cocaine
Table of Contents
cocaine
see also:
history
- the 1st LA discovered, pure alkaloid isolated 1860 from leaves of Erythroxylon coca a bush in Andes growing @ 1000-3000m altitude;
- studied as LA, Mx of morphine withdrawal, spinal anaesthetic from 1884;
- used as LA eye but ceased as caused corneal ulcers;
pharmacology
- Absorption: rapidly absorbed from mucosa & s/c esp. if inflammation;
action
- prevents generation & conduction of nerve impulses by blockade of voltage-gated Na channel;
- potentiates noradrenergic systems as inhibits NA uptake;
metabolism & excretion
- degraded by plasma esterases; T½ plasma 1hr;
adverse effects of cocaine
- euphoria/dysphoria → garrulousness & excitement → tremors
- vomiting (effect on vomiting centre)
- bradycardia (central vagal stimulation) → tachycardia (central & periph. effect)
- → vasoconstriction (increased sympathetic stimulation) → hypertension → hypotension
- cocaine fever
- tolerance, dependence
toxic effects
- usually if > 6mg/kg
CNS:
- initial seizures (effect of inhib.neurons)
- subsequent coma, resp. arrest (all neurons affected)
CVS:
- decreased myocardial excitability, decreased conduction, decreased contractility;
- heart block or VF esp. if inadvertent i/vascular injection;
- AMI;
cocaine.txt · Last modified: 2011/05/16 05:38 by 127.0.0.1