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LECOM pharmacology notecards > chapter 13- Dopaminergic neurotransmission > Flashcards

chapter 13- Dopaminergic neurotransmission Flashcards

1
Q

what is the precursor of all catecholamines

A

tyrosine

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2
Q

what enzyme has the key function to terminate the action of catecholamines in the brain and periphery

A

MAO

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3
Q

where is MAO-A expressed

A

brain and periphery

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4
Q

where is MAO-B expressed

A

CNS

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5
Q

what do D1 and D5 dopamine receptors lead to

A

increased cAMP

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6
Q

what do D2, D3, and D4 dopamine receptors lead to

A

inhibits cAMP generation

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7
Q

where are D1 and D2 expressed at high levels

A

striation as well as nucleus accumbens and olfactory tubercle

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8
Q

what dopamine receptor is expressed highly in anterior pituitary gland

A

D2

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9
Q

where is D3 expressed at high levels

A

limbic system

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10
Q

where is D4 localized

A

frontal cortex, diencephalon, brainstem

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11
Q

where is D5 mainly located

A

hippocampus, olfactory tubercle and hypothalamus

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12
Q

what is the clinical application of levodopa

A

parkinson disease

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13
Q

what stages of parkinson disease is levodopa particularly effective

A

early stages

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14
Q

what are some common side effects of levodopa

A

dyskinesia, orthostatic hypotension, loss of appetite

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15
Q

what side effect with basically be for sure to happen with levodopa within 5 years of use

A

dyskinesia

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16
Q

what are some contraindications for levodopa use

A

history of melanoma; narrow angle glaucoma; concomitant use of MAO-inhibitor

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17
Q

what are some contraindications for rasagiline and selegiline

A

concomitant use of cyclobenzaprine, mirtazapine, st johns wort; concomitant use of dextromethorphan

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18
Q

what is levodopa almost always administered with

A

carbidopa

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19
Q

what is the mechanism of action of carbidopa

A

inhibitor of DOPA decarboxylase

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20
Q

what is the clinical application of pramipexole and ropinirole

A

parkinson disease

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21
Q

what is another clinical application of ropinirole besides parkinson

A

restless leg syndrome

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22
Q

what are some adverse effects seen with pramipexole and ropinirole

A

orthostatic hypotension, extrapyramidal movements, hallucinations

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23
Q

what are some cognitive effects seen with pramipexole and ropinirole

A

excessive sedation, vivid dreams and hallucinations

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24
Q

what does rasagiline and selegiline inhibit

A

MAO-B

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25
Q

what are some adverse effects seen with rasagiline and selegiline

A

bundle branch block, GI hemorrhage insomnia (selegiline), confusion (selegiline)

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26
Q

what is the mechanism of action of tolcapone

A

inhibit COMT and inhibit breakdown of levodopa by COMT in periphery

27
Q

what is the clinical application of tolcapone and entacapone

A

parkinson disease

28
Q

what parkinson drug can cause orthostatic hypotension, hyperpyrexia, fulminant hepatic failure and rhabdomyolysis

A

tolcapone

29
Q

what is the main difference between tolcapone and entacapone

A

tolcapone is highly lipid-soluble agent that can cross the BBB, while entacapone distributes only to periphery

30
Q

what rare toxicity has been reported with tolcapone use

A

fatal hepatic toxicity

31
Q

what is the mechanism of action of amantadine in respect to parkinson disease

A

antagonism of excitatory NMDA receptors

32
Q

what is the mechanism of action of trihexyphenidyl

A

muscarinic receptor antagonist that reduces cholinergic tone in the CNS by modifying the actions of striatal cholinergic interneurons

33
Q

what is the mechanism of action of benztropine

A

muscarinic receptor antagonist that reduces cholinergic tone in the CNS by modifying the actions of striatal cholinergic interneurons

34
Q

what are some adverse rxns seen with trihexphenidyl and benztropine use

A

angle-closure glaucoma, increased intraocular pressure, psychosis, xerostomia

35
Q

what are some contraindications for trihexyphenidyl and benztropine use

A

narrow angle glaucoma; younger than 3 years; tragic dyskinesias (for trihexyphenidyl)

36
Q

what is the clinical application of phenothiazines and derivatives

A

psychotic disorder

37
Q

what is the additional clinical application of chlorpromazine and perphenazine specifically

A

nausea and vomiting

38
Q

what is the mechanism of action of phenothiazines and derivatives

A

antagonize mesolimbic and possibly mesocortical D2 receptors

39
Q

how is fluphenazine administered

A

intramuscularly every 3-4 weeks

40
Q

what are the butyrophenones

A

haloperidol and droperidol

41
Q

what is the clinical application of haloperidol

A

psychoses and tourettes syndrome

42
Q

what is the clinical application of droperidol

A

nausea and vomiting; anesthesia adjunct

43
Q

what is the most widely used butyrophenone

A

haloperidol

44
Q

what is the clinical application of pimozide

A

psychotic disorders; tourettes syndrome

45
Q

what does molindone exert its antipsychotic effects on

A

ascending reticular activating system in the absence of muscle relaxation and incoordination effects

46
Q

what atypical antipsychotics are effective at antagonizing dopamine D2 and serotonin 5-HT2 receptors but also dopamine D4 receptor antagonist

A

clozapine and olanzapine

47
Q

what is the clinical application of risperidone

A

psychotic disorders; bipolar disorder

48
Q

what is the clinical application of clozapine

A

schizophrenia refractory to other antipsychotics

49
Q

what is the clinical application of olanzapine

A

psychotic disorders; bipolar disorder

50
Q

what is the clinical application of quetiapine

A

psychotic disorders; bipolar disorder

51
Q

what is the clinical application of ziprasidone

A

psychotic disorders; bipolar disorder

52
Q

what are some adverse reactions seen with clozapine

A

mild extrapyramidal symptoms; agranulocytosis; anticholinergic symptoms

53
Q

what are some contraindications for clozapine use

A

history of clozapine-induced agranulocytosis or severe granulocytopenia; myeloproliferative disorders

54
Q

what receptors does clozapine bind to

A

D1-5, 5-HT2, alpha1, H1, muscarinic receptors

55
Q

what receptors does olanzapine bind to

A

D1-4, 5-HT2, alpha1, H1, M1-M5 receptors

56
Q

what does aripiprazole bind to

A

D2 and 5-HT1A partial agonist and 5-HT2a antagonist

57
Q

what is the clinical application of paliperidone

A

schizophrenia; schizoaffective disorder

58
Q

what are some adverse reactions seen with paliperidone

A

agranulocytosis, tachyarrhymthmia, ischemia, death; hyperprolactinemia, akathisia, extrapyramidal disease, somnolence

59
Q

what is the active metabolite of risperidone

A

paliperidone

60
Q

what receptors does paliperidone effect

A

D2 and 5-HT2a antagonist and alpha1 adrenergic, alpha2 adrenergic, and H1 histaminergic antagonist to lesser degree

61
Q

what is the clinical application of Iloperidone

A

schizophrenia

62
Q

what are some adverse reactions seen with Iloperidone

A

stroke, TIA, prolonged QT interval, suicidal intent, dizziness

63
Q

what receptors does iloperidone effect

A

D2 and 5HT2a antagonist, with higher affinity for 5-HT2a than D2

LECOM pharmacology notecards (22 decks)

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