Zuclopenthixol is an antipsychotic medicine with a piperazine side chain that blocks postsynaptic dopaminergic brain receptors.
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Dosage in Schizophrenia:
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Its acetate form is used for short-term acute treatment (initial treatment for acute psychosis or exacerbation of psychosis associated with schizophrenia)
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Decanoate injection is mainly intended for long-term management
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Tablets can be used in the initial or maintenance phase.
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Zuclopenthixol Dose in Adults
Management of schizophrenia/ psychoses:
Dosage in the treatment of Acute psychosis:
Acute psychosis:
- Initially, 10 to 50 mg/day is given in 2 to 3 divided doses
- Then increase the dose by 10 to 20 mg every 2 to 3 days
- The usual therapeutic range is 20 to 40 mg/day
- The maximum dose is 100 mg/day
Maintenance therapy:
- Target lowest effective dose
- The usual maintenance dose is 20 to 40 mg/day. It can be given as a single dose
- IM: Zuclopenthixol acetate:
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Normal dose is 50 to 150 mg
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It can be repeated in 2 to 3 day
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The maximum dose given is no more than 400 mg or 4 injections should be given in the course of treatment.
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Duration of treatment should exceed 2 weeks.
Shifting of patients from IM acetate to oral tablets:
- Give a gap of 2 to 3 days after final injection before initiating oral therapy:
- 50 mg of acetate injection given every 2 to 3 days can be replaced with 20 mg daily of oral tablets
- 100 mg of acetate injection given every 2 to 3 days can be replaced with 40 mg daily of oral tablets
- 150 mg of acetate injection given every 2 to 3 days can be replaced with 60 mg daily of oral tablets
Long-term management of psychosis:
Zuclopenthixol decanoate:
Maintenance therapy:
- Usual maintenance dose:
- It is given 150 to 300 mg Intramuscular given every 2 to 4 weeks
- Dose can be increased or reduced
- Frequent administration is needed in some patients.
- Maintain lowest effective dose.
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Transfer of patients from oral tablets to IM decanoate:
Additional oral dosing, with subsequent tapering, might be required during the transition period.
- ≤20 mg daily of oral tablets can be replaced with 100 mg of decanoate injection every 2 weeks
- 25 to 40 mg daily of oral tablets can be replaced with 200 mg of decanoate injection every 2 weeks
- 50 to 75 mg daily of oral tablets can be replaced with 300 mg of decanoate injection every 2 weeks
- >75 mg/day of oral tablets can be replaced with 400 mg of decanoate injection every 2 weeks
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Shifting of patients from IM acetate to IM decanoate:
When starting maintenance therapy with decanoate, give initial dose concomitantly with final acetate injection:
- 50 mg of acetate injection every 48-72 hours can be replaced with 100 mg of decanoate injection every 2 weeks
- 100 mg of acetate injection every 48-72 hours can be replaced with 200 mg of decanoate injection every 2 weeks
- 150 mg of acetate injection every 48-72 hours can be replaced with 300 mg of decanoate injection every 2 weeks
Zuclopenthixol Dose in Children
Not recommended for use in Children.
Pregnancy Risk Factor: C
- In animal reproduction studies, adverse events were observed.
- Use of antipsychotics in the last trimester is associated with abnormal muscle movements (extrapyramidal signs [EPS]), and withdrawal symptoms in infants after delivery.
- The symptoms of a newborn's illness include agitation, feeding disorder and hypotonia.
- These effects can be self-limiting, or may require hospitalization.
Zuclopenthixol Dose in Renal Disease:
Manufacturer's labels do not contain any dosage adjustments (hasn't been studied).
Zuclopenthixol Dose in Liver Disease:
- There are no dosage adjustments given in manufacturer's labeling.
- Use cautiously as zuclopenthixol undergoes extensive hepatic metabolism.
Common Side Effects of Zuclopenthixol Include:
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Central nervous system:
- Drowsiness
- Hypertonia
- Anxiety
- Insomnia
- Akathisia
- Extrapyramidal Reaction
- Dizziness
- Dystonia
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Gastrointestinal:
- Xerostomia
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Neuromuscular & Skeletal:
- Tremor
- Weakness
- Hypokinesia
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Ophthalmic:
- Accommodation disturbance
Less Common Side Effects of Zuclopenthixol Include:
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Cardiovascular:
- Tachycardia
- Orthostatic Hypotension
- Hypotension
- Palpitations
- Syncope
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Central Nervous System:
- Agitation
- Depression
- Lack Of Concentration
- Headache
- Vertigo
- Amnesia
- Apathy
- Confusion
- Hallucination
- Tardive Dyskinesia
- Abnormal Dreams
- Abnormal Gait
- Malaise
- Pain
- Paresthesia
- Anorgasmia
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Dermatologic:
- Diaphoresis
- Seborrhea
- Pruritus
- Pallor
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Endocrine & Metabolic:
- Weight Gain
- Decreased Libido
- Weight Loss
- Menstrual Disease
- Increased Thirst
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Gastrointestinal:
- Constipation
- Sialorrhea
- Anorexia
- Vomiting
- Nausea
- Increased Appetite
- Diarrhea
- Dyspepsia
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Genitourinary:
- Urination Disorder
- Ejaculatory Disorder
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Neuromuscular & skeletal:
- Myalgia
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Ophthalmic:
- Visual disturbance
Contraindication to Zuclopenthixol Include:
- Hypersensitivity to zuclopenthixol, Thioxanthenes, and any part of the formulation
- Acute intoxication (ethanol, barbiturate or opioid)
- CNS depression, coma
- Subcortical brain injury suspected or confirmed
- Circulatory collapse
Warnings and precautions
- Modified cardiac conduction
- It could alter cardiac conduction. Life-threatening arrhythmias can be caused by therapeutic doses.
- Patients with QT prolongation should be avoided.
- Decanoate can have long-lasting adverse effects.
- Anticholinergic effects
- It can cause constipation, xerostomia and blurred vision.
- Patients with reduced gastrointestinal motility, paralytic and ileus, urinary retentions, BPH, xerostomia, and visual impairments should be cautious.
- Zuclopenthixol's cholinergic blockade has been shown to be lower than other neuroleptics.
- Patients should be advised to immediately report any onset or worsening anticholinergic effects.
- Blood dyscrasias
- Clinical trials and postmarketing reports involving antipsychotic use have shown leukopenia and neutropenia.
- Before initiation, take blood samples and continue to do so periodically.
- Depression in the CNS:
- It can lead to CNS depression that can cause mental or physical impairments.
- Patients should be warned about driving or operating machinery that requires mental alertness.
- Aspiration/Esophageal dysmotility/Esophageal dysmotility
- Aspiration and esophageal dysmotility have been linked to antipsychotic use.
- Your risk of developing it increases as you age.
- Patients at high risk of aspiration pneumonia (ie Alzheimer disease) should be treated with caution, especially patients over 75 years.
- Extrapyramidal symptoms
- It can cause extrapyramidal signs (EPS), such as pseudo-parkinsonism and acute dystonic reactions.
- Higher doses of antipsychotics and use of antipsychotics for men, younger patients, and males can increase the risk of dystonia.
- The following factors are associated with higher vulnerability to tardive dyskinesia: older age, female gender, postmenopausal status, previous brain damage, diabetes, alcoholism and Parkinson disease, pseudoparkinsonism symptoms, affective disorder (especially major depressive disorder), poor treatment response, high doses antipsychotics, and poor treatment.
- Stop treating tardive dyskinesia symptoms and signs.
- Hyperglycemia
- Patients without a history of hyperglycemia have had cases of diabetic ketoacidosis.
- Before initiation, measure blood glucose and weight and check again periodically.
- Hyperprolactinemia
- Increased prolactin levels are associated with the use of this drug
- Clinically significant hyperprolactinemia may require dosage adjustments or even stopping.
- Patients with breast cancer, prolactin-dependent tumors and pituitary tumors should be cautious.
- Hypogonadism and prolonged hyperprolactinemia can lead to decreased bone mineral density in males and females.
- Neuroleptic malignant Syndrome (NMS):
- NMS can be caused by antipsychotic drugs, such as zuclopenthixol. Monitor for mental status changes and muscle rigidity.
- With the onset NMS, stop treating immediately
- Patients who have been treated with antipsychotic therapy for a second time have experienced recurrence.
- Ocular:
- Similar drugs can be used to treat pigmentary retinopathy, corneal deposit, and photosensitivity.
- Orthostatic hypotension
- It can lead to orthostatic hypotension
- Patients at high risk for this effect should be supervised.
- Sexual dysfunction
- Reports of decreased libido and ejaculation failure, menstrual problems, erectile dysfunction (including rare priapism) have been made
- A dosage adjustment or complete discontinuation may be necessary for severe dysfunction.
- Discontinuation can cause effects that are irreversible.
- Temperature regulation
- It is possible to have impaired core body temperature regulation
- Be aware of the dangers associated with exercise, heat, dehydration, or concomitant anticholinergic medication.
- Venous thromboembolism, (VTE)
- VTE has been reported with antipsychotics. Ensure that you assess VTE risk prior to and during therapy.
- Withdrawal syndrome
- When withdrawing from therapy, be careful
- Reduce slowly and be aware of withdrawal symptoms.
- An abrupt cessation of treatment can lead to (rarely) severe withdrawal symptoms, such as nausea, vomiting, and insomnia.
- Symptoms are usually felt within four days and disappear within one to two weeks.
- Cardiovascular disease
- Patients with heart disease should be cautious.
- Dementia
- Antipsychotics have a higher death rate than placebo for dementia-related psychosis in the elderly.
- The majority of deaths were caused by either infectious (eg pneumonia) or cardiovascular problems in nature.
- Elderly patients with dementia-related psychosis have a higher incidence of cerebrovascular adverse event (including fatalities).
- Zuclopenthixol has not been approved for elderly patients suffering from dementia or dementia-related psychosis.
- Hepatic impairment
- Patients with hepatic impairment should be cautious; hepatic metabolism is affected.
- Renal impairment
- Patients with impaired renal function should be cautious. This has not been tested.
- Seizure disorder
- Patients at high risk of seizures should be treated with caution
Zuclopenthixol (United States: Not available): Drug Interaction
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Acetylcholinesterase Inhibitors |
May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. |
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Acetylcholinesterase Inhibitors (Central) |
May enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients. |
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Ajmaline |
May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). |
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Alcohol (Ethyl) |
CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). |
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Alizapride |
May enhance the CNS depressant effect of CNS Depressants. |
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Amifampridine |
Agents With Seizure Threshold Lowering Potential may enhance the neuroexcitatory and/or seizure-potentiating effect of Amifampridine. |
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Amphetamines |
Antipsychotic Agents may diminish the stimulatory effect of Amphetamines. |
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Anticholinergic Agents |
May enhance the adverse/toxic effect of other Anticholinergic Agents. |
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Botulinum Toxin-Containing Products |
May enhance the anticholinergic effect of Anticholinergic Agents. |
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Brexanolone |
CNS Depressants may enhance the CNS depressant effect of Brexanolone. |
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Brimonidine (Topical) |
May enhance the CNS depressant effect of CNS Depressants. |
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Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
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Cannabis |
May enhance the CNS depressant effect of CNS Depressants. |
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Chloral Betaine |
May enhance the adverse/toxic effect of Anticholinergic Agents. |
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Chlorphenesin Carbamate |
May enhance the adverse/toxic effect of CNS Depressants. |
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CloBAZam |
May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). |
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CNS Depressants |
May enhance the adverse/toxic effect of other CNS Depressants. |
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CYP2D6 Inhibitors (Moderate) |
May decrease the metabolism of CYP2D6 Substrates (High risk with Inhibitors). |
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CYP3A4 Inducers (Strong) |
May decrease the serum concentration of Zuclopenthixol. |
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CYP3A4 Inhibitors (Moderate) |
May increase the serum concentration of Zuclopenthixol. |
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Deutetrabenazine |
May enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, the risk for akathisia, parkinsonism, or neuroleptic malignant syndrome may be increased. |
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Dimethindene (Topical) |
May enhance the CNS depressant effect of CNS Depressants. |
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Doxylamine |
May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. |
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Dronabinol |
May enhance the CNS depressant effect of CNS Depressants. |
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Esketamine |
May enhance the CNS depressant effect of CNS Depressants. |
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Gastrointestinal Agents (Prokinetic) |
Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). |
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Glucagon |
Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. |
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Guanethidine |
Antipsychotic Agents may diminish the therapeutic effect of Guanethidine. |
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Haloperidol |
QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTcprolonging effect of Haloperidol. |
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HydrOXYzine |
May enhance the CNS depressant effect of CNS Depressants. |
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Imatinib |
May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). |
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Itopride |
Anticholinergic Agents may diminish the therapeutic effect of Itopride. |
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Kava Kava |
May enhance the adverse/toxic effect of CNS Depressants. |
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Lithium |
May enhance the neurotoxic effect of Antipsychotic Agents. Lithium may decrease the serum concentration of Antipsychotic Agents. Specifically noted with chlorpromazine. |
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Lofexidine |
May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
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Lumefantrine |
May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). |
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Magnesium Sulfate |
May enhance the CNS depressant effect of CNS Depressants. |
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Methylphenidate |
Antipsychotic Agents may enhance the adverse/toxic effect of Methylphenidate. Methylphenidate may enhance the adverse/toxic effect of Antipsychotic Agents. |
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MetyroSINE |
CNS Depressants may enhance the sedative effect of MetyroSINE. |
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MetyroSINE |
May enhance the adverse/toxic effect of Antipsychotic Agents. |
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Mianserin |
May enhance the anticholinergic effect of Anticholinergic Agents. |
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Minocycline |
May enhance the CNS depressant effect of CNS Depressants. |
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Mirabegron |
Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. |
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Mirtazapine |
CNS Depressants may enhance the CNS depressant effect of Mirtazapine. |
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Nabilone |
May enhance the CNS depressant effect of CNS Depressants. |
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Nitroglycerin |
Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. |
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Panobinostat |
May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). |
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Peginterferon Alfa-2b |
May decrease the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Peginterferon Alfa-2b may increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). |
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Perhexiline |
CYP2D6 Substrates (High risk with Inhibitors) may increase the serum concentration of Perhexiline. Perhexiline may increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). |
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QT-prolonging Agents (Highest Risk) |
QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
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Quinagolide |
Antipsychotic Agents may diminish the therapeutic effect of Quinagolide. |
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QuiNINE |
May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). |
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Ramosetron |
Anticholinergic Agents may enhance the constipating effect of Ramosetron. |
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Rufinamide |
May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. |
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Selective Serotonin Reuptake Inhibitors |
CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. |
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Serotonin Modulators |
May enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Exceptions: Nicergoline. |
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Tetrabenazine |
May enhance the adverse/toxic effect of Antipsychotic Agents. |
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Tetrahydrocannabinol |
May enhance the CNS depressant effect of CNS Depressants. |
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Tetrahydrocannabinol and Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
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Thiazide and Thiazide-Like Diuretics |
Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. |
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Topiramate |
Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. |
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Trimeprazine |
May enhance the CNS depressant effect of CNS Depressants. |
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Risk Factor D (Consider therapy modification) |
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Abiraterone Acetate |
May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Management: Avoid concurrent use of abiraterone with CYP2D6 substrates that have a narrow therapeutic index whenever possible. When concurrent use is not avoidable, monitor patients closely for signs/symptoms of toxicity. |
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Anti-Parkinson Agents (Dopamine Agonist) |
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Asunaprevir |
May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). |
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Blonanserin |
CNS Depressants may enhance the CNS depressant effect of Blonanserin. |
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Buprenorphine |
CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. |
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Chlormethiazole |
May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. |
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CYP2D6 Inhibitors (Strong) |
May decrease the metabolism of CYP2D6 Substrates (High risk with Inhibitors). |
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CYP3A4 Inhibitors (Strong) |
May increase the serum concentration of Zuclopenthixol. Management: Consider zuclopenthixol dosage reduction with concomitant use of a strong CYP3A4 inhibitor (eg, ketoconazole) in poor CYP2D6 metabolizers or with strong CYP2D6 inhibitors (eg, paroxetine). Monitor for increased zuclopenthixol levels/toxicity. |
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Dacomitinib |
May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Management: Avoid concurrent use of dacomitinib with CYP2D6 subtrates that have a narrow therapeutic index. |
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Droperidol |
May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
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Flunitrazepam |
CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. |
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HYDROcodone |
CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
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Iohexol |
Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iohexol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iohexol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. |
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Iomeprol |
Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iomeprol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iomeprol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. |
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Iopamidol |
Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iopamidol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iopamidol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. |
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Mequitazine |
Antipsychotic Agents may enhance the arrhythmogenic effect of Mequitazine. Management: Consider alternatives to one of these agents when possible. While this combination is not specifically contraindicated, mequitazine labeling describes this combination as discouraged. |
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Methotrimeprazine |
CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. |
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Opioid Agonists |
CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
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OxyCODONE |
CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
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Perampanel |
May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. |
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Pramlintide |
May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. |
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Secretin |
Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. |
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Sodium Oxybate |
May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. |
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Suvorexant |
CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. |
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Tapentadol |
May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. |
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Zolpidem |
CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. |
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Risk Factor X (Avoid combination) |
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Aclidinium |
May enhance the anticholinergic effect of Anticholinergic Agents. |
|
Amisulpride |
Antipsychotic Agents may enhance the adverse/toxic effect of Amisulpride. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
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Azelastine (Nasal) |
CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). |
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Bromopride |
May enhance the adverse/toxic effect of Antipsychotic Agents. |
|
Bromperidol |
May enhance the CNS depressant effect of CNS Depressants. |
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Cimetropium |
Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. |
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Eluxadoline |
Anticholinergic Agents may enhance the constipating effect of Eluxadoline. |
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Glycopyrrolate (Oral Inhalation) |
Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). |
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Glycopyrronium (Topical) |
May enhance the anticholinergic effect of Anticholinergic Agents. |
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Ipratropium (Oral Inhalation) |
May enhance the anticholinergic effect of Anticholinergic Agents. |
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Levosulpiride |
Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. |
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Metoclopramide |
May enhance the adverse/toxic effect of Antipsychotic Agents. |
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Orphenadrine |
CNS Depressants may enhance the CNS depressant effect of Orphenadrine. |
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Oxatomide |
May enhance the anticholinergic effect of Anticholinergic Agents. |
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Oxomemazine |
May enhance the CNS depressant effect of CNS Depressants. |
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Paraldehyde |
CNS Depressants may enhance the CNS depressant effect of Paraldehyde. |
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Piribedil |
Antipsychotic Agents may diminish the therapeutic effect of Piribedil. Piribedil may diminish the therapeutic effect of Antipsychotic Agents. Management: Use of piribedil with antiemetic neuroleptics is contraindicated, and use with antipsychotic neuroleptics, except for clozapine, is not recommended. |
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Potassium Chloride |
Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. |
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Potassium Citrate |
Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. |
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Revefenacin |
Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. |
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Sulpiride |
Antipsychotic Agents may enhance the adverse/toxic effect of Sulpiride. |
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Thalidomide |
CNS Depressants may enhance the CNS depressant effect of Thalidomide. |
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Tiotropium |
Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. |
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Umeclidinium |
May enhance the anticholinergic effect of Anticholinergic Agents. |
Monitor:
- Mental health
- Vital signs (as indicated by a doctor)
- ECG for patients with QT prolongation, other cardiovascular disorders, or electrolyte disturbances
- Weight, height, waist circumference, and BMI (baseline) at each visit for the first six months. Visits are made quarterly with stable antipsychotic medication.
- CBC (as indicated by the doctor; patients with low WBC, or a history of drug-induced neutropenia/neutropenia should be monitored frequently in the first few months.
- Electrolytes and liver function (yearly and as indicated by a physician)
- Fasting plasma glucose level/ HbA
- lipid panel (baseline, repeat every 2 years if LDL levels are normal; repeat every 6 month if LDL levels exceed 130 mg/dL).
- Changes in menstruation, libido and development of galactorrhea (at each visit during the first 12 weeks following the antipsychotic's administration or until the dose becomes stable, then annually)
- Parkinsonian signs or abnormal involuntary movements (baseline; continue weekly until dose stabilization for at least two weeks after introduction, and for at most 2 weeks following any significant dose increases).
- Tightening of the teeth (every 6 to 12 months; high-risk patients, every 3 months).
- Visual changes (inquire annually)
- Ocular examinations (yearly for patients over 40 years old; every 2 years for younger patients).
How to administer Zuclopenthixol?
Intramuscular: Acetate or decanoate:
- Apply the medication by injecting deeply into the gluteal area.
- Two injection sites should be used for injection volumes exceeding 2 milliliters.
- You can mix the decanoate and acetate formulations together in one syringe to administer the injections as a single dose.
Oral:
- Tablets should be taken in divided doses of 2 to 3 tablets after initial dosing
- It could switch to once-daily administration at night during maintenance treatment. It can be administered at night without regard for meals.
Mechanism of action of Zuclopenthixol:
- Zuclopenthixol, a thioxanthene antipsychotic that also includes a piperazine side-chain, is called Zuclopenthixol.
- It is closely related to fluphenazine. The cis(z]-clopenthixol active isomer is this neuroleptic.
- It blocks brain receptors for postsynaptic dopaminergic D-1 and D-2 (D-1 & D-2).
- It has a strong affinity for alpha-1 and 5-HT adrenergic receptors and a weaker affinity to histamine -receptors.
The start of actionAcetate injection: Sedation in 2 Hours
TimeAcetate injections: 2 - 3 Days
Distribution: V: 20 L/kg
Protein bindingAlmost 98%
Metabolism: Mainly Hepatic via N-dealkylation and sulfoxidation It is also subject to glucuronidation. The metabolites are inactive.
Eliminating half-lifeTerminal: Oral: Almost 20 Hours; Depot: 19 Days
Time to reach peak: Tablet: 4 hours; Acetate injection: 24 to 48 hours; Decanoate inject: 3-7 Days
Excretion: Mainly feces and urine (10%, minimal amount as unmodified drug).
International Brands of Zuclopenthixol:
- Ciatyl-Z
- Ciatyl-Z Acuphase
- Ciatyl-Z Depot
- Cisordinol
- Cisordinol Acutard
- Cisordinol Depot
- Cisordinol-Acutard
- Cisordinol-Acutard[inj.]
- Clopixol
- Clopixol Acuphase
- Clopixol Acutard
- Clopixol Depot
- Klopiksol
Zuclopenthixol brands in Pakistan:
|
Zuclopenthixol [Inj 25 Mg/Ml] |
|
| Clopenia | Ipram International |
|
Zuclopenthixol [Inj 50 Mg/Ml] |
|
| Clopenia | Ipram International |
| Clopixol | Lundbeck Pakistan (Pvt) Ltd. |
| Clopixol | Lundbeck Pakistan (Pvt) Ltd. |
| Xopixol | Genetics Pharmaceuticals |
| Xopixol Acuphase | Reko Pharmacal (Pvt) Ltd. |
|
Zuclopenthixol [Inj 100 Mg/Ml] |
|
| Zucloact | Nabiqasim Industries (Pvt) Ltd. |
|
Zuclopenthixol [Inj 200 Mg/Ml] |
|
| Xopixol La | Genetics Pharmaceuticals |
| Zuclodept | Nabiqasim Industries (Pvt) Ltd. |
|
Zuclopenthixol [Inj Sr 200 Mg/Ml] |
|
| Clopixol | Lundbeck Pakistan (Pvt) Ltd. |
|
Zuclopenthixol [Tabs 2 Mg] |
|
| Clopixol | Lundbeck Pakistan (Pvt) Ltd. |
| Zulpram | Ameer Pharma |
|
Zuclopenthixol [Tabs 10 Mg] |
|
| Clopixol | Lundbeck Pakistan (Pvt) Ltd. |
| Zulpram | Ameer Pharma |
|
Zuclopenthixol [Tabs 25 Mg] |
|
| Clopixol | Lundbeck Pakistan (Pvt) Ltd. |
| Zulpram | Ameer Pharma |
