GI PHARM Flashcards
MOA of Serotonin receptor antagonists
Prevent nausea and vomitting by blocking serotonin receptors at two sites
- chemoreceptor trigger zone
- afferent vagal nerves
Example Sertoninin receptor antagonists
OndanSETRON
ganiSETRON
dolaSETRON
palonoSETRON
Indication for serotonin receptor antagonists
Nausea and vomiting
- post operative
- chemotherapy induced
- pregnancy
- gastritis
Contraindications
Serotonin receptor antagonists
Prolonged QT interval
Cardiac abnormalities:
Bradydysrhythmias
heart failure
MOA
Antihistamines H1 receptor antagonists
Block H1 receptor in the vomiting centre
Prevent signal from inner ear to vomiting centre
Prevention of N/V/motion sickness
SE
H1 receptor antagonists
Muscarinic blockade: dry mouth, constipation, urinary retention, glaucoma, blurred vision, sedation, delirium/paradoxical reaction
H1 receptor blockade: hypertension
Contraindications
H1 receptor antagonists
Third trimester pregnancy - neonatal sedation
breast feeding - neonatal sedation
Conditions made worse by muscarinic blockade: asthma, BPH, constipation, elderly, children
Infants < 6 months
Examples of H1 receptor antagonists
Dimenhydramine (benadryll)
Dimenhydrinate (gravel)
Meclizine
Cyclizine
MOA
Glucocorticoids (for N/V)
unknown mechanism of action
synergistic for N/V if given with other anti-emetics
SE
Glucocorticoids
Bones: osteoporosis, growth suppression, fractures
Skin: infections, striation, poor wound healing
GI: ulcers, perforations, hemorrhages
Cushingoid appearance: central fat, degradation muscles, moon face, hump back; adrenal suppression
Electrolytes: hyperglycaemia, hypernatremia, hypokalemia, FVO, weight gain
Eyes: glaucoma, cataracts
CSN: mania, depression
Contraindications
Glucocorticoids
pregnancy / breastfeeding - teratogenic
Caution: children and elderly, growth suppression, fractures, adrenal insufficiency
Example
Antacids
magnesium hydroxide
aluminum hydroxide
calcium carbonate
sodium bicarbonate
MOA
Ant-acids
- neutralize HCl –> rise in pH
- prevent activation pepsinogen to pepsin
- activation prostaglandin –> increase mucous, bicarb, blood flow mucosa barrier
SE
antacids
calcium carbonate - constipation, acid rebound
magnesium hydroxide - magnesium toxicity, diarrhea
sodium bicarbonate - metabolic alkalosis, hypernatremia
Contraindications
ant-acids
sodium bicarbonate
- metabolic alkalosis, hypernatremia, heart failure or kidney disease
Increase clearance of acidic drugs in urine
prevent absorption of drugs - give 1 hour apart
Magnesium hydroxide
Kidney failure or disease
MOA
H2 receptor antagonists
Prevents gastric acid secretion
Blocks H2 receptors on parietal cells. Prevents cAMP signal which H/K ATPase excretes H+ into gastric lumen (blocked)
increase pH stomach
SE
H2 receptor antagonists
CNS: depression, hallucinations, agitation
pneumonia: increase bacterial colonization stomach, secondary respiratory infections (aspiration)
Contraindications
H2 receptor antagonists
Caution: pregnancy, breast feeding (sedation)
Caution: kidney and hepatic impairment (dose adjustment)
Drug interactions: CYP450 inhibitor (increase warfarin, phenytoin) ; antacids prevent H2 receptor antagonist absorption
Examples
H2 receptor antagonists
raniTIDINE
cimeTIDINE
famoTIDINE
nizaTIDINE
Indication
H2 receptor antagonists
- Treatment PUD
- Ulcer healing
Duration 8-12 weeks gastric
Duration 4-6 weeks duodenal - GERD
MOA
proton pump inhibitors
Prevent secretion and synthesis of HCl
Block H/K ATPase in the parietal cells. Irreversible inhibition. Lasts lifetime of cell (3-5 days)
Indications
PPIs
- Prophylaxis and treatment of PUD
- GERD
- erosive esophagitis
- Zollinger-Ellison syndrome
SE
PPIs
Hypomagnesium - cramps, dysrhythmias, tremors
Hypocalcemia - fractures (convulsions, reflex hyperactive, anorexia, muscle spasms/tetany, positive trauseau, chvostek, parenthesia)
Pneumonia
C. Diff diarrhea
Acid rebound - wean, do not D/C abruptly, PRN H2 receptor antagonist
Contraindications
PPI
pneumonia
osteoporosis
hypomagnesemia, hypocalcemia
C. diff diarrhea
DRUG INTERACTIONS
clopidogrel - decrease conversion to active form (PRN PPI for gastric protection)