STAMLO M

Active material: Amlodipine
When ATH: C08CA01
CCF: Kalьcievыh channel blocker
ICD-10 codes (testimony): I10, i20, I20.1
When CSF: 01.03.02
Manufacturer: DR. REDDY`S LABORATORIES LTD. (India)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills white or nearly white, round, flat, Embossed “R 177” on one side and Valium – on the other side.

Excipients: microcrystalline cellulose, sodium starch glycolate, Colloidal anhydrous silica, magnesium stearate.

14 PC. – blisters (2) – cardboard boxes.

Pills white or nearly white, Oval, lenticular, Embossed “R” on one side and “178” – on the other side.

Excipients: microcrystalline cellulose, sodium starch glycolate, Colloidal anhydrous silica, magnesium stearate.

14 PC. – blisters (2) – cardboard boxes.

Pharmacological action

Calcium channel blocker slow II generation, dihydropyridine derivative. It has antihypertensive and antianginal.

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 constriction of the coronary arteries (incl. caused by smoking).

In patients with angina and single daily dose Stamlo^® M 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 nitrates.

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). 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.

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 metabolism and lipid content in the blood plasma.

The therapeutic effect develops after 2-4 no, duration – 24 no.

Pharmacokinetics

Absorption

After oral administration of amlodipine is slowly absorbed from the gastrointestinal tract. Receipt time and composition of the food does not affect the degree of absorption of the drug. The absolute bioavailability of 64%. C_max achieved through 6-9 no. Revealed linear dependence of the content of amlodipine in the blood of the dose Stamlo^® M.

Food intake does not alter the bioavailability of amlodipine.

Distribution

Average V_d is 21 l / kg, which indicates, that most of the drug is in the tissues, and relatively less – in blood. C_ss achieved through 7 days of continuous use of the drug.

The binding to plasma proteins – 95%. It penetrates through the BBB.

Metabolism

Amlodipine podvergaetsya medlennomu, but extensive metabolism (90%) in the liver into inactive metabolites, exposed effect “first pass” through the liver. Metabolites not possess significant pharmacological activity.

Deduction

After a single oral T_1/2 It varies between 31 to 48 no, and for re-appointment is about 45 no. In the liver, about biotransformiroetsa 90% amlodipine into inactive metabolites. Report the news: 60% as metabolites, 10% – in unchanged form; with feces – 20-25% as metabolites. Provided with breast milk. The total clearance of 0.116 ml / sec / kg (7 ml / min / kg, 0.42 L / h / kg).

Pharmacokinetics in special clinical situations

Elderly patients over 65 s elimination of amlodipine slowed (T_1/2 – 65 no) compared to younger patients, However, this difference has no clinical significance.

Patients with hepatic insufficiency is expected elongation T_1/2 and assigning prolonged drug accumulation in the body is higher (T_1/2 increases to 60 no).

Renal failure does not significantly affect the kinetics of amlodipine.

When hemodialysis is not removed.

Testimony

- Arterial hypertension (as monotherapy or in combination with other antihypertensives);

- Angina;

- Angiospastic angina (Prinzmetal angina).

Dosage regimen

At hypertension and angina starting dose is 5 mg 1 time / day. Maintenance dose hypertension – 5 mg / day. The maximum dose - 10 mg 1 time / day.

At angina and vasospastic angina – 5-10 mg 1 time / day.

No dose adjustment Stamlo^® M, while the use of thiazide diuretics, beta-blockers, ACE inhibitors, long-acting nitrates and sublingual nitroglycerin.

Elderly patients, patients of small stature, patients with reduced body weight, patients with impaired liver function as antihypertensive agents are administered in an initial dose of 2.5 mg, as anti-anginal agents – 5 mg.

At renal failure dose adjustment 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 – arrhythmias (bradycardia, ventricular tachycardia, auricular flutter), chest pain, orthostatic hypotension; rarely – development or exacerbation of congestive heart failure, arrythmia, migraine.

CNS: headache, dizziness, fatiguability, drowsiness, mood changes, convulsions; rarely – loss of consciousness, gipesteziya, nervousness, paresthesia, tremor, vertigo, asthenia, malaise, insomnia, depression, unusual dreams; rarely – 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; rarely – gastritis, increased appetite.

With the genitourinary system: rarely – thamuria, tenesmus, nocturia, sexual dysfunction (incl. reduced potency); rarely – dizurija, polyuria.

Dermatological reactions: rarely – dermatoxerasia, alopecia, dermatitis, purpura, livor.

The respiratory system: rarely – dyspnoea; rarely – cough, rhinitis.

On the part of the musculoskeletal system: rarely – arthralgia, arthrosis, backache, myalgia (prolonged use); rarely – myasthenia.

From the senses: rarely – diplopia, conjunctivitis, sore eyes, blurred vision, conjunctivitis, tinnitus; rarely – parosmija, dysgeusia, ccomodation, xerophthalmia.

From the hematopoietic system: rarely – thrombocytopenia, leukopenia.

Allergic reactions: itching, rash (incl. эritematoznaya, maculo-papular rash, hives), angioedema.

Other: rarely – gynecomastia, increase / decrease in body weight, giperglikemiâ, nose bleed, increased perspiration, thirst; rarely – cold clammy sweat.

Contraindications

- Severe hypotension (systolic blood pressure less than 90 mmHg.);

- Collapse;

- Cardiogenic shock;

- Unstable angina (except Prinzmetal angina);

- Pregnancy;

- Lactation (breast-feeding);

- Childhood and adolescence up 18 years (efficacy and safety have not been established);

- Hypersensitivity to amlodipine and other ingredients;

- Hypersensitivity to dihydropyridine.

FROM caution It should appoint a drug in the human liver, SSS (vыrazhennaya bradycardia, tachycardia), chronic heart failure decompensated, mild or moderate hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and for 1 Months after), diabetes, lipid metabolism disorders, elderly patients.

Pregnancy and lactation

The drug is contraindicated in pregnancy and lactation (breast-feeding).

Cautions

TIRED^® M may be used as monotherapy in most patients. At insufficient antihypertensive effect may be combined with an ACE inhibitor, thiazide diuretics, angiotensin II receptor antagonists, alpha-blockers or beta-blockers.

TIRED^® M may also be administered as monotherapy or in combination with other antianginal drugs in patients, refractory to treatment with nitrates and / or beta-blockers in adequate doses.

During treatment requires monitoring of body weight and sodium intake, the appointment of 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 regimen for elderly patients 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.

TIRED^® M did not affect the plasma concentrations of potassium, Glucose, triglycerides, total cholesterol, LDL, Uric acid, creatinine and urea nitrogen.

Effects on ability to drive vehicles and management mechanisms

There were no reports on the effect of Stamlo^® M on driving or using machinery. Nonetheless, some patients, preferably at the beginning of treatment, may experience drowsiness or dizziness. If this happens, the patient has to take special precautions while driving and operating 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 – use of vasopressors (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade – in / with the introduction of calcium gluconate. Hemodialysis is not effective.

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.

Antihypertensive effect of weakening the NSAID, especially indomethacin (sodium retention and blockage of prostaglandin synthesis by the kidneys), alpha adrenostimulyatorov, Estrogens (sodium retention), sympathomimetic.

Calcium reduces the effect of calcium channel blockers slow.

And thiazide “loop” Diuretic, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and hypotensive effects.

Amiodarone, quinidine, alpha₁-adrenoblokatorы, antipsychotic drugs (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.

In a joint application with lithium may increase symptoms of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, noise in ears).

Prokaynamyd, quinidine and other drugs, causing prolongation of the QT interval, while the use of amlodipine reinforce the negative inotropic effect and may increase risk of significant lengthening of the QT interval.

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, dark place at a temperature no higher than 25 ° C. Shelf life – 2 year.