Pharmocology-Autonomics1.3/DA
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| known functions are mediated by what receptor family? | D2
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| D2 receptors are implicated in what disease? | schitzophrenia
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| a deficiency of what neurons is associated with parkinsons? | nigrostriatal dopaminergic neurons
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| behavior effects of excess DA can be reproduced by what agents? | amphetamines (DA releaseing) and DA agonists (apomorphine)
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| what hormones released are DA mediated? | anterior pitutary prolactin and GH
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| What zone does DA act on that produces N/V? | chemoreceptor trigger zone
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| Amantadine? | may stimulate release, may inhibit DA reuptake, does block NDMA glutamate receptors, which are stimulatory and thought to cause akinesis. has anticholinergic effects.
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| carbidopa? | carbidopa-peripheral decarboxylase inhibitor to allow more L-dopa to reach brain to decrease peripheral side effects. does not cross BBB
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| levodopa? | gets into CNS, rapid decarboxylation, may increase DA release, or exog DA flooding the synapse and upregulate DA receptors
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| 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)
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| 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)
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| apomorphine? | D1 and D2 agonist with short 1/2 life. given SC with a continuous pump. response identical to levodopa
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| 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.
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| cabergoline? | ergotamine derivative, longer 1/2 life, less motor fluctuation, high rates of adverse effects (hallucination, confusion, dementia, gastritis, pulmHTN)
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| Pergolide? | ergotamine derivative
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| pramipexole? | non-ergotamine, 8 hour 1/2 life, renal elimination, adverse effects (somnolence 27% of pts, sleep attacks or narcolepsy, but rare)
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| ropinrole? | nonergotamine, 1/2 life 6 hours, hepatic metabolism. adverse effects: nausea and hallucinations common, sedation and sleep attacks
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| 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
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| 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)
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| entacapone? | peripheral COMT inhibitor, adjunct tx to sinomet, side effects: diarrhea, orthostatic hypotension, dyskinesia, hallucination, confusion, hyperreflexia, NO liver toxicity
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| schitzophrenia drug Tx? | DA antagonists: thioridazine, haloperidol (can cause PD like symptoms
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| Parkinsons Disease tx? | dopamine enhancement: levodopa, carbidopa, selegiline, bromocriptine. give anticholineric/antimuscarinic, DA agonist or MAO inhibitor
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| Prolactin tx? | DA agonist to inhibit prolactin secretion: bromocriptine
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| Nausea and vomiting Tx? | antagonists: metoclopramide
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| What is PD? | degenerative disease of basal ganglia causing loss of DA, with relative excess of Ach (increase in cholinergic activity)
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| how do you go about tx newly dx PD? | start with antimuscarinic, then sinomet, then D2 selective then entacapone
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