Drugs for Rhinitis and allergies, Martin, Lec

Question 1

What are the H1 1st generation classic antihistamines

Answer 1

chloropheniramine
diphendydramine (benadryl)
promethazine (phenergan)

Question 2

What are the H1 snd generation non-sedating antihistamines

Answer 2

cetirizine (zyrtec)
fexofenadine (generic Allegra)
desloratadine (clarinex)
loratadine (claritin)

Question 3

What are the H2 blockers (gastric acid inhibitors)

Answer 3

cmietidine
famotidine
nizatidine
ranitidine

Question 4

where is histamine natrually stored

Answer 4

mast cells
basophils
CNS and peripheral nerves as NT

Question 5

Activation of H1 R results in what

Answer 5

bronchoconstriction
exocrine excretion
increase cpaillary permability
contraction intestinal smooth m
stimulation sensory nerve ending

Question 6

how does H1 R signaling owrk

Answer 6

couples Gq and phospholipase C to increase hydrolysis, increase IP3 and DAG, increase intracel Ca

Question 7

Where are H1 R found

Answer 7

smooth muscle
endothelial cells
brain

Question 8

What are the effects of H2 stimulation

Answer 8

increase gastric H+ secretion!!!
cardiac effects
vasodilatory effects

Question 9

mechanism of H2 R

Answer 9

inc adenyly cyclase so increase cAMP

Question 10

where are H2 R found

Answer 10

gastric mucosa, heart, mast cells, brain

Question 11

What are the CV effects of histamine

Answer 11

dec BP increase HR

increase force and rate of contraction

Question 12

difference of low does histamine and higher dose on heart

Answer 12

low does activate H1
high dose activate H2
local edema and dilations
histamine headache
histamine shock

Question 13

what is the triple response of lewis related to histamine release in skin

Answer 13

localized red spot- local dilation, seconda
flush or flare- axon reflex
wheal- local edema within 1-2 min

Question 14

effects of histamine on non-vascular smooth muscle

Answer 14

bronchiolar constriction (asthmatics sensitive)

Question 15

histamine affects on exocrine glands

Answer 15

gastric acid secretion via H2 R

Question 16

effects of histamine on nervous system

Answer 16

pain, itching and lewis response in periphery

central is NT release

Question 17

What leads to histamine release

Answer 17

IgE mediated (type I HS)
IgG or IgM mediated immune reactions
drug or chemical indued
physical release

Question 18

what drugs can lead to release histamine

Answer 18

morphine, organinc bases (antibiotics)

Question 19

why are the 2nd generation antihistamines non-drowsy

Answer 19

do not readily enter CNS

Question 20

H1 blockers don’t work where?

Answer 20

H2 or preventing histmaine release

Question 21

how do 1st generation H1 blockers lead to sedation effect

Answer 21

bing muscarinic cholinergic R and cross CNS

Question 22

what type antihistamine is effective in preventing motion sickness

Answer 22

H1 1st generation, antiemesis and antinausea

Question 23

which antihistamine is widely used as antiemetic

Answer 23

promethazine (phenergan)

Question 24

indications for antihistamines

Answer 24

allergic conditions, motion sickness

insomnia

Question 25

side effects antihistamines

Answer 25

sedation
CNS
nausea, vomiting
antimuscarinint (dryness mouth, nasal passages, urinary retention)
HS reactions

Question 26

What are signs of overdose antihistamines

Answer 26

child- excitation, hallucination, ataxia, convulsions
fixed dilated pupils with flushed face and fever
can cause coma and cardiorespiratory collapse

Question 27

why what terfenadine removed from market

Answer 27

caused torsades de pointes because mess with P 450 and CYP3A4

Question 28

which H1 blokcer has antiserotonin activity

Answer 28

cyproheptadine

Question 29

indications for H2 blokcer

Answer 29

peptic ulcer, gastric ulcer, zollinger-ellison syndrome

GERD

Question 30

adverse effects H@ blockers

Answer 30

antiandrogenic, gynecomastia, galactorrhea
GI constipation, nausea, vomiting, diarrhea
CNS- HA dizzinesss hallucinations
hematologic- agranulocytosis, thrombocytopenia
liver toxicity

Question 31

drug interactions cimetidine

Answer 31

inhibits CYP 450 oxidative drug metabolism system

so monitor when coadministered with P 450 metabolized drugs