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QuickView for Cyclizine (compound)

Summary
General Info

PubChem

PubChem Compound 517299

PubChem Compound 517299

Name:	Cyclizine
PubChem Compound ID:	517299
Description:	A histamine H1 antagonist given by mouth or parenterally for the control of postoperative and drug-induced vomiting and in motion sickness. (From Martindale, The Extra Pharmacopoeia, 30th ed, p935)
Molecular formula:	C₁₈H₂₃ClN₂
Molecular weight:	302.841 g/mol
Synonyms:	Cyclizine hydrochloride

DrugBank

Identification

Name:	Cyclizine
Name (isomeric):	DB01176
Drug Type:	small molecule
Description:	A histamine H1 antagonist given by mouth or parenterally for the control of postoperative and drug-induced vomiting and in motion sickness. (From Martindale, The Extra Pharmacopoeia, 30th ed, p935)
Synonyms:	Ciclizina [INN-Spanish]; Cyclizine Chloride; Cyclizinum [INN-Latin]; Cyclizine Hydrochloride
Brand:	Neo-Devomit, Nautazine, Reis-Fit, Valoid, Marazine, Wellcome, Ne-Devomit, Marezine Hydrochloride, Marzine, Marezine, Emoquil
Category:	Histamine H1 Antagonists, Antiemetics, Piperazine Derivatives
CAS number:	82-92-8

Pharmacology

Indication:	For prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness, and vertigo (dizziness caused by other medical problems).
Pharmacology:	Cyclizine is a piperazine-derivative antihistamine used as an antivertigo/antiemetic agent. Cyclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus. Although the mechanism by which ... show more » Cyclizine is a piperazine-derivative antihistamine used as an antivertigo/antiemetic agent. Cyclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus. Although the mechanism by which cyclizine exerts its antiemetic and antivertigo effects has not been fully elucidated, its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects. show less «
Mechanism of Action:	Vomiting (emesis) is essentially a protective mechanism for removing irritant or otherwise harmful substances from the upper GI tract. Emesis or vomiting is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesses neurons which are rich in muscarin... show more » Vomiting (emesis) is essentially a protective mechanism for removing irritant or otherwise harmful substances from the upper GI tract. Emesis or vomiting is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesses neurons which are rich in muscarinic cholinergic and histamine containing synapses. These types of neurons are especially involved in transmission from the vestibular apparatus to the vomiting centre. Motion sickness principally involves overstimulation of these pathways due to various sensory stimuli. Hence the action of cyclizine which acts to block the histamine receptors in the vomiting centre and thus reduce activity along these pathways. Furthermore since cyclizine possesses anti-cholinergic properties as well, the muscarinic receptors are similarly blocked. show less «
Biotransformation:	Cyclizine is metabolised to its N-demethylated derivative, norcyclizine, which has little antihistaminic (H1) activity compared to Cyclizine.
Half Life:	20 hours
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Avoid alcohol.

Food may reduce irritation.

Take without regard to meals.

Drug interaction:

Trimethobenzamide	Trimethobenzamide and Cyclizine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Donepezil	Possible antagonism of action
Rivastigmine	Possible antagonism of action
Tacrine	The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Cyclizine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
Galantamine	Possible antagonism of action

Targets

Histamine H1 receptor

Estrogen sulfotransferase

Enzymes

Cytochrome P450 2C9