Antiemetics

Author: Prof. Dr. med. Peter Altmeyer

Last updated on: 20.05.2022

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 for chemotherapy-induced nausea and vomiting, also for brain filiae in metastatic malignant melanoma.

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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:

Dimenhydrinate
Meclizine
Diphenhydramine.

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
Antihistamines	Meclizine	Postadoxin		25-50 mg p.o.		12(-24)	B, C	sedation, dry mouth

Neuroleptics	Phenothiazines (Thiethylperazine)	Torecan		10-30 mg p.o./i.m./rectal		(6-8)	C	Sedation
Neuroleptics	Butyrophenones (Haloperidol)	Haloperidol		0.3-0.5 mg p.o./i.v.		8-12	C	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