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Pharmacology > Antihistamines > Flashcards

Antihistamines Flashcards

1
Q

Which antibody is a major role player for the release of histamine?

A

IgE attaches to a mast cell.

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2
Q

How are mast cells activated to release histamine?

A
  1. Mast cells are resident cells that roam waiting for a pathogen.
  2. Post a pathogen being detected mast cells have their FceR1 bound by the FC portion of the IgE antibody(produced by naive B-cells post activation).
  3. Upon binding mast cells release histamine which would result in:
    -Inflammatory effects
    -N & V
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3
Q

What is the receptor classification of histamine

A

G-protein coupled receptors

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4
Q

What is a G-protein coupled receptor?

A

Receptors that respond to a sign form a neurotransmitter/ligand and have a response attained via second-messenger( cAMP, cGMP, DAG, IP3)

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5
Q

What are the four types of histamine receptors and their sites?

A

H1- Smooth muscle contraction(bronchi, gut, large blood vessels) & Relaxes small arterioles

H2-Gastric acid secretion

H3- Localised on nerve terminals, modulates neurotransmitter release in CNS

H4-Expressed in mast cells, basophils, eosinophils-inflammatory

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6
Q

Where are H1 receptors expressed mainly?

A

Endothelial cells
Brain
Vascular cells
Peripheral nerve terminals

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7
Q

What are the effects of H1 receptors?

Brain
Vessels
Skin
Bronchus

A
  1. Brain
    -Causes wakefulness and appetite suppression
  2. Vessels
    -Causing blood vessels to dilate permeability leading to redness and oedema
  3. Skin
    NO causes pain & itching on the skin
  4. Bronchus
    Causes bronchoconstriction
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8
Q

Where is the H2 receptor localized and what is the main effects?

A

Mainly in gastric parietal cells

Release of histamine causes increased gastric secreteion

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9
Q

What are the mediators of histamine release?

A
  1. Allergic reaction
  2. Tissue injury
  3. Drugs & foreign chemicals
  4. Venom/wasp
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10
Q

What are examples of drugs that cause histamine release?

A

Tubocurarine
Succinlycholine
Morphine
Antibiotics (some)
Radiocontrast media
Carbohydrate plasma expander

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11
Q

Histamine-1 antagonists?

A

Competitive antagonist

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12
Q

When do you increase efficacy of H1 antagonist drugs?

A

When given before histamine release

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13
Q

What effect does it have on histamine released from storage site?

A

No effect

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14
Q

H1 antagonist and LA’S?

A

Many H1 antagonists are local anesthetics

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15
Q

What effect does H1 antagonist have H2 receptors?

A

Negligible effects on H2 receptors

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16
Q

H1 Antagonists admin?

A

Oral
IV
Topical administrations

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17
Q

What is the half-life for 1st generation antihistamines?

A

4-12hrs(short acting)

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18
Q

Which receptors do 1st generation drugs block?

A

Histamine receptors
Cholinergic receptors
Alpha-adrenergic receptors
Serotonin receptors
Calcium channel blockers

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19
Q

What are the S/E of 1st gen H1 antagonist?

A
  1. Cholinergic/Muscuranic blockade:
    -Xerostomia
    -Urinary retention
    -Sinus tachycardia
  2. 5-HT blockade:
    -Increased appetite
    -Increased weight gain
  3. Alpha-blockade
    -Postural Hypotension
    -Increased dizziness
  4. Cardiac ion channel blockade(Na+ & K+)
    -Increased Ventilation arrhythmia
    -Increase QT interval(the section on an electrocardiogram (ECG) report that represents the time it takes your heart muscle to contract and then recover)
  5. CNS
    -Decreased alertness, cognition, learning, memory and psychomotor
    -Increased impairment with or without sedation
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20
Q

H1 antagonist CI?

A

BDZ
Alcohol

21
Q

Which drugs are H1 antagonists?

A

My Drugs(3) Come(4) Pretty Bloody first there, Ace!

Meclizine
Diphenhydramine
Dimenhydrinate
Doxylamine
Cinnarizine
Chlorpheniramine
Cyclizine
Cyproheptadine
Promethazine
Betahistine
Tripolidine
Alimemazine

22
Q

Which H1 antagonist drugs have decreased sedative and autonomic effects?

A

All the C drugs

Chlorpheniramine
Cyclizine
Cyproheptadine

23
Q

Which H1 antagonist is a good antiemetic ?

A

Cyclizine

24
Q

Which H1 antagonist has anti-serotonin activity?

A

Cyproheptadine

25
Q

Which antihistamines are used for anti-motion sickness drugs?

A

First generation drugs

Diphenhydramine
Promethazine
Cyclizine
Cinnarizine
Meclizine

26
Q

Which antihistamines are used for nausea and vomiting?

A

Cyclizine
Meclizine

27
Q

Which antihistamines are for Meniere’s disease & vertigo?

A

Cinnarizine
Betahistine

28
Q

Which antihistamine is used to treat chemotherapy-induced vomitting?

A

Diphenydramine

29
Q

Which antihistamine is used for peri-operative premedication?

A

“PHA”(fires)-operations are just as painful as operations

Promethazine
Hydroxyzine
Alimemazine

30
Q

Which antihistamine is used as over-the-counter sleep aids?

A

Diphenhydramine
Promethazine

31
Q

Which antihistamine is used for allergies(hay fever and urticaria?

A

Second Generation Antihistamines

Loratidine
Cetirizine
Acrivistine
Fexofenadine

32
Q

Why do first-generation antihistamines cause motion sickness?

A

Due to their anticholinergic effects on the vomiting center

33
Q

What are second-generation antihistamines?

A

RACE My Famous Legs

Rupatadine
Acrivistine
Ceteririzine
Ebastine
Mizolastine
Fexofendadine
Loratadine

34
Q

What is the active metabolite of loratadine?

A

Desloratadine

35
Q

What the active metabolite of terfenadrine?

A

Fexofenadine

36
Q

What is the metabolite of hydroxizine?

A

Cetirizine

37
Q

What is the relationship between levocetirizine, cetirizine and hydroxyzine?

A

Levocetirizine > Cetirizine > Hydroxizine

38
Q

What is the active metabolite of cetirizine?

A

levocetirizine

39
Q

Which drugs treat Parkinson’s tremors and which one does not?

A

Diphenhydramine treats Parkinson tremor

Promethazine(on any drug with a Phenothiazine derivative) do not treat Parkinson tremor

40
Q

Which drugs prolong QT interval?

A

RHAME(Shame her heart is not beating)

Ebastine
Mizolastine
Azelastine
Rupatadine
Hydroxizine

41
Q

Which generation does Doxylamine belong to?

A

First generation

42
Q

Which drug treats atopic dermatitis ?

A

Diphenhydramine

43
Q

Which drug treats rhinorrhoea in colds and flus?

A

First generation drugs

Antimuscuranic effects of the first generation drugs (My drugs came pretty blood first)

44
Q

Which drugs is the antidote for serotonin syndrome?

A

Cyproheptadine

45
Q

Which drugs are used as local aneathetics?

A

Diphenhydramine & Promethazine

46
Q

H1 receptor antagonists DI?

A

Hepatic enzyme inhibitors (caution with ketoconazole, itranazole and macrolides)

&

Drugs with arrhythmia potential (interact with some 2nd generation agents)

47
Q

Which drugs treat pruritus?

A

Diphenhydramine, Hydrozoxine, and Promethiazine

48
Q

Cromolyglycic acid?

A

Inhibits degranulation of mast cell

&

Inhibit chemotactic factors on mast cell

Pharmacology (44 decks)

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