Carvedilol

Chemical

Mixed antagonist of α1 & β adrenoreceptors with no intrinsic sympathomimetic activity

Use

  1. HF
  2. Hypertension

Presentation

Tablets

Dose

6 – 25mg PO

Route

Oral

Onset

?

MoA

  • Non-selective β1/β2 & α1 blocker
  • S (-) enantiomer → B blockade
  • S (-) & (+) blockade
  • β receptors → ↓HR & FoC, ↓symp outflow → ↓CO
  • α receptors → VD → ↓BP

PD

CVS

  • ↓BP
  • ↓PAP
  • ↓CO

PK

A

OBA 25%

Significant 1st pass

D

115L, >98% PPB

M

Hepatic oxidation & glucuronidation

E

<2% unchanged

Metabolites in urine

t ½ B 10hrs

Adverse Effects

  • ↓BP
  • Dizziness
  • Fatigue
  • Diarrhoea
  • Weakness
  • Heart block
  • Erectile dysfunction