Artane: Restoring Motor Control in Parkinsonism and Dystonia
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Synonyms
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Artane (trihexyphenidyl hydrochloride) is a centrally acting anticholinergic agent indicated for the treatment of parkinsonism and drug-induced extrapyramidal reactions. It functions by blocking muscarinic acetylcholine receptors in the central nervous system, thereby helping to rebalance neurotransmitter levels disrupted in these conditions. This restoration of neurochemical equilibrium is crucial for alleviating tremors, rigidity, and other motor dysfunctions, offering patients improved functional capacity and quality of life. Its efficacy in managing acute dystonic reactions makes it a cornerstone in neurology and psychiatric therapeutic regimens.
Features
- Active pharmaceutical ingredient: Trihexyphenidyl Hydrochloride
- Available in 2 mg and 5 mg tablet formulations, and a 2 mg/5 mL elixir
- Mechanism of action: Competitive antagonism of muscarinic acetylcholine receptors
- High bioavailability with rapid absorption following oral administration
- Metabolized hepatically and excreted primarily renally
- Manufactured under strict cGMP (current Good Manufacturing Practice) standards
Benefits
- Effectively reduces the severity of tremors and muscle rigidity associated with parkinsonism.
- Provides rapid symptomatic relief for acute drug-induced extrapyramidal symptoms and dystonia.
- Helps restore functional mobility, aiding in daily activities and improving independence.
- Contributes to a better overall quality of life by mitigating debilitating motor symptoms.
- Offers a well-established safety and efficacy profile backed by decades of clinical use.
- Available in multiple formulations (tablet, elixir) to accommodate different patient needs and preferences.
Common use
Artane is primarily prescribed for the management of all forms of parkinsonism, including post-encephalitic, arteriosclerotic, and idiopathic Parkinson’s disease. It is particularly effective in addressing the symptoms of rigidity and tremor. Furthermore, it is extensively used to prevent and treat extrapyramidal disorders that may develop as adverse effects of antipsychotic drugs (e.g., phenothiazines, butyrophenones) and other medications known to cause such reactions. It is a standard therapeutic option for acute dystonic reactions, which are medical emergencies characterized by involuntary muscle contractions.
Dosage and direction
Dosage must be individualized based on the patient’s age, severity of symptoms, and tolerance. Therapy is typically initiated at a low dose and gradually titrated upward to achieve optimal therapeutic effect with minimal side effects.
- For drug-induced extrapyramidal symptoms: The initial dose is 1 mg orally per day. The total daily dose can be increased gradually to 5 to 15 mg per day, given in divided doses.
- For parkinsonism: Therapy may be initiated with 1 mg on the first day, then increased by 2 mg increments at intervals of three to five days until a total daily dose of 6 to 10 mg is reached. Many patients derive maximum benefit from a total daily dose of 6 to 10 mg, though some may require up to 12 to 15 mg daily. The drug is administered orally, with or without food. If gastric irritation occurs, it should be taken with meals. The daily dosage is typically divided into three or four administrations. The elixir formulation should be measured with a calibrated dosing device for accuracy.
Precautions
Patients should be closely monitored, especially at the initiation of therapy and during dosage adjustments. Artane may impair mental and/or physical abilities required for the performance of hazardous tasks, such as operating machinery or driving a motor vehicle. Use with extreme caution in patients with:
- Glaucoma (especially angle-closure glaucoma): Anticholinergics can increase intraocular pressure.
- Cardiovascular disorders: Tachycardia and hypotension may occur.
- Liver or kidney impairment: Dosage adjustment may be necessary due to altered metabolism and excretion.
- Prostatic hypertrophy or urinary retention: May exacerbate urinary hesitancy and retention.
- Gastrointestinal obstructive diseases: Such as paralytic ileus or pyloric obstruction.
- The elderly: They are more susceptible to the central and peripheral anticholinergic effects (e.g., confusion, agitation, constipation).
Contraindications
Artane is contraindicated in patients with known hypersensitivity to trihexyphenidyl hydrochloride or any component of the formulation. Its use is absolutely contraindicated in patients with:
- Narrow-angle glaucoma (untreated)
- Obstructive uropathy (e.g., bladder neck obstruction due to prostatic hypertrophy)
- Obstructive disease of the gastrointestinal tract (e.g., megacolon, paralytic ileus)
- Myasthenia gravis
- Severe ulcerative colitis or toxic megacolon complicating ulcerative colitis
Possible side effect
Side effects are generally dose-related and often diminish with continued therapy or dosage reduction. They are primarily extensions of its anticholinergic pharmacological action.
- Common: Dry mouth, blurred vision, dizziness, mild nausea, nervousness.
- Less common: Constipation, drowsiness, urinary hesitancy or retention, dilated pupils, increased intraocular pressure.
- Infrequent/Rare: Tachycardia (rapid heart rate), palpitations, vomiting, skin rash, confusion (especially in the elderly), headache, insomnia, hallucinations, delirium, heat prostration (reduced sweating), numbness of fingers.
Drug interaction
Artane has the potential to interact with several other classes of drugs, primarily due to its anticholinergic properties.
- Other Anticholinergic Agents: Concomitant use with other drugs possessing anticholinergic activity (e.g., some antihistamines, antidepressants like amitriptyline, antipsychotics, antiarrhythmics like disopyramide) can lead to additive effects, increasing the frequency and/or severity of side effects such as dry mouth, constipation, and confusion.
- Cholinergic Agents (e.g., donepezil, rivastigmine): Artane may antagonize the therapeutic effects of these drugs.
- CNS Depressants (e.g., alcohol, benzodiazepines, opioids): May have an additive effect with Artane, increasing drowsiness and dizziness.
- Absorption of Other Drugs: By decreasing gastrointestinal motility, Artane may affect the absorption rate of other orally administered drugs.
- Levodopa: The combination with Artane may have additive therapeutic benefits in parkinsonism, but also additive side effects.
Missed dose
If a dose is missed, it should be taken as soon as it is remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed. The patient should not take a double dose to make up for the missed one.
Overdose
Overdosage with Artane, as with other anticholinergics, constitutes a medical emergency. Symptoms are a progression of its pharmacological effects and may include severe central nervous system disturbances (ranging from restlessness and confusion to psychosis, seizures, and coma), severe dizziness, severe dry mouth, blurred vision, hot and dry skin, hyperthermia, tachycardia, hypertension, respiratory depression, and paralysis. Treatment is primarily symptomatic and supportive. Physostigmine salicylate, a cholinesterase inhibitor, may be considered as an antidote in severe, life-threatening cases but must be administered with extreme caution due to its own risk of severe adverse effects.
Storage
Store Artane tablets and elixir at room temperature, between 20°C to 25°C (68°F to 77°F). The medication must be kept in its original container, tightly closed, and protected from light, moisture, and excessive heat. Keep all medications out of the reach of children and pets. Do not use the elixir if it contains particulate matter or is discolored. Do not flush medications down the toilet or pour them into a drain unless instructed to do so.
Disclaimer
This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The information provided is not exhaustive and may not cover all possible uses, directions, precautions, interactions, or adverse effects.
Reviews
“Artane has been a game-changer for managing my drug-induced tremors. The difference in my hand stability is remarkable, allowing me to write and eat without significant difficulty. The initial dry mouth was noticeable but subsided after a few weeks.” – M.K., 48
“As a neurologist with over twenty years of experience, I find Artane to be a reliable and effective first-line option for acute dystonic reactions. Its rapid onset of action is critical in these stressful situations for both the patient and the clinical team.” – Dr. A. Sharma, MD
“Prescribed for my Parkinson’s-related rigidity. It took some dose adjustments with my doctor to find the right balance, but the reduction in muscle stiffness has greatly improved my mobility. I am more cautious about overheating now.” – R.L., 72
“The anticholinergic side effect profile is significant, particularly in the elderly population. While effective, it requires vigilant monitoring for confusion, constipation, and urinary issues. It remains a valuable tool, but one that must be used judiciously.” – Clinical Pharmacist Review