Peringatan Keamanan

Data regarding an overdose with a topical testosterone product is not readily available.L8983,L8935,L8938,L8986,L8989,L8992,L8995 In the case of overdose with an injectable product, patients may present with a cerebrovascular event.L8983,L8935,L8938,L8986,L8989,L8992,L8995 Treat overdoses by stopping testosterone products, washing off any topical products with soap and water, and initiating symptomatic and supportive treatments.L8983,L8935,L8938,L8986,L8989,L8992,L8995

Testosterone

DB00624

small molecule approved investigational

Deskripsi

Testosterone is a steroid sex hormone indicated to treat primary hypogonadism and hypogonadotropic hypogonadism.L8983,L8935,L8938,L8986,L8989,L8992,L8995 Testosterone antagonizes the androgen receptor to induce gene expression that causes the growth and development of masculine sex organs and secondary sexual characteristics.A187114,L8983,L8935,L8938,L8986,L8989,L8992,L8995

Testosterone was isolated from samples and also synthesized in 1935.A186943

Struktur Molekul 2D

Berat 288.4244
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 is highly variable, ranging from 10-100 minutes.[L8983,L8935,L8938,L8986,L8989,L8992,L8995]
Volume Distribusi The volume of distribution of testosterone in elderly men is 80.36±24.51L.[A187033]
Klirens (Clearance) The mean metabolic clearance in middle aged men is 812±64L/day.[A187108]

Absorpsi

A single 100mg topical dose of testosterone has an AUC of 10425±5521ng\*h/dL and a Cmax of 573±284ng/dL.L8983 Testosterone is approximately 10% bioavailable topically.L8983,L8938,L8992

Metabolisme

Testosterone is metabolized to 17-keto steroids through two different pathways. The major active metabolites are estradiol and dihydrotestosterone (DHT).L8983,L8935,L8938,L8986,L8989,L8992,L8995 Testosterone can be hydroxylated at a number of positions by CYP3A4, CYP2B6, CYP2C9, and CYP2C19;A187006,A15135 glucuronidated by UGT2B17;A187090,A187099 sulfated;A187099 converted to estradiol by aromatase;A187087 converted to dihydrotestosterone (DHT) by 5?-reductase;A187009 metabolized to androstenedione by CYP3A4, CYP2C9, and CYP2C19;A187006 or converted to DHT glucuronide.A187102 Androstenedione undergoes metabolism by aromatase to form estrone,A187087 which undergoes a reversible reaction to form estradiol.A187102 Androstenedione can also be converted to 5?-androstanedioneA187009 by 5?-reductase,A187084 which can be further metabolized to 5?-androsterone.A187009 DHT can be glucuronidatedA187102 or sulfated, or metabolized to 5?-androstanediol,A187009 androstane-3?,17?-diol, or androstane-3?,17?-diol.A187087 DHT can also be reversibly converted to 5?-androstanedione.A187009

Rute Eliminasi

90% of an intramuscular dose is eliminated in urine, mainly as glucuronide and sulfate conjugates.L8983,L8935,L8938,L8986,L8989,L8992,L8995 6% is eliminated in feces, mostly as unconjugated metabolites.L8983,L8935,L8938,L8986,L8989,L8992,L8995

Interaksi Obat

1493 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Testosterone.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Testosterone.
Dabrafenib The serum concentration of Testosterone can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Testosterone can be increased when it is combined with Luliconazole.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Testosterone.
Perampanel The metabolism of Perampanel can be increased when combined with Testosterone.
Prasterone The serum concentration of Testosterone can be increased when it is combined with Prasterone.
Warfarin The metabolism of Warfarin can be increased when combined with Testosterone.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Testosterone.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Testosterone.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Testosterone.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Testosterone.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Testosterone.
Lumacaftor The serum concentration of Testosterone can be decreased when it is combined with Lumacaftor.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Testosterone.
Cyclosporine The risk or severity of liver damage can be increased when Testosterone is combined with Cyclosporine.
Insulin human Testosterone may increase the hypoglycemic activities of Insulin human.
Insulin lispro Testosterone may increase the hypoglycemic activities of Insulin lispro.
Insulin glargine Testosterone may increase the hypoglycemic activities of Insulin glargine.
Insulin pork Testosterone may increase the hypoglycemic activities of Insulin pork.
Glimepiride Testosterone may increase the hypoglycemic activities of Glimepiride.
Acetohexamide Testosterone may increase the hypoglycemic activities of Acetohexamide.
Miglitol Testosterone may increase the hypoglycemic activities of Miglitol.
Phenformin Testosterone may increase the hypoglycemic activities of Phenformin.
Gliquidone Testosterone may increase the hypoglycemic activities of Gliquidone.
Mitiglinide Testosterone may increase the hypoglycemic activities of Mitiglinide.
Exenatide Testosterone may increase the hypoglycemic activities of Exenatide.
Mecasermin Testosterone may increase the hypoglycemic activities of Mecasermin.
Pramlintide Testosterone may increase the hypoglycemic activities of Pramlintide.
Glisoxepide Testosterone may increase the hypoglycemic activities of Glisoxepide.
Insulin aspart Testosterone may increase the hypoglycemic activities of Insulin aspart.
Insulin detemir Testosterone may increase the hypoglycemic activities of Insulin detemir.
Insulin glulisine Testosterone may increase the hypoglycemic activities of Insulin glulisine.
Glymidine Testosterone may increase the hypoglycemic activities of Glymidine.
AICA ribonucleotide Testosterone may increase the hypoglycemic activities of AICA ribonucleotide.
Buformin Testosterone may increase the hypoglycemic activities of Buformin.
Vildagliptin Testosterone may increase the hypoglycemic activities of Vildagliptin.
Voglibose Testosterone may increase the hypoglycemic activities of Voglibose.
NN344 Testosterone may increase the hypoglycemic activities of NN344.
AMG-222 Testosterone may increase the hypoglycemic activities of AMG-222.
Bisegliptin Testosterone may increase the hypoglycemic activities of Bisegliptin.
Liraglutide Testosterone may increase the hypoglycemic activities of Liraglutide.
Gosogliptin Testosterone may increase the hypoglycemic activities of Gosogliptin.
Glibornuride Testosterone may increase the hypoglycemic activities of Glibornuride.
Benfluorex Testosterone may increase the hypoglycemic activities of Benfluorex.
Albiglutide Testosterone may increase the hypoglycemic activities of Albiglutide.
Dulaglutide Testosterone may increase the hypoglycemic activities of Dulaglutide.
Insulin beef Testosterone may increase the hypoglycemic activities of Insulin beef.
Insulin degludec Testosterone may increase the hypoglycemic activities of Insulin degludec.
Insulin peglispro Testosterone may increase the hypoglycemic activities of Insulin peglispro.
Insulin tregopil Testosterone may increase the hypoglycemic activities of Insulin tregopil.
Ipragliflozin Testosterone may increase the hypoglycemic activities of Ipragliflozin.
Dutogliptin Testosterone may increase the hypoglycemic activities of Dutogliptin.
Allicin Testosterone may increase the hypoglycemic activities of Allicin.
Tofogliflozin Testosterone may increase the hypoglycemic activities of Tofogliflozin.
2,4-thiazolidinedione Testosterone may increase the hypoglycemic activities of 2,4-thiazolidinedione.
Teneligliptin Testosterone may increase the hypoglycemic activities of Teneligliptin.
Omarigliptin Testosterone may increase the hypoglycemic activities of Omarigliptin.
Carmegliptin Testosterone may increase the hypoglycemic activities of Carmegliptin.
Gemigliptin Testosterone may increase the hypoglycemic activities of Gemigliptin.
Anagliptin Testosterone may increase the hypoglycemic activities of Anagliptin.
Evogliptin Testosterone may increase the hypoglycemic activities of Evogliptin.
Sotagliflozin Sotagliflozin may decrease the excretion rate of Testosterone which could result in a higher serum level.
Remogliflozin etabonate Testosterone may increase the hypoglycemic activities of Remogliflozin etabonate.
Carbutamide Testosterone may increase the hypoglycemic activities of Carbutamide.
Guar gum Testosterone may increase the hypoglycemic activities of Guar gum.
Metahexamide Testosterone may increase the hypoglycemic activities of Metahexamide.
Semaglutide Testosterone may increase the hypoglycemic activities of Semaglutide.
Taspoglutide Testosterone may increase the hypoglycemic activities of Taspoglutide.
Englitazone Testosterone may increase the hypoglycemic activities of Englitazone.
Tirzepatide Testosterone may increase the hypoglycemic activities of Tirzepatide.
Gastric inhibitory polypeptide Testosterone may increase the hypoglycemic activities of Gastric inhibitory polypeptide.
Repaglinide Testosterone may increase the hypoglycemic activities of Repaglinide.
Netoglitazone Testosterone may increase the hypoglycemic activities of Netoglitazone.
Rivoglitazone Testosterone may increase the hypoglycemic activities of Rivoglitazone.
Ciglitazone Testosterone may increase the hypoglycemic activities of Ciglitazone.
Balaglitazone Testosterone may increase the hypoglycemic activities of Balaglitazone.
Pioglitazone Testosterone may increase the hypoglycemic activities of Pioglitazone.
Bromocriptine Testosterone may increase the hypoglycemic activities of Bromocriptine.
Empagliflozin Testosterone may increase the hypoglycemic activities of Empagliflozin.
Acarbose Testosterone may increase the hypoglycemic activities of Acarbose.
Ticlopidine The metabolism of Testosterone can be decreased when combined with Ticlopidine.
Lansoprazole The metabolism of Testosterone can be decreased when combined with Lansoprazole.
Fluvoxamine The metabolism of Testosterone can be decreased when combined with Fluvoxamine.
Fluoxetine The metabolism of Testosterone can be decreased when combined with Fluoxetine.
Zafirlukast The metabolism of Testosterone can be decreased when combined with Zafirlukast.
Chloramphenicol The metabolism of Testosterone can be decreased when combined with Chloramphenicol.
Isoniazid The metabolism of Testosterone can be decreased when combined with Isoniazid.
Imipramine The metabolism of Testosterone can be decreased when combined with Imipramine.
Eslicarbazepine acetate The metabolism of Testosterone can be decreased when combined with Eslicarbazepine acetate.
Nabilone The metabolism of Testosterone can be decreased when combined with Nabilone.
Felbamate The metabolism of Testosterone can be decreased when combined with Felbamate.
Sulfinpyrazone The metabolism of Testosterone can be decreased when combined with Sulfinpyrazone.
Iproniazid The metabolism of Testosterone can be decreased when combined with Iproniazid.
Medical Cannabis The metabolism of Testosterone can be decreased when combined with Medical Cannabis.
Imatinib The metabolism of Testosterone can be decreased when combined with Imatinib.
Fluconazole The metabolism of Testosterone can be decreased when combined with Fluconazole.
Floxuridine The metabolism of Testosterone can be decreased when combined with Floxuridine.
Nicardipine The metabolism of Testosterone can be decreased when combined with Nicardipine.
Miconazole The metabolism of Testosterone can be decreased when combined with Miconazole.

Target Protein

Androgen receptor AR
Estrogen receptor ESR1
Mineralocorticoid receptor NR3C2

Referensi & Sumber

Synthesis reference: Merle G. Wovcha, Frederick J. Antosz, John M. Beaton, Alfred B. Garcia, Leo A. Kominek, "Process for preparing 9.alpha.-OH testosterone." U.S. Patent US4221868, issued November, 1977.
Artikel (PubMed)
  • PMID: 30959485
    Nieschlag E, Nieschlag S: ENDOCRINE HISTORY: The history of discovery, synthesis and development of testosterone for clinical use. Eur J Endocrinol. 2019 Jun 1;180(6):R201-R212. doi: 10.1530/EJE-19-0071.
  • PMID: 9753206
    White CM, Ferraro-Borgida MJ, Moyna NM, McGill CC, Ahlberg AW, Thompson PD, Chow MS, Heller GV: The pharmacokinetics of intravenous testosterone in elderly men with coronary artery disease. J Clin Pharmacol. 1998 Sep;38(9):792-7.
  • PMID: 15181080
    Wang C, Catlin DH, Starcevic B, Leung A, DiStefano E, Lucas G, Hull L, Swerdloff RS: Testosterone metabolic clearance and production rates determined by stable isotope dilution/tandem mass spectrometry in normal men: influence of ethnicity and age. J Clin Endocrinol Metab. 2004 Jun;89(6):2936-41. doi: 10.1210/jc.2003-031802.
  • PMID: 24024843
    Handelsman DJ: Mechanisms of action of testosterone--unraveling a Gordian knot. N Engl J Med. 2013 Sep 12;369(11):1058-9. doi: 10.1056/NEJMe1305307.
  • PMID: 24837363
    Ferraldeschi R, Welti J, Luo J, Attard G, de Bono JS: Targeting the androgen receptor pathway in castration-resistant prostate cancer: progresses and prospects. Oncogene. 2015 Apr 2;34(14):1745-57. doi: 10.1038/onc.2014.115. Epub 2014 May 19.
  • PMID: 15764715
    Choi MH, Skipper PL, Wishnok JS, Tannenbaum SR: Characterization of testosterone 11 beta-hydroxylation catalyzed by human liver microsomal cytochromes P450. Drug Metab Dispos. 2005 Jun;33(6):714-8. doi: 10.1124/dmd.104.003327. Epub 2005 Mar 11.
  • PMID: 128323
    Price VH: Testosterone metabolism in the skin. A review of its function in androgenetic alopecia, acne vulgaris, and idiopathic hirsutism including recent studies with antiandrogens. Arch Dermatol. 1975 Nov;111(11):1496-1502. doi: 10.1001/archderm.111.11.1496.
  • PMID: 9732386
    Ekins S, Vandenbranden M, Ring BJ, Gillespie JS, Yang TJ, Gelboin HV, Wrighton SA: Further characterization of the expression in liver and catalytic activity of CYP2B6. J Pharmacol Exp Ther. 1998 Sep;286(3):1253-9.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 125 • International brands: 20
Produk
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International Brands
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  • Nebido — Bayer
  • Sustanon — Organon
  • Synandrol F
  • Testamone 100

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