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BenzodiazepineAka: Sedative-Hypnotic

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  1. Indications
    1. Anxiety Disorder
    2. Sedation
      1. Insomnia
      2. Surgical, Medical and Psychiatric procedures
    3. Muscle spasm
    4. Seizure disorder
    5. Alcohol Withdrawal and withdrawal from other drugs
  2. Mechanism
    1. Potentiates activity of gamma-aminobutyric acid (GABA)
    2. GABA is an inhibitory neurotransmitter in the CNS
      1. Muscle relaxant
      2. Anticonvulsant
      3. Anxiolytic
      4. Anti-aggressiveness
      5. Sedation
  3. Advantages
    1. Rapid onset of action
      1. Anxiolytic effect within 1-2 days
    2. Tolerance develops rapidly to adverse effects
    3. Tolerance does not develop for Anxiolytic effect
    4. Few drug interactions
    5. Good safety profile
  4. Preparations
    1. Long Acting Benzodiazepines
      1. Chlordiazepoxide (Librium)
      2. Diazepam (Valium, Valrelease)
      3. Flurazepam (Dalmane)
      4. Chlorazepate (Tranxene)
      5. Clonazepam (Klonopin)
      6. Quazepam (Doral)
      7. Halazepam (Paxipam)
    2. Medium Acting Benzodiazepines
      1. Lorazepam (Ativan)
      2. Temazepam (Restoril)
    3. Short acting Benzodiazepines
      1. Oxazepam (Serax)
      2. Alprazolam (Xanax)
      3. Triazolam (Halcion)
      4. Estazolam (Prosom)
      5. Midazolam (Versed)
  5. Absorption
    1. Preparations with most rapid absorption
      1. Diazepam (Valium)
      2. Clorazepate
      3. Alprazolam (Xanax) taken sublingually
    2. Preparations with slowest absorption
      1. Oxazepam (Serax)
      2. Co-administration of benzodiazepine with medication
        1. Maalox
        2. Gelusil
  6. Metabolism
    1. Hepatic Metabolism
      1. Microsomal oxidation
      2. Conjugation by glucuronyl transferases
    2. Renal Excretion
  7. Dosing strategies
    1. Initiate treatment with low dose benzodiazepine
    2. Prevent symptoms completely by using a regular regimen
    3. Escalate dose slowly, no more often than every 2 weeks
    4. Maintain lowest effective dose for several months
    5. Periodically attempt to lower dose
    6. Start taper at 25% decrements and slow when below 50%
    7. Decrease dose slowly, no more often than every 4 weeks
    8. Change to longer half-life drug if symptom breakthrough
      1. Example: Switch from Xanax to Klonopin
  8. Equivalent Dosing to Valium 60 mg (for withdrawal)
    1. High Potency Benzodiazepines
      1. Alprazolam (Xanax) 6 mg
      2. Clonazepam (Klonopin) 24 mg
      3. Lorazepam (Ativan) 12 mg
    2. Low Potency Benzodiazepines
      1. Chlordiazepoxide (Limbitrol) 150 mg
      2. Flurazepam (Dalmane) 90 mg
      3. Halazepam (Paxipam) 240 mg
      4. Oxazepam (Serax) 60 mg
      5. Temazepam (Restoril) 60 mg
  9. Pregnancy and Lactation
    1. Pregnancy Category: D
    2. Lactation: Not allowed
  10. References
    1. Tasman (1997) Psychiatry :
    2. Katzung (1989) Pharmacology :

Benzodiazepines (C0005064)

Definition (MSH)A group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring. Permitted is any degree of hydrogenation, any substituents and any H-isomer.
Definition (CSP)bicyclic structure consisting of fused benzene and diazepine rings; many compounds with this structure have psychotropic and neurotropic properties, and are used as sedatives, anticonvulsants, muscle relaxants, and in related applications.
Definition (NCI)Drugs from this chemical class are used for their central nervous system depressant properties including sedation, facilitation of sleep, seizure control, general anesthesia, anxiolytic, amnestic, and for detoxification from similar (cross tolerant) drugs
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD001569
Englishbenzodiazepine, Benzodiazepine antiepileptic, Benzodiazepine Compounds, BENZODIAZEPINE CPDS, Benzodiazepines
Spanishbenzodiacepina, benzodiazepina
Parent ConceptsBenzazepines (C0005034), diazepine (C0596434), Anti-Anxiety Agents (C0040616), anxiolytic, sedative, and hypnotic agent (C0280078), Anticonvulsants (C0003286), Hypnotics (C0020591), Anxiolytic, sedative AND/OR hypnotic (C1268921), Drug allergen (C1320237), Duplicate concept (C1274013)
SourcesAOD, CSP, LCH, LNC, MSH, MTH, NCI, NDFRT, PDQ, SCTSPA, SNOMEDCT
Derived from the NIH UMLS (Unified Medical Language System)



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