Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Norvasc
Active ingredient: Amlodipine
Available dosage forms: 2,5, 5, 10 mg
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Amlodipine general information
Superior blood pressure is also recognized as hypertension. In the event the superior blood pressure isn’t controlled it can bring about health problems like stroke, heart attack as well as heart disease. Don’t grow the dose of the medicine by yourself. Before using the Amlodipine medicine you need to know complete information regarding the medicine so as to prevent any serious side effect. You must avoid drinking alcoholic beverages if you’re taking Amlodipine Tablets. Amlodipine medicines shouldn’t use in children, unless it’s recommended by the physician.
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Amlodipine (Amlodipine): instruction, and the use of a formula
Amlodipinum ( genus. Amlodipini)
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)
Feature substance Amlodipine
dihydropyridine derivative ; II generation calcium antagonist. White crystalline powder, slightly soluble in water, sparingly soluble in ethanol.
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.
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.
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).
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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