Active ingredient: Biperiden - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Antiparkinson Agents
• Antidyskinetics
• Muscarinic Antagonists
• Parasympatholytics

Dosage Forms

• Tablet

Brands / Synonyms

Akineton; Akineton Hydrochloride; Akinophyl; Beperiden; Biperiden Hydrochloride; Biperiden [Usan:Ban:Inn:Jan]; Biperidene Hydrochloride; Biperidene [Inn-French]; Biperideno [Inn-Spanish]; Biperidenum [Inn-Latin]; Biperidine; Biperidine Hydrochloride

Indications

For use as an adjunct in the therapy of all forms of parkinsonism and control of extrapyramidal disorders secondary to neuroleptic drug therapy.

Pharmacology

Biperiden is a weak peripheral anticholinergic agent. It has, therefore, some antisecretory, antispasmodic and mydriatic effects. In addition, biperiden possesses nicotinolytic activity. The parenteral form of biperiden is an effective and reliable agent for the treatment of acute episodes of extrapyramidal disturbances sometimes seen during treatment with neuroleptic agents. Akathisia, akinesia, dyskinetic tremors, rigor, oculogyric crisis, spasmodic torticollis, and profuse sweating are markedly reduced or eliminated. With parenteral biperiden, these drug-induced disturbances are rapidly brought under control.

Mechanism of Action

Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as biperiden is considered to relate to competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance.

Absorption

87% bioavailability

Toxicity

LD₅₀=760 mg/kg (Orally in rats). Signs of overdose include dilated and sluggish pupils, warm, dry skin, facial flushing, decreased secretions of the mouth, pharynx, nose, and bronchi, foul-smelling breath, elevated temperature, tachycardia, cardiac arrhythmias, decreased bowel sounds, urinary retention, delirium, disorientation, anxiety, hallucinations, illusions, confusion, incoherence, agitation, hyperactivity, ataxia, loss of memory, paranoia, combativeness, and seizures.

Biotrnasformation / Drug Metabolism

The metabolism of biperiden is not completely understood, but does involve hydroxylation.

Contraindications

1) Hypersensitivity to biperiden 2) Narrow angle glaucoma 3) Bowel obstruction 4) Megacolon

Drug Interactions

Drug Interactions:    The central anticholinergic syndrome can occur when anticholinergic agents such as AKINETON are administered concomitantly with drugs that have secondary anticholinergic actions, e.g., certain narcotic analgesics such as meperidine, the phenothiazines and other antipsychotics, tricyclic antidepressants, certain antiarrhythmics such as the quinidine salts, and antihistamines. See OVERDOSAGE section for signs and symptoms of the central anticholinergic syndrome, and for treatment.