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BMB Test 4 Leesy > B7.071 - Drugs Affecting the CNS Dopamine Systems > Flashcards

B7.071 - Drugs Affecting the CNS Dopamine Systems Flashcards

1
Q

primary strategy of parkinsons treatment

A

replace or mimic dopamine in the neostriatum

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2
Q

families of dopamine receptors in the brain

A

D1-like (D2, D5) and D2 like (D2, D3, D4)

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3
Q

D2 receptors

A

appear to be most important in parkinsons pathology, (indirect pathway)

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4
Q

D3 receptors

A

may mediate neuroprotective effects

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5
Q

secondary strategies of treating Parkinsosn

A

Anticholinergics

Amantidine

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6
Q

L-DOPA

A

dopamine precursor, DOPA does not cross BBB

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7
Q

motor effects of L-DOPA

A

reversal of rigidity, tremor and bradykinesia and reduced facial expression

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8
Q

psychic pharm effects of LDOPA

A

improved mental function

sense of well being

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9
Q

GI AEs of LDOPA

A

nausea and vomiting due to stimulation of D2 receptors in CTZ

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10
Q

cardiovascular AEs of LDOPA

A

orthostatic hypotension d/t stimulation of dopamine receptors in kidney and vasculature

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11
Q

long term motor AEs of LDOPA

A

fluctuations in efficacy (on off or bradykinetic episodes

wearing off effects

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12
Q

neuro AEs of LDOPA

A

abnormal involuntary movements, dystonia, dyskinesias, chorea, oral movements

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13
Q

psychic AEs of LDOPA

A

hallucinations, paranoia, mania, anxiety, depression, problems with impulse control d/t stimulation of dopamine receptors in targets of mesolimbic and mesocortical pathways

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14
Q

Pimavanserin

A

specifically indicated of PD psychosis, mechanism involved inverse agonist and antagonist activity at 5-HT2A and 2C receptors

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15
Q

neuroendocrine AEs of Pimvaserin

A

renewed sexual interest and behavior, hypersexuality

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16
Q

pharmacokinetics of LDOPA

A

Oral, absorption GI Transit time dependent
Peak levels 1/2-2 hrs
t1/2 1-3 hrs

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17
Q

metabolism and excretion of LDOPA

A

95% decarboxylated in periphery and excreted in urine which is why you need CARBIDOPA bihhhh

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18
Q

Carbidopa

A

blocks AADCin periphery

decreases levodopa dose and side effects

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19
Q

MAO-B inhibitors

A

Selegeline
Rasagiline
MAO-B preferentially metabolizes DA (as opposed to MAO-A 5-HT and NE)

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20
Q

COMT inhibitors

A

Tolcapone - hepatotoxicity

Entacapone - peripheral only

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21
Q

contraindications of LDOPA

A

abrupt discontinuation
close angle glaucoma - can stimulate beta rec
melanoma - LDOPA precursor to melanin
breast feeding - inh prolactin secretion

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22
Q

which conditions should LDOPA be used with caution

A

psychosis
cardiac disease
peptic ulcer
open angle glaucoma

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23
Q

dopamine agonists monotherapy or add on

A

pramipexole - D2/3 agonist, monotherapy or add on

ropinerole - D2/3

24
Q

dopamine agonists add on with LDOPA

A

bromocriptine - D2 agonist (also used for hyperprolactinemia)

25
Q

mechanism of dopamine agonists

A

ag at D2 and other dopamine receptors

26
Q

AEs of dopamine agonists

A

nausea, vomiting, postural hypotension, hallucinations,

27
Q

anticholinergics

A

benztropine

procyclidine

28
Q

mech of benztropine and procyclidine

A

block actions of striatal cholinergic neurons
Generallly leses effectve than LDOPA
can be used alone early on

29
Q

side effects of benzyropine and procyclidine

A

constipation, urinary hesitance, confusion, hallucinations

30
Q

amantadine

A

unknown mech, may release dopamine and/or have anticholinergic properties

31
Q

use of amantidine

A

monotherapy or adjunct to levodopa

32
Q

SEs of amantidine

A

similar to dopamine
anticholinergic effects
livedo reticularis, peripheral edema, headache

33
Q

antipsychotic drugs

A

primarily used to treat schizophrenia aka major tranquilizers or neuroleptics

34
Q

mech of antipsychotics

A

antagonists of D2 dopamine receptor
Serotonin receptors esp 5-HT2 and/or novel D2 like receptors may be involved
Antipsychotics also interact with a variety of other receptors which contribute to side effects

35
Q

pharm effects of antipsychotics

A

initially sedation, decreased agitation
+ sx improve over weeks to months
- sx may be improve by newer drugs but not older/typical
antiemetic d/t Dop blockade

36
Q

Early side effects of antipsychotics

A

neuro - extrapyramidal effects (EPS), dystonia, akathisia, parkinsonian sx d/t blockade of striatal dopamine receptors
can be treated with anticholinergics

37
Q

other SE of antipsychotics

A

increased prolactin release leading to amenorrhea, gynecomastia, galactorrhea
weight gain, metabolic syndrome, DM

38
Q

long term SE of antipsychotics

A

tardive dyskinesia (sterotyped movements and facial disfigurement)
perioral tremor
blood dyscrasias and agranulocytosis can occur with clozapine**

39
Q

pharmacokinetics of antipsychotics

A

IM, IV, PO
highly lipophilic (x BBB, stored in adipose)
Extensive hepatic metabolism

40
Q

typical antipsychotics work for

A

positive (not -) sx

produce EPS and tardive dyskinesia

41
Q

MOA of typical antipsychotics

A

All are D2 antagonists

most are antagonists at a variety of other receptors

42
Q

phenothiazines (typical antipsychotics)

A 
chlorpromazine
Fluphenazine
Thioridazine
haloperidol
thiothixene
43
Q

haloperidol

A

historically the most widely prescribed antipsychotic
relatively more selective for dopamine
highest incidence of EPS**

44
Q

atypical antipsychotics featues

A

NO EPS or tardive dyskinesia

Antagonist at 5-HT receptors

45
Q

Clozapine

A 
5-HT2>D2
activity at broad spectrum of rec
no EPS or tardive dyskinesia
causes agranulocytosis
approved for treatment resistant pts
46
Q

newer antipsychotics

A

risperidone
lurasidone
paliperidone

47
Q

risperidone

A

5-HT2=D2

EPS at higher doses

48
Q

Lurasidone

A

5-HT2, D2, 5HT7

49
Q

paliperidone

A

primary metabolite of risperidone with lower affinity for 5HT2A receptor

50
Q

which newer antipsychotics have the lowest risk of EPS and tardive dyskinesia

A

Olanzapine
Quetiapine
Ziprasidone
Aripiprazole

51
Q

olanzapine

A

5-HT2>D2

high incidence of weight gain and metabolic syndrome

52
Q

Quetiapine

A

5-HT2=D2

High incidence of weight gain and metabolic syndrome

53
Q

Ziprasidone

A

D2, 5-HT1D antagonist
5-HT1A agonist
also inhibits NE and 5-HT reuptake

54
Q

Aripiprazole

A

D2 & 5-HT1A partial agonist
5-HT2A antagonist
Partial agonism at D2 receptors may allow for sufficient stimulation to prevent EPS, while preventing over stimulation

55
Q

other uses of antipsychotics

A

Management of agintation and psychotic symptoms in acute mania & bipolar, delerium, dementia (associated with increased risk of mortality), alc hallucinosis DURING heavy drinking

56
Q

parkinsons drugs

A
  1. levodopa
  2. carbidopa
  3. pramipexole
  4. ropinirole
  5. bromocriptine
  6. selegiline
  7. entacapone
  8. benztropine
  9. procyclidine
  10. amantadine
  11. pimavanserin
57
Q

antipsychotics

A
  1. chlorpromazine
  2. fluphenazine
  3. thioridazine
  4. haloperidol
  5. thiothixene
  6. clozapine
  7. risperidone
  8. lurasidone
  9. paliperidone
  10. olanzapine
  11. Quetiapine
  12. ziprasidone
  13. aripiprazole

BMB Test 4 Leesy (4 decks)

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