CNS Drugs Flashcards
What is the receptor for glutamate? What is the mechanism?
NMDA
- excitatory
- increase Na+ Ca++ K+ ion ch. conductance
What is the receptor for GABA? What is the mechanism?
GABAa and GABAb
- inhibitory (more -ve inside)
- GABAa: incr. Cl- conductance
- GABAb: incr. K+ conductance
What is the receptor for dopamine? What is the mechanism?
D2
- inhibitory (decr. cAMP)
- Presynaptic: incr. K+ conductance
- Postsynaptic: decr. Ca++ conductance
What is the receptor for serotonin? What is the mechanism?
5-HT
- 5HT2a: excitatory - incr. IP3 & DAG
- 5HT1a: inhibitory - decr. cAMP
What is the receptor for opioids?
mu
- opioids are mu agonists
- naloxone is a mu aNTAGonist
What is the receptor for cannabinoids? What is the mechanism?
CNS: CB1
PNS: CB2
- inhibit GABA and glutamate release
What is the receptor for acetylcholine? What is the mechanism?
M1, M3, M5 M2, M4 N - cholinergic (PSNS) receptors - incr. IP3 & DAG conductance; decr. K+ conductance - decr. cAMP conductance
What is the receptor for norepinephrine? What is the mechanism?
in the CNS a1, a2, b1, b2 - adrenergic (SNS) receptors - incr. IP3 & DAG conductance; decr. K+ conductance - decr. cAMP (inhibitory) - incr. cAMP
What is the mechanism of action of L-DOPA?
- increase dopamine synthesis
What is the mechanism of action Ropinerole?
- D2 receptors
- receptor agonist (parkinsons = too little dopamine)
- treats ms. stiffness and tremors
What is the mechanism of action of Selegiline?
- inhibit MAO-B
- MAO-B metabolizes MPTP to toxic MPP+ (dopamine breakdown)
What is the mechanism of action of Benztropine?
- anti-muscarinic
- block ACh to balance low dopamine levels
- prevents sweating, muscle stiffness, and constriction of smooth muscles
What is the mechanism of action of Cocaine?
- incr. dopamine transmission
- prevent reuptake of dopamine
- drug induced psychosis –> schiz.
(also prevents reuptake of serotonin and NE) - drug of abuse
What is the mechanism of action of Amphetamine?
- incr. dopamine transmission
- incr. release of dopamine
- drug induced psychosis –> schiz.
(also incr. release of NE and serotonin) - drug of abuse
What is the mechanism of action of PCP?
- NMDA receptor aNTAGgonist (glutamate)
- hallucinogen: visual illusions and perceptual distortions
- drug of abuse
- Adverse: panic rxn, psychosis, flashbacks
- OD is fatal
(glutamate and serotonin imbalance = psychosis)