Normodipine, pills 5mg, 30pcs

Composition

Active ingredient:

amlodipine;

Auxiliary substances:

magnesium stearate;

sodium carboxymethyl starch;

calcium hydrophosphate anhydrous;

MCC

Pharmacological action

Normodipine has an antianginal, antihypertensive effect.

A slow calcium channel blocker, a dihydropyridine derivative, has an antianginal and antihypertensive effect. Binding to the S6 segments of the III and IV domains of the alpha-1 subunit of the L-type calcium channel, it blocks calcium channels and reduces the transmembrane transfer of calcium ions into the cell (more to vascular smooth muscle cells than to cardiomyocytes).

The antianginal effect is caused by the expansion of coronary and peripheral arteries and arterioles: in angina pectoris, it reduces the severity of myocardial ischemia; by expanding peripheral arterioles, it reduces OPSS, reduces preload on the heart, and reduces the need for oxygen in the myocardium.

Dilates the coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases oxygen supply to the myocardium (especially in vasospastic angina); prevents the development of coronary artery spasm (including caused by smoking). In patients with stable angina, a single daily dose increases exercise tolerance, slows down the development of angina and “ischemic” ST-segment depression, reduces the frequency of angina attacks and consumption of nitroglycerin and other nitrates.

It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to the direct vasodilating effect on vascular smooth muscles. In arterial hypertension, a single dose provides a clinically significant reduction in blood pressure for 24 hours (in the patient’s “lying” and “standing” positions).

Orthostatic hypotension with the appointment of amlodipine is quite rare. It does not cause a decrease in exercise tolerance, left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy.

It does not affect the contractility and conduction of the myocardium, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases the glomerular filtration rate, and has a weak natriuretic effect. In diabetic nephropathy, it does not increase the severity of microalbuminuria.

It does not have any adverse effect on the metabolism and concentration of plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes mellitus and gout.

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

. Pharmacokinetics

Suction

When taken orally, it is slowly and almost completely absorbed from the gastrointestinal tract. Food intake does not affect absorption. Cmax in blood plasma is reached in 6-9 hours, both in elderly and young patients. The average absolute bioavailability is 64%.

The distribution

of Css of amlodipine in blood plasma is achieved after continuous use for 7-8 days.

Vd is approximately 21 l / kg, which indicates a predominant distribution in the tissues. Penetrates through the BBB and into breast milk.

Binding to plasma proteins is 97%.

Metabolism

About 90% of amlodipine is biotransformed in the liver to form inactive metabolites.

Deduction

Amlodipine is excreted in the urine (10% of the dose is unchanged and 60% in the form of inactive metabolites) and in the faeces (20-25% in the form of metabolites). Elimination is two-phase, T1 / 2 averages 31-48 hours.

The total clearance of amlodiline is 7 ml / min / kg. During hemodialysis, amlodipine is not removed.

Pharmacokinetics in special clinical cases

In elderly patients (over 65 years of age), the elimination of amlodipine is slowed (T1/2 – 65 hours) compared to young patients, but these differences are not clinically significant.

Prolongation of T1 / 2 in patients with hepatic insufficiency suggests that with prolonged use, the accumulation of the drug in the body will be higher (T1 / 2-up to 60 hours).

The presence of renal insufficiency in the patient does not significantly affect the pharmacokinetics of amlodipine.

Indications

• arterial hypertension (as monotherapy or in combination with other antihypertensive agents);
• stable tension angina (as monotherapy or in combination with other antianginal agents);
• vasospastic angina (Prinzmetal angina) (as monotherapy or in combination with other antianginal agents).

Use during pregnancy and lactation

Contraindicated.

Contraindications

pregnancy; lactation; age up to 18 years (due to lack of clinical experience); severe hypotension (systolic blood pressure less than 90 mm Hg); collapse; cardiogenic shock; clinically significant aortic stenosis; unstable angina (except Prinzmetal angina pectoris); hypersensitivity to amlodipine and other dihydropyridine derivatives. With caution: the drug should be prescribed in patients with impaired liver function, SSSU (severe bradycardia, tachycardia), chronic heart failure of non-ischemic etiology of NYHA functional class III-IV, arterial hypotension, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and for 1 month after it), elderly patients.

Side effects

Allergic reactions: infrequently-pruritus of the skin, rash (including erythematous, maculopapular rash); very rarely-urticaria, angioedema, erythema multiforme. From the genitourinary system: rarely-frequent urination, painful urination, nocturia, impotence; very rarely-dysuria, polyuria. From the cardiovascular system: often-palpitations, peripheral edema (swelling of the ankles and feet), flushes of blood to the skin of the face; infrequently-excessive decrease in blood pressure; very rarely-development or aggravation of the course of heart failure, rhythm disorders (bradycardia, ventricular tachycardia, atrial fibrillation), myocardial infarction, chest pain, orthostatic hypotension, vasculitis. From the central and peripheral nervous system: often-headache, dizziness, increased fatigue, drowsiness; infrequently-asthenia, general malaise, hypesthesia, paresthesia, peripheral neuropathy, tremor, vertigo, fainting, insomnia, mood lability, unusual dreams, increased excitability, depression, anxiety; very rarely – apathy, ataxia, agitation, amnesia. From the digestive system: often-nausea, abdominal pain; sometimes-vomiting, constipation or diarrhea, flatulence, dyspepsia, anorexia, dry oral mucosa, thirst; rarely-gum hyperplasia, increased appetite; very rarely-pancreatitis, gastritis, jaundice (due to cholestasis), hyperbilirubinemia, increased activity of liver transaminases, hepatitis. Hematopoietic disorders: very rare – thrombocytopenic purpura, leukopenia, thrombocytopenia. From the skin: rarely-dermatitis; very rarely-purpura, xeroderma, skin pigmentation disorder. Musculoskeletal disorders: sometimes-muscle cramps, myalgia (with prolonged use), arthralgia, back pain, osteoarthritis; rarely-myasthenia gravis. From the sensory organs: rarely-visual disturbances, diplopia, conjunctivitis, eye pain, xerophthalmia, tinnitus. Others: rarely-alopecia, gynecomastia, hyperuricemia, weight gain/loss, dyspnoea, nosebleeds, increased sweating; very rarely-cold sticky sweat, cough, rhinitis, parosmia, taste disorders, accommodation disorders, hyperglycemia.

Interaction

Cimetidine does not affect the pharmacokinetics of amlodipine. In vitro studies, amlodipine did not affect the binding of digoxin, phenytoin, warfarin, and Indometacin to blood proteins. Simultaneous single use of 240 mg grapefruit juice and 10 mg amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine. Amlodipine can be safely used for the treatment of hypertension together with thiazide diuretics, alpha-blockers, beta-blockers or ACE inhibitors. In patients with stable angina, the drug can be combined with other antianginal agents, for example, with prolonged-acting nitrates, beta-blockers or short-acting nitrates. Amlodipine can be used simultaneously with NSAIDs (especially Indometacin), antibacterial agents and hypoglycemic agents for oral use. It is possible to enhance the antianginal and antihypertensive effects of dihydropyridine slow calcium channel blockers when combined with thiazide and loop diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates, as well as to enhance their hypotensive effect when combined with alpha-1-blockers, neuroleptics. Although no negative inotropic effects have usually been observed in studies of amlodipine, however, some slow calcium channel blockers may increase the severity of the negative inotropic effects of antiarrhythmic agents that cause prolongation of the QT interval (for example, amiodarone and quinidine). A single dose of sildenafil 100 mg in patients with essential hypertension does not affect the pharmacokinetics of amlodipine. Repeated use of amlodipine at a dose of 10 mg and atorvastatin at a dose of 80 mg is not accompanied by significant changes in the pharmacokinetics of atorvastatin.Amlodipine with a single and repeated use in a dose of 10 mg does not affect the pharmacokinetics of ethanol (drinks containing alcohol). Antiviral agents (ritonavir) increases plasma concentrations of slow calcium channel blockers, including amlodipine. Antipsychotics and isoflurane enhance the hypotensive effect of dihydropyridine derivatives. Calcium supplements may reduce the effect of slow calcium channel blockers. When amlodipine is co-administered with lithium preparations, it is possible to increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Amlodipine does not alter the pharmacokinetics of cyclosporine. It does not affect the serum concentration of digoxin and its renal clearance. It does not significantly affect the effect of warfarin (prothrombin time).

How to take, course of use and dosage

Inside, the initial dose for the treatment of arterial hypertension and angina pectoris is 5 mg / day. The maximum daily dose is 10 mg once. In case of arterial hypertension, the maintenance dose may be 5 mg / day (1 tablet of 5 mg).

In elderly patients, T_1/2 of amlodipine may increase and creatinine clearance may decrease. No dose changes are required, but patients should be monitored more closely.

No dose adjustment is required when administered concomitantly with thiazide diuretics, beta-blockers, and ACE inhibitors.

No dose adjustment is required in patients with renal insufficiency.

Overdose

Symptoms: tachycardia, marked decrease in blood pressure, excessive peripheral vasodilation (risk of severe and persistent hypotension, including with the development of shock and death). Treatment: gastric lavage, use of activated charcoal, maintenance of the cardiovascular system, monitoring of heart and lung function, elevated, above head level, position of the lower extremities, control of BCC and diuresis. To restore vascular tone — the use of vasoconstrictors (in the absence of contraindications to their use); in order to eliminate the consequences of calcium channel blockade — intravenous use of calcium gluconate. Hemodialysis is ineffective.

Special instructions

Effects on motor vehicle driving ability and mechanism management There have been no reports of the effect of Normodipine® on driving or working with mechanisms. However, some patients, especially at the beginning of treatment, may experience drowsiness, dizziness and other side effects from the nervous system. If they occur, the patient should take special precautions when driving a car and working with complex mechanisms. During treatment with Normodipine®, it is necessary to monitor body weight and sodium intake, and prescribe an appropriate diet. It is necessary to maintain dental hygiene and follow up with a dentist (to prevent soreness, bleeding and gum hyperplasia). Patients with low body weight, short stature, and severe hepatic impairment may require a lower dose. If liver function is impaired, T1 / 2 of the drug may also be prolonged. Therefore, Normodipine should be administered with caution in such patients. Despite the fact that discontinuation of Normodipine is not accompanied by the development of withdrawal syndrome, discontinuation of treatment should be carried out by gradually reducing the dose of the drug. The efficacy and safety of the drug in hypertensive crisis has not been established.

Tablet Form of production

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Amlodipine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Angina