Pharmacopeia
METARAMINOL
Core pharmacology
- Class Group
ADRENERGIC
- Legacy Cicm Level
Level 2
- Introduction
synthetic noncatecholamine with both direct and indirect
sympathomimetic actions.- Indications Uses
short term correction of BP in the setting of regional anaesthesia and off label for short term BP correction
- Presentation
clear solution 10mg/mL in one mL vials and usually diluted to
10mg in 10ml or 20ml- Main Action
both direct and indirect
sympathomimetic actions. It acts mainly via alpha1/2 adrenoceptors to cause
vasoconstriction but also has some minor beta activity.- Mechanism of action
through ↑TPR
May be transient bradycardia due to baroreceptor feedback upon infusion initiation.
↑Pulmonary vascular resistance. ↑coronary artery flow by an indirect mechanism (stimulates NA release)- Physiological effects
CVS:
- Increased SVR leading to an increase in diastolic and systolic BP
- Reflex bradycardia may occur despite B1 effects
- It has positive inotropic effects but cardiac output is more likely to decrease as a result of increased afterload
- Coronary artery blood flow increases as an indirect mechanism
- Increased PVRCNS:
- Doesn’t cross BBB
- Causes cerebral vasoconstriction but increases CPPRenal/GU
- Renal vasoconstriction but re-established renal perfusion pressure in hypotension
- Uterine contraction and reduces uterine blood flowMetabolic
- Inhibits insulin release and increases lipolysis
- May increase VO2- Adverse Effects Toxicity
Caution should be exercised in patients with pulmonary hypertension. May cause
severe hypertension in some patients- Absorption
IV. BA 100%
0.1-0.2mg boluses titrated to BP
onset / dur imm / up to 20 mins- Distribution
limited data on pharmacokinetics
- Metabolism
Hepatic
- Excretion
Unknown
- Half-life
short
- Route And Dose
IV boluses or infusion