Sedative Hypnotics Flashcards
classification of sedative-hypnotic Drugs
MN BOOBS
Melatonin Receptor agonists
Non Benzo Benzo-Receptor Agonists (NBBRAs)
Benzodiazepines Older Sedative Hypnotics Others: beta blockers, alpha 2 agonists, antihistaminics Barbiturates Serotonin 5-HT1A partial agonists
what are the benzodiazepines
DMC FLOATT
Diazepam
Midazolam
Clonazepam
Flurazepam Lorazepam Oxazepam Temazepam Triazolam
mechanism of action of benzodiazepines (name them)
diazepam, midazolam, clonazepam, flurazepam, lorazepam, oxazepam, temazepam, triazolam
bind to GABA-A receptors at an allosteric site as a positive allosteric modulator –> activates GABA’s inhibitory actions –> opens Cl channels –> influx of Cl –> hyperpolarization –> inhibits triggering of action potential
what are the agonists of benzodiazepine receptors and what effects do they lead to
All the benzos plus the Non-benzo benzo receptor agonist (NBBRAs)
anxiolytic and anticonvulsant effects
name the benzodiazepine receptor antagonist and its effects
Flumazenil
blocks action of benzos and NBBRAs
what are inverse agonist and its effect
act as negative allosteric modulators of GABA receptor function –> anxiety and seizures
action of benzos
Sedation
Anti convulsants
Anesthesia
Muscle relaxation
classify the benzos in terms of length of action
Long acting (1-3 days): Diazepam and Flurazepam Intermediate acting (10-20 hrs): Lorazepam, Alprazolam, Temazepam Short acting (3 - 8 hrs): Oxazepam and Triazolam
what do benzos undergo when being metabolized
Phase I: done by CYP3A4
Phase 2: conjugation to glucuronides to be excreted in urine
which benzos don’t undergo the phase I of metabolism and its importance
LOT
Lorazepam, Oxazepam, Temazepam
their metabolism is not affected by liver disease since they skip phase I with CYP3A4 and go right into conjugation to glucuronides
benzo used in muscular disorder and why
benzo is a muscle relaxant
Diazepam is used in skeletal muscle spasms and spasticity from degenerative disorders such as MS and Cerebral Palsy
benzos used in seizures
Clonazepam: some types of epileptic seizures
Lorazepam: status epilepticus
benzos used in management of alcohol withdrawal
DOCC for Ethanol
Diazepam
Oxazepam
Chlordiazepoxide
Clorazepate
benzos prescribed for sleep disorders
Flurazepam
Temazepam
Triazolam
AE of benzos
Drowsiness and confusion
Ataxia
Cognitive impairment
Psychological effects
what is the benzo antagonist and what is it used for
Flumazenil
reverse CNS effects caused by benzo overdose
barbituates used as sedative-hypnotics
Phenobarbital
Pentobarbital
Thiopental
mechanism of barbiturates used as sedatives (name them)
phenobarbital, pentobarbital, thiopental
- potentiates effects of GABA by increase duration of GABA gated chloride channel opening
- block glutamate receptors
- block high frequency Na channels
action of barbiturates in sedative hypnotics
CNS depression
Respiratory depression
Enzyme induction
therapeutic uses of barbiturates (aka name what each drug is used for)
- Thiopental - Anesthesia
- Phenobarbital - anticonvulsant; treat hyperbilirubinemia and kernicterus by increasing glucuronyl transferase and bilirubin binding Y protein activity
AE of barbiturates (name them)
phenobarbital, thiopental, pentobarbital
CCP3 RAPs in HHD
CNS effects (drowsiness, sluggishness etc)
CYP450 induction
Paradoxical excitement (opp of expected)
Pulmonary insufficiency –> resp depression
Porphyrin Synthesis
Respiratory Depression
Addiction
Poisoning (lead to death)
Heart collapse
Hypersensitivity (allergic rxn)
Drug hangover (effects seen after sleeping)
contraindication of barbiturates (name them)
thiopental, pentobarbital, phenobarbital
- Pulmonary insufficiency –> resp depression
- Due to porphyrin synthesis, acute intermittent porphyria, variegate porphyria, hereditary copropporphyria, or symptomatic porphyria
what are the non-benzodiazepine benzodiazepine receptor agonists (NBBRAs)
Zolpiden
Zaleplon
Eszopiclone
mechanism of non-benzo benzo receptor agonists (NBBRAs) (name them)
zolpiden, zaleplon, eszopiclone
act on BZ1 subtype of benzodiazepine receptors which contain alpha 1 subunit
what antagonizes zolpiden
flumazenil - benzo receptor antagonist
clinical use of Zolpiden
short term treatment of insomnia characterized by difficulty initiating sleep
what metabolizes Zaleplon
aldehyde oxidase and CYP3A4
clinical use of Eszopiclone
insomnia –> decreases sleep latency and improves sleep maintenance
what is the serotonin 5-HT1A partial agonist
Buspirone
action of 5-HT1A partial agonist and what it is used to treat
anxiolytic
anxiety disorders or short term relief of anxiety
what is the melatonin receptor agonist and its mechanism
Ramelteon - MT1 and MT2 melatonin receptor agonist
what is melatonin receptor agonist used for
Ramelteon
insomnia characterized by difficulty with sleep onset
AE of Ramelteon
decrease in testosterone
increase in prolactin
what are the older drugs that were used as sedatives
Chloral Hydrate
Meprobamate
Paraldehyde
what are the other classes of sedatives
alpha 2 agonist: Clonidine
beta blocker: Propanolol (specific situational phobias and performance anxiety)
histamine receptor blockers: Diphenhydramine, Doxylamine, Hydroxyzine
