section name header

Pronunciation

hye-DRAL-a-zeen

Classifications

Therapeutic Classification: antihypertensives

Pharmacologic Classification: vasodilators

Indications

REMS


Unlabeled Use:
  • New York Heart Associated Class III or IV HF with reduced ejection fraction (in combination with isosorbide dinitrate).

Action

  • Direct-acting peripheral arteriolar vasodilator.
Therapeutic effects:
  • Lowering of BP in hypertensive patients and decreased afterload in patients with HF.

Pharmacokinetics

Absorption: Rapidly absorbed following oral administration; well absorbed from IM sites. IV administration results in complete bioavailability.

Distribution: Widely distributed.

Metabolism/Excretion: Mostly metabolized by the GI mucosa and liver by N-acetyltransferase (rate of acetylation is genetically determined [slow acetylators have hydralazine levels and risk of toxicity; fast acetylators have hydralazine levels and response]).

Half-Life: 2–8 hr.

Time/Action Profile

(antihypertensive effect)

ROUTEONSETPEAKDURATION
PO45 min2 hr2–4 hr
IM10–30 min1 hr3–8 hr
IV5–20 min15–30 min2–6 hr





Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: tachycardia, angina, arrhythmias, edema, orthostatic hypotension

Derm: rash

GI: diarrhea, nausea, vomiting

MS: arthralgias, arthritis

Neuro: dizziness, drowsiness, headache, peripheral neuropathy

Misc: drug-induced lupus syndrome

Interactions

Drug-drug:

Route/Dosage

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

IV Administration:

Patient/Family Teaching

Evaluation/Desired Outcomes

Canadian Brand Names

Apresoline