Dimenhydrinate (Gravinate) is a first-generation antihistamine that is used in the treatment of patients with nausea, vomiting, vertigo, and motion sickness.

Dimenhydrinate Uses:

• US labeling:

  • Motion sickness: Treatment and prevention of nausea, vertigo, and vomiting due to motion sickness.

• Canadian labeling:

  • Nausea, vomiting, and/or vertigo:
    • Treatment and prevention of nausea, vomiting, and/or vertigo due to motion sickness, radiation sickness, postoperative recovery, use of other drugs, Mènière disease, and other complex disorders.

• Off Label Use of Dimenhydrinate in Adults:

  • Nausea and vomiting during pregnancy

Read: Meclizine (Bonine)

Dimenhydrinate (Gravinate) Dose in Adults

US labeling:

Dimenhydrinate (Gravinate) Dose in the treatment of 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:

Dimenhydrinate (Gravinate) Dose in the treatment of Nausea/vomiting or vertigo:

• Motion sickness:

  • Oral: 50 to 100 mg every 4 hours as needed (maximum: 400 mg/day);
  • Long-lasting formulation: 100 mg every 8 to 12 hours (maximum: 300 mg/day)
  • Rectal: 50 to 100 mg every 6 to 8 hours as required.

• Postoperative nausea/vomiting:

  • Oral: 50 to 100 mg prior to the procedure then 50 to 100 mg post-procedure; repeat as needed (maximum: 400 mg/day)
  • IM, IV: 50 mg prior to treatment then 50 mg post-procedure; repeat as required (maximum: 400 mg/day)

• Radiation sickness:

  • IM, IV: 50 to 100 mg half an hour to 1 hour before treatment; 50 mg 1.5 and 3 hours after treatment. Repeat dose as needed (maximum: 400 mg/day)
  • Rectal: 50 to 100 mg half an hour to 1 hour before treatment; repeat as required (maximum: 400 mg/day)

Dimenhydrinate (Gravinate) Dose in the treatment of Nausea and vomiting of pregnancy (off-label):

• Oral, rectal:
  • 50 to 100 mg every 4 to 6 hours;
  • The 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

Dimenhydrinate (Gravinate) Dose in Childrens

Dimenhydrinate (Gravinate) Dose for the prophylaxis of Motion sickness, nausea/vomiting, or vertigo:

• Oral products:
  • Fixed-dose: Give the first dose half an hour to an hour before travel/activity
    • Children ≥2 to <6 years:
      • Oral: 12.5 to 25 mg every 6 to 8 hours;
      • The maximum every day dose: 75 mg per day.
    • Children ≥6 years to <12 years:
      • Oral: 25 to 50 mg every 6 to 8 hours;
      • The maximum daily dose: 150 mg per day
    • Children ≥12 years and Adolescents:
      • Oral: 50 to 100 mg every 4 to 6 hours;
      • The maximum daily dose: 400 mg per day

  • Weight-based dosing:

    • Children 2 to 12 years:
      • Oral: Limited data available: 1 to 1.5 mg/kg/dose every 6 hours;
      • The maximum dose: 25 mg/dose.
      • The first dose should be administered an hour before travel.

• ---

  Parenteral products: IM:

  • Weight-based dosing:

    • Infants, Children, and Adolescents:
      • IM: 1.25 mg/kg/dose 4 times a day;
      • The maximum daily dose: 300 mg/day

  • BSA-based dosing:

    • Infants, Children, and Adolescents:
      • IM: 37.5 mg/m /dose 4 times a day;
      • The 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 a further dosage is necessary, contact the health care provider
  • Children 6 to 7 years:
    • Rectal: 12.5 to 25 mg every 8 to 12 hours as required
  • Children 8 to 11 years:
    • Rectal: 25 to 50 mg every 8 to 12 hours as required
  • Children ≥12 years and Adolescents:
    • Rectal: 50 mg every 8 to 12 hours as required

Dimenhydrinate (Gravinate) Dose in Postoperative nausea and vomiting (PONV): 

• Prevention:

  • Infants, Children, and Adolescents:
    • IV: 0.5 mg/kg/dose;
    • The maximum dose: 25 mg/dose.

• Treatment:

  • Weight-directed:

    • Infants, Children, and Adolescents:
      • IV: 0.5 mg/kg/dose;
      • The 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.

  • Fixed-dose:

    • Children 6 to 7 years: IM, IV: 15 to 25 mg twice or thrice a day
    • Children 8 to 12 years: IM, IV: 25 to 50 mg twice or thrice a day
    • Children ≥12 years and Adolescents: IM, IV: 50 mg twice or thrice a day

Pregnancy Risk Factor B

• The placental barrier is crossed by Dimenhydrinate
• There was no increase in the risk of fetal defect after maternal use at any stage of pregnancy of dimenhydrinate.
• For nausea and vomiting during pregnancy, dimenhydrinate can be used as an adjunctive treatment.
• If used during labor, dimenhydrinate can have an oxytocic action.

Use during breastfeeding:

• Breast milk contains dimenhydrinate.
• Breastfed infants who were exposed to antihistamines have shown lethargy or irritability. One infant was exposed to dimenhydrinate.
• Manufacturer recommends that decision-making regarding whether to discontinue or continue breastfeeding during treatment be based on the risks to the infant as well as the benefits to the mother.
• If a baby who is breastfed has been exposed to an antihistamine of the first generation via breast milk, they should be checked for signs such as irritability and lethargy.
• Second-generation antihistamines can be used to treat a breastfeeding mother who needs an antihistamine.
• Pregnancy antihistamines can reduce maternal serum prolactin levels.

Dose in Kidney Disease:

There is no dosage modification given in the manufacturer's labeling.

Dose in Liver disease:

There is no dosage modification given in the manufacturer's labeling; Use cautiously.

Side effects of Dimenhydrinate (Gravinate):

• 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

Contraindications to Dimenhydrinate (Gravinate):

• Sensitivity of dimenhydrinate and any other element in the formulation
• New-borns (injection contains benzyl alcohol)

Canadian labeling:

• Sensitivity of dimenhydrinate, its constituents (8chlorotheophylline or diphenhydramine), or any other element in the formulation.
• Use of monoamine oxidase inhibitors simultaneously or within two weeks;
• Glaucoma with narrow angles
• Chronic lung disease;
• Prostatic hypertrophy
• Patients younger than 2 years old.

Warnings and precautions

• CNS depression:

  • CNS depression can lead to mental or physical impairments. Patients should be aware that driving or operating machinery requires mental attention.
  • Other CNS effects that may be observed, especially at higher doses, include confusion, hallucinations and paranoia.

• Dermatologic reactions

  • Rarely are there any cases of severe skin reactions, such as Stevens-Johnson Syndrome, toxic epidermal Necrolysis, or erythema multife. If you notice a skin rash, stop using the product and consult your health care provider.

• Cardiovascular disease

  • Patients with cardiovascular disease (including hypertension, arrhythmias and ischemic heart diseases) should be cautious.

• Hepatic impairment

  • Patients with severe hepatic disease should be cautious.

• Glaucoma and increased intraocular pressure:

  • Patients with high intraocular pressures or angle-closures glaucoma should be cautious.

• Prostatic hyperplasia, urinary obstruction

  • Patients with prostatic hyperplasia or GU obstruction should use caution.

• Occlusion of the pyloroduodenum:

  • Patients with pyloroduodenal obstruction (including those suffering from stenotic peptic ulcer) should be used cautiously.

• Respiratory disease

  • Patients with asthma or other symptoms of the lower respiratory tract should use this medication cautiously.

• Seizures:

  • Patients with seizure disorders should be vigilant in using this medication.

• Thyroid dysfunction:

  • Patients with thyroid dysfunction should be vigilant about using it.

Monitoring Parameters

None mentioned.

How to administer Dimenhydrinate (Gravinate)?

Oral:

• To treat motion sickness, administer half an hour to an hour before travel.

Solution for injection:

• IM: Administer undiluted
• 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).
• Rectal suppository [Canadian product]: To prevent motion sickness, nausea/vomiting, or vertigo, administer half an hour before travel.

Mechanism of action of Dimenhydrinate (Gravinate):

It competes against histamine to be the H-1 receptor site on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It reduces vestibular stimulation and blocks the chemoreceptor trigger area.

Notification:

• Dimenhydrinate can be a salt of Diphenhydramine (53 to 55%) or 8chlorotheophylline (44 to 47%).

The beginning of action:

• Antiemetic:
  • IV: immediate; IM: 20 to 30 minutes;
  • Oral: 15 to 30 minutes.

Duration:

• 4 to 6 hours.

Absorption:

• Well absorbed when administered orally.

Protein binding:

• 70% to 85%.

Metabolism:

• Extensive in the liver to metabolites (diphenyl-methoxy-ethylamine, diphenylmethoxy-acetic, diphenyl-methoxy-N-methylamine)

Half-life elimination:

• 5 to 8 hours.

Excretion:

• Renal.

International Brand Names of Dimenhydrinate:

• Dramamine
• Driminate
• Motion Sickness
• Gravol
• Agolene
• Amosyt
• Anautin
• Antemin
• Antivomit
• Asdim
• Aviomarin
• Biodramina
• Bonaling-A
• Cinfamar
• Daedalon
• Dekatravel
• Desick
• Devom
• Dimenate
• Dimenhidrinato
• Dimenidrinato
• Dimicaps
• Divonal
• Dizinil
• Doang
• Dramamine
• Dramanyl
• Dramavol
• Dramenex
• Dramin
• Dramina
• Driminate Supp
• Dromyl
• Gravamin
• Gravinate
• Gravol
• Hydrinate
• Lomarin
• Mareamin
• Menito
• Motivan
• Motozina
• Nauseol
• Nausicalm
• Navamin
• Novomin
• Paranausine
• Pasedol
• Pharmamin
• RubieMen
• Travamin
• Travel Well
• Travel-Gum
• Trawell
• Trimin
• Vagomine
• Valontan
• Vertigmine
• Vertirosan
• Vomidrine
• Vomina
• Vomisin
• Votmine
• Xamamina
• Yi Han Ning

Dimenhydrinate Brand Names in Pakistan: