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histamine/PG Flashcards

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

A

H3 blocker

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

chlorbenpropit

A

H3 blocker

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

idophenpropit

A

H3 blocker

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

cromolyn

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

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

A

PGE1 (prostaglandin)

relaxes SM
keeps ductus arteriosis opens for neonates awating cardiac surgery

second line treatment for ED

23
Q

dinoprostone

A

PGE2

given vaginally for abortion

can also be used to incue labor

24
Q

misoprostol

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
Q

aspirin

A

salicylate NSAID

26
Q

salicyclic acid

A

salicylate NSAID

27
Q

celecoxib

A

COX2 inhibitor

28
Q

rofecoxib

A

cox2 inhibitor (discontinued)

29
Q

valdecoxib

A

cox2 inhibitor (discontinued)

30
Q

Ibuprofen

31
Q

indomethacin

32
Q

ketorolac

33
Q

naproxen

34
Q

oxaprozin

35
Q

piroxicam

36
Q

sulindac

37
Q

ketoprofen

38
Q

diclofenac

39
Q

montelukast

A

leukotriene inhibitor

asthma

40
Q

ziluteon

A

leukotriene inhibitor

asthma

IC (32 decks)

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