Antihistamine Flashcards

1
Q

Physiological antagonist of histamine

A

epinephrine

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2
Q

Therapeutic use of epinephrine

A

anaphylactic shock

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3
Q

what is the MOA of cromolyn sodium

A

blocks histamine release from lung mast cells.

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4
Q

Therapeutic use of cromolyn sodium

A

Prophylactic aerosol for asthma, hay fever.

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5
Q

First generation antihistamines

A

diphenhydramine, chlorpheniramine, promethazine, meclizine, doxylamine

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6
Q

Second generation antihistamines

A

Fexofenadine, Cetirizine

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7
Q

First generation features

A

Enter CNS, sedation and anti-cholinergic (atropine-like)

More GI problems

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8
Q

Second generation features

A

Do not enter CNS, not sedative, less muscarinic

Metabolized by CYP 3A4, drug interactions

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9
Q

Pharmacokinetics of antihistamines

A

oral administration
Distributed widely, CNS differs between generations
Topical intranasal or opthalmic agents
Metabolized by P450s (1st gen) CYP3A4s (2nd gen)

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10
Q

What combination formulations exist

A

pseudoephedrine, phenylephrine to enhance relief of nasal congestion

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11
Q

Applications specific to 1st gen antihistamines

A

prophylaxis for motion sickness and vertigo
anti-emetic
insomnia/sedative

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12
Q

best antihistamine for motion sickness

A

promethazine

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13
Q

Consideration for taking fexofenadine

A

do not take with fruit juices

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14
Q

Which of the second generation drugs causes more drowsiness

A

Cetirizine

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15
Q

Therapeutic use of diphenhydramine (4)

A

allergic rhinitis
dermatologic pain and itching
sleep aid
motion sickness- muscarinic effect

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16
Q

Adverse effects of diphenhydramine (4)

A

Sedation is prominent
Topical allergic responses
May reduce lactation and enters breast milk
Caution or avoid in narrow angle glaucoma

17
Q

Therapeutic use of chlorpheniramine (3)

A

Allergic rhinitis
Dermatologic pain and itching
OTC cold remedies

18
Q

Adverse effects of chlorpheniramine (2)

A

sedation, but less than diphenhydramine

Less muscarinic effect- glaucoma, reduced lactation

19
Q

Therapeutic use of promethazine

A

similar to other 1st gens, ANTI-EMETIC, sedative

20
Q

Adverse effects of promethazine

A

similar to other 1st gens, PHOTOSENSITIVITY

21
Q

Therapeutic use of meclizine

A

VERTIGO, preventing motion sickness

22
Q

Adverse effects of meclizine

A

less sedating than other 1st gens

23
Q

Therapeutic use of Doxylamine

A

Morning sickness in pregnancy

24
Q

Which prototype 2nd gen antihistamine has more drug interactions

A

Cetirizine, metabolized by CYP3A4

25
Q

Pharmacokinetics of cetirizine

A

oral prep, long duration