Sedative Hypnotic And Anxiolytic Drugs Flashcards
A 43-year-old man with severe hepatic cirrhosis requires a sedative for insomnia. Which of the following sedatives would be the best choice for this patient?
A
Phenobarbital
B
Diazepam
C
Lorazepam
D
Secobarbital
E
Flurazepam
C
Lorazepam
A 19-year-old college student has overdosed on phenobarbital. After standard supportive care, the physician in the ER should do which of the following to hasten the elimination of phenobarbital?
A
Acidify the urine
B
Acidify the blood
C
Alkalinize the blood
D
Alkalinize the urine
E
Use a drug to stimulate hepatic CYP 2C19
D
Alkalinize the urine
A 32-year-old woman is taking ramelteon for chronic insomnia. Ramelteon binds to
A
melatonin receptors M1 and M2.
B
muscarinic receptors M3.
C
nicotinic receptors.
D
α1-adrenergic receptors.
E
D2 dopaminergic receptors.
A
melatonin receptors M1 and M2.
A 43-year-old woman is prescribed a benzodiazepine for anxiety. The choice of which benzodiazepine to prescribe should be based on
A
volume of distribution.
B
plasma half-life.
C
protein binding.
D
the indications approved by the FDA.
E
creatinine clearance.
B
plasma half-life.
53-year-old man with 15 years of alcohol abuse has developed weakness in his legs and the onset of heart failure. The primary treatment is
A
digoxin.
B
metoprolol.
C
creatine.
D
abstinence from alcohol.
E
thiamine.
D
abstinence from alcohol.
A 33-year-old Japanese man becomes flushed and light-headed after one glass of wine. This reaction is likely due to
A
the rate he drank the glass of wine.
B
increased absorption of the alcohol.
C
inhibition of monoamine oxidase.
D
decreased renal excretion of alcohol.
E
a variant in aldehyde dehydrogenase.
E
a variant in aldehyde dehydrogenase.
Which of the following molecular processes best
describes the mechanism of action of benzodiazepines?
(A) potentiating the effect of GABA at chloride ion channels
(B) blocking glutamate excitation
(C) blocking the inactivation of sodium ion channels
(D) binding to opioid receptors to produce sedation
(E) potentiating the action of the inhibitory amino acid, glycine
(A) potentiating the effect of GABA at chloride ion channels
Benzodiazepines are noted for altering which one of the following aspects of sleep?
(A) increasing the time to sleep onset
(B) decreasing stage 2 NREM sleep
(C) increasing slow-wave sleep
(D) decreasing the REM stage of sleep
(E) increasing sleep awakenings
(D) decreasing the REM stage of sleep
Which one of the following statements best describes flumazenil?
(A) does not produce withdrawal seizures
(B) has the longest elimination half-life
(C) is not metabolized into an active agent
(D) is also used for the treatment of epilepsy
(E) is a selective benzodiazepine antagonist
(E) is a selective benzodiazepine antagonist
Zaleplon differs from zolpidem in which one of the following ways?
(A) produces withdrawal seizures
(B) has a shorter elimination half-life
(C) has a different chemical structure than benzodiazepines
(D) shows less tolerance to sedative effects
(E) produces greater morning sedation
(B) has a shorter elimination half-life
Which one of the following anxiolytic drugs is noted for its lack of sedation?
(A) hydroxyzine
(B) diazepam
(C) oxazepam
(D) alprazolam
(E) buspirone
(E) buspirone
Clinical antipsychotic potency for “typical” antipsychotics correlates with actions at which receptor?
(A) dopamine D2 receptors
(B) α2-adrenergic receptors
(C) muscarinic receptors
(D) histamine receptors
(E) serotonin
(A) dopamine D2 receptors
Which of the following agents is an antipsychotic that can improve both positive and negative symptoms of schizophrenia?
(A) chlorpromazine
(B) haloperidol
(C) thiothixene
(D) risperidone
(E) thioridazine
(D) risperidone
Which one of the following is not a class of antidepressant medications?
(A) SNRIs
(B) TCAs
(C) MAOIs
(D) acetylcholinesterase inhibitors
(E) SSRIs
(D) acetylcholinesterase inhibitors
The older TCAs share all of the following adverse effects except which one?
(A) orthostatic hypotension
(B) sedation
(C) seizures
(D) weight gain
(E) sexual dysfunction
(E) sexual dysfunction
Foods containing tyramine should be avoided when taken with which class of medications?
(A) TCAs
(B) MAOIs
(C) SSRIs
(D) atypical antidepressants
(E) antihypertensive medications
(B) MAOIs
A 38-year-old man is taking Tranylcypromine an MAO inhibitor, for depression. After a celebratory dinner, he develops a severe headache and chest pain. At hospital his blood pressure is 190/135 mm Hg. His hypertensive crisis is likely due to the ingestion of
A. Green salad
B. Chocolate cake
C. Red wine
D. Broiled salmon
E. Wheat bread
C. Red wine
A 32-year-old woman is taking sertraline for mild depression. This drug increases the availability of serotonin (5-HT) at the postsynaptic membrane because it
A. Stimulates 5-HT4 receptors
B. Enhances the release of 5-HT from presynaptic nerve endings
C. Inhibits the presynaptic uptake of 5-HT
D. Blocks MAO which degrades 5-HT
E. Enhances the synthesis of 5-HT
C. Inhibits the presynaptic uptake of 5-HT
Which of the following can greatly enhance the toxicity when combined with the use benzodiazepines or barbiturate medications?
A. Cocaine
B. Alcohol
C. Methamphetamine
D. Marijuana
B. Alcohol
How is MOA different than other Benzodiazepines?
Oxazepam, Temazepam, and Lorazepam
bypass phase I oxidation and are metabolized only by phase II conjugation and are safer to use in the elderly
Shorter acting Benzodiazepines are….
alprazolam, estazolam, midazolam and triazolam
Longer acting Benzodiazepines are…
chlordiazepoxide, diazepam, flurazepam
Drugs of choice for Insomia are…..
Zolpidem, Zaleplon, Eszopiclone, Ramelteon
Benzodiazepines: MOA
- facilitating the activity of y-aminobutyric acid (GABA) at various sites in the CNS.
- binding site is located at the interface between a and y subunits at a different site of binding than GABA and bind to a1 and a2 subunits.
- BDZ increase the frequency with which the channel is opened.
Benzodiazepines: Side Effect
anterograde amnesia
Midazolam (Versed)
- Benzodiazepines
- Used IV as an anesthetic for patients undergoing procedures (EGD/Colonoscopy)
Clonazepam (Klonopin)
- Benzodiazepines
- Used for treatment of panic disorder, anxiety, and seizure disorders
- It does not have active metabolites
- One of the easier drugs in this class to taper off of in cases of dependence
Triazolam
Triazolam is short acting and coming off of this medication may cause rebound insomnia
Flurazepam
- Benzodiazepines
- is long acting and may cause significant hangover effect with somnolence the next day
Flumazenil (Romazicon)
- Competitive benzodiazepine receptor antagonist
- Used to counteract the adverse effects of benzodiazepine such as respiratory depression in cases of accidental or intentional overdose
- Adverse effects include seizures, arrhythmia, blurred vision, emotional lability, and dizziness
Barbiturates: MOA
- Bind to allosteric site on the GABAa receptor chloride ion channel that is distinct from the site BDZ bind.
- Increases the affinity of the receptor for GABA and the duration of time the chloride channel remains open
- Directly increases chloride influx in the absence of GABA