Exam 4; Biogenic Amines Flashcards

1
Q

What is used to convert histamine to histamine

A

histadine decarboxylase

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2
Q

What are four functions of histamine

A

growth and regeneration
neurotransmission
regulator of microcirculation
defense mechanisms

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3
Q

Histamine is released following a tissue injury, and has what four effects

A

inflammatory response
mechanical, thermal, chemical, or radiant injury
warning system via stimulation of sensory neurons
enhancer of the immune system

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4
Q

What is the mechanism of action of histamine

A

it binds to specific histamine receptor

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5
Q

What are four physiologic effects involving histamine and the vascular system

A

constricts larger vessels
dilate smaller vessels
cause pooling of the blood at the injury site
cause endothelial cell leakage; “wheal”

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6
Q

What is the “triple response” to injected histamine

A

central red spot; due to vasodilation
flare
wheal

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7
Q

What are the two neuronal physiologic effects of histamine

A

stimulation of sensory neuron; itching/pain

CNS effects increasing alertness

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8
Q

What are two physiologic effects of histamine regarding the smooth muscle

A

constricts bronchioles; bronchoconstriction

constricts metastmeal muscle; diarrhea

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9
Q

What is the physiologic effect of histamine regarding exocrine secretion

A

stimulates bronchial, salivary, and digestive secretions

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10
Q

What is the mechanism behind anti-histamine actions

A

blocks the histamine receptor

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11
Q

What are the CNS effects of H1 blockers

A

sedative (can be excitatory in children and the elderly)
anti-emetic
anti-nausea

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12
Q

H1 blockers cause the drying of this

A

mucous membranes

histamine stimulates the secretion

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13
Q

How does H1 blockers affect the peripheral nervous system

A

acts as a local anesthetic

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14
Q

Hows does H1 blockers affect the smooth muscle

A

it is a dilator; bronchial smooth muscle dilator

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15
Q

H1 blockers inhibit the secretion of what

A

interleukins, which are stimulators of the immune system and other inflammatory mediators

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16
Q

H2 blockers affect gastric secretion how

A

histamine is required to stimulate gastric secretion from parietal cells, an H2 blockade leads to a decrease in acid secretion

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17
Q

What three things under the category of “dermatoses” are the first generation classes H1 anti-histamines used for

A

urticarias (itching)
insect stings/bites
allergic rhinitis and allergic conjunctivitis

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18
Q

What are H1 antihistamines NOT of value in treating

A

asthma or the common cold

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19
Q

H1 anti-histamines are used for these two things besides dermatoses

A
motion sickness (anti-emetic, anti-nauseant)
sedative
20
Q

This first generation h1 blocker has sedative effects and is used for motion sickness

A

diphenyhydramine

21
Q

This first generation h1 blocker is used for motion sickness

A

clemastine

22
Q

This first generation h1 blocker is not used for motion sickness

A

chlopheniramine

23
Q

This first generation h1 blocker is used as a sedative and anti-itch

A

hydroxyzine

24
Q

This first generation h1 blocker was a precursor of the first anti-psychotic drugs and is a strong sedative/anti-emetic

A

promethazine

25
Q

This first generation h1 blocker is a sedative and has local anesthetic effects

A

tripelennamine

26
Q

True or False

The first generation h1 blockers can ever the CNS

A

True; because they are not ionized

27
Q

All of the first generation h1 blockers can act on what

A

the peripheral and central histamine receptors

28
Q

What are the four second generation h1 blockers

A
the "-ines"
lortadine
fexofenadine
desloratadine
cetirizine
29
Q

The second generation H1 blockers have less this than compared to the first generation

A

CNS effects; all are ionized in the blood

30
Q

What are the three toxicities and contraindications for ALL h1 blockers

A

high therapeutic index
first generations can react with other CNS depressants
anti-mucarinic effects

31
Q

What are the four H2 blockers

A
(-tidine's)
cimetidine
rantidine
famotidine
nazitidine
32
Q

What is the side effects of cimetidine

A
H2 blocker
anti-androgen effects
breast growth in males
lactation in women
low sperm count
33
Q

The -tidine drugs do not cross what

A

the blood brain barrier

H2 blockers

34
Q

What is serotonin synthesized from

A

tryptophan

35
Q

What are the four physiologic effects of serotonin

A

smooth muscle constriction
itching and pain
central neurotransmission (important neurotransmitter)
can cause nausea

36
Q

What is carcinoid syndrome

A

tumor of enterochromaffin cells (where serotonin is found)

37
Q

What are the five effects of an increase in serotonin

A
diarrhea
bronchospasm
sin flushing
fibrosis of heart valves 
no CNS effects; produced peripherally
38
Q

How is the role of serotonin in migraines inferred

A

by the effect of certain drugs useful in treating migraines

39
Q

How do the agents that affect migraines alter the serotonin system

A

agonists or partial agonists of serotonin receptor

40
Q

The serotonin agonists that act on migraines all cause what

A

vasoconstriction

41
Q

What are the agents that act on serotonin receptors

A

the “-triptan’s”

sumatriptan

42
Q

The triptan drugs should never be given with these drugs, would lead to a synergistic effect

A

SSRIs or MAO inhibitors

43
Q

What is serotonin syndrome

A

hyperthermia and muscle twitching

44
Q

What are the two ergot alkaloids

A

ergotamine

dihydrogotamine

45
Q

How do the ergot alkaloids affect serotonin

A

partial serotonin agonists; can also affect adrenergic and dopaminergic receptors

46
Q

What are the for side effects of ergot alkaloids

A
ergotism; excess of ergot alkaloids
"St. Anthony's fire"
hallucinations
uterine contractions
severe vasospasms; gangrene
47
Q

What is the pregnancy category of ergot alkaloids (ergotamine and dihydrogotamine)

A

X