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

Description:Ploskotsilindricheskie tablets with a facet from white to white with kremovatym a shade of color. Light marble is allowed. Tablets with a dosage of 10 mg have a dividing risk on one side.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.01 Amlodipine

Pharmacodynamics:

Derivative of dihydropyridine - blocker of "slow" calcium channels (BCCI) of the second generation, has an antianginal and hypotensive effect.Linking with dihydropyridine receptors, blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (mostly in smooth muscle cells of blood vessels, rather than in cardiomyocytes).

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 the main 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 stable angina, a single daily dose increases exercise tolerance, slows the development of angina pectoris and the "ischemic" depression of the segment ST, reduces the incidence of angina attacks and consumption of nitroglycerin and other nitrates.

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 (BP) for 24 hours (in the patient's position "lying" and "standing"). Orthostatic hypotension in the appointment of amlodipine is rare. Does not cause a decrease in exercise tolerance, a fraction of the ejection of the left ventricle. Reduces the degree of myocardial hypertrophy of the left ventricle. Does not affect the contractility and conductance of the myocardium, nc causes 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 effect on the metabolism and concentration of plasma lipids and can be used in the treatment of patients with 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.

The intake of food 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 elimination half-life (T1 / 2) varies from 31 to 48 hours, with a re-appointment of T1 / 2 of approximately 45 hours. About 60% of the dose taken internally is excreted by the kidneys mainly in the form of metabolites, 10% - unchanged, and 20-25% - through the intestine, as well as breast milk. The total clearance of amlodipine is 0.116 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's stenocardia);
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:

Violations of liver function, syndrome of sinus node weakness (pronounced bradycardia, tachycardia), chronic heart failure of non-ischemic etiology III-1V 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), in old age.

Pregnancy and lactation:

The safety of the use of amlodipine during pregnancy and during lactation is not established, so the drug amlodipine should not be given to pregnant women and during lactation.

Dosing and Administration:

Vnutppm, the initial dose for treatment arterial hypertension and angina pectoris is 5 mg of the drug once a day. The maximum dose can be increased to 10 mg once a day. With arterial hypertension the maintenance dose can be 2.5 - 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.

Do not require dose changes with simultaneous administration with thiazide diuretics, beta-blockers and inhibitors angiotensin-converting enzyme (AG1F).

He Dose changes are required in patients with renal insufficiency.

Side effects:

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

very often, more than 1/10

often more than 1/100 and less than 1/10

sometimes more than 1/1000 and less than 1/100

rarely - more than 1/10000 and less than 1/1000

very rarely - less than 1/10000, including individual messages.

From the side of the cardiovascular system: often - palpitations, peripheral edema (swelling of the ankles and feet), "tides" of blood to the skin of the face: sometimes - excessive decrease in blood pressure; very rarely - fainting, shortness of breath, vasculitis, orthostatic hypotension, development or aggravation of the course of heart failure, disorders heart rhythm (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain.

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

From the digestive system: often - nausea, pain in the abdomen; sometimes - 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: sometimes - frequent urination, painful urination, nocturia, impotence, very rarely - dysuria, polyuria.

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

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

Allergic reactions: itching, rash (including erythematous, maculopapular rash, urticaria), angioneurotic edema, erythema multiforme.

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

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

Overdose:

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

Treatment: gastric lavage, the appointment of activated charcoal, maintenance of cardiovascular function, control of heart and lung function, elevated, above the level of the head, the position of the lower limbs, control of the volume of circulating blood and diuresis. For restoration of 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 calcium channels - intravenous introduction of calcium gluconate. Hemodialysis is ineffective.

Interaction:

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

Amlodipine 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 antihypertensive effect of BCCC when combined with thiazide and loop diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates, as well as enhance their hypotensive effect when combined with alpha 1-adrenoblockers, neuroleptics.

Although no negative inotropic effects were usually observed in the study of amlodipine, nevertheless, some BCCCs can increase the severity of the negative inotropic effect of antiarrhythmics and elongate the interval QT (eg, amiodarone and quinidine).

A single dose of 100 mg of sildenafil in patients with essential hypertension does not affect the parameters of pharmacokinetics 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 concentration 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 administration 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-PRANA 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).

Patients with low body weight, low growth patients and patients with severe liver function impairment may need a smaller dose.

Elderly patients may be lengthened T1/2 and clearance of the drug. Dose 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-PRANA must be administered with caution. Despite the fact that the termination of admission AMLODIPINE-PRANA is not accompanied by the development of the syndrome of "cancellation", it is desirable to cease treatment, gradually reducing the dose of the drug. The effectiveness and safety of the drug in hypertensive crisis is not established.

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

During treatment should be observed caution when driving vehicles and engage in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Tablets of 5 mg or 10 mg.

Packaging:

10 tablets per contour cell package or 40, 50, 60, 70, 80, 90, 100 tablets in polymeric to the bank.

Each jar or 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 contour cell packings together with the instructions for use are placed in a pack of cardboard.

Storage conditions:In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000849/10

Date of registration:10.02.2010 / 16.05.2017

Expiration Date:Unlimited

The owner of the registration certificate:PRANAFARM, LLC PRANAFARM, LLC Russia

Manufacturer: & nbsp

PRANAFARM, LLC Russia

Information update date: & nbsp24.07.2017

Illustrated instructions

Instructions

Amlodipine-Prana (Amlodipine-prana)