Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Plendil
Active ingredient: Felodipine
Available dosage forms: 2,5, 5, 10 mg
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Felodipine general information
We’ve got automatic devices which are now utilised to measure blood pressure. This is generally a problem due to high blood pressure. The greater number (systolic) measures the pressure within the arteries as soon as the heart beats (as soon as the heart muscle contracts). There wasn’t any substantial difference between both groups.
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Felodipine (Felodipine): instruction, and the use of a formula
The nosological classification (ICD – 10)
Feature substances Felodipine
calcium channel blocker from the group of 1,4 – dihydropyridine. Slightly yellow crystalline powder, insoluble in water, soluble in dichloromethane and ethanol. Molecular weight 384,26.
Mode of action – antihypertensive, antianginal, diuretic, natriuretic.
Interfaces with the dihydropyridine receptors and inhibits the passage of calcium ions into cells. It is acting on the inner side of the membrane and binds more effectively depolarized membrane calcium channels changing their function. It lowers the concentration of calcium ions mainly in vascular smooth muscle cells, including coronary, and to a lesser extent in cardiomyocytes. It is the expansion of peripheral blood vessels (arterioles, arteries), reduces round. It lowers blood pressure (possible slight reflex tachycardia). No effect on the smooth muscles of the veins (does not cause orthostatic hypotension).
Antianginal effect due to dilation of coronary vessels, increasing oxygen delivery to the myocardium, the improvement in coronary blood flow, as well as weakening the afterload on the heart, which leads to a reduction of myocardial wall tension and myocardial oxygen demand. It improves the ratio of delivery / consumption of oxygen in the myocardium. It suppresses the activity of sine – atrial or atrio – ventricular node. The reflex increase in heart rate in response to the vasodilation offset the negative inotropic effect. The diuretic effect is a consequence of the lowering of tubular reabsorption of sodium. It does not alter glomerular filtration, the daily excretion of potassium and albumin excretion. Against the backdrop of the filtration renal function increases glomerular filtration rate. No effect on the concentration of blood glucose and lipid profile.
The action develops within 2 – 5 hours, lasts 24 hours, and correlated with the severity of the effect of dose and blood concentration. The antihypertensive effect persists while taking NSAIDs. Conducting prolonged antihypertensive therapy leads to regression of left ventricular hypertrophy. In patients with stable angina improves the tolerability of the load and reduces the frequency of attacks. Reduces symptomatic and latent myocardial ischemia in vasospastic angina. It is effective in older patients, including patients with asthma and other chronic lung diseases accompanied by BOS syndrome, severe renal impairment, diabetes mellitus, gout, hyperlipidaemia, Raynaud’s disease. After kidney transplantation (patients taking cyclosporine), felodipine reduces blood pressure. improves renal blood flow, glomerular filtration rate increases and improves graft function.
Almost completely absorbed from the gastrointestinal tract. completeness and rate of absorption is independent of food intake, bioavailability of 15 – 20% (the effect of “first pass” through the liver). C max is achieved through 2,5 – 5 h Maximum equilibrium concentration of about 20% higher in plasma than after a single dose.. It circulates in protein-bound (mainly albumin) form (99%). Elimination is a multi-phase nature of the final value of T 1/2 ; 11 –. 16 hrs from blood plasma clearance of 200 ml / min. Biotransformation in the liver to form 6 metabolites whose activity is 23% of felodipine activity. Cumulation with prolonged use is not observed. It passes through GEB and placental barrier in small amounts into breast milk. As metabolites excreted in unaltered form (less than 0.5%), in the kidney (70%), as well as bile and feces (10%). Felodipine concentration in blood increases in patients of advanced age or with reduced liver function (compared to younger patients). Renal impairment does not affect the pharmacokinetics of performance.
In experimental studies revealed no carcinogenic and mutagenic activity. In animal studies (rats, mice, rabbits, monkeys) revealed embryotoxic and teratogenic properties (adequate and well-controlled studies have been conducted in humans).
Application of the substance Felodipine
Hypertension, angina (stable angina, including Prinzmetal angina, in unstable form in case of intolerance or ineffectiveness of beta – blockers or nitrates), Raynaud’s syndrome.
Hypersensitivity (including to other derivatives of dihydropyridine), severe hypotension, acute myocardial infarction and for 1 month after myocardial infarction, cardiogenic shock, clinically significant aortic stenosis, decompensated heart failure, pregnancy, breast-feeding.
Restrictions on the use
Unstable angina, strongly marked bradycardia or heart failure, severe liver dysfunction, children under 18 years of age (safety and efficacy have not been determined).
Application of pregnancy and breastfeeding
is contraindicated in pregnancy.
Category effects on the fetus by FDA ; C.
breast-feeding should be discontinued at the time of treatment.
Side effects of substance Felodipine
From the cardio – vascular system and blood (blood, hemostasis) . & Ge; 1% ; hot flashes; 0,1 – 1% ; tachycardia; 0,01 – 0,1% ; fainting.
From the nervous system and sensory organs) . & Ge; 1% ; headache; 0,1 – 1% ; fatigue, weakness, dizziness, paresthesia; & Lt; 0,01% ; myalgia.
From the of the genitourinary system. & Ge; 1% ; peripheral edema (ankles, feet, legs); & Lt; 0,01% ; increase in frequency of urination; 0,01 – 0,1% ; sexual dysfunction, impotence.
From the digestive tract . 0,1 – 1% ; nausea; 0,01 – 0,1% ; vomiting; & Lt; 0,01% ; gingival hyperplasia, increased liver enzymes.
From the musculo – skeletal system . 0,01 – 0,1% ; arthralgia.
For the skin . 0,1 – 1% ; rash, itching; & Lt; 0,01% ; photosensitivity.
Allergic reactions: 0,01 – 0,1% ; hives; & Lt; 0,01% ; fever, angioneurotic edema.
Others . 0,01 – 0,1% ; gynecomastia (after long-term therapy in elderly patients).
The hypotensive effect of felodipine strengthen other antihypertensives, including beta – blockers, verapamil, diuretics and alcohol. C max increase in blood felodipine inhibitors of cytochrome P450: cimetidine (50%), erythromycin, some flavonoids present in grapefruit juice; lower ; inducers of microsomal enzymes (phenytoin, carbamazepine, rifampicin, barbiturates). Felodipine increases the concentration of digoxin in plasma.
Symptoms: severe hypotension, bradycardia.
Treatment: symptomatic therapy. In severe hypotension patient to give a horizontal position with raised legs, if you want to increase the volume of plasma (a glucose solution, sodium chloride or dextran), administered agonists with a primary effect on the alpha 1 – adrenergic receptors; bradycardia used atropine (0,5 – 1 mg / in).
Dosing and Administration
Inside, is not liquid, squeezed water, 1 time a day (in the morning). Dosage is determined strictly individually. When hypertension: an initial dose of ; 5 mg (for elderly patients and abnormal liver function 2.5mg), if necessary, adjust the dose, usually the maintenance dose ; 5 & ndash; 10 mg. When angina: initial dose of ; 5 mg, if necessary ; to 10 mg. The maximum daily dose of ; 20 mg.
Precautions substances Felodipine
With caution is prescribed for heart failure, especially in combination with beta – blockers. In patients with angina pectoris in rare cases may develop severe hypotension, leading to deterioration of myocardial perfusion. There is currently no data on the feasibility of using the drug for secondary prevention of myocardial infarction. If abnormal liver function requires correction dose. Patients who during treatment with felodipine there is weakness and dizziness, you should refuse from driving motor vehicles and work requiring high concentration.
Trading names of drugs with working substance