Benzodiazepines: allosteric binding site

that binds to a site adjacent to the GABA

receptor to increase the influx of Cl- ions
resulting in hyperpolarization =
inhibition of neural stimulus. Highly lipid
soluble cross barriers easily. Cross
placenta secreted in breast milk. Hepatic
metabolism. Oxidation, hydroxylation,
conjufation w/ glucoronic acid (exc. Lore
and oxa). Drowsiness and confusion,
ataxia if high doses, cognitive
impairment, potentiate alcohol and other
CNS depresents. Withdrawl can occur:
anxiety, insomnia, irritability, muscle
weakness. Longer halflife= lower
symptoms. Use titration to wean them
off the drug. Decreased responsiveness
after continuous exposure. Cause
dependence if given long term.
Short Acting: OXAZEPAM: use for elderly,
hepatic disease, no metab.
Intermediate Acting:
Lorazepam: use for elderly, hepatic
disease, no metab.
Alprazolam:
Long Acting:
Chlordiazepoxide:
Diazepam:
Clorazepate: dont use in liver disease
ANTAGONIST: Flumazenil: comp
antagonizes BDZs. BDZ overdose,
reversal of sedative effects produced by
BDZs. Anesthesia, diagnostic,
therapeutic procedures
Azapirones: Buspirone: mediated by
serotonin receptors 5HT1a>autoreceptors coupled to G proteins
regulating K+ membrane channels.
Increase opening causes
hyperpolarization. Partial agonist.
Selevtive anxiolytic effect. Adv: NO:
physical dependence, withdrawl,
potentiation of CNS dep and alcohol,
cross tolerance with BDZs, muscle
relaxation or anticonvulsant. Low SE
(headache, dizzy), Use long term
therapy. Disadv: slow OA, 2wks.
SSRI: inhibit serotonin reuptake at
trasporter by blocking major NT removal.
Adv: same as above. Disadv. Same as
above. Highly protein bound. Met. In
liver (cimetidine may increase t1/2). CNS:
Insomnia, tremor. CV: palpitations,
postural hypotension, vasodilation GI:
anorexia, N.V.D GU: loss of libido, sexual
dysfunction. Monoamine Oxidase
Inhibitors: can be fatal, wait 14 day
intervals in between two drugs>hyperthermia, muscle rigidity,
myoclonus and rapid mental changes
(increase in tricyclic antidepressents due
to met inhibition). Tryptophan: serotonin
precursor. Warfarin: increased bleeding.
Paroxetine: social anxiety disorder.
Sertraline: PTSD-(kids too)
Escitalopram
SNRI: blocks both serotonin and NE
reuptake. General anxiety disorder.
Similar to SSRI, may cause HTN. Slowly