Antiemetics

Last updated on: 29.10.2020

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Definition
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Medicine against nausea and vomiting. The treatment of these symptoms in the context of chemotherapy is discussed below. The process of vomiting is controlled by the vomiting centre in the brain (Formatio reticularis as part of the medulla oblongata near the respiratory centre). Through contractions of the abdominal and diaphragmatic muscles, the chyme is transported back. In addition to the psychological stress of patients with severe and frequent vomiting, there are health effects caused by electrolyte and water losses, which then make the treatment of vomiting urgently necessary.

Indication
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Prophylactic in chemotherapy-induced nausea and vomiting, also in brain filia in metastatic malignant melanoma.

Dosage and method of use
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Treatment options (MASCC guidelines = Multinational Association of Supportive Care in Cancer)
Emetogenic risk Acute therapy (day 1) Follow-up treatment (peroral, from day 2)
High 5-HT3 + Dex, Aprepitant Dex + MCP, Aprepitant or 5-HT3
Moderately high 5-HT3 + Dex Dex or Dex + 5HT3 or 5-HT3
Low to medium Dex or others none
Low none none
5-HT3 = 5-HT3 antagonists (serotonin antagonists); Dex = dexamethasone; MCP = metoclopramide

Note(s)
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  • For the treatment of nausea and vomiting, the following pharmacological classes of substances are used:
    • H1 antihistamines
    • 5-HT3 antagonists
    • Neuroleptics.
  • Gastrointestinal movement promoting substances:
    • Herbal remedies
    • Homeopathic remedies
    • H1 antihistamines.
  • Antihistamines: Antihistamines block the effects of the body's own substance histamine. The different effects of histamine result from the binding of the substance to different receptors, of which three types are currently known. For the treatment of nausea and vomiting, the H1 receptors are important, which are blocked by the H1 antihistamines.
  • The H1 antagonists are divided into 1st and 2nd generation drugs. Of importance here is that the H1 antihistamines of the 1st generation have a sedative effect, i.e. they make you tired. This effect is exploited when some H1 antihistamines are administered as sleeping pills. When the substances are used as a remedy against nausea and vomiting, the tiring effect is sometimes a desirable side effect.
  • The following H1 antihistamines are used as remedies against nausea and vomiting:
  • Serotonin antagonists (5-HT3-antagonists): 5-HT3-antagonists bind to serotonin receptors and thus prevent the effects of the body's own substance serotonin. They are a relatively newly developed class of substances that are very effective against vomiting caused by treatment with cytostatic drugs or during radiotherapy. For this reason, 5-HT3 antagonists are often used as an accompanying treatment in the context of tumour therapy. The substances are characterised by their good effectiveness against vomiting which occurs early, i.e. within the first 24 hours after administration of the cytostatic drug. In the case of vomiting occurring later, i.e. two to three days after the application of the tumour drug, the 5-HT3 antagonists are generally no longer sufficiently effective. For the treatment of nausea and vomiting can be used:
    • Granisetron
    • Ondansetron
    • Tropisetron
    • Dolasetron.
  • Neuroleptics: Neuroleptic drugs are often used in antiemetic therapy to treat nausea and vomiting, in particular:
    • Sulpiride
    • Triflupromazine
    • Haloperidol
    • Perphenazine.
  • Gastrointestinal movement stimulants, prokinetics: nausea and vomiting can also be treated by accelerating gastric emptying and small intestinal passage. This shortens the time food stays in the upper gastrointestinal tract and reduces the effects of stimuli that cause nausea and vomiting. The following substances promote gastrointestinal movement:
    • Metoclopramide
    • Bromoprid
    • Cisapride
    • Domperidone
    • Herbal remedies.
  • In "folk medicine", herbal remedies are used relatively frequently for complaints in the digestive tract and thus also for nausea and vomiting, although the use of the respective plants or parts of plants is handled differently. There are official recommendations for ginger root.
  • Homeopathic remedies: As homeopathic remedies for nausea and vomiting the following medicines can be used:
    • Hervertigon Tbl. or Hervertigon injection solution
    • Vertigo-Hervert Tbl. (pharmacy-only, but not prescription and therefore suitable for self-medication).
    • Cocculus Oligoplex Liquidum (pharmacy-only, but not prescription and therefore suitable for self-medication).

Tables
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Overview of the most frequently used antiemetics

Freiname

Preparations

Dose Day 1

Dose for follow-up treatment (from day 2)

Interval

(hrs.)

Place of action

Comment

Antihistamines

Dimenhydrinate

Vomex A

100-200 mg p.o./i.v./rectal

8

B, C

sedation, dry mouth

Meclizine

Postadoxin

25-50 mg p.o.

12(-24)

Neuroleptics

Phenothiazines (Thiethylperazine)

Torecan

10-30 mg p.o./i.m./rectal

(6-8)

C

Sedation

Butyrophenones (Haloperidol)

Haloperidol

0.3-0.5 mg p.o./i.v.

8-12

not sedating in this dosage

Anticholinergics

Scopolamine

Scopoderm TTS

1 patch (= 1.5 mg)

3(?4) days

B

slightly sedating, dry mouth, mydriasis

Prokinetics

Metoclopramide

Paspertin

10-40 mg p.o./i.v./i.m.

no application

4-5

G, C

possibly dyskinesia, light sedation

Domperidone

Motilium

20-40 mg (max. 80 mg) p.o.

4-6

Alizapride

Vergentan

50-300 mg p.o./i.v./i.m.

4-6

5-HT3 antagonists

Dolasetron

Anemet

1,8 mg/kg bw (100 mg) i.v.; Alternatively: 100 mg p.o.

100 mg/day p.o.

24

B

no extrapyramidal NW, possible constipation

Granisetron

Kevatril

0,01 mg/kg bw (1 mg) i.v.; Alternatively: 2 mg p.o.

once/day 2 mg p.o.

8-12

B

no extrapyramidal NW, possible constipation

Ondansetron

Zofran

0,15 mg/kg bw (8 mg) i.v.; Alternatively: 24 mg p.o.

2 times/day 8 mg p.o.

8-12

B

no extrapyramidal NW, possible constipation

Tropisetron

Navoban

5 mg i.v.; Alternatively: 5 mg p.o.

5 mg p.o. once/day

24

B

no extrapyramidal NW, possible constipation

Neurokinin-1 (NK1) antagonists

Aprepitant

Emend

once/day 125 mg p.o.

on days 2 and 3 80 mg p.o. each

24

B

no extrapyramidal NW, possible loss of appetite, weight gain.

Glucocorticoids

Dexamethasone

Fortecortin

High ematogenic risk

20 mg i.v.; Alternatively: 20 mg p.o.

2 times/day 8 mg i.v. or p.o.

6-24

in case of increased intracranial pressure due to peritumorous oedema and in case of vomiting caused by cytostatics, a higher dose may be necessary

Moderate to high ematogenic risk

10-20 mg i.v.; Alternatively: 12-20 mg p.o.

2 times/day 4-8 mg

6-24

Low to medium ematogenic risk

4-20 mg i.v.; Alternatively: 4-20 mg p.o.

none

6-24


High emetogenic potential (> 90%)

Moderate emetogenic potential (30-90%)

Low emetogenic potential (10-30%)

Minimum emetogenic potential (< 10%)

intravenous drugs

Cisplatin

Oxaliplatin

Paclitaxel

Bleomycin

Mechloroethamine

Carboplatinum

docetaxel

Busulfan

Streptozotocin

Ifosfamide

Mitoxantrone

2-chlorodeoxyadenosine

Carmustin

Doxorubicin

Topotecan

Fludarabine

Dacarbacin

Daunorubicin

Etoposide

Vinblastine

Dactinomycin

Epirubicin

Permetrexed

Vincrist

Idarubicin

Methotrexate

Vinorelbine

Irinotecan

Mitomycin

Bevacizumab

Gemcitabine

Rituximab

5-fluoroacil

Bortezomib

Cetuximab

Trastuzumab

orally administered drugs

Hexamethylmelamine

Cyclophosphamide

Capecitabine

Chlorambucil

Procarbacin

Etoposide

Fludarabine

Hydroxyurea

Temozolomide

L-Pheylalanine mustard

Vinorelbine

6-thioguanine

Imatinib

Methotrexate

Erlotinib

Last updated on: 29.10.2020