Gravinate

An alkaloid from Solanaceae, especially Datura metel L. and Scopola carniolica. Gravinate and its quaternary derivatives act as antimuscarinics like atropine, but may have more central nervous system effects. Among the many uses are as an anesthetic premedication, in urinary incontinence, in motion sickness, as an antispasmodic, and as a mydriatic and cycloplegic.

Gravinate Injection, USP is indicated for the prevention and treatment of nausea, vomiting, or vertigo of motion sickness.

Gravinate is an antihistamine that reduces the effects of natural chemical histamine in the body.

Gravinate is used to treat or prevent nausea, vomiting, and dizziness associated with motion sickness.

Gravinate may also be used for purposes not listed in this medication guide.

Dosage Forms

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]

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

Dosing: Geriatric

Avoid use (Beers Criteria [AGS 2019]).

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/m/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 Gravinate 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

See also:
What is the most important information I should know about Gravinate?

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

Canadian labeling: Hypersensitivity to Gravinate, 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

Use Gravinate chewable tablets as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Gravinate chewable tablets may be taken with or without food.
• Chew thoroughly before swallowing.
• Use Gravinate chewable tablets exactly as directed on the package, unless instructed differently by your doctor. If you are taking Gravinate chewable tablets without a prescription, follow any warnings and precautions on the label.
• Take the first dose at least 30 minutes before activity or travel.
• If you miss a dose of Gravinate chewable tablets and you are taking it regularly, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Gravinate chewable tablets.

Gravinate is an antihistamine used to prevent and treat nausea, vomiting and dizziness caused by motion sickness when medication cannot be given by mouth.

Gravinate injection should not be used in newborns because of an increased risk of side effects.

OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.

Gravinate is also used to treat symptoms of other motion and balance problems such as feelings of dizziness/spinning (vertigo) and inner ear problems (e.g., Meniere's disease). It may also be used to treat nausea and vomiting due to surgery, radiation sickness, side effects of drug treatment, and other causes.

How to use Gravinate injection

This medication is injected into a vein (IV), or it can be injected into a muscle by a health care professional, as directed by your doctor. Your dosage is based on your medical condition and response to therapy.

Tell your doctor if your condition persists or worsens.

See also:
What other drugs will affect Gravinate?

The absorption of oral medications may be decreased during the concurrent use of scopolamine because of decreased gastric motility and delayed gastric emptying.

Gravinate should be used with care in patients taking other drugs that are capable of causing CNS effects such as sedatives, tranquilizers, or alcohol. Special attention should be paid to potential interactions with drugs having anticholinergic properties; e.g., other belladonna alkaloids, antihistamines (including meclizine), tricyclic antidepressants, and muscle relaxants.

Laboratory Test Interactions

Gravinate will interfere with the gastric secretion test.

See also:
What are the possible side effects of Gravinate?

Applies to Gravinate: oral solution, oral tablets, parenteral injection

Side effects include:

Drowsiness, headache, blurred vision, tinnitus, dryness of the mouth and respiratory passages, incoordination, palpitation, dizziness, hypotension.

Paradoxical CNS stimulation in pediatric patients and occasionally in adults.

With IM injection: Pain at the injection site.

Because Gravinate (the active ingredient contained in Gravinate) contains diphenhydramine, the possibility of other diphenhydramine-related adverse effects should also be considered.