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PCM Exam 2 > Autoacoids And Autacoid Antagonists > Flashcards

Autoacoids And Autacoid Antagonists Flashcards

1
Q

Pupillary sphincter is interacted by _______________

A

M3

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2
Q

Radial muscle of the eye is innervated by

A

Autonomic system (PNS/CNS)

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3
Q

What compounds are autacoids?

A
  • histamine
  • serotonin
  • eicosanoids
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4
Q

All histamine receptors are _________ protein linked and have ___________ activity

A

G protein; constitutive activity (the receptors still have some activity even in the absence of agonists)

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5
Q

Where can Histamine 1 (H1) receptors be found?

What kind of G protein does it have?

A
  • endothelium
  • smooth muscle cells
  • nerve endings

-Gq protein (PLC)

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6
Q

Where can H2 receptors be found and what type of G protein are the coupled with?

A
  • gastric mucosa
  • cardiac muscle cells
  • some immune cells

-Gs (adenylyl cyclase)

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7
Q

Which H receptor is found in the gastric mucosa?

A

H2

MUCOSA not smooth muscle

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8
Q

H2 receptors cause vasodilation by _______________ while H1 receptors cause vasodilation by ______

A

Acting on vascular smooth muscle and uses cAMP;

Acting on endothelial cells and cause production of NO

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9
Q

What is the effect of H2 receptors on the heart

A

↑ contractility and ↑ pacemaker rate

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10
Q

Which histamine receptors are found on the heart?

A

H2

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11
Q

Histamine induced edema results form the action of histamine on ________ receptors in blood vessels

A

H1

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12
Q

What is the effect on ____ (histamine) receptor on bronchial and GI smooth muscle?

A

H1; CONTRACTION

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13
Q

What is the effect of the activation of H2 receptors on gastric parietal cells?

A

Powerful stimulant of gastric acid secretion

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14
Q

What are the three classes of drugs that are histamine antagonists

A
  • physiological antagonists
  • release inhibitors
  • receptor antagonists
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15
Q

__________ in a physiological antagonist to histamine

A

Epinephrine

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16
Q

___________ and ________ are release inhibitors which are histamine antagonists

A

Cromolyn; nedocromil

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17
Q

Is the MOA of cromolyn and nedocromil and what kind of drugs are they?

A

They are release inhibitors that act as histamine antagonists

Reduce immunologic mast cell degranulation

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18
Q

_______ agonists appear to be bale to ↓ histamine release

A

β2

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19
Q

What are two types of H1 receptor antagonists and what is a key difference?

A

1st generation: sedative effects and anti muscarinic effects

2nd generation: less sedating effect because they have P glycoproteins and less liposoluble

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20
Q

________ generation of H1 receptor antagonists have less sedative effects because of: (2)

A

2nd generation

  • less liposoluble
  • P glycoproteins
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21
Q

Examples of first generation H1 receptor antagonist (7)

A
  • chlorpheniramine
  • cyclizine
  • diphenhydramine
  • dimenhydrinate
  • hydroxyzine
  • meclizine
  • promethazine
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22
Q

What 3 drugs are 2nd generation H1 receptor antagonists

A
  • fexofenadine
  • loratadine
  • cetirizine
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23
Q

H1 blockers are now know to be _______________ because the H1 receptors have constitutive activity

A

Inverse agonists

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24
Q

H1 receptor antagonists are useful for treating __________ but NOT for __________

A

Allergic conditions;

NOT useful in treating bronchial asthma because histamine is not the only mediator in that condition

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25
Q

Which class of drugs is useful for treating motion sickness and nausea? MOA?

A
  • 1st generation H1 receptor antagonists
  • block central H1 and M1 (emesis) receptors
  • second generation is not as full because cant enter CNS as well and dont have the ability to block M1 receptor
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26
Q

What kind of drug is diphenhydramine and what can it be used for?

A
  • 1st generation H1 receptor antagonist

- treat insomnia, allergic reactions

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27
Q

What four drugs are H2 receptor antagonists?

A
  • cimetidine
  • ranitidine
  • famotidine
  • nizatidine

-tidine

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28
Q

What is the main clinical use of cimetidine and other similar drugs?

A

Inhibits gastric acid secretion (competitively blocks H2 receptors on parietal cells)

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29
Q

Clinical uses for H2 receptor antagonists:

A
  • peptic ulcers
  • acute stress ulcers
  • GERD
30
Q

H2 receptor antagonists are very safe drugs except for _________ especially in patients with ________

A

Cimetidine;

Elderly patients or those who have renal or hepatic dysfunction

31
Q

What are some adverse effects of cimetidine?

A
  • Confusion, hallucinations, and agitation when given IV to elderly patients or those with renal/hepatic dysfunction
  • inhibits P450
  • had antiadrogenic effects: gynecomastia, ↓ sperm count and galactorrhea in women
32
Q

All of sertonin receptors are G protein coupled except _________ which is __________

A

5 HT3; ligand gated ion channel

33
Q

______ is the only monoamine NT receptor that functions as a ligand gated ion channel

A

5-HT3 receptor

34
Q

What are the two serotonin receptor agonists class of drugs?

A

5HT 1D/1B

5 HT4

35
Q

What is the suffix for 5HT 1D/1B receptor agonists?

A
  • -triptan
36
Q

5 HT 1D/1B receptor agonists are contraindicated in ________

A

Patients with coronary artery disease or angina because they can cause coronary vasospasm

37
Q

Triptans are the first line therapy for ________________

A

TREATMENT of acute severe migraine attacks

38
Q

What drug is useful in the prophylaxis for migraines?

A

Propranolol (β blocker)

39
Q

What is the MOA of 5- HT1D/1B receptor agonists in treating migraines?

A
  1. Can bind to the 5-HT 1D receptor on the nerve terminal which then inhibits the release of CGRP form the nerve terminal and thus preventing vasodilation
  2. Can bind to the 5 HT 1B receptor on the blood vessel which causes vasoconstriction
40
Q

Vasodilation/vasoconstriction is what causes migraines

A

Vasodilation

41
Q

Where is 5HT 1D receptor located and what is the effect when triptans bind to it?

A

On the nerve terminal;

Prevents the release of CGRP and thus prevents vasodilation

42
Q

___________ and ________ are 5HT4 receptor agonists

A

Metoclopramide; cisapride

Both are prokinetic agents

43
Q

Metoclopramide is a _________ agonist and is a prokinetic agent. How? (2 ways)

A

5 HT4 receptor;
Prokinetic effect: facilitates gut motility

  1. Facilitates release of Ach from enteric neurons → contractions
  2. Counteracts the inhibitory effects dopamine has on cholinergic neurons
44
Q

What are some adverse effects of metoclopramide?

A
  • somnolence (drowsiness), nervousness and dystonic reactions
  • extrapyrmaidal effects and tardive dyskinesia (rare) because it blocks the dopamine effects
45
Q

________ is no longer given as a prokinetic agent due to cardiac adverse effects due to _________

A

Cisapride; prolonged QT interval

46
Q

Classes of drugs that are sertonin antagonists

A
  • 5 HT2 receptor antagonists
  • 5 HT3 receptor antagonists
  • ergot alkaloids
47
Q

Cyproheptadine is a _________________ that is used for _______________

A

5 HT2 receptor antagonist;

Allergic rhinitis, vasomotor rhinitis, and management of serotonin syndrome

48
Q

Which drug also also potent H1 blocking actions?

A

Cyproheptadine (5 HT2 receptor antagonist)

This is why it can be used to treat allergic rhinitis

49
Q

__________ is a 5 HT3 receptor antagonist that is used for _________

A

Ondansetron;

Anti emetic that is used for severe nausea and vomiting that occurs with chemotherapy

50
Q

Ergot alkaloids are useful for treating migraine pain; specifically _________ and _________

A

(triptans are preferred)

Ergotamine and dhihydroergotamine

51
Q

What class and specific drugs would be used to treat hyperprolactinemia caused by a pituitary tumor?

A

Ergot alkaloids;

Bromocriptine and cabergoline

52
Q

If oxytocin is ineffective in controlling postpartum hemorrhage, give ______ or ________

A

Ergonovine or methylergonovine IM

Ergot alkaloids

53
Q

Ergonovine given via IM can be used to treat ____________ but if given via IV, can be used for __________

A

Postpartum hemorrhage (if oxytocin is ineffective)

Diagnosis of variant angina because it causes coronary spasm in patients with it

54
Q

_____________ of variant angina can be done via what ergot alkaloid?

A

Diagnosis;

Ergonovine given via IV

55
Q

What are some clinical uses that ergot alkaloids are used for?

A
  • treatment of migraines (ergotamine and dihydroergotamine)
  • hyperprolactinemia (bromocriptine and cabergoline)
  • post partum hemorrhage ( ergonovine or methylergonovine)
  • diagnosis of variant angina (ergonovine)
56
Q

What are adverse effects of ergot alkaloids and when is it contraindicated?

A
  • vasospasm

Contraindicated in:

  • pregnant women
  • patients with peripheral vascular disease, coronary artery disease, HTN, and impaired hepatic/renal function
  • don’t give with drugs that cause vasoconstriction
57
Q

What are the main subgroups of eicosanoids and what is the main course of eicosanoids ?

A

Subgroups:

  • prostaglandins
  • prostacyclins
  • thromboxanes
  • leukotrienes

Arachadonic acid is the main source

58
Q

COX 1 is found in ___________ as a ________ and is involved in _______

A

Most cells; constitutive enzyme; normal homeostasis

59
Q

COX 2 is found in __________

A

Inflammatory cells; induced by inflammatory stimuli

60
Q

____________ and _______ are leukotrienes that are potent _________ and secreted in asthma and anaphylaxis

A

LTC4 and LTD4;

Bronchoconstrictors

61
Q

The contractile effects of eicosanoids on smooth muscle are mediated by ______ while the relaxing effects are mediated by _______

A

Calcium; cAMP

62
Q

____________ is an eicasanoid analog (_____ analog) that is used to prevent peptic ulcers in patients taking high doses of NSAIDS

A

Misoprostol; PGE1 analog

Reasoning: NSAIDs block COX1 and thus prevent the formation of prostaglandins which are protective in the gastric mucosa and prevent erosion.

63
Q

Which eicasanoid drug is a PGE2 analog?

A

Dinoprostone

Ripens cervix near term and is an abortifacient

64
Q

____________ is a ______ analog that is used to maintain patency of the ductus arteriosus and is also used for _______

A

Alprostadil; PGE1 analog

Also used for impotence

65
Q

Epoprostenol, a _____ analog is used for (2)

A
  • severe pulmonary hypertension
  • prevent platelet aggregation in dialysis machines

Analog of a prostacyclin

66
Q

What is the use of latanoprost?

A

It is a PGF2α derivative used for glaucoma

67
Q

What are the three classes of drugs that are eicosanoid antagonists?

A
  • leukotrienes pathway inhibitors: 5-lypoxygenase inhibitors and LTD4 receptor antagonists
  • glucocorticoids
  • NSAIDs
68
Q

Zileuton inhibits ______

A

5-lypoxygenase (enzyme)

69
Q

What are the two antagonists against LTD4 RECEPTORS

A
  • zafirlukast and montelukast
70
Q

Glucocorticoids inhibits __________ and also inhibits the synthesis of _________

A
  • PLA2 → no release of arachadonic acid

- synthesis of COX 2

PCM Exam 2 (32 decks)

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