Amlodipin cardio

General characteristics. Structure:

Active ingredient: 5 mg or 10 mg of an amlodipin (in the form of a bezilat) in 1 tablet.

Excipients: gipromelloz (gidroksipropilmetiltsellyuloz), potato starch, lactose (sugar milk), magnesium stearate (magnesium stearate), talc.

Drug reduces load of heart, reduces the frequency of attacks of stenocardia, possesses soft hypotensive action.

Pharmacological properties:

Pharmacodynamics. Derivative dihydropyridine – the blocker of "slow" calcium channels (BMKK) of the II generation, has anti-anginal and hypotensive effect. Contacting a S6 III and IY segment of domains an alpha of a 1-subunit calcium channel of L-type.

Anti-anginal action is caused by expansion of coronary and peripheral arteries and arterioles: at stenocardia reduces expressiveness of ischemia of a myocardium; expanding peripheral arterioles, reduces the general peripheric vascular resistance (GPVR), reduces preload of heart, reduces the need of a myocardium for oxygen. Expands coronary arteries and arterioles in not changed and ischemic zones of a myocardium, increases intake of oxygen in a myocardium (especially at vasospastic stenocardia); prevents development of a spasm of coronary arteries (including caused by smoking). At patients with stenocardia the single daily dose of an amlodipin increases time of performance of an exercise stress, development of an attack of stenocardia and depression of a segment of ST detains (on 1 mm) during its performance, reduces the frequency of attacks of stenocardia and consumption of Tabulettaes Nitroglycerini and other nitrates. Renders long-term dozozavisimy hypotensive effect.

Hypotensive action is caused by direct vazodilatiruyushchy impact on unstriated muscles of vessels. At arterial hypertension the single dose provides clinically significant lowering of arterial pressure (ABP) for 24 h (in position of the patient "lying" and "standing"). Orthostatic hypotension at purpose of the drug Omelar® of Kardio meets rather seldom. Reduces degree of a hypertrophy of a myocardium of a left ventricle. Does not exert impact on contractility and conductivity of a myocardium, does not cause reflex increase in the heart rate (HR), slows down aggregation of thrombocytes, raises a glomerular filtration rate, possesses a weak natriuretic effect.

At a diabetic nephropathy does not increase expressiveness of a microalbuminuria.

Does not exert any adverse impact on a metabolism and concentration of lipids of a blood plasma and it can be applied at treatment of patients with the accompanying bronchial asthma, a diabetes mellitus and gout. Significant decrease in the ABP is observed in 6-10 hours, effect duration 24 hours.

Pharmacokinetics. After intake амлодипин it is slowly absorbed from the digestive tract (DT). Average absolute bioavailability makes 64%, the maximum concentration (Cmax) in blood serum is observed in 6-9 hours. Equilibrium serumal concentration (Css) are reached after 7-8 days of therapy.

Meal does not influence absorption of an amlodipin. The average volume of distribution makes 21 l/kg of body weight that indicates that the most part of drug is in fabrics, and rather smaller – in blood. The most part of the drug which is in blood (95%) contacts proteins of a blood plasma. Amlodipin is exposed to slow, but active metabolism in a liver in the absence of significant effect of "the first passing". Metabolites have no essential pharmacological activity.

After a single dose inside the elimination half-life (T1/2) varies from 31 to 48 hours, at repeated reception of T1/2 makes about 45 hours. About 60% of the dose accepted inside are allocated with kidneys preferential in the form of metabolites, 10% - in not changed look, 20-25% - through intestines, and also with breast milk. The general clearance of an amlodipin makes 0,116 ml / with/kg (7 ml/min., 0,42 l/h/kg).

At elderly patients (65 years are more senior) removal of an amlodipin is slowed down (T1/2 - 65 h) in comparison with young patients, however this difference has no clinical value. Lengthening of T1/2 at patients with a liver failure assumes that at long appointment cumulation of drug in an organism will be higher (T1/2 - to 60 h).

The renal failure has no significant effect on kinetics of an amlodipin. Drug gets through a blood-brain barrier. At a hemodialysis is not removed.

Indications to use:

● Arterial hypertension (monotherapy or in a combination with other anti-hypertensive means).

● the Stable angina of exertion and vasospastic stenocardia (Printsmetal's stenocardia) (monotherapy or in a combination with other anti-anginal means).

Route of administration and doses:

Inside, the initial dose for treatment of arterial hypertension and stenocardia makes 5 mg of drug once a day. The maximum daily dose - 10 mg once. At arterial hypertension the maintenance dose can be 2,5 – 5 mg (1/2 tablets on 5 mg - 1 tablet on 5 mg) in days.

At patients of advanced age T1/2 of an amlodipin can increase and decrease the clearance of creatinine (CC). Change of doses is not required, but more careful observation of patients is necessary.

Change of a dose at co-administration with thiazide diuretics, beta adrenoblockers and inhibitors of an angiotensin-converting enzyme (APF) is not required.

Change of a dose is not required from patients with a renal failure.

Features of use:

Pregnancy and period of a lactation: safety of use of an amlodipin at pregnancy and during feeding by a breast is not established therefore it is not necessary to appoint drug during pregnancy and a lactation.

During treatment by drug it is necessary to control the body weight and consumption of sodium, purpose of the corresponding diet. Maintenance of hygiene of teeth and observation at the stomatologist is necessary (for prevention of morbidity, bleeding and a hyperplasia of gums).

At elderly patients T1/2 and clearance of drug can be extended. Change of doses for elderly patients is not required; at increase in a dose more careful observation of patients is necessary.

At an abnormal liver function drug T1/2 can be also extended. Therefore such patients of Omelar® of Kardio need to appoint with care. In spite of the fact that the termination of administration of drug of Omelar® of Kardio is not followed by development of a syndrome of "cancellation", it is desirable to carry out the termination of treatment, gradually reducing a drug dose.

Efficiency and safety of drug at hypertensive crisis is not established.

Influence on ability to driving and other difficult mechanisms. There were no messages on influence of drug on control of vehicles or work with mechanisms. Nevertheless, at some patients, it is preferential in an initiation of treatment, there can be a drowsiness and dizziness and other side effects from TsNS. At their emergence the patient has to observe special precautionary measures at control of vehicles and work with difficult mechanisms.

Side effects:

Classification of frequency of development of side effects of the World Health Organization (WHO): very often> 1/10; often> 1/100 and <1/10; infrequently> 1/1000 and <1/100; seldom> 1/10000 and <1/1000; very seldom <1/10000, including separate messages.

From cardiovascular system: often – a heart consciousness, peripheral hypostases (puffiness of anklebones and feet), "inflows" of blood to face skin; infrequently – excessive decrease in the ABP; very seldom – a syncope, an asthma, a vasculitis, orthostatic hypotension, development or aggravation of a course of heart failure, disturbance of a heart rhythm (including bradycardia, ventricular tachycardia and atrial fibrillation), a myocardial infarction, thorax pains.

From the central and peripheral nervous system: often – a headache, dizziness, increased fatigue, drowsiness; infrequently – an adynamy, a febricula, hyperesthesias, paresthesias, peripheral neuropathy, a tremor, sleeplessness, lability of mood, unusual dreams, nervousness, a depression, uneasiness, it is very rare – migraine, the increased sweating, apathy.

From the alimentary system: often - nausea, abdominal pains; infrequently – vomiting, a lock or diarrhea, a meteorism, dyspepsia, anorexia, dryness of a mucous membrane of an oral cavity, thirst; seldom – a hyperplasia of gums, increase in appetite; very seldom – the pancreatitis, gastritis, jaundice (caused by a cholestasia), a hyperbilirubinemia, increase in activity of "hepatic" transaminases, hepatitis.

From bodies of a hemopoiesis: very seldom – a Werlhof's disease, a leukopenia, thrombocytopenia.

From urinogenital system: infrequently – the speeded-up urination, an urodynia, a nocturia, impotence, is very rare – a dysuria, a polyuria, a gynecomastia.

From respiratory system: infrequently – short wind, rhinitis, it is very rare – cough.

From integuments: seldom – dermatitis, it is very rare – an alopecia, a xerodermia, "cold" sweat, disturbance of a xanthopathy.

Allergic reactions: skin itch, rash (including erythematic, makulopapulezny rash, small tortoiseshell), Quincke's disease, multiformny erythema.

From a musculoskeletal system: infrequently – muscular spasms, a mialgiya, an arthralgia, a dorsodynia, arthrosis, it is rare - a myasthenia.

Others: infrequently – a ring in ears, a diplopia, accommodation disturbance, a xerophthalmia, conjunctivitis, eye pain, a fever, nasal bleeding, it is very rare – a parosmiya, a hyperglycemia.

Interaction with other medicines:

Drug can safely be used for treatment of arterial hypertension together with thiazide diuretics, alpha adrenoblockers, beta adrenoblockers or APF inhibitors.

At patients with stable stenocardia drug can be combined with other anti-anginal means, for example, with nitrates of the prolonged action, beta adrenoblockers or nitrates of short action.

Drug can be used at the same time with non-steroidal anti-inflammatory drugs (NPVP) (especially indometacin), antibacterial agents and hypoglycemic means for intake.

Strengthening of anti-anginal and hypotensive action of BMKK at combined use with thiazide and "loopback" diuretics, verapamil, APF inhibitors, beta adrenoblockers and nitrates, and also strengthening of their hypotensive action at combined use with alfa1-adrenoblockers, neuroleptics is possible.

Though when studying an amlodipin of negative inotropic effect usually did not observe, nevertheless, some BMKK can increase expressiveness of negative inotropic effect of the antiarrhytmic means capable to cause lengthening of an interval of QT (for example, Amiodaronum and quinidine).

The single dose of 100 mg of a sildenafil at patients with essential hypertensia does not exert impact on parameters of pharmacokinetics of an amlodipin.

Repeated use of an amlodipin in a dose of 10 mg and an atorvastatina in a dose of 80 mg is not followed by considerable changes of indicators of pharmacokinetics of an atorvastatin.

Ethanol (the drinks containing alcohol): амлодипин at single and repeated use in a dose of 10 mg does not influence ethanol pharmacokinetics.

Antiviral means (ритонавир) increases plasma concentration of BMKK, including amlodipin.

Neuroleptics and изофлуран – strengthening of hypotensive action of derivatives of dihydropyridine.

Drugs of calcium can reduce effect of BMKK.

At combined use of an amlodipin with drugs of lithium strengthening of manifestation of a neurotoxicity (nausea, vomiting, diarrhea, an ataxy, a tremor, a sonitus) is possible.

Amlodipin does not change cyclosporine pharmacokinetics.

Also its renal clearance does not exert impact on concentration in blood serum of digoxin.

Has no significant effect on effect of warfarin (prothrombin time).

Cimetidinum does not influence pharmacokinetics of an amlodipin.

In the researches in vitro амлодипин does not influence linkng with blood proteins of digoxin, Phenytoinum, warfarin and indometacin.

Grapefruit juice: the concomitant single dose of 240 mg of grapefruit juice and 10 mg of an amlodipin inside is not followed by essential change of pharmacokinetics of an amlodipin.

Contraindications:

● Hypersensitivity to an amlodipin, derivatives of dihydropyridine and other components of drug;

● the Expressed arterial hypotension (systolic the ABP less than 90 mm hg);

● Collapse, cardiogenic shock;

● Unstable stenocardia (except for Printsmetal's stenocardia);

● Clinically significant stenosis of an aorta;

● Pregnancy and period of a lactation;

● Age up to 18 years (efficiency and safety are not studied);

● Lactose intolerance, deficit of lactase or glyukozo-galaktozny malabsorption.

With care: Abnormal liver functions, the sick sinus syndrome (SSS) (the expressed bradycardia, tachycardia), chronic heart failure of not ischemic etiology of the III-IV functional class on NYHA classification, arterial hypotension, an aortal stenosis, a mitral stenosis, a hypertrophic subaortic stenosis (GOKMP), an acute myocardial infarction (and within 1 month after a myocardial infarction), advanced age.

Overdose:

Symptoms: an excessive peripheral vazodilatation with the expressed and perhaps long decrease in the ABP, a collapse, shock.

Treatment: the patient should accept horizontal position with the lower extremities raised higher than the level of the head. A gastric lavage, purpose of absorbent carbon, maintenance of function of cardiovascular system, control of indicators of function of heart and lungs, control of volume of the circulating blood and a diuresis.

For recovery of a tone of vessels – use of vasoconstrictors (in the absence of contraindications to their use); for the purpose of elimination of effects of blockade of slow calcium channels – intravenous administration of calcium of a gluconate. The hemodialysis is inefficient.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 5 mg and 10 mg. On 7, 10, 14 or 20 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3, 4 or 5 blister strip packagings together with the application instruction place in a pack from a cardboard.