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Levitra > vardenafil levitra


High fat meals had no effect on vardenafil AUC or Tmax in healthy volunteers, but reduced the Cmax by 35%.

When the orally disintegrating vardenafil tablets were administered with water, the vardenafil AUC was reduced

Database entry date

Levitra/Staxyn/Vardenafil/Vardenafil Hydrochloride Oral Tab: 2.5mg, 5mg, 10mg, 20mgStaxyn Oral Tab Orally Dis: 10mg For regular tablets (e.g., Levitra), 20 mg/day PO. For orally disintegrating tablets (e.g., Staxyn), 10 mg/day PO. The physiologic mechanism of erection of the penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. Nitric oxide then activates the enzyme guanylate cyclase, which results in increased levels of cGMP. Cyclic guanosine monophosphate causes smooth muscle relaxation in the corpus cavernosum thereby allowing inflow of blood; the exact mechanism by which cGMP stimulates relaxation of smooth muscles has not been determined.

Oral phosphodiesterase-5 inhibitors and hormonal treatments for erectile dysfunction: A systematic review and meta-analysis

Phosphodiesterase type 5 is responsible for degradation of cGMP in the corpus cavernosum. Vardenafil enhances the effect of NO by inhibiting PDE5, thereby raising concentrations of cGMP in the corpus cavernosum. Vardenafil has no direct relaxant effect on isolated human corpus cavernosum and, at recommended doses, cheap levitra prices has no effect in the absence of sexual stimulation. Vardenafil has a greater selectivity for PDE5 versus PDE6, an enzyme found in the retina and involved in phototransduction. Sildenafil, another PDE inhibitor, has a lower selectivity for PDE5 versus PDE6 and is associated with abnormalities related to color vision with higher doses or plasma concentrations of the drug.

What conditions is Levitra approved to treat?

The mean steady-state volume of distribution is 208L, indicating extensive distribution throughout the body. Vardenafil and its major metabolite (M1) are highly bound to plasma proteins (approximately 95% for parent drug and M1). Vardenafil is metabolized predominantly in the liver by CYP3A4 (there is some contribution by CYP3A5 and CYP2C isoforms). The major metabolite M1 is the result of desethylation at the piperazine moiety of vardenafil and is further metabolized. M1 has phosphodiesterase selectivity similar to that of vardenafil and an in vitro inhibitory potency for phosphodiesterase 5 (PDE5) that is 28% of that of vardenafil. by 29% and the median Tmax was shortened by 60 minutes, while Cmax was not affected.

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Vardenafil is not indicated for use in females.

Medication Active Ingredient Onset of Action Duration Typical Dose Cost
Vardenafil (Levitra) Vardenafil 25-60 min Up to 5 hours 10 mg Moderate
Sildenafil (Viagra) Sildenafil 30-60 min 4-6 hours 50 mg Moderate
Tadalafil (Cialis) Tadalafil 30-60 min Up to 36 hours 10-20 mg Higher

There are no adequate and well-controlled trials of vardenafil in humans during pregnancy.

Key Takeaways

M1 accounts for about 7% of the total pharmacological activity. Vardenafil is excreted as metabolites predominantly in the feces (approximately 91% to 95% of an oral dose) and to a lesser extent in the urine (about 2% to 6% of an oral dose). The elimination half-life of vardenafil and M1 is about 4 to 5 hours with the use of the film-coated tablets. The elimination half-life of vardenafil is 4 to 6 hours and the elimination half-life of MI is 3 to 5 hours with the use of the orally disintegrating tablets. Affected Cytochrome P450 (CYP450) isoenzymes and drug transporters: CYP3A4, P-glycoprotein (P-gp)Vardenafil is primarily a substrate of CYP3A4.

What are the most common side effects of vardenafil?

Concomitant use of vardenafil with moderate or strong CYP3A4 inhibitors may require a reduction in vardenafil dosage to reduce the risk of adverse effects. In vitro data suggest that vardenafil may inhibit P-gp at therapeutic doses. While concomitant use of vardenafil did not significantly increase plasma concentrations of digoxin (a P-gp substrate), the effect of vardenafil on plasma concentrations of P-gp substrates more sensitive than digoxin (e.g., dabigatran) is unknown. Oral film-coated tablets:Vardenafil is rapidly absorbed with absolute bioavailability of approximately 15%. In healthy volunteers, peak plasma concentrations (Cmax) following administration of a single 20 mg oral tablet dose are usually reached between 30 minutes and 2 hours (median 60 minutes) in the fasted state. In animal reproduction studies, no adverse developmental outcomes were observed during organogenesis at exposures for unbound vardenafil and

its major metabolite at 100 and 29 times, respectively, the maximum recommended human dose (MRHD) of 20 mg.

Patient characteristics

Venlafaxine: (Moderate) Concomitant use of vardenafil and venlafaxine may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Verapamil: (Major) Do not use vardenafil orally disintegrating tablets with verapamil due to increased vardenafil exposure; do not exceed a single dose of 5 mg per 24-hour period of vardenafil oral tablets. Vericiguat: (Contraindicated) Use of vericiguat and vardenafil is contraindicated due to the risk of hypotension. PDE5 inhibitors, including vardenafil, may potentiate the hypotensive effects of vericiguat. Vigabatrin: (Major) Vigabatrin should not be used with phosphodiesterase inhibitors, which is associated with serious ophthalmic effects (e.g., retinopathy or glaucoma) unless the benefit of treatment clearly outweighs the risks.

Serious Side Effects

Voclosporin: (Moderate) Concomitant use of vardenafil and voclosporin may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. The degree of QT prolongation associated with voclosporin is not clinically significant when administered within the recommended dosage range; QT prolongation has been described at 3 times the maximum recommended dose. Vonoprazan; Amoxicillin; Clarithromycin: (Major) Do not use vardenafil orally disintegrating tablets with clarithromycin due to increased vardenafil exposure; do not exceed a single dose of 2.5 mg per 24-hour period of vardenafil oral tablets. Voriconazole: (Major) Do not use vardenafil orally disintegrating tablets with voriconazole due to increased vardenafil exposure; do not exceed a single dose of 2.5 mg per 24-hour period of vardenafil oral tablets. Vardenafil is primarily metabolized by CYP3A4/5; voriconazole is a strong CYP3A4 inhibitor.

Pharmacotherapy for erectile dysfunction

In addition, voriconazole has been associated with QT prolongation and rare cases of torsade de pointes. Vorinostat: (Moderate) Concomitant use of vardenafil and vorinostat may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Voxelotor: (Major) Do not use vardenafil orally disintegrating tablets with voxelotor due to increased vardenafil exposure; do not exceed a single dose of 5 mg per 24-hour period of vardenafil oral tablets. Vardenafil is primarily metabolized by CYP3A; voxelotor is a moderate CYP3A inhibitor. Ziprasidone: (Major) Concomitant use of ziprasidone and vardenafil increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Vardenafil is not indicated for use in females and is therefore not recommended during breast-feeding.

Condition Caution Reason
Use with Nitrates Contraindicated Risk of severe hypotension
Severe Liver Impairment Use with caution Metabolism may be affected
Heart Disease Consult doctor before use Potential cardiovascular risks
Retinitis Pigmentosa Avoid Possible risk of vision loss
Hypotension or Hypertension Caution or avoid Blood pressure effects

There is no information on the presence of vardenafil and its major metabolite in

human milk, the effects on the breast-fed infant, or the effects on milk production.

Proper Use

Thioridazine: (Contraindicated) Avoid concomitant use of vardenafil and thioridazine due to an increased risk for torsade de pointes (TdP) and QT/QTc prolongation. Tipranavir: (Major) Do not use vardenafil orally disintegrating tablets with tipranavir boosted with ritonavir due to increased vardenafil exposure; do not exceed a single dose of 2.5 mg per 72-hour period of vardenafil oral tablets. Tolterodine: (Major) Due to the potential for QT prolongation and torsade de pointes (TdP), caution is advised when administering tolterodine with vardenafil. Tolterodine has been associated with dose-dependent prolongation of the QT interval, especially in poor CYP2D6 metabolizers. Therapeutic (10 mg) and supratherapeutic (80 mg) doses of vardenafil also produce an increase in QTc interval (e.g., 4 to 6 msec calculated by individual QT correction).

Achieving treatment optimization with sildenafil citrate (Viagra(R)) in patients with erectile dysfunction

Toremifene: (Major) Concomitant use of vardenafil and toremifene increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Trandolapril; Verapamil: (Major) Do not use vardenafil orally disintegrating tablets with verapamil due to increased vardenafil exposure; do not exceed a single dose of 5 mg per 24-hour period of vardenafil oral tablets. Vardenafil is primarily metabolized by CYP3A and verapamil is a moderate CYP3A inhibitor. Trazodone: (Major) Concomitant use of vardenafil and trazodone increases the risk of QT/QTc prolongation and torsade de pointes (TdP). Triclabendazole: (Moderate) Concomitant use of triclabendazole and vardenafil may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients.

Sustained efficacy and tolerability of vardenafil (Levitra®), a highly potent, selective phosphodiesterase-5 inhibitor, in men with erectile dysfunction: results of a randomized, double-blind, 26-week placebo-controlled pivotal trial

Trifluoperazine: (Minor) Use vardenafil with caution in combination with trifluoperazine as concurrent use may increase the risk of QT prolongation. Trifluoperazine is associated with a possible risk for QT prolongation. Triptorelin: (Moderate) Concomitant use of vardenafil and androgen deprivation therapy (i.e., triptorelin) may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Tucatinib: (Major) Do not use vardenafil orally disintegrating tablets with tucatinib due to increased vardenafil exposure; do not exceed a single dose of 2.5 mg per 24-hour period of vardenafil oral tablets. Vardenafil is primarily metabolized by CYP3A4/5; tucatinib is a strong CYP3A4 inhibitor. Vardenafil is excreted into the milk of lactating rats at concentrations approximately 10-fold greater than found in the plasma; following

a single oral dose of 3 mg/kg, 3.3% of the administered dose was excreted into the milk within 24 hours.

Authors' conclusions

High-fat meals reduced Cmax by 18% to 50%. The onset of action is within 1 hour of administration.Orally disintegrating tablets:The orally disintegrating vardenafil tablets provide a higher systemic exposure than the film-coated tablets. In a study of patients with erectile dysfunction, the mean AUC was increased by 21% to 29% and the mean Cmax was decreased by 19% in geriatric patients and 8% in younger patients (18 to 45 years) as compared to the 10 mg film-coated tablets. In a study of healthy male volunteers (18 to 50 years), the mean Cmax was 15% higher and the mean AUC was 44% higher compared to the 10 mg film-coated tablets. The median time to reach Cmax in a fasted stated was 1.5 hours (range: 45 minutes to 2.5 hours).