Get your patient on Testosterone Cypionate - Testosterone Cypionate injection (Testosterone Cypionate)

Testosterone cypionate 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)-gonadotropin or LHRH deficiency, or pituitary-hypothalamic injury from tumors, trauma, or radiation.

Safety and efficacy of testosterone cypionate in men with "age -related hypogonadism" (also referred to as "late-onset hypogonadism") have not been established.

Prior to initiating testosterone cypionate injection, confirm the diagnosis of hypogonadism by ensuring that serum testosterone concentrations have been measured in the morning on at least two separate days and that these serum testosterone concentrations are below the normal range.

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.

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 pregnant (see PRECAUTIONS, Pregnancy)
5. Patients with serious cardiac, hepatic or renal disease (see WARNINGS)

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.

Cardiovascular disorders: myocardial infarction, stroke.

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.

Vascular disorders: Venous thromboembolism.

Special senses: Rare cases of central serous chorioretinopathy (CSCR)

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

Testosterone cypionate, 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)-, (17ß)-. Its molecular formula is C ₂₇ H ₄₀ O ₃ , and the molecular weight 412.61.

The structural formula is represented below:

Testosterone cypionate injection, USP 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

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.

Testosterone cypionate injection, USP is a clear colourless to pale yellow solution and is available as:

100 mg/mL

10 mL vials                                                  NDC 69097-536-37

200 mg/mL

1 mL vials                                                    NDC 69097-537-31

10 mL vials                                                  NDC 69097-537-37

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

This product's label may have been updated. For current full prescribing information, please visit www.ciplausa.com

Rx only

Manufactured by: Cipla Ltd.

At M/s LSNE-Le n SLU

C/Nicostrato Vela s/n 24009 Le n, Spain

Manufactured for: Cipla USA, Inc.

10 Independence Boulevard, Suite 300,

Warren, NJ 07059

Revised: 01/2022