EsKordi Work
Active material: Amlodipine
When ATH: C08CA01
CCF: Kalьcievыh channel blocker
ICD-10 codes (testimony): I10
When CSF: 01.03.02
Manufacturer: ACTAVIS GROUP hf. (Iceland)
DOSAGE FORM, STRUCTURE AND PACKAGING
Pills light yellow, flat, shaped with beveled edges, with an inscription “A” on one side and “2.5” – another.
| 1 tab. | |
| amlodipine (in the form of bezilata) | 2.5 mg |
Excipients: microcrystalline cellulose, lactose, colloidal silicon dioxide, magnesium stearate, Croscarmellose sodium, iron oxide yellow.
10 PC. – blisters (3) – packs cardboard.
Pills yellow color, flat, shaped with beveled edges, with an inscription “A” on one side and “5” – another.
| 1 tab. | |
| amlodipine (in the form of bezilata) | 5 mg |
Excipients: microcrystalline cellulose, lactose, colloidal silicon dioxide, magnesium stearate, Croscarmellose sodium, iron oxide yellow.
10 PC. – blisters (3) – packs cardboard.
Pharmacological action
Calcium channel blocker slow, dihydropyridine derivative. It has antianginal and hypotensive action. Communicating with digidropiridinovmi receptors S(-) amlodipine is a more potent compared to R(+) isomer, blocking calcium channels, reduces the transmembrane passage of calcium ions into the cell (mainly in vascular smooth muscle cells, than cardiomyocytes).
It has a long dose-dependent hypotensive effect. The antihypertensive effect is due to the direct vasodilating effect on vascular smooth muscle. When hypertension single dose provides a clinically significant reduction in blood pressure over 24 no (with the patient lying down and standing up). The time of onset of effect – 2-4 no, duration of effect – 24 no.
Pharmacokinetics
Absorption
Once inside the single dose 2.5 mg S(-) amlodipine is absorbed from the digestive tract. Eating does not affect the removals S(-) amlodipina. The average absolute bioavailability of 65%. Cmax serum (8.30± 803 ng/ml) is a 2.73 ± 0.88 h.
Distribution
Cssmax achieved after 7 days of therapy.
The binding to plasma proteins – 93%.
Average Vd is 21 l / kg: a large portion of the drug is in the tissues, the relatively smaller – in blood.
Metabolism
It has the effect of “first pass” through the liver. S(-) amlodipine is subjected to slow, but extensive metabolism (90%) in the liver into inactive metabolites.
Deduction
After a single oral T1/2 It varies between 14.62 to 68.88 no. When reappointing the T1/2 approximately 45 no. About 60% adopted inside dose appears mostly in the form of metabolites kidneys; unchanged – 10%, with breast milk and faeces – 20-25%. The total klirens S(-) amlodipine is 0.116 ml / sec / kg (7 ml / min / kg, 0.42 L / h / kg).
Pharmacokinetics in special clinical situations
Patients older 65 years of excretion S(-) Amlodipine inhibited by (T1/2 about 65 no) as compared to younger patients, However, this difference has no clinical significance.
Extension T1/2 in patients with hepatic insufficiency involves, that with long-term use of cumulation of drug in the body is higher (T1/2 – to 60 no).
Kidney failure does not significantly affect the farmakokinetiku S(-) amlodipina.
The drug crosses the blood-brain barrier. When hemodialysis is not removed.
Testimony
-arterial hypertension (I) (soft) severity (in combination with other antigipertenzivei means or as monotherapy).
Dosage regimen
The recommended initial dose JesKordi Bark – 2.5 mg 1 time / day. With insufficient therapeutic effect dose can be increased to 5 mg 1 time / day.
Side effect
The respiratory system: rarely – dyspnoea, nose bleed; rarely – cough.
Cardio-vascular system: heartbeat, breathlessness, marked reduction in blood pressure, fainting, vasculitis, swelling (swelling of the ankles and feet), flushing; rarely – rhythm (bradycardia, ventricular tachycardia, auricular fibrillation), chest pain, orthostatic hypotension; rarely – development or exacerbation of congestive heart failure, migraine.
From the central and peripheral nervous system: dizziness, headache, fatiguability, drowsiness, mood changes; rarely – convulsions, loss of consciousness, giperstezii, nervousness, paresthesia, tremor, vertigo, asthenia, malaise, insomnia, depression, unusual dreams; rarely – ataxia, apathy, ažitaciâ, amnesia.
From the digestive system: nausea, vomiting, epigastric pain; rarely – elevated liver enzymes, jaundice (caused by cholestasis), pancreatitis, dry mouth, flatulence, giperplaziya right, constipation, diarrhea; rarely – gastritis, increased appetite, dysgeusia.
With the genitourinary system: rarely – thamuria, tenesmus, nocturia, reduced potency; rarely – dizurija, polyuria.
On the part of the musculoskeletal system: rarely – arthralgia, arthrosis, myalgia (prolonged use); rarely – myasthenia.
From the senses: rarely – blurred vision, conjunctivitis, diplopia, sore eyes, tinnitus; rarely – rhinitis, parosmija, ccomodation, xerophthalmia.
Dermatological reactions: rarely – dermatoxerasia, alopecia, dermatitis, purpura, livor.
Allergic reactions: itching, rash (in t. no. эritematoznaya, maculo-papular rash, hives), angioedema.
Other: rarely – gynecomastia, poliurikemiâ, increase / decrease in body weight, thrombocytopenia, leukopenia, giperglikemiâ, increased perspiration, thirst, backache; rarely – cold clammy sweat.
Contraindications
- Prinzmetal angina;
- Severe hypotension;
- Collapse;
- Cardiogenic shock;
- Pregnancy;
- Lactation (breast-feeding);
- Childhood and adolescence up 18 years (efficacy and safety have not been established);
-hypersensitivity to S(-) Amlodipine and other derivative digidropiridina;
FROM caution apply when abnormal liver function, SSS (vыrazhennaya bradycardia, tachycardia), chronic heart failure neishemicheskoj etiology in the stage of decompensation, arterial hypotension of moderately, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and for 1 months after), diabetes, violation of the lipid profile, in elderly patients.
Pregnancy and lactation
Do not use this drug during pregnancy and lactation (breast-feeding).
Cautions
During drug treatment JesKordi Cor necessary to monitor body weight and sodium consumption, the appointment of an appropriate diet. It is necessary to maintain dental hygiene and frequent visits to the dentist (prevent soreness, bleeding and gingival overgrowth).
In elderly patients may lengthen T1/2 and clearance of the drug. The dosage regimen for the elderly is 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.
Effects on ability to drive vehicles and management mechanisms
Some patients, preferably at the beginning of treatment, may experience drowsiness or dizziness. When they do occur special precautions should be observed when driving and working with machinery.
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, kontroly for OCK and diurezom. To restore vascular tone – applying sossoudossoujiwath funds (in the absence of contraindications to their use). To deal with the consequences of the blockade of calcium channels – in / with the introduction of calcium gluconate. Hemodialysis is not effective.
Drug Interactions
Inhibitors mikrosomalnogo oxidation increase concentration in the blood plasma of amlodipine, increasing the risk of side effects, and inducers of microsomal liver enzymes – reduce.
Gipotenzivny effect weaken Alpha adrenostimuljatory, Estrogens (sodium retention), sympathomimetic.
And thiazide “loop” Diuretic, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and hypotensive effects.
Amiodarone, quinidine, alpha1-adrenoblokatorы, antipsychotics (neuroleptics) and calcium channel blockers slow may increase the hypotensive effect.
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 appearances their 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
The drug should be stored out of reach of children, dry place at temperatures no higher than 25 ° C. Shelf life – 2 year.
