Zuclopenthixol

Indications

Zuclopenthixol is indicated for the management of the manifestations of schizophrenia. This is intended for the initial treatment of acute psychotic episodes or exacerbation of psychosis associated with schizophrenia.

Pharmacology

Zuclopenthixol, a thioxanthene derivative, has high affinity for both dopamine D1 receptors and dopamine D2 receptors. Zuclopenthixol also has high affinity for α1 -adrenergic and 5 HT2 receptors. It has weaker histamine H1 receptor blocking activity, and even lower affinity for muscarinic cholinergic and α2 -adrenergic receptors.

Dosage & Administration

Zuclopenthixol Tablets: When initiating treatment with Zuclopenthixol tablets, it is recommended that the drug be given in divided doses (BID or TID). During the maintenance phase of treatment Zuclopenthixol tablets may be given as a single nighttime dose. For acute psychosis, the usual starting dose is 10-50 mg/day, which may be increased by 10-20 mg every 2-3 days, according to the patient’s response. The usual therapeutic range is 20 mg to 60 mg daily. However, as with other antipsychotic drugs, some patients may require lower, while others may require higher dosage in order to obtain optimal benefit. Daily dosage higher than 100 mg is not recommended. For maintenance therapy, dosage should be reduced to the lowest level compatible with symptom control. The usual maintenance dose is 20-40 mg/day.

Zuclopenthixol Acuphase: Dosage should be individually adjusted according to the patient’s condition. The usual dose is 50-150 mg (1-3 ml) administered intramuscularly and repeated if necessary, at intervals of 2-3 days. Some patients may need an additional injection 1 or 2 days after the first injection.

Zuclopenthixol Depot: Close supervision is required during the period following initiation of Zuclopenthixol Depot treatment, in order to minimize the risk of over-medication or insufficient suppression of psychotic symptoms. Supplemental oral antipsychotic medication may be required in diminishing dosage during this period. The usual maintenance dose is 150-300 mg intramuscularly, every 2-4 weeks. Some patients may require higher or lower doses, or shorter intervals between doses.

Interaction

Drugs that may interact with Zuclopenthixol include:
  • tricyclic antidepressant medicines
  • guanethidine and similar medicines (used to lower the blood pressure)
  • barbiturates and similar medicines
  • levodopa and similar medicines (used to treat Parkinson’s disease)
  • metoclopramide (used in the treatment of gastro-intestinal disorders)
  • other antipsychotic medicines (e.g. thioridazine)
  • medicines that change the heartbeat (e.g. quinidine, amiodarone, sotalol, erythromycine, moxifloxacin, lithium)

Contraindications

  • Acute alcohol, barbiturate or opiate intoxication.
  • CNS depression due to any cause, comatose states, suspected or established subcortical brain damage or circulatory collapse.
  • Patients with known hypersensitivity to thioxanthenes, zuclopenthixol or to any ingredient in the formulation or component of the container.

Side Effects

Common side effects are Racing heart (tachycardia), a sensation of a rapid, forceful, or irregular beating of the heart (palpitations) Tremor, twisting or repetitive movements or abnormal postures due to sustained muscle contractions (dystonia), increased muscle stiffness (hypertonia).

Pregnancy & Lactation

The safe use of zuclopenthixol during pregnancy has not been established. Zuclopenthixol is excreted in human milk. The safe use of zuclopenthixol during lactation has not been established.

Precautions & Warnings

Caution should be taken if-
  • you have used zuclopenthixol or any other treatment for schizophrenia before and if you had any problems
  • you are taking any other prescription or non-prescription medicines
  • you are pregnant or thinking of becoming pregnant, or if you are breast-feeding
  • you regularly drink a lot of alcohol
  • you have any liver problems, Parkinson’s disease or have ever had seizures
  • you have dementia
  • you have glaucoma
  • you have any kidney problems
  • you have risk factors for stroke (e.g. smoking, high blood pressure).
  • you have hypokalemia or hypomagnesia (too little potassium or magnesium in your blood)
  • you have a history of cardiovascular disorders
  • you or someone in your family has a history of blood clots
  • you are being treated for cancer (applies to zuclopenthixol Depot only)
  • you use any other antipsychotic medicine

Use in Special Populations

The safety and efficacy of zuclopenthixol in children under the age of 18 years have not been established, therefore its use is not recommended.

Overdose Effects

Symptoms of overdose may include: somnolence, coma, unusual movements, convulsions, shock, high or low body temperature

Therapeutic Class

Phenothiazine related drugs

Storage Conditions

Should be stored between 15°C and 25°C. Protect from light.