Stamlo M - instructions for use, doses, side effects, contraindications

Active substance: Amlodipine maleate 6.42 mg, equivalent to 5 mg of amlodipine. Excipients: cellulose microcrystalline 148.33 mg, sodium arboxymethyl starch (type A) 2.25 mg, silicon dioxide colloid 0.75 mg, magnesium stearate 2.25 mg.

Tablets 10 mg: each tablet contains:

Active substance: Amlodipine maleate 12.84 mg, equivalent to 10 mg of amlodipine. Excipients: cellulose microcrystalline 296.66 mg, sodium carboxymethyl starch (type A) 4.50 mg, silicon dioxide colloid 1.50 mg, magnesium stearate 4.50 mg.

Description:

Tablets 5 mg: white or almost white round flat tablets with bevel, embossed "R 177 "on one side and the dividing risk on the other side.

Tablets 10 mg: white or almost white oval biconvex tablets with embossing "R" on one side and "178" on the other side.

Pharmacotherapeutic group:blocker of "slow" calcium channels

ATX: & nbsp

C.08.C.A.01 Amlodipine

Pharmacodynamics:

The dihydropyridine derivative, the "slow" calcium channel blocker (BCCI), has an antianginal and antihypertensive effect.

Blocking calcium channels, reduces the transmembrane passage of calcium ions into the cell (mainly in vascular smooth muscle cells than cardiac myocytes). The mechanism of antihypertensive action of amlodipine is due to a direct relaxing effect on the smooth muscle of the vessels.

Reduction of myocardial ischemia occurs due to the expansion of coronary and peripheral arteries and arterioles in unchanged and in ischemic zones of the myocardium, reduction of the total peripheral resistance of blood vessels (OPSS), reduction of afterload and reduction of myocardial oxygen demand. Increases oxygen supply to the myocardium in patients with vasospastic angina (Prinzmetal angina); prevents the development of coronary artery spasm caused by smoking.In patients with angina, a single daily dose increases the time of exercise, delays the development of another Angina pectoris and depression of the segment ST (by 1 mm) with physical activity, reduces the incidence of angina attacks and the consumption of nitroglycerin and other nitrates. Has a long-term dose-dependent antihypertensive effect.

Antihypertensive effect is due to direct vasodilating effect on smooth muscles of blood vessels. With arterial hypertension, a single daily dose provides a clinically significant decrease in blood pressure (BP) for 24 hours in both the "lying" and "standing" positions.

Patients with cardiovascular diseases (including coronary atherosclerosis with one vessel and up to stenosis of three or more arteries, arteriosclerosis of the carotid arteries) who have had myocardial infarction, percutaneous transluminal angioplasty of the coronary arteries, or patients with angina pectoris, the use of amlodipine prevents the thickening of the intima- media of carotid arteries, reduces the lethality from myocardial infarction, stroke, transluminal angioplasty, aorto-coronary shunting; leads to a decrease in the number of hospitalizations for unstable angina and progression of chronic heart failure (CHF); reduces the frequency of interventions aimed at restoring coronary blood flow. It has anti-thrombotic, cardioprotective and anti-atherosclerotic effects.Does not increase the risk of death or development of complications and deaths in patients with CHF (III-IV class on NYHA) on the background of therapy with digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors. In patients with CHF (III-IV class on NYHA) non-ischemic etiology in the use of amlodipine, there is a possibility of pulmonary edema.

It does not cause a sharp decrease in blood pressure, a decrease in exercise tolerance, left ventricular ejection fraction. Reduces the degree of myocardial hypertrophy of the left ventricle.

Does not affect the contractility and conductance of the myocardium, does not cause a reflex increase in the number of cardiac contractions (HR), inhibits platelet aggregation, increases the rate of glomerular filtration, has a weak natriuretic effect. When diabetic nephropathy does not increase the severity of microalbuminuria. Can be used in the treatment of patients with bronchial asthma, diabetes and gout.Does not have adverse effects on the metabolism and lipids of blood plasma.

The time of onset of the effect is 2-4 hours; duration - 24 hours.

Pharmacokinetics:

Absorption and distribution. After oral administration amlodipine is slowly absorbed from the gastrointestinal tract. The time of intake and the composition of food do not affect the absorption of the drug. Biological availability is 64-80%. The concentration of the drug in the plasma reaches a maximum after 6-12 hours. A linear dependence of the amlodipine content in the blood plasma on the dose of the drug is revealed. Average volume of distribution (Vd) is 20-21 l / kg body weight, indicating that most of the drug is in the tissues, and relatively less in the blood. The equilibrium concentration in plasma (Css) is achieved after 7-8 days of constant intake of the drug. Communication with blood proteins - 95%. Penetrates through the blood-brain barrier.

Metabolism and excretion. After a single oral intake, the elimination half-life (T1 / 2) varies from 31 to 48 hours, and with a repeated appointment is about 45 hours. The liver biotransforms about 90% of amlodipine with the formation of inactive metabolites. It is excreted by the kidneys: 60% in the form of metabolites, 10% - in unchanged form; with bile and through the intestines - 20-25% in the form of metabolites, as well as with breast milk.The total clearance is 0.116 ml / s / kg (7 ml / min / kg).

Pharmacokinetics in special clinical cases. With heart failure - III-IV functional class for NYHA area under the distribution curve (AUC) increases by 40-60%. T1 / 2 in patients with arterial hypertension - 48 hours, in elderly patients increases to 65 hours, with hepatic insufficiency - up to 60 hours, similar magnification parameters T1 / 2 are observed and with severe CHF, with a violation of kidney function - does not change. Hemodialysis is not effective.

Indications:

Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs);

Stable exertional angina, vasospastic angina (in monotherapy or in combination with other antianginal agents)

Contraindications:

Hypersensitivity (including other dihydropyridines), severe arterial hypotension (SBP less than 90 mm Hg), cardiogenic shock; unstable angina (with the exception of vasospastic), obstruction of the left ventricular outflow tract (including clinically significant aortic stenosis).

Carefully:

Arterial hypotension, aortic stenosis, CHF of non-ischemic etiology (III-IV class on NYHA), hepatic insufficiency, acute myocardial infarction (and within the first 28 days), sinus node weakness syndrome (SSSU), age under 18, elderly age.

Pregnancy and lactation:

The safety of the use of amlodipine in pregnancy is not established, so use in pregnancy is possible only if the benefit to the mother exceeds the potential risk to the fetus.

There is no evidence of excretion, amlodipine with breast milk. However, it is known that other blockers of "slow" calcium channels - dihydropyridine derivatives, excreted in breast milk. In this connection, if it is necessary to prescribe Stamlo® M during lactation, the question of stopping breastfeeding should be solved.

Dosing and Administration:

Inside, once a day, washing down with the necessary amount of water (up to 100 ml).

With arterial hypertension and angina, the initial dose is 5 mg 1 time / day; If necessary, the daily dose can be increased to 10 mg, in a single dose.

In elderly patients, the drug is recommended for use in an average therapeutic dose, dose adjustment is not required.

In patients with impaired liver function, despite the fact that T1 / 2 amlodipine, like all BCCC increases, dose adjustment is usually not required.

In patients with renal insufficiency it is recommended to use Stamlo® M in usual doses, however, it is necessary to take into account the possible slight increase in T1 / 2 amlodipine.

No dosage adjustment is required for simultaneous administration with thiazide diuretics, beta-blockers and ACE inhibitors.

Side effects:

Determination of the frequency of adverse reactions: very often> 1/10; often> 1/100, <1/10; infrequently> 1/1000, <1/100; rarely> 1/10000, <1/1000; very rarely <1/10000, including individual messages.

From the side of the cardiovascular system: often - peripheral edema (ankles and feet), a feeling of palpitations; infrequently - excessive reduction of blood pressure, orthostatic hypotension, vasculitis, flushing of blood to the face; rarely - development or aggravation of the course of chronic heart failure; very rarely - rhythm disturbances (bradycardia, ventricular tachycardia, atrial fibrillation), myocardial infarction, chest pain.

From the nervous system: often - headache, dizziness, increased fatigue,drowsiness; infrequent - general malaise, fainting, asthenia, hypoesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, emotional lability, unusual dreams, increased excitability, depression, anxiety; rarely cramps, apathy, agitation; very rarely - ataxia, amnesia, migraine.

From the digestive system: often - nausea, abdominal pain; infrequent - vomiting, constipation, diarrhea, flatulence, indigestion, diarrhea, anorexia, dryness of the oral mucosa, thirst; rarely - gingival hyperplasia, increased appetite; very rarely - gastritis, pancreatitis, hyperbilirubinemia,jaundice (usually cholestatic), increased activity of "hepatic" transaminases, hepatitis.

From the hematopoiesis: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.

From the genitourinary system: infrequently - pollakiuria, painful urination, nocturia, impotence; very rarely - dysuria, polyuria.

From the musculoskeletal system: infrequently - arthralgia, muscle cramps, myalgia, back pain, arthrosis; rarely - myasthenia gravis.

From the respiratory system: infrequently - shortness of breath, rhinitis, nosebleeds; very rarely - cough.

Allergic reactions: infrequently - itchy skin, rash; very rarely - angioedema, erythema multiforme, urticaria.

From the sense organs: very rarely - parosmia; infrequent - ringing in the ears, impaired vision, diplopia, disruption of accommodation, xerophthalmia, conjunctivitis, pain in the eyes, perversion of taste.

From the skin: rarely - dermatitis; very rarely - alopecia, a violation of skin pigmentation, increased sweating, cold sticky sweat.

Other: infrequently - gynecomastia, increase / decrease in body weight, chills; rarely - hyperglycemia.

Overdose:

Symptoms: marked decrease in blood pressure - with the possible development of reflex tachycardia and excessive peripheral vasodilation (the risk of severe and persistent arterial hypotension, including with the development of shock and death).

Treatment: gastric lavage, the appointment of activated charcoal, maintenance of cardiovascular functions, monitoring of heart and lung function indicators, elevated position of the lower limbs, control of the volume of circulating blood and diuresis,symptomatic and supportive therapy, intravenous administration of calcium gluconate and dopamine.Hemodialysis is not effective.

Interaction:

Inhibitors of microsomal oxidation can increase the concentration of amlodipine in plasma, increasing the risk of side effects, and inducers of microsomal enzymes of the liver - reduce.

Unlike other BCCI, there is no clinically significant interaction with non-steroidal anti-inflammatory drugs, especially indomethacin.

Thiazide and "loop" diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal or antihypertensive effects.

Does not affect the pharmacokinetic parameters of digoxin and warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine.

Calcium preparations can reduce the effect of BCCC.

Antiviral drugs (ritonavir) increase plasma concentrations of BCCM, including amlodipine.

Neuroleptics and isoflurane increase the antihypertensive action of dihydropyridine derivatives.

Special instructions:

The drug Stamlo® M can be used as a monotherapy in most patients. With insufficient antihypertensive effect can be combined with ACE inhibitors, thiazide diuretics, alpha-adrenoblockers or beta-blockers.

The drug Stamlo® M can also be prescribed as a monotherapy or in combination with other antianginal agents in patients refractory to treatment with nitrates and / or beta-adrenoblockers in adequate doses. During the period of treatment, it is necessary to control the body weight and sodium intake, the appropriate diet.

It is necessary to maintain dental hygiene and frequent visits to the dentist (to prevent soreness, bleeding, and gingival hyperplasia). The dosage regimen for elderly patients is the same as for patients of other age groups. When increasing the dose, careful monitoring of elderly patients is necessary.

Despite the lack of "slow" calcium channels of the syndrome of "cancellation" in blockers, a gradual decrease in doses is recommended before cessation of treatment. Stamlo®M does not affect the content of potassium ions, glucose, triglycerides, total cholesterol, low-density lipoproteins (LDL), uric acid, creatinine and uric acid nitrogen.

Patients with low body weight, low growth patients and patients with severe liver function impairment may need a smaller dose of the drug.

The efficacy and safety of the use of amlodipine in hypertensive crisis is not established.

Effect on the ability to drive transp. cf. and fur:Care should be taken when managing vehicles and other complex mechanisms, especially at the beginning of treatment and with increasing doses.

Form release / dosage:

Tablets 5 mg or 10 mg.

Packaging:For 14 tablets in a blister of (PVC / AL / PA) foil / aluminum foil. 2 blisters with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002091

Date of registration:17.10.2011

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

DR. REDDY`S LABORATORIES, LTD. India

Representation: & nbspDR REDDY'S LABORATORIS LTD. DR REDDY'S LABORATORIS LTD. India

Information update date: & nbsp17.10.2011

Illustrated instructions

Instructions

Stamlo® M (Stamlo® M)