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Phase 1b - Pharmacology & Therapeutics > Pharmacology of Gastro-Oesophageal Reflux Disease (GORD) / Peptic Ulcer Disease > Flashcards

Pharmacology of Gastro-Oesophageal Reflux Disease (GORD) / Peptic Ulcer Disease Flashcards

Non-steroidal anti-inflammatory drugs (NSAIDs) Proton pump inhibitors (PPIs) Histamine (H2) receptor antagonists Acetaminophen

1
Q

What are non-steroidal anti-inflammatory drugs (NSAIDs) used for?

A

Used as:

  • Analgesics for relief of mild to moderate pain
  • Antipyretics to reduce fever
  • Anti-inflammatory for chronic control fo inflammatory disease

An NSAID is used to treat:

  • Rheumatoid arthritis
  • Osteoarthritis
  • Ankylosing spondylitis
  • Polyarticular juvenile idiopathic arthritis
  • Tendinitis
  • Bursitis
  • Acute gout
  • Primary dysmenorrhea
  • Mild to moderate pain
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2
Q

What is the primary drug target of non-steroidal anti-inflammatory drugs (NSAIDs)?

A
  • Cyclo-oxygenase (COX) enzyme
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3
Q

What is the drug target type of non-steroidal anti-inflammatory drugs (NSAIDs)?

A
  • Enzyme inhibitor
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4
Q

What are the locations of action of non-steroidal anti-inflammatory drugs (NSAIDs)?

A
  • Nerve endings (COX-2)
  • Intestinal mucosa (COX-1)
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5
Q

What is the mechanism of action of non-steroidal anti-inflammatory drugs (NSAIDs)?

A
  • NSAIDs are non-selective COX inhibitor
  • Inhibits the activity of COX-1 & COX-2
  • Inhibition of COX-1 is thought to cause some of the side effects of NSAIDs
  • Inhibition of COX-2 decreases the synthesis of prostaglandins
  • Inhibition of the pain, fever, swelling and inflammation
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7
Q

What are the main adverse effects of non-steroidal anti-inflammatory drugs (NSAIDs) (10)?

A
  • Common:
    • Gastric irritation
    • Ulceration
    • Bleeding
  • Rare:
    • Perforation
    • Reduced creatine clearance
    • Allergies
    • Possible nephritis
    • Bronchocostriction
    • Skin vasles
    • Dizziness
    • Tinnitus
  • Cardiovascular effects (may occur after prolonged use or in patients with pre-existing CV risk):
    • Hypertension
    • Stroke
    • MI
  • Chronic renal failure (associated with prolonged analgesic abuse)
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8
Q

Give 4 examples of non-steroidal anti-inflammatory drugs (NSAIDs).

A
  • Ibuprofen
  • Diclofenac
  • Naproxen
  • Aspirin
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9
Q

What is the main adverse effect of aspirin (special non-steroidal anti-inflammatory drugs (NSAIDs))?

A
  • Rare but serious post-viral encephalitis in children
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10
Q

What is the main action of aspirin different from the rest of non-steroidal anti-inflammatory drugs (NSAIDs)?

A
  • Anti-aggregatory agent to inhibit platelet aggregation in patients who are at risk of stroke or MI
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11
Q

What is the action of the cyclo-oxygenase (COX) enzyme?

A
  • Production of prostanoids (prostaglandins & thromboxanes) from the parent arachidonic acid
    • Prostanoids act through a large number of prostanoid receptors to produce a highly complex array of actions
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12
Q

What are proton pump inhibitors (PPIs) used for?

A

Proton pump inhibitors are used to:

  • Help gastrointestinal ulcers heal
  • Treat symptoms of gastroesophageal reflux disease (GERD)
  • Eradicate Helicobacter pylori
  • Treat hypersecretory conditions such as Zollinger-Ellison Syndrome
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13
Q

What is the primary drug target of proton pump inhibitors (PPIs)?

A
  • H+/K+ ATPase (Proton pump)
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14
Q

What is the drug target type of proton pump inhibitors (PPIs)?

A
  • Ion channel antagonist
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15
Q

What is the mechanism of action of proton pump inhibitors (PPIs)?

A
  • Weak bases that accumulate in the acid environment of the canaliculi of the pariteal cells
  • This concentrates their action there and prolongs their duration of action
  • Inhibit basal and stimulated gastric acid secretion by >90%
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16
Q

What is the location of action of proton pump inhibitors (PPIs)?

A
  • Gastric parietal cells
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18
Q

What are the main adverse effects of proton pump inhibitors (PPIs) (7)?

A
  • Uncommon:
    • Headache
    • Diarrhoea
    • Bloating
    • Abdominal pain
    • Rashes
  • Omeprazole is an inhibitor of cytochrome P2C19 and has been reported to reduce the activity of other drugs
  • PPIs may mask the symptoms of gastric cancer
19
Q

Give 2 examples of proton pump inhibitors (PPIs).

A
  • Omeprazole
  • Lansoprazole
20
Q

Why are proton pump inhibitors (PPIs) generally administered orally as capsules containing enteric-coated granules?

A
  • PPIs are pro-drugs which, at low pH, are converted into 2 reactive species which react with sulphydryl groups in the H+/K+ ATPase responsible for transporting H+ ions out of the parietal cells, however they degrade rapidly at low pH.
21
Q

What are histamine (H2) receptor antagonists used for?

A
  • Histamine (H2) antagonists are used to treat duodenal ulcers, Zollinger-Ellison syndrome, gastric ulcers, GERD, and erosive esophagitis
22
Q

What is the primary drug target of histamine (H2​) receptor antagonists?

A
  • Histamine (H2​) receptor
23
Q

What is the mechanism of action of histamine (H2​) receptor antagonists?

A
  • Histamine (H2​) receptor antagonists inhibit histamine (H2​) receptors in the gastric parietal cells of the stomach
  • Gastrin does not bind on the histamine (H2​) receptor reducing the gastric acid secretion by approximately 60%
24
Q

What is the drug target type of histamine (H2​) receptor antagonists?

A
  • Receptor antagonist
25
Q

What is the location of action of histamine (H2​) receptor antagonists?

A
  • ECL cells on the gastric parietal cells
27
Q

What are the main adverse effects of histamine (H2​) receptor antagonists (3)?

A
  • ​Diarrhoea
  • Dizziness
  • Muscle pains
28
Q

What are the cimetidine specific adverse effects?

A
  • Inhibits cytochrome P450 and may retard the metabolism and potentiate the effects of a range of drugs (incl. oral anticoagulants & TCAs)
29
Q

Give 2 examples of histamine (H2) receptor antagonists.

A
  • Ranitidine
  • Cimetidine
30
Q

What is acetaminophen used for?

A
  • Acetaminophen is an analgesic drug used alone or in combination with opioids for pain management (including GORD / Peptic Ulcer Disease), and as an antipyretic agent
    • Not an NSAID → little anti-inflammatory activity
31
Q

What is the primary drug target of acetaminophen?

A
  • Not well defined. Possible targets:
    • COX-3 isoform
    • Cannabinoid receptors
    • Endogenois opioids
    • 5HT3 receptors
32
Q

What is the drug target type of acetaminophen?

A
  • Probably inhibitor / antagonist
33
Q

What is the location of action of acetaminophen?

A
  • Peripheral & Central Nervous System
34
Q

What is the mechanism of action of acetaminophen?

A
  • Unknown
35
Q

What are the main adverse effects of acetaminophen (2)?

A
  • Rare: Allergic skin reaction
  • In case of overdose: Hepatotoxicity
36
Q

Give 1 example of acetaminophen.

A
  • Paracetamol
37
Q

What are the symptoms of of paracetamol overdose (common method of suicide) (3)?

A
  • Nausea
  • Vomiting
  • Onset of right subcostal pain after 24 hours indicate hepatic necrosis
38
Q

How is paracetamol overdose (common method of suicide) managed?

A
  • < 8 hours: Activated charcoal + Acetylsteine + Antiemetic
  • 8 - 24 hours: Acetylsteine + Antiemetic
  • > 24 hours: Acetylsteine + Antiemetic

Phase 1b - Pharmacology & Therapeutics (12 decks)

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