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Aspirin
drug data and news
Aspirin drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Aspirin | ||
| Brand Names/Synonyms | -Acetylsalicyclic Acid; A.S.A.; A.S.A. Empirin; AC 5230; ASA; Acenterine; Acesal; Acetal; Aceticyl; Acetilsalicilico; Acetilum Acidulatum; Acetisal; Acetol; Acetonyl; Acetophen; Acetosal; Acetosalic Acid; Acetosalin; Acetoxybenzoic Acid; Acetylin; Acetyls | ||
| Indication | For use as an analgesic, antipyretic, anti-inflammatory and as prophylaxis to reduce the risk of death and/or nonfatal myocardial infarction in patients with a previous infarction or unstable angina pectoris | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Aspirin (acetylsalicylic acid) is an analgesic, antipyretic, antirheumatic, and anti-inflammatory agent. It is used 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. 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. | ||
| Mechanism Of Action | Aspirin inhibits fatty acid cyclo-oxygenase (COX1 and COX2) by acetylation of the active site of the enzyme. The pharmacological effects of Aspirin are due to the inhibition of the formation of cyclo-oxygenase products including prostglandins, thromboxanes, and prostacyclin. Prostaglandins are local hormones (paracrine) produced in the body and have diverse effects in the body, including but not limited to transmission of pain information to the brain, modulation of the hypothalamic thermostat and inflammation. Thromboxanes are responsible for the aggregation of platelets that form blood clots. Heart attacks are primarily caused by blood clots, and their reduction with the introduction of small amounts of aspirin has been seen to be an effective medical intervention. The side effect of this is that the ability of the blood in general to clot is reduced, and excessive bleeding may result from the use of aspirin. Aspirin also uncouples oxidative phosphorylation in cartilaginous (and hepatic) mitochondria. It also induces the formation of NO-radicals in the body that enable the white blood cells (leucocytes) to fight infections more effectively. | ||
| Aspirin News (When available) |
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| Dosage Forms | TABLET; TABLET (ENTERIC-COATED) | ||
| Drug_Category | Fibrinolytic Agents; Anti-inflammatory Agents; Anticoagulants; Salicylates; | ||
| Absorption | Rapidly absorbed | ||
| Interactions | Interactions for Aspirin: Uricosuric Agents: Aspirin may decrease the effects of probenecid, sulfinpyrazone, and phenylbutazone. Alcohol: Has a synergistic effect with aspirin in causing gastrointestinal bleeding. Corticosteroids: Concomitant administration with aspirin may increase the risk of gastrointestinal ulceration and may reduce serum salicylate levels. Pyrazolone Derivatives (phenylbutazone, oxyphenbutazone, and possibly dipyrone): Concomitant administration with aspirin may increase the risk of gastrointestinal ulceration. Nonsteroidal Antiinflammatory Agents: Aspirin is contraindicated in patients who are hypersensitive to nonsteroidal anti-inflammatory agents. Urinary Alkalinizers: Decrease aspirin effectiveness by increasing the rate of salicylate renal excretion. Phenobarbital: Decreases aspirin effectiveness by enzyme induction. Phenytoin: Serum phenytoin levels may be increased by aspirin. Propranolol: May decrease aspirin's anti-inflammatory action by competing for the same receptors. Antacids: Enteric Coated Aspirin should not be given concurrently with antacids, since an increase in the pH of the stomach may effect the enteric coating of the tablets. | ||
| Toxicity | Aspirin can cause anaphylactic shock and other severe allergic reactions. May also result in significant bleeding in patients with peptic ulcers. LD50=1500 mg/kg (rats); LD50=1750 mg/kg (humans) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 2-acetyloxybenzoic acid | ||
| Chemical Formula | C9H8O4 | ||
| Molecular Weight | 180.157 g/mol | ||
| Smiles String | CC(=O)OC1=CC=CC=C1C(=O)O | ||
| Melting Point | 135 °C | ||
| Water Solubility | 4600 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 1.426 | ||
| Isoelectric Point | 3.49 | ||
| Biotransformation | Aspirin is mainly hydrolyzed to salicylic acid and distributed to all body tissues and fluids. The biotransformation of aspirin occurs primarily in the hepatocytes. The major metabolites are salicyluric acid (75%), the phenolic and acyl glucuronides | ||
| Half Life | 15 minutes (for salicylic acid), 3 hours for total salicylates | ||
| Protein Binding [%] | 50-80% loosely bound to plasma proteins | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Aspirin.html http://www.rxlist.com/cgi/generic/asa.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00264 | ||
| CAS Registry Number | 50-78-2 | ||
| KEGG Compound ID | C01405 | ||
| PubChem ID | SID:4594 | ||
| PharmGKB ID | PA448497 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2237726 |
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