Cypionate

Cypionate

What is Cypionate®?

Cypionate – 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.

In addition, Drugs in this class also cause retention of nitrogen, sodium, potassium, and phosphorous, and decrease  urinary excretion of calcium.

Moreover, Researchers reports that androgens increase protein anabolism and decrease protein catabolism. Sufficient intake of calories and protein is necessary to improve nitrogen balance.

 

Androgens

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. Furthermore, Researchers reports that androgens stimulate the production of red blood cells by enhancing the production of erythropoietic stimulation factor.

In addition, During the exogenous administration of androgens, endogenous testosterone release inhibits through feedback inhibition of pituitary luteinizing hormone (LH). Moreover, At large doses of exogenous androgens, spermatogenesis may also suppress through feedback inhibition of pituitary follicle-stimulating hormone (FSH).
There is no 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 absorb slowly from the lipid phase; Therefore, one can administer testosterone cypionate at intervals of two to four weeks.

Testosterone in plasma is 98 percent bind 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.

The body excretes about 90 percent of a dose of testosterone in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites. The body excretes approximately 6 percent of a dose in the feces, mainly in the unconjugated form.

In addition, The liver primarily carries out the inactivation of testosterone. Testosterone undergoes metabolism into various 17-keto steroids through two different pathways.

The half-life of testosterone cypionate, when Injects 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. Moreover, the steroid-receptor complex transports itself to the nucleus, which initiates transcription events and induces cellular changes associates with androgen action.

 

Indications And Usage:

Males with conditions associated with symptoms of deficiency or absence of endogenous testosterone can use Cypionate® as a replacement therapy.

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

Second : Hypogonadotropic hypogonadism (congenital or acquires)-idiopathic gonadotropin or LHRH deficiency, or pituitary-hypothalamic Injury from tumors, trauma, or radiation.

 

Contraindications:

First : Know hypersensitivity to the drug
Second : Males with carcinoma of the breast
Third : Males with known or suspects carcinoma of the prostate gland
Fourth : Women who are or who may become pregnant
Fifth : Patients with serious cardiac, hepatic or renal disease.

 

Warnings:

Hypercalcemia may occur in immobilizes patients. If this occurs, the drug should discontinue.  In addition, Prolong use of high doses of androgens (principally the 17-delta alkyl-androgens) has been associates with development of hepatic adenomas. Also,  hepatocellular carcinoma, and peliosis hepatis- all potentially life-threatening complications.

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

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

Moreover, Patients treats for hypogonadism may develop gynecomastia, which can occasionally persist.

Thus, This product contains benzyl alcohol. Reports have associates benzyl alcohol with a fatal “Gasping Syndrome” in premature infants.

 

Androgen

Cautious use of androgen therapy recommends for healthy males with delayed puberty. In addition, the effect on bone maturation should be carefully monitored by assessing the 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. Moreover, This adverse effect may result in compromises adult stature. Furthermore, The younger the child, the greater the risk of compromising final mature height.

Thus, This drug is not safe and effective for enhancing athletic performance. Because of the potential risk of serious adverse health effects, this drug should not be use for such purposes.

 

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.

Therefore, if any of these effects appear, one should stop the androgen and, if restarted, use a lower dosage. You should not use Cypionate® interchangeably with testosterone propionate due to differences in their duration of action.

Cypionate® is not for intravenous use.

Important information for patients: Please promptly report any of the following symptoms to your healthcare provider: nausea, vomiting, changes in skin color, ankle swelling, 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/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.Researchers have tested testosterone through 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 the Injection of testosterone into some strains of female mice increases their susceptibility to hepatoma.

Researchers have reported that testosterone increases tumor incidence and decreases the degree of differentiation in chemically-induced liver carcinomas 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 should not use Cypionate®. Cypionate® is also not recommended for pediatric use.

 

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.

 

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 hepatic (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:

Testosterone is classified as a controlled substance under the Anabolic Steroids Control Act. Cypionate® is specifically been assigning to Schedule III.

 

Overdosage:

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

 

Dosage And Administration:

Cypionate® is for intramuscular use only. It is important to note that testosterone should not be administered intravenously. When administering intramuscular injections, it recommends to administer the injection deep into the gluteal muscle.

The suggested dosage for Cypionate® varies depending on the age, sex, and diagnosis of the individual patient. Dosage adjusts according to the patient’s response and the appearance of adverse reactions.

Healthcare providers employ various dosage regimens 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 in maintenance levels.

Other experts have emphasized that higher dosages are necessary to induce pubertal changes, whereas lower dosages can be utilized for maintenance after puberty.

The initial dose and subsequent adjustments should be based on the chronological and skeletal ages. In the case of hypogonadal males who requires replacement therapy, it is recommend to administer a dosage of 50-400 mg every two to four weeks.

Parenteral drug products should be inspects 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.

Patients should store the vials of Cypionate® Injection, Solution-Intramuscular-200 mg/ml at controlled room temperatures, specifically between 15-30°C (59-86°F), and protect them from light.

 

Last Recommendation and Contact Info

HOW SUPPLY- Cypionate® Injection, Solution-Intramuscular-200 mg/ml is supply in 1 ml vial.

Sidney Gordon – President – Cell. 561-213-7772

Visit Core Medical Group  website for more information. Ph. 866-641-CORE (2673)

Fax. 866-686-5280

 

Post by admin

Comments are closed.