Tadalis(Tadalafil)

Therapeutic Group: Urological

Presentation

Tadalis 10 tablet: Each tablet contains 10 mg of Tadalafil INN.

Description

Tadalafil is a 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.

CLINICAL PHARMACOLOGY

Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) enhances erectile function by increasing the amount of cGMP. Tadalafil inhibits PDE5. Because sexual stimulation is required to initiate the local release of nitric oxide, the inhibition of PDE5 by Tadalafil has no effect in the absence of sexual stimulation. The effect of PDE5 inhibition on cGMP concentration in the corpus cavernosum and pulmonary arteries is also observed in the smooth muscle of the prostate, the bladder and their vascular supply. The mechanism for reducing BPH symptoms has not been established.

Indications

Treatment of erectile dysfunction, benign prostatic hyperplasia and erectile dysfunction with benign prostatic hyperplasia.

Dosage & Administration

Erectile dysfunction:
For oral use. In order for Tadalafil to be effective, sexual stimulation is required.
Use in adult men
The recommended dose is 10 mg taken prior to anticipated sexual activity and without regard to food. In those patients in whom Tadalafil 10 mg does not produce an adequate effect, 20 mg might be tried. It can be taken from 30 minutes to 12 hours prior to sexual activity. Efficacy of Tadalafil may persist up to 24 hours post-dose. The maximum recommended dosing frequency is once per day.
Benign prostatic hyperplasia:
5 mg, taken at approximately the same time every day.
Erectile dysfunction with benign prostatic hyperplasia:
5 mg, taken at approximately the same time every day.
Use in elderly men:
Dosage adjustments are not required in elderly patients.
Use in men with impaired renal function:
There are no available data about the administration of doses higher than 10 mg of Tadalafil to patients with renal impairment.
Use in men with impaired hepatic function:
There are no available data about the administration of doses higher than 10 mg of Tadalafil to patients with hepatic impairment.
Use in men with diabetes:
Dosage adjustments are not required in diabetic patients.
Use in children:
Tadalafil should not be used in individuals below 18 years of age.

Side Effects

The most commonly reported adverse reactions are headache, dizziness, flushing and dyspepsia, nasal congestion, back pain, myalgia, swelling of eyelids is uncommon adverse reactions. The adverse events reported with Tadalafil were transient, and generally mild or moderate.

Precautions

• Prior to initiating any treatment for erectile dysfunction, physicians should consider the cardiovascular status of their patients, since there is a degree of cardiac risk associated with sexual activity.
• Tadalafil has vasodilator properties, resulting in mild and transient decreases in blood pressure
• There is limited clinical data on the safety of Tadalafil in the following groups; if prescribed, a careful individual benefit/risk evaluation should be undertaken by the prescribing physician:
• Patients with severe renal insufficiency
• Patients with severe hepatic insufficiency
• Tadalafil should not be administered to patients with hereditary problems of galactose intolerance.
• The safety and efficacy of combinations of Tadalafil and other treatments for erectile dysfunction have not been studied. Therefore, the use of such combinations is not recommended.
• Caution should be exercised when Tadalafil is administered to patients with anatomical deformation of the penis.
• Patients who suffer from problems that increase the possibility of Priapism (sickle-cell anemia, multiple myeloma, leukemia) should use this product with caution.

Use in Pregnancy & Lactation

Tadalafil is not indicated for use by women. There are no studies of Tadalafil in pregnant women.