Summary

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

Background
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

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

COMBINED PRODUCT APPROVAL AGE PATIENT DOSE

INDICATION TYPE INDICATION DETAILS LEVEL GROUP CHARACTERISTICS FORM
Used in combination for Dizziness Combination Product in Prescription
symptomatic treatment combination
of with: Pyridoxine
(DB00165)
Symptomatic treatment Labyrinthine Prescription
of disorder
Symptomatic treatment Meniere's Prescription
of disease
Used in combination to Morning Combination Product in Prescription
treat sickness combination
with: Pyridoxine
(DB00165)
Prophylaxis of Motion sickness OTC Use

Pharmacodynamics
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

TARGET ACTIONS ORGANISM

AHistamine H1 receptor antagonist Humans
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

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

Toxicity
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

Indications and Dosage

Intramuscular, Intravenous Motion sickness, Nausea and vomiting, Vertigo

Adult: 50-100 mg 4 hourly via IM or IV inj over 2 minutes.

Child: 1.25 mg/kg or 37.5 mg/m² 4 times daily via IM inj. Max: 10 mg daily.

Oral
Motion sickness, Nausea and vomiting, Vertigo

Adult: 50-100 mg 4-6 hourly. Max: 300-400 mg daily. For prevention of motion sickness,
give 30 minutes to 1 hour before activity. Dosage recommendations may vary among
countries or individual products. Refer to specific product guidelines.

Child: 2-5 years 12.5-25 mg 6-8 hourly. Max: 75 mg daily; 6-<12 years 25-50 mg 6-8 hourly.
Max: 150 mg daily; ≥12 years Same as adult dose. Dosage recommendations may vary
among countries or individual products. Refer to specific product guidelines.

Rectal
Motion sickness, Nausea and vomiting, Vertigo

Adult: 1-2 supp (50-100 mg) 6-8 hourly. For prevention of motion sickness, insert into the
rectum 30 minutes (preferably 1-2 hours) before travelling.

Child: 8-12 years 1 supp (50 mg) 8-12 hourly.

Administration

tab: May be taken with or without food.

Reconstitution

IV: Dilute each mL (50 mg) of solution in 10 mL of 0.9% NaCl inj.

Incompatibility

IV: Incompatible with phenothiazine derivatives, reserpine, methoxamine

hydrochloride, pentobarbital Na, thiamylal Na, nicotinic acid, pyridoxine
hydrochloride and certain antibiotic solutions (e.g. chloramphenicol succinate).

May cause precipitation when mixed with solutions of tetracycline hydrochloride in

dextrose inj and when mixed with novobiocin Na in NaCl solution.

Special Precautions

Patient with CV disease (e.g. arrhythmias, hypertension, ischaemic heart disease), prostatic
hyperplasia and/or genitourinary obstruction, pyloroduodenal obstruction (e.g. stenotic
peptic ulcer), history of asthma or lower respiratory tract symptoms, seizure disorders,
thyroid dysfunction, increased intraocular pressure or angle-closure glaucoma. Hepatic
impairment. Children and elderly. Pregnancy and lactation.

Adverse Reactions
Significant: Sedation; excitation in children.
Cardiac disorders: Tachycardia.
Eye disorders: Blurred vision.
Gastrointestinal disorders: Dry mouth, epigastric distress.
General disorders and administration site conditions: Lassitude.
Metabolism and nutrition disorders: Anorexia.
Musculoskeletal and connective tissue disorders: Muscular weakness.
Nervous system disorders: Dizziness, headache.
Psychiatric disorders: Nervousness, restlessness, insomnia (especially in children).
Renal and urinary disorders: Difficult or painful urination.
Respiratory, thoracic and mediastinal disorders: Thickening of bronchial
secretions, dry nose and throat.
Skin and subcutaneous tissue disorders: Rash.
Vascular disorders: Hypotension.

Pregnancy Category (US FDA)

IM/IV/Parenteral/PO/Rectal: B

Patient Counseling Information

This drug may cause CNS depression (e.g. drowsiness, impaired mental alertness), if
affected, do not drive or operate machinery.

Monitoring Parameters
Monitor for anticholinergic side effects (e.g. confusion, constipation).
Overdosage

Symptoms: Dilated pupils, flushed face, excitation, hallucinations, confusion,

ataxia, intermittent clonic convulsions, coma, cardiorespiratory collapse (children); extreme
difficulty in speech and swallowing, cycle of CNS excitation, seizures and postictal
depression (adult). Management: Symptomatic and supportive treatment. In the absence of
seizures, performing early gastric lavage (with an endotracheal tube with cuff inflated in
place to prevent aspiration of gastric contents) is beneficial. In case of seizures, may give
diazepam (in adults) or phenobarbital (in children). Mechanical respiratory assistance may be
necessary.

Drug Interactions

May mask the warning symptoms of ototoxicity by ototoxic drugs (e.g. aminoglycoside
antibiotics). May potentiate the effects of anticholinergic drugs (e.g TCAs) and
antiparkinsonian drugs (e.g. trihexyphenidyl). May enhance the effects of CNS depressants
(e.g. narcotic analgesics, barbiturates).

Food Interaction
May enhance the CNS depressant effect of alcohol.

Action

Description:

Mechanism of Action:
Dimenhydrinate is a monoethanolamine derivative with CNS depressant, anticholinergic,
antiemetic, antihistaminic and local anaesthetic effects. Its exact mechanism of antiemetic
action is unknown; however, it is believed to inhibit acetylcholine. It has a central
anticholinergic activity that blocks the chemoreceptor trigger zone, diminishes vestibular
stimulation, and reduces labyrinthine function. Additionally, it competes with histamine in
binding for H₁-receptor sites on effector cells in the gastrointestinal tract, blood vessels,
and respiratory tract.

Onset: Antiemetic: 15-30 minutes (oral); immediate (IV); 20-30 minutes (IM).

Duration: 3-6 hours.

‫ ديمينهيدرينات مع الطعام لتجنب اضطراب المعدة‬،‫تناول سيناريزين‬

:‫عدد الجرعات‬
.‫مرات في اليوم‬: 3 – 4 ‫الجرعة اليومية‬
.‫ ساعة‬24 ‫مرة الل‬: 1 ‫الجرعة القصوى‬
:‫الجرعة‬
.‫ملليغرام يومييا‬50 - 400