biperiden hydrochloride

biperiden lactate
Akineton

Available forms
Available by prescription only
Injection: 5 mg/ml in 1-ml ampule
Tablets: 2 mg

Indications and dosages
 Extrapyramidal disorders. Adults: 2 mg P.O. daily, b.i.d., or t.i.d., depending on severity. Usual dosage is 2 mg daily. For treatment of extrapyramidal symptoms induced by drugs, give 2 mg I.M. or slow I.V. q 30 minutes, not to exceed 8 mg in a 24-hour period.
 Parkinsonism. Adults: 2 mg P.O. t.i.d. or q.i.d. For prolonged therapy, adjust to maximum of 16 mg daily.
 Treatment of unrelated spastic disorders (such as spinal cord injury) ◇. Adults: 2 mg P.O. b.i.d. to t.i.d.

Pharmacodynamics
Antiparkinsonian action: Drug blocks central cholinergic receptors, helping to balance cholinergic activity in the basal ganglia. It also may prolong the effects of dopamine by blocking dopamine reuptake and storage at central receptor sites.

Pharmacokinetics
Absorption: Well absorbed from the GI tract.
Distribution: Metabolized in the liver.
Metabolism: Unknown.
Excretion: Excreted in urine as unchanged drug and metabolites. After oral therapy, small amounts are probably excreted as unabsorbed drug.

Contraindications and precautions
Contraindicated in patients hypersensitive to drug and in those with angle-closure glaucoma, bowel obstruction, or megacolon. Use cautiously in patients with prostatic hyperplasia, arrhythmias, or seizure disorders.

Interactions
Drug-drug. Amantadine: Increases anticholinergic adverse effects of biperiden, such as confusion and hallucinations. Decrease biperiden dosage before amantadine administration.
Antacids, antidiarrheals: Decrease biperiden absorption. Administer biperiden at least 1 hour before these drugs.
CNS depressants: Increase sedative effects of biperiden. Use together cautiously.
Digoxin: May elevate plasma digoxin levels. Monitor digoxin level.
Haloperidol, phenothiazines: May decrease antipsychotic effectiveness of these drugs, possibly by direct CNS antagonism. Monitor patient for clinical effect.
Phenothiazines: Increase risk of anticholinergic adverse effects. Avoid use together.
Drug-lifestyle. Alcohol use: Increases sedative effects of biperiden. Discourage alcohol use.

Adverse reactions
CNS: disorientation, euphoria, drowsiness, agitation.
CV: transient orthostatic hypotension.
EENT: blurred vision.
GI: dry mouth, constipation.
GU: urine retention.

Effects on lab test results
None reported.

Overdose and treatment
Overdose may cause central stimulation followed by depression and psychotic symptoms, such as disorientation, confusion, hallucinations, delusions, anxiety, agitation, and restlessness. Peripheral effects may include dilated, nonreactive pupils; blurred vision; hot, dry, flushed skin; dry mucous membranes; dysphagia; decreased or absent bowel sounds; urine retention; hyperthermia; headache; tachycardia; hypertension; and increased respiration.
 Treatment is primarily symptomatic and supportive, as needed. Maintain patent airway. If the patient is alert, induce emesis (or use gastric lavage) and follow with a saline solution cathartic and activated charcoal to prevent further absorption of orally administered drug. In severe cases, physostigmine may be administered to block antimuscarinic effects of biperiden. Give fluids, as needed, to treat shock; diazepam to control psychotic symptoms; and pilocarpine (instilled into the eyes) to relieve mydriasis. If urine retention occurs, catheterization may be needed.

Special considerations
• Adverse reactions are dose-related and may resemble atropine toxicity.
• When giving drug parenterally, keep patient supine; parenteral administration may cause transient orthostatic hypotension and disturbed coordination.
• When giving biperiden I.V., inject drug slowly.
• Because biperiden may cause dizziness, patient may need assistance when walking.
• If patient has severe parkinsonism, tremors may increase when drug is given to relieve spasticity.
• Monitor patient for adverse reactions related to anticholinergics.
• Monitor patient for tolerance to drug.
Breast-feeding patients
• Drug may appear in breast milk, possibly resulting in infant toxicity. Drug may also decrease milk production. Avoid use of drug in breast-feeding women.
Pediatric patients
• Drug isn’t recommended for children.
Geriatric patients
• Use cautiously in geriatric patients. Lower doses are indicated.

Patient education
• Tell patient that tolerance to therapeutic and adverse effects can occur with long-term drug use.
• Advise patient that drug may increase sensitivity of the eyes to light.
• Instruct patient to take drug with food to avoid GI upset.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use