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27 Cards in this Set
- Front
- Back
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Sed-hyp metabolism
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most but NOT ALL:
metabolized by CYP3A4 & CYP2C19 ALL: conjugated to form glucuronides (urine) |
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Metabolites accumulate
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diazepam, flurazepam
This can lead to excessive sedation (HAVE A FLOWERY DAY WITH ACCUMULATED METABOLITES) |
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Shorter half-lives
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oxazepam & lorazepam
they are conjugated directly Lo-ox (locks are quick) |
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rapid metablism in the liver
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zolpidem, zaleplon, eszopiclone
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MOA: benzodiazapine
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increase frequency of Gaba-mediated Cl- channel opening, which facilitates the inhibitory actions of GABA & depresses neuronal excitability
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Flumazenil
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antagonist at BZ receptors & reverses effects of BZ
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barbituates: MOA
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prolong effects of inhibitory neurotransmitters GABA and glycine (non-competitive, increase duration)
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BUSPIRONE
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selective anxiolytic, with min. CNS depressant effects
diff. mech than benzos |
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PD: sedation
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sedation with relief from anxiety--> all drugs in this class
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PD: hypnosis
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promotes sleep onset, increase duration of sleep, decrease REM
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PS: anesthesia
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loss of consciousness may occur at high doses, anterograde amnesia is more common with benzos
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PD: anticonvulsant w/ minimal sedation
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clonazepam & phenolbarbitol
(don't sedate or let seize clowns on barbed wire) |
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PD: muscle relaxation
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occurs at low doses
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Diazepam
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effective at sedative dose levels for spacticity, including cerebral palsy
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meprobamate
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some selectivity as muscle relaxant
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medullary depression
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high doses: medullary depression--> resperatory arrest, hypotension and cardiovascular collapse
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Tolerance leads to...
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down regulation of BZ receptors with a rapid rebound of BZ receptors when benzos are terminated
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dependance (physio) leads to...
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an altered state that leads to withdrawl state when discontinued
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signs of withdrawl?
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anxiety, tremors, hyperreflexia, seizures
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Greatest efficacy in panic disorders?
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Alaprazolam and clonazepam
(ALPINE CLIMBING) |
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Dependancy on ethanol or sedative-hypnotics?
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chlordiazpoxide, diazapam
(if your drinking to much you should jump in the pool and have a CHLORINE DAY) |
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Why dose sedation occur with benzos?
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it's due to changes in brain function, not in liver rate metabolism
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Additive effects?
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EtOH, antihistamine, antipsychotic, opioid, TCA
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Flumazenil in OD
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may reverse CNS depression with benzos, zolpidem, zaleplon... not not with others
ALSO, must be administered repeatedly |
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What inhibits benza metabolism ?
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ketoconazole, cimetidine, erythromycin, clarithromycin
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drug with the highest lipid solubility.... how used and why?
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thiopental, used in induction of anesthesia because it enters the CNS rapidly
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what to use to treat status epilepticus?
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lorazepam, diazepam, phenobarbitol (IV)
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