Peringatan Keamanan

Testosterone enanthate has been tested in preclinical carcinogenesis trials. In this studies, it is suggested that the exposure to this drug may increase the susceptibility to hematoma as well as the number of tumors and decrease the degree of differentiation of chemically induced carcinomas of the liver.FDA label

Testosterone enanthate is not indicated for use in females and is contraindicated in pregnant women. Testosterone is teratogenic and may cause fetal harm when administered to a pregnant woman based on data from animal studies and its mechanism of action. F1941

During treatment with large doses of exogenous androgens, including testosterone enanthate, spermatogenesis may be suppressed through feedback inhibition of the hypothalamic-pituitary-testicular axis F1941. Reduced fertility is observed in some men taking testosterone replacement therapy and the impact on fertility may be irreversible F1941.

Safety and effectiveness of testosterone enanthate in pediatric patients less than 18 years old have not been established F1941. Improper use may result in the acceleration of bone age and premature closure of epiphyses F1941.

Geriatric patients treated with androgens may also be at risk for worsening of signs and symptoms of Benign Prostatic Hyperplasia F1941.

Testosterone enanthate

DB13944

small molecule approved

Deskripsi

Testosterone enanthate is an esterified variant of testosterone that comes as an injectable compound with a slow-release rate. This slow release is achieved by the presence of the enanthate ester functional group attached to the testosterone molecule.A31615 This testosterone derivative was first approved on December 24, 1953.L8941

In 2017, about 6.5 million retail prescriptions for testosterone therapy were filled L4659. The majority of the prescriptions written were for injectable (66%) and topical (32%) testosterone products. As recent as 1 October 2018, the US FDA approved Antares Pharma Inc.'s Xyosted - a subcutaneous testosterone enanthate product for once-weekly, at-home self-administration with an easy-to-use, single dose, disposable autoinjector L4659. As the first subcutaneous autoinjector product designed for testosterone replacement therapy, this innovative formulation removes transfer concerns commonly associated with testosterone gels and potentially reduces the need for in-office/in-clinic injection procedures that may inconvenience patients with frequent visits to the clinic L4659.

Struktur Molekul 2D

Berat 400.594
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Testosterone enanthate presents a long half-life in the range of 7-9 days.[A31616]
Volume Distribusi The volume of distribution following intravenous administration of testosterone is of approximately 1 L/kg.[L1155]
Klirens (Clearance) -

Absorpsi

The pharmacokinetic profile of testosterone enanthate was studied in a regime of multiple dosing and the testosterone level was reported to present a Cmax above 1200 ng/dl after 24 hours of the last dose. The concentration decreased sequentially until it reached 600 ng/dl after one week. The pharmacokinetic profile of testosterone enanthate presented differences depending on the administered dose in which the tmax was shifted to a range of 36-48 hours. The plasma testosterone level plateaued below the therapeutic range after 3-4 weeks. This reports showed that the different formulation of testosterone enanthate and testosterone cypionate generates a different profile and thus, they are not therapeutically equivalent.A31613

Metabolisme

To start its activity, testosterone enanthate has to be processed by enzymes in the bloodstream. These enzymes will catalyze the molecule at the ester location of the moiety. Once processed in this manner, the testosterone enanthate molecule is metabolized to various 17-keto steroids through two different pathways. Subsequently, the major active metabolites are estradiol and DHTd. 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, F1941

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, F1941 The inactivation of testosterone occurs primarily in the liver.F1941

Interaksi Obat

1550 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Testosterone enanthate.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Testosterone enanthate.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Testosterone enanthate.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Testosterone enanthate.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Testosterone enanthate.
Colchicine The metabolism of Colchicine can be decreased when combined with Testosterone enanthate.
Fentanyl Fentanyl may decrease the excretion rate of Testosterone enanthate which could result in a higher serum level.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Testosterone enanthate.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Testosterone enanthate.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Testosterone enanthate.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Testosterone enanthate.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Testosterone enanthate.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Testosterone enanthate.
Exenatide Exenatide can cause a decrease in the absorption of Testosterone enanthate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Thalidomide Testosterone enanthate may increase the thrombogenic activities of Thalidomide.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Testosterone enanthate.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Testosterone enanthate.
Mifepristone The serum concentration of Testosterone enanthate can be increased when it is combined with Mifepristone.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Testosterone enanthate.
Perampanel The metabolism of Perampanel can be increased when combined with Testosterone enanthate.
Prasterone The serum concentration of Testosterone enanthate can be increased when it is combined with Prasterone.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Testosterone enanthate.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Testosterone enanthate.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Testosterone enanthate.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Testosterone enanthate.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Testosterone enanthate.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Testosterone enanthate.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Testosterone enanthate.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Testosterone enanthate.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Testosterone enanthate.
Tranexamic acid Testosterone enanthate may increase the thrombogenic activities of Tranexamic acid.
Clobazam The serum concentration of Testosterone enanthate can be decreased when it is combined with Clobazam.
Griseofulvin The metabolism of Testosterone enanthate can be increased when combined with Griseofulvin.
Clobetasol propionate The serum concentration of Clobetasol propionate can be increased when it is combined with Testosterone enanthate.
Fluocinonide The serum concentration of Fluocinonide can be increased when it is combined with Testosterone enanthate.
Hydrocortisone butyrate The serum concentration of Hydrocortisone butyrate can be increased when it is combined with Testosterone enanthate.
Desoximetasone The serum concentration of Desoximetasone can be increased when it is combined with Testosterone enanthate.
Mometasone The serum concentration of Mometasone can be increased when it is combined with Testosterone enanthate.
Fluocortolone The serum concentration of Fluocortolone can be increased when it is combined with Testosterone enanthate.
Prednisolone acetate The serum concentration of Prednisolone acetate can be increased when it is combined with Testosterone enanthate.
Fluorometholone The serum concentration of Fluorometholone can be increased when it is combined with Testosterone enanthate.
Difluocortolone The serum concentration of Difluocortolone can be increased when it is combined with Testosterone enanthate.
Flumethasone The serum concentration of Flumethasone can be increased when it is combined with Testosterone enanthate.
Methylprednisolone aceponate The serum concentration of Methylprednisolone aceponate can be increased when it is combined with Testosterone enanthate.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Testosterone enanthate.
Bosentan The serum concentration of Testosterone enanthate can be decreased when it is combined with Bosentan.
Carbamazepine The serum concentration of Testosterone enanthate can be decreased when it is combined with Carbamazepine.
Phenoxymethylpenicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Phenoxymethylpenicillin.
Carbenicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Carbenicillin.
Hetacillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Hetacillin.
Benzylpenicilloyl polylysine The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Benzylpenicilloyl polylysine.
Mezlocillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Mezlocillin.
Cyclacillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Cyclacillin.
Benzylpenicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Benzylpenicillin.
Azlocillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Azlocillin.
Cloxacillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Cloxacillin.
Amdinocillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Amdinocillin.
Bacampicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Bacampicillin.
Meticillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Meticillin.
Pivampicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Pivampicillin.
Pivmecillinam The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Pivmecillinam.
Ticarcillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Ticarcillin.
Azidocillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Azidocillin.
Carindacillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Carindacillin.
Sultamicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Sultamicillin.
Temocillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Temocillin.
Epicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Epicillin.
Pheneticillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Pheneticillin.
Carfecillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Carfecillin.
Propicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Propicillin.
Clometocillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Clometocillin.
Sulbenicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Sulbenicillin.
Penamecillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Penamecillin.
Talampicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Talampicillin.
Aspoxicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Aspoxicillin.
Metampicillin The therapeutic efficacy of Testosterone enanthate can be decreased when used in combination with Metampicillin.
Cyclosporine The risk or severity of liver damage can be increased when Testosterone enanthate is combined with Cyclosporine.
Mycophenolate mofetil The serum concentration of Testosterone enanthate can be decreased when it is combined with Mycophenolate mofetil.
Mycophenolic acid The serum concentration of Testosterone enanthate can be decreased when it is combined with Mycophenolic acid.
Nafcillin The metabolism of Testosterone enanthate can be increased when combined with Nafcillin.
Bexarotene The metabolism of Testosterone enanthate can be increased when combined with Bexarotene.
Modafinil The metabolism of Testosterone enanthate can be increased when combined with Modafinil.
Etravirine The metabolism of Testosterone enanthate can be increased when combined with Etravirine.
Avasimibe The metabolism of Testosterone enanthate can be increased when combined with Avasimibe.
Echinacea The metabolism of Testosterone enanthate can be increased when combined with Echinacea.
Dexamethasone acetate The serum concentration of Dexamethasone acetate can be increased when it is combined with Testosterone enanthate.
Flibanserin The risk or severity of adverse effects can be increased when Testosterone enanthate is combined with Flibanserin.
Telaprevir The serum concentration of Testosterone enanthate can be decreased when it is combined with Telaprevir.
Boceprevir The serum concentration of Testosterone enanthate can be increased when it is combined with Boceprevir.
Cobicistat The serum concentration of Testosterone enanthate can be decreased when it is combined with Cobicistat.
Elvitegravir The serum concentration of Testosterone enanthate can be decreased when it is combined with Elvitegravir.
Insulin human Testosterone enanthate may increase the hypoglycemic activities of Insulin human.
Insulin lispro Testosterone enanthate may increase the hypoglycemic activities of Insulin lispro.
Insulin glargine Testosterone enanthate may increase the hypoglycemic activities of Insulin glargine.
Insulin pork Testosterone enanthate may increase the hypoglycemic activities of Insulin pork.
Miglitol Testosterone enanthate may increase the hypoglycemic activities of Miglitol.
Phenformin Testosterone enanthate may increase the hypoglycemic activities of Phenformin.
Mitiglinide Testosterone enanthate may increase the hypoglycemic activities of Mitiglinide.
Mecasermin Testosterone enanthate may increase the hypoglycemic activities of Mecasermin.
Pramlintide Testosterone enanthate may increase the hypoglycemic activities of Pramlintide.

Target Protein

Androgen receptor AR
Estrogen receptor ESR1
Mineralocorticoid receptor NR3C2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 7817189
    Hoberman JM, Yesalis CE: The history of synthetic testosterone. Sci Am. 1995 Feb;272(2):76-81.
  • PMID: 24435052
    Nieschlag E, Nieschlag S: Testosterone deficiency: a historical perspective. Asian J Androl. 2014 Mar-Apr;16(2):161-8. doi: 10.4103/1008-682X.122358.
  • PMID: 26797061
    Kaminetsky J, Jaffe JS, Swerdloff RS: Pharmacokinetic Profile of Subcutaneous Testosterone Enanthate Delivered via a Novel, Prefilled Single-Use Autoinjector: A Phase II Study. Sex Med. 2015 Sep 17;3(4):269-79. doi: 10.1002/sm2.80. eCollection 2015 Dec.
  • 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.
  • 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: 18046048
    Amory JK, Kalhorn TF, Page ST: Pharmacokinetics and pharmacodynamics of oral testosterone enanthate plus dutasteride for 4 weeks in normal men: implications for male hormonal contraception. J Androl. 2008 May-Jun;29(3):260-71. doi: 10.2164/jandrol.107.004226. Epub 2007 Nov 28.

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