Aromenal

Aromenal may be available in the countries listed below.

Ingredient matches for Aromenal

Anastrozole

Anastrozole is reported as an ingredient of Aromenal in the following countries:

• Argentina

International Drug Name Search

Combantrin

Combantrin may be available in the countries listed below.

Ingredient matches for Combantrin

Albendazole

Albendazole is reported as an ingredient of Combantrin in the following countries:

• India

Pyrantel

Pyrantel is reported as an ingredient of Combantrin in the following countries:

• Bulgaria

Pyrantel embonate (a derivative of Pyrantel) is reported as an ingredient of Combantrin in the following countries:

• Austria


• Bahrain


• Canada


• Chile


• Colombia


• Ethiopia


• France


• Ghana


• Greece


• Guyana


• India


• Israel


• Italy


• Japan


• Jordan


• Kenya


• Kuwait


• Lebanon


• Liberia


• Malawi


• Mexico


• New Zealand


• Nigeria


• Peru


• Philippines


• Portugal


• Saudi Arabia


• Sierra Leone


• Sri Lanka


• Sudan


• United Arab Emirates


• Venezuela


• Vietnam

International Drug Name Search

Kontal

Kontal may be available in the countries listed below.

Ingredient matches for Kontal

Niclosamide

Niclosamide is reported as an ingredient of Kontal in the following countries:

• Finland

International Drug Name Search

Equiphen

In some countries, this medicine may only be approved for veterinary use.

Ingredient matches for Equiphen

Phenylbutazone

Phenylbutazone is reported as an ingredient of Equiphen in the following countries:

• United States

International Drug Name Search

Vicnite

Vicnite may be available in the countries listed below.

Ingredient matches for Vicnite

Diphenhydramine

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

• Mexico

International Drug Name Search

Librium

In the US, Librium (chlordiazepoxide systemic) is a member of the drug class benzodiazepines and is used to treat Alcohol Withdrawal, Anxiety, Burning Mouth Syndrome and Light Sedation.

US matches:

• Librium


• Librium Injection

Ingredient matches for Librium

Chlordiazepoxide

Chlordiazepoxide is reported as an ingredient of Librium in the following countries:

• Bahrain


• Germany


• Hong Kong


• Hungary


• India


• Indonesia


• Ireland


• South Africa

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

• Italy


• Malta


• United States

International Drug Name Search

Medopred

Medopred may be available in the countries listed below.

Ingredient matches for Medopred

Prednisolone

Prednisolone 21-(disodium phosphate) (a derivative of Prednisolone) is reported as an ingredient of Medopred in the following countries:

• Russian Federation

International Drug Name Search

Voltaren Oftalmico

Voltaren Oftalmico may be available in the countries listed below.

Ingredient matches for Voltaren Oftalmico

Diclofenac

Diclofenac sodium salt (a derivative of Diclofenac) is reported as an ingredient of Voltaren Oftalmico in the following countries:

• Chile


• Peru

International Drug Name Search

dirithromycin

Generic Name: dirithromycin (dir ith roe MYE sin)

Brand names: Dynabac, Dynabac D5-Pak

What is dirithromycin?

Dirithromycin is in a class of drugs called macrolide antibiotics. Dirithromycin fights bacteria in your body.

Dirithromycin is used to treat many different types of bacterial infections, such as bronchitis, pneumonia, tonsillitis, and skin infections.

Dirithromycin may also be used for purposes other than those listed in this medication guide.

What is the most important information I should know about dirithromycin?

Take all of the dirithromycin that has been prescribed for you even if you begin to feel better. Your symptoms may start to improve before the infection is completely treated. Take dirithromycin with food or within 1 hour of eating to increase the absorption of the drug by your body. Do not break, crush, or chew the tablets. Swallow them whole.

Who should not take dirithromycin?

Before taking dirithromycin, tell your doctor if you have liver disease. You may not be able to take dirithromycin, or you may require a lower dose or special monitoring during therapy.

Dirithromycin is in the FDA pregnancy category C. This means that it is not known whether dirithromycin will harm an unborn baby. Do not take this medication without first talking to your doctor if you are pregnant. It is not known whether dirithromycin passes into breast milk. Do not take this medication without first talking to your doctor if you are breast-feeding a baby. Dirithromycin has not been approved for use in children younger than 12 years of age.

How should I take dirithromycin?

Take dirithromycin exactly as directed by your doctor. If you do not understand these instructions, ask your pharmacist, nurse, or doctor to explain them to you.

Take each dose with a full glass (8 ounces) of water. Take dirithromycin with food or milk to increase the absorption of the drug into your body. Do not break, crush, or chew the tablets. Swallow them whole. Take all of the dirithromycin that has been prescribed for you even if you begin to feel better. Your symptoms may start to improve before the infection is completely treated. Store this medication at room temperature away from moisture and heat.

See also: Dirithromycin dosage (in more detail)

What happens if I miss a dose?

Take the missed dose as soon as you remember. However, if it is almost time for your next regularly scheduled dose, skip the missed dose and take the next one as directed. Do not take a double dose of this medication unless otherwise directed by your doctor.

What happens if I overdose?

Seek emergency medical attention.

Symptoms of a dirithromycin overdose include nausea, vomiting, diarrhea, and abdominal discomfort.

What should I avoid while taking dirithromycin?

Avoid prolonged exposure to sunlight. Dirithromycin may increase the sensitivity of your skin to sunlight. Use a sunscreen and wear protective clothing when exposure to the sun is unavoidable.

Dirithromycin side effects

If you experience any of the following serious side effects, stop taking dirithromycin and seek emergency medical attention:

• 
  

  an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives); or

  
  


• 
  

  liver damage (yellowing of the skin or eyes, nausea, abdominal pain or discomfort, unusual bleeding or bruising, severe fatigue).

  
  

Other, less serious side effects may be more likely to occur. Continue to take dirithromycin and talk to your doctor if you experience

• 
  

  nausea, vomiting, diarrhea, or abdominal pain;

  
  


• 
  

  dizziness, fatigue, or headache;

  
  


• 
  

  vaginal yeast infection; or

  
  


• 
  

  a rash.

  
  

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.

Dirithromycin Dosing Information

Usual Adult Dose for Bronchitis:

Moraxella Catarrhalis or Streptococcus Pneumoniae: 500 mg orally once a day for 7 days.

Usual Adult Dose for Tonsillitis/Pharyngitis:

Streptococcus Pyogenes: 500 mg orally once a day for 10 days.

Usual Adult Dose for Skin or Soft Tissue Infection:

Staphylococcus Aureus (methicillin-susceptible): 500 mg orally once a day for 7 days.

Usual Adult Dose for Legionella Pneumonia:

500 mg orally once a day for 14 days.

Usual Adult Dose for Mycoplasma Pneumonia:

500 mg orally once a day for 14 days.

Usual Adult Dose for Pneumonia:

500 mg orally once a day for 14 days.

Usual Adult Dose for Otitis Media:

500 mg orally once a day for 10 days.

Usual Adult Dose for Upper Respiratory Tract Infection:

500 mg orally once a day for 7 days.

Usual Pediatric Dose for Bronchitis:

Child > 12 years: Moraxella Catarrhalis or Streptococcus Pneumoniae: 500 mg orally once a day for 7 days.

Usual Pediatric Dose for Pneumonia:

Child > 12 years: Legionella Pneumophila, Mycoplasma Pneumoniae, or Streptococcus Pneumoniae: 500 mg orally once a day for 14 days.

Usual Pediatric Dose for Tonsillitis/Pharyngitis:

Child > 12 years: Streptococcus Pyogenes: 500 mg orally once a day for 10 days.

Usual Pediatric Dose for Skin or Soft Tissue Infection:

Child > 12 years: Staphylococcus Aureus (methicillin-susceptible): 500 mg orally once a day for 7 days.

What other drugs will affect dirithromycin?

Other drugs in the same class as dirithromycin have caused dangerous side effects when taken with terfenadine (Seldane). Although dirithromycin has not caused the same reaction, it should be used cautiously if at all while you are taking terfenadine (Seldane).

Before taking this medication, tell your doctor if you are taking any of the following drugs:

• 
  

  seizure medications such as carbamazepine (Tegretol), phenytoin (Dilantin), and valproic acid (Depakote, Depakene) may or may not be affected. Since these drugs are so important, your doctor may want to perform some special blood-monitoring tests.

  
  


• 
  

  anticoagulants (blood thinners) such as warfarin (Coumadin). These medications may have an increased effect, which could lead to bleeding. Your doctor may want to monitor your blood clotting.

  
  


• 
  

  heart medications for irregular heartbeats, such as digoxin (Lanoxin). These drugs may also have an increased effect. Your doctor may want to monitor your blood levels more closely.

  
  


• 
  

  other antibiotics. Do not use other antibiotics unless they are prescribed by your doctor.

  
  

Drugs other than those listed here may also interact with dirithromycin. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines.

More dirithromycin resources

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

• dirithromycin Advanced Consumer (Micromedex) - Includes Dosage Information


• Dirithromycin Professional Patient Advice (Wolters Kluwer)

Compare dirithromycin with other medications

• Bronchitis
• Legionella Pneumonia
• Mycoplasma Pneumonia
• Otitis Media
• Pneumonia
• Skin Infection
• Tonsillitis/Pharyngitis
• Upper Respiratory Tract Infection

Where can I get more information?

• Your pharmacist has additional information about dirithromycin written for health professionals that you may read.

What does my medication look like?

Dirithromycin is available with a prescription under the brand name Dynabac. Other brand or generic formulations may also be available. Ask your pharmacist any questions you have about this medication, especially if it is new to you.

• 
  

  Dynabac 250 mg--elliptical, white, enteric-coated tablets

  
  

See also: dirithromycin side effects (in more detail)

Rosken Skin Repair

Rosken Skin Repair may be available in the countries listed below.

Ingredient matches for Rosken Skin Repair

Dimeticone

Dimeticone is reported as an ingredient of Rosken Skin Repair in the following countries:

• Australia

International Drug Name Search

Tizanon

Tizanon may be available in the countries listed below.

Ingredient matches for Tizanon

Nizatidine

Nizatidine is reported as an ingredient of Tizanon in the following countries:

• Japan

International Drug Name Search

Menfegol

Scheme

Rec.INN

CAS registry number (Chemical Abstracts Service)

0057821-32-6

Chemical Formula

(C2-H4-O)n·C16-H24-O

Therapeutic Category

Contraceptive, spermicidal agent

Chemical Name

alfa-[p-(p-Menthyl)phenyl]-omega-hydroxypoly(oxyethylene)

Foreign Names

• Menfegolum (Latin)
• Menfegol (German)
• Menfegol (French)
• Menfegol (Spanish)

Generic Name

• Menphegol (IS)

Brand Names

• Neo Sampoon
  Eisai, Hong Kong; Eisai, Singapore



• Neosampoon
  Eisai, Taiwan

International Drug Name Search

Glossary

IS	Inofficial Synonym
Rec.INN	Recommended International Nonproprietary Name (World Health Organization)

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

Drixoral

In the US, Drixoral (dexbrompheniramine/pseudoephedrine systemic) is a member of the drug class upper respiratory combinations and is used to treat Cold Symptoms, Hay Fever, Nasal Congestion and Sinus Symptoms.

US matches:

• Drixoral


• Drixoral Cold/Flu Controlled-Release Tablets


• Drixoral Non-Drowsy Sustained-Release Capsules


• Drixoral Sinus Sustained-Release Tablets


• Drixoral Allergy Sinus


• Drixoral Cold and Flu


• Drixoral Cough/Sore Throat


• Drixoral Decongestant Non-Drowsy


• Drixoral Sinus

Ingredient matches for Drixoral

Dexbrompheniramine

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

• Indonesia

Pseudoephedrine

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

• United States

Pseudoephedrine sulfate (a derivative of Pseudoephedrine) is reported as an ingredient of Drixoral in the following countries:

• Indonesia

International Drug Name Search

Comadex

Comadex may be available in the countries listed below.

Ingredient matches for Comadex

Tamsulosin

Tamsulosin is reported as an ingredient of Comadex in the following countries:

• Ecuador

International Drug Name Search

Levosulpiride

Scheme

Rec.INN

ATC (Anatomical Therapeutic Chemical Classification)

N05AL07

CAS registry number (Chemical Abstracts Service)

0023672-07-3

Chemical Formula

C15-H23-N3-O4-S

Molecular Weight

341

Therapeutic Categories

Antiemetic

Neuroleptic

Chemical Name

(1)-N-[[(S)-1-Ethyl-2-pyrrolidinyl]methyl]-5-sulfamoyl-oanisamide

Foreign Names

• Levosulpiridum (Latin)
• Levosulpirid (German)
• Lévosulpiride (French)
• Levosulpirida (Spanish)

Generic Name

• (S)-(-)-Sulpirid (IS)

Brand Names

• Dislep
  Abbott, Mexico; Bagó, Argentina; Bagó, Ecuador; Biotoscana, Colombia; Ferrer, Costa Rica; Ferrer, Dominican Republic; Ferrer, Guatemala; Ferrer, Honduras; Ferrer, Nicaragua; Ferrer, Panama; Ferrer, Peru; Ferrer, El Salvador; Leti, Venezuela; Silesia, Chile



• Endacine
  Andromaco, Chile



• Levobren
  GiEnne, Italy



• Levogastrol
  Salvat, Spain



• Levopraid
  Abbott, Italy; CSC, Bulgaria; Hospira, Bulgaria; Knoll, Romania; Therabel, Belgium; Therabel, Luxembourg



• Pausedal
  Alter, Spain

International Drug Name Search

Glossary

IS	Inofficial Synonym
Rec.INN	Recommended International Nonproprietary Name (World Health Organization)

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

Ferrum Hausmann

Ferrum Hausmann may be available in the countries listed below.

In some countries, this medicine may only be approved for veterinary use.

Ingredient matches for Ferrum Hausmann

Ferrous Fumarate

Ferrous Fumarate is reported as an ingredient of Ferrum Hausmann in the following countries:

• Luxembourg


• Romania


• Switzerland

Iron Dextran

Iron Dextran is reported as an ingredient of Ferrum Hausmann in the following countries:

• Switzerland

Iron Polymaltose

Iron Polymaltose is reported as an ingredient of Ferrum Hausmann in the following countries:

• Dominican Republic


• El Salvador


• Germany


• Greece


• Guatemala


• Honduras


• Hong Kong


• Luxembourg


• Nicaragua


• Panama


• Portugal


• Romania


• Taiwan


• Turkey

International Drug Name Search

dirithromycin

dye-rith-roe-MYE-sin

Commonly used brand name(s)

In the U.S.

• Dynabac


• Dynabac D5-Pak

Available Dosage Forms:

• Tablet, Enteric Coated

Therapeutic Class: Antibiotic

Chemical Class: Macrolide

Uses For dirithromycin

Dirithromycin is used to treat bacterial infections in many different parts of the body. It works by killing bacteria or preventing their growth. However, dirithromycin will not work for colds, flu, or other virus infections.

Dirithromycin was available only with your doctor's prescription.

Dirithromycin is no longer available in the United States.

Before Using dirithromycin

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 dirithromycin, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to dirithromycin 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

Studies on dirithromycin have been only in adult patients, and there is no specific information comparing use of dirithromycin in children with use in other age groups.

Geriatric

dirithromycin has been tested in a limited number of elderly patients and has not been shown 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. When you are taking dirithromycin, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using dirithromycin with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Dihydroergotamine


• Ergoloid Mesylates


• Ergonovine


• Ergotamine


• Methylergonovine


• Methysergide


• Pimozide

Using dirithromycin with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Dofetilide

Using dirithromycin with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Cyclosporine


• Fentanyl

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 dirithromycin. Make sure you tell your doctor if you have any other medical problems, especially:

• Liver disease—Patients with moderate to severe liver disease may have an increased chance of side effects.

Proper Use of dirithromycin

Dirithromycin should be taken with food or within 1 hour after eating.

To help clear up your infection completely, keep taking dirithromycin for the full time of treatment, even if you begin to feel better after a few days. If you stop taking dirithromycin too soon, your symptoms may return.

Do not cut, crush, or chew dirithromycin tablets.

Dosing

The dose of dirithromycin 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 dirithromycin. 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 oral dosage form (tablets):
  
  • For bacterial infections:
    
    • Adults and teenagers—500 milligrams (mg) once a day for seven to fourteen days.
    
    
    • Children up to 12 years of age—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

If you miss a dose of dirithromycin, 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

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using dirithromycin

If your symptoms do not improve within a few days, or if they become worse, check with your doctor.

dirithromycin 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:

Rare

• Abdominal tenderness


• fever


• severe abdominal or stomach cramps and pain


• watery and severe diarrhea, which may also be bloody

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:

Less common

• Diarrhea


• dizziness


• headache


• nausea


• vomiting


• weakness

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: dirithromycin 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 dirithromycin resources

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

• dirithromycin Concise Consumer Information (Cerner Multum)


• Dirithromycin Professional Patient Advice (Wolters Kluwer)

Compare dirithromycin with other medications

• Bronchitis
• Legionella Pneumonia
• Mycoplasma Pneumonia
• Otitis Media
• Pneumonia
• Skin Infection
• Tonsillitis/Pharyngitis
• Upper Respiratory Tract Infection

Promote

Promote may be available in the countries listed below.

In some countries, this medicine may only be approved for veterinary use.

Ingredient matches for Promote

Tylosin

Tylosin is reported as an ingredient of Promote in the following countries:

• South Africa

International Drug Name Search

Diclofenac Diethylamine

Diclofenac Diethylamine may be available in the countries listed below.

Ingredient matches for Diclofenac Diethylamine

Diclofenac

Diclofenac Diethylamine (BANM) is known as Diclofenac in the US.

International Drug Name Search

Glossary

BANM	British Approved Name (Modified)

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

Bucoxidina

Bucoxidina may be available in the countries listed below.

Ingredient matches for Bucoxidina

Chlorhexidine

Chlorhexidine digluconate (a derivative of Chlorhexidine) is reported as an ingredient of Bucoxidina in the following countries:

• Peru

International Drug Name Search

H.A.C.

H.A.C. may be available in the countries listed below.

Ingredient matches for H.A.C.

Cetrimonium

Cetrimonium bromide (a derivative of Cetrimonium) is reported as an ingredient of H.A.C. in the following countries:

• Belgium

Chlorhexidine

Chlorhexidine digluconate (a derivative of Chlorhexidine) is reported as an ingredient of H.A.C. in the following countries:

• Belgium

International Drug Name Search

Carvedilol Normon

Carvedilol Normon may be available in the countries listed below.

Ingredient matches for Carvedilol Normon

Carvedilol

Carvedilol is reported as an ingredient of Carvedilol Normon in the following countries:

• Spain

International Drug Name Search

Camphor

In some countries, this medicine may only be approved for veterinary use.

Scheme

Ph. Eur.

ATC (Anatomical Therapeutic Chemical Classification)

C01EB02

CAS registry number (Chemical Abstracts Service)

0000076-22-2

Chemical Formula

C10-H16-O

Molecular Weight

152

Therapeutic Category

Antipruritic

Chemical Names

(1RS,4RS)-1,7,7-Trimethylbicylo[2.2.1]heptan-2-one (Ph. Eur.)

2-Bornanone (USP)

2-Camphanone

2-Keto-1,7,7-trimethyl-norcamphane

Bicyclo[2.2.1]heptane-2-one, 1,7,7-trimethyl- (USP)

DL-2-Bornanone

Foreign Names

• Camphora racemica (Latin)
• Kampfer, racemisch (German)
• Camphre racémique (French)
• Alcanfor racémico (Spanish)

Generic Names

• Camphre (OS: DCF)
• dl-Camphor (OS: JAN)
• Dextrocamphora (IS)
• Formosa camphor (IS)
• Gum camphor (IS)
• Laurel camphor (IS)
• Campher, racemischer (PH: Ph. Helv. 10)
• Camphor (PH: USP 32)
• Camphor Racemic (PH: Ph. Eur. 6, BP 2010)
• Camphre racémique (PH: Ph. Eur. 6)
• dl-Camphor (PH: JP XV)
• d-Camphor (OS: JAN)
• Dextrocamphora (IS)
• Japanese camphor (IS)
• Campher, D- (PH: Ph. Helv. 10)
• d-Camphor (PH: JP XV)
• D-Camphor (PH: Ph. Eur. 6)
• D-Camphre (PH: Ph. Eur. 6)
• Natural Camphor (PH: BP 2010)

Brand Names

• Camphenic (Camphor and Phenol)
  Agusa Nippon, Japan



• Camphoderm N
  Li-iL, Germany



• Camphor Spirit
  Fudjimi Seiyakushiyo, Japan



• Camphor
  Kozakai Seiyaku, Japan



• Camphorae Spiritus
  Chemax Pharma, Bulgaria



• Camphorin (Camphor and Salicylic Acid)
  Nisshin Seiyaku - Yamagata, Japan



• Camphrice de Canada
  Homme de Fer, France



• Dermacort (Camphor and Hydrocortisone)
  Tanabe, Indonesia



• Inongan (Camphor and Methyl Salicylate)
  Sofibel, France



• Murakami Camphenic (Camphor and Phenol)
  Agusa Nippon, Japan



• Pectocor N
  Riemser, Germany



• Reflexgel (Camphor and Methyl Salicylate)
  Reckitt Benckiser, Belgium



• Rheunervol
  Riemser, Germany



• Sanimastin (veterinary use)
  Virbac, Germany



• Unguentum Camphorato-Ichthamolicum (Camphor and Ichthammol)
  Vulm, Slovakia



• Vaopin
  Riemser, Germany



• Vicks Vaposteam
  Procter & Gamble, United States



• Vicks Inhaler N (Camphor and Levomenthol)
  Procter & Gamble, Switzerland



• Wick Inhalierstift (Camphor and Levomenthol)
  Wick, Germany



• Camphor
  Kozakai Seiyaku, Japan



• Canfora Afom
  AFOM, Italy



• Canfora Alvita
  Alvita, Italy



• Canfora Farmacologico
  Alvita, Italy



• Canfora Farve
  Farve, Italy



• Canfora Marco Viti
  Marco Viti, Italy



• Canfora New.Fa.Dem.
  New.Fa.dem., Italy



• Canfora Nova
  Nova Argentia, Italy



• Canfora Polifarma
  Polifarma, Italy



• Canfora Ramini
  Ramini, Italy



• Canfora Sella
  Sella, Italy



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Glossary

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IS	Inofficial Synonym
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OS	Official Synonym
PH	Pharmacopoeia Name
Ph. Eur.	European Pharmacopoeia
USP	Pharmacopoeia of the United States

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Octreotide

Generic Name: Octreotide acetate

Dosage Form: injection, solution
Octreotide Acetate Injection

Octreotide Description

Octreotide acetate injection, a cyclic octapeptide prepared as a clear sterile solution of Octreotide, acetate salt, in a buffered lactic acid solution for administration by deep subcutaneous (intrafat) or intravenous injection. Octreotide acetate, known chemically as L-Cysteinamide, D - phenylalanyl - L - cysteinyl - L - phenylalanyl - D - tryptophyl - L - lysyl - L - threonyl - N - [2 - hydroxy - 1 - (hydroxymethyl)propyl] - , cyclic (2→7)-disulfide; [R-(R*, R*)] acetate salt, is a long-acting octapeptide with pharmacologic actions mimicking those of the natural hormone somatostatin.

Octreotide acetate injection is available as: sterile 5 mL multi-dose vials in 2 strengths, containing 200 and 1000 mcg/mL of Octreotide (as acetate).

Each mL of the multi-dose vials also contains:

lactic acid, USP	3.4 mg
mannitol, USP	45 mg
phenol, USP	5.0 mg
sodium bicarbonate, USP	qs to pH 4.2 ± 0.3
water for injection, USP	qs to 1 mL

Lactic acid and sodium bicarbonate are added to provide a buffered solution, pH to 4.2 ± 0.3.

The molecular weight of Octreotide acetate is 1019.3 (free peptide, C49H66N10O10S2) and its amino acid sequence is:

Octreotide - Clinical Pharmacology

Octreotide acetate exerts pharmacologic actions similar to the natural hormone, somatostatin. It is an even more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin. Like somatostatin, it also suppresses LH response to GnRH, decreases splanchnic blood flow, and inhibits release of serotonin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide.

By virtue of these pharmacological actions, Octreotide acetate has been used to treat the symptoms associated with metastatic carcinoid tumors (flushing and diarrhea), and Vasoactive Intestinal Peptide (VIP) secreting adenomas (watery diarrhea).

Octreotide acetate substantially reduces growth hormone and/or IGF-I (somatomedin C) levels in patients with acromegaly.

Single doses of Octreotide acetate have been shown to inhibit gallbladder contractility and to decrease bile secretion in normal volunteers. In controlled clinical trials the incidence of gallstone or biliary sludge formation was markedly increased (see WARNINGS).

Octreotide acetate suppresses secretion of thyroid stimulating hormone (TSH).

Pharmacokinetics

After subcutaneous injection, Octreotide is absorbed rapidly and completely from the injection site. Peak concentrations of 5.2 ng/mL (100-mcg dose) were reached 0.4 hours after dosing. Using a specific radioimmunoassay, intravenous and subcutaneous doses were found to be bioequivalent. Peak concentrations and area under the curve values were dose proportional after intravenous single doses up to 200 mcg and subcutaneous single doses up to 500 mcg and after subcutaneous multiple doses up to 500 mcg t.i.d. (1500 mcg/day).

In healthy volunteers the distribution of Octreotide from plasma was rapid (tα1/2=0.2 h), the volume of distribution (Vdss) was estimated to be 13.6 L, and the total body clearance ranged from 7 L/hr to 10 L/hr. In blood, the distribution into the erythrocytes was found to be negligible and about 65% was bound in the plasma in a concentration-independent manner. Binding was mainly to lipoprotein and, to a lesser extent, to albumin.

The elimination of Octreotide from plasma had an apparent half-life of 1.7 to 1.9 hours compared with 1 to 3 minutes with the natural hormone. The duration of action of Octreotide acetate is variable but extends up to 12 hours depending upon the type of tumor. About 32% of the dose is excreted unchanged into the urine. In an elderly population, dose adjustments may be necessary due to a significant increase in the half-life (46%) and a significant decrease in the clearance (26%) of the drug.

In patients with acromegaly, the pharmacokinetics differ somewhat from those in healthy volunteers. A mean peak concentration of 2.8 ng/mL (100-mcg dose) was reached in 0.7 hours after subcutaneous dosing. The volume of distribution (Vdss) was estimated to be 21.6 ± 8.5 L and the total body clearance was increased to 18 L/h. The mean percent of the drug bound was 41.2%. The disposition and elimination half-lives were similar to normals.

In patients with renal impairment the elimination of Octreotide from plasma was prolonged and total body clearance reduced. In mild renal impairment (ClCR 40 to 60 mL/min) Octreotide t1/2 was 2.4 hours and total body clearance was 8.8 L/hr, in moderate impairment (ClCR 10 to 39 mL/min) t1/2 was 3.0 hours and total body clearance 7.3 L/hr, and in severely renally impaired patients not requiring dialysis (ClCR <10 mL/min) t1/2 was 3.1 hours and total body clearance was 7.6 L/hr. In patients with severe renal failure requiring dialysis, total body clearance was reduced to about half that found in healthy subjects (from approximately 10 L/hr to 4.5 L/hr).

Patients with liver cirrhosis showed prolonged elimination of drug, with Octreotide t1/2 increasing to 3.7 hr and total body clearance decreasing to 5.9 L/hr, whereas patients with fatty liver disease showed t1/2 increased to 3.4 hr and total body clearance of 8.2 L/hr.

Indications and Usage for Octreotide

Acromegaly

Octreotide acetate is indicated to reduce blood levels of growth hormone and IGF-I (somatomedin C) in acromegaly patients who have had inadequate response to or cannot be treated with surgical resection, pituitary irradiation, and bromocriptine mesylate at maximally tolerated doses. The goal is to achieve normalization of growth hormone and IGF-I (somatomedin C) levels (see DOSAGE AND ADMINISTRATION). In patients with acromegaly, Octreotide acetate reduces growth hormone to within normal ranges in 50% of patients and reduces IGF-I (somatomedin C) to within normal ranges in 50% to 60% of patients. Since the effects of pituitary irradiation may not become maximal for several years, adjunctive therapy with Octreotide acetate to reduce blood levels of growth hormone and IGF-I (somatomedin C) offers potential benefit before the effects of irradiation are manifested.

Improvement in clinical signs and symptoms or reduction in tumor size or rate of growth were not shown in clinical trials performed with Octreotide acetate; these trials were not optimally designed to detect such effects.

Carcinoid Tumors

Octreotide acetate is indicated for the symptomatic treatment of patients with metastatic carcinoid tumors where it suppresses or inhibits the severe diarrhea and flushing episodes associated with the disease.

Octreotide acetate studies were not designed to show an effect on the size, rate of growth or development of metastases.

Vasoactive Intestinal Peptide Tumors (VIPomas)

Octreotide acetate is indicated for the treatment of the profuse watery diarrhea associated with VIP-secreting tumors. Octreotide acetate studies were not designed to show an effect on the size, rate of growth or development of metastases.

Contraindications

Sensitivity to this drug or any of its components.

Warnings

Single doses of Octreotide acetate have been shown to inhibit gallbladder contractility and decrease bile secretion in normal volunteers. In clinical trials (primarily patients with acromegaly or psoriasis), the incidence of biliary tract abnormalities was 63% (27% gallstones, 24% sludge without stones, 12% biliary duct dilatation). The incidence of stones or sludge in patients who received Octreotide acetate for 12 months or longer was 52%. Less than 2% of patients treated with Octreotide acetate for 1 month or less developed gallstones. The incidence of gallstones did not appear related to age, sex or dose. Like patients without gallbladder abnormalities, the majority of patients developing gallbladder abnormalities on ultrasound had gastrointestinal symptoms. The symptoms were not specific for gallbladder disease. A few patients developed acute cholecystitis, ascending cholangitis, biliary obstruction, cholestatic hepatitis, or pancreatitis during Octreotide acetate therapy or following its withdrawal. One patient developed ascending cholangitis during Octreotide acetate therapy and died.

Precautions

General

Octreotide acetate alters the balance between the counter-regulatory hormones, insulin, glucagon and growth hormone, which may result in hypoglycemia or hyperglycemia. Octreotide acetate also suppresses secretion of thyroid stimulating hormone, which may result in hypothyroidism. Cardiac conduction abnormalities have also occurred during treatment with Octreotide acetate. However, the incidence of these adverse events during long-term therapy was determined vigorously only in acromegaly patients who, due to their underlying disease and/or the subsequent treatment they receive, are at an increased risk for the development of diabetes mellitus, hypothyroidism, and cardiovascular disease. Although the degree to which these abnormalities are related to Octreotide acetate therapy is not clear, new abnormalities of glycemic control, thyroid function and ECG developed during Octreotide acetate therapy as described below.

Risk of Pregnancy with Normalization of IGF-1 and GH

Although acromegaly may lead to infertility, there are reports of pregnancy in acromegalic women. In women with active acromegaly who have been unable to become pregnant, normalization of GH and IGF-1 may restore fertility. Female patients of childbearing potential should be advised to use adequate contraception during treatment with Octreotide.

The hypoglycemia or hyperglycemia which occurs during Octreotide acetate therapy is usually mild, but may result in overt diabetes mellitus or necessitate dose changes in insulin or other hypoglycemic agents. Hypoglycemia and hyperglycemia occurred on Octreotide acetate in 3% and 16% of acromegalic patients, respectively. Severe hyperglycemia, subsequent pneumonia, and death following initiation of Octreotide acetate therapy was reported in one patient with no history of hyperglycemia.

In patients with concomitant Type I diabetes mellitus, Octreotide acetate injection and Octreotide acetate for injectable suspension are likely to affect glucose regulation, and insulin requirements may be reduced. Symptomatic hypoglycemia, which may be severe, has been reported in these patients. In non-diabetics and Type II diabetics with partially intact insulin reserves, Octreotide acetate injection or Octreotide acetate for injectable suspension administration may result in decreases in plasma insulin levels and hyperglycemia. It is therefore recommended that glucose tolerance and antidiabetic treatment be periodically monitored during therapy with these drugs.

In acromegalic patients, 12% developed biochemical hypothyroidism only, 8% developed goiter, and 4% required initiation of thyroid replacement therapy while receiving Octreotide acetate. Baseline and periodic assessment of thyroid function (TSH, total and/or free T4) is recommended during chronic therapy.

In acromegalics, bradycardia (<50 bpm) developed in 25%; conduction abnormalities occurred in 10% and arrhythmias occurred in 9% of patients during Octreotide acetate therapy. Other EKG changes observed included QT prolongation, axis shifts, early repolarization, low voltage, R/S transition, and early R wave progression. These ECG changes are not uncommon in acromegalic patients. Dose adjustments in drugs such as beta-blockers that have bradycardia effects may be necessary. In one acromegalic patient with severe congestive heart failure, initiation of Octreotide acetate therapy resulted in worsening of CHF with improvement when drug was discontinued. Confirmation of a drug effect was obtained with a positive rechallenge.

Several cases of pancreatitis have been reported in patients receiving Octreotide acetate therapy.

Octreotide acetate may alter absorption of dietary fats in some patients.

In patients with severe renal failure requiring dialysis, the half-life of Octreotide acetate may be increased, necessitating adjustment of the maintenance dosage.

Depressed vitamin B12 levels and abnormal Schilling’s tests have been observed in some patients receiving Octreotide acetate therapy, and monitoring of vitamin B12 levels is recommended during chronic Octreotide acetate therapy.

Information for Patients

Careful instruction in sterile subcutaneous injection technique should be given to the patients and to other persons who may administer Octreotide acetate injection.

Laboratory Tests

Laboratory tests that may be helpful as biochemical markers in determining and following patient response depend on the specific tumor. Based on diagnosis, measurement of the following substances may be useful in monitoring the progress of therapy:

Acromegaly

Growth Hormone, IGF-I (somatomedin C) Responsiveness to Octreotide acetate may be evaluated by determining growth hormone levels at 1 to 4 hour intervals for 8 to 12 hours post dose. Alternatively, a single measurement of IGF-I (somatomedin C) level may be made two weeks after drug initiation or dosage change.

Carcinoid

5-HIAA (urinary 5-hydroxyindole acetic acid), plasma serotonin, plasma Substance P

VIPoma

VIP (plasma vasoactive intestinal peptide)

Baseline and periodic total and/or free T4 measurements should be performed during chronic therapy (see PRECAUTIONS: General).

Drug Interactions

Octreotide acetate has been associated with alterations in nutrient absorption, so it may have an effect on absorption of orally administered drugs. Concomitant administration of Octreotide acetate with cyclosporine may decrease blood levels of cyclosporine and result in transplant rejection.

Patients receiving insulin, oral hypoglycemic agents, beta blockers, calcium channel blockers, or agents to control fluid and electrolyte balance, may require dose adjustments of these therapeutic agents.

Concomitant administration of Octreotide and bromocriptine increases the availability of bromocriptine. Limited published data indicate that somatostatin analogs might decrease the metabolic clearance of compounds known to be metabolized by cytochrome P450 enzymes, which may be due to the suppression of growth hormones. Since it cannot be excluded that Octreotide may have this effect, other drugs mainly metabolized by CYP3A4 and which have a low therapeutic index (e.g., quinidine, terfenadine) should therefore be used with caution.

Drug Laboratory Test Interactions

No known interference exists with clinical laboratory tests, including amine or peptide determinations.

Carcinogenesis/Mutagenesis/Impairment of Fertility

Studies in laboratory animals have demonstrated no mutagenic potential of Octreotide acetate.

No carcinogenic potential was demonstrated in mice treated subcutaneously for 85 to 99 weeks at doses up to 2000 mcg/kg/day (8x the human exposure based on body surface area). In a 116-week subcutaneous study in rats, a 27% and 12% incidence of injection site sarcomas or squamous cell carcinomas was observed in males and females, respectively, at the highest dose level of 1250 mcg/kg/day (10x the human exposure based on body surface area) compared to an incidence of 8% to 10% in the vehicle-control groups. The increased incidence of injection site tumors was most probably caused by irritation and the high sensitivity of the rat to repeated subcutaneous injections at the same site. Rotating injection sites would prevent chronic irritation in humans. There have been no reports of injection site tumors in patients treated with Octreotide acetate for up to 5 years. There was also a 15% incidence of uterine adenocarcinomas in the 1250 mcg/kg/day females compared to 7% in the saline-control females and 0% in the vehicle-control females. The presence of endometritis coupled with the absence of corpora lutea, the reduction in mammary fibroadenomas, and the presence of uterine dilatation suggest that the uterine tumors were associated with estrogen dominance in the aged female rats which does not occur in humans.

Octreotide acetate did not impair fertility in rats at doses up to 1000 mcg/kg/day, which represents 7x the human exposure based on body surface area.

Pregnancy Category B

There are no adequate and well-controlled studies of Octreotide use in pregnant women. Reproduction studies have been performed in rats and rabbits at doses up to 16 times the highest recommended human dose based on body surface area and revealed no evidence of harm to the fetus due to Octreotide. However, because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

In postmarketing data, a limited number of exposed pregnancies have been reported in patients with acromegaly. Most women were exposed to Octreotide during the first trimester of pregnancy at doses ranging from 100 to 300 mcg/day of Octreotide acetate s.c. or 20 to 30 mg/month Octreotide acetate LAR, however some women elected to continue Octreotide therapy throughout pregnancy. In cases with a known outcome, no congenital malformations were reported.

Nursing Mothers

It is not known whether Octreotide is excreted into human milk. Because many drugs are excreted in human milk, caution should be exercised when Octreotide is administered to a nursing woman.

Pediatric Use

Safety and efficacy of Octreotide injection in the pediatric population have not been demonstrated.

No formal controlled clinical trials have been performed to evaluate the safety and effectiveness of Octreotide in pediatric under age 6 years. In post-marketing report, serious adverse events, including hypoxia, necrotizing enterocolitis, and death, have been reported with Octreotide use in children, most notably in children under 2 years of age. The relationship of these events to Octreotide has not been established as the majority of these pediatric patients had serious underlying co-morbid conditions.

Geriatric Use

Clinical studies of Octreotide acetate did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Adverse Reactions

Gallbladder Abnormalities

Gallbladder abnormalities, especially stones and/or biliary sludge, frequently develop in patients on chronic Octreotide acetate therapy (see WARNINGS).

Cardiac

In acromegalics, sinus bradycardia (<50 bpm) developed in 25%; conduction abnormalities occurred in 10% and arrhythmias developed in 9% of patients during Octreotide acetate therapy (see PRECAUTIONS: General).

Gastrointestinal

Diarrhea, loose stools, nausea and abdominal discomfort were each seen in 34% to 61% of acromegalic patients in U.S. studies although only 2.6% of the patients discontinued therapy due to these symptoms. These symptoms were seen in 5% to 10% of patients with other disorders.

The frequency of these symptoms was not dose-related, but diarrhea and abdominal discomfort generally resolved more quickly in patients treated with 300 mcg/day than in those treated with 750 mcg/day. Vomiting, flatulence, abnormal stools, abdominal distention, and constipation were each seen in less than 10% of patients.

In rare instances, gastrointestinal side effects may resemble acute intestinal obstruction, with progressive abdominal distention, severe epigastric pain, abdominal tenderness and guarding.

Hypo/Hyperglycemia

Hypoglycemia and hyperglycemia occurred in 3% and 16% of acromegalic patients, respectively, but only in about 1.5% of other patients. Symptoms of hypoglycemia were noted in approximately 2% of patients.

Hypothyroidism

In acromegalics, biochemical hypothyroidism alone occurred in 12% while goiter occurred in 6% during Octreotide acetate therapy (see PRECAUTIONS: General). In patients without acromegaly, hypothyroidism has only been reported in several isolated patients and goiter has not been reported.

Other Adverse Events

Pain on injection was reported in 7.7%, headache in 6% and dizziness in 5%. Pancreatitis was also observed (see WARNINGS and PRECAUTIONS).

Other Adverse Events 1% to 4%

Other events (relationship to drug not established), each observed in 1% to 4% of patients, included fatigue, weakness, pruritus, joint pain, backache, urinary tract infection, cold symptoms, flu symptoms, injection site hematoma, bruise, edema, flushing, blurred vision, pollakiuria, fat malabsorption, hair loss, visual disturbance and depression.

Other Adverse Events <1%

Events reported in less than 1% of patients and for which relationship to drug is not established are listed: Gastrointestinal: hepatitis, jaundice, increase in liver enzymes, GI bleeding, hemorrhoids, appendicitis, gastric/peptic ulcer, gallbladder polyp; Integumentary: rash, cellulitis, petechiae, urticaria, basal cell carcinoma; Musculoskeletal: arthritis, joint effusion, muscle pain, Raynaud’s phenomenon; Cardiovascular: chest pain, shortness of breath, thrombophlebitis, ischemia, congestive heart failure, hypertension, hypertensive reaction, palpitations, orthostatic BP decrease, tachycardia; CNS: anxiety, libido decrease, syncope, tremor, seizure, vertigo, Bell’s Palsy, paranoia, pituitary apoplexy, increased intraocular pressure, amnesia, hearing loss, neuritis; Respiratory: pneumonia, pulmonary nodule, status asthmaticus; Endocrine: galactorrhea, hypoadrenalism, diabetes insipidus, gynecomastia, amenorrhea, polymenorrhea, oligomenorrhea, vaginitis; Urogenital: nephrolithiasis, hematuria; Hematologic: anemia, iron deficiency, epistaxis; Miscellaneous: otitis, allergic reaction, increased CK, weight loss.

Evaluation of 20 patients treated for at least 6 months has failed to demonstrate titers of antibodies exceeding background levels. However, antibody titers to Octreotide acetate were subsequently reported in three patients and resulted in prolonged duration of drug action in two patients. Anaphylactoid reactions, including anaphylactic shock, have been reported in several patients receiving Octreotide acetate.

Overdosage

A limited number of accidental overdoses of Octreotide acetate in adults have been reported. In adults, the doses ranged from 2,400 to 6,000 micrograms/day administered by continuous infusion (100 to 250 micrograms/hour) or subcutaneously (1,500 micrograms t.i.d.). Adverse events in some patients included arrhythmia, hypotension, cardiac arrest, brain hypoxia, pancreatitis, hepatitis steatosis, hepatomegaly, lactic acidosis, flushing, diarrhea, lethargy, weakness, and weight loss.

Octreotide acetate injection given in intravenous boluses of 1 mg (1000 mcg) to healthy volunteers did not result in serious ill effects, nor did doses of 30 mg (30,000 mcg) given intravenously over 20 minutes and of 120 mg (120,000 mcg) given intravenously over 8 hours to research patients.

If overdose occurs, symptomatic management is indicated. Up-to-date information about the treatment of overdose can often be obtained from the National Poison Control Center at 1-800-222-1222.

Drug Abuse and Dependence

There is no indication that Octreotide acetate has potential for drug abuse or dependence. Octreotide acetate levels in the central nervous system are negligible, even after doses up to 30,000 mcg.

Octreotide Dosage and Administration

Octreotide acetate may be administered subcutaneously or intravenously. Subcutaneous injection is the usual route of administration of Octreotide acetate for control of symptoms. Pain with subcutaneous administration may be reduced by using the smallest volume that will deliver the desired dose. Multiple subcutaneous injections at the same site within short periods of time should be avoided. Sites should be rotated in a systematic manner.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration. Do not use if particulates and/or discoloration are observed. Proper sterile technique should be used in the preparation of parenteral admixtures to minimize the possibility of microbial contamination. Octreotide acetate is not compatible in Total Parenteral Nutrition (TPN) solutions because of the formation of a glycosyl Octreotide conjugate which may decrease the efficacy of the product.

Octreotide acetate is stable in sterile isotonic saline solutions or sterile solutions of dextrose 5% in water for 24 hours. It may be diluted in volumes of 50 to 200 mL and infused intravenously over 15 to 30 minutes or administered by IV push over 3 minutes. In emergency situations (e.g.: carcinoid crisis) it may be given by rapid bolus.

The initial dosage is usually 50 mcg administered twice or three times daily. Upward dose titration is frequently required. Dosage information for patients with specific tumors follows.

Acromegaly

Dosage may be initiated at 50 mcg t.i.d. Beginning with this low dose may permit adaptation to adverse gastrointestinal effects for patients who will require higher doses. IGF-I (somatomedin C) levels every 2 weeks can be used to guide titration. Alternatively, multiple growth hormone levels at 0 to 8 hours after Octreotide acetate administration permit more rapid titration of dose. The goal is to achieve growth hormone levels less than 5 ng/mL or IGF-I (somatomedin C) levels less than 1.9 U/mL in males and less than 2.2 U/mL in females. The dose most commonly found to be effective is 100 mcg t.i.d., but some patients require up to 500 mcg t.i.d. for maximum effectiveness. Doses greater than 300 mcg/day seldom result in additional biochemical benefit, and if an increase in dose fails to provide additional benefit, the dose should be reduced. IGF-I (somatomedin C) or growth hormone levels should be re-evaluated at 6-month intervals.

Octreotide acetate should be withdrawn yearly for approximately 4 weeks from patients who have received irradiation to assess disease activity. If growth hormone or IGF-I (somatomedin C) levels increase and signs and symptoms recur, Octreotide acetate therapy may be resumed.

Carcinoid Tumors

The suggested daily dosage of Octreotide acetate during the first 2 weeks of therapy ranges from 100 to 600 mcg/day in 2 to 4 divided doses (mean daily dosage is 300 mcg). In the clinical studies, the median daily maintenance dosage was approximately 450 mcg, but clinical and biochemical benefits were obtained in some patients with as little as 50 mcg, while others required doses up to 1500 mcg/day. However, experience with doses above 750 mcg/day is limited.

VIPomas

Daily dosages of 200 to 300 mcg in 2 to 4 divided doses are recommended during the initial 2 weeks of therapy (range 150 to 750 mcg) to control symptoms of the disease. On an individual basis, dosage may be adjusted to achieve a therapeutic response, but usually doses above 450 mcg/day are not required.

How is Octreotide Supplied

Octreotide acetate injection is available as:

200 mcg/mL Octreotide (as acetate):

NDC 0781-3165-75 box of one 5 mL multi-dose vial

1000 mcg/mL Octreotide (as acetate):

NDC 0781-3164-75 box of one 5 mL multi-dose vial

Storage

For prolonged storage, Octreotide acetate multi-dose vials should be stored at refrigerated temperatures 2°C-8°C (36°F-46°F) and protected from light. At room temperature, (20°C-30°C or 70°F-86°F), Octreotide acetate is stable for 14 days if protected from light. The solution can be allowed to come to room temperature prior to administration. Do not warm artificially. After initial use, multiple-dose vials should be discarded within 14 days.

*Thomson Healthcare, Inc.

09-2010M

U46043518

Manufactured in Canada by

Sandoz Canada Inc. for

Sandoz Inc.

Princeton, NJ 08540

mcg/mL Carton

NDC 0781-3165-75

Octreotide

Acetate

Injection

200 mcg/mL

(0.2 mg/mL)

For

Subcutaneous

Injection

Rx only

Total Volume 5 mL

Multi-Dose Vial

SANDOZ

mcg/mL Carton

NDC 0781-3164-75

Octreotide

Acetate

Injection

1000 mcg/mL

(1.0 mg/mL)

For

Subcutaneous

Injection

Rx only

Total Volume 5 mL

Multi-Dose Vial

SANDOZ

Octreotide ACETATE  Octreotide acetate  injection, solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0781-3165 Route of Administration INTRAVENOUS, SUBCUTANEOUS DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength Octreotide ACETATE (Octreotide) Octreotide 200 ug  in 1 mL

Inactive Ingredients Ingredient Name Strength LACTIC ACID 3.4 mg  in 1 mL MANNITOL 45 mg  in 1 mL PHENOL 5 mg  in 1 mL SODIUM BICARBONATE   WATER

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0781-3165-75 1 VIAL In 1 BOX contains a VIAL, MULTI-DOSE 1 5 mL In 1 VIAL, MULTI-DOSE This package is contained within the BOX (0781-3165-75)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NDA	NDA019667	10/21/1988

Octreotide ACETATE  Octreotide acetate  injection, solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0781-3164 Route of Administration INTRAVENOUS, SUBCUTANEOUS DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength Octreotide ACETATE (Octreotide) Octreotide 1000 ug  in 1 mL

Inactive Ingredients Ingredient Name Strength LACTIC ACID 3.4 mg  in 1 mL MANNITOL 45 mg  in 1 mL PHENOL 5 mg  in 1 mL SODIUM BICARBONATE   WATER

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0781-3164-75 1 VIAL In 1 BOX contains a VIAL, MULTI-DOSE 1 5 mL In 1 VIAL, MULTI-DOSE This package is contained within the BOX (0781-3164-75)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NDA	NDA019667	10/21/1988

Labeler - Sandoz Inc (110342024)

Revised: 10/2011Sandoz Inc

More Octreotide resources

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

• Octreotide MedFacts Consumer Leaflet (Wolters Kluwer)


• octreotide Injection, Intramuscular Advanced Consumer (Micromedex) - Includes Dosage Information


• Octreotide Acetate Monograph (AHFS DI)


• Sandostatin Consumer Overview


• Sandostatin LAR Depot Kit MedFacts Consumer Leaflet (Wolters Kluwer)

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