SAI AVANA is an effective treatment option for males suffering from ED. Its main advantage over the other available PDE5 inhibitors is its faster onset of action (its onset of action is 15-30 minutes compared to about 60 minutes for the others). This allows for relatively little planning needed before the initiation of sexual activity, which is beneficial for its users. Additionally, all other agents in this class are also brand only so the aspect of cost should be comparable;
Mechanism of Action
Nitric oxide increases levels of cGMP, which relaxes smooth muscles in corpus cavernosum to allow inflow of blood to achieve and maintain penile erection. Avanafil, a selective inhibitor ofcGMP-specific phosphodiesterase type 5 (PDE-5), enhances the effect of nitric oxide by inhibiting PDE-5, which degrades cGMP in the corpus cavernosum. Sexual stimulation is required to initiate the local release of nitric oxide. Avanafil has no direct relaxant effect on corpus cavernosum
Sai Avana 100
Each film coated tablet contains:
Avanafil............................100mg
Excipients..............................q.s.
SAI AVANA is an effective treatment option for males suffering from ED. Its main advantage over the other available PDE5 inhibitors is its faster onset of action (its onset of action is 15-30 minutes compared to about 60 minutes for the others). This allows for relatively little planning needed before the initiation of sexual activity, which is beneficial for its users. Additionally, all other agents in this class are also brand only so the aspect of cost should be comparable;
Mechanism of Action
Nitric oxide increases levels of cGMP, which relaxes smooth muscles in corpus cavernosum to allow inflow of blood to achieve and maintain penile erection. Avanafil, a selective inhibitor ofcGMP-specific phosphodiesterase type 5 (PDE-5), enhances the effect of nitric oxide by inhibiting PDE-5, which degrades cGMP in the corpus cavernosum. Sexual stimulation is required to initiate the local release of nitric oxide. Avanafil has no direct relaxant effect on corpus cavernosum
Pharmacokinetics
Avanafil is cleared predominantly by hepatic metabolism, mainly by the CYP3A4 enzyme and to a minor extent by CYP2C. The plasma concentrations of the major circulating metabolites, M4 and M16, are approximately 23% and 29% that of the parent compound, respectively. The M4 metabolite has an in vitro inhibitory potency for PDE5 18% of that of avanafil and M4 accounts for approximately 4% of the pharmacologic activity of avanafil. The M16 metabolite was inactive against PDE5.
After oral administration, avanafil is excreted as metabolites predominantly in the feces (approximately 62% of administered oral dose) and to a lesser extent in the urine (approximately 21% of the administered oral dose)
Contraindications
Nitrates: Consistent with its known effects on the nitric oxide/cGMP pathway, avanafil may potentiate the hypotensive effects of organic nitrates and nitrites. Patients receiving nitrates in any form are not to receive avanafil. This includes any patient who receives intermittent nitrate therapies. In a life-threatening situation, nitrate therapy should only be considered if at least 12 hours has elapsed since the last dose of avanafil; medical supervision is warranted.
Hypersensitivity Reactions: Avanafil is contraindicated in patients with a known hypersensitivity to any component of the tablet. Hypersensitivity reactions have been reported, including pruritis and eyelid swelling.
Precautions
Colour Discrimination: May cause problems with patients ability to discriminate between colour. This appears to be a dose-related impairment. Use caution in patients with retinitis pigmentosa; a minority have genetic disorders of retinal phosphodiesterases (no safety information available).
Hearing Loss: Sudden decrease or loss of hearing has been reported rarely; hearing changes may be accompanied by tinnitus and dizziness. A direct relationship between therapy and hearing loss has not been determined.
Hypotension: Drops in blood pressure may occur due to avanafils vasodilatory properties. Use with caution in patients with left ventricular outflow obstruction (aortic stenosis or hypertrophic obstructive cardiomyopathy). These patients may be more sensitive to hypotensive actions.
Priapism: Has been reported (rarely) with use. Instruct patients to seek immediate medical attention if erection persists for greater than 4 hours. Use with caution in patients
who have conditions which may predispose them to priapism (sickle cell anemia, multiple myeloma, leukemia).
Anatomical Penis Deformation: Use with caution in patients with anatomical deformation of the penis (angulation, cavernosal fibrosis, or Peyronie's disease).
Bleeding Disorders: Use with caution in patients with bleeding disorders; safety and efficacy have not been established
Hepatic Impairment: Safety and efficacy have not been studied in patients with severe hepatic impairment (Child-Pugh class C); therefore, use in these patients is not recommended.
Peptic Ulcer Disease: Use with caution in patients with active peptic ulcer disease; safety and efficacy have not been established
Renal Impairment: Safety and efficacy have not been studied in patients with severe renal impairment or end-stage renal disease requiring dialysis, therefore, use in these patients is not recommended.
Adverse Effects
Headache , Flushing ECG abnormal Dizziness Back pain Nasopharyngitis Nasal congestion
Upper respiratory infection
Abdominal discomfort Angina Arthralgia Balanitis Bronchitis
Color vision change, Urinary tract infection Vertigo Vision loss (temporary or permanent)Vomiting, Wheezing
Drug Interactions
Nitrates
If avanafil is co-administered with an alpha-blocker, patients should be stable onalpha-blocker therapy prior to initiating treatment with avanafil, and initiate avanafil therapy with 50 mg dose
Dosing/Administration
Adult Dosing
Recommended starting dose of avanafil is 100 mg orally as needed 30 minutes prior to sexual activity. Maximum frequency of use is once daily. Use the lowest effective dose. Based on clinical response, the dose may be decreased to 50 mg or increased to a maximum 200 mg
Pediatrics
Use of avanafil is not indicated in pediatric patients under the age of 18. Safety and efficacy have not been established in this population
Elderly
No dosage adjustment needed. Refer to adult dosing
Pregnancy
Pregnancy Category C. Based on data from animal reproduction studies, avanafil is predicted to have a low risk for major developmental abnormalities in humans. Avanafil is not indicated for use in women. There are no adequate and well- controlled human studies of avanafil in pregnant women
Lactation
Avanafil is not indicated for use in females and is therefore not recommended duringbreast-feeding. It is not known if avanafil is excreted in human breast milk
Overdose
Single doses up to 800 mg have been given to healthy subjects, and multiple doses up to 300 mg have been given to patients. In cases of overdose, standard supportive measures should be adopted as required. Renal dialysis is not expected to accelerate clearance because avanafil is highly bound to plasma proteins and is not significantly eliminated in the urine