Autacoids Flashcards
________ are chemical mediators that are synthesized and fusion in a localized tissue or area, and participate in the physiologic or pathophysiologic response to injury
Autacoids
What are the groups of allergy drugs?
Antihistamines (H1)
Leukotiriene inhibitors
Janus kinase inhibitors
What two groups to the behavior modifying drugs fall into ?
Serotonin (5-HT) altering
Tricyclic antidepressants
Histamine is synthesized form?
Dietary histidine
Where is histamine stored int he body ?
Tissue - lung, skin, stomach
Cellular - mast cells and basophils
What are triggers for histamine release?
Immune-mediated (degraulation of mast cells/basophils)
Drug-induced (hypersensitivity )
Plant/animal stings
Physical injury (disrupt mast cells)
What are the histamine receptors
Type 1- Gq coupled
Type 2- Gs coupled
Type 3- presynaptic neuron
Type 4 - inflammatory cells
What type of reaction are type 1 histamine receptors involved in?
Gq coupled -> Ca and protein kinase C
Contraction of smooth muscle
Increase bronchial secretion
Inflammation
Relax vascular smooth muscle
Increase capillary permeability
Pruritus
What type of reaction are type 2 histamine receptors involved in?
Gas-coupled -> adenylyl cyclase -> increase cAMP
Relaxation of vascular smooth muscle and increased gastric acid secretion
What are targets for antihistamine drugs?
Prevent release from mast cells
- glucocorticoids
- chromolyn sodium
Histamine antagonist
-catecholamines physiologically antagonize effects
Block histamine receptors
Type 1 receptor antagonist will have what effects?
Relax bronchiolar and intestinal smooth muscle
Inhibit vasodilation by histamine
Inhibit pruritus (local anesthesia and reduce sensation)
What is a common side effect, especially by 1st generation, antihistamines?
Sedation
How are Type 1 receptor antagonists administered and metabolized?
Orally - well distributed
Metabolized by P450
How are type 1 receptor antagonists excreted?
First gen -> kidney
Second gen -> feces
What are the adverse effects of type 1 receptor antagonists?
CNS depression Antimuscarinic signs (dry mouth and increased IOP)
Drug tolerance
Rarely hypersensitivity
What are the first gen type 1 receptor antagonists?
Diphenhydramine
Hydroxyzine
Trimeprazine
Ketotifen -ophthalmic
What are the second gen type 1 receptor antagonists?
Loratadine (human, little info in vet patients)
Most well tolerated
What is the primary use of type 2 receptor antagonists?
Treat/prevent gastric ulcers and gastritis associated with hyperacidity