Dimenhydrinate is a medication used to prevent and treat nausea, vomiting, vertigo, and motion sickness.

Brand Names
Dramamine, Driminate, Gravol
Generic Name
DrugBank Accession Number

Dimehydrinate was first described in the literature in 1949,5 and patented in 1950.11 Early research into dimenhydrinate focused on its role as an antihistamine for urticaria; the treatment of motion sickness was an accidental discovery.7

Dimenhydrinate, also known as B-dimethylaminoethyl benzohydrol ether 8-chlorotheophyllinate, is indicated to prevent nausea, vomiting, and dizziness caused by motion sickness.9,10,11 Dimenhydrinate is a combination of Diphenhydramine and 8-chlorotheophylline in a salt form, with 53%-55.5% dried diphenhydramine, and 44%-47% died 8-chlorotheophylline.10

The antiemetic properties of dimenhydrinate are primarily thought to be produced by diphenhydramine's antagonism of H1 histamine receptors in the vestibular system2 while the excitatory effects are thought to be produced by 8-chlorotheophylline's adenosine receptor blockade.3

When used in large doses, dimenhydrinate has been shown to cause a "high" characterized by hallucinations, excitement, incoordination, and disorientation.1

Dimenhydrinate was granted FDA approval on 31 May 1972.8

Small Molecule
Average: 469.97
Monoisotopic: 469.1880675
Chemical Formula
  • (O-benzhydryl(dimethylamino)ethanol) 8-chlorotheophyllinate
  • 8-chloro-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione - 2-(diphenylmethoxy)-N,N-dimethylethanamine (1:1)
  • Benzhydryl-β-dimethylaminoethylether 8-chlorotheophylline
  • Dimenhidrinato
  • Dimenhydrinate
  • Dimenhydrinatum
  • diphenhydramine 8-chlorotheophyllinate
  • diphenhydramine 8-chlorotheophylline
  • Diphenhydramine theoclate
  • N,N-dimethyl-2-diphenylmethoxyethylamine 8-chlorotheophyllinate
  • O-benzhydryldimethylaminoethanol 8-chlorotheophyllinate
  • β-dimethylaminoethyl benzhydryl ether 1,3-dimethyl-8-chloroxanthine



Dimenhydrinate is indicated for the prevention and treatment of nausea, vomiting, or vertigo of motion sickness.9,10

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Associated Conditions
Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug events
Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events & improve clinical decision support.
Learn more

Dimenhydrinate is indicated for the prevention and treatment of nausea, vomiting, or vertigo of motion sickness.9,10 It has a short duration of action of 4-8 hours.4 Patients should be counselled regarding pronounced drowsiness, avoiding alcohol and other sedatives, and exercising caution when operating a motor vehicle or heavy machinery.9

Mechanism of action

Dimenhydrinate is a theoclate salt that separates into diphenhydramine and 8-chlorotheophylline.10,13 While the exact mechanism of action is unknown, diphenhydramine is theorized to reduce disturbances to equilibrium through antimuscarinic effects or histamine H1 antagonism.7 8-chlorotheophylline may produce excitation through blocking adenosine receptors, reducing the drowsiness produced by diphenhydramine.13

AHistamine H1 receptor

A 50 mg oral film coated tablet reaches a Cmax of 72.6 ng/mL with a Tmax of 2.7 hours.12 A 100 mg suppository reaches a Cmax of 112.2 ng/mL with a Tmax of 5.3 hours.13

Volume of distribution

The volume of distribution of dimenhydrinate is 3-4 L/kg.12

Protein binding

Dimenhydrinate is 70-85% protein bound in plasma.12


Dimenhydrinate is a theoclate salt that separates into diphenhydramine and 8-chlorotheophylline.10 diphenhydramine can either be N-glucuronidated by UGTs to diphenhydramine N-glucuronide or N-demethylated by CYP2D6, CYP1A2, CYP2C9, and CYP2C19 to N-desmethyldiphenhydramine.6 N-desmethyldiphenhydramine can be N-demethylated again by the same enzymes to N,N-didesmethyldiphenhydramine, which undergoes oxidative deamination to form diphenylmethoxyacetic acid.6

Hover over products below to view reaction partners

Route of elimination

Dimenhydrinate is predominantly eliminated in the urine.12 1-3% of the dissociated diphenhydramine is eliminated in the urine unchanged, while 64% of diphenhydramine is eliminated in the urine as metabolites.13 The elimination of dimenhydrinate has not been fully studied.13


The plasma elimination half life of dimenhydrinate is 5-8 hours.12


Not Available

Adverse Effects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Learn more
Improve decision support & research outcomes with our structured adverse effects data.
Learn more

Infants and children experiencing an overdose may lead to hallucinations, convulsions, or death.10 Adults experiencing an overdose may present with drowsiness, convulsions, coma, or respiratory depression.10 Treat overdoses with symptomatic and supportive measures including mechanically assisted ventilation.10

In mice the oral LD50 is 203 mg/kg, while in rats it is 1320 mg/kg.10 The intraperitoneal LD50 in mice is 149 mg/kg.10

Not Available
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with 1,2-Benzodiazepine.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Dimenhydrinate.
AcetophenazineThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Acetophenazine.
AclidiniumDimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
AcrivastineThe risk or severity of QTc prolongation can be increased when Acrivastine is combined with Dimenhydrinate.
AdenosineThe risk or severity of QTc prolongation can be increased when Adenosine is combined with Dimenhydrinate.
AgomelatineThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Agomelatine.
AjmalineThe risk or severity of QTc prolongation can be increased when Ajmaline is combined with Dimenhydrinate.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Dimenhydrinate.
AlfuzosinThe risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Dimenhydrinate.
Identify potential medication risks
Easily compare up to 40 drugs with our drug interaction checker.
Get severity rating, description, and management advice.
Learn more
Food Interactions
  • Avoid alcohol.


Drug product information from 10+ global regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
Active Moieties
Product Images
International/Other Brands
Gravol (Church & Dwight) / Vertirosan (Astellas) / Vomex A (Astellas) / Xamamina (Adilna)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Dimenhydrinate Inj 10mgLiquid10 mg / mLIntravenousSandoz Canada Incorporated1973-12-31Not applicableCanada flag
Dimenhydrinate Inj 10mg/mlLiquid10 mg / mLIntravenousAstra Pharma Inc.1986-12-311999-07-29Canada flag
Dimenhydrinate Inj 50mg USPLiquid50 mg / mLIntramuscular; IntravenousSandoz Canada Incorporated1973-12-31Not applicableCanada flag
Dimenhydrinate Injection 50mg/mlSolution50 mg / mLIntramuscular; IntravenousAstra Zeneca1986-12-312005-05-31Canada flag
Dimenhydrinate Injection USPSolution250 mg / 5 mLIntramuscular; IntravenousHikma Canada Limited2016-01-28Not applicableCanada flag
Dimenhydrinate Injection USPSolution50 mg / mLIntramuscular; IntravenousHikma Canada Limited2016-01-28Not applicableCanada flag
Dimenhydrinate Injection USP 250mg/5ml (50mg/ml)Solution50 mg / mLIntramuscular; IntravenousTeligent Ou2008-06-262022-02-01Canada flag
Dimenhydrinate Injection, USPSolution50 mg / mLIntramuscular; IntravenousMylan Pharmaceuticals1994-12-31Not applicableCanada flag
Gravol ImSolution50 mg / mLIntramuscularChurch & Dwight Canada Corp1953-12-31Not applicableCanada flag
Gravol IV AmpoulesSolution10 mg / mLIntravenousChurch & Dwight Canada Corp1953-12-312008-07-30Canada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DimenhydrinateInjection, solution50 mg/1mLIntramuscular; IntravenousFresenius Kabi USA, LLC2004-11-29Not applicableUS flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ag-dimenhydrinateTablet50 mgOralAngita Pharma Inc.Not applicableNot applicableCanada flag
Airmit AceTablet25 mg/1OralSato Pharmaceutical Co., Ltd.2005-03-11Not applicableUS flag
Anti-nauseantTablet50 mgOralVita Health Products Inc2000-05-01Not applicableCanada flag
Anti-nauseantTablet50 mgOralPharmascience IncNot applicableNot applicableCanada flag
Anti-nauseantTablet50 mgOralPharmascience Inc2002-08-23Not applicableCanada flag
Anti-nauseantTablet50 mgOralApotex Corporation2013-07-02Not applicableCanada flag
Anti-nauseantTablet50 mgOralTEVA Canada LimitedNot applicableNot applicableCanada flag
Anti-nauseant Liquid GelsCapsule50 mgOralVita Health Products Inc2020-08-04Not applicableCanada flag
Anti-nauseant TabletTablet50 mgOralStanley Pharmaceuticals, A Division Of Vita Health Products Inc.1998-05-262008-08-07Canada flag
Apo Dimenhydrinate Tab 50mgTablet50 mgOralApotex Corporation1977-12-31Not applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Arlevert 20 mg/40 mg TablettenDimenhydrinate (40 mg) + Cinnarizine (20 mg)TabletOralHennig Arzneimittel Gmb H & Co Kg2007-09-06Not applicableAustria flag
Gravergol CapsulesDimenhydrinate (50 mg) + Caffeine (100 mg) + Ergotamine tartrate (1 mg)CapsuleOralCan Med Pharma Inc.1957-12-312011-12-07Canada flag
Neo - Emedyl - DrageesDimenhydrinate (50 mg) + Caffeine (50 mg)Tablet, sugar coatedOralPharmazeutische Fabrik Montavit Gmb H1965-05-20Not applicableAustria flag
Vertirosan Vitamin B6 - ZäpfchenDimenhydrinate (50 mg) + Pyridoxine hydrochloride (50 mg)SuppositoryRectalSigmapharm Arzneimittel Gmb H1962-03-29Not applicableAustria flag
มาโนไดสิคDimenhydrinate (50 MG) + Pyridoxine (20 MG)Tabletบริษัท โรงงานเภสัชกรรมแหลมทองการแพทย์ จำกัด จำกัด1986-12-30Not applicableThailand flag
เวนซิกซ์Dimenhydrinate (50 MG) + Pyridoxine (10 MG)Capsuleบริษัท โมเดิร์น ฟาร์มา จำกัด2013-01-14Not applicableThailand flag
เวอร์ตามินDimenhydrinate (25 MG) + Pyridoxine (25 MG)Tablet, sugar coatedOralห้างหุ้นส่วนจำกัด โรงงานเลิศสิงห์เภสัชกรรม1985-04-02Not applicableThailand flag


ATC Codes
R06AA11 — Dimenhydrinate
Drug Categories
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

CAS number
InChI Key
8-chloro-1,3-dimethyl-2,3,6,9-tetrahydro-1H-purine-2,6-dione; [2-(diphenylmethoxy)ethyl]dimethylamine


Synthesis Reference

Cusic, J.W.; U.S. Patent 2,499,058; February 28,1950; assigned to G.D. Searle & Co. Cusic, J.W.; U.S. Patent 2,534,813; December 19,1950; assigned to G.D. Searle & Co.

General References
  1. Halpert AG, Olmstead MC, Beninger RJ: Mechanisms and abuse liability of the anti-histamine dimenhydrinate. Neurosci Biobehav Rev. 2002 Jan;26(1):61-7. [Article]
  2. Jaju BP, Wang SC: Effects of diphenhydramine and dimenhydrinate on vestibular neuronal activity of cat: a search for the locus of their antimotion sickness action. J Pharmacol Exp Ther. 1971 Mar;176(3):718-24. [Article]
  3. Spealman RD: Psychomotor stimulant effects of methylxanthines in squirrel monkeys: relation to adenosine antagonism. Psychopharmacology (Berl). 1988;95(1):19-24. [Article]
  4. Koch A, Cascorbi I, Westhofen M, Dafotakis M, Klapa S, Kuhtz-Buschbeck JP: The Neurophysiology and Treatment of Motion Sickness. Dtsch Arztebl Int. 2018 Oct 12;115(41):687-696. doi: 10.3238/arztebl.2018.0687. [Article]
  5. FLEMING JF: New drug effective in motion sickness. Hosp Top. 1949 Mar;27(3):26. [Article]
  6. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
  7. FERMIN H, van DEINSE JB, HAMMELBURG E: The effect of dimenhydrinate upon the labyrinth; (an experimental study). Acta Otolaryngol. 1950 Dec;38(6):543-9. doi: 10.3109/00016485009118417. [Article]
  8. FDA Approved Drug Products: Dimenhydrinate Oral Liquid (Discontinued) [Link]
  9. Dailymed: Dimenhydrinate Oral Tablet [Link]
  10. Dailymed: Dimenhydrinate Intramuscular and Intravenous Injection [Link]
  11. US Patent: US2499058A [Link]
  12. Sandoz Canada: Dimenhydrinate Intramuscular and Intravenous Injection [Link]
  13. Heads of Medicines Agencies Public Assessment Report: Dimenhydrinate Oral Lozenge [Link]
Human Metabolome Database
PubChem Compound
PubChem Substance
Therapeutic Targets Database
PA449338 Drug Page
Download (72 KB)

Clinical Trials

Clinical Trials
4CompletedPreventionPost Operative Nausea and Vomiting (PONV)1
4CompletedTreatmentNausea / Vertigo / Vomiting1
4CompletedTreatmentPain / Postoperative pain1
4CompletedTreatmentVertigo, Peripheral1
3Unknown StatusTreatmentVertigo, Peripheral1
2CompletedTreatmentPost Operative Nausea and Vomiting (PONV)1
1CompletedTreatmentHealthy Subjects (HS)1
Not AvailableCompletedTreatmentNausea / Vomiting1


  • App pharmaceuticals llc
  • Baxter healthcare corp anesthesia and critical care
  • Watson laboratories inc
  • Wyeth ayerst laboratories
  • Alra laboratories inc
  • Heather drug co inc
  • Nexgen pharma inc
  • APP Pharmaceuticals
  • C.O. Truxton Inc.
  • Consolidated Midland Corp.
  • Dispensing Solutions
  • Hospira Inc.
  • Ivax Pharmaceuticals
  • Major Pharmaceuticals
  • Martin Surgical Supply
  • Medisca Inc.
  • Nexgen Pharma Inc.
  • Pfizer Inc.
  • Pharmacia Inc.
  • Prescript Pharmaceuticals
  • Southwood Pharmaceuticals
Dosage Forms
TabletOral25 mg/1
Tablet, coatedOral50 mg
SolutionOral15 mg / 5 mL
SuppositoryRectal50 mg
Injection, solutionIntramuscular; Intravenous50 mg/1mL
Tablet50 MG
TabletOral50 mg/1
Tablet, film coatedOral50 mg/1
LiquidIntravenous10 mg / mL
LiquidIntramuscular; Intravenous50 mg / mL
SolutionIntramuscular; Intravenous50 mg / mL
SolutionIntramuscular; Intravenous250 mg / 5 mL
LiquidOral15 mg / 5 mL
TabletOral50.0 mg
Tablet, chewableOral50 mg/1
Tablet, chewableOral25 mg/1
Capsule, liquid filledOral50 mg/1
Capsule, extended releaseOral75 mg
Tablet, chewableOral50 mg
TabletOral15 mg
SolutionIntramuscular50 mg / mL
Tablet, multilayerOral100 mg
SolutionIntravenous10 mg / mL
Tablet, extended releaseOral75 mg
SuppositoryRectal100 mg
TabletOral25 mg
Tablet, chewableOral15 mg
SyrupOral15 mg / 5 mL
SuppositoryRectal25 mg
SyrupOral25 mg/5ml
Tablet, coatedOral50 mg/1
TabletOral0.05 g
SolutionOral0.25 g
SyrupOral3 mg / mL
Gum, chewingOral
Gum, chewingOral20 MG
Tablet, sugar coatedOral
Tablet, coatedOral100 MG
Tablet, coatedOral25 MG
Injection, solutionIntramuscular; Intravenous150 mg/ml
Injection, solutionIntramuscular; Intravenous50 mg/ml
Solution / dropsOral92.5 mg/ml
Tablet, coatedOral
Tablet, orally disintegratingSublingual
SuppositoryRectal150 MG
SuppositoryRectal70 MG
SuppositoryRectal40 MG
Tablet, orally disintegratingSublingual50 MG
InjectionIntramuscular; Intravenous
InjectionIntramuscular; Intravenous50 mg/ml
CapsuleOral50 mg
Tablet, film coatedOral50 mg
Tablet, sugar coatedOral
Solution50 mg/1ml
TabletOral50 mg
Tablet, sugar coatedOral50 mg
SyrupOral15 mg/5ml
Unit descriptionCostUnit
Dimenhydrinate 50 mg/ml vial5.7USD ml
Dimenhydrinate I.M. 50 mg/ml1.17USD ml
Meclizine 12.5 mg tablet0.62USD tablet
Dramamine less drowsy tablet0.42USD tablet
Dimenhydrinate I.V. 10 mg/ml0.32USD ml
Dramamine 50 mg tablet0.28USD tablet
Novamine 15% iv solution0.09USD ml
Dimenhydrinate 100% powder0.07USD g
Driminate 50 mg tablet0.05USD tablet
Dimenhydrinate 50 mg tablet0.03USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Not Available


Experimental Properties
melting point (°C)103-104Cusic, J.W.; U.S. Patent 2,499,058; February 28,1950; assigned to G.D. Searle & Co. Cusic, J.W.; U.S. Patent 2,534,813; December 19,1950; assigned to G.D. Searle & Co.
water solubility3000 mg/LMERCK INDEX (1996); approx.
Predicted Properties
Water Solubility9.86 mg/mLALOGPS
pKa (Strongest Basic)8.87ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.47 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity79.93 m3·mol-1ChemAxon
Polarizability30.02 Å3ChemAxon
Number of Rings4ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Human Intestinal Absorption+0.9975
Blood Brain Barrier+0.8551
Caco-2 permeable+0.5198
P-glycoprotein substrateSubstrate0.7863
P-glycoprotein inhibitor INon-inhibitor0.6923
P-glycoprotein inhibitor IIInhibitor0.6502
Renal organic cation transporterNon-inhibitor0.6507
CYP450 2C9 substrateNon-substrate0.7536
CYP450 2D6 substrateNon-substrate0.8181
CYP450 3A4 substrateSubstrate0.7086
CYP450 1A2 substrateInhibitor0.5287
CYP450 2C9 inhibitorNon-inhibitor0.6308
CYP450 2D6 inhibitorNon-inhibitor0.8589
CYP450 2C19 inhibitorNon-inhibitor0.5817
CYP450 3A4 inhibitorNon-inhibitor0.9028
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5738
Ames testNon AMES toxic0.5629
BiodegradationNot ready biodegradable0.8211
Rat acute toxicity2.4087 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5364
hERG inhibition (predictor II)Inhibitor0.5405
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)


Mass Spec (NIST)
Not Available
Not Available


Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Pharmacological action
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
Uniprot ID
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. Halpert AG, Olmstead MC, Beninger RJ: Mechanisms and abuse liability of the anti-histamine dimenhydrinate. Neurosci Biobehav Rev. 2002 Jan;26(1):61-7. [Article]

Drug created at June 13, 2005 13:24 / Updated at October 04, 2022 23:16