Index of drugs

Treatment of pulmonary arterial hypertension (PAH) class II and III according to WHO classification, to improve exercise capacity in adults. The medicine has been shown to be effective in the treatment of idiopathic pulmonary arterial hypertension (IPAH) and pulmonary arterial hypertension associated with collagen vascular disease.

1 tabl powl. contains 20 mg tadalafil. The drug contains lactose.

A selective, potent, reversible phosphodiesterase inhibitor of cyclic guanosine monophosphate (cGMP) type 5 (PDE5). Pulmonary arterial hypertension is associated with impaired release of nitric oxide from the vascular endothelium and, consequently, a decrease in cGMP levels in the pulmonary smooth muscle. PDE5 is the dominant type of phosphodiesterase present in the pulmonary blood vessels. Inhibition of PDE5 by tadalafil results in increased cGMP concentration, as a result of which the smooth muscle of the blood vessels relaxes and the pulmonary vasculature widens. The effect of tadalafil on PDE5 is stronger than on other phosphodiesterases. Tadalafil is rapidly absorbed after oral administration and the mean peak plasma concentration is reached on average 4 hours after administration. Food does not affect the rate and extent of absorption of tadalafil. 94% of tadalafil in plasma is associated with proteins. Tadalafil is primarily metabolised by CYP3A4, methylcathechol glucuronide (clinically inactive) is the major metabolite in the bloodstream. Medium T_0,5 is 16 hours. Tadalafil is mainly excreted in the form of inactive metabolites, primarily in the faeces (about 61% of the dose) and to a lesser extent in the urine (about 36% of the dose).

Hypersensitivity to the active substance or to any of the excipients. acute myocardial infarction in the last 90 days. Severe hypotension (<90 / 50mm Hg). The use of tadalafil is contraindicated in patients using organic nitrates in any form. Patients who lost vision in one eye due to non-arteritic anterior ischemic optic neuropathy (NAION) regardless of whether it was related to or not related to previous PDE5 inhibitor exposure.

Tadalafil is not recommended for use in patients (no clinical data available): with clinically significant aortic valve and mitral valve defect; with constrictive pericarditis; with congestive or restrictive cardiomyopathy; with significant left ventricular dysfunction; with life-threatening cardiac arrhythmias; with symptomatic coronary heart disease; with uncontrolled hypertension; with obliterative disease of the pulmonary veins; with known hereditary degenerative changes of the retina, including retinitis pigmentosa; severe renal impairment; with severe cirrhosis. Tadalafil has the property of dilating blood vessels, which may cause a transient decrease in blood pressure. Care should be taken to consider whether adverse effects due to vasodilation may occur in patients with certain underlying medical conditions, such as severe narrowing of the left ventricle outflow pathway, excessive fluid loss, hypotension due to autonomic or hypotensive abnormalities. In men taking PDE5 inhibitors, cases of priapism have been reported; patients should be advised to immediately seek medical attention if the erection lasts for 4 hours or more. If you do not receive immediate treatment for priapism, you may damage the member's tissues and permanently lose potency. The drug should be used with caution in patients with anatomical distortion (such as bending, fibrosis or Peyronie's disease) or in patients with conditions that may predispose to priapism (such as sickle cell disease, multiple myeloma, leukemia). The safety and efficacy of the medicine in children and adolescents has not yet been established.The drug contains lactose - patients with rare hereditary problems of galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose should not take this drug.

As a precautionary measure, avoid using it during pregnancy. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal / fetal development, parturition or postnatal development. Tadalafil is excreted in breast milk, a danger to a breast-fed baby can not be ruled out. The drug should not be used during breastfeeding.

Very common: headache, flushing of the face, nasopharyngeal inflammation (including nasal and sinus congestion, and rhinitis), nausea, indigestion (including abdominal pain or abdominal discomfort), muscle pain, back pain, limb pain (including ailments within the limb). Common: hypersensitivity reactions, syncope, migraine, blurred vision, chest pain, palpitations, hypotension, epistaxis, vomiting, gastro-oesophageal reflux, rash, increased uterine bleeding, face edema, chest pain. Uncommon: convulsions, transient amnesia, sudden cardiac death, tachycardia, hypertension, urticaria, hyperhidrosis, priapism. Not known: angioneurotic edema, stroke (including haemorrhagic events), non-arteritic anterior ischemic optic neuropathy, retinal vascular occlusion, visual field defects, sudden hearing loss, unstable angina, ventricular arrhythmias, myocardial infarction, Stevens-Johnson syndrome , exfoliative dermatitis, prolonged erection.

Orally. Treatment should be initiated and supervised only by a doctor who has experience in the treatment of pulmonary arterial hypertension. Adults. The recommended dose is 40 mg (2 x 20mg) taken daily for any meal. Elderly patients do not need to adjust their dosage. In patients with mild or moderate renal impairment, a starting dose of 20mg once a day is recommended. Depending on the patient's effectiveness and tolerability, the dose may be increased to 40 mg once a day. Tadalafil is not recommended for people with severe kidney problems. In patients with mild to moderate cirrhosis (Child-Pugh Class A and B), a single 10-mg dose may be considered for a starting dose of 20 mg once a day. When starting treatment with tadalafil, the prescribing physician should carefully assess the benefit-risk ratio of the patient. In patients with severe cirrhosis (Child-Pugh Class C), it is not recommended.