Buclizine (Systemic)


VA CLASSIFICATION
Primary: GA609

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).

*Not commercially available in the U.S.

Not commercially available in Canada.



Category:


Antiemetic—

Indications

Accepted

Motion sickness (prophylaxis)—Buclizine is indicated for the prophylaxis of nausea, vomiting, and dizziness associated with motion sickness. {01} {02} {07}


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    505.96 {08}

Mechanism of action/Effect:

Antiemetic—The mechanism by which buclizine exerts its antiemetic and antimotion sickness effects is not precisely known but may be related to its central anticholinergic actions. It diminishes vestibular stimulation and depresses labyrinthine function. An action on the medullary chemoreceptive trigger zone may also be involved in the antiemetic effect. {03}


Other actions/effects:

Buclizine also has antihistaminic, anticholinergic, antivertigo, central nervous system (CNS) depressant, and local anesthetic effects. {03}

Duration of action:

4 to 6 hours. {03}


Precautions to Consider

Pregnancy/Reproduction

Pregnancy—
Problems in humans have not been documented.

In studies in rats, buclizine has been shown to be teratogenic at doses above the human therapeutic range. {01} {02} {07}

Breast-feeding

Buclizine may be distributed into breast milk. However, problems in humans have not been documented.

Because of its anticholinergic actions, buclizine may inhibit lactation. {04}

Pediatrics

No information is available on the relationship of age to the effects of buclizine in pediatric patients. However, it is known that pediatric patients exhibit increased sensitivity to anticholinergics, which are related pharmacologically to buclizine.


Geriatrics


No information is available on the relationship of age to the effects of buclizine in geriatric patients. However, it is known that geriatric patients exhibit increased sensitivity to anticholinergics, {04} which are related pharmacologically to buclizine. Therefore, constipation, dryness of mouth, and urinary retention (especially in males) are more likely to occur in the elderly.

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):


Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.

» Alcohol or
» CNS depression–producing medications, other (See Appendix II )    (concurrent use may potentiate the CNS depressant effects of either these medications or buclizine {03})


Anticholinergics or other medications with anticholinergic activity (See Appendix II ){06}    (concurrent use with buclizine may potentiate anticholinergic effects {03})


Apomorphine{05}    (prior administration of buclizine may decrease the emetic response to apomorphine)



Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With diagnostic test results
Skin tests using allergen extracts    (use of buclizine may inhibit the cutaneous histamine response, thus producing false-negative results; it is recommended that buclizine be discontinued at least 72 hours before testing begins {03})


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problems exist
Bladder neck obstruction or
Prostatic hyperplasia, symptomatic    (anticholinergic effects of buclizine may precipitate urinary retention {03})


Gastroduodenal obstruction    (decrease in motility and tone may occur, aggravating obstruction and gastric retention {05})


Glaucoma, angle-closure, or predisposition to    (increased intraocular pressure may precipitate an attack of angle-closure glaucoma {03})


Sensitivity to buclizine{07}


Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
    
Drowsiness{01}{07}

Incidence less frequent
    
Blurred vision
    
dryness of mouth,{01}{07} nose, and throat
    
headache{01}{07}
    
nervousness, restlessness,{01}{07} or trouble in sleeping
    
upset stomach{03}





Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Meclizine/Buclizine/Cyclizine (Systemic)

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to buclizine

Pregnancy—Animal studies have shown buclizine to be teratogenic at doses above therapeutic range





Breast-feeding—May be distributed into breast milk; may inhibit lactation due to anticholinergic effects





Use in children—Possible increased susceptibility to anticholinergic side effects






Use in the elderly—Possible increased susceptibility to anticholinergic side effects
Other medications, especially other CNS depressants

Proper use of this medication
Not taking more medication than the amount recommended

» Proper dosing
Missed dose (if on a regular dosing regimen): Taking as soon as possible; not taking if almost time for next dose; not doubling doses

» Proper storage

Precautions while using this medication
Possible interference with skin tests using allergens; need to inform physician of use of this medication

» Avoiding use of alcohol or other CNS depressants

» Caution if drowsiness occurs

Possible dryness of mouth; using sugarless gum or candy, ice, or saliva substitute for relief


General Dosing Information
For prophylaxis against motion sickness, this medication should be taken at least 30 minutes before exposure to conditions that may precipitate motion sickness. {01}


Oral Dosage Forms

BUCLIZINE HYDROCHLORIDE CHEWABLE TABLETS

Usual adult and adolescent dose
Motion sickness (prophylaxis)
Oral, 50 mg thirty minutes before travel. Dose may be repeated every four to six hours as needed. {01} {07}


Usual adult prescribing limits
Up to 150 mg daily. {01}

Usual pediatric dose
Dosage has not been established. {01} {07}

Usual geriatric dose
See Usual adult and adolescent dose.

Note: Geriatric patients may be more sensitive to the effects of the usual adult dose.


Strength(s) usually available
U.S.—
Not commercially available. {09}

Canada—
Not commercially available.

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), in a well-closed container, unless otherwise specified by manufacturer. Protect from light. {07}

Auxiliary labeling:
   • May cause drowsiness.
   • Avoid alcoholic beverages.
   • May be chewed or allowed to dissolve in mouth. {07}



Revised: 01/03/1996



References
  1. Bucladin-S package insert (Stuart—US), Rev 6/87, Rec 10/88.
  1. Drug evaluations subscription. Chicago: American Medical Association, Spring 1992: 414.
  1. McEvoy GK, editor. AHFS Drug information 92. Bethesda, MD: American Society of Hospital Pharmacists, 1992: 1745.
  1. Knoben J, Anderson P. Handbook of clinical drug data. 6th ed. Hamilton, IL: Drug Intelligence Publications.
  1. Cyclizine injection package insert (Marezine, Burroughs Wellcome—US), Rev 5/89, Rec 11/89.
  1. McInnes G, Brodie M. Drug interactions that matter. Drugs 1988; 36: 83-110.
  1. Bucladin-S package insert (ZENECA—US), Rev 7/90, Rec 10/8/93.
  1. Fleeger CA, editor. USP dictionary of USAN and international drug names 1996. Rockville, MD: The United States Pharmacopeial Convention, Inc., 1995: 106.
  1. Personal communication, Medical Information Manager, ZENECA Pharmaceutical Group, 8/11/95.
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