Dimenhydrinate

Pronunciation

Class: Antihistamines
ATC Class: A04AD
CAS Number: 523-87-5
Brands: DMH, Dramamine, TripTone

Introduction

Ethanolamine-derivative antihistamine containing a diphenhydramine moiety; antiemetic.b

Uses for Dimenhydrinate

Motion Sickness

Used principally in the prevention and treatment of nausea, vomiting, and/or vertigo associated with motion sickness, although scopolamine, promethazine, or meclizine may be more effective.b

Most effective when given prophylactically.b

Slideshow: Is it Safe to Give Human Medicine to Pets?

Always get your pet's drug and dose recommendation from the veterinarian.

Ménière’s Disease and Other Vestibular Disturbances

Has been used for symptomatic treatment (e.g., nausea, vomiting, vertigo) of Ménière’s disease and other vestibular disturbances.b

Nausea and Vomiting

May be less effective than phenothiazines in controlling nausea and vomiting not related to vestibular stimulation.b

Allergic Conditions

Although a histamine antagonist, use in allergic conditions has not been evaluated.b

Dimenhydrinate Dosage and Administration

Administration

Administer orally or by IM or IV injection.a b

IV Injection

For solution and drug compatibility information, see Compatibility under Stability.

Dilution

Each 50 mg must be diluted with 10 mL of 0.9% sodium chloride injection.b

Rate of Administration

Inject IV slowly over a period of 2 minutes.b

Dosage

Pediatric Patients

Motion Sickness
Oral

For prevention, take 30 minutes before exposure to motion.b

Children <2 Years of Age: Give only under the direction of a clinician.100 101

Children 2 to <6 Years of Age: 12.5–25 mg every 6–8 hours, not to exceed 75 mg in 24 hours, or as directed by a clinician.100 101 102

Children 6 to <12 Years of Age: 25–50 mg every 6–8 hours, not to exceed 150 mg in 24 hours, or as directed by a clinician.100 101 102

Children ≥12 Years of Age: Usually, 50–100 mg every 4–6 hours, not to exceed 400 mg in 24 hours, or as directed by a clinician.100 101 102

Children: Alternatively, 1.25 mg/kg or 37.5 mg/m2 4 times daily, up to a maximum of 300 mg daily.b

IM

Children: 1.25 mg/kg or 37.5 mg/m2 4 times daily, up to a maximum of 300 mg daily.b

IV

Not established for children.b

Adults

Motion Sickness
Oral

For prevention, take 30 minutes before exposure to motion.b

Usually 50–100 mg every 4–6 hours, not to exceed 400 mg in 24 hours, or as directed by a clinician.100 101 102

IM

50–100 mg every 4–6 hours, not to exceed 400 mg in 24 hours, or as directed by a clinician.b

IV

50–100 mg every 4–6 hours, not to exceed 400 mg in 24 hours, or as directed by a clinician.b

Ménière’s Disease and Other Vestibular Disturbances
Maintenance of Symptomatic Relief
Oral

25–50 mg has been given 3 times daily.b

Acute Attacks
IM

50 mg.b

Prescribing Limits

Pediatric Patients

Motion Sickness
Oral

Children 2 to <6 Years of Age: Maximum 75 mg in 24 hours, or as directed by a clinician.100 101 102

Children 6 to <12 Years of Age: Maximum 150 mg in 24 hours, or as directed by a clinician.100 101 102

Children ≥12 Years of Age: Maximum 400 mg in 24 hours, or as directed by a clinician.100 101 102

Children: Alternatively, maximum 300 mg daily when given as 1.25 mg/kg or 37.5 mg/m2.b

IM

300 mg daily.b

Adults

Motion Sickness
Oral

Maximum 400 mg in 24 hours, or as directed by a clinician.100 101 102

IM

Maximum 400 mg in 24 hours, or as directed by a clinician.b

IV

Maximum 400 mg in 24 hours, or as directed by a clinician.b

Special Populations

Hepatic Impairment

No specific dosage recommendations for hepatic impairment.a b

Renal Impairment

No specific dosage recommendations for renal impairment.a b

Geriatric Patients

No specific geriatric dosage recommendations.a

Cautions for Dimenhydrinate

Contraindications

  • Dimenhydrinate contains 53–55.5% diphenhydramine.a b Concomitant use with other preparations containing diphenhydramine, including oral and topical preparations, is contraindicated.

  • Known hypersensitivity to dimenhydrinate, other antihistamines with similar chemical structure, or any ingredient in the formulation.

Warnings/Precautions

Warnings

Concomitant Diseases

Patients with glaucoma, respiratory conditions (e.g., emphysema, chronic bronchitis), or difficulty urinating due to prostatic hypertrophy should consult a clinician before initiating therapy with dimenhydrinate.a b

Use with caution in patients with increased IOP, narrow-angle glaucoma, stenosing peptic ulcer, pyloroduodenal obstruction, bladder-neck obstruction, symptomatic prostatic hypertrophy, active or a history of lower respiratory disease (e.g., bronchial asthma), hyperthyroidism, or cardiovascular disease (e.g., hypertension).a b

CNS Effects

Risk of marked drowsiness.c Among first generation antihistamines, ethanolamines (e.g., dimenhydrinate) considered the most sedating.c

Performance of activities requiring mental alertness or physical coordination may be impaired.a b

Concurrent use of other CNS depressants may cause additive or potentiated CNS depression.a

Diphenhydramine Toxicity

Dimenhydrinate contains 53–55.5% diphenhydramine.a b Risk of diphenhydramine toxicity. (See Pediatric Use under Cautions.) Do not use more often than directed for any condition or use concomitantly with other diphenhydramine-containing preparations, including oral and topical preparations.

Sensitivity Reactions

Tartrazine Sensitivity

Dramamine chewable tablets contain tartrazine (FD&C yellow No. 5), which may cause allergic reactions including bronchial asthma in susceptible individuals.a b Incidence of tartrazine sensitivity is low, but it frequently occurs in patients who are sensitive to aspirin.b

General Precautions

Anticholinergic Effects

Consider anticholinergic effects in patients with conditions aggravated by anticholinergic therapy (e.g., angle-closure glaucoma, enlargement of the prostate gland).b (See Concomitant Diseases under Cautions.)

Ototoxic Drugs

Symptoms of ototoxicity may be masked by dimenhydrinate; administer with caution in patients receiving known ototoxic drugs and closely monitor.b

Seizure Disorders

Use with caution in seizure disorders.b

Specific Populations

Pregnancy

Category C.PDH

Lactation

Distributed into milk.b Discontinue nursing or the drug.b

Pediatric Use

Do not use in children <2 years of age unless directed by a clinician.a

Risk of diminished mental alertness. Risk of excitation in young pediatric patients.b

Risk of diphenhydramine toxicity (e.g., dilated pupils, flushed face, hallucinations, ataxic gait, urinary retention) when used concomitantly with other diphenhydramine-containing preparations, including oral and topical preparations. (See Diphenhydramine Toxicity under Cautions.)

Common Adverse Effects

Drowsiness, headache, blurred vision, tinnitus, dryness of the mouth and respiratory passages, incoordination, palpitation, dizziness, hypotension.b

Paradoxical CNS stimulation in pediatric patients and occasionally in adults.b

With IM injection: Pain at the injection site.b

Because dimenhydrinate contains diphenhydramine, the possibility of other diphenhydramine-related adverse effects should also be considered.b

Interactions for Dimenhydrinate

Drugs Metabolized by Hepatic Microsomal Enzymes

Although dimenhydrinate has been reported to induce hepatic microsomal enzymes in animals, there is no clinical evidence that it influences the metabolism of other drugs in humans.b

Specific Drugs

Drug

Interaction

Comments

Anticholinergic drugs

Anticholinergic effects may be potentiatedb

Antidepressants, tricyclic

Anticholinergic effects may be potentiatedb

CNS depressants

May enhance the effects of other CNS depressants, including alcoholb

Use concomitantly with cautionb

Ototoxic drugs

May mask the early manifestations of ototoxicityb

Use concomitantly with caution and closely monitorb

Dimenhydrinate Pharmacokinetics

Absorption

Bioavailability

Well absorbed after oral or parenteral administration.b

Onset

IV injection: Antiemetic effects occur almost immediately.b

Oral administration: Antiemetic effects within 15–30 minutes.b

IM injection: Antiemetic effects within 20–30 minutes.b

Duration

3–6 hours.b

Distribution

Extent

Probably widely distributed into body tissues.b

Crosses the placenta.b

Small amounts are distributed into milk.b

Elimination

Metabolism

Metabolized by the liver.b

Elimination Route

Excreted in urine.b

Stability

Storage

Well-closed containers at room temperature.b d

Oral

Solution

Tight containers.b d Avoid freezing.b

Tablets

Well-closed containers at room temperature.b d

Parenteral

Injection

Avoid freezing.b

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution CompatibilityHID

Compatible

Dextrose–Ringer’s injection combinations

Dextrose–Ringer’s injection, lactated, combinations

Dextrose–saline combinations

Dextrose 5% in sodium chloride 0.9%

Dextrose 2.5, 5, or 10% in water

Ionosol products

Ringer’s injection

Ringer’s injection, lactated

Sodium chloride 0.45 or 0.9%

Sodium lactate (1/6) M

Drug Compatibility
Admixture CompatibilityHID

Compatible

Amikacin sulfate

Ammonium chloride

Chloramphenicol sodium succinate

Heparin sodium

Hydroxyzine HCl

Norepinephrine bitartrate

Penicillin G potassium

Pentobarbital sodium

Phenobarbital sodium

Potassium chloride

Prochlorperazine edisylate

Vancomycin HCl

Variable

Aminophylline

Hydrocortisone sodium succinate

Y-site CompatibilityHID

Compatible

Acyclovir sodium

Ciprofloxacin

Fluconazole

Metronidazole

Pantoprazole sodium

Actions

  • Most actions are believed to result principally from its diphenhydramine moiety.b

  • Has CNS depressant, anticholinergic, antiemetic, antihistaminic, and local anesthetic effects.b

  • Has been shown to inhibit vestibular stimulation, acting first on the otolith system, and in larger doses on the semicircular canals.b

  • Inhibits acetylcholine; this may be its primary mechanism of action, since cholinergic stimulation in the vestibular and reticular systems may be responsible for the nausea and vomiting of motion sickness.b

  • Tolerance to CNS depressant effects usually occurs after a few days of treatment, and some decrease in antiemetic effectiveness may be noted after prolonged use.b

Advice to Patients

  • Potential for drug to impair mental alertness or physical coordination; avoid driving or operating machinery until effects on individual are known.a b

  • Importance of warning patients with tartrazine or aspirin sensitivity that Dramamine chewable tablets contain the dye tartrazine (FD&C yellow No. 5), which may cause allergic reactions including bronchial asthma.a b .

  • Importance of not using multiple diphenhydramine-containing preparations (either oral or topical) simultaneously because of risk of toxicity. (See Diphenhydramine Toxicity under Cautions.)

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs as well as any concomitant illnesses.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Dimenhydrinate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Solution

12.5 mg/5 mL*

DMH Syrup

Alra

Dramamine Children’s

Pfizer

Tablets

50 mg*

Dramamine (scored)

Pfizer

Tablets, chewable

50 mg

Dramamine Children’s (scored)

Pfizer

Tablets, film-coated

50 mg

TripTone Caplets (scored)

Del

Parenteral

Injection

50 mg/mL*

Dimenhydrinate Injection

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions June 20, 2013. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

100. Food and Drug Administration. Antiemetic drug products for over-the-counter human use; final monograph. Fed Regist. 1987; 52:15886-93.

101. Richardson-Vicks Inc. Dramamine Liquid, Dramamine tablets, and Dramamine Chewable tablets prescribing information. In: Huff BB, ed. Physicians’ desk reference. 42nd ed. Oradell, NJ: Medical Economics Company Inc; 1988(Suppl A):A30-1.

102. Food and Drug Administration. Over-the-counter drug products; final monographs for antiemetic, antitussive, bronchodilator, and antihelmintic drug products; updating and technical changes Fed Regist. 1988; 53:35808-10. (21 CFR Parts 336, 341, and 357 [Docket No. 88N-0070])

556. Food and Drug Administration. Labeling of diphenhydramine-containing drug products for over-the-counter human use. 21 CFR Parts 336, 338, 341, 348. Proposed rule. [Docket No. 97N-0128] Fed Regist. 1997; 62:45767-74.

557. Chan CYJ, Wallander KA. Diphenhydramine toxicity in three children with varicella- zoster infection. DICP. 1991; 25:130-2. [IDIS 278321] [PubMed 2058184]

575. McGann KP, Pribanich S, Graham JA et al. Diphenhydramine toxicity in a child with varicella: a case report. J Fam Pract. 1992; 35:210,213-4. [PubMed 1645115]

576. Woodward GA, Baldassano RN. Topical diphenhydramine toxicity in a five year old with varicella. Pediatr Emerg Care. 1988; 4:18-20. [PubMed 3362727]

672. Food and Drug Administration. Labeling of diphenhydramine-containing drug products for over-the-counter human use. 21 CFR Parts 336, 338, 341, 348. Final rule. [Docket No. 97N-0128] Fed Regist. 2002; 67:72555-9.

a. Pharmacia Consumer Healthcare. Dramamine (dimenhydrinate) Original Formula and Chewable tablets prescribing information. Peapack, NJ: 2004 Apr.

b. AHFS drug information 2004. McEvoy GK, ed. Dimenhydrinate. American Society of Health-System Pharmacists; 2004: 2786-7.

c. AHFS drug information 2004. McEvoy GK, ed. Antihistamines general statement. American Society of Health-System Pharmacists; 2004:2-9.

d. The United States pharmacopeia, 27th rev, and The national formulary, 22nd ed. Rockville, MD: The United States Pharmacopeial Convention, Inc; 2004:10,628-31.

PDH. Schilling McCann JA, Publisher. Pharmacists drug handbook. 2nd ed. Philadelphia, PA: Lippincott Williams and Wilkins and American Society of Health-System Pharmacists; 2003.

HID. Trissel LA. Handbook on injectable drugs. 17th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2013:372-6.

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