cocaine

midterm

• source:

• derived from coca plant

  • alkaloid ester

  • lipophilic: easily passes through blood-brain barriers

  • form: coca paste, cocaine hydrochloride, cocaine base (free base), crack cocaine

  • schedule 2 drugs: very high potential for abuse

absorption

• all sites (gastrointestinal, injection, inhaled, mucus, dermal)

• topical/mucus membrane: medical use

  • upper raspatory system: anesthetic

• fast as 8 sec

• coke powder

  • nasal

    • vasoconstrictive

• crack cocaine

  • inhaled

  • peak effect 1-3 min

distribution

• concentrations: cerebral cortex/brain, spleen, kidneys, lung, heart, muscles

metabolism/ excretion

• liver

• excreted → kidneys → urine

• alcohol + cocaine

  • toxic metabolite = coca ethylene

• half-life: 50 min

pharmacodynamics

• 1)local anesthetic

  • blocks calcium channels in the axon

• 2) vasoconstrictor

• 3) psychostimulant:

  • block of presynaptic transporters responsible for the re-uptake of monoamines

    • serotonin

    • dopamine

    • noradrenalin

  • indirect agonist

dopamine:

• euphoric rush

serotonin

• mood Addiction

noradrenalin:

• vasoconstriction, cardiac

characteristics of use: first: Moderate

• euphoria

• alert, concentration

• increase sex motivation

• well-being

• reduced fatigue, appetite

characteristics of use: then

• insomnia

• anxiety

• irritability

• increase in impulsive behavior

• extremely addictive

characteristics of use acute use:

• cardiac symptoms

• tremors

• seizures

• body pain

• hyperactive muscles

• stroke

• organ failure