Amlodipine: instructions for use
- Amlodipine: instructions for use
ATX code: C08CA01 (Amlodipine).
Dosage form: biconvex tablets of round shape, white. One side is smooth, the other side is engraved "АВ 5".
Clinico-pharmacological group: blocker of slow calcium channels.
Pharmacotherapeutic group: antihypertensive, antianginal.
Actively active substance : amlodipine besylate.
Excipients: microcrystalline cellulose, anhydrous calcium hydrophosphate, magnesium stearate, sodium carboxylmethyl starch (type A).
Amlodipine besylate, which is a derivative of dihydropyridine, has a blocking effect on calcium channels, reducing the transmembrane transition of calcium ions into smooth muscle vascular cells. Its ability to expand coronary vessels is due to the expansion of arteries and arterioles, a reduction in overall peripheral vascular resistance. With the development of angina pectoris, this drug reduces the severity of ischemia, increases the flow of oxygen into the myocardium, reduces the load on the heart, prevents spasm of the coronary arteries, increases exercise tolerance, reduces the frequency of angina attacks.
The hypotensive effect of amlodipine is due to a direct vasodilator effect on the smooth muscle of the vessels. In patients suffering from hypertension, when taking a single dose of the drug for 24 hours, there is a clinically significant decrease in blood pressure. The development of orthostatic hypotension with the use of a drug is quite a rare phenomenon. Reduces the degree of hypertrophy of the left ventricular myocardium, does not affect cardiac contractility and conductivity, does not lead to a reflex increase in the heart rate. Under the influence of Amlodipine, which has a weak natriuretic effect, the glomerular filtration rate increases, platelet aggregation is inhibited.
In patients with diabetic nephropathy, the severity of microalbuminuria does not increase. The drug does not affect the metabolic processes and the concentration of lipids in the blood plasma. It can be used in the treatment of patients with gout, diabetes mellitus and bronchial asthma.
With pathologies of the cardiovascular system (coronary atherosclerosis with lesions from 1 to 3 arteries, after myocardial infarction, percutaneous transluminal angioplasty, and with angina pectoris), amlodipine prevents thickening of carotid intima-media, reduces the frequency of surgical interventions aimed at restoring coronary blood flow , Progression of chronic heart failure and the development of unstable angina.
In patients with CHF III-IV st. Non-ischemic etiology the use of the drug may provoke pulmonary edema.
Amlodipine is slowly adsorbed from the digestive tract. The average absolute bioavailability is 64%, reaching a maximum serum concentration in 6-9 hours after administration. To achieve an equilibrium concentration, 7-8 days of use are required.
The drug is allowed to take regardless of the time of food intake. Most of it is absorbed into the tissue, the smaller remains in the blood. The average volume of distribution is 21 l / kg body weight. Slowly but actively decays in the liver. Metabolites lack significant pharmacological activity.
The half-life after a single dose is 35-50 hours, with a repeated administration - 45 hours. 10% of the drug is excreted by the kidneys unchanged, about 60% - in the form of metabolites, 20-25% - along with bile, through the intestine. The total clearance is 0.116 ml / s / kg. Half-life in advanced patients is 65 hours, but this difference is not critical. The drug is able to penetrate the blood-brain barrier, while hemodialysis is not removed.
Indications for use
- Arterial hypertension;
- Stable angina ;
- Vasospastic angina pectoris (Princmetal).
Dosing and Administration
At treatment of an initial degree of a stenocardia and an arterial hypertensia - 5 mg once a day. Gradually, within 7-10 the dose of the drug is increased to 10 mg / day.
The maintenance dose for arterial hypertension is 5 mg / day, once.
Vasospastic angina and angina pectoris are 5-10 mg / day, once.
With simultaneous use of ACE inhibitors, beta adrenoblockers and thiazide diuretics, a dose change is not required.
From the side of the central nervous system : dizziness, fatigue, headaches, drowsiness, general malaise, sleep disturbance, emotional lability, depressive state, increased anxiety, increased sweating. It is rare enough migraine, ataxia, amnesia, convulsions ;
Gastrointestinal tract : nausea, vomiting, abdominal pain, stool disorders, flatulence, anorexia, thirst, drying out of the mucous membrane of the mouth. Very rarely - increased appetite, gingival hyperplasia, cholestatic jaundice, hepatitis, pancreatitis .
Lymphatic and hematopoietic systems : thrombocytopenia, thrombocytopenic purpura, and leukopenia.
Cardiovascular system : palpitation, flushing of the face, development of peripheral edema, excessive lowering of blood pressure, vasculitis , orthostatic hypotension, aggravation of chronic heart failure, shortness of breath, heart rhythm disturbance, fainting, chest pain, pulmonary edema, myocardial infarction.
Excretory system : painful urination, urination, polyuria, dysuria, nocturia, pollakiuria.
Respiratory system : runny nose, dyspnea, cough.
Reproductive system : impotence, gynecomastia.
Musculoskeletal system - arthralgia, myalgia, muscle cramps, back pain, myasthenia gravis, arthrosis.
Skin : itching, rashes, hives , erythema multiforme, angioedema, alopecia.
Organs of the senses : visual disturbances, ringing in the ears, conjunctivitis , pain in the eyes, parosmia.
Other : hyperglycemia, a decrease or increase in body weight, nosebleeds, chills, taste perversions.
Interaction with other drugs
With the simultaneous use of inhibitors of microsomal oxidation, the concentration of amlodipine increases, and when microsomal enzymes are taken, the concentration decreases.
NSAIDs, alpha-adrenostimulators, sympathomimetics and estrogens weaken the hypotensive effect of the drug. Beta-adrenoblockers, diuretics, nitrates, antipsychotic drugs, slow calcium channel blockers and ATP inhibitors increase the vasodilator and hypotensive effect.
The pharmacokinetics of amlodipine are not affected by warfarin, digoxin, cimetidine.
With simultaneous use with lithium drugs, nausea, vomiting, stool, tinnitus, tremor, and ataxia are possible.
The drug effect of amlodipine may decrease potassium preparations.
Drugs that extend the QT interval can increase the negative ionotropic effect.
- Hypersensitivity to the components of the drug;
- Cardiogenic shock;
- Pronounced arterial hypotension;
- Unstable angina (with the exception of vasospastic);
- Pregnancy and lactation;
- Age to 18 years.
During treatment, the patient should adhere to a special diet, constantly monitor body weight and sodium intake. To prevent the development of complications from the oral cavity requires frequent visits to the dentist and a thorough maintenance of dental hygiene.
For elderly patients, with an increase in the dose of the drug, constant medical supervision is required.
When discontinuing treatment, the dose should be reduced gradually.
When driving vehicles and working with various mechanisms, special precautions must be taken.
Terms of implementation
Amlodipine tablets refer to prescription drugs, i.e. Are released on prescription.
Store in a dark place, protected from light and moisture, inaccessible to children, at a temperature not exceeding 25 ° C.
The drug is suitable for use for 3 years from the date of release. Use the product at the expiry date indicated on the package is prohibited.
Analogues of amlodipine
- Amlovas (tablets);
- Vero-amlodipine (tablets);
- Normodipine (tablets);
- Norvascus (tablets).
Prices for Amlodipine
Amlodipine tablets 10 mg, 30 pcs. - from 27r.