Psynor

Psynor

chlorpromazine

Manufacturer:

Swiss Pharma

Distributor:

PHARMASIA
Full Prescribing Info
Contents
Chlorpromazine hydrochloride.
Description
Each film-coated tablet contains Chlorpromazine, USP 100 mg or 200 mg.
Action
Pharmacology: Pharmacodynamics: Mechanism of Actions: Chlorpromazine is readily absorbed from the gastro-intestinal tract but is subject to considerable first-pass metabolism in the gut wall. It is also extensively metabolized in the liver and is excreted in the urine and faeces in the form of numerous active and inactive metabolites; there is evidence of enterohepatic recycling. Owing to the first-pass effect, plasma concentrations following oral administration are much lower than those following intramuscular administration. Moreover, there is very wide intersubject variation in plasma concentrations of Chlorpromazine and its metabolites, and their therapeutic effect. Patch of metabolism of Chlorpromazine include hydroxylation and conjugation with glucuronic acid, N-oxidation, oxidation of a sulfur atom, and dealkylation. Although the plasma half-life of Chlorpromazine has been reported to be only a few hours, it has a very prolonged terminal elimination phase of up to about 3 weeks. Its duration of therapeutic effect can range from a few days to several weeks or possibly longer.
Chlorpromazine is very extensively bound to plasma proteins. It is widely distributed in the body and crosses the bloodbrain barrier to achieve higher concentrations in the brain than in the plasma. Chlorpromazine and its metabolites also cross the placental barrier and excreted in milk (see Precautions).
A review of the literature on the absorption and fate of Chlorpromazine; blood and urinary studies by and large favour a fairly short sojourn of the bulk of Chlorpromazine in the body. For the blood studies, this is in the range of 2 to 3 days, and for urinary studies up to about 18 days. There is no doubt, however, that Chlorpromazine brings about changes that can persist much longer than this, after drug discontinuation. The exact relationship of persisting therapeutic effects to administered Chlorpromazine is uncertain. There is the possibility that minute amounts of Chlorpromazine and/or metabolites persist at active sites in slowly reversible or relatively irreversible ways. It also seems that some Chlorpromazine is stored in adipose tissue and slowly mobilized after stopping Chlorpromazine administration.
Indications/Uses
General Medicine: Excessive anxiety, tension and agitation as seen in neurosis. Nausea, vomiting, and intractable hiccups. Cancer and severe pain to reduce apprehension, suffering and to reduce narcotic requirements; to control nausea and vomiting. Alcohol withdrawal in hospitalized patients or those who can be kept under similar, close supervision, for agitation, delirium tremens, nausea and vomiting.
Surgery: To control nausea and vomiting, restlessness and apprehension prior to surgery.
Porphyria: For the control of acute intermittent porphyria.
Tetanus: As an adjunct in the treatment of tetanus.
Psychiatry: For the management of the manifestations of psychotic disorders. For control of involutional melancholia or of the manifestations of manic-depressive illness (manic phase). For control of moderate to severe agitation, hyperacidity or aggressiveness in disturbed children.
Dosage/Direction for Use
Adjust dosage to individual and the severity of condition. It is important to increase dosage until symptoms are controlled. Dosage should be increased more gradually in elderly and emaciated patients. In continued therapy, gradually reduce dosage to the lowest effective maintenance level.
General Medicine: Adults: Excessive Anxiety, Tension and Agitation: 10 mg 3 or 4 times a day or 25 mg 2 or 3 times a day.
More Severe Cases: 25 mg 3 times a day. After 1 or 2 days, daily dosage may be increased by 20-50 mg semi-weekly, until patient becomes calm and cooperative. (Maximum improvement may not be seen for weeks or even months).
Continue optimum dosage for 2 weeks; then gradually reduce to maintenance level. Daily dosage of 200 mg is not usual.
Some patients require higher dosages (e.g. 800 mg daily is not uncommon in discharged mental patients).
Nausea and Vomiting: 10-25 mg every 4-6 hours.
Intractable Hiccups: 25-50 mg 3 or 4 times a day.
Alcohol Withdrawal: Agitated but Manageable: 50 mg followed by 25-50 mg 3 times a day.
Ambulatory patients with withdrawal symptoms: 10 mg 3 or 4 times a day; or 25 mg 2 or 3 times a day.
Children: Nausea and Vomiting: Chlorpromazine should not be used in conditions for which specific children's dosages have not been established. Oral: 1/4 mg/lb body weight every 4-6 hours.
Surgery: Adults: Preoperative: 25-50 mg, 2-3 hours before the operation.
Children: Preoperative: 1/4 mg/lb body weight, 2-3 hours before operation.
Psychiatry: Adults: Office Patients or Outpatients: 10 mg 3 or 4 times a day or 25 mg 2 or 3 times a day.
More Severe Cases: 25 mg 3 times a day. After 1 or 2 days, daily dosage may be increased by 20-50 mg at semi-weekly intervals until patient becomes calm and cooperative.
Hospitalized Patients: Less Acutely Agitated: 25 mg 3 times a day. Increase gradually until effective dose is reached, usually 400 mg daily.
Children: Office Patients or Outpatients: 1/4 mg/lb body weight every 4-6 hours, if necessary.
Hospitalized Patients: Start with low doses and increase dosage gradually. In severe personality and behavior disorders or psychotic conditions, higher dosages (50-100 mg daily, and in older children, 200 mg daily or more) may be necessary or as prescribed by the physician.
Overdosage
Symptoms: 1 of 3 clinical pictures may be seen: Extreme Somnolence: Patient can usually be roused with prodding, but if permitted will fall asleep. General condition is usually satisfactory, skin, though pale, is warm and dry. Slight blood pressure, respiratory and pulse changes may occur but are not problems.
Mild to moderate drop in blood pressure (whether conscious or unconscious). Skin is markedly gray but warm and dry. Nail beds are pink. Respiration is slow and regular. Pulse is strong but rate slightly increased.
Severe hypotension, possibly accompanied by weakness, cyanosis, perspiration, rapid thready pulse and respiratory depression.
Treatment: Essentially symptomatic and supportive. Early gastric lavage and intestinal purges may help. Centrally-acting emetics will not help because of the antiemetic effect of Chlorpromazine. Severe hypotension usually responds to measures described under hypotensive effects. Additional measures include pressure bandages to lower limbs, oxygen, and IV fluids. If stimulant is desired, use amphetamine, dextroamphetamine, or caffeine and sodium benzoate.
Avoid stimulants that may cause convulsions (eg, picrotoxin and pentylenetetrazol).
Limited experience with dialysis indicates that it is not helpful.
Contraindications
Comatose states, presence of large amounts of CNS depressants (alcohol, barbiturates, narcotics, etc) and in the presence of bone marrow depression.
Special Precautions
Patients who have demonstrated a hypersensitivity reaction should not be re-exposed to any phenothiazine, including Chlorpromazine, unless in the judgment of the physician, the potential benefits of treatment outweight the possible hazard. Chlorpromazine should be administered cautiously to patients with cardiovascular or liver disease. Because of its CNS depressant effect, it should be used with caution in patients with chronic respiratory disorders e.g. severe asthma, emphysema and acute respiratory infections, particularly in children. Use with caution in persons who will be exposed to extreme heat organophosphorus insecticides, and in persons receiving atropine or related drugs. The use of Chlorpromazine during pregnancy has not been established.
Adverse Reactions
Drowsiness, usually mild to moderate, may occur, particularly during the first or second week, after which, it generally disappears. If troublesome, lower dosage or administer small amounts of dextroamphetamine.
Jaundice: Overall incidence has been low, regardless of indication or dosage. Most investigators conclude that it is a sensitivity reaction.
Agranulocytosis: Observe patients regularly for sudden appearance of sore throat or other signs of infection. If white blood counts and differential smears indicate cellular depression, stop treatment and start antibiotic and other suitable therapy.
EKG Changes: Particularly nonspecific, usually reversible Q and T-wave distortions have been observed in some patients. Their relationship to myocardial damage has not been confirmed.
CNS Effects: Neuromuscular extrapyramidal reactions, closely resembling parkinsonism and motor restlessness have occurred most frequently in psychiatric patients receiving high dosages.
Behavioral Effects: Psychotic symptoms and catatonic-like states have been reported rarely.
Persistent Abnormal Movements: Persistent dyskinesia, most commonly involving the face, tongue and jaw. These phenomena have been reported most frequently in elderly patients with organic brain damage.
Endocrine Disorders: Lactation and moderate breast engorgement may occur in females on large doses. If persistent, lower dosage or withdraw the drug. Amenorrhea, gynecomastia, hyperglycemia and glycosuria have been reported.
Autonomic Reactions: Occasional dry mouth, nasal congestion, constipation, adynamic ileus, miosis and mydriasis.
Special Considerations in Long-Term Therapy: Skin pigmentation and ocular changes have occurred in some patients.
Drug Interactions
The use of alcohol with Chlorpromazine should be avoided due to possible additive effects and hypotension. Chlorpromazine may counteract the antihypertensive effect of guanethidine and related compounds. Chlorpromazine prolongs and intensifies the action of CNS depressants, eg anesthetics, barbiturates and narcotics. When Chlorpromazine is administered concomitantly, about 1/4 to 1 /2, the usual dosage of such agents is required. When Chlorpromazine is not being administered for potentiation, it is best to stop such depressants before starting Chlorpromazine treatment. These agents may subsequently be reinstated at low doses and increased as needed.
Note: Chlorpromazine does not intensify the anticonvulsant action of barbiturates. Therefore, dosage of anticonvulsants, including barbiturates should not be reduced if Chlorpromazine is started. Instead, start Chlorpromazine at low doses and increase as needed.
Storage
Store at temperature not exceeding 30°C. Protect from light.
MIMS Class
ATC Classification
N05AA01 - chlorpromazine ; Belongs to the class of phenothiazine antipsychotics with aliphatic side-chain.
Presentation/Packing
Tab 100 mg x 100's. 200 mg x 100's.
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