Buy Avanafil Online
Avanafil is a PDE-5 inhibitor approved for the treatment of erectile dysfunction.
Avanafil is a PDE-5 inhibitor approved for the treatment of erectile dysfunction. The advantage of avanafil is the very rapid onset of action compared to other PDE-5 inhibitors. Sexual stimulation is required for effectiveness.
Avanafil is a PDE-5 inhibitor indicated for the treatment of erectile dysfunction. Avanafil is on the US market under the brand name Stendra
Avanafil is intended for oral use.
The physiological process underlying the vasodilation and thus the increased blood flow or erection is the release of nitric oxide (NO) by vascular endothelial cells. From there, NO diffuses to nearby vascular smooth muscle cells and activates soluble guanylate cyclase, which converts guanosine triphosphate (GTP) to cyclic guanosine monophosphate (cGMP), the main effector of the system. In the penis, the release of NO during sexual stimulation leads to relaxation of the smooth vessels of the corpus cavernosum, resulting in vasocongestion and a sustained erection.
Avanafil inhibits phosphodiesterase-5 (PDE-5), which is responsible for the breakdown of cGMP. This leads to increased cGMP levels, which allows for vasodilation and thus increased blood flow in the penis. Avanafil’s mechanism of action kicks in when NO is released in conjunction with sexual stimulation.
- Avanafil is rapidly absorbed.
- Peak plasma concentrations are reached within 0.5 to 0.75 hours after oral administration in the fasted state.
- When avanafil is taken with a high-fat meal, the rate of absorption decreases with a mean Tmax delay of 1.25 hours and a mean Cmax decrease of 39%.
- There were no effects on the level of exposure (AUC).
- The clinical significance of these small changes in C max is considered minimal.
- Avanafil is approximately 99% bound to plasma proteins.
- Protein binding is independent of total drug concentration, age, and renal and hepatic function.
- No accumulation in plasma was detected when the drug was taken at a dose of 200 mg twice daily for 7 days.
- Measurements of avanafil in the semen of healthy subjects, taken 45 to 90 minutes after application of the drug, indicated that less than 0.0002% of the applied amount may appear in the semen.
- Avanafil is primarily metabolised by the isoenzymes CYP3A4 (major route) and CYP2C9 (minor route).
- The plasma concentrations of the main circulating metabolites M4 and M16 are approximately 23% and 29% of the parent substance.
- The M4 metabolite exhibits a phosphodiesterase selectivity profile similar to that of avanafil and an in vitro PDE5 inhibitory potential that is 18% of avanafil.
- M4 accounts for about 4% of the total pharmacological activity.
- The metabolite M16 is inactive towards the PDE5.
- Avanafil is extensively metabolized in humans.
- After oral administration, avanafil is excreted primarily as metabolites in the faeces (about 63% of the administered oral dose) and to a lesser extent in the urine (about 21% of the administered oral dose).
Avanafil is recommended at a dose of 100 mg as needed approximately 15 to 30 minutes before sexual activity. Depending on individual effectiveness and tolerability, the dose can be increased to a maximum of 200 mg or reduced to 50 mg. Avanafil should be taken no more than once a day.
The most common side effects associated with Avanafil use are:
- feeling hot
- nasal congestion
- Sinus secretion congestion (blockage of the sinuses)
- back pain
Interactions with the following compounds may occur when using Avanafil:
- Alpha-blockers: Increased risk of symptomatic hypotension.
- CYP3A4 Inhibitors: Concomitant use of avanafil with strong CYP3A4 inhibitors such as ketoconazole or ritonavir is contraindicated
- Other PDE-5 inhibitors or other therapies for erectile dysfunction: a combination should not be used
- Alcohol: The likelihood of symptomatic hypotension occurring is increased.
- Nitrates: Avanafil enhances the hypotensive effects of nitrates.
- Drugs that lower systemic blood pressure: Because avanafil is a vasodilator, it may lower systemic blood pressure. With concomitant use, the additive effects may result in symptomatic hypotension (e.g. dizziness, lightheadedness, syncope or presyncope).
- Inducers of CYP3A4 (eg, bosentan , carbamazepine , efavirenz , phenobarbital , and rifampicin ). Concomitant use is not recommended as it may reduce the effectiveness of avanafil.
- Riociguat: additive systemic antihypertensive effect. Simultaneous use is contraindicated.
Avanafil should not be used in the following circumstances:
- Hypersensitivity to the active substance
- Taking organic nitrates or nitric oxide donors (such as amyl nitrite )
- Use of guanylate cyclase stimulators such as riociguat
- Patients who have had a heart attack, stroke, or life-threatening arrhythmia within the last 6 months
- Persistent hypotension (blood pressure <90/50 mmHg) or hypertension (blood pressure >170/100 mmHg)
- Unstable angina, angina during intercourse, or congestive heart failure (congestive heart failure) NYHA Stage 2 or greater
- Severe hepatic impairment (Child-Pugh stage C)
- Severe renal impairment (creatinine clearance < 30 mL/min)
- Patients suffering from loss of vision in one eye due to non-arteritic anterior ischemic optic neuropathy (NAION), whether or not this episode is related to previous exposure to a PDE-5 inhibitor
- Hereditary degenerative retinal diseases
- Use of strong CYP3A4 inhibitors such as ketoconazole, ritonavir, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, saquinavir, and telithromycin
Avanafil has a minor influence on the ability to drive and use machines. Because dizziness and visual disturbances have been reported in clinical trials with the use of avanafil , patients should be aware of how they react before driving or using machines.
Before starting treatment for erectile dysfunction, the doctor should assess the patient’s cardiovascular status, since sexual activity is associated with some risk to the heart.
If the erection lasts four hours or more after taking avanafil (priapism), a doctor should be consulted immediately. If priapism is not treated promptly, it can result in damage to penile tissue and permanent loss of potency.
Visual disturbances and cases of nonarteritic anterior ischemic optic neuropathy (NAION) can occur when taking PDE-5 inhibitors. If you experience any effects on your vision, you should stop taking Avanafil and see a doctor.
PDE-5 inhibitors by themselves have no effect on platelet aggregation, but at supratherapeutic doses, they can potentiate the anti-aggregation effect of the nitric oxide donor sodium nitroprusside in vitro. In humans, PDE-5 inhibitors alone or in combination with acetylsalicylic acid appear to have no effect on bleeding time.
Patients should be cautioned to stop taking PDE-5 inhibitors, including avanafil, and seek immediate medical attention in the event of a sudden decrease or loss of hearing.
Other active ingredients for the treatment of erectile dysfunction are:
- Aviptadil in combination with phentolamine ( Invicorp )
All PDE5 inhibitors are indicated for the treatment of erectile dysfunction. Sildenafil and tadalafil can also be used to treat pulmonary hypertension and tadalafil to treat the benign prostatic syndrome.
Molar mass:483.95 g mol -1
Can patients get Avanafil over the counter?
PDE-5 inhibitors require a prescription. Therefore, patients receive avanafil only by prescription. During an online consultation, a specialist can determine whether the drug is suitable and issue an avanafil prescription.
What is special about Avanafil?
Avanafil is considered to be significantly better tolerated than the first-generation PDE-5 inhibitors. Since avanafil appeared much later than sildenafil or tadalafil, the desired effect could be researched more specifically. The active ingredient is characterized by a particularly rapid onset of action and few side effects.
Is Avanafil generic?
no, Since the active ingredient has only recently been approved, patent rights still exist for the active ingredient. Generics can be approved from 2024 at the earliest.