Viagrazen 50 mg (Tablet)

Title

• Viagrazen

Categories

• Medicine
• Drugs for Erectile Dysfunction

Description

• Selective, reversible inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5)
• Causes smooth muscle relaxation and inflow of blood into the penile tissues

Indications

• Treatment of men with erectile dysfunction
• Also indicated in pulmonary arterial hypertension

Mechanism of Action

• Inhibition of PDE5 by Viagrazen produces increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood into the penile tissues

Pharmacokinetics

• Rapidly absorbed after oral administration
• Mean absolute bioavailability of 41%
• Eliminated predominantly by hepatic metabolism
• Converted to an active metabolite with similar properties to the parent

Dosage & Administration

• Recommended dose for erectile dysfunction: 50 mg, taken approximately 1 hour before sexual activity
• May be increased to a maximum recommended dose of 100 mg or decreased to 25 mg based on effectiveness and toleration
• Maximum recommended dosing frequency is once per day
• Recommended dose for pulmonary arterial hypertension: 20 mg three times a day

Interactions

• Metabolism is mediated by the cytochrome P450 isoforms 3A4 and 2C9
• Inhibitors of these isoenzymes may reduce clearance, while inducers may increase clearance

Contraindications

• Hypersensitivity to any component of the medication
• Concomitant use with organic nitrates

Side Effects

• Includes various cardiovascular, digestive, hemic and lymphatic, nervous, respiratory, and urogenital adverse reactions

Pregnancy & Lactation

• Pregnancy category B
• Not indicated for use by women

Precautions & Warnings

• Caution advised when co-administered with alpha-blockers
• Potential for cardiac risk in patients with preexisting cardiovascular disease

Overdose Effects

• Adverse events similar to lower doses, but with increased incidence rates and severities

Storage Conditions

• Keep in a dry place, away from light and heat
• Keep out of the reach of children

Pharmacology

• Release of nitric oxide in the corpus cavernosum during sexual stimulation
• Activation of guanylate cyclase and increased levels of cGMP
• Rapidly absorbed, reaching maximum plasma concentrations within 30 to 120 minutes
• Cleared by hepatic microsomal isoenzymes

Special Populations

• Reduced clearance in healthy elderly volunteers (65 years or over)

Affecting Factors

• Age >65
• Hepatic impairment
• Severe renal impairment
• Concomitant use of potent cytochrome P450 3A4 inhibitors

Pharmacokinetics in Special Populations

• Reduced clearance in healthy elderly volunteers

Potential Drug Interactions

• Inhibitors or inducers of cytochrome P450 isoforms may affect clearance

Clinical Data

• No controlled clinical data on safety or efficacy in certain patient groups

Sensitivity

• Patients with left ventricular outflow obstruction
• Patients with severely impaired autonomic control of blood pressure

Additional Precautions

• Viagrazen has systemic vasodilatory properties that could affect patients with underlying cardiovascular disease
• Patients with certain conditions may be particularly sensitive to vasodilators

Risks

• Potential for symptomatic hypotension when co-administered with alpha-blockers

Cardiac Risk

• Use of Viagrazen in men for whom sexual activity is inadvisable due to underlying cardiovascular status should be carefully considered

Sensitive Patient Groups

• Patients with preexisting cardiovascular risk factors
• Patients with specific cardiovascular conditions

Long-term Effects

• No controlled clinical data on safety or efficacy in certain patient groups

Possible Adverse Outcomes

• Prolonged erection greater than 4 hours and priapism
• Adverse cardiac, cerebrovascular, and vascular events

Evaluation

• Evaluation of potential underlying causes of erectile dysfunction
• Identification of appropriate treatment following a complete medical assessment

Hypersensitive Reactions

• Possible allergic reaction to any component of the medication

Vasodilatory Effects

• Viagrazen has systemic vasodilatory properties

Symptomatic Hypotension

• Concomitant use with alpha-blockers may lead to symptomatic hypotension

Urogenital Adverse Reactions

• Includes cystitis, urinary frequency, abnormal ejaculation, and genital edema

Potential Risks for Patients

• Potential cardiac risk of sexual activity in patients with preexisting cardiovascular disease

Blood Pressure-lowering Effects

• Vasodilators like Viagrazen and alpha-adrenergic blocking agents can have an additive effect on blood pressure

Recommendations

• Initiation of PDE5 inhibitors at the lowest dose in stable alpha-blocker therapy

Considerations

• Consideration should be given to certain patient groups, including those with bleeding disorders and active peptic ulceration

Potential Cardiac Risk

• Viagrazen should not be generally used in men for whom sexual activity is inadvisable due to underlying cardiovascular status

Drug Combinations

• Safety and efficacy of combinations with other treatments for erectile dysfunction have not been studied

Cardiac Risk of Sexual Activity

• There is a potential for cardiac risk of sexual activity in patients with preexisting cardiovascular disease

Coronary Artery Disease

• Viagrazen should not be generally used in patients with coronary artery disease causing unstable angina

Resting Hypotension

• Viagrazen safety is unknown in patients with resting hypotension (BP <90/50) or hypertension (BP >170/110)

Contraindications in Patients

• Viagrazen should be used with caution in patients with anatomical deformation of the penis
• Contraindicated in patients using organic nitrates

Overdose

• Standard supportive measures should be adopted as required
• Renal dialysis not expected to accelerate clearance due to high plasma protein binding

Animal Studies

• Animal study shows no evidence of teratogenicity or embryotoxicity

Plasma Levels

• Hepatic metabolism plays a significant role in determining plasma levels

Adverse Events

• Incidence rates and severities of adverse events increase with higher doses

Clinical Trials

• Patients on multiple antihypertensive medications were included in the pivotal clinical trials for Viagrazen

Potential for Adverse Events

• Decrease the chance of adverse events by decreasing Viagrazen dosage when prescribed to patients taking ritonavir

Safety and Efficacy

• No controlled clinical data on safety or efficacy in certain patient groups

Unstudied Groups

• No controlled clinical data on safety or efficacy in certain patient groups

Incidence Rates

• Adverse events at higher doses have increased incidence rates

Binding to Plasma Proteins

• Highly bound to plasma proteins, leading to slow clearance

Potentiation of Hypotensive Effects

• Viagrazen potentiates the hypotensive effects of nitrates

Drug Metabolism

• Viagrazen metabolism is principally mediated by specific cytochrome P450 isoforms

Erectile Dysfunction Therapy

• Recommended evaluation and identification of potential underlying causes

Phosphodiesterase Type 5 Inhibitors

• Caution is advised when co-administered with alpha-blockers

Vasodilatory Properties

• Viagrazen has systemic vasodilatory properties

Effects on Blood Pressure

• Combination with alpha-blockers may lead to additive effects on blood pressure

Vascular Events

• Reports of serious cardiovascular, cerebrovascular, and vascular events post-marketing

Blood Pressure-lowering Effect

• Concomitant use with other antihypertensive medications may lead to additional blood pressure reduction

Vascular Risk

• Reports of serious cardiovascular, cerebrovascular, and vascular events post-marketing

Pre-existing Risk Factors

• Patients with preexisting cardiovascular risk factors may be at increased risk of adverse events

Risk of Prolonged Erection

• Potential for prolonged erection greater than 4 hours and priapism

Interaction with Alpha-blockers

• Caution advised when Viagrazen is co-administered with alpha-blockers, leading to potential for symptomatic hypotension

Effect on Blood Pressure

• Viagrazen has been shown to lead to transient decreases in supine blood pressure in healthy volunteers

Reduction of Blood Pressure

• Combination with amlodipine led to additional blood pressure reduction in hypertensive patients

Secondary Effects

• Adverse events at higher doses have increased incidence rates and severities

Precautionary Measures

• Recommendation for initiation at the lowest dose in patients taking optimized doses of PDE5 inhibitors

Combination with Antihypertensive Medications

• Viagrazen has systemic vasodilatory properties and may augment the blood pressure-lowering effect of other antihypertensive medications

Age-related Factors

• Reduced clearance in healthy elderly volunteers

Hepatic Metabolism

• Predominantly eliminated by hepatic metabolism, particularly by cytochrome P450 3A4

Plasma Clearance

• Cytochrome P450 inhibitors or inducers may affect plasma clearance of Viagrazen

Blood Pressure-lowering Interaction

• Potential for blood pressure-lowering interaction with alpha-blockers

Blood Pressure Control

• Caution advised when combining with other anti-hypertensive drugs

Blood Pressure Reduction

• Combination with other antihypertensive medications may lead to additional blood pressure reduction

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