The conductivity and contractility of vascular smooth muscle is inhibited by affecting the calcium channels of cell membranes.
Due to the high selectivity to smooth muscle of the arterioles, felodipine in therapeutic doses has no negative inotropic effect on cardiac parabolan contractility or conductivity.
felodipine relaxes airway smooth muscle.
it is shown that felodipine has little effect on the motility of the gastrointestinal tract. Felodipine for prolonged use has no clinically significant effect on the blood lipids. In patients with type 2 diabetes when using felodipine within 6 months no clinically significant effect on metabolic processes (NA1s).
Can also be used in patients with impaired left ventricular function who receive standard therapy Felodipine, and patients with asthma, diabetes, . gout or hyperlipidaemia antihypertensive effect: . decrease in blood pressure while taking felodipine due to a decrease in peripheral vascular resistance felodipine is effective in reducing blood pressure in patients with hypertension in the supine position and in the sitting position and standing at rest and during exercise. Since felodipine no effect on smooth muscle veins or adrenergic vasomotor control, the development of orthostatic hypotension occurs. At the beginning of treatment, due to a decrease in blood pressure in the patients receiving felodipine, may be a temporary reflex increase in heart rate (HR), and cardiac output. The increase in heart rate prevents simultaneous with felodipine application (β-blockers. The action of felodipine on blood parabolan pressure and peripheral vascular resistance is correlated with plasma concentrations of felodipine. in the equilibrium state the clinical effect is maintained between the reception of doses and blood pressure reduction is maintained for 24 hours. felodipine treatment results in regression of left ventricular hypertrophy. felodipine has a natriuretic and diuretic effect and has no kaliyureticheskim effect. When administered felodipine decreased tubular sodium reabsorption . and water, which explains the absence of a delay of salts and fluids in the body Felodipine reduces vascular resistance in the kidney and increases the renal perfusion Felodipine has no effect on glomerular filtration and albumin excretion.. in a study of HOT (Hypertension optimal Treatment study – study on optimal Therapy of Hypertension) , involving 18790 patients with hypertension mild – moderate, Plendila use in combination with inhibitors, beta-blockers and / or diuretics, if necessary, reduced diastolic blood pressure less than 90 mmHg in 93% of patients. In the same study, the incidence of cardiovascular complications in patients with type 2 diabetes (n = 1,501) was significantly lower (50%) in the group of patients who have succeeded in reducing diastolic blood pressure to a level of ≤ 80 mm.
Hg (11.9 / 100 patient-years) compared with the group, where the level of diastolic blood pressure was <90 mm.rt. Art. (24.4 / 1000 patient-years). The STOP-2 study where Plendil used as one of two blocker “slow” calcium channels, involving 6614 patients, aged 70 to 84 years, it has been parabolan shown that the use of dihydropyridine calcium antagonists as initial therapy, followed by addition of beta-blockers, where appropriate, no effect on mortality from cardiovascular disease compared with traditional therapy of beta-blockers and / or diuretics. can be used as monotherapy for the treatment of hypertension Plendil or in combination with other antihypertensive agents, such as beta-blockers, diuretics or ACE inhibitors. Anti-ischemic effect: Application of felodipine leads to improved myocardial perfusion due to dilatation of the coronary vessels. Reducing the load on the heart is provided by reducing peripheral resistance (decrease in load overcomes the heart muscle), resulting in a decrease in myocardial oxygen demand. Felodipine relieves spasm of the coronary vessels. Felodipine improves motility and reduces the frequency of angina attacks in patients with stable angina. At the beginning of therapy, a temporary increase in heart rate, currently treated appointment of beta-blockers may occur.The effect occurs within 2 hours and lasts for 24 hours. For the treatment of stable angina felodipine can be used in combination with beta blockers or as monotherapy.
Systemic bioavailability of felodipine is approximately 15% and is independent of food intake. However, absorption rate, but its degree may vary depending on the meal, and the maximum concentration in plasma, thus increases by about 65%.
The maximum plasma parabolan concentration is reached after 5.3 hours.
The drug binds to the plasma protein at 99%. The volume of distribution at steady state is 10 L / kg. The half-life is about 25 hours, a plateau phase is reached for about 5 days. Not accumulates even at long reception.
The total plasma clearance of an average of 1200 ml / min.
Reduced clearance in elderly patients and in patients with reduced liver function leads to increased felodipine plasma concentrations. At the same time a sign of age is only partially explains the individual changes in the plasma concentration of felodipine. Felodipine is metabolised in the liver and all identified metabolites have no effect vazodilyatornym (hemodynamic activity). About 70% of the accepted dose is excreted as metabolites in the urine and the rest – with the feces. Less than 0.5% is excreted in the urine in unchanged form. In violation of the plasma concentration of felodipine does not change in renal function, but there is accumulation of inactive metabolites. Felodipine does not appear in hemodialysis.
- Arterial hypertension
Hypersensitivity to felodipine or other components of the drug
Heart failure decompensated
acute myocardial infarction,
Age 18 years (effectiveness parabolan and safety have not been established)
Use with caution: aortic stenosis, labile blood pressure, abnormal liver function, severe renal insufficiency (creatinine clearance <30 mL / min), heart failure after acute myocardial infarction.