Dimenhydrinate

469.97

469.18800

208-350-8

JB937PER5C

756740|117855

DTXSID9025087

C28992

CRYSTALS|WHITE POWDER

2933990090

81.8

-0.39

Dimenhydrinate is a crystalline white powder. (NTP, 1992)

1.2586 (rough estimate)

102-107 °C

343.7°C at 760 mmHg

101.5ºC

H2O: Slightly soluble (0.1-1 g/100 mL at 22 ºC);soluble in ethanol

Keep in a cool, dry, dark location in a tightly sealed container or cylinder. Keep away from incompatible materials, ignition sources and untrained individuals. Secure and label area. Protect containers/cylinders from physical damage.

ODORLESS

SATURATED SOLN HAS PH BETWEEN 6.8 & 7.3

Slightly soluble in water. Slightly acidic.

Amides and Imides

NONH for all modes of transport

3

22-61-36/37/38

22-26-36/37/39-53

XH5082000

Xn,Xi

P301 + P312 + P330

H302

Flash point data for this compound are not available but it is probably non-flammable. (NTP, 1992)

|Danger|H302 (99.03%): Harmful if swallowed [Warning Acute toxicity, oral]|P260, P261, P264, P270, P271, P280, P284, P301+P312, P302+P352, P304+P340, P305+P351+P338, P310, P312, P320, P321, P322, P330, P332+P313, P337+P313, P361, P362, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 103 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Fires involving this compound should be controlled using a dry chemical, carbon dioxide, foam or Halon extinguisher. (NTP, 1992)

SMALL SPILLS AND LEAKAGE: Should a spill occur while you are handling this chemical, you should dampen the solid spill material with alcohol, then transfer the dampened material to a suitable container. Use absorbent paper dampened with alcohol to pick up any remaining material. Seal the absorbent paper, and any of your clothes, which may be contaminated, in a vapor-tight plastic bag for eventual disposal. Solvent wash all contaminated surfaces with alcohol followed by washing with a strong soap and water solution. Do not reenter the contaminate area until the Safety Officer (or other responsible person) has verified that the area has been properly cleaned. STORAGE PRECAUTIONS: You should store this material in a refrigerator. (NTP, 1992)

RECOMMENDED RESPIRATOR: Where the neat test chemical is weighed and diluted, wear a NIOSH-approved half face respirator equipped with an organic vapor/acid gas cartridge (specific for organic vapors, HCl, acid gas and SO2) with a dust/mist filter. (NTP, 1992)

Symptoms of overdose include delerium, hallucinations, and excitment. Patients may be violent and confused.

Despite widespread use, dimenhydrinate has not been linked to liver test abnormalities or to clinically apparent liver injury. The reason for its safety may relate to its limited duration of use.

CHLORPHENIRAMINE COULD THEORETICALLY PREVENT BETA-ADRENERGIC BLOCKING EFFECT OF PROPRANOLOL & ENHANCE ITS QUINIDINE-LIKE EFFECT. .../ANTIHISTAMINES/ ARE SIMILAR TO CHLORPHENIRAMINE IN THEIR ACTIONS. OTHER ANTIHISTAMINES INCL...DIMENHYDRINATE...|PATIENTS RECEIVING ANTIHISTAMINES SHOULD BE WARNED AGAINST THE CONCOMITANT USE OF ALCOHOLIC BEVERAGES OR OTHER DRUGS THAT DEPRESS CNS... /ANTIHISTAMINES/

98 to 99%.

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

Dimenhydrinate is a first generation antihistamine that is used for treatment or prevention of motion sickness or symptoms of nausea and dizziness. Dimenhydrinate has not been linked to instances of clinically apparent acute liver injury.

Antihistamines

Antiemetics; Histamine H1 Antagonists|ABILITY TO INHIBIT EFFECTS OF HISTAMINE ON CAPILLARY PERMEABILITY & ON VASCULAR, BRONCHIAL, & MANY OTHER TYPES OF SMOOTH MUSCLE IS PROPERTY THAT CHARACTERIZES H1 ANTAGONISTS & THAT PROVIDES BASIS FOR THEIR PREVALENT CLINICAL USE... /ANTIHISTAMINES/|"FLARE" COMPONENT OF TRIPLE RESPONSE & ITCHING CAUSED BY INTRADERMAL INJECTION OF HISTAMINE... H1-BLOCKING DRUGS SUPPRESS BOTH. ...HAVE LOCAL ANESTHETIC PROPERTIES... H1-BLOCKING DRUGS SELECTIVELY SUPPRESS STIMULANT EFFECT OF HISTAMINE ON ADRENAL CHROMAFFIN CELLS.../&/ AUTONOMIC GANGLION CELLS. /ANTIHISTAMINES/|...EFFICACY...IN COUNTERING HYPERSENSITIVITY REACTIONS WILL VARY, DEPENDING ON DEG TO WHICH SYMPTOMS ARE DUE TO HISTAMINE. ...IN MAN...SOME PHENOMENA, INCL EDEMA FORMATION & ITCH, ARE FAIRLY WELL CONTROLLED; OTHERS, SUCH AS HYPOTENSION ARE LESS SO; & BRONCHOCONSTRICTION...LITTLE IF AT ALL. /ANTIHISTAMINES/|For more Therapeutic Uses (Complete) data for DIMENHYDRINATE (12 total), please visit the HSDB record page.

SEE ANTIHISTAMINICS. CONSIDERABLE MARGIN OF SAFETY SEPARATES THERAPEUTIC DOSE FROM USUAL LETHAL ONE. HOWEVER, BECAUSE CONVULSANT DOSE LIES NEAR LETHAL DOSE, CONVULSIONS INDICATE POOR PROGNOSIS. ADULTS HAVE SURVIVED SINGLE DOSES OF 2.5-5.0 G. CHILDREN...30-60 MG/KG HAS PRODUCED...POISONINGS. /ANTIHISTAMINICS/|IN THERAPEUTIC DOSES, ALL H1 ANTAGONISTS ELICIT SIDE EFFECTS. ...RARELY SERIOUS & OFTEN DISAPPEAR...SOMETIMES...DRUG MUST BE WITHDRAWN. SOME DIFFERENCE...WITH DIFFERENT PREPN IS DISCERNIBLE...MARKED VARIATION IN RESPONSES OF INDIVIDUAL SUBJECTS... /ANTIHISTAMINES/|...ANTICHOLINERGIC ACTIVITY, WHICH ACCOUNTS FOR DRYNESS OF MOUTH...&... DIFFICULTY IN MICTURATION & IMPOTENCE. SOME INTENSIFY RESPONSES TO NOREPINEPHRINE OR STIMULATION OF ADRENERGIC NERVES & INHIBIT RESPONSES TO TYRAMINE... RAPID IV INJECTION OF H1 ANTAGONISTS CAUSES TRANSIENT FALL IN BLOOD PRESSURE... /ANTIHISTAMINES/|H1 ANTAGONISTS CAN BOTH STIMULATE & DEPRESS CNS. ...CENTRAL EXCITATION IS STRIKING FEATURE OF POISONING WITH ANTIHISTAMINES & CAN RESULT IN CONVULSIONS, PARTICULARLY IN INFANTS. CENTRAL DEPRESSION...IS USUAL ACCOMPANIMENT OF THERAPEUTIC DOSES. /ANTIHISTAMINES/|PERSONS TAKING ANTIHISTAMINES SHOULD BE ALERTED TO THEIR SEDATIVE EFFECTS & SHOULD BE CAUTIONED NOT TO DRIVE AN AUTOMOBILE, FLY AN AIRPLANE, OR OPERATE HAZARDOUS MACHINERY... /ANTIHISTAMINES/

Dimenhydrinate is an antiemetics drug combination that contains diphenhydramine and theophylline. It is not effective in the treatment of nausea associated with cancer chemotherapy. Dimenhydrinate directly inhibits the stimulation of certain nerves in the brain and inner ear to suppress nausea, vomiting, dizziness, and vertigo. Diphenhydramine and dimenhydinate both reduce vestibular neuronal excitation due to angular or linear acceleration motions.

Drugs used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)|Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. (See all compounds classified as Histamine H1 Antagonists.)

Well absorbed after oral administration.|DIMENHYDRINATE (ETHANOLAMINES): DURATION OF ACTION (HR) 4-6. /FROM TABLE/|H1 ANTAGONISTS ARE READILY ABSORBED FROM GI TRACT & PARENTERAL SITES OF ADMIN. FOLLOWING ORAL ADMIN, EFFECTS START WITHIN 15 TO 30 MIN, ARE FULLY DEVELOPED WITHIN 1 HR, & LAST ABOUT 3 TO 6 HR, ALTHOUGH SOME...ACT LONGER. /ANTIHISTAMINES/

Hepatic (cytochrome P-450 system).|EXTENSIVE STUDIES OF METABOLIC FATE OF ANTIHISTAMINES HAVE BEEN LIMITED TO A FEW COMPD. ... MAIN SITE OF METABOLIC TRANSFORMATION IS LIVER. /ANTIHISTAMINES/

1 to 4 hours

The mechanism by which some antihistamines exert their antiemetic, anti-motion sickness, and anti-vertigo effects is not precisely known but may be related to their central anticholinergic actions. They diminish vestibular stimulation and depress labyrinthine function. An action on the medullary chemoreceptive trigger zone may also be involved in the antiemetic effect. Dimenhydrinate is a competitive antagonist at the histamine H1 receptor, which is widely distributed in the human brain. Dimenhydrinate's anti-emetic effect is probably due to H1 antagonism in the vestibular system in the brain.|IT IS ESSENTIAL TO NOTE THAT NEITHER H1...BLOCKERS INHIBIT HISTAMINE RELEASE. ...EFFECTS OF HISTAMINE ANTAGONISTS...FACILITATE RELEASE. BENEFICIAL EFFECTS OF HISTAMINE ANTAGONISTS ARE THUS CONFINED TO ANTAGONISM OF RESPONSES TO HISTAMINE THAT IS RELEASED. /ANTIHISTAMINES/|DRUGS USED TO BLOCK HISTAMINE RECEPTORS FALL INTO THAT LARGE GROUP OF PHARMACOLOGICAL ANTAGONISTS THAT APPEAR TO ACT BY OCCUPYING "RECEPTIVE SITES" ON EFFECTOR CELL, TO EXCLUSION OF AGONIST MOLECULES, WITHOUT THEMSELVES INITIATING RESPONSE. TYPICALLY...COMPETITIVE & REVERSIBLE. /ANTIHISTAMINES/|...ANTIHISTAMINES EFFECTIVE IN MOTION SICKNESS ACT BY VIRTUE OF CENTRAL ANTAGONISM OF ACH... ACT BY BLOCKING EXCITATORY LABYRINTHINE IMPULSES @ CHOLINERGIC SYNAPSES IN REGION OF VESTIBULAR NUCLEI. /ANTIHISTAMINES/|...MOTION SICKNESS. ...STIMULATION OF VESTIBULAR APPARATUS...& THAT VESTIBULAR CEREBELLAR MIDBRAIN "INTEGRATIVE VOMITING CENTER" & MEDULLARY CHEMORECEPTIVE TRIGGER ZONE ARE SOMEHOW INVOLVED. /ANTIHISTAMINES/

SYMPTOMS: Symptoms associated with this compound include: drowsiness, lethargy, fatigue hypnosis and coma. Initial sedation may be followed by central nervous system hyperexcitability. Also, the victim may experience dry mouth, anorexia, nausea, vomiting, abdominal distress, constipation, and/or diarrhea. (NTP, 1992)

EYES: First check the victim for contact lenses and remove if present. Flush victim's eyes with water or normal saline solution for 20 to 30 minutes while simultaneously calling a hospital or poison control center. Do not put any ointments, oils, or medication in the victim's eyes without specific instructions from a physician. IMMEDIATELY transport the victim after flushing eyes to a hospital even if no symptoms (such as redness or irritation) develop. SKIN: IMMEDIATELY flood affected skin with water while removing and isolating all contaminated clothing. Gently wash all affected skin areas thoroughly with soap and water. If symptoms such as redness or irritation develop, IMMEDIATELY call a physician and be prepared to transport the victim to a hospital for treatment. INHALATION: IMMEDIATELY leave the contaminated area; take deep breaths of fresh air. If symptoms (such as wheezing, coughing, shortness of breath, or burning in the mouth, throat, or chest) develop, call a physician and be prepared to transport the victim to a hospital. Provide proper respiratory protection to rescuers entering an unknown atmosphere. Whenever possible, Self-Contained Breathing Apparatus (SCBA) should be used; if not available, use a level of protection greater than or equal to that advised under Protective Clothing. INGESTION: DO NOT INDUCE VOMITING. If the victim is conscious and not convulsing, give 1 or 2 glasses of water to dilute the chemical and IMMEDIATELY call a hospital or poison control center. Be prepared to transport the victim to a hospital if advised by a physician. If the victim is convulsing or unconscious, do not give anything by mouth, ensure that the victim's airway is open and lay the victim on his/her side with the head lower than the body. DO NOT INDUCE VOMITING. IMMEDIATELY transport the victim to a hospital. (NTP, 1992)

...POSSESS SIGNIFICANT ANTICHOLINERGIC ACTIVITY & HAVE PRONOUNCED TENDENCY TO INDUCE SEDATION. /ETHANOLAMINES/|SIDE EFFECT WITH HIGHEST INCIDENCE...IS SEDATION. ... OTHER...REFERABLE TO CENTRAL ACTIONS INCL DIZZINESS, TINNITUS, LASSITUDE, INCOORDINATION, FATIGUE, BLURRED VISION, DIPLOPIA, EUPHORIA, NERVOUSNESS, INSOMNIA, & TREMORS. /ANTIHISTAMINES/|...SIDE EFFECTS...DIGESTIVE TRACT...LOSS OF APPETITE, NAUSEA, VOMITING, EPIGASTRIC DISTRESS, & CONSTIPATION OR DIARRHEA. ...DRYNESS OF MOUTH, THROAT & RESP PASSAGES...COUGH; URINARY FREQUENCY & DYSURIA; PALPITATION, HYPOTENSION, HEADACHE; TIGHTNESS OF CHEST; & TINGLING, HEAVINESS & WEAKNESS OF HANDS. /ANTIHISTAMINES/|IN SMALL CHILD, DOMINANT EFFECT IS EXCITATION...INCL HALLUCINATIONS, EXCITEMENT, ATAXIA, INCOORDINATION, ATHETOSIS, & CONVULSIONS. ...OF INTERMITTENT TONIC-CLONIC TYPE... FIXED, DILATED PUPILS WITH FLUSHED FACE & FEVER... TERMINALLY...DEEPENING COMA WITH CARDIORESPIRATORY COLLAPSE & DEATH... /ANTIHISTAMINES/|For more Human Toxicity Excerpts (Complete) data for DIMENHYDRINATE (9 total), please visit the HSDB record page.

Apo Dimenhydrinate

INJECTION: 50 MG/ML; SUPPOSITORIES: 100 MG; SYRUP USP: 15 MG/5 ML; TABLETS USP: 50 MG.|...CONTAINS 53-55.5% OF DIPHENYLHYDRAMINE (C17-H21-N-O), & 44.47% OF 8-CHLOROTHEOPHYLLINE (C7-H7-CL-N4-O2).

1H-Purine-2,6-dione, 8-chloro-3,7-dihydro-1,3-dimethyl-, compd. with 2-(diphenylmethoxy)-N,N-dimethylethanamine (1:1): ACTIVE

THIN LAYER CHROMATOGRAPHY, FRENCH, WN AND WEHRLI, A, J PHARM SCI 54, 1515 (1965).

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients