Cystorelin

Dosage Form: FOR ANIMAL USE ONLY
Cystorelin®

(Gonadorelin Diacetate Tetrahydrate)

FOR INJECTION

For the treatment of cystic ovaries in cattle

CAUTION

Federal (U.S.A.) law restricts this drug to use by or on the order of a licensed veterinarian.

Cystorelin Description

Cystorelin® is a sterile solution containing 50 micrograms of gonadorelin (GnRH) diacetate tetrahydrate per milliliter suitable for intramuscular or intravenous administration. Gonadorelin is a decapeptide composed of the sequence of amino acids–

 

5-oxoPro-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2–

a molecular weight of 1182.32 and empirical formula C55H75N17O13. The diacetate tetrahydrate ester has a molecular weight of 1374.48 and empirical formula C59H91N17O21.

Gonadorelin is the hypothalamic releasing factor responsible for the release of gonadotropins (e.g., LH, FSH) from the anterior pituitary. Synthetic gonadorelin is physiologically and chemically identical to the endogenous bovine hypothalamic releasing factor.

PHARMACOLOGY AND TOXICOLOGY

Endogenous gonadorelin is synthesized and/or released from the hypothalamus during various stages of the bovine estrus cycle following appropriate neurogenic stimuli. It passes via the hypophyseal portal vessels, to the anterior pituitary to effect the release of gonadotropins (e.g. LH, FSH) Synthetic gonadorelin administered intravenously or intramuscularly also causes the release of endogenous LH or FSH from the anterior pituitary.

Gonadorelin diacetate tetrahydrate has been shown to be safe. The LD50 for mice and rats is greater than 60 mg/kg, and for dogs, greater than 600 mcg/kg, respectively. No untoward effects were noted among rats or dogs administered 120 mcg/kg/day or 72 mcg/kg/day intravenously for 15 days.

It has no adverse effects on heart rate, blood pressure, or EKG to unanesthetized dogs at 60 mcg/kg. In anesthetized dogs it did not produce depression of myocardial or system hemodynamics or adversely affect coronary oxygen supply or myocardial oxygen requirements.

The intravenous administration of 60 mcg/kg/day of gonadorelin diacetate tetrahydrate to pregnant rats and rabbits during organogenesis did not cause embryotoxic or teratogenic effects.

The intramuscular administration of 1000 mcg to normally cycling dairy cattle had no effect on hematology or blood chemistry.

Further, Cystorelin does not cause irritation at the site of intramuscular administration in dogs. The dosage administered was 72 mcg/kg/day for seven (7) days.

INDICATIONS AND DOSAGE

Cystorelin® is indicated for the treatment of ovarian follicular cysts in dairy cattle. Ovarian cysts are non-ovulated follicles with incomplete luteinization which result in nymphomania or irregular estrus.

Historically, cystic ovaries have responded to an exogenous source of luteinizing hormone (LH) such as human chorionic gonadotropin. Cystorelin initiates release of endogenous LH to cause ovulation and luteinization.

The recommended intravenous or intramuscular dosage of Cystorelin is 100 mcg (2 mL) per cow.

Each mL of Cystorelin contains:
Gonadorelin diacetate tetrahydrate	50 mcg
Benzyl Alcohol	9 mg
Sodium Chloride	7.47 mg
Water for Injection, U.S.P.	q.s.
pH adjusted with potassium phosphate (monobasic and dibasic).

Precautions

Not for use in humans.

Keep this and all drugs out of reach of children.

The Material Safety Data Sheet (MSDS) contains more detailed occupational safety information. To report adverse effects in users, to obtain an MSDS, or for assistance call 1-888-637-4251.

KEEP REFRIGERATED: 2–8°C (36–46°F).

Discard remaining product 90 days after first use.

How is Cystorelin Supplied

Cystorelin is available in a concentration of 50 mcg/mL pH adjusted with potassium phosphate (monobasic and dibasic).

Cystorelin is supplied in multi-dose vials containing 10 mL and 30 mL of sterile solution.

Marketed by:

Merial LLC

Duluth, GA 30096-4640 U.S.A.

Technical Support 1-888-637-4251

® Cystorelin and the Cattle Head Logo are registered trademarks of Merial.

© 2010 Merial. All Rights Reserved.

Rev. 01/2010

1050-2907-00

NADA 098-379, Approved by FDA

Item No. 82830201

PRINCIPAL DISPLAY PANEL - 10 mL Carton

Cystorelin®

(Gonadorelin Diacetate Tetrahydrate)

(50 mcg/mL) Sterile Solution

FOR ANIMAL USE ONLY

NOT FOR HUMAN USE

KEEP OUT OF THE REACH OF CHILDREN

NADA 098-379, Approved by the FDA

CAUTION: Federal law

restricts this drug to use by

or on the order of a licensed

veterinarian.

Item No. 82830201

NET CONTENTS:

1 × 10 mL

MERIAL

PRINCIPAL DISPLAY PANEL - 30 mL Carton

Cystorelin®

(Gonadorelin Diacetate Tetrahydrate)

(50 mcg/mL) Sterile Solution

Item No. 72010

Carton contains 150 doses

NET CONTENTS: 10 × 30 mL

MERIAL

Cystorelin  gonadorelin diacetate tetrahydrate  injection, solution

Product Information Product Type PRESCRIPTION ANIMAL DRUG NDC Product Code (Source) 50604-8283 Route of Administration INTRAVENOUS, INTRAMUSCULAR DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength gonadorelin diacetate tetrahydrate (gonadorelin) gonadorelin diacetate tetrahydrate 50 ug  in 1 mL

Inactive Ingredients Ingredient Name Strength Benzyl Alcohol   Sodium Chloride   Water

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 50604-8283-1 1 BOTTLE In 1 CARTON contains a BOTTLE, GLASS 1 10 mL In 1 BOTTLE, GLASS This package is contained within the CARTON (50604-8283-1) 2 50604-8283-3 10 BOTTLE In 1 CARTON contains a BOTTLE, GLASS (50604-8283-2) 2 50604-8283-2 30 mL In 1 BOTTLE, GLASS This package is contained within the CARTON (50604-8283-3)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NADA	NADA098379	03/10/1978

Labeler - Merial Limited (034393582)

Revised: 09/2010Merial Limited