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31 Cards in this Set
- Front
- Back
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All sedative/hypnotics can cause CNS depression progressing to death except?
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BDZ's
BDZ's can cause death in presence of other sedative hypnotics |
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This drug class has reasoable seperation between anxiolysis and sedation
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BDZ's
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BDZ's volume of distribution
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High lipid distribution, but also high plasma binding, so volume of distribution is lower than expected (1-3 L/kg)
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BDZ adsorption and excretion
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Fully absorbed orally and metabolized be the liver. Half life from 6 hrs to 1 days (liver disease can extend)
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Mechanism of action: BDZ
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Binds to GABA receptors and increases Cl influx causing inhibition. Preference for brain, due to subunit variation. No effect without GABA stimulation (unlike others)
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subunit specificity
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alpha 1 - sedation
alpha 2 - anxiolytic |
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BDZ peripheral effects
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respiratory problems in those with COPD and OSA
no analgesia Effects like drinking alcohol |
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BDZ dependence
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Mostly psychological, not physical.
Less withdrawl with long acting BDZ's Tolerance develops to all symptoms except anxiolytic |
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BDZ's used for insomnia
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Flurazepam (long T1/2, little hangover)
Temazepam (med. T1/2, no hangover) Estazolam (short T1/2, early moring wakening) |
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Florazepam
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Long T1/2 used to treat insomnia
Redistribution leads to little hangover, but morning levels still like DWI Tolerance develops after 3 weeks |
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Long acting BDZ for tx of insomnia
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Flurazepam
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Temazepam
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Intermediate action for tx of insomnia
Refreshing in morning, but DWI levels presist if a high dose was used |
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Intermediated BDZ for tx of insomnia
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Temazepam
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Estazolam
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Short acting BDZ for insomnia
May cause early morning awakenings |
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Short acting BDZ for tx of insomnia
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Estazolam
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Zolpidem
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Not BDZ but acts at alpha subunit. T1/2 of 1.5 hours so can be readministered during the night without risk of OD
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Non BDZ with short half life used to tx insomnia
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Zolpidem
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BDZ used for anxiety
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Alprazolam, Clonazepam and Lorazepam
Lont t1/2 in divided doses for low steady levels |
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Midazolam
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Used as preanesthetic to reduced anxiety
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Used as preanesthetics to reduce pre-op anxiety
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Midazolam or Lorazepam
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Tx for absence seizures
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Clonazepam
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Clonazepam
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Used for tx of anxiety and abscence seizures
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BDZ used for muscle spasticity
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Diazepam
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Flumazenil
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BDZ antagonist with short T1/2
May need repeat administration for tx of long acting BDZ. Binds to same site but without effect |
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Buspirone
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anxiolytic only! without sedation, muscle relaxant ect.
No side effects, tolerance, withdrawl Agonist for 5-HT receptors |
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Phenobarbital
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Very long T1/2 (days) used as anticonvulsant
Powerful induction of P450 Has lower GABA independent effects than other barbits |
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Thiopental
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very short acting used for anesthesia
T1/2 - 10 mins |
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Side effects of barbituates not common to BDZ's
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hyperalgesia
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Barbituates effects at GABA receptors
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Effects Cl transmission, but at high doses induces Cl tranmission even without GABA
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Disulfiram
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Prevent conversion of acetaldehyde to acetic acid. Makes alcoholics feel sick when drinking
May cause encephalopathy in patients exposed to Pb and Ni |
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Alcohol withdrawl symtoms and tx
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Delerium tremens
Tx with BDZ's, rehydrated, electrolytes and carbamazepine for seizure |
