First Aid: Pharmacology Flashcards
What are histamine-1 blockers?
What is the clinical use of their first-generation drugs?
They are reversible inhibitors of H1 histamine receptors
They are clinically used for allergies, motion sickness and for sleep aid
What are some adverse effects of first-generation histamine-1 blockers? Name two examples
Sedation, antimuscarinic, anti-alpha-adrenergic
Examples: doxylamine, diphenhydramine
What is the clinical use of second-generation Histamine-1 blockers and how do their effects compare to first-generation?
Used for allergies, they are far less sedating than the 1st generation due to decreased entry into the CNS
What is the role of Guaifenesin? What doesn’t it do?
It is an expectorant that thins the respiratory secretions (mucus) in order to promote mucus drainage! It doesn’t suppress the cough reflex
What is the normal job of a drug that is an ‘expectorant’
They promote the secretion of sputum by the air passages, used to treat coughs.
What is N-acetylcysteine’s mechanism of action and what else can it be used to treat?
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
What is dextromethorphan? What effect does it have in excess and what can be given for overdose?
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.
What is the mechanism and clinical use for pseudoephedrine and phenylephrine?
They are alpha-adrenergic agonists that reduce hyperemia and edema (used as nasal decongestants) that open obstructed Eustachian tubes
What does the eustachian tube do?
Connects the middle ear to the nasopharynx and controls the pressure in the middle ear (making it equal to atmospheric pressure)
What are some adverse effects of pseudoephedrine and phenylephrine?
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)
Name three drugs used in pulmonary hypertension
- Endothelin receptor antagonists
- PDE-5 inhibitors
- Prostacyclin analogs
Name two examples of second-generation histamine-1 blockers
Loratadine, fexofenadine
What drug can cause serotonin syndrome if combined with other serotonergic agents?
Dextromethorphan
What is the mechanism of endothelin receptor antagonists? Name one example
Mechanism: competitively antagonizes endothelin-1 receptors which decrease pulmonary vascular resistance
BosENtan
What is an important ‘clinical note’ of endothelin receptor antagonists?
They are hepatoxic and LFTs should be monitored