NSAIDs Flashcards

1
Q

Classify an NSAIDs

A
  1. Nonselective COX inhibitors
    a) salicylates
    b) propanoic acid derivatives
    c) fenamic acid derivatives
    d) acetic acid derivatives
    e) enolic acid derivatives
  2. Preferential COX2 inhibitors
  3. highly selective COX2 inhibitors
  4. analgesic and antipyretics with poor anti-inflammatory effect
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2
Q

Name nonselective COX inhibitors that are salicylates

A
  1. Aspirin
  2. diflunisal
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3
Q

Name nonselective COX inhibitors that are propanoic acid derivatives

A
  1. Ibuprofen
  2. naproxen
  3. ketoprofen
  4. Flurbiprofen
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4
Q

Name fenamic Acid derivatives of nonselective COX inhibitors

A
  1. Mefenamic acid
  2. Flufenamic
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5
Q

Name nonselective COX inhibitors that are ascetic acid derivatives

A
  1. Ketorolac
  2. Indomethacin
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6
Q

Name nonselective COX inhibitors that are in enolic acid derivatives

A
  1. Piroxicam
  2. Tenoxicam
  3. Lornoxicam
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7
Q

Name preferential COX2 inhibitors

A
  1. Diclofenac
  2. meloxicam
  3. Aceclofenac
  4. Nimesulide
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8
Q

Name highly selective COX2 inhibitors

A
  1. Etroicoxib
  2. Patecoxib
  3. Lumiracoxib
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9
Q

Name analgesic and antipyretic with poor anti-inflammatory effect

A
  1. Paracetamol
  2. Nefopam 
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10
Q

What is the mechanism of action of NSAIDs

A

Inhibit both COX1 and COX2 Isoforms. Thereby decreasing PGs and thromboxane synthesis.

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11
Q

All NSAIDs Cause reversible inhibition of COX enzyme except for which drug

A

Aspirin

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12
Q

Name the pharmacological action of NSAIDs

A
  1. Analgesic effect
  2. Anti-pyretic effect by inhibition of PGs in hypothonimus
  3. anti-inflammatory effect by inhibition of PG synthesis
  4. antiplatelet effect: inhibits TXA2 synthesis
  5. Acid base electrolyte balance
  6. GIT produces vomiting and Irritates gastric mucosa
  7. CVS: sodium and water retention can cause CCF and hyper tension
  8. urate excretion
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13
Q

What is the dosage of regimen of aspirin for analgesic dose

A

2 to 3 g /day in divided doses

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14
Q

What is the dosage regimen of anti-inflammatory dose of aspirin

A

4 to 6 g /day in divided doses

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15
Q

What is the dosage regimen for aspirin for antiplatelet dose

A

50 to 325 mg/day 

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16
Q

What are the adverse effects of NSAIDs

A
  1. GIT: Nausea, vomiting, dyspepsia, epigastric pain, acute gastritis, aspiration and G.I. bleeding
  2. Hypersensitivity:  skin rashes, Urticara, Rhinitis, bronchial spasm, angioneurotic edema And rarely anaphylactic reaction
  3. People with G6PD deficiency haemolytic anaemia
  4. Decreased synthesis of clotting factors, interference with vitamin K
  5. Reye’s syndrome
  6. Pregnancy: Delay onset of labour and increase chances of postpartum hemorrhage.
  7. Analgesic nephropathy
  8. Salicylism (Vertigo, tinnitus, headache, confusion, nausea, vomiting, diarrhea, sweating, electrolyte imbalance, etc.)
17
Q

What are the manifestations of acute salicylate poisoning

A
  1. Vomiting, dehydration
  2. acid base and electrolyte imbalance
  3. restlessness, confusion, convulsions
  4. cardiovascular collapse, pulmonary oedema
  5. hyperpyrexia and death
18
Q

What is the treatment of acute salicylate poisoning

A
  1. Hospitalization
  2. gastric Lavage followed by administration of active charcoal
  3. Maintain fluid and electrolyte balance. Correct acid base disturbances
  4. IV sodium bicarbonate to treat metabolic acidosis
  5. external cooling
  6. haemodialysis in severe cases
  7. vitamin K1 and blood transfusion if there is bleeding
19
Q

What are the drug interactions of NSAIDs

A
  1. NSAIDs x glucocorticoids: G.I. complications such as nausea, vomiting, dyspepsia, epigastric pain, acute gastritis, ulceration, G.I. bleeding
  2. NSAIDs x thiazides/furosemide decrease their diuretic efficacy by inhibiting PG synthesis which promote sodium and water retention
  3. NSAIDs potential the effects of oral anticoagulants, hypoglycaemic agents and methotric sa by displacing them from plasma protein binding sites
  4. NSAIDs impair clearance of lithium leading to its toxicity 
20
Q

What are the clinical uses of NSAIDs

A
  1. As an analgesic
  2. antipyretic
  3. osteoarthritis
  4. rheumatoid arthritis
  5. acute rheumatic fever
  6. thromboembolic disorders such as transit ischaemic attacks and MI
  7. others including:
    a) medical closure of patent ductus arteriosus
    b) colon and rectal cancer
    c) reduce the risk and onset of Alzheimer’s disease
    d) control radiation induced diarrhoea
    e) control pruritus and flushing
    f)useful in pre-eclampsia
21
Q

What are the actions and uses of indomethacin

A
  1. Inhibits migration of neutrophils to inflamed area
  2. is very effective in ankylosing spondylitis
  3. acute gout
  4. psoriatic arthritis
22
Q

Which drug is most useful in cancer pain

A

Ketorolac

23
Q

Which drugs inhibit the migration of leucocytes

A
  1. Naproxen
  2. Indomethacin 
24
Q

What are the uses of paracetamol

A
  1. Antipyretic
  2. an analgesic
25
Q

What are the side effects/adverse effects of paracetamol

A
  1. Skin rashes, nausea
  2. hepatotoxicity
  3. nephrotoxicity
26
Q

 What are the manifestations of acute paracetamol poisoning

A
  1. Vomiting, diarrhea, abdominal pain
  2. Hypoglycaemia
  3. hypotension 
  4. hypoprothrombinemia
  5. coma 
27
Q

What are the two major differences between nonselective COX inhibitors and selective COX2 inhibitors

A
  1. G.I. side effects are more in nonselective COX inhibitor as compared to selective COX2 inhibitors
  2. There is no platelet effect in selective COX2 inhibitors while there is anti-platelet effect in nonselective COX inhibitors
28
Q

what is the antidote for paracetamol poisoning

A

N-acetylcysteine

29
Q

 What is the treatment for paracetamol toxicity

A
  1. Is detoxified by conjugation with glutathione
  2. N-acetylcysteine oral methionine replenish glutathione stores in the liver
  3. Activated charcoal is administer to decrease the absorption of ParacetamolFrom the gut.
  4. Haemodialysis may be required in acute renal failure
30
Q

Name topical NSAIDs 

A
  1. Ibuprofen
  2. diclofenac
  3. naproxen
  4. Flurbiprofen