Amlodipine Alkaloid, tablets 10 mg 30 pcs

A dihydropyridine derivative. It has antihypertensive and antianginal action. It blocks the entry of calcium ions through cell membranes into myocardial and vascular smooth muscle cells.

Antianginal action is due to dilation of coronary and peripheral arteries and arterioles: in angina reduces the severity of myocardial ischemia; by dilating peripheral arterioles, it reduces myocardial hypertension, reduces postload on the heart, reduces myocardial oxygen demand. By dilating the main coronary arteries and arterioles in the 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 tolerance, slows down the development of angina and “coronary depression” segment S-T, reduces the frequency of angina attacks and nitroglycerin consumption.

It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to direct vasodilating effect on vascular smooth muscle. In arterial hypertension a single dose provides clinically significant BP reduction for 24 hours (in “lying” and “standing” positions). It does not cause a sharp decrease in BP, decreases exercise tolerance and LV ejection fraction. It reduces the degree of LV myocardial hypertrophy, has anti-atherosclerotic and cardioprotective effect in CHD. It does not increase the risk of death in patients suffering from CHF (III-IV class according to NYHA), against the background of digoxin, diuretics and ACE inhibitors therapy.

It has no effect on myocardial contractility and conduction, does not cause reflex increase of HR, inhibits platelet aggregation, increases glomerular filtration rate, has weak natriuretic effect. In diabetic nephropathy it does not increase the severity of microalbuminuria. It does not have adverse effects on metabolism and plasma lipids and is suitable for treatment of patients with concomitant bronchial asthma and diabetes.

Pharmacokinetics:

Absorption – slow, does not depend on food intake, is about 90%, bioavailability – 60-65%. The tCmax when taken orally is 6-12 hours. Css is formed in 7-8 days after continuous use. The volume of distribution is 21 l/kg. Binding with plasma proteins is 90-97%. It penetrates through the BBB.
Intensively (90%) metabolized in the liver to form inactive metabolites, has “first pass” effect through the liver. T1/2 averaged 35 hours. Total clearance is 500 ml/min.

T1/2 in patients with arterial hypertension-48 hours in elderly patients is increased up to 65 hours, in hepatic insufficiency – up to 60 hours, similar parameters of T1/2 increase are observed in severe CHF, in renal impairment – unchanged. In hemodialysis it is not eliminated.
Excreted by the kidneys-60% as metabolites, 10% unchanged, with the bile and intestine-20-25% as metabolites, as well as with breast milk.

Indications

Arterial hypertension, angina pectoris, vasospastic angina pectoris.

Active ingredient

Amlodipine

Composition

One tablet contains amlodipine (as amlodipine besylate) 10,000 to 13,869 mg.

Auxiliary substances:

Lactose monohydrate,

Magnesium stearate,

Cellulose microcrystalline.

How to take, the dosage

Orally, the initial daily dose is 5 mg at a single dose with a gradual increase over 7-14 days to 10 mg/day once; with arterial hypertension, the maintenance dose is 2.5-5 mg/day.

In angina pectoris and vasospastic angina the dose is 5-10 mg/day once; for prevention of angina attacks – 10 mg/day.

Elderly and frail patients, patients with liver dysfunction are prescribed the initial dose of 2.5 mg as a hypotensive drug; 5 mg as an anti-angina drug.

No adjustment of amlodipine dose is required with concomitant use of thiazide diuretics, beta-adrenoblockers or angiotensin-converting enzyme inhibitors.

Interaction

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

Hypotensive effect is weakened by NSAIDs, especially indomethacin, (Na+ retention and blockade of Pg synthesis by kidneys), alpha-adrenergic stimulants, estrogens (Na+ retention), sympathomimetics.

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

Amiodarone, quinidine, alpha 1-adrenoblockers, antipsychotic drugs (neuroleptics) and BMCC may increase the hypotensive effect.

Does not affect pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect pharmacokinetics of amlodipine.

In concomitant use with the drugs Li+ there may be increased manifestations of their neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Ca2+ preparations may reduce the effect of PBMC.

Procainomide, quinidine and other drugs that cause Q-T interval prolongation increase the negative inotropic effect and may increase the risk of significant Q-T interval prolongation.

Special Instructions

During the treatment it is necessary to control body weight and see a dentist (to prevent soreness, bleeding and gum hyperplasia).

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

Despite the absence of “withdrawal” syndrome in BMCC, a gradual reduction in doses is recommended before discontinuing treatment.

Contraindications

.

Side effects

Nervous system: headache, dizziness, excessive fatigue, drowsiness, mood changes, seizures; rarely – loss of consciousness, hypoesthesia, paresthesia, tremor, asthenia, malaise, insomnia, nervousness, depression, unusual dreams, anxiety; very rarely – ataxia, apathy, agitation, amnesia.

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

Cardiovascular system: palpitation, edema of ankles and feet, dyspnea, blood “rushes” to the face, rare – arrhythmia (bradycardia, ventricular tachycardia, atrial flutter), chest pain, marked BP decrease, orthostatic hypotension; very rare – the development or worsening of heart failure, extrasystole, vasculitis, migraine.

Genitourinary system: rarely – pollakiuria, urge to urination, nycturia, sexual dysfunction (including decreased potency), very rarely – dysuria, polyuria.

Musculoskeletal system: rare – arthralgia, arthrosis, myalgia (with long-term use), very rare – myasthenia.

Skin: very rare – xeroderma, alopecia, dermatitis, purpura. Allergic reactions: skin itching, rash (including erythematous, maculopapular rash, urticaria).

Other: rare- visual disturbance, conjunctivitis, diplopia, eye pain, accommodation disturbance, xerophthalmia, tinnitus, gynecomastia, back pain, sensation of heat and blood “rushes” to face, chills, weight gain, dyspnea, nasal bleeding, increased sweating, thirst; very rare-cold sticky sweat, cough, rhinitis, parosmia, perversion of taste.

Overdose

Symptoms: excessive peripheral vasodilation, marked BP decrease, tachycardia.

Treatment: gastric lavage, administration of activated charcoal, maintenance of cardiac function, control of heart and lung function, elevated extremities, control of circulating blood volume (CBV) and diuresis, symptomatic and supportive therapy, intravenous calcium gluconate and dopamine. Hemodialysis is ineffective.

Similarities

Norvask, Amlodipine-Teva, Normodipine, Kalchek, Cardilopine, Amlodipine, Amlorus, Amlotop, Amlodipine-Teva