Motion Sickness

Also known as: Airsickness / Motion sickness NOS / Travel sickness / Travel sickness NOS

DrugDrug NameDrug Description
DB08936ChlorcyclizineChlorcyclizine is a first generation phenylpiperazine class antihistamine used to treat urticaria, rhinitis, pruritus, and other allergy symptoms. Chlorcyclizine also has some local anesthetic, anticholinergic, and antiserotonergic properties, and can be used as an antiemetic.
DB01176CyclizineA 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)
DB00985DimenhydrinateDimenhydrinate, also known as Dramamine or Gravol, is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness. Dimenhydrinate is a combination drug composed of [DB01075] and [DB14132] in a salt form, with 53%-55.5% of diphenhydramine, and not less than 44%-47% of 8-chlorotheophylline, calculated on the dried basis. The antiemetic properties of dimenhydrinate are primarily thought to be produced by diphenhydramine's antagonism of H1 histamine receptors in the vestibular system [A1540] while the excitatory effects are thought to be produced by 8-chlorotheophylline's adenosine receptor blockade [A33889]. The addition of 8-chlorotheophylline was initially intended to counteract the sedative effects of diphenhydramine. When used in large doses, dimenhydrinate has been shown to cause a "high" characterized by hallucinations, excitement, incoordination, and disorientation [A1539].
DB01075DiphenhydramineDiphenhydramine, also known commercially as Benadryl, is a first generation antihistamine that is used primarily for the treatment of seasonal allergies. However, it also has antiemetic, antitussive, hypnotic, and antiparkinson properties. As histamine receptors exist both peripherally and in the central nervous system, diphenhydramine has been shown to cause sedation due to its competitive antagonism of histamine H1 receptors within the central nervous system. While its use in in allergies has largely fallen out of favour due to this sedative effect, diphenhydramine has been repurposed for use within many OTC (over the counter) cough-and-cold medications that have been marketed for "night time" use. Diphenhydramine is also used in combination with [DB14132] as the anti-nausea drug [DB00985] where it is utilized primarily for its antagonism of H1 histamine receptors within the vestibular system [A1540]. Diphenhydramine has also been shown to be implicated in a number of neurotransmitter systems that affect behaviour including dopamine, norepinephrine, serotonin, acetylcholine, and opioid [A1539]. As a result, diphenhydramine is being investigated for its anxiolytic and anti-depressant properties.
DB00737MeclizineA histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. [PubChem]
DB01069PromethazineA phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals. [PubChem]
DB00747ScopolamineAn alkaloid from Solanaceae, especially Datura metel L. and Scopola carniolica. Scopolamine and its quaternary derivatives act as antimuscarinics like atropine, but may have more central nervous system effects. Among the many uses are as an anesthetic premedication, in urinary incontinence, in motion sickness, as an antispasmodic, and as a mydriatic and cycloplegic. [PubChem]
DrugDrug NameTargetType
DB08936ChlorcyclizineHistamine H1 receptortarget
DB01176CyclizineHistamine H1 receptortarget
DB01176CyclizineEstrogen sulfotransferasetarget
DB01176CyclizineCytochrome P450 2C9enzyme
DB00985DimenhydrinateHistamine H1 receptortarget
DB01075DiphenhydramineHistamine H1 receptortarget
DB01075DiphenhydramineCytochrome P450 2D6enzyme
DB01075DiphenhydramineCytochrome P450 1A2enzyme
DB01075DiphenhydramineCytochrome P450 2C9enzyme
DB01075DiphenhydramineCytochrome P450 2C19enzyme
DB01075DiphenhydramineCytochrome P450 2C18enzyme
DB01075DiphenhydramineCytochrome P450 2B6enzyme
DB01075DiphenhydramineSolute carrier family 22 member 2transporter
DB01075DiphenhydramineSolute carrier family 22 member 1transporter
DB01075DiphenhydramineSolute carrier family 22 member 5transporter
DB01075DiphenhydramineProstaglandin G/H synthase 1enzyme
DB01075DiphenhydramineMuscarinic acetylcholine receptor M2target
DB00737MeclizineHistamine H1 receptortarget
DB00737MeclizineCytochrome P450 1A2enzyme
DB00737MeclizineNuclear receptor subfamily 1 group I member 3target
DB01069PromethazineD(2) dopamine receptortarget
DB01069PromethazineHistamine H1 receptortarget
DB01069PromethazineMuscarinic acetylcholine receptor M4target
DB01069PromethazineMuscarinic acetylcholine receptor M1target
DB01069PromethazineMuscarinic acetylcholine receptor M5target
DB01069PromethazineAlpha-1A adrenergic receptortarget
DB01069Promethazine5-hydroxytryptamine receptor 2Atarget
DB01069PromethazineMuscarinic acetylcholine receptor M2target
DB01069PromethazineMuscarinic acetylcholine receptor M3target
DB01069PromethazineCalmodulintarget
DB01069PromethazineCytochrome P450 2D6enzyme
DB01069PromethazineCytochrome P450 2B6enzyme
DB01069PromethazineMultidrug resistance protein 1transporter
DB01069PromethazineCytochrome P450 2C9enzyme
DB01069PromethazineHistamine H2 receptortarget
DB00747ScopolamineMuscarinic acetylcholine receptor M1target
DB00747ScopolamineSucrase-isomaltase, intestinaltarget
DB00747ScopolamineMuscarinic acetylcholine receptor M2target
DB00747ScopolamineMuscarinic acetylcholine receptor M3target
DB00747ScopolamineMuscarinic acetylcholine receptor M4target
DB00747ScopolamineMuscarinic acetylcholine receptor M5target
DB00747ScopolamineMultidrug resistance protein 1transporter
DB00747ScopolamineNeuronal acetylcholine receptor subunit alpha-4target
DB00747ScopolamineNeuronal acetylcholine receptor subunit beta-2target
DrugDrug NamePhaseStatusCount
DB00747Scopolamine2Completed1
DB00747Scopolamine2 / 3Terminated1