Artane: Restore Motor Control in Parkinsonism and Dystonia

Artane
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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 as a selective muscarinic receptor antagonist, effectively counteracting the relative cholinergic excess that contributes to the motor dysfunction characteristic of these conditions. By modulating neurotransmitter balance in the basal ganglia, Artane helps alleviate tremors, rigidity, and sialorrhea, thereby significantly improving functional mobility and quality of life for affected patients. Its well-established efficacy profile and decades of clinical use make it a cornerstone therapy in neurological and psychiatric practice.
Features
- Active Pharmaceutical Ingredient: Trihexyphenidyl Hydrochloride
- Available Formulations: 2 mg and 5 mg scored tablets; 2 mg/5 mL elixir
- Pharmacologic Class: Anticholinergic (Antimuscarinic Agent)
- Mechanism of Action: Competitive antagonism of acetylcholine at central muscarinic receptors (M1 subtype)
- Bioavailability: High oral bioavailability with rapid absorption from the GI tract
- Half-life: Approximately 3-12 hours, supporting a BID or TID dosing regimen
- Metabolism: Hepatic, via hydroxylation
- Excretion: Primarily renal
Benefits
- Reduces Parkinsonian Tremor and Rigidity: Directly targets the core motor symptoms of parkinsonism, leading to smoother, more controlled movements.
- Manages Drug-Induced Dystonia: Effectively counteracts acute dystonic reactions and other extrapyramidal symptoms (EPS) caused by antipsychotic medications, allowing for continued necessary psychiatric treatment.
- Decreases Sialorrhea (Excessive Salivation): Its anticholinergic action reduces salivary secretions, addressing a common and socially limiting symptom.
- Improves Functional Mobility and Gait: By alleviating muscle stiffness and tremor, patients often experience a meaningful improvement in the ability to perform activities of daily living.
- Adjunctive Therapy in Parkinson’s Disease: Can be used alongside levodopa to enhance overall symptomatic control, particularly for tremor-predominant cases.
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 highly effective as symptomatic treatment for the rigidity and tremor associated with these conditions. A major and critical use is in the treatment of medication-induced extrapyramidal reactions, such as dystonia, akathisia, and parkinsonism, which are adverse effects commonly seen with typical antipsychotic drugs (e.g., haloperidol, chlorpromazine) and some antiemetics. It is not used for the prophylaxis of these reactions but for their active treatment once they occur. Its use in treating sialorrhea is also well-documented.
Dosage and direction
Dosage must be individualized and titrated slowly to achieve optimal efficacy while minimizing side effects. Therapy is typically initiated at a low dose and gradually increased.
- For Drug-Induced Extrapyramidal Symptoms: The initial dose is 1 mg on the first day. The dose may be increased by 2 mg increments at intervals of three to five days until satisfactory control is achieved. The usual maintenance dose is 5 to 15 mg per day, though some patients may require higher doses, given in divided doses (e.g., BID or TID).
- For Parkinsonism: Therapy is usually initiated with 1 mg on the first day, and the dose is increased by 2 mg increments at intervals of three to five days until a total of 6 to 10 mg per day is reached. The total daily dose is typically given in divided doses (TID or QID). Many patients derive maximum benefit from 6 to 10 mg daily, though some may require up to 12-15 mg daily.
- Administration: Tablets should be taken orally with or without food. If gastrointestinal upset occurs, administration with meals is advised. The elixir formulation allows for more precise titration and is useful in patients with difficulty swallowing.
- Geriatric Patients: Elderly patients are more susceptible to anticholinergic effects (e.g., confusion, drowsiness). A more conservative dosing strategy is mandatory, often starting at 0.5 to 1 mg at bedtime and increasing very slowly.
Precautions
Artane must be used with caution in patients with the following conditions due to its systemic anticholinergic properties:
- Glaucoma (particularly angle-closure glaucoma): May increase intraocular pressure.
- Prostatic Hypertrophy or Bladder Outlet Obstruction: Can cause urinary retention and hesitancy.
- Tachycardia, Cardiac Arrhythmias, or Congestive Heart Failure: May exacerbate these conditions.
- Liver or Kidney Impairment: Dosage adjustment may be necessary due to altered metabolism and excretion.
- Gastrointestinal Disorders: Ulcerative colitis, intestinal atony, or obstructive disease (e.g., paralytic ileus).
- Myasthenia Gravis: May markedly reduce neuromuscular transmission.
- Psychiatric Conditions: May aggravate psychosis or precipitate toxic psychosis, especially in the elderly.
- Hyperthyroidism: Patients may have an increased responsiveness to the drug.
- Pregnancy and Lactation: Use only if the potential benefit justifies the potential risk to the fetus or infant. Artane is excreted in human milk.
Patients should be advised that Artane may impair mental and/or physical abilities required for the performance of hazardous tasks, such as operating machinery or driving a motor vehicle.
Contraindications
Artane is contraindicated in patients with:
- Known hypersensitivity to trihexyphenidyl hydrochloride or any component of the formulation.
- Narrow-angle glaucoma (untreated).
- Obstructive disease of the gastrointestinal tract (e.g., paralytic ileus, megacolon).
- Obstructive uropathy (e.g., bladder neck obstruction due to prostatic hypertrophy).
- Myasthenia gravis (in most cases).
- Severe ulcerative colitis or toxic megacolon.
Possible side effect
Side effects are primarily extensions of its pharmacological anticholinergic action and are often dose-related. Common side effects include:
- Central Nervous System: Drowsiness, dizziness, nervousness, insomnia, confusion, euphoria, agitation, hallucinations (especially in the elderly), headache.
- Ocular: Blurred vision, mydriasis (dilated pupils), increased intraocular pressure.
- Gastrointestinal: Dry mouth, nausea, vomiting, constipation.
- Genitourinary: Urinary hesitancy or retention.
- Cardiovascular: Tachycardia (fast heart rate), palpitations.
- Dermatological: Decreased sweating, which can lead to heat prostration and fever in hot weather, skin rash.
- Other: Weakness, numbness of fingers.
Drug interaction
Artane has the potential to interact with several other drug classes:
- Other Anticholinergic Agents: Concomitant use with other drugs possessing anticholinergic properties (e.g., some antihistamines, tricyclic antidepressants, phenothiazines, disopyramide) will result in additive effects and increased side effects.
- Cholinergic Agents (e.g., Donepezil, Rivastigmine): Artane will antagonize the effects of these drugs.
- Levodopa: The effects of Artane and levodopa in Parkinson’s disease are additive. Concomitant use may permit a reduction in the dosage of levodopa.
- CNS Depressants (e.g., Alcohol, Benzodiazepines, Opioids): May have an additive sedative effect.
- Absorption of Other Drugs: May delay gastric emptying, thereby affecting the absorption of other orally administered drugs.
- Antacids/Antidiarrheals: May reduce the absorption of Artane.
- Amantadine: May enhance the anticholinergic side effects.
- Haloperidol: Serum concentrations of haloperidol may be reduced, potentially decreasing its efficacy. The anticholinergic effects are additive.
- Ketoconazole/MAO Inhibitors: May enhance the anticholinergic effects of Artane.
Missed dose
If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. The patient should not double the dose to make up for the missed one. Maintaining a consistent dosing schedule is important for stable symptom control.
Overdose
Overdose with Artane is characterized by intensification of its known pharmacological effects. Symptoms may include severe central nervous system disturbances (agitation, confusion, hallucinations, seizures), severe dizziness, severe dry mouth, blurred vision, hot and dry skin, hyperthermia, tachycardia, respiratory depression, and cardiovascular collapse. Treatment is primarily symptomatic and supportive. Gastric lavage may be considered if ingestion was recent. Physostigmine, a cholinesterase inhibitor, may be used as an antidote for severe, life-threatening central anticholinergic effects in a hospital setting, but its use carries significant risk and requires extreme caution. Temperature should be monitored and controlled.
Storage
Store Artane tablets and elixir at controlled room temperature, 20°C to 25°C (68°F to 77°F), in a tight, light-resistant container. Keep the bottle tightly closed and the elixir formulation protected from light. Keep all medications out of the reach of children and pets. Do not use after the expiration date printed on the container.
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 before starting, stopping, or changing any prescribed part of your care plan. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from various sources believed to be accurate but cannot be guaranteed. The manufacturer’s official prescribing information should be consulted for complete details.
Reviews
- Neurologist, 15 years experience: “Artane remains a fundamental tool in my arsenal for managing drug-induced dystonias. Its rapid onset of action is invaluable in the ER setting. For parkinsonian tremor, it’s a reliable option, especially as an adjunct. The side effect profile is predictable and manageable with careful titration.”
- Clinical Pharmacist: “Requires diligent patient education. We emphasize the dry mouth and constipation side effects upfront and counsel on preventative measures (sugar-free gum, increased fiber/water). Monitoring for CNS effects in the elderly is critical to prevent falls and confusion.”
- Patient with Parkinson’s Disease: “It took some time to get the dose right, but it made a noticeable difference in the stiffness in my arms and legs. The dry mouth is bothersome, but drinking water constantly helps. It gave me back some independence with dressing and eating.”
- Patient on Antipsychotics: “I had a severe reaction to my new medication—my neck twisted painfully. A single dose of Artane in the clinic relieved it within an hour. I now have a prescription to take as needed, and it gives me peace of mind.”