Brand Name
Apresoline
Broad Category
Antihypertensive
Pharmacological Class
Direct Acting Vasodilator
MOA
Direct systemic arterial vasodilator, produces direct relaxation of small arteries and arterioles while sparing venous capacitance vessels (reduces SVR and LV afterload while leaving preload unaffected)
Proposed mechanisms
- activation of KATP channels, decreasing free intracellular calcium, and blocking calcium release from SR
- Potential increase in cGMP through induced increase in vascular NO (not confirmed)
Indications / Clinical uses
HTN
Heart Failure
Eclampsia
Hypertensive Asthmatics
Bolus Dosing
2.5-5 mg titrated every 20-30 mins
(2.5- 20mg really lol)
Onset
15-30 mins (delayed)
Duration
4-6 hours
Concentration
20 mg/mL
CV effects
Baroreceptor mediated Reflex
- Tachycardia
- increased Contractility
- Increased SV
- Increased Overall CO
Decreased SVR
Can aggravate angina (Contraindicated in CAD)
CNS effects
Increased CBF and ICP
* inhibits CBF autoregulation
HA
Dizziness
N/V
tremors
Other effects
Fluid retention
nasal congestion
Contraindications (Absolute)
CAD: increases myocardial oxygen demand precipitating ischemia
Precautions
Elevated ICP
Slow acetylators
- induces lupus-like syndrome with chronic, high-dose admin
Beneficial Drug-Drug interactions?
BB with hydralazine (propranolol) prevents baroreceptor reflex
Metabolism
Hepatic
- acetylation
- hydroxylation
Excretion
Renal