Amlodipine Alkaloid - instructions for use, dose, side effects, contraindications

The dihydropyridine derivative. Has antihypertensive, antianginal action. It blocks the flow of calcium ions through the cell membranes into the smooth muscle cells of the myocardium and vessels.

Antianginal effect is due to the expansion of coronary and peripheral arteries and arterioles: with angina decreases the severity of myocardial ischemia; expanding peripheral arterioles, reduces OPSS, reduces afterload on the heart, reduces the need for myocardium in oxygen. Expanding the main coronary arteries and arterioles in unchanged and in ischemic zones of the myocardium increases the flow of oxygen into the myocardium (especially with vasospastic angina); prevents the development of constriction of the coronary arteries (including caused by smoking). In patients with angina, a single daily dose increases exercise tolerance, slows the development of angina pectoris and the "ischemic depression" of the segment S-T, reduces the incidence of angina attacks and consumption of nitroglycerin.

Has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilating effect on smooth muscle vessels. With arterial hypertension, a single dose provides a clinically significant decrease in blood pressure over a period of 24 hours (in the patient's position "lying" and "standing"). Does not cause a sharp decrease in blood pressure, a decrease in exercise tolerance, LV ejection fraction.Reduces the degree of hypertrophy of the myocardium of the LV, has antiatherosclerotic and cardioprotective action in IHD. Does not increase the risk of death in patients with CHF (III-IV class on NYHA), on the background of therapy with digoxin, diuretics and ACE inhibitors.

Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the rate of glomerular filtration, has a weak natriuretic effect. When diabetic nephropathy does not increase the severity of microalbuminuria. It has no adverse effects on the metabolism and plasma lipids, it is suitable for the treatment of patients with concomitant bronchial asthma, diabetes mellitus.

Pharmacokinetics:

Absorption is slow, does not depend on food intake, is about 90%, bioavailability is 60-65%. TSmah at oral reception-6-12 hours At constant reception Css is created in 7-8 days. The volume of distribution is 21 l / kg. The connection with plasma proteins is 90-97%. Penetrates through the BBB.

Intensively (90%) is metabolized in the liver with the formation of inactive metabolites, has the effect of "first passage" through the liver. T_1/2on the average -35 hours.Total clearance is 500 ml / min.

T_1/2 in patients with arterial hypertension-48 hours in elderly patients increases to 65 hours, with hepatic insufficiency - up to 60 hours, similar magnification parameters T_1/2 are observed and with severe CHF, with a violation of kidney function, does not change. When hemodialysis is not removed.

It is excreted by the kidneys-60 % in the form of metabolites, 10% unchanged; with bile and through the intestines-20-25 % in the form of metabolites, as well as with breast milk.

Indications:Arterial hypertension, stress angina, vasospastic angina.

Contraindications:

Hypersensitivity to the drug and other dihydropyridine derivatives, severe arterial hypotension, collapse, unstable angina (with the exception of Prinzmetal angina), pregnancy, lactation.

Carefully:

Arterial hypotension, aortic stenosis, chronic heart failure, liver failure, acute myocardial infarction (and within 1 month after), hypertrophic obstructive cardiomyopathy (GICM), sinus node syndrome (SSS) and mitral stenosis, age 18 years (efficacy and safety of application are not established), advanced age.

Pregnancy and lactation:

Safety of use in pregnancy and lactation is not established. Experience of use in children is absent.

Dosing and Administration:

Inside, the initial daily dose is 5 mg per treatment with a gradual increase in 7-14 days to 10 mg / day once; with arterial hypertension, the maintenance dose is 2.5-5 mg / day.

For angina pectoris and vasospastic angina, the dose is 5-10 mg / day once; for the prevention of attacks of angina pectoris -10 mg / day.

Elderly and weakened patients, patients with impaired liver function as an antihypertensive drug are prescribed in an initial dose of 2.5 mg; as an antianginal drug - 5 mg.

Any adjustment to the dose of amlodipine with simultaneous use of thiazide diuretics, beta-blockers or angiotensin-converting enzyme inhibitors is not required.

Side effects:

From the nervous system: headache, dizziness, excessive fatigue, drowsiness, mood changes, convulsions; rarely - loss of consciousness, hypoesthesia, paresthesia, tremor, asthenia, malaise, insomnia, nervousness, depression,extraordinary dreams, anxiety; very rarely - ataxia, apathy, agitation, amnesia.

From the digestive system: nausea, abdominal pain; hyperbilirubinemia, jaundice, increased activity of "hepatic" transaminases; rarely dry mouth, vomiting, anorexia, constipation or diarrhea, dyspepsia, flatulence, gingival hyperplasia; very rarely - gastritis, pancreatitis.

From the CAS side: palpitation, edema of the ankles and feet, dyspnea, blood flushes to the face, rarely - rhythm disturbances (bradycardia, ventricular tachycardia, atrial flutter), chest pain, pronounced blood pressure lowering, orthostatic hypotension; very rarely - the development or aggravation of heart failure, extrasystole, vasculitis, migraine.

From the genitourinary system: rarely - pollakiuria, painful urge to urinate, nocturia, violation of sexual function (including decreased potency); very rarely - dysuria, polyuria.

From the musculoskeletal system: rarely - arthralgia, arthrosis, myalgia (with prolonged use); very rarely - myasthenia gravis.

From the skin: very rarely - xeroderma, alopecia, dermatitis, purpura. Allergic reactions: skin itching, rash (incl.erythematous, maculopapular rash, hives).

Other: rarely - visual impairment, conjunctivitis, diplopia, eye pain, accommodation disorder, xerophthalmia, ringing in the ears, gynaecomastia, back pain, fever and tidal flashes, chills, weight gain, dyspnoea, epistaxis, increased perspiration, thirst; very rarely-cold sticky sweat, cough, rhinitis, parosmia, perversion of taste.

Overdose:

Symptoms: excessive peripheral vasodilation, marked decrease in blood pressure, tachycardia.

Treatment: gastric lavage, the appointment of activated charcoal, the maintenance of CAS functions, the monitoring of heart and lung function indicators, the elevated position of the limbs, the control of circulating blood volume (bcc) and diuresis, symptomatic and maintenance therapy, intravenous calcium gluconate and dopamine. Hemodialysis is ineffective.

Interaction:

Inhibitors of microsomal oxidation increase the concentration of amlodipine in plasma, increasing the risk of side effects, and inductors of microsomal liver enzymes are reduced.

The hypotensive effect weakens NSAIDs, especially indomethacin, (delay Na⁺ and synthesis blockade Pg kidneys), alpha-adrenostimulators, estrogens (delay Na⁺), sympathomimetics.

Thiazide and "loop" diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and hypotensive effects.

Amiodarone, quinidine, alpha1-adrenergic blockers, antipsychotic drugs (neuroleptics) and BCCC may increase the hypotensive effect.

Does not affect the pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine.

When combined with drugs Li+ it is possible to intensify the manifestations of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Preparations of Ca2 + can reduce the effect of BCCC.

Procainamide, quinidine and other drugs that cause lengthening of the interval Q-T, reinforce the negative inotropic effect and may increase risk of significant lengthening of the interval Q-T.

Special instructions:

During treatment, it is necessary to monitor the body weight observed at the dentist (to prevent soreness, bleeding and gingival hyperplasia).

Amlodipine does not affect plasma concentrations of K +, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and urea nitrogen.

Despite the absence of the "cancellation" syndrome in BCC, before the cessation of treatment a gradual reduction of doses is recommended.

Form release / dosage:Tablets 5 mg, 10 mg.

Packaging:

Tablets 5 mg.

For 10 tablets in a perforated blister of aluminum foil and PVC film.

3 blisters together with instructions for use are placed in a cardboard pack.

Tablets 10 mg.

For 15 tablets in a perforated blister of aluminum foil and PVC film.

2 blisters together with instructions for use are placed in a cardboard pack.

Storage conditions:

In the dark place at a temperature of 15 to 25 ° C, inaccessible to children.

Shelf life:

3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000877/09

Date of registration:09.02.2009

Expiration Date:Unlimited

The owner of the registration certificate:Alkaloid, JSCAlkaloid, JSC Macedonia

Manufacturer: & nbsp

ALKALOID, AD Macedonia

Information update date: & nbsp10.08.2017

Illustrated instructions

Instructions

Amlodipine Alkaloid (Amlodipine Alkaloid)