Uro-genital drugs
Tadalafil 20 mg
4Coated Tablets
T37
708/2004
30/12/2004
Excipients | Crosscarmellose sodium,Hyproxypropyl cellulose , Hypromellose , Iron oxide , Lactose monohydrate , Magnesium stearate , Microcreystalline cellulose, Sodium lauryl sulfate , Talc , Titanium dioxide , Triacetin . |
Mechanism Of Action | 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. The vascular relaxation in smooth muscles of the prostate and the bladder increases blood perfusion which may be the mechanism by which symptoms of benign prostatic hyperplasia are reduced. |
INDICATIONS | • TADALAFIL is indicated for Treatment of erectile dysfunction in adult males. • In order for Tadalafil to be effective for the treatment of erectile dysfunction, sexual stimulation is required. • 5 mg only: Treatment of the signs and symptoms of benign prostatic hyperplasia in adult males. • TADALAFIL is not indicated for use by women |
CONTRAINDICATIONS | • Hypersensitivity to the active substance or to any of the excipients. • Tadalafil augments the hypotensive effects of nitrates. Therefore, administration of the drug to patients who are using any form of organic nitrate is contraindicated. • The drug must not be used in men with cardiac disease for whom sexual activity is inadvisable. Physicians should consider the potential cardiac risk of sexual activity in patients with pre-existing cardiovascular disease. • The use of Tadalafil is contraindicated in patients with: Myocardial infarction within the last 90 days, Heart failure or stroke in the last 6 months. Unstable angina or angina occurring during sexual intercourse. Uncontrolled arrhythmias, hypotension (<90/50mmHg), or uncontrolled hypertension. • The drug is contraindicated in patients who have loss of vision in one eye because of non-arteritic anterior ischemic optic neuropathy (NAION), regardless of whether this episode was in connection or not with previous PDE5 inhibitor exposure. |
Side EFFECTS | The most common adverse reactions are headache, flushing, nasal congestion, dyspepsia, gastro-oesophageal reflux, back pain, myalgia, and pain in extremity. |
WARNINGS | • A medical history and physical examination should be undertaken to diagnose erectile dysfunction or benign prostatic hyperplasia and determine potential underlying causes, before pharmacological treatment is considered. 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. • Serious cardiovascular events, including myocardial infarction, sudden cardiac death, unstable angina pectoris, ventricular arrhythmia, stroke, transient ischaemic attacks, chest pain, palpitations and tachycardia, have been reported. Most of the patients in whom these events have been reported had pre-existing cardiovascular risk factors. • Prior to initiating treatment with Tadalafil for benign prostatic hyperplasia patients should be examined to rule out the presence of carcinoma of the prostate. • Visual defects and cases of NAION have been reported. The patient should be advised that in case of sudden visual defect, he should stop taking the drug and consult a physician immediately. • Due to increased Tadalafil exposure in renal and hepatic impairment, dose adjustments may be required. • Patients who experience erections lasting 4 hours or more should be instructed to seek immediate medical assistance. • The drug should be used with caution in patients with anatomical deformation of the penis or in patients who have conditions which may predispose them to priapism (such as sickle cell anaemia, multiple myeloma, or leukaemia). • Patients should not take the drug in combination with other PDE5 inhibitors or other treatments for erectile dysfunction. • A decrease in sperm concentration may be seen in some men taking the drug. • The drug contains lactose, patients with galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this drug. • The drug has negligible influence on the ability to drive or use machines. |
DRUG INTERACTIONS | • CYP3A4 inhibitors, such as Ketoconazole, Ritonavir and other protease inhibitors, Erythromycin, Clarithromycin, Itraconazole, and grapefruit juice, should be co-administered with caution, as they would be expected to increase plasma concentrations of Tadalafil. • Inducers of CYP3A4, such as Rifampicin, Phenobarbital, Phenytoin, and Carbamazepine, may decrease plasma concentrations of Tadalafil. • Administration of Tadalafil to patients using any form of organic nitrate is contraindicated, at least 48 hours should have elapsed after the last dose of Tadalafil before nitrate administration is considered and under close medical supervision. Co-administration of Doxazosin and Tadalafil increases the blood pressure-lowering effect of Doxazosin. Caution should be exercised when using Tadalafil with any alpha-blocker, notably in the elderly, and treatments should be initiated at minimal dose and progressively adjusted. Appropriate advice should be given to patients regarding a possible decrease in blood pressure when they are treated with antihypertensives. • Caution should be exercised when Tadalafil is co-administered with 5-alpha reductase inhibitors. • When Tadalafil is administered with Theophylline there may be a small increase in heart rate. • Tadalafil increases in the oral bioavailability of Ethinylestradiol and Terbutaline. • In co-administration with alcohol (0.7g/kg) postural dizziness and orthostatic hypotension were observed, in some subjects. but were not observed with lower doses of alcohol |
Dosage And Administration | • Erectile dysfunction in adult Men: the recommended dose is 10 mg taken at least 30 minutes prior to anticipated sexual activity with or without food. If 10 mg does not produce an adequate effect, 20 mg might be tried. The maximum dose frequency is once per day. In patients who anticipate a frequent use (once daily regimen): the recommended dose is 5 mg taken once a day at approximately the same time of day. The dose may be decreased to 2.5 mg once a day based on individual tolerability. • Benign prostatic hyperplasia in adult men: The recommended dose is 5 mg, taken at approximately the same time every day with or without food. For adult men being treated for both benign prostatic hyperplasia and erectile dysfunction the recommended dose is also 5 mg taken at approximately the same time every day. Patients who are unable to tolerate Tadalafil 5 mg should consider an alternative therapy as the efficacy of 2.5 mg for the treatment of benign prostatic hyperplasia has not been demonstrated. • Dose adjustments are not required in elderly patients and diabetic patients. • Dose adjustments are not required in patients with mild to moderate renal impairment. For patients with severe renal impairment, 10 mg is the maximum recommended dose for on-demand treatment and once-a-day dosing of Tadalafil is not recommended. • The recommended dose for on-demand treatment in hepatic impairment is 10 mg taken prior to anticipated sexual activity with or without food. A careful individual benefit/risk evaluation should be undertaken by the prescribing physician if prescribed in Once-a-day dosing in hepatic Impairment and in patients with severe hepatic impairment both for the treatment of erectile dysfunction and benign prostatic hyperplasia, as it has not been evaluated |
OVERDOSE | In high doses, adverse events were similar to those seen at lower doses. In cases of overdose, standard supportive measures should be adopted as required. Haemodialysis contributes negligibly to Tadalafil elimination. |
Storage Conditions | Store below 30° C , in A dry place Out of reach of children |