CNS Drugs Flashcards
Name the barbiturates
phenobarbital, pnetobarbital, thiopental, secobarbital
Mechanism of barbiturates
facilitate GABAa action by increasing duration of Cl- channel opening, thus decrease neuron firing (increases duration)
Contraindication of barbiturates
in porphyria
Use of barbiturates
sedative for anxiety, seizures, insombia, induction of anesthesia (thiopental)
Toxicity of barbiturates
respiratory and cardiovascular depression
CNS depression (EtOH exacerbated)
INDUCES cytochrome p450
Overdose tx of barbiturates
supportive (assist respiration and maintain BP)
Name the benzodiazepines
diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, clordiazepoxide, alprazolam
Mechanism of benzodiazepines
facilitate GABAa action by increasing frequency of Cl- channel opening
decreases REM sleep
Name the benzos with short-half lives and NO active metabolites
Alprazolam, triazolam, oxazepam, midazolam –> higher addictive potential
Use of benzodiazepines
anxiety, spasticity, status epilepticus, detoxification (especially alcohol withdrawal and DTs), night terrors, sleepwalking, general anesthetic (amnesia, muscle relaxation), hypnotic (insomnia)
Which benzos used for status epilepticus?
lorazepam and diazepam
Toxicity of benzodiazepines
dependence, additive CNS depression effects with alcohol
less risk of respiratory depression and coma than with barbiturates
Overdose tx for benzos
with flumazenil (competitive antagonist at GABA benzodiazepine receptor)
Name the non-benzo hypnotics
zlopidem, zaleplon, esZopiclone
Mechanism of the non-benzo hypnotics
act via the BZ1 subtype of the GABA receptor
effects reversed by flumazenil
Use of non-benzo hypnotics
insomnia
Toxicity of non-benzo hypnotics
ataxia, headaches, confusion
short duration because of rapid metabolism by liver enzymes
only cause modest day-after psychomotor depression and few amnestic effects
decreased dependence risk than benzos
Name the dopamine agonists
ergot - bromocriptine
non-ergot (preferred) - pramipexole, ropinirole
Parkinson disease NT levels
loss of dopaminergic neurons and excess cholinergic activity
Name drug that increases dopamine availability
Amantadine
Mechanism of amantadine
increase dopamine release and decrease dopamine reuptake
Uses for amantadine
PARKINSON
antiviral against influenza A and rubella