DRUGS and RECEPTORS Flashcards
Cromoglycate
aka. Cromolyn
- Mast cell stabilizer
Diphenhydramine
aka. Benadryl
- H1 antihistamine
- first generation
- crosses BBB and causes sedation
Cimetidine
aka. Tagamet
- H2-histamine antagonist
Epinephrine
-functional antagonist to allergic responses
H1
- neurons, smooth muscle, endothelial and epithelial cells
- increase free intracellular Ca2+
- increase capillary permeability, itching and pain
H2
- neurons, parietal cells, heart, endothelial and epithelial cells
- increase cAMP
- increase gastric acid secretion
Chlorpheniramine
aka. Chlor-Trimeton
- H1 antihistamine
- first generation
- crosses BBB and causes sedation
Chlorpheniramine
aka. Chlor-Trimeton
- H1 antihistamine
- first generation
- crosses BBB and causes sedation
Pyrilamine
aka. Histavet-P
- H1 antihistamine
- first generation
- crosses BBB and causes sedation
Pyrilamine
aka. Histavet-P
- H1 antihistamine
- first generation
- crosses BBB and causes sedation
Meclizine
aka. Bonine
- H1 antihistamine
- first generation
- crosses BBB and causes sedation
Meclizine
aka. Bonine
- H1 antihistamine
- first generation
- crosses BBB and causes sedation
Cetirizine
aka. Zyrtec
- H1 antihistamine
- second generation
- doesn’t cause drowsiness
- active metabolite of hydroxyzine
Cetirizine
aka. Zyrtec
- H1 antihistamine
- second generation
- doesn’t cause drowsiness
- active metabolite of hydroxyzine
Loratidine
aka. Claritin
- H1 antihistamine
- second generation
- doesn’t cause drowsiness
- may alleviate some types of pain
Loratidine
aka. Claritin
- H1 antihistamine
- second generation
- doesn’t cause drowsiness
- may alleviate some types of pain
Fexofenadine
aka. Allegra
- H1 antihistamine
- second generation
- doesn’t cause drowsiness
Fexofenadine
aka. Allegra
- H1 antihistamine
- second generation
- doesn’t cause drowsiness
H1-HR Antagonists
-rapid PO administration
-extensively bound to PP
-undergo extensive hepatic biotransformation
-excretion in urine or bile
-act as competitive antagonists
-decrease allergic actions of histamine, sedation, anti-emetic effects, anti-pruritic
-Side effects: muscarinic cholinergic–> xerostomia, urine retention, sinus tachycardia
Alpha-adrenergic –> hypotention –> reflex tachycardia
-high therapeutic index
-can produce vomiting, lethargy, ataxia, hyper excitability, seizures
H1-HR Antagonists
-rapid PO administration
-extensively bound to PP
-undergo extensive hepatic biotransformation
-excretion in urine or bile
-act as competitive antagonists
-decrease allergic actions of histamine, sedation, anti-emetic effects, anti-pruritic
-Side effects: muscarinic cholinergic–> xerostomia, urine retention, sinus tachycardia
Alpha-adrenergic –> hypotention –> reflex tachycardia
-high therapeutic index
-can produce vomiting, lethargy, ataxia, hyper excitability, seizures
COX-1
- ubiquitous expression
- maintenance of cellular function
COX-1
- ubiquitous expression
- maintenance of cellular function
COX-2
- macrophages, vascular endothelium, fibroblasts, mesangial cells, chondrocytes
- induced expression after LPS, IL-1, mitogens, activation of NF-kB
- Inflammation, pain and fever, but also cell regeneration and tissue repair
- more flexible binding pocket
COX-2
- macrophages, vascular endothelium, fibroblasts, mesangial cells, chondrocytes
- induced expression after LPS, IL-1, mitogens, activation of NF-kB
- Inflammation, pain and fever, but also cell regeneration and tissue repair
- more flexible binding pocket