Clariget

Clariget may be available in the countries listed below.

Ingredient matches for Clariget

Clarithromycin

Clarithromycin is reported as an ingredient of Clariget in the following countries:

• Philippines

International Drug Name Search

Acébutolol

Acébutolol may be available in the countries listed below.

Ingredient matches for Acébutolol

Acebutolol

Acébutolol (DCF) is known as Acebutolol in the US.

International Drug Name Search

Glossary

DCF	Dénomination Commune Française

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

Salbutol

Salbutol may be available in the countries listed below.

Ingredient matches for Salbutol

Salbutamol

Salbutamol is reported as an ingredient of Salbutol in the following countries:

• Argentina

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

• Argentina


• Peru

International Drug Name Search

Silberan

Silberan may be available in the countries listed below.

Ingredient matches for Silberan

Vidarabine

Vidarabine is reported as an ingredient of Silberan in the following countries:

• Japan

International Drug Name Search

Ziagen

Ziagen is a brand name of abacavir, approved by the FDA in the following formulation(s):

ZIAGEN (abacavir sulfate - solution; oral)

• 
  Manufacturer: VIIV HLTHCARE
  
  Approval date: December 17, 1998
  
  Strength(s): EQ 20MG BASE/ML ^[RLD]

ZIAGEN (abacavir sulfate - tablet; oral)

• 
  Manufacturer: VIIV HLTHCARE
  
  Approval date: December 17, 1998
  
  Strength(s): EQ 300MG BASE ^[RLD]

Has a generic version of Ziagen been approved?

No. There is currently no therapeutically equivalent version of Ziagen available.

Note: Fraudulent online pharmacies may attempt to sell an illegal generic version of Ziagen. These medications may be counterfeit and potentially unsafe. If you purchase medications online, be sure you are buying from a reputable and valid online pharmacy. Ask your health care provider for advice if you are unsure about the online purchase of any medication.

See also: About generic drugs.

Related Patents

Patents are granted by the U.S. Patent and Trademark Office at any time during a drug's development and may include a wide range of claims.

• 
  Therapeutic nucleosides
  Patent 5,034,394
  Issued: July 23, 1991
  Inventor(s): Daluge; Susan M.
  Assignee(s): Burroughs Wellcome Co.
  The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. Also provided are pharmaceutical formulations and processes for the preparation of compounds according to the invention.
  
  Patent expiration dates:
  
  
  • December 18, 2011
    
    ✓ 
    Drug substance
    ✓ 
    Drug product
  
  
  
  • June 18, 2012
    
    ✓ 
    Pediatric exclusivity
  
  



• 
  Carbocyclic nucleoside hemisulfate and its use in treating viral infections
  Patent 6,294,540
  Issued: September 25, 2001
  Inventor(s): Brodie; Alastair Couper & Jones; Martin Francis & Seager; John Frederick & Wallis; Christopher John
  Assignee(s): Glaxo Wellcome Inc.
  The hemisulfate salt of (1S,4R)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene- 1-methanol or a solvate of it is used in the treatment of viral infections.
  
  Patent expiration dates:
  
  
  • May 14, 2018
    
    ✓ 
    Patent use: METHOD OF TREATMENT OF A PATIENT INFECTED WITH HIV
    ✓ 
    Drug substance
    ✓ 
    Drug product
  
  
  
  • November 14, 2018
    
    ✓ 
    Patent use: METHOD OF TREATMENT OF A PATIENT INFECTED WITH HIV
    ✓ 
    Pediatric exclusivity
  
  



• 
  Pharmaceutical compositions
  Patent 6,641,843
  Issued: November 4, 2003
  Inventor(s): Nikki Thoennes; Brooks
  Assignee(s): SmithKline Beecham Corporation
  The present invention relates to pharmaceutical compostions of (1S,4R)-cis-4-[2-amino-6-cyclopropylamino}-9H-purin-9-yl]-2-cyclopentene-1-methanol (1592U89).
  
  Patent expiration dates:
  
  
  • February 4, 2019
    
    ✓ 
    Drug product
  
  
  
  • August 4, 2019
    
    ✓ 
    Pediatric exclusivity
  
  

See also...

• Ziagen Consumer Information (Wolters Kluwer)
• Ziagen Solution Consumer Information (Wolters Kluwer)
• Ziagen Consumer Information (Cerner Multum)
• Ziagen Advanced Consumer Information (Micromedex)
• Ziagen AHFS DI Monographs (ASHP)
• Abacavir Consumer Information (Wolters Kluwer)
• Abacavir Solution Consumer Information (Wolters Kluwer)
• Abacavir Consumer Information (Cerner Multum)
• Abacavir Advanced Consumer Information (Micromedex)
• Abacavir Sulfate AHFS DI Monographs (ASHP)

Succinilcolina Rivero

Succinilcolina Rivero may be available in the countries listed below.

Ingredient matches for Succinilcolina Rivero

Suxamethonium Chloride

Suxamethonium Chloride is reported as an ingredient of Succinilcolina Rivero in the following countries:

• Argentina

International Drug Name Search

Propacetamol

Scheme

Rec.INN

ATC (Anatomical Therapeutic Chemical Classification)

N02BE05

CAS registry number (Chemical Abstracts Service)

0066532-85-2

Chemical Formula

C14-H20-N2-O3

Molecular Weight

264

Therapeutic Category

Analgesic and antipyretic

Chemical Name

Glycine, N,N-diethyl-, 4-(acetylamino)phenyl ester

Foreign Names

• Propacetamolum (Latin)
• Propacetamol (German)
• Propacetamol (French)
• Propacetamol (Spanish)

Generic Names

• Propacetamol (OS: BAN)
• UP 34101 (IS: UPSA)
• Propacétamol (chlorhydrate de) (PH: Ph. Eur. 6)
• Propacetamol Hydrochloride (PH: BP 2010, Ph. Eur. 6)
• Propacetamolhydrochlorid (PH: Ph. Eur. 6)
• Propacetamoli hydrochloridum (PH: Ph. Eur. 6)

Brand Name

• Pro-Dafalgan
  Bristol-Myers Squibb, Luxembourg

International Drug Name Search

Glossary

BAN	British Approved Name
IS	Inofficial Synonym
OS	Official Synonym
PH	Pharmacopoeia Name
Rec.INN	Recommended International Nonproprietary Name (World Health Organization)

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

Ostridose

Ostridose may be available in the countries listed below.

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

Ingredient matches for Ostridose

Fenbendazole

Fenbendazole is reported as an ingredient of Ostridose in the following countries:

• South Africa

International Drug Name Search

Aceptin-R

Aceptin-R may be available in the countries listed below.

Ingredient matches for Aceptin-R

Ranitidine

Ranitidine is reported as an ingredient of Aceptin-R in the following countries:

• Bangladesh

International Drug Name Search

Hydrocortison acis

Hydrocortison acis may be available in the countries listed below.

Ingredient matches for Hydrocortison acis

Hydrocortisone

Hydrocortisone is reported as an ingredient of Hydrocortison acis in the following countries:

• Germany

International Drug Name Search

Bifonazolo

Bifonazolo may be available in the countries listed below.

Ingredient matches for Bifonazolo

Bifonazole

Bifonazolo (DCIT) is also known as Bifonazole (Rec.INN)

International Drug Name Search

Glossary

DCIT	Denominazione Comune Italiana
Rec.INN	Recommended International Nonproprietary Name (World Health Organization)

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

Brevoxyl Gel

benzoyl peroxide

Dosage Form: gel
Brevoxyl® - 4 Gel (benzoyl peroxide 4%)

Brevoxyl® - 8 Gel (benzoyl peroxide 8%)

AQUEOUS BASE ACNE GEL

FOR TOPICAL USE

Rx only

Brevoxyl Gel Description

Brevoxyl® -4 Gel and Brevoxyl® -8 Gel are topical preparations containing benzoyl peroxide 4% and 8%, respectively, as the active ingredient in a gel vehicle containing ceteareth-20, cetyl alcohol, dimethyl isosorbide, fragrance, purified water, simethicone, stearyl alcohol.

The structural formula of benzoyl peroxide is:

Brevoxyl Gel - Clinical Pharmacology

The exact method of action of benzoyl peroxide in acne vulgaris is not known. Benzoyl peroxide is an antibacterial agent with demonstrated activity against Propionibacterium acnes. This action, combined with the mild keratolytic effect of benzoyl peroxide is believed to be responsible for its usefulness in acne.

Benzoyl peroxide is absorbed by the skin where it is metabolized to benzoic acid and excreted as benzoate in the urine.

Indications and Usage for Brevoxyl Gel

Brevoxyl® -4 Gel and Brevoxyl® -8 Gel are indicated for use in the topical treatment of mild to moderate acne vulgaris. Brevoxyl® -4 Gel or Brevoxyl® -8 Gel may be used as an adjunct in acne treatment regimens including antibiotics, retinoic acid products, and sulfur/salicylic acid containing preparations.

Contraindications

Brevoxyl® -4 Gel and Brevoxyl® -8 Gel should not be used in patients who have shown hypersensitivity to benzoyl peroxide or to any of the other ingredients in the product.

Precautions

General

For external use only. Avoid contact with eyes and mucous membranes. AVOID CONTACT WITH HAIR, FABRICS OR CARPETING AS BENZOYL PEROXIDE WILL CAUSE BLEACHING.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Based upon all available evidence, benzoyl peroxide is not considered to be a carcinogen. However, data from a study using mice known to be highly susceptible to cancer suggest that benzoyl peroxide acts as a tumor promoter. The clinical significance of the findings is not known.

Pregnancy

Category C

Animal reproduction studies have not been conducted with benzoyl peroxide. It is also not known whether benzoyl peroxide can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Benzoyl peroxide should be used by a pregnant woman only if clearly needed.

Nursing Mothers

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

Pediatric Use

Safety and effectiveness in children below the age of 12 have not been established.

Adverse Reactions

Contact sensitization reactions are associated with the use of topical benzoyl peroxide products and may be expected to occur in 10 to 25 of 1000 patients. The most frequent adverse reactions associated with benzoyl peroxide use are excessive erythema and peeling which may be expected to occur in 5 of 100 patients. Excess erythema and peeling most frequently appear during the initial phase of drug use and may normally be controlled by reducing frequency of use.

Brevoxyl Gel Dosage and Administration

Therapy may be initiated with either Brevoxyl® -4 Gel or Brevoxyl® -8 Gel. The medication should be applied once or twice daily to the affected areas. Frequency of use should be adjusted to obtain the desired clinical response. Gentle cleansing of the affected areas prior to application of Brevoxyl® -4 Gel or Brevoxyl® -8 Gel may be beneficial. Clinically visible improvement will normally occur by the third week of therapy. Maximum lesion reduction may be expected after approximately eight to twelve weeks of drug use. Continuing use of the drug is normally required to maintain a satisfactory clinical response.

How is Brevoxyl Gel Supplied

Brevoxyl® -4 Gel is supplied in 42.5 g (1.5 oz) tubes NDC 0145-2374-06.

Brevoxyl® -8 Gel is supplied in 42.5 g (1.5 oz) tubes NDC 0145-2384-06.

Store at controlled room temperature 15º – 30ºC (59º – 86ºF).

Questions? call 1-888-500-DERM (3376). Serious side effects associated with use of this product may be reported to this number.

BREVOXYL, STIEFEL, and STIEFEL & Design are registered trademarks of Stiefel Laboratories, Inc.

© 2009 Stiefel Laboratories, Inc.                                                                   301323

Rev. April 2009

STIEFEL®

Stiefel Laboratories, Inc.

255 Alhambra Circle

Coral Gables, FL 33134-7412 USA

Principal Display Panel

NDC 0145-2374-06

Brevoxyl®-4

Gel

(benzoyl peroxide 4%)

Rx only

AQUEOUS BASE GEL

FOR TOPICAL USE

Net Wt

42.5 g (1.5 oz)

Usual Dosage: Apply to affected areas once or twice daily or as directed by physician. See package insert.

Contains: Benzoyl peroxide 4% in a gel vehicle containing ceteareth-20, cetyl alcohol, dimethyl isosorbide, fragrance, purified water, simethicone, stearyl alcohol.

Avoid contact with eyes and mucous membranes. AVOID CONTACT WITH HAIR, FABRICS OR CARPETING AS BENZOYL PEROXIDE WILL CAUSE BLEACHING.

Store at controlled room temperature, 15o-30oC (59o - 86oF). Expiration date and lot number on crimp.

Questions? Call 1-888-500-DERM (3376). Serious side effects associated with use of this product may be reported to this number.

Stiefel Laboratories, Inc.

255 Alhambra Circle

Coral Gables, FL 33134-7412 USA

©2009 Stiefel Laboratories, Inc.

BREVOXYL, STIEFEL, AND STIEFEL & Design are registered trademarks of Stiefel Laboratories, Inc.

FG: 2374-6

303007

Principal Display Panel

NDC 0145-2384-06

Brevoxyl®-8

Gel

(benzoyl peroxide 8%)

Rx only

AQUEOUS BASE GEL

FOR TOPICAL USE

Net Wt

42.5 g (1.5 oz)

Usual Dosage: Apply to affected areas once or twice daily or as directed by physician. See package insert.

Contains: Benzoyl peroxide 8% in a gel vehicle containing ceteareth-20, cetyl alcohol, dimethyl isosorbide, fragrance, purified water, simethicone, stearyl alcohol.

Avoid contact with eyes and mucous membranes. AVOID CONTACT WITH HAIR, FABRICS OR CARPETING AS BENZOYL PEROXIDE WILL CAUSE BLEACHING.

Store at controlled room temperature, 15o-30oC (59o - 86oF). Expiration date and lot number on crimp.

Questions? Call 1-888-500-DERM (3376). Serious side effects associated with use of this product may be reported to this number.

Stiefel Laboratories, Inc.

255 Alhambra Circle

Coral Gables, FL 33134-7412 USA

©2009 Stiefel Laboratories, Inc.

BREVOXYL, STIEFEL, AND STIEFEL & Design are registered trademarks of Stiefel Laboratories, Inc.

FG: 2384-6

303008

BREVOXYL  benzoyl peroxide  gel

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0145-2374 Route of Administration TOPICAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength BENZOYL PEROXIDE (BENZOYL PEROXIDE) BENZOYL PEROXIDE 40 mg  in 1 g

Inactive Ingredients Ingredient Name Strength CETYL ALCOHOL   DIMETHYL ISOSORBIDE   WATER   DIMETHICONE 410   STEARYL ALCOHOL

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0145-2374-06 42.5 g In 1 TUBE None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
Unapproved drug other		08/27/2009	03/04/2011

BREVOXYL  benzoyl peroxide  gel

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0145-2384 Route of Administration TOPICAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength BENZOYL PEROXIDE (BENZOYL PEROXIDE) BENZOYL PEROXIDE 80 mg  in 1 g

Inactive Ingredients Ingredient Name Strength CETYL ALCOHOL   DIMETHYL ISOSORBIDE   WATER   DIMETHICONE 410   STEARYL ALCOHOL

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0145-2384-06 42.5 g In 1 TUBE None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
Unapproved drug other		08/27/2009	03/04/2011

Labeler - Stiefel Laboratories Inc (808842343)

Revised: 10/2010Stiefel Laboratories Inc

More Brevoxyl Gel resources

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

Compare Brevoxyl Gel with other medications

• Acne
• Perioral Dermatitis

Clindopax

Clindopax may be available in the countries listed below.

Ingredient matches for Clindopax

Clindamycin

Clindamycin is reported as an ingredient of Clindopax in the following countries:

• Argentina

International Drug Name Search

Celex

Celex may be available in the countries listed below.

Ingredient matches for Celex

Clonixin

Clonixin lysine salt (a derivative of Clonixin) is reported as an ingredient of Celex in the following countries:

• Chile

International Drug Name Search

Piroxicam AbZ

Piroxicam AbZ may be available in the countries listed below.

Ingredient matches for Piroxicam AbZ

Piroxicam

Piroxicam is reported as an ingredient of Piroxicam AbZ in the following countries:

• Germany

International Drug Name Search

Citalopram Germed

Citalopram Germed may be available in the countries listed below.

Ingredient matches for Citalopram Germed

Citalopram

Citalopram hydrobromide (a derivative of Citalopram) is reported as an ingredient of Citalopram Germed in the following countries:

• Czech Republic


• Estonia


• Hungary


• Latvia


• Lithuania

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

• Italy

International Drug Name Search

Clabact

Clabact may be available in the countries listed below.

Ingredient matches for Clabact

Clarithromycin

Clarithromycin is reported as an ingredient of Clabact in the following countries:

• Vietnam

International Drug Name Search

Cepim

Cepim may be available in the countries listed below.

Ingredient matches for Cepim

Cefepime

Cefepime Hydrochloride (a derivative of Cefepime) is reported as an ingredient of Cepim in the following countries:

• Italy

International Drug Name Search

Cimetidine Prafa

Cimetidine Prafa may be available in the countries listed below.

Ingredient matches for Cimetidine Prafa

Cimetidine

Cimetidine is reported as an ingredient of Cimetidine Prafa in the following countries:

• Indonesia

International Drug Name Search

Mepigobbi

Mepigobbi may be available in the countries listed below.

Ingredient matches for Mepigobbi

Mepivacaine

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

• Argentina

International Drug Name Search

Flagystatine

Flagystatine may be available in the countries listed below.

Ingredient matches for Flagystatine

Metronidazole

Metronidazole is reported as an ingredient of Flagystatine in the following countries:

• Peru

Nystatin

Nystatin is reported as an ingredient of Flagystatine in the following countries:

• Peru

International Drug Name Search

Evetant

Evetant may be available in the countries listed below.

Ingredient matches for Evetant

Dopamine

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

• Japan

International Drug Name Search

Bétahistine Teva

Bétahistine Teva may be available in the countries listed below.

Ingredient matches for Bétahistine Teva

Betahistine

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

• France

International Drug Name Search

CO Clomipramine

CO Clomipramine may be available in the countries listed below.

Ingredient matches for CO Clomipramine

Clomipramine

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

• Canada

International Drug Name Search

Colimy Foam

Colimy Foam may be available in the countries listed below.

Ingredient matches for Colimy Foam

Colistin Sulfate

Colistin sulfate (a derivative of Colistin) is reported as an ingredient of Colimy Foam in the following countries:

• Japan

Neomycin

Neomycin sulfate (a derivative of Neomycin) is reported as an ingredient of Colimy Foam in the following countries:

• Japan

International Drug Name Search

Eco Iodine

Eco Iodine may be available in the countries listed below.

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

Ingredient matches for Eco Iodine

Povidone Iodine

Povidone-Iodine is reported as an ingredient of Eco Iodine in the following countries:

• South Africa

International Drug Name Search

Canolen

Canolen may be available in the countries listed below.

Ingredient matches for Canolen

Ciclopirox

Ciclopirox olamine (a derivative of Ciclopirox) is reported as an ingredient of Canolen in the following countries:

• Bosnia & Herzegowina


• Turkey

International Drug Name Search

Ketoconazol Fabra

Ketoconazol Fabra may be available in the countries listed below.

Ingredient matches for Ketoconazol Fabra

Ketoconazole

Ketoconazole is reported as an ingredient of Ketoconazol Fabra in the following countries:

• Argentina

International Drug Name Search

Calcium Polycarbophil

Calcium Polycarbophil may be available in the countries listed below.

Ingredient matches for Calcium Polycarbophil

Polycarbophil

Calcium Polycarbophil (USAN) is known as Polycarbophil in the US.

International Drug Name Search

Glossary

USAN	United States Adopted Name

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

Sertranat

Sertranat may be available in the countries listed below.

Ingredient matches for Sertranat

Sertraline

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

• Slovakia

International Drug Name Search

Perbilen

Perbilen may be available in the countries listed below.

Ingredient matches for Perbilen

Piretanide

Piretanide is reported as an ingredient of Perbilen in the following countries:

• Spain

International Drug Name Search

Citrato Espresso S.Pellegrino

Citrato Espresso S.Pellegrino may be available in the countries listed below.

Ingredient matches for Citrato Espresso S.Pellegrino

Magnesium Hydroxide

Magnesium Hydroxide is reported as an ingredient of Citrato Espresso S.Pellegrino in the following countries:

• Italy

International Drug Name Search

Gastrolets

Gastrolets may be available in the countries listed below.

Ingredient matches for Gastrolets

Ranitidine

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

• Argentina

International Drug Name Search

Bisbentiamine

Scheme

Rec.INN

CAS registry number (Chemical Abstracts Service)

0002667-89-2

Chemical Formula

C38-H42-N8-O6-S2

Molecular Weight

770

Therapeutic Category

Vitamin B₁

Chemical Name

Formamide, N,N'-[dithiobis[2-[2-(benzoyloxy)ethyl]-1-methyl-2,1-ethenediyl]]bis[N-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-

Foreign Names

• Bisbentiaminum (Latin)
• Bisbentiamin (German)
• Bisbentiamine (French)
• Bisbentiamina (Spanish)

Generic Names

• Bisbentiamine (OS: JAN)
• Benzoylthiamine disulfide (IS)
• BTD (IS)

Brand Names

• Beston
  Tanabe, Indonesia; Tanabe Mitsubishi, Japan

International Drug Name Search

Glossary

IS	Inofficial Synonym
JAN	Japanese Accepted Name
OS	Official Synonym
Rec.INN	Recommended International Nonproprietary Name (World Health Organization)

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

Niltro

Niltro may be available in the countries listed below.

Ingredient matches for Niltro

Loratadine

Loratadine is reported as an ingredient of Niltro in the following countries:

• Argentina

International Drug Name Search

Depo-Testosterone

testosterone cypionate

Dosage Form: injection, solution
Depo®-Testosterone

testosterone cypionate injection, USP    CIII

Depo-Testosterone Description

Depo-Testosterone Injection, for intramuscular injection, contains testosterone cypionate which is the oil-soluble 17 (beta)- cyclopentylpropionate ester of the androgenic hormone testosterone.

Testosterone cypionate is a white or creamy white crystalline powder, odorless or nearly so and stable in air. It is insoluble in water, freely soluble in alcohol, chloroform, dioxane, ether, and soluble in vegetable oils.

The chemical name for testosterone cypionate is androst-4-en-3-one,17-(3-cyclopentyl-1-oxopropoxy)-, (17β)-. Its molecular formula is C27H40O3, and the molecular weight 412.61.

The structural formula is represented below:

Depo-Testosterone Injection is available in two strengths, 100 mg/mL and 200 mg/mL testosterone cypionate.

Each mL of the 100 mg/mL solution contains:

    Testosterone cypionate................................................................................... 100 mg

    Benzyl benzoate .............................................................................................. 0.1 mL

    Cottonseed oil ................................................................................................ 736 mg

    Benzyl alcohol (as preservative) ..................................................................... 9.45 mg

Each mL of the 200 mg/mL solution contains:

    Testosterone cypionate .................................................................................. 200 mg

    Benzyl benzoate .............................................................................................. 0.2 mL

    Cottonseed oil ................................................................................................ 560 mg

    Benzyl alcohol (as preservative) ..................................................................... 9.45 mg

Depo-Testosterone - Clinical Pharmacology

Endogenous androgens are responsible for normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. These effects include growth and maturation of the prostate, seminal vesicles, penis, and scrotum; development of male hair distribution, such as beard, pubic, chest, and axillary hair; laryngeal enlargement, vocal cord thickening, and alterations in body musculature and fat distribution. Drugs in this class also cause retention of nitrogen, sodium, potassium, and phosphorous, and decreased urinary excretion of calcium. Androgens have been reported to increase protein anabolism and decrease protein catabolism. Nitrogen balance is improved only when there is sufficient intake of calories and protein.

Androgens are responsible for the growth spurt of adolescence and for eventual termination of linear growth, brought about by fusion of the epiphyseal growth centers. In children, exogenous androgens accelerate linear growth rates, but may cause disproportionate advancement in bone maturation. Use over long periods may result in fusion of the epiphyseal growth centers and termination of the growth process. Androgens have been reported to stimulate production of red blood cells by enhancing production of erythropoietic stimulation factor.

During exogenous administration of androgens, endogenous testosterone release is inhibited through feedback inhibition of pituitary luteinizing hormone (LH). At large doses of exogenous androgens, spermatogenesis may also be suppressed through feedback inhibition of pituitary follicle stimulating hormone (FSH).

There is a lack of substantial evidence that androgens are effective in fractures, surgery, convalescence, and functional uterine bleeding.

Pharmacokinetics

Testosterone esters are less polar than free testosterone. Testosterone esters in oil injected intramuscularly are absorbed slowly from the lipid phase; thus, testosterone cypionate can be given at intervals of two to four weeks.

Testosterone in plasma is 98 percent bound to a specific testosterone-estradiol binding globulin, and about 2 percent is free. Generally, the amount of this sex-hormone binding globulin in the plasma will determine the distribution of testosterone between free and bound forms, and the free testosterone concentration will determine its half-life.

About 90 percent of a dose of testosterone is excreted in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about 6 percent of a dose is excreted in the feces, mostly in the unconjugated form. Inactivation of testosterone occurs primarily in the liver. Testosterone is metabolized to various 17-keto steroids through two different pathways.

The half-life of testosterone cypionate when injected intramuscularly is approximately eight days.

In many tissues the activity of testosterone appears to depend on reduction to dihydrotestosterone, which binds to cytosol receptor proteins. The steroid-receptor complex is transported to the nucleus where it initiates transcription events and cellular changes related to androgen action.

Indications and Usage for Depo-Testosterone

Depo-Testosterone Injection is indicated for replacement therapy in the male in conditions associated with symptoms of deficiency or absence of endogenous testosterone.

1. Primary hypogonadism (congenital or acquired)-testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome; or orchidectomy.

2. Hypogonadotropic hypogonadism (congenital or acquired)-idiopathic gonadotropin or LHRH deficiency, or pituitary-hypothalamic injury from tumors, trauma, or radiation.

Contraindications

1. Known hypersensitivity to the drug


2. Males with carcinoma of the breast


3. Males with known or suspected carcinoma of the prostate gland


4. Women who are or who may become pregnant


5. Patients with serious cardiac, hepatic or renal disease

Warnings

Hypercalcemia may occur in immobilized patients. If this occurs, the drug should be discontinued.

Prolonged use of high doses of androgens (principally the 17-α alkyl-androgens) has been associated with development of hepatic adenomas, hepatocellular carcinoma, and peliosis hepatis —all potentially life-threatening complications.

Geriatric patients treated with androgens may be at an increased risk of developing prostatic hypertrophy and prostatic carcinoma although conclusive evidence to support this concept is lacking.

Edema, with or without congestive heart failure, may be a serious complication in patients with pre-existing cardiac, renal or hepatic disease.

Gynecomastia may develop and occasionally persists in patients being treated for hypogonadism.

This product contains benzyl alcohol. Benzyl alcohol has been reported to be associated with a fatal "Gasping Syndrome" in premature infants.

Androgen therapy should be used cautiously in healthy males with delayed puberty. The effect on bone maturation should be monitored by assessing bone age of the wrist and hand every 6 months. In children, androgen treatment may accelerate bone maturation without producing compensatory gain in linear growth. This adverse effect may result in compromised adult stature. The younger the child the greater the risk of compromising final mature height.

This drug has not been shown to be safe and effective for the enhancement of athletic performance. Because of the potential risk of serious adverse health effects, this drug should not be used for such purpose.

Precautions

General

Patients with benign prostatic hypertrophy may develop acute urethral obstruction. Priapism or excessive sexual stimulation may develop. Oligospermia may occur after prolonged administration or excessive dosage. If any of these effects appear, the androgen should be stopped and if restarted, a lower dosage should be utilized.

Testosterone cypionate should not be used interchangeably with testosterone propionate because of differences in duration of action.

Testosterone cypionate is not for intravenous use.

Information for patients

Patients should be instructed to report any of the following: nausea, vomiting, changes in skin color, ankle swelling, too frequent or persistent erections of the penis.

Laboratory tests

Hemoglobin and hematocrit levels (to detect polycythemia) should be checked periodically in patients receiving long-term androgen administration.

Serum cholesterol may increase during androgen therapy.

Drug interactions

Androgens may increase sensitivity to oral anticoagulants. Dosage of the anticoagulant may require reduction in order to maintain satisfactory therapeutic hypoprothrombinemia.

Concurrent administration of oxyphenbutazone and androgens may result in elevated serum levels of oxyphenbutazone.

In diabetic patients, the metabolic effects of androgens may decrease blood glucose and, therefore, insulin requirements.

Drug/Laboratory test Interferences

Androgens may decrease levels of thyroxine-binding globulin, resulting in decreased total T4 serum levels and increased resin uptake of T3 and T4. Free thyroid hormone levels remain unchanged, however, and there is no clinical evidence of thyroid dysfunction.

Carcinogenesis

Animal data

Testosterone has been tested by subcutaneous injection and implantation in mice and rats. The implant induced cervical-uterine tumors in mice, which metastasized in some cases. There is suggestive evidence that injection of testosterone into some strains of female mice increases their susceptibility to hepatoma. Testosterone is also known to increase the number of tumors and decrease the degree of differentiation of chemically induced carcinomas of the liver in rats.

Human data

There are rare reports of hepatocellular carcinoma in patients receiving long-term therapy with androgens in high doses. Withdrawal of the drugs did not lead to regression of the tumors in all cases.

Geriatric patients treated with androgens may be at an increased risk of developing prostatic hypertrophy and prostatic carcinoma although conclusive evidence to support this concept is lacking.

Pregnancy

Teratogenic Effects

Pregnancy Category X. (See CONTRAINDICATIONS.)

Nursing mothers

Depo-Testosterone is not recommended for use in nursing mothers.

Pediatric use

Safety and effectiveness in pediatric patients below the age of 12 years have not been established.

Adverse Reactions

The following adverse reactions in the male have occurred with some androgens:

Endocrine and urogenital: Gynecomastia and excessive frequency and duration of penile erections. Oligospermia may occur at high dosages.

Skin and appendages: Hirsutism, male pattern of baldness, seborrhea, and acne.

Fluid and electrolyte disturbances: Retention of sodium, chloride, water, potassium, calcium, and inorganic phosphates.

Gastrointestinal: Nausea, cholestatic jaundice, alterations in liver function tests, rarely hepatocellular neoplasms and peliosis hepatis (see WARNINGS).

Hematologic: Suppression of clotting factors II, V, VII, and X, bleeding in patients on concomitant anticoagulant therapy, and polycythemia.

Nervous system: Increased or decreased libido, headache, anxiety, depression, and generalized paresthesia.

Allergic: Hypersensitivity, including skin manifestations and anaphylactoid reactions.

Miscellaneous: Inflammation and pain at the site of intramuscular injection.

Drug Abuse and Dependence

Controlled Substance Class

Testosterone is a controlled substance under the Anabolic Steroids Control Act, and Depo-Testosterone Injection has been assigned to Schedule III.

Overdosage

There have been no reports of acute overdosage with the androgens.

Depo-Testosterone Dosage and Administration

Depo-Testosterone Injection is for intramuscular use only.

It should not be given intravenously. Intramuscular injections should be given deep in the gluteal muscle.

The suggested dosage for Depo-Testosterone Injection varies depending on the age, sex, and diagnosis of the individual patient. Dosage is adjusted according to the patient's response and the appearance of adverse reactions.

Various dosage regimens have been used to induce pubertal changes in hypogonadal males; some experts have advocated lower dosages initially, gradually increasing the dose as puberty progresses, with or without a decrease to maintenance levels. Other experts emphasize that higher dosages are needed to induce pubertal changes and lower dosages can be used for maintenance after puberty. The chronological and skeletal ages must be taken into consideration, both in determining the initial dose and in adjusting the dose.

For replacement in the hypogonadal male, 50–400 mg should be administered every two to four weeks.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Warming and shaking the vial should redissolve any crystals that may have formed during storage at temperatures lower than recommended.

How is Depo-Testosterone Supplied

Depo-Testosterone Injection is available as follows:

100 mg/mL

    10 mL vials                    NDC 0009-0347-02

200 mg/mL

    1 mL vials                      NDC 0009-0417-01

    10 mL vials                    NDC 0009-0417-02

Vials should be stored at controlled room temperature 20° to 25°C (68° to 77°F) [see USP]. Protect from light.

Rx only

LAB-0245-2.0

September 2006

PRINCIPAL DISPLAY PANEL - 100 mg/mL Vial Carton

NDC 0009-0347-02

One 10 mL Vial

Multiple-Dose

Rx only

Depo®-

Testosterone

testosterone cypionate

injection, USP

CIII

For intramuscular use only

100 mg/mL

Pfizer

Distributed by

Pharmacia & Upjohn Co

Division of Pfizer Inc, NY, NY 10017

PRINCIPAL DISPLAY PANEL - 200 mg/mL Vial Carton

NDC 0009-0417-02

One 10 mL Vial

Multiple-Dose

Rx only

Depo®-

Testosterone

testosterone cypionate

injection, USP

CIII

For intramuscular use only

200 mg/mL

Pfizer

Distributed by

Pharmacia & Upjohn Co

Division of Pfizer Inc, NY, NY 10017

Depo-Testosterone  testosterone cypionate  injection, solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0009-0347 Route of Administration INTRAMUSCULAR DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength testosterone cypionate (testosterone) testosterone cypionate 100 mg  in 1 mL

Inactive Ingredients Ingredient Name Strength benzyl benzoate 0.1 mL  in 1 mL cottonseed oil 736 mg  in 1 mL benzyl alcohol 9.45 mg  in 1 mL

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0009-0347-02 10 mL In 1 VIAL None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA085635	07/25/1979

Depo-Testosterone  testosterone cypionate  injection, solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0009-0417 Route of Administration INTRAMUSCULAR DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength testosterone cypionate (testosterone) testosterone cypionate 200 mg  in 1 mL

Inactive Ingredients Ingredient Name Strength benzyl benzoate 0.2 mL  in 1 mL cottonseed oil 560 mg  in 1 mL benzyl alcohol 9.45 mg  in 1 mL

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0009-0417-01 1 mL In 1 VIAL None 2 0009-0417-02 10 mL In 1 VIAL None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA085635	07/25/1979

Labeler - Pharmacia and Upjohn Company (829076566)

Establishment
Name	Address	ID/FEI	Operations
Pharmacia and Upjohn Company		829076566	MANUFACTURE

Revised: 02/2010Pharmacia and Upjohn Company

More Depo-Testosterone resources

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

• Depo-Testosterone MedFacts Consumer Leaflet (Wolters Kluwer)


• Testosterone Professional Patient Advice (Wolters Kluwer)


• Testosterone Monograph (AHFS DI)


• AndroGel Gel MedFacts Consumer Leaflet (Wolters Kluwer)


• Androderm Patch MedFacts Consumer Leaflet (Wolters Kluwer)


• Androderm Advanced Consumer (Micromedex) - Includes Dosage Information


• Androgel Advanced Consumer (Micromedex) - Includes Dosage Information


• Androgel Consumer Overview


• Axiron Solution MedFacts Consumer Leaflet (Wolters Kluwer)


• Axiron Consumer Overview


• Delatestryl MedFacts Consumer Leaflet (Wolters Kluwer)


• Fortesta Consumer Overview


• Fortesta Gel MedFacts Consumer Leaflet (Wolters Kluwer)


• Striant MedFacts Consumer Leaflet (Wolters Kluwer)


• Striant Consumer Overview


• Striant Advanced Consumer (Micromedex) - Includes Dosage Information


• Testim Gel MedFacts Consumer Leaflet (Wolters Kluwer)

Compare Depo-Testosterone with other medications

• Breast Cancer, Palliative
• Delayed Puberty, Male
• Hypogonadism, Male
• Postpartum Breast Pain

BPO Foaming Cloths

Generic Name: benzoyl peroxide topical (BEN zoyl per OX ide)

Brand Names: Acne Treatment, Acne-Clear, Benzac AC, Benzac W, Benzashave 10, Benzashave 5, BenzEFoam, Benziq, Benziq Wash, BPO Foaming Cloths, Brevoxyl, Brevoxyl Acne Wash Kit, Brevoxyl-4 Creamy Wash Complete Pack, Brevoxyl-8 Creamy Wash Complete Pack, Breze, Clearplex, Clearskin, Clinac BPO, Desquam-E, Desquam-X 10, Desquam-X 5, Desquam-X Wash, Fostex Bar 10%, Fostex Gel 10%, Fostex Wash 10%, Inova, Lavoclen-4, Lavoclen-8, Loroxide, NeoBenz Micro, Neutrogena Acne Mask, Neutrogena On Spot Acne Treatment, Oscion, Oscion Cleanser, Oxy 10 Balance, Oxy Balance, Oxy Daily Wash Chill Factor, Oxy-10, Pacnex, PanOxyl, Panoxyl 10, Panoxyl 5, Panoxyl Aqua Gel, PanOxyl Maximum Strength Foaming Acne Wash, Persa-Gel, Seba-Gel, SoluCLENZ Rx, Triaz, Triaz Cleanser, Zaclir

What is BPO Foaming Cloths (benzoyl peroxide topical)?

Benzoyl peroxide has an antibacterial effect. It also has a mild drying effect, which allows excess oils and dirt to be easily washed away from the skin.

Benzoyl peroxide topical (for the skin) is used to treat acne.

Benzoyl peroxide topical may also be used for purposes not listed in this medication guide.

What is the most important information I should know about BPO Foaming Cloths (benzoyl peroxide topical)?

There are many brands and forms of benzoyl peroxide available and not all brands are listed on this leaflet.

Do not use benzoyl peroxide topical while you are also using tretinoin (Altinac, Avita, Renova, Retin-A, Tretin-X). Using these medications together could cause severe skin irritation.

Use this medication exactly as directed on the label, or as prescribed by your doctor. Do not use it in larger amounts or for longer than recommended.

Avoid getting this medication in your mouth or eyes. If it does get into any of these areas, rinse with water. Do not use benzoyl peroxide topical on sunburned, windburned, dry, chapped, irritated, or broken skin. Also avoid using benzoyl peroxide topical on wounds or on areas of eczema. Wait until these conditions have healed before using this medication.

Avoid using skin products that can cause irritation, such as harsh soaps, shampoos, or skin cleansers, hair coloring or permanent chemicals, hair removers or waxes, or skin products with alcohol, spices, astringents, or lime. Do not use other medicated skin products unless your doctor has told you to.

Benzoyl peroxide may bleach hair or fabrics. Avoid allowing this medication to come into contact with your hair or clothing.

It may take several weeks before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve.

What should I discuss with my healthcare provider before using BPO Foaming Cloths (benzoyl peroxide topical)?

Do not use benzoyl peroxide topical while you are also using tretinoin (Altinac, Avita, Renova, Retin-A, Tretin-X). Using these medications together could cause severe skin irritation. FDA pregnancy category C. It is not known whether benzoyl peroxide topical will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication. It is not known whether benzoyl peroxide passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I use BPO Foaming Cloths (benzoyl peroxide topical)?

Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.

Wash your hands before and after applying this medication. Shake the lotion well just before each use.

Clean and pat dry the skin to be treated. Apply benzoyl peroxide in a thin layer and rub in gently.

Do not cover the treated skin area unless your doctor has told you to.

Benzoyl peroxide topical is usually applied one to three times daily. Follow your doctor's instructions.

Benzoyl peroxide may bleach hair or fabrics. Avoid allowing this medication to come into contact with your hair or clothing.

It may take several weeks before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve.

Store at room temperature away from moisture and heat.

What happens if I miss a dose?

Use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while using BPO Foaming Cloths (benzoyl peroxide topical)?

Avoid getting this medication in your mouth or eyes. If it does get into any of these areas, rinse with water. Do not use benzoyl peroxide topical on sunburned, windburned, dry, chapped, irritated, or broken skin. Also avoid using benzoyl peroxide topical on wounds or on areas of eczema. Wait until these conditions have healed before using this medication.

Avoid using skin products that can cause irritation, such as harsh soaps, shampoos, or skin cleansers, hair coloring or permanent chemicals, hair removers or waxes, or skin products with alcohol, spices, astringents, or lime. Do not use other medicated skin products unless your doctor has told you to.

Avoid using sunscreen containing PABA on the same skin treated with benzoyl peroxide, or skin discoloration may occur.

BPO Foaming Cloths (benzoyl peroxide topical) side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using benzoyl peroxide and call your doctor at once if you have severe stinging or burning of your skin.

Less serious side effects may include:

• 
  

  mild stinging or burning;

  
  


• 
  

  itching or tingly feeling;

  
  


• 
  

  skin dryness, peeling, or flaking; or

  
  


• 
  

  redness or other irritation.

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect BPO Foaming Cloths (benzoyl peroxide topical)?

It is not likely that other drugs you take orally or inject will have an effect on topically applied benzoyl peroxide topical. But many drugs can interact with each other. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

More BPO Foaming Cloths resources

• BPO Foaming Cloths Side Effects (in more detail)
• BPO Foaming Cloths Use in Pregnancy & Breastfeeding
• BPO Foaming Cloths Drug Interactions
• 0 Reviews for BPOing Cloths - Add your own review/rating

• Acne Treatment Cream MedFacts Consumer Leaflet (Wolters Kluwer)


• BenzEFoam Foam MedFacts Consumer Leaflet (Wolters Kluwer)


• Benzac Topical Advanced Consumer (Micromedex) - Includes Dosage Information


• Benzac AC Wash MedFacts Consumer Leaflet (Wolters Kluwer)


• Benzefoam Prescribing Information (FDA)


• Benzefoam Ultra Prescribing Information (FDA)


• Brevoxyl Gel MedFacts Consumer Leaflet (Wolters Kluwer)


• Brevoxyl Creamy Wash Prescribing Information (FDA)


• Desquam-X Wash Prescribing Information (FDA)


• Inova Pads MedFacts Consumer Leaflet (Wolters Kluwer)


• NeoBenz Micro Wash Plus Pack Cream MedFacts Consumer Leaflet (Wolters Kluwer)


• Neobenz Micro SD Prescribing Information (FDA)


• Neobenz Micro Wash Plus Pack Prescribing Information (FDA)


• Oxy Balance Topical Advanced Consumer (Micromedex) - Includes Dosage Information


• Pacnex LP Prescribing Information (FDA)


• PanOxyl Bar MedFacts Consumer Leaflet (Wolters Kluwer)


• Triaz Cloths MedFacts Consumer Leaflet (Wolters Kluwer)


• Triazolam Monograph (AHFS DI)

Compare BPO Foaming Cloths with other medications

• Acne
• Perioral Dermatitis

Where can I get more information?

• Your pharmacist can provide more information about benzoyl peroxide topical.

See also: BPOing Cloths side effects (in more detail)

Rectiv Ointment

nitroglycerin

Dosage Form: rectal ointment
FULL PRESCRIBING INFORMATION

Indications and Usage for Rectiv Ointment

RECTIV™ (nitroglycerin) Ointment 0.4% is indicated for the treatment of moderate to severe pain associated with chronic anal fissure.

Rectiv Ointment Dosage and Administration

Apply 1 inch of ointment (375 mg of ointment equivalent to 1.5 mg of nitroglycerin) intra-anally every 12 hours for up to 3 weeks. A finger covering, such as plastic-wrap, disposable surgical glove or a finger cot, should be placed on the finger to apply the ointment. To obtain a 1.5 mg dose of nitroglycerin, the covered finger is laid alongside the 1 inch dosing line on the carton.

Refer to carton for accurate dosage guide.

The tube is gently squeezed until a line of ointment the length of the measuring line is expressed onto the covered finger. The ointment is gently inserted into the anal canal using the covered finger no further than to the first finger joint and the ointment is applied around the side of the anal canal. If this cannot be achieved due to pain, application of the ointment should be made directly to the outside of the anus. Treatment may be continued for up to three weeks.

Rectiv Ointment is not for oral, ophthalmic, or intravaginal use. Hands should be washed after application of the ointment.

See Patients Instruction for Use.

Dosage Forms and Strengths

Ointment, 0.4% w/w (4 mg/1 g) in 30 g tubes.

Contraindications

PDE5 inhibitor use

Administration of RECTIV is contraindicated in patients who are using a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), such as sildenafil, vardenafil, and tadalafil, as these are shown to potentiate the hypotensive effects of organic nitrates [see 7.1 DRUG INTERACTIONS].

Severe anemia

RECTIV is contraindicated in patients with severe anemia.

Increased intracranial pressure

RECTIV is contraindicated in patients with increased intracranial pressure.

Hypersensitivity

RECTIV is contraindicated in patients who have shown hypersensitivity to it or to other nitrates or nitrites. Skin reactions consistent with hypersensitivity have been observed with organic nitrates.

Warnings and Precautions

Cardiovascular disorders

Venous and arterial dilatation as a consequence of nitroglycerin treatment including RECTIV, can decrease venous blood returning to the heart and reduce arterial vascular resistance and systolic pressure. Exercise caution when treating patients with any of the following conditions: blood volume depletion, existing hypotension, cardiomyopathies, congestive heart failure, acute myocardial infarction, or poor cardiac function for other reasons. If patients with any of these conditions are treated with RECTIV, monitor cardiovascular status and clinical condition. The adverse reactions of RECTIV are likely to be more pronounced in the elderly.

Headache

RECTIV produces dose-related headaches, which may be severe. Tolerance to headaches occurs.

Adverse Reactions

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

The most common adverse reaction of RECTIV (nitroglycerin) Ointment 0.4% applied to the anal canal is headache.

Headache may be recurrent following each dose. Headaches are typically of short duration and can be treated with an analgesic, e.g. acetaminophen, and are reversible upon discontinuation of treatment.

In Study REC-C-001, a double-blind, placebo-controlled trial in patients with a painful chronic anal fissure, the most frequent (≥ 2%) adverse reactions reported were as follows (Table 1):

Table 1: Incidence of Adverse Reactions (≥ 2%) in Study REC-C-001

	RECTIV N = 123		Placebo N = 124
System Organ Class    Preferred term	Patients n (%)	Events n	Patients n (%)	Events n
Nervous system disorders
Headache	79 (64)	938	51 (41)	225
Dizziness	6 (5)	26	0	0

Hypotension

Transient episodes of light-headedness, occasionally related to blood pressure changes, also may occur. Hypotension (including orthostatic hypotension) occurs infrequently, but in some patients may be severe enough to warrant discontinuation of therapy.

Allergic Reactions

Flushing, allergic reactions and application site reactions (including drug rash and exfoliative dermatitis) have been reported rarely.

Methemoglobinemia

In rare cases, therapeutic doses of organic nitrates have caused methemoglobinemia (see 10 OVERDOSAGE).

Drug Interactions

PDE5 inhibitors

Phosphodiesterase type 5 (PDE5) inhibitors such as sildenafil, vardenafil, and tadalafil have been shown to potentiate the hypotensive effects of organic nitrates.

The time course of the interaction appears to be related to the half-life of the PDE5 inhibitor, however, the dose dependence of this interaction has not been studied. Use of RECTIV within a few days of PDE5 inhibitors is contraindicated.

Antihypertensives

Patients receiving antihypertensive drugs, beta-adrenergic blockers, and other nitrates should be observed for possible additive hypotensive effects when using RECTIV. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly.

Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with RECTIV in patients with angina pectoris, additional hypotensive effects may occur.

Aspirin

Coadministration of aspirin (at doses between 500 mg and 1000 mg) and nitroglycerin has been reported to result in increased nitroglycerin maximum concentrations by as much as 67% and AUC by 73% when administered as a single dose. The pharmacological effects of RECTIV may be enhanced by concomitant administration of aspirin.

Tissue-type Plasminogen Activator (t-PA)

Intravenous administration of nitroglycerin decreases the thrombolytic effect of tissue-type plasminogen activator (t-PA). Plasma levels of t-PA are reduced when coadministered with nitroglycerin. Therefore, caution should be observed in patients receiving RECTIV during t-PA therapy.

Heparin

Although an interaction has been reported between intravenous heparin and intravenous nitroglycerin (resulting in a decrease in the anticoagulant effect of heparin), the data are not consistent. If patients are to receive intravenous heparin and RECTIV concurrently, the anticoagulation status of the patient must be checked.

Ergotamine

Oral administration of nitroglycerin markedly decreases the first-pass metabolism of dihydroergotamine and consequently increases its oral bioavailability. Ergotamine is known to precipitate angina pectoris. Therefore the possibility of ergotism in patients receiving RECTIV should be considered.

Alcohol

The vasodilating effects of nitroglycerin have been shown to be additive to the effects observed with alcohol.

USE IN SPECIFIC POPULATIONS

Pregnancy

Pregnancy Category C

Animal reproduction and teratogenicity studies have not been conducted with RECTIV. Nitroglycerin was not teratogenic when administered by topical or dietary route. There are no adequate and well-controlled studies in pregnant women. RECTIV should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Teratology studies in rats and rabbits were conducted with topically applied nitroglycerin ointment at doses up to 80 mg/kg/day and 240 mg/kg/day, respectively. No toxic effects on dams or fetuses were seen at any dose tested.

A teratogenicity study was conducted in rats with nitroglycerin administered in the diet at levels up to 1% content (approximately 430 mg/kg/day) on days 6 to 15 of gestation. In offspring of the high-dose group, an increased but not statistically significant incidence of diaphragmatic hernias was noted together with decreased hyoid bone ossification. The latter finding probably reflects delayed development, thus indicating no clear evidence of a potential teratogenic effect of nitroglycerin.

Nursing Mothers

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

Pediatric Use

The safety and effectiveness of RECTIV in pediatric patients under 18 years of age have not been established.

Geriatric Use

Clinical studies of RECTIV did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Clinical data from the published literature indicate that the elderly demonstrate increased sensitivity to nitrates, which may be therapeutic but also manifest by more frequent or severe hypotension and related dizziness or fainting. Increased sensitivity may reflect the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Overdosage

Nitroglycerin toxicity is generally mild. The estimated adult oral lethal dose of nitroglycerin is 200 mg to 1,200 mg. Infants may be more susceptible to toxicity from nitroglycerin. Consultation with a poison center should be considered.

Laboratory determinations of serum levels of nitroglycerin and its metabolites are not widely available, and such determinations have, in any event, no established role in the management of nitroglycerin overdose.

No data are available to suggest physiological maneuvers (e.g., maneuvers to change the pH of the urine) that might accelerate elimination of nitroglycerin and its active metabolites. Similarly, it is not known which if any of these substances can usefully be removed from the body by hemodialysis.

No specific antagonist to the vasodilator effects of nitroglycerin is known, and no intervention has been subject to controlled study as a therapy of nitroglycerin overdose. Because the hypotension associated with nitroglycerin overdose is the result of venodilatation and arterial hypovolemia, prudent therapy in this situation should be directed toward increase in central fluid volume. Passive elevation of the patient's legs may be sufficient, but intravenous infusion of normal saline or similar fluid may also be necessary.

The use of epinephrine or other arterial vasoconstrictors in this setting is not recommended.

In patients with renal disease or congestive heart failure, therapy resulting in central volume expansion is not without hazard. Treatment of RECTIV overdose in these patients may be subtle and difficult, and invasive monitoring may be required.

Methemoglobinemia

Methemoglobinemia has been rarely reported with organic nitrates. The diagnosis should be suspected in patients who exhibit signs of impaired oxygen delivery despite adequate arterial PO2. Classically, methemoglobinemic blood is described as chocolate brown, without color change on exposure to air.

If methemoglobinemia is present, intravenous administration of methylene blue, 1 to 2 mg/kg of body weight, may be required.

Rectiv Ointment Description

Nitroglycerin is 1,2,3,-propanetriol trinitrate, an organic nitrate whose structural formula is as follows:

CH2-ONO2

 |

CH-ONO2

 |

CH2-ONO2

and whose molecular weight is 227.09. RECTIV (nitroglycerin) Ointment 0.4% contains 0.4% nitroglycerin w/w (4 mg nitroglycerin/1 g ointment), propylene glycol, lanolin, sorbitan sesquioleate, paraffin wax, and white petrolatum. RECTIV (nitroglycerin) Ointment 0.4% is available in tubes with a one-inch dosing line on the carton allowing the measurement of approximately 375 mg of nitroglycerin ointment 0.4% (1.5 mg nitroglycerin) for application.

Rectiv Ointment - Clinical Pharmacology

Mechanism of Action

Nitroglycerin forms free radical nitric oxide (NO), which activates guanylate cyclase, resulting in an increase of guanosine 3',5'-monophosphate (cyclic GMP) in smooth muscle and other tissues. This leads to dephosphorylation of myosin light chains, which regulates the contractile state in smooth muscle and results in vasodilatation.

Pharmacodynamics

The principal pharmacological action of nitroglycerin is relaxation of vascular smooth muscle. Intra-anal application of nitroglycerin reduces sphincter tone and resting intra-anal pressure.

Pharmacokinetics

Absorption: In six healthy subjects, the average absolute bioavailability of nitroglycerin applied to the anal canal as a 0.2% w/w ointment was approximately 50% of the 0.75 mg nitroglycerin dose.

Distribution: The volume of distribution of nitroglycerin following intravenous administration is about 3 L/kg. At plasma concentrations between 50 and 500 ng/mL, the binding of nitroglycerin to plasma proteins is approximately 60%, while that of 1,2- and 1,3-dinitroglycerin is 60% and 30%, respectively.

Metabolism: Nitroglycerin is metabolized by a liver reductase enzyme to glycerol di- and mononitrate metabolites and ultimately to glycerol and organic nitrate. Known sites of extrahepatic metabolism include red blood cells and vascular walls. In addition to nitroglycerin, the two major metabolites, 1,2- and 1,3- dinitroglycerols are found in plasma. The contribution of metabolites to the relaxation of the internal anal sphincter is unknown. The dinitrates are further metabolized to nonvasoactive mononitrates and ultimately to glycerol and carbon dioxide.

Elimination: Metabolism is the primary route of drug elimination. Nitroglycerin plasma concentrations decrease rapidly with a mean elimination half-life of two to three minutes. Half-life values range from 1.5 to 7.5 minutes. Clearance (13.6 L/min) greatly exceeds hepatic blood flow.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Animal carcinogenicity studies with topically applied nitroglycerin have not been performed.

Rats receiving up to 434 mg/kg/day of dietary nitroglycerin for 2 years developed dose-related fibrotic and neoplastic changes in liver, including carcinomas, and interstitial cell tumors in testes. At the highest dose, the incidence of hepatocellular carcinomas was 52% compared to 0% in untreated controls. Incidence of testicular tumors were 52% vs. 8% in controls. Lifetime dietary administration of up to 1058 mg/kg/day of nitroglycerin was not tumorigenic in mice.

Nitroglycerin was mutagenic in the in vitro bacterial reverse mutation (Ames) assay with Salmonella typhimurium. A similar mutation in this S. typhimurium was also reported with other NO donors. There was no evidence of clastogenic potential in multiple assays including a rodent dominant lethal assay, an in vitro Chinese Hamster Ovary assay that was conducted in the absence of metabolic activation, and several in vivo chromosomal aberration assays conducted in rats and dogs.

In a three-generation reproduction study, rats received dietary nitroglycerin at doses up to approximately 434 mg/kg/day for 6 months prior to mating of the F0 generation with treatment continuing through successive F1 and F2 generations. The high dose was associated with decreased feed intake and body weight gain in both sexes at all matings. No specific effect on the fertility of the F0 generation was seen. Infertility noted in subsequent generations, however, was attributed to increased interstitial cell tissue and aspermatogenesis in the high-dose males.

Clinical Studies

Rectiv Ointment was evaluated in a 3-week double-blind, randomized, multi-center, placebo-controlled study. Patients with a painful chronic anal fissure for at least 6 weeks and moderate or severe pain prior to treatment (≥ 50 mm on the 100 mm visual analog scale, VAS) were randomized to receive 0.4% (1.5 mg) nitroglycerin or placebo ointment applied to the anal canal every 12 hours. Pain as assessed by the change in VAS from baseline to Days 14-18 was lower in patients receiving 0.4% ointment compared to placebo. The mean change from baseline was 44 mm for RECTIV and 37 mm for placebo. The difference in the mean change in pain between RECTIV and placebo was -7.0 mm (95% Confidence Interval: -13.6 to -0.4 mm).

How Supplied/Storage and Handling

RECTIV (nitroglycerin) Ointment 0.4% is available in 30 g (NDC 42747-235-30) aluminum tubes with polyethylene screw caps.

Store at 20°-25°C (68°-77°F); excursions permitted between 15°-30°C (59°-86°F). [See USP Controlled Room Temperature].

Keep the tube tightly closed. Use within 8 weeks of first opening.

Patient Counseling Information

See FDA-approved patient labeling (Patient Information and Instructions for Use)

Interaction with PDE5 inhibitors

Advise patient not to use RECTIV with medications for erectile dysfunction such as Viagra (sildenafil), Levitra (vardenafil), and Cialis (tadalafil). These products have been shown to increase the hypotensive effects of RECTIV and other nitrate drugs.

Hypotension

Advise patients that treatment with RECTIV may be associated with light-headedness on standing, especially just after rising from a lying or seated position. The effect may be more frequent in patients who have also consumed alcohol, since alcohol use contributes to hypotension. Advise patients to stand up from the supine or sitting position slowly.

Headaches

Advise patients that headaches sometimes accompany treatment with RECTIV. For patients who get these headaches, the headaches may indicate the activity of the drug. Tolerance to headaches develops. Advise patients that if they experience headache they should not alter the schedule of their RECTIV treatment to avoid the occurrence of headache. An analgesic, such as acetaminophen, may be used to prevent or relieve the headaches.

Dizziness

Advise patients that dizziness has been reported as a side-effect of treatment with RECTIV.

Advise patients not to drive or operate machinery immediately after applying RECTIV.

FDA-Approved Patient Labeling

Patient Information

RECTIV™ [REC-tiv]

(Nitroglycerin) Ointment 0.4%

IMPORTANT: For intra-anal use only

Read the Patient Information that comes with RECTIV before you start using the product and each time you get a refill because there may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or your treatment. If you have any questions about RECTIV, ask your healthcare provider.

What is RECTIV?

RECTIV is a prescription medicine used to treat moderate to severe pain caused by chronic anal fissures. An anal fissure is a tear in the skin lining the anal canal.

RECTIV is not suitable for children and adolescents under the age of 18 years because it has not been assessed in people in this age group.

Who should not use RECTIV?

Do not use RECTIV if you:

• are taking a medicine for erectile dysfunction (male impotence), for example Viagra (sildenafil), Cialis (tadalafil) or Levitra (vardenafil).


• have been told by your doctor that you have severe anemia (low numbers of red blood cells in your blood)


• have increased intracranial pressure or high pressure within your skull e.g. following head trauma or bleeding in your brain


• are allergic to any of the ingredients in RECTIV or if you have had allergic reactions to similar medicines in the past. See the end of this leaflet for a list of ingredients in RECTIV.

What should I tell my healthcare provider before using RECTIV?

Tell your healthcare provider about all your medical conditions, including if you:

• have low blood pressure


• have recently had a heart attack


• have heart or blood vessel disorders


• suffer from migraine or recurrent headaches


• are pregnant or plan to become pregnant. It is not known if RECTIV will harm your unborn baby.


• are breast-feeding or plan to breast-feed. It is not known if the components of RECTIV will harm your child if you breast-feed.

RECTIV may lower your blood pressure. When getting up from a lying or sitting position, you should get up slowly, otherwise you might feel faint.

Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins and herbal supplements. Other medicines may affect how RECTIV works. RECTIV may also affect how other medicines work.

Specifically, tell your doctor if you are taking any of the following:

• other nitroglycerin containing products


• a medicine for erectile dysfunction (male impotence), for example sildenafil, tadalafil or vardenafil (see the section above 'Who should not use RECTIV')


• medicines used to treat high blood pressure


• are taking aspirin, ergotamine (used to treat migraine) or are receiving tissue-type plasminogen activator (used to help dissolve blood clots formed in blood vessels in the heart, lungs and brain)


• are to be given heparin. If so, close monitoring of your blood will be required as your dose of heparin may need to be altered. Please discuss with your doctor before stopping RECTIV.

How should RECTIV be used?

Use RECTIV exactly as prescribed. See detailed Patient Instructions for Applying RECTIV at the end of this Patient Information leaflet.

Treatment may be continued for up to 3 weeks. If your anal pain does not get better after using RECTIV you should talk to your doctor.

What should I avoid while using RECTIV?

Do not drive or operate machinery immediately after applying RECTIV. If you feel dizzy or light-headed after applying the ointment do not drive or operate machinery until the dizziness has stopped.

Avoid consuming alcohol while you are being treated with RECTIV as your blood pressure is more likely to be affected if you consume alcoholic beverages.

What are the possible side effects of RECTIV?

RECTIV can cause serious side-effects: Stop using the ointment and seek medical attention immediately if you have an allergic reaction. You may have swelling of the face, lips, tongue or throat, or difficulty breathing.

Common side-effects of RECTIV are:

• Headaches, which can be severe. You could take painkillers for this (such as acetaminophen). If the headaches are unpleasant, you may need to ask your doctor whether you should stop using RECTIV.


• Dizziness, faintness on standing, or light-headedness

These are not all the possible side effects of RECTIV. Tell your healthcare provider if you have any side effect that bothers you or that does not go away. For more information, ask your healthcare provider or pharmacist.

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

How should I store RECTIV?

• Store at 20°-25°C (68°-77°F); excursions permitted between 15°-30°C (59°-86°F). [See USP Controlled Room Temperature].


• Keep the tube tightly closed.


• Use within 8 weeks of first opening.

Keep RECTIV out of the reach of children.

Do not use RECTIV after the expiry date which is stated on the label and carton after 'EXP.' The expiry date refers to the last day of that month.

General information about RECTIV

Medicines are sometimes prescribed for conditions that are not mentioned in Patient Information leaflets. Do not use RECTIV for a condition for which it is not prescribed. Do not give RECTIV to other people, even if they have the same symptoms you have. It may harm them.

This Patient Information leaflet summarizes the most important information about RECTIV. If you would like more information, talk to your healthcare provider. You can ask your pharmacist or healthcare provider for information about RECTIV that is written for health professionals.

For more information call 1-800-6RECTIV or visit www.RECTIV.com.

Patient Instructions for Use

When do I apply the ointment?

Apply the ointment every 12 hours exactly as your doctor has told you to.

How do I apply the ointment?

Cover your finger with plastic-wrap, a disposable surgical glove or a finger cot.

Lay the covered finger alongside the 1 inch dosing line marked on the side of the medicine box (see figure below) so that the tip of your finger is at one end of the dosing line. Starting at the tip of the finger, squeeze the ointment onto your finger for the same length marked on the box.

Refer to carton for accurate dosage guide.

Gently insert the finger with the ointment into the anal canal, up to the first finger joint. Carefully smear the ointment around the inner sides of the anal canal. If this cannot be achieved due to pain, application of the ointment should be made directly to the outside of the anus.

What do I do after I have applied the ointment?

Throw away the finger covering in the garbage, out of the reach of children and pets. Wash your hands.

What are the ingredients in RECTIV?

Active ingredient: nitroglycerin

Inactive ingredients: propylene glycol, lanolin, sorbitan sesquioleate, paraffin wax and white petrolatum.

Manufactured by:

PHARBIL Waltrop GmbH

Im Wirrigen 25

45731 Waltrop

Germany

Manufactured for:

ProStrakan, Inc.

Bedminster, NJ 07921

Revised: June 2011

PRINCIPAL DISPLAY PANEL - OINTMENT 0.4%

NDC 42747-235-30

RECTIV

(nitroglycerin)

Ointment 0.4%

For Intra-anal Use Only

30 g

 

RECTIV  nitroglycerin  ointment

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 42747-235 Route of Administration RECTAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength NITROGLYCERIN (NITROGLYCERIN) NITROGLYCERIN 4 mg  in 1 g

Inactive Ingredients Ingredient Name Strength PROPYLENE GLYCOL   LANOLIN   SORBITAN SESQUIOLEATE   PARAFFIN   PETROLATUM

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 42747-235-30 1 TUBE In 1 CARTON contains a TUBE 1 30 g In 1 TUBE This package is contained within the CARTON (42747-235-30)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NDA	NDA021359	06/21/2011

Labeler - ProStrakan, Inc. (014778321)

Establishment
Name	Address	ID/FEI	Operations
Pharbil Waltrop GmbH		343740283	manufacture

Revised: 06/2011ProStrakan, Inc.

More Rectiv Ointment resources

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

Compare Rectiv Ointment with other medications

• Anal Fissure and Fistula