testosterone cypionate

Action and Spectrum

Actions and spectrum: 

Two primary mechanisms underlie the effects of testosterone in humans and other vertebrates: first, it activates the androgen receptor (either directly or as DHT); second, it converts to estradiol and activates specific estrogen receptors.

Target tissue cells receive free testosterone (T) via the cytoplasm, where it can attach to the androgen receptor or be broken down by the cytoplasmic enzyme 5-alpha-reductase to 5-alpha-dihydrotestosterone (DHT).

DHT has an androgenic potency that is roughly 2.5 times greater than T’s due to its even stronger binding to the same androgen receptor. A structural alteration enables the T-receptor or DHT-receptor complex to enter the cell nucleus and attach itself directly to particular chromosomal DNA nucleotide sequences. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Excess duration of penile erections 

At high doses, oligospermia may occur 

Hirsutism 

Seborrhea 

Myocardial infarction 

Retention of potassium, sodium, calcium, water, chloride, etc. 

Polycythemia 

Headache 

Depression 

Anxiety 

Generalized paresthesia 

Thromboembolism 

Inflammation at injection site 

Central serous chorioretinopathy 

Black Box Warning

Black Box Warning  

For intramuscular use only 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

Hypersensitivity 

Suspected or known prostate gland carcinoma in males 

Breast carcinoma in males 

Pregnancy in women 

Hepatic failure 

Renal failure 

Cardiac diseases 

Caution: 

May cause hypercalcemia in immobilized patients 

Life-threatening: 

Prolonged use may cause  

hepatocellular carcinoma  

peliohepatis 

hepatic adenoma 

Post-marketing events 

Pulmonary embolism 

Deep vein thrombosis 

Hypogonadism  

Pregnancy / Lactation

Pregnancy consideration:  

USFDA pregnancy category: Contraindicated for use in pregnancy as it can harm the fetus. The effects of virilization on the female fetus may be seen if administered during pregnancy.  

Lactation:  

It is not recommended for use in lactating mothers 

Pregnancy category:  

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There was a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology: 

Testosterone cypionate is an oil-soluble 17(beta)- cyclopentyl propionate ester of AHT (androgenic hormone testosterone) 

Pharmacodynamics: 

When testosterone ester derivatives, such as testosterone cypionate, are administered, the serum testosterone levels rise to 400% of the baseline within 24 hours. Three to five days following the first dosage, these androgen levels don’t go down. Following intramuscular testosterone cypionate injection, there is a persistent fluctuation in plasma testosterone levels, which causes mood swings, libido swings, and mild local inflammation. 

Pharmacokinetics:  

Absorption 

Since testosterone cypionate constitutes an esterified anabolic, it has a higher degree of fat solubility than homologous molecules, causing its release and absorption to happen more slowly. 200 mg of testosterone cypionate injected intramuscularly resulted in a mean supratherapeutic Cmax of 1122 ng/dl four to five days after injection. Following the fifth day, the average amount of testosterone cypionate in plasma dropped to 400 ng/dl. 

Distribution 

The volume of distribution of testosterone cypionate is found to be around 1 liter/kg. 98% of testosterone converted is bound to plasma proteins, i.e., globulins. 

Metabolism 

Enzymes in the bloodstream are required for the processing of testosterone cypionate. These enzymes will break the link between the testosterone and the cypionate ester moiety. Following their separation, testosterone is metabolized via two distinct pathways to produce 17-keto steroids. Dihydrotestosterone (DHT) and estradiol are the two primary active metabolites. The steroid 5α-reductase found in the skin, liver, and urogenital tract converts testosterone to DHT. DHT undergoes additional metabolism in reproductive tissues to produce androstanediol. 

Elimination and excretion 

90% of testosterone administered through i.m is excreted in urine as sulfuric acid and glucuronide conjugates  

Half-life: 

Eight days 

Adminstartion

Administration: 

To be administered intramuscularly to the buttock  muscle 

Patient Information Leaflet

Patient information leaflet 

Generic Name: testosterone cypionate 

Why do we use testosterone cypionate? 

In males with conditions resulting from a lack or deficiency of endogenous testosterone, testosterone cypionate is used. These conditions are 1) primary hypogonadism, which is testicular failure resulting from bilateral torsion, idiopathic gonadotropin, orchitis, vanishing testis syndrome, or orchidectomy; and 2) hypogonadotropic hypogonadism, which is characterized by pituitary-hypothalamic injury from radiation, trauma, tumors, or deficiency of LHRH.