In vitro data suggest that vardenafil has the potential to inhibit P-glycoprotein (P-gp) at therapeutic doses.
| Study/Source | Sample Size | Success Rate | Notes |
|---|---|---|---|
| Clinical Trial A | 150 men | 80% | Significant improvement in erectile function |
| Clinical Trial B | 200 men | 75% | Better outcomes with 10 mg dose compared to placebo |
| Real-world Reports | 300 patients | 78% | Effective in various age groups and conditions |
Nifedipine: Vardenafil 20 mg (film-coated tablets), when co-administered with slow-release nifedipine 30 mg or 60 mg once daily, did not affect the relative AUC or Cmax of nifedipine, a drug that is metabolized via CYP3A4. Vardenafil hydrochloride orally disintegrating tablets, when co-administered with slow-release nifedipine 30 mg or 60 mg once daily in patients whose hypertension was controlled with nifedipine, produced mean additional supine systolic/diastolic blood pressure reductions of 3/4 mmHg (age group 65 to 69 years) and 5/5 mmHg (age group 70 to 80 years) compared to placebo. indinavir, the Cmax and AUC of indinavir were reduced by 40% and 30%, respectively.
Cited by (58)
Do not use vardenafil hydrochloride orally disintegrating tablets in patients with moderate to severe hepatic impairment [see Warnings and Precautions (5.8) and Dosage and Administration (2). ]8.7 Renal ImpairmentDo not use vardenafil hydrochloride orally disintegrating tablets in patients on renal dialysis.In volunteers with mild renal impairment (CLcr = 50 to 80 mL/min), the pharmacokinetics of vardenafil 20 mg film-coated tablets were similar to those observed in a control group with normal renal function. In the moderate (CLcr = 30 to 50 mL/min) or severe (CLcr <30 mL/min) renal impairment groups, the AUC of vardenafil fildena 200 mg was 20 to 30% higher compared to that observed in a control group with normal renal function (CLcr >80 mL/min). Vardenafil hydrochloride orally disintegrating tablets can be used in patients with mild, moderate or severe renal impairment. Do not use vardenafil hydrochloride orally disintegrating tablets in patients on renal dialysis as vardenafil has not been evaluated in such patients [see Dosage and Administration (2.3) and Warnings and Precautions (5.9)].
What should I tell my healthcare provider before taking vardenafil?
Vardenafil hydrochloride orally disintegrating tablets are not indicated for use in females. There are no data with the use of vardenafil hydrochloride orally disintegrating tablets in pregnant women to inform any drug-associated risks. In animal reproduction studies conducted in pregnant rats and rabbits, no adverse developmental outcomes were observed with oral administration of vardenafil during organogenesis at exposures for unbound vardenafil and its major metabolite at approximately 100 and 29 times, respectively, the maximum recommended human dose (MRHD) of 20 mg based on AUC(see Data). No evidence of specific potential for teratogenicity, embryotoxicity or fetotoxicity was observed in rats and rabbits that received vardenafil at up to 18 mg/kg/day during organogenesis. This dose is approximately 100 fold (rat) and 29 fold (rabbit) greater than the AUC values for unbound vardenafil and its major metabolite in humans given the maximum recommended human dose (MRHD) of 20 mg. Aspirin: Vardenafil 10 mg and 20 mg did not potentiate the increase in bleeding time caused by aspirin (two 81 mg tablets). Other Interactions: Vardenafil had no effect on the pharmacodynamics of glyburide (glucose and insulin concentrations) and warfarin (prothrombin time or other pharmacodynamic parameters). 8 USE IN SPECIFIC POPULATIONS 8.1 PregnancyRisk SummaryVardenafil hydrochloride orally disintegrating tablets are not indicated for use in females.There are no data with the use of vardenafil hydrochloride orally disintegrating tablets in pregnant women to inform any drug-associated risks.
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| Cialis Generic | 10mg | 10 Pills | 31.41€ 29.91€ | |
| Levitra Soft Tabs | 20mg | 270 + 10 Pills | 521.78€ 496.93€ | |
| Viagra Generic | 25mg | 30 + 4 Pills | 47.97€ 45.69€ | |
| Cialis Generic | 2.5mg | 180 + 10 Pills | 154.86€ 147.49€ | |
| Cialis Generic | 20mg | 10 Pills | 31.49€ 29.99€ | |
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| Viagra Professional | 100mg | 10 Pills | 44.09€ 41.99€ | |
| Viagra Soft Tabs | 100mg | 90 + 6 Pills | 205.31€ 195.53€ | |
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| Levitra Generic | 20mg | 120 + 10 Pills | 224.15€ 213.48€ | |
| Apcalis SX Oral Jelly | 20mg | 17 + 4 Sachets | 95.52€ 90.97€ | |
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In animal reproduction studies conducted in pregnant rats and rabbits, no adverse developmental outcomes were observed with oral administration of vardenafil during organogenesis at exposures for unbound vardenafil and its major metabolite at approximately 100 and 29 times, respectively, the maximum recommended human dose (MRHD) of 20 mg based on AUC(see Data).DataAnimal DataNo evidence of specific potential for teratogenicity, embryotoxicity or fetotoxicity was observed in rats and rabbits that received vardenafil at up to 18 mg/kg/day during organogenesis. This dose is approximately 100 fold (rat) and 29 fold (rabbit) greater than the AUC values for unbound vardenafil and its major metabolite in humans given the maximum recommended human dose (MRHD) of 20 mg.In the rat pre-and postnatal development study, the NOAEL (no observed adverse effect level) for maternal toxicity was 8 mg/kg/day. Retarded physical development of pups in the absence of maternal effects was observed following maternal exposure to 1 and 8 mg/kg possibly due to vasodilatation and/or secretion of the drug into milk. The number of living pups born to rats exposed pre- and postnatally was reduced at 60 mg/kg/day. Based on the results of the pre- and postnatal study, the developmental NOAEL is less than 1 mg/kg/day. Based on plasma exposures in the rat developmental toxicity study, 1 mg/kg/day in the pregnant rat is estimated to produce total AUC values for unbound vardenafil and its major metabolite comparable to the human AUC at the MRHD of 20 mg.8.2 LactationRisk SummaryVardenafil hydrochloride orally disintegrating tablets are not indicated for use in females.There is no information on the presence of vardenafil and its major metabolite in human milk, the effects on the breastfed infant, or the effects on milk production. Vardenafil is present in rat milk of lactating rats (see Data).DataVardenafil was secreted 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.8.4 Pediatric UseVardenafil hydrochloride orally disintegrating tablets are not indicated for use in pediatric patients.
Dose Adjustments
The majority of these subjects experienced reversible back pain/myalgia and/or “abnormal vision.” Single doses up to 80 mg vardenafil and multiple doses up to 40 mg vardenafil administered once daily over 4 weeks were tolerated without producing serious adverse side effects.When 40 mg of vardenafil was administered twice daily, cases of severe back pain were observed. No muscle or neurological toxicity was identified.In cases of overdose, standard supportive measures should be taken as required. Renal dialysis is not expected to accelerate clearance because vardenafil is highly bound to plasma proteins and is not significantly eliminated in the urine. Safety and efficacy in children has not been established.8.5 Geriatric UseVardenafil AUC and Cmax in elderly males 65 years or older taking vardenafil hydrochloride orally disintegrating tablets were increased by 39% and 21%, respectively, in comparison to patients aged 45 years and below. No overall differences in safety or effectiveness were observed between patients ≥65 years old and those < 65 years old in placebo-controlled clinical trials [see Clinical Pharmacology (12.3)].8.6 Hepatic ImpairmentDo not use vardenafil hydrochloride orally disintegrating tablets in patients with moderate or severe hepatic impairment.In volunteers with mild hepatic impairment (Child-Pugh A), the Cmax and AUC following a 10 mg vardenafil (film-coated tablets) dose were increased by 22% and 17%, respectively, compared to healthy control subjects. Vardenafil hydrochloride orally disintegrating tablets can be used in patients with mild hepatic impairment. In volunteers with moderate hepatic impairment (Child-Pugh B), the Cmax and AUC following a 10 mg vardenafil (film-coated tablets) dose were increased by 130% and 160%, respectively, compared to healthy control subjects. Vardenafil has not been evaluated in patients with severe (Child-Pugh C) hepatic impairment. Do not use vardenafil hydrochloride orally disintegrating tablets in patients with moderate to severe hepatic impairment [see Warnings and Precautions (5.8) and Dosage and Administration (2). ]8.7 Renal ImpairmentDo not use vardenafil hydrochloride orally disintegrating tablets in patients on renal dialysis.In volunteers with mild renal impairment (CLcr = 50 to 80 mL/min), the pharmacokinetics of vardenafil 20 mg film-coated tablets were similar to those observed in a control group with normal renal function. In the moderate (CLcr = 30 to 50 mL/min) or severe (CLcr <30 mL/min) renal impairment groups, the AUC of vardenafil fildena 200 mg was 20 to 30% higher compared to that observed in a control group with normal renal function (CLcr >80 mL/min). Vardenafil hydrochloride orally disintegrating tablets can be used in patients with mild, moderate or severe renal impairment.
What can cause erectile dysfunction?
The number of living pups born to rats exposed pre- and postnatally was reduced at 60 mg/kg/day. Based on the results of the pre- and postnatal study, the developmental NOAEL is less than 1 mg/kg/day. Based on plasma exposures in the rat developmental toxicity study, 1 mg/kg/day in the pregnant rat is estimated to produce total AUC values for unbound vardenafil and its major metabolite comparable to the human AUC at the MRHD of 20 mg.8.2 LactationRisk SummaryVardenafil hydrochloride orally disintegrating tablets are not indicated for use in females.There is no information on the presence of vardenafil and its major metabolite in human milk, the effects on the breastfed infant, or the effects on milk production. Vardenafil is present in rat milk of lactating rats (see Data).DataVardenafil was secreted 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.8.4 Pediatric UseVardenafil hydrochloride orally disintegrating tablets are not indicated for use in pediatric patients.
What should I do if I miss a dose of vardenafil?
Safety and efficacy in children has not been established.8.5 Geriatric UseVardenafil AUC and Cmax in elderly males 65 years or older taking vardenafil hydrochloride orally disintegrating tablets were increased by 39% and 21%, respectively, in comparison to patients aged 45 years and below. No overall differences in safety or effectiveness were observed between patients ≥65 years old and those < 65 years old in placebo-controlled clinical trials [see Clinical Pharmacology (12.3)].8.6 Hepatic ImpairmentDo not use vardenafil hydrochloride orally disintegrating tablets in patients with moderate or severe hepatic impairment.In volunteers with mild hepatic impairment (Child-Pugh A), the Cmax and AUC following a 10 mg vardenafil (film-coated tablets) dose were increased by 22% and 17%, respectively, compared to healthy control subjects. Vardenafil hydrochloride orally disintegrating tablets can be used in patients with mild hepatic impairment. In volunteers with moderate hepatic impairment (Child-Pugh B), the Cmax and AUC following a 10 mg vardenafil (film-coated tablets) dose were increased by 130% and 160%, respectively, compared to healthy control subjects. Vardenafil has not been evaluated in patients with severe (Child-Pugh C) hepatic impairment. Do not use vardenafil hydrochloride orally disintegrating tablets in patients on renal dialysis as vardenafil has not been evaluated in such patients [see Dosage and Administration (2.3) and Warnings and Precautions (5.9)]. Vardenafil hydrochloride orally disintegrating tablets are not indicated for use in females. There are no data with the use of vardenafil hydrochloride orally disintegrating tablets in pregnant women to inform any drug-associated risks.
Results and discussion
Do not use vardenafil hydrochloride orally disintegrating tablets in patients with moderate or severe hepatic impairment. In volunteers with mild hepatic impairment (Child-Pugh A), the Cmax and AUC following a 10 mg vardenafil (film-coated tablets) dose were increased by 22% and 17%, respectively, compared to healthy control subjects. Do not use vardenafil hydrochloride orally disintegrating tablets in patients with moderate to severe hepatic impairment [see Warnings and Precautions (5.8) and Dosage and Administration (2).] Do not use vardenafil hydrochloride orally disintegrating tablets in patients on renal dialysis. In volunteers with mild renal impairment (CLcr = 50 to 80 mL/min), the pharmacokinetics of vardenafil 20 mg film-coated tablets were similar to those observed in a control group with normal renal function. 10 OVERDOSAGE The maximum dose of vardenafil for which human data are available is a single 120 mg dose of the film–coated tablets administered to healthy male volunteers. In animal reproduction studies conducted in pregnant rats and rabbits, no adverse developmental outcomes were observed with oral administration of vardenafil during organogenesis at exposures for unbound vardenafil and its major metabolite at approximately 100 and 29 times, respectively, the maximum recommended human dose (MRHD) of 20 mg based on AUC(see Data). No evidence of specific potential for teratogenicity, embryotoxicity or fetotoxicity was observed in rats and rabbits that received vardenafil at up to 18 mg/kg/day during organogenesis. This dose is approximately 100 fold (rat) and 29 fold (rabbit) greater than the AUC values for unbound vardenafil and its major metabolite in humans given the maximum recommended human dose (MRHD) of 20 mg.
503A vs 503B
In the rat pre-and postnatal development study, the NOAEL (no observed adverse effect level) for maternal toxicity was 8 mg/kg/day. Based on plasma exposures in the rat developmental toxicity study, 1 mg/kg/day in the pregnant rat is estimated to produce total AUC values for unbound vardenafil and its major metabolite comparable to the human AUC at the MRHD of 20 mg. There is no information on the presence of vardenafil and its major metabolite in human milk, the effects on the breastfed infant, or the effects on milk production. Vardenafil is present in rat milk of lactating rats (see Data). Vardenafil was secreted 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. Vardenafil hydrochloride orally disintegrating tablets are not indicated for use in pediatric patients. Safety and efficacy in children has not been established.
- Vardenafil efficacy depends on proper dosage and timing.
- It is generally safe when used as directed.
- Patients should avoid heavy meals before intake.
- Follow-up with your healthcare provider regularly.
Vardenafil AUC and Cmax in elderly males 65 years or older taking vardenafil hydrochloride orally disintegrating tablets were increased by 39% and 21%, respectively, in comparison to patients aged 45 years and below. No overall differences in safety or effectiveness were observed between patients ≥65 years old and those < 65 years old in placebo-controlled clinical trials [see Clinical Pharmacology (12.3)].
- Vardenafil is sometimes prescribed off-label for pulmonary hypertension.
- It is not suitable for women or children.
- Patients should report any unexplained vision loss.
- Avoid using grapefruit juice with vardenafil.
Do not use vardenafil hydrochloride orally disintegrating tablets in patients with moderate or severe hepatic impairment. In volunteers with mild hepatic impairment (Child-Pugh A), the Cmax and AUC following a 10 mg vardenafil (film-coated tablets) dose were increased by 22% and 17%, respectively, compared to healthy control subjects. Do not use vardenafil hydrochloride orally disintegrating tablets in patients with moderate to severe hepatic impairment [see Warnings and Precautions (5.8) and Dosage and Administration (2).] Do not use vardenafil hydrochloride orally disintegrating tablets in patients on renal dialysis.
| Side Effect | Frequency | Severity | Recommended Action |
|---|---|---|---|
| Headache | Common | Mild | Take analgesics, hydration |
| Flushing | Common | Mild | Cool environment, hydrate |
| Nasal Congestion | Moderate | Mild | Use decongestants if needed |
| Dizziness | Less common | Mild | Sit or lie down immediately |
| Muscle Pain | Rare | Mild | Consult doctor if persists |
In volunteers with mild renal impairment (CLcr = 50 to 80 mL/min), the pharmacokinetics of vardenafil 20 mg film-coated tablets were similar to those observed in a control group with normal renal function.
8.4 Pediatric Use
In vitro data suggest that vardenafil has the potential to inhibit P-glycoprotein (P-gp) at therapeutic doses. Nifedipine: Vardenafil 20 mg (film-coated tablets), when co-administered with slow-release nifedipine 30 mg or 60 mg once daily, did not affect the relative AUC or Cmax of nifedipine, a drug that is metabolized via CYP3A4. Vardenafil hydrochloride orally disintegrating tablets, when co-administered with slow-release nifedipine 30 mg or 60 mg once daily in patients whose hypertension was controlled with nifedipine, produced mean additional supine systolic/diastolic blood pressure reductions of 3/4 mmHg (age group 65 to 69 years) and 5/5 mmHg (age group 70 to 80 years) compared to placebo. indinavir, the Cmax and AUC of indinavir were reduced by 40% and 30%, respectively. Aspirin: Vardenafil 10 mg and 20 mg did not potentiate the increase in bleeding time caused by aspirin (two 81 mg tablets).
Sensitive determination of anticancer drug imatinib in spiked human urine samples by differential pulse voltammetry on anodically pretreated boron-doped diamond electrode
Other Interactions: Vardenafil had no effect on the pharmacodynamics of glyburide (glucose and insulin concentrations) and warfarin (prothrombin time or other pharmacodynamic parameters). 8 USE IN SPECIFIC POPULATIONS 8.1 PregnancyRisk SummaryVardenafil hydrochloride orally disintegrating tablets are not indicated for use in females.There are no data with the use of vardenafil hydrochloride orally disintegrating tablets in pregnant women to inform any drug-associated risks. In animal reproduction studies conducted in pregnant rats and rabbits, no adverse developmental outcomes were observed with oral administration of vardenafil during organogenesis at exposures for unbound vardenafil and its major metabolite at approximately 100 and 29 times, respectively, the maximum recommended human dose (MRHD) of 20 mg based on AUC(see Data).DataAnimal DataNo evidence of specific potential for teratogenicity, embryotoxicity or fetotoxicity was observed in rats and rabbits that received vardenafil at up to 18 mg/kg/day during organogenesis. This dose is approximately 100 fold (rat) and 29 fold (rabbit) greater than the AUC values for unbound vardenafil and its major metabolite in humans given the maximum recommended human dose (MRHD) of 20 mg.In the rat pre-and postnatal development study, the NOAEL (no observed adverse effect level) for maternal toxicity was 8 mg/kg/day. Retarded physical development of pups in the absence of maternal effects was observed following maternal exposure to 1 and 8 mg/kg possibly due to vasodilatation and/or secretion of the drug into milk. 10 OVERDOSAGE The maximum dose of vardenafil for which human data are available is a single 120 mg dose of the film–coated tablets administered to healthy male volunteers. The majority of these subjects experienced reversible back pain/myalgia and/or “abnormal vision.” Single doses up to 80 mg vardenafil and multiple doses up to 40 mg vardenafil administered once daily over 4 weeks were tolerated without producing serious adverse side effects.When 40 mg of vardenafil was administered twice daily, cases of severe back pain were observed. No muscle or neurological toxicity was identified.In cases of overdose, standard supportive measures should be taken as required. Renal dialysis is not expected to accelerate clearance because vardenafil is highly bound to plasma proteins and is not significantly eliminated in the urine.
Why is a prescription required for erectile dysfunction medicines?
In the rat pre-and postnatal development study, the NOAEL (no observed adverse effect level) for maternal toxicity was 8 mg/kg/day. Based on plasma exposures in the rat developmental toxicity study, 1 mg/kg/day in the pregnant rat is estimated to produce total AUC values for unbound vardenafil and its major metabolite comparable to the human AUC at the MRHD of 20 mg. There is no information on the presence of vardenafil and its major metabolite in human milk, the effects on the breastfed infant, or the effects on milk production. Vardenafil is present in rat milk of lactating rats (see Data). Vardenafil was secreted into the milk of lactating rats at concentrations approximately 10-fold greater than found in the plasma.
What should I do if I accidentally take too much vardenafil?
Following a single oral dose of 3 mg/kg, 3.3% of the administered dose was excreted into the milk within 24 hours. Vardenafil hydrochloride orally disintegrating tablets are not indicated for use in pediatric patients. Safety and efficacy in children has not been established. Vardenafil AUC and Cmax in elderly males 65 years or older taking vardenafil hydrochloride orally disintegrating tablets were increased by 39% and 21%, respectively, in comparison to patients aged 45 years and below. No overall differences in safety or effectiveness were observed between patients ≥65 years old and those < 65 years old in placebo-controlled clinical trials [see Clinical Pharmacology (12.3)].
