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31 Cards in this Set

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All sedative/hypnotics can cause CNS depression progressing to death except?
BDZ's

BDZ's can cause death in presence of other sedative hypnotics
This drug class has reasoable seperation between anxiolysis and sedation
BDZ's
BDZ's volume of distribution
High lipid distribution, but also high plasma binding, so volume of distribution is lower than expected (1-3 L/kg)
BDZ adsorption and excretion
Fully absorbed orally and metabolized be the liver. Half life from 6 hrs to 1 days (liver disease can extend)
Mechanism of action: BDZ
Binds to GABA receptors and increases Cl influx causing inhibition. Preference for brain, due to subunit variation. No effect without GABA stimulation (unlike others)
subunit specificity
alpha 1 - sedation
alpha 2 - anxiolytic
BDZ peripheral effects
respiratory problems in those with COPD and OSA

no analgesia

Effects like drinking alcohol
BDZ dependence
Mostly psychological, not physical.

Less withdrawl with long acting BDZ's

Tolerance develops to all symptoms except anxiolytic
BDZ's used for insomnia
Flurazepam (long T1/2, little hangover)

Temazepam (med. T1/2, no hangover)

Estazolam (short T1/2, early moring wakening)
Florazepam
Long T1/2 used to treat insomnia

Redistribution leads to little hangover, but morning levels still like DWI

Tolerance develops after 3 weeks
Long acting BDZ for tx of insomnia
Flurazepam
Temazepam
Intermediate action for tx of insomnia

Refreshing in morning, but DWI levels presist if a high dose was used
Intermediated BDZ for tx of insomnia
Temazepam
Estazolam
Short acting BDZ for insomnia

May cause early morning awakenings
Short acting BDZ for tx of insomnia
Estazolam
Zolpidem
Not BDZ but acts at alpha subunit. T1/2 of 1.5 hours so can be readministered during the night without risk of OD
Non BDZ with short half life used to tx insomnia
Zolpidem
BDZ used for anxiety
Alprazolam, Clonazepam and Lorazepam

Lont t1/2 in divided doses for low steady levels
Midazolam
Used as preanesthetic to reduced anxiety
Used as preanesthetics to reduce pre-op anxiety
Midazolam or Lorazepam
Tx for absence seizures
Clonazepam
Clonazepam
Used for tx of anxiety and abscence seizures
BDZ used for muscle spasticity
Diazepam
Flumazenil
BDZ antagonist with short T1/2

May need repeat administration for tx of long acting BDZ.

Binds to same site but without effect
Buspirone
anxiolytic only! without sedation, muscle relaxant ect.

No side effects, tolerance, withdrawl

Agonist for 5-HT receptors
Phenobarbital
Very long T1/2 (days) used as anticonvulsant

Powerful induction of P450

Has lower GABA independent effects than other barbits
Thiopental
very short acting used for anesthesia

T1/2 - 10 mins
Side effects of barbituates not common to BDZ's
hyperalgesia
Barbituates effects at GABA receptors
Effects Cl transmission, but at high doses induces Cl tranmission even without GABA
Disulfiram
Prevent conversion of acetaldehyde to acetic acid. Makes alcoholics feel sick when drinking

May cause encephalopathy in patients exposed to Pb and Ni
Alcohol withdrawl symtoms and tx
Delerium tremens

Tx with BDZ's, rehydrated, electrolytes and carbamazepine for seizure