1. Phenothiazines (2)
    • 1. Prochlorperazine (Compazine)
    • 2. Chlorpromazine (Thorazine)

    most widely used antiemetics

    AE: extrapyramidal effects, hypersensitivity, excessive sedation, anticholinergic effects, bone marrow suppression, skin reactions
  2. Aloxi

    -NEW injectable annit-vomiting and anti-nausea agent for chemotherapy

    5-HT3 receptor antagonist

    LONG half-life (40 hrs)
  3. Emend

    -substance P/neurokinin 1 receptor antagonist for anti-vomitiing

    -used in chemotherapy

    -CYP 450 inhibitor

    -oral and IV
  4. Promethazine

    antihistamine and anticholinergic agent used for simple N/V, motion sickness, vertigo

    -IM and supp
  5. Trimethopbenzamide

    antihistamine and anticholinergic agent used for simple N/V, motion sickness, vertigo

    -IM and supp
  6. Meclizine
    (Antivert or Bonine)

    antihistamine and anticholinergic agent used for simple N/V, motion sickness, vertigo
  7. Dimenhydrinate

    antihistamine and anticholinergic agent used for simple N/V, motion sickness, vertigo
  8. Scopolamine
    (Transderm Scop)

    antihistamine and anticholinergic agent used for simple N/V, motion sickness, vertigo

    -patch best for prevention of motion sickness
  9. AE for anticholinergics and antihistamines (5)
    • 1. dry mouth
    • 2. urinary retention
    • 3. drowsiness
    • 4. blurred visino
    • 5. caution in BPH and narrow angle glaucoma
  10. Butyrophenones (2)


    • 1. Droperidol (Inapsine)
    • 2. Haloperidol (Haldol)

    -used for complex cases of vomiting in anesthesia and chemo

    -blocks stimulation of the CTZ

    AE: sedation, dystonia, EP reactions which can be relieved by diphenhydramine

    QT prolongation, ECG is recommended before treatment

    increased risk of sudden cardiac death
  11. Metoclopramide

    used for complex N/V and for gastroparesis associated with diabetic autonomic neuropathy

    AE: EP effects, restlessness, drowsiness, diarrhea (may need to give with IV diphenhydramine)
  12. Corticosteroids (2) for N/V
    • 1. Dexamethasone
    • 2. Methylprednisolone (IV)

    -for post-op and chemo induced

    -increases appetite and feelings of well-being

    AE: mood changes, HA, metallic taste, hyperglycemia and itchy throat
  13. Selective Serotonin Antagonist (3)
    • 1. Ondasetron
    • 2. Granisetron
    • 3. Dolasetron

    -block 5HT receptor for chemo N/V

    AE: HA, diarrhea, dizziness, constipation
  14. Cannibinoids (2)
    • 1. Dronabinol (Marinol)
    • 2. Nabilone (Cesamet) - less euphoria
  15. for CINV (4)
    1. Combination of two or more agents

    2. May combine metoclopramide, diphenhydramine and dexamethasone

    3. Use a selective serotonin antagonist with dexamethasone for delayed effects

    4. Benzodiazepines such as lorazepam are useful for anticipatory N/V
  16. For PONV (4)
    1. Common esp. with women, increased age and obesity

    2. Selective serotonin antagonists are effective but expensive

    3. Dexamethasone is effective as well

    4. May use antihistamines in combination as well
  17. For pregnancy related N/V
    -use antihistamines like deminhydrinate, meclizine, and promethazine
  18. Migraine headache antiemetics
    -associated with dopamine (metoclopramide, prochlorperazine)
  19. Vestibular nausea treatment
    anticholinergics and antihistamines
  20. Gastroenteritis antiemetics
    • -1st line is DA antagonist
    • -2nd line is serotonin (5HT) antagonist
  21. Post-op N/V antiemetics
    Prevention: 5HT antagonists, dexamethasone, droperidol

    Treatment: DA antagonists, 5HT antagonists, drexamethasone
  22. Gaviscon
    Antacid for heartburn

    -neutralizes gastric acids

    AE: aluminum causes constipation and magnesium can cause diarrhea

    interferes with absorption of other drugs, Al salts may cause problems in renal insufficiency pts, cancium carbonate can form gas-bloating
  23. H2 Blockers (4)
    1. Cimetidine (Tagamet) - most effect on cytochrome P450 --> drug interactions

    2. Ranitidine (Zantac) - can be used w/ infants

    3. Famotidine (Pepcid) - longest duration

    4. Nizatidine (Axid)

    -useful for mild to moderate GER

    -not as effective as PPIs
  24. PPIs (5)
    • 1. Esomeprazole (Nexium)
    • 2. Omeprazole (Prilosec)
    • 3. Lansoprazole (Prevacid)
    • 4. Rabeprazole (Aciphex)
    • 5. Pantoprazole (Protonix)


    -P450 metabolism so drug interactions occur

    -pregnancy cat B
  25. Sulcrafate
    agent of GERD

    -sticky and viscous gel protects tissue

    AE: constipation
  26. Three types of PUD
    1. H. pylori induced - duodenal

    2. NSAID induced - gastric , deeper more GI bleeds

    3. Stress ulcers - 10% of Americans develop it
  27. Treatment of H.pylori
    Three drug: 2 abx (clarithromycin & metronidazole OR clarithromycin & amoxicillin) + PPI for 14 days

    4 drug: 2 abx (tetracylcine & metronidazole) + bismuth + PPI
  28. Pylera
    new 4 drug formulation to fight H.pylori

    -Bismuth subcitrate potassium & metronidazole & tetracycline & omeprazole
  29. Prevention of NSAID induced ulcers
    PPIs are more effective in reducing gastric and duodenal ulcers (preferred choice)

    H2 blockers should NOT be used as cotherapy with nonselective NSAID for prophylaxis
  30. Arthrotec
    -cotherapy with misprostol and a prostaglandin analog for prevention of NSAID induced ulcers
  31. Misoprostol
    synthetic prostaglandin analog that protect gastric mucosa; added w/ NSAID therapy to protect against ulcers

    -Cat X!
  32. Isoniazid (INH) MOA, AE, and required monitoring
    MOA: prodrug which is activated to block mycolic acid synthesis, components of mycobacterial cell walls; Penetrates well into cells, CNS and infected tissue including granulomas

    AE: hepatitis & peripheral neuropathy

    monitor w/ LFTS; neuropathy avoided by pyridoxime
  33. Rifampin MOA, AE, and drug metabolism issues
    MAO: binds to beta subunit of bacterial DNA dependent RNA polmerase and inhibits RNA synthesis

    AE: Harmless reddish orange discoloration of body fluids; may cause hepatitis, cholestasis w/ jaundice, and nephritis

    Drug interactions -- induced P450, which increases elimination of oral contraceptives and protease inhibitors (HIV meds)
  34. Pyrazinamide AE
    AE: hepatotoxicity, polyarthralgia (40%), N/V, hyperuricemia
  35. Ethambutol AE
    AE: retrobulbar neuritis causing loss of color vision (green >> red) and loss of visual acuity
  36. 4 drug regiment for active TB
    • 1. Isoniazid (INH)
    • 2. Rifampin (RIF)
    • 3. Pyrazinamide (PZA)
    • 4. ethambutol
  37. Treatment course for uncomplicated primary active pulmonary TB
    4 drug regiment + vitamin B6 for 2 month (initiation phase) followed by 18 week of INH and RIF (continuation phase)
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