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Drug fever can be caused by various mechanisms, although it is ascribed most

commonly to a hypersensitivity reaction. Other mechanisms include the

pharmacologic action of the drug (e.g., cell destruction from antineoplastic agents

releases endogenous pyrogens); altered thermoregulatory function (e.g., increased

metabolic rate from thyroid hormone); decreased sweating from drugs with

anticholinergic properties (e.g., atropine, tricyclic antidepressants, and

phenothiazines); drug-administration-related fever (e.g., amphotericin B and

bleomycin); and idiosyncratic reactions (e.g., neuroleptic malignant syndrome from

haloperidol, malignant hyperthermia from inhaled anesthetics).

67

CASE 32-3, QUESTION 2: What agent is the most likely cause of drug fever in M.M.?

Most of the information available on drug fever is based on case reports or small

case series and reviews of the literature.

68,69 Unfortunately, the literature is

inconsistent with regard to the frequency of drug fever (e.g., very common, common,

uncommon) and such descriptions are not supported by good clinical data.

Nevertheless, some drugs are more commonly associated with drug fever than others.

These include anti-infectives as a class (especially β-lactam antibiotics),

antiepileptics, and antineoplastics. Drug fever has also been reported frequently with

amphotericin B, azathioprine, hydroxyurea, methyldopa, procainamide, quinidine,

and quinine.

68–70

In M.M.’s case, ceftriaxone or azithromycin is the most likely cause of her ongoing

fever, given the timing of the reaction relative to beginning the antibiotics and the

frequency of febrile reactions attributed to them, especially to β-lactam antibiotics.

Febrile reactions have not been associated with acetaminophen, and famotidine is

rarely a cause of fever without other symptoms of an allergic reaction. Although

diuretics such as hydrochlorothiazide can cause fever, M.M. was taking this

medication before admission without any ill effects, making this drug an unlikely

culprit.

CASE 32-3, QUESTION 3: How should M.M.’s drug fever be treated? Can M.M. receive cephalosporins in

the future?

Because M.M. has responded clinically, her antibiotics should be discontinued

and her fever curve, WBC count, heart rate, and respiratory status followed. An oral

antibiotic from another drug class (e.g., a fluoroquinolone) should be started to

complete a 7-day to 10-day antibiotic course of therapy. Acetaminophen and other

antipyretics should be avoided unless M.M. becomes uncomfortable from the fever

because they can mask the response to the discontinuation of her antibiotics.

As with any hypersensitivity reaction, rechallenge with the offending drug can

cause a similar, or sometimes greater, response. In M.M.’s case, reexposure to

ceftriaxone (or another β-lactam antibiotic) or a macrolide might cause a febrile

reaction. It is unclear, however, how large the risk of reexposure truly is. Although

drug fever sometimes precedes more serious hypersensitivity reactions, evidence

suggests there may be little risk to reexposure. Should M.M. require ceftriaxone (or

another β-lactam or macrolide antibiotic) in the future, it would be prudent to

administer the drug in a setting where M.M. can be monitored, at least initially, to

ensure prompt treatment if an immediate hypersensitivity reaction develops.

Hypersensitivity Vasculitis

CASE 32-4

QUESTION 1: M.G., a 26-year-old woman with cystic fibrosis, is admitted for treatment of pneumonia.

Sputum cultures obtained before admission reveal Alcaligenes xylosoxidans sensitive only to minocycline and

chloramphenicol. M.G. is initiated on appropriate doses of these two antibiotics for a 2-week course. On day 8

of therapy, M.G. begins to complain of a rash on her legs. Physical examination reveals palpable purpura and a

maculopapular rash on both lower extremities. Laboratory data reveal an elevated ESR and leukocytosis. What

is the likely cause of M.G.’s rash and laboratory abnormalities?

M.G.’s presentation is suggestive of a diagnosis of hypersensitivity vasculitis.

Hypersensitivity vasculitis, also called cutaneous leukocytoclastic angiitis, is

characterized by inflammation of the small blood vessel walls. These reactions occur

when immune complex deposition within the small veins and arterioles activates

complement, causing the release of chemotactic factors. These factors attract

polymorphonuclear cells that cause vessel damage.

71–74

p. 690

p. 691

Drug-induced Vasculitis

Approximately 10% of cases of cutaneous vasculitis are believed to be drugrelated.

73 Approximately 100 drugs have been identified as causing vasculitis,

including β-lactams, fluoroquinolones, NSAIDs, antiepileptics, and tumor necrosis

factor blockers.

72–75

Interested readers are referred to more in-depth reviews.

74–76 The

diagnosis of hypersensitivity vasculitis is based on five clinical criteria (Table 32-

7), three of which must be present.

76 M.G. meets three of the five criteria, including

age greater than 16 years, palpable purpura, and a maculopapular rash. In addition,

minocycline, a medication that she was taking at the onset of the rash, has been

associated with serum sickness and vasculitic-type reactions. Onset of symptoms

typically occurs 7 to 10 days after initiation of drug therapy but can occur sooner on

reexposure. Purpuric papules and macular eruptions, the most commonly observed

findings, are usually symmetric and occur on the extremities (Table 32-8).

71

Hypersensitivity vasculitis can involve multiple organ systems. Renal damage,

ranging from microscopic hematuria to nephrotic syndrome and acute renal failure, is

common in patients with disseminated disease.

76 An enlarged liver with elevated

enzymes is indicative of hepatocellular involvement. Although the lungs and ears can

be involved as well, clinical manifestations are usually mild.

71 Arthralgia is also

commonly observed. Laboratory examinations usually show nonspecific

abnormalities of inflammation such as an elevated ESR and leukocytosis. In patients

with cystic fibrosis experiencing acute pneumonia, these laboratory abnormalities

could already be present and, therefore, will not be helpful in establishing the

diagnosis of hypersensitivity vasculitis in M.G.

Table 32-7

Criteria for the Classification of Hypersensitivity Vasculitis

Development of symptoms after age 16

Medication at disease onset that may have been a precipitating factor

Slightly elevated purpuric (hemorrhagic) rash over one or more areas of the skin that does not blanch with

pressure and is not related to thrombocytopenia

Maculopapular rash over one or more areas of the skin

Biopsy showing granulocytes around an arteriole or venule

The diagnosis of hypersensitivity vasculitis can be made if a patient exhibits at least three of these criteria.

Source: Calabrese LH et al. The American College of Rheumatology 1990 criteria for the classification of

hypersensitivity vasculitis. Arthritis Rheum. 1990;33:1108.

Table 32-8

Hypersensitivity Reactions to Drugs: Clinical Manifestations of Drug-Induced

Vasculitis

Palpable purpura and maculopapular rash occurring symmetrically predominantly on the lower extremities

Multiple organ systems may be involved:

Renal: microscopic hematuria to nephrotic syndrome and acute renal failure

Liver: enlarged liver, elevated enzymes

Joints: arthritis

Gastrointestinal: abdominal pain

Laboratory data usually show nonspecific abnormalities of inflammation: elevated erythrocyte sedimentation

rate and leukocytosis. Peripheral eosinophilia may be present and serum complement concentrations can be

low. Histologic findings on biopsy revealsmall blood vessels with leukocytoclastic or necrotizing vasculitis

Onset typically 7–21 days after initiation of therapy

Source: Valeyrie-Allanore L et al. Drug-induced skin, nail and hair disorders. Drug Saf. 2007;30:1011.

CASE 32-4, QUESTION 2: What additional workup could be performed to confirm the diagnosis of druginduced vasculitis in M.G.?

In addition to the previous workup, other laboratory and diagnostic procedures

might demonstrate peripheral eosinophilia and low serum complement

concentrations. A biopsy, which typically reveals granulocytes in the wall of a

venule or arteriole and eosinophils at any location, would provide more definitive

information.

CASE 32-4, QUESTION 3: How should M.G.’s hypersensitivity vasculitis be treated?

The first step is to discontinue the minocycline therapy. Drug-induced vasculitic

reactions typically resolve on their own without additional interventions. If the

reaction is severe, corticosteroids can be used.

Autoimmune Drug Reactions

CASE 32-5

QUESTION 1: R.F., a 24-year-old white male medical student, has been treated for 5 months with isoniazid

because of a positive skin test for tuberculosis. He now is in the clinic with complaints of new-onset myalgias

and arthralgias. Laboratory values obtained the morning of the visit are within normal limits except for a positive

ANA titer and an elevated ESR. What is the likely cause of R.F.’s symptoms and laboratory abnormalities?

Some drugs can induce an autoimmune process characterized by the presence of

autoantibodies and, in some instances, clinical features of an autoimmune disorder. A

drug-induced syndrome resembling SLE is usually characterized by myalgias,

arthralgias, positive ANA titers, and an elevated ESR (see Chapter 33, Systemic

Lupus Erythematosus). All of these characteristics are manifested by R.F.

The first case of drug-induced lupus erythematosus (DILE) was recognized more

than 60 years ago and was associated with sulfadiazine.

77 Subsequently, more than 80

drugs have been associated with DILE including isoniazid, chlorpromazine,

quinidine, methyldopa, and minocycline; however, hydralazine and procainamide are

the drugs most frequently associated with this syndrome.

78–80 As with idiopathic SLE,

DILE can be separated into systemic, subacute cutaneous, and chronic cutaneous

lupus. An exact incidence of DILE is difficult to ascertain because of changing

patterns of drug use; however, it is estimated that 10% of SLE cases are druginduced with 15,000 to 30,000 cases in the United States annually.

73

CASE 32-5, QUESTION 2: How can the diagnosis of drug-induced lupus be differentiated from SLE in

R.F.?

In contrast to idiopathic SLE, DILE is less likely to affect women and black

patients.

79 On average, patients with DILE are twice as old as those with idiopathic

SLE at the time of diagnosis. Individuals with a slow acetylator phenotype have a

greater tendency to exhibit DILE; ANA after exposure to lupus-inducing drugs also

p. 691

p. 692

appear more rapidly.

81

In general, DILE is a milder disease than idiopathic SLE.

Many patients with DILE, however, could fulfill the diagnostic criteria for SLE

according to the American Rheumatism Association.

81–83 Arthralgias or myalgias

accompanied by a positive ANA test can be the only clinical features for some

patients with drug-induced lupus. Symptoms usually appear abruptly after several

months to years of continuous therapy with the offending drug. Common complaints

include fever, malaise, arthralgias, myalgias, pleurisy, and slight weight loss. Mild

splenomegaly and lymphadenopathy have been reported occasionally. The skin is

affected in about 25% of cases manifesting as photosensitivity on light exposed

surfaces. The classic butterfly malar rash, discoid lesions, oral mucosal ulcers,

Raynaud’s phenomenon, and alopecia are unusual features in DILE in contrast to

idiopathic SLE. In addition, the central nervous system and kidneys rarely are

affected.

84 Laboratory abnormalities commonly include anemia and an elevated ESR.

The evidence supporting a diagnosis of drug-induced lupus in R.F. includes white

male predominance, abrupt onset and relatively mild symptomatology, and lack of the

classic butterfly malar rash. More definitive tests include determining whether

antibodies to single-stranded (indicative of drug-induced lupus) or double-stranded

DNA (indicative of SLE) are present.

CASE 32-5, QUESTION 3: Should ANA have been monitored in an effort to detect drug-induced lupus at an

earlier stage in this patient?

No. Although all patients with symptomatic drug-induced lupus test positive for

ANA (which consist predominantly of single-stranded DNA and antihistone

antibodies),

84 many patients taking lupus-inducing drugs become ANA positive

without going on to experience lupus. In patients treated with procainamide, about

50% to 75% are positive for ANA after 12 months and 90% after 2 years or more of

continuous therapy; only 10% to 20% of those patients actually experience lupus

symptoms.

84–86 Similarly, up to 44% of patients are ANA positive after 3 years of

hydralazine therapy, but DILE occurs in only 6.7% of patients after 3 years of

treatment.

84

It is not necessary to discontinue therapy in asymptomatic patients with

positive ANA because most of them will never exhibit clinical symptoms.

79

CASE 32-5, QUESTION 4: How should R.F.’s drug-induced lupus be treated?

Musculoskeletal complaints can be treated with aspirin or an NSAID. More severe

symptoms from pleuropulmonary or pericardial involvement may require the use of

corticosteroids. Clinical features of DILE usually subside and disappear in days to

weeks with discontinuation of the offending drug. Occasionally, these symptoms

linger or recur over a course of several months before eventually disappearing.

Serologic tests tend to resolve more slowly: ANA may persist for a year or

longer.

79,87 Drug-induced lupus does not predispose patients to the subsequent

development of idiopathic SLE.

88

In most instances, lupus-inducing drugs do not

increase the risk of exacerbation of idiopathic SLE

89

; however, long-term treatment

with isoniazid may worsen preexisting SLE.

90 Since R.F. has not yet completed his 6-

to 9-month course of isoniazid therapy, an alternative agent should be prescribed for

R.F. with appropriate monitoring (see Chapter 68, Tuberculosis).

ORGAN-SPECIFIC REACTIONS

The drug allergies in this chapter have been grouped into categories of generalized

reactions, organ-specific reactions, and pseudoallergic reactions. The generalized

reactions have been described first, the organ-specific hypersensitivity drug

reactions affecting the blood, liver, lung, kidney, and skin are described next, and

pseudoallergic reactions follow.

Blood: Immune Cytopenias

Drug-induced immune cytopenias (e.g., granulocytopenia, thrombocytopenia, and

hemolytic anemia) result from type II–mediated allergic reactions (Table 32-1). A

drug or drug metabolite binds to the surface of blood elements such as granulocytes,

platelets, and red blood cells. IgG or IgM antibodies are formed and are directed

against the drug or drug metabolite bound to the cell (i.e., hapten–cell reaction).

27

Typical symptoms associated with immune thrombocytopenia include chills, fever,

petechiae, and mucous membrane bleeding. Granulocytopenia generally manifests

with chills, fever, arthralgias, and a precipitous drop in the leukocyte count.

Symptoms of hemolytic anemia can be subacute or acute and can be sufficiently

severe to cause renal failure. The Coombs test is useful in identifying antibodies

bound to red cells or circulating immune complexes directed against red cells.

Antibiotics are the most commonly implicated class of drugs causing either

neutropenia or hemolytic anemia.

Liver

Hypersensitivity reactions involving the liver can be classified as cholestatic or

cytotoxic. Jaundice is usually the first sign of a cholestatic reaction, in addition to

pruritus, pale stools, and dark urine. Cholestatic reactions usually are reversible on

discontinuation of the offending agent. Cytotoxic reactions can involve hepatocellular

necrosis or steatosis and can result in irreversible damage if not recognized early.

Lung

Pulmonary manifestations of drug hypersensitivity include asthma and infiltrative

reactions. Asthma typically occurs as part of a generalized systemic reaction. Most

reactions to drugs that involve asthma alone represent a pharmacologic side effect

rather than a true allergic reaction.

Infiltrative reactions typically develop 2 to 10 days after exposure and manifest

with cough, dyspnea, fever, chills, and malaise.

26

Infiltrative reactions vary in

presentation from eosinophilic pneumonitis to acute pulmonary edema.

Kidney

The most common hypersensitivity reaction involving the kidney is interstitial

nephritis. Typical findings include fever, rash, and eosinophilia. Methicillin is the

drug most commonly associated with interstitial nephritis, although penicillins,

sulfonamides, and cimetidine also have been implicated in renal hypersensitivity

reactions.

27

(See Chapter 29, Acute Kidney Injury, for hypersensitivity reactions to

specific drugs that adversely affect the kidney.)

Skin

Adverse reactions involving the skin are the most common clinical manifestation of

drug allergy. Although several different types of cutaneous reactions are possible,

most drug-induced skin eruptions can be classified as erythematous, morbilliform, or

maculopapular in appearance.

27

In a surveillance study of drug-induced skin

reactions, amoxicillin was the most common cause, followed by trimethoprim–

sulfamethoxazole and ampicillin. Overall, allergic skin reactions were identified in

2% of hospitalized patients.

14

p. 692

p. 693

Treatment of skin reactions includes discontinuation of the offending drug and

general supportive care (see Chapter 39, Dermatotherapy and Drug-Induced Skin

Disorders).

PSEUDOALLERGIC REACTIONS

CASE 32-6

QUESTION 1: C.C., a 37-year-old man with no known allergies, is hospitalized for treatment of methicillinresistant S. aureus (MRSA) bacteremia associated with an infected central line. His medical history is

significant for short-bowel syndrome requiring parenteral nutrition and one previous episode of MRSA line

infection successfully treated with vancomycin. Similar to his last admission, vancomycin 750 mg IV for 60

minutes every 12 hours is begun. A trough level taken after the fifth dose, however, is 8 mg/L and the

vancomycin dose is doubled to 1,500 mg IV every 12 hours, to be administered at the same rate. Fifteen

minutes after the new dose of vancomycin is begun, C.C. experienced hypotension (100/70 mm Hg),

tachycardia (85 beats/minute), generalized pruritus, and facial flushing. C.C. is diagnosed as having a

pseudoallergic reaction to vancomycin. What subjective and objective data in C.C. are important in

differentiating vancomycin pseudoallergic reaction from a true allergic reaction?

Pseudoallergic reactions (also called nonallergic hypersensitivity reactions) are

drug reactions that exhibit clinical signs and symptoms of an allergic response but are

not immunologically mediated.

91 They can manifest as relatively benign symptoms or

as severe, life-threatening events indistinguishable from anaphylaxis (Table 32-9).

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