Pharmacopeia

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Field EPHEDRINE
Cardiovascular · Cardiovascular · Level 3
METARAMINOL
Cardiovascular · Cardiovascular · Level 2
Mechanism of action

direct and indirect sympathomimetic with alpha and beta activity

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

1. CVS
- Effects similar to adrenaline but longer duration as drug is not metabolized by MAO or COMT
- Positive inotrope, chronotrope. Increases CO MVO2
- Increases coronary blood flow
- Increased SVR and PVR

2. Resp
- Respiratory stimulant
- Bronchodilation

3. CNS
- Stimulatory effect similar to amphetamine
- Cerebral blood flow increases
- Mydriasis occurs
- Has local anesthetic effects

4. GIT
- Relaxes GI smooth muscle
- Splanchnic vasoconstriciton

5. GU
- Decreased RBF
- Contracts bladder sphincter and relaxes detrusor muscle- acute urinary retention
- Does not cause uterine constriction

6. Metabolic
- Increased hepatic glycogenolysis
- Increased BMR

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 PVR

CNS:
- Doesn’t cross BBB
- Causes cerebral vasoconstriction but increases CPP

Renal/GU
- Renal vasoconstriction but re-established renal perfusion pressure in hypotension
- Uterine contraction and reduces uterine blood flow

Metabolic
- Inhibits insulin release and increases lipolysis
- May increase VO2

Absorption

- Rapidly absorbed orally

IV. BA 100%
0.1-0.2mg boluses titrated to BP
onset / dur imm / up to 20 mins

Distribution

- Widely distributed and crosses BBB, placenta and breast milk

limited data on pharmacokinetics

Metabolism

- Resistant to MAO and COMT. Hepatic metabolism with a major metabolite being active and may have central effects

Hepatic

Excretion

- 50-90% excreted unchanged in urine. Urinary elimination is pH dependent (enhanced by acidic urine)
- Tachyphylaxis rapidly occurs

Unknown

Half-life

Elimination T1/2 is 6 hours

short

Adverse Effects Toxicity

Insomnia, anxiety, tremor, headache, dysrhythmias, nausea and vomiting, and chest pain
irritant to mucous membranes
Acute hypertensive crisis with: MAOIs, doxapram, beta-blockers, oxytocin, and ergot alkaloids

Caution should be exercised in patients with pulmonary hypertension. May cause
severe hypertension in some patients

Class Group

ADRENERGIC

ADRENERGIC

Indications Uses

1. Hypotension during surgery
2.Nocturnal enureisis
3. Diabetic autonomic neuropathy
4.Hiccups
5. Nasal decongestant

short term correction of BP in the setting of regional anaesthesia and off label for short term BP correction

Introduction

Synthetic direct and indirect sympathomimetic with alpha and beta activity

synthetic noncatecholamine with both direct and indirect
sympathomimetic actions.

Legacy Cicm Level

Level 2

Level 2

Main Action

alpha and beta activity

both direct and indirect
sympathomimetic actions. It acts mainly via alpha1/2 adrenoceptors to cause
vasoconstriction but also has some minor beta activity.

Presentation

- Clear colourless solution for injection (3-9mg slow injection, dose repeated ever 3-4 min)
- Oral tablets
- Nasal spray

clear solution 10mg/mL in one mL vials and usually diluted to
10mg in 10ml or 20ml

Route And Dose

IV 3-6mg bolus

IV boluses or infusion