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DimenhyDRINATE


General


Pronunciation

(dye men HYE dri nate)


Brand Names: U.S.

  • Dramamine [OTC]
  • Driminate [OTC]
  • Motion Sickness [OTC]

Indications


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, M ƒ ¨ni ƒ ¨re disease and other labyrinthine disturbances.


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


Dosing and Administration


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)


Dosing: Geriatric

Refer to adult dosing.


Dosing: Pediatric

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

Oral:

Children 2 to 5 years: 12.5 to 25 mg every 6 to 8 hours, maximum: 75 mg daily

Children 6 to 12 years: 25 to 50 mg every 6 to 8 hours, maximum: 150 mg daily

IM: Children: 1.25 mg/kg or 37.5 mg/m2 4 times daily; maximum: 300 mg daily

Canadian labeling: Nausea/vomiting or vertigo:

Motion sickness:

Oral:

Children 2 to 5 years: 15 to 25 mg every 6 to 8 hours as necessary (maximum: 75 mg/day)

Children 6 to 11 years: 25 to 50 mg every 6 to 8 hours as necessary (maximum: 150 mg/day)

Children ≥12 years and Adolescents: 50 mg every 4 to 6 hours as necessary (maximum: 400 mg/day)

Rectal:

Children 2 to 5 years: 12.5 mg to 25 mg one time; consult health care provider if additional dosing is considered necessary

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

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

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

Postoperative nausea/vomiting: IM, IV:

Children 6 to 7 years: 15 to 25 mg IM or IV 2 to 3 times daily

Children 8 to 12 years: 25 to 50 mg IM or IV 2 to 3 times daily

Adolescents: 50 mg IM or IV 2 to 3 times daily


Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturers labeling.


Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturers labeling; use with caution.


Reconstitution

Solution for injection:

IM: No dilution required.

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


Administration

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

Solution for injection:

IM: Administer undiluted

IV: Dilute and inject over 2 minutes

Rectal suppository [Canadian product]: 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

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

Suppository [Canadian product]: Store at 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F).


Dosage Forms/Strengths


Dosage Forms

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

Solution, Injection:

Generic: 50 mg/mL (1 mL)

Tablet, Oral:

Dramamine: 50 mg

Dramamine: 50 mg [scored]

Driminate: 50 mg [scored]

Motion Sickness: 50 mg [scored]

Generic: 50 mg

Tablet Chewable, Oral:

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

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


Drug Interactions

AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Monitor therapy

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

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

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

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

Analgesics (Opioid): Anticholinergic Agents may enhance the adverse/toxic effect of Analgesics (Opioid). Specifically, the risk for constipation and urinary retention may be increased with this combination. Monitor therapy

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

Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). 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. Consider therapy modification

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

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Consider therapy modification

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

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 patches (Butrans brand) at 5 mcg/hr in adults when used with other CNS depressants. Consider therapy modification

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

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

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

Dimethindene: May enhance the CNS depressant effect of CNS Depressants. 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. Monitor therapy

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

Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Consider therapy modification

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

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Consider therapy modification

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

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Avoid combination

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

Hyaluronidase: Antihistamines may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving antihistamines (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required. Consider therapy modification

HYDROcodone: CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Consider starting with a 20% to 30% lower hydrocodone dose when using together with any other CNS depressant. Dose reductions in the other CNS depressant may also be warranted. Consider therapy modification

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

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

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

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

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

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

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Consider therapy modification

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

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

Minocycline: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

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

Mirtazapine: CNS Depressants may enhance the CNS depressant effect of Mirtazapine. Monitor therapy

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

OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Monitor therapy

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

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

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: When oxycodone is combined with another CNS depressant, a dose reduction of one or both agents should be considered. The extended release oxycodone starting dose should be reduced 50% to 67% when initiated in patients already receiving CNS depressants. Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. 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. Consider therapy modification

Piribedil [INT]: CNS Depressants may enhance the CNS depressant effect of Piribedil [INT]. Monitor therapy

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. Avoid combination

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

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

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

RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Monitor therapy

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

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

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

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid using drugs with substantial anticholinergic effects in patients receiving secretin whenever possible. If such agents must be used in combination, monitor closely for a diminished response to secretin. Consider therapy modification

Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Monitor therapy

Sodium Oxybate: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. 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. Consider therapy modification

Tapentadol: May enhance the CNS depressant effect of CNS Depressants. Management: Start tapentadol at a dose of one-third to one-half of the normal dose if being initiated in a patient who is taking another drug with CNS depressant effects. Monitor closely for evidence of excessive CNS depression. Consider therapy modification

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

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

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

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

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

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

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. 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. Consider therapy modification


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


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 (contraindicated in the Canadian labeling).

- Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia (contraindicated in the Canadian labeling) 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. The Canadian labeling contraindicates in patients with chronic pulmonary disease.

- 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.

- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

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. The Canadian labeling contraindicates use in patients <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 manufacturers 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).


Pregnancy Risk Factor

B


Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies. Dimenhydrinate crosses the placenta. The risk of fetal abnormalities was not increased following maternal use of dimenhydrinate during any trimester of pregnancy. Dimenhydrinate is recommended for the treatment of nausea and vomiting of pregnancy. Dimenhydrinate may have an oxytocic effect if used during labor.


Actions


Pharmacology

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


Absorption

Well absorbed


Distribution

3 to 4 L/kg (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)


Excretion

Renal (Gravol Canadian labeling 2016)


Onset of Action

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


Duration of Action

4 to 6 hours (Gravol Canadian labeling 2016)


Half-Life Elimination

5 to 8 hours (Gravol Canadian labeling 2016)


Protein Binding

70% to 85% (Gravol Canadian labeling 2016)


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience dizziness, fatigue, dry mouth, or nasal dryness. Have patient report immediately to prescriber difficult urination, painful urination, tachycardia, blurred vision, or severe anxiety (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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