Term
| What is the MOA of NSAID's? |
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Definition
| Inhibits Cycloxegenase (COX) synthesis thus in turn inhibiting production of prostaglandins.. results in reduction of inflammation |
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Term
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Definition
•Aspirin
•Naproxen
•Diclofenac sodium
•Ibuprofen, Indomethacin
•Acetaminophen (Paracetomol)
•Ketorolac, Nabumatone, Diflunisal
•Celecoxib ,Etoricoxib, Valdecoxib
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Term
| Name the NSAID which has a poor anti-inflammatory but strong analgesic action |
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Definition
Potent Analgesic but poor anti inflammatory Drugs
Ex: Acetaminophen ( Paracetamol), Ketorolac |
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Term
What are the outcomes of COX 1 activation
What ADR is associated wit its inhibition? |
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Definition
GI - cyto protection
Platelet aggregation
GI ulcers |
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Term
| What are the out comes of COX 2 activation |
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Definition
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Term
| What are the 2 types of NSAID's |
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Definition
Non Selective COX Inhibitors (inhibit both COX-1
&2) - Potent Analgesic and potent
antiinflammatory Drugs - Aspirin, Diclofenac,
Naproxen, Ibuprofen, Indomethacin
Highly selective COX-2 inhibitors
Ex: Celecoxib, valdecoxib, etoricoxib
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Term
| What is the specific MOA of Aspirin? |
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Definition
Non selective IRREVERSIBLE COX inhibitor
All the other NSAID's are reversible |
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Term
| What are the Drug interactions associated with NSAID's? |
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Definition
| NSAID's is highly protein boud |
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Term
| What are the ADR's of NSAID's? |
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Definition
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Gastric and duodenal ulcers - Most of NSAIDs
reduce mucus secretion (PGs required for mucus)
This adverse effect is not seen or rarely seen with
selective cox-2 inhibitors .
2.Renal and hepatic toxicity
3.Precipitation of Bronchial asthma by increasing
the production of leukotreines (since cox is
inhibited all arachidonic acid is now diverted
to produce more leukotriens which mediates
bronchoconstriction)
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Term
| Which is the only NSAID with an antiplatelet action & why |
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Definition
| ASPRIN - due to the irreversible inhibition of COX via acetylation |
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Term
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Definition
1. In acute reuhmatic fever very HIGH dose
2. Anti platelet drug - transient ischemic attack (TIA) or MI - very LOW dose |
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Term
| What are the ADR's of ASPIRIN? |
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Definition
•Gastric duodenal ulcers, hepatotoxicity, asthma
•Reyes syndrome …after treating with Aspirin
hepatic encephalopathy in children having viral infection
•Salicylism with higher dose…..Vomiting, Tinnitus, Vertigo, loss of hearing- reversible
•Acute salicylate poisoning- common in children-
Clinical Features: Vomiting, dehydration ( due to
metabolic acidosis), delirium, hyperthermia,
convulsions, coma and death due to respiratory
failure
•At toxic salicylate levels- respiratory alkalosis followed by metabolic acidosis
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Term
What NSAID causes acute poisoning?
How is it treated? |
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Definition
Aspirin
External cooling by tepid sponging, IV
fluids, NaHCO3 (sodium bicarbonate),gastric lavage, forced alkaline diuresis and haemodialysis |
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Term
When is Indomethacin the DOC?
What are the ADR's |
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Definition
•More potent anti-inflammatory action than other NSAIDs
•USES: This drug is preferred over other NSAID in following conditions
•Rheumatoid arthritis
•Gout
•Ankylosing spondylitis
•Patient Ductus Arteriosus
•A/E: pain abdomen, GI haemorrhage
•15-25%- headache
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Term
| When is Ketorolac used & why? |
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Definition
| Post opp pain (mild) as it is a poor anti-inflammatory but a very good analgesic |
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Term
COXIB's
Drugs?
MOA
Use?
ADR? |
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Definition
Celecoxib , rofecoxib valdecoxib
Selectively block COX 2 - no GI effects, no
antiplatelet action
•Use: rheumatoid arthritis, osteoarthritis
•A/E: renal toxicity, cardiovascular thrombotic events (Rofecoxib)
•Avoid them in Patients allergic to sulfonamides (cross allergy as both drugs are chemically related)
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Term
Acetominophen (paracetamol)
MOA?
Use?
ADR |
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Definition
Blocks COX 3 better than COX 1 & 2
Fever & non inflammatory pain - tooth ache, headach etc.
Hepatotoxicity & acute tubular necrosis. |
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Term
What is responsible for the hepatotoxicity seen with Acetominophen/ Paracetamol?
How is it treated? |
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Definition
•N-acetyl benzoquinone is the minor metabolite
which is detoxified by glutathione conjugation.
In poisoning- more quantity of minor metabolite
is formed which cannot be detoxified and
accumulates to cause Hepatic cell necrosis.
•Tx - N-acetyl cysteine which replenishes the
glutathione stores of liver.
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Term
| What drugs are used in treating RA? |
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Definition
Acute RA - NSAID's (stops the inflammation and pain associated wit the disease ONLY) - INDOMETHACIN - if inflammation is not controlled then corticosteriods are used - PREDNISONE
Chronic RA - Disease Modifying Anti Rheumatoid drugs (DMARD) (this stops the progression of the disease) |
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Term
| Name the Disease Modifying Anti Rheumatoid drugs (DMARD's) |
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Definition
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1.Chloroquine
2.D-pencillamine
3.Gold
4.Sulfasalazine
5.Infliximab - Blocks TNF- a
6.Etanercept - Blocks TNF- a
7.Anakinra - Blocks IL-1
8. immunosuppressants - anticancer drugs (methotrexate ( LOW DOSE FOR RA), cyclophosphamide)
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Term
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Definition
RA- DMARD's
1. Sulfapyridine
2. 5-Amino Salicylic Acid (5-ASA)
–Sufapyridine: is the active moiety when treating R.arthritis
–5-ASA: is the active moiety when treating Inflammatory Bowel Disease (ulcerative colitis and Chrohn’s disease)
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Term
Patient comes in with swelling, redness, pain in the joints & elevated Uric acid levels
What is the diagnosis?
What is the treatment? |
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Definition
Acute Gout
NSAID & Colchicine |
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Term
Uric acid stones in kidney
Repeated hyperuricemic levels
Diagnosis
Treatment |
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Definition
Chronic Gout
1. promote excretion of Uric acid - probinicid
2. inhibit the synthesis of uric acid - allopurinol |
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Term
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Definition
| inhibits the release of glycoproteins - which are involved in the process of inflammation and joint distraction in ACUTE gout |
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Term
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Definition
Inhibits the tubular reabsorption of uric acid, thus reducing the blood levels
Used in CHRONIC gout
Secondary hyperurecemias (cancer induced)
prolong the action of penicillin |
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Term
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Definition
Decreases the production of uric acid by inhibiting the Xanthine Oxidase enzyme (this usually converts Hypoxanthine to uric acid).
CHRONIC gout
Secondary hyperurecemias |
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