Amlodipine

Pharmacological properties

amlodipine - a blocker of slow calcium channels, inhibits the transmembrane transport of calcium ions into the smooth muscle cells of the walls of blood vessels and myocardium.

The mechanism of the antihypertensive effect of amlodipine is based on its direct relaxing effect on the smooth muscles of the walls of blood vessels.

In patients with hypertension, amlodipine at a dosage of 1 time per day clinically significantly reduces blood pressure. Due to the slow effect of amlodipine, taking the drug does not lead to acute hypotension and tachycardia.

In patients with angina pectoris, amlodipine increases exercise tolerance, delays the occurrence of anginal pain and ST segment depression on the ECG; however, both the frequency of anginal attacks and the frequency of nitroglycerin are reduced.

Pharmacokinetics During oral administration of a therapeutic dose, amlodipine is well absorbed; C_max in blood plasma are reached approximately 6-12 hours after taking the drug. Absolute bioavailability reaches 64–80%. The distribution volume is approximately 21 l / kg body weight. The time of use and the nature of the food do not affect the absorption of amlodipine.

In vitro studies have shown that about 97.5% of circulating amlodipine is associated with plasma proteins.

T_½ is 35–50 hours, stable plasma concentrations are achieved after 7–8 days of continuous use of the drug. To a large extent, amlodipine is biotransformed in the liver and turns into inactive metabolites.

Amlodipine is excreted in the urine: 10% of the dose is unchanged, 60% in the form of inactive metabolites.

Amlodipine is not dialyzed.

Indications

AH, stable angina pectoris and angina pectoris.

Application

Apply inside. the tablet is swallowed whole, washed down with a sufficient amount of water.

The initial dose is 5 mg 1 time per day. Over time, the dose can be increased to 10 mg, taking into account the individual response of the patient.

The duration of treatment depends on the clinical effect and tolerability of the drug.

Elderly patients may take the drug in the general recommended dosage.

Contraindications

Hypersensitivity to amlodipine or any component of the drug; arterial hypotension; During pregnancy and breastfeeding; children under 18 years old.

Side effects

During treatment, the following side effects may occur: headache, swelling of the legs, increased fatigue, drowsiness, nausea, pain in the abdomen, flushing, tachycardia, dizziness.

Relatively rare side effects include: alopecia, impaired peristalsis, joint pain, shortness of breath, asthenia, back pain, muscle cramps, dyspepsia, gingival hyperplasia, gynecomastia, hyperglycemia, impotence, increased urination, leukopenia, pancreatitis, hyperhidrosis, vasculitis, mood changes, peripheral neuropathy, lethargy, dry mouth, muscle pain, and visual impairment.

Infrequently, an allergic reaction can occur, accompanied by itching, skin rash, angioedema, and erythema multiforme.

special instructions

Similarly to other calcium channel blockers, t½ of amlodipine is increased in patients with reduced liver function. in these cases, the drug must be used with extreme caution (up to 2.5 mg / day).

Particular care must be taken in patients with arterial hypotension, hypertrophic obstructive cardiomyopathy, unstable angina pectoris.

The ability to influence the reaction rate when driving vehicles and working with other mechanisms. The drug can cause headache, fatigue, drowsiness, so its use can affect the activity required by a high speed of mental and physical reactions, making quick decisions (for example, driving vehicles, servicing machinery, working at height, etc.).

Interactions

Amlodipine can be used simultaneously with thiazide diuretic drugs, α- and β-adrenoreceptor blockers, apf inhibitors, long-acting nitrates, nitroglycerin, NSAIDs, antibiotics, oral antidiabetic agents.

During specialized studies, it was found that the simultaneous use of amlodipine with digoxin by healthy volunteers does not cause changes in serum digoxin levels, as well as its renal clearance, the combined use of amlodipine with cimetidine does not change the pharmacokinetics of amlodipine.

The simultaneous use of amlodipine with warfarin by healthy male volunteers did not have a significant effect on prothrombin time.

During pharmacokinetic studies with cyclosporine, it was proved that amlodipine does not cause significant changes in the pharmacokinetics of this immunosuppressive agent.

Grapefruit juice can increase plasma levels of amlodipine, but this does not have a significant effect on blood pressure and heart rate.

Overdose

May lead to prolonged systemic hypotension.

Treatment: gastric lavage, monitoring of the respiratory system and heart function is recommended.

To restore vascular tone and blood pressure, vasoconstrictors (vasoconstrictors) are used, but only if they are not contraindicated. To inhibit the effect of calcium channel blockers, it is useful to administer calcium gluconate iv.

Storage conditions

In the original packaging. does not require special storage conditions.