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RCS > Autocoids and Autocoid Antagonist > Flashcards

Autocoids and Autocoid Antagonist Flashcards

1
Q

What are the 3 different autacoids?

A
  1. Histamine
  2. Serotonin
  3. Eicosanoids
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2
Q

Name the histamine receptors their MOA and location?

A
  • H1: (Gq) endothelium, smooth muscle cells, and nerve endings
  • H2: (Gs) gastric mucosa, cardiac muscle cells, some immune cells
  • H3: reduces transmitter relase from histaminergic and other neurons
  • H4: mainly on leukocytes in bone marrow/circulating blood
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3
Q

What are the effects of histamine receptors on the cardiovascular system, extravascular smooth muscle, nervous system, and secretory tissue?

A

CVS:

  • vasodilation by H1 (endothelial cells stimulate formation of NO) and H2 receptors (vascular smooth muscle increas cAMP)
  • increase contractility and pacemaker rate (mainly H2)
  • Increase capillary permeability by H1

Extravascular SM:

  • GI tract smooth muscle contraction by H1
  • Bronchoconstriction H1

Nervous System:

  • powerful stimulant of sensory nerve endings (pain, ithching) by H1

Secretory Tissue:

  • powerful stimulant of gastric acid secretion by H2 in gastric parietal cells
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4
Q

What is a use of histamine?

A
  • Pulmonary Function Testing using Histamine aerosol to test for nonspecific bronchial hyperactivity
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5
Q

What is a physiological histamine antagonist?

A
  • Epinephrine has smooth muscule actions opposite to those of histamine
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6
Q

What are the histamine release inhibitors and their mechanism?

A

Cromolyn and Nedocromil

M: reduce immunologic mast cell degranulation

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7
Q

What is the difference between the first and second generation H1 receptors antagonists?

A
  • First gen: sedative effects and are more likely to block autonomic receptors
  • Second gen: less sedating bc are less liposoluble

Both are substrates of the P-glycoprotein transporter

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8
Q

What are examples of first generation H1 receptor antagonists?

A

Chlorpheniramine, Cyclizine, Diphenhydramine, Dimenhydrinate, Hydroxyzine, Meclizine, Promethazine

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9
Q

What are examples of second genereation H1 receptor antagonists?

A
  • Fexofenadine (Allergra)
  • Loratadine (Claritin)
  • Cetirizine (Zyrtec)
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10
Q

What are the uses and adverse effects of H1 receptor antagonists?

A

Uses:

  • DOC for allergic rhinitis and urticaria
  • First gen prevent motion sickness
  • First gen strong somnifacients to Tx insomnia

AE:

  • Sedations (less common with 2nd gen)
  • Dry mouth (anticholinergic effects)
  • Frist gen have additional effects due to blocking of cholinergic, alpha-andrenergic, serotoninc receptors, and Na+ channels
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11
Q

What are the H2 receptors antagonists, mechanism, uses, and adverse effects:

A

Cimetidine (tagamet), Ranitidine (Zantac), Famotidine (Pepcid), Nizatidine (Axid)

M: inhibition of gastric acid secretion (competitive blocker)

Uses: Peptic ulcers, acute stress ulcers, GERD

AE: headache, dizziness, diarrhea, muscular pain, constipation; when given by IV confusion, hallucinations, agitation; more common with Cimetidine because it inhibits cytochrome P450 and binds androgen receptors (men gynecomastia/reduced sperm and women galactorrhea)

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12
Q

What is the MOA of serotonin

A

MOA: there are seven families of 5-HT receptors 6 of them are G protein-coupled receptors while 5-HT3 receptor is a ligand-gated ion channel

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13
Q

What is the 5-HT1D/B receptor agonist, MOA, uses?

A

Sumatriptan (triptans)

MOA: vasoconstriction by 5-HT1B, inhibition of CGRP/vasodilating mediators by 5-HT1d, and inhibition of pain transmission by trigeminal nerve

CA: DOC for acute severe migraine headaches

TCo: pts with coronary artery disease or angina

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14
Q

What are the 5-HT4 receptor agonists?

A

Metoclopramide and Cisapride

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15
Q

Metoclopramide

A

M: 5-HT4 receptor agonist

CA: prokinetic agent facilitating ACh relase from enteric neurons, coordinated contractions that enhance transit; antinauseant and antiemetic

AE: somnolence, nervousness, and dystonic reactions; rarely extrapyramidal effects and tardive dyskinesia

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16
Q

Cisapride

A

M: 5-HT4 receptor agonists

CA: used as a prokinetic

AE: QT interval prolongation (no longer used in US)

17
Q

What are the types of serotonin antagonists?

A
  • 5-HT2 receptor antagonists
  • 5-HT3 receptor antagonists
  • Ergot Alkaloids
18
Q

Cyproheptadine

A

M: 5-HT2 receptor antagonists (also potent H1 blocking)

CA: allergic rhinitis, vasomotor rhinitis, management of serotonin syndrome

19
Q

Ondansetron

A

M: 5-HT3 receptor antagonists

CA: anti-emetic particulary for chemotherapy

20
Q

What are the Ergot Alkaloids, MOA, CA, AE, TCo?

A

Egrotamine, Dihydroergotamine, Bromocriptine, Cabergoline, Ergonovine, Methylergonovine

M: agonist/partial agonist/antagonist actions at alpha-andrenoceptors and 5-HT receptors; agonist/partial agonist actions at CNS dopamine receptors

CA: Migraine (ergotamine, dihydroergotamine), Hyperprolactinemia (bromocriptine, cabergoline), Postpartum Hemorrhage (ergonovine, methylergonovine), Dx of variant angina (ergonovine)

AE: vasospasm

TCo: pregnant women, PVD, CAD, HTN, impaired renal/hepatic function, and pts on other vasoconstrictors

21
Q

Ecosanoids MOA?

A

M: contracile effects on smooth muscle mediated by Ca2+, relaxing effects mediated by cAMP

22
Q

Misoprostol

A

M: PGE1 analog

CA: prevention of peptic ulcers in pts taking high doses of NSAIDS, ripen cervix at/near term, management of postpartum hemorrhage, abortifacient in combination with antiprogestin mifepristone/methotrexate

23
Q

Dinoprostone

A

M: PGE2

CA: to ripen cervix at/near term, abortifacient

24
Q

Alprostadil

A

M: PGE1

CA: maintain patency of ductus arteriosus, impotence

25
Q

Epoprostenol

A

M: PGI2

CA: severe pulmonary HTN, prevent platelet aggregation in dialysis machine

26
Q

Latanoprost

A

M: PGF2alpha derivative

CA: glaucoma

27
Q

What are the two classes of leukotriene pathway inhibitors?

A
  • Inhibitors of 5-lypoxygenase: Zileuton
  • Antagonists of LTD4 receptors: Zafirlukast, Montelukast
28
Q

What is the MOA of glucocorticoids?

A
  • Inhibit PLA2 blocking the release of arachidonic acid
  • inhibit synthesis of COX-2
29
Q

What is the MOA of NSAIDs?

A
  • primarily inhibits cyclooxygenase
  • have antipyretic, analgesix, and anti-inflammatory activities

RCS (8 decks)

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