Antihistamines and NSAIDs

Question 1

Cetirizine

Answer 1

• H1 antihist – 2nd generation
• Block histamine at H1 receptors – highly selective
• Allergic rhinitis

Question 2

Cyclizine

Answer 2

• H1 antihist – 1st generation
• Block histamine at H1 receptors and antimuscarinic
• Sedation, dry mouth, urine retention, tachycardia
• Motion sickness

Question 3

Dimenhydrinate

Answer 3

• H1 antihist – 1st generation
• Block histamine at H1 receptors and antimuscarinic (for motion sickness)
• Sedation, dry mouth, urine retention, tachycardia, local anesthesia
• Motion sickness, allergic rhinitis

Question 4

Fexofenadine

Answer 4

• H1 antihist – 2nd generation
• Block histamine at H1 receptors – highly selective
• Allergic rhinitis

Question 5

Loratadine

Answer 5

• H1 antihist– 2nd generation
• Block histamine at H1 receptors – highly selective
• Allergic rhinitis

Question 6

Promethazine

Answer 6

• H1 antihist – 1st generation
• Block histamine at H1 receptors and antimuscarinic (for motion sickness)
• Sedation, dry mouth, urinary retention, tachycardia, local anesthesia
• Motion sickness

Question 7

Adalimumab

Answer 7

• Anti-TNFa agents
• Humanized antibody binds to TNFa – prevents interaction with receptor and reduces circulating levels
• Increased infections (URI, urinary)
• Parenteral only – rheumatoid arthritis and Crohn’s disease

Question 8

Etanercept

Answer 8

• Anti-TNFa agents
• Fusion protein containing ligand binding domain of TNFa receptor and Fc domain of human IgG
• Increased infections (URI, urinary)
• Parenteral only – rheumatoid arthritis and Crohn’s disease

Question 9

Infliximab

Answer 9

• Anti-TNFa agents
• Humanized antibody binds to TNFa – prevents interaction with receptor and reduces circulating levels
• Increased infections (URI, urinary)
• Parenteral only – rheumatoid arthritis and Crohn’s disease

Question 10

Anakinra

Answer 10

• Anti-IL1 agents
• Competitive IL-1 receptor antagonist
• Increased infections
• Rheumatoid arthritis (short ½ life, daily injection)

Question 11

Tofacitnib

Answer 11

• Jak kinase inhibitors
• Inhibits all activities of cytokines for adaptive immunity and many inflammatory cytokines (doesn’t inhibit TNFa or IL-1)
• Anemia, neutropenia, myelosuppression, increased infection (herpes zoster)
• Rheumatoid arthritis (oral – 5mg bid)

Question 12

Aspirin

Answer 12

• Nonselective COX inhibitors
• Irreversible – selectivity 4.4
• Increased bleeding, gastric ulcers, salicylism, Reye’s syndrome, dyspepsia, renal issues
• OTC analgesic, antipyretic, cardiovascular prophylaxis, anti-inflammatory

Question 13

Diclofenac

Answer 13

• Nonselective COX inhibitors
• Selectivity 0.3
• Increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events
• Rx arthritis/anti-inflammatory

Question 14

Diclofenac w/ misoprostol

Answer 14

• Nonselective COX inhibitors
• Selectivity 0.3 – protects against COX1 inhibition to reduce ulcers
• Increased bleeding, dyspepsia, renal issues, CV events
• Rx arthritis/anti-inflammatory

Question 15

Ibuprofen

Answer 15

• Nonselective COX inhibitors
• Selectivity – 2.6
• Increased bleeding, gastric ulcers. dyspepsia, renal issues, CV events
• OTC analgesic, antipyretic, anti-inflammatory

Question 16

Indomethacin

Answer 16

• Nonselective COX inhibitors
• Selectivity – 10
• High intolerance - increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events
• High intolerance - increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events
• Rx arthritis/anti-inflammatory

Question 17

Ketorolac

Answer 17

• Nonselective COX inhibitors
• Selectivity – 395
• Increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events
• Post-surgical analgesic

Question 18

Naproxen

Answer 18

• Nonselective COX inhibitors
• Selectivity – 3.8
• Increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events
• OTC analgesic, antipyretic, Rx anti-inflammatory

Question 19

Acetaminophen

Answer 19

• Nonselective COX inhibitors
• Activity is reduced in presence of peroxides
• Well tolerated – hepatotoxicity with overdose
• Analgesic and antipyretic effects (not anti-inflamm)

Question 20

Celecoxib

Answer 20

• COX-2 selective inhibitors
• 10-20 times more selective – for chronic NSAID users – reduced GI effects
• Renal toxicity, increased risk of cardiovascular events
• Anti-inflammatory, antipyretic, analgesic – osteoarthritis and rheumatoid

Question 21

Rofecoxib

Answer 21

• COX-2 selective inhibitors
• 200 times more selective – for chronic NSAID users – reduced GI effects
• Renal toxicity, increased risk of cardiovascular events – removed from market
• Anti-inflammatory, antipyretic, analgesic – osteoarthritis and rheumatoid