Label: VARDENAFIL tablet, orally disintegrating

In a single dose study in 25 normal males, vardenafil (film-coated tablets) 40 mg, twice the maximum daily recommended dose, did not alter visual acuity, intraocular pressure, fundoscopic and slit lamp findings. In another double-blind, placebo-controlled clinical trial, at least 15 doses of 20 mg vardenafil were administered over 8 weeks versus placebo to 52 males. Two patients on vardenafil in the trial reported episodes of transient cyanopsia (objects appear blue). There was no effect on sperm motility or morphology after single 20 mg oral doses of vardenafil film-coated tablets in healthy volunteers. The pharmacokinetics of vardenafil and its M1 metabolite from vardenafil hydrochloride orally disintegrating tablets have been evaluated in healthy male volunteers (18 to 50 years) and in young (18 to 45 years) and elderly (≥ 65 years) erectile dysfunction patients. Studies have shown that vardenafil hydrochloride orally disintegrating tablets provides higher systemic exposure of vardenafil compared to vardenafil 10 mg film-coated tablets. Mean vardenafil plasma concentrations measured after the administration of a single oral dose vardenafil hydrochloride orally disintegrating tablets to patients with erectile dysfunction (18 to 45 years) are depicted in Figure 8.

Key Takeaways

In a single dose study in 25 normal males, vardenafil (film-coated tablets) 40 mg, twice the maximum daily recommended dose, did not alter visual acuity, intraocular pressure, fundoscopic and slit lamp findings. In another double-blind, placebo-controlled clinical trial, at least 15 doses of 20 mg vardenafil were administered over 8 weeks versus placebo to 52 males. Two patients on vardenafil in the trial reported episodes of transient cyanopsia (objects appear blue). There was no effect on sperm motility or morphology after single 20 mg oral doses of vardenafil film-coated tablets in healthy volunteers. The pharmacokinetics of vardenafil and its M1 metabolite from vardenafil hydrochloride orally disintegrating tablets have been evaluated in healthy male volunteers (18 to 50 years) and in young (18 to 45 years) and elderly (≥ 65 years) erectile dysfunction patients.

What is vardenafil, and what is it used for?

Studies have shown that vardenafil hydrochloride orally disintegrating tablets provides higher systemic exposure of vardenafil compared to vardenafil 10 mg film-coated tablets. Mean vardenafil plasma concentrations measured after the administration of a single oral dose vardenafil hydrochloride orally disintegrating tablets to patients with erectile dysfunction (18 to 45 years) are depicted in Figure 8. Figure 8: Vardenafil Plasma Concentration (Mean ± SD) Profile for Vardenafil Hydrochloride Orally Disintegrating Tablets in men age 18to 45 years with erectile dysfunction Vardenafil was not found to accumulate in plasma when vardenafil hydrochloride orally disintegrating tablets was dosed daily over ten days. Effect of food: A high fat meal had no effect on vardenafil AUC and Tmax from vardenafil hydrochloride orally disintegrating tablets in healthy volunteers and reduced Cmax by 35%. Effect of water: When vardenafil hydrochloride orally disintegrating tablets were swallowed with water, the AUC of vardenafil was reduced by 29% and median Tmax was shortened by 60 minutes while Cmax was not affected. Figure 8: Vardenafil Plasma Concentration (Mean ± SD) Profile for Vardenafil Hydrochloride Orally Disintegrating Tablets in men age 18to 45 years with erectile dysfunction Vardenafil was not found to accumulate in plasma when vardenafil hydrochloride orally disintegrating tablets was dosed daily over ten days. Effect of food: A high fat meal had no effect on vardenafil AUC and Tmax from vardenafil hydrochloride orally disintegrating tablets in healthy volunteers and reduced Cmax by 35%.

Effect of water: When vardenafil hydrochloride orally disintegrating tablets were swallowed with water, the AUC of vardenafil was reduced by 29% and median Tmax was shortened by 60 minutes while Cmax was not affected. Vardenafil hydrochloride orally disintegrating tablets should be taken without liquid. Following a single oral dose of 20 mg vardenafil film-coated tablet in healthy volunteers, a mean of 0.00018% of the administered dose was obtained in semen 1.5 hours after dosing. 13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of FertilityCarcinogenesisVardenafil was not carcinogenic in rats and mice when administered daily for 24 months.

How To Get Vardenafil

Subscribe to MedicineNet's Men's Health Newsletter

In these studies systemic drug exposures (AUCs) for unbound (free) vardenafil and its major metabolite were approximately 400- and 170-fold for male and female rats, respectively, and 21-and 37-fold for male and female mice, respectively, the exposures observed in human males given the maximum recommended human dose (MRHD) of 20 mg.MutagenesisVardenafil was not mutagenic as assessed in either the in vitro bacterial Ames assay or the forward mutation assay in Chinese hamster V79 cells.

5.2 Potential for Drug Interactions with Strong or Moderate CYP3A4 Inhibitors

Report Problems to the Food and Drug Administration

Vardenafil was not clastogenic as assessed in either the in vitro chromosomal aberration test or the in vivo mouse micronucleus test.Impairment of FertilityVardenafil did not impair fertility in male and female rats administered doses up to 100 mg/kg/day for 28 days prior to mating in males, and for 14 days prior to mating and through day 7 of gestation in females. In a corresponding 1-month rat toxicity study, this dose produced an AUC value for unbound vardenafil 200 fold greater than AUC in humans at the MRHD of 20 mg.

• Vardenafil is ineffective without sexual arousal.
• It does not protect against sexually transmitted infections.
• Avoid excessive mental or physical exertion while on medication.
• Consult a healthcare professional if unsure about interactions.
• Don't take vardenafil if you've had recent heart attack.
• Use with caution if you have a bleeding disorder.
• Medication may cause a temporary drop in blood pressure.
• Avoid using if you have a known hypersensitivity.
• The pill should be taken as part of a treatment plan.
• Keep track of how you respond to the medication.

Vardenafil was not carcinogenic in rats and mice when administered daily for 24 months. In these studies systemic drug exposures (AUCs) for unbound (free) vardenafil and its major metabolite were approximately 400- and 170-fold for male and female rats, respectively, and 21-and 37-fold for male and female mice, respectively, the exposures observed in human males given the maximum recommended human dose (MRHD) of 20 mg. Vardenafil was not mutagenic as assessed in either the fildena purple pill in vitro bacterial Ames assay or the forward mutation assay in Chinese hamster V79 cells. Vardenafil did not impair fertility in male and female rats administered doses up to 100 mg/kg/day for 28 days prior to mating in males, and for 14 days prior to mating and through day 7 of gestation in females.

What is the competitive landscape?

14 CLINICAL STUDIES The efficacy and safety of vardenafil hydrochloride orally disintegrating tablets were evaluated in two identical multi-national, randomized, double-blind, placebo-controlled trials (studies 1 and 2). Vardenafil hydrochloride orally disintegrating tablets were dosed without regard to meals on an as-needed basis in men with erectile dysfunction (ED), many of whom had multiple other medical conditions. In both pivotal studies, randomization was stratified so that approximately 50% of patients were ≥65 years old. Primary efficacy assessment was by means of the Erectile Function (EF) Domain score of the validated International Index of Erectile Function (IIEF) Questionnaire and two questions from the Sexual Encounter Profile (SEP) dealing with the ability to achieve vaginal penetration (SEP2), and the ability to maintain an erection long enough for successful intercourse (SEP3). The primary endpoints were assessed at 3 months.Study 1 evaluated 355 mainly European (Belgium, France, Germany, Spain, South Africa, and Netherlands) patients (mean age 61.9; 67% White, 4% Black, 3% Asian, 26% Unknown).

From Rybelsus to the Ozempic Pill: What Pharmacists Need to Know About the Next Generation of Oral Semaglutide

The mean baseline EF domain scores were 13 for both placebo and vardenafil hydrochloride orally disintegrating tablets groups. Study 2 evaluated 331 mainly North American (USA, Canada, Mexico, and Australia) patients (mean age 61.7; 69% White, 5% Black, 4% Asian, 22% Hispanic). The mean baseline EF domain scores were 12 for vardenafil hydrochloride orally disintegrating tablets and 13 for placebo.In both studies vardenafil hydrochloride orally disintegrating tablets demonstrated clinically meaningful and statistically significant improvements over placebo in all 3 primary efficacy variables (see Table 7).Table 7: Change from Baseline for the Primary Efficacy Variables in Studies 1 and 214.1 Other Vardenafil Clinical Trials Using Film-Coated TabletsPatients with ED and Diabetes MellitusVardenafil demonstrated clinically meaningful and statistically significant improvement in erectile function in a prospective, fixed-dose [10 and 20 mg vardenafil film-coated tablets], double-blind, placebo-controlled trial of patients with diabetes mellitus (n=439; mean age 57 years, range 33 to 81; 80% White, 9% Black, 8% Hispanic, and 3% Other).Significant improvements in the EF Domain were shown in this study (EF Domain scores of 17 on 10 mg vardenafil and 19 on 20 mg vardenafil compared to 13 on placebo; p <0.0001).Vardenafil significantly improved the overall per-patient rate of achieving an erection sufficient for penetration (SEP2) (61% on 10 mg and 64% on 20 mg vardenafil compared to 36% on placebo; p <0.0001).Vardenafil demonstrated a clinically meaningful and statistically significant increase in the overall per-patient rate of maintenance of erection to successful intercourse (SEP3) (49% on 10 mg, 54% on 20 mg vardenafil compared to 23% on placebo; p <0.0001).Patients with ED after Radical ProstatectomyVardenafil demonstrated clinically meaningful and statistically significant improvement in erectile function in a prospective, fixed-dose 10 and 20 mg vardenafil film-coated tablets, double-blind, placebo-controlled trial in postprostatectomy patients (n=427, mean age 60, range 44 to 77 years; 93% White, 5% Black, 2% Other).Significant improvements in the EF Domain were shown in this study (EF Domain scores of 15 on 10 mg vardenafil and 15 on 20 mg vardenafil compared to 9 on placebo; p <0.0001).Vardenafil significantly improved the overall per-patient rate of achieving an erection sufficient for penetration (SEP2) (47% on 10 mg and 48% on 20 mg vardenafil compared to 22% on placebo; p <0.0001).Vardenafil demonstrated a clinically meaningful and statistically significant increase in the overall per-patient rate of maintenance of erection to successful intercourse (SEP3) (37% on 10 mg, 34% on 20 mg vardenafil compared to 10% on placebo; p <0.0001). The efficacy and safety of vardenafil hydrochloride orally disintegrating tablets were evaluated in two identical multi-national, randomized, double-blind, placebo-controlled trials (studies 1 and 2). The primary endpoints were assessed at 3 months. 14 CLINICAL STUDIES The efficacy and safety of vardenafil hydrochloride orally disintegrating tablets were evaluated in two identical multi-national, randomized, double-blind, placebo-controlled trials (studies 1 and 2).

What happens if the prescriber decides treatment is not suitable?

Study 1 evaluated 355 mainly European (Belgium, France, Germany, Spain, South Africa, and Netherlands) patients (mean age 61.9; 67% White, 4% Black, 3% Asian, 26% Unknown). The mean baseline EF domain scores were 12 for vardenafil hydrochloride orally disintegrating tablets and 13 for placebo. In both studies vardenafil hydrochloride orally disintegrating tablets demonstrated clinically meaningful and statistically significant improvements over placebo in all 3 primary efficacy variables (see Table 7). Table 7: Change from Baseline for the Primary Efficacy Variables in Studies 1 and 2 Vardenafil demonstrated clinically meaningful and statistically significant improvement in erectile function in a prospective, fixed-dose [10 and 20 mg vardenafil film-coated tablets], double-blind, placebo-controlled trial of patients with diabetes mellitus (n=439; mean age 57 years, range 33 to 81; 80% White, 9% Black, 8% Hispanic, and 3% Other). Significant improvements in the EF Domain were shown in this study (EF Domain scores of 17 on 10 mg vardenafil and 19 on 20 mg vardenafil compared to 13 on placebo; p <0.0001).

Navigating the MS Therapy Explosion: Strategies for Proactive Initiation and Smart Treatment Switching

Vardenafil significantly improved the overall per-patient rate of achieving an erection sufficient for penetration (SEP2) (61% on 10 mg and 64% on 20 mg vardenafil compared to 36% on placebo; p <0.0001). Vardenafil demonstrated a clinically meaningful and statistically significant increase in the overall per-patient rate of maintenance of erection to successful intercourse (SEP3) (49% on 10 mg, 54% on 20 mg vardenafil compared to 23% on placebo; p <0.0001). Vardenafil demonstrated clinically meaningful and statistically significant improvement in erectile function in a prospective, fixed-dose 10 and 20 mg vardenafil film-coated tablets, double-blind, placebo-controlled trial in postprostatectomy patients (n=427, mean age 60, range 44 to 77 years; 93% White, 5% Black, 2% Other). Vardenafil hydrochloride orally disintegrating tablets were dosed without regard to meals on an as-needed basis in men with erectile dysfunction (ED), many of whom had multiple other medical conditions.

In both pivotal studies, randomization was stratified so that approximately 50% of patients were ≥65 years old. Primary efficacy assessment was by means of the Erectile Function (EF) Domain score of the validated International Index of Erectile Function (IIEF) Questionnaire and two questions from the Sexual Encounter Profile (SEP) dealing with the ability to achieve vaginal penetration (SEP2), and the ability to maintain an erection long enough for successful intercourse (SEP3). The primary endpoints were assessed at 3 months.Study 1 evaluated 355 mainly European (Belgium, France, Germany, Spain, South Africa, and Netherlands) patients (mean age 61.9; 67% White, 4% Black, 3% Asian, 26% Unknown). The mean baseline EF domain scores were 13 for both placebo and vardenafil hydrochloride orally disintegrating tablets groups. Study 2 evaluated 331 mainly North American (USA, Canada, Mexico, and Australia) patients (mean age 61.7; 69% White, 5% Black, 4% Asian, 22% Hispanic). The mean baseline EF domain scores were 12 for vardenafil hydrochloride orally disintegrating tablets and 13 for placebo.In both studies vardenafil hydrochloride orally disintegrating tablets demonstrated clinically meaningful and statistically significant improvements over placebo in all 3 primary efficacy variables (see Table 7).Table 7: Change from Baseline for the Primary Efficacy Variables in Studies 1 and 214.1 Other Vardenafil Clinical Trials Using Film-Coated TabletsPatients with ED and Diabetes MellitusVardenafil demonstrated clinically meaningful and statistically significant improvement in erectile function in a prospective, fixed-dose [10 and 20 mg vardenafil film-coated tablets], double-blind, placebo-controlled trial of patients with diabetes mellitus (n=439; mean age 57 years, range 33 to 81; 80% White, 9% Black, 8% Hispanic, and 3% Other).Significant improvements in the EF Domain were shown in this study (EF Domain scores of 17 on 10 mg vardenafil and 19 on 20 mg vardenafil compared to 13 on placebo; p <0.0001).Vardenafil significantly improved the overall per-patient rate of achieving an erection sufficient for penetration (SEP2) (61% on 10 mg and 64% on 20 mg vardenafil compared to 36% on placebo; p <0.0001).Vardenafil demonstrated a clinically meaningful and statistically significant increase in the overall per-patient rate of maintenance of erection to successful intercourse (SEP3) (49% on 10 mg, 54% on 20 mg vardenafil compared to 23% on placebo; p <0.0001).Patients with ED after Radical ProstatectomyVardenafil demonstrated clinically meaningful and statistically significant improvement in erectile function in a prospective, fixed-dose 10 and 20 mg vardenafil film-coated tablets, double-blind, placebo-controlled trial in postprostatectomy patients (n=427, mean age 60, range 44 to 77 years; 93% White, 5% Black, 2% Other).Significant improvements in the EF Domain were shown in this study (EF Domain scores of 15 on 10 mg vardenafil and 15 on 20 mg vardenafil compared to 9 on placebo; p <0.0001).Vardenafil significantly improved the overall per-patient rate of achieving an erection sufficient for penetration (SEP2) (47% on 10 mg and 48% on 20 mg vardenafil compared to 22% on placebo; p <0.0001).Vardenafil demonstrated a clinically meaningful and statistically significant increase in the overall per-patient rate of maintenance of erection to successful intercourse (SEP3) (37% on 10 mg, 34% on 20 mg vardenafil compared to 10% on placebo; p <0.0001). The efficacy and safety of vardenafil hydrochloride orally disintegrating tablets were evaluated in two identical multi-national, randomized, double-blind, placebo-controlled trials (studies 1 and 2). The primary endpoints were assessed at 3 months.

Usual Geriatric Dose for Erectile Dysfunction

Vardenafil hydrochloride orally disintegrating tablets should be taken without liquid. Following a single oral dose of 20 mg vardenafil film-coated tablet in healthy volunteers, a mean of 0.00018% of the administered dose was obtained in semen 1.5 hours after dosing. 13 NONCLINICAL TOXICOLOGY 13.1 Carcinogenesis, Mutagenesis, Impairment of FertilityCarcinogenesisVardenafil was not carcinogenic in rats and mice when administered daily for 24 months. In these studies systemic drug exposures (AUCs) for unbound (free) vardenafil and its major metabolite were approximately 400- and 170-fold for male and female rats, respectively, and 21-and 37-fold for male and female mice, respectively, the exposures observed in human males given the maximum recommended human dose (MRHD) of 20 mg.MutagenesisVardenafil was not mutagenic as assessed in either the in vitro bacterial Ames assay or the forward mutation assay in Chinese hamster V79 cells. Vardenafil was not clastogenic as assessed in either the in vitro chromosomal aberration test or the in vivo mouse micronucleus test.Impairment of FertilityVardenafil did not impair fertility in male and female rats administered doses up to 100 mg/kg/day for 28 days prior to mating in males, and for 14 days prior to mating and through day 7 of gestation in females.

How should I store vardenafil?

In a corresponding 1-month rat toxicity study, this dose produced an AUC value for unbound vardenafil 200 fold greater than AUC in humans at the MRHD of 20 mg. Vardenafil was not carcinogenic in rats and mice when administered daily for 24 months. In these studies systemic drug exposures (AUCs) for unbound (free) vardenafil and its major metabolite were approximately 400- and 170-fold for male and female rats, respectively, and 21-and 37-fold for male and female mice, respectively, the exposures observed in human males given the maximum recommended human dose (MRHD) of 20 mg. Vardenafil was not mutagenic as assessed in either the fildena purple pill in vitro bacterial Ames assay or the forward mutation assay in Chinese hamster V79 cells. Vardenafil did not impair fertility in male and female rats administered doses up to 100 mg/kg/day for 28 days prior to mating in males, and for 14 days prior to mating and through day 7 of gestation in females. Study 1 evaluated 355 mainly European (Belgium, France, Germany, Spain, South Africa, and Netherlands) patients (mean age 61.9; 67% White, 4% Black, 3% Asian, 26% Unknown). The mean baseline EF domain scores were 12 for vardenafil hydrochloride orally disintegrating tablets and 13 for placebo. In both studies vardenafil hydrochloride orally disintegrating tablets demonstrated clinically meaningful and statistically significant improvements over placebo in all 3 primary efficacy variables (see Table 7). Table 7: Change from Baseline for the Primary Efficacy Variables in Studies 1 and 2 Vardenafil demonstrated clinically meaningful and statistically significant improvement in erectile function in a prospective, fixed-dose [10 and 20 mg vardenafil film-coated tablets], double-blind, placebo-controlled trial of patients with diabetes mellitus (n=439; mean age 57 years, range 33 to 81; 80% White, 9% Black, 8% Hispanic, and 3% Other).

• Side effects can include headache, flushing, or stomach upset.
• Serious side effects are rare but require immediate medical attention.
• Vardenafil may cause changes in color vision.
• Use caution if using other medication for blood pressure.
• The medication helps improve erectile function temporarily.
• Do not share tablets with others.
• Follow storage instructions to maintain efficacy.
• Report any allergic reactions promptly.
• The drug should be used only under medical supervision.
• Used responsibly, vardenafil can improve quality of life.

Significant improvements in the EF Domain were shown in this study (EF Domain scores of 17 on 10 mg vardenafil and 19 on 20 mg vardenafil compared to 13 on placebo; p <0.0001).

Adverse Effects

What should I tell my healthcare provider before taking vardenafil?

Vardenafil significantly improved the overall per-patient rate of achieving an erection sufficient for penetration (SEP2) (61% on 10 mg and 64% on 20 mg vardenafil compared to 36% on placebo; p <0.0001). Vardenafil demonstrated a clinically meaningful and statistically significant increase in the overall per-patient rate of maintenance of erection to successful intercourse (SEP3) (49% on 10 mg, 54% on 20 mg vardenafil compared to 23% on placebo; p <0.0001). Vardenafil demonstrated clinically meaningful and statistically significant improvement in erectile function in a prospective, fixed-dose 10 and 20 mg vardenafil film-coated tablets, double-blind, placebo-controlled trial in postprostatectomy patients (n=427, mean age 60, range 44 to 77 years; 93% White, 5% Black, 2% Other).