Xopixol Acuphase

Xopixol Acuphase Uses, Dosage, Side Effects, Food Interaction and all others data.

Xopixol Acuphase has high affinity for D1 and D2 receptors and α-adrenoreceptors. It also has slight antihistamine properties and blocks serotonergic properties.

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

Trade Name Xopixol Acuphase
Generic Zuclopenthixol
Zuclopenthixol Other Names Zuclopenthixol, Zuclopenthixolum, Zuclopentixol
Weight 50mg/ml
Type Injection
Formula C22H25ClN2OS
Weight Average: 400.965
Monoisotopic: 400.137611829
Protein binding

98-99%

Groups Approved, Investigational
Therapeutic Class Phenothiazine related drugs
Manufacturer Reko Pharmacal (pvt) Ltd,
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am
Xopixol Acuphase
Xopixol Acuphase

Uses

Bipolar mania, Psychosis, Schizophrenia

Xopixol Acuphase is also used to associated treatment for these conditions: Acute Exacerbation of Psychosis, Acute Schizophrenia, Chronic Schizophrenia, Organic Mental Disorder, Schizophrenia, Acute Manic episode

How Xopixol Acuphase works

Xopixol Acuphase is a typical antipsychotic neuroleptic drug of the thioxanthene class. It mainly acts by antagonism of D1 and D2 dopamine receptors. Xopixol Acuphase 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.

Dosage

Xopixol Acuphase dosage

Intramuscular-

Chronic psychosis:

  • Adult: As decanoate ester: Initially, a test dose of 100 mg by deep IM into the upper outer buttock or lateral thigh to access tolerance, followed after at least 1 wk by 200-500 mg or more, repeated at 1-4 wkly intervals according to response. Max dose: 600 mg wkly. Inj >2 ml to be distributed between 2 inj sites.
  • Elderly: Reduce dose to ¼ or ½ of usual initial dose.

Psychoses:

  • Adult: As acetate: 50-150 mg via deep IM inj. May repeat, if needed, after 2-3 days. An additional dose 1-2 days after the 1st dose may be required in some patients. Not >4 inj should be given in a max course of 2 wk and total dose should not exceed 400 mg. Maintenance: May start oral zuclopenthixol HCl 2-3 days after the last acetate inj or begin IM inj of decanoate with the last inj of the acetate.
  • Elderly: As acetate ester: Dose reduction may be needed. Max: 100 mg/dose.

Oral-

Psychoses:

  • Adult: Initially, 20-30 mg daily in divided doses. Usual maintenance dose: 20-50 mg daily. Up to 150 mg daily for severe or resistant cases.

May be taken with or without food.

Side Effects

Drowsiness, blurred vision, tachycardia, nausea, dizziness, headache, excitement, postural hypotension, hyperprolactinaemia, sexual dysfunction, ECG changes (prolongation of QT interval and T wave changes), hyperthermia. Extrapyramidal symptoms may occur, especially during the early phase of treatment; urinary frequency or incontinence; tardive dyskinesia.

Toxicity

Although there have not been any cases of overdosage reported, the symptoms are likely to be somnolence, coma, extrapyramidal symptoms, convulsions, hypotension, shock, or hyper- or hypothermia.

Neuroleptic malignant syndrome may occur. Xopixol Acuphase may potentiate anticholinergic effects of concurrent medications. Xopixol Acuphase has a demonstrated antiemetic effect in animals, and may mask signs of toxicity due to other drug overdoses, or may mask symptoms of disease.

Precaution

Hepatic and renal impairment, heart disease, recent acute MI, arrhythmias, significant bradycardia (<50 beats/min), severe respiratory disease, epilepsy (and conditions at risk of epilepsy, e.g. alcohol withdrawal or brain damage), Parkinson's disease, acute angle glaucoma, prostatic hypertrophy, hypothyroidism, hyperthyroidism, myasthenia gravis, phaeochromocytoma. Patients at risk of stroke and QT interval prolongation. Avoid abrupt withdrawal. Ability to drive a car or operate machinery may be impaired.

Interaction

Xopixol Acuphase may enhance the sedative effects of alcohol and the effects of barbiturates and other CNS depressants. Xopixol Acuphase reduces the antihypertensive effect of guanethidine. Concomitant use of metoclopramide and piperazine with zuclopenthixol increases the risk of extrapyramidal symptoms. Increased risk of severe neurotoxicity with lithium and sibutramine. Increased anticholinergic side effects with drugs with anticholinergic properties.

Food Interaction

  • Avoid alcohol. Acute alcohol intoxication is a contraindication for zuclopenthixol therapy.
  • Take with or without food.

Volume of Distribution

20 L/kg.

Elimination Route

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.

Half Life

20 hours (range 12-28 hours) for the tablet form, 19 days for the depot form.

Clearance

approximately 0.9 L/min.

Elimination Route

Primarily in the feces with approximately 10% in the urine.

Pregnancy & Breastfeeding use

Pregnancy Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

Hypersensitivity. Comatose states e.g. alcohol, barbiturate and opiate intoxications; porphyria. children.

Special Warning

Renal Impairment: Intramuscular:

  • Chronic psychosis: Dose reduction may be needed.
  • Psychoses: Renal failure: Half of the normal dose.

Oral: Dose reduction may be needed.Hepatic Impairment: Intramuscular:

  • Chronic psychosis: Dose reduction may be needed.
  • Psychoses: Half of the normal recommended dose.

Oral: Dose reduction may be needed.

Acute Overdose

Symptoms: Somnolence, extrapyramidal symptoms, convulsions, hypotension, shock, hyper or hypothermia, ECG changes e.g. QT prolongation, torsade de pointes, cardiac arrest, ventricular arrhythmias and coma. Management: Treatment is symptomatic and supportive with close monitoring of the respiratory and CV systems. Do not use adrenaline (epinephrine) in these patients.

Storage Condition

Store below 25° C. Protect from light.

Innovators Monograph

You find simplified version here Xopixol Acuphase

Xopixol Acuphase contains Zuclopenthixol see full prescribing information from innovator Xopixol Acuphase Monograph, Xopixol Acuphase MSDS, Xopixol Acuphase FDA label

FAQ

What type of drug is Xopixol Acuphase?

Xopixol Acuphase is a typical antipsychotic neuroleptic drug of the thioxanthene class. It mainly acts by antagonism of D1 and D2 dopamine receptors. Xopixol Acuphase also has high affinity for alpha1-adrenergic and 5-HT2 receptors.

What is Xopixol Acuphase used for?

Xopixol Acuphase is a psychiatric medication (antipsychotic-type) that works by helping to restore the balance of certain natural substances in the brain (neurotransmitters). This medication can improve the symptoms of schizophrenia, making it easier to function in everyday life.

How quickly does Xopixol Acuphase work?

It may take between four and six months before you feel better. Your doctor will decide the duration of treatment

How long does Xopixol Acuphase stay in my system?

Xopixol Acuphase decanoate is a depot injection which slowly releases Xopixol Acuphase into your body to prevent your symptoms from coming back. It is given every 1-4 weeks.

What are the main side effects of Xopixol Acuphase acetate?

Dizziness, lightheadedness, drowsiness, constipation, headache, dry mouth, blurred vision, difficulty urinating, tiredness, or pain/redness at the injection site may occur. If these effects persist or worsen, tell your doctor or pharmacist promptly. Dizziness and lightheadedness can increase the risk of falling.

How do I administer Xopixol Acuphase?

Xopixol Acuphase acetate is to be administered by deep intramuscular injection, into the upper outer buttock or lateral thigh. Onset and duration of Action: The sedative effects usually begin to be seen 2 hours after the injection and peak at around 36 hours.

How do I give Xopixol Acuphase decanoate?

Test dose 100 mg, dose to be administered into the upper outer buttock or lateral thigh, followed by 200–500 mg after at least 7 days, then 200–500 mg every 1–4 weeks, adjusted according to response, higher doses of more than 500mg can be used; do not exceed 600 mg weekly.

Is Xopixol Acuphase a sedating?

Xopixol Acuphase is a sedative drug. Alertness may be impaired, especially at the start of treatment, or following the consumption of alcohol; patients should be warned of this risk and advised not to drive or operate machinery until their susceptibility is known. Patients should not drive if they have blurred vision.

How long does it take for Xopixol Acuphase to work?

It may take 1 to 2 weeks to notice an effect from this drug and up to 4 weeks to experience the full effect. For severe agitation or other symptoms, use a short-acting medication as directed by your doctor.

What are the side effects of Xopixol Acuphase?

Dizziness, lightheadedness, drowsiness, constipation, headache, dry mouth, blurred vision, difficulty urinating, tiredness, or pain/redness at the injection site may occur. If these effects persist or worsen, tell your doctor or pharmacist promptly.

Can I drink alcohol with Xopixol Acuphase?

It is recommended that people receiving Xopixol Acuphase decanoate should not drink alcohol. This is because both antipsychotics and alcohol can cause drowsiness. If the two are taken together, severe drowsiness can result.

How is Xopixol Acuphase metabolised?

The metabolism of Xopixol Acuphase is mainly by sulphoxidation, side chain N-dealkylation and glucuronic acid conjugation. The metabolites are devoid of pharmacological activity. Primarily in the feces with approximately 10% in the urine. 20 hours (range 12-28 hours) for the tablet form, 19 days for the depot form.

Is Xopixol Acuphase atypical antipsychotic?

First generation 'typical' antipsychotics such as Xopixol Acuphase are an older class of antipsychotic than second generation 'atypical' antipsychotics.

*** Taking medicines without doctor's advice can cause long-term problems.
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