Pharmacology: Cocaine

Administration
IV/oral/intra-nasal (paste or cocaine-HCL) and inhalation (crack cocaine).

Inhalation formula
Crack cocaine. Alkaline precipitate, “freebase” with non-polar solvent.

Pharmacokinetics
Fast administration, fast euphoria, but fast metabolism.

Oral administration
Slower absorption (ionised, pka 8.7).

Metabolism route
Blood and liver cholinesterase enzymes.

Metabolites
ecgonine methyl ester, benzoylecogonine.

T1/2
Varies from 20 – 90 min, all metabolised by 2 hrs.

Addiction
Fast loss of metabolism equates with fast loss of euphoria, contributes to intense addiction.

Mechanism
MAO and serotonin/noradrenaline uptake inhibitor. Increase synaptic dopamine, 5-TH, N/A. Also a Na channel blocker.

4 Effects?
Local anaesthetic, sympathetic stimulation, platelet activation and euphoria (positive and reinforcing).

Sympathetic stimulation causes…
Hyperpyrexia (vasoconstriction), seizures in epileptics.

Platelet activation by…
NA receptors, causes haemodyamic changes.

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