Biperiden

Biperiden: Uses, Side Effects and Mechanism of Action

What is Biperiden?

A cholinergic antagonist drug biperiden is used to treat Parkinsonism.

Biperiden Hydrochloride

Biperiden Hydrochloride is the salt from the drug Biperiden. Tablet dosage forms of it include the drug in this chemical form. A central and peripheral nerve system muscarinic antagonist. Arteriosclerotic, idiopathic, and postencephalitic parkinsonism have all been treated with it. Extrapyramidal symptoms caused by phenothiazine derivatives and reserpine have also been treated with it.

What type of drug Biperiden is?

The drug can be classified as

  • Anticholinergic
  • Anti-muscarinic
  • Anti-Parkinsonism

Pharmacokinetics

  • Absorption

After oral treatment, biperiden is promptly and fully absorbed, with peak plasma concentrations occurring 1.5 hours later. For parenteral administration, lactate salt is utilized.

  • Metabolism of the drug

Due to high first-pass metabolism, bioavailability is rather poor (29%). Approximately 95% of the drug is bound to plasma proteins.

  • The volume of Distribution

The fact that there is a large volume of distribution implies that there is good tissue penetration. On the bi-cycloheptene ring and the piperidine portion of the molecule, more than 90% of the chemical is hydroxylated.

  • Half-life

The drug shows a plasma half-life of approximately 18 hours.

  • Excretion

No unchanged drug is excreted through kidneys.

Pharma Dynamics

Biperiden is a mild anticholinergic agent. It possesses antisecretory, antispasmodic, and mydriatic properties. Additionally, it has nicotinolytic properties. In parenteral form it is an efficient and dependable therapy for acute bouts of extrapyramidal abnormalities that might occur during neuroleptic treatment.

The symptoms of akinesia, dyskinesia, dyskinetic tremors, rigidity, oculogyric crises, spasmodic torticollis, and excessive perspiration are significantly decreased or abolished. These drug-induced abnormalities are quickly brought under control with parenteral biperiden.

Biperiden Mechanism of Action

A muscarinic receptor antagonist Biperiden targets the M1 receptor subtype with a high degree of selectivity. It also inhibits the N-methyl-D-aspartate (NMDA) receptor.

What is Biperiden used for?

It is used to treat Parkinson’s disease. It’s also used to treat drug-induced parkinsonism, oculogyric crises, and acute dystonic responses caused by neuroleptic medications.

Indications

Biperiden Hydrochloride (HCL)

  • Parkinson’s disease (dosage = oral) 

Two tablets of biperiden hydrochloride are taken twice a day.

The dosage is progressively raised to 2 mg three times a day, with a daily maintenance dose of 3–12 mg divided into three doses. Use the lower end of the range for the elderly.

Biperiden Lactate

  • Parkinson’s disease (dosage = 2.5-5mg IM, IV)

Biperiden lactate can be taken up to four times per day. Use the lower end of the range for the elderly.

Contraindications

Contraindications of this drug include:

  1. Tardive dyskinesia
  2. Tachycardia caused by ischemic heart disease
  3. Narrow-angle glaucoma
  4. Mechanical stenosis of the gastrointestinal tract or megacolon
  5. Ileus
  6. Hypersensitivity

Adverse effects

  • Dry mouth
  • Gastrointestinal (GI) disturbances
  • Dizziness
  • Blurred vision
  • Urinary retention (less common)
  • Tachycardia
  • Hypersensitivity
  • Nervousness
Biperiden Adverse Effects

Side effects in special population

  • Mental confusion, excitation, and psychiatric problems in vulnerable individuals, such as the elderly.
  • The injection might induce hypotension and produce sleepiness.

Drug Interactions

Following drugs are known to interact with Biperiden

  • Amantadine
  • Antidepressants (Tricyclic)
  • Antihistamines
  • Clozapine
  • Disopyramide
  • Domperidone
  • Ketoconazole
  • Levodopa
  • MAOIs (Monoamine oxidase inhibitors)
  • Metoclopramide
  • Nefopam
  • Nitrates
  • Parasympathomimetic
  • Phenothiazines

Is Biperiden safe in pregnancy?

It is a pregnancy Category C drug. It has not been subjected to animal reproduction experiments. It’s also unclear whether the drug can damage a fetus or alter reproductive ability when given to a pregnant woman. Only if absolutely necessary should the drug Biperiden be administered to a pregnant woman.

Use of Biperiden during lactation

Lactation can be hampered by anticholinergic medications. It is thought to enter into breast milk due to the chemical nature of the active ingredient. This is the reason weaning is advised.

Biperiden during lactation

Biperiden Brand names

Akineton by Abbott

References

https://www.sciencedirect.com/science/article/pii/B9780080552323613224
https://www.sciencedirect.com/science/article/pii/B9780128012383649218
https://go.drugbank.com/drugs/DB00810
https://www.rxlist.com/akineton-drug.htm
https://go.drugbank.com/salts/DBSALT000804

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