Felodipine and isradipine: new calcium-channel-blocking agents for the treatment of hypertension. 1993

T Walton, and L R Symes
Department of Pharmacy, Charleston Area Medical Center, WV 25326.

The chemistry, pharmacology, pharmacokinetics, clinical uses, adverse effects, and dosage of felodipine and isradipine are reviewed. Felodipine and isradipine are new calcium-channel-blocking agents with FDA-approved labeling for use in the treatment of essential hypertension. Both agents are members of the dihydropyridine class of calcium antagonists, which also includes nifedipine and nicardipine. Like those agents, felodipine and isradipine affect blood pressure by producing peripheral vasodilation. Felodipine and isradipine undergo extensive first-pass metabolism; their bioavailabilities are approximately 15% and 17%, respectively. The drugs are highly protein bound but do not affect serum digoxin concentrations. Anticonvulsants may reduce the elimination half-life of felodipine. Felodipine and isradipine are effective antihypertensive agents when used alone or in combination with beta blockers or diuretics. Both agents have shown some benefit in the treatment of angina pectoris in limited studies. Clinical data do not support the use of either agent for the treatment of congestive heart failure or Raynaud's phenomenon. Felodipine and isradipine have similar adverse-effect profiles, and their adverse effects resemble those of other agents in the class. Common adverse effects are peripheral edema and increased heart rate. The initial dosage of isradipine for the treatment of hypertension is 2.5 mg twice daily. Felodipine should be started at a dosage of 5 mg once daily. Felodipine and isradipine are effective antihypertensive drugs but have not demonstrated clear advantages over other dihydropyridine calcium-channel blockers.

UI MeSH Term Description Entries
D006973 Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more. Blood Pressure, High,Blood Pressures, High,High Blood Pressure,High Blood Pressures
D007668 Kidney Body organ that filters blood for the secretion of URINE and that regulates ion concentrations. Kidneys
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D006333 Heart Failure A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION. Cardiac Failure,Heart Decompensation,Congestive Heart Failure,Heart Failure, Congestive,Heart Failure, Left-Sided,Heart Failure, Right-Sided,Left-Sided Heart Failure,Myocardial Failure,Right-Sided Heart Failure,Decompensation, Heart,Heart Failure, Left Sided,Heart Failure, Right Sided,Left Sided Heart Failure,Right Sided Heart Failure
D006439 Hemodynamics The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM. Hemodynamic
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000787 Angina Pectoris The symptom of paroxysmal pain consequent to MYOCARDIAL ISCHEMIA usually of distinctive character, location and radiation. It is thought to be provoked by a transient stressful situation during which the oxygen requirements of the MYOCARDIUM exceed that supplied by the CORONARY CIRCULATION. Angor Pectoris,Stenocardia,Stenocardias
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D015736 Felodipine 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. Agon,Felo Biochemie,Felo-Puren,Felobeta,Felocor,Felodipin 1A Pharma,Felodipin AL,Felodipin AZU,Felodipin AbZ,Felodipin Dura,Felodipin Heumann,Felodipin Stada,Felodipin Von Ct,Felodipin-Ratiopharm,Felodur,Felogamma,Fensel,Flodil,H 154-82,Modip,Munobal,Perfudal,Plendil,Renedil,Felo Puren,Felodipin Ratiopharm,H 154 82,H 15482,Heumann, Felodipin,Von Ct, Felodipin
D017275 Isradipine A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure. Dynacirc,Isradipine, (+-)-Isomer,Isradipine, (R)-Isomer,Isradipine, (S)-Isomer,Lomir,PN 200-110,PN 205-033,PN 205-034,PN-200-110,PN-205-033,PN-205-034,PN 205 033,PN 205 034,PN 205033,PN 205034,PN205033,PN205034

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