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Autonomics-1.3
Pharmocology-Autonomics1.3/DA
| Question | Answer |
|---|---|
| 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 |