Amlodipine - instructions for use, analogs, reviews and release forms (5 mg and 10 mg tablets) for the treatment of blood pressure and its reduction in adults, children and pregnancy
In this article, you can read the instructions for using the drug Amlodipine. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Amlodipine in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of amlodipine in the presence of existing structural analogs. Use for the treatment of blood pressure and its reduction, stenocardia in adults, children, as well as during pregnancy and lactation.
Amlodipine - dihydropyridine derivative - slow calcium channel blocker (BCCI) of the 2nd generation, has antianginal and hypotensive action. Linking with dihydropyridine receptors, blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (mostly in smooth muscle cells of blood vessels, rather than in cardiomyocytes).
Antianginal effect is due to the expansion of coronary and peripheral arteries and arterioles: with angina decreases the severity of myocardial ischemia; expanding peripheral arterioles, reduces OPSS, reduces preload on the heart, reduces the need for myocardium in oxygen. Expands the main coronary arteries and arterioles in unchanged and ischemic zones of the myocardium, increases the flow of oxygen into the myocardium (especially with vasospastic angina); prevents the development of spasm of the coronary arteries (including those caused by smoking). In patients with stable angina, a single daily dose increases exercise tolerance, slows the development of angina pectoris and "ischemic" depression of the ST segment, reduces the incidence of angina attacks and the consumption of Nitroglycerin and other nitrates.
Has a long-term dose-dependent hypotensive effect.The hypotensive effect is due to a direct vasodilating effect on smooth muscle vessels. With arterial hypertension, a single dose provides a clinically significant decrease in blood pressure over a period of 24 hours (in the position of the patient lying down and standing). Orthostatic hypotension in the appointment of amlodipine is rare.
Does not cause a decrease in exercise tolerance, a fraction of the ejection of the left ventricle. Reduces the degree of myocardial hypertrophy of the left ventricle, has antiatherosclerotic and cardioprotective action in IHD. Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the rate of glomerular filtration, has a weak natriuretic effect.
When diabetic nephropathy does not increase the severity of microalbuminuria. Does not have any adverse effect on the metabolism and concentration of plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes and gout.
A significant reduction in blood pressure is observed after 6-10 h, the duration of the effect is 24 h.With prolonged therapy, the maximum decrease in blood pressure occurs 6-12 hours after taking amlodipine by mouth. If after prolonged treatment with amlodipine abolished, an effective reduction in blood pressure persists for 48 hours after the last dose. Then the blood pressure indicators gradually return to the baseline within 5-6 days.
Pharmacokinetics
After ingestion, amlodipine is slowly absorbed from the digestive tract. Food intake does not affect the absorption of amlodipine. Most of the drug in the blood (95%), binds to blood plasma proteins. Amlodipine undergoes a slow but active metabolism in the liver in the absence of a significant "first pass" effect. Metabolites do not have significant pharmacological activity. About 60% of the dose taken internally is excreted by the kidneys mainly in the form of metabolites, 10% - unchanged, and 20-25% - through the intestine, as well as breast milk.
The drug penetrates the blood-brain barrier. When hemodialysis is not removed.
In elderly patients (over 65 years), amlodipine excretion is slowed compared to young patients, but this difference is not clinically significant.
Indications
- Arterial hypertension (in monotherapy or in combination with other drugs);
- angina pectoris tension;
- vasospastic angina (Prinzmetal angina).
Forms of release
Tablets 5 mg and 10 mg. Can be produced in combination with other dosage forms (combination drugs).
Instructions for use and dosing regimen
Inside, the initial dose for the treatment of hypertension and angina is 5 mg once a day. The maximum daily dose is 10 mg once.
With arterial hypertension, the maintenance dose can be 2.5-5 mg (1/2 tablets of 5 mg - 1 tablet of 5 mg) per day
With angina pectoris and vasospastic angina pectoris, 5-10 mg per day, once. In order to prevent attacks of angina pectoris - 10 mg per day.
Patients with impaired hepatic function as an antihypertensive agent Amlodipine is administered with caution, at an initial dose of 2.5 mg (1/2 tablet at 5 mg), as an antianginal agent - 5 mg.
Do not require dose changes with simultaneous administration with thiazide diuretics, beta-blockers and ACE inhibitors.
Do not require dose changes in patients with renal insufficiency.
Side effect
- palpitation;
- peripheral edema (swelling of the ankles and feet);
- "tides" of blood to the skin of the face;
- excessive decrease in blood pressure;
- dyspnea;
- vasculitis;
- orthostatic hypotension;
- development or exacerbation of heart failure;
- heart rhythm disturbances (including bradycardia, ventricular tachycardia and atrial fibrillation);
- myocardial infarction;
- pain in the chest;
- headache;
- dizziness;
- increased fatigue;
- drowsiness;
- asthenia;
- paresthesia;
- insomnia;
- mood lability;
- unusual dreams;
- nervousness;
- depression;
- anxiety;
- migraine;
- increased sweating;
- nausea;
- stomach ache;
- vomiting;
- constipation or diarrhea;
- flatulence;
- dyspepsia;
- anorexia;
- dry mouth;
- thirst;
- increased appetite;
- gastritis;
- thrombocytopenic purpura, leukopenia, thrombocytopenia;
- frequent urination;
- painful urination;
- impotence;
- gynecomastia;
- dyspnea;
- rhinitis;
- cough;
- dermatitis;
- violation of skin pigmentation;
- itching;
- rash (including erythematous, maculopapular rash, urticaria);
- angioedema;
- muscle cramps;
- backache;
- tinnitus;
- Pain in the eyes;
- chills;
- nose bleed.
Contraindications
- severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
- collapse, cardiogenic shock;
- unstable angina (with the exception of Prinzmetal's stenocardia);
- clinically significant aortic stenosis;
- pregnancy and lactation;
- age under 18 years (effectiveness and safety not studied);
- deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;
- increased sensitivity to amlodipine, dihydropyridine derivatives and other components of the drug.
Application in pregnancy and lactation
There was no evidence of teratogenicity of amlodipine in the study on animals, but there is no clinical experience of its use in pregnancy and lactation. Therefore, amlodipine should not be given to pregnant women during lactation, as well as to women of childbearing age, unless they use reliable contraceptive methods.
special instructions
During the period of Amlodipine treatment, it is necessary to control the body weight and sodium intake, the purpose of the appropriate diet. It is necessary to maintain dental hygiene and supervision at the dentist (to prevent soreness, bleeding and gingival hyperplasia).
Patients with low body weight, low growth patients and patients with severe liver function impairment may need a smaller dose.
Despite the fact that stopping the use of amlodipine is not accompanied by the development of the "withdrawal" syndrome, it is desirable to stop the treatment, gradually reducing the dose of the drug.
The effectiveness and safety of the drug in hypertensive crisis is not established.
Impact on the ability to drive vehicles and manage mechanisms
There were no reports of Amlodipine's influence on driving or working with machinery. However, some patients, mainly at the beginning of treatment, may experience drowsiness and dizziness. When they occur, the patient must observe special precautions when driving and working with complex mechanisms.
Drug Interactions
Amlodipine can safely be used to treat hypertension along with thiazide diuretics, alpha-adrenoblockers, beta-blockers, or ACE inhibitors. In patients with stable angina, the drug can be combined with other antianginal agents, for example, with long-acting nitrates, beta-blockers or short-acting nitrates.
Amlodipine can be used simultaneously with non-steroidal anti-inflammatory drugs (especially indomethacin), antibacterial agents and hypoglycemic agents for oral administration.
It is possible to strengthen the anti-anginal and hypotensive action of BCCC when combined with thiazide and loop diuretics, verapamil, ACE inhibitors, beta-adrenoblockers and nitrates, as well as enhance their hypotensive effect when combined with alpha-blockers, antipsychotics.
Although no negative inotropic effects were usually observed in the study of amlodipine, nevertheless, some BCCCs can increase the negative inotropic effect of antiarrhythmic agents that cause prolongation of the QT interval (eg, Amiodarone and quinidine).
A single dose of 100 mg of Sildenafil (Viagra) in patients with essential hypertension does not affect the pharmacokinetics of amlodipine.
The repeated use of amlodipine in a dose of 10 mg and Atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.
Ethanol (alcohol-containing beverages): Amlodipine in single and repeated application at a dose of 10 mg does not affect the pharmacokinetics of ethanol (alcohol).
Antiviral agents (ritonavir) increase the plasma concentrations of BCCI, incl. amlodipine.
Neuroleptics and isoflurane - strengthening of hypotensive action of dihydropyridine derivatives.
Calcium preparations can reduce the effect of BCCC.
When amlodipine is used together with lithium preparations, it is possible to intensify manifestations of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Amlodipine does not change the pharmacokinetics of cyclosporine.
Does not affect the concentration of serum Digoxin and its renal clearance.
Has no significant effect on the effect of Warfarin (prothrombin time).
Cimetidine does not affect the pharmacokinetics of amlodipine.
Grapefruit juice: simultaneous single intake of 240 mg of grapefruit juice and 10 mg of amlodipine inwards is not accompanied by a significant change in the pharmacokinetics of amlodipine.
Analogues of the drug Amlodipine
Structural analogs for the active substance:
- Acridipine;
- Amlovas;
- Amlodak;
- Amlodigamma;
- Amlodipine Alkaloid;
- Amlodipine Zentiva;
- Amlodipine Cardio;
- Amlodipine Sandoz;
- Amlodipine-Ajio;
- Amlodipine-Biocom;
- Amlodipine-3T;
- Amlodipine-Prana;
- Amlodipine-Teva;
- Amlodipine-Chaikafarma;
- Amlodipine besylate;
- Amlodipina besilat;
- Amlodipine maleate;
- Amlodipharm;
- Amlocard-Sanovel;
- Amlong;
- Ammonorm;
- Amrorus;
- Amlotop;
- Vero-Amlodipine;
- Kalchek;
- Cardilopin;
- Corvadil;
- Cordy Cor;
- Norvasc;
- Normodipine;
- Omerar Cardio;
- Stamlo;
- Tenox.
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