Dimenhydrinate

Pharmacologic Category

Ethanolamine Derivative; Histamine H1 Antagonist; Histamine H1 Antagonist, First Generation

Dosing: Adult

US labeling: Motion sickness, nausea/vomiting, or vertigo:

Oral: 50 to 100 mg every 4 to 6 hours (maximum: 400 mg/day)

IM, IV: 50 mg every 4 hours; maximum: 100 mg every 4 hours

Canadian labeling: Nausea/vomiting or vertigo:

Motion sickness:

Oral: 50 to 100 mg every 4 hours as necessary (maximum: 400 mg/day); Long acting formulation: 100 mg every 8 to 12 hours (maximum: 300 mg/day)

Rectal: 50 to 100 mg every 6 to 8 hours as necessary

Postoperative nausea/vomiting:

Oral: 50 to 100 mg prior to procedure then 50 to 100 mg post-procedure; repeat as necessary (maximum: 400 mg/day)

IM, IV: 50 mg prior to treatment then 50 mg post-procedure; repeat as necessary (maximum: 400 mg/day)

Radiation sickness:

IM, IV: 50 to 100 mg 30 to 60 minutes prior to treatment; 50 mg 1.5 and 3 hours after treatment. Repeat dose as necessary (maximum: 400 mg/day)

Rectal: 50 to 100 mg 30 to 60 minutes prior to treatment; repeat as necessary (maximum: 400 mg/day)

Nausea and vomiting of pregnancy (off-label use) (Arsenault 2002):

Oral, rectal: 50 to 100 mg every 4 to 6 hours; maximum dose: 200 mg/day (when taking four doxylamine/pyridoxine tablets per day) or 400 mg/day

IV: 50 mg every 4 to 6 hours

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

* See Dosage and Administration in AHFS Essentials for additional information.

Dosing: Geriatric

Avoid use (Beers Criteria [AGS 2019]).

Dosing: Renal Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling; use with caution.

Dosing: Pediatric

Motion sickness, nausea/vomiting, or vertigo, prophylaxis:

Oral products:

Fixed dose: Administer initial dose 30 to 60 minutes before travel/activity

Children ≥2 to <6 years: Oral: 12.5 to 25 mg every 6 to 8 hours; maximum daily dose: 75 mg/24 hours

Children ≥6 years to <12 years: Oral: 25 to 50 mg every 6 to 8 hours; maximum daily dose: 150 mg/24 hours

Children ≥12 years and Adolescents: Oral: 50 to 100 mg every 4 to 6 hours; maximum daily dose: 400 mg/24 hours

Weight-based dosing: Children 2 to 12 years: Oral: Limited data available: 1 to 1.5 mg/kg/dose every 6 hours; maximum dose: 25 mg/dose. First dose should be administered 60 minutes prior to travel (CDC 2017).

Parenteral products: IM:

Weight-based dosing: Infants, Children, and Adolescents: IM: 1.25 mg/kg/dose 4 times daily; maximum daily dose: 300 mg/day

BSA-based dosing: Infants, Children, and Adolescents: IM: 37.5 mg/m2/dose 4 times daily; maximum daily dose: 300 mg/day

Canadian labeling: Rectal suppository [Canadian product]:

Children 2 to ≤5 years: Rectal: 12.5 mg to 25 mg once; if more doses needed, contact health care provider

Children 6 to 7 years: Rectal: 12.5 to 25 mg every 8 to 12 hours as needed

Children 8 to 11 years: Rectal: 25 to 50 mg every 8 to 12 hours as needed

Children ≥12 years and Adolescents: Rectal: 50 mg every 8 to 12 hours as needed

Postoperative nausea and vomiting (PONV): Limited data available:

Prevention: Infants, Children, and Adolescents: IV: 0.5 mg/kg/dose; maximum dose: 25 mg/dose (Gan 2014)

Treatment:

Weight-directed: Infants, Children, and Adolescents: IV: 0.5 mg/kg/dose; maximum dose: 25 mg/dose; for treatment of PONV, use only if prophylaxis fails and dimenhydrinate is from a different pharmacologic class than prophylactic drug (Gan 2014)

Fixed dose (Gravol prescribing information [Canada] 2016):

Children 6 to 7 years: IM, IV: 15 to 25 mg two or three times daily

Children 8 to 12 years: IM, IV: 25 to 50 mg two or three times daily

Children ≥12 years and Adolescents: IM, IV: 50 mg two or three times daily

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Renal Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; use with caution.

Use: Labeled Indications

US labeling: Motion sickness: Treatment and prevention of nausea, vertigo, and vomiting associated with motion sickness.

Canadian labeling: Nausea, vomiting and/or vertigo: Treatment and prevention of nausea, vomiting and/or vertigo associated with motion sickness, radiation sickness, postoperative recovery, use of other drugs, Ménière disease and other labyrinthine disturbances.

* See Uses in AHFS Essentials for additional information.

Use: Off-Label: Adult

​Nausea and vomiting of pregnancyLevel of Evidence [B, G]

Data from a limited number of clinical trials suggest that dimenhydrinate may be beneficial for the treatment of nausea and vomiting of pregnancy (NVP) Ref.

Based on the American College of Obstetricians and Gynecologists (ACOG) and the Society of Obstetricians and Gynaecologists of Canada practice guidelines, dimenhydrinate given for the treatment of NVP is an effective adjunct to doxylamine/pyridoxine in the management of this condition when doxylamine/pyridoxine alone does not provide symptom improvement Ref. The Royal College of Obstetricians & Gynaecologists in the UK recommends antihistamines (including dimenhydrinate) and phenothiazines as first-line therapy Ref.

Level of Evidence Definitions

​Level of Evidence Scale

Clinical Practice Guidelines

Ménière disease

American Academy of Otolaryngology–Head and Neck Surgery Foundation, "Clinical Practice Guideline: Ménière's Disease," April 2020

Administration: IM

Administer undiluted.

Administration: IV

Dilute and inject over 2 minutes. When using for nausea and vomiting of pregnancy, administer dose (diluted in 50 mL of normal saline) over 20 minutes (Arsenault 2002).

Administration: Oral

To prevent motion sickness, administer 30-60 minutes prior to exposure.

Administration: Rectal

Rectal suppository [Canadian product]: To prevent motion sickness, nausea/vomiting, or vertigo, administer 30 minutes prior to event.

Administration: Pediatric

Oral: Motion sickness: Administer 30 to 60 minutes before travel/activity that causes motion sickness

Parenteral:

IM: Administer undiluted

IV: Although not recommended (per manufacturer), may further dilute and administer IV over 2 minutes; do not inject intra-arterially (Gravol Canadian labeling 2016)

Rectal: Rectal suppository [Canadian product]: Children ≥2 years and Adolescents: Remove outer wrapper and smooth any edges (for comfort); may need to cut suppository to achieve appropriate dose. To prevent motion sickness, nausea/vomiting, or vertigo, administer 30 minutes prior to event.

Dietary Considerations

Tablets may be taken with food or water. Some products may contain phenylalanine.

Storage/Stability

Solution for injection: Store at 20°C to 25°C (68°F to 77°F). Protect from light.

Suppository [Canadian product]: Store at ≤27°C (≤80°F).

Preparation for Administration: Adult

Solution for injection:

IM: No dilution required.

IV: Must dilute each 50 mg in 10 mL NS or D5W (Gravol Canadian labeling 2016).

Preparation for Administration: Pediatric

Parenteral:

IM: No dilution required

IV: Dilute each 50 mg in 10 mL NS

Medication Patient Education with HCAHPS Considerations

What is this drug used for?

• It is used to help motion sickness.

• It is used to treat or prevent upset stomach and throwing up.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Dizziness

• Fatigue

• Dry mouth

• Dry throat

• Anxiety

• Headache

• Lack of appetite

• Trouble sleeping

• Loss of strength and energy

• Nasal dryness

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Difficult urination

• Painful urination

• Fast heartbeat

• Blurred vision

• Agitation

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Medication Safety Issues

​Sound-alike/look-alike issues:

​Geriatric Patients: High-Risk Medication:

Contraindications

Hypersensitivity to dimenhydrinate or any component of the formulation; neonates (injection contains benzyl alcohol)

Canadian labeling: Hypersensitivity to dimenhydrinate, its components (diphenhydramine or 8-chlorotheophylline) or any component of the formulation; concurrent use of or use within 14 days following therapy with a monoamine oxidase inhibitor; narrow angle glaucoma; chronic pulmonary disease; prostatic hypertrophy; patients <2 years of age

Warnings/Precautions

Concerns related to adverse effects:

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Other CNS effects which may be observed, particularly at higher dosages include euphoria, hallucinations, confusion, temporary amnesia and paranoia.

• Dermatologic reactions: Rare cases of serious skin reactions (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme) have been reported; discontinue use if skin rash develops and consult health care provider.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with cardiovascular disease (including arrhythmias, hypertension and ischemic heart disease).

• Hepatic impairment: Use with caution in patients with hepatic impairment.

• Increased intraocular pressure/glaucoma: Use with caution in patients with increased intraocular pressure or angle-closure glaucoma.

• Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction.

• Pyloroduodenal obstruction: Use with caution in patients with pyloroduodenal obstruction (including stenotic peptic ulcer).

• Respiratory disease: Use with caution in patients with a history of asthma or lower respiratory tract symptoms.

• Seizures: Use with caution in patients with seizure disorders.

• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.

Concurrent drug therapy issues:

• Antibiotics: Use caution if used in conjunction with antibiotics that have the potential to cause ototoxicity. Dimenhydrinate may mask symptoms of ototoxicity.

Special populations:

• Elderly: Use with caution in the elderly; may be more sensitive to adverse effects.

• Pediatric: Antihistamines may cause excitation in young children. Not for OTC use in children <2 years of age.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity ("gasping syndrome") in neonates; the "gasping syndrome" consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP 1997; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer's labeling.

• Parenteral formulations: Do not inject intra-arterially.

• Phenylalanine: Some products may contain phenylalanine.

• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer's labeling.

• Propylene glycol: Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated with hyperosmolality, lactic acidosis, seizures and respiratory depression; use caution (AAP 1997; Zar 2007). See manufacturer's labeling.

Other warnings/precautions:

• Abuse/withdrawal: Has abuse potential due to its hallucinogenic and euphoric effects; discontinuation after chronic abuse may lead to withdrawal symptoms (eg, lethargy, agitation, hostility, hallucinations, confusion, aggression, nausea/vomiting).

* See Cautions in AHFS Essentials for additional information.

Geriatric Considerations

Monitor for anticholinergic side effects (confusion, constipation, etc); if possible, limit use to short-term therapy.

Warnings: Additional Pediatric Considerations

Some dosage forms may contain propylene glycol; in neonates large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Shehab 2009).

Pregnancy Risk Factor

B

Pregnancy Considerations

Dimenhydrinate crosses the placenta. The risk of fetal abnormalities was not increased following maternal use of dimenhydrinate during any trimester of pregnancy.

Dimenhydrinate may be used for the adjunctive treatment of nausea and vomiting of pregnancy (ACOG 189 2018; Campbell [SOGC] 2016). Dimenhydrinate may have an oxytocic effect if used during labor.

Breast-Feeding Considerations

Dimenhydrinate is present in breast milk.

Drowsiness and irritability have been reported in breastfed infants exposed to antihistamines; of these effects, irritability was reported in one infant exposed to dimenhydrinate (Ito 1993). The manufacturer recommends that the decision to continue or discontinue breastfeeding during therapy should take into account the risk of exposure to the infant and the benefits of treatment to the mother. In general, if a breastfed infant is exposed to a first generation antihistamine via breast milk, they should be monitored for irritability or drowsiness (Butler 2014).

Antihistamines may decrease maternal serum prolactin concentrations when administered prior to the establishment of lactation (Messinis 1985).

Lexicomp Pregnancy & Lactation, In-Depth

• DimenhyDRINATE

Briggs' Drugs in Pregnancy & Lactation

• Dimenhydrinate

Adverse Reactions

Frequency not defined.

Cardiovascular: Tachycardia

Central nervous system: Dizziness, drowsiness, excitement, headache, insomnia, lassitude, nervousness, restlessness

Dermatologic: Skin rash

Gastrointestinal: Anorexia, epigastric distress, nausea, xerostomia

Genitourinary: Dysuria

Ophthalmic: Blurred vision

Respiratory: Thickening of bronchial secretions

* See Cautions in AHFS Essentials for additional information.

Allergy and Idiosyncratic Reactions

• H1 Antihistamine Allergy

Toxicology

• Histamine H1 Antagonists, First Generation

Metabolism/Transport Effects

None known.

Drug Interactions Open Interactions

Acetylcholinesterase Inhibitors: Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Acetylcholinesterase Inhibitors may diminish the therapeutic effect of Anticholinergic Agents. Risk C: Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Amezinium: Antihistamines may enhance the stimulatory effect of Amezinium. Risk C: Monitor therapy

Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy

Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification

Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider therapy modification

Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider therapy modification

Cannabidiol: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Cannabis: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy

Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider therapy modification

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination

CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider therapy modification

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Risk C: Monitor therapy

Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Risk D: Consider therapy modification

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination

Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination

Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Hyaluronidase: Antihistamines may diminish the therapeutic effect of Hyaluronidase. Risk D: Consider therapy modification

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy

Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider therapy modification

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination

Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Risk C: Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Methotrimeprazine: May enhance the CNS depressant effect of CNS Depressants. CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider therapy modification

Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy

Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Oxybate Salt Products: CNS Depressants may enhance the CNS depressant effect of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interupt oxybate salt treatment during short-term opioid use. Risk D: Consider therapy modification

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Risk D: Consider therapy modification

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy

Pitolisant: Antihistamines may diminish the therapeutic effect of Pitolisant. Risk X: Avoid combination

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Risk X: Avoid combination

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider therapy modification

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Tetrahydrocannabinol and Cannabidiol: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider therapy modification

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Injection:

Generic: 50 mg/mL (1 mL)

Tablet, Oral:

Dramamine: 50 mg

Driminate: 50 mg

Driminate: 50 mg [scored]

GoodSense Motion Sickness: 50 mg [scored]

Motion Sickness: 50 mg [DSC]

Generic: 50 mg [DSC]

Tablet Chewable, Oral:

Dramamine: 50 mg [contains aspartame, fd&c yellow #6 aluminum lake]

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Injection:

Gravol: 50 mg/mL (1 mL, 5 mL)

Generic: 10 mg/mL (5 mL); 50 mg/mL (1 mL, 5 mL)

Anatomic Therapeutic Chemical (ATC) Classification

• R06AA02

Generic Available (US)

May be product dependent

Pricing: US

Chewable (Dramamine Oral)

50 mg (per each): $0.35

Solution (dimenhyDRINATE Injection)

50 mg/mL (per mL): $12.04

Tablets (Dramamine Oral)

50 mg (per each): $0.30

Tablets (Driminate Oral)

50 mg (per each): $0.07

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Mechanism of Action

Competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract; blocks chemoreceptor trigger zone, diminishes vestibular stimulation, and depresses labyrinthine function through its central anticholinergic activity

Pharmacodynamics/Kinetics

Note: Dimenhydrinate is a salt of two drugs: Diphenhydramine (53% to 55.5%) and 8-chlorotheophylline (44% to 47%). Refer to DiphenhydrAMINE (Systemic) monograph.

Onset of action: Antiemetic: IV: immediate; IM: 20 to 30 minutes; Oral: 15 to 30 minutes (Gravol Canadian labeling 2016)

Duration: 4 to 6 hours (Gravol Canadian labeling 2016)

Absorption: Well absorbed

Distribution: 3 to 4 L/kg (Gravol Canadian labeling 2016)

Protein binding: 70% to 85% (Gravol Canadian labeling 2016)

Metabolism: Extensive in the liver to metabolites (diphenyl-methoxy-ethylamine, diphenyl-methoxy-acetic, diphenyl-methoxy-N-methylamine) (Gravol Canadian labeling 2016)

Half-life elimination: 5 to 8 hours (Gravol Canadian labeling 2016)

Excretion: Renal (Gravol Canadian labeling 2016)

Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions

Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Significant xerostomia (normal salivary flow resumes upon discontinuation).

Effects on Bleeding

No information available to require special precautions

Related Information

• Beers Criteria 2019: Potentially Inappropriate Medication Use in Older Adults ≥65 Years of Age

References

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Brand Names: International

Agirax (AR); Agolene (BE); Amosyt (SE); Anautin (DK, EC); Antivomit (FI); Asdim (ET); Aviamarin (RU); Aviomarin (HR, PL); Biodramina (ES, MT); Bonaling-A (KR); Calma (SE); Cinfamar (ES); Daedalon (HU); Dekatravel (BE); Desick (VN); Devom (PK); Dimate (HK); Dimenate (MY); Dimenhidrinato (MX); Dimenidrinato (IT); Dimicaps (MX); Divonal (PE); Dizinil (AE, BH, KW, QA, SA); Doang (TW); Dramamine (AE, AR, AU, BB, BD, BE, BF, BJ, BM, BS, BZ, CI, CO, CR, DO, ET, GB, GH, GM, GN, GT, GY, HN, ID, IE, IN, JM, JP, KE, KR, KW, LR, LU, MA, ML, MR, MU, MW, MX, NE, NG, NI, NL, PA, PR, SC, SD, SL, SN, SR, SV, TN, TT, TW, TZ, UG, VE, ZA, ZM, ZW); Dramavit (BR); Dramavol (CR, DO, GT, HN, NI, PA, SV); Dramenex (EG); Dramin (BR); Dramina (HR, RU, UA); Driminate Supp (MY); Dromyl (NO); Gravamin (PE); Gravinate (LK); Gravol (CR, DO, GT, HK, HN, IN, LB, NI, PA, PE, PH, SV); Hydrinate (MY); Lomarin (IT); Mareamin (CL); Menito (TW); Motivan (TH); Motozina (IT); Nausicalm (FR); Navamin (TH); Novomin (HK, MY); Paranausine (BE, LU); Pasedol (CO, EC); Pharmamin (TH); Siel (RU); Superpep (DE); Symtiver (PL); Travamin (IL); Travel Gum (CN); Travel Well (ES); Travel-Gum (CZ, IT, TR); Travelgum (AT); Trawell (CH); Trimin (TW); Vagomine (BE, LU); Valontan (IT); Vertigmine (AR); Vertirosan (AT); Vomidrine (PT); Vomina (VN); Vomisin (CR, DO, GT, HN, MX, NI, PA, SV); Votmine (MY); Xamamina (IT); Yi Han Ning (CN)

Last Updated 10/16/20