Included in the formulation
АТХ:C.08.C.A Dihydropyridine derivatives
C.08.C.A.01 Amlodipine
Pharmacodynamics:S (-) (levorotatory) isomer of amlodipine, selective calcium channel blocker II class. Has antianginal and hypertensive action. Prevents the entry of extracellular calcium into the muscle cells of the coronary and peripheral arteries. In high doses, it inhibits the release of calcium ions from intracellular stores. Does not affect the tone of the veins.
Strengthens the coronary blood flow, improving the blood supply of ischemic zones of the myocardium, does not cause a "robbery syndrome". Expands peripheral arteries, reduces overall peripheral resistance, postnagruzku and the need for myocardium in oxygen. Does not affect the pacemaker: the sinoatrial and atrioventricular nodes. Has a weak antiarrhythmic effect.
It enhances kidney blood flow, causes a moderate natriuresis.
The clinical effect is noted 2-4 hours after administration and lasts for 1 day.
Pharmacokinetics:After oral administration, it is absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is reached after 2-2.5 hours. It binds to plasma proteins by 65%. Penetrates through the blood-brain barrier. Metabolised in the liver.
The half-life is 14-19 hours. For repeated use, it is up to 45 hours.
Elimination in the form of inactive metabolites: 70 % - with feces, 30 % - with urine. It is not removed during hemodialysis.
Indications:Used to treat arterial hypertension as a monotherapy, or in a composition with other antihypertensive drugs.
IX.I10-I15.I15 Secondary Hypertension
IX.I10-I15.I10 Essential [primary] hypertension
Contraindications:- Acute myocardial infarction.
- Aortic stenosis.
- Aortic hypotension.
- Individual intolerance.
Carefully:- Stenosis of the mitral valve.
- Acute disorders of cerebral circulation.
- Renal and hepatic insufficiency.
Pregnancy and lactation:Recommendations for FDA - Category C. During pregnancy and lactation, the drug is contraindicated.
Dosing and Administration:Inside the morning at the same time, regardless of meals 2.5 mg once a day. If necessary, the dose gradually increases to 5 mg per day. The drug may continue for an indefinite period of time.
The highest daily dose: 5 mg.
The highest single dose: 2.5 mg.
Side effects:Central and peripheral nervous system: dizziness, headache, with prolonged use - paresthesia of the extremities, depression.
The cardiovascular system: possibly exacerbation of angina in the first days of taking the drug, flushing of the blood to the skin of the face, tachycardia.
Musculoskeletal system: myalgia, convulsions of the upper and lower extremities.
Digestive system: nausea, gingival hyperplasia.
Urinary system: rarely - polyuria.
Allergic reactions.
Overdose:Symptoms: headache, arrhythmia; in severe cases - loss of consciousness, coma.
Treatment: symptomatic. Antidotes are calcium preparations. Hemodialysis is ineffective, it is recommended that plasmapheresis is performed.
Interaction:Incompatible with alcohol.
The intake of grapefruit juice slows the absorption of the drug.
Simultaneous use of the drug with antihypertensive drugs, as well as inhalational anesthetics, tricyclic antidepressants, nitrates, cimetidine, diuretics leads to an intensification of the hypotensive effect.
It is not compatible with rifampicin, since it accelerates the metabolism of slow calcium channel blockers.
Levamladipin increases the concentration of indirect anticoagulants in the blood plasma.
Special instructions:Stop taking the drug should be gradual.
Before an operative intervention it is necessary to inform the anesthesiologist about taking the drug by the patient.