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

Active ingredient

Composition

1 tablet contains:

The active ingredient:

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

Auxiliary substances:

anhydrous lactose,

microcrystalline cellulose,

corn starch (dry),

talk,

silica colloidal anhydrous silica,

magnesium stearate.

How to take, the dosage

Ingestion, regardless of meals.

To treat arterial hypertension and prevent attacks of angina pectoris and vasospastic angina: The initial daily dose of Amlodipine is 5 mg in 1 dose.

If necessary, the dose may be increased to a maximum of 10 mg/day in a single dose.

Patients with low body weight or short stature and with severe hepatic impairment: lower doses may be required.

Patients with renal insufficiency and elderly patients: no dose adjustment is necessary.

Dose adjustment is not required when concomitantly administered with thiazide diuretics, beta-adrenoblockers and ACE inhibitors.

Interaction

Microsomal oxidation inhibitors may increase the plasma concentration of amlodipine, increasing the risk of side effects, and microsomal liver enzyme inducers may decrease it.

In contrast to other slow calcium channel blockers, there are no clinically significant interactions with NSAIDs, especially with indomethacin.

Tiazide and “loop” diuretics, beta-adrenoblockers, verapamil , ACE inhibitors and nitrates increase antianginal or hypotensive effects.

There is no effect on the pharmacokinetic parameters of digoxin and warfarin.

Cimetidine does not affect the pharmacokinetics of amlodipine.

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

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

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

Special Instructions

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

Although slow calcium channel blockers have no withdrawal syndrome, gradual dose reduction is recommended before discontinuing treatment.

Amlodipine may be prescribed in combination with thiazide diuretics, alpha- and beta-adrenoblockers, ACE inhibitors, sustained-release nitrates, sublingual nitroglycerin , NSAIDs, antibiotics, oral hypoglycemic agents.

Amlodipine has no adverse effect on metabolism and blood plasma lipids, therefore the drug can be used in patients with bronchial asthma, diabetes mellitus and gout.

Impact on ability to drive and operate machinery

The use of amlodipine does not affect the ability to drive or operate vehicles, but due to possible excessive decrease of BP, slower reaction time due to development of Dizziness, headache, increased fatigability and others.

Particular attention should be paid to the individual effect of the drug at the start of treatment and when changing the dosing regimen.

Contraindications

With caution: hepatic impairment, mild to moderate arterial hypotension, acute myocardial infarction and within the first month after it, aortic stenosis, decompensated chronic heart failure, CHF, hypertrophic obstructive cardiomyopathy, advanced age.

Side effects

Classification of side effects when using the drug by frequency of occurrence:

CNS and peripheral nervous system: frequently – headache, dizziness, fatigue, drowsiness, mood lability; rarely – asthenia, syncope, seizures, peripheral neuropathy, increased sweating, insomnia, depression; very rarely – apathy, ataxia, migraine.

Cardiovascular system disorders: frequently – palpitations, dyspnea, “flushes” of blood to the face, peripheral edema; rarely – pain in the chest, excessive reduction of BP, orthostatic hypotension; very rarely – cardiac rhythm disorders (ventricular tachycardia, atrial fibrillation), myocardial infarction, worsening of heart failure.

The digestive system: frequently – nausea, dry mouth, abdominal pain; rarely – dyspepsia, constipation, diarrhea, gum hyperplasia, pancreatitis; very rarely – gastritis, jaundice, increased liver transaminase activity.

Since the urinary system: rarely – pollakiuria.

As to the sexual system: rarely – impairment of sexual function, gynecomastia.

Muscular system: often – back pain; rarely – myalgia, arthralgia, muscle cramps.

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

Others: rare – visual disturbances, dyspnea, alopecia; very rare – hyperglycemia, thrombocytopenia.

Overdose

Symptoms: excessive peripheral vasodilation with clinically pronounced BP reduction with possible development of reflex tachycardia.

Treatment: Administration of activated charcoal (in the first 2 h after overdose), gastric lavage, elevated position of the extremities, control of cardiovascular and respiratory system functions, OBC and diuresis, active maintenance of cardiovascular functions, possible prescription of vasoconstrictors to restore vascular tone and increase BP, to eliminate the effects of calcium channel blockade – intravenous injection of calcium gluconate. Hemodialysis is ineffective.

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