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Anti - Inflammatory Drugs Flashcards

1
Q

What is an example of an autacoid and what causes its release?

A

Tissue injury causes the release of autocoids. An example is prostaglandins

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2
Q

What do autacoids cause?

A

Vasodilation, increased vascular permeability, chemotaxis, pain

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3
Q

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) - Mechanism of Action

A

Also known as Cyclooxygenase Inhibitors

Inhibits cyclooxygenase (COX)

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4
Q

What is COX

A

COX is the enzyme that converts arachidonic acid into prostanoids

It induces an undesirable inflammatory effect

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5
Q

What are the 4 properties of NSAIDs

A

Analgesic
Anti-inflammatory
Antipyretic (fever reducing)
Antirheumatic (arthritis treatment)

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6
Q

NSAID - Indication

A
  • Mild to moderate pian
  • Acute gout
  • Various bone, joint, and muscle pain
  • Osteo/rheumatoid/juvenile arthritis
  • Dysmenorrhea (menstrual cramps)
  • Fever
    etc
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7
Q

What does the Antipyretic property of NSAID inhibit?

A

Prostaglandin E2 within the hypothalamus (where the temperature is controlled)

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8
Q

What is the role of Non-selective NSAIDs?

A

To inhibit COX-1 and COX-2

  • Alleviate mild to moderate pain
  • Inflammatory disorders (arthritis, bursitis)
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9
Q

Examples of Non-Selective NSAIDs

A

Acetylsalicylic acid (ASA, ASPIRIN)
Ibuprofen (Motrin, Advil)
Naproxen (Aleve)

Can be combine with mild opioids (codeine) or caffeine

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10
Q

What is the standard NSAID?

A

Acetylsalicylic acid (ASA, Aspirin)

Made in 1899

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11
Q

What are the 4 properties of ASA?

A
  1. Anti-inflammatory
    The reduction in tissue levels of prostaglandins may be responsible for ASA’s analgesic and anti-inflammatory effects.
  2. Analgesic
    “”
  3. Antipyretic
    - ASA lowers body temperature mainly through inhibition of prostaglandin E1 synthesis in the brain. Heat production is not affected but dissipation of heat is enhanced via increased blood flow through the skin and sweating.
  4. Antiplatelet
    Inhibition of thromboxane A2 synthesis which plays an essential role in platelet aggregation. ASA prevents thromboxane A2 formation by inhibiting COX. This is irreversible and lasts the lifetime of a platelet (8 days)
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12
Q

Platelet Activation Balance

A

Balance between TXA2 and PGI2

Platelets - Endothelial cells
Prothrombotic - Anti-thrombotic
TXA2 - PGI2/NO

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13
Q

ASA - Contraindications

A

Pregnancy - in late trimester connected with low weight, intracranial bleed, and even death
- Also excreted in breast milk

Influenza and chickenpox in kids/teens to avoid *Reye’s syndrome

Bleeding disorders, 1 week pre op, and in renal/hepatic dysfunction patients

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14
Q

What are the symptoms of Reye’s syndrome?

A
  • Vomiting
  • Liver damage
  • CNS problems (encephalopathy) including confusion, seizures, coma.
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15
Q

Salicylate Toxicity - Drugs and Symptoms

A

Caused by ASA, Na salicylate, Mg salicylate

Adult symptoms:
- Tinnitus and hearing loss

Children
- Hyperventilation and CNS effects

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16
Q

ASA - Interactions

A

*Increased bleeding with anticoagulants

Glucocorticoids - gastric ulcers

Non ASA NSAIDs
- Reduce antiplatelet effects of ASA

17
Q

Which drugs inhibit COX-1 and COX-2, but are reversible?

A

All non-ASA NSAIDs

18
Q

Do Non-ASA NSAIDs protect against MI and Stroke?

A

No. Only ASA does.

19
Q

Ibuprofen - Contraindications

A
  • Severe renal/hepatic dysfunction
  • Asthma
  • GI bleeding or ulcerations-
  • Bleeding disorders, hypertension
  • Breastfeeding
20
Q

Ibuprofen - Interactions

A
  • Increased bleeding with oral anticoagulants
  • Decreased effect of ASA antiplatelet
  • Increased effects of phenytoin sulfonamids (liver metabolism)
  • Increased adverse effects of lithium (reduced kidney function)
21
Q

All NSAIDs - Adverse Effects

A

Gastrointestinal

  • GI bleeding
  • Dyspepsia (indigestion) , heartburn, epigastric distress, nausea
  • Gastric ulceration (erosions)

Renal

  • Reductions in creatinine clearance (estimates GFR)
  • Acute tubular necrosis with renal failure
22
Q

NSAIDs - Contraindications

A
  • Allergy
  • Conditions with bleeding as risk (vitamin K deficiency, and peptic ulcer disease)
  • Severe renal or hepatic disease
  • Breastfeeding
23
Q

What is COX-2 responsible for?

A

Inflammatory mediators

24
Q

Example of COX-2 Inhibitor

A

Celecoxib (Celebrex)

25
Why/ why not use COX-2 Inhibitors?
Use: - Just as effective as traditional NSAIDs in pain/inflammations management - Lower risk of GI side effects Not use: - Can impair renal function, cause hypertension and edema - *Increased risk of MI and stroke
26
What can be used with NSAIDs to reduce GI ulcerations?
Misoprostol (cyotec) - It inhibits the parietal cells in the stomach from creating acid, increases stomach pH and allows ulcers to heal
27
NSAIDs - Client Implications
- Assess for GI lesions, peptic ulcer disease, or bleeding disorders - Educate about adverse effects - Watch for dark or black colour in stool - Drug interactions (alcohol, heparin, steroids etc) - Monitor therapeutic effects (decrease in swelling, pain etc)
28
What are 3 Antigout Agents and what are their functions?
1. Allopurinol (aloprin, zyloprim)- to prevent attacks (prophylactic). Reduces production of uric acid 2. Colchicine - used for acute attacks. Reduces inflammatory response to the deposits of urate crystals 3. Probenecid (sulfinpyrazone). Increased excretion of uric acid in the urine
29
What drug suppresses inflammatory associated with Rheumatoid Arthritis?
DMARDs - Disease modifying antirheumatic drugs - Slow onset of action up to several weeks * Methotrexate - Most common, can be used in combination
30
What is an example of a Non- Opioid Analgesic? What are the functions of this analgesic?
Acetaminophen - Mild-moderate analgesic and antipyretic - Little to no anti-inflammatory effects - Does not affect platelets - Antipyretic effect is caused by the inhibition of prostaglandin E2 in the temperature regulating centre of the hypothalamus - The analgesic effect is through the inhibition of prostaglandin synthetase in the CNS - Inhibits COX in CNS
31
What are the maximum dosages /day for Acetaminophen?
4000 mg per day for adult 2400 for 11-12 years - Sliding scale based on age/weight - Extreme caution in alcohol abusers
32
What are typical single tablet dosage sizes?
325, 500 and 650 mg Tylenol 1, 2, 3, 4 all have 300 mg of acetaminophen, and 8, 15, 30, 60 mg of codeine respectively
33
Acetaminophen - Contraindications
- Severe hepatic disease - Severe renal disease - Alcoholism - Drug allergy
34
Acetaminophen - Toxicity and Antidotes
Overdose - Can be intentional or chronic unintentional misuse - *Hepatic necrosis (drug-induced hepatitis) Long-term ingestion of large doses also causes nephropathy Antidote: Acetylcysteine (Mucomyst) - Max protection within 8-10 hours (IV or PO)

Pharmacology (29 decks)

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