At Any Age, It Does Matter:
Substance Abuse and Older Adults (for Professionals)

Supplements

Anxiolytics

A variety of anxiolytics are frequently prescribed for acute or chronic anxiety in older adults. Benzodiazepines are designated both as anxiolytics and sedative-hypnotics based on properties related to marketing. Some physicians may choose, for example, to use lorazepam (Ativan) as either an anxiolytic or sedative depending on the circumstances.

Commonly Prescribed Anxiolytics

Class Drug Brand Name Elimination Half-Life for Older Adults*
Benzodiazepines Alprazolam Xanax 9-20 hours
  Chlordiazepoxide Librium 5-30 hours, with short- and long-acting active metabolites
  Diazepam Valium 20-50 hours, with short- and long-acting active metabolites effective up to 200 hours
  Lorazepam Ativan 18-24 hours; clearance may be reduced in older adults
  Oxazepam Serax 3-25 hours
Serotonin agonist Buspirone BuSpar 1-11 hours

*Refer to product information insert for each drug as to its suitability for use in older adults.

An estimated 95 percent of benzodiazepine prescriptions for older adults in this country are ordered for anxiety and insomnia. Only 5 percent are used as adjuncts for general anesthesia, as muscle relaxants, or as anticonvulsants.1

Numerous studies have concluded that use of these agents is appropriate for the most part. There is only occasional overprescribing by physicians for some patient subgroups or misuse by patients.2-5

Misuse and Abuse

A small group of people has acknowledged taking benzodiazepines without a prescription. Most borrowed pills from significant others and used them for symptom relief, not recreational purposes. Moreover, worldwide experience with the short-term use of benzodiazepines to relieve acute anxiety, situational stress, and transient insomnia indicates that these medications are safe and effective.

The likelihood of dose increases, prolonged use, and addictive dependence is low.4 However, these drugs are often inappropriately used to treat depression, psychosis, and chronic insomnia.

Although most people use benzodiazepines for short periods without developing problems, others take them past the point where they are effective. These people risk adverse effects, including tolerance and abuse. By 1990, as many as a fourth of anxiolytic users had taken these medications for a year or more.3

Several studies in the United States and Britain confirm that long-term users (a year or more) of benzodiazepines are likely to be older than age 45 and female. They have substantial psychological stress, dysphoric or depressive symptoms, and multiple chronic physical illnesses or somatic problems.3,4

Benzodiazepine use for longer than 4 months is of particular concern among older adults. Benzodiazepines have variable rates of absorption, with metabolism occurring primarily in the liver.

The longer acting benzodiazepines have active metabolites, some with very long half-lives (e.g., up to 200 hours for flurazepam [Dalmane]). Thus, the duration of action is often longer than expected. They are also more likely to produce residual sedation and other adverse effects.

By contrast, some shorter acting benzodiazepines are not as likely to produce toxic or dependence-inducing effects with chronic dosing. One reason is that these drugs have no active metabolites.

An additional concern is that the oxidative pathway is often impaired in older adults and in those with liver disease. Therefore, it is best to choose drugs that are not metabolized this way. Such drugs include oxazepam (Serax) and lorazepam (Ativan). Because of the unpleasant and potentially hazardous side effects of many benzodiazepines, caution is needed in selecting the most appropriate benzodiazepine for elderly patients.

Withdrawal

Unfortunately, both long- and short-acting benzodiazepines tend to result in physiological dependence, even when taken at therapeutic doses and for as short as 2 months.7 Many of the most unpleasant withdrawal effects can be alleviated by gradually tapering the dose rather than stopping it abruptly. Even if the dose is tapered, however, withdrawal symptoms are experienced by 40 to 80 percent of people who discontinue benzodiazepines after 4 to 6 months of regular use.6,7

Symptoms that may occur after stopping either long or short half-life benzodiazepines include:

Symptoms usually peak toward the end of the tapered discontinuation and disappear altogether within 3 to 5 weeks.3,8 In a few psychiatric patients, the withdrawal syndrome has been known to persist for several months.9

The rebound effects experienced in withdrawal usually mimic the original symptoms for which the benzodiazepine was prescribed (e.g., anxiety, insomnia, panic). Those effects occur in as many as one-third to one-half of patients after even 1 or 2 months of benzodiazepine therapy. The effects may be more intense than before treatment began and are frequently misperceived by frightened patients as a return of the initial problem.4,8

Rebound effects are sudden and transient, whereas a relapse entails a gradual but persistent return of the original symptoms. Symptoms may continue unabated unless treatment resumes with benzodiazepines or other appropriate medications.8

Unfortunately, misperceived rebound effects may lead some patients to self-medicate by supplementing doses during withdrawal. This problem can be avoided if tapering is sufficiently gradual to ameliorate symptoms and the patient is counseled that these rebound effects are transient and to be expected.8

Unlike withdrawing from alcohol, the difficulty in abstaining during the acute phase of benzodiazepine withdrawal is not followed by any further craving once the patient is drug-free.3 It appears that most patients withdrawn from benzodiazepines can maintain abstinence. Although no protocol has been established for benzodiazepine withdrawal, some steps can be taken to manage it.

Benefits of Continued Use

The question of whether the benefits outweigh the disadvantages of chronic benzodiazepine therapy is far from settled. Followup studies have found that more than half of patients treated with benzodiazepine anxiolytics or hypnotics experience a relapse of the original symptoms within a year of stopping use.10 Half of these patients resume use of benzodiazepines. Longer followup studies indicate that a majority eventually resume use, whether intermittently or chronically.11

The reasons for discontinuation have to be examined in an individually calculated risk-benefit model by weighing the linkage between untreated anxiety or insomnia and alcoholism, depression, and suicide.7 Many researchers argue that anxiety is undermedicated with benzodiazepines. As many as 60 percent of patients who have legitimate medical or psychological reasons for high levels of stress and anxiety do not seek or obtain relief for these conditions.12

Salzman4 argues that chronic benzodiazepine use may be appropriate for older, but not necessarily elderly, patients with a number of chronic illnesses and compromised physical and psychosocial functioning. This group includes patients who are often in pain, dysphoric, or depressed as well as anxious, suffering from insomnia, or willing to visit their physicians.

Chronic users of this type may experience side effects from benzodiazepines or incur mild interactions with other drugs they are taking. However, they are not purposefully abusing psychoactive drugs or mixing them with alcohol.

Alternatives

One new drug, the serotonin agonist buspirone (BuSpar), is a promising alternative to benzodiazepines for the treatment of chronic anxiety with associated depressive symptoms. The advantages of BuSpar are:

Buspirone does not have the muscle relaxant or anticonvulsant properties of benzodiazepines. However, it does have some side effects at higher doses, and it is not immediately or invariably effective in easing anxiety.

The efficacy of buspirone for older patients is still being examined; it may precipitate some manic effects. Also, dosages should be reduced for those with decreased kidney or liver function.1,3,13,14

References

  1. Ray, W.A.; Thapa, P.B.; and Shorr, R.I. Medications and the older driver. Clinics in Geriatric Medicine 1993, 9(2):413-438.
  2. Woods, J.H., and Winger, G. Current benzodiazepine issues. Psychopharmacology 1995, 118:107-115.
  3. Winger, G. Other abused drugs: Benzodiazepines and sedatives. In: Fourth Triennial Report to Congress on Drug Abuse and Drug Abuse Research From the Secretary, Department of Health and Human Services. Rockville, MD: U.S. Department of Health and Human Services, 1993.
  4. Salzman, C. Issues and controversies regarding benzodiazepine use. In: Cooper, J.R.; Czechowicz, D.J.; Molinari, S.P.; and Petersen, R.C., eds. Impact of Prescription Drug Diversion Control Systems on Medical Practice and Patient Care. NIDA Research Monograph Series, Number 131. NIH Pub. No. 93-3507. Washington, DC: U.S. Government Printing Office, 1993, pp. 68-88.
  5. Salzman, C. (Task Force Chair). Benzodiazepine Dependence, Toxicity, and Abuse: A Task Force Report of the American Psychiatric Association. Washington, DC: American Psychiatric Press, 1990.
  6. Miller, F.; Whitcup, S.; Sacks, M.; and Lynch, P.E. Unrecognized drug dependence and withdrawal in the elderly. Drug and Alcohol Dependence 1985, 15:177.
  7. Speirs, C.J.; Navey, F.L.; Broods, D.J.; and Impallomeni, M.G. Opisthotonos and benzodiazepine withdrawal in the elderly. Lancet 1986, 2:1101.
  8. Rickels, K., and Schweizer, E. Anxiolytics: Indications, benefits, and risks of short- and long-term benzodiazepine therapy: Current research data. In: Cooper, J.R.; Czechowicz, D.J.; Molinari, S.P.; et al., eds. Impact of Prescription Drug Diversion Control Systems on Medical Practice and Patient Care. NIDA Research Monograph Series, Number 131. NIH Pub. No. 93-3507. Washington, DC: U.S. Government Printing Office,1993, pp. 51-67.
  9. Solomon, K.; Manepalli, J.; Ireland, G.A.; and Mahon, G.M. Alcoholism and prescription drug abuse in the elderly: St. Louis University grand rounds. Journal of the American Geriatric Society 1993, 41(1):57-69.
  10. Atkinson, R.M.; Ganzini, L.; and Bernstein, M.J. Alcohol and substance-use disorders in the elderly. In: Birren, J.E.; Sloane, R.B.; and Cohen, G.D., eds. Handbook of Mental Health and Aging, 2nd ed. San Diego, CA: Academic Press, 1992, pp. 515-555.
  11. Finlayson, R.E. Prescription drug abuse in older persons. In: Atkinson, R.M., ed. Alcohol and Drug Abuse in Old Age. Washington, DC: American Psychiatric Press, 1984, pp. 61-70.
  12. Salzman, C. Benzodiazepine treatment of panic and agoraphobia syndromes: Use, dependence, toxicity, abuse. Journal of Psychiatric Research 1993, 27:97-110.
  13. Weiss, K.J. Management of anxiety and depression syndromes in the elderly. Journal of Clinical Psychiatry 55(suppl. 2):5-12, 1994.
  14. Bezchlibnyk-Butler, K.Z., and Jeffries, J.J., eds. Clinical Handbook of Psychotropic Drugs, 5th ed. Toronto, Canada: Hogrefe-Huber, 1995.
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