Pharmacology Exam 1

mast cells

Histamine is primarily stored in vesicles of what cells?

morphine, antibiotics

Common drugs that can cause histamine release

wheal and flare

Histamine in the epidermis can cause what kind of response?

mucous membranes

What kind of tissue are mast cells located?

prone to injury

Mast cells are located in tissues that are _ _ _.

basophils

Major site of histamine in the blood.

relaxation

What impact does H1 receptor activation on vascular endothelium have on smooth muscle?

vasodilation

What happens to vasculature upon H1 receptor activation?

increased

How is the permeability of capillaries impacted by histamine release?

edema

What is the side effect of increased capillary permeability?

contract

Do bronchial smooth muscles relax or contract upon H1 activation?

Lewis Triple Response

Another name for Triple Response of Lewis

direct H1 vasodilation

What forms the initial red spot seen at the injection site in a Lewis Response?

indirect H1 vasodilation

What forms the flare seen at the injection site in a Lewis Response?

edema

What forms the wheal seen at the injection site in a Lewis Response?

allergic rhinitis, urticaria

H1 receptor antagonists (H1RA) can be used to treat what?

competitive

H1RAs are what kind of antaonists?

T

T/F Some H1RAs are inverse agonists.

1st gen

What has more CNS distribution? 1st gen or 2nd gen H1RAs?

antimuscarinics, opioids, sedatives, alcohol

What classes of drugs are additive with 1st gen H1RAs

1 hr before motion

When should H1RAs for motion sickness be administered?

dimenhydrinate, cyclizine, meclizine, promethazine

What H1RAs are for motion sickness?

dimenhydrinate, meclizine

H1RAs used for vertigo

diphenhydramine

H1RA used for sedation

acute attacks

H1RA should NOT be used alone to treat _______________ in asthma.

1st gen, crosses BBB

Which generation is better at treating motion sickness and why is that?

allergic rhinitis, motion sickness, vertigo. sedation

4 uses for H1RAs

asthma, anaphylaxis, angioedema, contact dermatitis

4 conditions where H1RAs are non-primary treatment

F

T/F H1RAs are effective at treating common cold.

SOB, chest tightness, wheezing, coughing

4 clinical features of asthma

IgE

What is synthesized upon allergen exposure?

mast cells

Where does IgE act causing sensitization?

histamine, PGD2, leukotriene, tryptase, PAF

Mediators that lead to bronchoconstriction

edema, mucus hypersecretion, smooth muscle contraction, late asthmatic response

What are the responses to eosinophil and neutrophil activation?

allergen, pathological mucus, IL-5/13, airway changes, IgE, eosinophils, mast cells, basophils

Key inflammatory mediators and factors in asthma

large mucus layer with goblet cells, enlarged smooth muscle, much more WBCs

Structural changes in airway is asthma

beta agonists, methylxanthines, tiotropium

What drug classes target smooth muscle?

inhaled corticosteroids

What drug classes target inflammatory mediators?

cromones

What drug classes target mast cells?

What drug classes target IL-5/13

airway obstruction, inflammation, hyper-responsiveness

Big 3 pathophysiological occurrences in asthma

eosinophils

What cell type is seen in asthma but not COPD?

neutrophils, macrophages, cytotoxic T cells

Inflammatory mediators in COPD

small airways

What is predominantly affected in COPD?

fibrosis, emphysema

What kinds of damage can occur to the small airways in COPD?

destruction of alveolar walls

What is emphysema?

expiration

In COPD is airway obstructed on inspiration or expiration?

air trapping, hyperinflation

In COPD, closure of the airway upon expiration leads to what?

floppy airway, inflamed mucus membrane, wall thickening, inelastic muscle fibers, exudate present

Physical description of a COPD airway

COPD

COPD or Asthma?: Progressively worsening airflow obstruction

asthma

COPD or Asthma?: Improvement with bronchodilators and steroids

COPD

COPD or Asthma?: Maintenance with bronchodilators

asthma

COPD or Asthma?: IgE mediated

COPD

COPD or Asthma?: Neutrophils, macrophages, cytotoxic T cells, lymphocytes

asthma

COPD or Asthma?: Reversibility with treatment

COPD

COPD or Asthma?: Alveolar destruction, mucus hypersecretion, fibrosis

asthma

COPD or Asthma?: Airway remodeling

COPD

COPD or Asthma?: Emphysema

oral first pass metabolism

Why is inhalation the best drug delivery method in COPD and asthma?

10-20%

About what percentage of drug actually enters the lower airway with an inhaler?

B2 receptors on bronchial smooth muscle

Site of action of β-2 agonists

PDE in bronchial smooth muscle

Site of action of theophylline

methylxanthine

Drug class of theophylline

M3 receptors on bronchial smooth muscle

Site of action of anticholinergic agents

cAMP

The bronchodilator response from beta 2 agonist is due to an increase in __________.

cAMP

Theophylline inhibits PDE to increase levels of____.

adenosine

Theophilline can also inhibit what receptors to reduce bronchoconstriction?

acetylcholine

Muscarinic antagonists inhibit what neurotransmitter to reduce bronchoconstriction?

reduced mediator release from mast cells, prevent microvascular leakage to reduce edema, enhance mucociliary clearance, inhibit acetylcholine release

Indirect effects of β-2 agonists

exercise, cold air, allergens

Common asthma triggers that SABAs protect against

B2 agonists

Best bronchodilator option in treating acute severe asthma.

R

What isomer of albuterol is levalbuterol?

F

T/F Levalbuterol is seen to have better efficacy and lower toxicity then albuterol when treating asthma and COPD.

rifaximin

Recommended antibiotic for Traveler’s diarrhea prophylaxis

none, rehydration

Antibiotics used for treatment of mild traveler’s diarrhea

azithromycin, rifaximin, rifamycin

Antibiotics used for treatment of moderate traveler’s diarrhea

antibiotics + loperamide

Treatment for severe traveller’s diarrhea

can cause reye’s syndrome

Why is bismuth subsalicylate not used in young children

black stool and tongue

Visual adverse effect of bismuth subsalicylate use

balance microflora

How do probiotics assist in treating diarrhea

Lactobacillus GG, S. boulardii

Species where probiotics are an effective option

Imodium

Name brand of loperamide

stimulate mu and d opioid receptors in GI tract

What is the mechanism of loperamide?

T

T/F Loperamide is much more potent then morphine as an antidiarrheal, more effective than diphenoxylate and diphenoxin

stimulates mu and d opioid receptors in GI tract

Mechansim of diphenoxylate and difenoxin

difenoxin

What is the active drug: Diphenoxylate or difenoxin

anticholinergic

What is the drug category of atropine?

atropine

What is combined with diphenoxylate to decrease GI motility and reduce abuse potential?

T

T/F At high doses diphenoxylate can cross the BBB

sedation, constipation, toxic megacolon

Adverse effects of diphenoxylate

dry mouth, blurred vision, etc

Anticholinergic effects caused by atropine

Paregoric

Name brand of camphorated tincture of opium

0.4mg/mL

Morphine equivalent concentration of camphorated tincture of opium

Laudanum

Name brand of deodorized tincture of opium

10mg/mL

Morphine equivalent concentration of 10% deodorized tincture of opium

abuse potential, overdose

Why are tinctures of opium and codeine not preferred to treat diarrhea?

Viberzi

Name brand of eluxadoline

eluxadoline

Generic of Viberzi

IBS with diarrhea

Indication of eluxadoline

mu, k receptor agonist and d opioid receptor antagonist

MOA of eluxadoline