AMLORUS
Active material: Amlodipine
When ATH: C08CA01
CCF: Kalьcievыh channel blocker
ICD-10 codes (testimony): I10, i20, I20.1
When CSF: 01.03.02
Manufacturer: Synthesis of (Russia)
DOSAGE FORM, COMPOSITION AND PACKAGING
Pills white, round, ploskotsilindricheskoy form chamfered.
| 1 tab. | |
| amlodipine (in the form of bezilata) | 2.5 mg |
| – ” – | 5 mg |
| – ” – | 10 mg |
Excipients: lactose, potato starch, povidone, krospovydon, microcrystalline cellulose, calcium stearate, talc.
10 PC. – packings Valium planimetric (3) – packs cardboard.
Pharmacological action
Calcium channel blocker slow II generation, dihydropyridine derivative. Provides antianginalnoe and antihypertensive activity. Svyazыvayas with dyhydropyrydynovыmy receptors, blocking calcium channels, reduces the transmembrane passage of calcium ions into the cell (mainly in vascular smooth muscle cells, than cardiomyocytes).
Antianginal effect is due to expansion of the coronary and peripheral arteries and arterioles: When strokes reduces the severity of cerebral infarction; expanding peripheral arterioles, reduces round, reduces cardiac afterload, reducing myocardial oxygen demand. Expanding the major coronary arteries and arterioles in the unaltered and ischemic areas of the myocardium, increases the supply of oxygen to the myocardium (especially in vasospastic angina); prevents the development of coronary artery konstrikcii (incl. caused by smoking). In patients with angina and single daily dose increases the run-time physical activity, slows the development of angina pectoris and ischemic ST-segment depression, reduces the frequency of angina attacks and consumption of nitroglycerin.
It has a long dose-dependent hypotensive effect. Antihypertensive activity due to the direct influence of vazodilatiruûŝim on smooth muscle receptacles.
When hypertension single dose provides a clinically significant reduction in blood pressure over 24 no (with the patient lying down and standing up). It does not cause a sharp decline in blood pressure, reducing exercise tolerance, left ventricular ejection fraction.
Reduces the degree of left ventricular hypertrophy, It has anti-atherosclerotic and cardioprotective effect in ischemic heart disease. No effect on the myocardial contractility and conductivity, It does not cause a reflex increase in heart rate, agregatia stops platelets, increases glomerular filtration rate, It has a weak natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria. It has no adverse effects on metabolism and plasma lipids.
The time of onset of effect – 2-4 no, duration of effect 24 no.
Pharmacokinetics
Absorption
After oral administration of amlodipine is slowly absorbed from the gastrointestinal tract. The average absolute bioavailability of 64-90%. Cmax in the blood plasma through 6-9 no. Css achieved after 7 days of therapy. Food does not affect absorption of amlodipine.
Distribution
Average Vd is 21 l / kg, which indicates, that most of the drug is in the tissues, and relatively less – in blood. The binding to plasma proteins – 95%.
The drug crosses the blood-brain barrier. Provided with breast milk.
Metabolism
Amlodipine podvergaetsya medlennomu, but extensive metabolism (90%) in the liver into inactive metabolites, exposed effect “first pass” through the liver. Metabolites do not have clinically significant pharmacological activity.
Deduction
After a single oral administration of T1/2 It varies between 31 to 48 no, when reappointment T1/2 approximately 45 no. About 60% adopted inside the dose appears in the urine mainly as metabolites, 10% – in unchanged form, 20-25% – with feces. The total clearance of amlodipine 0.116 ml / sec / kg (7 ml / min / kg, 0.42 L / h / kg).
Pharmacokinetics in special clinical situations
Elderly patients (senior 65 years) elimination of amlodipine slowed (T1/2 – 65 no) compared to younger patients, However, this difference has no clinical significance. Patients with hepatic insufficiency is expected elongation T1/2, and assigning prolonged drug accumulation in the body is higher (T1/2 – to 60 no).
Kidney failure does not significantly affect the farmakokinetiku amlodipine.
When hemodialysis is not removed.
Testimony
- Arterial hypertension (as monotherapy or in combination with other antihypertensives: Diuretics, beta-blockers, ACE inhibitors);
- Stable angina, vasospastic angina (Prinzmetal angina) (as monotherapy or in combination with other antianginalnami means).
Dosage regimen
The drug is prescribed inside.
When treating hypertension and angina initial is 5 mg 1 time / day. If necessary dose can be increased up to a maximum of 10 mg 1 time / day. At hypertension maintenance dose may be 5 mg / day.
At vasospastic angina (Prinzmetal angina) – 5-10 mg/day 1 reception.
You do not need to change the doses together with tiazidnami dioretikami, beta-blockers and ACE inhibitors.
You do not need to change the doses in patients with renal insufficiency.
In Patients with liver failure, elderly patients initial dose when hypertension can be 2.5 mg.
Side effect
Cardio-vascular system: heartbeat, breathlessness, marked reduction in blood pressure, fainting, vasculitis, swelling (swelling of the ankles and feet), flushing; rarely – arrhythmias (bradycardia, ventricular tachycardia, auricular flutter), chest pain, orthostatic hypotension; in some cases – development or exacerbation of congestive heart failure, arrythmia, migraine.
From the central and peripheral nervous system: headache, dizziness, fatiguability, drowsiness, mood changes, convulsions; rarely – loss of consciousness, gipesteziya, nervousness, paresthesia, tremor, vertigo, asthenia, malaise, insomnia, depression, unusual dreams; in some cases – ataxia, apathy, ažitaciâ, amnesia.
From the digestive system: nausea, vomiting, epigastric pain, rarely – increase in liver enzymes and jaundice (caused by cholestasis), pancreatitis, dry mouth, flatulence, giperplaziya right, constipation or diarrhea; in some cases – gastritis, increased appetite.
From the urinary system: rarely – thamuria, tenesmus, nocturia; in some cases – dizurija, polyuria.
On the part of the reproductive system: rarely – sexual dysfunction (incl. reduced potency), gynecomastia.
Dermatological reactions: in some cases – dermatoxerasia, alopecia, dermatitis, purpura, livor.
Allergic reactions: itching, rash (in t. no. эritematoznaya, maculopapular rash, hives), angioedema.
On the part of the musculoskeletal system: rarely – arthralgia, arthrosis, myalgia (prolonged use); in some cases – myasthenia.
Metabolism: rarely – poliurikemiâ, increase / decrease in body weight, giperglikemiâ, increased perspiration, thirst; in some cases – cold clammy sweat.
From the hematopoietic system: rarely – thrombocytopenia, leukopenia.
From the senses: rarely – blurred vision, diplopia, conjunctivitis, sore eyes, tinnitus, parosmija, dysgeusia, ccomodation, xerophthalmia.
The respiratory system: rarely – dyspnoea, nose bleed, cough, rhinitis.
Other: rarely – backache.
Contraindications
- Severe hypotension;
- Collapse;
- Cardiogenic shock;
- Unstable angina (except Prinzmetal angina);
- Pregnancy;
- Lactation;
- Up to 18 years (efficacy and safety have not been established);
- Hypersensitivity to amlodipine and other dihydropyridine derivatives.
FROM caution use in patients with abnormal liver function, SSS (vыrazhennaya bradycardia, tachycardia), chronic heart failure, decompensated, If mild or moderate arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, in acute myocardial infarction (and for 1 months after it), diabetes, violation of the lipid profile, in elderly patients.
Pregnancy and lactation
The drug is contraindicated in pregnancy and lactation (breast-feeding).
Cautions
During treatment necessary to monitor body weight, sodium intake, You must assign an appropriate diet.
It is necessary to maintain dental hygiene and frequent visits to the dentist (to prevent pain, krovotochivosti and giperplazii right).
The dosage for elderly patients the same, as well as for patients in other age groups.
By increasing the dose should be closely monitored for elderly patients.
Despite the lack of calcium channel blockers slow withdrawal, before the termination of treatment is recommended a gradual reduction in dose.
Amlodipine has no effect on plasma concentrations of potassium, Glucose, TG, total cholesterol, LDL, Uric acid, creatinine and urea nitrogen.
Effects on ability to drive vehicles and management mechanisms
On the influence of amlodipine on the ability to drive or to work with mechanisms of messages are missing. Nonetheless, some patients, preferably at the beginning of treatment, may experience drowsiness or dizziness. When they occur, the patient should observe special precautions for potentially hazardous activities.
Overdose
Symptoms: marked reduction in blood pressure, tachycardia, chrezmernaya perifericheskaya vasodilation.
Treatment: gastric lavage, appointment of activated carbon, To maintain the function of the cardiovascular system, control performance of the heart and lungs, elevated position limbs, control of BCC, diuresis. To restore vascular tone – use of vasopressors (in the absence of contraindications to their use); to deal with the consequences of the blockade calcium channels-in/with the introduction of Calcium Gluconate. Hemodialysis nyeeffyektivyen.
Drug Interactions
Inhibitors of microsomal oxidation increase the concentration of amlodipine in plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes – reduce.
Reducing gipotenzivnogo effect of amlodipine cause NSAIDS, especially indomethacin (sodium retention and blockage of prostaglandin synthesis by the kidneys), alpha adrenostimulyatorov, Estrogens (sodium retention), sympathomimetic.
And thiazide “loop” Diuretic, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and hypotensive effects.
Amiodarone, quinidine, alpha1-adrenoblokatorы, antipsychotic drugs (neuroleptics) and slow calcium channels blockers may increase gipotenzivny effect of amlodipine.
No effect on the pharmacokinetic parameters of digoxin and warfarin.
Cimetidine have no influence on amlodipine farmakokinetiku.
When coupled with the use of lithium may increase manifestations neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, noise in ears).
Calcium can reduce the effect of calcium channel blockers slow.
Prokaynamyd, quinidine and other drugs, causing prolongation of the QT interval, reinforce the negative inotropic effect and may increase risk of significant lengthening of the QT interval.
Grapefruit juice may reduce the concentration of amlodipine in plasma, however, this decrease is so small, that does not significantly alter the effect of amlodipine.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be kept out of the reach of children, dry, dark place at a temperature no higher than 25 ° C. Shelf life – 2 year.
