Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):ONLS
АТХ:
C.07.A.B.04 Acebutolol
Pharmacodynamics:Has antianginal, antiarrhythmic, hypotensive effect. Blocks beta1-adrenoreceptors, possesses sympathomimetic activity and membrane-stimulating properties. Normalizes systolic and diastolic blood pressure, keeping the heart rate and the minute volume of the heart.
Antihypertensive effect is manifested due to the inhibition of the central nervous system, reduction of cardiac output, suppression of synthesis and activity of renin, reduction of peripheral sympathetic influences due to restoration of sensitivity of baroreceptors.
Antiarrhythmic action is due to the suppression of the automatism of the sinus node and the elongation of the refractory period.
Pharmacokinetics:After ingestion, 87% is absorbed in the gastrointestinal tract. Bioavailable in 40%, because with the "first pass" through the liver turns into an active metabolite - diacetolol.
The maximum concentration of acebutolol in the blood plasma is achieved after 2.5 hours, diacetolol - after 3.5 hours. Connection with plasma proteins: acebutolol - by 26%; diacetolol - by 9%.
Half-Elimination (half-life) of the drug is 12 hours and 16 hours respectively.It penetrates through the histohematological barriers, including through the placental barrier. It enters the breast milk. Elimination of the gastrointestinal tract by 60% (acebutolol) and kidneys - by 40% (diacetolol).
Indications:It is used for myocardial infarction, hypertrophic cardiomyopathy, mitral valve prolapse, thyrotoxicosis.
IX.I10-I15.I10 Essential [primary] hypertension
IX.I20-I25.I20.90 Angina pectoris unspecified with hypertension
IX.I20-I25.I20.10 Angina with documented spasm with hypertension
IX.I10-I15.I15 Secondary Hypertension
IX.I20-I25.I20.8 Other forms of angina pectoris
IX.I20-I25.I25.8 Other forms of chronic ischemic heart disease
IV.E00-E07.E05 Thyrotoxicosis [hyperthyroidism]
Contraindications:Cardiogenic shock, atrioventricular block II-III degree, bradycardia, chronic heart failure - resistant to the action of cardiac glycosides, bronchial asthma, renal and hepatic insufficiency.
Individual intolerance.
Carefully:Chronic bronchitis with asthmatic component, obliterating arterial diseases, atrioventricular block I degree, disturbance of water-electrolyte balance.
Pregnancy and lactation:Pregnancy and lactation: recommendations for Food and Drug Administration (US Food and Drug Administration) - Category B. Not applicable in pregnancy and lactation.
Dosing and Administration:It is taken orally at the initial dosage of 200 mg twice a day. If necessary, the dose slowly rises to 1200 mg per day.
The highest daily dose: 1200 mg.
The highest single dose: 600 mg.
Side effects:Central nervous system: dizziness, insomnia, asthenia.
Respiratory system: dyspnea, rarely - bronchospasm.
Cardiovascular system: bradycardia, atrioventricular block, cold extremities.
System of blood: neutropenia, thrombocytopenia.
Sense organs: "dry eye syndrome", transient visual impairment.
Gastrointestinal tract: indigestion, diarrhea or constipation.
Reproductive system: decreased potency.
Skin: Hyperhidrosis.
Allergic reactions.
Overdose:Pronounced bradycardia, arterial hypotension.
Treatment. Intravenous 1-2 mg atropine, 2.5 mcg / kg dobutamine, intravenously bolus 10 mg glucagon, intravenously drip 10-20 mcg isoprenaline at a rate of not more than 5 mcg per minute.
Interaction:Strengthens the effect of lidocaine in systemic application.
Negative dromo-, foreign, chromotropic influences are intensified with simultaneous admission with amiodarone, anesthetics, antiarrhythmics, digoxin, diltiazem, verapamil.
Special instructions:With angina pectoris in the selection of the dose should be guided by the heart rate of no more than 110 beats per minute with the load, but not at rest.
The drug is withdrawn within 2 weeks to avoid serious complications: arrhythmia, myocardial infarction.
It is not recommended to receive drivers and persons whose professional activity requires increased concentration of attention.