Description

Simple

A medication used to treat erectile dysfunction.

Clinical

A phosphodiesterase 5 inhibitor used to treat erectile dysfunction.

Overview

Vardenafil (Levitra) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

Pharmacology

Indication

Used for the treatment of erectile dysfunction

Pharmacodynamic

Vardenafil is used to treat male erectile dysfunction (impotence) and pulmonary arterial hypertension (PAH). Part of the physiological process of erection involves the release of nitric oxide (NO) in the corpus cavernosum. This then activates the enzyme guanylate cyclase which results in increased l... Read more

Mechanism of action

Vardenafil inhibits the cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum located around the penis. Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries an... Read more

Absorption

Vardenafil is rapidly absorbed with absolute bioavailability of approximately 15%.

Protein binding

95%

Volume of distribution

208 L

Clearance

56 L/h

Half life

4-5 hours

Route of elimination

After oral administration, vardenafil is excreted as metabolites predominantly in the feces (approximately 91-95% of administered oral dose) and to a lesser extent in the urine (approximately 2-6% of administered oral dose).

Toxicity

Symptoms of overdose include vision changes and back and muscle pain.

Adverse Effects

Contraindications

  • Regions: US
  • With Categories Coadmin:
      • Name: Soluble Guanylate Cyclase Stimulator
      • Drugbank Id: DBCAT003503
  • Regions: US
  • With Drugs Coadmin:
      • Name: Nitrate
      • Drugbank Id: DB14049
  • Regions: US
  • With Categories Coadmin:
      • Name: Nitric Oxide Donors
      • Drugbank Id: DBCAT000756
      • Mesh Id: D020030

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
6-Deoxyerythronolide B
The metabolism of Vardenafil can be decreased when combined with 6-Deoxyerythronolide B.
7-ethyl-10-hydroxycamptothecin
The metabolism of Vardenafil can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
Abatacept
The metabolism of Vardenafil can be increased when combined with Abatacept.
Abemaciclib
The serum concentration of Vardenafil can be increased when it is combined with Abemaciclib.
Abexinostat
The risk or severity of QTc prolongation can be increased when Vardenafil is combined with Abexinostat.
Acalabrutinib
The metabolism of Vardenafil can be decreased when combined with Acalabrutinib.
Acebutolol
Vardenafil may increase the antihypertensive activities of Acebutolol.
Acepromazine
The risk or severity of hypotension, dyspepsia, and headache can be increased when Vardenafil is combined with Acepromazine.
Aceprometazine
The risk or severity of QTc prolongation can be increased when Vardenafil is combined with Aceprometazine.
Acetaminophen
The metabolism of Vardenafil can be decreased when combined with Acetaminophen.
Acetazolamide
The metabolism of Vardenafil can be decreased when combined with Acetazolamide.
Acetyldigoxin
Vardenafil may decrease the excretion rate of Acetyldigoxin which could result in a higher serum level.
Acetylsalicylic acid
The serum concentration of Acetylsalicylic acid can be increased when it is combined with Vardenafil.
Acrivastine
The risk or severity of QTc prolongation can be increased when Vardenafil is combined with Acrivastine.
Adalimumab
The metabolism of Vardenafil can be increased when combined with Adalimumab.
Adenosine
The risk or severity of QTc prolongation can be increased when Vardenafil is combined with Adenosine.
Afatinib
The serum concentration of Afatinib can be increased when it is combined with Vardenafil.
Afelimomab
The metabolism of Vardenafil can be increased when combined with Afelimomab.
Ajmaline
The risk or severity of QTc prolongation can be increased when Vardenafil is combined with Ajmaline.
Aldesleukin
The metabolism of Vardenafil can be decreased when combined with Aldesleukin.