DRUGS and RECEPTORS Flashcards

1
Q

Cromoglycate

A

aka. Cromolyn

- Mast cell stabilizer

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2
Q

Diphenhydramine

A

aka. Benadryl
- H1 antihistamine
- first generation
- crosses BBB and causes sedation

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3
Q

Cimetidine

A

aka. Tagamet

- H2-histamine antagonist

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4
Q

Epinephrine

A

-functional antagonist to allergic responses

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5
Q

H1

A
  • neurons, smooth muscle, endothelial and epithelial cells
  • increase free intracellular Ca2+
  • increase capillary permeability, itching and pain
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6
Q

H2

A
  • neurons, parietal cells, heart, endothelial and epithelial cells
  • increase cAMP
  • increase gastric acid secretion
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7
Q

Chlorpheniramine

A

aka. Chlor-Trimeton
- H1 antihistamine
- first generation
- crosses BBB and causes sedation

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7
Q

Chlorpheniramine

A

aka. Chlor-Trimeton
- H1 antihistamine
- first generation
- crosses BBB and causes sedation

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8
Q

Pyrilamine

A

aka. Histavet-P
- H1 antihistamine
- first generation
- crosses BBB and causes sedation

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8
Q

Pyrilamine

A

aka. Histavet-P
- H1 antihistamine
- first generation
- crosses BBB and causes sedation

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9
Q

Meclizine

A

aka. Bonine
- H1 antihistamine
- first generation
- crosses BBB and causes sedation

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9
Q

Meclizine

A

aka. Bonine
- H1 antihistamine
- first generation
- crosses BBB and causes sedation

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10
Q

Cetirizine

A

aka. Zyrtec
- H1 antihistamine
- second generation
- doesn’t cause drowsiness
- active metabolite of hydroxyzine

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10
Q

Cetirizine

A

aka. Zyrtec
- H1 antihistamine
- second generation
- doesn’t cause drowsiness
- active metabolite of hydroxyzine

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11
Q

Loratidine

A

aka. Claritin
- H1 antihistamine
- second generation
- doesn’t cause drowsiness
- may alleviate some types of pain

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11
Q

Loratidine

A

aka. Claritin
- H1 antihistamine
- second generation
- doesn’t cause drowsiness
- may alleviate some types of pain

12
Q

Fexofenadine

A

aka. Allegra
- H1 antihistamine
- second generation
- doesn’t cause drowsiness

12
Q

Fexofenadine

A

aka. Allegra
- H1 antihistamine
- second generation
- doesn’t cause drowsiness

13
Q

H1-HR Antagonists

A

-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

13
Q

H1-HR Antagonists

A

-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

14
Q

COX-1

A
  • ubiquitous expression

- maintenance of cellular function

14
Q

COX-1

A
  • ubiquitous expression

- maintenance of cellular function

15
Q

COX-2

A
  • 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
15
Q

COX-2

A
  • 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
16
Misoprostil
aka. Cytotec - increase mucosal cytoprotection - used for GI ulcers - PGE derivative
16
Misoprostil
aka. Cytotec - increase mucosal cytoprotection - used for GI ulcers - PGE derivative
17
Cloprostenol
aka. Estrumate | - sythetic PGF2 derivative
17
Cloprostenol
aka. Estrumate | - sythetic PGF2 derivative
18
Dinoprost
aka. Lutalyse | - sythetic PGF2 derivative
18
Dinoprost
aka. Lutalyse | - sythetic PGF2 derivative
19
Travoprost
aka. Travatan | sythetic PGF2 derivative applied to eye
19
Travoprost
aka. Travatan | sythetic PGF2 derivative applied to eye
20
Latanoprost
aka. Xalatan | sythetic PGF2 derivative applied to eye
20
Latanoprost
aka. Xalatan | sythetic PGF2 derivative applied to eye
21
NSAIDs
-Inhibit prostanoid formation (COX-1 vs. COX-2) and 5-lipoxygenase activity Beneficial: reduce inflammation, relief of stomach pain, decrease body temp. Adverse: gastropathy, clotting alterations, nephropathy, hepatotoxicity, etc -weak acids, low Vd, high PP binding -hepatic metabolism w/ excretion in bile -inhibition of NK-kB, free radicals and decreased neutrophil adherance and activation
21
NSAIDs
-Inhibit prostanoid formation (COX-1 vs. COX-2) and 5-lipoxygenase activity Beneficial: reduce inflammation, relief of stomach pain, decrease body temp. Adverse: gastropathy, clotting alterations, nephropathy, hepatotoxicity, etc -weak acids, low Vd, high PP binding -hepatic metabolism w/ excretion in bile -inhibition of NK-kB, free radicals and decreased neutrophil adherance and activation
22
Tepoxalin
- "Dual inhibitor" of COX-1+2 and 5-LOX - excellent antiinflammatory activity w/ less gastropathic effects - reduces formation of LTB4
22
Tepoxalin
- "Dual inhibitor" of COX-1+2 and 5-LOX - excellent antiinflammatory activity w/ less gastropathic effects - reduces formation of LTB4