antiemetics,motility

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antiemetics,motility

  1. 1. ANTIEMETICS
  2. 2. Regulation of vomiting <ul><li>medulla oblongata </li></ul><ul><ul><li>the vomiting centre </li></ul></ul><ul><ul><li>chemoreceptor trigger zone (area postrema) </li></ul></ul><ul><ul><ul><li>emetogenic substances, apomorphine, morphine, chemotherapy, motion sickness </li></ul></ul></ul><ul><ul><li>Ach, histamine, 5-HT, Dop </li></ul></ul>
  3. 4. Clinical use of anti-emetic drugs: <ul><li>H 1 -receptor antagonists: </li></ul><ul><li>cylizine - motion sickness </li></ul><ul><li>cinnarizine - motion sickness, vestibular disorders (e.g. </li></ul><ul><li>Meniére´s disease) </li></ul><ul><li>promethazine - severe morning sickness of pregnancy (only </li></ul><ul><li>if absolutely essential) </li></ul><ul><li>D 2 -receptor antagonists: </li></ul><ul><li>phenothiazines (e.g. thiethylperazine) - vomiting caused </li></ul><ul><li>by uraemia, radiation, viral gastroenteritis (drugs of choice); </li></ul><ul><li>severe morning sickness of pregnancy (if absolutely essential) </li></ul><ul><li>metoclopramide - vomiting caused by uraemia, radiation, </li></ul><ul><li>gastrointestinal disorders, cytotoxic drugs </li></ul>
  4. 5. <ul><li>Muscarinic-receptor antagonists: </li></ul><ul><li>hyoscine - motion sickness (drug of choice) </li></ul><ul><li>5-HT 3 receptor antagonists: </li></ul><ul><li>ondansetron - vomiting caused by cytotoxic anticancer </li></ul><ul><li>drugs (drug of choice), postoperative vomiting; radiation- </li></ul><ul><li>induced vomiting </li></ul><ul><li>Cannabinoids: </li></ul><ul><li>nabilone - for vomiting caused by cytotoxic anticancer drugs </li></ul>
  5. 6. laxatives antidiarhoeal drugs Motility of GIT
  6. 8. LAXATIVES <ul><li>bulk laxatives </li></ul><ul><ul><li>=increasing the volume, not absorbed </li></ul></ul><ul><ul><li>methylcelulose, agar, psyllium seeds </li></ul></ul><ul><ul><li>no serious unwanted effects </li></ul></ul><ul><li>osmotic l. </li></ul><ul><ul><li>not absorbed, osmosis - distension of colon </li></ul></ul><ul><ul><li>magnesium sulphate, magnesium hydroxide, lactulose </li></ul></ul><ul><ul><li>ADR: flatulence, cramps, diarhoea, electrolyte dist., tolerance </li></ul></ul><ul><li>stimulant l. </li></ul><ul><ul><li>stimulation of enteric nerves -  secretion, motility </li></ul></ul><ul><ul><li>bisacodyl, senna preparations </li></ul></ul><ul><ul><li>! only for short-term use - nerve reduction </li></ul></ul>
  7. 9. antidiarrhoeal agents I <ul><li>secretion, motility, decreased absorption </li></ul><ul><li>! fluid and electrolyte balance - rehydration </li></ul><ul><li>antiinfective agents…gastroenteritis </li></ul><ul><ul><li>sever cases of Campylobacter - erythromycin, ciprofloxacin </li></ul></ul><ul><li>antidiarrhoeal agents </li></ul>
  8. 10. antidiarrhoeal agents II <ul><li>antimotility agents </li></ul><ul><ul><li>opiates , morphine - constipation, sphincter contraction </li></ul></ul><ul><ul><li>codeine, diphenoxylate, loperamide </li></ul></ul><ul><ul><li>! drowsiness, dizziness, paralytic ileus </li></ul></ul><ul><li>adsorbents </li></ul><ul><ul><li>adsorbing microorganisms and toxins </li></ul></ul><ul><ul><li>kaolin, pectin, charcoal </li></ul></ul>
  9. 11. motility stimulants <ul><li>= prokinetic drug </li></ul><ul><li>domperidone (Motilium) - D 2 antagonist, also antiemetic </li></ul><ul><ul><li> oesophageal sphincter pressure…GERD </li></ul></ul><ul><ul><li>! hyperprolactinemia </li></ul></ul><ul><li>metoclopramide (Paspertin) - DA antagonist and Ach agonist </li></ul><ul><ul><li>increases gastric emptying - GERD </li></ul></ul><ul><ul><li>! extrapyramidal side effects </li></ul></ul><ul><li>cisapride (Prepulsid) - 5-HT 4 rec. agonist….Ach release </li></ul><ul><ul><li> gut motility, no antiemetic action </li></ul></ul><ul><ul><li>withdrawn due to QT prolongation </li></ul></ul>

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