2010/09/21

Aronar

Composition, structure and packing

Tablets are white or white with kremovatym color ploskotsilindricheskie, with beveled and risks.

1 tab. amlodipine (in the form bezilata) 5 mg.

Excipients: microcrystalline cellulose, potato starch, lactose monohydrate, calcium hydrogen phosphate dihydrate, croscarmellose sodium, magnesium stearate, aerosil (colloidal silicon dioxide).

Clinico-pharmacological group: Calcium channel blockers.

Pharmacological action

Blocker "slow" calcium channels from the group dihydropyridine derivatives. Antihypertensive and antianginal effects. Blocks the flow of calcium ions across cell membranes in smooth muscle cells of blood vessels and myocardium.

Mechanism of antihypertensive action is due to the direct relaxing effect on smooth muscles of blood vessels. Antianginal effect of the drug due to its ability to expand the peripheral arterioles, which leads to a decrease in TPVR, a reduction in afterload leads to a decrease in myocardial oxygen demand. In addition, amlodipine increases coronary arteries and arterioles, which leads to an increase in the supply of oxygen to the myocardium (the mechanism is particularly important when angiospastic angina). Amlodipine has no adverse effect on metabolism and lipid content of blood plasma, has antiateroskleroticheskoy, antithrombotic activity, increases the glomerular filtration rate, has a weak natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria.

Pharmacokinetics

Absorption

If ingestion is absorbed from the gastrointestinal tract, slowly and almost completely (90%). Cmax plasma levels achieved within 6-12 hours Bioavailability - 60-65%.

Distribution

Css achieved after 7-8 days of continuous use. Relationship to plasma proteins - more than 95%. Vd - about 20 l / kg. It penetrates through the blood-brain barrier, is excreted in breast milk. Metabolism Biotransformiruetsya mainly in the liver with the formation of inactive metabolites.

Withdrawal

T1 / 2 - 35-45 hours, which allows you to assign it 1 time / day. Less than 10% accepted oral dose excreted unchanged in about 60% excreted in the urine as inactive metabolites, 20-25% of output in the form of metabolites with bile and feces.

Pharmacokinetics in special clinical situations

T1 / 2 in arterial hypertension can increase up to 48 hours in elderly patients - up to 65 h, with liver problems - up to 60 hours in case of breach of kidney function - does not change.

Statement
hypertension (as monotherapy and as part of combination therapy);
Stable angina;
angiospastic angina (Prinzmetal angina).

Dosage regimen

When hypertension Aronar administered in an initial dose of 2.5 mg / d for the prevention of angina attacks - 5 mg / day. The recommended maintenance dose in arterial hypertension and angina - 5 mg / day. If necessary, the daily dose may be increased to 10 mg. Do not exceed the recommended initial daily dose in patients with impaired liver function, elderly patients and patients with reduced body weight. The maximum daily dose - 10 mg.

With simultaneous use of thiazide diuretics, beta-blockers or ACE inhibitors correct dosing regimen Aronara not required. Patients with impaired renal function correct dosing regimen is also not required.

Side effect
Since the cardiovascular system: heart rate, shortness of breath, excessive lowering of blood pressure, syncope, vasculitis, edema ankles and feet, facial flush, rarely, cardiac arrhythmias - (bradycardia, ventricular tachycardia, atrial flutter), chest pain, orthostatic hypotension, in rare cases - the development or worsening symptoms of heart failure, arrythmia, migraines.
From the central nervous system and peripheral nervous system: dizziness, headache, drowsiness, fatigue, rarely - asthenia, mood changes, seizures, visual disturbances, paresthesia, tinnitus.
On the part of the musculoskeletal system: rarely - arthralgia, arthrosis, myalgia (with prolonged use), in isolated cases - myasthenia gravis.
On the part of the digestive system: dyspepsia, nausea, abdominal pain, rarely - increased activity of hepatic transaminases, jaundice (caused by cholestasis), gingival hyperplasia, pancreatitis, taste perversion, dry mouth, changes in bowel movements.
Dermatological reactions: skin rash, itching, rarely - erythema multiforme, skin discoloration, dermatitis.
From the urinary system: rarely - thamuria, tenesmus, nocturia, in rare cases - dysuria, polyuria.
On the part of the hemopoietic system: rarely - thrombocytopenia, leukopenia.
Other: rarely - gynecomastia, violation of sexual function (including reduction of potency), the increase / decrease in body weight, hyperglycemia, conjunctivitis, eye pain, nosebleeds, increased sweating, thirst.

Contraindications
hypotension;
tachycardia
collapse;
cardiogenic shock;
aortic stenosis;
mitral stenosis;
childhood and adolescence to 18 years;
Hypersensitivity to amlodipine and other derivatives of dihydropyridine.

Precautions should be prescribed drug in violation of liver and kidney function, chronic heart failure, III and IV functional class (classification NYHA), SSS, and mild to moderate hypotension, hypertrophic obstructive cardiomyopathy during the acute phase of myocardial infarction, diabetes, disorders lipid metabolism, in elderly patients.

Pregnancy and lactation

Application Aronara during pregnancy and lactation is possible only when the intended benefits to the mother outweighs the potential risk to the fetus or baby (due to lack of reliable clinical data supporting the safety of the drug in these periods).

If necessary, the appointment Aronara during lactation should decide the issue of termination of breastfeeding.

Application for violations of liver function

Precautions should be prescribed the drug in violation of liver function.

Application for violations of renal function

Precautions should be prescribed the drug in violation of renal function.

Cautions

During the administration of the drug requires monitoring of body weight, diet (especially limiting sodium intake), the maintenance of oral hygiene and regular dental visits (to prevent soreness, bleeding and gingival hyperplasia). Care should be exercised in appointing Aronara elderly patients, especially with increasing dose. Despite the absence of a drug withdrawal syndrome upon termination of treatment Aronarom recommend a gradual reduction in dose. Appointment Aronara not affect the plasma concentrations of potassium, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and urea nitrogen.

Possible joint use Aronara with thiazide diuretics, alpha-and beta-blockers, ACE inhibitors, nitrates (including prolonged), NSAIDs, antibiotics, oral hypoglycemic drugs.

Use in Pediatrics

Safety and effectiveness in pediatric practice Aronara not installed. Effects on ability to drive vehicles and management mechanisms have been no reports on the impact Aronara on ability to drive a car or operate machinery.

Nevertheless, some patients, mainly at the beginning of treatment, there may be drowsiness and dizziness. When they occur, the patient must observe special precautionary measures while driving and using machinery.

Overdose

Symptoms: marked reduction of blood pressure, tachycardia, excessive peripheral vasodilatation.

Treatment: gastric lavage, activated charcoal appointment, the patient should be given to a horizontal position with legs raised, hold the control performance of the heart and lungs, BCC, diuresis, carry out activities aimed at maintaining the function of the cardiovascular system. To restore the tone of the vessels used vasoconstrictive drugs (in the absence of contraindications to their use) to eliminate the effects of calcium channel blockade in / injected calcium gluconate. Hemodialysis is ineffective.

Drug Interactions

With simultaneous use of thiazide and loop "diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and antihypertensive effects Aronara.

At simultaneous application with Aronarom inhibitors of microsomal liver enzymes increase the concentration of amlodipine in plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes - reduce its concentration. The simultaneous use of Aronara and digoxin did not change the concentration in serum and renal clearance of digoxin.

Joint application Aronara and cimetidine does not alter the pharmacokinetics of amlodipine.

The simultaneous use Aronara not significantly modify the effect of warfarin on prothrombin time in healthy male volunteers. Antihypertensive effect Aronara weaken NSAIDs, especially indomethacin (there is a delay of sodium and blocking the synthesis of prostaglandins by the kidneys), as well as sympathomimetic and estrogens (cause sodium retention). When the joint application of funds for inhalation anesthesia (derivatives of hydrocarbons), amiodarone, quinidine may increase the hypotensive effect Aronara.

When combined with the use of lithium therapy may be a manifestation of neurotoxicity.

Terms and Conditions of storage

List of BN drug should be stored in a dry place protected from light, out of reach of children. Shelf life - 2 years.