CNS Drugs Flashcards

1
Q

What is the receptor for glutamate? What is the mechanism?

A

NMDA

  • excitatory
  • increase Na+ Ca++ K+ ion ch. conductance
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is the receptor for GABA? What is the mechanism?

A

GABAa and GABAb

  • inhibitory (more -ve inside)
  • GABAa: incr. Cl- conductance
  • GABAb: incr. K+ conductance
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is the receptor for dopamine? What is the mechanism?

A

D2

  • inhibitory (decr. cAMP)
  • Presynaptic: incr. K+ conductance
  • Postsynaptic: decr. Ca++ conductance
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is the receptor for serotonin? What is the mechanism?

A

5-HT

  • 5HT2a: excitatory - incr. IP3 & DAG
  • 5HT1a: inhibitory - decr. cAMP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is the receptor for opioids?

A

mu

  • opioids are mu agonists
  • naloxone is a mu aNTAGonist
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is the receptor for cannabinoids? What is the mechanism?

A

CNS: CB1
PNS: CB2
- inhibit GABA and glutamate release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is the receptor for acetylcholine? What is the mechanism?

A
M1, M3, M5
M2, M4
N
- cholinergic (PSNS) receptors
- incr. IP3 & DAG conductance; decr. K+ conductance
- decr. cAMP conductance
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is the receptor for norepinephrine? What is the mechanism?

A
in the CNS
a1, a2, b1, b2
- adrenergic (SNS) receptors
- incr. IP3 & DAG conductance; decr. K+ conductance
- decr. cAMP (inhibitory)
- incr. cAMP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is the mechanism of action of L-DOPA?

A
  • increase dopamine synthesis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is the mechanism of action Ropinerole?

A
  • D2 receptors
  • receptor agonist (parkinsons = too little dopamine)
  • treats ms. stiffness and tremors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is the mechanism of action of Selegiline?

A
  • inhibit MAO-B

- MAO-B metabolizes MPTP to toxic MPP+ (dopamine breakdown)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is the mechanism of action of Benztropine?

A
  • anti-muscarinic
  • block ACh to balance low dopamine levels
  • prevents sweating, muscle stiffness, and constriction of smooth muscles
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is the mechanism of action of Cocaine?

A
  • incr. dopamine transmission
  • prevent reuptake of dopamine
  • drug induced psychosis –> schiz.
    (also prevents reuptake of serotonin and NE)
  • drug of abuse
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is the mechanism of action of Amphetamine?

A
  • incr. dopamine transmission
  • incr. release of dopamine
  • drug induced psychosis –> schiz.
    (also incr. release of NE and serotonin)
  • drug of abuse
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is the mechanism of action of PCP?

A
  • 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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What is the mechanism of action of LSD?

A
  • 5HT2A receptor agonist (serotonin)
  • hallucinogen: visual illusions and perceptual distortions
  • drug of abuse
  • Adverse: panic rxn, psychosis, flashbacks
  • OD causes strong uterine contractions
    (glutamate and serotonin imbalance = psychosis)
17
Q

What is the mechanism of action of Haloperidol?

A
  • D2 receptor aNTAgonist > 5HT2a aNTAgonist
  • anti-psychotic
  • butyrophene derivative
  • action: to decr. dopamine activity (that causes psychosis in limbic)
18
Q

What is the mechanism of action of Olanzapine

A
  • 5HT2a aNTAGonist > D2 aNTAGonist
  • newer anti-psychotic
  • atypical drug
  • action:
  • decr. dopamine activity in limbic
  • incr. dopamine in cortex
  • incr. glutamate in cortex
19
Q

What is the glutamate hypothesis?

A
  • decr. glutamate function = NMDA aNTAGonists
    induces psychosis/hallucinations
  • decr. glutamate = incr. dopamine (limbic) = psychosis (+ve)
  • decr. glutamate = decr. dopamine (cortex) = -ve symptoms
20
Q

What are the adverse effects of anti-psychotics?

A

CNS
- parkinson’s like symptoms (D2 is aNTAGonized in striatum)
- hormal/metabolic dysfunction (D2 aNTAGonized in diencephalon)
- sedation H1 and a1 receptors aNTAGonized
ANS
- a1 aNTAgonized = hypotension (low BP)
- M aNTAgonized = anti-muscarinic = atropine like effects (dry mouth, constipation - inhibit gland secretion and sm. ms. mvts)