Carvedilol
Chemical
Mixed antagonist of α1 & β adrenoreceptors with no intrinsic sympathomimetic activity
Use
- HF
- 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