Instructions for the use of "Amlodipine"
In the membranes of smooth muscle cells of arteries, cardiomyocytes, sinus and atrioventricular nodes, there are voltage-dependent slow Ca2+ L- and T-type channels. "Amlodipine" slows down the transport of calcium ions into the cytoplasm, preventing the interaction of the contractile proteins actin and myosin.
The drug belongs to the subgroup of antagonists of the dihydropyridine series, which have a vasodilating effect without altering myocardial contractility and the automatism of the sinus node. Therefore, "Amlodipine" is considered a vasoselective representative of the class.
The main effects of the medication:
- Antihypertensive. The drug acts mainly on the smooth muscles of peripheral arterioles of medium and small caliber. The blockade of calcium entry into the cytoplasm causes relaxation of the cell, the lumen expands, the total vascular resistance and afterload on the heart muscle decreases.
- Antianginal. Expansion of the coronary vessels and prevention of re-spasm ensures adequate blood supply to the working myocardium. In addition, oxygen consumption is reduced when correcting the afterload on the left heart, muscle relaxation is optimized in diastole (the phase of blood filling of the coronary vessels).
Reception of "Amlodipine" by patients with coronary artery disease (IHD) prolongs the period of physical activity until the appearance of chest pain and changes in the ECG. The drug reduces the number of seizures and the need to take Nitroglycerin tablets.
- Improvement of microcirculation in the kidneys (regulation of renin production), as a result of which one of the links of arterial hypertension is blocked. The renal vascular resistance decreases, the glomerular filtration and plasma flow increase.
- Increase cerebral circulation, prevent ischemic damage (stroke).
- Decrease in blood viscosity, inhibition of platelet aggregation, increase in the fibrinolytic ability of plasma. The improvement in rheological properties has a positive effect on systemic hemodynamics, especially in patients with a long history of coronary heart disease.
- Antiatherogenic action. "Amlodipine" prevents the introduction of low density lipoproteins into the cell membranes of the endothelium, preventing damage to the vascular wall.
- Stimulation of the release of nitric oxide from the vascular endothelium.
For prolonged antihypertensive drugs, the main criterion of effectiveness is the possibility of "overlapping" the 24-hour interval, prolongation of the action until the next dose of the drug. The half-life of "Amlodipine" exceeds 35 hours.
The drug has the most consistently high bioavailability in comparison with the rest of the class (65-70%). Due to the slow increase in the peak concentration in the tissues and the long elimination, a stable blood pressure curve is provided throughout the day.
Indications: what does it help and at what pressure is it prescribed?
The drug "Amlodipine" is optimal for long-term treatment regimens for chronic conditions. The main groups of indications are presented in the table.
| Disease | Peculiarities |
|---|---|
| Hypertension (HD) |
|
| Ischemic heart disease |
|
| Concomitant pathologies against the background of ischemic heart disease or hypertension |
|
"Amlodipine" is suitable for the treatment of hypertension in pregnant women, dark-skinned patients and children over 6 years of age.
Calcium antagonists have a relaxing effect on the muscles of the uterus, which must be taken into account when prescribing a drug in the last weeks of pregnancy.
Method of administration and dosage: how to take?
Reception of "Amlodipine" does not depend on the time of day and diet. The recommended starting dose of saturation is 5 mg once a day. Correction is carried out depending on the patient's sensitivity to therapy and blood pressure indicators. The regimen of admission is assessed and corrected after 14 days from the beginning of the course.
The concentration of "Amlodipine" (active metabolic products) in tissues is stabilized after 7 days of systematic use. Due to the smooth increase in the hypotensive effect, there is no risk of reflex pulse acceleration, addiction with long-term treatment.
"Amlodipine" is used for basic monotherapy and in combination with anti-ischemic drugs of other classes for patients with coronary artery disease.
Simultaneous treatment with several antihypertensive drugs does not require revision of the dosage of "Amlodipine".
The medicine is used for hypertension in children over 6 years old. Recommended regimen: starting dose - 2.5 mg / day, with insufficient hypotensive effect - correction after 28 days (up to 5 mg / day).
Patients with renal or hepatic insufficiency, elderly people - an increase in the dose of the drug is allowed with constant monitoring of hemodynamics.
A sharp restriction or discontinuation of the drug does not cause withdrawal symptoms.
Special instructions and symptoms of overdose
Amlodipine is a widely used drug, therefore it is necessary to use safe combinations with:
- diuretics ("hydrochlorothiazide")
- blockers of adrenergic receptors ("Metoprolol", "Bisoprolol" and others);
- ACE inhibitors (Ramipril, Lisinopril);
- long-acting nitrates ("Sustak", "Nitrosorbit").
Simultaneous reception of "Amlodipine" and high doses of "Simvastatin" contribute to the disruption of the metabolism of the latter. The maximum amount of lipid-lowering drugs should be limited to 20 mg.
The joint use of alcohol with "Amlodipine" does not affect the metabolic rate of ethanol. International clinical protocols for the treatment of cardiovascular pathologies recommend limiting the amount of alcohol in patients with hypertension or coronary artery disease.
In the first weeks of therapy, the drug affects the ability to drive vehicles and work with complex mechanisms. A decrease in the severity of the reaction is accompanied by migraine, dizziness and bouts of nausea. At the initial stage of treatment, it is recommended to limit these types of activities.
In case of poisoning with "Amlodipine" there is a drop in tone and expansion of peripheral vessels, which is accompanied by tachycardia, dizziness, collapse (severe arterial hypotension).
Treatment of an overdose of "Amlodipine":
- gastric lavage;
- the introduction of drugs that constrict blood vessels;
- infusion of glucose solution with calcium;
- constant monitoring of the parameters of cardiac activity, central venous pressure, urine output;
- drug correction of emerging disorders.
"Amlodipine" has strong connections with plasma globulins, so dialysis is ineffective.
Contraindications
The use of "Amlodipine" is not recommended for such conditions:
- intolerance to dihydropyridine or other components;
- severe arterial hypotension;
- shock conditions;
- obstruction of the outflow tract of the left ventricle (critical stenosis of the aortic valve);
- unstable hemodynamic state for 14 days, in patients with myocardial infarction;
- progressive angina pectoris;
- systolic dysfunction of the left heart (ejection fraction less than 40%);
- strings of pregnancy up to 12 weeks.
Side effects
Undesirable effects during the treatment with "Amlodipine" are rare, the main symptoms of which are indicated in the table.
| Frequent reactions |
|
| Rare unwanted effects |
|
Analogues of "Amlodipine": how to replace the drug?
The manufacturer of the original drug with the name "Norvask" (pharmaceutical company Pfizer, USA) produces the drug in a dosage of 5 and 10 mg.
Generics are medicines with an identical amount of active ingredient, but at a lower cost. The high price of the original drug, high demand due to the frequent prescription of this group of drugs are the main reasons for the appearance on the Russian market of analogues of domestic and imported production:
- Amlodipine Russia;
- Agen, Tengisal Czech Republic;
- Azomex, Amlovas, Amlogen, Vasodipin India;
- Amlo-Sandoz Poland / Slovenia;
- Amlodipine-Pfizer Germany;
- Amlokard-Sanovel, Norvadin Turkey;
- Amlokor Bulgaria;
- Amlodipine-Zentiva Israel;
- Normodipin, Emlodine Hungary;
- Tenox Slovenia.
Substitutes for a drug are drugs with a similar pharmacodynamic effect and a list of indications due to the influence of another active ingredient. The main substitutes for "Amlodipine" are representatives of calcium channel blockers of other classes:
- "Nifedipin" ("Corinfar", "Kordipin", "Osmo-Adalat");
- Lekardipin (Lerkamen);
- Felohexal Germany;
- Nitresal Czech Republic;
- "Nimodipine".
The pharmaceutical market offers combined preparations of "Amlodipine" with other antihypertensive drugs. It is strictly forbidden to take a substitute without consulting a doctor. Different active substances differ in the spectrum and severity of the effects, compatibility with the medications taken.
Conclusions
A single use of "Amlodipine" by patients with arterial hypertension provides a stable decrease in pressure for 24 hours. Due to the smooth increase in the pharmacological effect, there are no symptoms of acute hypotension.
Pleiotropic (multidirectional) action of "Amlodipine" controls the course of diseases that often accompany hypertension - diabetes mellitus, metabolic syndrome, atherosclerosis, obstructive pulmonary disease and gout.
Before using "Amlodipine" it is necessary to consult a doctor and carefully study the instructions.
