The pharmacology, pharmacokinetics, drug interactions, adverse effects
, indications for use, efficacy, dosage, and pattern of use of antipsy
chotics in adults older than 65 years are reviewed. Most available ant
ipsychotic agents block dopamine type 2 postsynaptic receptors. Antips
ychotics also bind to cholinergic, alpha-adrenergic, histamine type 1,
and serotonin receptors. The affinities of a given agent for receptor
s determine its adverse effects and probably its efficacy. There are m
any obstacles to therapeutic drug monitoring. Many antipsychotics are
metabolized into multiple active compounds. Drug clearance from brain
tissue may be slower than from plasma. Therapeutic steady-state concen
trations are difficult to define. Age-related physiological changes al
ter the pharmacokinetic and pharmacodynamic characteristics of antipsy
chotics, placing the elderly adult at heightened risk for adverse effe
cts. Agents that may interact with the antipsychotics include carbamaz
epine, phenytoin, phenobarbital, tricyclic antidepressants, and lithiu
m. Adverse effects frequently observed in the elderly are orthostatic
hypotension, anticholinergic effects, pseudoparkinsonism, and tardive
dyskinesia. Neuroleptic malignant syndrome is a rare but potentially f
atal reaction. The antipsychotics carry approved labeling for use in t
reating psychotic disorders; many antipsychotics are approved for use
in treating other conditions as well, such as behavioral problems. The
Omnibus Budget Reconciliation Act of 1987 established dosage and docu
mentation guidelines for antipsychotic drug use in residents of nursin
g homes. The guidelines specify that antipsychotics should not be used
in this population if the only indication is a problem behavior like
wandering. Although antipsychotics are often prescribed for behavioral
control in older adults, most studies show only modest efficacy, whil
e some show worsening of symptoms. As needed orders for antipsychotics
are controversial. Antipsychotics can relieve symptoms in the older a
dult, but lower dosages and more frequent assessments are necessary th
an for younger adults.