Amlodipine-Vertex, tablets 5 mg 30 pcs

Amlodipine is a dihydropyridine derivative, a “slow” calcium channels blocker (BMCC) of II generation, has antianginal and hypotensive effects. By binding to dihydropyridine receptors, it blocks calcium channels, reduces transmembrane transfer of calcium ions into cells (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; by dilation of peripheral arterioles it reduces total peripheral vascular resistance; reduces cardiac preload and myocardial oxygen demand.

Dilates main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases oxygen supply to the myocardium (especially in vasospastic angina); prevents development of coronary artery spasm (including that caused by smoking).

In patients with 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 nitroglycerin consumption. Amlodipine has a long-term dose-dependent hypotensive effect, which is due to a direct vasodilator effect on vascular smooth muscle. In arterial hypertension a single daily dose of amlodipine provides clinically significant reduction of arterial pressure (BP) for 24 hours (in “lying” and “standing” position of the patient).

Limits the degree of myocardial hypertrophy of the left ventricle, has anti-atherosclerotic and cardioprotective effect in CHD. It does not affect myocardial contractility and conduction, inhibits platelet aggregation, increases glomerular filtration rate, has a weak natriuretic effect.

In diabetic nephropathy it does not increase the severity of microalbuminuria. It has no adverse effect on metabolism and concentration of blood plasma lipids. Time of onset of therapeutic effect is 2-4 hours, duration – 24 hours.

Indications

Active ingredient

Composition

1 tablet contains:

The active ingredient:

amlodipine besylate (in terms of amlodipine) – 5 mg.

Excipients:

calcium stearate,

potato starch,

lactose (milk sugar),

magnesium stearate,

microcrystalline cellulose.

How to take, the dosage

Ingestion, regardless of meals.

For the treatment of arterial hypertension and prevention of attacks of angina pectoris and vasospastic angina:

The initial dose of Amlodipine is 5 mg once daily. If necessary, the daily dose can be increased to a maximum of 10 mg (once daily).

Interaction

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

Unlike other DMARDs, amlodipine has no clinically significant interactions with nonsteroidal anti-inflammatory drugs, especially indomethacin.

Thiazide and “loop” diuretics, beta-adrenoblockers, verapamil, ACE inhibitors and nitrates enhance the antianginal or hypotensive effects of amlodipine.

Amiodarone, quinidine, alpha 1-adrenoblockers, antipsychotics (neuroleptics) and isoflurane may increase the hypotensive effects of amlodipine.

Calcium preparations may decrease the effect of BMCC.

The co-administration of amlodipine with lithium preparations may increase the neurotoxicity of the latter (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Amlodipine has no effect on the pharmacokinetic parameters of digoxin and warfarin.

Cimetidine has no effect on the pharmacokinetics of amlodipine.

The antiviral agents (ritonavir) contribute to increased plasma concentrations of PBMCs (including amlodipine).

Special Instructions

Application in hepatic impairment: Patients with hepatic impairment as a hypotensive agent Amlodipine is prescribed with caution, in an initial dose of 2.5 mg, as an antianginal agent – 5mg.

Use in renal impairment:No dose changes are required in patients with renal impairment.

In elderly patients:The T 1/2 may be increased and creatinine clearance (CK) may be decreased. No dose changes are required, but closer monitoring of patients is necessary.

Dose changes are not required when concomitantly administered with thiazide diuretics, beta-adrenoblockers and angiotensin-converting enzyme (ACE) inhibitors.

Amlodipine treatment requires monitoring patients’ body weight and sodium salt intake; an appropriate low-salt diet is indicated. Dental hygiene should be maintained and regular visits to the dentist (to prevent soreness, bleeding and gum hyperplasia).

The dosing regimen of Amlodipine in elderly patients is similar to that in patients of other age groups. Careful monitoring of elderly patients is necessary when increasing the dose. Although there is no withdrawal syndrome in AMLs, a gradual dose reduction is recommended before discontinuing treatment.

Amlodipine does not affect plasma concentrations of potassium ions, glucose, triglycerides, total cholesterol, low-density lipoproteins, uric acid, creatinine and urea nitrogen. Abrupt withdrawal of the drug should be avoided because of the risk of worsening the course of angina pectoris. Amlodipine tablets are not recommended for hypertensive crisis.

Patients of low body weight, short stature, and patients with significant liver dysfunction may require a lower dose.

Influence on driving and operating machinery

There have been no reports about the effect of Amlodipine on driving or operating machinery. However, drowsiness and Dizziness may occur in some patients, mainly at the beginning of treatment. If they occur, caution should be exercised when driving motor transport and engaging in potentially dangerous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Side effects

Cardiovascular system: often – palpitations, peripheral edema (swelling of ankles and feet); infrequent – excessive reduction of BP, orthostatic hypotension, vasculitis; rare – development or aggravation of chronic heart failure; very rare – rhythm disturbances ( bradycardia, ventricular tachycardia, atrial fibrillation), myocardial infarction, chest pain, migraine .

From the central nervous system: often – headache, dizziness, increased fatigue; infrequent – malaise, fainting, neuropsychiatric asthenization, hypoesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, emotional lability, unusual dreams, nervousness, depression, anxiety; rarely – convulsions, apathy, agitation; very rarely – ataxia, amnesia.

Hematopoietic organs:very rarely – thrombocytopenia, leukopenia, thrombocytopenic purpura.

In the respiratory system: infrequent – shortness of breath, rhinitis; very rare – cough.

From the digestive tract: often – nausea, abdominal pain; infrequent – vomiting, changes in defecation (including constipation, flatulence), dyspepsia, diarrhea, anorexia, dry oral mucosa, thirst; rarely – gingival hyperplasia, increased appetite; very rarely – gastritis, pancreatitis, hyperbilirubinemia, jaundice (usually cholestatic), increased activity of “liver” transaminases, hepatitis.

Urogenital system disorders: infrequent – pollakiuria, painful urge to urinate, nycturia, impotence; very rare – dysuria, polyuria.

Skin disorders: seldom – increased sweating; very rare – cold sticky sweat, xeroderma, alopecia, dermatitis, purpura, changes in skin color.

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

Musculoskeletal system: infrequent – arthralgia, muscle cramps, arthrosis, myalgia (with long-term use), back pain; rarely – myasthenia.

Others: infrequent – alopecia, tinnitus, gynecomastia, weight gain/decrease, visual disturbance, diplopia, accommodation disturbance, xerophthalmia, conjunctivitis, eye pain, perversion of taste, chills, nosebleed, increased sweating; rarely – dermatitis; very rarely – cold sticky sweat, parosmia, skin pigmentation disorders, hyperglycemia.

Overdose

Symptoms:

A pronounced decrease in BP with possible development of reflex tachycardia and excessive peripheral vasodilation (risk of severe and persistent arterial hypotension, including development of shock and death).

Treatment:

Gastric lavage, administration of activated charcoal (especially in the first 2 hours after overdose), maintenance of cardiovascular function, control of cardiac and pulmonary function parameters, Trendelenburg posture, control of circulating blood volume and diuresis. To restore vascular tone – the use of vasoconstrictors (if there are no contraindications for their use); to eliminate the effects of calcium channel blockade – intravenous injection of calcium gluconate. Hemodialysis is not effective.

Pregnancy use

There has been no teratogenicity of amlodipine in animal studies, but there is no clinical experience with its use in pregnancy and lactation.

Therefore, amlodipine should not be administered to pregnant and lactating women or to women of childbearing age unless they use reliable contraception.

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