Amlodipine, pills 10mg, 30pcs

$7.0

Active ingredient:	Amlodipine
Dosage form:	Pills

Categories: Cardiovascular system, Hypertension, Medication

Description
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Composition

1 tablet contains:

Active ingredient:

Amlodipine bezylate (amlodipine) -13.888 mg (10.00 mg).

Auxiliary substances: Microcrystalline cellulose, calcium hydrophosphate (anhydrous), sodium carboxymethyl starch (type A), magnesium stearate.

Pharmacological action

Pharmacotherapeutic group

blocker of “slow” calcium channels

ATX Code: C08CA01

Pharmacodynamics :

Slow calcium channel blocker A second – generation dihydropyridine derivative-slow calcium channel blocker (BMCC) has an antianginal and antihypertensive effect. Blocks calcium channels reduces the transmembrane transfer of calcium ions into the cell (more to vascular smooth muscle cells than to cardiomyocytes).

Antianginal effect is due to the expansion of coronary and peripheral arteries and arterioles: with angina reduces the severity of myocardial ischemia; expanding peripheral arterioles reduces total peripheral vascular resistance (OISS) reduces afterload on the heart reduces the need for myocardial oxygen. Dilating the coronary arteries and arterioles in unchanged and ischemic areas of the myocardium increases oxygen supply to the myocardium (especially in vasospastic angina pectoris); prevents spasm of the coronary arteries (including those caused by smoking). In patients with stable angina, a single daily dose increases exercise tolerance increases the time to angina attack and “ischemic” ST-segment depression reduces the frequency of angina attacks and consumption of nitroglycerin in other nitrates. It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to the direct vasodilating effect on vascular smooth muscles. In patients with arterial hypertension, a single dose provides a clinically significant reduction in blood pressure (BP) for 24 hours (in the patient’s “lying” and “standing”positions). Orthostatic hypotension with the appointment of amlodipine is quite rare. It does not cause a decrease in the left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy. It does not affect the contractility and conduction of the myocardium does not cause a reflex increase

in heart rate (HR) inhibits platelet aggregation increases the glomerular filtration rate has a weak natriuretic effect.

In diabetic nephropathy, it does not increase the severity of microalbuminuria. It 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 mellitus and gout. A significant decrease in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours.

In patients with diseases of the cardiovascular system including coronary atherosclerosis with damage to one vessel and before stenosis of 3 or more arteries carotid artery atherosclerosis after myocardial infarction percutaneous transluminal angioplasty (TLAP) of the coronary arteries or patients with angina, the use of amlodipine prevents the development of thickening of the intima-media of the carotid arteries reduces mortality from myocardial infarction stroke TLAP aorto-coronary artery bypass grafting; reduces the incidence of unstable angina and the progression of chronic heart failure (CHF); reduces the frequency of interventions aimed at restoring coronary blood flow.

It does not increase the risk of death or complications and deaths in patients with CHF (NYHA functional class III-IV) during digoxin therapy with diuretics and anthotensin converting enzyme (ACE) inhibitors. In patients with CHF (NYHA functional class III-IV) of non-ischemic etiology, amlodipine is likely to cause pulmonary edema.

Pharmacokinetics:

After oral use, amlodipine is slowly absorbed from the gastrointestinal tract (GI). The average absolute bioavailability is 64%. The maximum concentration (Cmax) in the blood serum is observed after 6-9 hours. Steady-state concentrations (SSS) are reached after 7-8 days of therapy.

Food intake does not affect the absorption of amlodipine. The average volume of distribution is 21 l / kg of body weight, which indicates that most of the drug is in the tissues and less in the blood. Most of the drug in the blood (95%) binds to plasma proteins. Amlodipine undergoes slow but active metabolism in the liver in the absence of a significant “first pass” effect. The metabolites do not have significant pharmacological activity. After a single dose, the half-life (T 1/2) varies from 35 to 50 hours with repeated use of T 1/2 is approximately 45 hours. About 60% of the oral dose is excreted by the kidneys mainly in the form of metabolites,10% – unchanged, and 20-25% – through the intestines with bile. The total clearance of amlodipine is 0116 ml / s / kg (7 ml / min / kg 042 l / h/kg).

In elderly patients (older than 65 years), the elimination of amlodipine is slowed (T 1/2 is 65 hours) compared to young patients, but this difference is not clinically significant. Prolongation of T 1/2 in patients with hepatic insufficiency suggests that with prolonged use, the accumulation of the drug in the body will be higher (T 1/2-up to 60 hours). Renal failure does not significantly affect the kinetics of amlodipine. In patients with impaired renal function, changes in the concentration of amlodipine in blood plasma do not correlate with the degree of renal failure. A slight increase in T 1/2 is possible.

Amlodipine penetrates the blood-brain barrier. It is not removed during hemodialysis.

Active ingredients

During therapy with Amlodipine-Teva, it is necessary to monitor body weight and sodium intake and prescribe an appropriate diet.

It is necessary to maintain oral hygiene and follow-up with a dentist (to prevent painful bleeding and gum hyperplasia).

When using Amlodipine-Teva in patients with chronic heart failure of NYHA functional class III and IV, pulmonary edema may develop.

In acute myocardial infarction, Amlodipine-Teva is prescribed after stabilization of hemodynamic parameters (see the section “Contraindications”).

Patients with hepatic insufficiency should be under the supervision of a doctor if necessary to take Amlodipine-Teva.

In elderly patients, T 1/2 may increase and drug clearance may decrease. No dose changes are required, but more careful monitoring of patients in this category is necessary.

In patients with impaired renal function, monitoring of the condition is necessary. The efficacy and safety of Amlodipine-Teva in hypertensive crisis has not been established.

Despite the absence of “withdrawal” syndrome in BMCC, discontinuation of treatment with Amlodipine-Teva should be carried out gradually reducing the dose of the drug.

Influence on the ability to drive vehicles and mechanisms:

Although taking Amlodipine-Teva did not have any negative effects on the ability to drive vehicles or other complex mechanisms, however, due to a possible excessive decrease in blood pressure, the development of dizziness, drowsiness and other adverse reactions, caution should be exercised in these situations, especially at the beginning of treatment and when increasing the dose.

Indications

-arterial hypertension.

stable exertional angina and vasospastic angina.

Use during pregnancy and lactation

In experimental studies, the fetotoxic and embryotoxic effects of the drug have not been established, but use during pregnancy is possible only if the benefit to the mother exceeds the potential risk to the fetus.

There are no data indicating the excretion of amlodipine in breast milk. However, other BMCC dihydropyridine derivatives are known to be excreted in breast milk. Therefore, if it is necessary to prescribe the drug Amlodipine-Teva during lactation, the issue of stopping breastfeeding should be resolved.

Contraindications

– hypersensitivity to amlodipine other derivatives of dihydropyridine and other components of the drug;

– severe hypotension (systolic BP less than 90 mm Hg. St. )

– cardiogenic shock;

acute myocardial infarction (during the first 28 days);

– unstable angina (with the exception of prinzmetals angina);

– obstruction of the outflow tract of the left ventricle;

– clinically significant aortic stenosis;

– age under 18 years (effectiveness and safety not established).

With caution:

liver function disorders sinus node weakness syndrome (severe bradycardia tachycardia) CHF of non-ischemic etiology W-IV functional class according to NYHA classification arterial hypotension aortic stenosis mitral stenosis acute myocardial infarction (after the first 28 days) elderly age impaired renal function.

Side effects

the Frequency of adverse reactions listed below were determined according to the following (classification of the world health organization): very often – at least 10%; often – not less than 1% but less than 10%; infrequently – not less than 01% but less than 1%; rarely – not less than 001% but less than 01%; very rarely – less than 001% including individual messages.

From the central nervous system-often-headache (especially at the beginning of treatment) dizziness increased fatigue drowsiness; infrequently-general malaise hypesthesia asthenia paresthesia peripheral neuropathy tremor insomnia emotional lability unusual dreams nervousness increased excitability depression anxiety increased sweating; rarely-convulsions apathy agitation; very rarely-ataxia amnesia migraine.

From the digestive system: often-nausea abdominal pain; infrequently-vomiting anorexia dry oral mucosa thirst; rarely-gum hyperplasia increased appetite; very rarely-pancreatitis gastritis jaundice (usually cholestatic) hyperbilirubinemia increased activity of “liver” transaminases hepatitis.

From the cardiovascular system: often-peripheral edema (ankles and feet) palpitations “flushes” of blood to the skin of the face; infrequently-excessive decrease in blood pressure orthostatic hypotension vasculitis; rarely-development or aggravation of the course of CHF; very rarely-fainting shortness of breath cardiac arrhythmias (including bradycardia ventricular tachycardia and atrial fibrillation) myocardial infarction chest pain pulmonary edema.

From the hematopoietic and lymphatic systems: very rarely – thrombocytopenic purpura leukopenia thrombocytopenia.

From the stroma of the urinary system: infrequently-pollakiuria painful urge to urinate nocturia; very rarely-dysuria polyuria.

From the reproductive system and mammary glands: infrequently-gynecomastia impotence.

Respiratory system disorders: infrequently-shortness of breath, rhinitis; very rarely – cough.

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

From the side of the skin: infrequently-alopecia; rarely-dermatitis; very rarely-alopecia xeroderma cold sticky sweat skin pigmentation disorder.

Allergic reactions: rarely-itchy skin rash (including erythematous maculopapular rash); very rarely-urticaria angioedema multiiform erythema.

From the side of the senses: infrequently-tinnitus visual disturbances diplopia accommodation disorders xerophthalmia conjunctivitis eye pain; very rarely-parosmia.

From the side of metabolism: very rarely – hyperglycemia.

Other services: infrequently-weight loss weight gain taste distortion nosebleeds chills.

Interaction

Amlodipine can be safely used for the treatment of arterial hypertension together with thiazide diuretics, alpha-blockers or ACE inhibitors. In patients with stable angina, amlodipine can be combined with other antianginal agents, such as long-acting or short-acting nitrates.

Unlike other BMCs, no clinically significant interaction of amlodipine (second generation BMCs) was found when co-administered with anti-inflammatory drugs (NSAIDs), including Indometacin. It is possible to enhance the antianginal and hypotensive effects of BMCC when combined with thiazide and loop diuretics, ACE inhibitors and nitrates, as well as to enhance their hypotensive effect when combined with alpha-1-blockers.

Erythromycin when used together increases the Cmax of amlodipine in young patients by 22% and in the elderly-by 50%.

Beta-blockers, when used concomitantly with amlodipine, can cause an exacerbation of the course of heart failure.

Although no negative inotropic effects have usually been observed in studies of amlodipine, some BMCs may increase the severity of the negative inotropic effects of antiarrhythmic agents that cause prolongation of the QT interval (for example, amiodarone and quinidine).

A single dose of 100 mg of sildenafil in patients with arterial hypertension does not affect the pharmacokinetics of amlodipine.

Repeated use of amlodipine at 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 (beverages containing alcohol): amlodipine with a single and repeated use in a dose of 10 mg does not affect the pharmacokinetics of ethanol.

Antiretroviral drugs (ritonavir) increase the plasma concentrations of BMCC, including amlodipine.

Neuroleptics and isoflurane-increase the hypotensive effect of dihydropyridine derivatives.

Calcium supplements can reduce the effect of BMCC.

When amlodipine is co-administered with lithium preparations, it is possible to increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Amlodipine does not alter the pharmacokinetics of cyclosporine.

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

It does not significantly affect the effect of warfarin (prothrombin time). Cimetidine does not affect the pharmacokinetics of amlodipine.

In vitro studies, amlodipine did not affect the plasma protein binding of digoxin, phenytoin, warfarin, and Indometacin.

Grapefruit juice: concomitant single oral use of 240 mg grapefruit juice and 10 mg amlodipine is not accompanied by a significant change in the pharmacokinetics of amlodipine.

Aluminum-or magnesium-containing antacids: their single use does not significantly affect the pharmacokinetics of amlodipine.

How to take, course of use and dosage

Inside once a day with the necessary amount of water (100 ml).

For arterial hypertension and angina pectoris, the initial dose is 5 mg once a day. In the absence of a therapeutic effect for 2-4 weeks, the dose of the drug can be increased to 10 mg/day. once.

In elderly patients

No dose adjustment is required.

In patients with impaired liver function

Although the T 1/2 of amlodipine, like all BMCC, increases in patients with impaired liver function, no dose adjustment is usually required (see section “Special instructions”).

In patients with renal insufficiency

It is recommended to use Amlodipine-Teva in normal doses (see the section “Special instructions”).

Overdose

Symptoms: a marked decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilation (risk of severe and persistent hypotension, including shock and death).

Treatment: gastric lavage use of activated charcoal (especially in the first 2 hours after overdose) maintenance of the cardiovascular system elevated position of the lower extremities monitoring of the heart and lungs control of the volume of circulating blood (BCC) and diuresis. To restore vascular tone – the use of vasoconstrictors (in the absence of contraindications to their use); to eliminate the consequences of calcium channel blockade – intravenous use of calcium gluconate. Hemodialysis is ineffective.

Special instructions