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Pharmacology > Autocoids > Flashcards

Autocoids Flashcards

1
Q

Dinoprostone class

A

Eicosanoid

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2
Q

Dinoprostone description

A

PGE2

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3
Q

Dinoprostone mechanism

A 
Autocrine and paracrine signalling 
Binds GPCR (Gs, Gi, Gq)

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

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4
Q

Carboprost Tromethamine Mechanism

A 
Autocrine and paracrine signalling 
Binds GPCR (Gs, Gi, Gq)

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

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5
Q

Misoprostol mechanism

A 
Autocrine and paracrine signalling 
Binds GPCR (Gs, Gi, Gq)

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

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6
Q

Alprostadil mechanism

A 
Autocrine and paracrine signalling 
Binds GPCR (Gs, Gi, Gq)

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

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7
Q

Epoprostenol mechanism

A 
Autocrine and paracrine signalling 
Binds GPCR (Gs, Gi, Gq)

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

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8
Q

Latanoprost mechanism

A 
Autocrine and paracrine signalling 
Binds GPCR (Gs, Gi, Gq)

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

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9
Q

Carboprost Tromethamine class

A

Eicosanoids

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10
Q

Misoprostol class

A

Eicosanoids

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11
Q

Alprostadil class

A

Eicosanoids

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12
Q

Epoprostenol

A

Eicosanoids

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13
Q

Eicosanoids mechanism

A 
Autocrine and paracrine signalling 
Binds GPCR (Gs, Gi, Gq)

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

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14
Q

Dinoprostone indication

A

Ripens cervix @ term

Induces abortion

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15
Q

Carboprost Tromethamine description

A

15-methyl-PGF2alpha

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16
Q

Carboprost Tromethamine indication

A

Abortion, post partum hemorrhage

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17
Q

Misoprostil description

A

PGE1 derivative

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18
Q

Misoprostil indication

A

Aboriton
used with methotrexate-ripen cervix, post partum hemorrhage
Prevention of PUD in patients with chronic NSAID use

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19
Q

Alprostadil description

A

PGE1

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20
Q

Alprostadil indication

A

Maintains patency of ductus arteriousus

Impotence

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21
Q

Epoprostenol description

A

PGl2

Prostacyclin

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22
Q

Epoprostenol indication

A

Severe pulmonary HTN

Prevent platelet aggregation on dialysis machine

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23
Q

Latanoprost description

A

PGF2alpha derivative

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24
Q

Latanoprost adverse

A

Glaucoma (gold standard)

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25
Q

Zileuton description

A

leukotriene inhibitor

inhibits 5-lipoxygenase (LOX)

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26
Q

Zileuton indication

A

Asthma, 2nd line treatment

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27
Q

Zafirlukast, Montelukast description

A

Leukotriene inhibitor

Inhibits binding of LTD4 to receptor in target tissues

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28
Q

Zafirlukast, Montelukast adverse

A

Asthma, 2nd line treatment

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29
Q

Eicosanoids info

A

Glucocorticoids inhibit PLA2 thus blocking the release of AA; they also inhibit the synthesis of COX-2
NSAIDS inhibit both COX’s -> decreased prostaglandins

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30
Q

Serotonin (5-HTs) indication

A

Anaphylaxis

31
Q

Sumatriptan drug class

A

5-HT1D/1B agonist

32
Q

Metoclopramide and Cisapride mechanism

A

Prokinetic agent: promote and organize gut motility

33
Q

Sumatriptan indication

A

DOC for acute severe migraines

34
Q

Sumatriptan adverse

A

Don’t use in patients with coronary heart disease

35
Q

Metoclopramide, Cisapride drug class

A

5-HT4 agonist

36
Q

Metoclopramide, Cisapride description

A

Prokinetic agent: promote and organize gut motility

37
Q

Metoclopramide, Cisapride indication

A

Gstroparesis, emesis

38
Q

Metoclopramide, Cisapride adverse

A

Cisapride is no longer in use do to serious cardiac adverse effects

39
Q

Cyproheptadine drug class

A

5-HT2 antagonist

40
Q

Cyproheptadine description

A

Also blocks H1

41
Q

Cyproheptadine indication

A

Allergic/vasomotor rhinitis

Carcinoid (Serotonin) syndrome

42
Q

Ondansetron, Granisetron class

A

5-HT3 antagonist

43
Q

Ondansetron, Granisetron description

A

Very powerful anti-emetics

44
Q

Ondansetron, Granisetron indication

A

Severe nausea and vomiting associated with cancer therapy

45
Q

Ergotamine, Dihydroergotamine class

A

5-HT antagonist

46
Q

Ergotamine, Dihydroergotamine description

A

Effects on alpha adrenergic, 5-HT, and CNS dopamine receptors

Very non selective
Partial agonists and antagonists

47
Q

Bromocriptine, Cabergoline description

A

Effects on alpha adrenergic, 5-HT, and CNS dopamine receptors

Very non selective
Partial agonists and antagonists

48
Q

Ergonovine, Methylergonovine description

A

Effects on alpha adrenergic, 5-HT, and CNS dopamine receptors

Very non selective
Partial agonists and antagonists

49
Q

Ergotamine, Dihydroergotamine indication

A

migraine

second line after triptans

50
Q

Bromocriptine, Cabergoline indication

A

5-HT antagonists

Dopamine agonists used to treat hyperprolactinemia (pituitary tumor)

51
Q

Ergonovine, Methylergonovine indication

A

5-HT antagonists
Post partum hemorrhage
Ergonovine-> provoke/dx variant angina

52
Q

Cimetidine, Ranitidine, Famotidine, Nizatidine class

A

H2 antagonists

53
Q

Cimetidine, Ranitidine, Famotidine, Nizatidine description

A

Inhibits gastric acid secretion

54
Q

Cimetidine, Ranitidine, Famotidine, Nizatidine mechanism

A

Competitive inhibition of H2 receptors -> decrease gastric acid secretion

55
Q

Cimetidine, Ranitidine, Famotidine, Nizatidine indication

A

PUD (promotes healing)
Acute stress ulcers
GERD (prevention and Tx)

56
Q

Cimetidine, Ranitidine, Famotidine, Nizatidine adverse

A

Very Safe

Cimetidine inhibits CYP450 and has anti-androgen effects (gynecomastia, galactorrhea, etc)

57
Q

Fexofenadine, Loratadine, Cetirizine, Astemizole, Terfenadine class

A

H1 antagonists second generation

58
Q

Fexofenadine, Loratadine, Cetirizine, Astemizole, Terfenadine description

A

Less sedating -> decrease lipid solubility and actively pumped out of brain by P-glycoprotein

59
Q

Fexofenadine, Loratadine, Cetirizine, Astemizole, Terfenadine mechanism

A

Inverse agonist -> decrease constitutive activity

60
Q

Fexofenadine, Loratadine, Cetirizine, Astemizole, Terfenadine indication

A

DOC for allergic rhinitis and urticaria (not used in asthma… many other mediators)
Motion sickness and nausea
Somnifacient: Tx of insomnia (less likely in second gen)

61
Q

Fexofenadine, Loratadine, Cetirizine, Astemizole, Terfenadine adverse

A

Astemizole and Terfenadine cause ventricular arrhythmia when used in combination with CYP3A4 inhibitors (block cardiac K+ channels responsible for repolarization)

62
Q

Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Promethazine class

A

H1 antagonists 1st gen

63
Q

Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Promethazine description

A

Crosses BBB -> more likely to block autonomic receptors -> sedation

64
Q

Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Promethazine mechanism

A

Inverse agonist -> decrease constitutive activity

1st gen also block cholinergic, alpha adrenergic, serotonin and local anesthetic receptors (sodium channels)

65
Q

Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Promethazine indication

A

DOC for allergic rhinitis and urticaria (not used in asthma … many other mediators)

Motion sickness and nausea

Somnifacient: Tx of insomnia

66
Q

Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Promethazine adverse

A 
Dry mouth (anti cholinergic effect)
Sedation
67
Q

Histamine receptor/mechanism

A

G protein linked
Constitutive activity -> active even in the absence of histamine
Some antihistamines are actually inverse agonist

68
Q

H1 mechanism

A

Gq -> PLC -> IP3/DAG and calcium

Present on endothelium, smooth muscle and nerve endings

69
Q

H2 mechanism

A

Gs -> Adenylyl cyclase -> increase cAMP

Gastric mucosa, cardiac muscle cells and some immune cells

70
Q

H3 mechanism

A

Reduces NT release from histaminergic and other neurons

71
Q

H4 mechanism

A

Chemotactic for EOS and mast cells; found on leukocytes in BM and blood
Inflammation and allergies

72
Q

Histamine indications/effect

A

CVS:

  • Vasodilation via H1 and H2,
  • increase contractility and HR via H2,
  • increase capillary permeability -> edema via H1 especially at the post capillary venules

Triple response: intradermal injection causes a localized red spot, flare and wehal

GIT: H1 mediated contraction
Bronchiolar: H1 mediated bronchoconstriciton (esp. in asthmatics)

Nervous: stimualtes nerve endings causing pain and itching (H1)

Secretory tissue: H2 mediated gastric acid secretion

Clinical use: Pulmonary function testing -> aerosol used to test nonspecific bronchial hyperreactivity

73
Q

Histamine adverse

A

Anaphylaxis

Dose related toxicity: flushing, hypotension, tachycardia, HA, wehals, bronchoconstriction, GI upset

DO NOT give to asthmatics or patients with peptic ulcer disease/GI bleed

74
Q

Histamine storage and release

A

Immunologic (Type 1 HS):
Ag binds IgE on surface of mast cells and basophils -> calcium mediated degranulation -> release of histamine, ATP and other mediators

Chemical and mechanical:
Amines (morphine and tubocurarine displace bound histamine from heparin complex in nrg independent fashion)

Pharmacology (24 decks)

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