Autocoids Flashcards Preview

Pharmacology > Autocoids > Flashcards

Flashcards in Autocoids Deck (74):
1

Dinoprostone class

Eicosanoid

2

Dinoprostone description

PGE2

3

Dinoprostone mechanism

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

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

4

Carboprost Tromethamine Mechanism

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

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

5

Misoprostol mechanism

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

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

6

Alprostadil mechanism

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

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

7

Epoprostenol mechanism

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

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

8

Latanoprost mechanism

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

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

9

Carboprost Tromethamine class

Eicosanoids

10

Misoprostol class

Eicosanoids

11

Alprostadil class

Eicosanoids

12

Epoprostenol

Eicosanoids

13

Eicosanoids mechanism

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

Contractile effects on smooth muscle via calcium
Relaxation via cAMP

14

Dinoprostone indication

Ripens cervix @ term
Induces abortion

15

Carboprost Tromethamine description

15-methyl-PGF2alpha

16

Carboprost Tromethamine indication

Abortion, post partum hemorrhage

17

Misoprostil description

PGE1 derivative

18

Misoprostil indication

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

19

Alprostadil description

PGE1

20

Alprostadil indication

*Maintains patency of ductus arteriousus*
Impotence

21

Epoprostenol description

PGl2
*Prostacyclin*

22

Epoprostenol indication

Severe *pulmonary HTN*
Prevent platelet aggregation on dialysis machine

23

Latanoprost description

PGF2alpha derivative

24

Latanoprost adverse

Glaucoma (gold standard)

25

Zileuton description

leukotriene inhibitor
inhibits 5-lipoxygenase (LOX)

26

Zileuton indication

Asthma, 2nd line treatment

27

Zafirlukast, Montelukast description

Leukotriene inhibitor
Inhibits binding of LTD4 to receptor in target tissues

28

Zafirlukast, Montelukast adverse

Asthma, 2nd line treatment

29

Eicosanoids info

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

30

Serotonin (5-HTs) indication

Anaphylaxis

31

Sumatriptan drug class

5-HT1D/1B agonist

32

Metoclopramide and Cisapride mechanism

Prokinetic agent: promote and organize gut motility

33

Sumatriptan indication

**DOC for acute severe migraines**

34

Sumatriptan adverse

Don't use in patients with coronary heart disease

35

Metoclopramide, Cisapride drug class

5-HT4 agonist

36

Metoclopramide, Cisapride description

Prokinetic agent: promote and organize gut motility

37

Metoclopramide, Cisapride indication

Gstroparesis, emesis

38

Metoclopramide, Cisapride adverse

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

39

Cyproheptadine drug class

5-HT2 antagonist

40

Cyproheptadine description

Also blocks H1

41

Cyproheptadine indication

Allergic/vasomotor rhinitis
Carcinoid (Serotonin) syndrome

42

Ondansetron, Granisetron class

5-HT3 antagonist

43

Ondansetron, Granisetron description

Very powerful anti-emetics

44

Ondansetron, Granisetron indication

Severe nausea and vomiting associated with cancer therapy

45

Ergotamine, Dihydroergotamine class

5-HT antagonist

46

Ergotamine, Dihydroergotamine description

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

Very non selective
Partial agonists and antagonists

47

Bromocriptine, Cabergoline description

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

Very non selective
Partial agonists and antagonists

48

Ergonovine, Methylergonovine description

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

Very non selective
Partial agonists and antagonists

49

Ergotamine, Dihydroergotamine indication

migraine
second line after triptans

50

Bromocriptine, Cabergoline indication

5-HT antagonists
Dopamine agonists used to treat *hyperprolactinemia* (pituitary tumor)

51

Ergonovine, Methylergonovine indication

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

52

Cimetidine, Ranitidine, Famotidine, Nizatidine class

H2 antagonists

53

Cimetidine, Ranitidine, Famotidine, Nizatidine description

Inhibits gastric acid secretion

54

Cimetidine, Ranitidine, Famotidine, Nizatidine mechanism

Competitive inhibition of H2 receptors -> decrease gastric acid secretion

55

Cimetidine, Ranitidine, Famotidine, Nizatidine indication

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

56

Cimetidine, Ranitidine, Famotidine, Nizatidine adverse

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

57

Fexofenadine, Loratadine, Cetirizine, Astemizole, Terfenadine class

H1 antagonists second generation

58

Fexofenadine, Loratadine, Cetirizine, Astemizole, Terfenadine description

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

59

Fexofenadine, Loratadine, Cetirizine, Astemizole, Terfenadine mechanism

Inverse agonist -> decrease constitutive activity

60

Fexofenadine, Loratadine, Cetirizine, Astemizole, Terfenadine indication

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

Fexofenadine, Loratadine, Cetirizine, Astemizole, Terfenadine adverse

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

62

Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Promethazine class

H1 antagonists 1st gen

63

Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Promethazine description

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

64

Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Promethazine mechanism

Inverse agonist -> decrease constitutive activity
1st gen also block cholinergic, alpha adrenergic, serotonin and local anesthetic receptors (sodium channels)

65

Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Promethazine indication

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

Motion sickness and nausea

Somnifacient: Tx of insomnia

66

Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Promethazine adverse

Dry mouth (anti cholinergic effect)
Sedation

67

Histamine receptor/mechanism

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

68

H1 mechanism

Gq -> PLC -> IP3/DAG and calcium
Present on endothelium, smooth muscle and nerve endings

69

H2 mechanism

Gs -> Adenylyl cyclase -> increase cAMP
*Gastric mucosa*, cardiac muscle cells and some immune cells

70

H3 mechanism

Reduces NT release from histaminergic and other neurons

71

H4 mechanism

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

72

Histamine indications/effect

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

Histamine adverse

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

Histamine storage and release

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)