Amlodipine Cardio, 30 pcs., 5 mg, tablets
Amlodipine Cardio 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, long-acting nitrates, beta-blockers or short-acting nitrates,
Amlodipine Cardio can be used simultaneously with non-steroidal anti-inflammatory drugs (NSAIDs) (especially indomethacin), antibacterial agents and oral hypoglycemic agents.
It is possible to enhance the antianginal and hypotensive effect of BMCC when used together with thiazide and loop diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates, as well as enhance their hypotensive effect when used together with alpha 1-blockers, antipsychotics.
Although negative inotropic effects have generally not been observed in amlodipine studies, some CBMCs may enhance the negative inotropic effects of antiarrhythmic drugs that can prolong the QT interval (eg, amiodarone and quinidine). A single dose of 100 mg of sildenafil in patients with essential hypertension does not affect the pharmacokinetic parameters 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.
Ethanol (drinks containing alcohol): amlodipine with single and repeated use in a dose of 10 mg does not affect the pharmacokinetics of ethanol. Antiviral agents (ritonavir) increase plasma concentrations of BMCC, incl. amlodipine.
Neuroleptics and isoflurane - enhance the hypotensive effect of dihydropyridine derivatives.
Calcium supplements may reduce the effect of BMCC.
When amlodipine is used together with lithium preparations, it is possible to increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Amlodipine does not change the pharmacokinetics of cyclosporine.
Does not affect the serum concentration of digoxin and its renal clearance.
Does not have a significant effect on the effect of warfarin (prothrombin time).
Cimetidine does not affect the pharmacokinetics of amlodipine.
In in vitro studies, amlodipine does not affect the binding of digoxin, phenytoin, warfarin and indomethacin to blood proteins.
Grapefruit juice: simultaneous single administration of 240 mg of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine.
Amlodipine Cardio tablet 10 mg pack cont cell/pack card x30
ATX code: C08CA01 Registration number: PN 003062/01
Dosage form: tablets
Composition: for 1 tablet:
active substance: amlodipine besilate, in terms of amlodipine 5 mg or 10 mg
excipients: hypromellose (hydroxypropyl methylcellulose), potato starch, lactose (milk sugar), magnesium stearate (magnesium stearate), talc
Description: tablets of white or almost white color, with a dosage of 5 mg - oblong in shape with rounded edges with a score, with a dosage of 10 mg - flat-cylindrical in shape with a chamfer and a score.
Pharmacotherapeutic group: blocker of “slow” calcium channels.
Pharmacodynamics: The dihydropyridine derivative is a second generation blocker of “slow” calcium channels (SCCC), has an antianginal and hypotensive effect. By binding to the S6 segment of the III and IY domains of the alpha 1 subunit of the L-type calcium channel.
The antianginal effect is due to the expansion of coronary and peripheral arteries and arterioles: during angina pectoris, it reduces the severity of myocardial ischemia, expanding peripheral arterioles, reduces total peripheral vascular resistance (TPVR), reduces preload on the heart, and reduces myocardial oxygen demand. Expands coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases the supply of oxygen to the myocardium (especially with vasospastic angina), and prevents the development of spasm of the coronary arteries (including those caused by smoking). In patients with angina pectoris, a single daily dose of amlodipine increases the time of physical activity, delays the development of an attack of angina and ST segment depression (by 1 mm) during exercise, reduces the frequency of angina attacks and the consumption of nitroglycerin tablets and other nitrates. It has a long-term dose-dependent hypotensive effect.
The hypotensive effect is due to a direct vasodilating effect on vascular smooth muscle. For arterial hypertension, a single dose provides a clinically significant reduction in blood pressure (BP) over 24 hours (in the patient’s “lying” and “standing” position). Orthostatic hypotension when prescribing Omelar® Cardio is quite rare. Reduces the degree of left ventricular myocardial hypertrophy. It has no effect on myocardial contractility and conductivity, does not cause a reflex increase in heart rate (HR), 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 metabolism and plasma lipid concentrations and can be used in the treatment of patients with concomitant bronchial asthma, diabetes mellitus and gout. A significant decrease in blood pressure is observed after 6-10 hours, the duration of the effect is 24 hours.
Pharmacokinetics: After oral administration, amlodipine is slowly absorbed from the gastrointestinal tract (GIT). The average absolute bioavailability is 64%, the maximum concentration (Cmax) in the blood serum is observed after 6-9 hours. Steady-state serum concentrations (Css) are achieved after 7-8 days of therapy.
Food intake does not affect the absorption of amlodipine. The mean volume of distribution is 21 L/kg body weight, indicating that most of the drug is in the tissues and a relatively smaller portion is in the blood. Most of the drug in the blood (95%) binds to blood plasma proteins. Amlodipine undergoes slow but active metabolism in the liver with no significant first-pass effect. Metabolites do not have significant pharmacological activity.
After a single oral dose, the half-life (T1/2) varies from 31 to 48 hours; with repeated administration, T1/2 is approximately 45 hours. About 60% of the dose taken orally is excreted by the kidneys mainly in the form of metabolites, 10% - unchanged, 20-25% - through the intestines, as well as in breast milk. The total clearance of amlodipine is 0.116 ml/s/kg (7 ml/min/kg, 0.42 l/h/kg).
In elderly patients (over 65 years of age), the elimination of amlodipine is slower (T1/2 - 65 hours) compared to young patients, but this difference is not clinically significant. Prolongation of T1/2 in patients with liver failure suggests that with long-term administration, the accumulation of the drug in the body will be higher (T1/2 - up to 60 hours).
Renal failure does not significantly affect the kinetics of amlodipine. The drug penetrates the blood-brain barrier. It is not removed by hemodialysis.
Indications for use:
● Arterial hypertension (monotherapy or in combination with other antihypertensive drugs).
● Stable exertional angina and vasospastic angina (Prinzmetal's angina) (monotherapy or in combination with other antianginal drugs).
Contraindications:
● Hypersensitivity to amlodipine, dihydropyridine derivatives and other components of the drug,
● Severe arterial hypotension (systolic blood pressure less than 90 mm Hg),
● Collapse, cardiogenic shock,
● Unstable angina (with the exception of Prinzmetal angina),
● Clinically significant aortic stenosis,
● Pregnancy and lactation,
● Age under 18 years (efficacy and safety have not been studied),
● Lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
With caution: Liver dysfunction, sick sinus syndrome (SSNS) (severe bradycardia, tachycardia), chronic heart failure of non-ischemic etiology of functional class III-IV according to the NYHA classification, arterial hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy (HOCM) , acute myocardial infarction (and within 1 month after myocardial infarction), old age.
Pregnancy and lactation: The safety of amlodipine during pregnancy and lactation has not been established, therefore Omelar® Cardio should not be prescribed during pregnancy and lactation.
Method of administration and dosage: Orally, the initial dose for the treatment of arterial hypertension and angina pectoris is 5 mg of the drug once a day. The maximum daily dose is 10 mg once. For arterial hypertension, the maintenance dose can be 2.5 - 5 mg (1/2 tablet of 5 mg - 1 tablet of 5 mg) per day.
In elderly patients, T1/2 of amlodipine may increase and creatinine clearance (CC) may decrease. No dose changes are required, but patients should be monitored more closely.
No dose change is required when administered concomitantly with thiazide diuretics, beta-blockers and angiotensin-converting enzyme (ACE) inhibitors.
No dose changes are required in patients with renal failure.
Side effects: World Health Organization (WHO) side effect frequency classification:
very often >1/10
often > 1/100 and infrequently > 1/1000 and rarely >1/10000 and very rarely From the cardiovascular system: often - palpitations, peripheral edema (swelling of the ankles and feet), "flushes" of blood to the facial skin, infrequently - excessive decrease in blood pressure, very rarely - syncope, shortness of breath, vasculitis, orthostatic hypotension, development or worsening of heart failure, heart rhythm disturbances (including bradycardia, ventricular tachycardia and atrial fibrillation), myocardial infarction, chest pain.
From the central and peripheral nervous system: often - headache, dizziness, fatigue, drowsiness, infrequently - asthenia, general malaise, hyperesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability, unusual dreams, nervousness, depression, anxiety, very rarely - migraine, increased sweating, apathy.
From the digestive system: often - nausea, abdominal pain, infrequently - 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.
From the hematopoietic organs: very rarely - thrombocytopenic purpura, leukopenia, thrombocytopenia.
From the genitourinary system: infrequently - frequent urination, painful urination, nocturia, impotence, very rarely - dysuria, polyuria, gynecomastia.
From the respiratory system: infrequently - shortness of breath, rhinitis, very rarely - cough.
From the skin: rarely – dermatitis, very rarely – alopecia, xeroderma, “cold” sweat, skin pigmentation disorder.
Allergic reactions: skin itching, rash (including erythematous, maculopapular rash, urticaria), angioedema, erythema multiforme.
From the musculoskeletal system: infrequently - muscle cramps, myalgia, arthralgia, back pain, arthrosis, rarely - myasthenia gravis.
Other: infrequently - tinnitus, diplopia, accommodation disturbance, xerophthalmia, conjunctivitis, eye pain, chills, nosebleeds, very rarely - parosmia, hyperglycemia.
Overdose: Symptoms: excessive peripheral vasodilation with a pronounced and possibly prolonged decrease in blood pressure, collapse, shock.
Treatment: the patient should take a horizontal position with the lower limbs raised above the level of the head,
Gastric lavage, administration of activated charcoal, maintaining the function of the cardiovascular system, monitoring indicators of heart and lung function, monitoring circulating blood volume 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 blockade of slow calcium channels - intravenous administration of calcium gluconate. Hemodialysis is ineffective.
Interactions with other drugs: Omelar® Cardio can be safely used for the treatment of arterial 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, long-acting nitrates, beta-blockers or short-acting nitrates.
Omelar® Cardio can be used simultaneously with non-steroidal anti-inflammatory drugs (NSAIDs) (especially indomethacin), antibacterial agents and oral hypoglycemic agents.
It is possible to enhance the antianginal and hypotensive effect of BMCC when used together with thiazide and loop diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates, as well as enhance their hypotensive effect when used together with alpha1-blockers, antipsychotics.
Although negative inotropic effects have generally not been observed in amlodipine studies, some CBMCs may enhance the negative inotropic effects of antiarrhythmic drugs that can prolong the QT interval (eg, amiodarone and quinidine).
A single dose of 100 mg of sildenafil in patients with essential hypertension does not affect the pharmacokinetic parameters 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.
Ethanol (drinks containing alcohol): amlodipine with single and repeated use in a dose of 10 mg does not affect the pharmacokinetics of ethanol.
Antiviral agents (ritonavir) increase plasma concentrations of BMCC, incl. amlodipine.
Neuroleptics and isoflurane - enhance the hypotensive effect of dihydropyridine derivatives.
Calcium supplements may reduce the effect of BMCC.
When amlodipine is used together with lithium preparations, it is possible to increase the manifestation of neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Amlodipine does not change the pharmacokinetics of cyclosporine.
Does not affect the serum concentration of digoxin and its renal clearance.
Does not have a significant effect on the effect of warfarin (prothrombin time).
Cimetidine does not affect the pharmacokinetics of amlodipine.
In in vitro studies, amlodipine does not affect the binding of digoxin, phenytoin, warfarin and indomethacin to blood proteins.
Grapefruit juice: simultaneous single administration of 240 mg of grapefruit juice and 10 mg of amlodipine orally is not accompanied by a significant change in the pharmacokinetics of amlodipine.
Special instructions: During treatment with Omelar® Cardio, 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 pain, bleeding and gum hyperplasia).
In elderly patients, T1/2 and drug clearance may be prolonged. No dose changes are required for elderly patients; when increasing the dose, more careful monitoring of patients is necessary.
If liver function is impaired, T1/2 of the drug may also be prolonged. Therefore, Omelar® Cardio should be prescribed to such patients with caution. Despite the fact that discontinuation of Omelar® Cardio is not accompanied by the development of withdrawal syndrome, it is advisable to discontinue treatment by gradually reducing the dose of the drug.
The effectiveness and safety of the drug in hypertensive crisis have not been established.
Impact on the ability to drive a car and other complex mechanisms
There have been no reports of the effects of Omelar® Cardio on driving or operating machinery. However, some patients, mainly at the beginning of treatment, may experience drowsiness and dizziness and other central nervous system side effects. If they occur, the patient must take special precautions when driving vehicles and working with complex mechanisms.
Release form: Tablets of 5 mg and 10 mg.
7, 10, 14 or 20 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.
1, 2, 3, 4 or 5 blister packs along with instructions for use are placed in a cardboard pack.
Storage conditions: List B. In a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children.
Shelf life: 2 years. Do not use after the expiration date stated on the packaging.
Conditions for dispensing from pharmacies: By prescription.
Comparison of the effectiveness of Amlodipine and Amlodipine cardia
The effectiveness of Amlodipine is quite similar to Amlodipine cardio - this means that the ability of the drug substance to provide the maximum possible effect is similar.
For example, if the therapeutic effect of Amlodipine is more pronounced, then using Amlodipine cardia even in large doses will not achieve this effect.
Also, the speed of therapy is an indicator of the speed of therapeutic action for Amlodipine and Amlodipine cardia are approximately the same. And bioavailability, that is, the amount of a drug reaching its site of action in the body, is similar. The higher the bioavailability, the less it will be lost during absorption and use by the body.
Comparison of side effects of Amlodipine and Amlodipine cardia
Side effects or adverse events are any adverse medical event that occurs in a subject after administration of a drug.
Amlodipine has more adverse events than Amlodipine cardia. This implies that the frequency of their occurrence is low with Amlodipine, and the frequency with Amlodipine is low. Frequency of occurrence is an indicator of how many cases of an undesirable effect from treatment are possible and registered. The undesirable effect on the body, the strength of influence and the toxic effect of drugs are different: how quickly the body recovers after taking it and whether it recovers at all. When using Amlodipine, the body's ability to recover faster is higher than that of Amlodipine cardia.
Comparison of the safety of Amlodipine and Amlodipine cardia
The safety of a drug includes many factors.
At the same time, in Amlodipine it is quite similar to Amlodipine cardio. It is important where the drug is metabolized: drugs are excreted from the body either unchanged or in the form of products of their biochemical transformations. Metabolism occurs spontaneously, but most often involves major organs such as the liver, kidneys, lungs, skin, brain and others. When assessing the metabolism of Amlodipine, as well as Amlodipine Cardia, we look at which organ is the metabolizing organ and how critical the effect on it is.
The risk-benefit ratio is when the prescription of a drug is undesirable, but justified under certain conditions and circumstances, with the obligatory observance of caution in use. At the same time, Amlodipine does not have any risks when used, just like Amlodipine cardia.
Also, when calculating safety, it is taken into account whether only allergic reactions occur or possible dysfunction of the main organs. In other matters, as well as the reversibility of the consequences of using Amlodipine and Amlodipine cardia.
Comparison of addiction between Amlodipine and Amlodipine cardia
Like safety, addiction also involves many factors that must be considered when evaluating a drug.
So, the totality of the values of such parameters as “syndrome o” in Amlodipine is quite similar to the similar values in Amlodipine cardia. Withdrawal syndrome is a pathological condition that occurs after the cessation of intake of addictive or dependent substances into the body. And resistance is understood as initial immunity to a drug; in this it differs from addiction, when immunity to a drug develops over a certain period of time. The presence of resistance can only be stated if an attempt has been made to increase the dose of the drug to the maximum possible. At the same time, Amlodipine has a fairly low incidence of “syndrome”, just like Amlodipine cardia.
