GI Drugs Flashcards
Name the major receptors involved in nausea/vomiting. (7)
H1, M1, chemoreceptors, D2, NK1, 5-HT3, mechanoreceptors
Scopolomine’s best application for N/V?
Prophylactic
What antihistamine is often used for Meniere’s Disease?
Meclizine (Antivert)
Name 2 highly emetogenic chemotherapeutic drugs.
Cisplatin, Cyclophosphamide
What drug class is the “biggest player” in an antiemetic regimen for chemotherapy-induced N/V? What can you add for higher levels of N/V?
5HT3 antagonist; corticosteroid and Aprepitant (NK1 antag)
What drug class is the cornerstone of chemotherapy anti-emesis regimens?
5-HT3 antagonists
Which 5-HT2 Antagonist has a half-life of 40 hours and is effective for delayed emsis?
Palonosetron
What antiemetic class can have major P450 enzyme interactions?
Neurokinin Receptor-1 antagonists
Name 2 NK-1 antagonists
Aprepitant
Netupitant
What is the advantage of CINVANTI over fosaprepitant?
It is a lipid emulsion of aprepitant rather than a prodrug like fosaprepitant and can be given by IV push rather than as a 30 minute infusion
What is Akynzeo?
A combination of (fos)netupitant (NK-1 antag) and palonosetron (5-HT3 antag); both drugs have a longer half-life; this prep can be given IV or PO
Name some D2 dopamine receptor antagonists used as antiemetics.
Benadryl
Phenergan
Benzos
Reglan
What are 2 contraindications for the use of laxatives?
Fecal impaction
Bowel obstruction
Name some bulk-forming laxatives.
Methylcellulose, Psyllium (Metamucil, Citrucel)
What drug class is the agent of choice for relief of temporary constipation?
Bulk-forming laxatives; safest class
Name some surfactant laxatives
Docusate salts, colace
Describe the MOA of surfactant laxatives
Anionic surfactant (soap-like) allows oil and water to penetrate stool
What is the most abused class of laxatives?
Stimulant laxatives; eating disorders
Name some stimulant laxatives
Bisacodyl (Dulcolax, Correctol), Senna (Ex-Lax, Senokot), Castor Oil
What mechanism of stimulant laxatives can lead to a common side effect?
Direct stimulation of GI motility can lead to severe stomach cramping
What class of laxatives is used for bowel prep?
Osmotic laxatives
Name some subclasses and drugs of osmotic laxatives.
Magnesium Salts (Milk of Magnesia) Polyethylene Glycol/PEG (Miralax, GoLytely)
What is a concern with osmotic laxatives for older and renal-impaired patients?
Hypermagnesemia with Mg2+ salts
What are 3 characteristics of the antimotility/antisecretory agent Bismuth (Pepto-Bismol)?
Antimotility
Anti-inflammatory
Antimicrobial
What formulation of diphenoxylate (chemically related to meperidine) decreases its abuse potential?
Combination with atropine