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

Derivative of dihydropyridine - blocker of "slow" calcium channels (BCCC) II generation, has antianginal and hypotensive effects. Linking to the segment S6 III and IY domains of the alpha 1-subunit of the calcium channel L-type.

Antianginal action is due to the expansion of coronary and peripheral arteries and arterioles: with angina reduces severity of myocardial ischemia; expanding peripheral arterioles, reduces the overall peripheral vascular resistance (OPSS), reduces preload on the heart, reduces the need for myocardium in oxygen. Expands coronary arteries and arterioles in unchanged and ischemic zones of the myocardium, increases the flow of oxygen into the myocardium (especially with vasospastic angina); prevents the development of spasm of the coronary arteries (including those caused by smoking). In patients with angina, a single daily dose of amlodipine increases the time of exercise, delays the development of angina attack and depression of the segment ST (by 1 mm) during its implementation, reduces the frequency of angina attacks and the consumption of tablets of nitroglycerin and other nitrates. Has a long-term dose-dependent hypotensive effect.

Hypotensive effect is caused by a direct vasodilating effect on the smooth muscles of the vessels. With arterial hypertension, a single dose provides a clinically significant decrease in blood pressure (BP) for 24 hours (in the patient's position "lying" and "standing"). Orthostatic hypotension in the appointment of the drug Amlodipine Cardio is rare. Reduces the degree of myocardial hypertrophy of the left ventricle. Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in the heart rate (HR), inhibits platelet aggregation, increases the rate of glomerular filtration, has a weak natriuretic effect.

When diabetic nephropathy does not increase the severity of microalbuminuria.

Does not have any adverse effects on the metabolism and concentration of plasma lipids and can be used in the treatment of patients with concomitant bronchial asthma, diabetes and gout. A significant reduction in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours.

Pharmacokinetics:

After oral administration amlodipine slowly absorbed from the gastrointestinal tract (GIT).The average absolute bioavailability is 64%, the maximum concentration (Cmah) in the serum is observed after 6-9 hours. Equilibrium serum concentrations (Css) are achieved after 7-8 days of therapy.

Food intake does not affect the absorption of amlodipine. The average volume of distribution is 21 l / kg body weight, indicating that most of the drug is in the tissues, and relatively less in the blood. Most of the drug in the blood (95%), binds to blood plasma proteins. Amlodipine is subjected to a slow but active metabolism in the liver in the absence of a significant "first passage" effect. Metabolites do not have significant pharmacological activity.

After a single oral intake, the half-life period (T1 / 2) varies from 31 to 48 hours, with repeated admission T1 / 2 is approximately 45 hours. About 60% of the dose taken internally is excreted by the kidneys mainly in the form of metabolites, 10% - in unchanged form, 20-25% - through the intestine, as well as with breast milk. The total clearance of amlodipine is OD 16 ml / s / kg (7 ml / min / kg, 0.42 l / h / kg). In elderly patients (over 65 years), amlodipine withdrawal is slowed (T1 / 2 - 65 h) compared with young patients, but this difference is not clinically significant.Elongation of T1 / 2 in patients with hepatic insufficiency suggests that with prolonged administration, the cumulation of the drug in the body will be higher (T1 / 2 - up to 60 hours). Renal failure does not significantly affect the kinetics of amlodipine. The drug penetrates the blood-brain barrier. When hemodialysis is not removed.

Indications:

Arterial hypertension (monotherapy or in combination with other antihypertensive agents).

Stable exertional angina and vasospastic angina (Prinzmetal angina) (monotherapy or in combination with other antianginal drugs).

Contraindications:

Hypersensitivity to amlodipine, dihydropyridine derivatives and other components of the drug;
Severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
Collapse, cardiogenic shock;
Unstable angina (with the exception of Prinzmetal angina);
Clinically significant aortic stenosis;
Pregnancy and lactation;
Age under 18 years (effectiveness and safety not studied);
Lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Carefully:

Dysfunction of the liver, syndrome of weakness of the sinus node (SSSU) (pronounced bradycardia, tachycardia), chronic heart failure of non-ischemic etiology III-IV functional class by classification NYHA, arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy (GOKMP), acute myocardial infarction (and within 1 month after myocardial infarction), elderly age.

Pregnancy and lactation:

The safety of the use of amlodipine during pregnancy and during lactation is not established, so Amlodipine Cardio should not be prescribed during pregnancy and lactation.

Dosing and Administration:

Inside, the initial dose for treatment arterial hypertension and angina pectoris is 5 mg once a day. The maximum daily dose is 10 mg once. With hypertension, the maintenance dose may be 2.5 to 5 mg (1/2 tablets of 5 mg - 1 tablet of 5 mg) per day.

In elderly patients, T1 / 2 amlodipine may increase and creatinine clearance (CC) decrease. Dose changes are not required, but more careful monitoring of patients is necessary.

There is no need for dose changes with concomitant administration with thiazide diuretics, beta-blockers and inhibitors of angiotensin-converting enzyme (ACE).

Do not require dose changes in patients with renal insufficiency.

Side effects:

Classification of the frequency of development of side effects of the World Organization Health (WHO):

very often> 1/10

often> 1/100 and <1/10

infrequently> 1/1000 and <1/100

rarely> 1/10000 and <1/1000

very rarely <1/10000, including individual messages.

From the side of the cardiovascular system: often - a feeling of palpitations, peripheral swelling (swelling of the ankles and feet), "tides" of blood to the skin of the face; infrequent reduction of blood pressure; very rarely syncope, dyspnea, vasculitis, orthostatic hypotension, development or aggravation of the course of heart failure, heart rhythm disturbances (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain.

From the central and peripheral nervous system: often - headache, dizziness, fatigue, drowsiness; infrequently - asthenia, general malaise, hyperesthesia, paresthesia,peripheral neuropathy, tremor, insomnia, mood lability, unusual dreams, nervousness, depression, anxiety, very rarely - migraine, increased sweating, apathy.

From the digestive system: often - nausea, abdominal pain; infrequent - vomiting, constipation or diarrhea, flatulence, dyspepsia, anorexia, dryness of the oral mucosa, thirst; rarely - gingival hyperplasia, increased appetite; very rarely - pancreatitis, gastritis, jaundice (caused by cholestasis), hyperbilirubinemia, increased activity of "liver" transaminases, hepatitis.

From the hematopoiesis: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.

From the genitourinary system: infrequently - frequent urination, painful urination, nocturia, impotence, very rarely - dysuria, polyuria, gynecomastia.

From the respiratory system: infrequently - shortness of breath, rhinitis, very rarely - cough.

From the side of the bone: rarely - dermatitis, very rarely - alopecia, xeroderma, "cold" sweat, a violation of skin pigmentation.

Allergic reactions: pruritus, rash (including erythematous, maculopapular rash, urticaria), angioedema, erythema multiforme.

From the musculoskeletal system: infrequently - muscle cramps, myalgia, arthralgia, back pain, arthrosis, rarely - myasthenia gravis.

Other: infrequent - ringing in the ears, diplopia, accommodation disorder, xerophthalmia, conjunctivitis, eye pain, chills, nosebleeds, very rarely - parosmia, hyperglycemia.

Overdose:

Symptoms: excessive peripheral vasodilation with a pronounced and possibly long-term decline in blood pressure, collapse, shock.

Treatment: The patient should take a horizontal position with the lower limbs raised above the level of the head.

Gastric lavage, the appointment of activated charcoal, maintenance of cardiovascular function, monitoring of heart and lung function, control of the volume of circulating blood and diuresis. To restore the vascular tone - the use of vasoconstrictor (in the absence of contraindications to their use); with the purpose of elimination of consequences of blockade of slow calcium channels - intravenous introduction of calcium gluconate. Hemodialysis is ineffective.

Interaction:

Amlodipine Cardio can safely be used to treat arterial hypertension along with thiazide diuretics, alpha-blockers, beta-blockers or ACE inhibitors.In patients with stable angina, the drug can be combined with other antianginal agents, for example, with long-acting nitrates, beta-blockers or short-acting nitrates,

Amlodipine Cardio can be used simultaneously with non-steroidal anti-inflammatory drugs (NSAIDs) (especially indomethacin), antibacterial agents and hypoglycemic agents for oral administration.

It is possible to strengthen the anti-anginal and hypotensive action of BCCC when combined with thiazide and loop diuretics, verapamil, ACE inhibitors, beta-adrenoblockers and nitrates, as well as enhance their hypotensive effect when combined with alpha 1-blockers, antipsychotics.

Although no negative inotropic effects were observed in the study of amlodipine, nevertheless, some BCCI can increase the severity negative inotropic action of antiarrhythmic agents capable of causing lengthening of the interval QT (eg, amiodarone and quinidine). A single dose of 100 mg of sildenafil in patients with essential hypertension does not affect the pharmacokinetics of amlodipine.

The repeated use of amlodipine in a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.

Ethanol (drinks containing alcohol): amlodipine at a single and repeated application in a dose of 10 mg does not affect the pharmacokinetics of ethanol. Antiviral drugs (ritonavir) increases the plasma concentrations of BCCI, incl. amlodipine.

Neuroleptics and isoflurane - Increased hypotensive effect of dihydropyridine derivatives.

Calcium preparations can reduce the effect of BCCC.

When amlodipine is used together with lithium preparations, it is possible to intensify manifestations of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Amlodipine does not change the pharmacokinetics of cyclosporine.

Does not affect the concentration of serum digoxin and its renal clearance.

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

Cimetidine does not affect the pharmacokinetics of amlodipine.

In studies in vitro Amlodipine does not affect the binding to blood proteins of digoxin, phenytoin, warfarin and indomethacin.

Grapefruit juice: simultaneous single intake of 240 mg grapefruit juice and 10 mg of amlodipine inside is not accompanied by a significant change in the pharmacokinetics of amlodipine.

Special instructions:

During the period of treatment with Amlodipine Cardio, it is necessary to control the body weight and sodium intake, the purpose of the appropriate diet. It is necessary to maintain dental hygiene and supervision at the dentist (to prevent soreness, bleeding and gingival hyperplasia).

In elderly patients, T1 / 2 and the clearance of the drug may be prolonged. Dosage changes for elderly patients are not required; with increasing the dose, more careful monitoring of patients is necessary.

If the liver function is also impaired, T1 / 2 of the drug may be prolonged. Therefore, such patients Amlodipine Cardio should be administered with caution. Despite the fact that discontinuation of the drug Amlodipine Cardio is not accompanied by the development of the "withdrawal" syndrome, it is desirable to stop treatment, gradually reducing the dose of the drug. Efficacy and safety of the drug for hypertensive crisis is not installed.

Effect on the ability to drive transp. cf. and fur:

There have been no reports of the effects of Amlodipine Cardio on vehicle management or work with machinery.Nevertheless, some patients, mainly at the beginning of treatment, may experience drowsiness and dizziness and other side effects from the CNS. When they occur, the patient must observe special precautions when driving vehicles and working with complex mechanisms.

Form release / dosage:

Tablets of 5 mg and 10 mg.

Packaging:

By 7, 10, 14 or 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 2, 3, 4 or 5 contour squares, together with the instructions for use, are placed in a pack of cardboard.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003062 / 01

Date of registration:20.11.2008 / 14.02.2017

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Representation: & nbspOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCRussia

Information update date: & nbsp24.07.2017

Illustrated instructions

Instructions

Amlodipine Cardio (Amlodipine cardio)