Communicating with the dihydropyridine receptor blocking “slow” calcium channels inhibits the transmembrane transfer of calcium into the cells of smooth muscles of the heart and blood vessels (mainly – in the vascular smooth muscle cells than cardiac myocytes). It has hypotensive and antianginal effects. The mechanism buy equipoise of the antihypertensive action of amlodipine is due to a direct relaxing effect on vascular smooth muscle. Amlodipine reduces myocardial ischemia following two ways: 1. Extends arterioles and thus, reduces the total peripheral resistance (afterload), the heart rate does not change substantially, resulting in lower energy consumption and myocardial . It extends the coronary and peripheral arteries and arterioles both in normal and in ischemic areas of the myocardium, which increases the supply of oxygen to the myocardium in patients with vasospastic angina (Prinzmetal angina) and prevents the development of coronary spasm induced by smoking. Patients with hypertension single daily dose Kalcheka ® provides reduction of blood pressure (BP) for 24 hours (as in the position of “lying” and “standing”). Due to the slow onset of action of amlodipine does not cause a sharp decrease buy equipoise in blood pressure. In patients with angina single daily dose increases the run-time physical activity, retards the development of the next angina and ST segment depression (1 mm) on the background of physical activity, reduces the frequency of angina attacks and consumption of nitroglycerin patients with cardiovascular disease (including coronary atherosclerosis with the defeat of the vessel and to the stenosis 3 or more of the arteries and atherosclerosis of the carotid artery), myocardial infarction, percutaneous transluminal angioplasty of the coronary arteries .
After oral administration of amlodipine slowly absorbed (about 90%) from the gastrointestinal tract. The absolute bioavailability of 64-80%, the maximum concentration in serum is observed after 6-9 hours.The equilibrium concentrations are achieved after 7-8 days of drug therapy. Ingestion of amlodipine does not affect the absorption. The mean volume of distribution of 21 l / kg of body weight, indicating that most of the drug remain in the tissues and relatively smaller -. Blood
Most of the drug present in the blood (97%), bind to plasma proteins.
– Hypersensitivity to amlodnpinu and / or other components of the drug, as well as to other dihydropyridine derivatives;
– severe hypotension buy equipoise (systolic blood pressure less than 90 mm ??Hg),
– unstable angina (except Prinzmetal’s angina)
– pronounced stenosis aorta
– the age of 18 years (effectiveness and safety have been established).
With caution: liver dysfunction, sick sinus syndrome (bradycardia, tachycardia), chronic heart failure, non-ischemic etiology (III-IV functional class NYHA classification), hypotension, aortic stenosis, mitral stenosis, hypertrophic obstructive cardiomyopathy, acute myocardial infarction (and for 1 month after), advanced age.
Pregnancy and lactation
The safety of amlodipine in pregnancy has not been established, therefore use during pregnancy is possible only when the benefit to the mother outweighs risk to the fetus.
There is no evidence of amlodipine buy equipoise excretion in breast milk.
However, it is known that other BCCI – dihydropyridine derivatives are excreted in breast milk. If necessary, amlodipine appointment during lactation should decide the issue of termination of breastfeeding.
Dosing and Administration
Inside, the initial dose for treatment of hypertension and angina is 5 mg 1 time per day. The dose may be as much as possible to be increased to 10 mg once a day.
When hypertension maintenance dose may be 5 mg daily.
Do not need to change the dose while the appointment with thiazide diuretics, beta-blockers or angiotensin-converting enzyme (ACE).
Not required dose modification in patients with renal insufficiency.
in patients with impaired hepatic function dose adjustment is usually not required.
in elderly patients, it is recommended to use in high therapeutic doses, dose adjustment is required.
Side effect On the part of the cardiovascular system: heart rate, marked reduction in blood pressure, peripheral edema (swelling of the ankles and feet), rarely – a violation of cardiac rhythm (bradycardia, ventricular tachycardia, atrial flutter), heart attack, chest pain, orthostatic hypotension, vasculitis, very rare – development or exacerbation of congestive heart failure, arrythmia, migraine. On the part of the central nervous system: headache, dizziness, fatigue, heat sensation and “tides” of blood to the skin of the face, drowsiness, mood changes, seizures, rare – loss consciousness, hypoesthesia, nervousness, paresthesia, peripheral neuropathy, tremor, vertigo, fatigue, malaise, syncope, insomnia, emotional lability, depression, anxiety, abnormal dreams, very rarely – ataxia, apathy, agitation, amnesia. From the digestive system: nausea , vomiting, epigastric pain, rarely – increased activity of “liver” transaminases, hyperbilirubinemia, jaundice (caused by cholestasis), pancreatitis, dry mucous membranes of the mouth, thirst, hepatitis, flatulence, gingival hyperplasia, constipation, diarrhea, anorexia, rarely – gastritis, increased appetite. From the side of hematopoiesis: rarely – thrombocytopenic purpura, leukopenia, thrombocytopenia. The respiratory system: dyspnea, rhinitis, very rarely – cough. With the genitourinary system: rare – pollakiuria, tenesmus, nocturia, sexual dysfunction (including reduced potency); very rarely – dysuria, polyuria. For the skin: very rarely – dermatoxerasia, dermatitis, purpura, violation of skin pigmentation. Allergic reactions: itching, rash (including erythematous, maculopapular rash, urticaria), angioedema, erythema multiforme. From the musculoskeletal system: rarely – arthralgia, muscle cramps, arthritis, back pain, myalgia (with prolonged use); very rarely – myasthenia gravis. The other: seldom – gynecomastia, ginerurikemiya, increase / decrease in body weight, hyperglycemia, impaired vision, diplopia, conjunctivitis, eye pain, tinnitus, dyspnea, epistaxis, increased sweating; very rarely – a cold clammy sweat, parosmiya, taste disturbance, disturbance of accommodation, xerophthalmia.
Overdose Symptoms: marked reduction of blood pressure, tachycardia, excessive peripheral vasodilatation (risk of severe and persistent hypotension, including shock development). Treatment: gastric lavage, the appointment of activated carbon (especially in the first 2 hours after the overdose), the maintenance of cardiovascular function -sosudistoy system control parameters of the heart and lung function, elevated position limbs, control of blood volume and diuresis. To restore vascular tone – use of a vasoconstrictor (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade – intravenous calcium gluconate. Hemodialysis is ineffective.
Interaction with other medicinal products
can be expected that inhibitors of microsomal liver enzymes will increase plasma amlodipine concentrations, increasing the risk of side effects, and inducers of microsomal liver enzymes -. Reduce
Unlike other BCCI not observed clinically significant interactions with non-steroidal anti-inflammatory drugs, especially with indomethacin.
Thiazide and “loop” diuretics, beta-blockers, verapamil, ACE and nitrate inhibitors increase antianginal and antihypertensive effect of amlodipine.
Amiodarone, quinidine, means for inhalation anesthesia (derivatives of hydrocarbons), alpha 1-blockers, antipsychotic drugs (neuroleptics) and BCCI may enhance the hypotensive effect.
amlodipine has no effect on the pharmacokinetic parameters of digoxin and warfarin.
Cimetidine: while the use of amlodipine with cimetidine pharmacokinetics of amlodipine is not changed.
when combined amlodipine with drugs lithium may increase manifestations of neurotoxicity (nausea, vomiting, diarrhea, . ataxia, tremor, tinnitus)
calcium supplementation may reduce the effect of BCCI.
Antiviral drugs (ritonavir) increase the plasma concentrations of BCCI, including amlodipine.
Isoflurane – strengthen hypotensive action dihydropyridine derivatives.
in a joint application BCCI with drugs lithium may increase neurotoxicity.
Re-administration of amlodipine 10 mg and atorvastatin 80 mg is not accompanied by a significant change in the pharmacokinetics of atorvastatin.
Simultaneous administration of 240 ml greynfrutovogo juice and 10mg amlodipine is not accompanied by significant changes in the pharmacokinetics of amlodipine.
Co-administration of 100 mg of sildenafil in patients with essential hypertension has no impact on the pharmacokinetic parameters of amlodipine.
During treatment requires monitoring of body weight and sodium intake, the appointment of an appropriate diet.
It is necessary to maintain dental hygiene and frequent visits to the dentist (to prevent soreness, bleeding and gingival hyperplasia).
The dosage regimen for elderly patients is the same as for patients other age groups. By increasing the dose should be carefully monitored for elderly patients.
Despite the lack of BCCI “cancellation” syndrome, before stopping treatment recommended a gradual reduction in dose.
Amlodipine has no effect on the plasma concentrations of potassium ions, glucose, triglycerides, total cholesterol, low density lipoprotein, uric acid , creatinine, uric acid and nitrogen.
patients with low body weight, patients of small stature, and in patients with severe impaired liver function may need a lower dose.
Efficacy and safety of the drug Kalchek ® has not been established for hypertensive crisis.
Effects on ability to drive vehicles and mechanisms
During treatment caution should be exercised when driving and occupation of other activities that require concentration and speed of psychomotor reactions, because of the possibility of dizziness and drowsiness.
of 10 or 14 tablets in blisters (blister) aluminum foil and PVC film. 2 blisters containing 14 tablets, or 3 blisters containing 10 tablets in cardboard pack, complete with instructions for use. Buy muscle labs usa online