Cardilopin pills 5 mg 30 pcs
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Amlodipine
Release form
Pills
Composition
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, anhydrous colloidal silica - 0.75 mg.
Pharmacological effect
Calcium channel blocker. Amlodipine inhibits transmembrane incoming calcium ion current in the smooth muscle cells of the heart and blood vessels by blocking slow calcium channels .; The antihypertensive effect of amlodipine is due to a direct relaxing effect on vascular smooth muscle cells, which leads to a decrease in the resistance of peripheral vessels .; The mechanism of antianginal action is not completely clear, however, most likely it is associated with the following two effects: 1. Expansion of peripheral arterioles reduces OPSS, i.e. afterload Since amlodipine does not cause reflex tachycardia, myocardial energy and oxygen consumption is reduced .; 2. The expansion of the large coronary arteries and coronary arterioles improves the oxygen supply of both normal and ischemic areas of the myocardium. Thanks to these effects, myocardial oxygen supply is improved, 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 throughout the 24-hour interval between doses of the drug. Due to the slow development of the effect of the drug does not cause acute arterial hypotension. In patients with angina, taking the drug 1 time / day increases the total time for performing possible physical activity before developing an attack of stenocardia and the time until a significant decrease in the ST interval, and also reduces the frequency of angina attacks and the need for sublingual nitroglycerin intake .; No negative effect of amlodinin on metabolism was found. The drug does not affect serum lipid, glucose and uric acid levels. Safe for patients with bronchial asthma.
Pharmacokinetics
After taking the drug inside, amlodipine is well absorbed from the gastrointestinal tract; at the same time, Cmax of amlodipine in plasma is noted after 6-12 hours.Simultaneous food intake does not alter the absorption of amlodipine. Absolute bioavailability is approximately 64-80%.; Distribution; Apparent Vd - 21 l / kg. Plasma protein binding is 93-98%. Css is reached 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 dose taken 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 derived mainly in the form of metabolites: 60% - with urine, 20-25% - with feces, about 10% is excreted unchanged with urine. T1 / 2 - 30-35 h (which allows you to prescribe the drug 1 time / day) .; Pharmacokinetics in special clinical situations; Pharmacokinetic parameters of amlodipine do not change in renal failure .; In elderly people, 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 prescribed in smaller doses.
Indications
- arterial hypertension (as monotherapy or, if necessary, as part of combination therapy with other antihypertensive drugs); - stable angina (as monotherapy or as part of combination therapy with other antianginal agents); - angiospastic stenocardia (Prinzmetal's stenocardia) (as monotherapy or as part of combination therapy with other antianginal agents).
Contraindications
- unstable angina; - clinically significant aortic stenosis; - severe hypotension; - children's and teenage age up to 18 years (due to the lack of clinical experience); - pregnancy; - lactation period (breastfeeding); - Hypersensitivity to amlodipine and other components of the drug .; The drug should be prescribed with caution in abnormal liver function, SSS (severe bradycardia, tachycardia), chronic heart failure in the decompensation stage, mild or moderate arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and myocardial infarction); months after), diabetes mellitus, elderly patients.
Use during pregnancy and lactation
Given the lack of clinical experience with the use of amlodipine during pregnancy and lactation, the drug should not be given to pregnant women and women of reproductive age who do not use effective methods of contraception, unless the therapeutic benefit of the drug justifies the possible risk .; If necessary, the use of the drug during lactation should stop breastfeeding.
Dosage and administration
For the treatment of hypertension or angina, the usual initial dose is 5 mg 1 time / day (preferably at the same time). Given the response of the patient, the initial dose may be increased to 10 mg 1 time / day. The dose of Cardilopin does not change in the case of its simultaneous use with diuretics from the thiazide group, beta-blockers or ACE inhibitors .; In case of renal failure and in elderly patients, dosing regimen adjustment is not required .; When prescribing Cardilopin in patients with impaired liver function, the recommended dose is 2.5 mg / day, since in these patients the drug T1 / 2 increases.
Side effects
On the part of the nervous system: headache, dizziness, excessive fatigue, drowsiness, mood changes, convulsions; rarely - loss of consciousness, hypesthesia, 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 - taste perversion, gastritis, increased appetite, pancreatitis .; On the part of the cardiovascular system: palpitations, swelling of the ankles and feet, shortness of breath, flushing of the face; rarely - rhythm disturbances (bradycardia, ventricular tachycardia, atrial flutter), chest pain, excessive decrease in blood pressure, orthostatic hypotension; very rarely - the development or aggravation of heart failure, extrasystoles, migraine .; On the part of the urogenital system: rarely - pollakiuria, painful urge to urinate, nocturia, a violation of sexual function (includingdecrease in potency); very rarely - dysuria, polyuria .; On the part of the respiratory system: rarely - dyspnea; very rarely - cough, rhinitis .; From the senses: rarely - blurred vision, conjunctivitis, diplopia, eye pain, accommodation disturbance, xerophthalmia, tinnitus .; On the part of the musculoskeletal system: rarely - arthralgia, arthrosis, myalgia (with prolonged use), back pain; very rarely - myasthenia .; On the part of the skin: very rarely - xerodermia, alopecia, dermatitis, purpura .; Allergic reactions: pruritus, rash (including erythematous, maculo-papular rash, urticaria) .; Other: rarely - gynecomastia, feeling of heat, chills, weight gain, nosebleeds, increased sweating, thirst; very rarely - cold sticky sweat, parosmia, hyperglycemia.
Overdose
Symptoms: marked reduction in blood pressure, tachycardia, excessive peripheral vasodilation .; Treatment: the patient should be given a horizontal position with raised legs. Conduct gastric lavage, the appointment of activated carbon, maintaining the function of the cardiovascular system, monitoring indicators of the function of the heart and lungs, monitoring of BCC and diuresis. Conduct intensive symptomatic therapy. To restore vascular tone, the use of vasoconstrictor drugs is shown (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade - in / in the introduction of calcium gluconate. Hemodialysis is not effective.
Interaction with other drugs
Perhaps the simultaneous use of amlodipine with thiazide diuretics, beta-blockers, long-acting nitrates, sublingual nitroglycerin preparations, NSAIDs, antibiotics and oral hypoglycemic agents .; Thiazide and “loop” diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates enhance the antianginal and hypotensive effects of amlodipine .; Amiodarone, quinidine, alpha1-blockers, antipsychotic drugs (antipsychotics), and slow calcium channel blockers may enhance the hypotensive effect of amlodipine .; Calcium preparations can reduce the effect of slow calcium channel blockers (including amlodipine) .; Inhibitors of microsomal oxidation, increasing the concentration of amlodipine in the blood plasma,increase the risk of side effects, and inducers of liver microsomal enzymes - reduce .; The antihypertensive 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 prolong the QT interval increase the negative inotropic effect of amlodipine and may increase the risk of 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 serum, but this does not lead to significant changes in blood pressure.
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 studies involving patients with heart failure III-IV functional class according to the NYHA classification showed that amlodipine does not increase the frequency of cardiovascular disorders or mortality when used together with ACE inhibitors, diuretics or digoxin .; During the period of treatment, it is necessary to maintain dental hygiene and a visit to the dentist (to prevent pain, bleeding and gingival hyperplasia) .; Dosing regimen for the elderly is the same as for patients of other age groups. Increasing the dose requires careful monitoring of elderly patients .; The vasodilator effect of amlodipine develops gradually. Therefore, acute hypotension after its use is very rare, however, before discontinuing treatment, a gradual decrease in dosage is recommended .; Amlodipine does not affect plasma concentrations of potassium, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and nitrogen of uric acid .; Impact on the ability to drive vehicles and control mechanisms; There were no reports of the effect of amlodipine on driving or working with mechanisms.However, in some patients, drowsiness and dizziness may occur predominantly at the beginning of treatment. When they occur, the patient must observe special precautions when driving and working with mechanisms.