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 winstrol only cycle mechanism of the antihypertensive action of amlodipine is due to a direct relaxing effect on vascular smooth muscle.
Amlodipine reduces myocardial ischemia following two ways:
- Increase peripheral arterioles and thus, reduces the total peripheral resistance (afterload), the heart rate does not change substantially, resulting in lower energy consumption and myocardial oxygen demand.
- 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 koronarosnazma caused by smoking.
In patients with arterial hypertension single daily dose of Norvasc provides the reduction of blood pressure (BP) for 24 hours (as in the “lying” and “standing”). Due to the slow onset of action of amlodipine does not cause a sharp decrease 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 nitroglycerin consumption.
Use in patients with coronary heart disease (CHD)
patients with cardiovascular disease (including coronary atherosclerosis with the defeat of the vessel and to the stenosis 3 or more of the arteries and carotid atherosclerosis), myocardial infarction, percutaneous transluminal angioplasty of the coronary arteries ( TLO) or suffering from angina, Norvasc use prevents the development of thickening intima-media carotid arteries, significantly reduces mortality from cardiovascular causes, myocardial infarction, stroke, TLO. coronary artery bypass surgery, reduces the number of hospitalizations for unstable angina and progression of chronic heart failure (CHF), reduces the frequency of interventions aimed at restoring coronary blood flow.
Use in patients with heart failure
Norvasc does not increase the risk of death or complications and deaths in patients with chronic heart failure (CHF) III-IV functional class (NYHA on) on the background therapy with digoxin, diuretics and ACE inhibitors. In patients with CHF I1I-IV NYHA functional class is not in the application of ischemic etiology Norvasc there is a possibility of occurrence of pulmonary edema. Norvasc not exert any adverse effect on metabolism and lipid concentration in blood plasma.
Absorption. After oral administration of therapeutic doses of amlodipine is well absorbed, reaching peak blood concentrations 6-12 hours after administration. The absolute bioavailability of 64-80%. The volume of distribution is approximately 21 l / kg. Relationship to plasma proteins is approximately 97.5%. Ingestion not affect the absorption of amlodipine, penetrates the blood-brain barrier.
Stable equilibrium concentration in plasma is reached after 7-8 days of continuous use of amlodipine, it is metabolized in the liver to inactive metabolites; 10% of the parent drug and 60% of the metabolites excreted in urine. Excretion in breast milk is unknown. During hemodialysis is not removed. Use in renal failure patients. Tyr plasma of patients with renal failure is increased to 60 hours. Change amlodipine plasma concentrations are not correlated with the degree of renal dysfunction.
Application of the elderly. In older time required for maximum concentration of amlodipine in plasma, and its value does not differ substantially from those of younger people. In the elderly, suffer from heart failure, reducing the tendency to amlodipine clearance, which leads to an increase in the area under the winstrol only cycle concentration-time curve, and T1 / 2 of 65 hours.
- Arterial hypertension (in both monotherapy and in combination with other antihypertensive agents).
- Stable angina pectoris and vasospastic angina (Prinzmetal angina) (both in monotherapy and in combination with other antianginal drugs).
- Hypersensitivity to amlodipine digidropiridipa and other derivatives, as well as the excipients included in the preparation.
- Severe hypotension
WITH CARE prescribed to patients with liver failure, heart failure of ischemic etiology is not class III-IV, aortic stenosis, acute myocardial infarction (and for 1 month. After him), at the age of 18 years (effectiveness and safety have not been established for sure).
As for the appointment of other BCCI should be careful while taking amlodipine patients with sick sinus syndrome, mitral stenosis, hypertrophic obstructive cardiomyopathy, hypotension.
Pregnancy and lactation
The safety of Norvasc in pregnancy and lactation has not been established, therefore use during pregnancy is possible only when the benefit to the mother outweighs the risk to the fetus and newborn. For the period of lactation should stop taking the drug either, or breast-feeding (data on amlodipine excretion in breast milk are not available).
DOSAGE AND ADMINISTRATION
Inside, once a day, washing down the necessary volume of water (100 ml).
When hypertension and angina the usual initial dose is 5 mg, depending on the individual response of the patient can be increased up to a maximum – 10 mg.
Application of the elderly. It is recommended to use in normal doses, dose modification is not required.
Use in patients with impaired liver function. In spite of the fact that T1 / 2, Norvasc, like all BCCI is increased in patients with this disorder, any dosage change winstrol only cycle the drug in patients with impaired liver function is not usually required (see. Section “Special instructions”).
Use in renal impairment. Recommended for use in normal doses, but must take into account a possible slight increase in T1 / 2. Changing the metering mode Norvasc, while the use of thiazide diuretics, beta-blockers or ACE inhibitors is not required.
Further, under the frequency of adverse reactions is understood: frequent (> 1%), infrequent (<1%), rare (<0.1%), very rare (<0.01%).
Cardiovascular system: peripheral edema (ankles and feet), palpitations, not often – an excessive fall in blood pressure, orthostatic hypotension, vasculitis; rarely – the development or exacerbation of congestive heart failure; very rarely – cardiac arrhythmias (including bradycardia, ventricular tachycardia and atrial fibrillation), heart attack, chest pain, migraine.
From the musculoskeletal system: rarely – arthralgia, muscle cramps, myalgia, back pain, arthritis, rarely – myasthenia gravis.
Central and peripheral nervous system: sensation of heat and “tides” of blood to the skin of the face, fatigue, dizziness, headache, drowsiness, rarely – malaise, fainting, sweating, fatigue, hypoesthesia, paresthesia, peripheral neuropathy, tremor, insomnia, mood lability, abnormal dreams, anxiety, depression, anxiety; rarely – seizures, lethargy, agitation; very rarely – ataxia, amnesia.
Digestive tract: abdominal pain, nausea, rarely – vomiting, changes in bowel movement modes (including constipation, flatulence), indigestion, diarrhea, anorexia, dry mouth, thirst, rarely – gingival hyperplasia, increased appetite, very rarely – gastritis, pancreatitis, hyperbilirubinemia, jaundice (usually cholestatic), increased activity of “liver” transaminases, hepatitis.
Hemopoietic system: very rarely – thrombocytopenic purpura, leukopenia, thrombocytopenia.
Metabolic disorders: very rarely – hyperglycemia.
Respiratory system: rarely – dyspnea, rhinitis, very rarely – cough.
Genito-urinary system: rarely – frequent urination, painful urination, nocturia, impotence, rarely – dysuria, polyuria.
Allergic reactions: rarely – itching, rash, very rarely – angioneurotic edema, erythema multiforme, urticaria.
Other: rare – alopecia, “ringing” in the ears, gynecomastia, increase / decrease in body weight, blurred vision, diplopia, disturbance of accommodation, xerophthalmia, conjunctivitis, eye pain, taste perversion, chills, nasal bleeding, rarely – dermatitis; very rarely – parosmiya, dermatoxerasia, “cold” sweat violation of skin pigmentation.