Antihistamines

Question 1

chlorpheniramine

Answer 1

1st generation

in OTC cold meds

Question 2

diphrenhydramine

Answer 2

(Benadryl)
1st generation
anti-motion sickness
OTC sleep aid

Question 3

dimenhydrinate

Answer 3

(Dramamine)
1st generation
anti-motion sickness

Question 4

loratadine

Answer 4

(Claritin) 2nd gen

Question 5

ceterizine

Answer 5

(Zyrtec) 2nd gen

Question 6

fexofenadine

Answer 6

(Allegra) 2nd gen

Question 7

cromolyn sodium

Answer 7

mast cell stabilizer

Question 8

histamines are referred to as an _________, a compound that is released and acts locally in periphery

Answer 8

Autacoid

Question 9

Which receptor subtype is in the smooth muscle, endothelium, and CNS?

Answer 9

H1

Question 10

Which receptor is in the vascular smooth muscle?

Answer 10

H2

Question 11

what drug stimulates histamine release?

Answer 11

opioids

Question 12

what drug blocks histamine release?

Answer 12

epinephrine/cromolyn (epi pen)

Question 13

In the endothelium, binding to the H1 receptor causes:

Answer 13

increase of NO and cGMP

Question 14

effect (symptoms) of histamine stimulating peripheral nerve endings

Answer 14

itching

pain

Question 15

effect (symptoms) of histamine in the CNS

Answer 15

wakefulness
appetite
body temperature

Question 16

which of the following conditions is NOT primarily histamine-mediated?
Anaphylaxis
Urticaria
Allergic rhinitis/conjunctivitis

Answer 16

Anaphylaxis

Question 17

which generation of antihistamines penetrates the BBB (more CNS effects)?

Answer 17

1st generation

Question 18

In addition to H1 receptor, 1st generation antihistamines also block __________ receptors, with related side effects.

Answer 18

cholinergic

also…
muscarinic (vision changes)
alpha-adrenergic (tachycardia)
serotonin

Question 19

Antihistamines have no demonstrated effect in treating ____________, ___________ and ____________.

Answer 19

the common cold (but anticholinergic effects in 1st gen drugs dry up secretions)

anaphylaxis

asthma

Question 20

2nd generation are effective at treating:

Answer 20

allergic rhinitis
allergic conjunctivitis
urticaria

Question 21

1st generation are effective at treating:

Answer 21

motion sickness

insomnia

Question 22

which drug won’t work as well if you drink grapefruit/apple juice?

Answer 22

fexofenadine

Question 23

which generation of drugs has the longer half life?

Answer 23

2nd gen (12-24 hours)

Question 24

antihistamines have a ________ distribution and is cleared by the _________

Answer 24

wide

kidney

Question 25

contraindications to 1st gen

Answer 25

impaired liver or kidney function

elderly

pregnant/lactating

neonates/children