Hydralazine
Chemical
Hydrazinophthalazine
Use
Hypertension
Presentation
Tablets
Powder for reconstitution → NOT to be reconstituted with D5W because it degrades the drug quickly!
Dose
IV: 3 – 20mg every 30 mins
PO: 25mg QID
Route
PO/IV
Onset
5 – 30 mins
MoA
?Unclear
Vascular smooth m → inhibits Ca2+ entry or prohibits intrac. Ca2+ store releases
PD
CVS: ↓SVR, compensatory ↑HR
CNS: ↑CBF
GI: ↑RBF 2° ↑CO → ↑renin activity
PK
A
Extensive 1st pass
35% OBA
D
90% PPB
VD = 4L/kg
M
Acetylation & oxidation, then conjugation
E
90% in urine
1% unchanged
t ½ B 0.5 – 3.5hrs
Adverse Effects
- Headache
- Flushing
- Nausea & vomiting
- May precipitate angina
- Tachyphylaxis