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D1 Spring > Pharmacology - Histamine and Anti-histamines (Exam 3) > Flashcards

Pharmacology - Histamine and Anti-histamines (Exam 3) Flashcards

1
Q

Chemically classified as an amine, an organic molecule based on the structure of ammonia

A

Histamine

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2
Q

Formed by the decarboxylation of the amino acid histidine

A

Histamine

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3
Q

Where are the highest levels of histamine storage?

A

Lungs
Intestinal mucosa
Skin

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4
Q

What is histamine stored in?

A

Vesicles within mast cells (mostly)

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5
Q

These cells synthesize histamine and store it within a complex w/ heparin or chondroitin sulfate in secretory granules

A

Mast cells

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6
Q

How is histamine released from secretory granules?

A

Exocytosis
Degranulation

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7
Q

Riya is allergy prone to bananas, and she makes large amounts of banana antibody and these ________ antibodies will attach themselves to ________ cells.

A

IgE; mast

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8
Q

True or False: The 1st time Riya experiences an allergic rxn to bananas is going to be much worse than the 2nd

A

FALSE, the 2nd time is much worse

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9
Q

3 major causes of histamine release

A

1) tissue injury
2) allergic rxns
3) drugs & foreign substances

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10
Q

Histamine release in response to tissue injury?

A

initial sharp phase of release (within minutes) that’s sustained over several hours

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11
Q

Initial histamine release ________ vascular permeability

A

increases

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12
Q

Antihistamines work best in the _________ phase of histamine release, rather than the sustained phase

A

initial

(once you go into anaphylaxis, it is too late for antihistamines)

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13
Q

What are some drugs that people are allergic to?

A

Morphine
Dextran
Antimalarial drugs
Antibiotics

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14
Q

Pharmacological effects of histamine on cardiovascular system

A

Vasodilation (decrease BP)
Increased permeability (edema)
Systemic hypotension

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15
Q

What is the triple effect (caused by histamine)?

A
  1. Redding @ injection site due to vasodilation
  2. Wheal or disc of edema within 1-2 mins
  3. Large bright crimson flare/halo surrounding the wheal
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16
Q

Pharmacological effects of histamine on smooth muscle of bronchioles

A

contraction of vascular smooth muscle -> difficult to breathe!

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17
Q

Histamine increases the secretion of ___________ glands

A

exocrine

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18
Q

Pharmacological effects of histamine on peripheral nervous system

A

Itching
Pain

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19
Q

How many histamine receptors are there?

A

4 receptors
H1, H2, H3, H4 (but we only care about H1 and H2)

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20
Q

What kind of receptors are histamine receptors?

A

GPCRs

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21
Q

What are H1 receptors responsible for causing?

A

Allergic conditions

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22
Q

What are H2 receptors responsible for causing?

A

Gastric acid secretions

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23
Q

Distribution of H1 receptors

A

Smooth muscle
Endothelium
CNS
Heart

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24
Q

Distribution of H2 receptors

A

Vascular smooth muscle
CNS
Heart
Neutrophils
Gastric parietal cells
Uterus

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25
Q

Function of H1 receptors (7 things)

A

Bronchoconstriction
Vasodilation
Separation of endothelial cells
Itching
Pain
Allergic rhinitis
Motion sickness

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26
Q

Function of H2 receptors (3 things)

A

Gastric acid secretion
Vasodilation
Inhibition of IgE dependent degranulation

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27
Q

________________ competitively block the action of histamine @ the histamine receptors

A

histamine antagonists aka anti-histamines

28
Q

T/F: Anti-histamines have no impact on histamine formation or release

A

True

29
Q

Difference between 1st and 2nd generation H1 receptor antagonists

A

1st generation: crosses BBB, have sedative effects

2nd generation: significantly decreased BBB penetration, significantly decreased sedation

30
Q

T/F: A pregnant person can take 1st generation H1 receptor antagonists

A

FALSE

31
Q

The side effects of 1st generation H1 receptor antagonists are due to?

A

CNS depression

32
Q

Newer 2nd generation H1-antihistamines are more selective for?

A

peripheral histamine receptors -> less side effects

33
Q

Drug interactions of 1st generation H1-antihistamines

A

Opioids
Sedatives
Alcohol
Analgesics

34
Q

H1 antihistamines potentiate other _____ _________

A

CNS depressants

35
Q

1st generation H1 antihistamines are well absorbed from the ____ ________

A

GI tract

36
Q

1st generation H1 antihistamines are widely distributed because they can do what 2 things?

A

Cross BBB
Placental transfer

37
Q

Oldest and most effective antihistamine on the market

A

Diphenyhydramine (benadryl)

38
Q

What effects does diphenhydramine (benadryl) have?

A

Sedative effects

39
Q

What is the active ingredient in Tylenol PM and dramamine?

A

diphenhydramine (benadryl)

40
Q

What is the mechanism of diphenhydramine (benadryl)?

A

Inhibits histamine binding to H1 receptors

Inhibits reuptake of serotonin

41
Q

This is the active ingredient in NyQuil and has potent anti-cholinergic effects

A

doxylamine succinate

42
Q

Dimenhydrinate (dramamine) is a combo of?

A

Diphenhydramine (benadryl) + 8-chlorotheophillinate (similar to caffeine)

43
Q

What drug is used to treat motion sickness by acting on H1 receptors?

A

Diphenhydramine (benadryl)

44
Q

This drug has been shown to have antidepressant properties and inhibit the reuptake of serotonin

A

Chlorphenamine

45
Q

What drug is used for the antihistamine component of Visine-A?

A

Pheniramine

46
Q

Used to treat motion sickness, vertigo, nausea and vomiting

A

Piperazines

47
Q

Used to treat motion sickness, vertigo, and post-op following administration of general anesthesia and opiods

A

Cyclizine

48
Q

Structurally related to the ethylenediamines and the ethanolamines and thus produce significant anti-cholinergic effects

A

Piperazines

49
Q

Used to treat nausea, vomiting, and vertigo; causes drowsiness

A

Meclizine

50
Q

This drug treats indoor and outdoor allergies and is safe to use in children as young as 2; considered a second generation drug

A

Cetirizine (zyrtec)

51
Q

This drug has extremely strong anticholinergic and sedative effects; also used as anti-nausea drug for morning sickness

A

Promethazine

52
Q

This drug is both an antihistamine & antiserotonergic agent; used to treat hay fever and stimulate appetite in people with anorexia

A

Cyprohepatidine

53
Q

This drug has severe side effects including drowsiness, weight gain, dry mouth, irritability, and nosebleeds

A

Ketotifen (Zaditor)

54
Q

Characteristics of 2nd generation H1 receptor antagonists

A

Bulky
Less lipophilic
Don’t cross BBB as readily

55
Q

These H1 antagonists are more selective for peripheral H1 receptors than CNS H1 receptors

A

2nd generation H1 antagonists

56
Q

This drug does not cross the BBB and has severe interactions with erythromycin and grapefruit juice

A

Astemizole (Hismantol)

57
Q

This drug has long lasting effects and does not cause drowsiness because it does not cross the BBB

A

Loratadine (claritin)

58
Q

Newer H1 antagonists are either the active ________ or _______ of a ____ generation drug

A

enantiomer; metabolite; 2nd

59
Q

This drug is the active enantiomer of Cetirizine and is not metabolized

A

Levocetirizine (Zyzal)

60
Q

This drug is an alternative to Terfenadine

A

Fexofenadine (allegra) - newer 2nd gen H1 receptor antagonist

61
Q

Name 2 H2 receptor antagonists

A

Cimetidine (Tagamet)
Famotidine (pepcid)

62
Q

Histamine binds to H2 receptors in the _______

A

Stomach

63
Q

Clinical uses of H2 receptor antagonists

A

Zollinger-ellison syndrome
Acid reflux

64
Q

Adverse effects of this H2 receptor antagonist are severe CNS effects in elderly people

A

Cimetidine

65
Q

All H2 antagonists, except for Famotidine (pepcid), increase the bioavailability of _______________

A

ethanol

66
Q

Agents that inhibit gastric secretion alter? (2 things)

A

1) bioavailability
2) rate of absorption of drugs

D1 Spring (47 decks)

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