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Therapeutics > Lecture 26: antihistamines > Flashcards

Lecture 26: antihistamines Flashcards

1
Q

H1 antagonists referred to as

A

antihistamines

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2
Q

H2 antagonists referred to as

A

acid blockers

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3
Q

H1 antagonists

A

-competitive
-inverse agonists

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4
Q

1st gen antihistamines

A

-alkylamines
-ethanolamines
-ethylenediamines
-phenothiazines
-piperadines
-piperazines

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5
Q

structures

A

slide 26

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6
Q

H1 Antagonist effects

A

-sedation
-anticholinergic effects (piss less, dry mouth)
-local anesthetic
-anti-serotonin
-extrapyramidal

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7
Q

Sedation (H1 antagonist)

A

-CNS effect
-block H1/H2 receptors in wakefullness-promoting circuits
-dif from sedatives/hypnotics

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8
Q

H1 Antagonist interactions

A

-alcohol
-anxiolytics
-antipsychotics

-drowsiness

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9
Q

most sedating H1 antagonists

A

-ethanolamines (diphenhydramine)
-phenothiazines (promethazine)

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10
Q

Anti-cholinergic mech of H1 antagonists

A

-anti-muscarinic (atropine-like)
-more lipid soluble = inc CNS access

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11
Q

H1 antagonist anticholinergic effects

A

-anti-motion sickness
-anti-emetic
-dec urination
-dry mouth

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12
Q

best H1 antagonist for motion sickeness/nausea

A

-promethazine
-dyphenhydramine
-only 1st generation drugs

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13
Q

Local anesthetic H1 Antagonists

A

-pyrilamine
-promethazine

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14
Q

anti-serotonin H1 antagonists

A

-cyproheptadine
-azatidine

-for headaches

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15
Q

a-adrenergic antagonism H1 antagonists

A

-phenothiazines

-hypOtension

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16
Q

extrapyramidal H1 antagonists

A

-phenothiazine
-promethazine

-dystonia,akathisia

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17
Q

1st generation antihistamines (H1 antagonists)

A

-brompheniramine
-cyproheptadine
-diphenhydramine
-promethazine
-hydroxyzine
-pyrilamine

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18
Q

2nd gen antihistamines (H1 antagonists)

A

-loratidine
-desloratadine
-fexofenadine (metabolized to terfenidine)
-cetrizine (metabolized to hydroxyzine)
-levocetirizine

19
Q

2nd gen antihistamines (H1 antagonists) traits

A

-dec lipid solubility
-efflux from CNS by P-glycoprotein transporter
-structures slide 31

20
Q

2nd gen antihistamine differences from 1st gen

A

-no sedation
-no antimuscarinic act
-no motion sickness/anti-emetic effect

21
Q

2nd gen antihistamine mech

A

-block H1
-may block LTC4, neutrophil migration, eosinophil infiltration

22
Q

Allergic rhinorrhea

A

-histamine indirectly stimulates mucus discharge via H1 on nerve endings

23
Q

common cold rhinorrhea

A

-virus stimulates reflex independent of peripheral H1 receptors
-use 1st gen
-2nd prob not as effective

24
Q

1st gen drug effect on common cold rhinorrhea

A

-act in brain to inhibit rhinorrhea and sneeze
-dont use 2nd gen they prob wont b effective

25
Q

Topical H1 antagonists

A

-olopatadine (eye drops/nasal spray)
-azelastine*
-ketotifen*

*approved for systemic use in europe

26
Q

Topical H1 antagonist effects

A

-indicated for treatment of seasonal allergic rhinitis and conjunctivitis
-all cause drowsiness if taken orally or as nasal spray

27
Q

clinical use of H1 antagonists

A

-seasonal and perennial allergic rhinoconjunctivitis
-chronic urticaria
-motion sickeness (diphenhydramine, meclizine, promethazine)
-w epinephrine for anaphylaxis (diphenhydramine give parenterally)

28
Q

Adverse effects of H1 receptor ANTAgonists

A

-sedation and interactions w other sedatives (1st gen only)
-anti-cholinergic effects

29
Q

1st gen drugs contraindicted in: (bc of anticholinergic effects)

A

-urinary retention
-narrow angle glaucoma

30
Q

how do sedative effects of antihistamines differ from sedatives/hypnotics?

A

-CNS stimulation at high dose
-paradoxical excitation in kids

31
Q

most sedative antihistamines

A

-ethanolamines and phenothiazines
-ex: diphenhydramine and promethazine

32
Q

Effect of 2nd gen antihistamines on CNS

A

-no sedation
-none to limited CNS affects

33
Q

OTC sleep aids

A

-sominex and nytol
-contain diphenhydramine

34
Q

Antihistamine patient information

A

-report history of glaucoma, urinary retention, pregnancy
-drowsiness/dizziness
-avoid alcohol and other CNS depressants
-report any involuntary movements w phenothiazines

35
Q

H2 antagonists

A

-famotidine
-cimetidine
-nizatidine
-ranitidine

36
Q

H2 antagonist use

A

-reduce gastric acid secretion
-peptic ulcer
-gerd

37
Q

H2 antagonist side effects

A

-CNS dysfunction
-antiandrogen (gynecomastia, galactorrhea)
-impotence
-blood dyscrasias
-hepatotoxicity

38
Q

GCs used in allergic rhinitis

A

-fluticasone
-budesonide
-mometasone

39
Q

GCs for allergic rhinitis characteristics

A

-nasal sprays
-slow onset (may take days)
-may suppress HPA axis w high doses

40
Q

Fluticasone absorption

A

-low absorption

41
Q

budesonide absorption

A

1/3 dose absorbed in less than hour

42
Q

Role of T cells in allergic rhinitis

A

-chemoattractant
-eosinophils/neutrophils/basophils
-inflammation

43
Q

GC effect on TH2 cells

A

-decrease cytokine expression

Therapeutics (78 decks)

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