Q3 Anxiolytics and Hypnotics Flashcards
a key component of anxiety seems to be hyperactivity of circuits in the _______
- amygdala
in amygdala circuit, serotonin stimulates what
- depolarization of glutaminergic neurons
- release glutamate into the amygdala
negative input of amygdala circuit
- GABAergic neurons inhibit or lower rate of firing of glutaminergic
the names of benzodiazepines end in ____ or ____
except
- lam or -pam
- except chlordiazepoxide
serotonin and glutamate ______ the rate of firing of ____synaptic neurons by binding to and activating corresponding response on the ____ synaptic neuron cell surface and promoting ________
- increase
- post synaptic
- post synaptic
- depolarization
GABA ______ the rate of ____synaptic neuron firing by promoting _________ of the _____synaptic neuron
- decreases
- post
- hyper polarization
- post
the post-synaptic GABA receptor is a ____ ion channel
this results in what
- Cl-
- hyperpolarization
MOA of benzodiazepines
- bind the GABA receptor in a different part than GABA binds. DO NOT OPEN CHLORIDE ION CHANNEL
- alters conformation of GABA channel so GABA can be more potent
- enhance inhibitory effect of GABA
benzodiazepines increase the ______ of GABA but do not increase its ______
- potency
- effectiveness
toxicities of benzodiazepines
if combined with alcohol
- psychomotor impairment
- respiratory depression
with extended use of benzodiazepines, patients may develop
why
how do you compensate
- tolerance
- brain increases release of glutamate from presynaptic neurons and expression of glutamate receptors on postsynaptic neurons
- increase drug levels
drugs that stimulate _______ release into the ________ are addictive
what pathway is this (where does it begin)
- dopamine
- nucleus accumbens
- mesolimbic (begins in VTA)
how do benzodiazepines cause addiction in mesolimbic pathway
- inhibit release of GABA onto dopaminergic neurons
- promotes more release of dopamine into nucleus accumbens
other indications for benzodiazepines
- insomina
- alcohol withdrawal
- surgical anesthesia
- seizures (status epilepticus)
effect of chronic ethanol use on glutamate
what about on GABA receptors
- increases glutamate release and receptor expression
- decreases GABA receptors
how do benzodiazepines help with alcohol withdarw
- reduce the effects of excessive glutamate stimulation
symptoms of alcohol withdrawal 0-24 hours
- anxiety
- GI upset
- tremors
symptoms of alcohol withdrawal 24-48 hours
- alcoholic hallucinosis
symptoms of alcohol withdrawal 2-5 days
- seizures
symptoms of alcohol withdrawal 3-7 days
- delirium tremes
reversal agent of benzodiazepines
MOA
- flumazenil
- competitive blocks binding of drug to GABA receptor
benzodiazepines are synergistic with
how
- alcohol
- CNS depressants
- alcohol and CNS depressants promote opening of GABA receptor chloride channel
the drugs with shortest times to onset are those that are the most
why
- hydrophobic
- can cross blood brain barrier
how do benzodiazepines produce sedation
- metabolized into active metabolites that produce sedation
- bind to different GABA-A receptors
