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Unit 2: Pharm > Histamine and Serotonin > Flashcards

Histamine and Serotonin Flashcards

1
Q

Name the 5 H1 receptor antagonists.

A
  1. Diphenhydramine
  2. Tripelennamine
  3. Cyclizine
  4. Promethazine
  5. Chlorpheniramine
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2
Q

What are the general properties of the 1st generation H1 receptor antagonists?

A

rapidly absorbed, widely distributed, rapidly metabolized, OTC, many actions outside of H1 receptor antagonism

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3
Q

What are the clinical uses for H1 receptor anatagonists?

A

Allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids

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4
Q

What is Tripelennamine primarily used for?

A

OTC sleep aid

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5
Q

What is Cyclizine primarily used for?

A

motion sickness

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6
Q

What is Promethazine primarily used for?

A

Anti-emetic

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7
Q

What is Chlorpheniramine usually a component of?

A

cold medications; less sedating than others so in day time medications

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8
Q

Which two H1 receptor antagonists exhibit anti-muscarinic effects and sedation?

A

diphenhydramine and promethazine

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9
Q

Name the 4 2nd generation H1 receptor antagonists.

A

Loratidine, fexofenadine, Azelastine and Certirizine

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10
Q

What can all 2nd generation H1 receptor antagonists be used to treat?

A

Allergic rhinitis

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11
Q

Which of the following is available as an intranasal spray or opthalmic solution to treat allergic rhinitis and allergic conjunctivitis respectively? Loratidine, fexofenadine, Azelastine and Certirizine

A

Azelastine

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12
Q

Do the 2nd generation H1 receptor antagonists produce sedation?

A

NO

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13
Q

Do the 2nd generation H1 receptor antagonists cross the BBB?

A

NO

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14
Q

Which of the 2nd generation H1 receptor antagonists can cause cardiovascular side effects at high doses?

A

loratidine and fexofenadine

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15
Q

Which type of drug are Cimetidine, Ranitidine, Famotidine and Nizatidine?

A

H2 receptor antagonist; blocks gastric acid secretion (primarily nocturnally)

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16
Q

What are the H2 receptor antagonists used to treat?

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

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17
Q

Which of the H2 receptor anatagonists has the most side effects? the least?

A

most-Cimetidine

least-Nizatidine

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18
Q

Which of the following can cause anti-androgen effects and can inhibit P-450 oxidative enzymes? Cimetidine, Ranitidine, Famotidine or Nizatidine

A

Cimetidine

19
Q

Which of the following can cause liver toxicity? Cimetidine, Ranitidine, Famotidine or Nizatidine

A

Ranitidine

20
Q

Which of the following can cause CNS dysnfunction? Cimetidine, Ranitidine, Famotidine or Nizatidine

A

ALL

21
Q

What is the mechanism of Cyproheptadine and what is it used to treat?

A

antihistaminic and antiserotinergic; skin allergies (anti-5HT1) and diarrhea of carcinoid system (anti-5HT2)

22
Q

What are the side effects of cyproheptadine?

A

anti-muscarinic effects and sedation

23
Q

What is the mechanism of Ketanserin and what is used to treat?

A

selective 5HT-2A, 2C antagonists and a1, H1 antagonist; antihypertensive and antiplatelet aggregation

24
Q

What is the mechanism of Odansetron and what is used to treat?

A

5HT3 receptor antagonist; nausea and vomiting in chemo

25
Q

As a class, what type of receptors do the Ergot Alkaloids effect and what side effects can they produce?

A

5HT and a-adrenergic; hallucinations and smooth muscle contraction (vascular and uterine)

26
Q

Name the 4 ergot alkaloids.

A

Ergotamine, Methysergide, Ergonovine, and Bromocriptine

27
Q

Which 3 receptors is ergotamine a partial agonist of and what is it used to treat?

A

5HT 1, 2 and a-adrenergic; prodrome of migraines

28
Q

Which 2 receptors does methysergide interact with?

A

5HT1-partial agonist

5HT2- antagonist

29
Q

What is ergonovine used to treat?

A

postpartum hemorrhage

30
Q

Which receptor does Bromocriptine interact with and what is it used to treat?

A

dopamine agonst; hyperprolactinemia

31
Q

What are triptans and which receptors do they interact with?

A

non ergot serotinin analogs; 5HT1B, D receptor agonist

32
Q

What are triptans used to treat?

A

migraines

33
Q

What are the side effects of ergotamine?

A

Nausea and vomitting, cumulative and prolonged vasoconstriction

34
Q

What are the side effects of methysergide?

A

GI disturbances, inflammatory fibrosis (chronic use), hallucinations; withdrawn from market because of these

35
Q

What are the effects of histamine on the lungs and through what receptor does it work?

A

bronchoconstriction; H1

36
Q

What are the effects of histamine on vascular smooth muscle and through what receptor does it work?

A

post capillary venule dilation, terminal arteriole dilation and venoconstriction; H1

37
Q

What are the effects of histamine on vascular endothelial cells and through what receptor does it work?

A

contraction and separation of endothelial cells; H1

38
Q

What are the effects of histamine on the nervous system and through what receptor does it work?

A

sensitization of afferent nerve terminals causing pain and itching: H1

39
Q

What are the effects of histamine on the heart and through what receptor does it work?

A

minor increase in HR and contractility; H2

40
Q

What are the effects of histamine on the stomach and through what receptor does it work?

A

increases gastric acid secretion; H2

41
Q

What are the effects of serotonin on the GI tract?

A

contraction of GI smooth muscle

42
Q

What are the effects of serotonin on the cardiovascular system?

A

vasoconstriction of smooth muscle, vasodilator in skeletal muscle and heart, reflex bradycardia and platelet aggregation

43
Q

What are the effects of serotonin on the nervous system?

A

sensitization of sensory receptors causing pain and itching

Unit 2: Pharm (11 decks)

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