Aspirin is a salicylate, also known as a non steroidal anti-inflammatory drug (NSAID). It is the generic name of acetylsalicylic acid and is used clinically to treat fever, pain and inflammation as it works by preventing the formation of prostaglandin. Prostaglandin is the active agent that is responsible for the sensitisation at the nerve endings. It can be administered orally, rectally or by intravenous route. (6)
Benzene ring Carboxylic acid Ester Alkane
Aspirin has a pKa of 3.49 and a melting point of 138-140 degrees Celsius. Aspirin molecule’s are insoluble in water that is why it must be sold in a solid form, there are no liquid forms of aspirin available. Aspirin is ionised in the stomach. Aspirin is easily hydrolysed as …show more content…
A salicylate, is mainly metabolised by the liver, due to hepatic conjugation with either glucuronic acid or glycine, in which both have different metabolic pathways. The primary pathway is the conjugation with glycine, which is saturable and approximately 90% of salicylate is metabolised through this pathway with low doses of aspirin. When the maximum capacity of this pathway is achieved, the other pathways with a lower clearance become more important. Therefore, the half-life of the salicylate depends on the significant metabolic pathway used at a given concentration, and with increasing dosage, it becomes longer. A salicylate is known to follow nonlinear kinetics at the upper limit of the dosing range. Certain studies report that there is much inter-subject variation with respect to the relative contribution of the dissimilar salicylate metabolic pathways.
Urinary excretion of an unchanged salicylate accounts for 10% of the full elimination of the salicylate. Elimination of a salicylate is the result of glomerular filtration, active proximal tubular secretion through the organic acid transporters and passive tubular reabsorption. Urinary elimination is clearly pH dependent and as the urinary pH rises from 5 to 8. The amount of free ionised salicylate eliminated is increased from 3% of the total salicylate dose to over 80%, due …show more content…
In majority of cases, some degree of acid-base disturbances exist. A mixed respiratory alkalosis and metabolic acidosis with either normal or high arterial pH (normal or decreased hydrogen ion conc.) is usual in adults and children ages 4 years or over. In children aged under 4 years, a dominant metabolic acidosis with low arterial pH (raised hydrogen ion concentration) is common. Increased acidity in the blood, may increase salicylate transfer across the blood brain barrier.