Zycloran

Zycloran

chlorpromazine

Manufacturer:

Shandong Xier Kangtai

Distributor:

JF Draf
Full Prescribing Info
Contents
Chlorpromazine hydrochloride.
Description
Each tablet contains Chlorpromazine (as hydrochloride) 100 mg or 200 mg.
Action
Pharmacology: Pharmacodynamics: Chlorpromazine has depressant actions on the Central Nervous System, with alpha-adrenergic blocking and anticholinergic activities. It inhibits Dopamine and Prolactin release-inhibitor factor, thus stimulating the release of Prolactin. It increases the turnover of Dopamine in the brain.
It has anti-emetic, anti-pruritic, serotonin-blocking and weak anti-histamine properties and slight ganglion blocking activity. It inhibits the heat regulating centre in the brain, and is analgesic and can relax skeletal muscle.
Due to its action on the autonomic system it produces vasodilatation, hypotension and tachycardia.
Salivary and gastric secretions are reduced.
Pharmacokinetics: Chlorpromazine is readily absorbed in the gastro-intestinal tract. It is subject to first pass metabolism in the gut wall. It is extensively metabolised in the liver and excreted in the urine and faeces. The plasma half-life is only a few hours but it has a prolonged terminal elimination phase of up to about 3 weeks. Chlorpromazine is extensively bound to plasma proteins.
Indications/Uses
For the management of psychotic disorders including manifestations of manic depressive illness.
For the management of schizophrenia.
To control nausea and vomiting.
For relief of severe hiccups and acute intermittent porphyria.
As an adjunct in the treatment of tetanus.
Dosage/Direction for Use
Adults: Oral: In most patients oral treatment may be used from the start, commencing with a dosage of 25 to 50 mg three times daily and increasing as necessary: daily doses of 75 mg may be given as a single dose at night. In some patients doses of 10 mg three times daily may be adequate. Maintenance doses, when required usually range from 25 to 100 mg three times daily, although psychotic patients may require daily doses of up to 1 g or more. Doses of 10 to 25 mg every 4 to 6 hours are recommended for control of nausea and vomiting.
Initial doses of Zycloran of one-third to one-half the normal adult dose have been recommended for elderly and debilitated patients; doses should be increased more gradually.
Children: Oral: Ages 1-5 years may be given in a dose of 500 μg per kg body-weight every 4 to 6 hours. For psychiatric indications the oral dose for children aged over 5 years is usually one-third to one-half of the adult dose. Daily doses should not normally exceed 40 mg for children aged 1 to 5 years or 75 mg for children over 5 years of age.
Overdosage
Symptoms: Parkinsonism, acute dystonias, somnolence, seizures, dry mouth, blurred vision, urinary retention, tachycardia, cardiac arrhythmias, hypotension, hypothermia or hyperthermia.
Treatment: Empty stomach using gastric lavage. Administer activated charcoal and a saline cathartic. Repeat activated charcoal and cathartic every 4 to 6 hrs to speed elimination. Support respiratory and cardiac functions as needed. Maintain fluid and electrolyte balance. Treat hypotension with i.v. fluids and by placing the patient in shock position. If unresponsive, dopamine may be required. Seizures may be treated with i.v. diazepam. Treat arrhythmias with phenytoin. Acute dystonic reactions may be treated with i.v. diphenhydramine, benztropine or trihexyphenidyl. Hemodialysis is ineffective. Hemoperfusion may be effective in severe cases but is usually not necessary.
Contraindications
Comatose or depressed states due to CNS depressants; blood dyscrasias; bone marrow depression; liver damage. Hypersensitivity to chlorpromazine.
Should be avoided in children or adolescents with symptoms suggestive of Reye's Syndrome. Its antiemetic effect may mask the signs and its CNS effect may be confused with the signs of Reye's Syndrome or other encephalopathies.
Warnings
The drug may impair the mental and physical ability for operating a motor vehicle or complex hazardous machinery.
Special Precautions
Should be used with extreme caution in patients who have impaired liver function, cardiovascular disease, chronic respiratory disorders, gastric ulcer, aggravation of preexisting ulcer has been reported.
Zycloran may intensify the effects of alcohol and CNS depressants. Use cautiously in patients with a history of seizures since the drug tends to lower the seizure threshold. It may impair sensitivity and adaptation to changes of environmental temperature so that fatal hyperthermia and heat stroke are possible complications.
Use In Pregnancy & Lactation
Safe use of Zycloran in pregnancy has not been established. Some side effects such as jaundice and movement disorders have occurred in a few newborns exposed to the drug during the first trimester. Therefore, they should be administered cautiously to women of childbearing potential particularly during the first trimester of pregnancy and near term.
Zycloran is distributed into milk. Use with caution during lactation because of possible sedative and anticholinergic side effects on the infant.
Adverse Reactions
Autonomic Nervous System: Blurred vision, dry mouth, constipation, ileus, nasal stuffiness, photophobia.
Cardiovascular: Hypotension can occur after oral administration. Tolerance to hypotensive effects generally develop over time, it can persist in some patients, especially the elderly.
Zycloran has peripheral alpha-adrenergic blocking activity. Its effects on the ECG include prolongation of the PR and QT intervals blunting of the T-wave and depression of the S-T segment. Ventricular arrhythmia and sudden death have occurred rarely.
CNS: Extrapyramidal reactions, including pseudoparkinsonism (with motor retardation, rigidity, drooling, tremors etc.), dystonic reactions (including perioral spasms, tics, torticollis, protrusion of the tongue etc.) and akathisia. Dizziness has been reported.
Tardive dyskinesia may appear in some patients on long term antipsychotic therapy.
Elderly patients are affected greatly, especially females. The symptoms are persistent and in some patients appear to be irreversible.
Dermatologic: Itching, skin rash, erythema, allergic purpura, exfoliative dermatitis, photosensitivity.
Endocrine: Increased prolactin secretion, gynecomastia, galactorrhea, mastalgia, altered libido, menstrual irregularities, weight gain, alterations in glucose tolerance and false positive pregnancy tests have occurred.
Gastrointestinal: Nausea, vomiting, increase or decrease in appetite, gastric irritation, constipation, paralytic ileus, rarely diarrhea.
Genitourinary: Urinary retention, priapism, inhibition of ejaculation.
Hematologic: Agranulocytosis, leukopenia, granulocytopenia, eosinophilia, thrombocytopenia, anemia, aplastic anemia, pancytopenia. Agranulocytosis occurs in fewer than 1 in 10,000 patients.
Hepatic: Jaundice usually occurs within 2 to 4 weeks of initiation of therapy and should be discontinued immediately. Rarely progression to chronic jaundice has occurred. Pre-existing liver dysfunction has not yet been proven to be a risk factor for this reaction. Signs and symptoms of cholestatic jaundice include upper abdominal pain, nausea, flu-like symptoms, yellow skin and conjunctiva, fever, elevated liver enzymes, biliuria.
Ophthalmologic: Pigmentation of areas of conjunctiva and/or discoloration of the exposed sclera and cornea. Patients receiving higher dose for prolonged periods should have periodic complete eye examinations.
Drug Interactions
Combinations contraindicated: Dopaminergics (quinagolide, cabergoline), not including dopaminergic antiparkinsonism agents, are contraindicated: reciprocal antagonism of the dopaminergic agent and neuroleptic.
Combinations not recommended: Dopaminergic antiparkinsonism agents (amantadine, bromocriptine, cabergoline, levodopa, lisuride, pergolide, piribedil, ropinirole) are not recommended: reciprocal antagonism of the antiparkinsonism agent and neuroleptic. Neuroleptic-induced extrapyramidal syndrome should be treated with an anticholinergic rather than a dopaminergic antiparkinsonism agent (dopaminergic receptors blocked by neuroleptics).
Levodopa: reciprocal antagonism of levodopa and the neuroleptic. In Parkinson's patients, it is recommended to use the minimal doses of each drug.
QT prolonging drugs: there is an increased risk of arrhythmias when chlorpromazine is used with concomitant QT prolonging drugs (including certain antiarrhythmics and other antipsychotics including sultopride) and drugs causing electrolyte imbalance.
Alcohol: alcohol potentiates the sedative effect of neuroleptics. Changes in alertness can make it dangerous to drive or operate machinery. Alcoholic beverages and medication containing alcohol should be avoided.
Lithium (high doses of neuroleptics): concomitant use can cause confusional syndrome, hypertonia and hyperreflexivity, occasionally with a rapid increase in serum concentrations of lithium.
Combinations requiring precautions: Antidiabetic agents: concomitant administration of high chlorpromazine doses (100 mg/day), and antidiabetic agents can lead to an increase in blood sugar levels (decreased insulin release). Forewarn the patient and advise increased self-monitoring of blood and urine levels. If necessary, adjust the antidiabetic dosage during and after discontinuing neuroleptic treatment.
Topical gastrointestinal agents (magnesium, aluminium and calcium salts, oxides and hydroxides): decreased GI absorption of phenothiazine neuroleptics. Do not administer phenothiazine neuroleptics simultaneously with topical GI agents (administer more than 2 hours apart if possible).
Combinations to be taken into consideration: Antihypertensive agents: potentiation of the antihypertensive effecte and risk of orthostatic hypotension (additive effects). Phenothiazines enhance the hypotensive effect of anaesthetics and calcium channel blockers. Severe postural hypotension may occur with concomitant administration of chlorpromazine and ACE inhibitors.
Storage
Store at temperatures not exceeding 30°C.
Protect from light.
MIMS Class
Antipsychotics
ATC Classification
N05AA01 - chlorpromazine ; Belongs to the class of phenothiazine antipsychotics with aliphatic side-chain.
Presentation/Packing
Tab 100 mg (white, circular film coated) x 100's. 200 mg (white, circular film coated and scored on one side) x 100's.
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