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