Drug reference

Vardenafil

Vasodilator · Erectile Dysfunction

Also known as Vardenafil hydrochloride trihydrate, Levitra

VasodilatorErectile Dysfunction

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

FDA category + note

Top interactionssee all 12 →

Organic NitratesContraindicatedTextbookG&G 14e · p999
SildenafilContraindicatedTextbookG&G 14e · p612
Isosorbide MononitrateContraindicatedDatabaseDDInter
NicorandilContraindicatedDatabase

Mechanism

Vardenafil is a selective PDE5 inhibitor structurally similar to sildenafil that inhibits cGMP degradation in corpus cavernosum smooth muscle, potentiating nitric oxide-mediated vasodilation during sexual stimulation. It has a plasma half-life of 4-5 hours (intermediate between sildenafil at ~4 hours and tadalafil at ~17 hours) and peak plasma levels in 30-120 minutes. Vardenafil is also approved for premature ejaculation in some countries, based on modulation of afferent signaling pathways.

Indications

Erectile dysfunctionErectile dysfunction (patients on alpha-blocker therapy)pulmonary hypertensionerectile dysfunction (ED)

Dosing

Adult: Tablets (General): Initially 10 mg (max. per dose 20 mg), taken approximately 25 –60 minutes before sexual activity. Subsequent doses adjusted according to response. Onset of effect may be delayed if taken with high-fat meal. Maximum 1 dose per day. Orodispersible Tablets (General): 10 mg, taken approximately 25 –60 minutes before sexual activity. Maximum 10 mg per day.…
Renal adjustment: Orodispersible tablets not suitable if eGFR less than 30 mL/minute/1.73 m2. Initial dose 5 mg if eGFR less than 30 mL/minute/1.73 m2.
Hepatic adjustment: Tablets: Initial dose reduction to 5 mg in mild to moderate impairment, increase according to response; max. 10 mg in moderate impairment. Orodispersible Tablets: Manufacturer advises initial dose reduction to 5 mg using film-coated tablets in mild impairment, increase according to response.
Geriatric: 5 mg
Max dose: 20 mg per day (tablets); 10 mg per day (orodispersible tablets)

Pharmacokinetics

Peak effect

30–120 min

Half-life

4–5 hours

Bioavailability

15 (8–25)%

Protein binding

93–95% (parent and M1)

Excretion

2–6%

Contraindications

Systolic blood pressure below 90 mmHg
Hereditary degenerative retinal disorders
Myocardial infarction
Patients in whom vasodilation or sexual activity are inadvisable
Previous history of non-arteritic anterior ischaemic optic neuropathy
Recent stroke
Unstable angina
hyperkalaemia
patients with long Q-T interval
patients receiving class IA antiarrhythmics
patients receiving class III antiarrhythmics
patients taking nitrates
coronary heart disease
liver disease (caution)
kidney disease (caution)
peptic ulcer (caution)
bleeding disorders (caution)
leukaemia (caution, predisposes to priapism)
sickle cell anaemia (caution, predisposes to priapism)
myeloma (caution, predisposes to priapism)
Use within 24 hours of nitroglycerin administration

Side effects

Common

transient blue-green tinting of visionbluish hazelight sensitivity

Serious

prolongs Q-T interval

Pregnancy & lactation

Pregnancy

Drug interactions

Organic Nitrates

Contraindicated

Textbook

Dangerously low blood pressures.

The administration of PDE5 inhibitors to patients receiving organic nitrates is contraindicated. The patient’s underlying cardiovascular status and concurrent use of hypotensive agents (e.g., nitrates, α adrenergic antagonists) must be considered prior to use of this class of drugs.

Source: G&G 14e · p999

Sildenafil

Contraindicated

Textbook

Extreme hypotension, potentially life-threatening.

PDE5 inhibitors should not be prescribed to patients receiving any form of nitrate. Patients should be warned not to use PDE5 inhibitors and nitrates concurrently. No PDE5 inhibitor should be used in the 24 hours prior to initiating nitrate therapy. If significant hypotension occurs, fluids and α adrenergic receptor agonists may be used for support.

Source: G&G 14e · p612

Isosorbide Mononitrate

Contraindicated

Database

Profound and prolonged systemic hypotension, syncope, myocardial ischemia, and even death.

Concomitant use is absolutely contraindicated. A minimum of 24 hours should elapse between the last dose of vardenafil and the administration of isosorbide mononitrate.

Source: DDInter

Nicorandil

Contraindicated

Database

Profound and prolonged systemic hypotension, syncope, myocardial ischemia, and even death.

Concomitant use is absolutely contraindicated. Patients on nicorandil should not be prescribed vardenafil or other PDE5 inhibitors (sildenafil, tadalafil).

Amiodarone

Severe

Database

Increased risk of severe cardiac arrhythmias.

Vardenafil should be avoided in patients receiving class III antiarrhythmics.

Source: DDInter

Amisulpride

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Amyl Nitrite