3.1 Bee stings, dander, and greasy cheeseburgers

Question 1

clinically relevant histamine synthesis Circulating granulocytes of the immune system-

Answer 1

basophils

Question 2

clinically relevant histamine synthesis tissue resident granulocytes of the immune system

Answer 2

mast cells

Question 3

clinically relevant histamine synthesis in the central nervous system that use histamine as a neurotransmitter-

Answer 3

neurons

Question 4

clinically relevant histamine synthesis in the gastric mucosa-

Answer 4

enterochromaffin-like cells

Question 5

Pyridoxal 5 phosphate the active form of B6 is a coenzyme that makes ______ from_____.

Answer 5

histamine histidine

Question 6

the slow turning over pool of histamines synthesis and storage-

Answer 6

mast cells and basophils

Question 7

Histamine is stored in the granules in these inflammatory cells-

Answer 7

mast cells and basophils

Question 8

A complete degranulation of these cells releases histamine

Answer 8

mast cells and basophils

Question 9

Release of histamine(degranulation) from mast cells and basophils is triggered by-

Answer 9

allergic processes-anaphylaxis or cell destruction

Question 10

the rapidly turning overpool/made on demand histamine synthesis and storage-

Answer 10

gastric mucosa-enterochromaffin-like cells

And neuron

Question 11

enterochromaffin-like cells And neuron do or do not store histamine?

Answer 11

do not store histamine

Question 12

Synthesis on demand involves up regulation induction of ?

Answer 12

histidine decarboxylase

Question 13

degranulation triggered by allergic processes, anaphylaxis(immunological release), IGE mediated hypersensitivity reaction requires what?

Answer 13

energy and calcium(exocytosis)

Question 14

Cellular injury or destruction by trauma(mechanical release), cytolytic release and chemically mediated release by peptides toxins or venoms, Does or does not require energy

Answer 14

does not require energy

Question 15

Triggered by allergic processes, anaphylaxis(immunological release), ige mediated hypersensitivity reaction, happens due to exposure of the appropriate antigen, requires energy and calcium(exocytosis)?

Answer 15

degranulation of mast cells /basophils

Question 16

Allergy induced mast cell degranulation requires¬______separate exposures to the allergen

what happens during the initial exposure?

what happens with the subsequent exposure?

Answer 16

two

initial exposure, b lymphocytes secrete allergen specific IgE antibodies. IgE molecules bind to FCeRI receptors on mast cells/basophils

subsequent exposure, allergen binds to the IgE/Fc receptor complexes on the mast cell surface and causes degranulation

Question 17

Ige mediated hypersensitivity reaction is the key feature of what condition?

Answer 17

asthma

Question 18

Name some drugs they prevent mast cell degranulation and the release of inflammatory mediators such as histamine, leukotrienes and cytokines-

Answer 18

Cromolyn
Nedocromil
Albuterol, Metaproterenol-beta two agonist

Question 19

histamine release causes five things. list them

Answer 19

vasodilation
increase vascular permeability, leading to edema
sensitization and activation of peripheral nerve endings
contraction of bronchial smooth muscle
contraction of gastrointestinal smooth muscle

Question 20

the triple response(red spot, edema, flare-involves what three cell types?

Answer 20

activation of histamine H1 receptor cells

• on the vascular endothelial cells-leads to endothelial cell contraction it causes increased capillary permeability edema, NO production causes relaxation of the vascular smooth muscle
• on vascular smooth muscle dilation of terminal arterioles, venous constriction-redness and erythema
• on sensory nerve endings depolarization of afferent nerve terminals causes sensization-which leads to tingling itch pain(flare)

Question 21

the H1 receptor is coupled with what type of G protein?

Answer 21

GQ
Phospholipase c 
IP3 
Dag
increase intracellular calcium

Question 22

Mast cell release of histamine activates Histamine H1 receptors, what does that do to peripheral nociceptors?

Answer 22

Lowers the threshold for action potential generation/sensitizes

direct depolarizing action on afferent nerve terminals-Activation of peripheral nerve endings(nociceptors)

Question 23

What four places does histamine cause contraction of smooth muscle cells?

Answer 23

lung
gastrointestinal tract
the iris
the uterus

Question 24

An ige mediated hypersensitivity reaction initiated by a previously sensitized individual the causes hypotension, bronchoconstriction, epiglottal swelling is termed?

Answer 24

Anaphylaxis

Question 25

a disorder characterized by mass cell proliferation and accumulation within various organs most commonly the skin

Answer 25

mastocytosis

Question 26

Name 5 situations in which a patient might have excess histamine

Answer 26

``` Mastocytosis Myelogenous leukemia carcinoid tumors histamine fish poisoning red wine consumption ```

Question 27

Histamine as a neurotransmitter in the CNS is important for what? 3

Answer 27

sleep wake cycle/circadian rhythm cognitive processes/attention, memory, learning feeding behavior/appetite suppression

Question 28

H1 antihistamines Are called inverse agonist why?

Answer 28

they turn down the basil rate/bind and stabilize the inactive confirmation of the H1 receptor, thereby shifting the equilibrium towards the inactive receptor state they do not inhibit or block the release of histamine they are reversible and competitive

Question 29

Benadryl is not selective for the H1 receptors what other receptors does it block at therapeutic doses

Answer 29

muscarinic -may lead to dry mouth blurred vision drowsiness or urinary retention A adrenergic Serotonergic can be used to prevent motion sickness and PONV

Question 30

promethazine/Phenergan readily crosses the blood brain barrier and besides H1 what receptors can it block

Answer 30

muscarinic | dopamine

Question 31

If someone had Meniere’s Disease/disorder of the inner ear, what might you give them to prevent motion sickness and PONV?

Answer 31

promethazine/Phenergan Benadryl also helpful in treating motion sickness and migraine related nausea and vomiting from chemotherapy

Question 32

which second generation antihistamine H1 is a prodrug

Answer 32

loratadine/Claritin

Question 33

Why do H1 antihistamines have limited effectiveness in asthma?

Answer 33

asthma bronchoconstriction is largely mediated by leukotrienes and cytokines

Question 34

h2 is what type of G protein? | Where are H2s found? 4

Answer 34

``` GS gastric parietal cells cardiac muscle mast cells brain ```

Question 35

gastrin released from G cells where? | 4

Answer 35

Pyloric antrum Stomach Duodenum Pancreas

Question 36

meal stimulated acid secretion is stimulated by

Answer 36

gastrin acetylcholine histamine

Question 37

Highly selective H2 receptor antagonist, reversibly bind, competitive antagonist. 3

Answer 37

Cimetidine Ranitidine Famotidine

Question 38

Effective and inhibiting nocturnal acid secretion, but only modest impact on meal stimulated acid secretion

Answer 38

Cimetidine Ranitidine Famotidine

Question 39

Adverse side effects include confusion, hallucinations, bradycardia, and hypotension.

Answer 39

Cimetidine Ranitidine Famotidine Adverse effects usually associated with IV administration rapidly

Question 40

What was the random ass H2 antihistamine from the slide that no one's ever heard of that's eliminated primarily by the kidney?

Answer 40

Nizatidine

Question 41

Decreased absorption of ketoconazole is caused by?

Answer 41

Cimetidine Ranitidine Famotidine

Question 42

Patients with liver or kidney failure require lower doses of what three drugs

Answer 42

Cimetidine Ranitidine Famotidine

Question 43

blocks renal organic cation transporter 2 to decrease renal tubular secretion of metformin, atenolol, procainamide, propranolol

Answer 43

cimetidine

Question 44

Inhibit CYPs it can increase the levels and therefore prolong the effects of drugs metabolized by these enzymes, such as acetaminophen, alfentanil, fentanyl, sufentanil, lidocaine, methadone, versed, dexamethasone *propofol(maybe)

Answer 44

cimetidine

Question 45

prodrugs, Convert to reactive sulfonamide form in acidic environments, covalently bind to the hydrogen potassium ATP as proton pump, decrease acid production by 80 to 95%,

Answer 45

proton pump inhibitors

Question 46

Why are proton pump inhibitors preferred over H2 antagonist for treatment of peptic ulcer disease?

Answer 46

greater decrease of gastric acid secretion, contribute to eradication of H PYLORI

Question 47

side effects of PPI | 4

Answer 47

Decrease B12, Iron, calcium, magnesium, absorption modest increase of risk of hip fracture increase risk of C diff increased enteric infections

Question 48

how are proton pump inhibitors metabolized?

Answer 48

CYP | Reduce dose in severe hepatic impairment

Question 49

what receptors do reglan hit?

Answer 49

D2 5 H T3 Increased acetylcholine release