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231 Pharmacology > 8 CNS Drugs > Flashcards

8 CNS Drugs Flashcards

1
Q

what are 2 types of CNS neurons

A
  • excitatory - activates post-synaptic receptors that increase Na+/Ca2+ influx
  • inhibitory - activate post-synaptic receptors that increase Cl- influx or K+ efflux
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2
Q

4 classifications of CNS neurotransmitters and some of their examples

A
  • amino acids
    • excitatory - glutamate
    • inhibitory - GABA
  • acetylcholine
  • monoamines
    • dopamine
    • norepinephrine
    • serotonin (5-HT)
  • peptides
    • opioids
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3
Q
  • causes of Alzheimer’s
  • tx
  • side effects
A
  • loss of cholinergic input to limbic system (impairs memory) and cortex (cognitive dysfunction)
  • no Tx affects neurodegeneration
  • acetylcholinesterase inhibitors (eg. donepezil) penetrates CNS, decreases loss of cognitive function in moderate AD
  • ANS side effects - nausea, diarrhea, vomiting
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4
Q

2 types of Parkinson’s

A
  • naturally occurring
  • drug-induced
    • reversible - neuroleptic drugs block dopamine receptor
    • irreversible - MPTP destroys dopaminergic neurons in substantia nigra
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5
Q

effects of dopamine and ACh in a normal vs Parkinsonian brain?

A
  • normal
    • substantia nigra produces dopamine, inhibits GABA
    • ACh excites GABA
  • Parkinsonian
    • substantia nigra doesn’t produce GABA, dopmaine agonists needed to inhibit GABA
    • antimuscarinic drugs needed to lower excitatory response to GABA
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6
Q

3 drugs used in Parkinsonism and overall purpose

A
  • Levodopa & dopamine agonists
  • MAO inhibitors
  • antimuscarinic drugs

increase dopamine activity in brain or decrease muscarinic cholinergic activity or both

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7
Q
  • levodopa and dopamine agonists MOA

- AE

A
  • levodopa converted to dopamine by DOPA decarboxylase
  • dopamine agonists bind to dopaminergic receptors in brain
  • improve sx until too few neurons left
  • levodopa metabolism to dopamine –> dyskinseia, nausea, joint stiffness
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8
Q
  • MAO inhibitor eg.
  • MOA
  • AE
A
  • eg. selegiline
  • selective inhibitor of MAO-B –> decreases dopamine metabolism –> prolongs action
  • adjunct to L-dopa
  • dyskinesia, hallucination hypotension
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9
Q
  • antimuscarinic drugs eg.
  • MOA
  • AE
A
  • eg. benztropine
  • decreases overactivity of cholinergic neurons in basal ganglia
  • used in early PD or with L-dopa
  • drowsiness, confusion, hallucinations
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10
Q

2 hypotheses of schizophrenia as related to the limbic system

A
  • dopamine hypothesis
    • functional excess of dopamine
    • antipsychotic drugs decrease dopamine synaptic activity (D2 blockade) to reduce symptoms
  • serotonin (5-HT) hypothesis
    • hallucinogenic drugs are 5-HT agonists
    • 5-HT receptors modulate dopamine release in limbic system, cortex, striatum
    • atypical antipsychotic drugs decrease serotonin synaptic activity (5-HT2a blockade)
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11
Q

what are antipsychotic effects reversed by?

A

increasing dopamine by levodope or amphetamine

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12
Q

2 typical antipsychotic drug types and examples

A
  • phenothiazine derivative - eg. chlorpromazine

- butyrophenone derivative - eg. haloperidol

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13
Q

1 typical antipsychotic drug example

A

clozapine

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14
Q

pharmacodynamics (blockade) or haloperidol and clozapine

A
  • haloperidol D2>D4>a1>5HT2A

- clozapine D4=a1>5HT2A>D2

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15
Q
  • clinical effects of all antispychotics? atypical (more so than typical)?
A
  • all - decrease positive sx (hallucinations, delusions)

- atypical - decrease negative sx (apathy, impaired attention)

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16
Q
  • side effects of antipsychotics
  • typical (more so than atypical)
  • all
  • atypical
A
  • general: block D2 –> increase cholinergic activity
  • typical&raquo_space; atypical - movement disorders, hyperactivity
  • all - a receptor blockade –> hypotension
  • atypical –> weight gain
17
Q

3 monoamines and what they are responsible for

A
  • norepinephrine - alertness, energy, anxiety, attention, interest
  • serotonin - anxiety, obsessions, compulsions
  • dopamine - attention, motivation, pleasure, reward, interest
18
Q
  • selective serotonin reuptake inhibitors (SSRI) eg.
  • uses
  • what’s serotonin syndrome?
A
  • eg. fluoxetine (Prozac)
  • less side effects than tricyclics
  • antidepressant, obesity, OCD, bulimia
  • serotonin syndrome when combined with other antidepressants (life-threatening seizures, CV instability etc)
19
Q

serotonin-NE reuptake inhibitors (SNRI)

A
  • increase [ ] of NE and serotonin in synaptic cleft
  • better than SSRi for major depressive disorders
  • low affinity for other NT receptors = low AE
20
Q
  • MAO inhibitor eg.
  • MOA
  • what’s hypertensive crisis?
A
  • eg. phenelzine
  • stops degradation of NE, dopamine and serotonin in nerve terminal
  • used if other antidepressants not effective
  • hypertensive crisis if tyramine-cntaining foods (cheese, beer, red wine) ingested with amphetamines
21
Q

clinical use of antidepressants?

A
  • SSRIs 1st
  • switch if ineffective
  • monoamine levels change after 1 dose, action may not be observed immediately
22
Q
  • bipolar disorder tx eg.

- side effects

A
  • eg. lithium carbonate
  • stabilizes mood, no drowsiness
  • prevents mania, depression
  • low TI, high toxicity, ataxia, tremors
23
Q
  • anxiety disorder tx - first line? others?
A
  • SSRI 1st
  • anxiolytics (sedative) - eg. benzodiazepine
  • risk of dependence
  • no motor effect
24
Q
  • benzodiazepine eg.

- MOA

A
  • eg. diazepam (valium)
  • enhances GABA (inhibitory) neutrotransmission
  • binds to GABAa receptor –> increase FREQUENCY of GABA-mediated opening of Cl- channel –> increases inhibition of neurons in brain
25
Q
  • barbiturates eg.

- MOA

A
  • eg. phenobarbital/pentobarbital

- same as diazepam but increase DURATION

26
Q

toxicity of anxiolytics-sedative/hypnotics

A
  • dose-dependent CNS depression - impaired judgement, amnesia, coma, death
  • additive CNS depression with other drugs
  • withdrawal when stopped
  • tolerance
  • increased toxicity if liver impaired
27
Q
  • antiepileptic drugs that modify ionic conductances - 2 eg.

- MOA

A
  • phenytoin, carbamazepine

- block Na+ channels (excitatory)

28
Q
  • antiepileptic drugs that enhance inhibitory transmission - 1 new eg, 2 old eg.
    MOA
A
  • eg. valproic acid
    • inhibits GABA transaminase –> terminates action of GABA
  • eg. diazepam and phenobarbital
    • opens GABA-mediated Cl- channel to enhance GABA neurotransmission
29
Q
  • 2 toxicity problems with anti-epileptic drugs
  • withdrawal
  • drug interactions
A
  • teratogenicity increases risk of fetal malformations (cardiac defects, cleft lip/palate [phenytoin, carbamazepine], neural tube effects [valproic acid])
  • overdosage - CNS/resp depression
  • withdraw drug gradually if seizure-free for 4 years
  • alter metabolism by inducing/inhibiting hepatic enzymes
  • change binding of another drug to plasma proteins

231 Pharmacology (10 decks)

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