Amlodipine pills 10mg, 90pcs

Composition

1 tablet contains:

Active ingredient:  

• amlodipine besylate, based on amlodipine 10 mg;

excipients:  

• calcium stearate 0.2 mg,

• potato starch 38.86 mg,

• colloidal silicon dioxide 1 mg,

• lactose monohydrate 100 mg,

• magnesium stearate 1.8 mg,

• microcrystalline cellulose 44.28 mg

Pharmacological action

Pharmacodynamics

Amlodipine, a dihydropyridine derivative, is a second-generation slow calcium channel blocker that has antianginal and antihypertensive effects.

Binding to dihydropyridine receptors, it blocks calcium channels, reduces the transmembrane transfer of calcium ions into the cell (to a greater extent in vascular smooth muscle cells than in cardiomyocytes).

The antianginal effect is caused by dilation of the coronary and peripheral arteries and arterioles:

when angina reduces the severity of myocardial ischemia; dilating peripheral arterioles, reduces the total peripheral vascular resistance; it reduces afterload on the heart, the need of myocardium in oxygen;

– dilates the main coronary arteries and arterioles in the intact and ischemic zones of the myocardium, increases the supply of oxygen to the myocardium (especially when vasospastic angina); prevents the development of spasm of the coronary arteries (including caused by Smoking).

In patients with stable angina, a single daily dose increases exercise tolerance, delays the development of another angina attack and “ischemic” ST-segment depression; reduces the frequency of angina attacks and consumption of nitroglycerin and other nitrates.

Amlodipine has a long-term dose-dependent hypotensive effect, which is due to the direct vasodilating effect on vascular smooth muscles. In patients with arterial hypertension, a single daily dose of amlodipine provides a clinically significant reduction in blood pressure (BP) over 24 hours (in the patient’s “lying” and “standing”positions).

Orthostatic hypotension with the use of amlodipine is quite rare. Amlodipine does not cause a decrease in exercise tolerance, 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, and 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.

The time of onset of the therapeutic effect is 2-4 hours, 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), who have suffered a myocardial infarction, percutaneous transluminal coronary angioplasty (PTCA) or in patients with angina pectoris, the use of amlodipine prevents the development of thickening of the intima-media of the carotid arteries, reduces mortality from myocardial infarction, stroke, PTCA, aorto-coronary bypass surgery; reduces the number of hospitalizations for 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 mortality rate or the development of complications and deaths in patients with CHF (NYHA functional class III-IV) during therapy with digoxin, diuretics, and angiotensin-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

Suction

After oral use, amlodipine is slowly absorbed from the gastrointestinal tract. Food intake does not affect the absorption of amlodipine. The average absolute bioavailability is 64-80%. The maximum concentration in the blood serum is observed after 6-12 hours. The equilibrium concentration is reached after 7-8 days of therapy. Simultaneous food intake does not affect the absorption of amlodipine.

Distribution

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 (97.5%) binds to plasma proteins.

Metabolism

Amlodipine undergoes slow but active metabolism (90-97%) in the liver in the absence of a significant “first pass” effect.

The metabolites do not have significant pharmacological activity.

Deduction

After a single dose, the half-life (T 1/2) varies from 35 to 50 hours. With repeated use, 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% in unchanged form,20-25% – with bile and through the intestine in the form of metabolites.

The total clearance of amlodipine is 0.116 ml / s / kg (7 ml / min / kg,0.42 l / h/kg).

Use in elderly patients

In elderly patients (over 65 years of age), the elimination of amlodipine is slowed (T 1/2 – 65 h) compared to young patients, but this difference is not clinically significant.

Use in patients with hepatic insufficiency

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).

Use in patients with renal insufficiency

Renal failure does not significantly affect the kinetics of amlodipine. Amlodipine penetrates the blood-brain barrier and is not removed by hemodialysis.

Indications

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

• stable angina and vasospastic angina (Prinzmetal angina or variant angina) both in monotherapy and in combination with other antianginal agents).

Use during pregnancy and lactation

The safety of using Amlodipine during pregnancy has not been established, so use during pregnancy is possible only if the benefit to the mother exceeds the risk to the fetus and newborn.

There are no data indicating the excretion of amlodipine in breast milk. However, other BMCC derivatives of dihydropyridine are known to be excreted in breast milk. In this regard, if it is necessary to use the drug Amlodipine during lactation, the question of stopping breastfeeding should be decided.

No effect of amlodipine on fertility was found in a rat study.

Contraindications

• hypersensitivity to amlodipine and other dihydropyridine derivatives;
• severe hypotension;
• collapse, cardiogenic shock;
• unstable angina (except Prinzmetal angina) 
• pregnancy and lactation;
• age up to 18 years (efficacy and safety have not been established).

With caution: impaired liver function, sinus node weakness syndrome (severe bradycardia, tachycardia), chronic heart failure in the decompensation stage, mild or moderate arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), diabetes mellitus, lipid profile disorders, elderly age.

Side effects

WHO classification of frequency of side effects:

very common – ≥1/10;

common – ≥1/100 to < 1/10;

uncommon – ≥1/1000 to <1/100;

rare – ≥1/10000 to <1/1000;

very rare – <1/10000, including individual reports;

frequency unknown – it is not possible to determine the frequency of occurrence according to available data.

From the cardiovascular system:

often, palpitations, peripheral edema (swelling of the ankles and feet), tides of blood to the face;

infrequently – excessive decrease in blood pressure;

rarely – fainting, shortness of breath, vasculitis, orthostatic hypotension, the development or the exacerbation of chronic heart failure, arrhythmias (including bradycardia, ventricular tachycardia, atrial fibrillation), myocardial infarction, pain in the chest.

From the musculoskeletal system:

infrequently-arthralgia, muscle cramps, arthrosis, myalgia (with prolonged use), back pain;

rarely-myasthenia gravis.

From the central nervous system:

often – headache, dizziness, fatigue;

rarely – malaise, syncope, asthenia, hypesthesia, paresthesia,

peripheral neuropathy, tremor, insomnia, emotional lability, unusual dreams, increased irritability, depression, anxiety, tinnitus, taste perversion;

very rarely – headache, increased sweating, lethargy, agitation, ataxia, amnesia;

frequency unknown – extrapyramidal disorders.

From the digestive system:

often – nausea, abdominal pain;

infrequently-vomiting, constipation or diarrhea, flatulence, dyspepsia, anorexia, dry oral mucosa, thirst;

rarely-gum hyperplasia, increased appetite;

very rarely-gastritis, pancreatitis, hyperbilirubinemia, jaundice (usually cholestatic), increased activity of liver transaminases, hepatitis.

From the side of hematopoietic organs:

very rarely – thrombocytopenia, leukopenia, thrombocytopenic purpura.

Respiratory system disorders:

infrequently – shortness of breath, rhinitis, nosebleeds;

very rarely-cough.

From the side of the senses:

infrequently – diplopia, accommodation disorders, xerophthalmia, conjunctivitis, eye pain, visual disturbances.

From the genitourinary system:

infrequently-frequent urination, painful urination, nocturia, erectile dysfunction;

very rarely-dysuria, polyuria.

From the side of the skin:

rarely-dermatitis;

very rarely-cold sweat, xeroderma, alopecia, skin pigmentation disorder.

Allergic reactions:

infrequently – skin pruritus, rash (including erythematous, maculopapular rash, urticaria);

very rarely-angioedema, erythema multiforme.

Laboratory parameters:

very rarely – hyperglycemia.

Other services:

infrequently – chills, gynecomastia, pain of unspecified localization, alopecia; very rarely – parosmia.

Interaction

Inhibitors of microsomal oxidation increase the concentration of amlodipine in blood plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes reduce.

The antihypertensive effect is weakened by nonsteroidal anti-inflammatory drugs, especially Indometacin (sodium retention and blockade of prostaglandin synthesis by the kidneys), alpha-adrenostimulants, estrogens (sodium retention), sympathomimetics.

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

Amiodarone, quinidine, alpha-1-adrenoblockers, antipsychotic drugs (neuroleptics), and slow calcium channel blockers may enhance the antihypertensive effect.

It does not affect the pharmacokinetic parameters of digoxin and warfarin.

Cimetidine does not affect the pharmacokinetics of amlodipine.

When combined with lithium preparations, it is possible to increase the manifestations of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Calcium supplements can reduce the effect of slow-acting calcium channel blockers. Procainamide, quinidine, and other drugs that cause prolongation of the QT interval increase the negative inotropic effect and may increase the risk of significant prolongation of the QT interval.

Grapefruit juice may reduce the concentration of amlodipine in the blood plasma, but this decrease is so small that it does not significantly change the effect of amlodipine.

How to take, course of use and dosage

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

With arterial hypertension, angina pectoris, the initial dose of amlodipine is usually 5 mg once a day. Depending on the therapeutic response, the daily dose can be increased to a maximum of 10 mg (once a day).

Use in elderly patients

Amlodipine is recommended for use in an average therapeutic dose, no dose adjustment is required.

Use in patients with impaired liver function

Despite the fact that T 1/2 of amlodipine, like all BMCC, increases in patients with impaired liver function, dose adjustment is usually not required (see the section “Special instructions”).

Use in patients with impaired renal function.

It is recommended to use amlodipine in normal doses, but it is necessary to take into account the possible slight increase in T 1/2.

No dose adjustment is required when co-administered with thiazide diuretics, beta-blockers, and angiotensin-converting enzyme (ACE) inhibitors.

Overdose

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

Treatment: gastric lavage, use of activated charcoal, maintenance of the cardiovascular system, monitoring of heart and lung function indicators, elevated position of the limbs, monitoring of the volume of circulating blood and diuresis. To restore vascular tone – the use of vasoconstrictor drugs (in the absence of contraindications to their use); to eliminate the consequences of calcium channel blockade – intravenous use of calcium gluconate. Hemodialysis is not effective.

Special instructions

During the treatment period, it is necessary to monitor body weight and sodium intake, prescribe an appropriate diet.

It is necessary to maintain dental hygiene and frequent visits to the dentist (to prevent soreness, bleeding and gum hyperplasia). The dosage regimen for the elderly is the same as for patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary.

Despite the absence of a “slow” calcium channel blocker withdrawal syndrome, a gradual dose reduction is recommended before discontinuing treatment.

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

Influence on the ability to drive a car and mechanisms

No effects of amlodipine on driving or working with machinery have been reported. However, some patients may experience drowsiness and dizziness primarily at the beginning of treatment. If they occur, the patient should take special precautions when driving a car and working with mechanisms.

Form of production

Pills.

Storage conditions

Store at a temperature not exceeding 25°C.

Shelf

life is 5 years.

Active ingredient

Amlodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Angina