Peringatan Keamanan

Healthy male volunteers given a single dose of 120 mg of vardenafil experienced reversible back pain, myalgia and abnormal vision. Patients given vardenafil once daily over 4 weeks in single doses up to 80 mg and multiple doses up to 40 mg did not present serious adverse side effects. Cases of severe back pain were observed when 40 mg of vardenafil was administered twice daily; however patients did not present muscle or neurological toxicity. In cases of overdose, standard supportive measures should be taken as required. Renal dialysis is not expected to accelerate clearance as vardenafil is highly bound to plasma proteins and not significantly eliminated in the urine.L45563,L45568

No carcinogenic effects were detected in rats and mice given vardenafil daily for 24 months. Vardenafil was not mutagenic or clastogenic, and did not have an effect in fertility in male and female rats given up to 100 mg/kg/day for 28 days prior to mating in males, and for 14 days prior to mating and through day 7 of gestation in females.L45563,L45568

Vardenafil

DB00862

small molecule approved

Deskripsi

Vardenafil is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) and an oral therapy for the treatment of erectile dysfunction.L45563,L45568 During sexual stimulation, nitric oxide (NO) is released from nerve endings and endothelial cells in the corpus cavernosum, activating the enzyme guanylate cyclase and increasing the synthesis of cGMP in the smooth muscle cells of the corpus cavernosum. PDE5 inhibitors, such as vardenafil, inhibit the degradation of cGMP and allow increased blood flow into the penis, resulting in an erection.A258303,L45563,L45568. Compared to sildenafil and tadalafil, vardenafil is a more potent inhibitor of PDE5; however, its selectivity for other PDE isoforms is lower than the one detected for tadalafil.A258318

The FDA approved the use of vardenafil for the treatment of erectile dysfunction in 2003. Although other PDE5 inhibitors such as sildenafil and tadalafil have been associated with rare cases of acute liver injury, the use of vardenafil has not been linked to hepatotoxic effects.A258313 The use of vardenafil as a monotherapy for the treatment of pulmonary arterial hypertension has also been evaluated.A258308

Struktur Molekul 2D

Berat 488.603
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Vardenafil and its primary metabolite (M1) have a terminal half-life of 4-5 hours.[L45563]
Volume Distribusi Vardenafil has a steady-state volume of distribution of 208 L.[L45563]
Klirens (Clearance) Vardenafil has a total body clearance of 56 L/h.[L45563]

Absorpsi

Over the recommended dose range, vardenafil has a dose-proportional pharmacokinetics profile. In healthy male volunteers given a single oral dose of 20 mg of vardenafil, maximum plasma concentrations were reached between 30 minutes and 2 hours (median 60 minutes) after oral dosing in the fasted state, and 0.00018% of the dose was detected in semen 1.5 hours after dosing. Vardenafil has a bioavailability of approximately 15%.L45563 High-fat meals cause a Cmax reduction of 18%-50%; however, no changes were detected in AUC or Tmax.L45563,L45568

Metabolisme

Vardenafil is mainly metabolized by CYP3A4 in the liver, although CYP3A5 and CYP2C isoforms also contribute to its metabolism. The major circulating metabolite, M1 (N-desethylvardenafil), results from desethylation at the piperazine moiety of vardenafil, and has a plasma concentration of approximately 26% of that of the parent compound. M1 has a phosphodiesterase selectivity profile similar to that of vardenafil and an in vitro inhibitory potency for PDE5 28% of that of vardenafil.L45563

Rute Eliminasi

Vardenafil is excreted as metabolites mainly through feces and urine. Approximately 91-95% of administered oral dose is found in feces, while 2-6% of administered oral dose is found in urine.L45563

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Vardenafil is metabolized by CYP3A4, and grapefruit products are CYP3A4 inhibitors; therefore, coadministration may increase serum levels of vardenafil and result in increased hypotension. .
  • 2. Take with or without food. High-fat meals reduce the Cmax of vardenafil; however, there are no changes in AUC or Tmax.

Interaksi Obat

1173 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Vardenafil.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Vardenafil.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Vardenafil.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Vardenafil.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Vardenafil.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Vardenafil.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Vardenafil.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Vardenafil.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Vardenafil.
Silodosin The excretion of Silodosin can be decreased when combined with Vardenafil.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Vardenafil.
Alprostadil The risk or severity of hypotension and priapism can be increased when Vardenafil is combined with Alprostadil.
Amyl Nitrite The risk or severity of hypotension can be increased when Vardenafil is combined with Amyl Nitrite.
Dapoxetine The risk or severity of orthostatic hypotension can be increased when Dapoxetine is combined with Vardenafil.
Riociguat Vardenafil may increase the hypotensive activities of Riociguat.
Everolimus The metabolism of Vardenafil can be decreased when combined with Everolimus.
Etoposide The metabolism of Vardenafil can be decreased when combined with Etoposide.
Isavuconazole The metabolism of Vardenafil can be decreased when combined with Isavuconazole.
Aldesleukin The metabolism of Vardenafil can be decreased when combined with Aldesleukin.
Octreotide The metabolism of Vardenafil can be decreased when combined with Octreotide.
Fluvoxamine The metabolism of Vardenafil can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Vardenafil can be decreased when combined with Fluconazole.
Citalopram The metabolism of Vardenafil can be decreased when combined with Citalopram.
Nelfinavir The metabolism of Vardenafil can be decreased when combined with Nelfinavir.
Lovastatin The metabolism of Vardenafil can be decreased when combined with Lovastatin.
Cabergoline The metabolism of Vardenafil can be decreased when combined with Cabergoline.
Diethylstilbestrol The metabolism of Vardenafil can be decreased when combined with Diethylstilbestrol.
Isradipine The metabolism of Vardenafil can be decreased when combined with Isradipine.
Valproic acid The metabolism of Vardenafil can be decreased when combined with Valproic acid.
Acetaminophen The metabolism of Vardenafil can be decreased when combined with Acetaminophen.
Dihydroergotamine The metabolism of Vardenafil can be decreased when combined with Dihydroergotamine.
Methadone The metabolism of Vardenafil can be decreased when combined with Methadone.
Terfenadine The metabolism of Vardenafil can be decreased when combined with Terfenadine.
Diltiazem The metabolism of Vardenafil can be decreased when combined with Diltiazem.
Methylergometrine The metabolism of Vardenafil can be decreased when combined with Methylergometrine.
Mefloquine The metabolism of Vardenafil can be decreased when combined with Mefloquine.
Clozapine The metabolism of Vardenafil can be decreased when combined with Clozapine.
Mirtazapine The metabolism of Vardenafil can be decreased when combined with Mirtazapine.
Sorafenib The metabolism of Vardenafil can be decreased when combined with Sorafenib.
Nitric Oxide The metabolism of Vardenafil can be decreased when combined with Nitric Oxide.
Cerivastatin The metabolism of Vardenafil can be decreased when combined with Cerivastatin.
Teniposide The metabolism of Vardenafil can be decreased when combined with Teniposide.
Chloramphenicol The metabolism of Vardenafil can be decreased when combined with Chloramphenicol.
Lansoprazole The metabolism of Vardenafil can be decreased when combined with Lansoprazole.
Quinine The metabolism of Vardenafil can be decreased when combined with Quinine.
Raloxifene The metabolism of Vardenafil can be decreased when combined with Raloxifene.
Cimetidine The metabolism of Vardenafil can be decreased when combined with Cimetidine.
Haloperidol The metabolism of Vardenafil can be decreased when combined with Haloperidol.
Erlotinib The metabolism of Vardenafil can be decreased when combined with Erlotinib.
Ciprofloxacin The metabolism of Vardenafil can be decreased when combined with Ciprofloxacin.
Zafirlukast The metabolism of Vardenafil can be decreased when combined with Zafirlukast.
Vinblastine The metabolism of Vardenafil can be decreased when combined with Vinblastine.
Fluticasone propionate The metabolism of Vardenafil can be decreased when combined with Fluticasone propionate.
Thiopental The metabolism of Vardenafil can be decreased when combined with Thiopental.
Imatinib The metabolism of Vardenafil can be decreased when combined with Imatinib.
Nicardipine The metabolism of Vardenafil can be decreased when combined with Nicardipine.
Efavirenz The metabolism of Vardenafil can be decreased when combined with Efavirenz.
Astemizole The metabolism of Vardenafil can be decreased when combined with Astemizole.
Dextropropoxyphene The metabolism of Vardenafil can be decreased when combined with Dextropropoxyphene.
Verapamil The metabolism of Vardenafil can be decreased when combined with Verapamil.
Epinephrine The metabolism of Vardenafil can be decreased when combined with Epinephrine.
Aprepitant The metabolism of Vardenafil can be decreased when combined with Aprepitant.
Tamoxifen The metabolism of Vardenafil can be decreased when combined with Tamoxifen.
Losartan Vardenafil may increase the antihypertensive activities of Losartan.
Midazolam The metabolism of Vardenafil can be decreased when combined with Midazolam.
Daunorubicin The metabolism of Vardenafil can be decreased when combined with Daunorubicin.
Ergotamine The metabolism of Vardenafil can be decreased when combined with Ergotamine.
Amprenavir The metabolism of Vardenafil can be decreased when combined with Amprenavir.
Delavirdine The metabolism of Vardenafil can be decreased when combined with Delavirdine.
Paroxetine The metabolism of Vardenafil can be decreased when combined with Paroxetine.
Tranylcypromine The metabolism of Vardenafil can be decreased when combined with Tranylcypromine.
Tetracycline The metabolism of Vardenafil can be decreased when combined with Tetracycline.
Methimazole The metabolism of Vardenafil can be decreased when combined with Methimazole.
Roxithromycin The metabolism of Vardenafil can be decreased when combined with Roxithromycin.
Phenelzine The metabolism of Vardenafil can be decreased when combined with Phenelzine.
Propofol The metabolism of Vardenafil can be decreased when combined with Propofol.
Acetazolamide The metabolism of Vardenafil can be decreased when combined with Acetazolamide.
Diazepam The metabolism of Vardenafil can be decreased when combined with Diazepam.
Mifepristone The metabolism of Vardenafil can be decreased when combined with Mifepristone.
Loperamide The excretion of Loperamide can be decreased when combined with Vardenafil.
Clofazimine The metabolism of Vardenafil can be decreased when combined with Clofazimine.
Tacrolimus The metabolism of Vardenafil can be decreased when combined with Tacrolimus.
Conivaptan The metabolism of Vardenafil can be decreased when combined with Conivaptan.
Ethanol The metabolism of Vardenafil can be decreased when combined with Ethanol.
Quinidine The metabolism of Vardenafil can be decreased when combined with Quinidine.
Metronidazole The metabolism of Vardenafil can be decreased when combined with Metronidazole.
Buprenorphine The metabolism of Vardenafil can be decreased when combined with Buprenorphine.
Tipranavir The metabolism of Vardenafil can be decreased when combined with Tipranavir.
Isoniazid The metabolism of Vardenafil can be decreased when combined with Isoniazid.
Dirithromycin The metabolism of Vardenafil can be decreased when combined with Dirithromycin.
Telithromycin The metabolism of Vardenafil can be decreased when combined with Telithromycin.
Doxorubicin The metabolism of Vardenafil can be decreased when combined with Doxorubicin.
Metyrapone The metabolism of Vardenafil can be decreased when combined with Metyrapone.
Sulfamethoxazole The metabolism of Vardenafil can be decreased when combined with Sulfamethoxazole.
Glyburide The metabolism of Vardenafil can be decreased when combined with Glyburide.
Irbesartan The metabolism of Vardenafil can be decreased when combined with Irbesartan.
Topotecan The metabolism of Vardenafil can be decreased when combined with Topotecan.
Norfloxacin The metabolism of Vardenafil can be decreased when combined with Norfloxacin.
Oxybutynin The metabolism of Vardenafil can be decreased when combined with Oxybutynin.
Mequitazine The metabolism of Vardenafil can be decreased when combined with Mequitazine.

Target Protein

cGMP-specific 3',5'-cyclic phosphodiesterase PDE5A
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma PDE6G
Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma PDE6H

Referensi & Sumber

Synthesis reference: Yogesh S. Deshpande, Sandra Brueck, Julia Schulze Nahrup, Birgit Schnitter, Ganesh Gat, Javed Hussain, "PROCESS FOR THE PREPARATION OF A MEDICAMENT COMPRISING VARDENAFIL HYDROCHLORIDE TRIHYDRATE." U.S. Patent US20100159003, issued June 24, 2010.
Artikel (PubMed)
  • PMID: 21890489
    Forstermann U, Sessa WC: Nitric oxide synthases: regulation and function. Eur Heart J. 2012 Apr;33(7):829-37, 837a-837d. doi: 10.1093/eurheartj/ehr304. Epub 2011 Sep 1.
  • PMID: 21471085
    Jing ZC, Yu ZX, Shen JY, Wu BX, Xu KF, Zhu XY, Pan L, Zhang ZL, Liu XQ, Zhang YS, Jiang X, Galie N: Vardenafil in pulmonary arterial hypertension: a randomized, double-blind, placebo-controlled study. Am J Respir Crit Care Med. 2011 Jun 15;183(12):1723-9. doi: 10.1164/rccm.201101-0093OC. Epub 2011 Mar 11.
  • PMID: 31644226
    Authors unspecified: Vardenafil. .
  • PMID: 14609619
    Rosen RC, Kostis JB: Overview of phosphodiesterase 5 inhibition in erectile dysfunction. Am J Cardiol. 2003 Nov 6;92(9A):9M-18M. doi: 10.1016/s0002-9149(03)00824-5.

Contoh Produk & Brand

Produk: 133 • International brands: 2
Produk
  • Ag-vardenafil
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Ag-vardenafil
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ag-vardenafil
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Apo-vardenafil
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Apo-vardenafil
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-vardenafil
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Jamp-vardenafil
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Jamp-vardenafil
    Tablet • 10 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 133 produk.
International Brands
  • Levitra — Bayer
  • Staxyn — GlaxoSmithKline

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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