MOA of Serotonin receptor antagonists
Prevent nausea and vomitting by blocking serotonin receptors at two sites
Example Sertoninin receptor antagonists
OndanSETRON
ganiSETRON
dolaSETRON
palonoSETRON
Indication for serotonin receptor antagonists
Nausea and vomiting
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
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
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
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)