Antianginal effect is due to the expansion of the coronary and peripheral arteries and arterioles: angina reduces the severity of myocardial ischemia; expanding peripheral arterioles, reducing the total peripheral vascular resistance deca durabolin side effects , reduces preload on the heart, reducing myocardial oxygen demand. Dilates coronary arteries and arterioles in the unaltered and ischemic myocardial areas, increases the supply of oxygen to the myocardium (especially in vasospastic angina); It prevents the development of coronary artery spasm (including those caused by smoking). In patients with angina single daily dose of amlodipine increases the run-time physical activity, retards the development of angina and ST segment depression (1 mm) during its execution, reduces the frequency of angina attacks and consumption of nitroglycerin tablets and other nitrates. It has a long dose-dependent hypotensive effect.
The antihypertensive effect is due to the direct vasodilating effect on vascular smooth muscle. When hypertension single dose provides a clinically significant reduction in blood pressure (BP) for 24 hours (in the position of the patient “lying” and “standing”). Orthostatic hypotension when administering the drug Omelar ®Cardio is quite rare. It reduces the degree of left ventricular hypertrophy. No effect on myocardial contractility and conductivity, does not cause reflex increase in heart rate (HR), inhibits platelet aggregation, increases glomerular filtration rate, has a weak natriuretic effect.
In diabetic nephropathy does not increase the severity of microalbuminuria.
It does not have any adverse effect on the metabolism and the concentration of plasma lipids and can be used in the treatment of patients with concomitant asthma, diabetes and gout. Significant blood pressure reduction is observed in 6-10 hours, the duration of effect of 24 hours.
Following oral amlodipine slowly absorbed from the gastrointestinal tract (GIT). The mean absolute bioavailability of 64%, the maximum concentration (C max ) in the blood serum is observed after 6-9 hours.Equilibrium serum concentrations (Css) are achieved after 7-8 days of treatment.
Ingestion of amlodipine does not affect the absorption. The mean volume of distribution of 21 l / kg body weight, indicating that most of the drug is in the tissues and relatively smaller – in the blood. Most of the drug present in the blood (95%), bind to plasma proteins. Amlodipine undergoes slow but active metabolism in the liver in the absence of a significant effect of “first pass”. Metabolites not possess significant pharmacological activity.
In elderly patients (65 years) amlodipine delayed excretion (T1 / 2 – 65 hr.) Compared to younger patients, but the difference has no clinical significance. Elongation T1 / 2 in patients with liver disease suggests that long-term administration with drug accumulation in the body is higher (T1 / 2 – 60 h).
Renal failure has no significant effect on the kinetics of amlodipine. The drug crosses the blood-brain barrier. When hemodialysis is not removed.
- Arterial deca durabolin side effects hypertension (monotherapy or in combination with other antihypertensive agents).
- Stable angina and vasospastic angina (Prinzmetal angina) (monotherapy or in combination with other antianginal drugs).
- Hypersensitivity to amlodipine, dihydropyridine derivatives and other ingredients;
- Severe hypotension (systolic blood pressure less than 90 mm Hg);
- The collapse, cardiogenic shock;
- Unstable angina (except Prinzmetal’s angina);
- Clinically significant aortic stenosis;
- Pregnancy and lactation;
- Age 18 years (effectiveness and safety have been studied);
- Lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
the liver, sick sinus syndrome (SSS) (bradycardia, tachycardia), chronic heart failure, non-ischemic etiology III-IV NYHA functional class classification, hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy (GOKMP) acute myocardial infarction (and for 1 month after myocardial infarction), advanced age.
Pregnancy and lactation
The safety of amlodipine during pregnancy and lactation has not been established, so Cardio should not be administered during pregnancy and lactation.
Dosing and Administration
Inside, the initial dose for treatment of hypertension and angina is 5 mg once daily. The maximum daily dose – 10 mg once daily. When hypertension maintenance dose may be 2.5 – 5 mg (2.1 mg tablet 5 – 1 5 mg tablet) daily.
Elderly patients may increase the T1 / 2 and amlodipine decrease in creatinine clearance (CC). Changes in dose is not required, but must be more careful monitoring of patients.
Do not you want to change the dose while the appointment with thiazide diuretics, beta-blockers and angiotensin-converting enzyme (ACE).
Not required dose modification in patients with renal insufficiency.
Since the cardiovascular system: often – palpitations, peripheral edema (swelling of the ankles and feet), “tides” of blood to the skin of the face; infrequently – an excessive fall in blood pressure; very rarely – syncope, dyspnoea, vasculitis, orthostatic hypotension, development or exacerbation of a heart failure, cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), heart attack, chest pain.
On the part of the central and peripheral nervous system: often – headache, dizziness, fatigue, drowsiness; -asteniya infrequently, malaise, hyperesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability, abnormal dreams, anxiety, depression, anxiety, very rarely – headache, increased sweating, lethargy.
From the digestive system: often – nausea, stomach pain; rarely – vomiting, constipation or diarrhea, flatulence, dyspepsia, anorexia, dryness of the oral mucosa, thirst; rarely – gingival hyperplasia, increased appetite; very rarely – pancreatitis, gastritis, jaundice (caused by cholestasis), hyperbilirubinemia, increased activity of “liver” transaminases, hepatitis.
From the side of hematopoiesis: rarely – trombotsitotsenicheskaya purpura, leukopenia, thrombocytopenia.
With the deca durabolin side effects genitourinary system: Infrequent – frequent urination, painful urination, nocturia, impotence, rarely – dysuria, polyuria, gynecomastia.
With the respiratory system: rarely – dyspnea, rhinitis, rarely -kashel.
For the skin: rarely – dermatitis, it is very rare – alopecia, dermatoxerasia, “cold” sweat violation of skin pigmentation.
Allergic reactions: itching, rash (including erythematous, maculopapular rash, urticaria), angioedema, erythema multiforme.
From the musculoskeletal system: rarely – muscle cramps, myalgia, arthralgia, back pain, arthritis, rarely – myasthenia gravis.
Other: rarely – ringing in the ears, diplopia, disturbance of accommodation, xerophthalmia, conjunctivitis, eye pain, fever, epistaxis, very rarely – parosmiya, hyperglycemia.
Overdose Symptoms: excessive peripheral vasodilation with marked and probably prolonged decrease in blood pressure, collapse, shock.
Treatment: The patient should take a horizontal position with raised above head level lower limbs;
Gastric lavage, the appointment of activated carbon, the maintenance function of the cardiovascular system, the control parameters of the heart and lung function, control of blood volume and diuresis. To restore vascular tone – use of a vasoconstrictor (in the absence of contraindications to their use); in order to eliminate the effects of calcium channel blockade slow – intravenous calcium gluconate.Hemodialysis is ineffective.
Interactions with other drugs
Omelar ® Cardio can be safely used for the treatment of hypertension with thiazide diuretics, alpha-blockers, beta-adrёnoblokatorami or ACE inhibitors. Patients with stable angina pectoris drug can be combined with other antianginal drugs, such as long-acting nitrates, beta-blockers or short-acting nitrates.
Omelar ® Cardio can be used simultaneously with nonsteroidal anti-inflammatory drugs (NSAIDs) (especially indomethacin), antibacterial agents and hypoglycemic agents for oral administration.
Perhaps strengthening anti-anginal and anti-hypertensive action BCCI when combined with thiazide and “loop” diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates, as well as strengthening their hypotensive effect when combined with alpha 1-blockers, neuroleptics.
Although the study of amlodipine negative inotropic action is not usually observed, however, some BCCI may increase the severity of the negative inotropic effects of antiarrhythmic agents capable of causing an elongation interval QT (e.g., amiodarone and quinidine).
A single dose of 100 mg of sildenafil in patients with essential hypertension has no impact on the pharmacokinetic parameters of amlodipine.
Re-administration of amlodipine 10 mg and atorvastatin 80 mg is not accompanied by significant changes in pharmacokinetic parameters of atorvastatin.
Ethanol (drinks containing alcohol) with amlodipine single and repeated administration of 10 mg did not affect the pharmacokinetics of ethanol.
Antiviral drugs (ritonavir) increase the plasma concentrations of BCCI, including amlodipine.
Antipsychotics and isoflurane – strengthen hypotensive action dihydropyridine derivatives.
Calcium can reduce the effect of BCCI.
When combined with amlodipine drugs lithium may increase neurotoxicity (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Amlodipine does not alter the pharmacokinetics of cyclosporin.
It has no effect on serum digoxin concentration and its renal clearance.
It does not have a deca durabolin side effects significant impact on the effect of warfarin (prothrombin time).
Cimetidine does not affect the pharmacokinetics of amlodipine.
In in vitro studies of amlodipine does not affect the plasma protein binding of digoxin, phenytoin, warfarin and indomethacin.
Grapefruit Juice: simultaneous single dose of 240 mg of grapefruit juice and 10mg amlodipine inside is not accompanied by a significant change in the pharmacokinetics of amlodipine.
During treatment with Omelar ® Cardio is necessary to control body weight and sodium intake, the appointment of an appropriate diet. It is necessary to maintain dental hygiene and seeing a dentist (to prevent soreness, bleeding and gingival hyperplasia).
Older patients may lengthen the T1 / 2 and the clearance of the drug. Changes dose for elderly patients is not required; by increasing the dose must be more careful monitoring of patients.
If abnormal liver function may also lengthen the T1 / 2 of the drug. Therefore, such patientsshould be administered with caution. Despite the fact that the discontinuation of the drug Omelar Cardio is not accompanied by the development of the syndrome of “cancellation”, discontinuation of treatment it is desirable to gradually reducing the dose of the drug.
The efficacy and safety of the drug for hypertensive crisis has not been established.
Effects on ability to drive a car and other complex mechanisms
There were no reports on the effect to drive vehicles or operate machinery. However, some patients, especially at the beginning of treatment, can occur drowsiness and dizziness and other side effects of CNS. If this happens, the patient must take special precautions pry driving and working with complex mechanisms.