Felodipine

  • Ethyl- methyl- [( 4RS ) -4 - (2,3- dichlorophenyl) -2,6- dimethyl-1 ,4 -dihydropyridine - 3,5- dicarboxylate ]
  • (±) -ethyl- methyl- [4 - (2,3- dichlorophenyl) -2,6- dimethyl-1 ,4 -dihydropyridine - 3,5- dicarboxylate ]
  • (RS) -ethyl- methyl-4- (2,3- dichlorophenyl) - 1,4- dihydro-2 ,6-dimethyl- 3,5- pyridinedicarboxylate
  • (±) -ethyl- methyl-4- (2,3- dichlorophenyl) - 1,4- dihydro-2 ,6-dimethyl- 3,5- pyridinedicarboxylate

C08CA02

Calcium antagonist

145 ° C

Attention

1050 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Felodipine is a drug from the group of calcium antagonists of the 1,4- dihydropyridine type and can reduce an extension of the smooth muscle of the vessels the blood pressure considerably. Therapeutically, it is used mainly for the treatment of arterial hypertension. The drug is used as a racemic mixture of atropisomers.

Mechanism of Action

Felodipine blocks the calcium influx into the cardiac muscle, smooth muscle, and in the excitement of education and conduction system of the heart. This leads to the heart to a reduced contractility ( negative inotropic ) and a reduced O2 consumption. On smooth muscle, it causes dilation of small arteries ( arterioles ) and thus a afterload. In therapeutic doses is the effect of felodipine and other dihydropyridine calcium antagonists hardly at heart, but almost exclusively on vessels.

Indications

Felodipine is approved in Germany for the treatment of essential arterial hypertension.

Side effects

Rarely, syncope, vomiting, and arthralgia. Very rarely occur restlessness, tinnitus, dyspnea, constipation, photosensitivity, pollakiuria, menorrhagia, weight gain.

For the enjoyment of fruits of the family of grapefruit can cause a delayed degradation of felodipine and thus to increased drug availability in the body.

Contraindications

In the following illnesses, administration of felodipine is contraindicated: acute myocardial infarction (within the first 8 weeks), congestive heart failure, hypertrophic obstructive cardiomyopathy, aortic stenosis higher grade, unstable angina pectoris, AV block, 2nd and 3rd degree, stroke within the last six months, severe renal impairment.

Trade names

Felobeta (D), Felocor (D), Modip (D), Munobal (D, A), Plendil (A, CH ), various generics (D, A, CH), Feloday (I)

Delmuno (D), Logimax (CH), Mobloc (D) Unimax (D),

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Calcium channel blocker Dangerous Substances Directive (67/548/EEC) Active ingredient Atrioventricular block
330317
de