Pharmacology Flashcards

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1
Q

Name the 1st generation H1-blockers (antihistamines)

A
  • Diphenhydramine
  • Dimenhydrinate
  • Chlorpheniramine
  • Doxylamine
  • AMine
  • Hydrinate
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2
Q

What are the uses of 1st generation H1-blockers (antihistamines)?

A
  • Allergy
  • Motion sickness
  • Vomitting in pregnancy
  • Sleep aid
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3
Q

What are the adverse effects of 1st generation H1-blockers (antihistamines)?

A
  • Sedation
  • Antimuscarinic
  • Anti-alpha adrenergic
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4
Q

NAme the 2nd generation H1-blockers (antihistamines)?

A
  • Loratadine
  • Fexofenadine
  • Desloratadine
  • Cetirizine
  • Mostly end in “-adine”
    Setirizine is Second gen
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5
Q

What is the clinical use of 2nd generation H1-blockers (antihistamines)?

A

Allergy

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6
Q

What is the advantage of 2nd generation H1-blockers (antihistamines)?

A

Far less sedating than 1st generation because of decreased entry into CNS

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7
Q

What is dextromethorphan used for clinically?

A

Antitussive - (cough medicine)

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8
Q

What are the adverse effects of dextromethorphan?

A
  • Opioid effects (naloxone given in overdose)

- Serotonin syndrome if combined w. other serotonergic agents

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9
Q

What does dextromethorphan bind to?

A

Antagonises NMDA glutamate receptors

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10
Q

What is dextromethorphan a synthetic analog of?

A

Codeine

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11
Q

What is the mechanism of action of pseudoephedrine and phenylephrine?

A

Activates alpha-adrenergic receptors in nasal mucosa -> vasoconstriction

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12
Q

What is the clinical use of pseudoephedrine and phenylephrine?

A
  • Reduce hyperemia
  • Edema (used as nasal decongestant)
  • Open obstructed eustachian tubes
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13
Q

What are the adverse effects of pseudoephedrine and phenylephrine?

A
  • Hypertension
  • Rebound congestion (rhinitis medicamentosa) if used for more than 4-6 days)
  • Tachyphylaxis
  • CNS stimulation and anxiety (pseudoephedrine)
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14
Q

What are examples of muscarinic agonists (used in asthma and COPD)?

A
  • Tiotropium (long acting)

- Ipratropium

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15
Q

What is the MOA of muscarinic agonists (ipratropium and tiotropium)?

A

Competitively block muscarinic receptors preventing bronchoconstriction

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16
Q

What are examples of inhaled corticosteroids?

A
  • Fluticasone

- Budesonide

17
Q

What is the MOA of inhaled corticosteroids?

A

Inhibit the synthesis of virtually all cytokines

- Inactivate NF-kB, the transcription factor that induces production of TNF-alpha and other inflammatory agents

18
Q

What is albuterol?

A

Short acting B2-agonist

19
Q

What is Formoterol?

A

Long-acting B2-agonist

20
Q

What are Montelukast and Zafirlukast and what receptor do they block?

A

Antileukotrienes

- Block leukotriene receptors (CysLTI)

21
Q

What is Zileuton?

A

Antileukotriene

- 5-Lipoxygenase pathway inhibitor (blocks arachadonic acid -> leukotrienes)

22
Q

What is the major adverse effect of Zileuton (5-Lipoxygenase pathway inhibitor)?

A

Hepatotoxic

23
Q

What are Montelukast and Zafirlukast especially good for treating?
- Antileukotrienes, Block leukotriene receptors (CysLTI)

A

Aspirin-induced and exercise-induced asthma

24
Q

What does Omalizumab bind to?

A

Binds mostly to unbound serum IgE and blocks binding to FcERI

25
Q

What is an example of a Methylxanthine?

A

Theophylline

26
Q

What is the MOA of Methylxanthines (e.g. Theophylline)?

A

Bronchodilation by inhibiting phosphodiesterase -> incr cAMP levels due to to decreased cAMP hydrolysis

27
Q

What are Methylxanthines (e.g. Theophylline) metabolised by?

A

Cytochrome P-450

- Leads to narrow therapeutic index

28
Q

What are the adverse effects of Methylxanthines (e.g. Theophylline)?

A
  • Cardiotoxicity, neurotoxicity (narrow therapeutic index)

- Also blocks the action of adenosine

29
Q

What is an example of a chromone (prevents mast cell degranulation - rarely used)?

A

Cromolyn

- Prevents acute asthma symptoms

30
Q

What are examples of Anti-IL-5 monoclonal therapies?

A
  • Mepolizumab, Reslizumab - IL-5

- Benralizumab - IL-5, receptor alpha

31
Q

What is the MOA of Anti-IL-5 monoclonal antiB?

A

Prevents eosinophil differentiation, maturation, activation and survival mediated by IL-5 stimulation

32
Q

What are Anti-IL-5 monoclonal therapies (Mepolizumab, Reslizumab, Benralizumab) used for?

A

Maintenance therapy in severe eosinophilic asthma