dimenhydrinate

[DIME(THYL) + (AMI)N(E) + hydrinate (HYDR(AM)IN(E) + -ATE²).]

trade names: CalmX, Dimentabs, Dinate, Drama-mine; drug class: antihistamine, H₁-receptor antagonist; actions: acts on blood vessels and gastrointestinal and respiratory systems by competing with histamine for H₁-receptor sites; decreases allergic response by blocking histamine; uses: motion sickness, nausea, vomiting.

Brand names: DMH®, Dramamine®, Driminate®, Triptone®, Uni-Calm®, Wal-Dram

Chemical formula:

Drug Forms:
• Dimenhydrinate Chewable tablet (below)
• Dimenhydrinate Oral tablet
• Dimenhydrinate Solution for injection
• Dimenhydrinate Oral solution

Español:
• Dimenhidrinato, Tableta masticable
• Dimenhidrinato, Tableta oral
• Dimenhidrinato, Solución para inyección
• Dimenhidrinato, Solución oral

Dimenhydrinate Chewable tablet

What is this medicine?

DIMENHYDRINATE is an antihistamine. It is used to prevent and to treat the nausea, vomiting, or dizziness of motion sickness.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• glaucoma
• heart disease
• liver disease
• lung or breathing disease, like asthma or emphysema
• pain or trouble passing urine
• phenylketonuria
• porphyria
• prostate trouble
• seizures
• an unusual or allergic reaction to dimenhydrinate, diphenhydramine, tartrazine, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Chew this medicine or take whole. Follow the directions on the prescription label. To prevent motion sickness start taking this medicine 1/2 to 1 hour before you travel. Take your medicine at regular intervals. Do not take it more often than directed.

Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as 2 years old for selected conditions, precautions do apply.

Patients over 65 years old may have a stronger reaction and need a smaller dose.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

What may interact with this medicine?

• alcohol
• MAOIs like Carbex, Eldepryl, Marplan, Nardil, and Parnate
• some medicines for allergies, cold, or cough
• medicines that make you sleepy

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular check ups. Tell your doctor or health care professional if your symptoms do not start to get better or if they get worse.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.

This medicine may cause dry eyes and blurred vision. If you wear contact lenses you may feel some discomfort. Lubricating drops may help. See your eye doctor if the problem does not go away or is severe.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• changes in vision
• confused, agitated, or nervous
• fast, irregular heartbeat
• feeling faint or lightheaded, falls
• ringing in the ears
• tremor
• trouble passing urine or change in the amount of urine
• unusual bleeding or bruising
• unusually weak or tired

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
• constipation or diarrhea
• dry mouth
• headache
• loss of appetite
• stomach upset, vomiting

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 25 degrees C (59 and 77 degrees F). Do not freeze. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

An antihistamine used as an antinauseant and antiemetic.

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Dimenhydrinate

Combination of
diphenhydramine	antihistamine
8-chlorotheophylline	stimulant
Identifiers
CAS number	523-87-5
ATC code	?
PubChem	10660
DrugBank	APRD00924
ChemSpider	10210
Therapeutic considerations
Pregnancy cat.	A(AU) B(US)
Legal status	OTC (U.S.)
Routes	Oral, I.V.
Y(what is this?)  (verify)

Dimenhydrinate (in US marketed under brand names Dramamine, Driminate, Gravol, Gravamin, Vomex, and Vertirosan) is an over-the-counter drug used to prevent nausea and motion sickness. It is marketed in Portugal as Viabomand in Brazil under the brand Dramin. It is most commonly used as pills, although it is also available in liquid form and in suppositories. This last is particularly useful in the case of persistent vomiting.

Chemically, dimenhydrinate is a salt of two drugs: diphenhydramine, and 8-chlorotheophylline, a chlorinated derivative of theophylline.

The effects of dimenhydrinate are very similar to those of diphenhydramine. The main differences are a lower potency, and a longer latency. 50 mg dimenhydrinate contains 27.2 mg of diphenhydramine, so it is less potent at equal doses. Also, dimenhydrinate must dissociate into diphenhydramine and its counterion in the body before it is active, so it produces effects more slowly than diphenhydramine.

Theophylline was added in order to counteract drowsiness. Theophylline is very closely related to caffeine and theobromine, mild central nervous system stimulants. It was thought that by combining the antiemetic effects of diphenhydramine with a stimulant, the extreme drowsiness induced by the former could be mitigated somewhat by the latter. The sedation caused by diphenhydramine, however, is substantially stronger than the stimulation caused by chlorotheophyllinate, so the overall effect is still mostly sedating. Diphenhydramine, an ethanolamine-class antihistamine, is found in most OTC sleep aids and allergy preparations, such as Tylenol PM and Benadryl. It is primarily a H₁-antagonist, but also possesses an antimuscarinic effect. It is used in Dramamine to prevent nausea and emesis; however, the development of the chemical meclizine has overtaken its usage (marketed as "Dramamine II") because meclizine doesn't produce as much drowsiness.

Contents 1 Recreational use 2 Veterinary use 3 See also 4 References

Recreational use

This article may contain original research or unverified claims. Please improve the article by adding references. See the talk page for details. (July 2009)

Dimenhydrinate is used as a deliriant at doses of 200 to 1200 mg, although it should be noted that body weight plays a significant part in dosing of any drug. Slang terms for Dramamine used this way include "dime," "dime tabs," "substance D," and "d-house." Frequent users of Dramamine are sometimes called Dramatists, a pun on the name. Tripping on Dramamine is sometimes referred to as Dramatizing or "going a dime a dozen," a reference to the amount of Dramamine tabs generally necessary for a mild trip. The LD-50 (the lethal dose at which 50% of animals tested produced fatal symptoms) for dimenhydrinate is 500 mg/kg in lab rats (LD50 levels can vary greatly between humans and other animals).

Many users report a side effect profile consistent with tropane glycoalkaloidal (e.g. atropine) poisoning as both show antagonism of muscarinic acetylcholine receptors in both the central and autonomic nervous system which inhibits various signal transduction pathways. In the CNS, dimenhydrinate readily crosses the blood-brain barrier, exerting effects within the visual and auditory cortex.

The auditory/visual hallucinations coupled with the ensuing confusion and short-term memory loss often leads to mild or intensive paranoia among the users. Though auditory hallucinations are more common than visual hallucinations, the visuals of a "Dramamine Trip" can seem very real. At higher doses the hallucinations are more frequent, realistic and in some cases, frightening. Taking Dramamine at higher doses is in no way advised or recommended as potential for overdose is a risk. Hallucinations induced by Dramamine abuse are sometimes shared among users; that is, it is common for Dramamine users to hear their own name being called, to see frightening creatures (such as insects or zombies), and to have conversations with non-existing people.

Other CNS effects occur within the limbic system and hippocampus, causing confusion and temporary amnesia due to decreased acetycholine. Toxicology also manifests in the autonomic nervous system, primarily at the neuromuscular junction, resulting in ataxia and extrapyramidal side-effects and the feeling of heaviness in the legs, and at sympathetic post-ganglionic junctions, causing urinary retention, pupil dilation, tachycardia, irregular urination, and dry red skin caused by decreased exocrine gland secretions, and mucous membranes. Considerable overdosage can lead to myocardial infarction (heart attack), serious ventricular dysrhythmias, coma and death. Such a side-effect profile is thought to give ethanolamine-class antihistamines a relatively low abuse liability. The specific antidote for dimenhydrinate poisoning is physostigmine, usually given by IV in a hospital.

Veterinary use

Dimenhydrinate has successfully been used as an antiemetic and sedative in housepets. It is commonly used to reduce the effects of idiopathic vestibular syndrome. The suggested dosage is 50 mg for dogs^[1] and 10 mg for cats; duration of effect is 8 hours.

See also

Cinnarizine

References

1. ^ 2-4 mg per pound

v • d • e Histaminergics Receptor Ligands H1 Agonists: 2-Pyridylethylamine • Betahistine • Histamine • HTMT • UR-AK49 Antagonists: 1st Generation: Alimemazine • Azatadine • Bamipine • Bepotastine • Bromazine • Brompheniramine • Buclizine • Carbinoxamine • Chlorcyclizine • Chloropyramine • Chlorothen • Chlorpheniramine • Chlorphenoxamine • Cinnarizine • Clemastine • Clobenzepam • Clocinizine • Cyclizine • Cyproheptadine • Dacemazine • Deptropine • Dexbrompheniramine • Dexchlorpheniramine • Dimetindene • Diphenhydramine • Diphenylpyraline • Doxylamine • Embramine • Etymemazine • Histapyrrodine • Hydroxyethylpromethazine • Hydroxyzine • Iproheptine • Isopromethazine • Isothipendyl • Meclizine • Mepyramine • Mequitazine • Methafurylene • Methapyrilene • Methdilazine • Moxastine • Niaprazine • Orphenadrine • Oxatomide • Oxomemazine • p-Methyldiphenhydramine • Pheniramine • Phenyltoloxamine • Promethazine • Pyrilamine • Pyrrobutamine • Setastine • Talastine • Thenalidine • Thenyldiamine • Thiazinamium • Thonzylamine • Tolpropamine • Tripelennamine • Triprolidine; 2nd Generation: Acrivastine • Antazoline • Astemizole • Azatadine • Azelastine • Bamipine • Cetirizine • Clemizole • Clobenztropine • Deptropine • Dimebon • Ebastine • Emedastine • Epinastine • Ketotifen • Levocabastine • Loratadine • Mebhydrolin • Mizolastine • Olopatadine • Phenindamine • Pimethixene • Pyrrobutamine • Rupatadine • Terfenadine • Thenalidine • Tritoqualine; 3rd Generation: Desloratadine • Fexofenadine • Levocetirizine; Miscellaneous: Tricyclic Antidepressants (Amitriptyline, Doxepin, Trimipramine, etc) • Tetracyclic Antidepressants (Mianserin, Mirtazapine, etc) • Serotonin Antagonists and Reuptake Inhibitors (Trazodone, Nefazodone) • Typical Antipsychotics (Chlorpromazine, Thioridazine, etc) • Atypical Antipsychotics (Clozapine, Olanzapine, Quetiapine, etc) H2 Agonists: Amthamine • Betazole • Dimaprit • Histamine • HTMT • Impromidine • UR-AK49 Antagonists: Cimetidine • Famotidine • Lafutidine • Metiamide • Niperotidine • Nizatidine • Ranitidine • Roxatidine H3 Agonists: α-Methylhistamine • Cipralisant • Histamine • Imetit • Immepip • Immethridine • Methimepip • Proxyfan Antagonists: A-349,821 • A-423,579 • ABT-239 • Betahistine • Burimamide • Ciproxifan • Clobenpropit • Conessine • GSK-189,254 • Impentamine • Iodophenpropit • JNJ-5,207,852 • MK-0249 • NNC-38-1,049 • SCH-79,687 • Thioperamide • Tiprolisant • VUF-5,681 H4 Agonists: 4-Methylhistamine • Histamine • VUF-8,430 Antagonists: JNJ-7,777,120 • Thioperamide • VUF-6,002 Reuptake Inhibitors Plasmalemmal ..... Vesicular VMAT Inhibitors Ibogaine • Reserpine • Tetrabenazine Enzyme Inhibitors Anabolism HDC Inhibitors α-FMH • Brocresine • Catechin • Cyanidanol-3 • McN-A-1293 • ME • Meciadanol • Naringenin • Thiazol-4-yimethoxyamine • Tritoqualine • Zy-15,029 Catabolism HNMT Inhibitors Amodiaquine • BW-301U • Diphenhydramine • Harmaline • Metoprine • Quinacrine • SKF-91,488 • Tacrine DAO Inhibitors 1,4-Diamino-2-butyne • Aminoguanidine Others Precursors L-Histidine Cofactors Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal → Pyridoxal Phosphate)

v • d • e Deliriants (anticholinergic hallucinogens) Tropanes Atropine • CAR-226,086 • Hyoscyamine • Scopolamine Benzilates Benactyzine • CAR-301,060 • CAR-302,196 • CAR-302,282 • CAR-302,368 • CAR-302,537 • CAR-302,668 • CS-27349 • Ditran • EA-3167 • EA-3443 • EA-3580 • EA-3834 • N-Ethyl-3-piperidyl benzilate • N-Methyl-3-piperidyl benzilate • 3-Quinuclidinyl benzilate • WIN-2299 Antihistamines Benzhydryl compounds (Cyclizine • Dimenhydrinate • Diphenhydramine), Doxylamine • Promethazine Others Benzydamine • Dicyclomine • Biperiden • Trihexyphenidyl

v • d • e Motion sickness Types Airsickness  · Seasickness  · Space adaptation syndrome Medicine Treatment Dramamine  · Bonine  · Marezine  · Promethazine Other treatment Acupressure wristbands

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