pulmonary drugs Flashcards
List first generation antihistamines
Diphenhydramine/Chlorpheniramine/Brompheniramine, Meclizine/Dimenhydrinate
List second generation antihistamines
Loratadine/Fexofenadine/Cetirizine
First generation antihistamine MOA
Reversible and competitive blocking of H1 receptors (no H2). Also block muscarinic receptors which leads to sedation (CNS), prevention of nausea and vomiting (CNS), and blocking secretions (ANS). Also blocks sodium channels for local anesthetic action (diphenhydramine) and blocks adrenergic receptors
Second generation antihistamine MOA
Blocks H1 receptor almost exclusively. Slight level of sedation possible, but do not penetrate CNS well.
Antihistamine pharmacokinetics
All: oral, rapid absorption, Metabolized by liver. First gen: duration of 4-8 hrs. Second gen: longer duration with metabolic and/or renal elimination. Fexofenadine lasts 12 hrs. Loratadine and cetirizine last 24 hrs
Clinical uses of antihistamines
allergic rhinitis or other allergic rxns via H1 block. Reduces sneezing, pruritus, rhinorrhea, and some congestion, but not inflammation. Also used for cough suppression via Na channel block, motion sickness (H1 and muscarinic block), nausea (H1 and muscarinic block) and sleep aid (H1 and muscarinic block)
Side effects of antihistamines
Sedation (mainly 1st gen), dry mouth (antimuscarinic actions), postural hypotension, GI upset
List topical decongestants
Phenylephrine, oxymetazoline
list oral decongestants
Pseudoephedrine, phenylephrine
Topical decongestants MOA
Stimulate α1-adrenergic receptors of vascular smooth muscle resulting in constriction of nasal blood vessels dilated by histamine or inflammatory response. Promotes drainage, improves breathing via decrease in congestion
Oral decongestants MOA
delivers drug via systemic circulation to nasal vascular bed, NOT associated with rebound congestion. Stimulates Stimulate α1-adrenergic receptors of vascular smooth muscle resulting in constriction of nasal blood vessels
Oral vs topical decongestants pharmacokinetcs
topical: prompt effect. Phenylephrine has short (4hr) duration. Oxymetazoline has longer duration (6-12hrs). Oral: Longer duration of action and unaffected y mucus, but less vasoconstriction than topical. Pseudoephedrine is safest, phenylephrine blood levels are hard to preduct due to differences in metabolism (hepatic).
Topical decongestants side effects
rebound congestion due to ischemia/local irritation
Oral decongestants side effects
Affects other vascular beds (not limited to nasal blood vessels) and can cause headaches, dizziness, nervousness, nausea, increased blood pressure / palpitations
decongestant uses
allergic rhinitis and viral cold infections