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7 Cards in this Set

  • Front
  • Back

Cocaine





Sympathomimetics: Local Anesthetic, Drug of Abuse


-Monoamine uptake blocker


-Cocaine blocks DAT (and NET and SERT).


This blockade potentiates and prolongs



the actions of the monoamines

Methylphenidate (Ritalin)





Sympathomimetics: Drug for ADHD, Narcolepsy

(MPH) increases DA and NE levels (blocks DAT and NET). MPH is structurally similar to amphetamine, but its effects are


similar to those of cocaine (they have similar affinity for DAT and act on the same brain sites).

Amphetamine





Sympathomimetics: drug of ADHD, narcolepsy and drug of abuse

-Vesicular monoamine transporter blocker


-Releases monoamines at synapses



-Inhibits uptake of monoamine


o Amph serves as a substrate for DAT, therefore competitively inhibiting DA reuptake (extracellular DA increases);


o Once inside the terminal, Amph disrupts the vesicular storage of monoamines, causing increase in cytoplasmic DA levels.


Monoamines are pumped out of the terminal (non-vesicularly) by a reverse action of DAT (extracellular DA increases).



Methamphetamine





Sympathomimetics: Drug of Abuse


Vesicular monoamine transporter blocker


-Amphetamine derivative (N- methylated); similar pharmacological effects to cocaine and amphetamine but longer duration.


-Methamphetamine is directly toxic to midbrain dopamine neurons. Chronic leads to


severe structural and functional changes in areas of the brain associated with emotion


and memory

MDMA





Sympathomimetics: Drug of abuse


Vesicular monoamine transporter blocker

Caffine





Methylxanthines

A. Translocation of extracellular calcium;


B. Increase in cAMP and cGMP caused by inhibition of phosphodiesterase;



C. Blockade of Adenosine Receptors, mainly A2a. (main)

Nicotine

Readily crosses the bbb. At low doses



it’s a stimulant.


• Peripheral effects: Causes an autonomic arousal, increases blood pressure



and heart rate, stimulates motility of GI tract and bladder.


-Nicotine acts on nAChRs in the VTA to


provoke dopamine release in the Nacc;


-Nicotine stimulates release of glutamate,


which act on Glu receptors on VTA


dopamine neurons, stimulating dopamine



release into the nucleus accumbens .