!sedatives, Hypnotics, And Anxiolytics

Front 1

Differentiate sedative drugs from hypnotic drug in terms of their ability to facilitate sleep.

Back 1

sedatives do not produce sleep while hypnotics produces drowsiness and facilitates the onset and maintenance of sleep

Front 2

Differentiate sedative drug s from hypnotic drugs in terms of the time of day there are usually give.

Back 2

sedatives are usually given during daytime hours while hypnotic drugs are given at night

Front 3

Complaint of inadequate sleep

Back 3

insomnia

Front 4

T/F. One of the symptoms of insomnia can be fatigue despite sleep of adequate duration

Back 4

T

Front 5

Unpleasant state tension, apprehension or uneasiness

Back 5

Anxiety

Front 6

Anxiety Disorder characterized by ongoing state of excessive anxiety lacking any clear reason or focus

Back 6

Generalized anxiety disorder

Front 7

Anxiety disorder characterized sudden attacks of overwhelming fear with somatic symptoms such as sweating, tachycardia, chest pains, trembling and choking

Back 7

Panic Disorder

Front 8

Anxiety disorder which is characterized by strong fears of specific objects or situations

Back 8

phobias

Front 9

Anxiety triggered by recall of past stressful experiences

Back 9

post-traumatic stress disorder

Front 10

Anxiety disorder which is characterized by ritualistic behavior driven by irrational anxiety

Back 10

Obsessive-compulsive disorder

Front 11

Barbiturates were formerly the mainstay agents in sedating patients or inducing and maintaining sleep. Why are they now replaced by benzodiazepines?

Back 11

Barbiturates induce 1)tolerance 2)drug-metabolizing enzymes 3)physical-dependence 4)severe-withdrawal symptoms 5)coma in toxic doses

Front 12

Describe the chemical structure of barbiturates

Back 12

w/ 2, 4, 6-trioxohydroxypyrimidine

Front 13

Describe the MOA of barbiturates

Back 13

they increase the duration of opening of GABA-gated chloride channels. They are GABA-mimetic-at high concentrations, it directly activates chloride channels. They also inhibit the excitatory neurotransmitter, glutamate by binding to AMPA receptor

Front 14

T/F. The multiplicity in sites of action of barbiturates may be the basis for their ability to induce full surgical anesthesia and for their more pronounced central depressant effects

Back 14

T

Front 15

Characterize the following barbiturates whether they are ultra-short-acting, short-acting, intermediate acting, or long acting: Thioamylal, Pentobarbital, Secobarbital, Amobarbital, Methohexital, Thiopental, Butabarital, Phenobarbital, Mephobarbital, and Methabarbital

Back 15

ultra-short-acting= Methohexital, Thiopental,Thioamylal ; short-acting= Pentobarbital, Secobarbital,; intermediate acting= Amobarbital, Butabarital; long acting=Phenobarbital, Mephobarbital, and Methabarbital

Front 16

What is the duration of action of barbiturates ultra-short-acting, short-acting, intermediate-acting, and long-acting?

Back 16

Ultra-short-acting= 20 minutes or less, short-acting= <3 hours, and intermediate-acting= 3-6 hours, and long-acting= >6 hours

Front 17

Ultra-short-acting barbiturates is for anesthetic. How about long-acting barbiturates?

Back 17

selective anticonvulsant

Front 18

Most commonly used barbiturates?

Back 18

Thiopental

Front 19

First-line anticonvulsant drug?

Back 19

Phenobarbital

Front 20

DOC for treatment of young children with recurrent febrile seizures?

Back 20

phenobarbital

Front 21

Long-acting barbiturate that is used as a long term management of tonic-clonic seizures, status epilepticus, and eclampsia

Back 21

phenobarbital

Front 22

What is the major complication of barbiturate anesthesia?

Back 22

Laryngospasm

Front 23

T/F/ Barbiturates may induce hypersensitivity causing Steven Johnson’s Syndrome.

Back 23

T

Front 24

With the chronic use of phenobarbital, what blood related AE can it produce?

Back 24

Megaloblastic anemia

Front 25

T/F. Barbiturates inhibit CYP450 system.

Back 25

F. They induce.

Front 26

Barbiturates increase _ synthesis?

Back 26

Porphyrin. It is contraindicated to patients with acute intermittent porphyria or porphyria variegata

Front 27

In severe toxicity with barbiturates, describe the AE related to breathing.

Back 27

Cheyne-stokes (irregular) respiration

Front 28

Treatment for Barbiturate toxicity?

Back 28

artificial respiration, forced alkaline diuresis, and hemodialysis- necessary only rarely

Front 29

Describe the chemical structure of benzodiazepines. What s essential for activity?

Back 29

w/ 1, 4-benzodiazepine; A Halogen or Nitro group on position 7 is essential for activity

Front 30

Describe the MOA of benzodiazepines

Back 30

they increase the frequency of opening of chloride channels; they induce inhibitory postsynaptic potential via hyperpolarization and decreased neuronal excitability

Front 31

Major inhibitory neurotransmitter in the CNS

Back 31

GABA (gamma-amino butyric acid) Receptors

Front 32

GABA Receptors are synthesized from? Via?

Back 32

Glutamate via glutamic acid decarboxylase

Front 33

Group the related terms. GABA-A Receptors, Metabotropic, coupled to g receptor and inhibit Ca2+ channels or activate K+ channels, Ionotropic, pentameric structures selectively permeable to Cl-, GABA-B Receptors,

Back 33

GABA-A Receptors,Ionotropic, pentameric structures selectively permeable to Cl-

GABA-B Receptors, Metabotropic, coupled to g receptor and inhibit Ca2+ channels or activate K+ channels

Front 34

GABA-A Receptor agonist

Back 34

Muscimol

Front 35

GABA-A Receptor antagonists

Back 35

Bicuculine/ Picrotoxin

Front 36

GABA-B Receptor Agonist

Back 36

Baclofen

Front 37

GABA-B Receptor Antagonist

Back 37

2-OH Saclofen

Front 38

T/F. The action of benzodiazepines is dose dependent

Back 38

T. At low doses, it is an anxiolytic/sedative drug; at high doses, it is a hypnotic drug.

Front 39

Characterize the following benzodiazepines whether they are short-acting, intermediate acting, or long acting: Midazolam, Alprazolam, Clorazepate, Chlordiazepoxide, Diazepam, Flurazepam, Estazolam, Oxazepam, Triazolam, Lorazepam, Temazepam, and Quazepam.

Back 39

Short-acting= Midazolam, Oxazepam, and Triazolam; Intermediate-acting= Alprazolam, Estazolam, Lorazepam, and Temazepam; Long-acting= Clorazepate, Chlordiazepoxide, Diazepam, Flurazepam, and Quazepam.

Front 40

Which benzodiazepine is used for short and long-term treatment of panic disorders?

Back 40

Alprazolam

Front 41

Which benzodiazepine is used for patients with anxiety that may require treatment for prolonged periods of time?

Back 41

Diazepam

Front 42

Which benzodiazepine can be used for the chronic treatment of epilepsy?

Back 42

Clonazepam

Front 43

Which benzodiazepine is used for the treatment of skeletal muscle spasms and spasticity from degenerative disorders (Multiple sclerosis and cerebral palsy)

Back 43

Diazepam

Front 44

DOC for grand mal seizures status epilepticus?

Back 44

Diazepam

Front 45

Which benzodiazepine is used to reduce both sleep induction time and the number of awakenings? It increases duration of sleep; it is long acting and can maintain effectiveness up to 4 weeks; it may cause little rebound insomnia and daytime sedation.

Back 45

Flurazepam

Front 46

Which benzodiazepine is used for patients who experience frequent wakening or those who have inability to stay asleep?

Back 46

Temazepam

Front 47

How should Temazepam be taken?

Back 47

Should be given several hours before bedtime

Front 48

Which benzodiazepine is used to induce sleep in patients with recurring insomnia? Used for patients who have difficulty in going to sleep?

Back 48

Triazolam

Front 49

Commonly used to sedate hospitalized patients.

Back 49

Triazolam

Front 50

Benzodiazepines that can induce Stage III Anesthesia (surgical anesthesia).

Back 50

Diazepam, Lorazepam, and Midazolam

Front 51

Benzodiazepines that can be used as acute treatment of alcohol withdrawal.

Back 51

Diazepam, Lorazepam, and Midazolam

Front 52

Describe the metabolism of benzodiazepines.

Back 52

Through hepatic metabolism; it undergoes microsomal oxidation (phase I reactions) and subsequently conjugated (phase II reactions) to form glucuronides that are secreted in the urine

Front 53

Which benzodiazepines have less probability of cumulative residual effects because they immediately undergo conjugation instead of oxidation then conjugation?

Back 53

Oxazepam and Lorazepam

Front 54

T/F. Benzodiazepines unlike barbiturates no longer produce dependence and tolerance.

Back 54

F. They still can occur if high doses are given over a prolonged period of time.

Front 55

What is the treatment for Benzodiazepine toxicity? Example is when the patient experiences severe respiratory depression (because it is given with other CNS depressants).

Back 55

Flumazenil (IV only)

Front 56

Flumazenil, aside from being a benzodiazepine receptor antagonist, also blocks the actions of what drugs?

Back 56

Eszopiclone, Zaleplon, and Zolpidem

Front 57

Other names of Chloral hydrate?

Back 57

Mickey Finn, Knockout drops

Front 58

Chloral hydrate is reduced to what compound which is a potent alcohol responsible for it pharmacologic activity?

Back 58

trichloroethanol

Front 59

Zolpidem, Flurazepam, and Triazolam shorten sleep latency. What is the advantage of Zolpidem over the other two?

Back 59

1) No withdrawal effects 2) Minimal rebound insomnia 3) Little or no tolerance occurs with prolonged use 4) rarely associated with respiratory depression even in overdose

Front 60

Both diazepam and Buspirone can be used to treat anxiety. What is the advantage of Buspirone?

Back 60

Minimal sedation and psychomotor and cognitive dysfunction 2) dependence is unlikely (Disadvantage: slow onset of action)

Front 61

This drug has antihistamine and antiemetic activity; it is used for patients with anxiety, who have a history of drug abuse; it is often used for sedation prior to dental procedures or surgery.

Back 61

Hydroxyzine

Front 62

This drug is indicated as a pediatric or geriatric hypnotic; it can be used as a preanesthetic agent for minor surgical and dental procedures.

Back 62

Chloral hydrate

Front 63

Non-Rx effective in treating mild types of insomnia but they have numerous side effects that make them less useful than benzodiazepines.

Back 63

Diphenhydramine and Doxylamine

Front 64

These drugs hypnotic drugs are unrelated to benzodiazepines but they share a similar MOA (binding to GABA-A receptor)

Back 64

Zaleplon and Eszopiclone

Front 65

New hypnotic drug; agonist at MT1 and MT2 melatonin receptors located in the suprachiasmatic nuclei of the brain; it appears to be distinctly more efficacious than melatonin as hypnotic

Back 65

Ramelteon

Front 66

What compound is in Sleepasil? What is significant regarding its onset of action?

Back 66

Melatonin. It takes 2 weeks before one experiences the hypnotic effect.

Front 67

Brand name of Methohexital?

Back 67

Brevital

Front 68

Brand name of Thiopental?

Back 68

Penthotal