Anixety,hypnotics,alcohol Flashcards
Which drug is not a CNS depressant?
Buspirone
Which drugs have steep dose-response curves?
Alcohol, barbiturate
What is major advantage of using benzodiazepines over barbiturates?
Bzds have a very shallow dose response curve, least likely to be fatal in overdose.
BZD are used to treat what conditions?
Anxiety in limbic system
Sedative/hypnotic in reticular activating system
Anticonvulsants in cerebral cortex
Muscle relaxation in internuncial polysynaptic reflexes in brainstem and spinal cord.
The MoA of BZD is?
BZD enhance the inhibitory effect of GABA. They bind to a separate receptor GABAa. GABA also must be present. Binding results in the opening of chloride channels. The influx of chloride causes a hyperpolarization and decreases neuronal firing.
Which BZDs can cause rebound anxiety?
Short acting such as triazolam.
Respiratory depression is associated with which BZD?
Midazolam used to induce surgical anesthesia
Cross tolerance and cross dependence occurs between what drug classes?
BZDs, barbiturates, and alcohol.
What are some signs of BZD toxicity?
Sedation, drowsiness, lightheaded, confusion, psychomotor impairment, slurred speech, ataxia, memory impairment, anterograde amnesia, increased aggression, euphoria, hangover.
What are signs of BZDs withdrawal?
Agitation, anxiety, irritability, insomnia, ab cramps, sweating, Seizures.
Treatment is weaning off by 10% every 3 days over 2-3 weeks.
BZDs alter sleep patterns in what ways?
Decrease latency, duration of stage 3/4, number of awakenings, duration of REM sleep.
Cessation can cause REM rebound resulting in increased frequency and intensity of dreams
If a person has trouble falling asleep, which BZD would help?
Triazolam
May cause rebound anxiety.
If a person has trouble staying asleep, which BZD is used?
Flurazepam
May cause hangover effect
Redistribution of which BZD is important for termination of drug action?
Diazepam
Which BZDs are not oxidized by the liver and therefore may be usedin patients with impaired liver function?
Lorazepam, oxazepam
How do BZDs differ from Barbs in respect to metabolizing liver enzymes?
BZD do not induce enzymes, barbs do.
What drugs can prolong action of BZDs?
Cimetidine, disulfiram, isoniazide
BZDs can increase the serum levels of?
Digoxin, phenytoin
Which drug is used to induce anesthesia?
Midazolam
Which BZDs are used for hypnotic effect?
Triazolam, temazepam, oxazepam, lorazepam
Which BZDs are used for anxiety?
Oxazepam, lorazepam, alpeazolam, clorazepate, chlordiazepoxide, diazepam
Which BZDs are used to suppress withdrawal?
Lorazepam, chlordiazepoxide, diazepam
Which BZDs is also a muscle relaxant?
Diazepam
Which barb is long acting and used as anticonvulsant?
Phenobarbital
Which barbs are used for sedative/hypnotic effects?
Pentobarabital, butalbital
Which barb is ultra short acting?
Thiopental
How is the MoA of barbs different from BZDs?
Barbs have ability to open chloride channels without GABA presence.
How to barbs differ from BZDs in terms of side effects?
Barbs suppress REM sleep more, REM rebound, hangover effect, respiratory depression.
Most barbs induce state of surgical anesthesia.
Redistribution is important for the termination of which barb?
Thiopental
Aggravation of acute intermittent porphyria is associated with which drug class?
Barbiturates
Phenbarbital can interact with which drug’s effect?
Warfarin
MAOI enhance CNS depression with which drug class?
Barbiturates
Which drug class canbe used as adjuncts for tension headache?
Barbiturates
Which drug is used for mild/moderate anxiety with minimal sedative/hypnotic, muscle relaxant, or respiratory depression effects?
Buspirone
How long for treatment with buspirone until effects are seen?
1-2 weeks
What is buspirone MOA?
Thought to be a partial agonist at 5-HT1a
What drug is a good choice to treat anxiety in patients with a history of alcohol or sedative abuse?
Buspirone
Buspirone interacts with MAOI and causes what?
Hypertension
Which drugs are thought to interact with BZD receptors, subtype omega-1, enhancing GABA effects?
Zolpidem, zaleplon, eszopiclone
Of zolpidem, zaleplon, eszopiclone which are long and which are short acting?
Zolpidem, eszopiclone are long acting.
Zaleplon is short acting
Which drug is an analog of GABA?
Gammahydroxybutyrate, GHB
Which drug has ergogenic effects, used by athletes?
GHB
Which antihistamine also has anti anxiety effects?
Hydroxyzine
Which drug acts as an agonist at melatonin receptors?
Ramelteon
What are cautions with use of ramelteon?
Impaired liver function patients
Increase prolactin, decrease testosterone.
Which drugs are useful for situational anxiety?
Beta blockers such as propranolol
Wch drug is an BZD antagonist, and reverses the CNS depressant effects?
Flumazenil
What is the major adverse effect of flumazenil?
Can trigger seizures, and preciptate withdrawal symptoms
The most effective muscle relaxants act at brainstem and spinal cord, which are they?
Diazepam, baclofen
Which drug is used to treat spasticity from MS, spinal cord injury
Baclofen
Which drug is an analog of GABA and acts as an agonist at GABAb ceptors?
Baclofen
Which muscle relaxant is structurally similar to tricyclic antipressants?
Cyclobenzaprene
What drug acts at brainstem to inhibit both GABA and alpha motor systems?
Cyclobenzaprene
Which muscle relaxant is used for muscle spasms of local origin?
Cyclobenzaprene
Which drug is an alpha-2 agonist used for skeletal muscle relaxation?
Tizanidine
What side effect is seen with tizanidine?
Hypotension
What follows zero order kinetics, metabolism is independent of time or concentration?
Alcohol
Alcohol dehydrogenase pathway is responsible for?
Dvelopment of acetaldehyde accumulation causing toxic effects
The microsomal ethanol oxidizing system is responsible for?
Alcohol tolerance, system is induced by chronic alcohol consumption
Which drug is an inhibitor of aldehyde dehydrogenase?
Disulfiram
What reaction occurs when alcohol is consumed with disulfiram?
Flushing, headache, nausea, confusion.
Drug is also hepatotoxic.
The initial phase of alcohol appears to be stimulatory, why?
Due to pression of inhibitory mechanisms in the brain
What is alcohol MoA inthe CNS?
Disorder of membrane lipids
Secondary change to neurotransmitter, receptor, ion channel
Enhance GABA effects
How does alcohol have a diuretic effect?
It inhibits the secretion of ADH
Alcohol can contribute to erosive gastritis by?
Stimulating secretion of gastric acid concentration
Which drug is given during alcohol withdrawal for autonomic effects?
Clonidine
Which drug is used to control seizures during alcohol withdraw?
Phenytoin
Which drug is used tocontrol hallucinations during alcohol withdraw?
Haloperidol
Which opioid antagonist is usedto reduce alcohol cravings?
Naltrexone
What drug is usedto reduce alcohol cravings, and help maintain abstinence in recovering alcoholics?
Acamprosate
Which drug is preferred for alcoholics with liver impairment?
Acamprosate
