AMLODIPINE PILLS 5 mg

Indications

- arterial hypertension (monotherapy or in combination with other antihypertensive drugs);

- stable exertional angina and vasospastic stenocardia (Prinzmetal stenocardia) (monotherapy or in combination with other antihypertensive drugs).

Dosage and administration

Inside, starting dose for treatment hypertension and angina pectoris is 5 mg of the drug 1 time / day. The maximum daily dose - 10 mg once.

At hypertension maintenance dose may be 2.5-5 mg (1/2 pills of 5 mg - 1 tab. 5 mg) / day.

At angina pectoris and vasospastic angina pectoris - 5-10 mg / day, once. In order to prevent attacks of stenocardia - 10 mg / day.

To patients with liver dysfunction As an antihypertensive, Amlodipine is prescribed with caution, in an initial dose of 2.5 mg (1/2 tab. 5 mg), as an antianginal medication - 5 mg.

In patients old age may increase t1/2 Amlodipine and decline QC. Changes in dose is not required, but more careful monitoring of patients is needed.

No dose changes are required when administered concomitantly with thiazide diuretics, beta-blockers and ACE inhibitors.

No dose changes are required in patients with renal failure.

Side effect

Classification of the incidence of side effects of the World Health Organization (WHO): very often> 1/10, often from> 1/100 to <1/10, sometimes from> 1/1000 to <1/100, rarely from> 1/10000 to <1/1000, very rarely from <1/10000, including individual messages.

Since the cardiovascular system: often - palpitations, peripheral edema (swelling of the ankles and feet), "tides" of blood to the skin of the face; sometimes - an excessive decrease in blood pressure; very rarely - syncope, shortness of breath, vasculitis, orthostatic hypotension, development or aggravation of heart failure, heart rhythm disturbances (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain.

From the central and peripheral nervous system: often - headache, dizziness, fatigue, drowsiness; sometimes - asthenia, general malaise, hypesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability, unusual dreams, nervousness, depression, anxiety; very rarely - migraine, increased sweating, apathy.

From the digestive system: often - nausea, abdominal pain; sometimes - vomiting, constipation or diarrhea, flatulence, dyspepsia, anorexia, dry mouth, thirst; rarely - gingival hyperplasia, increased appetite; very rarely - pancreatitis, gastritis, jaundice (due to cholestasis), hyperbilirubinemia, increased activity of hepatic transaminases, hepatitis.

From the side of blood-forming organs: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.

From the genitourinary system: sometimes - frequent urination, painful urination, nocturia, impotence, very rarely - dysuria, polyuria, gynecomastia.

On the part of the respiratory system: sometimes - shortness of breath, rhinitis, very rarely - cough.

From the skin: rarely - dermatitis, very rarely - alopecia, xeroderma, “cold” sweat, impaired skin pigmentation.

Allergic reactions: pruritus, rash (including erythematous, maculopapular rash, urticaria), angioedema, erythema multiforme.

From the musculoskeletal system: sometimes - muscle cramps, myalgia, arthralgia, back pain, arthrosis, rarely - myasthenia.

Other: sometimes - tinnitus, diplopia, disturbance of accommodation, xerophthalmia, conjunctivitis, eye pain, chills, nosebleeds, very rarely - parosmia, hyperglycemia.

Contraindications

- severe arterial hypotension (systolic blood pressure less than 90 mm Hg);

- collapse, cardiogenic shock;

- unstable angina (with the exception of Prinzmetal stenocardia);

- clinically significant aortic stenosis;

- pregnancy and lactation;

- age up to 18 years (efficacy and safety have not been studied);

- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

- Hypersensitivity to amlodipine, dihydropyridine derivatives and other components of the drug.

with caution in violations of liver function, sick sinus syndrome (SSS) (severe bradycardia, tachycardia), chronic heart failure of non-ischemic etiology of III-IV functional class according to NYHA classification, arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute isometry, isastrophritic ischemia, isometric infusion and within 1 month after myocardial infarction), in old age.

Use during pregnancy and lactation

The teratogenicity of amlodipine was not detected in an animal study, but there is no clinical experience with its use during pregnancy and lactation. Therefore, amlodipine should not be prescribed for pregnant women and during lactation, as well as for women of childbearing age, if they do not use reliable methods of contraception.

Application for violations of the liver

with caution with abnormal liver function

Application for violations of kidney function

No dose changes are required in patients with renal failure.

Use in elderly patients

with caution in old age.

special instructions

During the period of treatment with Amlodipine, it is necessary to control body weight and sodium intake, the appointment of an appropriate diet. It is necessary to maintain dental hygiene and observation at the dentist (to prevent pain, bleeding and gum hyperplasia).

Patients with low body mass, patients of short stature and patients with severe liver dysfunction may require a lower dose.

Elderly patients may lengthen T1/2 and clearance of the drug.Dose changes for elderly patients are not required; increasing the dose requires more careful monitoring of patients.

Abnormal liver function can also lengthen T1/2 drug. Therefore, these patients should be prescribed Amlodipine with caution.

Despite the fact that the discontinuation of Amlodipine is not accompanied by the development of "withdrawal" syndrome, it is advisable to stop the treatment, gradually reducing the dose of the drug.

The efficacy and safety of the drug in hypertensive crisis has not been established.

Influence on ability to drive motor transport and control mechanisms

There were no reports of the effect of Amlodipine on driving or working with machinery. However, in some patients, mainly at the beginning of treatment, drowsiness and dizziness may occur. When they occur, the patient must observe special precautions when driving and working with complex mechanisms.

Overdose

Symptoms: excessive peripheral vasodilation with a pronounced and possibly prolonged decrease in blood pressure, collapse, shock.

Treatment: gastric lavage, the appointment of Activated carbon, maintaining the function of the cardiovascular system, monitoring indicators of the function of the heart and lungs, elevated, above the level of the head, the position of the lower extremities, control of BCC and diuresis. To restore vascular tone - the use of vasoconstrictor agents (in the absence of contraindications to their use); in order to eliminate the effects of Calcium channel blockade - in / in the introduction of Calcium gluconate . Hemodialysis is ineffective.

Drug interaction

Amlodipine can be safely used to treat arterial hypertension along with thiazide diuretics, alpha-blockers, beta-blockers or ACE inhibitors. In patients with stable angina, the drug can be combined with other antianginal drugs, for example, with prolonged-acting nitrates, beta-blockers or short-acting nitrates.

Amlodipine can be used simultaneously with NSAIDs (especially indomethacin), antibacterial agents and hypoglycemic agents for oral administration.

It is possible to enhance the antianginal and hypotensive action of BMCA when used together with thiazide and "loop" diuretics, Verapamil, ACE inhibitors, beta-blockers and nitrates, as well as enhancing their hypotensive effect when used together with alpha-blockers, neuroleptics.

Although in the study of amlodipine, a negative inotropic effect was usually not observed, however, some BMCCs may increase the severity of the negative inotropic effect of antiarrhythmic drugs that cause prolongation of the QT interval (for example, Amiodarone and quinidine).

A single dose of 100 mg of Sildenafil in patients with essential hypertension does not affect the parameters of amlodipine pharmacokinetics.

Repeated use of amlodipine at 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, when taken once and again at a dose of 10 mg, does not affect the pharmacokinetics of ethanol.

Antiviral agents (ritonavir) increases plasma concentrations of BCCA, incl. amlodipine.

Neuroleptics and isoflurane - enhancing the hypotensive effect of dihydropyridine derivatives.

Calcium preparations can reduce the effect of BCCA.

The combined use of amlodipine with lithium preparations may increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).

Amlodipine does not alter the pharmacokinetics of cyclosporine.

Does not affect the concentration of serum Digoxin and its renal clearance.

It has no significant effect on the effect of Warfarin (prothrombin time).

Cimetidine does not affect the pharmacokinetics of amlodipine.

In in vitro studies, amlodipine does not affect the binding of blood proteins to digoxin, phenytoin, warfarin, and Indomethacin .

Grapefruit juice: a single dose of 240 mg of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine