Autacoids & Autacoid Antagonists

Front 1

Histamine receptors H1
location
coupled to _____
lead to formation of _______.
causes rapid release of _____.

Back 1

H1- endothelial cells-
coupled to PLC, IP3, DAG,
releases Ca2+.

Front 2

Histamine receptor H2
location
coupled to:
leads to stimulation of:
activation of:

Back 2

H2-
gastric mucosa & cardiac m,
stimulates Adenylate cyclase activation of cAMP

Front 3

Histamine receptor H4
location
function

Back 3

H4- on leukocytes- chemotactic effects on eosinophils

Front 4

All Histamine receptors behing to superfamily linked to ______.

Back 4

G-proteins

Front 5

Identify H1 receptor effects on organs (3)

Back 5

cardiovascular- Increase capillary permiability --> edema & hives

GI & Lungs: contraction

Nervous system: itching & pain

Front 6

What are the effects of H2 receptors? (2)

Back 6

Heart- increased contractility & pace maker rate

Histamine- powerful stimulant of gastric acid secretion

Front 7

Vasodilation involves _____ receptors.

Back 7

H1 and H2
H1- NO
H2- cAMP

Front 8

Antidote for histamine anaphylaxis.

Back 8

Epinephrine

Front 9

Adverse effects of Histimine

Back 9

flushing
hypotension- vasodilation (H1&H2) --> low BP --> reflex tachycardia

headache
wheals
brochoconstriction (H1)
GI upset

Front 10

contraindication

Back 10

asthmatics
peptic ulcer dx
gastric bleeding

Front 11

Identify 3 ways to decrease histamine levels.

Back 11

1. physiological antagonist
2. release inhibition
3. receptor antagonist

Front 12

identify 1 physiological antagonist

Back 12

epinephrine

Front 13

identify 2 release inhibitors of histamine

** inhibits degranulation of mast cells**

Back 13

CROMOLYN
NEDOCROMIL

beta -2 agonists

Front 14

Identify histamine receptor antagonists

Back 14

HI and H2 receptor antagonist

Front 15

H1:
first vs. second generation

Back 15

1st: sedative effects (cross BBB)

2nd: less sedative b/c less lipophilic

Front 16

Identify the uses of Histamine antagonists

Back 16

allergic rhinitis
urticaria
motion sickness
insomnia

NOT effective in bronchial asthma

Front 17

Adverse effects of Histamine antagonists

Back 17

sedation
dry mouth-anticholinergic

Front 18

Terfenadine
Astermizole
Grapefruit juice

Back 18

drug interaction - inhibit CYP3A4 --> ventricular arrythmia

Front 19

learn the HI antagonist drugs (14)

Back 19

review the packet for 14 HI antagonist drugs

Front 20

Identify 4 H2 receptor antagonists

Back 20

Ci-menti-dine
Ran-iti-dine
Famotidine
Nizatidine

Front 21

Main clinical use of H2 antagonists

Back 21

inhibit gastric acid secretion:
-peptic ulcers
-acute stress ulcers
-GERD

competative inhibitor of H2

Front 22

Adverse effects of Cimetidine

Back 22

inhibits CP450 --> slow metabolism of other drugs

binds androgen receptors --> gynecomastia, low sperm, galactorrhea

Front 23

Serotonin:
number of 5-HT receptors
what is special about 5-HT3?

Back 23

7 receptors
6 are G-protein coupled
1 is ligand gated (5-HT3)

Front 24

Sumatriptan

Back 24

5-HT 1d/1b
use: migranes

Front 25

Meto-clo-pramide

Back 25

5-HT4
use:contraction of GI in digestive problems

Front 26

Cisapride

Back 26

5-HT4
long longer used due ot AE: cardiac problems

Front 27

Tegaserod

Back 27

5-HT4
use: irritable bowel syndrome + constipation

** AE: taken off market

Front 28

Cypro-heptadine
use:

Back 28

5-HT2 receptor antagonist
also H1 blocker

use:
rhinitis
urticaria
dermatographism
tx of smooth muscle for carcinoid cancer
tx seritonin syndrome

Front 29

Ondansetron
Granisetron
Palonosetron
Dolasetron

Back 29

5-HT3 antagonist ***
use: severe nausea and vomiting with cancer chemo.

Front 30

Alkaloids affect 3 types of receptors. Name them.

Back 30

alpha-adrenoreceptors
dopamine receptors
5-HT receptors

Front 31

Ergotamine
Dihyro-ergototamine

use:

Back 31

Ergot alkaloids:
use: migranes

Front 32

Bromocriptine
Cabergoline

Back 32

ergot alkaloid
use: hyperprolactinemia

Front 33

Oxytocin
Ergonovine maleate

Back 33

ergot alkaloid
use: postpartum hemorrage

Front 34

Ergonovine

Back 34

ergot alkaloid
use: variant angina- provokes coronary artery spasm

Front 35

Identify the main eicosanoid subgroups

Back 35

prostaglandins
prostacyclines
thromboxanes
leukotrienes

Front 36

What is the main source of eicosanoids?

Back 36

arachnodonic acid (20 C, 4 dbl bonds)

Front 37

Identify the 2 major pathways in synthesis of eicosanoids

Back 37

1. cyclo-oxygenase
2. lipoxygenase

Front 38

cyclooxygenase (COX) initiates biosynthesis of _____.

Back 38

prostaglandins
prostacyclins
thromboxanes

Front 39

lipopxygenases synthesize _____.

Back 39

leukotrienes

Front 40

COX-1 vs. COX-2
function:

Back 40

COX1: involved in homeostasis

COX2: found in inflammatory cells, induced by inflammatory stimuli

Front 41

Leukotrienes LTC4 and LTD4
function

Back 41

bronchoconstrictors
secreted in asthma and anaphylaxis

Front 42

eicosanoids:
MOA:
contractile effects on smooth muscle mediated by _____.

relaxing effects mediated by ______.

Back 42

contractile--> Ca2+

relaxing --> cAMP

Front 43

Dinoprostone (PGE2)
use:

Back 43

ripen cervix before induction of labour by oxytocin

Front 44

Dinoprostone + carboprost tromethamine

Back 44

abortifacients

Front 45

Misoprostol
Mifepristone
Methotrexate

Back 45

abortifacient

Front 46

Alprostadil (PSE1) ***

Back 46

maintain patency of ductus arteriosis

Front 47

Prostacyclin (PGl2)

Back 47

severe pulmonary hypertension
prevent platlet aggregation in dialysis

Front 48

Misoprostol

Back 48

prevent peptic ulcers in patients taking NSAIDS for artritis

Front 49

Alprostadil (PGE1)

Back 49

used in impotence

Front 50

Latanoprost
Bimatoprost
Travoprost
Unoprostone

Back 50

PGF2a
used for glaucoma

Front 51

identify 2 ways to inhibit leukotriene pathway

Back 51

1. inhibit 5-lypoxygenase
2. inhibit binding of LTD4 to receptors

Front 52

Zileuton

Back 52

inhibits 5-lypoxygenase

Front 53

Zafirlukast
Montelukast

Back 53

inhibit binding of LTD4

Front 54

corticosteroids
MOA:

Back 54

inhibit production of arachnodonic acid by phospholipase

inhibits COX2

Front 55

NSAIDS
use:

Back 55

anti-inflammatory
inhibits cyclo-oxygenase