TENOKS
Active material: Amlodipine
When ATH: C08CA01
CCF: Kalьcievыh channel blocker. Antianginal and antihypertensive drug.
ICD-10 codes (testimony): I10, i20, I20.1
When CSF: 01.03.02
Manufacturer: KRKA d.d. (Slovenia)
Pharmaceutical form, composition and packaging
Pills white, round, lenticular, with a beveled edge and a notch on one side.
| 1 tab. | |
| amlodipine (in the form of maleate) | 5 mg |
| -“- | 10 mg |
Excipients: microcrystalline cellulose, pregelatinized starch, sodium starch glycolate, Colloidal anhydrous silica, magnesium stearate.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (9) – packs cardboard.
Pharmacological action
Kalьcievыh channel blocker, dihydropyridine derivative. It has antianginal and hypotensive action. 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 angina reduces the severity of myocardial ischemia; expanding peripheral arterioles, reduces peripheral vascular resistance, reduces preload on the heart, 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); It prevents the development of coronary artery spasm (incl. caused by smoking). In patients with angina and single daily dose increases the run-time physical activity, reduces the frequency of angina attacks and nitroglycerin consumption.
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. It does not lead to a sharp decrease in blood pressure, decrease in exercise tolerance and 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 myocardial contractility and conductivity, It does not cause a reflex increase in heart rate. It inhibits platelet aggregation, increases glomerular filtration rate, It has a weak natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria. No adverse effects on carbohydrate and lipid metabolism. The onset of action of the drug – 2-4 no, duration – 24 no.
Pharmacokinetics
Absorption
After oral administration of amlodipine is slowly absorbed from the gastrointestinal tract. The average absolute bioavailability of 64%, FROMmax observed through 6-9 no.
Distribution
The equilibrium state is established through 7 days of regular use. Eating does not affect the absorption of amlodipine.
Vd is 21 l / kg, which indicates, that most of the drug is in the tissues, and relatively less – in blood. Plasma protein binding is 95%. It penetrates through the BBB. Provided with breast milk.
Metabolism
Amlodipine medlenno, metabolized no ékstensïvno (to 90%) in the liver into inactive metabolites. Treated effect “first pass” through the liver. Metabolites not possess significant pharmacological activity.
Deduction
After a single oral T1/2 It varies between 31 to 48 no, when reappointment T1/2 approximately 45 no. About 60% excreted in the urine primarily as metabolites (10% – in unchanged form), 20-25% – with feces. The total clearance of amlodipine 7 ml / min / kg.
Pharmacokinetics in special clinical situations
In the elderly (senior 65 years) elimination of amlodipine slowed (T1/2 is 65 no) compared to younger patients, However, this difference has no clinical significance. With long-term use in patients with hepatic insufficiency T1/2 increases to 60 h and will be marked drug accumulation.
Renal failure does not significantly affect the kinetics of amlodipine. Amlodipine is not removed by hemodialysis.
Testimony
- Arterial Hypertension (as monotherapy or as part of combination antihypertensive therapy);
- Stable angina;
- Angiospastic (vasospastic) angina (Prinzmetal angina).
Dosage regimen
The initial dose hypertension and angina is 5 mg 1 time / day. The maximum dose – 10 mg 1 time / day. The maintenance dose is 2.5-5 mg / day.
At angina and vasospastic (vasospastic) angina the drug is prescribed in a dose 5-10 mg 1 time / day.
To prevent strokes – 10 mg / day.
Patients underweight or low growth, the elderly, patients with impaired liver function as antihypertensives Tenoks administered in an initial dose of 2.5 mg, as anti-anginal agents – 5 mg.
In appointing the drug patients with renal insufficiency does not require changes in the dosing regimen.
When used as part of combination therapy with thiazide diuretics, beta-blockers and ACE inhibitors correction dose is not required.
Side effect
Cardio-vascular system: heartbeat, breathlessness, marked reduction in blood pressure, fainting, vasculitis, swelling (swelling of the ankles and feet), flushing; rarely – Arrhythmia (bradycardia, ventricular tachycardia, auricular flutter), chest pain, orthostatic hypotension; rarely – development or exacerbation of congestive heart failure, arrythmia.
From the central and peripheral nervous system: headache, dizziness, fatiguability, drowsiness, mood changes, convulsions; rarely – loss of consciousness, gipestezii, nervousness, paresthesia, tremor, vertigo, asthenia, malaise, insomnia, depression, unusual dreams, backache; rarely – ataxia, apathy, ažitaciâ, amnesia, migraine.
From the senses: rarely – blurred vision, conjunctivitis, diplopia, sore eyes, tinnitus; rarely – parosmija, dysgeusia, ccomodation, xerophthalmia.
From the digestive system: nausea, vomiting, epigastric pain; rarely – increase in liver transaminases, jaundice (caused by cholestasis), pancreatitis, dry mouth, flatulence, giperplaziya right, constipation, diarrhea; rarely – gastritis, increased appetite.
From the urinary system: rarely – thamuria, tenesmus, nocturia, hyperuricemia; rarely – dizurija, polyuria.
On the part of the reproductive system: rarely – gynecomastia, sexual dysfunction (incl. reduced potency).
On the part of the musculoskeletal system: rarely – arthralgia, arthrosis, myalgia (prolonged use); rarely – myasthenia.
The respiratory system: rarely – dyspnoea, nose bleed; rarely – cough, rhinitis.
Metabolism: rarely – increase / decrease in body weight, giperglikemiâ, increased perspiration, thirst; rarely – cold clammy sweat.
From the hematopoietic system: rarely – thrombocytopenia, leukopenia.
Dermatological reactions: rarely – dermatoxerasia, alopecia, dermatitis, purpura, livor.
Allergic reactions: itching, rash (incl. эritematoznaya, rash maculo-paluleznaya), hives, angioedema.
Contraindications
- Severe hypotension,
- Collapse;
- Cardiogenic shock;
- Pregnancy;
- Lactation (breast-feeding);
- Children up to age 18 years (efficacy and safety have not been established);
- Hypersensitivity to amlodipine and other components of the drug;
- Hypersensitivity to other dihydropyridine derivatives.
FROM caution prescribe the drug in the human liver, SSS (bradycardia, tachycardia), In decompensated chronic heart failure, with mild to moderate hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and for 1 months after), for patients with diabetes, lipid metabolism disorders; elderly patients.
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation (breast-feeding).
Cautions
Against the background of the drug is necessary to monitor the patient's body weight, the appointment of an appropriate diet (control of sodium intake), and maintaining dental hygiene and frequent visits to the dentist (prevent soreness, bleeding and gingival overgrowth).
With increasing dose, careful monitoring of elderly patients.
Despite, that amlodipine does not cause withdrawal symptoms, Termination of treatment is recommended a gradual reduction in dose.
Effects on ability to drive vehicles and management mechanisms
No data are available on the effect of Tenoksa on ability to drive vehicles and operate machinery. Nonetheless, some patients, preferably at the beginning of treatment, may experience drowsiness or dizziness. In such cases, patients should be particularly careful when necessary performance, require high concentration and speed of psychomotor reactions.
Overdose
Symptoms: marked reduction in blood pressure, tachycardia, excessive expansion of peripheral vascular.
Treatment: gastric lavage, Activated carbon; control performance of the cardiovascular and respiratory system (including BCC and diuresis); if necessary, symptomatic therapy, aimed at maintaining the cardiovascular system; to restore vascular tone – use of vasopressors (in the absence of contraindications to their use); to eliminate the consequences of the blockade of calcium channels - in / in the introduction of calcium gluconate. Hemodialysis is not effective.
Drug Interactions
When combined inhibitors of microsomal liver enzymes increase the concentration of amlodipine in plasma (increase the risk of side effects), and enzyme inducers decrease the concentration of amlodipine.
The hypotensive effect of amlodipine is decreased while the use of NSAIDs, particularly with indomethacin (sodium retention and blockage of prostaglandin synthesis by the kidneys), alpha-agonists, Estrogen (sodium retention), simpatomimetikami.
And thiazide “loop” Diuretic, alpha, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and hypotensive effects of amlodipine.
Amiodarone, quinidine, alpha1-adrenoblokatorы, antipsychotic drugs (neuroleptics) and calcium channel blockers can increase the hypotensive effects of amlodipine
Amlodipine does not affect the pharmacokinetic parameters of digoxin and warfarin.
Cimetidine have no influence on amlodipine farmakokinetiku.
In a joint application with lithium, may increase the neurotoxicity of lithium (nausea, vomiting, diarrhea, ataxia, tremor, noise in ears).
Calcium can reduce the effects of calcium channel blockers.
Prokaynamyd, quinidine and other drugs, causing prolongation of the QT interval, reinforce the negative inotropic effect, it increases the risk of significant lengthening of the QT interval.
The pharmacokinetics of amlodipine is not changed while the appointment with cimetidine.
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 stored out of reach of children at or above 30 ° C. Shelf life – 2 year.
