Arkazine

Arkazine Tablet

Arkazine is one of the phenothiazine class of compounds and as such has many pharmacodynamic effects which relate to its therapeutic actions and side effects. The most notable action of phenothiazines is antagonism at dopamine receptors in the CNS. It is hypothesised that this action in the limbic system and associated areas of cerebral cortex is the basis of the antipsychotic action of phenothiazines, whilst in the medullary chemoreceptor trigger zone it appears to be responsible for the antiemetic effect of these agents.

Arkazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Arkazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.

Arkazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Arkazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.

Uses

Anxiety states: It controls excessive anxiety, tension, and agitation seen in neuroses or associated with somatic conditions. The treatment or prevention of nausea and vomiting of various causes. The management of psychotic disorders, such as acute or chronic catatonic, hebephrenic and paranoid schizophrenia; psychosis due to organic brain damage, toxic psychosis, and the manic phase of manic-depressive illness.

Arkazine is also used to associated treatment for these conditions: Agitation, Psychosis, Schizophrenia, Acute non-psychotic Anxiety

How Arkazine works

Arkazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.

Arkazine

Trade Name Arkazine
Availability Prescription only
Generic Trifluoperazine
Trifluoperazine Other Names Trifluoperazina, Trifluoperazine, Trifluopérazine, Trifluoperazinum, Trifluoroperazine, Trifluperazine
Related Drugs escitalopram, alprazolam, duloxetine, Lexapro, Xanax, quetiapine, Abilify, Cymbalta, Seroquel, aripiprazole
Type Tablet
Formula C21H24F3N3S
Weight Average: 407.496
Monoisotopic: 407.164303088
Groups Approved, Investigational
Therapeutic Class Phenothiazine drugs
Manufacturer Rkg Pharma Pvt Ltd
Available Country India
Last Updated: June 7, 2022 at 8:52 pm

Structure

Arkazine
Trifluoperazine Structure

Dosage

Arkazine dosage

Schizophrenia and other psychoses:

  • Adults and child over 12 years: Recommended starting dose is 2-5 mg b.i.d, increased by 5 mg daily after 1 week then at interval of 3 days, according to response.
  • Children (6-12 years): Dosage should be adjusted to the weight of the child and severity of the symptoms. The starting dosage is 1 mg b.i.d. Dosage may be increased gradually until symptoms are controlled or until side effects become troublesome. While it is usually not necessary to exceed dosages of 15 mg daily.
  • Elderly: Reduce initial dose by at least half

Short-term management of severe anxiety:

  • Adult and child over 12 years: 1-2 mg b.i.d, increased if necessary to 6 mg daily.
  • Child (3-5 years): 1 mg daily
  • Child (6-12 years): Up to 4 mg daily in divided dose.
  • Elderly: Reduce initial dose by at least half

Antiemetic:

  • Adult: 2-4 mg daily in divided doses; max. 6 mg daily;
  • Child 3-5 years: up to 1 mg daily, 6-12 years up to 4 mg daily.

Side Effects

Common side effects are transient restlessness, dystonias or may resemble parkinsonism. Other CNS Reactions are drowsiness, dizziness, fatigue, blurred vision, seizures. Without these Peripheral oedema, blood dyscrasias, jaundice may occasionally occur. Tachycardia, constipation, urinary hesitancy and retention and hyperpyrexia have been reported very rarely.

Toxicity

Symptoms of overdose include agitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, and restlessness.

Precaution

Care should be taken when treating elderly patients, and initial dosage should be reduced. Such patients can be specially sensitive, particularly to extra pyramidal and hypotensive effects. Patients with cardiovascular disease including arrhythmias should also be treated with caution. Care should be taken in patients with angina pectoris.

Interaction

Arkazine may diminish the effect of oral anticoagulants. Concomitant administration of propranolol with trifluoperazine results in increased plasma levels of both drugs. Antihypertensive effects of guanethidine and related compounds may be counteracted when phenothiazines are used concurrently. Potentiation may occur if antipsychotic drugs are combined with CNS depressants such as alcohol. hypnotics and anticonvulsant.

Food Interaction

  • Avoid excessive or chronic alcohol consumption. Ingesting alcohol may potentiate the sedative and CNS depressant effects of trifluoperazine.

Arkazine Alcohol interaction

[Moderate] GENERALLY AVOID:

Concurrent use of ethanol and phenothiazines may result in additive CNS depression and psychomotor impairment.

Also, ethanol may precipitate dystonic reactions in patients who are taking phenothiazines.

The two drugs probably act on different sites in the brain, although the exact mechanism of the interaction is not known.



Patients should be advised to avoid alcohol during phenothiazine therapy.

Arkazine Drug Interaction

Major: escitalopram, topiramate

Moderate: aripiprazole, amphetamine / dextroamphetamine, duloxetine, clonazepam, lamotrigine, lurasidone, lithium, pregabalin, metoprolol, brexpiprazole, quetiapine, valproic acid

Unknown: aspirin, acetaminophen, vortioxetine, multivitamin, ascorbic acid, cholecalciferol

Arkazine Disease Interaction

Major: dementia, acute alcohol intoxication, cardiovascular disease, CNS depression, head injury, liver damage

Moderate: anticholinergic effects, breast cancer, dystonic reactions, hematologic toxicity, NMS, parkinsonism, renal dysfunction, respiratory disorders, seizure disorders, tardive dyskinesia

Half Life

10-20 hours

Pregnancy & Breastfeeding use

Pregnancy: Safety for the use of trifluoperazine during pregnancy has not been established. Therefore, it is not recommended that the drug be given to pregnant patients except when, in the judgement of the physician, it is essential. The potential benefits should clearly outweigh possible hazards. There are reported instances of prolonged jaundices, extrapyramidal signs, hyperreflexia or hypoflexia in newborn infants whose mother received phenothiazines. 

Lactation: Adequate human data are not available in case of lactation.

Contraindication

Do not use Arkazine in comatose patients, or in those with existing blood dyscrasias or known liver damage, or in those hypersensitive to the active ingredient or related compounds.

Acute Overdose

Signs and symptoms will be predominantly extrapyramidal; hypotension may occur. Treatment consists of gastric lavage together with supportive and symptomatic measures. Do not induce vomiting. Extra pyramidal symptoms may be treated with an anticholinergic, antiparkinsonism drug. Treat hypotension with fluid replacement; if severe or persistent. nor adrenaline may be considered. Adrenaline is contraindicated.

Storage Condition

It should be store at room temperature between 15-30° C away from light and moisture.

Innovators Monograph

Arkazine contains Trifluoperazine see full prescribing information from innovator Arkazine Monograph, Arkazine MSDS, Arkazine FDA label

FAQ

What is Arkazine used for?

Arkazine is used to treat the symptoms of schizophrenia (a mental illness that causes disturbed or unusual thinking, loss of interest in life, and strong or inappropriate emotions).It is also used on a short-term basis to treat anxiety in people who have not been helped by other medications.

How safe is Arkazine?

This is the most serious warning from the Food and Drug Administration. A black box warning alerts doctors and patients about drug effects that may be dangerous.Arkazine can increase the risk of death in seniors with dementia-related psychosis.

What are the common side effects of Arkazine?

Arkazine may cause side effects are include.

  • dizziness, feeling unsteady, or having trouble keeping your balance
  • blurred vision
  • dry mouth
  • stuffed nose
  • nausea
  • difficulty urinating
  • widening or narrowing of the pupils (black circles in the middle of the eyes)
  • constipation
  • changes in appetite
  • weight gain
  • blank facial expression
  • shuffling walk
  • agitation
  • jitteriness
  • unusual, slowed, or uncontrollable movements of any part of the body
  • difficulty falling asleep or staying asleep
  • headache
  • extreme tiredness
  • weakness
  • breast enlargement
  • breast milk production
  • missed menstrual periods
  • decreased sexual ability in men

Is Arkazine safe during pregnancy?

Not formally assigned to a pregnancy category. Risk Summary: Neonates exposed during the third trimester are at risk of developing severe and prolonged side effects.

Is Arkazine safe during breastfeeding?

A safety scoring system finds Arkazine to be not recommended during breastfeeding.Because there is little published experience with Arkazine during breastfeeding, other antipsychotic agents may be preferred, especially wile nursing an newborn or preterm infant.

Can I take alcohol with Arkazine?

Don't take Arkazine with alcohol, as it may increase side effects of Arkazine like drowsiness, dizziness and fatigue.

Can I drive after taking Arkazine?

Avoid driving or hazardous activity until you know how Arkazine will affect you. Dizziness or drowsiness can cause falls, accidents, or severe injuries. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.

How long does it take for Arkazine to work?

Although you may notice some medication effects soon after starting, It may take 2 to 3 weeks before you get the full benefit of this drug.

Does Arkazine cause weight gain?

Arkazine is known to cause a range of adverse reactions including sedation and weight gain, but to a degree far less than other antipsychotics. Other adverse effects include postural hypotension, constipation, parkinsonism, priapism, and sexual dysfunction.

Does Arkazine make me sleepy?

Dizziness or drowsiness can cause falls, accidents, or severe injuries. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Avoid drinking alcohol. Avoid exposure to sunlight or tanning beds

Is Arkazine an antipsychotic?

Arkazine is in a group of medications called conventional antipsychotics.

How to use Arkazine?

Take Arkazine by mouth with or without food, usually once or twice daily or as directed by your doctor.

What is the half life of Arkazine?

The elimination of Arkazine from the blood is multiphasic with an α phase elimination half-life of about 3.6 hours and a terminal elimination half-life of about 22 hours.

Does Arkazine help with anxiety?

Clinical studies indicate that Arkazine produced clinically satisfactory improve- ment in the majority of patients suffering predominantly from anxiety; most of them were treated with only 0.5 mg. or less per day. Studies so far revealed minimal incidence of side effects.

How long does Arkazine stay in my system?

Arkazine has a half‐life of 6.8 to 9.6 days following IM administration.

How does Arkazine work in the body?

It works by affecting the balance of natural chemicals (neurotransmitters) in the brain.

How do I stop taking Arkazine?

Do not stop using Arkazine suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to safely stop using this medicine. Store at room temperature away from moisture, heat, and light.

What happen if I overdose on Arkazine?

If an overdose occurs call your doctor.You may need urgent medical care.