Testosterone Cipionate
Testosterone Cipionate Uses, Dosage, Side Effects, Food Interaction and all others data.
Testosterone Cipionate is a synthetic derivative of testosterone in the form of an oil-soluble 17 (beta)-cyclopentylpropionate ester. Its benefit compared to other testosterone derivatives is the slow rate of release after injection and longer half-life. The characteristics of testosterone cypionate and testosterone enanthate are very similar, therefore both of them tend to be interchangeable. It was developed by the company Pharmacia and Upjohn and FDA approved on July 25, 1979.
Testosterone Cipionate presents the same properties than its analog testosterone with the advantage that this molecule has a longer release rate and half-life. Administration of ester derivatives of testosterone as testosterone cypionate generates an increase in serum testosterone to levels reaching 400% from the baseline within 24 hours of administration. These androgen levels remain elevated for 3-5 days after initial administration. The continuous variation in plasma testosterone after intramuscular administration of testosterone cypionate results in fluctuations in mood and libido as well as some local inflammation.
| Trade Name | Testosterone Cipionate |
| Generic | Testosterone cypionate |
| Testosterone cypionate Other Names | Testosterone cipionate, Testosterone cyclopentanepropionate, Testosterone cyclopentylpropionate, Testosterone cypionate |
| Type | |
| Formula | C27H40O3 |
| Weight | Average: 412.614 Monoisotopic: 412.297745148 |
| Protein binding | Once absorbed, testosterone cypionate enters the bloodstream to be processed. Once modified, 40% of the resultant testosterone will bind to plasma globulin and 2% remains unbound or bound to albumin and other proteins. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Testosterone Cipionate is an androgen used to treat low or absent testosterone.
Testosterone Cipionate is used in males that present conditions derived from a deficiency or absence of endogenous testosterone. These conditions are 1) primary hypogonadism, defined as the testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome or orchidectomy; and 2) hypogonadotropic hypogonadism characterized by idiopathic gonadotropin, LHRH deficiency or pituitary-hypothalamic injury from tumors, trauma or radiation.
Testosterone Cipionate is also used to associated treatment for these conditions: Hypergonadotropic Hypogonadism, Hypogonadotrophic Hypogonadism
How Testosterone Cipionate works
The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects.
Toxicity
Preclinical studies with testosterone implants induced cervical-uterine tumors in mice which metastasized in some cases. Some reports indicate that administration of testosterone cypionate in females can augment the susceptibility to hepatoma as well as increase the number of tumors. Clinical studies have reported cases of hepatocellular carcinoma in long-term high-dose therapy.
Food Interaction
No interactions found.Volume of Distribution
The volume of distribution following intravenous administration of testosterone is of approximately 1 L/kg.
Elimination Route
Testosterone Cipionate is an esterified anabolic which allows it to present a greater degree of solubility in fats and thus, the release and absorption occur in a slow rate compare to homologous molecules. Intramuscular administration of 200 mg of testosterone cypionate produced a mean supratherapeutic Cmax of 1122 ng/dl which occurred 4-5 days post-injection. After the fifth day, the levels of testosterone cypionate in plasma went down reaching an average of 400 ng/dl.
Half Life
The half-life of testosterone cypionate is one of the longest, being approximately of 8 days.
Clearance
Testosterone Cipionate presents a lower clearance rate after intramuscular administration compared to other analogs of testosterone.
Elimination Route
About 90% of a dose of testosterone given intramuscularly is excreted in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about 6% of a dose is excreted in the feces, mostly in the unconjugated form.
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