Wednesday, October 12, 2016

Dimenhydrinate


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


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


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



Dextran 6% in dextrose 5%



Dextran 6% in sodium chloride 0.9%



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



Fructose 10% in sodium chloride 0.9%



Fructose 10% in water



Invert sugar 5 and 10% in sodium chloride 0.9%



Invert sugar 5 and 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



Calcium gluconate



Chloramphenicol sodium succinate



Heparin sodium



Hydroxyzine HCl



Norepinephrine bitartrate



Penicillin G potassium



Pentobarbital sodium



Phenobarbital sodium



Potassium chloride



Prochlorperazine edisylate



Vancomycin HCl



Vitamin B complex with C



Incompatible



Thiopental sodium



Variable



Aminophylline



Ammonium chloride



Amobarbital sodium



Hydrocortisone sodium succinate









Y-site CompatibilityHID

Compatible



Acyclovir sodium



Ciprofloxacin



Fluconazole



Metronidazole



Pantoprazole sodium


ActionsActions



  • 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 (with methylparaben)



Pfizer



Tablets



50 mg*



Dramamine (scored)



Pfizer



Tablets, chewable



50 mg



Dramamine Children’s (with sorbitol and tartrazine; scored)



Pfizer



Tablets, film-coated



50 mg



TripTone Caplets (scored)



Del



Parenteral



Injection



50 mg/mL*



Dimenhydrinate Injection (with propylene glycol and benzyl alcohol)



Abraxis



Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.


The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions August 2007. 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. 14th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2007:529-35.



More Dimenhydrinate resources


  • Dimenhydrinate Side Effects (in more detail)
  • Dimenhydrinate Use in Pregnancy & Breastfeeding
  • Drug Images
  • Dimenhydrinate Drug Interactions
  • Dimenhydrinate Support Group
  • 12 Reviews for Dimenhydrinate - Add your own review/rating


  • Dimenhydrinate MedFacts Consumer Leaflet (Wolters Kluwer)

  • Dimenhydrinate Prescribing Information (FDA)

  • Dimenhydrinate Professional Patient Advice (Wolters Kluwer)

  • Dramamine MedFacts Consumer Leaflet (Wolters Kluwer)

  • dimenhydrinate Concise Consumer Information (Cerner Multum)



Compare Dimenhydrinate with other medications


  • Motion Sickness
  • Nausea/Vomiting


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