Amlodipine Cardio
Amlodipine Cardio: 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 Cardio
ATX code: C08CA01
Active ingredient: amlodipine (Amlodipine)
Manufacturer: JSC "Pharmaceutical Enterprise" Obolenskoe "(Russia)
Description and photo update: 2019-10-07
Prices in pharmacies: from 62 rubles.
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Amlodipine Cardio is a second generation slow calcium channel blocker that has hypotensive and antianginal effects.
Release form and composition
Dosage form - tablets: almost white or white; dosage 5 mg - oblong biconvex shape, with rounded ends and a line; dosage of 10 mg - flat-cylindrical round shape with a line and a chamfer (7, 10, 14 or 20 tablets in blister strip packs; in a cardboard box 1-5 packs and instructions for the use of Amlodipine Cardio).
Composition of 1 tablet:
- active substance: amlodipine - 5 or 10 mg (amlodipine besylate - 6.95 or 13.9 mg);
- auxiliary components: lactose monohydrate, magnesium stearate, talc, potato starch, hypromellose.
Pharmacological properties
Pharmacodynamics
Amlodipine is an active substance of the drug, belongs to the number of dihydropyridine derivatives and is a second generation BMCC (slow calcium channel blocker), has hypotensive and antianginal effects (as a result of binding to the S6 segment III and IV of the alpha 1-subunit of the L-type calcium channel).
The antihypertensive effect of amlodipine is due to a direct vasodilating effect on vascular smooth muscle. A single dose of Amlodipine Cardio for hypertension provides a clinically significant decrease in blood pressure (blood pressure) in the patient's lying and standing position for 24 hours. The development of orthostatic hypotension during therapy is quite rare. Amlodipine helps to reduce the degree of left ventricular myocardial hypertrophy. The drug does not affect the conductivity and contractility of the myocardium, and does not cause a reflex increase in heart rate (heart rate). It has a weak natriuretic property, inhibits platelet aggregation, and increases the glomerular filtration rate.
The antianginal effect of amlodipine is associated with the expansion of peripheral and coronary arteries and arterioles: in patients with angina pectoris, the severity of myocardial ischemia decreases; due to the expansion of peripheral arterioles, there is a decrease in OPSS (total peripheral vascular resistance), there is a decrease in preload on the heart, a decrease in myocardial oxygen demand. Amlodipine in ischemic and unchanged areas of the myocardium dilates the coronary arteries and arterioles, increases the flow of oxygen to the myocardium (especially in patients with vasospastic angina); prevents the appearance of spasm of the coronary arteries (including those associated with smoking). A single daily dose of Amlodipine Cardio for angina pectoris helps to increase the time for performing physical activity,during its implementation, it delays the onset of an attack of angina pectoris and depression of the ST segment (by 1 mm), reduces the frequency of angina attacks, and the use of nitroglycerin and other nitrates for their relief. It has a long-term hypotensive dose-dependent effect.
The severity of microalbuminuria in diabetic nephropathy does not increase.
It does not have an adverse effect on metabolism and plasma lipid concentration and can be used in the treatment of patients with concomitant bronchial asthma, gout and diabetes mellitus. A significant decrease in blood pressure is noted after 6-10 hours, the duration of the therapeutic effect of Amlodipine Cardio is 24 hours.
Pharmacokinetics
Amlodipine is slowly absorbed from the gastrointestinal tract after oral administration. The average absolute bioavailability is 64%. The time to reach C max (maximum concentration) of a substance in the blood serum is from 6 to 9 hours, C ss (equilibrium serum concentrations) - 7–8 days of daily use.
Food intake does not affect the absorption of Amlodipine Cardio. Average V d (volume of distribution) - 21 l / kg of body weight, thus most of the dose is in the tissues, less than half of the absorbed dose enters the blood. Most (95%) of the amlodipine in the blood binds to blood plasma proteins. Metabolism occurs in the liver slowly but actively, while there is no significant first pass effect. The metabolites have no pronounced pharmacological activity.
T 1/2 (half-life) after a single dose of amlodipine inside is in the range of 31-48 hours, with repeated administration of Amlodipine Cardio, the value of this indicator is approximately 45 hours. Approximately 60% of the ingested dose is excreted by the kidneys, mainly in the form of metabolites, and in the form of an unchanged substance - 10%. Also, excretion is carried out through the intestines (20-25%) and in breast milk.
The total clearance of the substance is 16 ml / s / kg (0.42 l / h / kg, 7 ml / min / kg). The excretion of amlodipine in patients over 65 years of age slows down (T 1/2 is 65 hours) in comparison with young patients, but this difference has no clinical significance.
The lengthening of the T 1/2 value against the background of liver failure suggests that with prolonged administration, the cumulation of amlodipine in the body will be higher (T 1/2 - up to 60 hours). Renal failure does not significantly affect the kinetics of amlodipine. The drug is not removed during hemodialysis. Penetrates the blood-brain barrier.
Indications for use
- arterial hypertension: as monotherapy or in combination with other antihypertensive drugs;
- stable exertional angina and Prinzmetal angina (vasospastic angina): as monotherapy or in combination with other antianginal drugs.
Contraindications
Absolute:
- severe arterial hypotension (in patients with systolic pressure less than 90 mm Hg. Art.);
- unstable angina (except for Prinzmetal's angina);
- collapse, cardiogenic shock;
- clinically significant aortic stenosis;
- lactose intolerance, glucose-galactose malabsorption or lactase deficiency;
- pregnancy and lactation;
- age up to 18 years;
- individual intolerance to the components of the drug, as well as dihydropyridine derivatives.
Relative (Amlodipine Cardio tablets are prescribed under medical supervision):
- hepatic dysfunction;
- chronic heart failure with non-ischemic etiology (NYHA classification - III-IV functional class);
- sick sinus syndrome (severe bradycardia, tachycardia);
- aortic / mitral stenosis;
- arterial hypotension;
- acute myocardial infarction (and within one month after myocardial infarction);
- GOKMP (hypertrophic obstructive cardiomyopathy);
- elderly age.
Amlodipine Cardio, instructions for use: method and dosage
Amlodipine Cardio tablets are taken orally.
Recommended dosage regimen:
- arterial hypertension and angina pectoris: initial dose - 5 mg once a day; maximum - 10 mg per day once;
- arterial hypertension: maintenance dose - 2.5–5 mg per day.
When used in combination with thiazide diuretics, β-blockers and ACE (angiotensin converting enzyme) inhibitors, dose adjustment is not required.
Side effects
Taking Amlodipine Cardio can lead to the development of the following adverse events [> 10% - very often; (> 1% and 0.1% and 0.01% and <0.1%) - rarely; <0.01% - very rare]:
- nervous system: often - increased fatigue, dizziness, headache, drowsiness; infrequently - mood lability, paresthesia, general malaise, asthenia, hyperesthesia, peripheral neuropathy, insomnia, tremors, nervousness, anxiety, depression, unusual dreams; very rarely - increased sweating, apathy, migraine;
- cardiovascular system: often - flushing of the face, palpitations, peripheral edema (swelling of the feet and ankles); infrequently - excessive lowering of blood pressure; very rarely - development / aggravation of the course of heart failure, vasculitis, syncope, shortness of breath, orthostatic hypotension, cardiac arrhythmias (including bradycardia, atrial fibrillation and ventricular tachycardia), chest pain, myocardial infarction;
- digestive system: often - abdominal pain, nausea; infrequently - flatulence, anorexia, dyspepsia, vomiting, diarrhea or constipation, dryness of the oral mucosa, thirst; rarely - increased appetite, gingival hyperplasia; very rarely - increased activity of hepatic transaminases, hepatitis, hyperbilirubinemia, gastritis, pancreatitis, jaundice (due to cholestasis);
- genitourinary system: infrequently - painful / frequent urination, impotence, nocturia; very rarely - polyuria, dysuria, gynecomastia;
- musculoskeletal system: infrequently - arthrosis, arthralgia, myalgia, muscle cramps, back pain; rarely - myasthenia gravis;
- respiratory system: infrequently - rhinitis, shortness of breath; very rarely - cough;
- hematopoietic organs: very rarely - thrombocytopenia, leukopenia, thrombocytopenic purpura;
- bone integument: rarely - dermatitis; very rarely - xeroderma, alopecia, skin pigmentation disorders, cold sweat;
- allergic reactions: erythema multiforme, angioedema, pruritus, rash (including erythematous, maculopapular rash, urticaria);
- others: infrequently - conjunctivitis, chills, xerophthalmia, diplopia, ringing in the ears, violation of accommodation, nosebleeds, eye pain; very rarely - hyperglycemia, parosmia.
Overdose
Overdose is manifested by excessive peripheral vasodilation in combination with a pronounced and possibly prolonged decrease in blood pressure, as well as collapse and shock.
Therapy: the patient should take a horizontal position and raise the lower limbs above the level of the head. Shows gastric lavage, intake of activated carbon. Hemodialysis is ineffective.
It is necessary to maintain the function of the cardiovascular system, monitor the performance of the lungs and heart, the volume of circulating blood and urine output. In order to restore vascular tone, vasoconstrictor agents are prescribed (if the patient has no contraindications to their use); to eliminate the consequences of blockade of slow calcium channels, calcium gluconate is administered intravenously.
special instructions
During the period of therapy, it is necessary to maintain dental hygiene and be monitored by a dentist (in order to prevent soreness, hyperplasia and bleeding of the gums). Weight and sodium intake should be monitored and an appropriate diet followed.
With an increase in the dose of amlodipine in elderly patients, more careful monitoring of their condition is required, which is associated with an increase in T 1/2 and drug clearance. If hepatic function is impaired, Amlodipine Cardio is prescribed with caution, which is also associated with lengthening T 1/2.
Termination of therapy with the development of withdrawal syndrome is not accompanied, however, the abolition of Amlodipine Cardio is recommended to be carried out with a gradual dose reduction. In hypertensive crisis, the safety profile of amlodipine has not been established.
Influence on the ability to drive vehicles and complex mechanisms
In some patients, mainly at the beginning of taking Amlodipine Cardio, drowsiness, dizziness and other undesirable phenomena from the central nervous system may develop. In such cases, care must be taken when driving.
Application during pregnancy and lactation
The use of Amlodipine Cardio during pregnancy / lactation is contraindicated.
Pediatric use
Since the safety profile of Amlodipine Cardio in patients under 18 years of age has not been studied, the drug is not prescribed to this group of patients.
For violations of liver function
When prescribing Amlodipine Cardio for the condition of patients with impaired hepatic function, it is necessary to establish careful monitoring.
Use in the elderly
When prescribing Amlodipine Cardio, the condition of elderly patients must be carefully monitored.
Drug interactions
With stable angina pectoris, Amlodipine Cardio can be combined with other antianginal drugs, including prolonged / short-acting nitrates, β-blockers. For the treatment of arterial hypertension, the combined use of thiazide diuretics, α-blockers, ACE inhibitors or β-blockers is safe.
Possible combined use with non-steroidal anti-inflammatory drugs (especially with indomethacin), oral hypoglycemic agents and drugs with antibacterial action.
Other possible interactions:
- α1-blockers, antipsychotics: with combined use, an increase in the hypotensive effect of amlodipine is noted;
- diuretics (thiazide and loop), verapamil, ACE inhibitors, β-blockers and nitrates: with combined use, there is an increase in the hypotensive and antianginal effects of amlodipine;
- drugs with antiviral action (ritonavir): there is an increase in plasma concentrations of amlodipine;
- isoflurane, neuroleptics: the hypotensive effect of dihydropyridine derivatives is enhanced;
- lithium preparations: against the background of combined use, manifestations of neurotoxicity (in the form of nausea, vomiting, diarrhea, ataxia, tremor, tinnitus) may increase;
- calcium preparations: the effectiveness of amlodipine may decrease.
Analogs
Amlodipine Cardio analogs are Amlodipine, Acridipine, Amlodigamma, Amlovas, Amlorus, Amlodipine, Amlotop, Amlong, Kalchek, Corvadil, Cardilopin, Normodipin, Norvask, Stamlo, Tenox, etc.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Amlodipine Cardio
Reviews of Amlodipine Cardio are few. It is indicated that the drug has a rapid therapeutic effect, while the development of undesirable phenomena, in particular allergic reactions, is possible.
The price of Amlodipine Cardio in pharmacies
The approximate price for Amlodipine Cardio (30 tablets of 10 mg) is 77 rubles.
Amlodipine Cardio: prices in online pharmacies
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Drug name Price Pharmacy |
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Amlodipine Cardio 5 mg tablets 30 pcs. RUB 62 Buy |
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Amlodipine Cardio 10 mg tablets 30 pcs. 79 RUB Buy |
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Amlodipine Cardio 10mg tablets 30 pcs. 141 r Buy |
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!
