Instruction for Normodipin
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Normodipin is an antianginal and long-term dose-dependent antihypertensive drug; slow calcium channel blocker.
Release form and composition
Dosage form Normodipin - tablets: oblong-rounded, biconvex, almost white or white; at a dose of 5 mg - engraving "5" on one side; in a dose of 10 mg - engraving "10" on one side, on the other side - risk (10 pcs. in blisters, 3 blisters in a cardboard box).
1 tablet contains:
Active ingredient: amlodipine besylate - 6.944 or 13.889 mg (respectively, the content of amlodipine is 5 or 10 mg);
Auxiliary components: microcrystalline cellulose, anhydrous calcium hydrogen phosphate, sodium carboxymethyl starch (type A), magnesium stearate.
As a blocker of slow calcium channels, a derivative of dihydropyridine, the active component of Normodipin, amlodipine, has antianginal and hypotensive effects. By binding to the S6 segments of the III and IV domains of the α1-subunit of the L-type calcium channel, amlodipine blocks calcium channels, reducing the transmembrane transition of calcium ions into the cell (mainly in vascular smooth muscle cells, to a lesser extent in cardiomyocytes).
The antianginal efficacy of Normodipin is provided by the expansion of peripheral arteries and arterioles, as well as coronary arteries: in patients with angina pectoris, the severity of coronary heart disease (IHD) decreases; with the expansion of peripheral arterioles, the total peripheral vascular resistance (OPSR) decreases, the preload on the heart decreases, and the oxygen demand of the heart muscle decreases. Due to the expansion of the coronary arteries and arterioles in the ischemic and unchanged areas of the myocardium, the flow of oxygen into the heart muscle increases (especially in patients with vasospastic angina); prevents the development of spasm of the coronary arteries (including smokers). For patients with stable angina pectoris, taking a single daily dose increases exercise tolerance, slows down the development of ischemic ST segment depression and angina pectoris; reduces the frequency of angina attacks, reducing the need for nitroglycerin and other nitrates.
Amlodipine has a long-term hypotensive effect, depending on the dose, its hypotensive effect is determined by a direct vasodilating effect on vascular smooth muscle tissue. In patients with arterial hypertension, taking a single dose of Normodipin provides a clinically significant drop in blood pressure, in the patient's supine and standing position, for 24 hours.
Orthostatic hypotension due to the use of amlodipine is extremely rare. It does not cause a decrease in exercise tolerance and left ventricular ejection fraction, lowers the level of left ventricular myocardial hypertrophy, does not affect conduction and myocardial contractility, does not cause a reflex increase in heart rate (HR), inhibits platelet aggregation, increases the glomerular filtration rate and has weak natriuretic effect. In patients with diabetic nephropathy, the severity of microalbuminuria does not increase. Amlodipine does not have a negative effect on metabolism and plasma lipids; it can be used in the treatment of patients with bronchial asthma, gout and diabetes mellitus.
The effect of taking amlodipine occurs after 2-4 hours and lasts 24 hours.
absorption: when administered orally, the substance is absorbed from the gastrointestinal tract slowly and almost completely, food intake does not affect its absorption. In blood plasma, it reaches Cmax (maximum concentration) after 6-12 hours, regardless of the patient's age. Css (saturation stage) in plasma occurs after 7-14 days of intake; the bioavailability of the substance is 63–80%;
distribution to organs and tissues: Vd (volume of distribution) is 21 l / kg, which is an indicator of the predominant distribution in tissues. Up to 97% of amlodipine binds to plasma proteins. The substance penetrates the BBB (blood-brain barrier), as well as into breast milk;
metabolism: up to 90% of amlodipine is biotransformed in the liver, forming inactive metabolites;
excretion: up to 10% of amlodipine is excreted in the urine unchanged and up to 60% in the form of metabolites; with feces in the form of metabolites - 20-25%. Excretion is two-phase, the average T1 / 2 (half-life) is 35-50 hours. The total clearance of the substance is 7 ml / min / kg. Amlodipine is not excreted during hemodialysis.
In elderly patients over 65 years of age and patients with moderate and severe chronic heart failure, the clearance of amlodipine decreases with a subsequent increase in AUC (area under the concentration-time curve) by 40-60%, which requires the appointment of reduced initial doses of Normodipin. A similar decrease in AUC is observed due to impaired liver function.
Renal failure has no significant effect on the pharmacokinetics of amlodipine.
Indications for use
According to the instructions, Normodipin is indicated for use for monotherapy or as part of the combined treatment of the following diseases / conditions:
Stable exertional angina;
Prinzmetal angina (vasospastic angina).
Severe arterial hypotension with systolic blood pressure (BP) below 90 mm Hg;
Clinically significant aortic stenosis;
Unstable angina (except for Prinzmetal's angina);
The period of pregnancy and breastfeeding (lactation);
Children and adolescents up to 18 years of age (there is no clinical experience of use);
Hypersensitivity to amlodipine and other dihydropyridine derivatives.
Relative (Normodipin tablets are taken with caution due to the increased likelihood of complications):
Sick sinus syndrome (SSS) with severe bradycardia, tachycardia;
Chronic heart failure of non-ischemic etiology according to NYHA classification III-IV functional class;
Hypertrophic obstructive cardiomyopathy;
Acute myocardial infarction, including the period within 1 month after it;
Instructions for the use of Normodipin: method and dosage
Normodipin tablets are taken orally.
For the treatment of angina pectoris and arterial hypertension, it is recommended to take Normodipin in an initial dose of 5 mg once a day. The maximum dose is 10 mg per day. The maintenance dose for hypertension is 5 mg per day.
In the case of simultaneous administration with β-blockers, thiazide diuretics and angiotensin-converting enzyme (ACE) inhibitors, a change in the dose of amlodipine is not required.
An increase in T1 / 2 (half-life) of amlodipine and a decrease in creatinine clearance in elderly patients is possible. No dose adjustment is required, but more careful monitoring of patients is required.
With renal failure, a change in the dose of Normodipin is not required.
Cardiovascular system: often - peripheral edema (especially swelling of the feet and ankles), flushing of the face, palpitations; infrequently - an excessive decrease in blood pressure (BP); very rarely - vasculitis, development or exacerbation of heart failure, cardiac arrhythmias (ventricular tachycardia, bradycardia, atrial fibrillation), sternum pain, myocardial infarction, orthostatic hypotension;
Central and peripheral nervous system: often - drowsiness, fatigue, dizziness, headache; infrequently - general malaise, asthenia, hypesthesia, paresthesia, tremor, vertigo, peripheral neuropathy, fainting, insomnia, unusual dreams, mood lability, increased excitability, anxiety, depression; very rarely - ataxia, amnesia, agitation, apathy;
Digestive system: often - abdominal pain, nausea; sometimes - diarrhea or constipation, flatulence, vomiting, dyspepsia, anorexia, thirst, dryness of the oral mucosa; rarely - increased appetite, gingival hyperplasia; very rarely - gastritis, pancreatitis, jaundice (caused by cholestasis), increased activity of hepatic transaminases, hyperbilirubinemia, hepatitis;
Hematopoietic organs: very rarely - leukopenia, thrombocytopenic purpura, thrombocytopenia;
Genitourinary system: rarely - impotence, painful urination, frequent urination, nocturia; very rarely - polyuria, dysuria;
Skin: rarely - dermatitis; very rarely - xeroderma, purpura, skin pigmentation disorders;
Allergic reactions: infrequently - rash (including erythematous and maculopapular), pruritus; very rarely - angioedema, urticaria, erythema multiforme;
Musculoskeletal system: sometimes - myalgia (with prolonged use of Normodipin), muscle cramps, arthralgia, arthrosis, back pain; rarely - myasthenia gravis;
Sense organs: rarely - ringing in the ears, diplopia, xerophthalmia, visual impairment, conjunctivitis, eye pain;
Other: rarely - gynecomastia, alopecia, dyspnea, hyperuricemia, weight loss / increase, epistaxis, hyperhidrosis; very rarely - cough, rhinitis, cold clammy sweat, parosmia, violation of accommodation, violation of taste, hyperglycemia.
The following gradation of the frequency of adverse reactions is used:> 1/10 - very often,> 1 / 100- <1/10 - often,> 1/1000 - <1/100 - infrequently,> 1/10 000- <1/1000 - rare, <1/10 000 - very rare, including single messages.
Symptoms of an overdose of Normodipin are: tachycardia, a marked decrease in blood pressure, hypertrophied peripheral vasodilation with the risk of developing severe and persistent arterial hypotension, up to shock and death, inclusive.
Therapy: the patient should be in the supine position with the legs raised above the level of the head; it is recommended to take activated charcoal, gastric lavage, support the function of the cardiovascular system, control the volume of circulating blood, urine output, indicators of heart and lung function. In order to restore vascular tone, it is necessary to use vasoconstrictor drugs, if there are no contraindications to their use. To eliminate the consequences of calcium channel blockade, intravenous administration of calcium gluconate is required.
Hemodialysis with an overdose of Normodipin is ineffective.
During therapy, control of body weight and sodium intake should be carried out. It is also recommended to adhere to an appropriate diet, oral hygiene, regular teeth sanitation in order to prevent bleeding, soreness and gingival hyperplasia.
A reduced dose of Normodipin may be required in patients with severe liver dysfunction, patients of short stature and / or low body weight.
In patients with impaired liver function, the T1 / 2 lengthening of amlodipine is possible, so they need to take the drug with caution.
It is recommended to complete therapy with Normodipin by gradually decreasing the dose of amlodipine, despite the fact that the termination of administration is not accompanied by the development of a withdrawal syndrome.
In hypertensive crisis, the safety and efficacy of the drug have not been established.
Influence on the ability to drive vehicles and complex mechanisms
Some patients, mainly at the beginning of therapy, who experience dizziness, drowsiness, and other adverse reactions from the nervous system as a result of taking the drug, should take additional precautions when driving complex mechanisms and driving vehicles.
Application during pregnancy and lactation
Due to the lack of clinical experience with the use of the drug during pregnancy and lactation, the drug should not be prescribed to pregnant and lactating women, as well as to patients of childbearing age who do not use reliable methods of protection.
The use of Normodipin in pediatrics is contraindicated for the treatment of children and adolescents under 18 years of age.
With impaired renal function
With renal failure, no change in the dose of the drug is required, since its concentration in the blood plasma does not depend on the degree of decrease in renal function.
For violations of liver function
Patients with impaired liver function should be prescribed the drug with caution.
Use in the elderly
In old age, Normodipin should be taken with caution.
The effect of concurrently taken substances / drugs on blockers of slow calcium channels of the dihydropyridine series, including amlodipine:
Thiazide and "loop" diuretics, nitrates, verapamil, ACE inhibitors, β-blockers - can enhance the hypotensive and antianginal effect;
Antipsychotics, α1-blockers - enhance the hypotensive effect;
Antiviral drugs (including ritonavir) - increase plasma concentration;
Isoflurane, antipsychotics - enhance the hypotensive effect;
Calcium preparations - can reduce the therapeutic effect.
Due to the simultaneous use of lithium preparations with amlodipine, the effects of neurotoxicity may increase: ataxia, diarrhea, nausea, vomiting, tinnitus, tremor.
It is safe to use amlodipine for the treatment of arterial hypertension in conjunction with α-blockers, β-blockers, thiazide diuretics or ACE inhibitors. With stable angina pectoris, the drug can be taken with other antianginal drugs: nitrates of short or prolonged action, β-blockers.
Amlodipine can be used with antibacterial, non-steroidal anti-inflammatory drugs (NSAIDs), especially indomethacin, and hypoglycemic drugs for oral administration.
Sildenafil at a dose of 100 mg with a single dose in patients with essential hypertension does not affect the pharmacokinetics of amlodipine.
Repeated administration of amlodipine (10 mg) with atorvastatin (80 mg) does not cause clinically significant changes in the pharmacokinetic action of atorvastatin.
Grapefruit juice (240 mg) and Normodipin (10 mg), when taken simultaneously, do not significantly change the pharmacokinetics of amlodipine.
Single and repeated use of amlodipine (10 mg) does not affect the pharmacokinetics of ethanol (alcoholic beverages).
Amlodipine does not affect the pharmacokinetics of cyclosporine, renal clearance and serum digoxin concentration, as well as the effectiveness of warfarin (prothrombin time).
The pharmacokinetics of amlodipine is not affected by combined use with cimetidine.
According to in vitro studies, with the combined use of digoxin, phenytoin, warfarin and indomethacin with Normodipin, amlodipine has no effect on their binding to blood proteins.
Terms and conditions of storage
Store out of the reach of children at temperatures up to 30 ° C.
Shelf life is 3 years.
Reviews about Normodipin
In most reviews, Normodipin is characterized as an effective drug of a wide spectrum of therapeutic action, relatively safe and convenient to use (taken once a day).
The disadvantages are the high cost of the drug and some side effects.
Terms of sell
You don't need a prescription to buy Normodipin.