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ANTIEMETICS

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:

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ANTIEMETICS

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  1. ANTIEMETICS

  2. 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

  3. Clinical use of anti-emetic drugs: • H1-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) D2-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

  4. Muscarinic-receptor antagonists: • hyoscine - motion sickness (drug of choice) 5-HT3receptor 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

  5. Motility of GIT laxatives antidiarhoeal drugs

  6. 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

  7. antidiarrhoeal agents I • secretion, motility, decreased absorption • ! fluid and electrolyte balance - rehydration • antiinfective agents…gastroenteritis • sever cases of Campylobacter - erythromycin, ciprofloxacin • antidiarrhoeal agents

  8. 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

  9. motility stimulants • = prokinetic drug • domperidone (Motilium) - D2 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-HT4 rec. agonist….Ach release •  gut motility, no antiemetic action • withdrawn due to QT prolongation

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