Peringatan Keamanan

Symptoms of overdose are expected to be similar to typical adverse effects which may include headache, dyspepsia, back pain, myalgia, nasopharyngitis, and dizziness.L39095, L39100 Standard supportive care is recommended. Hemodialysis is not expected to contribute significantly to tadalafil clearance.

Tadalafil

DB00820

small molecule approved investigational

Deskripsi

Tadalafil is a selective phosphodiesterase-5 inhibitor that is used in the treatment of erectile dysfunction (ED), pulmonary arterial hypertension (PAH), and benign prostatic hypertrophy.L39100, L39105 It was first approved in 2003 by the FDA for use in ED and later in 2009 for PAH. In contrast to other PDE5 inhibitors like sildenafil, tadalafil has greater selectivity for PDE5 and a longer half-life which has made it a more suitable option for chronic once-daily dosing in the treatment of PAH.A242287

Struktur Molekul 2D

Berat 389.404
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean half-life of elimination of tadalafil is 15-17.5h in healthy adults.[A242270, L39095, L39100] The mean half-life of elimination in adults with PAH is reported as 35h.[L39100]
Volume Distribusi Tadalafil has a mean apparent volume of distribution of 63L in healthy adults.[A242270, L39095] The mean apparent volume of distribution is reported as 77L in adults with PAH.[L39100]
Klirens (Clearance) The mean apparent oral clearance of tadalafil is 2.5-3.4L/h in healthy adults.[A242270, L39095, L39100] The mean apparent oral clearance in adults with PAH is reported as 3.5L/h

Absorpsi

Tadalafil has a tmax of 0.5-6h with a median of 2h in healthy adults. A242270, L39095 The tmax in adults with PAH is reported as 2-8h with a median of 4h.L39100 There does not appear to be a significant effect on absorption when tadalafil is taken with food.A242270

Metabolisme

Tadalafil undergoes hepatic metabolism via CYP3A4 to a catechol metabolite.A242270, A242387, L39095, L39100 This catechol metabolite undergoes subsequent methylation and glucuronidation with the methyl-glucuronide metabolite becoming the primary metabolite in circulation. None of the known metabolites are considered to be active.

Rute Eliminasi

Tadalafil is primarily eliminated via hepatic metabolism.A242270, L39095, L39100 These metabolites are mainly excreted in the feces (61%) and to a lesser extent in the urine (36%)

Interaksi Makanan

3 Data
  • 1. Avoid excessive or chronic alcohol consumption. Ingesting excess amounts of alcohol (more than four drinks in a short time) may potentiate the hypotension and dizziness caused by tadalafil.
  • 2. Avoid grapefruit products. Tadalafil is metabolized by CYP3A4, and grapefruit products are CYP3A4 inhibitors; therefore, coadministration may increase serum levels of tadalafil and result in increased hypotension.
  • 3. Take with or without food.

Interaksi Obat

1220 Data
Alfuzosin Alfuzosin may increase the hypotensive activities of Tadalafil.
Amifostine Tadalafil may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Tadalafil.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Tadalafil.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Tadalafil.
Obinutuzumab Tadalafil may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Tadalafil.
Rituximab Tadalafil may increase the hypotensive activities of Rituximab.
Midodrine Midodrine may decrease the antihypertensive activities of Tadalafil.
Isoetharine Isoetharine may decrease the antihypertensive activities of Tadalafil.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Tadalafil.
Protriptyline Protriptyline may decrease the antihypertensive activities of Tadalafil.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Tadalafil.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Tadalafil.
Doxapram Doxapram may decrease the antihypertensive activities of Tadalafil.
Atropine Atropine may decrease the antihypertensive activities of Tadalafil.
Metaraminol Metaraminol may decrease the antihypertensive activities of Tadalafil.
Methoxamine Methoxamine may decrease the antihypertensive activities of Tadalafil.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Tadalafil.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Tadalafil.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Tadalafil.
Ritodrine Ritodrine may decrease the antihypertensive activities of Tadalafil.
Bitolterol Bitolterol may decrease the antihypertensive activities of Tadalafil.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Tadalafil.
Naratriptan Naratriptan may decrease the antihypertensive activities of Tadalafil.
Formoterol Formoterol may decrease the antihypertensive activities of Tadalafil.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Tadalafil.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Tadalafil.
Arbutamine Arbutamine may decrease the antihypertensive activities of Tadalafil.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Tadalafil.
Fenoterol Fenoterol may decrease the antihypertensive activities of Tadalafil.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Tadalafil.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Tadalafil.
Ephedrine Ephedrine may decrease the antihypertensive activities of Tadalafil.
Mephentermine Mephentermine may decrease the antihypertensive activities of Tadalafil.
Procaterol Procaterol may decrease the antihypertensive activities of Tadalafil.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Tadalafil.
Bambuterol Bambuterol may decrease the antihypertensive activities of Tadalafil.
MMDA MMDA may decrease the antihypertensive activities of Tadalafil.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Tadalafil.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Tadalafil.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Tadalafil.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Tadalafil.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Tadalafil.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Tadalafil.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Tadalafil.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Tadalafil.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Tadalafil.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Tadalafil.
Amineptine Amineptine may decrease the antihypertensive activities of Tadalafil.
Amibegron Amibegron may decrease the antihypertensive activities of Tadalafil.
Naluzotan Naluzotan may decrease the antihypertensive activities of Tadalafil.
Solabegron Solabegron may decrease the antihypertensive activities of Tadalafil.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Tadalafil.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Tadalafil.
Xylometazoline Xylometazoline may decrease the antihypertensive activities of Tadalafil.
Isometheptene Isometheptene may decrease the antihypertensive activities of Tadalafil.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Tadalafil.
Naphazoline Naphazoline may decrease the antihypertensive activities of Tadalafil.
Saralasin Saralasin may decrease the antihypertensive activities of Tadalafil.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Tadalafil.
Cinitapride Cinitapride may decrease the antihypertensive activities of Tadalafil.
Tyramine Tyramine may decrease the antihypertensive activities of Tadalafil.
Adrafinil Adrafinil may decrease the antihypertensive activities of Tadalafil.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Tadalafil.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Tadalafil.
Etilefrine Etilefrine may decrease the antihypertensive activities of Tadalafil.
Butriptyline Butriptyline may decrease the antihypertensive activities of Tadalafil.
Olodaterol Olodaterol may decrease the antihypertensive activities of Tadalafil.
Dosulepin Dosulepin may decrease the antihypertensive activities of Tadalafil.
Cirazoline Cirazoline may decrease the antihypertensive activities of Tadalafil.
Synephrine Synephrine may decrease the antihypertensive activities of Tadalafil.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Tadalafil.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Tadalafil.
Racepinephrine Racepinephrine may decrease the antihypertensive activities of Tadalafil.
Amitraz Amitraz may decrease the antihypertensive activities of Tadalafil.
Medetomidine Medetomidine may decrease the antihypertensive activities of Tadalafil.
Xylazine Xylazine may decrease the antihypertensive activities of Tadalafil.
Atipamezole Atipamezole may decrease the antihypertensive activities of Tadalafil.
Ractopamine Ractopamine may decrease the antihypertensive activities of Tadalafil.
Romifidine Romifidine may decrease the antihypertensive activities of Tadalafil.
Detomidine Detomidine may decrease the antihypertensive activities of Tadalafil.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Tadalafil.
Anisodamine Anisodamine may decrease the antihypertensive activities of Tadalafil.
PF-00610355 PF-00610355 may decrease the antihypertensive activities of Tadalafil.
Ritobegron Ritobegron may decrease the antihypertensive activities of Tadalafil.
Abediterol Abediterol may decrease the antihypertensive activities of Tadalafil.
Tulobuterol Tulobuterol may decrease the antihypertensive activities of Tadalafil.
Dopexamine Dopexamine may decrease the antihypertensive activities of Tadalafil.
Piclozotan Piclozotan may decrease the antihypertensive activities of Tadalafil.
Idazoxan Idazoxan may decrease the antihypertensive activities of Tadalafil.
Higenamine Higenamine may decrease the antihypertensive activities of Tadalafil.
Reproterol Reproterol may decrease the antihypertensive activities of Tadalafil.
Theodrenaline Theodrenaline may decrease the antihypertensive activities of Tadalafil.
Opipramol Opipramol may decrease the antihypertensive activities of Tadalafil.
Tramazoline Tramazoline may decrease the antihypertensive activities of Tadalafil.
Mephedrone Mephedrone may decrease the antihypertensive activities of Tadalafil.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Tadalafil.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Tadalafil.
Quinupramine Quinupramine may decrease the antihypertensive activities of Tadalafil.

Target Protein

cGMP-specific 3',5'-cyclic phosphodiesterase PDE5A
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A PDE11A
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma PDE6G

Referensi & Sumber

Synthesis reference: Ben-Zion Dolitzky, Dov Diller, "Preparation of tadalafil intermediates." U.S. Patent US20060276652, issued December 07, 2006.
Artikel (PubMed)
  • PMID: 16487221
    Forgue ST, Patterson BE, Bedding AW, Payne CD, Phillips DL, Wrishko RE, Mitchell MI: Tadalafil pharmacokinetics in healthy subjects. Br J Clin Pharmacol. 2006 Mar;61(3):280-8. doi: 10.1111/j.1365-2125.2005.02553.x.
  • PMID: 29667180
    Andersson KE: PDE5 inhibitors - pharmacology and clinical applications 20 years after sildenafil discovery. Br J Pharmacol. 2018 Jul;175(13):2554-2565. doi: 10.1111/bph.14205. Epub 2018 Apr 25.
  • PMID: 21762988
    Arif SA, Poon H: Tadalafil: a long-acting phosphodiesterase-5 inhibitor for the treatment of pulmonary arterial hypertension. Clin Ther. 2011 Aug;33(8):993-1004. doi: 10.1016/j.clinthera.2011.06.008. Epub 2011 Jul 16.
  • PMID: 30901259
    Monica FZ, De Nucci G: Tadalafil for the treatment of benign prostatic hyperplasia. Expert Opin Pharmacother. 2019 Jun;20(8):929-937. doi: 10.1080/14656566.2019.1589452. Epub 2019 Mar 22.
  • PMID: 19146377
    Dalvie D, Obach RS, Kang P, Prakash C, Loi CM, Hurst S, Nedderman A, Goulet L, Smith E, Bu HZ, Smith DA: Assessment of three human in vitro systems in the generation of major human excretory and circulating metabolites. Chem Res Toxicol. 2009 Feb;22(2):357-68. doi: 10.1021/tx8004357.
  • PMID: 27188339
    Yafi FA, Jenkins L, Albersen M, Corona G, Isidori AM, Goldfarb S, Maggi M, Nelson CJ, Parish S, Salonia A, Tan R, Mulhall JP, Hellstrom WJ: Erectile dysfunction. Nat Rev Dis Primers. 2016 Feb 4;2:16003. doi: 10.1038/nrdp.2016.3.

Contoh Produk & Brand

Produk: 510 • International brands: 0
Produk
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    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
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    Tablet • 5 mg • Oral • Canada • Generic • Approved
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    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ach-tadalafil
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Act Tadalafil
    Tablet • 2.5 mg • Oral • Canada • Approved
  • Act Tadalafil
    Tablet • 5 mg • Oral • Canada • Approved
  • Act Tadalafil
    Tablet • 10 mg • Oral • Canada • Approved
  • Act Tadalafil
    Tablet • 20 mg • Oral • Canada • Approved
Menampilkan 8 dari 510 produk.

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