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Pharmacology > NSAIDs > Flashcards

NSAIDs Flashcards

1
Q

Mechanism of action of NSAIDs ?

A

NSAIDs inhibit cyclo-oxygenase (COX) enzymes, decreasing production of prostaglandins, thus reducing inflammation, pain, and fever.

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2
Q

Types of COX?

A

COX-1: Constitutive (Its concentration remains stable)
 Produces prostaglandins supporting platelets and protecting stomach.
 Their reduction (as by salicylate) cause stomach ulcers and bleeding
 COX-2: Induced (only formed as inflammatory response),
 COX-3: in brain, mediate central action of prostaglandins (pain & fever
only)

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3
Q

Classification of NSAIDs according to COX selectivity ?

A 
  Nonselective COX-1,COX-2 Inhibitors:
as acetyl salicylic acid, ibuprufen, indomethacin, diclofenac
  Preferential COX-2 inhibitors:
Meloxicam
  Selective COX-2 Inhibitors:
Celecoxib, rofecoxib
  COX-3 inhibitors:
Paracetamol
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4
Q

Pharmacological actions of NSAIDs?

A

 Analgesic:
- Reduce prostaglandins at nerve endings reducing pain
 Anti-pyretic:
- Reduce prostaglandins at thermoregulatory center decreasing fever  Anti-inflammatory: (all except paracetamol)
- Reduce prostaglandins causing signs of inflammation (redness,
hotness and swelling)
partial relief in the remaining.
 Anti-platelet: (Mainly by salicylates in low dose)
- By interfering with platelet thromboxane A2 synthesis
 Dysmenorrhoea:
- NSAIDs lower uterine PG levels—afford excellent relief in 60–70% and

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5
Q

Clinical uses of NSAIDs?

A 
  Treatment of mild to moderate pain:
 Headache and migraine
 Dental pain
 Dysmenorrhea
 Arthritis and myositis
  Treatment of fever
  Treatment of inflammatory conditions, especially to decrease
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6
Q

Common side effects of NSAIDs?

A

 Gastrointestinal upset and Gastric ulceration

 Bleeding:

 Decrease renal blood flow causing sodium and water retention

 Inhibition of uterine contraction

 Asthma and anaphylaxis:

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7
Q

How can NSAIDs cause Gastrointestinal upset and Gastric ulceration? How can u counteract it?

A 
If we use NSAIDS they will inhibit COX 
= 
Reduces the mucus 
= 
Mucosal ischaemia 
= mucosal damage 
= 
GI upset and gastric ulceration
  • give PG analogues ( misoprostol ) administered concurrently with NSAIDs counteract their gastric toxicity
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8
Q

How can NSAIDs cause Bleeding ?

A 
COX-1 will help in platelet  function 
= due to inhibition of platelet thromboxane A2 synthesis
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9
Q

How can NSAIDs cause Decrease renal blood flow causing sodium and water retention?

A

COX1 helps in renal tract when it’s blocked

If someone is hypovolaemia, hepatic cirrhosis, renal disease and in patients receiving diuretics or antihypertensives

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10
Q

How can NSAIDs effect Inhibition of uterine contraction?

A

= causing delayed labor

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11
Q

How can NSAIDs cause Asthma and anaphylaxis ?

A

due to increased leukoterienes

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12
Q

General contraindications of NSAIDs?

A

 Gastric ulcer
 Patients taking anticoagulants drugs or hemophilic patients
 Renal failure
 Asthmatic patients

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13
Q

Beneficial actions due to PG

synthesis inhibition ?

A 
- Analgesia:  prevention  of  pain nerve ending sensitization 
• Antipyresis
 • Anti-inflammatory
 •Antithrombotic
•  Closure  of  ductus  arteriosus  in
newborn
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14
Q

Shared toxicities due to PG

synthesis inhibition ?

A 
• Gastric mucosal damage
• Bleeding: inhibition of platelet
function
 • Limitation of renal blood flow :
Na+ and water retention 
• Delay/prolongation of labour
 • Asthma and anaphylactoid
reactions in susceptible
individuals
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15
Q

Salicylate mechanism of action?

A
  • Non-selective irreversible COX inhibition. ( both COX 1 and 2 )
  • Antiinflammatory action is exerted at high doses
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16
Q

Pharmacokinetics of Salicylate?

A 
1. Gastric toxicity : 
Cause Salicylate is an acid
=  
will be absorbed in an acidic medium 
- but when it enters the mucosal cell ( basic ) 
= 
It ionizes 
= 
Can’t diffuse ( ion trapping) 
=
Enhance gastric toxicity
  1. Strongly bound to plasma protein
  2. Alkalinization ( basic ) of urine increase its excretion ( cause it acidic )
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17
Q

Specific uses of salicylate?

A
  1. Cardio-protective: reduces the incidence of myocardial infarction (in low dose aspirin
  2. post-infarct patients
  3. new onset’
  4. ‘sudden worsening’ angina
  5. Pregnancy-induced hypertension
  6. pre-eclampsia
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18
Q

Why is salicylate used in Pregnancy-induced hypertension and pre-eclampsia?

A 
They are caused by 
= 
imbalance between  TXA2  and  PGI2
=
When given aspirin
= 
selectively  suppressing  TXA2 production 
= 
Restore balance
19
Q

Specific side effects of salicylate?

A
  1. Effect on uric acid:
    - Small dose = inhibiting urinary secretion of uric acid = hyperuricemia
  • Large dose = due to reduced urinary re-absorption = hypouricemia
  1. Reye’s syndrome
    - In children it is used in viral (varicella,
    influenza) infection
    - Progressive damage to the liver and brain- a rare form of hepatic
    encephalopathy
20
Q

Which medication is best suitable for children?

A

paracetamol

21
Q

Toxicity of salicylate?

A
  1. Chronic toxicity (Salicylism) :
    - Due to chronic use of large dose – Antiinflammatory doses
  2. Acute salicylate intoxication :
    - Start as salicylism followed by fever and convulsions.
22
Q 
Chronic toxicity (Salicylism)
Symptoms and what happens to respiratory center.
A
  • Symptoms: headache, dizziness, tinnitus, reversible decrease of hearing and vision, vertigo and vomiting
  • dose has to be titrated to one which is just below that producing these symptoms; tinnitus is a good guide
  • Early stimulation = respiratory center cause hyperventilation and respiratory alkalosis
  • Late respiratory = accumulation of salicylate = metabolic acidosis= depression of respiratory center
23
Q

Treatment of Acute salicylate intoxication

A

 Gastric lavage and charcoal to reduce absorption
 Monitor salicylate level and correct acid-base abnormalities
 Reduce fever by ice packs
 For convulsions, give intravenous (IV) diazepam
 Forced alkaline diuresis (IV furosemide+sodium bicarbonate) increase
excretion and Hemodialysis in severe cases
 Blood transfusion and vitamin K for bleeding

24
Q

Precautions and contraindications for use salicylates (aspirin )

A
  1. People who are sensitive to it
  2. peptic ulcer, bleeding tendencies, in children suffering from chicken pox or influenza.
  3. Cautious use in chronic liver disease = hepatic necrosis have been reported.
  4. Aspirin should be stopped 1 week before elective surgery.
  5. It should be avoided by breastfeeding mothers.
  6. Avoid high doses in G-6PD deficient individuals—haemolysis can occur
25
Q

Action of

Celecoxib

A

Selective COX-2 inhibitor -10–20 times more selective for COX-2 than for COX-1. Little effect on gastric PGs

26
Q

Which is Suitable for patients with risk of gastro-intestinal bleeding
?

A

Celecoxib

Only inhibits COX-2 = only causes inflammation normally

27
Q

Which drug reduce endothelial PGI2 production (vasodilator) ?

A

Celecoxib

28
Q

Juxtaglomerular COX-2 is constitutive

A

inhibition can cause salt and
water retention; pedal edema, precipitation of CHF and rise in BP can
occur with all coxibs.

29
Q

Celecoxib main side effects?

A

 Cardiovascular side effects  Chest pain & shortness of breath

30
Q

Paracetamol (Acetaminophen)

Mechanism of action?

A

Inhibit central COX-3 inhibiting central PG synthesis. the
central component of analgesic action involve inhibition of PG synthesis in the
spinal dorsal horn neurones as well as in brain.

31
Q

Pharmacological actions of paracetamol ?

A
  • Analgesic/antipyretic effects
  • No anti-inflammatory effect
    because of its inability to inhibit COX in the presence of peroxides which are generated at sites of inflammation
32
Q

Adverse effects of paracetamol?

A
  • No gastric erosion, effect on platelet aggregation, or uric acid - - only allergy
  • increase hepatic enzymes (well tolerated)
33
Q

Overdosage of paracetamol? Treated by ?

A 
- Over dosage (15 g) 
= 
 fatal hepatotoxicity 
\+  renal tubular necrosis by (NAPQI) 
= 
 this metabolite binds covalently to proteins
=
Nausea, vomiting, abdominal pain and bleeding
  • Treated by:
    1. Gastric lavage
    2. Liver support (N-acetyl cysteine to restore liver glutathione which detoxifies NAPQI)
34
Q

Patient with Mild-to-moderate pain with little inflammation what drug do you give him?

A
  1. paracetamol

2. low-dose ibuprofen.

35
Q

Patient with Acute musculoskeletal which drug to give?

A

paracetamol, ibuprofen or diclofenac.

36
Q

Patient with osteoarthritic which drug to give?

A

paracetamol, ibuprofen or diclofenac.

37
Q

Patient with osteoarthritic injury associated pain which drug to give?

A

paracetamol, ibuprofen or diclofenac.

38
Q

Patient who has Gastric intolerance to traditional NSAIDs?

A
  1. selective COX-2 inhibitor
    (Celecoxib, rofecoxib)
  2. paracetamol.
39
Q

Patient who has Patients with history of asthma?

A

Selective COX-2 inhibitor

Celecoxib, rofecoxib

40
Q

Patients with anaphylactoid reaction to aspirin/other

NSAIDs

A

Selective COX-2 inhibitor

Celecoxib, rofecoxib

41
Q

Patients with hypertension or other risk factor for heart attack/stroke give?

A

ibuprofen or aspirin may be used at the lowest

dose for the shortest period.

42
Q

Patients with hypertension or other risk factor for heart attack/stroke avoid?

A

selective COX-2 inhibitor

43
Q

selective COX-2 inhibitor give?

A

only paracetamol, ibuprofen

44
Q

A pregnant patient give which drug?

A

paracetamol is the safest; lowdose aspirin is probably the second best.

Pharmacology (4 decks)

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