Navafil50 mg

Navafil is a phosphodiesterase type 5 (PDE5) inhibitor that is FDA-approved for one established indication:

• Erectile dysfunction (ED) in adult men — Navafil is indicated for the treatment of erectile dysfunction, a condition in which a man cannot achieve or maintain an erection sufficient for satisfactory sexual activity. Navafil works only in the presence of sexual stimulation and does not increase sexual desire.

Navafil is not indicated for use in women or children, and it does not treat premature ejaculation, low libido, or infertility. It also does not protect against sexually transmitted infections (STIs), including HIV.

Each film-coated tablet contains Avanafil as the active pharmaceutical ingredient, commonly available in strengths of 50 mg, 100 mg, and 200 mg. Tablets also contain standard inactive excipients such as diluents, binders, disintegrants, and film-coating agents, which may vary by manufacturer.

Navafil is an orally administered, highly selective phosphodiesterase type 5 (PDE5) inhibitor developed for the on-demand treatment of erectile dysfunction. It belongs to the same pharmacological class as sildenafil, tadalafil, and vardenafil, but has a distinct chemical (pyrimidine) structure that is associated with a rapid onset of action.

Navafil is supplied as a film-coated oral tablet in 50 mg, 100 mg, and 200 mg strengths and is intended to be taken as needed, not on a fixed daily schedule.

Navafil belongs to the therapeutic class of Phosphodiesterase type 5 (PDE5) inhibitors, used in the management of erectile dysfunction.

Avanafil is a potent and highly selective inhibitor of phosphodiesterase type 5 (PDE5), the enzyme responsible for the degradation of cyclic guanosine monophosphate (cGMP) in the smooth muscle of the corpus cavernosum of the penis.

Sexual stimulation causes local release of nitric oxide, which activates guanylate cyclase, increasing cGMP levels and producing smooth muscle relaxation and inflow of blood into the corpus cavernosum. By inhibiting PDE5, Avanafil enhances this natural erectile response by prolonging the smooth-muscle-relaxant effect of cGMP; it has no direct effect in the absence of sexual stimulation.

Pharmacokinetics: Avanafil is rapidly absorbed, reaching peak plasma concentration in approximately 30–45 minutes, and can be taken with or without food (a high-fat meal delays but does not markedly reduce overall absorption). It is highly protein bound (>99%), extensively metabolized in the liver primarily via the CYP3A4 enzyme, and has a mean elimination half-life of approximately 6–17 hours. It is excreted mainly in the feces, with a smaller amount in urine.

Navafil is taken orally, by mouth, with a glass of water, with or without food. It should be taken on an as-needed basis, roughly 15–30 minutes before planned sexual activity, and not more than once per day. Navafil is only effective in the presence of sexual stimulation; it will not cause an erection on its own.

Navafil is metabolized mainly by the CYP3A4 enzyme, so drugs that affect this pathway can significantly change Navafil exposure. Clinically important interactions include:

• Organic nitrates (e.g., nitroglycerin, isosorbide) — concurrent use is contraindicated because Navafil potentiates the hypotensive effect of nitrates, risking severe, potentially fatal, blood pressure drops (see Contraindications).
• Guanylate cyclase (GC) stimulators (e.g., riociguat) — concurrent use is contraindicated for the same hypotensive-interaction reason (see Contraindications).
• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir and other HIV protease inhibitors, clarithromycin, telithromycin) — markedly increase Navafil blood levels; concurrent use is contraindicated.
• Moderate CYP3A4 inhibitors (e.g., erythromycin, fluconazole, diltiazem, verapamil, grapefruit juice) — increase Navafil exposure; if co-administration is necessary, the Navafil dose should not exceed 50 mg in 24 hours.
• Alpha-blockers (e.g., tamsulosin, doxazosin) and other antihypertensive medicines — additive blood-pressure-lowering effect that can cause symptomatic hypotension; alpha-blocker therapy should be stable before starting Navafil, generally beginning at the lowest Navafil dose.
• Alcohol — substantial alcohol intake (e.g., more than 3 standard units) with Navafil can increase the risk of orthostatic hypotension (light-headedness, dizziness on standing).
• Other PDE5 inhibitors or ED therapies — combination with Navafil has not been studied and is not recommended.

The most commonly reported side effects of Navafil (occurring in approximately 2% or more of users) include:

• Headache
• Flushing (facial redness/warmth)
• Nasal congestion
• Nasopharyngitis (common cold-like symptoms)
• Back pain
• Dizziness

Less common but more serious effects that require prompt medical attention include:

• Prolonged, painful erection (priapism) lasting more than 4 hours.
• Sudden decrease or loss of vision in one or both eyes.
• Sudden decrease or loss of hearing, sometimes with ringing in the ears (tinnitus) or dizziness.
• Chest pain, palpitations, or symptoms of a heart problem during or after sexual activity.

Most side effects of Navafil are mild to moderate and transient. If any side effect is severe, persistent, or concerning, medical advice should be sought.

Navafil is not indicated for use in women, so there is no established human data on its use during pregnancy or breastfeeding. Animal reproduction studies have not shown evidence of harm to the fetus at exposures several times the maximum recommended human dose, but this has not been confirmed in humans. As Navafil has no approved use in females, it should not be taken by women who are pregnant, planning pregnancy, or breastfeeding.

Before using Navafil, the following precautions should be observed:

• Cardiovascular risk of sexual activity: Sexual activity carries a degree of cardiac risk; a physician should assess a patient's cardiovascular status before prescribing Navafil, particularly in patients with underlying heart disease. Navafil is generally not recommended in patients who have had a heart attack, stroke, life-threatening irregular heartbeat, or uncontrolled high or low blood pressure within the preceding 6 months.
• Priapism: Rarely, PDE5 inhibitors including Navafil can cause prolonged erections lasting more than 4 hours. This is a medical emergency requiring immediate treatment to avoid permanent damage to the penis, and is a particular concern in patients with sickle cell disease, multiple myeloma, leukemia, or an anatomically deformed penis (e.g., Peyronie's disease).
• Vision changes: Sudden decreased or loss of vision in one or both eyes, associated with non-arteritic anterior ischemic optic neuropathy (NAION), has been reported rarely with PDE5 inhibitors. Navafil should be stopped and a physician contacted immediately if this occurs.
• Hearing changes: Sudden decrease or loss of hearing has been reported rarely; Navafil should be discontinued and medical evaluation sought if this occurs.
• Blood pressure effects with alpha-blockers: Concurrent use with alpha-blockers can cause symptomatic low blood pressure (see Interactions).
• Not a protection against STIs: Navafil does not protect against sexually transmitted infections, including HIV.
• Hepatic/renal impairment: Caution advised in mild-to-moderate impairment; not recommended in severe impairment (see Use in Special Populations).

Doses of Navafil higher than recommended may increase the likelihood of side effects such as headache, flushing, dizziness, and hypotension. In case of a suspected overdose of Navafil, seek immediate medical attention or contact a poison control center/emergency services. Treatment of overdose is supportive; because Navafil is highly protein-bound, hemodialysis is unlikely to significantly accelerate its removal from the body. Do not attempt to manage a suspected overdose at home without medical guidance.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Renal Impairment

No dose adjustment of Navafil is needed in mild-to-moderate renal impairment. Navafil is not recommended in patients with severe renal impairment or those requiring dialysis, as it has not been studied in this population.

Hepatic Impairment

No dose adjustment is needed in mild-to-moderate hepatic impairment. Navafil is not recommended in patients with severe hepatic impairment.

Elderly

No overall differences in safety were observed between elderly and younger patients in clinical trials, and no dose adjustment is required based on age alone; however, elderly patients often have more comorbidities and use more concomitant medications, so individual assessment is advised.

Pediatric Use

Navafil is not indicated for use in individuals under 18 years of age; safety and efficacy have not been established in this age group (see Pediatric Uses).

Female Patients

Navafil is not indicated for use in women.

Navafil is intended for on-demand (as-needed) use before sexual activity, not for continuous or fixed daily dosing. There is no fixed treatment duration; it may be used intermittently for as long as erectile dysfunction treatment is needed, under a physician's ongoing guidance, with no more than one dose taken per day.

Avanafil belongs to the drug class of phosphodiesterase type 5 (PDE5) inhibitors, which also includes sildenafil, tadalafil, and vardenafil.

Avanafil selectively inhibits phosphodiesterase type 5 (PDE5), the enzyme that breaks down cyclic GMP (cGMP) in penile smooth muscle. By blocking PDE5, Avanafil allows cGMP levels to remain elevated during sexual stimulation, sustaining smooth muscle relaxation and blood flow into the penis, which helps produce and maintain an erection.

Navafil is not indicated for use in children or adolescents under 18 years of age. Its safety and efficacy in this population have not been established, and it should not be given to pediatric patients.