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Norvasc Amlodipine 2,5, 5, 10 mg
Most popular brand: Norvasc
Active ingredient: Amlodipine
Available dosage forms: 2,5, 5, 10 mg
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Amlodipine (Amlodipine): instruction, and the use of a formula

Amlodipinum ( genus. Amlodipini)

Chemical name

2 – [(2 – Aminoethoxy) methyl] – 4 – (2 – chlorophenyl) – 1,4 – dihydro – 6 – methyl – 3,5 – pyridine dicarboxylic acid 3 – ethyl 5 – methyl ester (as besylate and maleate)

Gross – formula

Therapeutic substance Amlodipine

The nosological classification (ICD – 10)

Code CAS

Feature substance Amlodipine

dihydropyridine derivative ; II generation calcium antagonist. White crystalline powder, slightly soluble in water, sparingly soluble in ethanol.

Pharmacology

Mode of action – vasodilating, anti-hypertensive, anti-anginal, antispasmodic.

Associated with the dihydropyridine receptors, blocking calcium channels inhibits the transmembrane passage of calcium ions into the cell (mostly ; in vascular smooth muscle cells than in cardiomyocytes). It has prolonged dose-dependent hypotensive effect. The antihypertensive effect is due to direct relaxing effect on smooth muscle of blood vessels, lowering systemic vascular resistance. It reduces the severity of myocardial ischemia due to the expansion of peripheral arterioles and decrease total peripheral vascular resistance against the backdrop of a changing heart rate a little. As a result of the weakening of the heart load decreases myocardial oxygen demand; expansion of large coronary arteries and the coronary arterioles in unmodified as well as in ischemic areas of the heart muscle increases the oxygen supply to the myocardium. Weakly affects the sinus and sine – atrial node, significantly slows AV conduction. It inhibits platelet aggregation; increases glomerular filtration rate, sodium excretion and urine output. The effect is a 1 – 2 hours after administration and lasts about 24 hours With the gradual manifestation of action and prolonged effect causes a gradual decline in blood pressure and a minimum reflex stimulation of the sympathetic nervous system.. With hypertension reduces the degree of left ventricular hypertrophy; It has antiatherosclerotic and cardioprotective effect in ischemic heart disease. Do not increase the risk of death in patients with heart failure (III – IV class NYHA), during therapy with digoxin, diuretics and ACE inhibitors,.

Absorbed (regardless of the meal) is slowly but almost completely. Bioavailability ; 60 – 65% (due to the effect of “first pass” through the liver). C max in the blood is achieved through 6 – 12 hours Linking plasma proteins .; 97 – 98%. With constant taking the equilibrium concentration is created in 7 – 8 days. The volume of distribution ; 20 l / kg. It passes through the BBB. Biotransformiroetsa in the liver to inactive metabolites; elimination of the two-phase: The first phase of ; short, the second lasts 35 – 50 hours total clearance of .; 0.5 l / min. Excreted in the urine (60% as metabolites, 10% ; in unchanged form) in the bile (20 – 25% as metabolites), and in breast milk. T 1/2 with impaired hepatic function and in elderly patients is prolonged, in violation of renal function ; unchanged.

Application of the substance Amlodipine

Arterial hypertension (monotherapy or in combination with other antihypertensive drugs), angina, stable and vasospastic (Prinzmetal), including patients resistant to therapy with nitrates or beta – blockers.

Contraindications

Hypersensitivity (including to other dihydropyridine), hypotension (less than 90 mm Hg. Art.), Shock, acute myocardial infarction (including the period of 1 month after it).

Restrictions on the use

Unstable angina, marked aortic stenosis, heart failure, liver dysfunction, age 18 years (safety and efficacy have not been determined).

Application of pregnancy and breastfeeding

It is possible during pregnancy if the expected effect of therapy outweighs the potential risk to the fetus.

Category effects on the fetus by FDA ; C.

breast-feeding should be discontinued at the time of treatment.

Side effects of substance Amlodipine

From the cardio – vascular system and blood (blood, hemostasis): facial flushing, palpitations; rare ; arrhythmias (bradycardia, ventricular tachycardia, atrial flutter), chest pain, hypotension (including orthostatic).

From the nervous system and sensory organs: fatigue, headache, dizziness, drowsiness; rare ; fatigue, asthenia, mood changes, visual disturbances.

With the genitourinary system: peripheral edema (swelling of the ankles and feet); rare ; increase in frequency of urination, impotence.

From the digestive tract: nausea, stomach pain; rare ; indigestion, change in bowel movement mode, jaundice.

From the respiratory system: rare ; shortness of breath.

From the musculo – skeletal system: rare ; arthralgia, myalgia, paresthesia and pain in the extremities (with prolonged use).

For the skin: rash, pruritus, rarely ; erythema multiforme.

Other: rare ; gingival hyperplasia, gynaecomastia, increase in liver enzymes.

Interaction

Compatible with major groups of antihypertensive drugs (diuretics, ACE inhibitors, beta -. Blockers), nitrates and hypoglycemic drugs. Means for inhalation anesthesia (derivatives of hydrocarbons), amiodarone, quinidine, and other calcium antagonists may increase the effects. NSAIDs (especially indomethacin) reduce the hypotensive effect (inhibit prostaglandin synthesis in the kidneys and natriuresis).

Overdose

Symptoms: excessive peripheral vasodilation, marked and prolonged decrease in blood pressure. tachycardia.

Treatment: gastric lavage, the appointment of activated carbon, giving the horizontal position of the patient with elevated legs, monitoring indicators of the heart and lungs, monitoring BCC and diuresis; symptomatic and supportive therapy, intravenously a liquid, calcium gluconate, dopamine, phenylephrine. Hemodialysis is not effective.

Dosing and Administration

Inside, starting dose ; 2,5 – 5 mg 1 time a day, the usual dose ; 5 mg per day dose can be gradually increased to a maximum if necessary; 10 mg 1 time a day.

Precautions substance Amlodipine

Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention (at the beginning of treatment may be dizziness and drowsiness).

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