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Pharmacology 200 > 1-OTC allergy and sleep > Flashcards

1-OTC allergy and sleep Flashcards

1
Q

old anti-histamine example

A

diphenhydraine

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2
Q

new anti-histamine example

A

Loratidine

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3
Q

what is histamine and what do

A

local hormone in periphery to communicate between cells, neurotransmitter in CNS

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4
Q

where is histamine most present

A

tissues exposed to environment (skin, GIT, lungs)

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5
Q

where histamine released from and when

A

mast cells and basophil

inflammation and immune responses

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6
Q

what kind of drug is antihistamine (antagonist, agonist)

A

inverse agonist

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7
Q

why were first gen anti-histamines sedating

A

crossed the blood brain barrier

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8
Q

why could first gen anti-histamines cross the BBB

A

neutral at physiological pH

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9
Q

why are second gen anti-histamines non sedating

A

can’t cross BBB

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10
Q

why can’t second gen anti-histamines cross the BBB

A

charged at physiological pH and P-glycoproteins pump them out

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11
Q

what do P-glycoproteins do

A

pump out drugs, like second gen anti-histamines

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12
Q

are anti-histamines selective

A

yes between H1 and H2, but not against other similar receptors

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13
Q

H1 receptor

G protein, effector and 2nd messengers

A

Gq
PLC
IP3, DAG mostly NO

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14
Q

what does NO do in cell

A

vasodilate

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15
Q

H2 receptor

G protein, effector and 2nd messengers

A

Gs
AC
cAMP
gastric acid release

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16
Q

3 main responses of H1 receptor activation

A

edema, sensitization of other receptors, vasodilation

17
Q

antagonist to H1 receptor

A

ADRENALINEEEE (epipen)

18
Q

wheal and flare

A

wheal middle where lots of sweling, flare is sides with redness

19
Q

which antibody production is associated to allergies

A

IgE

20
Q

common structure of gen 1 H1 antihistamines

A

2ar-X-c-c-N=
x is either
c=o
n

21
Q

common feature of gen 2 H1 antihistamines

A

all have carboxyl group that gets - at physiological pH

more structurally diverse

22
Q

which gen is more H1 selective and why

A

gen 2

their - charge makes them bind stronger to the + pocked

23
Q

why are gen 1 H1 antihistamines bad for blood pressure

A

blocks adrenergic receptors, causes low blood pressure because adrenaline can’t bind to it and they stay dilated (α adrenergic cause vasoconstriction)

24
Q

how do H1 antihistamines affect sleep

A

lots of H1 receptors found in areas that must be activated for wakefulness, blocking it makes you sleep

they also affect circadian rhythm

25
Q

what is the tuberommammillary nucleus

A

where all histamine releasing neurons originate

Pharmacology 200 (29 decks)

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