Inflammation Terlecky1

Question 1

What enzyme is responsible for histamine formation?

Answer 1

histidine decarboxylase

Question 2

What cofactor does the enzyme histidine decarboxylase require?

Answer 2

pyridoxal phosphate (activated vitamin B6)

Question 3

Histamine promotes WHAT?

Answer 3

*Vasodilation, smooth muscle contraction, increased vascular permeability, gastric secretion.

also, platelet aggregation, complement activation, mucous secretion, chemotactic attractant for inflame cells

Question 4

How does histamine exist in the blood?

Answer 4

complexed with heparin and proteoglycans in metachromatic secretory granules in basophils. slow turn over.

Question 5

What enzymes degrade histamine?

Answer 5

histamine n-methyltransferase (withMOA) converts to MIAA

or directly to imidazole acetic acid by diamine oxidase (histaminase)

Question 6

The release of histamine is energy dependent… what mediates this?

Answer 6

ATP and Ca+2!

Question 7

What does cromolyn sodium do?

Answer 7

blocks the influx of divalent ions (and so, histamine release). prophylactic tx of asthma

Question 8

What do compound 48/80 and polymixin B do?

Answer 8

Ionophores! soooo influx of ca andrelease of histamine

Question 9

Where do we find H1 receptors?

Answer 9

Smooth muscle of gut and bronchi, endothelium, brain.

Question 10

How do H1 receptors elicit their effects?

Answer 10

second messengers IP3, DAG, Ca2+, NFB

Question 11

where do we find h2 receptors?

Answer 11

Gastric mucosa (parietal cells), cardiac muscle cells, mast cells, brain.

Question 12

H2 post receptor mechanism?

Answer 12

cAMP production

Question 13

What are the cardiovascular effects of histamine?

Answer 13

Increased HR (via H2) decreased blood pressure (due to vasodilator effects H1)

Question 14

How does histamine cause itching?

Answer 14

H1 receptor mediated stimulation of sensory nerve endings

Question 15

What is an example of a physiological antagonist to histamine?

Answer 15

epinephrine! important for cases of systemic anaphylaxis

Question 16

How do inverse agonists work?

Answer 16

Block histamine receptors!

Question 17

What is the difference between first generation antihistamines and second gen anti histamines?

Answer 17

Sedative effects!!! 2nd gen do not have access to CNS

Question 18

What are examples of first generation antihistamines(h1 blocker)?

Answer 18

diphenhydramine and chlorpheniramine
(dimenhydrinate, hydroxyzine, meclizine, promethazine)

used to reduce symptoms of allergy, allergic rhinitis, uticaria

Question 19

2nd gen example/

Answer 19

loratadine, fexofenadine, desloratadine, cetirizine, levocabastine, acrivastine

Question 20

What is gastrin?

Answer 20

polypeptide hormone, secreted from mucosa of gastric antrum in response to eating or alkanization of the stomach. Causes gastric secretion of pepsin, HCl, promotes growth of GI mucosa

Question 21

WHat is pepsin?

Answer 21

Proteinase of gastric juice- elaborated and secreted by chief cells

Question 22

what is zollinger Ellison syndrome?

Answer 22

gastrin secreting tumor!

Question 23

How do we treat ulcerative and inflammatory GI diseases?

Answer 23

Neutralize the acid! reduce gastric acid secretion! enhance mucosal defenses through cytoprotective/antimicrobial intervention

Question 24

How do antacids also confer mucosal protection?

Answer 24

Stimulate mucosal prostaglandin production

Cytoprotective by binding irritating compounds

Question 25

examples of antacids

Answer 25

sodium bicarb, magnesium hydroxide, aluminum hydroxide, calcium carbonate, magnesium trisilicate

Question 26

what are three agonists that control gastric acid secretion?

Answer 26

histamine, acetylcholine, gastrin

Question 27

Antihistamines do what?

Answer 27

They are h2 antagonists, promote the healing of gastric and duodenal ulcers.

Question 28

examples of antihsitamines

Answer 28

cimetidine, famotidine, ranitidine, nazatidine

Question 29

how does omeprazole work?

Answer 29

Proton pump inhibitor! irreversibly inhibits the gastric parietal cell proton pump. Activated in acidic environment

Question 30

what is octreotide?

Answer 30

somatostatin analog that inhibits gastric secretion

Question 31

How do barrier drugs work

Answer 31

forms protective coating on ulcer crater | ex- sucralfate, bismuth subsalicylate

Question 32

What is the drug of choice for ulcers from NSAIDS?

Answer 32

Misoprostol!

Question 33

how does metoclopramide effect gastric motility?

Answer 33

cholinomimetic activity! dopamine antagon! stimulates motility of the upper GI tract without increasing gastric, biliary, pancreatic secretions. increases resting tone of lower esophageal sphincter: accelerates gastricemptying.alsoantiemitic.

Question 34

Metoclopramide side effect?

Answer 34

tardive dyskinesia

Question 35

How do we treat heliobacter pylori infection?

Answer 35

Two antibiotics (amoxicillin and clarithromycin) and a proton pump inhibitor

Question 36

Three basic steps involved in the process of vomiting?

Answer 36

1. Sensors-excitation of one of the many receptors for the diff types of vomiting 2. Vomiting center receives stim from chemoreceptor trigger zone (CTZ) on floor of 4th ventricle (dop agonists here) 3. effector side of response: inc pulse, salivation, dilation. contraction of the pylorusand relaxation of gastric smooth muscle, etc. REFLEX SLOWING of the heart! drop bp,

Question 37

Locally acting emetic?

Answer 37

Ipecac- irritant action on stomach wall and on CTZ

Question 38

what is a centrally acting agent?

Answer 38

Apomorphine! works primarily on CTZ as dopamine agonist

Question 39

where do most anti emetics work?

Answer 39

serotonin 5ht antagonists or neurokinin receptor antagonists at ctz

Question 40

5 ht antag

Answer 40

ondansetron | granisetron

Question 41

neurokinin antag

Answer 41

aprepitant

Question 42

what are the different classes of laxatives

Answer 42

1. irritants/stimulants 2. bulking agents- osmotic and fiber 3. softeners

Question 43

Two categories ofanti diarrheal agents?

Answer 43

motility and water absorption

Question 44

How do stool softeners work

Answer 44

Lubricate! promote laxation by coating and lubricating fecal matter (ex: mineral oil) prevent normal absorptionofwater

Question 45

What does glycerin do?

Answer 45

administered as a rectal suppository. both lubricating and produces local irritation to initiate defecation reflex.

Question 46

Examples of anti-diarrheal motility agents?

Answer 46

Opiates! promote sustained contraction of intestine and interrupt normal organized sequence of peristaltic contractions. exposure time of feces in colon increases and greater dessication occurs ex: loperamide + diphenoxylate/atropine

Question 47

Examples of absorbent anti-diarrheal agents?

Answer 47

Bismuth subsalicylate.. kaolin | absorb water and toxins and provide protective coating to inflamed intestine