CNS pharmacology Flashcards

1
Q

What are indications for antipsychotic drugs

A
  1. Schizophrenia
  2. tourettes syndrome
  3. Huntingtons Chorea
  4. OCD and others
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2
Q

What is the widely accepted cause of psychosis

A

hyperactive dopamine pathway

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3
Q

what are antipsychotic drugs

A

Dopamine Antagonists

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4
Q

What are typical antipsychotic drugs, and what are common ones

A

1st generation dopamine antagonists

  • phenothiazines
  • haloperidol
  • Thiothixene
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5
Q

what are atypical antipsychotic drugs, and what are the common ones

A
2nd generation dopamine antagonists
more specific than 1st gen antagonists = less tardive dyskinesia
- Clozapine
- Olanzipine
- Quetiapine
- Risperidone
- Ziprasidone
- Arpiprazole
- paliperidone
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6
Q

what is the most commonly prescribed 1st gen antipsychotic

A

Haloperidol

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7
Q

What are the side effects of dopamine receptor antagonists (antipsychotics)

A
  • tardive dyskinesias
  • parkinsons like symptoms
  • Dystonias (spasms)
  • Perioral tremor
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8
Q

what is the problem with the side effects of antipsychotics (dopamine antagonists)

A

the patients struggle to live with them so they stop taking their medications

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9
Q

What type of drug is used to manage the extrapyrimidal motor effects of antipsychotics (dopamine antagonists)

A

Antimuscarinic drugs

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10
Q

what is Neuroleptic Malignant syndrome

A

a life threatening neurological disorder from an adverse reaction to antipsychotic drugs. symptoms include: muscle rigidity, fever, autonomic instability, delerium.

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11
Q

adverse effects of antipsychotic use

A
otrhostatic hypotension
convulsions
photosensitivity
cardiac arrythmias (long QT
galactorrhea
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12
Q

what are the two types of depression

A

unipolar

bipolar

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13
Q

what is the monoamine theory of depression

A

depression is a result of low monoamine transmitters (Norepinephrine and 5-HT (serotonin)

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14
Q

what is the desired action of antidepressants

A

block the reuptake of monoamines

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15
Q

What are tricyclic antidepressants? and what are the common drugs

A

NE and 5-HT reuptake inhibitors (More NE)

  • Amitryptiline
  • Desipramine
  • Doxepin
  • Imipramine
  • Protryptiline
  • Maprotiline
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16
Q

What are SSRIs? and what are the common drugs

A

Selective serotonin reuptake inhibitors

  • prozac (Fluoxetine)
  • paroxetine
  • Sertraline
  • Fluvoxamine
  • Citalopram
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17
Q

what are SNRIs? and what are the common drugs

A

mixed NE and Serotonin (5-ht) reuptake inhibitors

  • Effexor (Venlafaxine)
  • Cymbalta (Duloxetine)
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18
Q

What is the drug that is an NE only reuptake inhibitor

A

Wellbutrin (bupropion)

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19
Q

What are MAOIs. what are the most common drugs

A

monoamine oxidase inhibitors

  • Phenelazine
  • tranylcypromine
  • selegiline
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20
Q

why are MAOIs and other antidepressants contraindicated

A

because it leads to excessive amounts of monoamines (seratonin and NE)

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21
Q

What is Mirtazapine

A

monoamine receptor agonist
(a2 adrenergic receptor blocker)

another antidepressant

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22
Q

What is Trazodone

A

antidepressant thought to potentiate 5-HT

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23
Q

What is St. Johns Wort

A

weak monoamine uptake inhibitor

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24
Q

What are other uses of TCA’s, SSRis?

A

TCA = neuropathic pain
TCA + SSRI = fibromyalgia
SSRI = anxiety disorders, ADHD
Buproprion = addiction

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25
Q

Why aren’t typical antidepressants used to treat bipolar disorder

A

they can induce the manic phase

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26
Q

What is the drug used to prophylactially prevent manic-depressive episodes

A

Lithium

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27
Q

what is the problem with lithium in treating bipolar disorder

A

it has a narrow TI which requires plasma monitoring.

causes nasuea, convulsions, coma, arrythmias

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28
Q

what are other options besides lithium in treating bipolar disorder

A

antiepileptic drugs: Valproate, carbamazepine, lamotrigine

Atypical antipsychotics: Zyprexa (Olanzapine)

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29
Q

What is the common method of action for sedative hypnotics

A

activating or enhancing Cl channels

GABA-A receptors

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30
Q

What are the uses for sedative hypnotics

A
antianxiety
anticonvulsants
amnesia
insomnia
panic disorders
sedation
skeletal muscle relaxation
31
Q

Adverse effects of sedative hypnotics

A
Ataxia
Amnesia
Altered sleep patterns
confusion
Excessive sedation
32
Q

What are the two main classes of sedative hypnotics and what is their mode of action

A

barbiturates and benzodiazepines

they are both modulators of GABA receptors that enhance the effect of GABA on them

33
Q

what are the subclasses of barbiturates and their drugs

A

long acting - phenobarbital
intermediate acting - pentobarbital, amobarbital
short acting - thiopental

34
Q

What is the long acting barbiturate and what is it used for

A

phenobarbital = antiepileptic

35
Q

what are the intermediate acting barbiturate and what are they for

A

pentobarbital, amobarbital = sleep induction

36
Q

what is the short acting barbiturate and what is it used for

A

thiopental = induction anesthetic

37
Q

what is a contraindication for barbiturates

A

Certain types of porphyria

38
Q

What is it about benzodiazepines that gives them a longer half life

A

they have active metabolites

39
Q

What are the benzodiazepines and what are their half lives

A
triazolam - 1,5 hrs
midazolam - 4 hours
oxazepam - 8 hrs
lorazepam - 14 hrs
diazepam - 48-100 hrs
flurazepam - 100 hrs
40
Q

What is a common sedative hypnotic used for conscious sedation in dentistry that is not a barbiturate or benzodiazepine

A

chloral hydrate

41
Q

what should you know about chloral hydrate before using it

A

that repetitive doses of it shouldn’t be used since toxicities can be very serious

42
Q

what is zolpidem and zalepon?

A

a sedative hypnotic that acts on GABAA receptors,
has low risk of dependence
and is used to treat insomnia

43
Q

what is the sleep hypnotic Buspirone used for and what is its mechanism

A

it is a 5HT1A agonist,

it is used for anxiety

44
Q

What is Baclophen, what is it used for

A

agonist at GABAB

its a muscle relaxant used to treat trigeminal neuralgia

45
Q

What is Diphenhydramine

A

Benadryl

its an antihistamine that causes sedation

46
Q

Ethanol can be used as a sedative narcotic but isn’t

A

yep, it affects multiple targets and one of them is GABAA

47
Q

What is Flumazenil, and what is it used for

A

its a GABA A receptor antagonist

it is used to reverse sedation drugs

48
Q

Methocarbamol, Carisprodol, and Cyclobenzaprine are used for what

A

sedative hypnotics (their mechanism of action isn’t fully understood)

49
Q

What are seizures, what different types are there

A

they are excessive and innapropriate activity of CNS neurons
they can be partial or generalized
they can be tonic-clonic or absence

50
Q

What are the 4 mechanisms of action in antiepileptics

A

Na v channel antagonists
Ca channel antagonists
Glutamate receptor antagonists (AMPA, NMDA)
Cl channel agonists

51
Q

What are the different drugs used to treat epilepsy, and what is their method of action

A
phenobarbital - GABA A modulator
phenytoin - Na v antagonist
Primidone - metabolized to phenobarbital
Carbamazepine - Na v antagonist
Gabapentin - unknown (not GABA)
Valproic acid (valproate) - GABA, Na v and Ca v antagonist
Ethosuxamide - Ca v antagonist
52
Q

What are the adverse effects of using phenobarbital as an antiepileptic

A

potential for drug-drug interactions
sedation
osteomalacia
respiratory depression

53
Q

What are the adverse effects of using phenytoin as an antiepileptic

A

eliminated by zero order kinetics = potential for overdose
gingival hyperplasia
osteomalacia

54
Q

What are the adverse effects of using primidone as an antiepileptic

A

acute systemic and CNS toxicity
sedation
ataxia
nystagmus

55
Q

What are the adverse effects of using carbamazepine as an antiepileptic

A

induces liver enzymes - drug drug interactions
diziness
ataxia

56
Q

What is carbamazepine used for besides as an antiepileptic

A

bipolar disorder and trigeminal neuralgia

57
Q

what is the antiepileptic with an unknown mechanism of action that is FDA approved for partial seizures

A

Gabapentin

58
Q

what is Gabapentin used for more often that epilepsy

A

neuralgia

59
Q

what is the antiepileptic that increases GABA and is an NA v and Ca V antagonist. and is approved by the FDA for partial seizures

A

valproic acid (valproate)

60
Q

what else is valproate (valproic acid) used for besides epilepsy

A

bipolar disorder

61
Q

What are the adverse effects of using valproate (valproic acid) as an antiepileptic

A

hair loss
hyperglycemia
hyperuricemia
teratogenic

62
Q

What is the antiepileptic drug that blocks Ca v and is approved by the FDA for absence seizures

A

Ethosuxamide

63
Q

What is the characteristic of parkinsons disease

A
progressive hypokinesia
loss of voluntary movement
tremor at rest
involuntary hyperkinesia
progresses to muscle rigidity
64
Q

What causes parkinsons disease

A

a defect in signaling in the basal ganglia
loss of DA cells
leads to less GABA action
leads to increased excitatory output to motor cortex

65
Q

What are the 3 treatment strategies for parkinsons

A

increase dopamine receptor activation in basal ganglia
block muscarinic receptors in basal ganglia
block NMDA glutamate receptors

66
Q

why does blocking muscarinic receptors in basal ganglia help with parkinsons

A

cholinergic function in the basal ganglia inhibits dopamine action

67
Q

What is the main drug used for parkinsons disease that is a prodrug for dopamine

A

levadopa (once it gets past the BBB it is converted into dopamine

68
Q

What is the drug used for to prevent levadopa from being converted into dopamine in the periphery due to its action as a dopa carboxylase inhibitor

A

carbidopa (it can’t cross the BBB but help L-dopa stay until L-dopa crosses the BBB)
reduces L-dopa needed by 90% and decreases side effects

69
Q

What drugs are used as DA receptor agonists that help dopamine bind more readily

A

Pramipexole
Ropinirole
Apomorphine
Bromocriptine

70
Q

What are the drugs that block COMT (catecholectamine O-methyl tranferase) from breaking down dopamine in CNS

A

tolcapone

Entacapone

71
Q

What are the drugs that block MAO-B from breaking down dopamine in the CNS

A
Rasagiline
Selegiline (don't use with antidepressants)
72
Q

How is diphenhydramine used to treat parkinsons

A

it blocks the H1 receptor and treats extrapyrimidal side effects

73
Q

What is the drug that used to be used as an antiflu but now is used for parkinsons

A

amantidine (blocks NMDA)

74
Q

how does benztropine help with parkinsons

A

it is an anticholinergic and tries to restore cholinergic and dopamine balance