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Pharm Exam 4 > Biogenic Amines > Flashcards

Biogenic Amines Flashcards

1
Q

What is histamine synthesized from

A

Histadine (by histadine decarboxylase)

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2
Q

Histamines mechanism of action

A

Binds to specific histamine receptors

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3
Q

Vascular histamine effects

A

Constricts larger vessels, dilates smaller vessels - local edema

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4
Q

What is the “triple response”

A

Central red spot, flare, wheal

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5
Q

Neuronal histamine effects

A

Stimulates sensory neurons - itching, pain

CNS: increases alertness

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6
Q

Smooth muscle histamine effects

A

Constricts bronchioles and intestinal muscle - diarrhea

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7
Q

Exocrine histamine effects

A

Stimulates bronchial, salivary and digestive secretions

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8
Q

Mechanism of action of antihistamine action

A

Blocks histamine receptor

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9
Q

H1 blocker effect of CNS

A

Sedative (enhanced in children and elderly)
Anti nausea
Anti emetic

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10
Q

How do H1 blockers affect mucous membranes

A

Dry membranes due to muscarinic effects

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11
Q

H1 blocker effect on peripheral nervous system

A

Acts as local anesthetic

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12
Q

How do H1 blockers affect bronchiole smooth muscle

A

Dilates it due to inhibition of interleukins and other inflammatory mediators

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13
Q

H2 blocker effect on gastric secretion

A

Decrease acid secretion because histamine is required to stimulate acid secretion from parietal cells

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14
Q

What are 4 therapeutic indications for 1st generation H1 antihistamines

A

Treatment of allergic responses, anti emetic, anti nauseant, sedatives

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15
Q

What 3 allergic responses do 1st generation H1 antihistamines treat

A

Dermatoses - urticaria (itching from insect stings and bites)
Allergic rhinitis
Allergic conjunctivitis - decreases congestion and sneezing

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16
Q

1st generation H1 blocker mechanism

A

Can act on peripheral and central H1 receptors

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17
Q

Why can 1st generation H1 blockers enter CNS

A

They are nonionized

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18
Q

Name 6 1st generation H1 blockers

A 
Diphenhydramine
Clesmastine
Chlorpheniramine
Hydroxyzine
Promethazine
Tripelennamine
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19
Q

Diphenhydramine

A

Sedative and motion sickness

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20
Q

Clemestine

A

Primarily for motion sickness

21
Q

Chlorpheniramine

A

Not a sedative

22
Q

Hydrozyzine

A

Sedative and anti itch

23
Q

Promethazine

A

Strong sedative and anti emetic

24
Q

Tripelennamine

A

Sedative with local anesthetic effects

25
Q

2nd generation H1 blocker effects

A

Fewer CNS effects - ionized in blood

Don’t cause drowsiness

26
Q

Is therapeutic index for H1 blockers high or low

A

High

27
Q

Toxicity of H1 blockers

A

Interact with other CNS depressants

28
Q

Toxicity of all H1 blockers

A

Antimuscarinic effects: dry mouth, blurred vision, constipatoin

29
Q

Why can’t H2 blockers get in CNS

A

Can’t cross blood brain barrier

30
Q

4 H2 blockers

A

Cimetidine, ranitidine, famotidine, nizatidine

31
Q

Cimetidine effect

A

Anti androgen effect

32
Q

What is 5HT synthesized from

A

Tryptophan

33
Q

Where is 5HT found

A

Enterchromaffin cells of the gut

34
Q

5HT mechanism

A

7 different 5HT receptors

35
Q

Physiological effects of 5HT

A

Smooth muscle constriction
Itching, pain
Central neurotransmission
Causes nausea

36
Q

What is carcinoid syndrome

A

Tumor of enterchromaffin cells leads to too much 5HT

37
Q

Symptoms of carcinoid syndrome

A

Diarrhea
Bronchospasm
Skin flushing
Fibrosis of heart valves

38
Q

Why does carcinoid syndrome have no CNS effects

A

Enterchromaffin cells are produced peripherally

39
Q

Cause of migraine

A

Hemicrania over time

40
Q

What happens to blood vessels during migraine

A

Strong dilation of blood vessels in dura and pia mater

41
Q

Side effects of migraine

A

Inflammation, swelling and throbbing pain

42
Q

What happens to 5HT when taking drugs for migraine

A

5HT is inferred by effect of the drugs

43
Q

What kind of migraine agents alter 5HT system

A

Agonists or partial agonists of 5HT receptor

44
Q

What can migraine agents cause

A

Vasoconstriction

45
Q

Group of agents that act on 5HT receptors

A

“TRIPTANs”

46
Q

Sumatriptan mechanism of action

A

5HT receptor agonist

47
Q

Sumatriptan mode of administration

A

Orally, nasal spray or injection

48
Q

What shouldn’t you use when taking sumatriptan

A

MAO inhibitors have synergistic effect leads to 5HT syndrome - hyperthermia and muscle twitching

Pharm Exam 4 (4 decks)

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