Dimenhydrinate is a medication primarily used to treat motion sickness and nausea. It's a combination drug consisting of diphenhydramine and 8-chlorotheophylline. Diphenhydramine is an antihistamine which helps in alleviating symptoms of motion sickness such as nausea, vomiting, and dizziness, while 8-chlorotheophylline is a mild stimulant that helps to counteract drowsiness caused by diphenhydramine.

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

Dimenhydrinate Uses:

• Canadian labeling:
  • Nausea, vomiting, and/or vertigo:
    • Treatment and prevention of motion sickness, radiation sickness, surgical recovery, medication usage, Mènière illness, and other complicated conditions that cause nausea, vomiting, and/or vertigo.
• US labeling:
  • Treatment and prevention of motion sickness-related nausea, dizziness, and vomiting.
• 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 therapy of Motion sickness, nausea/vomiting, or vertigo:

Dimenhydrinate helps with motion sickness, nausea, vomiting, or vertigo.

• For adults taking it by mouth, the typical dose is 50 to 100 milligrams every 4 to 6 hours. The most you should take in a day is 400 milligrams.
• If you're getting dimenhydrinate through an injection into a muscle (IM) or directly into a vein (IV), the usual dose is 50 milligrams every 4 hours. But don't take more than 100 milligrams every 4 hours.

 

Canadian labeling:

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

Motion sickness:

• By mouth: Take 50 to 100 milligrams every 4 hours as needed. Don't take more than 400 milligrams in a day.
• Long-acting formulation: Take 100 milligrams every 8 to 12 hours. The maximum is 300 milligrams in a day.
• Rectal: Take 50 to 100 milligrams every 6 to 8 hours as needed.

Postoperative nausea/vomiting:

• By mouth: Take 50 to 100 milligrams before the procedure, then another 50 to 100 milligrams after. Repeat as needed, but don't exceed 400 milligrams in a day.
• Injection into muscle (IM) or vein (IV): Take 50 milligrams before the procedure, then another 50 milligrams after. Repeat if necessary, but don't exceed 400 milligrams in a day.

Radiation sickness:

• IM or IV: Take 50 to 100 milligrams 30 to 60 minutes before treatment, then 50 milligrams 1.5 and 3 hours after treatment. Repeat if needed, but don't exceed 400 milligrams in a day.
• Rectal: Take 50 to 100 milligrams 30 to 60 minutes before treatment. Repeat as needed, but don't exceed 400 milligrams in a day.

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

• Oral or rectal: Take 50 to 100 milligrams every 4 to 6 hours. The maximum dose is 200 milligrams per day if you're also taking four doxylamine/pyridoxine tablets per day, or 400 milligrams per day if not.
• IV: Receive 50 milligrams every 4 to 6 hours.

Dimenhydrinate (Gravinate) Dose in Children

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

Oral Products:

• Fixed Dose: Take the first dose 30 to 60 minutes before travel or activity.
• For children aged 2 to under 6 years: Take 12.5 to 25 milligrams every 6 to 8 hours. The maximum daily dose is 75 milligrams within 24 hours.
• For children aged 6 to under 12 years: Take 25 to 50 milligrams every 6 to 8 hours. The maximum daily dose is 150 milligrams within 24 hours.
• For children aged 12 years and adolescents: Take 50 to 100 milligrams every 4 to 6 hours. The maximum daily dose is 400 milligrams within 24 hours.
• Weight-Based Dosing (for children 2 to 12 years): Limited data suggests 1 to 1.5 milligrams per kilogram of body weight per dose every 6 hours, with a maximum dose of 25 milligrams per dose. The first dose should be taken 60 minutes before travel.

Parenteral Products (Injection into Muscle - IM):

• Weight-Based Dosing (for infants, children, and adolescents): Administer 1.25 milligrams per kilogram of body weight per dose, four times daily. The maximum daily dose is 300 milligrams.
• BSA-Based Dosing (for infants, children, and adolescents): Administer 37.5 milligrams per square meter of body surface area per dose, four times daily. The maximum daily dose is 300 milligrams.

---

Canadian labeling:

For rectal suppository use of dimenhydrinate in Canada:

• Children aged 2 to 5 years: Use 12.5 milligrams to 25 milligrams once. If more doses are needed, consult a healthcare provider.
• Children aged 6 to 7 years: Use 12.5 milligrams to 25 milligrams every 8 to 12 hours as needed.
• Children aged 8 to 11 years: Use 25 milligrams to 50 milligrams every 8 to 12 hours as needed.
• Children aged 12 years and adolescents: Use 50 milligrams every 8 to 12 hours as needed.

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

Prevention:

• Infants, Children, and Adolescents: Intravenous (IV) administration of 0.5 milligrams per kilogram per dose, with a maximum dose of 25 milligrams per dose.

Treatment:

• Weight-directed: Infants, Children, and Adolescents: Intravenous (IV) administration of 0.5 milligrams per kilogram per dose, with a maximum dose of 25 milligrams per dose. This is used for treatment only if preventive measures fail and dimenhydrinate belongs to a different drug class than the preventive medication.
• Fixed Dose (per Gravol prescribing information [Canada] 2016):
  • Children aged 6 to 7 years: Intramuscular (IM) or IV: 15 to 25 milligrams two or three times daily.
  • Children aged 8 to 12 years: IM or IV: 25 to 50 milligrams two or three times daily.
  • Children aged 12 years and adolescents: IM or IV: 50 milligrams two or three times daily.

Pregnancy Risk Factor B

• Dimenhydrinate, which is commonly used to treat nausea and vomiting, is classified as Pregnancy Risk Factor B, meaning studies have not shown an increased risk of fetal abnormalities when used by pregnant individuals during any trimester.
• It can be safely used as an additional treatment for nausea and vomiting during pregnancy.
• However, if used during labor, dimenhydrinate might have an oxytocic effect, which could influence uterine contractions.

Use during breastfeeding:

• Dimenhydrinate can pass into breast milk, potentially causing drowsiness or irritability in breastfed infants, although such effects are generally rare.
• It's recommended that breastfeeding mothers weigh the benefits of treatment against the risk of exposing their infants to the medication.
• If a first-generation antihistamine like dimenhydrinate is necessary, infants should be monitored for signs of irritability or drowsiness.
• However, if possible, second-generation antihistamines are preferred for breastfeeding mothers, as they pose a lower risk to infants.
• Additionally, antihistamines taken before establishing lactation may reduce maternal prolactin levels.

Dose in Kidney Disease:

• According to the manufacturer's labeling, there are no specific dosage adjustments recommended for individuals with renal impairment.
• This suggests that dimenhydrinate can be used at standard doses in patients with kidney problems without the need for dosage modifications.

Dose in Liver disease:

• According to the manufacturer's labeling, there are no specific dosage adjustments recommended for individuals with hepatic impairment when using dimenhydrinate.
• However, caution should be exercised when using the medication in patients with liver problems.

Side effects of Dimenhydrinate (Gravinate):

• Central nervous system:
  • Dizziness
  • Drowsiness
  • Insomnia
  • Lassitude
  • Excitement
  • Headache
  • Nervousness
  • Restlessness
• Cardiovascular:
  • Tachycardia
• Dermatologic:
  • Skin rash
• Genitourinary:
  • Dysuria
• Gastrointestinal:
  • Epigastric distress
  • Nausea
  • Anorexia
  • Xerostomia
• Ophthalmic:
  • Blurred vision
• Respiratory:
  • Thickening of bronchial secretions

Contraindications to Dimenhydrinate (Gravinate):

According to both US and Canadian labeling, dimenhydrinate should not be used in individuals with hypersensitivity to dimenhydrinate itself or to any component of the formulation. Additionally, it's contraindicated in neonates due to the presence of benzyl alcohol in the injection formulation.

Canadian labeling specifies further contraindications, including concurrent use of or use within 14 days following therapy with a monoamine oxidase inhibitor, narrow-angle glaucoma, chronic pulmonary disease, prostatic hypertrophy, and in patients younger than 2 years of age.

Warnings and precautions

Dermatologic reactions

• Dimenhydrinate can rarely lead to serious skin reactions such as Stevens-Johnson syndrome, toxic epidermal necrolysis, and erythema multiforme.

CNS depression:

• Dimenhydrinate can cause central nervous system (CNS) depression, leading to impairment of physical and mental abilities.
• Patients should be warned about engaging in tasks that require mental alertness, such as operating machinery or driving, while taking this medication.
• Additionally, higher dosages of dimenhydrinate may result in other CNS effects, including euphoria, hallucinations, confusion, temporary amnesia, and paranoia.
• It's essential for patients to be aware of these potential side effects and to exercise caution when using dimenhydrinate, especially at higher doses.

Cardiovascular disease

• Dimenhydrinate should be used with caution in patients with cardiovascular disease, including conditions such as arrhythmias, hypertension, and ischemic heart disease.
• These patients may be more sensitive to the cardiovascular effects of dimenhydrinate, which could potentially worsen their condition.

Hepatic impairment

• Dimenhydrinate should be used cautiously in patients with hepatic impairment, meaning those who have liver problems.
• While specific dosage adjustments for hepatic impairment are not provided in the manufacturer's labeling, caution is advised because the metabolism of dimenhydrinate may be altered in individuals with liver issues.

Glaucoma and increased intraocular pressure:

• Dimenhydrinate should be used cautiously in patients with increased intraocular pressure or angle-closure glaucoma.
• These conditions involve increased pressure within the eye, and dimenhydrinate may further elevate intraocular pressure, potentially worsening symptoms or leading to complications.

Prostatic hyperplasia, urinary obstruction

• Dimenhydrinate should be used cautiously in patients with prostatic hyperplasia (enlargement of the prostate gland) and/or urinary obstruction.
• This caution is necessary because dimenhydrinate can potentially exacerbate urinary symptoms by causing urinary retention or worsening obstruction.

Occlusion of the pyloroduodenum:

• Dimenhydrinate should be used cautiously in patients with pyloroduodenal obstruction, which includes conditions such as stenotic peptic ulcer.
• These conditions involve narrowing or obstruction in the pylorus or duodenum, potentially leading to complications such as gastric outlet obstruction.
• Dimenhydrinate may exacerbate symptoms or delay gastric emptying in patients with pyloroduodenal obstruction.

Respiratory disease

• Dimenhydrinate should be used cautiously in patients with a history of asthma or lower respiratory tract symptoms.
• These individuals may be more susceptible to the respiratory depressant effects of dimenhydrinate, which could potentially exacerbate their respiratory symptoms or lead to complications such as bronchospasm.

Seizures:

• Dimenhydrinate should be used cautiously in patients with seizure disorders.
• This caution is necessary because dimenhydrinate can lower the seizure threshold, potentially increasing the risk of seizures in susceptible individuals.

Thyroid dysfunction:

• Dimenhydrinate should be used cautiously in patients with thyroid dysfunction.
• Thyroid dysfunction can affect various physiological processes in the body, and caution is warranted when using medications that can potentially interact with thyroid function.

Monitoring Parameters

None mentioned.

How to administer Dimenhydrinate (Gravinate)?

Oral:

• Take to prevent motion sickness 30 to 60 minutes before exposure.

Solution for Injection:

• IM: Administer undiluted.
• IV: Dilute the medication and inject it over 2 minutes. For nausea and vomiting of pregnancy, administer the dose diluted in 50 mL of normal saline over 20 minutes.

Rectal Suppository [Canadian Product]:

• Use to prevent motion sickness, nausea/vomiting, or vertigo by administering it 30 minutes before the event.

Mechanism of action of Dimenhydrinate (Gravinate):

• Dimenhydrinate works by competing with histamine for H-receptor sites on effector cells found in the gastrointestinal tract, blood vessels, and respiratory tract.
• By doing so, it blocks the chemoreceptor trigger zone, which helps reduce the sensation of nausea and vomiting.
• Additionally, dimenhydrinate diminishes vestibular stimulation and depresses labyrinthine function through its central anticholinergic activity, helping to alleviate symptoms related to motion sickness and vertigo.
• It's important to note that dimenhydrinate is a combination drug consisting of two active ingredients: diphenhydramine (53% to 55.5%) and 8-chlorotheophylline (44% to 47%).
• For more information on diphenhydramine, please refer to the Diphenhydramine (Systemic) monograph.

Onset of Action:

• Antiemetic:
  • IV: Immediate
  • IM: 20 to 30 minutes
  • Oral: 15 to 30 minutes

Duration:

• 4 to 6 hours

Absorption:

• Well absorbed

Distribution:

• 3 to 4 L/kg

Protein Binding:

• 70% to 85%

Metabolism:

• Extensively metabolized in the liver to metabolites such as diphenyl-methoxy-ethylamine, diphenylmethoxy-acetic, and 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:

Dimenhydrinate Injection 50 mg/ml in Pakistan
Corinate	Asian Agencies
Devom	Siza International (Pvt) Ltd.
Dimen	Munawar Pharma (Pvt) Ltd.
Dirinate	Elite Pharma
Drovid	Zinta Pharmaceuticals Industries
Emetox	Star Laboratories (Pvt) Ltd.
Ephadryl	Epharm Laboratories
Farnate	Farmaceutics International
Gravinate	Searle Pakistan (Pvt.) Ltd.
Grinit	Fumy Enterprises
Lawrvinate	Lawrence Pharma
Menate	Friends Pharma (Pvt) Ltd
Minate	Akson Pharmaceuticals (Pvt) Ltd.
Nilvom	Z-Jans Pharmaceutical (Pvt) Ltd.
Trivinate	Treat Pharmaceuticals

 

Dimenhydrinate Syrup 12.5 mg/4ml in Pakistan
Demax	Delux Chemical Industries
Devinate	Polyfine Chempharma (Pvt) Ltd.
Dimentin	Munawar Pharma (Pvt) Ltd.
Dymin	Stanley Pharmaceuticals (Pvt) Ltd.
Gravinate	Searle Pakistan (Pvt.) Ltd.
Hydrinate	Lisko Pakistan (Pvt) Ltd
Imcomine	Imco Pharmaceuticals Laboratories
Mephen	Mian Brothers Laboratories (Pvt) Ltd.
Vomac Oral	Mac & Rans Pharmaceuticals (Pvt) Ltd

 

Dimenhydrinate Syrup 12.5 mg/5ml in Pakistan
Dimate	Rock Pharmaceuticals
Dramine	Safe Pharmaceutical (Pvt) Ltd.
Sydinate	Sayyed Pharmaceuticals

 

Dimenhydrinate Liquid 12.5 mg/4ml in Pakistan
Gravinate	Searle Pakistan (Pvt.) Ltd.

 

Dimenhydrinate Tablets 50 mg in Pakistan
Dimentin	Munawar Pharma (Pvt) Ltd.
Dramine	Safe Pharmaceutical (Pvt) Ltd.
Dymin	Stanley Pharmaceuticals (Pvt) Ltd.
Emetox	Star Laboratories (Pvt) Ltd.
Gravinate	Searle Pakistan (Pvt.) Ltd.

Dimenhydrinate is a medication primarily used to treat motion sickness and nausea. It's a combination drug consisting of diphenhydramine and 8-chlorotheophylline. Diphenhydramine is an antihistamine which helps in alleviating symptoms of motion sickness such as nausea, vomiting, and dizziness, while 8-chlorotheophylline is a mild stimulant that helps to counteract drowsiness caused by diphenhydramine.

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

Dimenhydrinate Uses:

• Canadian labeling:
  • Nausea, vomiting, and/or vertigo:
    • Treatment and prevention of motion sickness, radiation sickness, surgical recovery, medication usage, Mènière illness, and other complicated conditions that cause nausea, vomiting, and/or vertigo.
• US labeling:
  • Treatment and prevention of motion sickness-related nausea, dizziness, and vomiting.
• 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 therapy of Motion sickness, nausea/vomiting, or vertigo:

Dimenhydrinate helps with motion sickness, nausea, vomiting, or vertigo.

• For adults taking it by mouth, the typical dose is 50 to 100 milligrams every 4 to 6 hours. The most you should take in a day is 400 milligrams.
• If you're getting dimenhydrinate through an injection into a muscle (IM) or directly into a vein (IV), the usual dose is 50 milligrams every 4 hours. But don't take more than 100 milligrams every 4 hours.

 

Canadian labeling:

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

Motion sickness:

• By mouth: Take 50 to 100 milligrams every 4 hours as needed. Don't take more than 400 milligrams in a day.
• Long-acting formulation: Take 100 milligrams every 8 to 12 hours. The maximum is 300 milligrams in a day.
• Rectal: Take 50 to 100 milligrams every 6 to 8 hours as needed.

Postoperative nausea/vomiting:

• By mouth: Take 50 to 100 milligrams before the procedure, then another 50 to 100 milligrams after. Repeat as needed, but don't exceed 400 milligrams in a day.
• Injection into muscle (IM) or vein (IV): Take 50 milligrams before the procedure, then another 50 milligrams after. Repeat if necessary, but don't exceed 400 milligrams in a day.

Radiation sickness:

• IM or IV: Take 50 to 100 milligrams 30 to 60 minutes before treatment, then 50 milligrams 1.5 and 3 hours after treatment. Repeat if needed, but don't exceed 400 milligrams in a day.
• Rectal: Take 50 to 100 milligrams 30 to 60 minutes before treatment. Repeat as needed, but don't exceed 400 milligrams in a day.

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

• Oral or rectal: Take 50 to 100 milligrams every 4 to 6 hours. The maximum dose is 200 milligrams per day if you're also taking four doxylamine/pyridoxine tablets per day, or 400 milligrams per day if not.
• IV: Receive 50 milligrams every 4 to 6 hours.

Dimenhydrinate (Gravinate) Dose in Children

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

Oral Products:

• Fixed Dose: Take the first dose 30 to 60 minutes before travel or activity.
• For children aged 2 to under 6 years: Take 12.5 to 25 milligrams every 6 to 8 hours. The maximum daily dose is 75 milligrams within 24 hours.
• For children aged 6 to under 12 years: Take 25 to 50 milligrams every 6 to 8 hours. The maximum daily dose is 150 milligrams within 24 hours.
• For children aged 12 years and adolescents: Take 50 to 100 milligrams every 4 to 6 hours. The maximum daily dose is 400 milligrams within 24 hours.
• Weight-Based Dosing (for children 2 to 12 years): Limited data suggests 1 to 1.5 milligrams per kilogram of body weight per dose every 6 hours, with a maximum dose of 25 milligrams per dose. The first dose should be taken 60 minutes before travel.

Parenteral Products (Injection into Muscle - IM):

• Weight-Based Dosing (for infants, children, and adolescents): Administer 1.25 milligrams per kilogram of body weight per dose, four times daily. The maximum daily dose is 300 milligrams.
• BSA-Based Dosing (for infants, children, and adolescents): Administer 37.5 milligrams per square meter of body surface area per dose, four times daily. The maximum daily dose is 300 milligrams.

---

Canadian labeling:

For rectal suppository use of dimenhydrinate in Canada:

• Children aged 2 to 5 years: Use 12.5 milligrams to 25 milligrams once. If more doses are needed, consult a healthcare provider.
• Children aged 6 to 7 years: Use 12.5 milligrams to 25 milligrams every 8 to 12 hours as needed.
• Children aged 8 to 11 years: Use 25 milligrams to 50 milligrams every 8 to 12 hours as needed.
• Children aged 12 years and adolescents: Use 50 milligrams every 8 to 12 hours as needed.

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

Prevention:

• Infants, Children, and Adolescents: Intravenous (IV) administration of 0.5 milligrams per kilogram per dose, with a maximum dose of 25 milligrams per dose.

Treatment:

• Weight-directed: Infants, Children, and Adolescents: Intravenous (IV) administration of 0.5 milligrams per kilogram per dose, with a maximum dose of 25 milligrams per dose. This is used for treatment only if preventive measures fail and dimenhydrinate belongs to a different drug class than the preventive medication.
• Fixed Dose (per Gravol prescribing information [Canada] 2016):
  • Children aged 6 to 7 years: Intramuscular (IM) or IV: 15 to 25 milligrams two or three times daily.
  • Children aged 8 to 12 years: IM or IV: 25 to 50 milligrams two or three times daily.
  • Children aged 12 years and adolescents: IM or IV: 50 milligrams two or three times daily.

Pregnancy Risk Factor B

• Dimenhydrinate, which is commonly used to treat nausea and vomiting, is classified as Pregnancy Risk Factor B, meaning studies have not shown an increased risk of fetal abnormalities when used by pregnant individuals during any trimester.
• It can be safely used as an additional treatment for nausea and vomiting during pregnancy.
• However, if used during labor, dimenhydrinate might have an oxytocic effect, which could influence uterine contractions.

Use during breastfeeding:

• Dimenhydrinate can pass into breast milk, potentially causing drowsiness or irritability in breastfed infants, although such effects are generally rare.
• It's recommended that breastfeeding mothers weigh the benefits of treatment against the risk of exposing their infants to the medication.
• If a first-generation antihistamine like dimenhydrinate is necessary, infants should be monitored for signs of irritability or drowsiness.
• However, if possible, second-generation antihistamines are preferred for breastfeeding mothers, as they pose a lower risk to infants.
• Additionally, antihistamines taken before establishing lactation may reduce maternal prolactin levels.

Dose in Kidney Disease:

• According to the manufacturer's labeling, there are no specific dosage adjustments recommended for individuals with renal impairment.
• This suggests that dimenhydrinate can be used at standard doses in patients with kidney problems without the need for dosage modifications.

Dose in Liver disease:

• According to the manufacturer's labeling, there are no specific dosage adjustments recommended for individuals with hepatic impairment when using dimenhydrinate.
• However, caution should be exercised when using the medication in patients with liver problems.

Side effects of Dimenhydrinate (Gravinate):

• Central nervous system:
  • Dizziness
  • Drowsiness
  • Insomnia
  • Lassitude
  • Excitement
  • Headache
  • Nervousness
  • Restlessness
• Cardiovascular:
  • Tachycardia
• Dermatologic:
  • Skin rash
• Genitourinary:
  • Dysuria
• Gastrointestinal:
  • Epigastric distress
  • Nausea
  • Anorexia
  • Xerostomia
• Ophthalmic:
  • Blurred vision
• Respiratory:
  • Thickening of bronchial secretions

Contraindications to Dimenhydrinate (Gravinate):

According to both US and Canadian labeling, dimenhydrinate should not be used in individuals with hypersensitivity to dimenhydrinate itself or to any component of the formulation. Additionally, it's contraindicated in neonates due to the presence of benzyl alcohol in the injection formulation.

Canadian labeling specifies further contraindications, including concurrent use of or use within 14 days following therapy with a monoamine oxidase inhibitor, narrow-angle glaucoma, chronic pulmonary disease, prostatic hypertrophy, and in patients younger than 2 years of age.

Warnings and precautions

Dermatologic reactions

• Dimenhydrinate can rarely lead to serious skin reactions such as Stevens-Johnson syndrome, toxic epidermal necrolysis, and erythema multiforme.

CNS depression:

• Dimenhydrinate can cause central nervous system (CNS) depression, leading to impairment of physical and mental abilities.
• Patients should be warned about engaging in tasks that require mental alertness, such as operating machinery or driving, while taking this medication.
• Additionally, higher dosages of dimenhydrinate may result in other CNS effects, including euphoria, hallucinations, confusion, temporary amnesia, and paranoia.
• It's essential for patients to be aware of these potential side effects and to exercise caution when using dimenhydrinate, especially at higher doses.

Cardiovascular disease

• Dimenhydrinate should be used with caution in patients with cardiovascular disease, including conditions such as arrhythmias, hypertension, and ischemic heart disease.
• These patients may be more sensitive to the cardiovascular effects of dimenhydrinate, which could potentially worsen their condition.

Hepatic impairment

• Dimenhydrinate should be used cautiously in patients with hepatic impairment, meaning those who have liver problems.
• While specific dosage adjustments for hepatic impairment are not provided in the manufacturer's labeling, caution is advised because the metabolism of dimenhydrinate may be altered in individuals with liver issues.

Glaucoma and increased intraocular pressure:

• Dimenhydrinate should be used cautiously in patients with increased intraocular pressure or angle-closure glaucoma.
• These conditions involve increased pressure within the eye, and dimenhydrinate may further elevate intraocular pressure, potentially worsening symptoms or leading to complications.

Prostatic hyperplasia, urinary obstruction

• Dimenhydrinate should be used cautiously in patients with prostatic hyperplasia (enlargement of the prostate gland) and/or urinary obstruction.
• This caution is necessary because dimenhydrinate can potentially exacerbate urinary symptoms by causing urinary retention or worsening obstruction.

Occlusion of the pyloroduodenum:

• Dimenhydrinate should be used cautiously in patients with pyloroduodenal obstruction, which includes conditions such as stenotic peptic ulcer.
• These conditions involve narrowing or obstruction in the pylorus or duodenum, potentially leading to complications such as gastric outlet obstruction.
• Dimenhydrinate may exacerbate symptoms or delay gastric emptying in patients with pyloroduodenal obstruction.

Respiratory disease

• Dimenhydrinate should be used cautiously in patients with a history of asthma or lower respiratory tract symptoms.
• These individuals may be more susceptible to the respiratory depressant effects of dimenhydrinate, which could potentially exacerbate their respiratory symptoms or lead to complications such as bronchospasm.

Seizures:

• Dimenhydrinate should be used cautiously in patients with seizure disorders.
• This caution is necessary because dimenhydrinate can lower the seizure threshold, potentially increasing the risk of seizures in susceptible individuals.

Thyroid dysfunction:

• Dimenhydrinate should be used cautiously in patients with thyroid dysfunction.
• Thyroid dysfunction can affect various physiological processes in the body, and caution is warranted when using medications that can potentially interact with thyroid function.

Monitoring Parameters

None mentioned.

How to administer Dimenhydrinate (Gravinate)?

Oral:

• Take to prevent motion sickness 30 to 60 minutes before exposure.

Solution for Injection:

• IM: Administer undiluted.
• IV: Dilute the medication and inject it over 2 minutes. For nausea and vomiting of pregnancy, administer the dose diluted in 50 mL of normal saline over 20 minutes.

Rectal Suppository [Canadian Product]:

• Use to prevent motion sickness, nausea/vomiting, or vertigo by administering it 30 minutes before the event.

Mechanism of action of Dimenhydrinate (Gravinate):

• Dimenhydrinate works by competing with histamine for H-receptor sites on effector cells found in the gastrointestinal tract, blood vessels, and respiratory tract.
• By doing so, it blocks the chemoreceptor trigger zone, which helps reduce the sensation of nausea and vomiting.
• Additionally, dimenhydrinate diminishes vestibular stimulation and depresses labyrinthine function through its central anticholinergic activity, helping to alleviate symptoms related to motion sickness and vertigo.
• It's important to note that dimenhydrinate is a combination drug consisting of two active ingredients: diphenhydramine (53% to 55.5%) and 8-chlorotheophylline (44% to 47%).
• For more information on diphenhydramine, please refer to the Diphenhydramine (Systemic) monograph.

Onset of Action:

• Antiemetic:
  • IV: Immediate
  • IM: 20 to 30 minutes
  • Oral: 15 to 30 minutes

Duration:

• 4 to 6 hours

Absorption:

• Well absorbed

Distribution:

• 3 to 4 L/kg

Protein Binding:

• 70% to 85%

Metabolism:

• Extensively metabolized in the liver to metabolites such as diphenyl-methoxy-ethylamine, diphenylmethoxy-acetic, and 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:

Dimenhydrinate Injection 50 mg/ml in Pakistan
Corinate	Asian Agencies
Devom	Siza International (Pvt) Ltd.
Dimen	Munawar Pharma (Pvt) Ltd.
Dirinate	Elite Pharma
Drovid	Zinta Pharmaceuticals Industries
Emetox	Star Laboratories (Pvt) Ltd.
Ephadryl	Epharm Laboratories
Farnate	Farmaceutics International
Gravinate	Searle Pakistan (Pvt.) Ltd.
Grinit	Fumy Enterprises
Lawrvinate	Lawrence Pharma
Menate	Friends Pharma (Pvt) Ltd
Minate	Akson Pharmaceuticals (Pvt) Ltd.
Nilvom	Z-Jans Pharmaceutical (Pvt) Ltd.
Trivinate	Treat Pharmaceuticals

 

Dimenhydrinate Syrup 12.5 mg/4ml in Pakistan
Demax	Delux Chemical Industries
Devinate	Polyfine Chempharma (Pvt) Ltd.
Dimentin	Munawar Pharma (Pvt) Ltd.
Dymin	Stanley Pharmaceuticals (Pvt) Ltd.
Gravinate	Searle Pakistan (Pvt.) Ltd.
Hydrinate	Lisko Pakistan (Pvt) Ltd
Imcomine	Imco Pharmaceuticals Laboratories
Mephen	Mian Brothers Laboratories (Pvt) Ltd.
Vomac Oral	Mac & Rans Pharmaceuticals (Pvt) Ltd

 

Dimenhydrinate Syrup 12.5 mg/5ml in Pakistan
Dimate	Rock Pharmaceuticals
Dramine	Safe Pharmaceutical (Pvt) Ltd.
Sydinate	Sayyed Pharmaceuticals

 

Dimenhydrinate Liquid 12.5 mg/4ml in Pakistan
Gravinate	Searle Pakistan (Pvt.) Ltd.

 

Dimenhydrinate Tablets 50 mg in Pakistan
Dimentin	Munawar Pharma (Pvt) Ltd.
Dramine	Safe Pharmaceutical (Pvt) Ltd.
Dymin	Stanley Pharmaceuticals (Pvt) Ltd.
Emetox	Star Laboratories (Pvt) Ltd.
Gravinate	Searle Pakistan (Pvt.) Ltd.