Pharm - Non- Narcotics Flashcards
What is the MOA of NSAID’s?
Inhibition of cyclo-oxygenase (COX) → inhibition of prostaglandin synthesis
Which enzyme is inducible enzyme; induced by cytokines & endotoxins in inflammation?
Cycolo-oxygenase 2 ( COX-2)
Where can COX -2 enzymes be found?
In macrophages, endothelial cells, fibroblasts, Leukocytes
Where can COX-1 enzymes be found?
Intestines
Stomach
Platelets
Kidneys
What are the classification of NSAIDS?
- Non-selective COX Inhibitors
- Selective COX-2 Inhibitors
What are examples of Selective COX-2 inhibitors?
Celecoxib (Celebrex)
Etoricoxib (Arcoxia)
What are examples of the Non - Selective COX inhibitors?
SALICYLATES: Aspirin (acetylsalicylic acid), sodium salicylate, diflunisal
ACETIC ACID DERIVATIVES: Indomethacin, diclofenac, aceclofenac
FENAMATES: Mefenamic acid, meclofenamate
PROPIONIC ACID DERIVATIVES: Ibuprofen, dexketoprofen, ketoprofen, fIurbiprofen, naproxen, oxaprozin
OXICAMS: Piroxicam, tenoxicam, meloxicam, lornoxicam
What are the examples of Acetic acid derivatives?
Indomethacin
Diclofenac
Aceclofenac
What are examples of Salicylic acid derivatives?
- Aspirin (acetylsalicylic acid), *Sodium salicylate
*Diflunisal
Fill in the blanks. “Mefenamic acid & meclofenamate are examples of _________.”
Fenamates
What are examples of Propionic acid derivatives?
- Ibuprofen
*Dexketoprofen - Ketoprofen
- FIurbiprofen
*Naproxen
*Oxaprozin
What are examples of Oxicams?
- Piroxicam
- Tenoxicam
- Meloxicam
- Lornoxicam
What are the Main pharmacological actions of NSAIDS?
- Analgesic effects
- Anti-inflammatory effects
- Antipyretic effects
- Anti-platelet activity
Fill in the blanks.” ____ & _______ mediate Vasodilation leading to oedema.”
PGE2 & PGI2
True or False? NSAIDs also inhibit migration of leukocytes & macrophages to site of inflammation.
TRUE!!
Which compound is responsible for platelet aggregation?
Thromboxane A2 ( TXA2)
Which drug irreversible inhibits platelet aggregation?
Aspirin
True or False? COX-2 inhibitors also have anti-platelet activity.
FALSE!! COX 2 inhibitors DO NOT have any antiplatelet activity
What is the lifespan of Aspirin anti-platelet activity?
7-10 days
Which drug can be used to ↑ ionization & elimination of salicylic acid in aspirin overdose?
Sodium bicarbonate
What are the adverse effects of Aspirin?
- GI effects: N,V, gastric bleeding, ulceration
- Hypersensitivity reactions (bronchospasm, rash, rhinitis)
- Prolonged bleeding time
- Reye’s Syndrome (↑ risk in children with viral infection leading to severe hepatic injury & encephalopathy)
Which drug is an additional mechanism of antagonizing PG receptors (especially in uterus) &
May reduce blood loss in menorrhagia?
Fenamates- Mefenamic acid
Which NSAID can cause closure of ductus arteriosus in premature infants ?
Indomethacin
What is the MOA for Selective COX-2 inhibitors?
Selective reversible inhibitor of COX 2, blocking arachidonic acid → PGG 2 & subsequent production of prostaglandins & thromboxanes
True or False? COX 2 inhibitors lack any antiplatelet activity .
TRUE!!
Which NSAID should be avoided in patients with a sulpha allergy?
Celecoxib
True or False? Acetaminophen should not be classified as an NSAID as it is not an anti-inflammatory agent.
TRUE!!!
How does Acetaminophen differ from NSAIDS?
Acetaminophen differs from NSAIDs in that it does not possess significant anti-platelet activity.
What is the Antidote for Acetaminophen toxicity?
Acetylcysteine (provides sulfhydryl group to inactivate toxic metabolite)
