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Overview
| Generic Names: | 2-Acetoxybenzenecarboxylic acid; 2-Acetoxybenzoic acid; 2-Carboxyphenyl acetate; A.S.A.; ASA; Acetilsalicilico; Acetilum acidulatum; Acetosalic acid; Acetoxybenzoic acid; Acetylsalicylate; Acetylsalicylic acid; Acetylsalicylsaure (GERMAN); Acetysalicylic acid; Acide acetylsalicylique (FRENCH); Acido O-acetil-benzoico; Acido acetilsalicilico; Acidum acetylsalicylicum; Kyselina 2-acetoxybenzoova; Kyselina acetylsalicylova; O-Acetylsalicylic acid; O-accetylsalicylic acid; Salicylic acid acetate; Salicylic acid, acetate; o-Acetoxybenzoic acid; o-Carboxyphenyl acetate |
|---|---|
| Trade Names: | 8-hour Bayer; A.S.A. Empirin; Acenterine; Acesal; Acetal; Aceticyl; Acetisal; Acetol; Acetonyl; Acetophen; Acetosal; Acetosalin; Acetylin; Acetylsal; Acimetten; Acisal; Acylpyrin; Adiro; Asagran; Asatard; Ascoden-30; Aspalon; Aspec; Aspergum; Aspirdrops; Aspirine; Aspro; Asteric; Bayer Extra Strength Aspirin For Migraine Pain; Benaspir; Bi-prin; Bialpirina; Bialpirinia; Bufferin; Caprin; Cemirit; Claradin; Clariprin; Colfarit; Contrheuma retard; Coricidin; Crystar; Decaten; Delgesic; Dolean pH 8; Duramax; ECM; Easprin; Ecolen; Ecotrin; Empirin; Endydol; Entericin; Enterophen; Enterosarein; Enterosarine; Entrophen; Extren; Globentyl; Globoid; Helicon; Idragin; Levius; Measurin; Micristin; Neuronika; Novid; Nu-seals; Nu-seals aspirin; Persistin; Pharmacin; Pirseal; Polopiryna; Premaspin; Rheumintabletten; Rhodine; Rhonal; Salacetin; Salcetogen; Saletin; Solfrin; Solprin; Solprin acid; Solpyron; Spira-Dine; St. Joseph; St. Joseph Aspirin for Adults; Supac; Tasprin; Temperal; Triaminicin; Triple-sal; Vanquish; Xaxa; Yasta |
| Brand Mixtures: | Aspirin Plus Stomach Guard (Acetylsalicylic Acid + Calcium Carbonate + Magnesium Carbonate + Magnesium Oxide); Aspirin Plus Stomach Guard Ext.Stgth.Caplet (Acetylsalicylic Acid + Calcium Carbonate + Magnesium Carbonate + Magnesium Oxide); Aspirin Plus Stomach Guard Extra Strength (Acetylsalicylic Acid + Calcium Carbonate + Magnesium Carbonate + Magnesium Oxide); Aspirin Plus Stomach Guard Tab (Acetylsalicylic Acid + Calcium Carbonate + Magnesium Carbonate + Magnesium Oxide); Aspirin with Stomach Guard (Acetylsalicylic Acid + Calcium Carbonate + Magnesium Carbonate + Magnesium Oxide); Aspirin with Stomach Guard Extra Strength - Tab (Acetylsalicylic Acid + Calcium Carbonate + Magnesium Carbonate + Magnesium Oxide); Extra Strength Aspirin Backache (Acetylsalicylic Acid + Methocarbamol) |
| PharmGKB Accession Id: | PA448497 |
Description
The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5) (source: unavailable)
Indication
For use in the temporary relief of various forms of pain, inflammation associated with various conditions (including rheumatoid arthritis, juvenile rheumatoid arthritis, systemic lupus erythematosus, osteoarthritis, and ankylosing spondylitis), and is also used to reduce the risk of death and/or nonfatal myocardial infarction in patients with a previous infarction or unstable angina pectoris. (source: Drug Bank)
ATC Therapeutic Categories
- A01AD:Other agents for local oral treatment
- B01AC:Platelet aggregation inhibitors excl. heparin
- N02BA:Salicylic acid and derivatives
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
The analgesic, antipyretic, and anti-inflammatory effects of aspirin are due to actions by both the acetyl and the salicylate portions of the intact molecule as well as by the active salicylate metabolite. Aspirin directly and irreversibly inhibits the activity of both types of cyclo-oxygenase (COX-1 and COX-2) to decrease the formation of precursors of prostaglandins and thromboxanes from arachidonic acid. This makes aspirin different from other NSAIDS (such as diclofenac and ibuprofen) which are reversible inhibitors. Salicylate may competitively inhibit prostaglandin formation. Aspirin's antirheumatic (nonsteroidal anti-inflammatory) actions are a result of its analgesic and anti-inflammatory mechanisms; the therapeutic effects are not due to pituitary-adrenal stimulation. The platelet aggregation–inhibiting effect of aspirin specifically involves the compound's ability to act as an acetyl donor to the platelet membrane; the nonacetylated salicylates have no clinically significant effect on platelet aggregation. Aspirin affects platelet function by inhibiting the enzyme prostaglandin cyclooxygenase in platelets, thereby preventing the formation of the aggregating agent thromboxane A2. This action is irreversible; the effects persist for the life of the platelets exposed. Aspirin may also inhibit formation of the platelet aggregation inhibitor prostacyclin (prostaglandin I2) in blood vessels; however, this action is reversible. (source: Drug Bank)
Pharmacology
Aspirin (acetylsalicylic acid) is an analgesic, antipyretic, antirheumatic, and anti-inflammatory agent. Aspirin's mode of action as an antiinflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. Aspirin appears to produce analgesia by virtue of both a peripheral and CNS effect. Peripherally, Aspirin acts by inhibiting the synthesis and release of prostaglandins. Acting centrally, it would appear to produce analgesia at a hypothalamic site in the brain, although the mode of action is not known. Aspirin also acts on the hypothalamus to produce antipyresis; heat dissipation is increased as a result of vasodilation and increased peripheral blood flow. Aspirin's antipyretic activity may also be related to inhibition of synthesis and release of prostaglandins. (source: Drug Bank)
Food Interactions
Avoid alcohol, alcohol appears to cause a 50 to 100% increases in ASA serum levels.
Avoid drastic changes in dietary habit.
Consult your doctor before taking large amounts of Vitamin K (Green leafy vegetables).
Take with a full glass of water.
Take with food to reduce irritation.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Aspirin is rapidly hydrolyzed primarily in the liver to salicylic acid, which is conjugated with glycine (forming salicyluric acid) and glucuronic acid and excreted largely in the urine. (source: Drug Bank)
Protein Binding
High (99.5%) to albumin. Decreases as plasma salicylate concentration increases, with reduced plasma albumin concentration or renal dysfunction, and during pregnancy. (source: Drug Bank)
Absorption
Absorption is generally rapid and complete following oral administration but may vary according to specific salicylate used, dosage form, and other factors such as tablet dissolution rate and gastric or intraluminal pH. (source: Drug Bank)
Toxicity
Oral, mouse: LD<sub>50</sub> = 250 mg/kg; Oral, rabbit: LD<sub>50</sub> = 1010 mg/kg; Oral, rat: LD<sub>50</sub> = 200 mg/kg. Effects of overdose include: tinnitus, abdominal pain, hypokalemia, hypoglycemia, pyrexia, hyperventilation, dysrhythmia, hypotension, hallucination, renal failure, confusion, seizure, coma, and death. (source: Drug Bank)
Isomeric SMILES Code:
CC(=O)Oc1ccccc1C(=O)O (source: Drug Bank)
Curated Annotations (
)
-
rs2768759
at chr1:155119087
in
NTRK1
This variant is associated with enhanced agonist-induced platelet aggragation and response to aspirin in both whites and african americans. The C allele was associated with increased aggregation of native platelets to collagen, epinephrine. The C allele was also associated with reduced platelet responsiveness to aspirin. (N=1486)- Related Drugs:
- aspirin
- Evidence:
-
PMID:18511696
-
rs2046934
at chr3:152540332
in
MED12L,
P2RY12
This is one of four SNPs that comprise H1/H2 haplotypes. The four SNPs (C139T, T744C, ins801A, G52T(=G50T) are in perfect LD, and T744C is frequently used as the tagging SNP. H1 is 139C/744T/no ins at 801A/52G. H2(minor haplotype) is 139T/744C/ins801A//52T. H2 haplotype has been found to be associated with enhanced platelet reactivity, peripheral artery disease, coronary artery disease(particularly in non-smokers)and with poor response to clopidogrel. In other studies, no association was found between haplotype and response to clopidogrel or aspirin or with cardiovascular events.- Variant Name:
- P2RY12:T744C,P2RY12:i-T744C
- Related Drugs:
- aspirin, clopidogrel
- Related Diseases:
- Coronary Artery Disease, Peripheral Vascular Diseases
- Evidence:
-
PMID:12912815
PMID:14662702
PMID:15795539
PMID:16181985
PMID:16405973
PMID:16581111
PMID:16769602
PMID:16961627
PMID:17337040
PMID:17803810
-
rs730012
at chr5:179153244
in
LTC4S
A two-family study indicates that aspirin-induced urticaria aggregates in families in which the C allele of this SNP is present.- Variant Name:
- LTC4S:-444C
- Related Drugs:
- aspirin
- Related Diseases:
- Urticaria
- Evidence:
-
PMID:16433794
-
rs730012
at chr5:179153244
in
LTC4S
Risk or phenotype-associated allele: C. Phenotype: A-444C was associated with aspirin-induced urticaria (AIU). The C allele was more frequent in patients with the cutaneous pattern of AIU and in patients with low skin reactivity to histamine. Study size: 110 patients with AIU and 165 nonallergic controls .- Variant Name:
- LTC4S: A-444C
- Related Drugs:
- aspirin
- Related Diseases:
- Urticaria
- Evidence:
-
PMID:19862937
-
rs3842787
at chr9:124173328
in
PTGS1
Risk-associated allele: not specified. Phenotype: Serum thromboxane (TXB2), urinary 11-dehydro-TXB(2) and arachidonic acid-induced aggregation were measured in the group (n=30) taking a four-week course of low-dose aspirin. None of the indices evaluated was significantly different (p>0.05) between carriers of the 50T allele (n=1 homozygous, n=4 heterozygous) and carriers of the 50C allele (n=25 homozygous) at any time point during aspirin treatment and after withdrawal. In conclusion, this study found no relationship between the 50T/-842G haplotype and PTGS1 sensitivity to aspirin.- Variant Name:
- PTGS1: P17L; (C>T)
- Related Drugs:
- aspirin
- Evidence:
-
PMID:19350112
-
rs5918
at chr17:42715729
in
ITGB3
Risk or phenotype-associated allele: C. Phenotype: In a study of clotting times of microvascular injury, the P1A2 allele (C variant) was associated with shorter bleeding time and less response to aspirin. Study size: 24. Study population/ethnicity: Healthy males 21-24 years. Significance metric(s): p = 0.003. Type of association: PD.- Variant Name:
- ITGB3:1565T>C, ITGB3:Leu33Pro, P1A2, PIA1/PIA2, Leu33Pro polymorphism of ß3 integrins, GP3A PIA2, GP IIIa HPA-1, HPA-1b
- Related Drugs:
- aspirin
- Evidence:
-
PMID:11723016
-
rs5918
at chr17:42715729
in
ITGB3
Risk or phenotype-associated genotype: T/T Phenotype: This study investigated the association of ITGB3 SNP with a greater prevalence of platelet hyperactivity (HPR) in stable coronary artery disease. HPR patients with inadequate aspirin inhibition were significantly more often homozygous PlA1/A1 (T/T) (65.4% vs. 47.7%, p=0.015). Study size: 188 Study population/ethnicity: patients with stable coronary artery disease, most of them were males (89.9%), current smokers (71.3%), type 2 diabetics (38.3%) or having hypertension (26.6%)- Variant Name:
- ITGB3:1565T>C, ITGB3:Leu33Pro, P1A2, PIA1/PIA2
- Related Drugs:
- aspirin
- Related Diseases:
- Coronary Artery Disease
- Evidence:
-
PMID:20138334
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
|
COMT |
|
Publications |
|
|
CYP3A4 |
|
Publications |
|
|
ITGA2 |
|
Publications |
|
|
ITGA2B |
|
Publications |
|
|
ITGB3 |
|
Publications, Variants |
|
|
LTC4S |
|
Publications, Variants |
|
|
MED12L |
|
Variants |
|
|
NAT2 |
|
Publications |
|
|
NR1I2 |
|
Publications |
|
|
NTRK1 |
|
Variants |
|
|
P2RY1 |
|
Publications |
|
|
P2RY12 |
|
Variants |
|
|
PEAR1 |
|
Publications |
|
|
PPARG |
|
Publications |
|
|
PTGS1 |
|
Publications, Variants |
|
|
PTGS2 |
|
Publications, Variants |
|
|
UGT1A6 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
|
|
Proton pump inhibitors |
|
Publications |
|
|
warfarin |
|
Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acenocoumarol |
|
The salicylate increases the effect of anticoagulant (source: Drug Bank) |
| acetazolamide |
|
The salicylate at high dose increases the effect of the carbonic anyhydrase (source: Drug Bank) |
| chlorpropamide |
|
The salicylate increases the effect of sulfonylurea (source: Drug Bank) |
| cortisone acetate |
|
The corticosteroid decreases the effect of salicylates (source: Drug Bank) |
| dexamethasone |
|
The corticosteroid decreases the effect of salicylates (source: Drug Bank) |
| dicumarol |
|
The salicylate increases effect of anticoagulant (source: Drug Bank) |
| ginkgo biloba |
|
Association of ASA/ginkgo increases risk of bleeding (source: Drug Bank) |
| glibenclamide |
|
The salicylate increases the effect of sulfonylurea (source: Drug Bank) |
| gliclazide |
|
The salicylate increases the effect of sulfonylurea (source: Drug Bank) |
| glipizide |
|
The salicylate increases the effect of sulfonylurea (source: Drug Bank) |
| griseofulvin |
|
Anticipate decrease of ASA efficiency in presence of griseofulvin (source: Drug Bank) |
| heparin |
|
Association of ASA/heparin increases risk of bleeding (source: Drug Bank) |
| hydrocortisone |
|
The corticosteroid decreases the effect of salicylates (source: Drug Bank) |
| ibuprofen |
|
Ibuprofen reduces ASA cardioprotective effects (source: Drug Bank) |
| insulin-glargine |
|
The salicylate increases the effect of insulin (source: Drug Bank) |
| ketorolac |
|
ASA increases toxicity of ketorolac (source: Drug Bank) |
| methazolamide |
|
The salicylate at high dose increases the effect of the carbonic anhydrase inhibitors (source: Drug Bank) |
| methotrexate |
|
The salicylate increases the effect and toxicity of methotrexate (source: Drug Bank) |
| methylprednisolone |
|
The corticosteroid decreases the effect of salicylates (source: Drug Bank) |
| prednisolone |
|
The corticosteroid decreases the effect of salicylates (source: Drug Bank) |
| prednisone |
|
The corticosteroid decreases the effect of salicylates (source: Drug Bank) |
| probenecid |
|
The salicylate decreases the uricosuric effect of probenecid (source: Drug Bank) |
| sulfinpyrazone |
|
The salicylate antagonizes the uricosuric effect of sulfinpyrazone (source: Drug Bank) |
| ticlopidine |
|
Increased effect of ticlopidine (source: Drug Bank) |
| tolbutamide |
|
The salicylate increases the effect of sulfonylurea (source: Drug Bank) |
| triamcinolone |
|
The corticosteroid decreases the effect of salicylates (source: Drug Bank) |
| valproic acid |
|
The salicylate increases the effect of valproic acid (source: Drug Bank) |
| warfarin |
|
The salicylate increases the effect of anticoagulant (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Acute coronary syndrome |
|
Publications |
|
|
Arteriosclerosis |
|
Publications |
|
|
aspirin-induced asthma |
|
Publications |
|
|
Asthma |
|
Publications |
|
|
Cardiovascular Diseases |
|
Publications |
|
|
Colorectal Neoplasms |
|
Publications |
|
|
Colorectal Neoplasms, Hereditary Nonpolyposis |
|
Publications |
|
|
Coronary Artery Disease |
|
Publications, Variants |
|
|
Coronary Disease |
|
Publications, Variants |
|
|
Death |
|
Publications |
|
|
Myocardial Infarction |
|
Publications |
|
|
Peripheral Vascular Diseases |
|
Publications, Variants |
|
|
Pre-Eclampsia |
|
Publications |
|
|
Stroke |
|
Publications |
|
|
Urticaria |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Curated Phenotype Datasets
These datasets are sorted alphabetically by title.
- ITPC Ethnicity Data Set, 2009




- PD
- PK
- GN
Submitted by Warfarin Consortium involving CYP2C9, VKORC1, amiodarone, aspirin, simvastatin, warfarin, and Atrial Fibrillation - IWPC Warfarin Data Set (NEJM 2009)




- PD
- PK
- GN
Submitted by Warfarin Consortium involving CYP2C9, VKORC1, amiodarone, aspirin, simvastatin, warfarin, and Atrial Fibrillation - Use of Pharmacogenetic and Clinical Factors to Predict the Therapeutic Dose of Warfarin




- PD
- PK
- GN
Submitted by Brian Gage, MD involving CYP2C9, VKORC1, amiodarone, aspirin, simvastatin, warfarin, , Atrial Fibrillation, post-orthopedic, Pulmonary Embolism, Stroke and Venous Thrombosis
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
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LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
