Thursday, October 8, 2020

NSAIDs :Uses .side effects .Mechanism of action

 NSAIDs :Machanis of action,side effects

NSAIDs


nsaids meaning -  Non steroidal antiinflammatory drugs

Mechanism of action -  Enzyme inhibitor
Biological target        -  COX-1 and COX-2

Classification of Non steroidal antiinflammatory drugs -

types of nsaids-

Non selective COX inhibitors (Traditional NSAIDs)

Salicylates - Aspirin

Acetic acid derivative - Ketorolac                                                                                                                    Indomaethacin                                                                                                            Nebumatone

Enolic acid derivative-                                                                                                                                       Piroxicam , Tenoxicam

Propionic acid derivative -                                                                                                                               Ibuprofen, Flurbiprofen, Ketoprofen, Naproxen

Fenamate-                

                                       Mephanamic acid

Pyrazolone derivative - 

                                       Phenyl butazone,Oxyphenbutaxone



Selective COX-2 inhibitor -

Etoricoxib

Celecoxib

Parecoxib


Preferential COX-2 inhibitor - 

Diclofenac

Acelofenac

Nimesulide

Meloxicam

Etodolac


Antipyretic-Analgesic with poor Antiinflammatory action - 

Para-aminophenol derivative : 

                                        Paracetamol(Acetaminphen)

Pyrazolone derivative : 

                                        Metamizol(Dipyrone),Propiphenazone

Benzoxazocine derivative : 

                                        Nefopam


Mechanism of action of NSAIDs

Prostaglandin synthesis inhibition

Prostaglandin, prostacyclin(PG I2) and Thromboxane a2(TXA2) are produced from arachidonic acid by the enzyme cyclooxygenase which exist in a constitutive  (COX-1) and an inducible (COX-2) isoform,the former serves physiological housekeeping function,while the latter normally present in minute quantities,is induced by cytokines and other signal molecules at the site of inflammation -->generation of PGs locally which mediate many of the inflammatory changes. However, COX-2 is constitutivaly present at some sites in brain, in juxtaglomerular cells and in foetus : It may serve physiological role at these sites. Most NSAIDs inhibit COX-1 and COX-2 nonselectivaly, but now some selective COX-2 inhibitors have been produced.  Features of non selective COX1COX2 inhibitors(traditional NSAIDs) and selective COX-2 inhibitors.It acts as Analgesic, antipyretic and antiinflammatory.


nsaids side effects

Gastric pain

Mucosal erosion

Peptic ulcer

Pregnancy - NSAID in late pregnacy has been found to promote premature closure of ductus in some cases.

Headache

Nausea

NSAIDs affect kidney


NSAIDs uses

Analgesic(Pain killer)

Antipyretic(Fever)

Antiinflammatory


Other questions - 

Which drugs are NSAIDs?

Mentioned above(Non steroidal antiinflammatory drugs)


Selective COX-2 inhibitor -

Etoricoxib

Celecoxib

Parecoxib


Non selective COX inhibitors (Traditional NSAIDs)

Salicylates - Aspirin

Acetic acid derivative - Ketorolac                                                                                                                    Indomaethacin                                                                                                            Nebumatone

Enolic acid derivative-                                                                                                                                       Piroxicam , Tenoxicam

Propionic acid derivative -                                                                                                                               Ibuprofen, Flurbiprofen, Ketoprofen, Naproxen

Fenamate-                

                                       Mephanamic acid

Pyrazolone derivative - 

                                       Phenyl butazone,Oxyphenbutaxone


Preferential COX-2 inhibitor - 

Diclofenac

Acelofenac

Nimesulide

Meloxicam

Etodolac


Antipyretic-Analgesic with poor Antiinflammatory action - 

Para-aminophenol derivative : 

                                        Paracetamol(Acetaminphen)

Pyrazolone derivative : 

                                        Metamizol(Dipyrone),Propiphenazone

Benzoxazocine derivative : 

                                        Nefopam


What are some common NSAIDs?

Paracetamol,Diclofenac ,Acelofenac

Is paracetamol an Nsaid?

Yes