Drug information of Zuclopenthixol


Drug group:

Zuclopenthixol, also known as Zuclopentixol or Zuclopenthixolum, is an antipsychotic agent. Zuclopenthixol is a thioxanthene-based neuroleptic with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors
It is used in the management of acute psychoses such as mania or schizophrenia. However, the use of zuclopenthixol acetate in psychiatric emergencies as an alternative to standard treatments (haloperidol, clotiapine, etc.) should be cautioned, since well executed and documented trials of zuclopenthixol acetate for this use have yet to be conducted. Zuclopenthixol acetate is not intended for long-term use

:Dosage Forms & Strengths
Tab: 10 mg
FC tab: 2 mg
Solution for injection: 200 mg/mL Zuclopenthixol decanoate
Solution for injection: 50 mg/mL Zuclopenthixol acetate

Mechanism of effect

Zuclopenthixol is a typical antipsychotic neuroleptic drug of the thioxanthene class. It mainly acts by antagonism of D1 and D2 dopamine receptors. Zuclopenthixol also has high affinity for alpha1-adrenergic and 5-HT2 receptors. It has weaker histamine H1 receptor blocking activity, and even lower affinity for muscarinic cholinergic and alpha2-adrenergic receptors


Zuclopenthixol is a thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors


Upon reaching the body water phase, the decanoate ester is slowly released from the oil depot, which is resultantly hydrolyzed to the active substance, zuclopenthixol. The decanoate ester provides a means of slow release since zuclopenthixol itself is a short-acting drug

Vd: 20 L/Kg
PB: 98-99%

The metabolism of zuclopenthixol is mainly by sulphoxidation, side chain N-dealkylation and glucuronic acid conjugation. The metabolites are devoid of pharmacological activity

Half-life: 20 hours (range 12-28 hours) for the tablet form, 19 days for the depot form
Clearance: approximately 0.9 L/min

Primarily in the feces with approximately 10% in the urine


:Acute psychosis
Initial:10 to 50 mg/day in 2 to 3 devided doses, may titrate dose upward by 10 to 20 mg every 2 to 3 days, usual therapeutic range: 20-40 mg/day, maximum dose: 100 mg/day
Maintenance therapy: maintain lowest effective dose, usual maintenace dose: 20-40 mg/day, may be given as a single dose

50-150mg, may be repeated in 2-3 days
Max: 400 mg or 4 injections and the duration of treatment: 2 weeks

Transfer of patients from IM to ORAL tablets: Allow 2-3 days after final injection before initiating oral therapy
50mg of acetate injection every 2-3 days = 20mg daily of oral tablets
100mg of acetate injection every 2-3 days = 40mg daily of oral tablets
150mg of acetate injection every 2-3 days = 60mg daily of oral tablets


Neuroleptic Malignant Syndrome: NMS has been associated with use of antipsychotic agents, including zuclopenthixol

Points of recommendation

:Adverse Effects
CNS: drowsiness, hypertonia, anxiety, insomnia, akathisia, extrapyramidal reaction, dizziness, dystonia, agitation, depression. lack of concentration, headache, vertigo, amnesia, apathy, confusion, hallucination, tardive dyskinesia, abnormal dreams, abnormal gait, malaise, pain, paresthesia, anorgasmia in females

Gastrointestinal: xerostomia, constipation, sialorrhea, anorexia, vomiting, nausea, increased appetite, diarrhea, dyspepsia

Neuromuscular & skeletal: tremor, weakness, hypokinesia, myalgia

Ophthalmic: accommodation disturbance, visual disturbance

CVD: tachycardia, orthostatic hypotention, hypotention, palpitaions. syncope

Dermatologic: diaphoresis, seborrhea, pruritus

Endocrine & Metabolic: weight gain, decreased libido, weight loss, menstrual disease, increased thirst

Genitourinary: urination disorder, ejaculatory disorder

Hypersensitivity to zuclopenthixol. thoxanthenes or any component of the formulation
Acute intoxication  » ethanol, barbiturate or opiood
Suspected or established subcortical brain damage
Circulatory collapse

Pregnancy level

Adverse events were observed in animal reproduction studies. Antipsychotic use during the third trimester of pregnancy has a risk for abnormal muscle movements (Extrapymidal Syndroms/EPS) and withdrawal symptoms in newborns following delivery. Symptoms in the newborn may include agitation, feeding disorder, hypertonia, hypotonia, respiratory distress, somnollence and tremor. these effects may be self-limiting or require hospitalization

Breast feeding warning

Data not available

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