Normodipine
Normodipin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Normodipine
ATX code: C08CA01
Active ingredient: amlodipine (amlodipine)
Manufacturer: Gedeon Richter-Rus, CJSC (Russia); Gedeon Richter (Hungary)
Description and photo update: 2019-20-08
Prices in pharmacies: from 308 rubles.
Buy
Normodipin is an antianginal and long-term dose-dependent antihypertensive drug; blocker of slow calcium channels.
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.
Pharmacological properties
Pharmacodynamics
As a blocker of slow calcium channels, a derivative of dihydropyridine, the active component of Normodipine, 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 into vascular smooth muscle cells, to a lesser extent into 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 artery disease (CHD) decreases; with 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 depression of the ST segment 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 the 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, when the patient is lying and standing, 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 exerts weak natriuretic effect. In patients with diabetic nephropathy, the severity of microalbuminuria does not increase. Amlodipine has no negative effect on metabolism and plasma lipids, and 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.
Pharmacokinetics
- 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 C max (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%. Withdrawal is two-phase, the average T 1/2 (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 in 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 Normodipine. 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;
- Arterial hypertension;
- Prinzmetal's angina (vasospastic angina).
Contraindications
Absolute:
- Severe arterial hypotension with systolic blood pressure (BP) below 90 mm Hg;
- Cardiogenic shock;
- Clinically significant aortic stenosis;
- Collapse;
- Unstable angina (except 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):
- Liver dysfunction;
- Sick sinus syndrome (SSSS) with severe bradycardia, tachycardia;
- Chronic heart failure of non-ischemic etiology according to NYHA classification III-IV functional class;
- Arterial hypotension;
- Mitral stenosis;
- Hypertrophic obstructive cardiomyopathy;
- Acute myocardial infarction, including the period within 1 month after it;
- Elderly age.
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 1 time per 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.
Perhaps an increase in T 1/2 ( half-life) of amlodipine and a decrease in creatinine clearance in elderly patients. 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.
Side effects
- 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), chest pain, myocardial infarction, orthostatic hypotension;
- Central and peripheral nervous system: often - drowsiness, increased 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;
- Urogenital 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 / 1000 -1/10 000- <1/1000 - rarely, <1/10 000 - very rarely, including single messages.
Overdose
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.
special instructions
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, in patients of short stature and / or low body weight.
In patients with impaired liver function, an increase in T 1/2 of amlodipine is possible, so they need to take the drug with caution.
It is recommended to complete therapy with Normodipine by gradually decreasing the dose of amlodipine, despite the fact that the termination of administration is not accompanied by the development of 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 develop dizziness, drowsiness, and other adverse reactions from the nervous system as a result of taking Normodipin, should take additional precautions when driving complex mechanisms and driving vehicles.
Application during pregnancy and lactation
Due to the lack of clinical experience in the use of Normodipin 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.
Pediatric use
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 Normodipin 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 Normodipin with caution.
Use in the elderly
In old age, Normodipin should be taken with caution.
Drug interactions
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, α 1 -adrenergic blockers - enhance the hypotensive effect;
- Antiviral drugs (including ritonavir) - increase plasma concentration;
- Isoflurane, antipsychotics - enhance the hypotensive effect;
- Calcium preparations - may 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 hypertension in conjunction with α-blockers, β-blockers, thiazide diuretics or ACE inhibitors. With stable angina, Normodipin 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.
Analogs
The analogues of Normodipine are: Amlodipine, Amlodipine-Teva, Amlodipine-Prana, Amlong, Norvask, Emlodin.
Terms and conditions of storage
Store out of the reach of children at temperatures up to 30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
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 adverse reactions.
Price for Normodipin in pharmacies
Approximate price of Normodipin for a pack containing 30 tablets:
- dosage 5 mg - 350-400 rubles;
- dosage 10 mg –650–800 rubles.
Normodipin: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Normodipin 5 mg tablets 30 pcs. 308 RUB Buy |
|
Normodipin tablets 5mg 30 pcs. RUB 314 Buy |
|
Normodipin 10 mg tablets 30 pcs. 575 RUB Buy |
|
Normodipin tablets 10mg 30 pcs. 653 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
