First Aid: Pharmacology Flashcards

1
Q

What are histamine-1 blockers?

What is the clinical use of their first-generation drugs?

A

They are reversible inhibitors of H1 histamine receptors

They are clinically used for allergies, motion sickness and for sleep aid

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2
Q

What are some adverse effects of first-generation histamine-1 blockers? Name two examples

A

Sedation, antimuscarinic, anti-alpha-adrenergic

Examples: doxylamine, diphenhydramine

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3
Q

What is the clinical use of second-generation Histamine-1 blockers and how do their effects compare to first-generation?

A

Used for allergies, they are far less sedating than the 1st generation due to decreased entry into the CNS

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4
Q

What is the role of Guaifenesin? What doesn’t it do?

A

It is an expectorant that thins the respiratory secretions (mucus) in order to promote mucus drainage! It doesn’t suppress the cough reflex

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5
Q

What is the normal job of a drug that is an ‘expectorant’

A

They promote the secretion of sputum by the air passages, used to treat coughs.

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6
Q

What is N-acetylcysteine’s mechanism of action and what else can it be used to treat?

A

It is a mucolytic; liquifies mucus in chronic bronchopulmonary diseases like COPD and CF by disrupting the disulphide bonds

It can also be used as an antidote for acetaminophen/paracetemol overdose

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7
Q

What is dextromethorphan? What effect does it have in excess and what can be given for overdose?

A

It’s an antitussive (antagonizes NMDA glutamate receptors) and relieves coughs because of cold or influenza. It has a mild opioid effect in excess and naloxone can be given if there is an overdose.

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8
Q

What is the mechanism and clinical use for pseudoephedrine and phenylephrine?

A

They are alpha-adrenergic agonists that reduce hyperemia and edema (used as nasal decongestants) that open obstructed Eustachian tubes

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9
Q

What does the eustachian tube do?

A

Connects the middle ear to the nasopharynx and controls the pressure in the middle ear (making it equal to atmospheric pressure)

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10
Q

What are some adverse effects of pseudoephedrine and phenylephrine?

A

Hypertension

Rebound congestion (constant nasal stuffiness from the overuse of nasal sprays (containing a decongestant medicine)) if used for more than 4-6 days

Can also cause CNS stimulation/anxiety (pseudoephedrine)

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11
Q

Name three drugs used in pulmonary hypertension

A
  1. Endothelin receptor antagonists
  2. PDE-5 inhibitors
  3. Prostacyclin analogs
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12
Q

Name two examples of second-generation histamine-1 blockers

A

Loratadine, fexofenadine

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13
Q

What drug can cause serotonin syndrome if combined with other serotonergic agents?

A

Dextromethorphan

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14
Q

What is the mechanism of endothelin receptor antagonists? Name one example

A

Mechanism: competitively antagonizes endothelin-1 receptors which decrease pulmonary vascular resistance

BosENtan

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15
Q

What is an important ‘clinical note’ of endothelin receptor antagonists?

A

They are hepatoxic and LFTs should be monitored

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16
Q

What is the mechanism of PDE-5 inhibitors, what else can they be used for other than treating pulmonary hypertension? Name one example.

A

Inhibit PDE-5 (which normally degrades cGMP) -> this leads to an increase in cGMP and a prolonged vasodilatory effect of NO and can also be used to treat ED!

Example: sildenafil

17
Q

When are PDE-5 inhibitors contraindicated and why?

A

When taking nitroglycerin or other nitrates due to the risk of severe hypotension

18
Q

What is the mechanism of prostacyclin analogs?

A

PGI2 (prostacyclin) has a direct vasodilatory effect on the pulmonary and systemic arterial vascular beds, it inhibits platelet aggregation

19
Q

Name two side effects and two examples of prostacyclin analogs

A

Side effects: flushing, jaw pain

Examples: epoprostenol, iloprost

20
Q

What pathways are targetted in asthma drugs?

A

Inflammatory process and parasympathetic tone are targetted to mediate asthmatic bronchoconstriction

21
Q

Name eight examples of asthma drugs!

A

AAA (all antis) can better my man-crush CBMMC

  1. anti leukotriene
  2. anti-IgE monoclonal therapy
  3. Anti-IL-5 monoclonal therapy
  4. B2 agonists
  5. Chromones
  6. Inhaled corticosteroids
  7. Muscarinic antagonists
  8. Methylxanthines
22
Q

Name two examples of B2 agonists? What is their individual mechanism of action? What adverse side effects can they both cause?

A
  1. Albuterol: short-acting B2 agonist that relaxes bronchial smooth muscle for acute exacerbations
  2. Salmeterol, (and formoterol): long-acting agents for prophylaxis

Both can cause tremor and arrhythmia `

23
Q

Name two examples of inhaled corticosteroids, what is their mechanism of action?

A

Fluticasone and budesonide: they inhibit the synthesis of virtually all cytokines by inactivating the NF-kB transcription factor that induces the production of TNF-a and other inflammatory agents

24
Q

How often are inhaled corticosteroids used to treat asthma, what should you do right after using them?

A

They are 1st line therapy for chronic asthma, should use a spacer or rinse mouth out after to prevent oral thrush

25
Q

What is the mechanism of action for muscarinic antagonists? Name two examples

A

They competitively block muscarinic receptors to prevent bronchoconstriction

Examples: Tiotropium and ipratropium

26
Q

What else can muscarinic antagonists be used for other than asthma?

A

COPD

27
Q

Name three examples of antileukotrienes and their mechanisms of action

A

MonteLUkast and zafirLUkast: block leukotriene receptors (CysLT1)

ZiLEUton: blocks the 5-lipoxygenase pathway which blocks the conversion of arachidonic acid to leukotrienes

28
Q

Which antileukotriene is hepatotoxic?

A

ZiLEUton

29
Q

Which types of asthma are monteLUkast and zafirLUkast especially good for treating?

A

Aspirin or exercise-induced asthma

30
Q

Name one example of an anti-IgE monoclonal therapy and describe its mechanism of action. When is it used?

A

Omalizumab: binds mostly to unbound serum IgE and block the binding to FC(backwards 3)RI (a high-affinity IgE receptor)

Used in allergic asthma with increased IgE level resistant to inhaled steroids and long-acting B2 agonists

31
Q

Name one example of a methylxanthine drug and describe its mechanism of action, what does it block the action of?

A

Theophylline: likely causes bronchodilation by inhibiting phosphodiesterase, this increases cAMP levels (due to decreased cAMP hydrolysis), blocks actions of adenosine

32
Q

What is adenosine and what is its role in normal function?

A

A neurotransmitter that promotes sleep and suppresses arousal

33
Q

Why does theophylline have a limited use? How is it metabolized?

A

It has a narrow therapeutic index (can cause neurotoxicity and cardiotoxicity), metabolized by cytochrome P-450 enzymes

34
Q

Name one example of a chromone drug and describe its mechanism of action. How often is it used?

A

Cromolyn; prevents mast cell degranulation to prevent acute asthma symptoms - rarely used

35
Q

What is the mechanism of action of Anti-IL-5 monoclonal drugs? What are they used for?

A

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

Used for maintenance therapy in severe eosinophilic asthma

36
Q

What was IL-5 originally discovered as?

A

An eosinophil colony-stimulating factor

37
Q

Name two examples of anti-IL-5 monoclonal drugs and what they specifically act against

A

Mepolizumab: against IL-5
Benralizumab: against IL-5 receptor alpha