Antihistaminics And Therapy Of Allergic Rhinitis

Front 1

diphenhydramine, dimenhydrinate, chlorpheniramine, promethazine, cyproheptadine, hydroxyzine, hydroxyzinepamoate

Back 1

1st generation antihistamines

Front 2

terfenadine, fexofenadine, loratadine, desloratadine, certirizine

Back 2

2nd generation antihistamines

Front 3

terfinadine MOA/structure

Back 3

2nd generation antihistamine/ prodrug with no antihistaminic activity

Front 4

terfinadine taken off market because?

Back 4

unchanged prodrug has caused fatal arrythmias (QT prolongation, torsades) when taken by pts with liver dz or concurrently on P450 inhibitors

Front 5

fexofenadine (Allegra)

Back 5

Primary active metabolite of terfenadine/2nd generation antihistamine

Front 6

desloratadine (Clarinex)

Back 6

active metabolite of loratadine/ 2nd generation antihistamine

Front 7

cetirizine (Zyrtec)

Back 7

faster onset and increased drowsiness when compared to loratadine

Front 8

1st generation antihistamines have variable amounts of activity with regards to ?

Back 8

antihistamine activity, sedation, anticholinergic effects, antipuritic activity, antiemetic activity

Front 9

Nonsedating antihistamines(2nd gen) have high _____, but little activity as _________.

Back 9

1. antihistaminic activity
2. sedatives, antiemetics,or anticholinergics

Front 10

2nd generation antihistamines have ______ duration of action, ______ onset, and ______the BBB.

Back 10

1. long duration of action
2. slow onset
3. do NOT penetrate

Front 11

___________has the highest activity in all aspects (antihistamine, sedative, anticholinergic, and antiemetic)

Back 11

promethazine
(Phenergan)

Front 12

__________is the 2nd most active in all aspects(antihistamine, sedative, anticholinergic, and antiemetic)

Back 12

diphenhydramine(Benadryl)
(significant sedation and anticholinergic activity)

Front 13

__________has the strongest sedative and antiemetic effects

Back 13

hydroxyzine (atarax)

Front 14

__________has significant antiserotonin activity

Back 14

cyproheptadine (periactin)

Front 15

MOA of antihistamines

Back 15

competitively antagonize endogenous histamine at H1 receptor site

Front 16

Name the antihistamines associated with these additional actions:
1. antipuritic
2. tx of vertigo
3. antiemetic

Back 16

1. hydroxyzine HCL(Atarax)
2. meclizine (Antivert)
3. dimenhydrinate (Dramanine)-chewable tablets

Front 17

indications of oral antihistamines

Back 17

-perrenial and seasonal allergic rhinitis, vasomotor rhinitis(chlorpheniramine/)
-rhinitis and sneezing due to common cold

Front 18

indications for parenteral antihistamines

Back 18

-adjunct to EPI and other measures in anaphylaxis (diphenhydramine/Benadryl)

Front 19

indications for diphenhydramine (Benadryl)

Back 19

-active and prophylactic tx for motion sickness
-anticholinergic effect on Parkinsonism

Front 20

indications for promethazine (Phenergan)

Back 20

-perioperative sedation
-adjunct to opioid analgesics for post op pain
-post op antiemetic effect

Front 21

indications for cyproheptadine (Periactin)

Back 21

unlabeled use to stimulate appetitie

Front 22

DI of antihistamines

Back 22

-additive/synergistic effects with CNS depressants
-1st generation and ETOH and Rx/OTC sedatives tranquilizers should be avoided
-cetirizine(Zyrtec) considered minimally sedating

Front 23

continuous use of a 2nd generation antihistamine is effective for tx of?

Back 23

SAR and PAR

Front 24

preferred 2nd generation antihistamines used that do not cross BBB and do not cause sedation

Back 24

fexofenadine, loratadine, and desloratadine
(Allegra, Claritin, Clarinex)

Front 25

most effective agents for all symptoms of allergic rhinits

Back 25

intranasal steroids

Front 26

1st and 2nd generation antihistamines and pregnancy

Back 26

considered safe and recommended for use

Front 27

MOA of antihistamines (H1 rec blockers)

Back 27

-inhibit early-phase rxn only and do not completely stop symptoms because other mediators involved
-decrease sneezing, nasal pruritis(DOC), lacrimation, rhinorrhea,
-DO NOT decrease nasal congestion

Front 28

ADR of antihistamines

Back 28

-1st generation and cetirizine=sedation
-anticholinergic effects prominent with 1st generation

Front 29

DOC for nasal congestion and 1st line agent for moderate severe allergic rhinitis

Back 29

intranasal steroids

Front 30

effects of intranasal steroids

Back 30

-decrease nasal congestion, nasal d/c, sneezing, postnasal drip, and pruritis
-no sedative or anticholinergic effects