Autocoids Flashcards

Question

Zileuton description

Answer 1

leukotriene inhibitor | inhibits 5-lipoxygenase (LOX)

Answer 2

Asthma, 2nd line treatment

Answer 3

Leukotriene inhibitor | Inhibits binding of LTD4 to receptor in target tissues

Answer 4

Asthma, 2nd line treatment

Answer 5

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

Answer 6

Anaphylaxis

Answer 7

5-HT1D/1B agonist

Answer 8

Prokinetic agent: promote and organize gut motility

Answer 9

**DOC for acute severe migraines**

Answer 10

Don't use in patients with coronary heart disease

Answer 11

5-HT4 agonist

Answer 12

Prokinetic agent: promote and organize gut motility

Answer 13

Gstroparesis, emesis

Answer 14

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

Answer 15

5-HT2 antagonist

Answer 16

Also blocks H1

Answer 17

Allergic/vasomotor rhinitis | Carcinoid (Serotonin) syndrome

Answer 18

5-HT3 antagonist

Answer 19

Very powerful anti-emetics

Answer 20

Severe nausea and vomiting associated with cancer therapy

Answer 21

5-HT antagonist

Answer 22

Effects on alpha adrenergic, 5-HT, and CNS dopamine receptors Very non selective Partial agonists and antagonists

Answer 23

Effects on alpha adrenergic, 5-HT, and CNS dopamine receptors Very non selective Partial agonists and antagonists

Answer 24

Effects on alpha adrenergic, 5-HT, and CNS dopamine receptors Very non selective Partial agonists and antagonists

Answer 25

migraine | second line after triptans

Answer 26

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

Answer 27

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

Answer 28

H2 antagonists

Answer 29

Inhibits gastric acid secretion

Answer 30

Competitive inhibition of H2 receptors -> decrease gastric acid secretion

Answer 31

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

Answer 32

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

Answer 33

H1 antagonists second generation

Answer 34

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

Answer 35

Inverse agonist -> decrease constitutive activity

Answer 36

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)

Answer 37

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

Answer 38

H1 antagonists 1st gen

Answer 39

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

Answer 40

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

Answer 41

DOC for allergic rhinitis and urticaria (not used in asthma ... many other mediators) Motion sickness and nausea Somnifacient: Tx of insomnia

Answer 42

``` Dry mouth (anti cholinergic effect) Sedation ```

Answer 43

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

Answer 44

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

Answer 45

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

Answer 46

Reduces NT release from histaminergic and other neurons

Answer 47

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

Answer 48

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

Answer 49

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

Answer 50

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)