Pharmacology Exam Iv (Fall 2006) (Card Set #1)

Front 1

Sometimes called autocoids, few clinical applications. Selective agonists and atagonists are clinically useful.

Back 1

Histamines

Front 2

How are histamines formed?

Back 2

By decarboxylation of amino acid L-histidine by histidine decarboxylase.

Front 3

Where are histamines found?

Back 3

Stored in granules in mast cells or basophils. Bound form is biologically inactive.

Front 4

Where are mast cells especially rich?

Back 4

Sites of potential injury
i.e. nose, mouth, feet, internal body surfaces, and blood vessels.

Front 5

What effects do histamines have on the CNS as a neurotransmitter?

Back 5

Neuroendocrine control, cardiovascular regulation, thermal and body weight and arousal

Front 6

What effects does Histamine have on the stomach?

Back 6

Cells in the fundus of the stomach cause the release of acid from parietal cells of the mucosa.

Front 7

True or False?
Release of His is energy and calcium required.

Back 7

True. His, ATP and other mediators are stored together.

Front 8

Where is negative feedback mediated?

Back 8

It is mediated by H2 receptors found in mast cells in skin and basophils but not in lung mast cells.

Front 9

What can displace Histamine from heparin-protein complex?

Back 9

Amines (morphine, tubocurarine)

Front 10

What causes degranulation and His release?

Back 10

Chemical and Mechanical mast cell injury.

Front 11

What type of release is not associated with mast cell injury or degradation?

Back 11

Chemical release

Front 12

What is compound 40/80?

Back 12

An experimental diamine polymer the induces histamine release from mast cells by exocytotic degranulation requiring energy and calcium.

Front 13

How many receptor subtypes does histamine have?

Back 13

Four

Front 14

What receptors are H1 more similiar to?

Back 14

Muscarinic receptors

Front 15

What receptors are H2 more similar to?

Back 15

Serotonin receptors

Front 16

Where are H1 receptors found?

Back 16

Located in smooth muscle, endothelium, and post synaptic membrane in brain.

Front 17

Where are H2 receptors found?

Back 17

Found in gastric mucosa, cardiac muscle, mast cells, and post synaptic membrane in brain

Front 18

True or False?
Only H1 receptors increase intracellular Ca++

Back 18

False both H1 and H2 receptors increase intracellular Ca++

Front 19

Where are H3 receptors found?

Back 19

On dopamine and GABA PRE-synaptic neurons in the basal ganglia

Front 20

Where are H4 receptors found?

Back 20

Mainly in bone marrow (eosinophils, neutrophils, CD4 cells) and WBC

Front 21

What receptors mediate urticarial response to insect and nettle stings and modulate respiration in some mammals?

Back 21

H1 receptors

Front 22

What effects does Histamine have on the cardiovascular system?

Back 22

Decrease in systolic and diastolic BP, vasodilation, tachycardia and reflex tachycardia.

Front 23

What does direct vasodilation of arterioles and precapillary sphincters cause?

Back 23

Flushing, warmth, headache

Front 24

How does Histine-induced edema occur?

Back 24

H1 mediated in post capillary vessels, actin and myocin contract separating endothelial cells.

Front 25

What are some cardiac effects of Histamine?

Back 25

Increase in contractility and pacemaker in some mammals decrease atrial muscle contractility in humans.

Front 26

Does histamine cause bronchoconstriction?

Back 26

Yes

Front 27

What is the only clinical use for histamine?

Back 27

Diagnose asthma or cystic fibrosis.

Front 28

True or False?
Histamine has significant effects on smooth muscle of the eye, genitourinary tract, and GI tract.

Back 28

False except pregnant women and histamine-induced contractions.

Front 29

At ordinary concentrations, what secretory effects can be seen?

Back 29

Secretion of gastric acid pepsin, and intrinsic factor modulated by H2 receptors.

Front 30

At high concentrations what kinds of secretions can histamine cause?

Back 30

Adrenal medullary discharge.

Front 31

Which receptor has been linked to obesity through increased food intake and decreased energy expenditure in mice?

Back 31

H3 receptors

Front 32

What is the triple resonse?

Back 32

Intradermal injection causes a "wheal and flare" response.
Three cell types; smooth muscle, capillary or venular dilation and sensory nerve endings cause sense of itching, flare caused by axon reflex, and wheal due to edema

Front 33

What two drugs have been shown to have analgesic effects similiar to opiods?

Back 33

Burimamide (H2 blocker)
Improgran (no H1, H2, or H3 activity)

Front 34

Ethanolomines, Ethylaninediamines, piperazine derivates, alkylating derivatives, Phenothiazine derivatives.

Back 34

First generation H1 Antagonists

Front 35

Carbinoxamine (Clistin), Dimenhydrinate (Salt of diphenhydramine; Dramamine), Diphenhydramine (Benadryl), Doxylamine

Back 35

Ethanolamines

Front 36

Ethylaminediamines

Back 36

Pyrilamine (Neo-Antergan), Tripelennamine (PBZ)

Front 37

Hydroxyzine (Atarax), Cyclizine (Marezine), Meclizine (Bonine)

Back 37

Piperazine derivatives

Front 38

Alkylamines derivatives

Back 38

Brompheniramine (Dimetane), Chlorpheniraine (Chlor-Trimeton)

Front 39

Phenothiazine derivatives

Back 39

Promethazine (Phenergan)

Front 40

What are some characteristics of second generation histamine Blockers (H1)

Back 40

Less lipid soluble; do not penetrate the BBB readily.
Longer acting such as meclazine (12-24 hrs), Metabolized by the CYP3A4 system

Front 41

True or False?
H1 receptor antagonists by reversible competitive inhibition?

Back 41

True

Front 42

What are some non specific actions of Histamine blockade?

Back 42

Sedation, antinausea, antiparkinsonism effects, anticholinergic actions, adrenoceptor blockade, serotonin blockade, local anesthesia

Front 43

True or False?
At toxic doses, antihistamines causes stimulation, agitation, and even convulsion in adults

Back 43

True

Front 44

What is the DOC for rhinitis and urticaria?

Back 44

H1 antagonists

Front 45

What drug was used for antinausea and vomitting during pregnancy in the 1970s, but is no longer used because of reports of fetal malformation?

Back 45

Doxylamine

Front 46

What are some common toxic effects of antihistamines?

Back 46

Sedation and antimuscarinic action

Front 47

What are the two mechanisms of action for H2 blockers?

Back 47

1. ECL HIS blocked from parietal cell H2
2. Gastrin or Ach stimulation of parietal cell

Front 48

True or False?
H2 blockers have high incidence of side effects.

Back 48

False
Side effects include diarrhea, headache, fatigue, and constipation and occur in 3% of patients