Pharm 2 (GI, antihyperlipidemics, Cardiovascular) Flashcards
Sodium Bicarbonate
Aluminum Hydroxide
Calcium Carbonate
Magnesium hydroxide
Antacids
Tx - GERD, peptic ulcers, dyspepsia
AE - Hypokalemia & can affect absorption, bioavailability, or urinary excretion of other drugs
- AH - Constipation, hypophosphatemia, proximal muscle weakness, osteodystrophy, seizures
- CC - Hypercalcemia, acid rebound, gas/bloating
- SB - metabolic acidosis, excess NaCl absorption, gas
- MH - Diarrhea, hyporeflexia, HoTN, cardiac arrest
Cimetidine
Ranitidine
Famotidine
Nizatidine
H2 blockers = reversibly block histamine H2-receptors = ↓H+ secretion by parietal cells
Tx - GERD, peptic ulcer, dyspepsia, gastritis
AE - C = potent inhibitor of cytochrome P-450, antiandrogenic effects (prolactin release, gynocomastia, impotence, ↓ libido in males), crosses BBB (confusion, dizziness, headaches) & placenta
- C&R = ↓ renal excretion of creatinine
Omeprazole Lansoprazole Esomeprazole Pantoprazole Dexlansoprazole Rabeprazole
Proton Pump Inhibitors = Irreversibly inhibit H+/K+ ATPase in stomach parietal cells
Tx - GERD, peptic ulcer, dyspepsia, gastritis, hyper-secretory disease (Zollinger-Ellison), NSAID & H. pylori associated ulcers
AE - ↑ risk of C. dif infection, pneumonia, hip fractures;
- ↓ serum Mg w/ long-term use
Bismuth
Sucralfate
Mucosal protective agent - bind to ulcer base, provide physical protection & allow HCO3- secretion to reestablish pH gradient in the mucous layer
Tx - ↑ ulcer healing, travelers’ diarrhea (bismuth)
AE - Bismuth - Blackening of stool & tongue
Bismuth subsalicylate also usee as antidiarrheal
Misoprostol
Mucosal protective agent - PGE1 analog = ↑ production & secretion of gastric mucous barrier, ↓ acid production
Tx - Prevent NSAID-induced peptic ulcers
- maintenance of a PDA - also used to induce labor (ripens cervix)
AE - Diarrhea, cramping
CI - women of childbearing potential (abortifacient)
Octreotide
Somatostatin receptor agonist (long-acting) = ↓ gut motility
Tx - acute variceal bleeds
- acromegaly, VIPoma, carcinoid tumors - secretory diarrhea
AE - Nausea, cramps, steatorrhea
Magnesium hydroxide
Magnesium citrate
Polyethylene glycol
Lactulose
Osmotic laxatives - provide osmotic load to draw water out (into the intestinal lumen)
Tx - Constipation
AE - Diarrhea, dehydration (may be abused by bulimics)
Lactulose also Tx - hepatic encephalopathy since gut flora degrade it into metabolites (lactic & acetic acid) that promote nitrogen excretion as NH4+
Infliximab
Monoclonal Ab (mouse/human chimeric) to TNF-α
Tx - Moderate to severe IBD (UC, CD), RA, ankylosing spondylitis, psoriasis
AE - Infection (including reactivation of latent TB), fever, HoTN
Sulfasalazine
Balsalazine
Sulfapyridine (antibacterial) & 5-ASA (anti-inflammatory), activated by colonic bacteria
Tx - UC & CD
AE - Malaise, nausea, sulfonamide toxicity, reversible oligospermia
Ondansetron
Antiemetic (central acting) - 5-HT3 antagonist; ↓ vagal stimulation;
Tx - control vomiting Post-op & in chemotherapy
AE - headache, constipation
- Prolonged QT
Metoclopramide
Prokinetic & antiemetic - D2 receptor antagonist; ↑ resting tone, contractility, LES tone, motility (does not influence colon transport time)
Tx - Diabetic & post-op gastroparesis, antiemetic
AE - ↑ parkinsonian effects (restlessness, drowsiness, fatigue, depression, nausea, diarrhea)
CI - Small bowel obstruction, Parkinson disease
RxI - digoxin & diabetic agents
Bethanechol
Prokinetic agent - Muscarinic receptor (M3) agonist
Tx - GERD, gastroparesis
AE - cholinergic side effects
Neostigmine
Prokinetic agent - AChE inhibitor
Tx - non-obstructive urinary retention, abdominal distension
AE - Cholinergic side effects
Erythromycin
Prokinetic agent - Motilin receptor agonist
Tx - gastroparesis
AE - Erythromycin mediated side effects
Methylcellulose
Psyllium
Bulk-forming laxative (fiber) - adds fecal bulk & retains water (must take w/ water)
Tx - constipation, minimize straining, prior to surgical/endoscopical procedures
AE - gas/bloating
Glycerin
Mineral oil
Surfactant/Stool-softening Laxative = coat stool w/ oil & penetrate w/ water & lipids
Tx - constipation, minimize straining, prior to surgical/endoscopical procedures
AE - nutrient malabsorption
Senna
Castor Oil
Phenophthalein
Stimulant Laxative = stimulate ENS, induce leaky mucosa, inhibit sodium uptake by the gut
Tx - constipation, minimize straining, prior to surgical/endoscopical procedures
AE - GI irritation
Lubiprostone
Laxative - Chloride Channel Activator (Prostaglandin derivative)
Tx - Chronic constipation
AE - N,V,D
Loperamide
Anti-diarrheal, opioid agonist = ↑ segmental contractions & ↓ peristaltic contractions (↑ absorption ↓ movement)
Tx - Diarrhea (IBS)
AE - Constipation
low to no ability to cross BBB
Diphenoxylate
Anti-diarrheal, opioid agonist = ↓ GI perception of GI distension
Tx - diarrhea
AE - CNS effects, Atropine-like effects
Kaolin & Pectin
Antidiarrheal; Add fecal bulk & absorb toxins
Kaolin = Magnesium aluminum silicate
Pectin = non-digestible sugar
Tx - Diarrhea
AE - constipation
Bismuth subsalicylate
Antidiarrheal agent - Absorb toxins & inhibit prostaglandin synthesis in intestines
Tx - nonspecific & travelers’ diarrhea
AE - Salicylate toxicity
Also used as a mucosal protective agent
Scopolamine
Antiemetic - Muscarinic (M1) antagonist
Tx - Motion sickness
AE - Antimuscarinic effects
Dimenhydrinate
Antiemetic - Histamine (H1) antagonist
Tx - Motion Sickness
AE - Drowsiness
Aprepitant
Antiemetic - NK1 antagonist
Tx - Chemotherapy related nausea/vomiting
- 2nd/3rd choice due to AE
AE - Fatigue, dizziness, diarrhea
CYP3A4 interactions
Prochlorperazine
Antiemetic - M1D2H1 antagonist
Tx - Severe nausea & vomiting
- 2nd/3rd choice due to AE
AE - Extrapyramidal (D), Drowsiness (H), Anticholinergic (M)
Lorazepam
Antiemetic - GABA agonist
Tx - Anxiety/chemotherapy
AE - drowsiness
Nabilone
Antiemetic - Cannabinoid agonist
Tx - chemotherapy
AE - dysphoria, sedation, increased appetite (can be beneficial if trying to ↑ caloric intake)
Dexamethasone
Antiemetic - Glucocorticoid agonist
Tx - Post-op & chemotherapy
- ↑ effectiveness of 5-HT antagonists (ondansetron, Alosetron etc.)