Amlodipine Sandoz, tablets 5 mg 30 pcs

Slow calcium channel blocker, dihydropyridine derivative. It has antihypertensive and antianginal action. By binding to dihydropyridine receptors it blocks calcium channels, reduces transmembrane transfer of calcium ions into cell (more in vascular smooth muscle cells than in cardiomyocytes).

The antianginal action is caused by the dilation of coronary and peripheral arteries and arterioles: in angina pectoris it reduces myocardial ischemia; dilation of peripheral arterioles reduces the total peripheral resistance of vessels, reduces the preload on the heart, reduces myocardial oxygen demand.

Dilating the main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases the flow of oxygen to the myocardium (especially in vasospastic angina); prevents the development of coronary artery constriction (including that caused by smoking). In patients with angina a single daily dose increases exercise time, slows the development of angina and ischemic ST-segment depression, reduces the frequency of angina attacks and nitroglycerin consumption.

It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to the direct vasodilating effect on the vascular smooth muscles. In arterial hypertension a single dose provides clinically significant reduction of BP during 24 hours (in a patient lying and standing position).

It does not cause sharp decrease of BP, decrease of tolerance to physical load, left ventricular ejection fraction. It reduces the degree of myocardial hypertrophy of the left ventricle, has anti-atherosclerotic and cardioprotective effect in coronary heart disease. It does not influence myocardial contractility and conduction, does not cause reflex increase of heart rate, inhibits platelet aggregation, increases glomerular filtration rate, has weak natriuretic effect.

In diabetic nephropathy it does not increase the severity of microalbuminuria. It has no adverse effect on metabolism and blood plasma lipids.

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

Indications

Arterial hypertension.
Stable exertional angina.
Vasospastic angina (Prinzmetal’s angina).

Pharmacological effect

Slow calcium channel blocker, dihydropyridine derivative. Has antihypertensive and antianginal effects. By binding to dihydropyridine receptors, it blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (more into vascular smooth muscle cells than into cardiomyocytes).

The antianginal effect is due to the expansion of the coronary and peripheral arteries and arterioles: in case of angina pectoris, it reduces the severity of myocardial ischemia; by expanding peripheral arterioles, it reduces Total peripheral vascular resistance, reduces preload on the heart, and reduces myocardial oxygen demand.

By expanding the main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, it increases the supply of oxygen to the myocardium (especially with vasospastic angina); prevents the development of constriction of the coronary arteries (including those caused by smoking). In patients with angina pectoris, a single daily dose increases the time of physical activity, slows down the development of angina and ischemic depression of the ST segment, reduces the frequency of angina attacks and nitroglycerin consumption.

It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilating effect on vascular smooth muscle. For arterial hypertension, a single dose provides a clinically significant reduction in blood pressure over 24 hours (with the patient lying and standing).

Does not cause a sharp decrease in blood pressure, exercise tolerance, or left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy, has an antiatherosclerotic and cardioprotective effect in coronary heart disease. It has no effect on myocardial contractility and conductivity, does not cause a reflex increase in heart rate, 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. Does not have an adverse effect on metabolism and blood plasma lipids.

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

Special instructions

It is optimal to use the drug every day at the same time.

Despite the absence of withdrawal symptoms with slow calcium channel blockers, a gradual dose reduction is recommended before stopping treatment.

Amlodipine can be prescribed in combination with thiazide diuretics, alpha and beta blockers, ACE inhibitors, long-acting nitrates, sublingual nitroglycerin, NSAIDs, antibiotics, and oral hypoglycemic agents.

Amlodipine does not have an adverse effect on metabolism and plasma lipids, so the drug can be used in patients with bronchial asthma, diabetes mellitus and gout.

Impact on the ability to drive vehicles and operate machinery

The use of amlodipine does not affect the ability to drive vehicles or other technical equipment, however, due to a possible excessive decrease in blood pressure, a slowdown in reaction speed due to the development of dizziness, headache, increased fatigue, etc. side effects, you should carefully consider the individual effect of the drug at the beginning of the course of treatment and when changing the dosage regimen.

Active ingredient

Amlodipine

Composition

1 tablet contains:

Active substance:

amlodipine besylate (which corresponds to the content of amlodipine 5 mg) – 6.934 mg.

Excipients:

lactose anhydrous,

microcrystalline cellulose,

corn starch (dry),

talc,

silicon dioxide colloidal anhydrous,

magnesium stearate.

Contraindications

Severe arterial hypotension.
Collapse.
Cardiogenic shock.
Unstable angina (with the exception of Prinzmetal’s angina).
Age up to 18 years (efficacy and safety have not been established).
Hereditary lactose intolerance, galactosemia (the drug contains lactose).
Hypersensitivity to the components of the drug.
Hypersensitivity to other dihydropyridine derivatives.

With caution: liver failure, mild or moderate arterial hypotension, acute myocardial infarction and during the first month after it, aortic stenosis, chronic heart failure in the stage of decompensation, cardiovascular disease, hypertrophic obstructive cardiomyopathy, old age.

Side Effects

Classification of side effects when using the drug according to frequency of occurrence:

Often (more than 1%).
Rarely (0.1% to 1%).
Very rare (less than 0.01%).

From the central nervous system and peripheral nervous system: often – headache, dizziness, fatigue, drowsiness, mood lability; rarely – asthenia, fainting, convulsions, peripheral neuropathy, increased sweating, insomnia, depression; very rarely – apathy, ataxia, migraine.

From the cardiovascular system: often – palpitations, shortness of breath, flushes of blood to the face, peripheral edema; rarely – chest pain, excessive decrease in blood pressure, orthostatic hypotension; very rarely – heart rhythm disturbances (ventricular tachycardia, atrial fibrillation), myocardial infarction, worsening heart failure.

From the digestive system: often – nausea, dry mouth, abdominal pain; rarely – dyspepsia, constipation, diarrhea, gingival hyperplasia, pancreatitis; very rarely – gastritis, jaundice, increased activity of liver transaminases.

From the urinary system: rarely – pollakiuria.

From the reproductive system: rarely – sexual dysfunction, gynecomastia.

From the musculoskeletal system: often – back pain; rarely – myalgia, arthralgia, muscle cramps.

Allergic reactions: rarely – skin itching, rash; very rarely – erythema multiforme, angioedema.

Other: rarely – visual impairment, dyspnea, alopecia; very rarely – hyperglycemia, thrombocytopenia.

Interaction

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

Unlike other slow calcium channel blockers, there is no clinically significant interaction with NSAIDs, especially indomethacin.

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

Does not affect the pharmacokinetic parameters of digoxin and warfarin.

Cimetidine does not affect the pharmacokinetics of amlodipine.

Calcium supplements may reduce the effect of slow calcium channel blockers.

Antivirals (ritonavir) increase plasma concentrations of slow calcium channel blockers.

Neuroleptics and isoflurane – enhance the hypotensive effect of dihydropyridine derivatives.

Overdose

Symptoms: excessive peripheral vasodilation with a clinically significant decrease in blood pressure with the possible development of reflex tachycardia.

Treatment: administration of activated carbon (in the first 2 hours after an overdose), gastric lavage, elevated position of the extremities, control of the functions of the cardiovascular and respiratory systems, blood volume and diuresis, active maintenance of the functions of the cardiovascular system, it is possible to prescribe vasoconstrictor drugs to restore vascular tone and increase blood pressure, to eliminate the consequences of calcium channel blockade – intravenous administration of calcium gluconate. Hemodialysis is ineffective.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25°C.

Shelf life

2 years.

Manufacturer

Lek d.d., Slovenia