Aseel® 20
Treatment of erectile dysfunction

Pharmacodynamic properties:-

  • Tadalafil is a potent, selective, reversible inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). When sexual stimulation causes the local release of nitric oxide, inhibition of PDE5 by Tadalafil produces increased levels of cGMP in the corpus cavernosum. This results in smooth muscle relaxation and inflow of blood into the penile tissues, thereby producing an erection. Tadalafil has no effect in the absence of sexual stimulation. 
  • Tadalafil administered to healthy subjects produced no significant difference compared to placebo in supine systolic and diastolic blood pressure, or in standing systolic and diastolic blood pressure, and no significant change in heart rate. 
  • There were no clinically relevant effects on sperm concentration, sperm count, motility or morphology after daily doses of  10 mg and 20 mg for 6 months. 

Pharmacokinetic properties:- 

  • Tadalafil is readily absorbed after oral administration and the mean maximum observed plasma concentration (Cmax) is achieved at a median time of 2 hours after dosing. 
  • The rate and extent of absorption of Tadalafil are  not influenced by food, thus Tadalafil may be taken with or without food. The time of dosing (morning versus evening) had no clinically relevant effects on the rate and extent of absorption. 
  • The mean volume of distribution is approximately 63 liters, indicating that Tadalafil is distributed into tissues. At therapeutic concentrations, 94% of Tadalafil in plasma is bound to proteins. Protein binding is not affected by impaired renal function. 
  • Less than 0.0005% of the administered dose appeared in the semen of healthy subjects. 
  • Tadalafil is predominantly metabolized by the cytochrome P450 (CYP3A4) isoform.
  • The mean oral clearance for Tadalafil is 2.5 L/hr and the mean half-life is 17.5 hours in healthy subjects. 
  • Tadalafil is excreted predominantly as inactive metabolites, mainly in the faeces (approximately 61% of the dose) and to a lesser extent in the urine (approximately 36% of the dose). 

Each film-coated tablet of  Aseel® 20 contains:

  • Tadalafil     20 mg

Each film-coated tablet of  Aseel® 10 contains:

  • Tadalafil     10 mg
  • Aseel® is indicated for treatment of erectile dysfunction
  • Aseel® is contraindicated in anyone taking organic nitrates as it may potentiate their hypotensive effects. 
  • Hypersensitivity to any component of the tablet. 
  • Aseel® is principally metabolized by CYP3A4; a selective inhibitor of CYP3A4, Ketoconazole increased tadalafil AUC by 107% and a CYP3A4 inducer, Rifampicin, reduced tadalafil AUC by 88% relative to the AUC values for Tadalafil alone. 
  • Simultaneous administration of an antacid (magnesium hydroxide/aluminum hydroxide) and Aseel® reduce the apparent rate of absorption of Tadalafil without altering exposure (AUC) to Tadalafil. 
  • Aseel® is not indicated for use in women. 
  • The most common side effects are headache and indigestion. 
  • less commonly reported side effects are back pain, muscle aches, flushing and nasal congestion. 

(These side effects usually go away after few hours).

Over dose:- 

  • Single doses of up to 500 mg have been given to healthy subjects, and multiple daily doses up to 100 mg have been given to patients. Adverse effects were similar to those seen at lower doses.
  • In cases of overdose, standard supportive measures should be adopted as required

Effects on ability to drive and use machines:-

  • Patients should be aware of how they react to Aseel®, before driving or operating machinery. 

  Use in adult men: 

  • Aseel® is given orally in a usual dose of 10 mg at least 30 minutes before sexual intercourse and without regard to food, the dose may be increased to 20 mg or decreased to 5 mg if necessary.

- Or as directed by physician.

  • Efficacy of Aseel® may persist up to 24 hours post dose.
  • The maximum recommended dosing frequency is once per day.

Use in elderly men:

  • Dosage adjustment are not required in elderly patients. Dosage recommendations described in use in adult men apply to elderly men. 
  • Dosage adjustments are not required in patients with mild or moderate renal impairment, hepatic impairment and in diabetic patients.
  • Aseel® should not be used in individuals below 18  years of age. 

 Aseel® should be used with caution in patients who have conditions 
  such as:

  • Patients with severe cardiovascular disease.
  • Patients with severe renal insufficiency.
  • Patients with severe hepatic insufficiency.
  • Patients who have conditions that might predispose them to priapism (such as sickle cell anaemia, multiple myeloma or leukaemia).
  • Patients with anatomical deformation of the penis
  • Blister of 2 tablets, pack of  two blisters. 
  • Store in the original package , at a temperature not exceeding  30o C.