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.
- Vardenafil Levitra is a prescription medication for erectile dysfunction.
- It works by increasing blood flow to the penis.
- Vardenafil is marketed under the brand name Levitra.
- It typically takes about 25-60 minutes to work.
- The effects of vardenafil last up to 4-5 hours.
- It should be taken on an empty stomach for faster results.
- Common side effects include headache and flushing.
- Vardenafil is contraindicated with nitrates.
- Do not consume alcohol with vardenafil.
- Always follow your doctor's dosage instructions.
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.
References (13)
In vitro data predicts inhibition or induction of CYP3A4 by stiripentol potentially resulting in clinically significant interactions. Sunitinib: (Moderate) Concomitant use of vardenafil and sunitinib may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Tacrolimus: (Moderate) Concomitant use of vardenafil and tacrolimus may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Tamoxifen: (Moderate) Concomitant use of tamoxifen and vardenafil may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Tamsulosin: (Moderate) Due to the potential for symptomatic hypotension, patients should be stable on tamsulosin therapy before initiating therapy with the lowest dose of vardenafil.
J. Urol.
Telavancin: (Moderate) Concomitant use of vardenafil and telavancin may increase the risk of QT/QTc prolongation and torsade de pointes (TdP) in some patients. Terazosin: (Moderate) Due to the potential for symptomatic hypotension, patients should be stable on alpha-blocker therapy before initiating therapy with the lowest dose of vardenafil. Tetrabenazine: (Major) Concomitant use of vardenafil and tetrabenazine increases the risk of QT/QTc prolongation and torsade de pointes (TdP). 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.
Participants included in the review
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). 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. M1 accounts for about 7% of the total pharmacological activity.
| 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 |
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.
- Levitra is manufactured by Bayer Pharmaceuticals.
- It is available in both tablet and generic forms.
- The drug can be prescribed for men aged 18 and above.
- Levitra's active ingredient is vardenafil hydrochloride.
- It helps achieve erections suitable for sexual activity.
- Taking fatty meals may delay the drug's onset.
- Levitra does not protect against sexually transmitted diseases.
- Use with caution if you have heart conditions.
- It is essential to inform your doctor of all medications.
- Vardenafil does not cure ED; it manages symptoms.
Affected Cytochrome P450 (CYP450) isoenzymes and drug transporters: CYP3A4, P-glycoprotein (P-gp)Vardenafil is primarily a substrate of CYP3A4. Concomitant use of vardenafil with moderate or strong CYP3A4 inhibitors may require a reduction in vardenafil dosage to reduce the risk of adverse effects.
| Product | Dosage | Quantity + Bonus | Price | |
|---|---|---|---|---|
| Levitra Original | 20mg | 34 + 2 Pills | 188.51€ 179.53€ | |
| Levitra Generic | 20mg | 180 + 10 Pills | 293.10€ 279.14€ | |
| Levitra Original | 20mg | 14 + 2 Pills | 102.27€ 97.40€ | |
| Levitra Original | 20mg | 12 Pills | 81.99€ 78.09€ | |
| Levitra Professional | 20mg | 20 Pills | 101.00€ 96.19€ | |
| Levitra Generic | 40mg | 120 + 8 Pills | 302.37€ 287.97€ | |
| Levitra Soft Tabs | 20mg | 10 Pills | 52.27€ 49.78€ | |
| Levitra Professional | 20mg | 10 Pills | 62.37€ 59.40€ | |
| Levitra Professional | 20mg | 120 + 4 Pills | 348.44€ 331.85€ | |
| Levitra Soft Tabs | 20mg | 360 + 20 Pills | 682.21€ 649.72€ | |
| Levitra Generic | 10mg | 90 + 8 Pills | 150.58€ 143.41€ | |
| Levitra Generic | 60mg | 120 + 8 Pills | 372.33€ 354.60€ |
In vitro data suggest that vardenafil may inhibit P-gp at therapeutic doses.
How To Get Vardenafil
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. 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.
What is Stendra?
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. 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.
Oral phosphodiesterase-5 inhibitors and hormonal treatments for erectile dysfunction: A systematic review and meta-analysis
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. 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. 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. High-fat meals reduced Cmax by 18% to 50%.
How and Where to Buy Levitra or Generic Vardenafil Safely
Vardenafil has no direct relaxant effect on isolated human corpus cavernosum and, at recommended doses, 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. 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). 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.
Study selection
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. In addition, voriconazole has been associated with QT prolongation and rare levitra shipping 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.
How were decisions on the relevance of primary studies made?
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). 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.
Why was Levitra discontinued?
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. 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. 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.
- Vardenafil requires a prescription; self-medicating is unsafe.
- Take Levitra approximately 60 minutes before intimacy.
- Do not take more than one dose per 24 hours.
- Symptoms like priapism need immediate medical attention.
- Levitra may cause nasal congestion or upset stomach.
- Combining vardenafil with other ED drugs increases risks.
- Alcohol can hinder the effectiveness of Levitra.
- Levitra is designed for occasional use, not daily.
- Precautions include monitoring for vision changes.
- Seek medical advice if you experience allergic reactions.
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