Pharm: Sedative Hypnotics

Front 1

Sedation vs Hypnosis

Back 1

Sedation: reduced alertness, decreased motor activity, and relaxation

Hypnosis: state of drowsiness which leads to sleep

Front 2

Ideal Anxiolytic

Back 2

calm without causing daytime drowsiness or dependence, physiological or psychological

Front 3

ideal Sedative-Hypnotic

Back 3

All the user to fall asleep quickly, stay asleep quickly, not cause "hangover" drowsiness, high margin of safety and not effect on REM sleep.

Front 4

what causes sleep

Back 4

Activation of GABAa receptor complex in the reticular formation, thalamus, and cerebral cortex

GABAa open chloride channels which hyperpolarizes the cells

causes depression of electrical activity, depressing the CNS

Front 5

Barbituates

Back 5

Pentobarbital, Phenobarbital, Thiopental

Bind to and ↑ duration of GABA action (inhibitory)
--[Rx] high ↑ Cl- flow elsewhere (GABA independent inhibition)

PhK: oral, induce p450; last up to full day effect, acidic (see toxicology)

Marked CNS depression with low margin of safety;
↓ alertness, jugdgment, motor skills; (±paradoxical excitement)
moodΔ's, euphoria, severe psysio & psych dependence; schedule 2 or 3

Synergistic, esp c ETOH: coma, ↓ repiratory drive, death; (stimulants ↑ mortality)

WD ≈ dose and duration: restlessness → hypotension → seizures

Contras: pulmonary insufficiency, porphyria (increase porphyrin synth).

Front 6

Thiopental

Back 6

An ultrashort acting barbituate used for anesthesia

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Barbituates: bind to and ↑ duration of GABA action (inhibitory)
--[Rx] high ↑ Cl- flow elsewhere (GABA independent inhibition)
PhK: oral, induce p450; last up to full day effect, acidic (see toxicology)
Marked CNS depression with low margin of safety;
↓ alertness, jugdgment, motor skills; (±paradoxical excitement)
moodΔ's, euphoria, severe psysio & psych dependence; schedule 2 or 3
Synergistic, esp c ETOH: coma, ↓ repiratory drive, death; (stimulants ↑ mortality)
WD ≈ dose and duration: restlessness → hypotension → seizures
Contras: pulmonary insufficiency, porphyria (increase porphyrin synth).

Front 7

Phenobarbital

Back 7

long-acting barbituate used as anticonvulsant

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Barbituates: bind to and ↑ duration of GABA action (inhibitory)
--[Rx] high ↑ Cl- flow elsewhere (GABA independent inhibition)
PhK: oral, induce p450; last up to full day effect, acidic (see toxicology)
Marked CNS depression with low margin of safety;
↓ alertness, jugdgment, motor skills; (±paradoxical excitement)
moodΔ's, euphoria, severe psysio & psych dependence; schedule 2 or 3
Synergistic, esp c ETOH: coma, ↓ repiratory drive, death; (stimulants ↑ mortality)
WD ≈ dose and duration: restlessness → hypotension → seizures
Contras: pulmonary insufficiency, porphyria (increase porphyrin synth).

Front 8

Sedatives contraindicated in pulmonary insufficiency

Back 8

Barbituates: Pentobarbital, Phenobarbital, Thiopental

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Barbituates: bind to and ↑ duration of GABA action (inhibitory)
--[Rx] high ↑ Cl- flow elsewhere (GABA independent inhibition)
PhK: oral, induce p450; last up to full day effect, acidic (see toxicology)
Marked CNS depression with low margin of safety;
↓ alertness, jugdgment, motor skills; (±paradoxical excitement)
moodΔ's, euphoria, severe psysio & psych dependence; schedule 2 or 3
Synergistic, esp c ETOH: coma, ↓ repiratory drive, death; (stimulants ↑ mortality)
WD ≈ dose and duration: restlessness → hypotension → seizures
Contras: pulmonary insufficiency, porphyria (increase porphyrin synth).

Front 9

CNS Rx contraindicated in porphyria

Back 9

Barbituates: Pentobarbital, Phenobarbital, Thiopental

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Barbituates: bind to and ↑ duration of GABA action (inhibitory)
--[Rx] high ↑ Cl- flow elsewhere (GABA independent inhibition)
PhK: oral, induce p450; last up to full day effect, acidic (see toxicology)
Marked CNS depression with low margin of safety;
↓ alertness, jugdgment, motor skills; (±paradoxical excitement)
moodΔ's, euphoria, severe psysio & psych dependence; schedule 2 or 3
Synergistic, esp c ETOH: coma, ↓ repiratory drive, death; (stimulants ↑ mortality)
WD ≈ dose and duration: restlessness → hypotension → seizures
Contras: pulmonary insufficiency, porphyria (increase porphyrin synth).

Front 10

Benzodiazepines

Back 10

[Rx]low: ↓ anxiety, [Rx]high: hypnosis;
Mech: BZD's; ↑ GABA-GABAa binding
PhK: Oral-Hepatic w/ active metabolites; (Benzo's ∅ΔCYP's)
SE: paradoxical excitement, CNS depression (tolerance dvlps); normal [Rx]+ETOH = fatal;
OD: ↓ GABA release at [Rx]high; intrinsic ceiling
WD: long λ's & active metabolites = good taper;
--seizures if chronic [Rx]high
Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 11

Elderly with Alzheimers Sx on an Rx

Back 11

Benzodiazepine (-zapam's)? Then it's probably a side effect.

Front 12

Diazepam (Valium)

Back 12

Benzodiazepine with unique uses & PhK

Uses: muscle relaxn vs spasm, anti-convulsant (IV vs status epilepticus), ETOH/Barbituate WD (Valium & Librium)

~2dλ → active nordiazepam~1dλ → active oxazepam 8hλ

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Bonzodiazepines: anxiolytics
--Mech: ↑ GABA-GABAa binding
--PhK: Oral-Hepatic: CYP3A4 & 2C19 (∅ΔCYP's)
--SE: paradoxical excitement, CNS depression (tolerance dvlps); normal [Rx]+ETOH = fatal;
--OD: ↓ GABA release at [Rx]high; intrinsic ceiling
--WD: long λ's & active metabolites = good taper;
----seizures if chronic [Rx]high
--Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)]

Front 13

Desmethyldiazepam
(Nordiazepam)

Back 13

active metabolic byproduct of diazepam (Valium) and chordiazepoxide (Librium); >24h λ, then to oxazepam (8h λ); good taper for withdrawal.

Front 14

Chlordiazepoxide (Librium)

Back 14

Benzodiazepine used to prevent seizures in ETOH/Barbituate withdrawal (like Valium)

PhK: Oral-Hepatic: CYP3A4 & 2C19; ~2dλ → active nordiazepam~1dλ → active oxazepam 8hλ); ↑ duratn by cimetidine; (also like Valium)

[Bonzodiazepines: anxiolytics
--Mech: ↑ GABA-GABAa binding
--SE: paradoxical excitement, CNS depression (tolerance dvlps); normal [Rx]+ETOH = fatal;
--OD: ↓ GABA release at [Rx]high; intrinsic ceiling
--WD: long λ's & active metabolites = good taper;
----seizures if chronic [Rx]high
--Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)]

Front 15

Flurazepam
(Dalmane)

Back 15

BZD used as hypnotic: less ↓ REM,

oral, 3dλ → long-active metabolite;
-- "hangover" effect, but useful vs early morning waking.

Side Effects: SLEEP DRIVING
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Bonzodiazepines: sedative-hypnotics/anxiolytics
--Mech: ↑ GABA-GABAa binding
--PhK: hepatic metzm by 3A4 & 2D6 w/ ∅↑↓CYP;
--SE: paradoxical excitement, CNS depression (tolerance dvlps); normal [Rx]+ETOH = fatal;
--OD: ↓ GABA release at [Rx]high; intrinsic ceiling
--WD: long λ's & active metabolites = good taper;
----seizures if chronic [Rx]high
--Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 16

Midazolam

Back 16

Versed: preparation for anesthesia and short surgical procedures

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

MUST BE GIVEN IV, 2hλ, short duration of action

Side Effects: Anterograde Amnesia

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 17

Versed

Back 17

Midazolam: preparation for anesthesia and short surgical procedures

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

MUST BE GIVEN IV, 2hλ, short duration of action

Side Effects: Anterograde Amnesia

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 18

Temazepam

Back 18

Restoril: Insomnia, causes less REM depression

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

Well absorbed orally, duration proportional to lipid solubility; Dooes not induce CYP;

Side Effects: SLEEP DRIVING, paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 19

Restoril:

Back 19

Temazepam: Insomnia, causes less REM depression

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

Well absorbed orally, duration proportional to lipid solubility; Dooes not induce CYP;

Side Effects: SLEEP DRIVING, paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 20

Triazolam

Back 20

Halcion: Insomnia, less REM depression, short λ good for someone who can't fall asleep but will stay asleep. May cause rebound insomnia.

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

Well absorbed orally, <3hλ proportional to lipid solubility; converted to short acting metabolite <6hλ. Does not induce CYP

Side Effects: SLEEP DRIVING, PSYCHOSIS in susceptible w/ chronic use; paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 21

Halcion

Back 21

Triazolam: Insomnia, less REM depression, short λ good for someone who can't fall asleep but will stay asleep. May cause rebound insomnia.

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

Well absorbed orally, <3hλ proportional to lipid solubility; converted to short acting metabolite <6hλ. Does not induce CYP

Side Effects: SLEEP DRIVING, PSYCHOSIS in susceptible w/ chronic use; paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 22

Alprazolam

Back 22

Xanax: Anxiolytic, esp w/ depression

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

Well absorbed orally, 12h λ proportional to lipid solubility; short acting metabolite <6hλ. Does not induce CYP

Side Effects: paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 23

Xanax:

Back 23

Alprazolam: Anxiolytic, esp w/ depression

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

Well absorbed orally, 12h λ proportional to lipid solubility; short acting metabolite <6hλ. Does not induce CYP

Side Effects: paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 24

Lorazepam

Back 24

Ativan/Alpazam: Anticonvulsant given IV for status epilepticus, Withdrawal from ETOH/barbituates

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

Well absorbed orally, 6-24hλ proportional to lipid solubility;conjugated directly to inactive metabolites

Side Effects: paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 25

Ativan

Back 25

Lorazepam: Anticonvulsant given IV for status epilepticus, Withdrawal from ETOH/barbituates

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

Well absorbed orally, 6-24hλ proportional to lipid solubility;conjugated directly to inactive metabolites

Side Effects: paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 26

Sedative-Hypnotic Rx contraindicated by pregnancy

Back 26

Benzodiazepines, Category D: Known Teratogen

Kava: no FDA safety data
Valerian: hepatotoxic

Front 27

Sedative-Hypnotic Rx contraindicated for children

Back 27

Benzodiazepines

Impair learning and memeory

Front 28

Sedative-Hypnotic Rx contraindicated for spleep apnics

Back 28

Benzodiazepines

Relax Pharyngeal Musculature

Front 29

Anxiety Disorders NOT treated with Benzodiazepines

Back 29

OCD: responds better to SSRI's

Agoraphobia/Banic Disorders: SSRI's or Antidepressants

PTSD: antidepressants

Anciety in Children and Adolescents: Impairs Learning and Memeory, use antidepressants

Front 30

Rx Anxiety

Back 30

Benzodiazepines: eg Diazepam (Valium), Alprazolam (Xanax) DOC for anxieties EXCEPT (OCD, Agoraphobia/panic, PTSD, children/adolescent anxieties); bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

Well absorbed orally, duration proportional to lipid solubility; active metabolites metabolized slowly, duration out of proportion to [Parent]. (See specific cards for specifics). [Rx]-low decreases anxiety, Rx[hi] hypnosis; Do Not Induce CYP;

Side Effects: paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 31

Benzodiazpeine Rx Insomnia

-Can't Fall Asleep
-Early Waking

Back 31

Benzodiazepines: Flurazepam (Dalmane), Temazepam (Restoril), Triazolam (Halcion). Less REM sleep depression. May cause SLEEP DRIVING.

Flurazepam: 74hλ, converted to long-active metabolite; causes hangover, good for pt with early morning waking

Triazolam: <3hλ, good for someone who can't fall asleep but will stay asleep. May cause rebound insomnia. Should not be used chronically: Psychosis. (Largely replaced by BZ1 specific Rx's: Zolpidem (ambien), Zalplon (Sonata), Eszpiclone (Lunesta))

Side Effects: paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 32

Rx Seizures

Back 32

Clonazepam (Klonopin) used to prevent absence seizures

Diazepam (Valium) and Lorazepam (Ativan) given IV for status epilepticus

Front 33

Rx sedation/anesthesia

Back 33

Midazolam (Versed): preparation for anesthesia and short surgical procedures

-zapam's; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

MUST BE GIVEN IV, 2hλ, short duration of action

Side Effects: Anterograde Amnesia

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 34

Rx Muscle Relaxant vs Spasm Injuries

Back 34

Diazepam (Valium): Benzodiazepine with unique uses & PhK

Uses: muscle relaxn vs spasm, anti-convulsant (IV vs status epilepticus), ETOH/Barbituate WD (Valium & Librium)

~2dλ → active nordiazepam~1dλ → active oxazepam 8hλ

Hint 34

Bonzodiazepines: anxiolytics
--Mech: ↑ GABA-GABAa binding
--PhK: Oral-Hepatic: CYP3A4 & 2C19 (∅ΔCYP's)
--SE: paradoxical excitement, CNS depression (tolerance dvlps); normal [Rx]+ETOH = fatal;
--OD: ↓ GABA release at [Rx]high; intrinsic ceiling
--WD: long λ's & active metabolites = good taper;
----seizures if chronic [Rx]high
--Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)]

Front 35

Rx withdrawal from ETOH and Barbituates

Back 35

Chlordiazepxide (Librium) and Diazepam (Valium): long half-lifes, active metabolites

Daizepam: 43h λ; Duration increased by cimetidine;

Both converted to desmethyldiazapam (>24h λ), then to oxazepam (8h λ);

benzodiazepine; bind to GABAa, enhances GABA binding, but inhibits GABA release at high [Rx]: produces intrinsic ceiling.

Side Effects: paradoxical excitement, CNS depression (tolerance dvlps), OD=long sleep, but normal [Rx]+ETOH = fatal; tol/dep w/ chronic use; abrupt stop= Sx rebound; high [Rx] long time = severe withdrawal (seizures)

Contras: children (LTP), preggers (D), sleep apnea (relaxes pharynx)

Front 36

Flumazenil (Romazicon)

Back 36

IV Benzodiazepine antagonist

to reverse CNS, respiratory depression

short λ, 30 minute duration, req's repeats vs long-acting BZD's

+Barb/EtOH/BZD dependence → seizures
+Barb/TCA OD → seizures

Front 37

Drug given to reverse respiratory depression of Midazolam

Back 37

Flumazenil (Romazicon): BZD antagonist

IV agent to reverse CNS, respiratory depression

short λ, 30 minute duration, req's repeats vs long-acting BZD's

+Barb/EtOH/BZD dependence → seizures
+Barb/TCA OD → seizures

Front 38

Zolpidem
(Ambien)

Back 38

strong, rapid sedation, preserves deep sleep (3&4) with minor effect on REM sleep; recommended for short term use.

not a benzodiazepine, binds to alpha1 subunit of BZ1 subtype benzodiazepine receptor: no anxiolytic, anti-convulsant, muscle relaxing actions

oral, peak in 30 min, CYP3A4, 2hλ, extended release form available

should be used only when 8 hours of sleep available

Side Effects: CNS Depression, SLEEP DRIVING, Blackouts, GI. Additive with other CNS depressants. ∅ rebound insomnia, tolerance, dependence, daytime drowsiness.

sleep benefit may persist after discontinuation.

Front 39

BZ1 specific Rx's

Back 39

Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta): strong, rapid sedation, preserves deep sleep (3&4) with minor effect on REM sleep

not benzodiazepines, binds to alpha1 subunit of BZ1 subtype benzodiazepine receptor: no anxiolytic, anti-convulsant, muscle relaxing actions

oral, CYP3A4; Zolpidem 2hλ, Zaleplon 1hλ, eszopiclone 6hλ All should be used only when 8 hours of sleep available.

Side Effects: CNS Depression, SLEEP DRIVING, Blackouts, GI. Additive with other CNS depressants. Does not produce rebound insomnia (Esz does), tolerance, dependence, daytime drowsiness. Prolonged eszopliclone use has demonstrated withdrawal Sx (anxiety, seizures)

Tolerance Rare, sleep benefit may persist after discontinuation.

Front 40

Sleep Driving

Back 40

Mostly Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta)

Less potently: Dalmane (flurazepam hydrochloride); Doral (quazepam); Halcion (triazolam); Lunesta (eszopiclone); Prosom (estazolam); Restoril (temazepam); Rozerem (ramelteon); Seconal (secobarbital sodium)

Front 41

Zaleplon

Back 41

Sonata: strong, rapid sedation, preserves deep sleep (3&4) with minor effect on REM sleep; approved for short term (7-10day) use

not a benzodiazepine, binds to alpha1 subunit of BZ1 subtype benzodiazepine receptor: no anxiolytic, anti-convulsant, muscle relaxing actions

oral, CYP3A4; Zaleplon 1hλ, should be used only when 8 hours of sleep available.

Side Effects: CNS Depression, SLEEP DRIVING, Blackouts, GI. Additive with other CNS depressants. Does not produce rebound insomnia, tolerance, dependence, daytime drowsiness.

Tolerance Rare, sleep benefit may persist after discontinuation.

Front 42

Sonata

Back 42

Zaleplon: strong, rapid sedation, preserves deep sleep (3&4) with minor effect on REM sleep; approved for short term (7-10day) use

not a benzodiazepine, binds to alpha1 subunit of BZ1 subtype benzodiazepine receptor: no anxiolytic, anti-convulsant, muscle relaxing actions

oral, CYP3A4; Zaleplon 1hλ, should be used only when 8 hours of sleep available.

Side Effects: CNS Depression, SLEEP DRIVING, Blackouts, GI. Additive with other CNS depressants. Does not produce rebound insomnia, tolerance, dependence, daytime drowsiness.

Tolerance Rare, sleep benefit may persist after discontinuation.

Front 43

Lunesta

Back 43

Eszopiclone: strong, rapid sedation, preserves deep sleep (3&4) with minor effect on REM sleep; approved for long term use.

not a benzodiazepine, binds to alpha1 subunit of BZ1 subtype benzodiazepine receptor: no anxiolytic, anti-convulsant, muscle relaxing actions

oral, CYP3A4; 6hλ, more likely to cause morning grogginess, should be used only when 8 hours of sleep available.

Side Effects: CNS Depression, SLEEP DRIVING, Blackouts, GI. Additive with other CNS depressants. Tolerance, dependence, daytime drowsiness. Does produce rebound insomnia. Prolonged eszopliclone use has demonstrated withdrawal Sx (anxiety, seizures).

Tolerance Rare, sleep benefit may persist after discontinuation.

Front 44

Eszopiclone

Back 44

Lunesta: strong, rapid sedation, preserves deep sleep (3&4) with minor effect on REM sleep; approved for long term use.

not a benzodiazepine, binds to alpha1 subunit of BZ1 subtype benzodiazepine receptor: no anxiolytic, anti-convulsant, muscle relaxing actions

oral, CYP3A4; 6hλ, more likely to cause morning grogginess, should be used only when 8 hours of sleep available.

Side Effects: CNS Depression, SLEEP DRIVING, Blackouts, GI. Additive with other CNS depressants. Tolerance, dependence, daytime drowsiness. Does produce rebound insomnia. Prolonged eszopliclone use has demonstrated withdrawal Sx (anxiety, seizures).

Tolerance Rare, sleep benefit may persist after discontinuation.

Front 45

Melatonin

Back 45

used as a sleep aid, effective in some people

Side effects include HA, rash, possible hormone interactions

Front 46

Ramelteon
(Rozerem)

Back 46

MT1 & MT2 melatonin receptors agonist

Regulate circadian rhythm: decreases both delay to sleep onset and total sleep time
No rebound insomnia/withdrawal, no effect on REM

Oral, CYP1A2 or CYP2A9, extensive first pass metabolism,

SE: rare, possible increase in prolactin, decrease in testosterone, adrenocortical insufficiency

Contra: Severe Liver Disease

Front 47

Antihistamines as Sedatives

Back 47

Diphenhydramine (Benadryl), Promethazine (Phenergan)

Active ingredients in most OTC sedatives

useful for occasional insomnia, esp in someone addicted to benzodiazpeines or ETOH

Front 48

Diphenhydramine

Back 48

Benadryl: Antihistamine, Blocks H1

Active ingredients in most OTC sedatives

useful for occasional insomnia, esp in someone addicted to benzodiazpeines or ETOH

Front 49

Benadryl

Back 49

Diphenhydramine: Antihistamine, Blocks H1

Active ingredients in most OTC sedatives

useful for occasional insomnia, esp in someone addicted to benzodiazpeines or ETOH

Front 50

Phenergan

Back 50

Promethazine: Antihistamine, Blocks H1

Active ingredients in most OTC sedatives

useful for occasional insomnia, esp in someone addicted to benzodiazpeines or ETOH

Front 51

Promethazine

Back 51

Phenergan: Antihistamine, Blocks H1

Active ingredients in most OTC sedatives

useful for occasional insomnia, esp in someone addicted to benzodiazpeines or ETOH

Front 52

Chloral Hydrate

Back 52

Notec, Somnos: used in children for conscious sedation during pediatric dental procedures: anxiolytic, sedative, analgesic

converted into body to trichloroethanol, causes sedation
acts similar to bbarbituates on GABAa

Tolerance and Dependence may occur

Side Effects: Unpleasant Taste, Nau/Vom, Gastric irritation, allergic rxn, cardiac arrythmias, long term use liver damage, fatal intoxication LOW MARGIN OF SAFETY: respiratory, vasomotor depression

Very cheap: used in nursing homes, chronic care

Front 53

Rx for conscious sedation in pediatric dental procedures

Back 53

Chloral Hydrate (Notec, Somnos): used in children for conscious sedation during pediatric dental procedures: anxiolytic, sedative, analgesic

converted into body to trichloroethanol, causes sedation
acts similar to bbarbituates on GABAa

Tolerance and Dependence may occur

Side Effects: Unpleasant Taste, Nau/Vom, Gastric irritation, allergic rxn, cardiac arrythmias, long term use liver damage, fatal intoxication LOW MARGIN OF SAFETY: respiratory, vasomotor depression

Very cheap: used in nursing homes, chronic care

Front 54

Rx Sedative of Nursing Homes

Back 54

Chloral Hydrate (Notec, Somnos): used in children for conscious sedation during pediatric dental procedures: anxiolytic, sedative, analgesic

converted into body to trichloroethanol, causes sedation
acts similar to bbarbituates on GABAa

Tolerance and Dependence may occur

Side Effects: Unpleasant Taste, Nau/Vom, Gastric irritation, allergic rxn, cardiac arrythmias, long term use liver damage, fatal intoxication LOW MARGIN OF SAFETY: respiratory, vasomotor depression

Very cheap: used in nursing homes, chronic care

Front 55

Buspirone
(Buspar)

Back 55

Relieves anxiety s producing sedation. Good choice for recovering alcoholics, addicts and elderly. (also PMS and autism)

Partial 5HT1A agonist:presynaptic hippocampal subtype (anxiety)
↓ 5HT from dorsal raphe
↑ noradrenergic and DA pathways (good for someone very anxious and slightly depressed)

takes about 2 weeks to develop, very low addiction potential
Does not potentiate CNS depression w/ ETOH/Benzos, will not prevent withdrawal Sx of ETOH/Benzos, no learning/memory impairment

PhK: Oral with first pass, CYP3A4

SE: Restlessness
Contra: w/ MAOI's (BP spike)

Front 56

Good Anxiolytic for recovering addicts

Back 56

Buspar: Releive anxiety without producing sedation. Good choice for recovering alcoholics, addicts and elderly. (also PMS and autism)

Partial 5HT1A agonist:presynaptic hippocampal subtype (anxiety)
Decreases 5HT from dorsal raphe, increases noradrenergic and DA pathways (good for someone very anxious and slightly depressed)

takes about 2 weeks to develop, very low addiction potential
Does not potentiate CNS depression w/ ETOH/Benzos, will not prevent withdrawal Sx of ETOH/Benzos, no learning/memory impairment

Oral with first pass, CYP3A4

Side Effx: Restlessness
Contra: w/ MAOI's (BP spike)

Front 57

Anxiolytic contraindicated with MAOI's

Back 57

Buspar: Releive anxiety without producing sedation. Good choice for recovering alcoholics, addicts and elderly. (also PMS and autism)

Partial 5HT1A agonist:presynaptic hippocampal subtype (anxiety)
Decreases 5HT from dorsal raphe, increases noradrenergic and DA pathways (good for someone very anxious and slightly depressed)

takes about 2 weeks to develop, very low addiction potential
Does not potentiate CNS depression w/ ETOH/Benzos, will not prevent withdrawal Sx of ETOH/Benzos, no learning/memory impairment

Oral with first pass, CYP3A4

Side Effx: Restlessness, HA's but tolerance dvlps
Contra: w/ MAOI's (BP spike)

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Kava

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Mild herbal OTC anxiolytic

potentiates CNS depressence

severe liver damage to the point of needing transplants

contraindicated during pregnancy: no safety data available

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Valerian

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herbal anxiolytic often combined with chamomile

MAY BE HEPATOTOXIC
should not be used in pregnancy

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Beta adrenergic anxiolytics

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such as proranolol prevent the ANS sx of stage fright but have no effect on the anxiety itself.