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NSAID
Types of drugs and their effect
Question | Answer |
---|---|
What does NSAID Stand for? | Non Steroidal Anti Inflammatory Drugs. |
What converts Arachidonic acid and what does it form into? | COX 1 and COX 2 enzymes, they form Prostaglandins(PG), P. Cyclins(PGI) and Thromboxane(TXA) |
What are Prostaglandins? | Prostaglandins are found in all cells, they are converted from Arachidonic acid. They cause pain, important in conception in females, maintain gut micro-biome, integrity of plasma membrane, cause inflammation, platlet agrigation and normal renal function |
How do NSAIDs work | NSAIDS work by inhibiting COX. Non selective NSAIDs block both COX 1 and COX 2,where as selective NSAIDs will inhibit COX 2. If the COX is inhibited, the formation of prostaglandins will be inhibited, reducing pain and inflammation amongst other things |
What are COX 1 Prostaglandins associated with? | GI mucosal integrity, Platelet function , renal function |
What are COX 2 Prostaglandins associated with? | Pain, fever, inflammation |
What are the 3 effects most NSAIDs have? | Analgesic, for pain. Anti inflammatory, for inflamation. Anti pyretic, for fever. |
Why are non-selective NSAIDs used over selective NSAIDS? | Inhibition of COX 2 will lead to an increase in COX-1-derived thromboxane which leads to cardiovascular events. |
What are the examples of Non selective NSAIDs? | Aspirin, Ibuprofen, Naproxen, Diclofenac, Ketorolac |
What are the examples of selective NSAIDs? | : Celecoxib, Etoricoxib, Parecoxib |
Aspirin | (Salicylate)Aspirin irreversibly inhibits COX by acetylation of the enzyme. Has a fourth effect, Anti-platelet. Inhabition of TXA will reduce platelet aggregation, prolonged bleeding. Used post-infarction and post-stroke: reduces risk of reinfarction. |
Adverse effects of Aspirin | Nausea , vomiting, epigastric distress, bleeding Hypersensitivity reactions: urticaria, asthma, angioneurotic edema Repeated anti-inflammatory dose can lead to SALICYLISM Tinnitus, dizziness, vertigo, hearing impairment. Not suitable for gout. |
Acute aspirin poisoning effects and how to treat | Vomiting, dehydration, electrolyte imbalance, hyperglycemia, petechial hemorrhages, hyperpyrexia, convulsions. External cooling and IV fluids ,Gastric lavage,Forced alkaline diuresis,Blood transfusion and Vit. K |
Ibuprofen uses and adverse effects | Soft tissue injuries, Dysmenorhoea, Rheumatoid Arthritis(RA), Osteo- Arthritis(OA), Closing patent ductus arteriosus in pre-term infants. GI eefect |
Diclofenac | More potent, Inhibit chemotaxis and superoxide production at the inflammatory site. Used more after dental surgeries, Rheumatoid arthritis and Osteoarthritis. Adverse effects are milder, Elevation of hepatic enzymes. |
KETOROLAC | Potent analgesic with moderate anti-inflammatory effect (Analgesic efficacy equals morphine). Used for Postsurgical, dental, musculoskeletal pain (Given I.M / I.V ). Side effects: GI and Renal toxicity |
Selective NSAIDs | Selectively inhibit COX-2 enzyme at the site of inflammation, same action of non selective NSAIDs except anti platelet effect. Lesser GI side effect. Uses: Long term: OA, RA, Gouty arthritis Short term: Post-operative pain, dental pain |
Adverse effect of selective NSAIDs | Thrombotic events due to increased COX 1 thromboxane Rofecoxib has been withdrawn due to increased risk of heart attack and stroke Nephrotoxicity Preferred in patients with high risk of peptic ulcer Start at lowest dose for shortest period of time |
Paracetamol (acetaminophen) | Weak COX1 ,COX2 inhibiter Inhibits COX3 in the weak COX 1 and COX 2 inhibitor. Inhibits COX 3 in CNS. Acts on the Hypothalamis(centre for pain temperature)Good Analgesic and antipyretic No antiplatelet, gastric irritation, or hypersensitivity |
Paracetamol toxicity | Paracetamol is the safest NSAID but can lead to liver failure if used excessively. In chronic alcoholics, even lower doses of paracetamol can cause hepatotoxicity. N-Acetylcysteine can be given to replenishes glutathione stores. |
Best NSAID for mild to mod. pain with little inflammation | paracetamol/ibuprofen |
Best NSAID for post-operative or acute short lasting pain | ketorolac, ibuprofen, diclofenac |
Best NSAID for acute musculoskeletal, osteoarthritis | ibuprofen, diclofenac, paracetamol |
Best NSAID for gastric intolerance | paracetamol |
Best NSAID for history of asthma | paracetamol |
Best NSAID for children | paracetamol, ibuprofen |
Best NSAID for pregnancy | paracetamol |