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Antivert

Pronunciation

Generic Name: meclizine hydrochloride
Dosage Form: tablet

Antivert®
Tablets/12.5 mg meclizine HCl
 
Antivert®/25
Tablets/25 mg meclizine HCl
 
Antivert®/50
Tablets/50 mg meclizine HCl

Antivert Description

Chemically, Antivert® (meclizine HCl) is 1-(p-chloro-α-phenylbenzyl)-4-(m-methylbenzyl) piperazine dihydrochloride monohydrate.

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Inert ingredients for the tablets are: dibasic calcium phosphate; magnesium stearate; polyethylene glycol; starch; sucrose. The 12.5 mg tablets also contain: Blue 1. The 25 mg tablets also contain: Yellow 6 Lake; Yellow 10 Lake. The 50 mg tablets also contain: Blue 1 Lake; Yellow 10 Lake.

Antivert - Clinical Pharmacology

Antivert is an antihistamine that shows marked protective activity against nebulized histamine and lethal doses of intravenously injected histamine in guinea pigs. It has a marked effect in blocking the vasodepressor response to histamine, but only a slight blocking action against acetylcholine. Its activity is relatively weak in inhibiting the spasmogenic action of histamine on isolated guinea pig ileum.

Pharmacokinetics

The available pharmacokinetic information for meclizine following oral administration has been summarized from published literature.

Absorption

Meclizine is absorbed after oral administration with maximum plasma concentrations reaching at a median Tmax value of 3 hours post-dose (range: 1.5 to 6 hours) for the tablet dosage form.

Distribution

Drug distribution characteristics for meclizine in humans are unknown.

Metabolism

The metabolic fate of meclizine in humans is unknown. In an in vitro metabolic study using human hepatic microsome and recombinant CYP enzyme, CYP2D6 was found to be the dominant enzyme for metabolism of meclizine.

The genetic polymorphism of CYP2D6 that results in extensive-, poor-, intermediate- and ultrarapid metabolizer phenotypes could contribute to large inter-individual variability in meclizine exposure.

Elimination

Meclizine has a plasma elimination half-life of about 5-6 hours in humans.

INDICATIONS

Based on a review of this drug by the National Academy of Sciences - National Research Council and/or other information, FDA has classified the indications as follows:

Effective: Management of nausea and vomiting, and dizziness associated with motion sickness.

Possibly Effective: Management of vertigo associated with diseases affecting the vestibular system.

Final classification of the less than effective indications requires further investigation.

Contraindications

Meclizine HCl is contraindicated in individuals who have shown a previous hypersensitivity to it.

Warnings

Since drowsiness may, on occasion, occur with use of this drug, patients should be warned of this possibility and cautioned against driving a car or operating dangerous machinery.

Patients should avoid alcoholic beverages while taking this drug.

Due to its potential anticholinergic action, this drug should be used with caution in patients with asthma, glaucoma, or enlargement of the prostate gland.

Usage in Children

Clinical studies establishing safety and effectiveness in children have not been done; therefore, usage is not recommended in children under 12 years of age.

Usage in Pregnancy

Pregnancy Category B. Reproduction studies in rats have shown cleft palates at 25–50 times the human dose. Epidemiological studies in pregnant women, however, do not indicate that meclizine increases the risk of abnormalities when administered during pregnancy. Despite the animal findings, it would appear that the possibility of fetal harm is remote. Nevertheless, meclizine, or any other medication, should be used during pregnancy only if clearly necessary.

Precautions

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when meclizine is administered to a nursing woman.

Hepatic Impairment

The effect of hepatic impairment on the pharmacokinetics of meclizine has not been evaluated. As meclizine undergoes metabolism, hepatic impairment may result in increased systemic exposure of the drug. Treatment with meclizine should be administered with caution in patients with hepatic impairment.

Renal Impairment

The effect of renal impairment on the pharmacokinetics of meclizine has not been evaluated. Due to a potential for drug/metabolite accumulation, meclizine should be administered with caution in patients with renal impairment and in the elderly as renal function generally declines with age.

Drug Interactions

There may be increased CNS depression when meclizine is administered concurrently with other CNS depressants, including alcohol, tranquilizers, and sedatives. (see WARNINGS)

Based on in-vitro evaluation, meclizine is metabolized by CYP2D6. Therefore there is a possibility for a drug interaction between meclizine and CYP2D6 inhibitors.

Adverse Reactions

Anaphylactoid reaction, drowsiness, dry mouth, headache, fatigue, vomiting and, on rare occasions, blurred vision have been reported.

Antivert Dosage and Administration

Vertigo

For the control of vertigo associated with diseases affecting the vestibular system, the recommended dose is 25 to 100 mg daily, in divided dosage, depending upon clinical response.

Motion Sickness

The initial dose of 25 to 50 mg of Antivert should be taken one hour prior to embarkation for protection against motion sickness. Thereafter, the dose may be repeated every 24 hours for the duration of the journey.

How is Antivert Supplied

Antivert: 12.5 mg tablets:
  Bottles of 100
    (NDC 0049-2100-66)

Antivert/25: 25 mg tablets:
  Bottles of 100
    (NDC 0049-2110-66)

Antivert/50: 50 mg tablets:
  Bottles of 100
    (NDC 0049-2140-66)

Rx only

LAB-0142-4.0
October 2012

PRINCIPAL DISPLAY PANEL - 12.5 mg Tablet Label

NDC 0049-2100-66

100 Tablets

Antivert®
(meclizine HCl)

12.5 mg

Pfizer
Distributed by
Roerig
Division of Pfizer Inc, NY, NY 10017

PRINCIPAL DISPLAY PANEL - 25 mg Tablet Label

NDC 0049-2110-66

100 Tablets

Antivert®
(meclizine HCl)

25 mg

Pfizer
Distributed by
Roerig
Division of Pfizer Inc, NY, NY 10017

PRINCIPAL DISPLAY PANEL - 50 mg Tablet Label

NDC 0049-2140-66

100 Tablets

Antivert®
(meclizine HCl)

50 mg

Pfizer
Distributed by
Roerig
Division of Pfizer Inc, NY, NY 10017

Antivert 
meclizine hydrochloride tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0049-2100
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
MECLIZINE HYDROCHLORIDE (MECLIZINE) MECLIZINE HYDROCHLORIDE 12.5 mg
Inactive Ingredients
Ingredient Name Strength
CALCIUM PHOSPHATE, DIBASIC, ANHYDROUS  
MAGNESIUM STEARATE  
POLYETHYLENE GLYCOLS  
SUCROSE  
FD&C BLUE NO. 1  
Product Characteristics
Color BLUE, WHITE Score no score
Shape OVAL Size 10mm
Flavor Imprint Code Antivert;210
Contains         
Packaging
# Item Code Package Description
1 NDC:0049-2100-66 100 TABLET in 1 BOTTLE
2 NDC:0049-2100-82 1000 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA010721 04/11/1997
Antivert 
meclizine hydrochloride tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0049-2110
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
MECLIZINE HYDROCHLORIDE (MECLIZINE) MECLIZINE HYDROCHLORIDE 25 mg
Inactive Ingredients
Ingredient Name Strength
CALCIUM PHOSPHATE, DIBASIC, ANHYDROUS  
MAGNESIUM STEARATE  
POLYETHYLENE GLYCOLS  
SUCROSE  
FD&C YELLOW NO. 6  
D&C YELLOW NO. 10  
ALUMINUM OXIDE  
Product Characteristics
Color YELLOW, WHITE Score no score
Shape OVAL Size 13mm
Flavor Imprint Code Antivert;211
Contains         
Packaging
# Item Code Package Description
1 NDC:0049-2110-66 100 TABLET in 1 BOTTLE
2 NDC:0049-2110-82 1000 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA010721 04/11/1997
Antivert 
meclizine hydrochloride tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0049-2140
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
MECLIZINE HYDROCHLORIDE (MECLIZINE) MECLIZINE HYDROCHLORIDE 50 mg
Inactive Ingredients
Ingredient Name Strength
CALCIUM PHOSPHATE, DIBASIC, ANHYDROUS  
MAGNESIUM STEARATE  
POLYETHYLENE GLYCOLS  
SUCROSE  
FD&C BLUE NO. 1  
D&C YELLOW NO. 10  
ALUMINUM OXIDE  
Product Characteristics
Color YELLOW, BLUE Score 2 pieces
Shape OVAL Size 16mm
Flavor Imprint Code Antivert;214
Contains         
Packaging
# Item Code Package Description
1 NDC:0049-2140-66 100 TABLET in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA010721 04/11/1997
Labeler - Roerig (829076996)
Establishment
Name Address ID/FEI Operations
UCB Pharma S.A. 372274485 MANUFACTURE(0049-2140, 0049-2110, 0049-2100)
Establishment
Name Address ID/FEI Operations
Pfizer Pharmaceuticals LLC 829084545 API MANUFACTURE(0049-2140)
Revised: 11/2012
 
Roerig
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