- Tadalafil 10 mg

- Pharmaceutical form: Tablets/4 Tabs

- Therapeutic category: Urogenital drug

Properties:

Tadalafil is a potent selective, reversible inhibitor of cyclic guanosine monophosphate (oGMP) -specific phosphodiesterase type 5 (PDE5). When sexual stimulation causes the local release of nitric oxide, inhibition of PDE5 by tadalafil produces increased levels of oGMP in the corpus cavernosum. This results in smooth muscle relaxation and inflow of the blood into penis tissues, thereby producing an erection.

 

Pharmokineticks:

Tadalafil is rapidly absorbed after oral administration and the mean maximum observed plasma time of 2 hours after dosing. The rate and extent of absorption of tadalafil are not influenced by food. The mean volume of distribution is approximately 63 L, 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. Tadalafil is excreted predominantly as inactive metabolites, mainly in the faeces (approximately 61% of the dose) and to a lesser extent in the urin (approximately 36 % of the dose). 

The half-life of tadalafil is 17.5 hours and clinical studies suggest significant activity 24 -36 hours post-dosing.

 

Indications:

Tadalafil is effective in the treatment of men with erectile dysfunction. ALEGRA effect starts to become active about 16 minutes after the drug has been taken already and lasts up to 36 hours longer, and causes no visual side effects. Tadalafil has no effect in the absence of sexual stimulation.

 

Contraindications:

- Tadalafil was shown to augment the hypotensive effects of nitrates. 

- ALEGRA should not be used in patient who are using any form of organic nitrate is contraindicated. 

- ALEGRA should not be used in patient with a known hypersensitivity to tadalafil or to any of the excipients. 

- Patient with unstable angina or angina occurring during sexual intercourse.

- Patient with uncontrolled arrhythmias hypotension.

- Patient with severe renal insufficiency (creatinine clearance ≤ 30 ml/min). 

- Patient with severe hepatic insufficiency (child-Pugh Class C).

- Dosage adjustments are not required in patient with mild or moderate renal or hepatic impairment. 

- Patients who or have had a recent heart attack. 

- Recent stroke during the last six months preceding the use of ALEGRA

- Low blood pressure (< 90/50mmHg) or uncontrolled high blood pressure.

- You should not use ALEGRA together with any other treatments for erectile dysfunction. 

- ALEGRA is not intended for use by women or by children under the age of 18.

 

Side Effects:

The most commonly reported side effects with ALEGRA were headache (14%), Pyrosis or heartburn (10%), muscle pain, upset stomach following meals, and back pain. These side effects were mild in nature and went away within a few hours after use.

Drugs and Interaction:

- Ketoconazole, increased Tadalafil AUC by 107%, while Rifapicin, reduced Tadalafil AUC by 88%.

- Simultaneous administration of an antacid and Tadalafil reduced the apparent rate of absorption of Tadalafil without altering exposure (AUC) to Tadalafil. 

- Tadalafil was shown to augment the hypotensive effects of nitrates. 

- Tadalafil does not inhibit or induce CYP450 isoforms, including CYP3A4, CYP1A2, CYP2D6, CYP2E1, and CYP2C9. 

- Tadalafil had no clinically significant effect on exposure (AUC) to S-warfarin or R-Warfarin. 

- Tadalafil did not potentiate the increase in bleeding time caused by acetyl salicylic acid. 

- Alcohol concentrations were not affected by co-administration with Tadalafil. 

- Tadalafil had no clinically significant effect on the pharmacokinetics or pharmacodynamics of theophylline.

Warnings:

- Doctor must carefully examine patients cardiac state before prescription this medicament because sexual activity carries a potential cardiac risk for patient with cardiovascular diseases. 

- Caution should be exercised when ALEGRA is administered to patients with galactose heredity intolerance . 

- ALEGRA should be used with caution in patients who have conditions that might predispose them to priapism such as sickle cell anaemia, multiple myeloma, or leukaemia or in patients with anatomical deformation of the penis. 

- Effects on ability to drive and use machines: patients should be aware of how they react to ALEGRA before driving or operating machinery.

Overdose:

Single doses of up to 500 mg have been given to health subjects and multiple daily doses up to 100 mg have been given to patients. Adverse events were similar to those seen at lower doses. 

In cases of overdoses, standard supportive measures should be adopted as required.

Dosage:

If you have chest pain, or other heart related symptoms during sex, seek immediate medical help. 

You should not take ALEGRA more than once a day. 

Tadalafil has no effect in the absence of sexual stimulation. 

10 mg to be taken before sexual activity with or without food. 

The recommended starting dose is one 10 mg tablet before sexual activity. If the effect of this dose is too weak your doctor may increase the dose to 20 mg.

Storage:

Do not store above 30 ºC.