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NSAID's
Pharm I - Block 3
26
Pharmacology
Not Applicable
07/16/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
What is the MOA of NSAID's?
Definition
Inhibits Cycloxegenase (COX) synthesis thus in turn inhibiting production of prostaglandins.. results in reduction of inflammation
Term
Name the NSAIDS
Definition

•Aspirin
•Naproxen
•Diclofenac sodium 
•Ibuprofen, Indomethacin
•Acetaminophen (Paracetomol)
•Ketorolac, Nabumatone, Diflunisal
•Celecoxib ,Etoricoxib, Valdecoxib

Term
Name the NSAID which has a poor anti-inflammatory but strong analgesic action
Definition

Potent Analgesic but poor anti inflammatory Drugs

  Ex: Acetaminophen ( Paracetamol), Ketorolac

Term

What are the outcomes of COX 1 activation

 

What ADR is associated wit its inhibition?

Definition

GI - cyto protection

Platelet aggregation

 

GI ulcers

Term
What are the out comes of COX 2 activation
Definition

Inflammation

Pain

Fever

Term
What are the 2 types of NSAID's
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

Term
What is the specific MOA of Aspirin?
Definition

Non selective IRREVERSIBLE COX inhibitor

 

All the other NSAID's are reversible

Term
What are the Drug interactions associated with NSAID's?
Definition
NSAID's is highly protein boud
Term
What are the ADR's of NSAID's?
Definition

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)

 

Term
Which is the only NSAID with an antiplatelet action & why
Definition
ASPRIN - due to the irreversible inhibition of COX via acetylation
Term
When is ASPIRIN the DOC?
Definition

1. In acute reuhmatic fever very HIGH dose

 

2. Anti platelet drug - transient ischemic attack (TIA) or MI - very LOW dose

Term
What are the ADR's of ASPIRIN?
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

Term

What NSAID causes acute poisoning?

How is it treated?

Definition

Aspirin

 

External cooling by tepid sponging, IV

fluids, NaHCO3 (sodium bicarbonate),gastric lavage, forced alkaline diuresis and haemodialysis

Term

When is Indomethacin the DOC?

What are the ADR's

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

Term
When is Ketorolac used & why?
Definition
Post opp pain (mild) as it is a poor anti-inflammatory but a very good analgesic
Term

COXIB's

Drugs?

MOA

Use?

ADR?

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)

Term

Acetominophen (paracetamol)

MOA?

Use?

ADR

Definition

Blocks COX 3 better than COX 1 & 2

 

Fever & non inflammatory pain - tooth ache, headach etc.

 

Hepatotoxicity & acute tubular necrosis.

Term

What is responsible for the hepatotoxicity seen with Acetominophen/ Paracetamol?

How is it treated?

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.

Term
What drugs are used in treating RA?
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)

Term
Name the Disease Modifying Anti Rheumatoid drugs (DMARD's)
Definition

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)

 

Term

Sulfasalazine

Use

MOA?

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)

Term

Patient comes in with swelling, redness, pain in the joints & elevated Uric acid levels

What is the diagnosis?

What is the treatment?

Definition

Acute Gout

 

NSAID & Colchicine

Term

Uric acid stones in kidney

Repeated hyperuricemic levels

 

Diagnosis

Treatment

Definition

Chronic Gout

 

1. promote excretion of Uric acid - probinicid

 

2. inhibit the synthesis of uric acid - allopurinol

Term

Colchicine

MOA

Use

Definition
inhibits the release of glycoproteins - which are involved in the process of inflammation and joint distraction in ACUTE gout
Term

Probinicid

MOA

Use?

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

Term

Allopurinol

MOA

Use?

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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