Nsaids: Salicylates
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NSAIDS: Salicylates
I would like to delve further to the most widely used class of drugs that is nonsteroidal anti-inflammatory drugs (NSAIDs). The first NSAID, which is the Aspirin, was developed in 1897 by a German chemist Felix Hoffmann, who was working for a pharmaceutical company Bayer (Connelly, 2014). The discovery or the medicine was due to adding up an acetyl group to salicylic acid that exhibited a decreased amount of its irritant properties, to which the company has patented the process (Connelly, 2014). To date, there are a number of NSAIDS that can be bought over the counter and some are only readily available with prescription making it the commonly encountered drug in any medical practice.
According to Ciccone, NSAIDs have numerous diverse features such as ability to lower inflammation, alleviate mild to moderate ache, and decrease increased body temperature associated with fever, and decrease blood clotting by obstructing plate accumulation (Ciccone, 2016, p. 219. UpToDate has highlighted that at present there are now 20 various nonsteroidal antiinflammatory drugs (NSAIDs), the six major classes that are classified by it chemical structures can be obtained in the United States (Solomon, 2015).
There is a clear individual variation in response to nonsteroidal anti-inflammatory drugs (NSAIDs) (Solomon, 2015, para. 15). In fact, it has been noted that some patients demonstrate better reaction to one drug than to others (Solomon, 2015). It is therefore important to breakdown the pharmacodynamics of particular NSAIDs down to its biochemical and physiological outcomes in order to determine its exact response and effectiveness (Solomon, 2015). NSAIDs have regulatory effects on the gene transcription and protein synthesis of multiple molecules involved in several inflammatory and neoplastic pathways (Stolfi, Simone, Pallone, & Monteleone, 2013, p. 17973). NSAIDs suppresses cyclooxygenase (COX) expression/activity and downstream signals, which are crucial for CRC cell growth, survival and diffusion (Stolfi et al., 2013, p. 17973). Hence, NSAIDs exert an analgesic effect through the peripheral inhibition of prostaglandin biosynthesis thereby producing therapeutic effects (Sinha et al., 2013).
For the purpose of thoroughly summarizing one of the six classes of the aforementioned medication, I will concentrate on Salicylates, particularly Aspirin.
Aspirin or Acetylsalicylic acid, have its place in the major group of drugs recognized as the salicylates (Ciccone, 2016). It has been in circulation for over a century due to its reasonable price and ease of use even without any prescription (Ciccone, 2016).
Indications
Salicylates is indicated to ease pain, swelling and fever. The drug is known to treat arthritis and rheumatic fever. It is commonly recommended by cardiologists to protect bypass grafts and stents in the heart. It is also utilized for the purpose of lowering the risk of heart attack, stroke and the prevention of premature death (“,” n.d.). Moreover, it can be taken to relieve musculoskeletal conditions such as sprains, strains, and low back pain (“Aspirin,” n.d.).
Mechanism of Action
Salicylates such as Aspirin, non-selectively and irreversibly inhibits cyclooxygenase, reducing prostaglandin and thromboxane A2 synthesis, producing analgesic, anti-inflammatory and antipyretic effects and reducing platelet aggregation (“Aspirin,” 2016).
These compounds appear to be hormones that act locally to help regulate cell function under normal and pathological conditions (Ciccone, 2016, p. 220). It is thought that preventing COX1 specifically aspirin, can lead to gastrointestinal bleeding and ulcers and inhibiting COX-2 causes anti inflammatory, analgesic and antipyretic effects. Primary function of COX-1 enzyme produces prostaglandins to help regulate and maintain cell activity for instance, protection of GI tract, renal homeostasis and platelet accumulation (Ciccone, 2016, p. 223).
Absorption
The bioavailability is 80-100%. The onset for aspirin taken by mouth is 5 to 30 minutes with a duration of 4 to 6 hours. On the other hand, it would take an hour or two if administered rectally with duration of less than 7 hours. Peak plasma time for oral medication is 0.25 to 3 hours. Peak plasma concentration for analgesic/antipyretic is at 30-100 mcg/mL while for inflammatory is set at 150-300 mcg/mL (“Aspirin,” n.d.).
Metabolism
Aspirin is metabolized in the liver through the microsomal enzyme system. It is an active metabolite. The enzymes it inhibits is Cyclooxygenase (“Aspirin,” n.d.).
Elimination
The drug is excreted in the urine at 8-100%. Its half-life on a low dosage is between 2-3 hours, while on the higher dosage is at 15-30 hours. Renal clearance are within 24-72 hours at 80-100%. It can also be eliminated in sweat, saliva and feces. It can be dialyzed.
Contraindications
Drug should be withheld to individuals with hypersensitivity to NSAIDs such as asthma, rhinitis, and nasal polyps. Caution should be indicated when the drug is prescribed to children or teenagers for treatment of viral infections, with or without fever. There is a limited record of any allergenic cross-reactivity for salicylates. But due to some similarities in the chemical structure, the likelihood of cross-sensitivity cannot be ruled out with forgone conclusion (“,” n.d.).
Adverse Reactions
According to UpToDate, like any other drugs that have a huge effect on hemostasis “ bleeding is associated with aspirin” (“,” n.d., para. 30). The possibility of hemorrhage is expected and may occur at any site. There are also certain “many adverse effects of aspirin are dose related, and are extremely rare at low dosages” (“,” n.d., p. 30).
There are several serious reactions of Aspirin such as Reye’s Syndrome, angioedema, GI perforation, DIC, nephrotoxicity and hepatoxicity among others. Common reactions to the drug would be nausea and vomiting, dyspepsia, abdominal pain, tinnitus, dizziness, hyperuricemia, ecchymosis, constipation and diarrhea.
Safety/Monitoring
Monitoring should be rigorous when the drug is given to a special population. In pediatric, if used for self-medication – children and teenagers who “have or are recovering from chickenpox or flu-like symptoms should not use this product” (“Aspirin,” 2016, para. 7). One should take note if there are any “changes