Amlodipine Brand And Generic Names

Pharmaceutical group

Calcium channel blockers of dihydropyridine class. Selective calcium antagonists with preferential action on the blood vessels. Due to the slow development of effects and long duration of action, it is considered less dangerous and more comfortable to use than other products of this group.

Pharmacological action

Pharmacological action - antianginal, hypotensive, vasodilator, antispasmodic. The drug blocks calcium channels, inhibits the transmembrane passage of calcium ions into the cell. Hypotensive effect occurs due to the direct relaxing effect on vascular smooth muscle, decreasing total peripheral vascular resistance. As a result of attenuation of the load on the heart, myocardial oxygen consumption is reduced. On the other hand, the drug increases oxygen transmission to the myocardium in patients with vasospastic angina (prinzmetal's or variant angina) and prevents the development of coronary vasoconstriction caused by smoking. Advantages: well absorbed into the blood; the maximum concentration is reached slowly, which is not accompanied by the development of the phenomenon of the first dose; food intake does not affect the rate of absorption of the drug. Potentiates the effect and reduces the negative effects of beta-blockers. Amlodipine is the only drug from the group approved by fda for the treatment of patients with heart failure, less frequently causing swelling of the limbs in comparison with other drugs of this group. This agent inhibits platelet aggregation, increases sodium excretion and diuresis. Effect develops within 1-2 hours after administration and lasts for about 24 hours. With the gradual manifestation of action and prolonged effect, amlodipine causes gradual decline in blood pressure and minimal reflex stimulation of the sympathetic nervous system. The agent is absorbed slowly but almost completely. The maximum concentration is reached after 6-12 hours. At constant reception, the equilibrium concentration is reached in 7-8 days. Excreted in the urine, bile, breast milk.

Indications

Hypertension (as first-line monotherapy or combination therapy), coronary heart disease (stable angina, vasospastic angina: prinzmetal's or variant angina). As a drug for monotherapy or in combination with other antianginal drugs, amlodipine is effective in patients resistant to treatment with nitrates or beta- blockers.

Contraindications

Hypersensitivity, hypotension, shock, acute myocardial infarction. Restrictions: marked aortic stenosis, heart failure, liver dysfunction, children's age (safety and efficacy have not been determined).

Adverse effects

Cardio- vascular system and blood: facial flushing, palpitations, rarely - arrhythmias, chest pain, hypotension (including orthostatic).
Nervous system and sensory organs: fatigue, headache, dizziness, drowsiness, rarely - mood changes, visual disturbances.
Genitourinary system: peripheral edema (swelling of the ankles and feet), rarely - increased frequency of urination, impotence.
Digestive tract: nausea, abdominal pain, rarely - indigestion, changes in bowel movements, jaundice.
Respiratory system: rarely - shortness of breath.
Musculoskeletal system: rarely - arthralgia, myalgia, paresthesia and pain in the limbs (with prolonged use).
For the skin: rash, itching, rarely - erythema multiforme.
Other: rarely - gingival hyperplasia, gynecomastia, high level of liver enzymes.

After discontinuation of the drug side effects usually disappear completely.

Interaction

Amlodipine is compatible with major groups of antihypertensive agents (diuretics, ace inhibitors, beta-blockers), nitrates and hypoglycemic agents. Amlodipine can be used simultaneously with nitroglycerin, which is used sublingually, with nonsteroidal anti-inflammatory drugs, antibiotics and oral hypoglycemic drugs. The simultaneous use of amlodipine and digoxin in healthy volunteers did not alter the level of digoxin in serum and its renal clearance, while co-administration of cimetidine does not alter the pharmacokinetics of amlodipine. Amlodipine in vitro did not affect protein binding of digoxin, phenytoin, warfarin and indomethacin. In healthy male volunteers, the simultaneous use of amlodipine did not change the impact of warfarin on prothrombin time. According to pharmacokinetic studies, amlodipine not affects the pharmacokinetics of cyclosporine. Drugs for inhalation anesthesia (hydrocarbon derivatives), amiodarone, quinidine and other calcium antagonists may exacerbate the effects of this medicine.

Administration and dosage

The drug is taken orally with or without food, 1 tablet (10 mg) 1 time per day. In hypertension and angina, the usual starting dose is 5 mg once a day; the dose can be increased up to a maximum dose of 10 mg, depending on the individual patient response.

In patients with renal insufficiency amlodipine is prescribed in normal doses.

In elderly patients, as well as those with impaired liver function, amlodipine is prescribed at a dose of 2.5 mg 1 time a day (using drugs with the possibility of such a dosage).

Overdose

Significant overdose can cause excessive peripheral vasodilatation and subsequent prolonged decrease in blood pressure.

Symptoms: excessive peripheral vasodilatation, expressed and prolonged decline in blood pressure, tachycardia, bradycardia, confusion, stupor, nausea, vomiting, metabolic acidosis, hyperglycemia. In addition to eliminating the use of the drug, the re-introduction of calcium supplements is recommended (to increase myocardial contractility).

Treatment: gastric lavage, usage of activated charcoal, horizontal position with feet up for patients, monitoring the function of the heart and lungs, control blood volume and diuresis, symptomatic and supportive therapy, intravenous administration of calcium gluconate, dopamine, mezaton. Emergency measures should primarily be aimed at the restoration of stable hemodynamics. If calcium intake is not enough effective, appropriate use of sympathomimetic agents (dopamine or norepinephrine) to stabilize blood pressure is indicated. Be very careful with infusion solutions, because it increases the danger of overloading the heart and pulmonary edema. Amlodipine is tightly associated with plasma proteins, therefore hemodialysis use is impractical.

Special instructions

Pregnancy and breast-feeding is possible if the effect outweighs possible risks to the fetus. Patients should stop breastfeeding at the time of treatment.

Throughout the whole period of treatment it is necessary to control body weight and sodium intake. Patients should follow an appropriate diet and daily monitor blood pressure.

Use in patients with impaired liver function: half-life of amlodipine, like other calcium antagonists, is increased in patients with impaired liver function. For this reason, use the drug in such patients with caution and under close medical supervision.

Use in patients with renal insufficiency: for this category of patients amlodipine is used in usual doses. Change in the concentration of amlodipine in plasma did not correlate with the severity of renal failure.

Use in elderly patients: elderly patients are recommended dose reduction.

Drinking alcohol during treatment is strictly contraindicated.

Storage

Store in a dry and dark place, at a temperature below 25°c.