ANXIOLYTICS is a topic covered in the Harrison's Manual of Medicine.

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Benzodiazepines bind to sites on the γ-aminobutyric acid receptor and are cross-tolerant with alcohol and with barbiturates. Four clinical properties: (1) sedative, (2) anxiolytic, (3) skeletal muscle relaxant, and (4) antiepileptic. Individual drugs differ in terms of potency, onset of action, duration of action (related to half-life and presence of active metabolites), and metabolism (Table 197-2). Benzodiazepines have additive effects with alcohol; like alcohol, they can produce tolerance and physiologic dependence, with serious withdrawal syndromes (tremors, seizures, delirium, and autonomic hyperactivity) if discontinued too quickly, especially for those with short half-lives.

TABLE 197-2: ANXIOLYTICS
NameEquivalent PO Dose, mgOnset of ActionHalf-Life, hComments
Benzodiazepines
 Diazepam (Valium)5Fast20–70Active metabolites; quite sedating
 Flurazepam (Dalmane)15Fast30–100Flurazepam is a prodrug; metabolites are active; quite sedating
 Triazolam (Halcion)0.25Intermediate1.5–5No active metabolites; can induce confusion and delirium, especially in elderly
 Lorazepam (Ativan)1Intermediate10–20No active metabolites, direct hepatic glucuronide conjugation, quite sedating, FDA approved for anxiety with depression
 Alprazolam (Xanax)0.5Intermediate12–15Active metabolites,; not too sedating, FDA approved for panic disorder and anxiety with depression, tolerance and dependence develop easily, difficult to withdraw
 Chlordiazepoxide (Librium)10Intermediate5–30Active metabolites, moderately sedating
 Oxazepam (Serax)15Slow5–15No active metabolites, direct glucuronide conjugation, not too sedating
 Temazepam (Restoril)15Slow9–12No active metabolites, moderately sedating
 Clonazepam (Klonopin)0.5Slow18–50No active metabolites, moderately sedating, FDA approved for panic disorder
 Clorazepate (Tranxene)15Fast40–200Low sedation, unreliable absorption
Nonbenzodiazepines
 Buspirone (BuSpar)7.52 weeks2–3Active metabolites, tid dosing—usual daily dose 10–20 mg tid, nonsedating; no additive effects with alcohol, useful for controlling agitation in demented or brain-injured pts

Buspirone is a nonbenzodiazepine anxiolytic that is nonsedating, is not cross-tolerant with alcohol, and does not induce tolerance or dependence. It requires at least 2 weeks at therapeutic doses to achieve full effects.

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TY - ELEC T1 - ANXIOLYTICS ID - 623498 Y1 - 2017 PB - Harrison's Manual of Medicine UR - https://harrisons.unboundmedicine.com/harrisons/view/Harrisons-Manual-of-Medicine/623498/all/ANXIOLYTICS ER -