Composition, form of production and packaging
Tablets are white, almost white or yellowish white, round, flat, chamfered, engraved in the form of the letter "E" on one side and number "251" - on the other.
1 tab.
Amlodipine besylate 3.475 mg,
which corresponds to the content of amlodipine 2.5 mg
Excipients: microcrystalline cellulose - 63.4 mg, sodium carboxymethyl starch (type A) - 2 mg, magnesium stearate - 0.75 mg, silicon dioxide colloidal anhydrous - 0.375 mg.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
Tablets are white, almost white or yellowish white, round, flat, with a facet, with an engraved "E" on one side and number "252" on the other.
1 tab.
amlodipine besylate 6.95 mg,
which corresponds to the content of amlodipine 5 mg
Excipients: microcrystalline cellulose - 126.8 mg, sodium carboxymethyl starch (type A) - 4 mg, magnesium stearate - 1.5 mg, silicon dioxide colloidal anhydrous - 0.75 mg.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
Tablets are white, almost white or yellowish white, round, flat, with a facet, with an engraved "E" on one side and number "253" on the other.
1 tab.
amlodipine besylate 13.9 mg,
which corresponds to the content of amlodipine 10 mg
Excipients: microcrystalline cellulose - 253.6 mg, sodium carboxymethyl starch (type A) - 8 mg, magnesium stearate - 3 mg, silicon dioxide colloidal anhydrous - 1.5 mg.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2010.
PHARMACHOLOGIC EFFECT
The calcium channel blocker. Amlodipine suppresses the transmembrane incoming current of calcium ions into the smooth muscle cells of the heart and vessels by blocking the slow calcium channels.
The antihypertensive effect of amlodipine is due to a direct relaxing effect on the smooth muscle cells of the vessels, which leads to a decrease in the resistance of peripheral vessels.
The mechanism of antianginal action is not completely understandable, however, it is most likely associated with the following two effects:
1. Expansion of peripheral arterioles reduces OPSS, i.e. afterloading. Since amlodipine does not cause reflex tachycardia, the consumption of energy and oxygen by the myocardium decreases.
2. Expansion of large coronary arteries and coronary arterioles improves the supply of oxygen to both normal and ischemic zones of the myocardium. Due to these effects, the supply of oxygen to the myocardium improves, even with spasm of the coronary arteries (Prinzmetal angina or unstable angina).
In patients with arterial hypertension, taking the drug 1 time / day causes a clinically significant decrease in blood pressure in the supine position and standing during the entire 24-hour interval between doses of the drug. Due to the slow development of the effect, the drug does not cause acute arterial hypotension. In patients with angina, taking the drug 1 time / day increases the total time of exercise possible physical exertion before the onset of an attack of angina and the time to a significant decrease in the ST interval, and also reduces the frequency of angina attacks and the need for sublingual administration of nitroglycerin.
There was no negative effect of amlodinin on the metabolism. The drug does not affect the serum lipids, glucose and uric acid levels. It is safe for patients with bronchial asthma.
PHARMACOKINETICS
Suction
After taking the drug inside, amlodipine is well absorbed from the digestive tract; while C max amlodipine in the blood plasma is observed after 6-12 hours. Simultaneous food intake does not change the absorption of amlodipine. Absolute bioavailability is approximately 64-80%.
Distribution
Apparent V d is 21 l / kg. The binding with plasma proteins is 93-98%. C ss is achieved on the 7-8 day of taking the drug and is 5-15 ng / ml.
Metabolism and excretion
Amlodipine undergoes intensive metabolism in the liver. Approximately 90% of the accepted dose is converted to inactive pyridine derivatives. The total clearance is 7 ml / min / kg (25 l / h for a patient with a body weight of 60 kg). It is excreted mainly in the form of metabolites: 60% - with urine, 20-25% - with feces, about 10% excreted unchanged in urine. T 1/2 - 30-35 h (which allows prescribing the drug 1 time / day).
Pharmacokinetics in special clinical cases
The pharmacokinetic parameters of amlodipine do not change with renal failure.
In the elderly, the total clearance is approximately 19 l / h, the remaining parameters do not change.
With a decrease in clearance in patients with hepatic insufficiency, the drug should be administered in smaller doses.
INDICATIONS
- arterial hypertension (in the form of monotherapy or if necessary as part of combination therapy with other antihypertensive drugs);
- stable angina pectoris (in the form of monotherapy or as part of combination therapy with other antianginal drugs);
- angiospastic angina (Prinzmetal angina) (in the form of monotherapy or as part of combination therapy with other antianginal agents).
DOSING MODE
For the treatment of hypertension or angina, the usual initial dose is 5 mg 1 time / day (preferably at the same time). Taking into account the patient's reaction, the initial dose can be increased to 10 mg 1 time / day. The dose of Cardilopin is not changed in case of its simultaneous use with diuretics from the group of thiazides, beta-adrenoblockers or ACE inhibitors.
With renal failure and in elderly patients, correction of the dosing regimen is not required.
In the appointment of Cardilopin to patients with a violation of liver function, the recommended dose is 2.5 mg / day, t. in these patients, T 1/2 of the drug is increased.
SIDE EFFECT
From the side of the nervous system: headache, dizziness, excessive fatigue, drowsiness, mood changes, convulsions; rarely - loss of consciousness, hypoesthesia, paresthesia, tremor, asthenia, malaise, insomnia, nervousness, depression, unusual dreams, anxiety; very rarely - ataxia, apathy, agitation, amnesia.
On the part of the digestive system: nausea, abdominal pain; rarely - hyperbilirubinemia, jaundice, increased activity of hepatic transaminases, dry mouth, anorexia, vomiting, constipation or diarrhea, dyspepsia, flatulence, gingival hyperplasia; very rarely - perversion of taste, gastritis, increased appetite, pancreatitis.
From the cardiovascular system: palpitation, swelling of the ankles and feet, shortness of breath, flushing of blood to the face; rarely - rhythm disturbances (bradycardia, ventricular tachycardia, atrial flutter), pain in the chest, excessive reduction in blood pressure, orthostatic hypotension; very rarely - the development or aggravation of heart failure, extrasystole, migraine.
From the genitourinary system: rarely - pollakiuria, painful urge to urinate, nocturia, violation of sexual function (including decreased potency); very rarely - dysuria, polyuria.
From the respiratory system: rarely - dyspnoea; very rarely - cough, rhinitis.
From the senses: rarely - visual impairment, conjunctivitis, diplopia, eye pain, accommodation disorder, xerophthalmia, ringing in the ears.
From the musculoskeletal system: rarely - arthralgia, arthrosis, myalgia (with prolonged use), back pain; very rarely - myasthenia gravis.
From the skin: very rarely - xeroderma, alopecia, dermatitis, purpura.
Allergic reactions: skin itching, rash (including erythematous, maculopapular rash, urticaria).
Other: rarely - gynecomastia, sensation of fever, chills, weight gain, nosebleeds, increased sweating, thirst; very rarely - cold sticky sweat, parosmia, hyperglycemia.
CONTRAINDICATIONS
- unstable angina;
- clinically significant aortic stenosis;
- severe arterial hypotension;
- children and adolescence under 18 (due to lack of clinical experience);
- Pregnancy;
- the period of lactation (breastfeeding);
- Hypersensitivity to amlodipine and other components of the drug.
With caution , the drug should be prescribed for violations of liver function, SSSU (severe bradycardia, tachycardia), chronic heart failure in the stage of decompensation, mild or moderate degree of arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and within 1 month after), diabetes, elderly patients.
PREGNANCY AND LACTATION
Given the lack of clinical experience with amlodipine during pregnancy and lactation, the drug should not be given to pregnant women, nor to women of reproductive age who do not use effective methods of contraception, unless the therapeutic benefit of the drug justifies the possible risk.
If it is necessary to use the drug during lactation, breastfeeding should be stopped.
APPLICATION FOR FUNCTIONS OF THE LIVER
If the renal function is not corrected, the dosage regimen is not required.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
In the appointment of Cardilopin to patients with a violation of liver function, the recommended dose is 2.5 mg / day, t. in these patients, T 1/2 of the drug is increased.
APPLICATION FOR CHILDREN
Contraindication: children and adolescents under 18 years of age (due to lack of clinical experience);
APPLICATION IN ELDERLY PATIENTS
Dosage regimen for the elderly is the same as for patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary.
SPECIAL INSTRUCTIONS
Studies in patients with heart failure II and III functional class according to the NYHA classification when taking amlodipine did not reveal a decrease in exercise tolerance, left ventricular ejection function or worsening of clinical symptoms. The results of clinical trials involving patients with heart failure III-IV functional class according to the NYHA classification showed that amlodipine does not increase the incidence of cardiovascular disorders or mortality when combined with ACE inhibitors, diuretics or digoxin.
During the treatment, it is necessary to maintain dental hygiene and visit the dentist (to prevent soreness, bleeding and gingival hyperplasia).
Dosage regimen for the elderly is the same as for patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary.
The vasodilator effect of amlodipine develops gradually. Therefore, acute arterial hypotension after its use is very rare, however, before the cessation of treatment, a gradual decrease in doses is recommended.
Amlodipine does not affect plasma concentrations of potassium, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and uric acid nitrogen.
Impact on the ability to drive vehicles and manage mechanisms
There were no reports of the effects of amlodipine on driving or working with machinery. However, some patients may experience drowsiness and dizziness at the beginning of treatment. When they occur, the patient must observe special precautions when driving and working with machinery.
OVERDOSE
Symptoms: marked decrease in blood pressure, tachycardia, excessive peripheral vasodilation.
Treatment: the patient should be given a horizontal position with raised legs. Gastric lavage, the appointment of activated charcoal, maintenance of cardiovascular function, control of heart and lung function, control of bcc and diuresis are carried out. Conduct intensive symptomatic therapy. To restore the vascular tone, the use of vasoconstrictive drugs is indicated (in the absence of contraindications to their use); to eliminate the effects of blockade of calcium channels - intravenous calcium gluconate. Hemodialysis is not effective.
DRUG INTERACTION
Possible simultaneous use of amlodipine with thiazide diuretics, beta-adrenoblockers, long-acting nitrates, sublingual preparations of nitroglycerin, NSAIDs, antibiotics and oral hypoglycemic agents.
Thiazide and looped diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates increase the antianginal and hypotensive effects of amlodipine.
Amiodarone, quinidine, alpha 1- adrenoblockers, antipsychotic drugs (antipsychotics) and slow calcium channel blockers can enhance the hypotensive effect of amlodipine.
Calcium preparations can reduce the effect of blockers of slow calcium channels (including amlodipine).
Inhibitors of microsomal oxidation, increasing the concentration of amlodipine in the blood plasma, increase the risk of side effects, and inductors of microsomal enzymes of the liver - reduce.
The hypotensive effect of amlodipine weakens NSAIDs, especially indomethacin (due to sodium retention and blockade of prostaglandin synthesis by the kidneys), alpha-adrenomimetics, estrogens (due to sodium retention), sympathomimetics.
Procainamide, quinidine and other drugs that cause prolongation of the QT interval increase the negative inotropic effect of amlodipine and may increase the risk of a significant prolongation of the QT interval.
Cimetidine does not affect the pharmacokinetics of amlodipine.
Amlodipine does not affect the pharmacokinetic parameters of digoxin and warfarin.
Grapefruit juice can slightly increase the level of amlodipine in the blood serum, but this does not lead to significant changes in blood pressure.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a place protected from light, inaccessible to children at a temperature of 15 В° to 25 В° C. Shelf life - 5 years.
