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60 Cards in this Set

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Sedation vs Hypnosis
Sedation: reduced alertness, decreased motor activity, and relaxation

Hypnosis: state of drowsiness which leads to sleep
Ideal Anxiolytic
calm without causing daytime drowsiness or dependence, physiological or psychological
ideal Sedative-Hypnotic
All the user to fall asleep quickly, stay asleep quickly, not cause "hangover" drowsiness, high margin of safety and not effect on REM sleep.
what causes sleep
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
Barbituates
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).
Thiopental
An ultrashort acting barbituate used for anesthesia

______________________________________
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).
Phenobarbital
long-acting barbituate used as anticonvulsant

______________________________________
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).
Sedatives contraindicated in pulmonary insufficiency
Barbituates: Pentobarbital, Phenobarbital, Thiopental

______________________________________
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).
CNS Rx contraindicated in porphyria
Barbituates: Pentobarbital, Phenobarbital, Thiopental

______________________________________
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).
Benzodiazepines
[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)
Elderly with Alzheimers Sx on an Rx
Benzodiazepine (-zapam's)? Then it's probably a side effect.
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

____________________________________
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)]
Desmethyldiazepam
(Nordiazepam)
active metabolic byproduct of diazepam (Valium) and chordiazepoxide (Librium); >24h λ, then to oxazepam (8h λ); good taper for withdrawal.
Chlordiazepoxide (Librium)
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)]
Flurazepam
(Dalmane)
BZD used as hypnotic: less ↓ REM,

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

Side Effects: SLEEP DRIVING
________________________
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)
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)
Versed
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)
Temazepam
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)
Restoril:
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)
Triazolam
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)
Halcion
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)
Alprazolam
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)
Xanax:
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)
Lorazepam
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)
Ativan
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)
Sedative-Hypnotic Rx contraindicated by pregnancy
Benzodiazepines, Category D: Known Teratogen

Kava: no FDA safety data
Valerian: hepatotoxic
Sedative-Hypnotic Rx contraindicated for children
Benzodiazepines

Impair learning and memeory
Sedative-Hypnotic Rx contraindicated for spleep apnics
Benzodiazepines

Relax Pharyngeal Musculature
Anxiety Disorders NOT treated with Benzodiazepines
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
Rx Anxiety
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)
Benzodiazpeine Rx Insomnia

-Can't Fall Asleep
-Early Waking
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)
Rx Seizures
Clonazepam (Klonopin) used to prevent absence seizures

Diazepam (Valium) and Lorazepam (Ativan) given IV for status epilepticus
Rx sedation/anesthesia
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)
Rx Muscle Relaxant vs Spasm Injuries
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
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)]
Rx withdrawal from ETOH and Barbituates
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)
Flumazenil (Romazicon)
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
Drug given to reverse respiratory depression of Midazolam
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
Zolpidem
(Ambien)
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.
BZ1 specific Rx's
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.
Sleep Driving
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)
Zaleplon
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.
Sonata
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.
Lunesta
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.
Eszopiclone
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.
Melatonin
used as a sleep aid, effective in some people

Side effects include HA, rash, possible hormone interactions
Ramelteon
(Rozerem)
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
Antihistamines as Sedatives
Diphenhydramine (Benadryl), Promethazine (Phenergan)

Active ingredients in most OTC sedatives

useful for occasional insomnia, esp in someone addicted to benzodiazpeines or ETOH
Diphenhydramine
Benadryl: Antihistamine, Blocks H1

Active ingredients in most OTC sedatives

useful for occasional insomnia, esp in someone addicted to benzodiazpeines or ETOH
Benadryl
Diphenhydramine: Antihistamine, Blocks H1

Active ingredients in most OTC sedatives

useful for occasional insomnia, esp in someone addicted to benzodiazpeines or ETOH
Phenergan
Promethazine: Antihistamine, Blocks H1

Active ingredients in most OTC sedatives

useful for occasional insomnia, esp in someone addicted to benzodiazpeines or ETOH
Promethazine
Phenergan: Antihistamine, Blocks H1

Active ingredients in most OTC sedatives

useful for occasional insomnia, esp in someone addicted to benzodiazpeines or ETOH
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
Rx for conscious sedation in pediatric dental procedures
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
Rx Sedative of Nursing Homes
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
Buspirone
(Buspar)
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)
Good Anxiolytic for recovering addicts
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)
Anxiolytic contraindicated with MAOI's
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)
Kava
Mild herbal OTC anxiolytic

potentiates CNS depressence

severe liver damage to the point of needing transplants

contraindicated during pregnancy: no safety data available
Valerian
herbal anxiolytic often combined with chamomile

MAY BE HEPATOTOXIC
should not be used in pregnancy
Beta adrenergic anxiolytics
such as proranolol prevent the ANS sx of stage fright but have no effect on the anxiety itself.