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 agonist….Ach release    gut motility, no antiemetic action withdrawn due to QT prolongation

antiemetics,motility

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