vardenafil (Rx)

Brand and Other Names:Levitra, Staxyn ODT
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet, film coated

  • 2.5mg
  • 5mg
  • 10mg
  • 20mg

tablet, orally disintegrating

  • 10mg

Erectile Dysfunction

Film-coated tablet: 10 mg PO ~1 hour before sexual activity; may be increased to 20 mg or reduced to 5 mg, depending on effectiveness and tolerance; not to exceed 1 dose/day

Orally disintegrating tablet (ODT): 10 mg PO placed on tongue ~1 hour before sexual activity; not to exceed 1 dose/day

10-mg ODT not interchangeable with 10-mg film-coated tablet; ODT provides higher systemic exposure at same dose; if higher or lower doses are required, film-coated tablet should be prescribed

Dosage Modifications

Coadministration with strong CYP3A4 inhibitor

  • Ketoconazole 200 mg/day or itraconazole 200 mg/day: Vardenafil dosage not to exceed 5 mg/day
  • Ketoconazole 400 mg/day or itraconazole 400 mg/day: Vardenafil dosage not to exceed 2.5 mg/day
  • Indinavir, saquinavir, atazanavir, or clarithromycin: Vardenafil dosage not to exceed 2.5 mg/day
  • Ritonavir (600 mg q12hr): Vardenafil dosage not to exceed 2.5 mg/72 hr

Coadministration with moderate CYP3A4 inhibitor

  • Erythromycin 500 mg q8hr: Vardenafil dosage not to exceed 5 mg/day

Coadministration with alpha blocker

  • Stabilized on alpha-blocker therapy (eg, alfuzosin, terazosin, tamsulosin): 5 mg/day PO initially
  • Stabilized on alpha-blocker therapy and taking moderate-to-strong CYP3A4 inhibitor: 2.5 mg/day PO initially

Renal impairment

  • Mild, moderate, severe impairment: Dosage adjustment not necessary
  • Hemodialysis: Not recommended

Hepatic impairment

  • Child-Pugh class A: Dosage adjustment not necessary
  • Child-Pugh class B: Film-coated tablet, 5 mg PO ~1 hour before sexual activity; not to exceed 10 mg once daily; ODT not recommended
  • Child-Pugh class C: Not recommended

Pulmonary Arterial Hypertension (Orphan)

Orphan designation for treatment of pulmonary arterial hypertension

Orphan sponsor

  • Respira Therapeutics, Inc; 5901 Indian School Road NE, suite 107; Albuquerque, New Mexico 87110

Not indicated

Erectile Dysfunction

<65 years

Film-coated tablet: 10 mg PO ~1 hour before sexual activity; may be increased to 20 mg or reduced to 5 mg, depending on effectiveness and tolerance; not to exceed 1 dose/day

Orally disintegrating tablet (ODT): 10 mg PO placed on tongue ~1 hour before sexual activity; not to exceed 1 dose/day; not interchangeable with 10-mg film-coated tablet; if higher or lower doses required, film-coated tablet should be prescribed

>65 years

Consinder 5 mg starting dose

AUC and Cmax increased by 39% and 21%, respectively, in elderly men (compared with men <45 years)

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Interactions

Interaction Checker

and vardenafil

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    No Interactions Found
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      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            >10%

            Headache (15%)

            Flushing (11%)

            1-10%

            Rhinitis (9%)

            Dyspepsia (4%)

            Flulike syndrome (3%)

            Sinusitis (3%)

            Back pain (2%)

            Dizziness (2%)

            Increased creatine phosphokinase (2%)

            Nausea (2%)

            <1%

            Anaphylaxis

            Angina

            Insomnia

            Myocardial infarction (MI)

            Postural hypotension

            Priapism

            Pruritus

            Rash

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            Warnings

            Contraindications

            Hypersensitivity

            Soluble guanylate cyclase (sGC) stimulators (eg, riociguat); concomitant use can cause hypotension

            Coadministration with nitrates

            • Coadministration with nitrates (either regularly and/or intermittently) and nitric oxide donors
            • Consistent with the effects of PDE5 inhibition on the nitric oxide/cyclic guanosine monophosphate pathway, PDE5 inhibitors may potentiate the hypotensive effects of nitrates
            • A suitable time interval following PDE5 dosing for the safe administration of nitrates or nitric oxide donors has not been determined

            Cautions

            Use with caution in anatomical deformation of the penis (such as angulation, cavernosal fibrosis, or Peyronie’s disease), cardiovascular disease, left ventricular outflow obstruction, bleeding disorders, active peptic ulcer disease, liver disease, renal impairment, multidrug antihypertensive regimens, retinitis pigmentosa, concomitant use of CYP3A4 inhibitors, patients who have conditions that may predispose them to priapism (such as sickle cell anemia, multiple myeloma, or leukemia)

            There have been rare reports of prolonged erections >4 hours and priapism (painful erections greater than 6 hours in duration) for this class of compounds, including vardenafil; in the event that an erection persists >4 hours, the patient should seek immediate medical assistance; if priapism is not treated immediately, penile tissue damage and permanent loss of potency may result

            Physicians should consider the cardiovascular status of their patients; there is a degree of cardiac risk associated with sexual activity; treatment for erectile dysfunction, should not be used in men for whom sexual activity is not recommended because of their underlying cardiovascular status

            Patients with left ventricular outflow obstruction, (for example, aortic stenosis and idiopathic hypertrophic subaortic stenosis) can be sensitive to the action of vasodilators including PDE5 inhibitors

            Until further information available, use is not recommended in unstable angina; hypotension (resting systolic blood pressure of <90 mmHg); uncontrolled hypertension (>170/110 mmHg); recent history of stroke, life-threatening arrhythmia, or myocardial infarction (within last 6 months); severe cardiac failure

            Consider counseling patients about protective measures necessary to guard against sexually transmitted diseases, including Human Immunodeficiency Virus (HIV); drug offers no protection against sexually transmitted diseases

            Patients taking Class 1A (eg, quinidine, procainamide) or Class III (eg, amiodarone, sotalol) antiarrhythmic medications or those with congenital QT prolongation, should avoid using drug

            Safety and efficacy of drug used in combination with other treatments for erectile dysfunction not studied; use of such combinations not recommended

            Not to be taken with other phosphodiesterase (PDE)-5 inhibitors (eg, sildenafil, tadalafil)

            Vision loss may occur rarely and may be a sign of non-arteritic anterior ischemic optic neuropathy (NAION); patient should seek medical assistance for sudden loss in one or both eyes; patients who have already experienced NAION are at increased risk of recurrence; use is not recommended in patients with known degenerative retinal disorders

            May increase risk of rare sudden vision loss attributed to nonarteritic ischemic optic neuropathy; if vision problems arise, discontinue, and contact physician

            The drug has systemic vasodilatory properties that resulted in transient decreases in supine blood pressure in healthy volunteers (mean maximum decrease of 7 mmHg systolic and 8 mmHg diastolic); while this normally would be expected to be of little consequence in most patients, physicians should carefully consider whether their patients with underlying cardiovascular disease could be affected adversely by such vasodilatory effects

            Physicians should advise patients to stop taking all PDE5 inhibitors, and seek prompt medical attention in event of sudden decrease or loss of hearing; these events, which may be accompanied by tinnitus and dizziness, have been reported in temporal association to intake of PDE5 inhibitors, including vardenafil; it is not possible to determine whether these events are related directly to use of PDE5 inhibitors or to other factors

            Alpha blocekrs (H4)

            • Caution advised when PDE5 inhibitors co-administered with alpha-blockers; PDE5 inhibitors, and alpha-adrenergic blocking agents are both vasodilators with blood-pressure lowering effects; when vasodilators are used in combination, an additive effect on blood pressure may be anticipated; in some patients, concomitant use of these two drug classes can lower blood pressure significantly leading to symptomatic hypotension (eg, fainting)
            • Patients should be stable on alpha-blocker therapy prior to initiating a PDE5 inhibitor; patients who demonstrate hemodynamic instability on alpha-blocker therapy alone are at increased risk of symptomatic hypotension with concomitant use of PDE5 inhibitors
            • In patients who are stable on alpha-blocker therapy, initiate PDE5 inhibitors at lowest recommended starting dose
            • In patients already taking optimized dose of PDE5 inhibitor, initiate alpha-blocker therapy at lowest dose; stepwise increase in alpha-blocker dose may be associated with further lowering of blood pressure in patients taking a PDE5 inhibitor
            • Safety of combined use of PDE5 inhibitors and alpha-blockers may be affected by other variables, including intravascular volume depletion and other anti-hypertensive drugs

            Drug interaction overview(H4)

            • Concomitant administration with potent CYP3A4 inhibitors (such as ritonavir, indinavir, ketoconazole) or moderate CYP3A4 inhibitors (such as erythromycin) increases plasma concentrations of drug; dosage adjustment is necessary when drug is administered with certain CYP3A4 inhibitors
            • Long-term safety information is not available on concomitant administration of drug with HIV protease inhibitors
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            Pregnancy & Lactation

            Pregnancy category: B

            Lactation: Unknown whether drug is distributed into breast milk; indicated for males

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Sexual stimulation causes nitric oxide to be released in corpus cavernosum, and nitric oxide activates guanylate cyclase, which in turn increases cyclic guanosine monophosphate (cGMP), thus causing smooth-muscle relaxation; PDE-5 inhibitors enhance smooth muscle-relaxing effects of nitric oxide in corpus cavernosum by inhibiting degradation of cGMP

            Absorption

            Rapidly absorbed

            Bioavailability: 15%

            Onset: 60 min

            Peak plasma time: 30-120 min

            Peak plasma concentration: 8-19% lower for ODT than for film-coated tablet

            Distribution

            Protein bound: 95%

            Vd: 208 L

            Metabolism

            Metabolized in liver by CYP3A4 and (in minor amounts) CYP2C9

            Metabolites: M1 (active; plasma concentration 26% of parent compound)

            Elimination

            Half-life: 3-6 hr

            Total body clearance: 56 L/hr

            Excretion: Feces (95%), urine (5%)

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            Administration

            Instructions

            Oral tablet or orally disintegrating tablet

            • Take about 60 minutes before sexual activity
            • Maximum dosing frequency is one tablet per day
            • May take with or without food

            Orally disintegrating tablet

            • Place on tongue where it will dissolve
            • Do not swallow
            • Take without liquid
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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.