Amlodipine-Prana
Amlodipine-Prana: 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. For violations of liver function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Amlodipine-Prana
ATX code: C08CA01
Active ingredient: amlodipine (amlodipinum)
Manufacturer: PRANAPHARM, LLC (Russia)
Description and photo update: 2018-25-10
Prices in pharmacies: from 35 rubles.
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Amlodipine-Prana is a slow calcium channel blocker (BMCC).
Release form and composition
Dosage form of the drug Amlodipine-Prana - tablets: flat-cylindrical, beveled, color from white to white with a creamy shade, slight marbling is possible; tablets in a dosage of 10 mg - with a dividing line on one side (10 pcs. in blister strip packs or 40, 50, 60, 70, 80, 90, 100 pcs. in polymer cans; in a cardboard box 1 can or 1-10 blisters).
Composition for 1 tablet:
- active substance: amlodipine - 5 or 10 mg (in the form of amlodipine besylate - 6.93 or 13.86 mg, respectively);
- auxiliary components: lactose, corn starch, magnesium stearate, microcrystalline cellulose.
Pharmacological properties
Pharmacodynamics
The active ingredient of the drug Amlodipine-Prana is amlodipine, a dihydropyridine derivative, II-generation BMCC, which has antianginal and antihypertensive effects. Due to binding to dihydropyridine receptors, 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 the substance is due to its expanding effect on coronary and peripheral arteries and arterioles; in patients with angina pectoris, the severity of cardiac muscle ischemia decreases. The expansion of peripheral arterioles helps to reduce the total peripheral vascular resistance (OPSR), reduces the preload on the heart and myocardial oxygen demand. The expansion of the main coronary arteries and arterioles in the ischemic and unchanged areas of the myocardium increases the supply of oxygen to the heart muscle (especially in patients with vasospastic angina pectoris), prevents the development of spasm of the coronary arteries (including those caused by tobacco smoking). In patients with stable angina pectoris, when taking a single daily dose of amlodipine, exercise tolerance increases,the development of angina pectoris and ischemic depression of the ST segment slows down, the frequency of angina attacks and the need for nitroglycerin and other nitrates decrease.
Amlodipine-Prana has a prolonged dose-dependent hypotensive effect due to its direct vasodilating effect on vascular smooth muscle. In patients with arterial hypertension, taking a single dose of amlodipine provides a decrease in blood pressure (BP) by a clinically significant amount within 24 hours, both in the supine position and in the standing position. Cases of development of orthostatic hypotension with the use of amlodipine are rare. The drug does not cause a decrease in exercise tolerance and a decrease in the left ventricular ejection fraction, reduces left ventricular myocardial hypertrophy. Amlodipine does not affect the contractility and conductivity of the heart muscle, does not cause a reflex increase in the heart rate (HR), inhibits platelet aggregation,potentiates the glomerular filtration rate and has a weak natriuretic effect. In patients with diabetic nephropathy, it does not affect the severity of microalbuminuria. It does not have an adverse effect on the metabolism and concentration of blood plasma lipids; it can be used in the treatment of patients with diabetes mellitus, bronchial asthma, and gout. A significant decrease in blood pressure occurs 6-10 hours after taking the drug, the effect lasts 24 hours.
Pharmacokinetics
The main pharmacokinetic characteristics of amlodipine:
- absorption: after oral administration, amlodipine is slowly absorbed from the gastrointestinal tract (GIT); the average absolute bioavailability is 64%; maximum concentration (C max) in blood serum reaches 6-9 hours after administration; equilibrium serum concentrations (C ss) are observed after 7–8 days of regular intake; diet and food quality do not have a clinically significant effect on the absorption of the substance;
- distribution: average volume of distribution (V d) - 21 l / kg body weight, which indicates the distribution of most of the substance in the tissues; less amlodipine entering the blood is 95% bound to plasma proteins;
- metabolism: a significant effect of presystemic metabolism (first pass through the liver) is absent in amlodipine; it undergoes a slow but active hepatic metabolism with the formation of metabolites that do not have significant pharmacological activity;
- Elimination: the half-life (T 1/2) after a single oral administration of the drug is from 31 to 48 hours, with repeated administration, the T 1/2 is ~ 45 hours; up to 60% of the dose taken orally is eliminated in the urine mostly in the form of metabolites, up to 10% - unchanged; up to 20-25% is excreted through the intestines and in breast milk. The indicator of the total clearance of amlodipine is 0.116 ml / s / kg, or 7 ml / min / kg, or 0.42 l / h / kg.
In elderly patients (over 65 years old), the excretion of amlodipine is slowed down in comparison with young patients, the T 1/2 index increases to 65 hours, but this fact is not clinically significant.
In liver failure, lengthening T 1/2 (up to 60 hours) suggests that prolonged use of amlodipine will increase its cumulation in the body.
Renal failure has no significant effect on the pharmacokinetics of the drug. Amlodipine is not removed during hemodialysis.
The drug crosses the blood-brain barrier.
Indications for use
Amlodipine-Prana is recommended for use in arterial hypertension for monotherapy or as part of a complex treatment with other antihypertensive drugs.
With stable exertional angina and vasospastic angina (Prinzmetal's angina) Amlodipine-Prana is used for monotherapy or as part of a complex treatment with other antianginal drugs.
Contraindications
Absolute:
- severe hypotension (systolic blood pressure <90 mm Hg);
- unstable angina, except for Prinzmetal's angina;
- collapse, cardiogenic shock;
- clinically significant aortic stenosis;
- lack of lactase, lactose intolerance, glucose-galactose malabsorption;
- period of pregnancy;
- breastfeeding (lactation);
- children and adolescents under 18 years of age;
- hypersensitivity to dihydropyridine derivatives, including amlodipine and other components of the drug.
With caution, Amlodipine-Prana is prescribed to patients with impaired liver function, sick sinus syndrome (with severe bradycardia, tachycardia), chronic heart failure (CHF) of non-ischemic etiology of III-IV functional class according to NYHA classification, arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy (GOKMP), acute myocardial infarction (and within 1 month after it), as well as in old age.
Instructions for the use of Amlodipine-Prana: method and dosage
Amlodipine-Prana tablets are intended for oral administration.
Recommended dosage:
- arterial hypertension and angina pectoris (treatment): initial dose - 5 mg once a day; the maximum dose is 10 mg once a day;
- arterial hypertension (maintenance therapy): dose - 2.5–5 mg (½ – 1 tablet of 5 mg) once a day.
Due to an increase in T 1/2 of amlodipine in elderly patients and a decrease in creatinine clearance (CC), dose changes are not required, but more careful monitoring of the patient's condition is required.
The appointment of Amlodipine-Prana for renal failure, as well as simultaneously with thiazide diuretics, β-blockers and angiotensin-converting enzyme (ACE) inhibitors, does not require dose adjustment.
Side effects
The incidence of side effects according to the classification of the World Health Organization (WHO) (very often -> 0.1; often -> 0.01 and 0.001 and 0.0001 and <0.001; extremely rare - <0.0001, incl. single messages):
- cardiovascular system: often - peripheral edema (swelling of the ankles / feet), palpitations, flushing of the face; sometimes - a significant decrease in blood pressure; extremely rarely - loss of consciousness, shortness of breath, orthostatic hypotension, vasculitis, development / worsening of heart failure, cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), chest pain, myocardial infarction;
- central and peripheral nervous system: often - dizziness, headache, drowsiness, increased fatigue; sometimes - general malaise, asthenia, paresthesia, hypesthesia, peripheral neuropathy, insomnia, unusual dreams, mood lability, tremors, increased excitability, anxiety, depression; extremely rare - migraine, hyperhidrosis, apathy;
- digestive system: often - nausea, abdominal pain; sometimes - constipation or diarrhea, vomiting, flatulence, anorexia, dyspepsia, dryness of the oral mucosa, thirst; rarely - increased appetite, gingival hyperplasia; extremely rarely - gastritis, pancreatitis, jaundice (a consequence of cholestasis), increased activity of hepatic transaminases, hyperbilirubinemia, hepatitis;
- hematopoietic organs: extremely rarely - leukopenia, thrombocytopenic purpura, thrombocytopenia;
- genitourinary system: sometimes - nocturia, frequent / painful urination, impotence; extremely rare - polyuria, dysuria;
- respiratory system: sometimes - rhinitis, shortness of breath; extremely rare - cough;
- skin and integument: rarely - dermatitis; extremely rare - alopecia, skin pigmentation disorders, xeroderma, cold sweat;
- hypersensitivity reactions: pruritus, skin rash (including erythematous, maculopapular and urticaria), erythema multiforme, angioedema;
- musculoskeletal system: sometimes - myalgia, arthralgia, muscle cramps, arthrosis, back pain; rarely - myasthenia gravis;
- other reactions: sometimes - diplopia, xerophthalmia, ringing in the ears, violation of accommodation, eye pain, conjunctivitis, nosebleeds, chills, gynecomastia; extremely rare - parosmia, hyperglycemia.
Overdose
Symptoms of an amlodipine overdose are excessive peripheral vasodilation with a pronounced and possibly prolonged decrease in blood pressure, collapse and shock.
For the treatment of the condition, it is recommended to wash the stomach, ensure the intake of activated charcoal, and take measures to maintain the work of the cardiovascular system under the control of indicators of heart and lung function. It is required to provide the patient with a horizontal position, raise the lower limbs above the level of the head. It is also necessary to control the volume of circulating blood (BCC) and urine output. In order to restore vascular tone, vasoconstrictors should be used (in the absence of contraindications), and calcium gluconate should be administered intravenously to eliminate the consequences of calcium channel blockade. Hemodialysis is ineffective.
special instructions
During therapy, body weight and sodium intake are monitored, and an appropriate diet is prescribed if necessary.
In order to prevent bleeding, soreness and gingival hyperplasia, oral hygiene should be observed and regularly sanitized by a dentist.
Patients with low body weight, short stature and severely impaired liver function may require dose adjustment towards its reduction.
Discontinuation of the drug Amlodipine-Prana does not cause withdrawal syndrome, despite this, it is desirable to complete therapy with a gradual dose reduction.
The safety and efficacy of taking the drug in hypertensive crisis has not been established.
Influence on the ability to drive vehicles and complex mechanisms
In connection with the possible development at the beginning of treatment of such adverse reactions as dizziness and drowsiness, special precautions are required when driving and performing other types of work that require increased concentration of attention.
Application during pregnancy and lactation
Amlodipine-Prana is prohibited for use by pregnant and lactating women, since the safety and effectiveness of such therapy for this group of patients has not been established.
Pediatric use
In pediatrics, the use of the drug for the treatment of children and adolescents under the age of 18 is contraindicated (safety and efficacy have not been established).
For violations of liver function
According to the instructions, Amlodipine-Prana is used with caution in patients with impaired liver function.
Use in the elderly
In elderly patients, it is possible to lengthen T 1/2 and clearance of amlodipine, which does not require correction of the dosage regimen, but with an increase in the dose, if necessary, their condition should be more carefully monitored.
Drug interactions
- antihypertensive drugs (thiazide diuretics, alpha-blockers, beta-blockers, ACE inhibitors): safe when used together with amlodipine for the treatment of hypertension;
- antianginal agents (long-acting or short-acting nitrates, beta-blockers): safe when used together with amlodipine for the treatment of stable angina pectoris;
- nonsteroidal anti-inflammatory drugs (NSAIDs) (especially indomethacin), antibacterial agents and hypoglycemic agents for oral administration: simultaneous use with amlodipine is possible;
- thiazide and loop diuretics, verapamil, ACE inhibitors, beta-blockers, nitrates: can enhance the antianginal and hypotensive effect of BMCC;
- alpha 1 -adrenergic blockers, antipsychotics: can enhance the antihypertensive effect of BMCC;
- antiarrhythmic drugs (amiodarone, quinidine): it should be borne in mind that some BMCCs can increase the severity of their negative inotropic action and cause prolongation of the QT interval;
- sildenafil: with a single dose of 100 mg in patients with essential hypertension, the pharmacokinetics of amlodipine does not affect;
- atorvastatin (at a dose of 80 mg): with repeated use with amlodipine (at a dose of 10 mg), significant changes in the pharmacokinetic parameters of atorvastatin are not observed;
- alcohol (drinks containing ethyl alcohol): with single and repeated use with amlodipine (at a dose of 10 mg), the pharmacokinetics of ethanol does not change;
- antiviral drugs (ritonavir): increase the plasma concentrations of BMCC, including amlodipine;
- antipsychotics, isoflurane: potentiate the hypotensive efficacy of dihydropyridine derivatives;
- calcium preparations: able to reduce the effect of BMCC;
- lithium preparations: an increase in the manifestations of neurotoxicity (ataxia, nausea / vomiting, diarrhea, tinnitus, tremor) is possible;
- cyclosporine: amlodipine does not alter its pharmacokinetics;
- digoxin: amlodipine does not affect its serum concentration and renal clearance;
- warfarin: amlodipine has no significant effect on its effectiveness (prothrombin time);
- cimetidine: does not affect the pharmacokinetics of amlodipine;
- digoxin, phenytoin, warfarin, indomethacin: according to in vitro studies, amlodipine does not affect their binding to blood proteins;
- grapefruit juice: with a simultaneous single oral administration of amlodipine (at a dose of 10 mg) and 240 ml of grapefruit juice, no significant changes in the pharmacokinetics of amlodipine were observed.
Analogs
Amlodipine-Prana analogs are: Amlovas, Amlodak, Amlodigamma, Amlodipine Zentiva, Amlodipine Cardio, Amlodipharm, Amlokard-Sanovel, Amlorus, Amlotop, Amlong, Vero-Amlodipine, Cardilopin, Karmagip, Kalchek, Stavodil, Normvaodskipin, …
Terms and conditions of storage
Store at temperatures up to 25 ° C in a dry, dark place. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Amlodipine-Prana
According to reviews, Amlodipine-Prana well and quickly reduces blood pressure, which, after taking the drug, stabilizes for a long time. As disadvantages, some patients note the appearance of puffiness.
The price of Amlodipine-Prana in pharmacies
The approximate price for Amlodipine-Prana, depending on the dosage and packaging, varies from 12 to 38 rubles.
Amlodipine Prana: prices in online pharmacies
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Drug name Price Pharmacy |
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Amlodipine-Prana 5 mg tablets 30 pcs. 35 RUB Buy |
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Amlodipine-Prana 5mg tablets 30 pcs. RUB 37 Buy |
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Amlodipine-Prana 10 mg tablets 30 pcs. RUB 47 Buy |
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Amlodipine-Prana 10mg tablets 30 pcs. RUB 48 Buy |
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Amlodipine-Prana 5 mg tablets 90 pcs. RUB 50 Buy |
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Amlodipine-Prana 5mg tablets 90 pcs. RUB 95 Buy |
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Amlodipine-Prana 10 mg tablets 90 pcs. RUB 98 Buy |
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Amlodipine-Prana 10mg tablets 90 pcs. 125 RUB Buy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, 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!
