new onset of decreased left ventricular ejection fraction reported, including in patients with few or no risk factors for decreased left ventricular ejection fraction.¹ Other heart failure events (e.g., acute pulmonary edema, pulmonary edema, cardiac failure, congestive cardiac failure, cardiogenic shock) also reported.¹ Risk of death from cardiogenic shock, CHF, cardiac arrest, or cardiopulmonary arrest.¹ Closely monitor patients with existing heart disease or patients with increased risk for heart disease.¹

Prolongation of QT_c interval reported; however, causal relationship with bortezomib not established.¹

Hypotension

Risk of severe (grade 3) hypotension, orthostatic hypotension, and syncope.¹

Use with caution in patients with history of syncope or who are dehydrated or receiving drugs associated with hypotension.¹

Orthostatic hypotension may be managed with adjustment of antihypertensive therapy, hydration, or administration of mineralocorticoids and/or sympathomimetics.¹

Respiratory Effects

Risk of dyspnea.¹ Fatal respiratory insufficiency/failure reported.¹ Pneumonitis, interstitial pneumonia, lung infiltration, and ARDS reported rarely; sometimes fatal.¹ Pulmonary hypertension (in absence of left heart failure or significant pulmonary disease) also reported.¹⁸

If onset or worsening of cardiopulmonary symptoms occurs, promptly conduct comprehensive diagnostic evaluation.¹⁸

Reversible Posterior Leukoencephalopathy Syndrome (RPLS)

RPLS reported.¹⁸ May manifest as seizures, hypertension, headache, lethargy, confusion, blindness, and other visual and neurologic disturbances.¹⁸ Brain imaging, preferably MRI, necessary to confirm diagnosis.¹⁸

If RPLS develops, discontinue bortezomib.¹⁸ Safety of reinitiating bortezomib in patients previously experiencing RPLS not known.¹⁸

GI Effects

Risk of nausea, diarrhea, constipation, and vomiting; ileus also may occur.^{1 18}

Adverse GI effects may be severe and require use of antiemetics and antidiarrheals.¹ Fluid and electrolyte replacement recommended to prevent dehydration.¹

Hematologic Effects

Risk of severe (grade 3 or 4) thrombocytopenia.¹ Platelet count nadir typically occurs on day 11 of each treatment cycle and returns to baseline by next cycle.¹ Pattern of platelet count decrease and recovery remains consistent over 8 treatment cycles of twice-weekly dosing; no evidence of cumulative thrombocytopenia.¹ Platelet count nadir averages approximately 40% of baseline.¹ Risk of GI and intracerebral hemorrhage associated with thrombocytopenia.¹

Risk of severe (grade 3 or 4) neutropenia.¹ Neutrophil count nadir typically occurs on day 11 of each treatment cycle and returns to baseline by next cycle.¹ Pattern of neutrophil count decrease and recovery remains consistent over 8 treatment cycles of twice-weekly dosing; no evidence of cumulative neutropenia.¹

Risk of febrile neutropenia and severe (grade 3) anemia.¹

Monitor platelet count prior to each dose.¹ In addition, regularly monitor CBC during treatment and adjust dosage as appropriate.^{1 18} (See Dosage under Dosage and Administration.) Consider transfusions when deemed necessary.¹

Tumor Lysis Syndrome

Possible tumor lysis syndrome following rapid lysis of malignant cells.¹ Increased risk in patients with large tumor burden; closely monitor such patients and take appropriate precautions.¹

Hepatic Effects

Acute liver failure reported in patients with serious underlying medical conditions who were receiving bortezomib with multiple concomitant drugs.²² Increases in hepatic enzyme concentrations, hyperbilirubinemia, and hepatitis also reported; may be reversible upon discontinuance of bortezomib.^{16 22} Information on results of rechallenge in these patients is limited.²² (See Hepatic Impairment under Dosage and Administration.)

Specific Populations

Pregnancy

Category D.¹ (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Lactation

Not known whether bortezomib is distributed into milk.¹ Discontinue nursing or the drug because of potential risk to nursing infants; consider importance of drug to the woman.¹⁸

Pediatric Use

Safety and efficacy not established in children <18 years of age.^{1 6}

Geriatric Use

No overall differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.¹ In clinical studies, patients ≥65 years of age with relapsed multiple myeloma had higher overall response rates and higher incidence of grade 3 or 4 adverse effects compared with younger adults.^{1 18}

Hepatic Impairment

Increased exposure to bortezomib in patients with moderate or severe hepatic impairment; reduce dosage and monitor closely for adverse effects.^{22 23} (See Hepatic Impairment under Dosage and Administration and Special Populations under Pharmacokinetics.)

Renal Impairment

Pharmacokinetics not affected by renal impairment.¹⁸ (See Renal Impairment under Dosage and Administration and Special Populations under Pharmacokinetics.)

Common Adverse Effects

Asthenic conditions (including fatigue, malaise, and weakness), diarrhea, nausea, constipation, peripheral neuropathy, vomiting, pyrexia, thrombocytopenia, psychiatric disorders, decreased appetite and anorexia, neutropenia, neuralgia, leukopenia, anemia.¹⁸

Interactions for Bortezomib

Appears to be metabolized principally by CYP isoenzymes 3A4, 2C19, and 1A2; metabolism by CYP2D6 and CYP2C9 is minor.^{1 5} May inhibit CYP2C19; poor inhibitor of CYP isoenzymes 1A2, 3A4, 2C9, and 2D6.¹ Does not induce CYP1A2 or CYP3A4 in vitro.¹

Drugs Affecting Hepatic Microsomal Enzymes

Inhibitors or inducers of CYP3A4: Potential pharmacokinetic interaction.¹ Closely monitor patients for potential toxicities or reduced efficacy.^{1 18}

Drugs Metabolized by Hepatic Microsomal Enzymes

Potential pharmacokinetic interaction (increased exposure to drugs metabolized by CYP2C19).¹

Specific Drugs

Drug	Interaction	Comment
Antidiabetic agents, oral	Possible hypoglycemia or hyperglycemia1 5	Monitor blood glucose concentrations carefully and adjust dosage of antidiabetic agent1
Hypotensive agents	Increased risk of hypotension1	Dosage adjustment of hypotensive agents may be necessary1
Ketoconazole	Increased bortezomib AUC18	Closely monitor for potential toxicities if used concomitantly18
Melphalan	Concomitant administration with melphalan and prednisone caused a 17% increase in mean bortezomib AUC18	Unlikely to be clinically relevant18
Omeprazole	Concomitant administration did not affect bortezomib exposure18
Prednisone	Concomitant administration with melphalan and prednisone caused a 17% increase in mean bortezomib AUC18	Unlikely to be clinically relevant18
Ritonavir	Possible increased bortezomib exposure18	Closely monitor for potential toxicities if used concomitantly18

Bortezomib Pharmacokinetics

Absorption

Bioavailability

Mean dose-normalized peak plasma concentration and AUC of bortezomib are comparable between male and female patients.¹⁸

Onset

Maximum inhibition of 20S proteasome activity (relative to baseline) in whole blood observed 5 minutes following administration.¹⁸ Maximum inhibition of 20S proteasome activity is comparable following administration of bortezomib doses of 1 mg/m² (70–84%) and 1.3 mg/m² (73–83%).¹⁸

Special Populations

Exposure increased about 60% in patients with moderate (i.e., bilirubin concentrations >1.5–3 times ULN with any AST concentrations) or severe (i.e., bilirubin concentrations >3 times ULN with any AST concentrations) hepatic impairment.^{22 23}

In patients with varying degrees of renal impairment or normal renal function, exposure (based on dose-normalized AUC and maximum plasma concentrations) was comparable among all the groups.¹⁸ Dialysis may decrease concentrations; administer after a dialysis procedure.¹⁸ (See Renal Impairment under Dosage and Administration.)

Mean dose-normalized peak plasma concentration and AUC of bortezomib are 25% lower in patients <65 years of age than in those ≥65 years of age.¹⁸

Distribution

Extent

Distributed extensively to peripheral tissues.¹⁸

Not known whether bortezomib is distributed into milk.¹

Plasma Protein Binding

83%.¹

Elimination

Metabolism

Metabolized principally by CYP3A4, 2C19, and 1A2 to inactive metabolites; metabolism by CYP2D6 and 2C9 is minor.^{1 5}

Elimination Route

Elimination pathways have not been characterized in humans.¹

Half-life

40–193 or 76–108 hours following multiple dosing with 1- or 1.3-mg/m² regimen, respectively.¹⁸

Stability

Storage

Parenteral

Powder for Injection

25°C (may be exposed to 15–30°C) in original package.¹ Protect from light.¹

Store reconstituted solution at 25°C in the original vial⁶ or in the syringe for up to 8 hours.¹

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility

Compatible1
Sodium chloride 0.9%

Actions

• 
  

  A modified dipeptidyl boronic acid.^{1 4 5}

  
  


• 
  

  Reversibly inhibits the 26S proteasome, a large protein complex that degrades ubiquitinated proteins, preventing targeted proteolysis and causing disruption of normal homeostatic mechanisms, which can lead to cell death.^{1 5}

  
  


• 
  

  Cytotoxic to a variety of cancer cell types in vitro.^{1 5}

  
  


• 
  

  Has been shown to delay tumor growth in tumor models, including multiple myeloma.¹

  
  

Advice to Patients

• 
  

  Risk of fatigue, dizziness, syncope, orthostatic hypotension, diplopia, or blurred vision; avoid driving or operating machinery if these symptoms occur.¹

  
  


• 
  

  Advise women to use an effective method of contraception and to avoid breast-feeding while receiving bortezomib therapy.¹ Importance of women informing a clinician immediately if they are or plan to become pregnant or plan to breast-feed.¹ Advise pregnant women of risk to the fetus.¹

  
  


• 
  

  Importance of taking appropriate measures to avoid dehydration caused by vomiting and/or diarrhea.¹ Importance of informing clinician if dizziness or light-headedness develops and immediately seeking medical attention if fainting occurs.¹

  
  


• 
  

  For patients with diabetes receiving oral antidiabetic agents, importance of monitoring blood glucose concentrations frequently and informing clinician of any unusual change.¹

  
  


• 
  

  Importance of informing clinician of new-onset or worsening symptoms of peripheral neuropathy (e.g., tingling, numbness, pain, burning sensation in hands or feet, weakness in arms or legs).¹

  
  


• 
  

  Importance of informing clinician if shortness of breath, cough, swelling (of the feet, ankles, or legs), rash, convulsion, persistent headache, reduced eyesight, increase in BP, or blurred vision occurs.^{1 18}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.¹

  
  


• 
  

  Importance of informing patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Bortezomib

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	For injection, for IV use only	3.5 mg	Velcade	Millennium

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions August 11, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Millennium Pharmaceuticals. Velcade(bortezomib) for injection prescribing information. Cambridge, MA; 2006 Mar.

2. Food and Drug Administration, Center for Drug Evaluation and Research. Drug information: questions and answers on Velcade. From FDA website.

3. Anon. Press release: FDA approves VELCADE (bortezomib) for injection for the treatment of relapsed and refractory multiple myeloma. May 13, 2003. From Millennium website.

4. Richardson PG, Barlogie B, Berenson J et al. A phase 2 study of bortezomib in relapsed, refractory myeloma. N Engl J Med. 2003; 348:2609-17. [IDIS 500112] [PubMed 12826635]

5. Anon. Bortezomomib (Velcade) for multiple myeloma. Med Lett Drugs Ther. 2003; 45:57-58. [PubMed 12865865]

6. Millennium, Cambridge, MA: Personal communication.

7. Multiple myeloma and other plasma cell neoplasms. From: PDQ. Physician data query (database). Bethesda, MD: National Cancer Institute; 2005 Apr 12.

8. Richardson PG, Sonneveld P, Schuster MW et al. Bortezomib or high-dose dexamethasone for relapsed multiple myeloma. N Engl J Med. 2005; 352:2487-98. [IDIS 535206] [PubMed 15958804]

9. Dispenzieri A. Bortezomib for myeloma—much ado about something. N Engl J Med. 2005; 352:2546-8. [IDIS 535212] [PubMed 15958811]

10. Jagannath S, Barlogie B, Berenson J et al. A phase 2 study of two doses of bortezomib in relapsed or refractory myeloma. Br J Haematol. 2004; 127:165-72. [PubMed 15461622]

11. Jagannath S, Barlogie B, Berenson JR et al. Bortezomib in recurrent and/or refractory multiple myeloma. Initial clinical experience in patients with impaired renal function. Cancer. 2005; 103:1195-200. [IDIS 530731] [PubMed 15690325]

12. Adult non-Hodgkin's lymphoma. From: PDQ. Physician data query (database). Bethesda, MD: National Cancer Institute; 2005 Jun 23.

13. Goy A, Younes A, McLaughlin P et al. Phase II study of proteasome inhibitor bortezomib in relapsed or refractory B-cell non-Hodgkin's lymphoma. J Clin Oncol. 2005; 23:667-75. [IDIS 532649] [PubMed 15613697]

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10002. Harousseau JL, Mathiot C, Attal M, et al. Velcade/Dexamethasone (Vel/D) versus VAD as induction treatment prior to autologous stem cell transplantation (ASCT) in newly diagnosed multiple myeloma (MM): updated results of the IFM 2005/01 trial. Blood. 2007; 110: Abstract 450 (presented at the 49th annual ASH meeting. Atlanta, GA: 2007 Dec 10).

10003. Cavo M, Patriarca F, Tacchetti P, et al. Bortezomib-thalidomide-dexamethasone (VTD) versus thalidomide-dexamethasone (TD) in preparation for autologous stem-cell (SC) transplantation (ASCT) in newly diagnosed multiple myeloma (MM). Blood. 2007. 110; Abstract 73 (presented at the 49th annual ASH meeting. Atlanta, GA: 2007 Dec 9).

10004. Palumbo A, Avonto I, Patriarca F et al. Bortezomib, pegylated-lyposomal-doxorubicin and dexamethasone followed by melphalan 100 mg/m2 in elderly new diagnosed patients: an interim analysis. Blood. 2007; 110: Abstract 448 (presented at the 49th annual ASH meeting. Atlanta, GA: 2007 Dec 10).

10005. Popat R, Oakervee H, Hallam S, et al. Bortezomib, doxorubicin, and dexamethasone (PAD) front line treatment of multiple myeloma: updated results after long term follow up. Br J Haematol. 2008; 141: 512-516.

10006. Reeder CB, Stewart AK, Hentz JG et al. Efficacy of induction with CyBorD in newly diagnosed multiple myeloma. J Clin Oncol. 2008; 26: Abstract 8517 (presented at the 44th Annual ASCO meeting. Chicago, IL: 2008 May 31).

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