Zuclopenthixol was introduced in 1962, by Lundbeck. It's the Cis(z) isomer of Clopenthixol. It's an aged Neuroleptic drug, used to cure Schizophrenia and psychoses. Zuclopenthixol drug that binds to and blocks a receptor Dopamine Zuclopenthixol has been utilized in the treatment of acute psychotic episodes, schizophrenia, and various other psychotic disorders.
It's veritably useful to manage aggressive geste. On the other hand, it can beget side goods like extrapyramidal symptoms (EPS), akathisia, include tardive dyskinesia.
BRAND NAMES
Cisordinol-The maximum amount to be taken at one time is 40mg.
CLOPIXOL-Acuphase -The recommended dosage range per day is 50-150mg.
Repeated if needed, preferably with a 2-3day gap.
MECHANISM OF ACTION
Zuclopenthixol, a typical counteracting psychosis, primarily works by blocking receptor dopamine. This action helps to reduce the overactivity of dopamine, a neurotransmitter involved in regulating mood, cognition, and behavior, which is often associated with psychotic disorders like schizophrenia. It also strongly binds to alpha1-adrenergic and 5-HT2 receptors, but has weaker effects on histamine H1 receptors, and even less on muscarinic cholinergic and alpha2-adrenergic receptors. This translates to its antipsychotic effects being mediated by dopamine receptor antagonism, with additional influences from other receptor interactions.
PHARMACOKINETICS
Absorption
Upon reaching the body's fluid compartment, the decanoate ester formulation acts like a slow-release system for the drug. The ester, being lipophilic (fat-loving), is stored in an oil depot, likely in the muscle or subcutaneous tissue where it's injected. Once in the body’s aqueous environment, the ester is gradually released and then hydrolyzed, releasing the active form of zuclopenthixol. This controlled release mechanism is essential, as the drug itself is rapidly cleared from the body.
Distribution
The usual apparent volume of distribution at steady state measures 20 L/kg.
Metabolism
Zuclopenthixol is primarily broken down in the body through three main processes: sulphoxidation, N-dealkylation of its side chain, and conjugation with glucuronic acid. The substances produced during these metabolic reactions (the metabolites) do not have any drug-like effects.
Excretion
The substance is primarily found in the stool, and a smaller portion is found in the urine.
Pharmacodynamics
Zuclopenthixol drug that binds to and blocks a receptor Dopamine, alpha1-adrenoceptors, and 5-HT2 receptors. However, it does not bind to muscarinic acetylcholine receptors. It exhibits a weak antagonistic effect on the histamine (H1) receptor. In vitro studies and clinical data, including therapeutic drug monitoring databases, indicate that Cytochrome P450 enzymes CYP2D6 and CYP3A4 play significant roles in the metabolism of zuclopenthixol.
Administration
Administered deep into the muscle of the upper outer buttock or the lateral thigh. As with all oil-based injections, it is important to ensure, by drawing back the plunger (aspirating) before injection, that accidental entry into a blood vessel does not occur.
Dosage and Strengths
Cisordinol-it is a long-acting intramuscular injection.
The strength of this injection is 200-500mg.
Clopixol-Acuphase- It is in the form of Injection.
The strength of this injection is 50mg/mL
Drug Interactions
• "Affecting heart rhythm" in the context of drug interactions refers to the potential of a medication, when combined with other substances, to cause changes in the electrical activity that controls the heart's beating pattern.
• Zuclopenthixol, for example, can cause QT prolongation, a specific type of electrical rhythm disturbance that can increase the risk of serious side effects like fast/irregular heartbeat, according to My Health Alberta.
• Such drug-induced changes in heart rhythm are also known as arrhythmias and can involve the heart beating too fast (tachycardia), too slow (bradycardia), or simply irregularly.
Food Interactions
avoid consuming alcohol while taking zuclopenthixol, because acute alcohol intoxication is an absolute contraindication for this treatment. Zuclopenthixol can be taken with or without food, but it's important to be mindful of potential interactions with beverages like alcohol, caffeinated drinks, and some herbal remedies.
Contraindications
A documented record of a patient experiencing a negative and potentially harmful reaction to a specific medication or any of the ingredients it contains, Compromised liver or kidney function, Conditions affecting the heart or blood vessels, A progressive disorder of the nervous system affecting movement, A neurological disorder characterized by seizures, An underactive thyroid gland, Enlargement of the prostate gland, A type of glaucoma that can cause rapid increases in eye pressure, A tumor of the adrenal gland, A chronic autoimmune neuromuscular disease characterized by muscle weakness.
Side Effects
Unsteadiness, vertiginous, lethargy, dyschezia, headache, dry mouth, blurred vision, urinary hesitancy, tiredness, or pain/redness at the injection site may occur. changes in body weight, insomnia, Feeling anxious, agitated, or irritable, Problems with sexual desire, arousal, orgasm, or pain during intercourse. Higher density in the breast tissue accompanied by painful cramps. Increased mouth watering, irregular heartbeat, Difficulty breathing. difficulty digesting food, the sensation of wanting to vomit, indigestion. Trembling or Quivering, sluggish motion, involuntary movements.
Overdose
Signs of an over dose may include:
• specific sedative causes fewer or less severe reductions in a person's level of awareness and their breathing rate compared to other types of sedatives.
• Feeling abnormally sleepy or tired.
• Insensibility
• Muscle rigidity or reduced range of motion.
• seizures
• sudden drop in blood pressure.
Toxicity
• Central Nervous System Effects
• Extrapyramidal Symptoms
• Cardiovascular Effects
• In addition to these, a rare but serious side effect known as Neuroleptic Malignant Syndrome (NMS) can occur, characterized by fever, muscle rigidity, confusion, and autonomic dysfunction.
Storage
Store below 25°C (77°F). Protect from light. Keep in a cool, dry place. Avoid storing it in bathrooms, near sinks, on windowsills, or in cars. Keep out of reach of children. The storage location should be in one and half meter distance in a closed area. Do not refrigerate or freeze zuclopenthixol injections.
Tablets- Store between 15°C and 25°C. Some strengths (like 2mg) may require storage in the original container for light protection.
Injections- It should be kept at a temperature between 15 degrees Celsius and 25 degrees Celsius. Some formulations do not require special temperature conditions but should be kept in the outer carton for light protection.
