ANXIOLYTICS & HYPNOTICS PART 2

Pharmacology 1
PREFINALS || (BS-Pharmacy, 2ND YR) | MAAM THESSALY NGO | 2ND SEMESTER 2023-2024

BARBITURATES

• Formerly the mainstay of treatment to sedate the patient

• largely replaced by the BNZ; barb induces tolerance, drug metabolizing enzyme, physical
dependence & associated w/ very severe withdrawal symptoms
• Has the ability to cause Coma
• Cannot be dispensed easily; must have S2 licensed & drug must be in double lock
• Need to maintain to 2-5 years
MECHANISM OF ACTION
- Selective hypnotic action of the barbiturates is due to their interaction with GABAA
receptors which enhances GABAAergic transmission
- Blocks excitatory glutamic receptors.
DURATION OF ACTION FOR BARBITURATES
ULTRA SHORT ACTING (20 SHORT ACTING LONG ACTING
mins) (3-8 hrs) (1-2 days)
Thiopental Pentobarbital Phenobarbital
Secobarbital
Amobarbital
THERAPEUTIC USES
ANESTHESIA - ultra-short acting barbiturates
- thiopental
- iv administration to induced anesthesia
ANTI CONVULSANT - MOST = Phenobarbital
FAMOUS
- DO = Febrile Seizures in children long term
- C management of tonic clonic seizure, status
epilepticus & eclampsia
- ECLAMPSIA = seizure/coma in a pregnant woman
- must be used cautiously to avoid child cognitive

ANXIETY - used as mild sedatives to relieve anxiety, nervous tension and

insomnia.
- when used as hypnotic, they suppress REM sleep
ADVERSE EFFECTS
- drowsiness
- impaired concentration
- mental & physical sluggishness
- a target for cytochrome P450; ↓ the duration of action to drugs that are metabolized by
these hepatic enzymes
- ↑ the porphyrin synthesis
- CONTRAINDICATION = pt. w/ acute intermittent porphyria
ANXIOLYTICS & HYPNOTICS PART 2
Pharmacology 1
PREFINALS || (BS-Pharmacy, 2ND YR) | MAAM THESSALY NGO | 2ND SEMESTER 2023-2024
- withdrawal is much more severe than associated w/ opiates that causes death
ETHANOL - CNS depressant effects of barbiturates synergized
- excessive drug hungover
POISONING - leading cause of death resulting drug overdose for many decades
- includes artificial respiration & purging the stomach from contents
- severe depression of respiration coupled w/ central cardiovascular
depression results in shock like condition
- alkalization of the urine often aids in the elimination of Phenobarb.

OTHER HYPNOTIC AGENTS

1. ZOLPIDEM
• not a benzodiazepine in action but acts on a subset of benzodiazepine receptor fam
• not anti-convulsant / muscle relaxant
• shows few withdrawal effects
• exhibits minimal rebound insomnia
• absorbed from the G.I tract
• little or no tolerance occurs w/ prolonged use
• HALF LIFE = 2-3 hours

2. ZALEPLON
• similar effects to zolpidem in its hypnotic action
• causes residual effects on psychomotor & cognitive functions
• has rapid elimination
• HALF LIFE = 1 hour

3. ESZOPICLONE
• oral non-benzodiazepines
• similar effects to zolpidem & zaleplon in its hypnotic action
• USES = treat insomnia
• DRUG EFFECT = up to 6 months compared to a placebo
•
•
• METABOLIZED IN = oxidation & demethylation via cytochrome enzyme system
• EXCRETION = urine
• DRUG ABSORPTION = 1 hour
• HALF LIFE = 6 hours

4. RAMELTEON
• USES = insomnia in which falling asleep (↑ sleep latency) is the primary complaint
ANXIOLYTICS & HYPNOTICS PART 2
Pharmacology 1
PREFINALS || (BS-Pharmacy, 2ND YR) | MAAM THESSALY NGO | 2ND SEMESTER 2023-2024
• minimal drug abuse
• no evidence for drug dependence / withdrawal
• prolactin levels
• ADVERSE EFFECT = fatigue &

5. CHLORAL HYDRATE
• AKA = Knock out drug
• ONSET OF ACTION = 30 minutes
• DURATION OF ACTION = 6 hours
• irritates the G.I tract
• has synergistic effect on Ethanol

6. ETHANOL
• anxiolytic & sedative effect • most abused drug
• ↓ DOSE = acts as stimulant
• ↑ DOSE = acts as depressant/hypnosis
• shallow dose response curve
• ROUTE OF ADMIN = orally
• METABOLIZED IN = liver (primary)
• acetaldehyde → alcohol dehydrogenase
• FUNCTIONAL GROUP = ACETATE → ESTER
• CARDIOMYOPATHY = heavy drinking
• CHEMICAL FORMULA = c2h6o1

7. DISULFIRAM
• CAUSE = excessive light hungover
• stops OH ingestion
• blocks the oxidation of acetaldehyde → acetic acid

• USES = pt. who wants to stop alcohol ingestion (stop drinking)

• CONTRAINDICATION = Metronidazole (antibiotic)

8. NALTREXONE
• DURATION OF ACTION = long acting
• opiate antagonist
• USES = antidote for opiate poisoning
• ROUTE OF ADMIN = orally or long acting injectable
ANXIOLYTICS & HYPNOTICS PART 2
Pharmacology 1
PREFINALS || (BS-Pharmacy, 2ND YR) | MAAM THESSALY NGO | 2ND SEMESTER 2023-2024

9. ACAMPROSATE
• stops alcoholism

ADDITIONAL NOTES

Other anxiolytic Drugs:

BUSPIRONE
 useful in the treatment of
generalized anxiety disorder.
 appear to be mediated by
serotonin receptors.

PROLACTIN
allow the production of
milk
OXYTOXIN
 opposite of the prolactine.
 letting the milk out.

HYDROXINE
 Anti-histamine with
antimemitic activity
 low tendency of
babitucitation.
ANXIOLYTICS & HYPNOTICS PART 2
Pharmacology 1
PREFINALS || (BS-Pharmacy, 2ND YR) | MAAM THESSALY NGO | 2ND SEMESTER 2023-2024
LORAZEPAM
 Used to treat insomnia
caused by anxiety or
temporary situational stress
 Used to relieve anxiety

SSRI
 Serotonin selective
reuptake inhibitor
TCA
 Tricyclic Anti-
depressant
MAD
 Monoamine oxidase

VENLAFAXINE AND DULOXETINE

 Treatment of major depressive disorder (MDD) and generalized anxiety disorder (GAD)