Académique Documents
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Pain[edit]
Uncoated aspirin tablets, consisting of about 90% acetylsalicylic acid, along with a
minor amount of inert fillers and binders
Aspirin is an effective analgesic for acute pain, but is generally considered inferior
to ibuprofen for the alleviation of pain because aspirin is more likely to cause
gastrointestinal bleeding.[22] Aspirin is generally ineffective for those pains caused
by muscle cramps, bloating, gastric distension, or acute skin irritation.[23] As with
other NSAIDs, combinations of aspirin and caffeine provide slightly greater pain
relief than aspirin alone.[24] Effervescent formulations of aspirin, such as AlkaSeltzer or Blowfish,[25] relieve pain faster than aspirin in tablets,[26] which makes
them useful for the treatment of migraines.[27]
Topical aspirin may be effective for treating some types of neuropathic pain.[28]
Headache[edit]
Aspirin, either by itself or in a combined formulation, effectively treats some types
of headache, but its efficacy may be questionable for others. Secondary headaches,
meaning those caused by another disorder or trauma, should be promptly treated
by a medical provider.
Fever[edit]
Like its ability to control pain, aspirin's ability to control fever is due to its action on
the prostaglandin system through its irreversible inhibition of COX.[31] Although
aspirin's use as an antipyretic in adults is well-established, many medical societies
and regulatory agencies (including the American Academy of Family Physicians, the
American Academy of Pediatrics, and the U.S. Food and Drug Administration (FDA)
strongly advise against using aspirin for treatment of fever in children because of
the risk of Reye's syndrome, a rare but often fatal illness associated with the use of
aspirin or other salicylates in children during episodes of viral or bacterial infection.
[32][33][34] Because of the risk of Reye's syndrome in children, in 1986, the FDA
required labeling on all aspirin-containing medications advising against its use in
children and teenagers.[35]
For a subset of the population, aspirin may help prevent heart attacks and strokes.
In lower doses, aspirin has been known to prevent the progression of existing
cardiovascular disease, and reduce the frequency of these events for those with a
history of them.[39][40] (This is known as secondary prevention.)
Aspirin appears to offer little benefit to those at lower risk of heart attack or stroke
for instance, those without a history of these events or with pre-existing disease.
(This is called primary prevention.) Some studies recommend aspirin on a case-bycase basis,[41][42] while others have suggested the risks of other events, such as
gastrointestinal bleeding, were significant enough to outweigh any potential benefit,
and recommended against using aspirin for primary prevention entirely.[43]
After surgery[edit]
After percutaneous coronary interventions (PCIs), such as the placement of a
coronary artery stent, a U.S. Agency for Healthcare Research and Quality guideline
recommends that aspirin be taken indefinitely.[50] Frequently, aspirin is combined
with an ADP receptor inhibitor, such as clopidogrel, prasugrel, or ticagrelor to
prevent blood clots. This is called dual antiplatelet therapy (DAPT). United States
and European Union guidelines disagree somewhat about how long, and for what
indications this combined therapy should be continued after surgery. U.S. guidelines
recommend DAPT for at least 12 months, while EU guidelines recommend DAPT for
612 months after a drug-eluting stent placement.[51] However, they agree that
aspirin be continued indefinitely after DAPT is complete.
Cancer prevention[edit]
Aspirin reduces the overall risk of both getting cancer and dying from cancer.[52]
This effect is particularly beneficial for colorectal cancer (CRC).[21][53][54][55]
Some conclude the benefits are greater than the risks due to bleeding in those at
average risk.[52] Other are unclear if the benefits are greater than the risk.[56][57]
Given this uncertainty, the 2007 United States Preventive Services Task Force
guidelines on this topic recommended against the use of aspirin for prevention of
CRC in people with average risk.[58]
Other uses[edit]
Aspirin is a first-line treatment for the fever and joint-pain symptoms of acute
rheumatic fever. The therapy often lasts for one to two weeks, and is rarely
indicated for longer periods. After fever and pain have subsided, the aspirin is no
longer necessary, since it does not decrease the incidence of heart complications
and residual rheumatic heart disease.[59][60] Naproxen has been shown to be as
effective as aspirin and less toxic, but due to the limited clinical experience,
naproxen is recommended only as a second-line treatment.[59][61]
Along with rheumatic fever, Kawasaki disease remains one of the few indications for
aspirin use in children[62] in spite of a lack of high quality evidence for its
effectiveness.[63]
Low-dose aspirin supplementation has moderate benefits when used for prevention
of pre-eclampsia.[64][65]
Resistance[edit]
For some people, aspirin does not have as strong an effect on platelets as for
others, an effect known as aspirin resistance or insensitivity. One study has
suggested women are more likely to be resistant than men,[66] and a different,
aggregate study of 2,930 patients found 28% were resistant.[67] A study in 100
Italian patients, though, found, of the apparent 31% aspirin-resistant subjects, only
5% were truly resistant, and the others were noncompliant.[68] Another study of
400 healthy volunteers found no subjects who were truly resistant, but some had
"pseudoresistance, reflecting delayed and reduced drug absorption".[69]
Dosage[edit]
Smaller doses are based on these standards, e.g., 75-mg and 81-mg tablets. The
81-mg tablets are called "baby-strength", though they are not intended to be
administered to infants and children. No medical significance occurs due to the
slight difference in dosage between the 75-mg and the 81-mg tablets. Of historic
interest, in the United States, a 325-mg dose is equivalent to the historic 5-grain
aspirin tablet in use prior to the metric system.[citation needed]
In general, for adults, doses are taken four times a day for fever or arthritis,[70]
with doses near the maximal daily dose used historically for the treatment of
rheumatic fever.[71] For the prevention of myocardial infarction (MI) in someone
with documented or suspected coronary artery disease, much lower doses are taken
once daily.[70]
Recommendations from the USPSTF[72] on the use of aspirin for the primary
prevention of coronary heart disease encourage men aged 4579 and women aged
5579 to use aspirin when the potential benefit of a reduction in MI for men or
stroke for women outweighs the potential harm of an increase in gastrointestinal
hemorrhage.[73] The WHI study said regular low-dose (75- or 81-mg) aspirin female
users had a 25% lower risk of death from cardiovascular disease and a 14% lower
risk of death from any cause.[73] Low-dose aspirin use was also associated with a
trend toward lower risk of cardiovascular events, and lower aspirin doses (75 or 81
mg/day) may optimize efficacy and safety for patients requiring aspirin for longterm prevention.[73]
In children with Kawasaki disease, aspirin is taken at dosages based on body weight,
initially four times a day for up to two weeks and then at a lower dose once daily for
a further six to eight weeks.[74]
The American College of Chest Physicians (ACCP), the American Stroke Association (ASA), and
AHA consider aspirin or the combination of aspirin and extended-release dipyridamole acceptable
antiplatelet regimens for secondary prevention of noncardioembolic ischemic stroke and TIAs; other
options include cilostazol or clopidogrel.990 1009 When selecting an appropriate antiplatelet regimen,
consider factors such as the patient's individual risk for recurrent stroke, tolerance, and cost of the
different agents.990
Oral anticoagulation (e.g., dabigatran, warfarin) rather than antiplatelet therapy is recommended in
patients with a history of ischemic stroke or TIA and concurrent atrial fibrillation; however, in patients
who cannot take or choose not to take oral anticoagulants (e.g., those with difficulty maintaining
stable INRs, compliance issues, dietary restrictions, or cost limitations), dual antiplatelet therapy with
aspirin and clopidogrel is recommended.1009
Also used for acute treatment of ischemic stroke in children.1013
patients at moderate to high risk of CHD783 (based on age and 10-year risk of cardiac event
>10%).668 832Use of aspirin in such patients is suggested over either warfarin or no antithrombotic
therapy.
Recommended by ADA for primary prevention in patients with type 1 or type 2 diabetes mellitus who
are at high risk for cardiovascular events (i.e., familial history of CHD, smoking, hypertension,
obesity, albuminuria, elevated blood cholesterol or triglyceride concentrations) and in whom aspirin is
not contraindicated.760 830 901
Benefit appears to be minimal or lacking in women at low risk for CHD, except possibly those 65
years of age; further study needed.846 847 848 849 850 851
Not currently recommended for primary prevention in the general population without known risk
factors.646 658 661 674 675 676 783 784 847
ACCP suggests primary prevention with low-dose aspirin in individuals 50 years of age who do not
have symptomatic cardiovascular disease.1010
ACCP and ACC/AHA suggest the use of low-dose aspirin for initial (i.e., first 3 months after valve
insertion) and long-term antithrombotic therapy in patients with a bioprosthetic heart valve in the
aortic position who are in sinus rhythm and have no other indications for warfarin. 996 1008 Aspirin also
may be considered after initial (3 months) warfarin therapy in patients with a bioprosthetic heart valve
in the mitral position who are in sinus rhythm.1008
Addition of an antiplatelet agent such as low-dose aspirin to warfarin therapy recommended in all
patients with mechanical heart valves who are at low risk of bleeding. 996 1008 Combination therapy with
aspirin and warfarin also recommended in patients with bioprosthetic heart valves who have
additional risk factors for thrombosis (e.g., atrial fibrillation, previous thromboembolism, left
ventricular dysfunction, hypercoagulable condition).996
May be added to therapy with a low molecular weight heparin (LMWH) or heparin (referring
throughout this monograph to unfractionated heparin) in pregnant women with prosthetic heart
valves who are at high risk for thrombosis.1012
Pericarditis
Drug of choice for the management of pain associated with acute pericarditis following MI.635 821
Kawasaki Disease
Treatment of Kawasaki disease; used in conjunction with immune globulin IV (IGIV).636 637 638 1013
Complications of Pregnancy
Has been used alone or in combination with other drugs (e.g., heparin, corticosteroids, immune
globulin) for prevention of complications of pregnancy (e.g., preeclampsia, pregnancy loss in
women with a history of antiphospholipid syndrome and recurrent fetal
loss).594 595 596 597 599 600 601 605626 627 628 648 650 651 652 653 654 705 706 707 708 709 710 711 712 713 714 715 726 817 857 1012
Low-dose aspirin in combination with sub-Q heparin or an LMWH is recommended by ACCP in
women with antiphospholipid antibody (APLA) syndrome and a history of multiple (3) pregnancy
losses.1012
Routine use of aspirin prophylaxis to reduce the incidence and severity of preeclampsia (even in
patients at increased risk of preeclampsia) generally not recommended; 634 705 706 707 712 713 715 can consider
prophylaxis in women with prior severe or early-onset preeclampsia, chronic hypertension, severe
diabetes, or moderate to severe renal disease.815 816 817 In women at high risk for preeclampsia, ACCP
recommends low-dose aspirin during pregnancy, starting from the second trimester. 1012 (See
Pregnancy under Cautions.)
Prevention of Cancer
Limited data (observational studies) suggest that aspirin or other NSAIAs may reduce the risk of
various cancers (e.g., colorectal, breast, gastric cancer);864 870 871 872 873 such results generally not
confirmed in randomized controlled trials.864 874 875 876
Regular use (e.g., daily) associated with a reduction in the risk of recurrent colorectal adenomas and
colorectal cancer in some studies.789 790 791 792 793 794 795 796 797 798 799 800 801 802 803 804 805 806 807 808 809 810811 812 813 814 815 Beneficial
effects of NSAIAs in reducing colorectal cancer risk dissipate following discontinuance of such
therapy. Preventive therapy with aspirin currently not recommended because aspirin does not
completely eliminate adenomas; aspirin therapy should not be considered a replacement for
colorectal cancer screening and surveillance.790 793 794 795 796 814
Administer orally; may administer rectally as suppositories in patients who cannot tolerate oral
therapy.a
Do not use aspirin preparation if strong vinegar-like odor is present. a
Oral Administration
Usually administer orally with food or a full glass of water (240 mL). a 836 m
Film-coated, extended-release, or enteric-coated may be associated with less GI irritation and/or
symptomatic GI disturbances than uncoated tablets.a
Do not use delayed-release or extended-release tablets if rapid response is required. a
Swallow delayed-release and extended-release tablets whole; do not crush or chew. a
Prepare oral solution by dissolving 2 tablets for solution (Alka-Seltzer) in 120 mL of water; ingest the
entire solution to ensure adequate dosing.838 843 844
Do not chew aspirin preparations for 7 days following tonsillectomy or oral surgery; 841 837 do not place
preparations directly on tooth or gum surface (possible tissue injury from prolonged contact). a
Rectal Administration
Do not administer aspirin tablets rectally.a
Dosage
When used for pain, fever, or inflammatory diseases, attempt to titrate to the lowest effective
dosage.a
When used in anti-inflammatory dosages, development of tinnitus can be used as a sign of elevated
plasma salicylate concentrations (except in patients with high-frequency hearing impairment). a
Pediatric Patients
Dosage in children should be guided by body weight or body surface area. a 841
Do not use in children and teenagers with varicella or influenza, unless directed by a clinician. 841(See
Contraindications under Cautions.)
Pain
Oral
Children 211 years of age: 1.5 g/m2 daily administered in 46 divided doses (maximum 2.5
g/m2 daily).a
Dose may be given every 4 hours as necessary (up to 5 times in 24 hours). 841
Dosage for Self-medication of Pain in Children <12 Years of Age841
Age
Weight
Oral Dose
<14.5 kg
Consult clinician
3<4 years
14.516 kg
160 mg
4<6 years
1620.5 kg
240 mg
6<9 years
20.530 kg
320 mg
9<11 years
3035 kg
320400 mg
11 years
3538 kg
320480 mg
For self-medication in children 12 years of age, 325650 mg every 4 hours (maximum 4 g daily) or
1 g every 6 hours as necessary.836 e
For self-medication in children 12 years of age, 454 mg (as chewing gum pieces) every 4 hours as
necessary (maximum 3.632 g daily).837
For self-medication in children 12 years of age, 650 mg (as highly buffered effervescent solution
[Alka-Seltzer Original]) every 4 hours (maximum 2.6 g daily); alternatively, 1 g (Alka-Seltzer Extra
Strength) every 6 hours (maximum 3.5 g daily).843 844
Rectal
Children 211 years of age: 1.5 g/m2 daily administered in 46 divided doses (maximum 2.5
g/m2 daily).a
Children 12 years of age: 325650 mg every 4 hours as necessary (maximum 4 g daily). a
Fever
Oral
Children 211 years of age: 1.5 g/m2 daily administered in 46 divided doses (maximum 2.5
g/m2 daily).a
Dose may be given every 4 hours as necessary (up to 5 times in 24 hours). 841
Dosage for Self-medication of Fever in Children <12 Years of Age841
Age
Weight
Oral Dose
<14.5 kg
Consult physician
3<4 years
14.516 kg
160 mg
4<6 years
1620.5 kg
240 mg
6<9 years
20.530 kg
320 mg
9<11 years
3035 kg
320400 mg
11 years
3538 kg
320480 mg
Rectal
Children 211 years of age: 1.5 g/m2 daily administered in 46 divided doses (maximum 2.5
g/m2 daily).a
Children 12 years of age: 325650 mg every 4 hours as necessary (maximum 4 g daily). a
Inflammatory Diseases
Juvenile Rheumatoid Arthritis
Oral
Initially, 90130 mg/kg daily in divided doses.c m Increase dosage as necessary for anti-inflammatory
efficacy; target plasma salicylate concentration is 150300 mcg/mL. c m Plasma concentrations >200
mcg/mL associated with an increased incidence of toxicity.c m
Rheumatic Fever
Oral
Initially, 90130 mg/kg daily given in divided doses every 46 hours for up to 12 weeks for maximal
suppression of acute inflammation, followed by 6070 mg/kg daily in divided doses for 16
weeks.a Adjust dosage based on response, tolerance, and plasma salicylate
concentrations.aGradually withdraw over 12 weeks.a
Various regimens suggested depending on severity of initial manifestations.a Consult published
protocols for more information on specific dosages and schedules.a
Thrombosis
Acute Arterial Ischemic Stroke
Oral
ACCP recommends 15 mg/kg daily initially until cerebral arterial dissection and cardioembolic
causes have been excluded; subsequently, continue same dosage for 2 years. 1013
In children with acute arterial ischemic stroke secondary to non-Moyamoya vasculopathy, at least 3
months of therapy recommended; ongoing antithrombotic therapy should be guided by repeat
cerebrovascular imaging.1013
Fontan Procedure
Oral
15 mg/kg daily recommended by ACCP; optimal duration of therapy unknown.1013
Kawasaki Disease
Oral
Initially, 80100 mg/kg daily given in 4 equally divided doses (in combination with IGIV) for up to 14
days; initiate within 10 days of onset of fever.636 637 638 639 640 1013 When fever subsides, decrease dosage to
15 mg/kg once daily.636 637 638 950 1013
Continue indefinitely in those with coronary artery abnormalities;638 950 1013 in the absence of such
abnormalities, continue low-dose aspirin for 68 weeks.638 950 1013
Adults
Pain
Oral
For self-medication, 325650 mg every 4 hours (maximum 4 g daily) or 0.51 g every 6 hours as
necessary.836 e
For self-medication, 454 mg (as chewing gum pieces) every 4 hours as necessary (maximum 3.632
g daily).837
Adults <60 years of age for self-medication: 650 mg (as a highly buffered effervescent solution [AlkaSeltzer Lemon-Lime or Original]) every 4 hours (maximum 2.6 g daily); alternatively, 1 g (AlkaSeltzer Extra Strength) every 6 hours (maximum 3.5 g daily).838 843 844
Adults 60 years of age for self-medication: 650 mg (as a highly buffered effervescent solution [AlkaSeltzer Lemon-Lime or Original]) every 4 hours (maximum 1.3 g daily); alternatively, 1 g (AlkaSeltzer Extra Strength) every 6 hours (maximum 1.5 g daily).838 843 844
Rectal
325650 mg every 4 hours as necessary (maximum 4 g daily). a
Fever
Oral
325650 mg every 4 hours as necessary (maximum 4 g daily). a
For self-medication, 454 mg (as chewing gum pieces) every 4 hours as necessary (maximum 3.632
g daily).837
Rectal
325650 mg every 4 hours as necessary (maximum 4 g daily). a
Inflammatory Diseases
Rheumatoid Arthritis and Arthritis and Pleurisy of SLE
Oral
Initially, 3 g daily in divided doses.c l m Increase dosage as necessary for anti-inflammatory efficacy;
target plasma salicylate concentration is 150300 mcg/mL.c l m Plasma concentrations >200 mcg/mL
associated with an increased incidence of toxicity.c l m
Osteoarthritis
Oral
Up to 3 g daily in divided doses.c m
Spondyloarthropathies
Oral
Up to 4 g daily in divided doses.c m
Rheumatic Fever
Oral
Initially, 4.97.8 g daily in divided doses given for maximal suppression of acute inflammation. aAdjust
dosage based on response, tolerance, and plasma salicylate concentrations. a
Various regimens suggested depending on severity of initial manifestations.a Consult published
protocols for more information on specific dosages and schedules.a
Acute Treatment
Oral
ACCP recommends 160325 mg daily, initiated ideally within 48 hours of stroke onset; may decrease
dosage after 12 weeks to reduce bleeding risk. 1009 (See Transient Ischemic Attacks and Acute
Ischemic Stroke: Secondary Prevention, under Dosage.)ACCP states that initiation of aspirin therapy
should be delayed for 24 hours following administration of recombinant tissue-type plasminogen
activator (r-tPA, e.g., alteplase).1009
Primary Prevention of MI
Oral
Some experts recommend 75162 mg once daily.681 682 760 783 Continue indefinitely, provided there are no
contraindications.681 682 760 783
ACCP suggests primary prevention with low-dose aspirin (75100 mg daily) in individuals 50 years
of age who do not have symptomatic cardiovascular disease. 1010
Combination aspirin (75100 mg daily) and warfarin therapy recommended by ACC/AHA for patients
with bioprosthetic heart valves and additional risk factors for thromboembolism.996
Aspirin 75325 mg once daily also recommended as an alternative to warfarin therapy in any patient
who is unable to take warfarin.996
Pericarditis
Acute Pericarditis Following MI
Oral
162325 mg daily.635 821 Higher dosages (e.g., 650 mg every 46 hours) may be required.635 821
Complications of Pregnancy
Oral
Antiphospholipid syndrome and a history of multiple ( 3) pregnancy losses: Antepartum
prophylaxis with aspirin (75100 mg daily) in combination with sub-Q heparin or an LMWH
recommended by ACCP.1012
Patients at risk for preeclampsia: ACCP recommends low-dose aspirin during pregnancy (starting
from the second trimester).1012
Prescribing Limits
Pediatric Patients
Pain
Oral
Children 211 years of age: Maximum 2.5 g/m2 daily.a
Children 12 years of age: Maximum 4 g daily.836 Maximum 2.6 g as highly buffered effervescent
solution (Alka-Seltzer Original) or 3.5 g (Alka-Seltzer Extra Strength) in 24 hours.843 844
For self-medication, do not exceed recommended daily dosage.841 Treatment duration for selfmedication for pain: 5 days.841 (See Advice to Patients.) Treatment duration for self-medicationof
sore throat pain using chewing gum: 2 days.837
Rectal
Fever
Oral
Children 211 years of age: Maximum 2.5 g/m2 daily.a
Children 12 years of age: Maximum 4 g daily.836
For self-medication, do not exceed recommended daily dosage.841 Treatment duration for selfmedication: <3 days.841 (See Advice to Patients.)
Rectal
Children 211 years of age: Maximum 2.5 g/m2 daily.a
Children 12 years of age: Maximum 4 g daily.a
Adults
Pain
Oral
Maximum 4 g daily.a Treatment duration for self-medication for pain: 10 days.841 Aspirin chewing gum
should not be used for self-medication of sore throat pain for longer than 2 days.837 (See Advice to
Patients.)
Adults <60 years of age taking highly buffered effervescent solutions: Maximum 2.6 g (AlkaSeltzerLemon-lime or Original) or 3.5 g (Alka-Seltzer Extra Strength) in 24 hours.838 843 844
Adults 60 years of age taking highly buffered effervescent solutions: Maximum 1.3 g (AlkaSeltzerLemon-lime or Original) or 1.5 g (Alka-Seltzer Extra Strength) in 24 hours.838 843 844
Rectal
Maximum 4 g daily.a
For self-medication, maximum 500 mg (in combination with acetaminophen 500 mg and caffeine 130
mg) in 24 hours.701
Fever
Oral or Rectal
Maximum 4 g daily.a
Special Populations
Geriatric Patients
Highly buffered effervescent solution: Maximum 1.3 g (Alka-SeltzerLemon-Lime or Original) or 1.5 g
(Alka-Seltzer Extra Strength) in 24 hours.838 843 844
Children or adolescents with viral infections (with or without fever) because of the possibility
that the infection may be one associated with an increased risk of Reyes syndrome. c m (See
Pediatric Use under Cautions.)
Warnings/Precautions
Warnings
Alcohol
Long-term heavy alcohol use (3 alcoholic beverages daily) associated with an increased risk of
aspirin-induced bleeding.c j m (See Advice to Patients.)
Hematologic Effects
Inhibits platelet aggregation and may prolong bleeding time. c m These effects may be particularly
important in patients with inherited (e.g., hemophilia) or acquired (e.g., liver disease, vitamin K
deficiency) bleeding disorders.c m
Because of the increased risk of bleeding, avoid aspirin-containing chewing gum tablets or gargles
for 1 week after tonsillectomy or oral surgery.h
GI Effects
Serious GI toxicity (e.g., bleeding, ulceration, perforation) can occur with or without warning
symptoms.c Increased risk in those with a history of GI bleeding or ulceration, geriatric patients,
those receiving an anticoagulant, receiving prolonged therapy, taking multiple NSAIAs concomitantly,
and consuming 3 alcohol-containing beverages daily.j
Avoid in patients with active peptic ulcer disease; can cause gastric mucosal irritation and
bleeding.c m
Sensitivity Reactions
Anaphylactoid reactions, severe urticaria, angioedema, or bronchospasm reported. 836 c h m
Immediate medical intervention and discontinuance for anaphylaxis.836
Contraindicated in patients with syndrome of asthma, rhinitis, and nasal polyps;c m caution in patients
with asthma.c
General Precautions
Sodium Content
Avoid highly buffered aspirin preparations in patients with CHF, renal failure, or other conditions in
which high sodium content would be harmful.c m
Specific Populations
Pregnancy
Category C (Category D in third trimester).
Use only if clearly needed.c m Avoid use in the third trimester because of possible premature closure
of the ductus arteriosus.c m Avoid 1 week prior to and during labor and delivery; aspirin use prior to
and during labor associated with excessive blood loss at delivery.c m
Maternal and fetal hemorrhagic complications observed with maternal ingestion of large doses (e.g.,
1215 g daily) of aspirin594 595 597 611 612 generally have not been observed in studies in which low doses
(60150 mg daily) of the drug were used for prevention of complications of
pregnancy.594 595 596 597 598 599 600 601 605 626 627 629 630 631 632
Lactation
Distributed into milk; use not recommended.c m High doses may result in adverse effects (rash,
platelet abnormalities, bleeding) in nursing infants.c m
Pediatric Use
Dosing recommendations for juvenile rheumatoid arthritis based on well controlled clinical
studies.c m High dosages that result in plasma concentrations >200 mcg/mL associated with an
increased incidence of toxicity.c m
Use in children with varicella infection or influenza-like illnesses reportedly is associated with an
increased risk of developing Reyes syndrome.166 167 168 169 468 538 549 638 US Surgeon General, AAP Committee
on Infectious Diseases, FDA, and other authorities advise that salicylates not be used in children and
teenagers with varicella or influenza, unless directed by a clinician. 466 467 554 638Generally avoid salicylates
in children and teenagers with suspected varicella or influenza and during presumed outbreaks of
influenza, since accurate diagnosis of these diseases may be impossible during the prodromal
period;466 use of salicylates in the management of viral infections in children or adolescents is
contraindicated, since the infection may be one associated with an increased risk of Reyes
syndrome.646 m
Use with caution in pediatric patients who are dehydrated (increased susceptibility to salicylate
intoxication).h
Safety and efficacy of aspirin in fixed combination with extended-release dipyridamole not
established.738
Risk of overdosage and toxicity (including death) in children <2 years of age receiving preparations
containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in
combination for relief of symptoms of upper respiratory tract infection. 937 939 Limited evidence of efficacy
for these preparations in this age group; appropriate dosages not established. 937 Use such
preparations in children <2 years of age with caution and only as directed by clinician. 937 939 Clinicians
should ask caregivers about use of OTC cough/cold preparations to avoid overdosage. 937
Hepatic Impairment
Avoid in patients with severe hepatic impairment.c m
Renal Impairment
Avoid in patients with GFR <10 mL/minute.c m
Specific Drugs
Drug
Interaction
Comments
ACE inhibitors
Monitor BPc
inhibitorsc
Possible attenuation of
hemodynamic actions of ACE
inhibitors in patients with CHFh
Reduced hyponatremic effect of
ACE inhibitorsc m
Alcohol
Alkalinizing
agents
Anticoagulants
(warfarin,
heparin)
Anticonvulsants
May displace phenytoin from binding Monitor patients receiving aspirin with
sites; possible decrease in total
valproic acidh
Antidiabetic
drugs
effectc m
(sulfonylureas)
-adrenergic
Reduced BP response to -
blocking agents
Monitor BPc
Carbonic
anhydrase
inhibitors
(acetazolamide)
Corticosteroids
concentrations
drugh
Diuretics
acetazolamide toxicitycm
Methotrexate
concentrationsh
Inhibition of renal clearance of
methotrexate leading to bone
marrow toxicity, especially in
geriatric patients or patients with
renal impairmentm
NSAIAs
recommendedc m p q r
or other complications861 m p q r
No consistent evidence that lowdose aspirin mitigates increased risk
of serious cardiovascular events
many NSAIAsh
aspirin858 859
ibuprofen858 859
of aspirin858 859
effects861
Pyrazinamide
Tetracycline
Thrombolytic
agents
effect579 580 581 582 583 584 585 586 587 588589 590
Uricosuric
agents
uricosuric agentsc m
(probenecid,
sulfinpyrazone)
Varicella virus
vaccine live
syndrome
638
Aspirin Pharmacokinetics
Absorption
Bioavailability
Well absorbed following oral administration.h m Rapidly metabolized to salicylic acid; plasma aspirin
concentrations are undetectable 12 hours after administration. m Peak plasma salicylic acid
concentrations attained within 12 hours following administration of uncoated tablets. m
Slowly and variably absorbed following rectal administration. h
Onset
Single oral doses of rapidly absorbed preparations: 30 minutes for analgesic and antipyretic effects. h
Rectal suppositories: 12 hours for antipyretic effects.h
Continuous oral therapy: 14 days for anti-inflammatory effect.h
Food
Food decreases rate but not extent of absorption; peak plasma concentrations of aspirin and
salicylate may be decreased.h
Plasma Concentrations
Plasma salicylate concentrations of 30100 mcg/mL produce analgesia and antipyresis; the
concentration required for anti-inflammatory effect is 150300 mcg/mL; toxicity noted at 300350
mcg/mL.h
Steady-state plasma salicylate concentrations increase more than proportionally with increasing
doses as a result of capacity-limiting processes.h
Special Populations
During the febrile phase of Kawasaki disease, oral absorption may be impaired or highly variable. h
Distribution
Extent
Widely distributed; aspirin and salicylate distribute into synovial fluid.a h m Crosses placenta and
distributed into milk.m
Elimination
Metabolism
Partially hydrolyzed to salicylate by esterases in the GI mucosa.a Unhydrolyzed aspirin subsequently
undergoes hydrolysis by esterases mainly in the liver but also in plasma, erythrocytes, and synovial
fluid.a
Salicylate is metabolized in the liver by the microsomal enzyme system.h
Elimination Route
Excreted in urine via glomerular filtration and renal tubular reabsorption as salicylate and its
metabolites.h Urinary excretion of salicylate is pH dependent; as urine pH increases from 5 to 8,
urinary excretion of salicylate is greatly increased.h
Half-life
Aspirin: 1520 minutes.a
Half-life of salicylate increases with increasing plasma salicylate concentrations. h m
Salicylate: 23 hours when aspirin administered in low doses (325 mg).h
Salicylate: 1530 hours when aspirin administered in higher dosages.h
Special Populations
Salicylate and its metabolites readily removed by hemodialysis and, to a lesser extent, by peritoneal
dialysis.h
Stability
Storage
Oral
Capsules
Aspirin in fixed-combination with extended-release dipyridamole: 25C (may be exposed to 15
30C).738 Protect from excessive moisture.738
Gum
1525C; protect from excessive moisture.837
Tablets
Room temperature (Bayer products, excluding Alka-Seltzer products);839 840 841 842 m avoid high humidity
and excessive heat (40C).840
1530C (Easprin).l
2025C (Anacin Extra Strength); protect from moisture.836
Protect from excessive heat (Alka-Seltzer products).838 843 844
Rectal
Suppositories
215C.a
Actions
The existence of 2 COX isoenzymes with different aspirin sensitivities and extremely different
recovery rates of their COX activity following inactivation by aspirin at least partially explains the
different dosage requirements and durations of aspirin effects on platelet function versus the
drugs analgesic and anti-inflammatory effects.1016
Effects on urinary excretion of uric acid are dose related; large dosages (e.g., 1.3 g 4 times
daily) enhance urinary excretion and decrease serum concentrations of uric acid , intermediate
dosages (e.g., 650 mg to 1 g 3 times daily) usually do not alter uric acid excretion, and low
dosages (e.g., <325 mg 3 times daily) inhibit excretion and may increase serum uric acid
concentrations.h
Advice to Patients
When used for self-medication, importance of reading the product labeling.836 841 e 837 838 843 844
When used for self-medication, importance of asking clinician whether to use aspirin or
another analgesic if alcohol consumption is 3 alcohol-containing drinks per day. 836 e 837 838 841843 844
Importance of informing patients about risk of bleeding associated with chronic, heavy
alcohol use while taking aspirin.j m
When used for self-medication in children, importance of basing the dose on the childs
weight or body surface area.841
In patients with drug-eluting stents (DES) receiving aspirin in combination with clopidogrel or
ticlopidine, importance of not discontinuing antiplatelet therapy without consulting cardiologist,
even if instructed to do so by other health-care professional (e.g., dentist).886
Importance of not using aspirin for chicken pox or flu symptoms in children or adolescents
without consulting a clinician.836 e 837 838 841 843 844
Patients receiving anticoagulants and those with asthma, gout, diabetes, arthritis, peptic
ulcers, bleeding problems, or stomach problems that persist or recur should consult a clinician
before using aspirin for self-medication.836 e 837 838 841 843 844
Discontinue and consult clinician if pain or fever persists or progresses, new symptoms
occur, redness or swelling is present in a painful area, or ringing in the ears or loss of hearing
occurs.836 e 837 838 841 843 844
Importance of women informing clinicians if they are or plan to become pregnant or to breastfeed.c Importance of avoiding aspirin in late pregnancy (third trimester) and during labor and
delivery.c
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some
individuals; consult specific product labeling for details.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary)
name