Antihistamines and NSAIDs Flashcards
Histamine is a mediator of _______ associated with _____ responses.
inflammation, allergic
Histamine is mostly released from which cell, In response to what?
- Mast Cells
- Released in response to IgE antibodies bound to an antigen (aka allergen)
Histamine acts on what receptors and where?
- H1 (Histamine 1) Receptors
- In the Central Nervous System
Histamine is involved in promoting states of _______.
Histamine is involved in promoting ______ in response to motion.
- wakefulness
- nausea
Diphenhydramine
1) Mechanism of Action
2) Use
3) Adverse Effects
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)
Dimenhydrinate
1) Mechanism of Action
2) Use
3) Adverse Effects
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
Loratadine
1) Mechanism of Action
2) Use
1) 2nd Generation Anti-histamine: Blocks H1 Receptors in the periphery
* Less CNS effects *Less interaction w/other receptors
2) OTC drug for allergies
Prostaglandins are converted from Arachadonic Acid by what enzyme?
Cyclooxygenase (COX-1 and/or COX-2)
Prostaglandins are produced in response to what?
Inflammatory stimuli like cytokines, antibody/antigen complexes, tissue damage
What drugs can be used to inhibit Prostaglandin formation?
Glucocorticoids
NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)
Is COX-1 or COX-2 more responsible for prostaglandin production?
COX-2 is responsible for production of most prostaglandins involved in inflammation
Indomethacin
1) Mechanism if Action
2) Use
3) Adverse Effect
1) NSAID-Least Selective COX inhibitor
2) Arthritis
3) High Frequency of Intolerance (GI Disturbances)
Aspirin
1) Mechanism if Action
2) Use
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
Naproxen
1)Mechanism of Action
1)NSAID- Non-selective COX-1 and COX-2 inhibitor
Ibuprofen
1)Mechanism of Action
1)NSAID- Non-selective COX-1 and COX-2 inhibitor
Meloxicam
1) Mechanism of Action
2) Use
1) NSAID- More selective for COX-2
2) Chronic Arthritis (Less GI Disturbances b/c less COX-1 inhibition)
What the general adverse effects of NSAIDs?
Abdominal pain d/t GI ulceration, Increased Bleeding time, Reduced Kidney Function (reduced renal blood flow)
Contraindicated in Asthmatics
Celecoxib
1) Mechanism of Action
2) Use
3) Adverse Effects
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)
What happens if one takes aspirin and ibuprofen together?
Ibuprofen will decrease the effectiveness of aspirin by antagonizing aspirin’s IRREVERSIBLE features.
Acetaminophen
1) Mechanism of Action
2) Use
3) Adverse Effects
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
