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49 Cards in this Set
- Front
- Back
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Sedative hypnotics and anti-anxiety Drugs
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Barbituates
Benzodiazepines Benzodiazepine antagonist Others (hypnotics) |
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Barbituates
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1) Phenobarbital
2) Pentobarbital 3) Secobarbital 4) Thiopental |
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Benzodiazepines
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Diazepam Temazepam
Chlordiazepoxide Triazolam flurazepam Alprazolam Etazolam Lorazepam Midazolam Clorazepate Oxazepam |
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Benzodiazepine antagonist
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Flumazenil
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Others
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Zolpidem(Ambien) chloral hydrate
Zaleplon(Sonata) Eszopiclone(Lunesta) Ramelteon Buspirone |
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Mechanism of Barbituates
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Increase duration of GABA action
May increase Cl- influx independent of GABA. CNS Depressant |
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Pharmacokinetics of Barbituates
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Absorbed orally and enter CNS easily
Metabolized by liver P450 inducer |
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Uses of Barbituates
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1) induction of anesthesia
2)Anticonvulsants 3) Decrease GI motility and spasms |
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Side effects of Barbituates
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CNS Depression
Decreased REM sleep Paradoxical excitement GI symptoms Allergies Vertigo |
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Toxicity of barbituates
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when combined with alcohol
Respiratory depression, coma and death Low margin of safety TX:alkalinization of urine, supportive |
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Contraindications for Barbituates
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Pulmonary insufficiency
Porphyria |
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Dependence of Barbituates
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Severe physiological and physical dependence
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Withdrawal of Barbituates
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Withdrawal can be life threatening seizures, hypotension, anxiety, hyperactive reflexes, weakness
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Benzodiazepines
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Most Commonly used anti-anxiety drugs. also used for hypnosis, muscle relaxation and anticonvulsant.
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Benzodiazepines
Mechanism of action |
bind receptor GABAa
Intesify GABA action Increased Benzodiazepine decreas GABA release. Ceiling effect |
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Benzodiazepines
Pharacokinetics |
Orally well absorbed
Given IV in emergencies Converted to active metabolites |
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Long acting Benzodiazepines
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Diazepam (t 0.5= 43hrs)
Flurazepam (t 0.5= 74hrs) Chlordiazepoxide Desmethyldiazepam(t 0.5= 24hrs |
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Intermediate acting Benzodiazepines
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Oxazepam
Lorazepam Both conjugated to inactive metabolites |
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Short acting Benzodiazepines
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Alprazolam (t 0.5= 12hrs)
Triazolam (t 0.5< 3hrs) Midazolam (t 0.5=2hrs) |
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Drug interactions of Benzodiazepines
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Extensive liver metabolism
Does not induce liver enzymes Cimetidine lengthens elimination t 0.5 of diazepam |
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Side effects of Benzodiazepines
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1)CNS depression
2)Blurred visions and hallucinations 3)Paradoxical excitement 4)Aggressive behavior 5)Learning and memory deficits in Children 6) Memory loss and confusion in elderly |
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Uses of Benzodiazepines
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1)Anxiety
2)Insomnia 3)Epilepsy and seizures 4)Sedation,amnesia, anesthesia 5)Muscle relaxation 6)Withdrawal from Alcohol and barbiturates |
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Anxiety disorders not treated with Benzodiazepines
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1)Obsessive complusive
2)Agoraphobia and panic 3)Anxiety in children and adolescents |
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Alprazolam (Xanax)
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anxiety and depression
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Benzodiazepines
Insomnia |
Flurazepam (long acting, hangover effect)
Temazepam Triazolam(Short acting, rebound insomnia) |
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Benzodiazepines
Epilepsy |
Clonazepam prevention of absence seizures
Diazepam and lorazepam IV for status eplepticus |
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Benzodiazepines
Sedation, amnesia, and anesthesia |
Midazolam- prep for anesthesia (IV), Rapid onset, short duration
Anterograde amnesia |
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Benzodiazepines
Muscle Relaxation |
Diazepam- acute muscle spasm or injury
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Benzodiazepines
Withdrawal from alcohol and barbiturates |
Chlordiazepoxide and diazepam provide tapered withdrawal
Prevent: seizures, hallucinations and delirium tremens |
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Contraindications for Benzodiazepines use
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Pregnancy
Children sleep apnea |
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Benzodiazepines
Overdose |
Long sleep duration 24-48 hrs
Fatal with Alcohol |
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Benzodiazepines
tolerance and dependence |
Abrupt discontinuation: rebound insomnia and anxiety
Withdrawal: Convulsions, GI, tremor, weight loss, Muscle weakness, hyperalgesia |
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Flumazenil
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Benzodiazepine antagonist
Reverse CNS depression SE: withdrawal and seizures especially in alcoholics or overdose with barbiturates, and TCA |
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Zolpidem, Zaleplon, Eszopiclone
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Z-BZ1, short term use
E-all three subtypes, long term use GABA Mediated inhibition Strong rapid sedation minor effect on REM |
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ZZE
Pharmacokinetics |
Orally, peak levels 30 min
Metabolized in liver(cyp3a4) Excreted by the kidneys |
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ZZE
Side effects |
1)GI,
2)CNS drowsiness, Blackouts 3)Amnesia, increase depressant effects of other sedatives 4)Low day time sedation 5)Less likely to cause dependency than barbiturates 6)Rebound insomnia 7)Withdrawal (E)- CNS stimulation, anxiety and seizures 8) Elderly: confusion, falls memory loss |
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ZZE
Difficulty waking up? |
only with eszopiclone
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Ramelteon
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MT1 agonist
shortens delay to sleep onset and sleep duration |
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Ramelteon
Pharmokinetics |
1)Orally absorbed
2)High first pass effect CYP1A2 3)Caution in mild-mod liver disease 4)Contraindicated in severe liver disease |
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Ramelteon
Drug interactions |
Additive sedation: Alcohol other sedatives
Rifampin increases Metabolism of Ramelteon |
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Ramelteon
Metabolism is inhibited by: |
Ketaconazole and fluconazole
HIV protease inhibitors, Fluvoxamine |
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Ramelteon
Side effects |
1)drowsiness
2)dizziness and nausea 3)increase serum prolactin 4)no effect on REM 5)Low incidence of rebound insomnia or withdrawal |
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Chloral hydrate
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Converted to trichloroethanol
Acts on GABAa Low margin of safety |
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Chloral Hydrate Uses
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Conscious sedation: pediatric dental procedures
Nursing homes as sedative hypnotic |
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Buspirone
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1)Decrease anxiety w/o producing sedation
2)Takes 2 weeks to develop 3)Low addiction potential 4)Does not potentiate CNS depression |
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Buspirone
Mechanism |
1)5HT1a partial agonist in hippocampus
2)Decrease release of Serotonin from Dorsal raphe nucleus 3)Increase activity of noradrenergic and dopaminergic pathways |
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Buspirone
Pharmacokinetics |
1)Oral absorption
2)High first pass metabolism 3)Metabolized in liver(CYP3A4) 4)Excreted by Kidney |
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Buspirone
Uses |
1)Anxiety and anxiety w/ depression
2)PMS 3)Autistic anxiety 4)Good for recovering alcoholics/addicts, elderly 5)Children w/ ADD 6)Not good for severe anx/panic |
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Buspirone
Side Effects |
1)Dizziness, light headedness, headache, drowsiness, N/V
2)Restlessness 3)Increase BP with MAOI |
