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histamine/PG Flashcards

(40 cards)

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1
Q

brompheniramine

A

first gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
  • These are all good at blocking the receptors - but the two generations are differetn in a few ways
    • 2nd gen don’t cross BBB - can relieve seasonal allergies without CNS issues
    • Many of the 1st gens have strong anticholinergic activity - this is primarily what cuases the CNS sedation, its also what makes some of them good at preventing motion sickness
    • Duration of action: 1st gen (4-6 hours), 2nd gen (12-24 hours)
  • Tox
    • Sedation
    • Antimuscarinic: urinary retention, blurred vision
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2
Q

CHLORPHENIRAMINE

A

first gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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3
Q

clemastine

A

first gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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4
Q

dimenhydrinate

A

first gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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5
Q

diphenhydramine

A

first gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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6
Q

hydroxyzine

A

first gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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7
Q

meclizine

A

first gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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8
Q

promethazine

A

first gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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9
Q

azelastine

A

Second gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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10
Q

cetirizine

A

second gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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11
Q

desloratadine

A

second gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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12
Q

fexofenadine

A

second gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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13
Q

loratadine

A

second gen H1 blocker

  • H1 receptor mediated response
    • Nervous system
      • Uticarial response, insect stings
      • Reqpiratory neuron signaling
    • CV
      • Vasodilation mediated by increased NO release (very similar to how ACH cuases reaction in vascular endothelium)
      • Reflex tachycardia
      • Edema: increased permeability of post capillary vessels
    • Bronchiolar SM
      • Bronchoconstriction (particularly in asthmatic patients)
    • GI smooth muscle
      • Contraction of intestinal smooth emucels (high doses produce diarrhea)
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14
Q

cimetidine, famotidine

A

H2 blocker

  • H2 receptor mediated response
    • CV
      • Higher dosese of histamine - cAMP dependent vasodilation and direct cardiac stimulation
        • Increase contractility and HR
      • H2 antagonists have little effect on cardiac function - you would have to give them in really high concentrations
    • Secretory tissue
      • Stimulation of parietal cells - gastric acid secretion
      • Ranitidine, cimetidine, nizatidine, famotidine
  • Clinical uses of H2 receptor antagonists
    • Reduceing gastric acid secretion
      • PUD, GERD,
    • Effective doses generally don’t impact
      • Intesitnal secretion
      • Other peripheral H2 receptor mediated effects (HR etc)
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15
Q

nizatidine

A

H2 blocker

  • H2 receptor mediated response
    • CV
      • Higher dosese of histamine - cAMP dependent vasodilation and direct cardiac stimulation
        • Increase contractility and HR
      • H2 antagonists have little effect on cardiac function - you would have to give them in really high concentrations
    • Secretory tissue
      • Stimulation of parietal cells - gastric acid secretion
      • Ranitidine, cimetidine, nizatidine, famotidine
  • Clinical uses of H2 receptor antagonists
    • Reduceing gastric acid secretion
      • PUD, GERD,
    • Effective doses generally don’t impact
      • Intesitnal secretion
      • Other peripheral H2 receptor mediated effects (HR etc)
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16
Q

ranitidine

A

H2 blocker

  • H2 receptor mediated response
    • CV
      • Higher dosese of histamine - cAMP dependent vasodilation and direct cardiac stimulation
        • Increase contractility and HR
      • H2 antagonists have little effect on cardiac function - you would have to give them in really high concentrations
    • Secretory tissue
      • Stimulation of parietal cells - gastric acid secretion
      • Ranitidine, cimetidine, nizatidine, famotidine
  • Clinical uses of H2 receptor antagonists
    • Reduceing gastric acid secretion
      • PUD, GERD,
    • Effective doses generally don’t impact
      • Intesitnal secretion
      • Other peripheral H2 receptor mediated effects (HR etc)
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17
Q

thioperamide

Study These Flashcards
A

H3 blocker

  • H3 receptor mediated responses
    • Nervous system
      • Presynaptic H3 receptor activation modulates neurotransmitter release
    • Metabolic effects
      • Ongoing studies,
18
Q

chlorbenpropit

Study These Flashcards
A

H3 blocker

  • H3 receptor mediated responses
    • Nervous system
      • Presynaptic H3 receptor activation modulates neurotransmitter release
    • Metabolic effects
      • Ongoing studies,
19
Q

idophenpropit

Study These Flashcards
A

H3 blocker

  • H3 receptor mediated responses
    • Nervous system
      • Presynaptic H3 receptor activation modulates neurotransmitter release
    • Metabolic effects
      • Ongoing studies,
20
Q

cromolyn

Study These Flashcards
A

histamine release inhibitors

  • Three main things that use it
    • Basophils/mast cells
      • High levels in potential sites of injury (nose, mouth, feet, blood vessels)
      • Cross linking of IgE on surface (via antigens) cause degranulation
        • There is feedback on the H2 receptors to inhibit more release
      • Released histamine
        • Type 1 allergic reactions - hay fever, acute uticaria
        • Inflammatory and immune modulation
          • Blood vessel dialation
          • Complement activation
          • Cytokine release
          • T cell and B cell modulation
    • Brain
      • Neurotransmitter function
    • Enterochromaffin like cells (ECL) in stomach
      • Activate acid production
    • Chemical induced histamine release
      • Morphine and tubocurarine
      • Compound 48/80
        • Drug used in the lab - it just makes the mast cells release histamine
      • Mast cell injury
  • There is no clinical use of histamine - toxic effects overshadow clinical benefit
  • How to modulate histamine clinicaly
    • Phsyiologic counteraction - epinephrine
    • Inhibitors of histamine release: cromolyn
    • Pharamcologic blockade of histamine receptros
      • Block them with antagonists
21
Q

nedocromil

Study These Flashcards
A

histamine release inhibitors

  • Three main things that use it
    • Basophils/mast cells
      • High levels in potential sites of injury (nose, mouth, feet, blood vessels)
      • Cross linking of IgE on surface (via antigens) cause degranulation
        • There is feedback on the H2 receptors to inhibit more release
      • Released histamine
        • Type 1 allergic reactions - hay fever, acute uticaria
        • Inflammatory and immune modulation
          • Blood vessel dialation
          • Complement activation
          • Cytokine release
          • T cell and B cell modulation
    • Brain
      • Neurotransmitter function
    • Enterochromaffin like cells (ECL) in stomach
      • Activate acid production
    • Chemical induced histamine release
      • Morphine and tubocurarine
      • Compound 48/80
        • Drug used in the lab - it just makes the mast cells release histamine
      • Mast cell injury
  • There is no clinical use of histamine - toxic effects overshadow clinical benefit
  • How to modulate histamine clinicaly
    • Phsyiologic counteraction - epinephrine
    • Inhibitors of histamine release: cromolyn
    • Pharamcologic blockade of histamine receptros
      • Block them with antagonists
22
Q

alprostadil

Study These Flashcards
A

PGE1 (prostaglandin)

relaxes SM
keeps ductus arteriosis opens for neonates awating cardiac surgery

second line treatment for ED

23
Q

dinoprostone

Study These Flashcards
A

PGE2

given vaginally for abortion

can also be used to incue labor

24
Q

misoprostol

Study These Flashcards
A

PGE1 analogue

1st and 2nd trimester abortion

  • Misoprostol - Methyl analog of PGE1
    • Binds to PG receptors on parietal cells to inhibit acid secretion
      • NSAIDs inhibit production of PG - but you can replace the PG in the stomach to stop the ulcers from forming
    • Use
      • Prevent NSAIDs ulcers from forming
    • AE
      • Diarrhea and abdominal pain
    • May cause abortion by stimulating uterine contractions
  • Misoprostol (PGE1 derivative) - cryoprotective

Reatment of ulcer approved for the treatment of NSAID induced ulcer

Combined with mifepristone for terminating early pregnancy

25
aspirin
salicylate NSAID
26
salicyclic acid
salicylate NSAID
27
celecoxib
COX2 inhibitor
28
rofecoxib
cox2 inhibitor (discontinued)
29
valdecoxib
cox2 inhibitor (discontinued)
30
Ibuprofen
NSAID
31
indomethacin
NSAID
32
ketorolac
NSAID
33
naproxen
NSAID
34
oxaprozin
NSAID
35
piroxicam
NSAID
36
sulindac
NSAID
37
ketoprofen
NSAID
38
diclofenac
NSAID
39
montelukast
leukotriene inhibitor asthma
40
ziluteon
leukotriene inhibitor asthma

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