Amlodipine tablets - a pharmaceutical product designed to treat certain forms of hypertension and angina pectoris, which has an ultra-long action. Lowers blood pressure, enhances the supply of oxygen to heart tissues with long-term preservation of the therapeutic effect.
Material Content:
The composition of the drug
The medicine is released in tablets of 5 and 10 mg. A pack can be 30, 60 or 90 units, which is determined by the manufacturer.
This is the basic treatment substance for the drug amlodipine (in the form of besylate). The composition also includes the inactive components of the drug necessary for preservation and morphogenesis.
What pills help
Amlodipine belongs to the second generation of “slow” calcium channel blockers (abbreviated as BMKK). The active component of the drug is a derivative of dihydropyridine. The drug inhibits the penetration of calcium ions through the membrane of tissue cells, which determines its pharmacological effect.
Main properties (pharmacodynamics)
The decrease in blood pressure occurs due to the fact that the drug relaxes the muscle fibers of the walls of blood vessels, increasing their lumen. In this case, the medicine does not cause heart palpitations.
As a result of the therapeutic effects of Amlodipine:
- The flow of blood to the heart muscle increases, its need for oxygen and energy decreases, the load on the myocardium decreases.
- Cardiac arteries and arterioles expand in healthy areas and in areas with insufficient blood supply, which provides oxygen to the heart during vascular spasm against angina pectoris.
- Due to the fact that the drug inhibits the clumping (aggregation) of platelet blood cells into clots, the formation of blood clots is prevented.
- Renal function improves when they become deficient and have diabetic nephropathy, which occurs due to an increase in the speed of renal blood flow.
- There is a reverse development of hypertrophied (thickened) tissues of the left ventricle - the main "pumping" chamber of the heart.
A major advantage of Amlodipine, in comparison with other calcium antagonists, is the longest duration of the therapeutic result - its antihypertensive effect lasts up to 36 hours.
Unlike drugs with a short duration of action, Amlodipine does not show sharp drops in blood concentration, which minimizes the risk of stroke or heart attack.
A number of pharmacological characteristics of the substance distinguishes it from other hypotensive and cardiovascular pharmaceuticals, since the drug:
- does not increase the tone of the bronchi;
- does not affect the heart rate and conduction processes in the heart muscle;
- does not lower physical and intellectual activity;
- does not cause sexual dysfunctions (such as beta-blockers and diuretics), depressive disorders (such as Reserpine, Clonidine);
- does not affect metabolic processes, the balance of electrolytes, including potassium levels (unlike diuretics).
Indications
The medication is safe, well tolerated and effective both as a single drug and as one of the drugs in the combined treatment of severe pathologies.
Amlodipine tablets help patients with the following diseases:
- hypertonic disease;
- essential ("causeless") hypertension;
- symptomatic hypertension, which is considered as a "symptom" of internal diseases (endocrine and renal pathologies, adrenal tumors, diabetic nephropathy, nephritis, long-term use of glucocorticosteroids);
- stable angina without spasm and spontaneous
- angina pectoris with spasm of blood vessels (Prinzmetal);
- angina pectoris of rest and tension;
- a combination of angina pectoris with a state of low heart rate (bradycardia), AV blockade.
Taking medication:
- increases the endurance of the heart to a lack of oxygen, stress, reduces the frequency of attacks;
- slows down the depression of the ST segment (DBT) on the cardiogram - the most indicative manifestation of cardiac ischemia with an unstable form of angina pectoris;
- reduces the need for nitrates (including nitroglycerin);
- reduces the number of hospitalizations of patients, the frequency of operations on coronary artery bypass grafting, reduces the likelihood of complications and mortality rates.
Calcium channel blocker can be used safely with diagnosed asthma, diabetes and diabetic nephropathy, gout.
Distribution and excretion (pharmacokinetics)
The drug is absorbed into the blood gradually, and its highest content is fixed in the range from 6 to 12 hours after the tablets enter the stomach. After 7-8 days of treatment, with a uniform intake, a stationary concentration of the drug (Css) is recorded.
Amlodipine is slowly processed by liver enzymes with the formation of intermediate substances that do not have significant therapeutic activity.
The time for elimination of half the dose received by the patient is from 31 to 45 hours.
Together with urine, approximately 60% of the active substance that enters the bloodstream, mainly in the form of intermediate compounds, is removed from the body, about 22-25% comes out with feces, 10% - with bile.
In patients with impaired liver and kidney function, as well as people over 65 years of age, the removal of the therapeutic substance slows down (half-life is approximately 60–65 hours), but this factor does not have a significant effect on the therapeutic effect.
Instructions for taking and dosage of Amlodipine
A marked decrease in blood pressure is observed 6-10 hours after internal administration and lasts about a day.
Since amlodipine tablets act slowly against pressure, they are not used for high blood pressure numbers, especially for hypertensive crisis.
Due to the slowly developing therapeutic effect and a gradual decrease in blood pressure, the therapy eliminates the threat of vasospasm and impaired cardiac or cerebral circulation (which happens with a sharp decrease in pressure).
The stable therapeutic effect of Amlodipine is manifested 5-7 days after the start of therapy. It is advisable to discontinue therapy mildly, slowly reducing the dosage.
5 mg tablets
The medication is taken without regard to eating food, once a day, washing down with the amount of water necessary for the patient (but not less than 100 ml).
To alleviate hypertension and prevent heart attacks, the prescribed standard dose is 5 mg. If the drug does not show a noticeable therapeutic effect within 15-30 days, the daily dose of the medicine can be increased to 2 tablets - 10 mg.
In diseases of the kidneys and liver in old age, most often a dose reduction is not required, but given the characteristics of each patient, it is recommended to start treatment with 2.5 mg (half a tablet). In this case, more careful monitoring of the patient's condition is necessary.
Amlodipine 10 mg
The drug in tablets with a high content of amlodipine is taken according to the same scheme and in similar doses. If they are prescribed once in a dose of 5 mg, the patient can take half a tablet of 10 mg.
During pregnancy and lactation
There is no reliable information on the effect of amlodipine on embryo development and gestation, therefore, medication is prohibited for pregnant patients.
It was established that the medicine passes into breast milk and its effect on the baby’s body is unpredictable, therefore it is advisable for nursing mothers to transfer the baby to artificial mixtures.
Drug interaction
Amlodipine can be combined with the following pharmacological products:
- ACE inhibitors, nitrates, diuretics, α- and β-blockers, but it must be borne in mind that its hypotensive effect may be enhanced;
- antibiotic medications and drugs that lower blood sugar;
- non-hormonal anti-inflammatory drugs, including indomethacin;
- Warfarin, Digoxin;
- aluminum-magnesium antacids (Fosfalugel, Maaloks, Almagel) with periodic intake.
Alcohol is undesirable to take during treatment with amlodipine, and although a single or double use of “hot” does not affect the rate of removal of ethanol from the body, a strong drop in pressure and fainting are possible.
Other interactions with Amlodipine
| Pharmacological Products | Probable reactions when combined |
|---|---|
| Erythromycin, ketoconazole, antiretroviral drugs (Norvir, Ritonavir), antipsychotics (Zeldox, Teraligen), inhibitors of the isoenzyme CYP3A4 (diltiazem), itraconazole (Rumikoz, Irunin) | increased concentration of amlodipine and increased action |
| Means with lithium, anesthetics, Isoflurane (Foran) | negative effects on the nervous system (diarrhea, weakness, vomiting, trembling, auditory disorders) |
| pharmaceutical products with calcium | reduction of therapeutic effect |
| Immunosuppressants Cyclosporine (Sandimmun Nizoral, Ecoral), Tacrolimus (Advagraf) | increased action of these drugs |
Grapefruit juice usually does not affect the therapeutic effect of Amlodipine, but in rare cases there is a strong decrease in blood pressure, which should be considered by a lover of such a drink.
Contraindications, side effects and overdose
It is forbidden to prescribe a medication in such conditions as:
- intolerance to any component of the medication, including other derivatives of dihydropyridine;
- severe hypotension (an indicator of systolic blood pressure of 90 mm RT. Art. and below);
- severe chronic myocardial failure not associated with ischemia (risk of pulmonary edema);
- cardiac infarction (use is possible only after stabilization of hemodynamic parameters);
- shock conditions;
- blood flow obstruction in the ventricular outflow tract (as well as severe aortic stenosis);
- patients under 18 years old, pregnant and lactating women.
Undesirable side effects usually occur when there is a violation of contraindications to the use of the drug, exceeding the dose or frequency of administration.
| Development frequency | Probable unwanted effects |
|---|---|
| 1 - 9 out of 100 patients | Palpitations, swelling of the feet, hot flashes, pain in the head and stomach, dizziness, nausea, lethargy |
| 2 - 9 people out of 1000 | • a strong decrease in pressure; • joint, vertebral and muscle pain, tic; • numbness of the skin, trembling fingers; • mood swings, nervousness; • sleep disorder, taste change; • constipation or loose stools, gas formation; • dry mouth, runny nose, shortness of breath; • double vision, conjunctivitis, nosebleeds, frequent urination; • weakening erection, weight changes; • itchy skin, rashes, chills |
| 2 - 9 out of 10 thousand patients | • fainting, vasculitis, pain behind the sternum; dermatitis, bleeding, swollen gums; • pressure drop during quick rise, darkening in the eyes; • worsening heart failure, arrhythmia |
| in 1 out of 10 thousand patients and even less often | • cough, migraine, sweating, memory disorders; • gastritis, inflammation of the liver, pancreas, jaundice (caused by stagnation of bile); • increase in blood bilirubin, sugar, liver enzymes; • decrease in the number of leukocytes and platelets; • thrombocytopenic purpura, • hair loss, ichthyosis, focal discoloration of the skin; • Quincke's edema, erythema |
Although there is no negative effect of Amlodipine on the ability to drive equipment and vehicles, it is advisable to take into account the possibility of dizziness and lethargy due to a sharp drop in blood pressure, especially when increasing the dose or at the beginning of therapy.
In case of overdose observed:
- abnormal decrease in pressure;
- increased myocardial contractions to high numbers;
- respiratory failure, loss of consciousness;
- development of a coma, life-threatening condition.
With such signs, immediately call an ambulance, lay the patient with his legs high. In the first hour after the appearance of signs of an overdose, they give (if possible) adsorbents (Polysorb). Intensive detoxification therapy is carried out in the hospital (gastric lavage, infusion of calcium gluconate, the use of vasoconstrictors and solutions to maintain heart function).
Hemodialysis is ineffective because amlodipine is 96% bound to blood proteins.
Amlodipine analogues
The analogues of Amlodipine containing the same active substance include medicines of various pharmaceutical companies: Tenox, Norvask, Normodipin, Amlotop, Amlovas, Kulchek, Cardilopin, Amlorus.
