Neuro pharm 4
Terms
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- phenothiazines
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- tricyclic ring typicals
- binds D1 and D2
- includes Chlorpromazine, thioridazine, trifluoperazine, perphenazine, Prochlorperazine
- overdosing can be fatal in
thioridazine, mesoridazine
- most noted for CV SE's like prolonged QT - Chlorpromazine
- low potency phenothiazine, typical
- thioridazine
- low potency phenothiazine, typical
- trifluoperazine
- higher potency phenothiazine, typical
- perphenazine
- higher potency phenothiazine, typical
- Prochlorperazine
- phenothiazine that doesn’t pass BBB, so its only an anti-emetic, would be typical
- Butyrophenones
- Haloperidol, Pimozide, droperidol - typicals
- Haloperidol
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- typical partially selective for D2 vs D1
- only used in long-term psych care and acute situations where rapid control needed
– EP SEs are a big problem
– approved for Tourette's and severe ADHD - Pimozide
- typical very selective for D2 and used for Tourette's
- droperidol
- typical used w/ fentanyl for anesthesia until “black boxâ€
- Clozapine
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- 1st atipcal w/ minimal SEs
– v. effective, risk of agranulocytosis, so monitor blood
- may block D2, D4, 5-HT
– SE's sedation, wt gain, postural hypotension, anticholinergic effects, arrhythmias - Olanzapine
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- atypical like clozapine, but only causes but wt gain and can give /w amantadine in 1st month to reduce it
– gets (+) and (-) sx and – approved for of acute mania of bipolar
– also for agitation and psychotic sx in dementia (Alzheimer’s) - Risperidone
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- atypical that blocks HT2C and D2 – gets mesocortical tract and stops (-) sx
– SE's low unless > 6 mg/day, then highest risk of EP SEs - Quetiapine
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- atypical potent blocker of 5-HT2 and only mildly gets D2
- get (+) and (-) w/out EP SEs
- blocks H1 and α1 so wt gain, sedation and postural hypotension - Ziprasidone
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- atypical, better w/ wt gain and depressive Sx of SCZ
– inhibits S/NE reuptake, activates 5-HT1A, and blocks 5-HT1D
– greatest risk of prolonged QT - Aripiprazole
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- atypical, partial agonist at D2, 5-HT1A and blocks 5-HT2A, stabilizing D and S
– improves (+) and (-) sx
- EP sx low - EP SE's Tx
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- from too much GABA
- switch to atypicals, or give anti-muscarinic drugs
– try benztropine and trihexyphenidyl (they will act on PNS) - TD tx
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- from not enough GABA
- discontinue or reduce current ASY and try atypical
– discontinue drugs w/ ACh action in CNS, like antiparkinsonism drugs and TCI’s
– add benzodiazepine may enhancing GABA - Neuroleptic malignant syndrome (NMS)
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- in v. sensitive pts, esp w/ Haloperidol and phenothiazines
- 1st muscle rigidity, then severe motor dysfunction, hyperthermia, altered consciousness, leukocytosis, and elevated CP
- stop therapy, then give amantadine (indirect D agonist) and bromocriptine (direct D agonist)
– muscle relaxants, like diazepam and dantrolene, are often also helpful - ASY pharmokinetics
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- single daily dosing OK
- metabolized by p450