Sedative-Hypnotic Drugs

Question 1

Compare Older Sedatives (barbituates) with Newer (benzos)

Answer 1

Older sedative-hypnotics (barbiturates) show a linear dose-response curve [no ceiling]

An increase in dose above that needed for hypnosis may lead to a state of general anesthesia.

At still higher doses they may depress respiratory and vasomotor centers in the medulla, leading to coma and death.

Benzodiazepines show a non-linear dose- response relationship. They are safer drugs. (have a plateu), overdose will not kill you.

Question 2

Name the BARBITURATES

Answer 2

Phenobarbital

Pentobarbital

Thiopental

Question 3

name the NON-BENZODIAZEPINE BENZODIAZEPINE-RECEPTOR AGONISTS (NBBRA)

“Z drugs”

Answer 3

Zolpiden

Zaleplon

EsZopiclone

Question 4

name the only 5-HT1A PARTIAL AGONISTS

Answer 4

Buspirone

Question 5

name the only MELATONIN RECEPTOR AGONISTS

Answer 5

Ramelteon

Question 6

name the OLDER SEDATIVE-HYPNOTICS (3)

Answer 6

Meprobamate

Chloral hydrate

Paraldehyde

Question 7

name the ANTIHISTAMINICS

Answer 7

Hydroxyzine

Diphenhydramine

Doxylamine

Question 8

name the only α2-AGONISTS in this lecture

Answer 8

Clonidine

Question 9

bind to GABAa receptors(which functions as a chloride channel, and is activated by the inhibitory neurotransmitter GABA) in neuronal membranes in the CNS.

is the MOA for which class of drugs

Answer 9

Benzos

Question 10

Do benzos DIRECTLY activate GABAa receptors?

Answer 10

NO!

Benzodiazepines potentiate GABAergic inhibition. Benzodiazepines don’t directly activate GABAA receptors: they enhance GABA’s effects allosterically. This enhancement takes the form of an increase in frequency of channel opening events.

Question 11

name the benzo ANTAGONIST (1)

Answer 11

flumazenil

Question 12

list the 3 benzos that fit the following description

are conjugated directly to their glucuronides, mainly in the liver, and are not metabolized by the P450 system. Their plasma levels are not significantly affected in liver disease. Other benzodiazepines may need dose adjustment in liver disease.

“L-O-T”

Answer 12

lorazepam

oxazepam
temazepam

Question 13

Benzos good for: MUSCULAR DISORDERS

Answer 13

Diazepam is useful in the treatment of skeletal muscle spasms such as occur in muscle strain, and in treating spasticity from degenerative disorders, like multiple sclerosis and cerebral palsy.

Question 14

Benzos good for SEIZURES

which one is specifically good for status epilepticus.

Answer 14

Clonazepam: used for some types of epileptic seizures.

Lorazepam : drug of choice in status epilepticus.

Question 15

benzos good for DRUG WITHDRAWAL

“C-C-O-D”

Answer 15

Chlordiazepoxide

clorazepat

oxazepam

diazepam

*useful in the management of withdrawal states in persons physiologically dependent on ethanol.

Question 16

which benzos are used for ANESTHESIA

Answer 16

diazepam, midazolam

are used as components of anesthesia protocols.

Question 17

which benzos are commonly used for SLEEP DISORDERS

Answer 17

The three most prescribed for sleep disorders are

1. long-acting flurazepam
2. intermediate-acting temazepam
3. short-acting triazolam

Question 18

which barbituate is being described:

acts within seconds and has a duration of action of about 30 min is used in the IV induction of anesthesia.

Answer 18

Thiopental

Question 19

which barbituate is being described

has a duration of action of >1 day is useful in treatment of seizures.

Answer 19

Phenobarbital

Question 20

Do barbituates induce or inhibit CYP450 enzymes

Answer 20

ENZYME INDUCTION

Barbiturates induce P-450 microsomal enzymes in the liver. Therefore, chronic barbiturate administration diminishes the action of many drugs that are dependent on P- 450 metabolism to reduce their concentration.

Question 21

Because hepatic glucuronyl transferase and the bilirubin-binding Y protein are increased by the barbiturates, (this barbituate) has been used successfully to treat hyperbilirubinemia and kernicterus in the neonate.

Answer 21

phenobarbital

Question 22

this class of drugs is absolutely contraindicated if pts have acute intermittent porphyria, variegate porphyria, hereditary coproporphyria or symptomatic porphyria.

Answer 22

BARBITUATES

Question 23

These drugs act only on the BZ1 subtype of benzodiazepine receptors

Answer 23

THE NON-BENZODIAZEPINE BENZODIAZEPINE- RECEPTOR AGONISTS (NBBRA)

Question 24

No hypnotic, anticonvulsant or muscle relaxant properties. Only anxiolytic.

Doesn’t interact with GABA receptors.

Indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety.

Answer 24

5-HT1A partial agonist.

BUSPIRONE

Question 25

mainly metabolized by CYP1A2.

should not be concurrently given with fluvoxamine, which inhibits CYP1A2.

Indicated for the treatment of insomnia characterized by difficulty with sleep onset.

Answer 25

Ramelteon

Question 26

Temazepam, triazolam, and flurazepam are category ______in pregnancy

Answer 26

category X.

Question 27

Most barbiturates are category_____ in pregnancy

Answer 27

D

Question 28

Eszopiclone, zaleplon, zolpidem and ramelteon are category__________ in pregnancy

Answer 28

C

Question 29

Buspirone is category________ in pregnancy

Answer 29

B

B for B!!!