Felodipine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Felodipine is a calcium channel blocker. It reversibly competes with nitrendipine and/or other calcium channel blockers for dihydropyridine binding sites, blocks voltage-dependent calcium currents in vascular smooth muscle and cultured rabbit atrial cells, and blocks potassium-induced contracture of the rat portal vein. By blocking the calcium channels, felodipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes and results in a decrease of peripheral vascular resistance.
Pharmacology
Felodipine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Felodipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Felodipine is similar to other peripheral vasodilators. Felodipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes blocking the calcium channels. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Felodipine¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include excessive peripheral vasodilation with marked hypotension and possibly bradycardia. Oral rat LD50 is 1050 mg/kg.
Drug Interactions
Felodipine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Amobarbital The barbiturate decreases the effect of felodipineAprobarbital The barbiturate decreases the effect of felodipineButabarbital The barbiturate decreases the effect of felodipineButalbital The barbiturate decreases the effect of felodipineButethal The barbiturate decreases the effect of felodipineCarbamazepine Carbamazepine decreases the effect of felodipineDihydroquinidine barbiturate The barbiturate decreases the effect of felodipineHeptabarbital The barbiturate decreases the effect of felodipineHexobarbital The barbiturate decreases the effect of felodipineMethohexital The barbiturate decreases the effect of felodipineMethylphenobarbital The barbiturate decreases the effect of felodipinePentobarbital The barbiturate decreases the effect of felodipinePhenobarbital The barbiturate decreases the effect of felodipinePrimidone The barbiturate decreases the effect of felodipineQuinidine barbiturate The barbiturate decreases the effect of felodipineSecobarbital The barbiturate decreases the effect of felodipineTalbutal The barbiturate decreases the effect of felodipineErythromycin Erythromycin increases the effect of felodipineJosamycin Erythromycin increases the effect of felodipineEthotoin The hydantoin decreases the effect of felodipineFosphenytoin The hydantoin decreases the effect of felodipineMephenytoin The hydantoin decreases the effect of felodipinePhenytoin The hydantoin decreases the effect of felodipineQuinupristin This combination presents an increased risk of toxicityItraconazole Itraconazole increases effect/toxicity of felodipineNelfinavir Nelfinavir increases the effect and toxicity of felodipineOxcarbazepine Oxcarbazepine decreases the levels of felodipineTacrolimus Felodipine increases tacrolimus levels
Felodipine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Grapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product.
Felodipine¿¡ ´ëÇÑ Description Á¤º¸ A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. [PubChem]
The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. FELODIPINE [GGT Increase] [Composite Activity] (Score)I (Marginal) 0 (Active) 0