Antianxiety Agents, Muscle Relaxants, Sedative Hypnotics & Alcohol Flashcards
Chlordiazepoxide (LIBRIUM)
Benzodiazepine.
PO, IM, IV
Long acting
Active metabs
Anxiolytic
Anticonvulsant
Withdrawal suppressant
Alprazolam (XANAX)
P.P.
Intermediate duration
No active metabolites
Anxiolytic
Diazepam (Valium)
A benzodiazepine.
PO, IM, IV
LONG ACTING
active metabs
Anxiolytic Anticonvulsant Anesthesia supplement Withdrawal suppressant Muscle relaxant
Lorazepam (Ativan)
A benzodiazepine.
PO, IM, IV
intermediate acting
No active metabs
Hypnotic
Anxiolytic
Anesthesia supplement
Withdrawal suppressant
Midazolam (Versed)
A benzodiazepine.
IV
SHORT ACTING
No active metab
Induction or supplement to anesthesia
Termazepam (Restoril)
A benzodiazepine.
PO
Intermediate acting
No active metab
Hypnotic
Triazolam (Halicon)
A Benzodiazepine.
PO
Short acting
No active metab
Hypnotic
Flumazenil (romazicon)
A benzodiazepine antagonist.
Use: reverses the CNS depressant effects of benzodiazepines particularly those use for surgical anesthesia such as Midazolam; Also used to tx benzo poisoning.
SE:
Can trigger seizures esp in epileptic patients or those currently dependent on benzos, barbs, or ETOH.
Can cause sxs of withdrawal in it and addicts.
Butalbital (florinal)
A barbiturate.
Intermediate/ short acting
Used mainly as sedative-hypnotics.
Pentobarbital ( Nembutal)
A barbiturate.
Intermediate/ short acting
Used mainly as sedative-hypnotics.
Phenobarbital
A barbiturate
Long-acting
Used mainly as anticonvulsants.
Thiopental (Pentothal)
A barbiturate.
Ultra short acting.
Balcofen (Lioresal)
Centrally acting muscle relaxant.
Analog of GABA that acts at GABA-B receptors –> acts in spinal cord to inhibit the release of excitatory transmitters & thus inhibits spasmogenic reflexes.
Use: tx spasticity from MS, spinal cord injuries, etc.
SE: CNS depression, before you, hallucinations, tremors, and seizures. Some degree of dependents me results from chronic use.
Cyclobenzaprine (Flexaril)
Centrally acting muscle relaxants.
Tx muscle spasms of local origin (sprains, strains)
SE: CNS depressing effects.
Diazepam (Valium)
A centrally acting muscle relaxant.
MOA: act at the levels of the brain stem and spinal cord where they modify the reflex arcs that modulate skull to muscle contraction.
Tx spasticity & acute muscle spasm.
Enhances presynaptic inhibition by facilitating the actions of GABA in the spinal cord.
Metaxalone (Skelaxin)
A centrally acting muscle relaxant.
Tizanidine (Zanaflex)
A centrally acting muscle relaxant.
Alpha 2 agonist.
SE: hypotension, sedation
Alcohol
Anxiolytic and sedative – hypnotic agent.
Over 90% of consumed alcohol is oxidized in the liver; the rest is excreted through the lungs and kidneys. Alcohol oxidation follows zero order kinetics – a constant amount is oxidized at a constant rate. A typical adult metabolizes 7-10 g of alcohol per hour (one drink).
Alcohol dehydrogenase pathway
ETOH–>acetaldehyde (toxic)
MEOS
ETOH–>acetaldehyde
Acetaldehyde metab
Acetaldehyde –>acetate–>H2O+ CO2
(Aldehyde dehydrogenase)
Graded depression of CNS
Release of inhibitions–> Anxiolytic effect–> sedation–> hypnosis–>anesthesia–> resp depression–> coma–> death
ETOH has a very steep dose response curve.
Depresses respiration and may cause respiratory arrest. And goal is to prevent or treat severe respiratory depression.
Effects on sleep:
Reduces sleep latency. Reduces the time spent in REM sleep and decreases the overall quality of sleep.
Overdosed treated w/ benzodiazepines
More content in notes.
Buspirone (Buspar)
An anxiolytic and sedative hypnotic agent.
Alleviates mild to moderate anxiety with minimal sedative – hypnotic, muscle relaxant, or respiratory depressant effects. takes one to two weeks to work.
Does not act through GABA mechanisms. May be a partial agonist at serotonin receptors.
Has very low abuse potential. Does not exhibit cross tolerance or cross dependence with the benzo’s, barbiturates, or alcohol. it’s cannot suppress the symptoms of alcohol withdrawal.
The drug of choice for the treatment of anxiety in patients with a history of alcohol or sedative abuse who have been brought through the acute withdrawal face.
Eszopiclone (Lunesta)
Long acting (6-8hrs) Helps to sleep
SEs: CNS depression, complex behaviors while unconscious (sleep driving, sleep eating, etc).
Less suppression of REM sleep & to produce less rebound insomnia (when discontinued) than benzos.
Non-benzo.
Enhances effects of GABA at the benzo receptor – Cl channel complex by interacting with the subtype of the benzo receptor.
Use: Anxiolytic and sedative – hypnotic agent.
Metab by liver- potential for drug interactions.
Drug interactions w/ other CNS depressants.
Gammahydroxybutyrate (GHB)
Anxiolytic and sedative – hypnotic agent.
Analog of GABA that can cross the BBB.
Use:
1. Ergogenic effect- abused by athletes
2. Date rape drug
High dose use can cause seizures & CNS depression –> coma & death
Chronic use can inducd. State of dependence
Melatonin
Anxiolytic and sedative – hypnotic agent.
Hormone produced by the pineal gland. Agonist at melatonin receptors.
Ramelton (Rozerem)
Anxiolytic and sedative-hypnotic agent.
Used w/ caution in Pts w/ impaired lived function.
Zolpidem (Ambien)
Long acting (6-8hrs) Helps to sleep
SEs: CNS depression, complex behaviors while unconscious (sleep driving, sleep eating, etc).
Less suppression of REM sleep & to produce less rebound insomnia (when discontinued) than benzos.
Non-benzo.
Enhances effects of GABA at the benzo receptor – Cl channel complex by interacting with the subtype of the benzo receptor.
Use: Anxiolytic and sedative – hypnotic agent.
Metab by liver- potential for drug interactions.
Drug interactions w/ other CNS depressants.
