Brand Name
Inderall
Broad category
Antihypertensive / Antiarrythmic / sympatholytic
Pharm Class
First gen nonselective beta-adrenergic antagonist
MOA
Primary: nonselective, competitive antagonist that binds to and inhibits both Beta-1 and Beta-2 receptors
- prevents actions of catecholamines and NE –> decreases arterial BP by decreasing contractility, lowers HR, and diminshes renin release
Indications / Clinical Uses
HTN
angina
acute MI
PHEOCHROMOCYTOMA
treat anxiety and panic attacks
Others:
Prophylaxis for migraines
Management of thyroid storm
IV dose
0.5 - 1 mg over 1 minute
Repeat dosing
0.5 mg q 3-5 mins
MAX dosing
0.1 mg/kg MAX
onset
2-3 mins
Duration
4-6 hours
CV effects
Decreased heart rate
decreased contractility
decreased CO
decreased systemic BP
Can precipitate acute CHF
may cause AV block
Respiratory effects
bronchospasm (can be fatal)
Metabolic effects?
Masks symptoms of hypoglycemia
Other concerns?
Withdrawal syndrome if not titrated down d/t upregulation
Contraindications (absolute)
Cardiogenic shock
Precautions
Bronchospastic disease (CAREFUL)
AV block
bradycardia
PVD
Metabolism
Hepatic: CYP 450
- CYP2D6
- CYP1A2
- CYP2C19
and conjugation
Elimination
Primarily renal
Elimination half-life
3-4 hours
Vd considerations
Large Vd
- highly lipophilic
- extensive tissue distribution
Clearance considerations
Reduced clearance with
- Hepatic impairment
- Low CO
Protein binding
90-95% high