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Flashcards in Sedative Hypnotics Deck (35):
1

classification of sedative-hypnotic Drugs

MN BOOBS

Melatonin Receptor agonists
Non Benzo Benzo-Receptor Agonists (NBBRAs)

Benzodiazepines
Older Sedative Hypnotics
Others: beta blockers, alpha 2 agonists, antihistaminics
Barbiturates
Serotonin 5-HT1A partial agonists

2

what are the benzodiazepines

DMC FLOATT

Diazepam
Midazolam
Clonazepam

Flurazepam
Lorazepam
Oxazepam
Temazepam
Triazolam

3

mechanism of action of benzodiazepines (name them)

diazepam, midazolam, clonazepam, flurazepam, lorazepam, oxazepam, temazepam, triazolam

bind to GABA-A receptors at an allosteric site as a positive allosteric modulator --> activates GABA's inhibitory actions --> opens Cl channels --> influx of Cl --> hyperpolarization --> inhibits triggering of action potential

4

what are the agonists of benzodiazepine receptors and what effects do they lead to

All the benzos plus the Non-benzo benzo receptor agonist (NBBRAs)

anxiolytic and anticonvulsant effects

5

name the benzodiazepine receptor antagonist and its effects

Flumazenil

blocks action of benzos and NBBRAs

6

what are inverse agonist and its effect

act as negative allosteric modulators of GABA receptor function --> anxiety and seizures

7

action of benzos

Sedation
Anti convulsants
Anesthesia
Muscle relaxation

8

classify the benzos in terms of length of action

Long acting (1-3 days): Diazepam and Flurazepam
Intermediate acting (10-20 hrs): Lorazepam, Alprazolam, Temazepam
Short acting (3 - 8 hrs): Oxazepam and Triazolam

9

what do benzos undergo when being metabolized

Phase I: done by CYP3A4
Phase 2: conjugation to glucuronides to be excreted in urine

10

which benzos don't undergo the phase I of metabolism and its importance

LOT
Lorazepam, Oxazepam, Temazepam

their metabolism is not affected by liver disease since they skip phase I with CYP3A4 and go right into conjugation to glucuronides

11

benzo used in muscular disorder and why

benzo is a muscle relaxant

Diazepam is used in skeletal muscle spasms and spasticity from degenerative disorders such as MS and Cerebral Palsy

12

benzos used in seizures

Clonazepam: some types of epileptic seizures
Lorazepam: status epilepticus

13

benzos used in management of alcohol withdrawal

DOCC for Ethanol

Diazepam
Oxazepam
Chlordiazepoxide
Clorazepate

14

benzos prescribed for sleep disorders

Flurazepam
Temazepam
Triazolam

15

AE of benzos

Drowsiness and confusion
Ataxia
Cognitive impairment
Psychological effects

16

what is the benzo antagonist and what is it used for

Flumazenil

reverse CNS effects caused by benzo overdose

17

barbituates used as sedative-hypnotics

Phenobarbital
Pentobarbital
Thiopental

18

mechanism of barbiturates used as sedatives (name them)

phenobarbital, pentobarbital, thiopental

-potentiates effects of GABA by increase duration of GABA gated chloride channel opening
-block glutamate receptors
-block high frequency Na channels

19

action of barbiturates in sedative hypnotics

CNS depression
Respiratory depression
Enzyme induction

20

therapeutic uses of barbiturates (aka name what each drug is used for)

-Thiopental - Anesthesia
-Phenobarbital - anticonvulsant; treat hyperbilirubinemia and kernicterus by increasing glucuronyl transferase and bilirubin binding Y protein activity

21

AE of barbiturates (name them)

phenobarbital, thiopental, pentobarbital

CCP3 RAPs in HHD

CNS effects (drowsiness, sluggishness etc)
CYP450 induction
Paradoxical excitement (opp of expected)
Pulmonary insufficiency --> resp depression
Porphyrin Synthesis

Respiratory Depression
Addiction
Poisoning (lead to death)

Heart collapse
Hypersensitivity (allergic rxn)
Drug hangover (effects seen after sleeping)

22

contraindication of barbiturates (name them)

thiopental, pentobarbital, phenobarbital

-Pulmonary insufficiency --> resp depression
-Due to porphyrin synthesis, acute intermittent porphyria, variegate porphyria, hereditary copropporphyria, or symptomatic porphyria

23

what are the non-benzodiazepine benzodiazepine receptor agonists (NBBRAs)

Zolpiden
Zaleplon
Eszopiclone

24

mechanism of non-benzo benzo receptor agonists (NBBRAs) (name them)

zolpiden, zaleplon, eszopiclone

act on BZ1 subtype of benzodiazepine receptors which contain alpha 1 subunit

25

what antagonizes zolpiden

flumazenil - benzo receptor antagonist

26

clinical use of Zolpiden

short term treatment of insomnia characterized by difficulty initiating sleep

27

what metabolizes Zaleplon

aldehyde oxidase and CYP3A4

28

clinical use of Eszopiclone

insomnia --> decreases sleep latency and improves sleep maintenance

29

what is the serotonin 5-HT1A partial agonist

Buspirone

30

action of 5-HT1A partial agonist and what it is used to treat

anxiolytic

anxiety disorders or short term relief of anxiety

31

what is the melatonin receptor agonist and its mechanism

Ramelteon - MT1 and MT2 melatonin receptor agonist

32

what is melatonin receptor agonist used for

Ramelteon

insomnia characterized by difficulty with sleep onset

33

AE of Ramelteon

decrease in testosterone
increase in prolactin

34

what are the older drugs that were used as sedatives

Chloral Hydrate
Meprobamate
Paraldehyde

35

what are the other classes of sedatives

alpha 2 agonist: Clonidine
beta blocker: Propanolol (specific situational phobias and performance anxiety)
histamine receptor blockers: Diphenhydramine, Doxylamine, Hydroxyzine

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