Sedative and Hypnotic Drugs Flashcards
Alprazolam
Pharmacokinetics (2), Indications (2) and Contraindications (3)
Intermediate half life (12-15 hours)
Fast onset
Anxiety
Panic Disorder
Acute angle glaucoma
Ketoconazole use
Itraconazole use
Midazolam
Pharmacokinetics (1) Indication, Black Box Warning
Short half life
Given IV or IM for pre-op sedation or anxiolysis
Respiratory depression or arrest especially in noncritical are settings
Diazepam
Pharmacokinetics (2) Metabolite, Indications (2) Contraindications (6)
Long half life (100 hours)
Very fast onset
N-desmethyldiazepam (active)
Anxiety
Acute Alcohol Withdrawal Symptoms
< 6 years old Myasthenia gravis Respiratory insufficiency Cirrhosis/Liver Insufficiency Sleep apnea Acute angle glaucoma
Oxazapam
Pharmacokinetics (2) and Indications (3)
Intermediate half life
Slow onset
Anxiety
Anxiety with depression
Acute alcohol withdrawal
Triazolam
Pharmacokinetics (2), Indication, Black Box Warning
Short half life
Intermediate onset
Short term relief of insomnia (7-10 days)
Use with opioids causes respiratory depression, coma and death
Chlordiazepoxide
Pharmacokinetics (2) Indications (3) and Black Box Warning
Long half life
Intermediate onset
Anxiety
Alcohol withdrawal
Pre-Op anxiety
Use with opioids causes respiratory depression, coma and death
Flurazepam
Pharmacokinetics (2) and Indication
Long half life
Fast onset
Short term relief of insomnia
Lorazepam
Pharmacokinetics (2) and Indications (3)
Intermediate half life
Intermediate onset
Seizures
Epilepsy
Pre-Op
Benzodiazepine Pharmacokinetics
Short Acting Drugs (5) and Long Acting Drugs (3)
Midazolam Oxazepam Alprazolam Temazepam Triazolam
Diazepam
Lorazepam
Clonazepam
Flumazenil
Mechanism of Action, Indications (2) and Black Box Warning
Competitive antagonist of Benzodiazepine receptors
Reverse sedation via anesthesia
Treat benzodiazepine overdose
Seizures possible especially with long term sedation or patient overdose
Barbiturates (“tal” drugs)
Indications (5)
Extreme insomnia Refractory seizures Tension headaches Counteract stimulant drugs Anesthesia
Thiopental
Administration, Pharmacokinetics, Indications (4) Side Effects (3)
IV only
Ultra short acting
Brief surgical procedures
Balanced anesthesia
Convulsions
Increased ICP
Respiratory depression
Myocardial depression
Arrhythmias
Secobarbital
Pharmacokinetics, Indications (2), Contraindications (3)
Short acting
Short term insomnia relief
Pre anesthetic
Porphyria
Liver failure
Obstructive lung disease
Phenobarbital
Pharmacokinetics, Indications (2) Contraindication, Side Effects (2)
Long acting
Sedation/Hypnosis
Seizures
Porhpyria
Exacerbates depression and suicidality
Strongly induces CYP450**
Buspirone
Indication, Timeline, Pertinent Negatives (5), Metabolism
Anxiety
Takes over a week for response
Does not cause:
Sedation, hypnosis, muscle relaxation, euphoria, anticonvulsive effects
CYP3A4 metabolized
Zaleplon
Mechanism of Action, Indication
acts on GABA-BZ receptor complex (GABAa)
Short term insomnia treatment
Zolpidem
Pharmacokinetics, Indication, Interactions (2), Side Effects (2)
Biphasic release formula
Relief of insomnia (up to 35 days)
CNS depressants
Alcohol has additive effect on psychomotor impairment
Worsens depression and suicidality
Ramelteon
Mechanism of Action, Indication, Metabolism
Full agonist of MT1/MT2 receptors
Treatment of insomnia with difficulty with sleep onset
CYP1A2 metabolized
Eszopiclone
Indication, Side Effects (8) Contraindications (5)
Insomnia
Unpleasant taste Headaches Respiratory infections Dizzy Dry mouth Rash Anxiety Hallucinations
Use with alcohol Liver failure Impaired respiratory function Impaired drug metabolism Clotting conditions
Meprobamate
Mechanism of Action and Use
Slows brain for anxiety treatment
Chloral Hydrate Uses (2)
Sedative for sleep
Alcohol withdrawal
