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Autonomics-1.3

Pharmocology-Autonomics1.3/DA

QuestionAnswer
known functions are mediated by what receptor family? D2
D2 receptors are implicated in what disease? schitzophrenia
a deficiency of what neurons is associated with parkinsons? nigrostriatal dopaminergic neurons
behavior effects of excess DA can be reproduced by what agents? amphetamines (DA releaseing) and DA agonists (apomorphine)
what hormones released are DA mediated? anterior pitutary prolactin and GH
What zone does DA act on that produces N/V? chemoreceptor trigger zone
Amantadine? may stimulate release, may inhibit DA reuptake, does block NDMA glutamate receptors, which are stimulatory and thought to cause akinesis. has anticholinergic effects.
carbidopa? carbidopa-peripheral decarboxylase inhibitor to allow more L-dopa to reach brain to decrease peripheral side effects. does not cross BBB
levodopa? gets into CNS, rapid decarboxylation, may increase DA release, or exog DA flooding the synapse and upregulate DA receptors
carbidopa/levodopa (sinomet) effects? nausea (excess DA in periphery), postural hypotension, motor fluctuations, dyskinesias (related to chronic therapy; peak dose chorea, cranio cervical dystonia, biphasic limb dystonia, mental changes)
dopamine agonists (D2 selective)? apomorphine, bromocriptine, cabergoline, pergolide, pramipexole, ropinrole. (ropinrole and pramipexole most selective, least overlapping, start at low dose, can cause schit-like symptoms)
apomorphine? D1 and D2 agonist with short 1/2 life. given SC with a continuous pump. response identical to levodopa
bromocriptine? ergotamine derivative, risk of retroperitoneal/pleuropulmonary fibrosis, reduce BP and inhibit baroreceptor reflex with postural change. Used with sinomet to minimize L-dopa phenomenon long term.
cabergoline? ergotamine derivative, longer 1/2 life, less motor fluctuation, high rates of adverse effects (hallucination, confusion, dementia, gastritis, pulmHTN)
Pergolide? ergotamine derivative
pramipexole? non-ergotamine, 8 hour 1/2 life, renal elimination, adverse effects (somnolence 27% of pts, sleep attacks or narcolepsy, but rare)
ropinrole? nonergotamine, 1/2 life 6 hours, hepatic metabolism. adverse effects: nausea and hallucinations common, sedation and sleep attacks
selegeline? irreversible MAO B inhibitor: metabolized to amphetamine and methamphetamine. Used in ADD, tourettes. controversial increased mortality. adverse effects: mood changes, dizziness, N/V, dyskinesias
Tolcapone? periph and central COMT inhibitor, adjunct tx for wearing off L-dopa. side effects: explosive diahrea, urine discoloration, DA effects, hepatotoxicity (monitor LFT's)
entacapone? peripheral COMT inhibitor, adjunct tx to sinomet, side effects: diarrhea, orthostatic hypotension, dyskinesia, hallucination, confusion, hyperreflexia, NO liver toxicity
schitzophrenia drug Tx? DA antagonists: thioridazine, haloperidol (can cause PD like symptoms
Parkinsons Disease tx? dopamine enhancement: levodopa, carbidopa, selegiline, bromocriptine. give anticholineric/antimuscarinic, DA agonist or MAO inhibitor
Prolactin tx? DA agonist to inhibit prolactin secretion: bromocriptine
Nausea and vomiting Tx? antagonists: metoclopramide
What is PD? degenerative disease of basal ganglia causing loss of DA, with relative excess of Ach (increase in cholinergic activity)
how do you go about tx newly dx PD? start with antimuscarinic, then sinomet, then D2 selective then entacapone
Created by: lmh9p4
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