meclizine

Dictionary: mec·li·zine   (mĕk'lĭ-zēn')

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A whitish crystalline powder, C₂₅H₂₇ClN₂, used to treat nausea and motion sickness.

[ME(THYLBENZENE) + C(H)L(ORO–) + alteration of (PIPER)AZINE.]

Key Terms: Antihistamine.

Definition

Meclizine is an antihistamine commonly used to control nausea, vomiting and dizziness. It is known by the over-the-counter name Bonine. In the United States, the prescription brand name is Antivert.

Purpose

Meclizine may be given to help control nausea and vomiting that often occurs with cancer treatment, other medical conditions, or motion sickness. It is also used as part of palliative care for patients with terminal cancer.

More recently, meclizine has been reported to be effective in the treatment of panic disorder.

Description

Meclizine acts as a central nervous system depressant. It is believed its therapeutic actions occur due to the drug's drying effects and its ability to depress conduction of nerve messages in the inner ear. Meclizine begins working about one hour after ingestion. It continues being effective for eight to 24 hours.

Recommended Dosage

The dosage to control nausea and vomiting associated with cancer treatment is 25 mg to 50 mg, every eight to 12 hours. When used to manage dizziness, patients generally take 25 mg to 100 mg daily in divided doses. Patients should not double up on this medication if a dose is missed.

Precautions

Patients with glaucoma, an enlarged prostate, bladder or bowel obstructions, or asthma or other breathing difficulties should discuss with the doctor the risks and benefits associated with this drug before taking it. Those who have experienced an allergic reaction to meclizine should not take it. The FDA recommends that youngsters under age 12 should not take this drug, except under the direction of a physician. Pregnant women and those trying to become pregnant should not take this medication. Animal reproductive studies have shown some deformities at elevated doses. Women who are breastfeeding should discuss this medication with their doctors prior to taking it.

Side Effects

Meclizine may cause drowsiness and fatigue. Drowsiness is the most common adverse reaction. Alcohol and other central nervous system depressants, such as pain medication and tranquilizers, may increase this effect. Patients should refrain from drinking alcoholic beverages, and avoid driving or operating machinery or appliances when taking this drug. Less frequently, the drug also may produce the opposite effect. Excitability, nervousness, restlessness, mood enhancement and difficulty sleeping may develop. Rarely, it may cause a patient to see or hear things that are not present (hallucinations). Despite being used to treat nausea and vomiting, it may produce this effect. It may also cause constipation, diarrhea, an upset stomach or a poor appetite (anorexia). Other side effects include frequent or difficult urination, incomplete emptying of the bladder, low blood pressure, a rapid heart rate or palpitations. It may cause vision changes, a dry nose and throat, ringing in the ears, and a rash or hives. Some of the side effects may be more pronounced in older adults.

Side effects may decrease as the body adjusts to the medication. Ice chips or sugarless hard candy or gum may help relieve the dry mouth. If the feeling of a dry mouth persists for more than two weeks, the doctor should be notified.

Interactions

Central nervous system depressants, including alcohol, may increase drowsiness associated with meclizine. Pain medications, other antihistamines, seizure medications, sleeping pills and muscle relaxants can depress the central nervous system. Taking this drug with some medications used to treat depression may increase the risk of side effects. Patients should inform the doctor of all medications being taken. Patients should not start or stop any drugs without the approval of the doctor. The herbal supplement henbane may increase some of meclizine's side effects, including dry mouth and difficulty urinating.

Resources

Books

Beers, Mark H., MD, and Robert Berkow, MD, editors. "Care of the Dying Patient." Section 21, Chapter 294 In The Merck Manual of Diagnosis and Therapy. Whitehouse Station, NJ: Merck Research Laboratories, 2004.

Beers, Mark H., MD, and Robert Berkow, MD, editors. "Motion Sickness." Section 20, Chapter 282 In The Merck Manual of Diagnosis and Therapy. Whitehouse Station, NJ: Merck Research Laboratories, 2004.

Periodicals

Kuykendall, J. R., and R. S. Rhodes. "Auditory Hallucinations Elicited by Combined Meclizine and Metaxalone Use at Bedtime." Annals of Pharmacotherapy 38 (November 2004): 1968–1969.

Sansone, R. A., and C. D. Sears. "The Successful Use of Meclizine in Panic Disorder." Journal of Clinical Psychiatry 65 (September 2004): 1285–1286.

Organizations

United States Food and Drug Administration (FDA). 5600 Fishers Lane, Rockville, MD 20857-0001. (888) INFO-FDA. .

Other

Food and Drug Administration. "Taming Tummy Turmoil." FDA Publication No. 96-3219. .

—Debra Wood, R.N.; Rebecca J. Frey, Ph.D.

Brand names: Antivert®, Bonikraft™, Dramamine® Less Drowsy, Medi-Meclizine®, Medivert™, Meni-D™, Travel Sickness Chewable, Wal-Dram II

Chemical formula:

Español:
• Tabletas, cápsulas o tabletas masticables de meclizina

Meclizine tablets, capsules or chewable tablets

What are meclizine tablets or capsules?

MECLIZINE (Antivert®, Bonine®) is an antihistamine. It helps to prevent nausea, vomiting, or dizziness associated with motion sickness, and to treat or prevent vertigo (extreme dizziness or a sensation that you or your surroundings are tilting or spinning around). Generic meclizine tablets and capsules are available.

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

They need to know if you have any of these conditions:
• asthma
• glaucoma
• prostate trouble
• stomach problems
• urinary problems
• an unusual or allergic reaction to meclizine, other medicines, foods, dyes, or preservatives
• breast-feeding

How should I take this medicine?

Take meclizine tablets or capsules by mouth. Follow the directions on the prescription label. Swallow the tablets or capsules with a drink of water (chewable tablets can be chewed or swallowed whole). If you are using meclizine to prevent motion sickness, take the dose at least 1 hour before travel. If meclizine upsets your stomach, take it with food or milk. Take your doses at regular intervals. Do not take your medicine more often than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What drug(s) may interact with meclizine?

• alcohol
• barbiturate medicines for inducing sleep or treating seizures (convulsions)
• certain antibiotics given by injection
• digoxin
• medicines for anxiety or sleeping problems, such as alprazolam, diazepam or temazepam
• medicines for hay fever and other allergies
• medicines for mental depression
• medicines for movement abnormalities as in Parkinson's disease, or for gastrointestinal problems
• medicines for pain
• medicines that relax skeletal muscle

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking meclizine?

If you are taking meclizine on a regular schedule, visit your prescriber or health care professional for regular checks on your progress.

You may get dizzy, drowsy or have blurred vision. Do not drive, use machinery, or do anything that needs mental alertness until you know how meclizine 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 can increase possible dizziness; avoid alcoholic drinks.

Meclizine may make your mouth dry. Chewing sugarless gum, sucking hard candy and drinking plenty of water may help. Visit your dentist regularly.

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

What side effects may I notice from taking meclizine?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• fainting spells
• fast or irregular heartbeat (palpitations)

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• blurred vision
• constipation
• difficulty passing urine
• difficulty sleeping
• drowsiness, dizziness
• dry mouth
• headache
• stomach upset

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep container tightly closed. 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.

A centrally acting antiemetic used as the hydrochloride to control motion sickness.

Meclizine
Systematic (IUPAC) name
1-[(4-chlorophenyl)(phenyl)methyl]-4-(3-methylbenzyl)piperazine
Identifiers
CAS number	569-65-3
ATC code	A04AB04 R06AE05
PubChem	4034
DrugBank	APRD00354
ChemSpider	3894
Chemical data
Formula	C25H27ClN2
Mol. mass	390.948 g/mol
SMILES	eMolecules & PubChem
Physical data
Boiling point	230 °C (446 °F)
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	6 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	B(US)
Legal status	OTC (US); OTC (Canada)
Routes	Oral

Meclizine (proposed INN is meclozine) is an antihistamine considered to be an antiemetic.^[1] It is sold under the brand names of Bonine, Bonamine, Antivert, Postafen, and Dramamine (Less Drowsy Formulation), and is most commonly used to inhibit nausea and vomiting. Emesafene is a combination of meclizine (1/3) and pyridoxine (2/3). An alternative to dimenhydrinate (Dramamine, Gravol, Gravamin, and Vertirosan), meclizine is considered to be equally effective, but with reduced side effects. Note that in Canada, Antivert (no longer available) was a combination of meclizine and nicotinic acid.

Meclizine is a first-generation antihistamine of the piperazine class. It differs from the protoype of this class, cyclizine, primarily in having a 12-hour duration of action.^{[citation needed]} Meclizine is less anticholinergic than many other antihistamines and other agents used for their anti-emetic and anti-pruritic effects.^{[citation needed]} Along with the aforementioned efficacy against nausea and itching, meclizine also shares the anxiolytic, analgesic-sparing (potentiating), sedative, and other effects of its chemical relatives cyclizine and hydroxyzine to varying extents.^{[citation needed]} Related to this is the reported ability of meclizine to potentiate the anti-spasmodic, anti-diarrhoeal, and other effects of diphenoxylate, loperamide, and difenoxin. Yet another use for Meclizine is for the potentiation of opioids, especially ones of the open-chain class like Methadone, Dextropropoxyphene and Dipipanone (originally combined with Meclizine's parent drug Cyclizine, which proved to provide a very euphoric rush when injected. The brand name of this combo-drug was/is Diconal) The trend of mixing piperazine antihistamines has caught on in the United States, with some Methadone users potentiating their doses with Meclizine or Hydroxyzine (as Cyclazine isn't available in the U.S.).^{[citation needed]}

Contents 1 Uses 1.1 Motion sickness 1.2 Vertigo 2 Risks of use 2.1 Drowsiness 2.2 Anticholinergics 3 References 4 External links

Uses

Motion sickness

Meclizine is effective in inhibiting the symptoms of motion sickness, such as nausea, vomiting, and dizziness.

Vertigo

Meclizine may be effective in relieving vertigo experienced as a result of inner ear infections or other conditions.

Risks of use

Drowsiness

Drowsiness may result as a side effect of taking meclizine. While the effects are less than those of dimenhydrinate, users are advised not to operate heavy machinery while under the influence. The consumption of alcohol while under the influence of meclizine may result in additional drowsiness.

Anticholinergics

Due to its possible anticholinergic action, meclizine should be used carefully with patients who suffer from asthma, glaucoma, or an enlarged prostate gland.

References

1. ^ Huang W, Zhang J, Wei P, Schrader WT, Moore DD (October 2004). "Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR". Molecular endocrinology (Baltimore, Md.) 18 (10): 2402–8. doi:10.1210/me.2004-0046. PMID 15272053. http://mend.endojournals.org/cgi/pmidlookup?view=long&pmid=15272053. 

External links

• University of Berlin's Institute of Biochemistry
• Numark Pharmacies Information Page on Meclizine
• Rxlist Medical Dictionary

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