Amlorus Valium 5mg 30 pcs synthesis

Description

Composition
Active substance:
1 tablet contains: amlodipine besylate (calculated as amlodipine) – 2.5 mg or 5 mg or 10 mg.
Excipients:
Lactose monohydrate (milk sugar) – 45.83 mg, 63.17 mg, 88.34 mg; Microcrystalline cellulose – 45.7 mg, 62.9 mg, 87.8 mg; crospovidone – 1.0 mg, 1.4 mg, 2.0 mg; colloidal silicon dioxide (Aerosil) – 0.5 mg, 0.7 mg, 1.0 mg; Talc – 2.5 mg, 3.5 mg, 5.0 mg; calcium stearate (cal) – 1.0 mg, 1.4 mg, 2.0 mg.
Product form:
Tablets of 2.5 mg, 5 mg, 10 mg.
At 10 or 20 tablets in blisters.
30 tablets in glass jars or plastics. 1, 2 or 3 blisters in a pack or jar enclosing the insert.
Contraindications
– increased sensitivity to amlodipine, to other dihydropyridine derivatives and other components of the formulation; – severe hypotension (systolic blood pressure less than 90 mmHg..); – cardiogenic shock; – acute myocardial infarction within 28 days; – unstable angina (except vasospastic); – obstruction of left ventricular outflow tract (including clinically significant aortic stenosis); – the age of 18; – lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Dosage
5 mg
Indications
Arterial hypertension (monotherapy or in combination with other antihypertensive agents). Stable angina, vasospastic angina (Prinzmetal’s angina) (monotherapy or in combination with other antianginal drugs).
Interaction with other drugs
Inhibitors of microsomal oxidation increase the concentration of amlodipine in the blood plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes decrease. Amlodipine does not affect the pharmacokinetic parameters of digoxin and warfarin do not affect changes in prothrombin time induced by warfarin. Cimetidine does not affect the pharmacokinetics of amlodipine. Calcium blockers can reduce the effect of “slow” calcium channels (including amlodipine). Unlike other blockers “slow” calcium channel significant interactions when combined with nonsteroidal antiinflammatory drugs (including inometatsinom) was not detected. Thiazide and “loop” diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and antihypertensive action of amlodipine. Alpha-1-adrenergic blockers, antipsychotics, amiodarone and quinidine – may enhance the antihypertensive effect of amlodipine in a joint application. Blockers “slow” calcium channels (including amlodipine) can increase the severity of the negative inotropic effects of antiarrhythmic drugs that cause lengthening of the interval QT (amiodarone, quinidine, procainamide). When combined with preparations of lithium may be increased manifestations of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). A single dose of sildenafil at a dose of 100 mg in patients with essential hypertension have not effect on the pharmacokinetic parameters of amlodipine. Repeated application of amlodipine 10 mg and atorvastatin 80 mg is not accompanied by a significant change in the pharmacokinetics of atorvastatin. Antivirals (ritonavir) increase the plasma concentration blockers “slow” calcium channels (including amlodipine). A single dose of aluminum and magnesium antacids have no significant effect on the pharmacokinetics of amlodipine. Grapefruit juice may reduce the plasma concentration of amlodipine, but simultaneous single dose of 240 mg of grapefruit juice and 10 mg amlodipine inwardly not accompanied by a significant change in the pharmacokinetics of amlodipine.
Overdose
Symptoms: marked decrease in blood pressure with the possible development of reflex tachycardia and excessive peripheral vasodilatation (there is the probability of severe and persistent hypotension, including with the development of shock and death).
Treatment: gastric lavage, the appointment of activated carbon, the maintenance of the cardiovascular system, the control performance of the heart and the lungs, an elevated position of the lower extremities, control of blood volume and diuresis. To restore vascular tone – application of vasoconstrictive drugs (in the absence of contraindications for their use); to eliminate the effects of calcium channel blockade – intravenous calcium gluconate. Since amlodipine is largely associated with serum proteins – hemodialysis ineffective.
pharmachologic effect
Pharmacodynamics:
Dihydropyridine derivative – blocker “slow” calcium channels, has an antihypertensive and anti-anginal action. Blocking calcium channels, reduces the transmembrane passage of calcium ions into the cell (mainly in vascular smooth muscle cells than cardiac myocytes). The antihypertensive action due to the direct vasodilatory effects on vascular smooth muscle. It has a long dose-dependent antihypertensive effect. Amlodipine reduces myocardial ischemia (has antianginal action) in two ways: 1) expands peripheral arterioles and thus reduces the total peripheral vascular resistance, decreases the afterload on the heart, the heart rate remains virtually unchanged, which leads to lower energy consumption and infarction needs oxygen; 2) dilates coronary and peripheral arteries and arterioles in the unaltered and in ischemic areas of the myocardium, increasing the oxygen supply to the myocardium (especially with vasospastic angina), reduce the severity of myocardial ischemia and prevent the development of coronary artery spasm (including those caused by smoking). When hypertension single dose provides a clinically significant reduction in blood pressure over 24 hours (in the patient’s position “lying” and “standing”). Due to the slow onset of action of amlodipine does not cause a sharp decrease in blood pressure. It does not reduce the exercise tolerance and left ventricular ejection fraction. In patients with angina single daily dose of amlodipine increases the run-time physical activity slows the development of angina and “ischemic” ST segment depression (1 mm), reduces the frequency of angina attacks and consumption of nitroglycerin and other nitrates. Reduces the degree of left ventricular hypertrophy, antiatherosclerotic and cardioprotective effect in ischemic heart disease (CHD). In patients with coronary artery disease (including coronary atherosclerosis with a lesion of the vessel and to stenosis three or more arteries and carotid atherosclerosis) underwent myocardial infarction, percutaneous transluminal angioplastinku coronary arteries (PTCA) or angina pectoris, amlodipine prevents the development of intimal thickening, medial carotid arteries, significantly reduces mortality from cardiovascular causes, myocardial infarction, stroke, PTCA, coronary artery bypass surgery, reduces the number of hospitalizations for not stable angina pectoris and chronic heart failure progresses, reduces the frequency of interventions to restore coronary blood flow. Amlodipine does not increase the risk of death or complications that lead to the deaths in patients with chronic heart failure (III-IV functional class according to the classification of New York Heart Association (NYHA)) during therapy with digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors. In patients with chronic heart failure (III-IV functional class NYHA classification) nonischemic etiology when using amlodipine there is a probability of occurrence of pulmonary edema. No effect on the myocardial contractility and conductivity, does not cause reflex increase of heart rate (HR), inhibits platelet aggregation and increases glomerular filtration rate, has a weak natriuretic action. In diabetic nephropathy does not increase the severity of microalbuminuria. It has no adverse effects on metabolism and lipid concentration in blood plasma and can be used in the treatment of patients with bronchial asthma, diabetes and gout. Time of onset of drug effect – 2-4 hour duration of effect – 24 hours. When long-term therapy the maximum reduction in blood pressure occurs within 6-12 hours after taking amlodipine inside. If, after prolonged treatment with amlodipine cancel, the effective reduction in blood pressure is maintained for 48 hours after the last dose. Then, blood pressure gradually returned to baseline levels within 5-6 days.
Pharmacokinetics:
Slow absorption is independent of food intake is about 90%. Bioavailability was 60-90%, the maximum serum concentration observed 6-12 hours after administration. The volume of distribution is approximately 21 l / kg of body weight, indicating that most of the drug is in the tissues, and relatively smaller – in the blood. Most of the drug present in the blood (95-97%), binds to plasma proteins. Amlodipine penetrates the blood-brain barrier. When hemodialysis is not removed. Equilibrium amlodipine plasma concentration (Css) is achieved after 7-8 days of continuous dosing. Amlodipine undergoes slow but extensive metabolism (90%) in the liver into inactive metabolites, has the effect of “primary” passing through the liver. Metabolites not possess significant pharmacological activity. After a single oral half-life (T1 / 2) ranges from 31 to 48 hours on repeated administration of T1 / 2 of approximately 45 hours – which corresponds prescribing 1 time per day. Total Amlodipine clearance is 0.116 ml / sec / kg (7 mL / min / kg, 0.42 L / h / kg). In elderly patients (over 65 years) the excretion of amlodipine slowed down (T1 / 2 is increased up to 65 hours) compared to younger patients. In the elderly and in young patients the time needed to achieve the maximum concentration of amlodipine in plasma, almost the same. Patients with liver failure and severe chronic heart failure, T1 / 2 is increased to 56-60 hours. T1 / 2 from the plasma of patients with renal failure is increased to 60 hours. Changing amlodipine plasma concentration does not correlate with the degree of renal dysfunction . About 60% of an oral dose is excreted mainly by the kidneys as metabolites, 10% unchanged, in the bile and through the intestine – 20-25% in the form of metabolites.
Pregnancy and breast-feeding
Safety of amlodipine in pregnancy has not been established, therefore use during pregnancy is possible only when the application of benefit to the mother outweighs the potential risk to the fetus. There is no evidence of amlodipine excretion in breast milk. However, we know that other blockers “slow” calcium channel blockers – dihydropyridine derivatives are excreted in breast milk. In this connection, if necessary Amlorus® appointment during lactation should decide the issue of termination of breastfeeding. Women of childbearing age should use reliable methods of contraception.
Conditions of supply of pharmacies
On prescription.
side effects
Under the frequency of adverse reactions is understood: very often 31/10; often 31/100,
With the cardiovascular system: often – peripheral edema (ankles and feet), palpitations, feeling of heat and “tides” of blood to the face skin; infrequently – excessive fall in blood pressure, orthostatic hypotension, vasculitis; rarely – the development or exacerbation of chronic heart failure; very rarely – cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), heart attack, chest pain.
Central nervous system: often – fatigue, dizziness, headache, drowsiness, headache; infrequently – malaise, fainting, sweating, asthenia, hypesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability, abnormal dreams, nervousness, depression, anxiety; rarely – seizures, lethargy, agitation; very rarely – ataxia, amnesia.
From the sensory organs: rarely – ringing in the ears, blurred vision, eye pain, double vision, xerophthalmia, conjunctivitis, accommodation disturbance, dysgeusia; very rarely – parosmiya.
From the digestive system: often – abdominal pain, nausea; infrequently – vomiting, constipation, flatulence, dyspepsia, diarrhea, anorexia, dryness of the oral mucosa, thirst; rarely – gingival hyperplasia, increased appetite; very rarely – gastritis, pancreatitis, hyperbilirubinemia, jaundice (usually cholestatic), increased activity of “liver” transaminases, hepatitis.
From the urinary system: rarely – frequent urination, painful urination, nocturia, impotence; very rarely – dysuria, polyuria.
The respiratory system: rarely – dyspnea, rhinitis, epistaxis; very rarely – cough.
On the part of the musculoskeletal system: rarely – arthralgia, muscle cramps, myalgia, back pain, arthritis; rarely – myasthenia gravis.
For the skin: rare – alopecia; rarely – dermatitis; very rarely – a violation of skin pigmentation, dermatoxerasia.
From the side of hematopoiesis: rarely – thrombocytopenia purpura, leukopenia, and thrombocytopenia.
From a metabolism: very rarely – hyperglycemia. Allergic reactions: rarely – itching, rash; very rarely – angioedema, erythema multiforme, urticaria.
Other: rare – a gynecomastia, increase / decrease in body weight, chills; very rarely – a cold sweat.
special instructions
When treating arterial hypertension Amlorus® may be used in combination with a thiazide diuretic, an alpha-blockers, beta-blockers and ACE inhibitors. For the treatment of angina Amlorus® can be combined with other antianginal agents, such as nitrates, prolonged or short-acting beta-blockers. Amlorus® it can be applied in cases where the patient is predisposed to vascular spasm (vasoconstriction). Amlorus® not affect the plasma potassium ion concentration, glucose, triglycerides, total cholesterol, low density lipoproteins, uric acid, creatinine and urea nitrogen, and can be used in the treatment of patients with bronchial asthma, diabetes and gout. Patients with low body weight, short stature patients and patients with severe hepatic dysfunction as an antihypertensive Amlorus® administered in an initial dose of 2.5 mg, as anti-anginal agents – 5 mg. During the treatment it is necessary to control body weight and intake of sodium, shows the assignment of an appropriate diet, observation at the dentist (to prevent pain, bleeding and gingival hyperplasia). Despite the lack of preparation syndrome “cancel” before the termination of treatment is recommended a gradual reduction in dose.
Effects on ability to drive vehicles and management mechanisms
The treatment should be careful when driving and other lesson potentially dangerous activities which require high concentration and psychomotor speed reactions.
Storage conditions
In a dry, protected from light at a temperature not higher than 25 C. Keep out of reach of children.
Dosing and Administration
Tablets are taken singly inwardly squeezed necessary amount of water (100 mL).
For the treatment of hypertension and angina is 5 initial dose of 1 mg of drug once a day. Depending on the individual response of the patient, if necessary dose can be increased to a maximum of 10 mg 1 time per day.
When hypertension maintenance dose can be 5 mg per day. When vasospastic angina (Prinzmetal’s angina) – 5.10 mg per day, once.
Do not need to change the dose while the appointment of thiazide diuretics, beta-blockers and ACE inhibitors.
Patients with liver failure, the elderly – may require a dose change, the initial dose in patients with arterial hypertension can be 2.5 mg.
In appointing the drug to patients with renal impairment is not required changing the dosing regime.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist