Sedative-Hypnotics, CNS muscle relaxants

Question 1

A drug that reduces excitement and calms the pt without inducing sleep

Answer 1

Sedative

Question 2

In therapeutic doses are _________ drugs

Answer 2

anxiolytic

Question 3

Most sedatives in larger doses produce _______

Answer 3

Hypnosis

Question 4

Site of action for sedatives

Answer 4

limbic system

Question 5

A drug that produces sleep

Answer 5

Hypnotic

Question 6

Used for initiation and maintenance of sleep

Answer 6

Hypnotic drugs

Question 7

Hypnotics in higher doses produce

Answer 7

general anaesthesia

Question 8

Site of action of hypnotics

Answer 8

midbrain and ascending RAS

Question 9

T or F: Most sedatives are analgesic

Answer 9

False

Question 10

Many sedatives induce _____

Answer 10

anterograde amnesia

Question 11

_____ is an unpleasant state of tension, apprehension, or uneasiness

Answer 11

Anxiety

Question 12

The agent which decreases worry

Answer 12

Anxiolytic

Question 13

Drug that affects skeletal muscle function and decreases the muscle tone; alleviates symptoms of muscle spasms, pain, and hyperreflexia

Answer 13

muscle relaxant

Question 14

These act by interfering with transmission at the neuromuscular end plate and have nocentral nervous system(CNS) activity

Answer 14

Neuromuscular blockers

Question 15

Often used during surgical procedures to cause temporaryparalysis

Answer 15

Neuromuscular blockers

Question 16

Centrally acting muscle relaxants

Answer 16

spasmolytics

Question 17

_______ alleviate musculoskeletal pain and spasms and to reduce spasticity in a variety of neurological conditions. They reduce muscle tone by acting on various levels of the motor pathway within the central nervous system

Answer 17

spasmolytics

Question 18

Most of these drugs act as _____ depressants and may produce spectrum of actions

Answer 18

CNS

Question 19

Sites of action for anxiolytics-sedative-hypnotics

Answer 19

anxiolysis and sedation: limbic system
sedation and hypnosis: RAS
general brain depression and coma: cerebral cortex

Question 20

Benzodiazepines with psychopharmacologic activity have an electronegative group at

Answer 20

R7

Question 21

A nitro moiety at R7 enhances ______ properties

Answer 21

antiseizure

Question 22

Benzodiazepines enhance inhibitory neurotransmission mediated by

Answer 22

GABA

Question 23

Two types of GABA receptors

Answer 23

GABA-A and GABA-B

Question 24

________ synapse with synthetic and catabolic enzymes, receptors, and transporters

Answer 24

GABAergic

Question 25

Benzodiazepines act on GABA-A receptors that are pentamers forming a

Answer 25

GABA-gated Cl-/HCO3- channel

Question 26

Consequences of benzodiazepine binding to GABA-A receptors

Answer 26

Increased frequency of Cl- channel opening when GABA is present: the Cl- current is up Hyperpolarization of the plasma membrane, increased duration of miniature IPSPs (postsynaptic GABA-A), decreased probability of synaptic vesicle release (presynaptic GABA-A) Reduced probability of excitation

Question 27

GABA is an

Answer 27

agonist

Question 28

Benzodiazepines

Answer 28

allosteric modulators

Question 29

benzodiazepines do not work in the absence of

Answer 29

GABA or another agonist

Question 30

Positive regulation of GABA-A receptors

Answer 30

Barbiturates: facilitates & mimics GABA action Benzodiazepines: facilitate GABA action (allosteric modulator) Alcohol, inhalation anaesthetics, propofol: open Cl channels directly

Question 31

Negative regulation of GABA-A receptors

Answer 31

Bicuculline: competitive antagonist at GABA Rc Flumazenil: competitive antagonist at BZD site (benzodiazepine antidote)!!! Picrotoxin: blocks Cl channel non-competitively

Question 32

Inverse agonists of GABA-A receptors

Answer 32

B-carbolines (DMCM): inverse agonist at BZD site

Question 33

Diversification of GABA-A receptors may explain _________ of some benzodiazepines to produce specific therapeutic effects

Answer 33

relative selectivity

Question 34

GABA-A receptors for anxiolytic activity

Answer 34

α2- and/or α3- containing receptors

Question 35

GABA-A receptors for hypnotic activity

Answer 35

α1 containing receptors

Question 36

Pharmacokinetics of benzodiazepines

Answer 36

Lipophilic Rapidly and completely absorbed after oral administration Penetrate into the CNS Longer acting drugs form active metabolites with long half-lives Cross the placental barrier and are excreted with milk

Question 37

Benzodiazepines are divided into groups differing by duration of their effects. What are they?

Answer 37

Short acting Intermediate acting Long acting

Question 38

Short acting benzodiazepines

Answer 38

Triazolam Oxazepam Midazolam

Question 39

Intermediate acting benzodiazepines

Answer 39

Alprazolam Estazolam Temazepam Lorazepam Nitrazepam

Question 40

Long acting benzodiazepines

Answer 40

Diazepam Flurazepam Clonazepam Chlordiazepoxide

Question 41

Benzos safe to use in pts with liver disease

Answer 41

Estazolam Lorazepam Oxazepam Temazepam

Question 42

Long acting benzos form

Answer 42

slowly eliminated active metabolites

Question 43

Benzos with reduced bioavailability after oral administration. Must be used with caution for pts with liver disease

Answer 43

Alprazolam Midazolam Triazolam all cause a-hydroxylation by hepatic CYP3A4

Question 44

Actions of benzodiazepines

Answer 44

Reduction of anxiety Sedative/hypnotic Anterograde amnesia Anticonvulsant Muscle relaxant Can also cause: respiratory depression, reduces BP, paradox rxns

Question 45

Toxic side effects of benzodiazepines (hypnosis, respiratory suppression, coma, death) are enhanced by

Answer 45

CNS depressants

Question 46

Toxic side effects of benzodiazepines may be enhanced by drugs that reduce their

Answer 46

phase I metabolism

Question 47

Drugs that can reduce their phase 1 metabolism

Answer 47

cimetidine, Ca2+ channel blockers: diltiazem, verapamil, Macrolids: erythromycin, clarithromycin, protease inhibitors (indinavir, nelfinavir, ritonavir), antimycotics (itraconazole, ketoconazole), antidepressants (fluoxetine, fluvoxamine, trazodone)

Question 48

Toxic side effects of benzodiazepines may be enhanced by

Answer 48

Old age Liver disease

Question 49

______ may be also used to speed up recovery from Benzodiazepine-induced sedation

Answer 49

Flumazenil

Question 50

The benzodiazepine antidote

Answer 50

Flumazenil

Question 51

Use of benzodiazepines may be associated with _____ and _____ its stopping may induce withdrawal

Answer 51

tolerance and dependence

Question 52

short acting benzos are more likely to cause ____ (triazolam)

Answer 52

withdrawal

Question 53

non-benzodiazepine structure but action on the same site of the GABA-A receptor

Answer 53

Z-hypnotics

Question 54

Procedure is directly correlated to the

Answer 54

drug duration (short procedure shorts acting)

Question 55

Not FDA-approved Potentially mutagenic No antidote Narrow therapeutic window Resedation after discharge (long acting metabolites – TCE)

Answer 55

Chloral Hydrate

Question 56

Diazepam effects on muscle tone are mostly

Answer 56

supraspinal

Question 57

Common precautions while using CNS depressants

Answer 57

no driving for 24 h after the use Watch for combination with ethanol and drugs of abuse Watch for combination with other CNS depressants Adjust doses for elderly