What is the therapeutic index of aspirin?
Therapeutic Index and Toxic Doses Therapeutic drug levels for aspirin are 150 to 300 mcg/mL (salicylate). Plasma levels of aspirin can range from 3 to 10 mg/dL for therapeutic doses to as high as 70 to 140 mg/dL for acute toxicity.
How aspirin is metabolized?
Therefore, aspirin has a very short half-life. Salicylate, in turn, is mainly metabolized by the liver. This metabolism occurs primarily by hepatic conjugation with glycin or glucuronic acid, each involving different metabolic pathways. The predominant pathway is the conjugation with glycin, which is saturable.
What is the prototype for aspirin?
Mechanisms of Action of Aspirin Aspirin is a prototype of non-steroidal anti-inflammatory drugs (NSAIDs), and member of the family of salicylates that have in common salicylic acid as the active agent. Salicylic acid is composed of a benzene ring and two radicals, one hydroxyl and one carboxyl.
What is a safe therapeutic index?
The larger the therapeutic index (TI), the safer the drug is. If the TI is small (the difference between the two concentrations is very small), the drug must be dosed carefully and the person receiving the drug should be monitored closely for any signs of drug toxicity.
How much therapeutic index is safe?
Drugs with TI’s greater than 10 are considered relatively safe while those with TI’s less than 3 typically require tighter controls on manufacturing (to ensure that the dosing is accurate) and patient monitoring.
How is aspirin metabolised and excreted?
Excretion of salicylates occurs mainly through the kidney, by the processes of glomerular filtration and tubular excretion, in the form of free salicylic acid, salicyluric acid, and, additionally, phenolic and acyl glucuronides Label.
Is aspirin rapidly metabolized?
It is rapidly hydrolyzed in the body to salicylic acid; the plasma concentration of the latter must be maintained within a relatively narrow range to obtain an adequate anti-inflammatory effect and to minimize systemic adverse effects.
What type of inhibitor is aspirin?
For example, aspirin is an irreversible inhibitor of cyclooxygenase activity.
Is aspirin a Cox-2 inhibitor?
Selectivity of COX inhibitors There are 3 classes of COX inhibitors: aspirin, nonselective NSAIDs (e.g., indomethacin), and a new class of selective COX-2 inhibitors known as the “coxibs” (e.g., celecoxib, rofecoxib).
How do you make aspirin from salicylic acid?
Aspirin Aspirin is synthesized by the acetylation of salicylic acid using acetic anhydride or acetyl chloride. 8. CONTINUED…
What is aspirin used for?
Aspirin is used in the treatment of migraine • Aspirin is an important part of treatment of those who have had a myocardial infraction (heart attack). • For a subset of the people, aspirin may help prevent heart attacks and strokes. In lower doses, aspirin prevents the progression of cardiovascular disease.
What are the chemical properties of aspirin?
Chemical properties •Aspirin decomposes rapidly in solutions of ammonium acetate or of the acetates, carbonates, citrates, or hydroxides of the alkali metals. It is stable in dry air, but gradually hydrolyses in contact with moisture to acetic and salicylic acids. 12.
Why is aspirin contraindicated in a peptic ulcer?
Aspirin act as an analgesic, antipyretic, Anti-inflammatory also inhibit platelet aggregation & prolongs bleeding time, because of its effect on G.I.T it is contraindicated in peptic ulcer, in this case we use paracetamol . Aspirin is not given to children because is may cause raye’s syndrome.