Peringatan Keamanan

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.L1153

Testosterone cypionate

DB13943

small molecule approved

Deskripsi

Testosterone cypionate 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. It was developed by the company Pharmacia and Upjohn and FDA approved on July 25, 1979.

Struktur Molekul 2D

Berat 412.614
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of testosterone cypionate is one of the longest, being approximately of 8 days.[L1151]
Volume Distribusi The volume of distribution following intravenous administration of testosterone is of approximately 1 L/kg.[L1155]
Klirens (Clearance) Testosterone cypionate presents a lower clearance rate after intramuscular administration compared to other analogs of testosterone.

Absorpsi

Testosterone cypionate 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.L1151 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.A31613

Metabolisme

To start its activity, testosterone cypionate has to be processed by enzymes in the bloodstream. These enzymes will break the bond between the cypionate ester moiety and the testosterone. Once separated, testosterone is metabolized to 17-keto steroids through two different pathways. The major active metabolites are estradiol and dihydrotestosterone (DHT). Testosterone is metabolized to DHT by steroid 5?-reductase in skin, liver and urogenital tract. In reproductive tissues DHT is further metabolized to androstanediol.L1153

Rute Eliminasi

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.L1153

Interaksi Obat

1444 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Testosterone cypionate.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Testosterone cypionate.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Testosterone cypionate.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Testosterone cypionate.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Testosterone cypionate.
Colchicine The metabolism of Colchicine can be decreased when combined with Testosterone cypionate.
Fentanyl Fentanyl may decrease the excretion rate of Testosterone cypionate which could result in a higher serum level.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Testosterone cypionate.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Testosterone cypionate.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Testosterone cypionate.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Testosterone cypionate.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Testosterone cypionate.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Testosterone cypionate.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Testosterone cypionate.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Testosterone cypionate.
Mifepristone The serum concentration of Testosterone cypionate can be increased when it is combined with Mifepristone.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Testosterone cypionate.
Perampanel The metabolism of Perampanel can be increased when combined with Testosterone cypionate.
Prasterone The serum concentration of Testosterone cypionate can be increased when it is combined with Prasterone.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Testosterone cypionate.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Testosterone cypionate.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Testosterone cypionate.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Testosterone cypionate.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Testosterone cypionate.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Testosterone cypionate.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Testosterone cypionate.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Testosterone cypionate.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Testosterone cypionate.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Testosterone cypionate.
Cyclosporine The risk or severity of liver damage can be increased when Testosterone cypionate is combined with Cyclosporine.
Insulin human Testosterone cypionate may increase the hypoglycemic activities of Insulin human.
Insulin lispro Testosterone cypionate may increase the hypoglycemic activities of Insulin lispro.
Insulin glargine Testosterone cypionate may increase the hypoglycemic activities of Insulin glargine.
Insulin pork Testosterone cypionate may increase the hypoglycemic activities of Insulin pork.
Glimepiride Testosterone cypionate may increase the hypoglycemic activities of Glimepiride.
Acetohexamide Testosterone cypionate may increase the hypoglycemic activities of Acetohexamide.
Miglitol Testosterone cypionate may increase the hypoglycemic activities of Miglitol.
Phenformin Testosterone cypionate may increase the hypoglycemic activities of Phenformin.
Gliclazide Testosterone cypionate may increase the hypoglycemic activities of Gliclazide.
Gliquidone Testosterone cypionate may increase the hypoglycemic activities of Gliquidone.
Mitiglinide Testosterone cypionate may increase the hypoglycemic activities of Mitiglinide.
Exenatide Testosterone cypionate may increase the hypoglycemic activities of Exenatide.
Mecasermin Testosterone cypionate may increase the hypoglycemic activities of Mecasermin.
Pramlintide Testosterone cypionate may increase the hypoglycemic activities of Pramlintide.
Glisoxepide Testosterone cypionate may increase the hypoglycemic activities of Glisoxepide.
Insulin aspart Testosterone cypionate may increase the hypoglycemic activities of Insulin aspart.
Insulin detemir Testosterone cypionate may increase the hypoglycemic activities of Insulin detemir.
Insulin glulisine Testosterone cypionate may increase the hypoglycemic activities of Insulin glulisine.
Glymidine Testosterone cypionate may increase the hypoglycemic activities of Glymidine.
AICA ribonucleotide Testosterone cypionate may increase the hypoglycemic activities of AICA ribonucleotide.
Buformin Testosterone cypionate may increase the hypoglycemic activities of Buformin.
Vildagliptin Testosterone cypionate may increase the hypoglycemic activities of Vildagliptin.
Voglibose Testosterone cypionate may increase the hypoglycemic activities of Voglibose.
NN344 Testosterone cypionate may increase the hypoglycemic activities of NN344.
AMG-222 Testosterone cypionate may increase the hypoglycemic activities of AMG-222.
Bisegliptin Testosterone cypionate may increase the hypoglycemic activities of Bisegliptin.
Liraglutide Testosterone cypionate may increase the hypoglycemic activities of Liraglutide.
Gosogliptin Testosterone cypionate may increase the hypoglycemic activities of Gosogliptin.
Glibornuride Testosterone cypionate may increase the hypoglycemic activities of Glibornuride.
Benfluorex Testosterone cypionate may increase the hypoglycemic activities of Benfluorex.
Albiglutide Testosterone cypionate may increase the hypoglycemic activities of Albiglutide.
Dulaglutide Testosterone cypionate may increase the hypoglycemic activities of Dulaglutide.
Insulin beef Testosterone cypionate may increase the hypoglycemic activities of Insulin beef.
Insulin degludec Testosterone cypionate may increase the hypoglycemic activities of Insulin degludec.
Insulin peglispro Testosterone cypionate may increase the hypoglycemic activities of Insulin peglispro.
Insulin tregopil Testosterone cypionate may increase the hypoglycemic activities of Insulin tregopil.
Ipragliflozin Testosterone cypionate may increase the hypoglycemic activities of Ipragliflozin.
Dutogliptin Testosterone cypionate may increase the hypoglycemic activities of Dutogliptin.
Allicin Testosterone cypionate may increase the hypoglycemic activities of Allicin.
Tofogliflozin Testosterone cypionate may increase the hypoglycemic activities of Tofogliflozin.
2,4-thiazolidinedione Testosterone cypionate may increase the hypoglycemic activities of 2,4-thiazolidinedione.
Teneligliptin Testosterone cypionate may increase the hypoglycemic activities of Teneligliptin.
Omarigliptin Testosterone cypionate may increase the hypoglycemic activities of Omarigliptin.
Carmegliptin Testosterone cypionate may increase the hypoglycemic activities of Carmegliptin.
Gemigliptin Testosterone cypionate may increase the hypoglycemic activities of Gemigliptin.
Anagliptin Testosterone cypionate may increase the hypoglycemic activities of Anagliptin.
Evogliptin Testosterone cypionate may increase the hypoglycemic activities of Evogliptin.
Sotagliflozin Sotagliflozin may decrease the excretion rate of Testosterone cypionate which could result in a higher serum level.
Remogliflozin etabonate Testosterone cypionate may increase the hypoglycemic activities of Remogliflozin etabonate.
Carbutamide Testosterone cypionate may increase the hypoglycemic activities of Carbutamide.
Guar gum Testosterone cypionate may increase the hypoglycemic activities of Guar gum.
Metahexamide Testosterone cypionate may increase the hypoglycemic activities of Metahexamide.
Semaglutide Testosterone cypionate may increase the hypoglycemic activities of Semaglutide.
Taspoglutide Testosterone cypionate may increase the hypoglycemic activities of Taspoglutide.
Englitazone Testosterone cypionate may increase the hypoglycemic activities of Englitazone.
Tirzepatide Testosterone cypionate may increase the hypoglycemic activities of Tirzepatide.
Gastric inhibitory polypeptide Testosterone cypionate may increase the hypoglycemic activities of Gastric inhibitory polypeptide.
Bromocriptine Testosterone cypionate may increase the hypoglycemic activities of Bromocriptine.
Empagliflozin Testosterone cypionate may increase the hypoglycemic activities of Empagliflozin.
Acarbose Testosterone cypionate may increase the hypoglycemic activities of Acarbose.
Fluvoxamine The metabolism of Testosterone cypionate can be decreased when combined with Fluvoxamine.
Fluoxetine The metabolism of Testosterone cypionate can be decreased when combined with Fluoxetine.
Nabilone The metabolism of Testosterone cypionate can be decreased when combined with Nabilone.
Felbamate The metabolism of Testosterone cypionate can be decreased when combined with Felbamate.
Sulfinpyrazone The metabolism of Testosterone cypionate can be decreased when combined with Sulfinpyrazone.
Iproniazid The metabolism of Testosterone cypionate can be decreased when combined with Iproniazid.
Medical Cannabis The metabolism of Testosterone cypionate can be decreased when combined with Medical Cannabis.
Troglitazone The metabolism of Testosterone cypionate can be decreased when combined with Troglitazone.
Imatinib The metabolism of Testosterone cypionate can be decreased when combined with Imatinib.
Abiraterone The metabolism of Testosterone cypionate can be decreased when combined with Abiraterone.

Target Protein

Androgen receptor AR
Estrogen receptor ESR1
Mineralocorticoid receptor NR3C2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11176375
    Freeman ER, Bloom DA, McGuire EJ: A brief history of testosterone. J Urol. 2001 Feb;165(2):371-3.
  • PMID: 7817189
    Hoberman JM, Yesalis CE: The history of synthetic testosterone. Sci Am. 1995 Feb;272(2):76-81.
  • PMID: 2333732
    Weinbauer GF, Jackwerth B, Yoon YD, Behre HM, Yeung CH, Nieschlag E: Pharmacokinetics and pharmacodynamics of testosterone enanthate and dihydrotestosterone enanthate in non-human primates. Acta Endocrinol (Copenh). 1990 Apr;122(4):432-42.
  • PMID: 28078214
    Shoskes JJ, Wilson MK, Spinner ML: Pharmacology of testosterone replacement therapy preparations. Transl Androl Urol. 2016 Dec;5(6):834-843. doi: 10.21037/tau.2016.07.10.

Contoh Produk & Brand

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  • Depo-Testosterone
    Injection, solution • 200 mg/1mL • Intramuscular • US • Generic • Approved
  • Depo-Testosterone
    Injection, solution • 200 mg/1mL • Intramuscular • US • Generic • Approved
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    Injection, solution • 200 mg/1mL • Intramuscular • US • Generic • Approved
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