1 tabl powl. contains 100 mg or 200 mg of celiprolol hydrochloride.
Action:
Cardioselective β-receptor antagonist1. It exhibits partial ß activity2 sympathomimetic, gently expands blood vessels. It lowers both resting and post-exercise blood pressure in patients with hypertension. The effect on the heart rate and minute capacity depends on the previous level of sympathetic tone. Under stress conditions, celiprolol relieves the chronotropic and isotropic response to sympathetic stimulation; during resting, the cardiac dysfunction is revealed. Bioavailability of celiprolol decreases under the influence of food. The pharmacodynamic effect persists for 24 h. It minimally metabolizes. T0,5 is 5-6 hours.
Contraindications:
Hypersensitivity to the components of the preparation. Atrio-ventricular block IIst. and IIIst .. Severe bradycardia. Uncompensated heart failure. Cardiogenic shock. Severe renal failure (creatinine clearance <15 ml / min). A severe form of bronchial asthma. Sick node syndrome (including sinoatrial block). Significant hypotension. Significant failure of peripheral arteries. Untreated phaeochromocytoma. Obstructive airway disease (except when there are clear clinical indications for the use of beta-blockers). The use is not recommended in patients concomitantly taking theophylline and in children.
Precautions:
Particularly cautiously use in elderly patients with impaired renal function (especially in the first week - to establish steady-state plasma celiprolol), impaired liver function, controlled congestive heart failure (when symptoms of decompensation occur, treatment should be discontinued). The drug should be discontinued at least 48 hours before the use of general anesthesia; if continued with celiprolol, particular care should be taken when using general ether, cyclopropane and trichlorethylene for anesthesia. Use with caution in patients with peripheral vascular insufficiency (including Raynaud's syndrome), atrioventricular block Ist, diabetes, hyperthyroidism. If the heart rate decreases to 50-55 beats / min at rest and symptoms associated with bradycardia occur, the dose of celiprolol should be reduced. In patients with psoriasis, use celiprolol only after careful consideration.
Pregnancy and lactation:
Pregnant should not use celiprolol unless its use is necessary. Beta blockers reduce the flow through the placenta, which may lead to intrauterine fetal death, premature delivery and premature birth. The fetus and newborn may experience side effects (especially hypoglycemia and bradycardia), and there is an increased risk of cardiac and pulmonary complications in newborns during the post-natal period. When breastfeeding, the use of celiprolol is not recommended.
Side effects:
Common: headaches and dizziness, drowsiness, nightmares and insomnia (sleep disorders), tremors and a feeling of cold in the extremities; palpitations, bradycardia, significant decrease in blood pressure, including when getting up from a lying position (orthostatic disorders); vomiting, nausea, stomach pain, discomfort; muscle cramps; swoon. Rare: increase in the amount of antinuclear antibodies (although clinical significance is not explained); single and reversible cases of lupus; depression, paraesthesia; Tinnitus; releasing atrioventricular conduction, worsening of heart failure with peripheral edema and / or exercise dyspnoea, Raynaud's disease, worsening of symptoms in patients with peripheral circulatory disorder (intermittent claudication, in patients with Raynaud's syndrome), in susceptible patients exacerbation of the existing atrioventricular block ; allergic pneumonia, bronchospasm, especially in patients with a history of bronchial asthma or asthmatic reactions; diarrhea, constipation; skin symptoms (e.g.itching, redness, rash, pruritus, urticaria, purpura); muscle weakness; decreased libido and impotence (in men). Very rare: hallucinations, psychosis; entanglement; visual disturbances, including sclerosis, dry eye with reduced tear secretion (this should be taken into account in the patient using contact lenses); the occurrence of psoriasis, worsening of the symptoms of the disease, or a rash similar to psoriasis. In addition, there may be an increase in transaminase levels, hypoglycaemia or hyperglycaemia. It may reveal latent diabetes and intensify the already existing one. Beta-blockers can mask the symptoms of hypoglycaemia and thyrotoxicosis
Dosage:
Orally. Adults: The starting dose is 100-200 mg once a day. In the absence of the expected therapeutic effect, the dose can be increased up to 400 mg once a day. In patients with a creatinine clearance of 15-40 ml / min, the dose of celiprolol should be halved.Way of giving. The drug should be taken in the morning, just after waking up, half an hour before a meal, drinking a glass of water.