Amlodipine Sandoz, pills 10mg, 30pcs

Composition

1 tablet contains amlodipine (in the form of bezylate) 10 mg.

Auxiliary substances:

microcrystalline cellulose – 142.73 mg,

calcium hydrophosphate dihydrate-75 mg,

sodium carboxymethyl starch (type A) – 4.8 mg,

magnesium stearate-3.6 mg

Pharmacological action

Pharmaceutical group:

blocker of “slow” calcium channels.

Pharmaceutical action:  

Amlodipine Sandoz is a slow calcium channel blocker, a dihydropyridine derivative. It has antihypertensive and antianginal 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).

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 for 24 hours (in the patient’s lying and standing positions). It does not cause a sharp decrease in blood pressure, reduced exercise tolerance, or left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy, has anti-atherosclerotic and cardioprotective effects in CHD. It does not affect the contractility and conduction of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the glomerular filtration rate, and has a weak natriuretic effect.

The antianginal effect is caused by the expansion of coronary and peripheral arteries and arterioles: in angina pectoris, it reduces the severity of myocardial ischemia; by expanding peripheral arterioles, it reduces OPSS, reduces preload on the heart, and reduces the need for oxygen in the myocardium. Dilating the main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases oxygen supply to the myocardium (especially in vasospastic angina); prevents the development of coronary artery constriction (including caused by smoking). In patients with angina pectoris, a single daily dose increases exercise time, slows down the development of angina and ST-segment ischemic depression, reduces the frequency of angina attacks and nitroglycerin consumption.

In diabetic nephropathy, it does not increase the severity of microalbuminuria. It does not adversely affect the metabolism and blood plasma lipids.

The time of onset of the effect is 2-4 hours, the duration of the effect is 24 hours

. Pharmacokinetics:

 Absorption After oral use, amlodipine is slowly absorbed from the gastrointestinal tract. The average absolute bioavailability is 64%, Cmax in blood plasma is observed in 6-9 hours. Css is reached after 7 days of therapy. Food intake does not affect the absorption of amlodipine.

Distribution The average Vd is 21 l / kg of body weight, which indicates 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 plasma proteins. Penetrates through the BBB.

Metabolismamlodipine undergoes a slow but extensive metabolism (90%) in the liver with the formation of inactive metabolites. It has a “first pass” effect through the liver. The metabolites do not have significant pharmacological activity.

Excretion After a single oral dose, T 1/2 varies from 31 to 48 hours, with repeated use, T 1/2 is approximately 45 hours. About 60% of the oral dose is excreted in the urine mainly in the form of metabolites,10% – unchanged, and 20-25% – with feces, as well as with breast milk. The total clearance of amlodipine is 0.116 ml / s / kg (7 ml / min / kg,0.42 l / h/kg).

Pharmacokinetics in special clinical cases

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.

In patients with hepatic insufficiency, T 1/2 is expected to be prolonged, and with prolonged use, the accumulation of the drug in the body will be higher (T 1/2 increases to 60 hours).

Renal failure does not significantly affect the kinetics of amlodipine.

It is not removed during hemodialysis.

Indications

Arterial hypertension (including in combination therapy), stable angina, unstable angina (including Prinzmetal angina).

Use during pregnancy and lactation

The safety of using Amlodipine during pregnancy and lactation has not been established.

Use is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus or child.

Contraindications

Severe arterial hypotension.

Hypersensitivity to dihydropyridine derivatives.

Side effects

From the cardiovascular system:  possible peripheral edema, palpitations, hyperemia of the skin; when used in high doses – hypotension, arrhythmias, shortness of breath.

From the digestive system:  nausea, abdominal pain; rarely gum hyperplasia.

From the central nervous system:  possible headaches, fatigue, drowsiness, dizziness.

Allergic reactions:  skin rash, itching.

Interaction

When Amlodipine is used concomitantly with other antihypertensive drugs, the hypotensive effect may increase; with inhaled anesthesia, the hypotensive effect may increase;

with lithium preparations, neurotoxicity may occur, including nausea, vomiting, diarrhea, ataxia, trembling and/or tinnitus; with sympathomimetics, the hypotensive effect may decrease.

Indometacin and other NSAIDs may reduce the hypotensive effect of amlodipine by inhibiting prostaglandin synthesis in the kidneys and / or causing fluid retention.

How to take, course of use and dosage

For adults, when taken orally, the initial dose is 5 mg 1 time/day.

If necessary, the dose can be increased.

Maximum dose:  when taken orally-10 mg / day.

Overdose

Symptoms: excessive peripheral vasodilation with a pronounced and possibly prolonged decrease in blood pressure, collapse, shock.

Treatment: gastric lavage, use of activated charcoal, maintenance of the cardiovascular system, monitoring of heart and lung function, elevated, above head level, position of the lower extremities, control of BCC and diuresis.

To restore vascular tone – the use of vasoconstrictors (in the absence of contraindications to their use); in order to eliminate the consequences of calcium channel blockade – intravenous use of calcium gluconate. Hemodialysis is ineffective.

Special instructions

Amlodipine is used with caution in patients with impaired liver function, aortic stenosis, and chronic heart failure.

Patients with impaired renal function, as well as elderly patients, do not need to reduce the dose.

It is possible to use amlodipine for the treatment of patients with dilated (non-ischemic) cardiomyopathy accompanied by severe chronic heart failure.

There are no clinical data on the use of amlodipine in children.

Form of production

Pills.

Storage conditions

Store in a dry place at a temperature not exceeding 25°C, out of the reach of children.

Shelf

life is 2 years.

Active ingredient

Amlodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults as directed by your doctor

Indications

Hypertension, Angina