Mechanism of Action
Trihexyphenidyl inhibits cholinergic transmission in the central nervous system. Its primary target is the $M_1$ muscarinic receptors of the neostriatum. By blocking these receptors, the drug restores the balance between the dopaminergic and cholinergic systems, which is disrupted in Parkinson's disease. An important pharmacological advantage over classic atropine is that trihexyphenidyl acts predominantly within the CNS, making its peripheral effects significantly weaker.
Pharmacological Effects
The drug exhibits moderate antiparkinsonian activity. Clinically, it primarily and selectively suppresses resting tremor and reduces muscle rigidity (stiffness). A key clinical nuance to keep in mind is that trihexyphenidyl has little effect on bradykinesia (slowness of movement).
Indications
Similar to its congener biperiden, trihexyphenidyl is prescribed for the following extrapyramidal disorders:
- Parkinson's disease (primarily in the early stages).
- Parkinsonian syndromes of various etiologies.
- Drug-induced parkinsonism — a specific indication for this drug class. It is used to prevent and manage extrapyramidal symptoms caused by antipsychotic medications (neuroleptics).
Side Effects and Overdose
Adverse reactions are classified according to their site of action (location of blocked receptors):
- Peripheral effects (resulting from peripheral muscarinic receptor blockade): dry mouth (xerostomia), constipation, tachycardia, urinary retention, and cycloplegia (impaired near vision).
- Central effects (resulting from central muscarinic receptor blockade): cognitive impairment, including memory loss and poor concentration. Elderly patients are at particularly high risk due to their heightened sensitivity to central adverse effects.
An overdose causes acute psychosis: psychomotor agitation and hallucinations (so-called anticholinergic delirium).
Contraindications
Given its pronounced anticholinergic profile, the drug is strictly contraindicated in:
- Glaucoma (due to the risk of increased intraocular pressure).
- Prostatic hyperplasia (high risk of acute urinary retention).
- Breastfeeding.
- Individual hypersensitivity.
Prescribing Guidelines and Dosage
The drug is available in 1 mg, 2 mg, and 5 mg tablets. It is administered orally during meals. The standard single dose is 1–2 mg.
- Maximum single dose (MSD): 10 mg.
- Maximum daily dose (MDD): 20 mg.
Prescription example: Rp.: Tab. Cyclodoli 0.002 D.t.d. N. 50 S. Take 1 tablet orally with meals.