GRAVINATE EFFECTS ON ABILITY TO DRIVE
(Dimenhydrinate B.P I. V/I.M)
Because of the potential for drowsiness, patients taking dimenhydrinate should
COMPOSITION be cautioned against operating automobiles or dangerous machinery
Each ampoule of 1 ml contains: Dimenhydrinate BP 50mg FERTILITY, PREGNANCY AND LACTATION
THERAPEUTIC INDICATIONS Pregnancy
Dimenhydrinate Injection, USP is indicated for the prevention and treatment of Pregnancy Category B.
nausea, vomiting, or vertigo of motion sickness
Reproduction studies have been performed in rats at doses up to 20 times the
DOSAGE AND ADMINISTRATION human dose, and in rabbits at doses up to 25 times the human dose (on a
mg/kg basis), and have revealed no evidence of impaired fertility or harm to the
Dimenhydrinate in the injectable form is indicated when the oral form is fetus due to dimenhydrinate. There are no adequate and well-controlled studies
impractical. in pregnant women. However, clinical studies in pregnant women have not
indicated that dimenhydrinate increases the risk of abnormalities when
Adults
administered in any trimester of pregnancy. It would appear that the possibility
Nausea or vomiting may be expected to be controlled for approximately 4 hours of fetal harm is remote when the drug is used during pregnancy. Nevertheless,
with 50 mg, and prevented by a similar dose every 4 hours. Its administration because the studies in humans cannot rule out the possibility of harm,
may be attended by some degree of drowsiness in some patients, and 100 mg dimenhydrinate should be used during pregnancy only if clearly needed.
every 4 hours may be given in conditions in which drowsiness is not
objectionable or is even desirable. Labor and Delivery
For intramuscular administration, each milliliter (50 mg) of solution is injected as
needed, but for intravenous administration, each milliliter (50 mg) of solution The safety of dimenhydrinate given during labor and delivery has not been
must be diluted in 10 mL of 0.9% Sodium Chloride Injection, USP and injected established. Reports have indicated dimenhydrinate may have an oxytocic
over a period of 2 minutes. effect. Caution is advised when this effect is unwanted or in situations where it
may prove detrimental.
Pediatric
Nursing Mothers
For intramuscular administration, 1.25 mg/kg of body weight or 37.5 mg/m 2 of
body surface area is administered four times daily. The maximum dose should Small amounts of dimenhydrinate are excreted in breast milk. Because of the
not exceed 300 mg daily. potential for adverse reactions in nursing infants from dimenhydrinate, a
Parenteral drug products should be inspected visually for particulate matter and decision should be made whether to discontinue nursing or to discontinue the
discoloration prior to administration, whenever solution and container permit drug, taking into account the importance of the drug to the mother.
CONTRAINDICATIONS ADVERSE DRUG REACTIONS
Neonates and patients with a history of hypersensitivity to dimenhydrinate or its The most frequent adverse reaction to dimenhydrinate is
components (diphenhydramine or 8-chlorotheophylline) should not be treated drowsiness. Dizziness may also occur. Symptoms of dry mouth, nose and
with dimenhydrinate. throat, blurred vision, difficult or painful urination, headache, anorexia,
nervousness, restlessness or insomnia (especially in pediatric patients), skin
SPECIAL WARNINGS AND PRECAUTIONS FOR USE
rash, thickening of bronchial secretions, tachycardia, epigastric distress,
WARNINGS lassitude, excitation, and nausea have been reported.
Reporting of suspected adverse reactions
Caution should be used when dimenhydrinate is given in conjunction with
certain antibiotics that may cause ototoxicity, since dimenhydrinate is capable
Reporting suspected adverse reactions after authorization of the medicinal
of masking ototoxic symptoms, and an irreversible state may be reached.
product is important. It allows continued monitoring of the benefit/risk balance of
the medicinal product. Healthcare professionals are asked to report any
This drug may impair the mental and/or physical abilities required for the
suspected adverse reactions at pv@searlecompany.com
performance of potentially hazardous tasks, such as driving a vehicle or
operating machinery. The concomitant use of alcohol or other central nervous
OVERDOSE
system depressants may have an additive effect. Therefore, patients should be
warned accordingly. Drowsiness is the usual clinical side effect. Convulsions, coma, and respiratory
depression may occur with massive overdosage. No specific antidote is
Dimenhydrinate should be used with caution in patients having conditions which
known. If respiratory depression occurs, mechanically assisted respiration
might be aggravated by anticholinergic therapy (i.e., prostatic hypertrophy,
should be initiated and oxygen should be administered. Convulsions should be
stenosing peptic ulcer, pyloroduodenal obstruction, bladder neck obstruction,
treated with appropriate doses of diazepam. Phenobarbital (5 to 6 mg/kg) may
narrow-angle glaucoma, bronchial asthma, or cardiac arrhythmias).
be given to control convulsions in pediatric patients.
The preparation should not be injected intra-arterially.
The oral LD 50 in mice and rats is 203 mg/kg and 1320 mg/kg,
Pediatric Patients respectively. The intraperitoneal LD 50 in mice is 149 mg/kg.
PHARMACOLOGICAL PROPERTIES
For infants and children especially, antihistamines in overdosage may cause
hallucinations, convulsions, or death.
Pharmacodynamic properties
As in adults, antihistamines may diminish mental alertness in pediatric
Dimenhydrinate is a theoclate salt of the ethanolamine derivative
patients. In the young child, particularly, they may produce excitation.
diphenhydramine. The content ratio varies from 53% - 55.5% for
PRECAUTIONS diphenhydramine, and 44% - 47% for 8- chlorotheophylline. The mechanism by
which dimenhydrinate exerts its antiemetic, anti-motion sickness, and
General antivertigo effects is not precisely known, but may possibly be related to its
central anticholinergic action. Other actions may involve an effect on the
Drowsiness may be experienced by some patients, especially with high medullary chemoreceptor trigger zone or dose-related inhibition of vestibular
dosage. This effect frequently is not undesirable in conditions for which the stimulation (i.e., first acting on the otolith system and in larger doses on the
drug is used. semicircular canals).
Pharmacokinetic properties
Dimenhydrinate is well absorbed after oral administration. Antiemetic effects
occur almost immediately after IV administration, within 20-30 minutes after IM
administration and 15-30 minutes after oral administration.
Serum concentrations (ng/mL) 1 and 2 hours after administration of a 50 mg
dimenhydrinate tablet were: 3.65 and 3.15. While not directly applicable to
dimenhydrinate, it is suggested that when plasma concentration of
diphenhydramine exceeds 70 ng/mL, sleep may occur. Dimenhydrinate, like
diphenhydramine, is widely distributed into body tissues, and crosses the
placenta. Small amounts of dimenhydrinate are distributed into milk. After oral
administration of 4x50 mg dimenhydrinate tablets, a distribution volume of 3-4
L/kg, and protein binding of 70- 85% for dimenhydrinate and 98-99% for
diphenhydramine were reported. The duration of effect and therapeutic plasma
level were respectively 4-6 hours and 0.1µg/mL. The plasma elimination half-life
was 5-8 hours. Dimenhydrinate is metabolized by the liver, and excreted in
urine. There are three known metabolites: diphenyl-methoxy-ethylamine,
diphenyl-methoxy-acetic acid, and diphenylmethoxy-N-methylamine
PRECLINICAL SAFETY DATA
Mutagenicity screening tests performed with dimenhydrinate, diphenhydramine,
and 8-chlorotheophylline produced positive results in the bacterial systems and
negative results in the mammalian systems. There are no human data that
indicate dimenhydrinate is a carcinogen or mutagen or that it impairs fertility.
PRESENTATION
Ampoules Box of 25 ampoules
STORAGE INSTRUCTIONS
To be sold on prescription of a registered medical practitioner only
Protect from moisture, freezing, Excessive heat and sunlight
Keep out of the reach of children
REGISTRATION NUMBER
014408
Mfg. USP Specs.
MANUFACTURED BY.
Searle IV Solutions (PVT) LTD.
Formerly Mac & Rains Pharmaceuticals (Pvt.) Ltd.
1.5 Km Manga Raiwind Road, Manga Mandi,
Distt. Lahore – Pakistan
DATE OF PUBLICATION
June 2021
SPL/SPC-GRA.I/621-000(001)
