Vardenafil


Generic Medicine Info
Indications and Dosage
Oral
Erectile dysfunction
Adult: As conventional tab: Usual dose: 10 mg as needed; may adjust according to response (range: 5-20 mg). As orodispersible tab: Max: 10 mg as needed. Dose is taken approx 25-60 minutes before sexual intercourse. Max dosing frequency: Once every 24 hours.
Elderly: As conventional tab: 5 mg as needed, at least 25-60 minutes before sexual intercourse. Max: 20 mg. Max dosing frequency: Once every 24 hours.
Special Patient Group
Patients taking α-blockers: As conventional tab: Max: 5 mg daily. As orodispersible tab: Co-administer within a 6 hour-interval.

Patient taking CYP3A4 inhibitors: As conventional tab: 2.5 mg once every 24 hours with ketoconazole 400 mg, itraconazole 400 mg, clarithromycin; 2.5 mg once every 72 hours with ritonavir; 5 mg once every 24 hours with erythromycin, ketoconazole 200 mg, itraconazole 200 mg.

Patient taking HIV-protease inhibitors: As conventional tab: 2.5 mg once every 24 hours.
Renal Impairment
CrCl (mL/min) Dosage
 <30 As conventional tab: Initially, 5 mg as needed, at least 25-60 minutes before sexual intercourse. Dose may be increased to 10-20 mg according to response.
Hepatic Impairment
Mild to moderate (Child-Pugh class A or B) As conventional tab: Initially, 5 mg as needed, at least 25-60 minutes before sexual intercourse. Max: 10 mg. Max dosing frequency: Once every 24 hours. Severe (Child-Pugh class C): Contraindicated.
Administration
May be taken with or without food.
Contraindications
Severe CV disorder or recent history of stroke or MI (within the last 6 months), unstable angina, retinitis pigmentosa, vision loss due to non-arteritic anterior ischaemic optic neuropathy (NAION), ESRD requiring dialysis, hypotension <90/50 mmHg, and other conditions wherein sexual intercourse is inadvisable. Severe hepatic impairment (Child-Pugh class C). Concomitant use with any form of organic nitrates/nitrites, guanylate cyclase stimulators
Special Precautions
Patient with CV disease, left ventricular outflow obstruction (aortic stenosis or hypertrophic obstructive cardiomyopathy), anatomical penile deformation, conditions which may predispose to priapism (e.g. sickle cell anaemia, multiple myeloma, leukaemia); bleeding disorders, peptic ulcer disease. Severe renal and mild to moderate hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Hypotension, color discrimination impairment, vision loss/NAION, sudden decrease or loss of hearing, tinnitus. Rarely, prolonged/painful erection or priapism.
Gastrointestinal disorders: Dyspepsia, nausea.
General disorders and administration site conditions: Flu-like symptoms.
Nervous system disorders: Headache, dizziness.
Respiratory, thoracic and mediastinal disorders: Nasal congestion, sinusitis.
Patient Counseling Information
This medicine may cause dizziness and blurred vision, if affected, do not drive or operate machinery.
Monitoring Parameters
Assess CV status prior to initiation of therapy. Monitor BP, heart rate, renal function, and LFT.
Overdosage
Symptoms: Back pain/myalgia, abnormal vision. Management: Supportive treatment.
Drug Interactions
May enhance hypotensive effect of α-blockers. Increased serum concentration with guanylate cyclase stimulators (e.g. riociguat), potent CYP3A4 inhibitors (e.g. ketoconazole) and moderate CYP3A4 inhibitors (e.g. clarithromycin), HIV protease inhibitors (e.g. ritonavir). May prolong Qt interval with class IA (e.g. quinidine, procainamide) or class III (e.g. amiodarone, sotalol) antiarrhythmics.
Potentially Fatal: Enhanced hypotensive effect with any form of organic nitrates/nitrites, guanylate cyclase stimulators (e.g. riociguat).
Food Interaction
Increased serum concentration with grapefruit juice.
Action
Description: Vardenafil is a potent phosphodiesterase inhibitor with the greatest selectivity for PDE type 5, which is responsible for the metabolism of cyclic guanosine monophosphate (cGMP) in the smooth muscle. Inhibition of PDE type 5 causes smooth muscle relaxation and increased blood flow into the corpus cavernosum of the penis during sexual stimulation, thereby producing an erection.
Onset: Approx 60 minutes.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Food, particularly high-fat meal, decreases rate of absorption. Bioavailability: Approx 15%. Time to peak plasma concentration: 0.5-2 hours.
Distribution: Widely distributed in the tissues. Volume of distribution: 208 L. Detected in the semen. Plasma protein binding: Approx 95% (parent drug and metabolite).
Metabolism: Metabolised in the liver primarily by CYP3A4 as well as CYP3A5 and CYP2C via desethylation into active metabolite.
Excretion: Mainly via faeces (approx 91-95%, as metabolites); urine (approx 2-6%). Terminal half-life: Approx 4-6 hours.
Chemical Structure

Chemical Structure Image
Vardenafil

Source: National Center for Biotechnology Information. PubChem Database. Vardenafil, CID=135400189, https://pubchem.ncbi.nlm.nih.gov/compound/Vardenafil (accessed on Jan. 23, 2020)

Storage
Store at 25°C.
ATC Classification
G04BE09 - vardenafil ; Belongs to the class of drugs used in erectile dysfunction.
References
Anon. Vardenafil. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 12/01/2018.

Buckingham R (ed). Vardenafil. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/01/2018.

Joint Formulary Committee. Vardenafil. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/01/2018.

Levitra Film Coated Tablet (GlaxoSmithKline LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 12/01/2018.

Disclaimer: This information is independently developed by MIMS based on Vardenafil from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
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