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In This Topic
Geriatrics
Drug Therapy in the Elderly
Drug Categories of Concern in the Elderly
Analgesics
Anticoagulants
Antidepressants
Antihyperglycemics
Antihypertensives
Antiparkinsonian drugs
Antipsychotics
Anxiolytics and hypnotics
Digoxin
Diuretics
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Topics in Drug Therapy in the Elderly
  • Introduction to Drug Therapy in the Elderly
  • Pharmacokinetics in the Elderly
  • Pharmacodynamics in the Elderly
  • Drug-Related Problems in the Elderly
  • Drug Categories of Concern in the Elderly
     
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    Drug Categories of Concern in the Elderly

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    Some drug categories (eg, analgesics, anticoagulants, antihypertensives, antiparkinsonian drugs, diuretics, hypoglycemic drugs, psychoactive drugs) pose special risks for elderly patients. Some, although reasonable for use in younger adults, are so risky as to be considered inappropriate for the elderly. The Beers Criteria are most commonly used to identify such inappropriate drugs (see Table 5: Drug Therapy in the Elderly: High-Risk Drugs in the Elderly (Based on the Beers Criteria)Tables). The Zhan expert panel further categorized some inappropriate drugs from the Beers Criteria into 3 groups:

    Table 5

    PrintOpen table in new window Open table in new window
    High-Risk Drugs in the Elderly (Based on the Beers Criteria)

    Class

    Drug

    Prescribing Concern

    Analgesics

    IndomethacinSome Trade Names
    INDOCIN
    Click for Drug Monograph
    *

    Of available NSAIDs, indomethacinSome Trade Names
    INDOCIN
    Click for Drug Monograph
    has the most CNS adverse effects and therefore should be avoided in the elderly.

    KetorolacSome Trade Names
    TORADOL
    Click for Drug Monograph

    Immediate- and long-term use should be avoided in the elderly because many of them have asymptomatic and undiagnosed GI disorders.

    MeperidineSome Trade Names
    DEMEROL
    Click for Drug Monograph
    †

    MeperidineSome Trade Names
    DEMEROL
    Click for Drug Monograph
    is not an effective oral analgesic and has many disadvantages compared with other opioids. It should be avoided in the elderly.

    Non–COX-selective NSAIDs (naproxenSome Trade Names
    ALEVE
    NAPROSYN
    Click for Drug Monograph
    , oxaprozinSome Trade Names
    DAYPRO
    Click for Drug Monograph
    , piroxicamSome Trade Names
    FELDENE
    Click for Drug Monograph
    )

    Long-term use of the maximum dosage may cause GI bleeding, renal failure, hypertension, and heart failure.

    PentazocineSome Trade Names
    TALWIN
    Click for Drug Monograph
    †

    PentazocineSome Trade Names
    TALWIN
    Click for Drug Monograph
    is an opioid analgesic that has CNS adverse effects (eg, confusion, hallucinations) more commonly than other opioids; it is a mixed agonist/antagonist. For both reasons, it should usually be avoided in the elderly.

    PropoxypheneSome Trade Names
    DARVON
    DOLENE

    ‡ and combination products that contain it

    PropoxypheneSome Trade Names
    DARVON
    DOLENE

    should usually be avoided in the elderly. It has few analgesic advantages over acetaminophenSome Trade Names
    GENAPAP
    TYLENOL
    VALORIN
    Click for Drug Monograph
    but has the adverse effects of other opioids.

    Antidepressants

    Cyclic antidepressants (eg, amitriptylineSome Trade Names
    ELAVIL
    ENDEP
    Click for Drug Monograph
    ,* doxepinSome Trade Names
    SINEQUAN
    ZONALON
    Click for Drug Monograph
    *)

    Because of strong anticholinergic and sedating effects, amitriptylineSome Trade Names
    ELAVIL
    ENDEP
    Click for Drug Monograph
    or doxepinSome Trade Names
    SINEQUAN
    ZONALON
    Click for Drug Monograph
    is rarely the antidepressant of choice for the elderly.

    FluoxetineSome Trade Names
    PROZAC
    SARAFEM
    Click for Drug Monograph
    (taken daily)

    FluoxetineSome Trade Names
    PROZAC
    SARAFEM
    Click for Drug Monograph
    has a long half-life, may cause excessive CNS stimulation and sleep disturbances, and may increase agitation. Safer alternative SSRIs exist.

    Antihistamines

    ChlorpheniramineSome Trade Names
    CHLOR-TRIMETON
    Click for Drug Monograph
    *

    CyproheptadineSome Trade Names
    PERIACTIN
    Click for Drug Monograph
    *

    DexchlorpheniramineSome Trade Names
    No US trade name
    Click for Drug Monograph

    DiphenhydramineSome Trade Names
    BENADRYL
    NYTOL
    Click for Drug Monograph
    *

    HydroxyzineSome Trade Names
    ATARAX
    VISTARIL
    Click for Drug Monograph
    *

    OrphenadrineSome Trade Names
    NORFLEX
    Click for Drug Monograph

    PromethazineSome Trade Names
    PHENERGAN
    Click for Drug Monograph
    *

    Tripelennamine

    All OTC and many prescription antihistamines have potent anticholinergic properties. Antihistamines are commonly included with other drugs in cough and cold preparations. However, many cough and cold preparations without antihistamines are available; they are safer alternatives for the elderly.

    Antipsychotics

    MesoridazineSome Trade Names
    SERENTIL

    ThioridazineSome Trade Names
    MELLARIL
    Click for Drug Monograph

    Risk of CNS and extrapyramidal adverse effects is increased. When used to treat dementia-related behaviors, 2nd-generation (atypical) antipsychotics may increase mortality risk.

    Cardiovascular drugs

    AmiodaroneSome Trade Names
    CORDARONE
    Click for Drug Monograph

    Adverse effects include QTc prolongation and risk of provoking torsades de pointes.

    ClonidineSome Trade Names
    CATAPRES
    Click for Drug Monograph

    Adverse effects include orthostatic hypotension and CNS effects.

    DigoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph

    Because renal clearance of digoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    is decreased in the elderly, doses should rarely exceed 0.125 mg/day, unless the patient is monitored.

    DipyridamoleSome Trade Names
    PERSANTINE
    Click for Drug Monograph
    *

    Immediate-release dipyridamoleSome Trade Names
    PERSANTINE
    Click for Drug Monograph
    frequently causes orthostatic hypotension in the elderly (the controlled-release formulation in combination products may be acceptable). The immediate-release formulation is beneficial only in patients with artificial heart valves. If possible, it should be avoided in the elderly.

    DisopyramideSome Trade Names
    NORPACE
    Click for Drug Monograph
    *

    Of all antiarrhythmics, disopyramideSome Trade Names
    NORPACE
    Click for Drug Monograph
    is the most potent negative inotrope and therefore may induce heart failure in the elderly. It is also strongly anticholinergic. If antiarrhythmics are needed, others should be used.

    DoxazosinSome Trade Names
    CARDURA
    Click for Drug Monograph

    Adverse effects include hypotension, dry mouth, and urinary problems.

    Ethacrynic acidSome Trade Names
    EDECRIN
    Click for Drug Monograph

    Adverse effects include hypertension and fluid imbalances.

    Guanethidine

    Guanadrel

    Adverse effects include orthostatic hypotension.

    MethyldopaSome Trade Names
    ALDOMET
    Click for Drug Monograph
    *

    MethyldopaSome Trade Names
    ALDOMET
    Click for Drug Monograph
    may cause bradycardia and exacerbate depression in the elderly. Alternate treatments for hypertension are generally preferred.

    NifedipineSome Trade Names
    ADALAT
    PROCARDIA
    Click for Drug Monograph
    (short-acting)

    Adverse effects include hypotension, constipation, and reflex tachycardia.

    ReserpineSome Trade Names
    SERPASIL
    Click for Drug Monograph
    *

    Doses > 0.25 mg pose unnecessary risks in the elderly by inducing depression, impotence, sedation, and orthostatic hypotension. Safer alternatives exist.

    TiclopidineSome Trade Names
    TICLID
    Click for Drug Monograph

    TiclopidineSome Trade Names
    TICLID
    Click for Drug Monograph
    is no better than aspirinSome Trade Names
    BUFFERIN
    ECOTRIN
    GENACOTE
    Click for Drug Monograph
    in preventing clotting and is considerably more toxic. It should be used only as a 2nd-line drug in the elderly.

    GI antispasmodics

    Belladonna alkaloids†

    Clidinium/chlordiazepoxideSome Trade Names
    LIBRIUM
    Click for Drug Monograph

    DicyclomineSome Trade Names
    BENTYL
    Click for Drug Monograph
    †

    HyoscyamineSome Trade Names
    HYOSINE
    LEVSIN
    Click for Drug Monograph
    †

    PropanthelineSome Trade Names
    PRO-BANTHINE
    Click for Drug Monograph
    †

    GI antispasmodics are highly anticholinergic and usually cause substantial toxicity in the elderly. Efficacy at doses tolerated by the elderly is questionable. All of these drugs are best avoided in the elderly, especially for long-term use.

    Hypoglycemics

    ChlorpropamideSome Trade Names
    DIABINESE
    Click for Drug Monograph
    †

    ChlorpropamideSome Trade Names
    DIABINESE
    Click for Drug Monograph
    has a prolonged half-life in the elderly and can cause prolonged, serious hypoglycemia. It is the only oral hypoglycemic that causes SIADH. It should be avoided in the elderly.

    Laxatives (stimulant)

    BisacodylSome Trade Names
    DULCOLAX
    Click for Drug Monograph

    Cascara

    Neoloid except when used with opioids

    With long-term use, stimulant laxatives may exacerbate bowel dysfunction.

    Muscle relaxants

    CarisoprodolSome Trade Names
    SOMA
    Click for Drug Monograph
    ‡

    ChlorzoxazoneSome Trade Names
    PARAFON FORTE DSC
    Click for Drug Monograph
    ‡

    CyclobenzaprineSome Trade Names
    FLEXERIL
    Click for Drug Monograph
    ‡

    MetaxaloneSome Trade Names
    SKELAXIN
    Click for Drug Monograph
    ‡

    MethocarbamolSome Trade Names
    ROBAXIN
    Click for Drug Monograph
    ‡

    OxybutyninSome Trade Names
    DITROPAN
    Click for Drug Monograph
    *

    Most muscle relaxants and antispasmodics are poorly tolerated by the elderly, resulting in anticholinergic effects, sedation, and weakness. Efficacy at doses tolerated by the elderly is questionable. If possible, they should not be used in the elderly. For extended-release oxybutyninSome Trade Names
    DITROPAN
    Click for Drug Monograph
    , the patch is better tolerated.

    Sedative-hypnotics

    AlprazolamSome Trade Names
    XANAX
    Click for Drug Monograph
    *, § 2 mg

    LorazepamSome Trade Names
    ATIVAN
    Click for Drug Monograph
    3 mg

    OxazepamSome Trade Names
    SERAX
    Click for Drug Monograph
    60 mg

    TemazepamSome Trade Names
    RESTORIL
    Click for Drug Monograph
    15 mg

    TriazolamSome Trade Names
    HALCION
    Click for Drug Monograph
    0.25 mg

    Because sensitivity to benzodiazepines is increased in the elderly, smaller doses may be effective as well as safer; total daily doses should rarely exceed those listed.

    Barbiturates† (except phenobarbitalSome Trade Names
    LUMINAL
    Click for Drug Monograph
    )

    Barbiturates have more adverse effects in the elderly than most other sedative-hypnotics and are highly addictive. They should not be started as new therapy in the elderly except to control seizures.

    ChlordiazepoxideSome Trade Names
    LIBRIUM
    Click for Drug Monograph
    ‡

    ChlordiazepoxideSome Trade Names
    LIBRIUM
    Click for Drug Monograph
    /amitriptylineSome Trade Names
    ELAVIL
    ENDEP
    Click for Drug Monograph

    ClorazepateSome Trade Names
    TRANXENE
    Click for Drug Monograph

    Clidinium/chlordiazepoxideSome Trade Names
    LIBRIUM
    Click for Drug Monograph

    DiazepamSome Trade Names
    VALIUM
    Click for Drug Monograph
    ‡

    FlurazepamSome Trade Names
    DALMANE
    Click for Drug Monograph
    †

    Halazepam

    Nitrazepam

    QuazepamSome Trade Names
    DORAL
    Click for Drug Monograph

    These long-acting benzodiazepines have a long half-life in the elderly (often days), causing prolonged sedation and increasing risk of falls and fractures. Short- or intermediate-acting benzodiazepines are preferred if a benzodiazepine is required.

    DiphenhydramineSome Trade Names
    BENADRYL
    NYTOL
    Click for Drug Monograph

    DiphenhydramineSome Trade Names
    BENADRYL
    NYTOL
    Click for Drug Monograph
    is potently anticholinergic and usually should not be used as a hypnotic in the elderly. When used to treat or prevent allergic reactions, it should be used in the smallest possible dose and with great caution.

    MeprobamateSome Trade Names
    EQUANIL
    MILTOWN
    Click for Drug Monograph

    MeprobamateSome Trade Names
    EQUANIL
    MILTOWN
    Click for Drug Monograph
    is a highly addictive and sedating anxiolytic. It should be avoided in the elderly. Elderly patients who take it for long periods may become addicted, and the drug may need to be withdrawn slowly.

    Other

    Amphetamines

    Anorexics

    These drugs may cause dependence, hypertension, angina, and MI. Amphetamines have CNS stimulant adverse effects (methylphenidateSome Trade Names
    CONCERTA
    RITALIN
    Click for Drug Monograph
    may be useful for certain elderly patients).

    CimetidineSome Trade Names
    TAGAMET
    Click for Drug Monograph

    CimetidineSome Trade Names
    TAGAMET
    Click for Drug Monograph
    has CNS adverse effects, including confusion.

    Cyclandelate

    Ergot mesylates

    These drugs in the doses studied have not been shown to be effective for treatment of dementia or any other disorder.

    Desiccated thyroid

    Cardiac effects are a concern. Safer alternatives exist.

    EstrogensSome Trade Names
    PREMARIN
    Click for Drug Monograph
    only (oral)

    Evidence suggests that estrogensSome Trade Names
    PREMARIN
    Click for Drug Monograph
    increase risk of breast and endometrial cancer and may increase risk of pulmonary embolism, stroke, and coronary artery disease in older women.

    Ferrous sulfateSome Trade Names
    FEOSOL
    FER-GEN-SOL
    FER-IN-SOL
    Click for Drug Monograph

    Doses > 325 mg/day do not substantially increase total absorption and are more likely to cause constipation.

    IsoxsuprineSome Trade Names
    VASODILAN
    Click for Drug Monograph

    IsoxsuprineSome Trade Names
    VASODILAN
    Click for Drug Monograph
    is not effective in the elderly.

    MethyltestosteroneSome Trade Names
    ORETON
    Click for Drug Monograph

    Adverse effects include benign prostatic hypertrophy and cardiac problems.

    Mineral oil

    Mineral oil may result in aspiration.

    NitrofurantoinSome Trade Names
    FURADANTIN
    MACROBID
    MACRODANTIN
    Click for Drug Monograph

    NitrofurantoinSome Trade Names
    FURADANTIN
    MACROBID
    MACRODANTIN
    Click for Drug Monograph
    is ineffective in patients with moderate to severe renal insufficiency; metabolites may cause peripheral neuropathy. Long-term use for UTI prevention can cause pulmonary fibrosis.

    TrimethobenzamideSome Trade Names
    TIGAN
    Click for Drug Monograph
    †

    TrimethobenzamideSome Trade Names
    TIGAN
    Click for Drug Monograph
    is one of the least effective antiemetics and can have extrapyramidal adverse effects. When possible, it should be avoided in the elderly.

    *Sometimes indicated but often misused according to the Zhan panel.

    †Always to be avoided according to the Zhan panel.

    ‡Rarely appropriate according to the Zhan panel.

    §Doses of alprazolamSome Trade Names
    XANAX
    Click for Drug Monograph
    may be higher when used to treat panic disorders.

    COX = cyclooxygenase; SIADH = syndrome of inappropriate antidiuretic hormone secretion.

    Adapted from Fick DM, Cooper JW, Wade WE, et al: Updating the Beers criteria for potentially inappropriate medication use in older adults. Archives of Internal Medicine 163:2716–2724, 2003.

    High-Risk Drugs in the Elderly (Based on the Beers Criteria)

    Class

    Drug

    Prescribing Concern

    Analgesics

    IndomethacinSome Trade Names
    INDOCIN
    Click for Drug Monograph
    *

    Of available NSAIDs, indomethacinSome Trade Names
    INDOCIN
    Click for Drug Monograph
    has the most CNS adverse effects and therefore should be avoided in the elderly.

    KetorolacSome Trade Names
    TORADOL
    Click for Drug Monograph

    Immediate- and long-term use should be avoided in the elderly because many of them have asymptomatic and undiagnosed GI disorders.

    MeperidineSome Trade Names
    DEMEROL
    Click for Drug Monograph
    †

    MeperidineSome Trade Names
    DEMEROL
    Click for Drug Monograph
    is not an effective oral analgesic and has many disadvantages compared with other opioids. It should be avoided in the elderly.

    Non–COX-selective NSAIDs (naproxenSome Trade Names
    ALEVE
    NAPROSYN
    Click for Drug Monograph
    , oxaprozinSome Trade Names
    DAYPRO
    Click for Drug Monograph
    , piroxicamSome Trade Names
    FELDENE
    Click for Drug Monograph
    )

    Long-term use of the maximum dosage may cause GI bleeding, renal failure, hypertension, and heart failure.

    PentazocineSome Trade Names
    TALWIN
    Click for Drug Monograph
    †

    PentazocineSome Trade Names
    TALWIN
    Click for Drug Monograph
    is an opioid analgesic that has CNS adverse effects (eg, confusion, hallucinations) more commonly than other opioids; it is a mixed agonist/antagonist. For both reasons, it should usually be avoided in the elderly.

    PropoxypheneSome Trade Names
    DARVON
    DOLENE

    ‡ and combination products that contain it

    PropoxypheneSome Trade Names
    DARVON
    DOLENE

    should usually be avoided in the elderly. It has few analgesic advantages over acetaminophenSome Trade Names
    GENAPAP
    TYLENOL
    VALORIN
    Click for Drug Monograph
    but has the adverse effects of other opioids.

    Antidepressants

    Cyclic antidepressants (eg, amitriptylineSome Trade Names
    ELAVIL
    ENDEP
    Click for Drug Monograph
    ,* doxepinSome Trade Names
    SINEQUAN
    ZONALON
    Click for Drug Monograph
    *)

    Because of strong anticholinergic and sedating effects, amitriptylineSome Trade Names
    ELAVIL
    ENDEP
    Click for Drug Monograph
    or doxepinSome Trade Names
    SINEQUAN
    ZONALON
    Click for Drug Monograph
    is rarely the antidepressant of choice for the elderly.

    FluoxetineSome Trade Names
    PROZAC
    SARAFEM
    Click for Drug Monograph
    (taken daily)

    FluoxetineSome Trade Names
    PROZAC
    SARAFEM
    Click for Drug Monograph
    has a long half-life, may cause excessive CNS stimulation and sleep disturbances, and may increase agitation. Safer alternative SSRIs exist.

    Antihistamines

    ChlorpheniramineSome Trade Names
    CHLOR-TRIMETON
    Click for Drug Monograph
    *

    CyproheptadineSome Trade Names
    PERIACTIN
    Click for Drug Monograph
    *

    DexchlorpheniramineSome Trade Names
    No US trade name
    Click for Drug Monograph

    DiphenhydramineSome Trade Names
    BENADRYL
    NYTOL
    Click for Drug Monograph
    *

    HydroxyzineSome Trade Names
    ATARAX
    VISTARIL
    Click for Drug Monograph
    *

    OrphenadrineSome Trade Names
    NORFLEX
    Click for Drug Monograph

    PromethazineSome Trade Names
    PHENERGAN
    Click for Drug Monograph
    *

    Tripelennamine

    All OTC and many prescription antihistamines have potent anticholinergic properties. Antihistamines are commonly included with other drugs in cough and cold preparations. However, many cough and cold preparations without antihistamines are available; they are safer alternatives for the elderly.

    Antipsychotics

    MesoridazineSome Trade Names
    SERENTIL

    ThioridazineSome Trade Names
    MELLARIL
    Click for Drug Monograph

    Risk of CNS and extrapyramidal adverse effects is increased. When used to treat dementia-related behaviors, 2nd-generation (atypical) antipsychotics may increase mortality risk.

    Cardiovascular drugs

    AmiodaroneSome Trade Names
    CORDARONE
    Click for Drug Monograph

    Adverse effects include QTc prolongation and risk of provoking torsades de pointes.

    ClonidineSome Trade Names
    CATAPRES
    Click for Drug Monograph

    Adverse effects include orthostatic hypotension and CNS effects.

    DigoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph

    Because renal clearance of digoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    is decreased in the elderly, doses should rarely exceed 0.125 mg/day, unless the patient is monitored.

    DipyridamoleSome Trade Names
    PERSANTINE
    Click for Drug Monograph
    *

    Immediate-release dipyridamoleSome Trade Names
    PERSANTINE
    Click for Drug Monograph
    frequently causes orthostatic hypotension in the elderly (the controlled-release formulation in combination products may be acceptable). The immediate-release formulation is beneficial only in patients with artificial heart valves. If possible, it should be avoided in the elderly.

    DisopyramideSome Trade Names
    NORPACE
    Click for Drug Monograph
    *

    Of all antiarrhythmics, disopyramideSome Trade Names
    NORPACE
    Click for Drug Monograph
    is the most potent negative inotrope and therefore may induce heart failure in the elderly. It is also strongly anticholinergic. If antiarrhythmics are needed, others should be used.

    DoxazosinSome Trade Names
    CARDURA
    Click for Drug Monograph

    Adverse effects include hypotension, dry mouth, and urinary problems.

    Ethacrynic acidSome Trade Names
    EDECRIN
    Click for Drug Monograph

    Adverse effects include hypertension and fluid imbalances.

    Guanethidine

    Guanadrel

    Adverse effects include orthostatic hypotension.

    MethyldopaSome Trade Names
    ALDOMET
    Click for Drug Monograph
    *

    MethyldopaSome Trade Names
    ALDOMET
    Click for Drug Monograph
    may cause bradycardia and exacerbate depression in the elderly. Alternate treatments for hypertension are generally preferred.

    NifedipineSome Trade Names
    ADALAT
    PROCARDIA
    Click for Drug Monograph
    (short-acting)

    Adverse effects include hypotension, constipation, and reflex tachycardia.

    ReserpineSome Trade Names
    SERPASIL
    Click for Drug Monograph
    *

    Doses > 0.25 mg pose unnecessary risks in the elderly by inducing depression, impotence, sedation, and orthostatic hypotension. Safer alternatives exist.

    TiclopidineSome Trade Names
    TICLID
    Click for Drug Monograph

    TiclopidineSome Trade Names
    TICLID
    Click for Drug Monograph
    is no better than aspirinSome Trade Names
    BUFFERIN
    ECOTRIN
    GENACOTE
    Click for Drug Monograph
    in preventing clotting and is considerably more toxic. It should be used only as a 2nd-line drug in the elderly.

    GI antispasmodics

    Belladonna alkaloids†

    Clidinium/chlordiazepoxideSome Trade Names
    LIBRIUM
    Click for Drug Monograph

    DicyclomineSome Trade Names
    BENTYL
    Click for Drug Monograph
    †

    HyoscyamineSome Trade Names
    HYOSINE
    LEVSIN
    Click for Drug Monograph
    †

    PropanthelineSome Trade Names
    PRO-BANTHINE
    Click for Drug Monograph
    †

    GI antispasmodics are highly anticholinergic and usually cause substantial toxicity in the elderly. Efficacy at doses tolerated by the elderly is questionable. All of these drugs are best avoided in the elderly, especially for long-term use.

    Hypoglycemics

    ChlorpropamideSome Trade Names
    DIABINESE
    Click for Drug Monograph
    †

    ChlorpropamideSome Trade Names
    DIABINESE
    Click for Drug Monograph
    has a prolonged half-life in the elderly and can cause prolonged, serious hypoglycemia. It is the only oral hypoglycemic that causes SIADH. It should be avoided in the elderly.

    Laxatives (stimulant)

    BisacodylSome Trade Names
    DULCOLAX
    Click for Drug Monograph

    Cascara

    Neoloid except when used with opioids

    With long-term use, stimulant laxatives may exacerbate bowel dysfunction.

    Muscle relaxants

    CarisoprodolSome Trade Names
    SOMA
    Click for Drug Monograph
    ‡

    ChlorzoxazoneSome Trade Names
    PARAFON FORTE DSC
    Click for Drug Monograph
    ‡

    CyclobenzaprineSome Trade Names
    FLEXERIL
    Click for Drug Monograph
    ‡

    MetaxaloneSome Trade Names
    SKELAXIN
    Click for Drug Monograph
    ‡

    MethocarbamolSome Trade Names
    ROBAXIN
    Click for Drug Monograph
    ‡

    OxybutyninSome Trade Names
    DITROPAN
    Click for Drug Monograph
    *

    Most muscle relaxants and antispasmodics are poorly tolerated by the elderly, resulting in anticholinergic effects, sedation, and weakness. Efficacy at doses tolerated by the elderly is questionable. If possible, they should not be used in the elderly. For extended-release oxybutyninSome Trade Names
    DITROPAN
    Click for Drug Monograph
    , the patch is better tolerated.

    Sedative-hypnotics

    AlprazolamSome Trade Names
    XANAX
    Click for Drug Monograph
    *, § 2 mg

    LorazepamSome Trade Names
    ATIVAN
    Click for Drug Monograph
    3 mg

    OxazepamSome Trade Names
    SERAX
    Click for Drug Monograph
    60 mg

    TemazepamSome Trade Names
    RESTORIL
    Click for Drug Monograph
    15 mg

    TriazolamSome Trade Names
    HALCION
    Click for Drug Monograph
    0.25 mg

    Because sensitivity to benzodiazepines is increased in the elderly, smaller doses may be effective as well as safer; total daily doses should rarely exceed those listed.

    Barbiturates† (except phenobarbitalSome Trade Names
    LUMINAL
    Click for Drug Monograph
    )

    Barbiturates have more adverse effects in the elderly than most other sedative-hypnotics and are highly addictive. They should not be started as new therapy in the elderly except to control seizures.

    ChlordiazepoxideSome Trade Names
    LIBRIUM
    Click for Drug Monograph
    ‡

    ChlordiazepoxideSome Trade Names
    LIBRIUM
    Click for Drug Monograph
    /amitriptylineSome Trade Names
    ELAVIL
    ENDEP
    Click for Drug Monograph

    ClorazepateSome Trade Names
    TRANXENE
    Click for Drug Monograph

    Clidinium/chlordiazepoxideSome Trade Names
    LIBRIUM
    Click for Drug Monograph

    DiazepamSome Trade Names
    VALIUM
    Click for Drug Monograph
    ‡

    FlurazepamSome Trade Names
    DALMANE
    Click for Drug Monograph
    †

    Halazepam

    Nitrazepam

    QuazepamSome Trade Names
    DORAL
    Click for Drug Monograph

    These long-acting benzodiazepines have a long half-life in the elderly (often days), causing prolonged sedation and increasing risk of falls and fractures. Short- or intermediate-acting benzodiazepines are preferred if a benzodiazepine is required.

    DiphenhydramineSome Trade Names
    BENADRYL
    NYTOL
    Click for Drug Monograph

    DiphenhydramineSome Trade Names
    BENADRYL
    NYTOL
    Click for Drug Monograph
    is potently anticholinergic and usually should not be used as a hypnotic in the elderly. When used to treat or prevent allergic reactions, it should be used in the smallest possible dose and with great caution.

    MeprobamateSome Trade Names
    EQUANIL
    MILTOWN
    Click for Drug Monograph

    MeprobamateSome Trade Names
    EQUANIL
    MILTOWN
    Click for Drug Monograph
    is a highly addictive and sedating anxiolytic. It should be avoided in the elderly. Elderly patients who take it for long periods may become addicted, and the drug may need to be withdrawn slowly.

    Other

    Amphetamines

    Anorexics

    These drugs may cause dependence, hypertension, angina, and MI. Amphetamines have CNS stimulant adverse effects (methylphenidateSome Trade Names
    CONCERTA
    RITALIN
    Click for Drug Monograph
    may be useful for certain elderly patients).

    CimetidineSome Trade Names
    TAGAMET
    Click for Drug Monograph

    CimetidineSome Trade Names
    TAGAMET
    Click for Drug Monograph
    has CNS adverse effects, including confusion.

    Cyclandelate

    Ergot mesylates

    These drugs in the doses studied have not been shown to be effective for treatment of dementia or any other disorder.

    Desiccated thyroid

    Cardiac effects are a concern. Safer alternatives exist.

    EstrogensSome Trade Names
    PREMARIN
    Click for Drug Monograph
    only (oral)

    Evidence suggests that estrogensSome Trade Names
    PREMARIN
    Click for Drug Monograph
    increase risk of breast and endometrial cancer and may increase risk of pulmonary embolism, stroke, and coronary artery disease in older women.

    Ferrous sulfateSome Trade Names
    FEOSOL
    FER-GEN-SOL
    FER-IN-SOL
    Click for Drug Monograph

    Doses > 325 mg/day do not substantially increase total absorption and are more likely to cause constipation.

    IsoxsuprineSome Trade Names
    VASODILAN
    Click for Drug Monograph

    IsoxsuprineSome Trade Names
    VASODILAN
    Click for Drug Monograph
    is not effective in the elderly.

    MethyltestosteroneSome Trade Names
    ORETON
    Click for Drug Monograph

    Adverse effects include benign prostatic hypertrophy and cardiac problems.

    Mineral oil

    Mineral oil may result in aspiration.

    NitrofurantoinSome Trade Names
    FURADANTIN
    MACROBID
    MACRODANTIN
    Click for Drug Monograph

    NitrofurantoinSome Trade Names
    FURADANTIN
    MACROBID
    MACRODANTIN
    Click for Drug Monograph
    is ineffective in patients with moderate to severe renal insufficiency; metabolites may cause peripheral neuropathy. Long-term use for UTI prevention can cause pulmonary fibrosis.

    TrimethobenzamideSome Trade Names
    TIGAN
    Click for Drug Monograph
    †

    TrimethobenzamideSome Trade Names
    TIGAN
    Click for Drug Monograph
    is one of the least effective antiemetics and can have extrapyramidal adverse effects. When possible, it should be avoided in the elderly.

    *Sometimes indicated but often misused according to the Zhan panel.

    †Always to be avoided according to the Zhan panel.

    ‡Rarely appropriate according to the Zhan panel.

    §Doses of alprazolamSome Trade Names
    XANAX
    Click for Drug Monograph
    may be higher when used to treat panic disorders.

    COX = cyclooxygenase; SIADH = syndrome of inappropriate antidiuretic hormone secretion.

    Adapted from Fick DM, Cooper JW, Wade WE, et al: Updating the Beers criteria for potentially inappropriate medication use in older adults. Archives of Internal Medicine 163:2716–2724, 2003.

    • Always to be avoided
    • Rarely appropriate
    • Sometimes indicated but often misused

    Analgesics: NSAIDs are used by > 30% of people aged 65 to 89, and half of all NSAID prescriptions are for people > 60. Several NSAIDs are available without prescription.

    The elderly may be prone to adverse effects of these drugs, and adverse effects may be more severe because of the following:

    • NSAIDs are highly soluble in lipids, and because adipose tissue increases with age, distribution of the drugs is extensive.
    • Plasma protein is often decreased, resulting in higher levels of unbound drug and exaggerated pharmacologic effects.
    • Renal function is reduced in many of the elderly, resulting in decreased renal clearance and higher drug levels.

    Serious adverse effects include peptic ulceration and upper GI bleeding; risk is increased when an NSAID is begun and when dose is increased. Risk of upper GI bleeding increases when NSAIDs are given with warfarinSome Trade Names
    COUMADIN
    Click for Drug Monograph
    , aspirinSome Trade Names
    BUFFERIN
    ECOTRIN
    GENACOTE
    Click for Drug Monograph
    , or other antiplatelet drugs (eg, clopidogrelSome Trade Names
    PLAVIX
    Click for Drug Monograph
    ). NSAIDs may increase risk of cardiovascular events and can cause fluid retention and, rarely, nephropathy.

    NSAIDs can also increase BP; this effect may be unrecognized and lead to intensification of antihypertensive treatment (a prescribing cascade). Thus, clinicians should keep this effect in mind when BP increases in elderly patients and ask them about their use of NSAIDs, particularly OTC NSAIDs.

    Selective COX-2 (cyclooxygenase-2) inhibitors (coxibs) cause less GI irritation and platelet inhibition than other NSAIDs. Nonetheless, coxibs have a risk of GI bleeding, especially for patients taking warfarinSome Trade Names
    COUMADIN
    Click for Drug Monograph
    or aspirinSome Trade Names
    BUFFERIN
    ECOTRIN
    GENACOTE
    Click for Drug Monograph
    (even at a low dose) and for those who have had GI events. Coxibs, as a class, appear to increase risk of cardiovascular events, but risk may vary by drug; they should be used cautiously. Coxibs have renal effects comparable to those of other NSAIDs.

    Lower-risk alternatives (eg, acetaminophenSome Trade Names
    GENAPAP
    TYLENOL
    VALORIN
    Click for Drug Monograph
    ) should be used when possible. If NSAIDs are used in the elderly, the lowest effective dose should be used, and continued need should be reviewed frequently. If NSAIDs are used long-term, serum creatinine and BP should be monitored closely, especially in patients with other risk factors (eg, heart failure, renal impairment, cirrhosis with ascites, volume depletion, diuretic use).

    Anticoagulants: Aging may increase sensitivity to the anticoagulant effect of warfarinSome Trade Names
    COUMADIN
    Click for Drug Monograph
    . Careful dosing and scrupulous monitoring can largely overcome the increased risk of bleeding in elderly patients taking warfarinSome Trade Names
    COUMADIN
    Click for Drug Monograph
    . Also, because drug interactions with warfarinSome Trade Names
    COUMADIN
    Click for Drug Monograph
    are common, closer monitoring is necessary when new drugs are added or old ones are stopped; computer drug interaction programs should be consulted if patients take multiple drugs.

    Antidepressants: Tricyclic antidepressants are effective but should rarely be used in the elderly. SSRIs and mixed serotonin/dopamineSome Trade Names
    INTROPIN
    Click for Drug Monograph
    reuptake inhibitors are as effective as tricyclic antidepressants and cause less toxicity; however, there are some concerns about some of these drugs:

    • FluoxetineSome Trade Names
      PROZAC
      SARAFEM
      Click for Drug Monograph
      : A possible disadvantage is the long elimination half-life, especially of its active metabolite.
    • ParoxetineSome Trade Names
      PAXIL
      Click for Drug Monograph
      : This drug is more sedating than other SSRIs, has anticholinergic effects, and, like some other SSRIs, can inhibit hepatic cytochrome P-450 2D6 enzyme activity, possibly impairing the metabolism of several drugs, including some antipsychotics, antiarrhythmics, and tricyclic antidepressants.
    • SertralineSome Trade Names
      ZOLOFT
      Click for Drug Monograph
      : This drug is more activating; diarrhea is a common adverse effect.

    Doses of these drugs should be reduced by up to 50%. Many SSRIs are available, but data on their use in the elderly are sparse.

    Antihyperglycemics: Doses of antihyperglycemics should be titrated carefully in patients with diabetes mellitus. Risk of hypoglycemia due to sulfonylureas may increase with age. ChlorpropamideSome Trade Names
    DIABINESE
    Click for Drug Monograph
    is not recommended because elderly patients are at increased risk of hyponatremia due to the syndrome of inappropriate antidiuretic hormone secretion (SIADH) and because the drug's long duration of action is dangerous if adverse effects or hypoglycemia occurs. Risk of hypoglycemia is greater with glyburideSome Trade Names
    DIABETA
    GLYNASE
    MICRONASE
    Click for Drug Monograph
    than with other oral antihyperglycemics because like chlorpropamideSome Trade Names
    DIABINESE
    Click for Drug Monograph
    , it is eliminated by the kidneys, and clearance can be reduced when renal function is impaired.

    MetforminSome Trade Names
    GLUCOPHAGE
    Click for Drug Monograph
    , a biguanide excreted by the kidneys, increases peripheral tissue sensitivity to insulin and can be effective given alone or with sulfonylureas. Risk of lactic acidosis, a rare but serious complication, increases with degree of renal impairment and with patient age. Heart failure is a contraindication.

    Antihypertensives: In many elderly patients, lower starting doses of antihypertensives may be necessary to reduce risk of adverse effects; however, for most elderly patients with hypertension, achieving BP goals requires standard doses and multidrug therapy. Initially, a thiazide-type diuretic is usually given alone or with one of the other classes shown to be beneficial (ACE inhibitors, angiotensin II receptor blockers, β-blockers, Ca channel blockers). Short-acting dihydropyridines (eg, nifedipineSome Trade Names
    ADALAT
    PROCARDIA
    Click for Drug Monograph
    ) may increase mortality risk and should not be used. Sitting and standing BP can be monitored, particularly when multiple antihypertensives are used, to check for orthostatic hypotension, which may increase risk of falls and fractures.

    Antiparkinsonian drugs: Levodopa clearance is reduced in elderly patients, who are also more susceptible to the drug's adverse effects, particularly orthostatic hypotension and confusion. Therefore, elderly patients should be given a lower starting dose of levodopa and carefully monitored for adverse effects (see Movement and Cerebellar Disorders: Levodopa). Patients who become confused while taking levodopa may also not tolerate newer dopamineSome Trade Names
    INTROPIN
    Click for Drug Monograph
    agonists (eg, pramipexoleSome Trade Names
    MIRAPEX
    Click for Drug Monograph
    , ropiniroleSome Trade Names
    REQUIP
    Click for Drug Monograph
    ). Because elderly patients with parkinsonism may be cognitively impaired, anticholinergic drugs should be avoided.

    Antipsychotics: In nonpsychotic, agitated patients, antipsychotics control symptoms only marginally better than placebos and can have severe adverse effects. Antipsychotics should be reserved for psychosis.

    When an antipsychotic is used, the starting dose should be about one quarter the usual starting adult dose and should be increased gradually. Clinical trial data relating to dosing, efficacy, and safety of these drugs in the elderly are limited.

    Antipsychotics can reduce paranoia but may worsen confusion (see also Schizophrenia and Related Disorders: Conventional antipsychotics). Elderly patients, especially women, are at increased risk of tardive dyskinesia, which is often irreversible. Sedation, orthostatic hypotension, anticholinergic effects, and akathisia (subjective motor restlessness) can occur in up to 20% of elderly patients taking an antipsychotic, and drug-induced parkinsonism can persist for up to 6 to 9 mo after the drug is stopped.

    The FDA has issued a warning regarding the use of 2nd-generation (atypical) antipsychotics, once thought to be safer, in the treatment of behavioral disorders in elderly patients with dementia; a review of placebo-controlled studies has shown a higher mortality rate associated with their use. Extrapyramidal dysfunction can develop when 2nd-generation antipsychotics (eg, olanzapineSome Trade Names
    ZYPREXA
    Click for Drug Monograph
    , quetiapineSome Trade Names
    SEROQUEL
    Click for Drug Monograph
    , risperidoneSome Trade Names
    RISPERDAL
    Click for Drug Monograph
    ) are used, especially at higher doses. Risks and benefits of using an antipsychotic should be discussed with the patient or the person responsible for the patient's care.

    Anxiolytics and hypnotics: Treatable causes of insomnia should be sought and managed before using hypnotics (see also Sleep and Wakefulness Disorders: Hypnotics). Nonpharmacologic measures and sleep hygiene (eg, avoiding caffeinated beverages, limiting daytime napping, modifying bedtime) should be tried first. If they are ineffective, nonbenzodiazepine hypnotics (eg, the imidazopyridines, alpidem and zolpidemSome Trade Names
    AMBIEN
    Click for Drug Monograph
    ) are options. These drugs bind mainly to a benzodiazepine receptor subtype. Imidazopyridines disturb the sleep pattern less than benzodiazepines and have a more rapid onset, fewer rebound effects, fewer next-day effects, and less potential for dependence. Short- or intermediate-acting benzodiazepines with half-lives of < 24 h (eg, alprazolamSome Trade Names
    XANAX
    Click for Drug Monograph
    , lorazepamSome Trade Names
    ATIVAN
    Click for Drug Monograph
    , oxazepamSome Trade Names
    SERAX
    Click for Drug Monograph
    , temazepamSome Trade Names
    RESTORIL
    Click for Drug Monograph
    ) are preferable to long-acting benzodiazepines but may have adverse effects, including those that lead to falls and fractures.

    Longer-acting benzodiazepines (eg, clonazepamSome Trade Names
    KLONOPIN
    Click for Drug Monograph
    , diazepamSome Trade Names
    VALIUM
    Click for Drug Monograph
    , flurazepamSome Trade Names
    DALMANE
    Click for Drug Monograph
    ) should be avoided because they have active metabolites, are likely to accumulate, and have adverse effects (eg, drowsiness, impaired memory, impaired balance leading to falls and fractures).

    Duration of anxiolytic or hypnotic therapy should be limited if possible because tolerance and dependence may develop; withdrawal may lead to rebound anxiety or insomnia.

    Antihistamines (eg, diphenhydramineSome Trade Names
    BENADRYL
    NYTOL
    Click for Drug Monograph
    , hydroxyzineSome Trade Names
    ATARAX
    VISTARIL
    Click for Drug Monograph
    ) are not recommended as anxiolytics or hypnotics because they have anticholinergic effects.

    BuspironeSome Trade Names
    BUSPAR
    Click for Drug Monograph
    , a partial serotonin agonist, can be effective for general anxiety disorder; elderly patients tolerate doses up to 30 mg/day well. The slow onset of anxiolytic action (up to 2 to 3 wk) can be a disadvantage in urgent cases.

    Digoxin: DigoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    , a cardiac glycoside, is used to increase the force of myocardial contractions and to treat supraventricular arrhythmias. However, it must be used with caution in patients with heart failure. In men with heart failure and a left ventricular ejection fraction of ≤ 45%, serum digoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    levels > 0.8 ng/mL are associated with increased mortality risk. Adverse effects are typically related to its narrow therapeutic index. One study found digoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    to be beneficial in women when serum levels were 0.5 to 0.9 ng/mL but possibly harmful when levels were ≥ 1.2 ng/mL. A number of factors increase the likelihood of digoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    toxicity in the elderly. Renal impairment, temporary dehydration, and NSAID use (all common among the elderly) can reduce renal clearance of digoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    . Furthermore, digoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    clearance decreases an average of 50% in elderly patients with normal serum creatinine levels. Also, if lean body mass is reduced, as may occur with aging, volume of distribution for digoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    is reduced. Therefore, starting doses should be low (0.125 mg/day) and adjusted according to response and serum digoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    levels (normal range 0.8 to 2.0 ng/mL). However, serum digoxinSome Trade Names
    DIGITEK
    LANOXIN
    Click for Drug Monograph
    level does not always correlate with likelihood of toxicity.

    Diuretics: Lower doses of thiazide diuretics (eg, hydrochlorothiazideSome Trade Names
    ESIDRIX
    HYDRODIURIL
    Click for Drug Monograph
    or chlorthalidoneSome Trade Names
    HYGROTON
    Click for Drug Monograph
    12.5 to 25 mg) can effectively control hypertension in many elderly patients and have less risk of hypokalemia and hyperglycemia than other diuretics (see also Hypertension: Diuretics). Thus, K supplements may be required less often.

    K-sparing diuretics should be used with caution in the elderly; the K level must be carefully monitored, particularly when these diuretics are given with ACE inhibitors.

    Last full review/revision September 2009 by J. Mark Ruscin, PharmD

    Content last modified February 2012

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