Antihistamines and NSAIDs

Question 1

Histamine is a mediator of _______ associated with _____ responses.

Answer 1

inflammation, allergic

Question 2

Histamine is mostly released from which cell, In response to what?

Answer 2

• Mast Cells

- Released in response to IgE antibodies bound to an antigen (aka allergen)

Question 3

Histamine acts on what receptors and where?

Answer 3

• H1 (Histamine 1) Receptors

- In the Central Nervous System

Question 4

Histamine is involved in promoting states of _______.

Histamine is involved in promoting ______ in response to motion.

Answer 4

• wakefulness

- nausea

Question 5

Diphenhydramine

1) Mechanism of Action
2) Use
3) Adverse Effects

Answer 5

1) 1st Generation Anti-histamine:Blocks H1 Receptors in the CNS (can block other receptors such as Muscarinic receptors)
2) OTC drug for allergies such as rhinitis (nasal congestion) and urticaria (hives)
3) Sedation(CNS effects), Anti-muscarinic effects(dry mouth, tachycardia, urinary retention, blurred vision)

Question 6

Dimenhydrinate

1) Mechanism of Action
2) Use
3) Adverse Effects

Answer 6

1) Blocks H1 Receptors in the CNS
2) Motion sickness/Nausea
3) Sedation(CNS effects), Anti-muscarinic effects(dry mouth, tachycardia, urinary retention, blurred vision)
* Less sedation than Diphenhydramine

Question 7

Loratadine

1) Mechanism of Action
2) Use

Answer 7

1) 2nd Generation Anti-histamine: Blocks H1 Receptors in the periphery
* Less CNS effects *Less interaction w/other receptors
2) OTC drug for allergies

Question 8

Prostaglandins are converted from Arachadonic Acid by what enzyme?

Answer 8

Cyclooxygenase (COX-1 and/or COX-2)

Question 9

Prostaglandins are produced in response to what?

Answer 9

Inflammatory stimuli like cytokines, antibody/antigen complexes, tissue damage

Question 10

What drugs can be used to inhibit Prostaglandin formation?

Answer 10

Glucocorticoids

NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)

Question 11

Is COX-1 or COX-2 more responsible for prostaglandin production?

Answer 11

COX-2 is responsible for production of most prostaglandins involved in inflammation

Question 12

Indomethacin

1) Mechanism if Action
2) Use
3) Adverse Effect

Answer 12

1) NSAID-Least Selective COX inhibitor
2) Arthritis
3) High Frequency of Intolerance (GI Disturbances)

Question 13

Aspirin

1) Mechanism if Action
2) Use

Answer 13

1) NSAID- IRREVERSIBLY inhibits COX-1 and COX-2
* Inhibits COX-1 for entire life of the platelet, therefore inhibiting Thromboxane (TXA2)
2) Cardiovascular Protection

Question 14

Naproxen

1)Mechanism of Action

Answer 14

1)NSAID- Non-selective COX-1 and COX-2 inhibitor

Question 15

Ibuprofen

1)Mechanism of Action

Answer 15

1)NSAID- Non-selective COX-1 and COX-2 inhibitor

Question 16

Meloxicam

1) Mechanism of Action
2) Use

Answer 16

1) NSAID- More selective for COX-2

2) Chronic Arthritis (Less GI Disturbances b/c less COX-1 inhibition)

Question 17

What the general adverse effects of NSAIDs?

Answer 17

Abdominal pain d/t GI ulceration, Increased Bleeding time, Reduced Kidney Function (reduced renal blood flow)
Contraindicated in Asthmatics

Question 18

Celecoxib

1) Mechanism of Action
2) Use
3) Adverse Effects

Answer 18

1) NSAID-ONLY COX-2 inhibitor
2) Chronic NSAID users unable to tolerate GI disturbances of other NSAIDs (like RA patients)
3) Heart Attack and Stroke d/t imbalance in Prostacyclin and Thromboxane, Reduced Kidney function (reduced renal blood flow)

Question 19

What happens if one takes aspirin and ibuprofen together?

Answer 19

Ibuprofen will decrease the effectiveness of aspirin by antagonizing aspirin’s IRREVERSIBLE features.

Question 20

Acetaminophen

1) Mechanism of Action
2) Use
3) Adverse Effects

Answer 20

1) Non-Selective Non-Anti-inflammatory COX-1 and COX-2 inhibitor
* Peroxides produced at sites of inflammation reduce acetaminophen activity-hence not used for inflammation
2) Pain, Fever
3) Liver Toxicity