Barbiturates

Serax

Oxazepam BN

Halcion

Triazolam BN

Klonopin, Rivotril

Clonazepam BN

Versed, Dormicum

Midazolam BN

Restoril

Temazepam BN

Ativan

Lorazepam BN

Xanax, Xanor

Alprazolam BN

Rohypnol

Flunitrazepam BN

Valium, Anxionil

Diazepam BN

Dalmane

Flurazepam BN

Librium

Chlordiazepoxide BN

Barbiturates

Former drug of choice for anxiety, insomnia

2, 4, 6-trioxohexahydropyrimidine

Barbiturates chemical name

Increase the duration of GABA mediated chloride in channel opening

GABA like action → ⬆ opening time of chloride channels → ⬆ conductance of chloride ion → hyperpolarization

Barbiturates MOA

Thiopental (Pentothal)

Ultra-short (20mins)

Pentobarbital (Nembutal)

Amobarbital (Amytal)

Short acting (3-8hrs)

Phenobarbital (Luminal)

Long-acting (1-2days)

Amobarbital (Amytal)

Butabarbital

Intermediate acting

Ultra short (20mins)

Thiopental (Pentothal)

Used as Pre anesthetic agent

Short acting (3-8hrs)

Pentobarbital (Nembutal)

Amobarbital (Amytal)

Have sedative-hyonotic activity

Long acting (1-2days)

Phenobarbital (Luminal)

Intermediate acting

Pentobarbital (Nembutal)

Amobarbital (Amytal)

With anticonvulsant activity

Thiopental (Pentothal)

Induction of anesthesia

Phenobarbital (Luminal)

For seizures in children

Pentobarbital (Nembutal)

Amobarbital (Amytal)

For anxiety

Addicting

Dependence

Effects of Barbiturates

Phenobarbital (Nembutal)

Capable of inducing the hepatic microsomal drug-metabolizing enzyme (CYP450)

Eszopiclone (Lunesta)

Zaleplon (Sonata)

Zolpidem (Ambien)

Newer hypnotics

Cyclopyyrrolone

Eszopiclone (Lunesta)

Pyrazalopyrimidine

Zaleplon (Sonata)

Imidazopyridine

Zolpidem (Ambien)

Sleep disorder

Newer hypnotics used in

Melatonin receptor agonist

Ramelteon (Rozerem) MOA

Ramelteon (Rozerem)

Activates MT1 and MT2 receptors in suprachiasmatic nuclei in the CNS

Ramelteon (Rozerem)

Rapid onset of effect with minimal rebound insomnia

Ramelteon (Rozerem)

Used with caution in patient with liver dysfunction

Dizziness, Somnolence, Fatigue, Endocrine changes (⬇Testosterone ⬆ Prolactin)

Ramelteon (Rozerem) ADRs

Ramelteon (Rozerem)

Metabolized by CYP1A2

Ciprofloxacin, Fluvoxamine, Tacrine, Zileuton

CYP1A2 inhibitors

Serotonin agonist

Buspirone MOA

Buspirone

Azapirone anxiolytic possess no anti-convulsant, muscle relaxant, hypnotic motor impairement and dependence properties

Buspirone

As serotonin partial agonist, it binds presynaptic to receptors in dorsal raphe and post synaptically to receptors in hippocampus and cortical brain areas

Generalized Anxiety Disorders

Buspirone is alternative for …

To patient who cannot tolerate the sedating effects and psychomotor impairment of Benzodiazepines

Buspirone

Possess both dopamine agonist and inderect dopamine antagonist properties

Management of chronic persistent anxiety

Buspirone is the agent of choice for the

Adrenergic blocking agents

Propanolol and other beta blockers

Propanolol or other beta blockers

Used as off label for anxiety

Propanolol and other beta blockers

May be useful in patient with prominent cardiovascular symptoms of anxiety

Propanolol and other beta blockers

Less effective anxiolytics than Benzodiazepines and their usefulness may be restricted to those anxiety patient with physical symptoms, especially cardiovascular complaints have not adequately responded to Benzodiazepines therapy

10 mg for stage fright

Propranolol … bid should be used initially and gradually titrated to anxiolytic response

Alcohols

Etchlorvynol

Chloral hydrate (Aquachloral)

Piperidinediones

Glutethimide

Methyprylon

Carbamates

Meprobamate

Old sedative hypnotics

Mickey Finn

Chloral hydrate (Aquachloral) associated to

Trichloroethanol

Chloral hydrate (Aquachloral) active metabolite

Trichloroacetic acid

Chloral hydrate (Aquachloral) toxic metabolite

Chloral hydrate (Aquachloral)

Accumulate with the nighty administration of the drug

Zolpidem (Ambien, Stilnox)

Not a Benzodiazepine but acts on Benzodiazepines receptor

Chloral hydrate (Aquachloral)

Knockout drops

For pre operative sedation

Chloral hydrate (Aquachloral) use

Diphenhydramine (Benadryl)

Doxylamine (Unisom)

Hydroxyzine (Atarax)

Antihistamines

Ambien, Stilnox

Zolpidem BN

(Aquachloral)

Chloral hydrate BN

(Benadryl)

Diphenhydramine BN

(Unisom)

Doxylamine BN

Atarax

Hydroxyzine BN

Etchlorvynol

Chloral hydrate (Aquachloral)

Alcohols

Glutethimide

Methyprylon

Piperidinediones

Meprobamate

Carbamates

Rozerem

Ramelteon BN

Pentothal

Thiopental BN

Nembutal

Pentobarbital BN

Amytal

Amobarbital

Luminal

Phenobarbital

Lunesta

Eszopiclone BN

Sonata

Zaleplon BN

Ambien

Zolpidem BN