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Pharmacology > Lecture 12 - Antihistamines and Respiratory Pharmacology > Flashcards

Lecture 12 - Antihistamines and Respiratory Pharmacology Flashcards

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1
Q

Define

Respiratory diseases

A

Any disease process that interferes with gas exchange in the lungs and causes serious changes in the concentration of oxygen and carbon dioxide in the blood

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2
Q

What causes cystic fibrosis?

A

Mutation in the CFTR gene on chromosome 7. The CFTR gene encodes a chloride channel. Alteration of this channel causes inbalance in salt and liquid homeostasis in epithelia –> mucus buildup

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3
Q

What happens inside the cells with Cystic Fibrosis?

A

Sodium enters the cells normally but chloride is unable to exit the cell leading to extra water entering the cell

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4
Q

Treatments of Cystic Fibrosis

A

1) Bronchodilators
2) Mucolytics to thin secretions
3) Antibiotics (against mucin fermenting bacteria)
4) Bronchoscopy with bronchoalveolar lavage to clear mucus plugs from intermediate and small airways

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5
Q

Define

Degranulation

A

A cellular process of immune cells that release inflammatory mediators or antimicrobial cytotoxic molecules from secretory granules

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6
Q

What are some of the substances immediately released when mast cells degranulate?

A

Histamine, heparin, serotonin, leukotrienes, platelets, cytokines, and eosinophil-activating factors

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7
Q

Function of Histamine

A

Histamine interacts with the membrane receptors in certain tissues to produce the symptoms of allergy (itching, redness, hives, stuffy nose)

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8
Q

Pathophysiology of the IgE-mediated hypersensitivity reaction

A

1) The first time a person comes into contact with an allergen, B cells produce antobodies (ex IgE)
2) IgE binds to Fc receptors on mast cells –> sensitization
3) Repeated exposure to an allergen will cross-link two IgE and trigger mast cell degranulation

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9
Q

How can an allergic reaction be blocked?

A
  • Preventing mast cells from releasing contents
  • Blocking the H1 receptors
  • Antibodies like Omalizumab that blocks IgE from binding to receptors
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10
Q

Mast Cell Stabilizers

Cromolyn

A

A prophylactic drug that acts selectively on the mast cells to inhibit IgE-mediated hypersensitivity reaction by preventing the antigen-stimulated release of histamine (also prevents release of leukotrienes and inhibits eosinophil chemotaxis)

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11
Q

When is cromolyn administered?

A

Before release of histamine

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12
Q

Where is histamine metabolized?

A

In the liver

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13
Q

Classical Monoamines

Imidazoleamines

A

Histamine

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14
Q

Classical Monoamines

Catecholamines

A

Adrenaline (EPI), Dopamine (DA), Noradrenaline (NE)

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15
Q

Classical Monoamines

Indolamines

A

Serotonin (5-HT), Melatonin (MT)

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16
Q

Histamine Receptors

What type of receptors are Histamine Receptors?

A

GPCRs

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17
Q

Histamine Receptors

H1 receptors

A
  • Found on skin capillaries, bronchiolar smooth muscle, nerve ending, brain, and intestinal smooth muscle
  • Gq/11 –> increased IP3, DAG, and intracellular Ca2+, activated NFkB
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18
Q

Histamine Receptors

H2 receptors

A
  • Found in stomach, heart, blood vessels, mast cells and uterine tissue
  • Gs –> increased cAMP
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19
Q

Histamine Receptors

H3 receptors

A
  • Found in CNS and some peripheral nerves
  • Gi/0 –> Decreased cAMP
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20
Q

Histamine Receptors

H4 receptors

A
  • Found in hematopoietic cells and gastric mucosa
  • Gi/0 –> decreased cAMP, increased intracellular Ca2+
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21
Q

Define

Antihistamines

A

Prevent interaction between histamines and histamine receptors
- not effective for asthma

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22
Q

Define

Antiallergic agents

A

Block the release of histamine from mast cells

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23
Q

Physiological response to histamine stimulation

Blood pressure

A
  • Hypotension
  • Receptors: H1, H2
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24
Q

Physiological response to histamine stimulation

Heart rate

A
  • Rapid heartbeat
  • H2
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25
# Physiological response to histamine stimulation Bronchioles
- Breathing difficulty (constriction) - H1
26
# Physiological response to histamine stimulation Intestines
- Constipation/diarrhea - H1
27
# Physiological response to histamine stimulation Skin capillaries
- Dilation, edema, redness, flare - H1
28
# Physiological response to histamine stimulation Nerves in spinothalamic tract
- Itching in specific fibers - H1
29
# Physiological response to histamine stimulation Gastric acid secretion
- Increased, nausea, heartburn - H2
30
Effects of histamine on blood vessels
- Temporary decrease in blood pressure - Hives - Angiodema
31
Effects of histamine on extravascular smooth muscle
- Intestinal disturbances, constipation - bronchoconstriction
32
# Define Antihistimine H1 antagonists
- Used to relieve the symptoms of allergic reactions after histamine has been released - Blocks histamine from binding to H1 receptors - Characterized into first generation and second generation
33
Antihistamines as inverse agonists
They bind and stabilize the inactive conformation of the H1 receptor which shifts the equilibrium toward the inactive receptor state
34
# Define First generation antihistmines
Non-selective interaction with peripheral and CNS histamine receptors, has a sedating effect Examples: Brompheniramine, chlorpheniramine, diphenhydramine, promethazine
35
# Define Second generation antihistamines
More selective for peripheral H1 receptors, not as sedating, less anticholinergic activity Ex cetirizine (claritin), fexofenadine, loratadine
36
# Define Third generation antihistamines
To develop therapeutically active metabolites that are devoid of cardiac toxicity Ex Fexofenadine, levocetirizine
37
Routes of administration for antihistamines
- Oral - Topical - Nasal spray - Eye drops | Not very effective for anaphylaxis and asthma
38
Asthma triggers
- Allergens - air pollutants - infections - exercise
39
Characteristics of asthma
- Bronchoconstriction - shortness of breath - wheezing - veiwed as an inflammatory disease
40
Leukotrienes in asthma
The most potent bronchoconstrictor
41
Zileuton
5-lipoxygenase inhibitor
42
Montelukast and Zafirlukast
CysLT1 receptor antagonist
43
Role of the Autonomic Nervous System in Asthma
1) Bronchodilation produces sympathetic stimulation 2) parasympathetic stimulation produces bronchoconstriction and increased mucus secretion 3) SYMPATHOMIMETIC drugs decrease parasympathetic activity (muscarinic antagonists, theophyline)
44
Asthma Treatments
1) Bronchodilator drugs 2) anti-inflammatory drugs 3) anti-allergic agents 4) Mucokinetics: mucolytics and expectorants
45
# Bronchodilator Drugs Non-selective Beta-adrenergic drugs (agonists)
Epinephrine and isoproterenol - stimulate beta-1 and beta-2 adrenergic receptors - may cause tachycardia and cardiac arrhythmias
46
# Bronchodilator Drugs Selective beta-2 adrenergic drugs
Albuterol, salmeterol, formoterol (long-lasting) - Used in chronic asthma and COPD - prevent mediators from being released by mast cells
47
# Bronchodilator Drugs Anticholinergics (antagonists)
- Blocks action of acetylcholine - not as potent as Beta-drugs - lowers volume of respiratory secretions - considered first line drugs for COPD - EX Ipatropium Bromide (Atrovent)
48
Methylxanthine drugs - Examples
Theophylline, caffeine, theobromine
49
Methylxanthine drugs - Mechanism of action
- Inhibits phosphodiesterase --> increased cAMP - Bronchodilating, increased respiratory contractility and mucociliary clearance
50
# Anti-inflammatory drugs Corticosteroids
- Most potent - interferes with all stages of the inflammatory and allergic response (antibody production, immune cell activity, release of mediators) - inhibits the inflammatory response that occurs in the respiratory airways
51
# Anti-inflammatory drugs Leukotriene inhibitor drugs - Zileuton
- Prevent synthesis of leukotriene - used in the chronic control of asthma
52
# Anti-inflammatory drugs Leukotriene receptor antagonist (CysLT1 receptor)
Montelukast and zafirlukast
53
# Antiallergic agents Cromolyn sodium
- Interferes with the antigen-antibody reaction to release mast cell mediators - Administered by inhalation, ingestion, or as an eye solution - Acts prophylactically, does not help an asthma attack that has started
54
# Antiallergic agents Omalizumab
- Binds to and inactivates IgE - reduces the severity and frequency of allergic asthma attacks
55
# Mucokinetics Mucolytics
- Liquefy bronchial mucus - enable removal of mucus by coughing or suction apparatus - N-Acetylcysteine (NAC) - breaks down the glycoproteins in bronchial secretions
56
# Mucokinetics Expectorants
- Facilitates removal of thickened mucus from the lungs and helps liquefy the mucus - Guaifenesin - used to provide relief of unproductive coughing - Signals the body to increase the amount or hydration of secretions, lubricates the irritated respiratory tract
57
How does Mucolytics affect the mucus mesh?
- Treatment with hypertonic saline increases the spacing within the mucus mesh - Treatment with NAC breaks disulfide bonds within the network of the mesh
58
What is N-Acetylcysteine (NAC)?
- Mucolytic agent and management of acetominophen poisoning - derivative of cyysteine with an acetly group attached to the amino group of cysteine - a pro-drug that is converted into cysteine and absorbed into the blood stream - replenishes glutathione stores
59
# Overall preferred therapy for Asthma Mild intermittent Asthma
- Beta-2 bronchodilator
60
# Overall preferred therapy for Asthma Mild Persistent Asthma
- Corticosteroid - Cromolyn - Anti-leukotriene
61
# Overall preferred therapy for Asthma Moderate Persistent Asthma
- Corticosteroids - Beta-2 bronchodilator
62
# Overall preferred therapy for Asthma Severe Persistent Asthma
- Corticosteroid - Beta adrenergic bronchodilator - anti-leukotriene

Pharmacology (23 decks)

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