Salicylates

Salicylates Struktur
CAS-Nr.
Englisch Name:
Salicylates
Synonyma:
Salicylates
CBNumber:
CB01306473
Summenformel:
Molgewicht:
0
MOL-Datei:
Mol file

Salicylates Eigenschaften

Sicherheit

Salicylates Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften

Aspirin is a weak organic acid and is one of the oldest known drugs for the relief of fever and pain. Aspirin remains the standard to which most NSAIDs are compared for efficacy.

Indications

The salicylates are useful in the treatment of minor musculoskeletal disorders such as bursitis, synovitis, tendinitis, myositis, and myalgia.They may also be used to relieve fever and headache. They can be used in the treatment of inflammatory disease, such as acute rheumatic fever, rheumatoid arthritis, osteoarthritis, and certain rheumatoid variants, such as ankylosing spondylitis, Reiter’s syndrome, and psoriatic arthritis. However, other NSAIDs are usually favored for the treatment of these chronic conditions because of their lower incidence of GI side effects. Aspirin is used in the treatment and prophylaxis of myocardial infarction and ischemic stroke.

Mechanism of action

Aspirin and related salicylates produce their pharmacological effects predominantly by inhibiting the synthesis of prostaglandins and to a lesser extent synthesis of the thromboxanes (implicated in platelet aggregation). The prostanoids are mediators of inflammatory responses in many cell types. Aspirin is unique among NSAIDs in that it irreversibly acetylates COX-1 and COX-2, which are required for the synthesis of prostanoids from arachidonic acid. COX-2 is induced during inflammation and is therefore considered to mediate most inflammatory responses. Aspirin acetylation of COX-1 permanently inactivates the enzyme, while acetylated COX-2 is capable of producing 15-HETE. New enzyme must be synthesized to overcome the effects of aspirin, which in the case of platelets can take as long as 11 days. The metabolite of aspirin, salicylic acid, is a reversible inhibitor of COX. Other NSAIDs have reversible effects at different sites on COX-1 and on COX-2. In addition, aspirin interferes with kinin-induced modulation of the inflammatory response.

Clinical Use

Aspirin and related salicylates are the primary treatment for mild to moderate pain, such as that associated with headache, joint and muscle pain, and dysmenorrhea. At higher doses aspirin is an effective analgesic in rheumatoid arthritis.The analgesic effects of salicylates are thought to be due to the inhibition of prostaglandin synthesis in the periphery and to a less well documented mechanism at cortical areas.
The salicylates are also potent antipyretic agents, with the exception of diflunisal, which is only weakly active. Aspirin acts at two distinct but related sites. It decreases prostaglandin-induced fever in response to pyrogens and induces a decrease in interleukin-1 modulation of the hypothalamic control of body temperature. Thus, the hypothalamic control of body temperature returns, vasodilation occurs, heat dissipates, and fever decreases. Other uses of aspirin include inhibition of platelet aggregation via inhibition of thromboxanes, which has been shown to decrease the incidence of blood clots, myocardial infarction, and transient ischemic attacks.

Nebenwirkungen

The most commonly observed side effects associated with the use of salicylates relate to disturbances of the GI tract. Nausea, vomiting, epigastric discomfort, intensification of symptoms of peptic ulcer disease (e.g., dyspepsia and heartburn), gastric ulcerations, erosive gastritis, and GI hemorrhage occur in individuals on high doses of aspirin. The incidence of these side effects is more rare at low doses, but a single dose of aspirin can cause GI distress in 5% of individuals.

Arzneimittelwechselwirkung

The salicylates displace a number of drugs from plasma protein binding sites, thereby leading to potential adverse effects by these agents. Since aspirin is an over-thecounter medication, patients may fail to inform the doctor of their aspirin consumption. Anticoagulants are potentiated by aspirin by displacement of the anticoagulants from plasma proteins and the intrinsic anticoagulant effect of aspirin. Thus, the dosage of drugs such as coumarin and heparin should be reduced in patients taking aspirin. A similar effect is observed in patients taking oral sulfonylureas (Orinase, DiaBeta) for non–insulin-dependent diabetes or phenytoin (Dilantin) for seizures. Displacement of the sulfonylureas or phenytoin from plasma binding necessitates a decrease in dosage to prevent an acute hypoglycemic event or sedation, respectively.Aspirin enhances the effects of insulin (leading to hypoglycemia), penicillins and sulfonamides (increasing acute toxicity), and corticosteroids. Aspirin increases the hypotensive effects of the cardiac drug nitroglycerin but decreases the effectiveness of the loop diuretics. In patients taking methotrexate for cancer chemotherapy, aspirin may increase retention of the drug, and severe toxicity may result.
Conversely, certain drugs modify the effectiveness or side effects of aspirin. Phenobarbital, occasionally used for seizures, induces liver enzymes that increase the metabolism and excretion of aspirin, β-adrenoceptor– blocking drugs, such as propranolol, and decrease the antiinflammatory effects of aspirin, whereas reserpine decreases its analgesic effects. Antacids decrease the absorption of aspirin. Alcohol consumption in combination with aspirin increases the latter’s ulcerogenic effects.

Salicylates Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Salicylates Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 1)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Scandinavian Formulas --
mikep@scandinavianformulas.com United States 1550 58

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