Advertisement

Topics

TESTOSTERONE CYPIONATE INJECTION USP FOR INTRAMUSCULAR USE ONLY C-III Rx only | Testosterone Cypionate

12:48 EDT 24th July 2014 | BioPortfolio

Note: While we endeavour to keep our records up-to-date one should not rely on these details being accurate without first consulting a professional. Click here to read our full medical disclaimer.

Testosterone Cypionate 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 CHO and the molecular weight 412.61.

The structural formula is represented below:

Each mL contains: Testosterone Cypionate 200 mg, Benzyl Benzoate 20%, with Benzyl Alcohol 0.9% as preservative in Cottonseed Oil q.s.

IMAGE testosterone-cypionate-injection-1.jpg

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 prostate, seminal vesicles, penis, and scrotum; development of male hair distribution, such as beard, pubic, chest and axillary hair; laryngeal enlargement, vocal chord thickening, and alterations in body musculature and fat distribution. Drugs in this class also cause retention of nitrogen, sodium, potassium, and phosphorus, 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.

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.

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

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.

Patients with benign prostatic hypertrophy may develop acute urethral obstruction. Priapism or excessive sexual stimulation may develop. Oligospermia may occur after prolonged administration of 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.

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.

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.

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.

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

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.

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 Category X (See CONTRAINDICATIONS ).

Testosterone Cypionate Injection is not recommended for use in nursing mothers.

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

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

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

Hirsutism, male pattern of baldness, seborrhea, and acne.

Retention of sodium, chloride, water, potassium, calcium, and inorganic phosphates.

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

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

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

Hypersensitivity, including skin manifestations and anaphylactoid reactions.

Inflammation and pain at the site of intramuscular injection.

Controlled Substance Class: Testosterone is a controlled substance under the Anabolic Steroids Control Act, and Testosterone Cypionate Injection has been assigned to Schedule III.

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

Testosterone Cypionate 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 Testosterone Cypionate 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.

Testosterone Cypionate Injection USP, 200 mg/mL is available in: 10 mL multiple dose vials, individually boxed.

Store at 20°-25°C (68°-77°F) [See USP Controlled Room Temperature].

PROTECT FROM LIGHT.

Literature revised: July 2010Product No.: 0256-10

Manufactured by: Hikma Farmaceutica (Portugal) S.A. 2705-906 Terrugem SNT, Portugal Distributed by: Watson Pharma, Inc. Corona, CA 92880 USA

PIN230-WAT/1

NDC 0591-3223-7910 mL Multiple Dose VialTestosterone CypionateInjection USP2,000 mg/10 mL(200 mg/mL)FOR INTRAMUSCULAR USE ONLY Watson    Rx only Sterile Each mL contains: Testosterone Cypionate 200 mg,Benzyl Benzoate 20%, with Benzyl Alcohol 0.9% as preservative, in Cottonseed Oil. Usual adult dosage: See package insert.

Store at 20°-25°C (68°-77°F) [See USP Controlled Room Temperature].

PROTECT FROM LIGHT.

Manufactured by: Hikma Farmaceutica (Portugal) S.A. 2705-906 Terrugem SNTPortugal Distributed by: Watson Pharma, Inc. Corona, CA 92880 USA

IMAGE testosterone-cypionate-injection-2.jpg

Manufacturer

Watson Laboratories, Inc.

Active Ingredients

Source

Drugs and Medications [57 Associated Drugs and Medications listed on BioPortfolio]

Testosterone cypionate [Teva Parenteral Medicines, Inc]

Testosterone Cypionate Injection, USP Multiple Dose Vials CIII

Testosterone cypionate [Paddock Laboratories, Inc.]

Testosterone Cypionate Injection, USP

Testosterone cypionate [Physicians Total Care, Inc.]

Testosterone Cypionate Injection, USP

Testosterone cypionate [Sandoz Inc]

Testosterone Cypionate Injection, USP100 mg/mL and 200 mg/mL

Depo-testosterone [Physicians Total Care, Inc.]

Depo-Testosteronetestosterone cypionate injection, USP    CIII

Clinical Trials [406 Associated Clinical Trials listed on BioPortfolio]

TESTO: Testosterone Effects on Short-Term Outcomes in Infants With XXY

This research study in infant males with Klinefelter syndrome (47,XXY) will learn more about the effect of testosterone on early health and development. The study is a total of three visit...

The Effect of Testosterone Replacement on Bone Mineral Density in Boys and Men With Anorexia Nervosa

Decreased bone strength is a common and serious medical problem present in many people with anorexia nervosa. Men with anorexia nervosa have lower levels of gonadal steroids such as testo...

Testosterone Revival Abolishes Negative Symptoms, Fosters Objective Response and Modulates Enzalutamide Resistance

Asymptomatic men with progressive metastatic CRPC post- treatment with abiraterone acetate (pre-chemotherapy for metastatic disease) will be treated on a randomized, multi-Institutional op...

Role of Anabolic Steroids on Intensive Care Unit-Acquired Weakness

We aim to investigate possible anabolic effects of bi-weekly exogenous testosterone administration during intensive care unit (ICU) stay for up to 8 weeks. Control group will receive stand...

Comparative Bioavailability of Two Injectable Suspension Formulations of Medroxyprogesterone Acetate+Estradiol Cypionate

This clinical trial evaluated the comparative bioavailability of two injectable suspension formulations of medroxyprogesterone acetate + estradiol cypionate, a test (Depomês®, 25 mg/mL m...

PubMed Articles [410 Associated PubMed Articles listed on BioPortfolio]

Population Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Depot Testosterone Cypionate in Healthy Male Subjects.

A randomized, double-blind clinical trial was conducted to investigate long-term abuse effects of testosterone cypionate. Thirty-one healthy males were randomized into a dose group of 100, 250 or 500m...

Recommendations for the Use of Testosterone in Male Transgender.

Gender incongruence is defined as a condition in which an individual self-identifies and desires to have physical characteristics and social roles that connote the opposite biological sex. Gender dysp...

Testosterone treatment and the risk of aggressive prostate cancer in men with low testosterone levels.

Testosterone treatment of men with low testosterone is common and, although relatively short-term, has raised concern regarding an increased risk of prostate cancer (CaP). We investigated the associat...

How low can you go? Analytical performance of five automated testosterone immunoassays.

Testosterone is commonly measured using immunoassays, yet concerns with the accuracy and quality of testing by these methods exist, particularly for low testosterone concentrations. Study objectives w...

The marketing of testosterone treatments for age-related low testosterone or 'Low T'.

To summarize the research evidence on promotion of testosterone for 'Low T', or age-related hypogonadism.

Advertisement
Quick Search
Advertisement
Advertisement

 

Relevant Topics

Endocrinology
Diabetes Diabetes Endocrine Obesity Oxycontin Renal Disease Thyroid Disorders Endocrinology is the study of the endocrine glands and the hormones that they secrete (Oxford Medical Dictionary). There are several groups of h...

Endocrine Disorders
Endocrine disorders are grouped into two categories: hormone imbalance - when a gland produces too much or too little of an endocrine hormone development of lesions (such as nodules or tumors) in the endocrine system, which may or may not affect...


Drugs and Medication Quicklinks


Searches Linking to this Drug Record