Drugs for Rhinitis and allergies, Martin, Lec Flashcards

1
Q

What are the H1 1st generation classic antihistamines

A

chloropheniramine
diphendydramine (benadryl)
promethazine (phenergan)

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2
Q

What are the H1 snd generation non-sedating antihistamines

A

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

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3
Q

What are the H2 blockers (gastric acid inhibitors)

A

cmietidine
famotidine
nizatidine
ranitidine

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4
Q

where is histamine natrually stored

A

mast cells
basophils
CNS and peripheral nerves as NT

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5
Q

Activation of H1 R results in what

A
bronchoconstriction
exocrine excretion
increase cpaillary permability
contraction intestinal smooth m
stimulation sensory nerve ending
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6
Q

how does H1 R signaling owrk

A

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

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7
Q

Where are H1 R found

A

smooth muscle
endothelial cells
brain

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8
Q

What are the effects of H2 stimulation

A

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

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9
Q

mechanism of H2 R

A

inc adenyly cyclase so increase cAMP

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10
Q

where are H2 R found

A

gastric mucosa, heart, mast cells, brain

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11
Q

What are the CV effects of histamine

A

dec BP increase HR

increase force and rate of contraction

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12
Q

difference of low does histamine and higher dose on heart

A
low does activate H1
high dose activate H2
local edema and dilations
histamine headache
histamine shock
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13
Q

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

A

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

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14
Q

effects of histamine on non-vascular smooth muscle

A

bronchiolar constriction (asthmatics sensitive)

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15
Q

histamine affects on exocrine glands

A

gastric acid secretion via H2 R

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16
Q

effects of histamine on nervous system

A

pain, itching and lewis response in periphery

central is NT release

17
Q

What leads to histamine release

A

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

18
Q

what drugs can lead to release histamine

A

morphine, organinc bases (antibiotics)

19
Q

why are the 2nd generation antihistamines non-drowsy

A

do not readily enter CNS

20
Q

H1 blockers don’t work where?

A

H2 or preventing histmaine release

21
Q

how do 1st generation H1 blockers lead to sedation effect

A

bing muscarinic cholinergic R and cross CNS

22
Q

what type antihistamine is effective in preventing motion sickness

A

H1 1st generation, antiemesis and antinausea

23
Q

which antihistamine is widely used as antiemetic

A

promethazine (phenergan)

24
Q

indications for antihistamines

A

allergic conditions, motion sickness

insomnia

25
Q

side effects antihistamines

A
sedation
CNS
nausea, vomiting
antimuscarinint (dryness mouth, nasal passages, urinary retention)
HS reactions
26
Q

What are signs of overdose antihistamines

A

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

27
Q

why what terfenadine removed from market

A

caused torsades de pointes because mess with P 450 and CYP3A4

28
Q

which H1 blokcer has antiserotonin activity

A

cyproheptadine

29
Q

indications for H2 blokcer

A

peptic ulcer, gastric ulcer, zollinger-ellison syndrome

GERD

30
Q

adverse effects H@ blockers

A

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

31
Q

drug interactions cimetidine

A

inhibits CYP 450 oxidative drug metabolism system

so monitor when coadministered with P 450 metabolized drugs