STEMETIL SUPPOSITORY

Kanada - anglų - Health Canada

Nusipirk tai dabar

Prekės savybės Prekės savybės (SPC)

02-11-2006

Veiklioji medžiaga:
PROCHLORPERAZINE
Prieinama:
SANOFI-AVENTIS CANADA INC
ATC kodas:
N05AB04
INN (Tarptautinis Pavadinimas):
PROCHLORPERAZINE
Dozė:
10MG
Vaisto forma:
SUPPOSITORY
Sudėtis:
PROCHLORPERAZINE 10MG
Vartojimo būdas:
RECTAL
Vienetai pakuotėje:
10
Recepto tipas:
Prescription
Gydymo sritis:
PHENOTHIAZINES
Produkto santrauka:
Active ingredient group (AIG) number: 0106181001; AHFS: 28:16.08.24
Autorizacija statusas:
APPROVED
Registracijos numeris:
01927795
Leidimo data:
2006-05-30

Page 1 of 19

PRODUCT MONOGRAPH

STEMETIL

®

Prochlorperazine mesylate injection

10 mg/2 mL prochlorperazine as prochlorperazine mesylate

Prochlorperazine Suppositories

10 mg

Antipsychotic - Antiemetic

sanofi-aventis Canada Inc.

Revision Date:

2150 St. Elzear Blvd. West

October 13, 2006

Laval, Quebec H7L 4A8

Submission Control No.: 107337

s-a version 3.0 dated

Page 2 of 19

PRODUCT MONOGRAPH

NAME OF DRUG

Stemetil

Prochlorperazine mesylate injection

Prochlorperazine Suppositories

THERAPEUTIC CLASSIFICATION

Antipsychotic - Antiemetic

ACTION

Stemetil

(prochlorperazine)

piperazine

phenothiazine

derivative

with

antipsychotic,

antiemetic and weak sedative activity.

Stemetil has actions similar to those of other phenothiazine derivatives but appears to be less

sedating and to have a weak propensity for causing hypotension or potentiating the effects of

CNS depressants and anesthetics. However, it produces a high incidence of extrapyramidal

reactions.

INDICATIONS

Stemetil (prochlorperazine) is indicated in the management of manifestations of psychotic

disorders such as agitation, confusion, delusion, tension and anxiety.

It is also effective in controlling nausea and vomiting due to stimulation of the chemoreceptor

trigger zone.

In selected patients, Stemetil may be of value for the relief of excessive anxiety, accompanied by

severe tension and agitation, associated with psychoneurotic or somatic conditions.

Page 3 of 19

CONTRAINDICATIONS

Stemetil (prochlorperazine) should not be administered in the presence of circulatory collapse,

altered states of consciousness or comatose states, particularly when these are due to intoxication

with

central depressant drugs (alcohol, hypnotics,

narcotics, etc.). It is contraindicated in

severely

depressed

patients,

presence

blood

dyscrasias,

liver

disease,

renal

insufficiency, pheochromocytoma, or in patients with severe cardiovascular disorders or a

history of hypersensitivity to phenothiazine derivatives.

with

other

phenothiazines,

Stemetil

contraindicated

patients

with

suspected

established

subcortical

brain

damage,

with

without

hypothalamic

damage,

since

hyperthermic reaction with temperatures above 40

C may occur, sometimes not until 14 to 16

hours after drug administration.

Phenothiazine compounds should not be used in patients receiving large doses of hypnotics, due

to the possibility of potentiation.

Stemetil is contraindicated in children undergoing surgery.

WARNINGS

The antiemetic action of Stemetil (prochlorperazine) may mask the signs and symptoms of

overdosage of other drugs and may obscure the diagnosis and treatment of other conditions such

as brain tumor or intestinal obstruction. Therefore the etiology of nausea and vomiting should be

established before using the drug.

The use of this drug may impair the mental and physical abilities required for the performance of

potentially hazardous tasks, such as driving a car or operating machinery. Potentiation of the

effects of alcohol may also occur.

As with other neuroleptics, very rare cases of QT interval prolongation have been reported with

Stemetil. Neuroleptic phenothiazines may potentiate QT interval prolongation, which increases

the risk of onset of serious ventricular arrhythmias of the torsade de pointes type, which is

potentially fatal (sudden death). QT prolongation is exacerbated, in particular, in the presence of

bradycardia, hypokalemia, and congenital or acquired (i.e., drug induced) QT prolongation. If the

clinical situation permits, medical and laboratory evaluations should be performed to rule out

possible risk factors before initiating treatment with a neuroleptic agent and as deemed necessary

during treatment (See also PRECAUTIONS and ADVERSE REACTIONS).

Page 4 of 19

Tardive Dyskinesia: As with all antipsychotic agents, tardive dyskinesia may appear in some

patients

long-term

therapy

after

drug

discontinuation.

syndrome

mainly

characterized by rhythmical involuntary movements of the tongue, face, mouth or jaw. The

manifestations may be permanent in some patients. The syndrome may be masked when

treatment is reinstituted, when the dosage is increased or when a switch is made to a different

antipsychotic drug. Stemetil should be prescribed in a manner that is most likely to minimize the

risk of tardive dyskinesia. The lowest effective dose and the shortest duration of treatment should

be used, and treatment should be discontinued at the earliest opportunity, or if a satisfactory

response cannot be obtained. If the signs and symptoms of tardive dyskinesia appear during

treatment, discontinuation of Stemetil should be considered.

Neuroleptic

Malignant

Syndrome:

Neuroleptic

malignant

syndrome

(NMS)

occur

patients receiving antipsychotic drugs. NMS is characterized by hyperthermia, muscle rigidity,

altered consciousness, and signs of autonomic instability including irregular blood pressure,

tachycardia, cardiac arrhythmias and diaphoresis. Additional signs may include elevated serum

creatine

kinase,

myoglobinuria

(rhabdomyolysis),

acute

renal

failure

leukocytosis.

Hyperthermia is often an early sign of this syndrome. Antipsychotic treatment should be

withdrawn immediately and appropriate supportive therapy and careful monitoring instituted.

Use in pregnancy: Safety for the use of Stemetil (prochlorperazine) during pregnancy has not

been established. Therefore, it is recommended that the drug be given to pregnant patients only

when, in the judgement of the physician, the potential benefit to the patient outweighs the

possible risk to the fetus.

Use in children: The drug should not be used in children under 2 years unless potentially life-

saving.

The extrapyramidal symptoms which can occur secondary to Stemetil may be confused with the

central nervous system signs of an undiagnosed primary disease responsible for the vomiting,

e.g. Reye’s syndrome or other encephalopathy. The use of prochlorperazine should be avoided in

children and adolescents whose signs and symptoms suggest Reye’s syndrome.

PRECAUTIONS

increased

incidence

seizures,

which

occasionally

occur

epileptics

started

antipsychotic medication, may be controlled by increasing the dosage of their anticonvulsant.

Patients with a familial history of seizures or febrile convulsions are more likely to develop

seizures than those who have no such history.

Page 5 of 19

Phenothiazines may increase the effects of general anesthetics, opiates, barbiturates, and other

CNS depressants and the doses of these drugs should be reduced if administered concomitantly

with Stemetil (prochlorperazine).

On long-term therapy, particularly during the first two or three months, it is advisable to perform

periodic liver function tests and blood counts as cholestatic jaundice and blood dyscrasias may

occur, necessitating discontinuation of treatment. Renal function should be monitored and, if

BUN (blood urea nitrogen) becomes abnormal, treatment should be discontinued.

To lessen the likelihood of adverse reactions related to drug accumulation, patients on long-term

therapy, particularly on high doses, should be evaluated periodically to decide whether the

maintenance dosage could be lowered or drug therapy discontinued.

Because of its anticholinergic action, Stemetil should be used with great caution in patients with

glaucoma or prostatic hypertrophy.

The effects of anticholinergic drugs may be potentiated by prochlorperazine. Paralytic ileus, even

resulting

death,

occur,

especially

elderly.

Caution

should

observed

constipation develops.

Retinal changes, lenticular and corneal deposits and abnormal skin pigmentation have been

observed with other phenothiazines and may occur after prolonged therapy. The possibility of

persistent tardive dyskinesia should also be borne in mind when patients are under long-term

treatment.

Patients receiving prochlorperazine should be cautioned against exposure to extreme heat or

organophosphorous insecticides.

False positive or negative pregnancy tests have occurred in patients receiving phenothiazine

therapy.

Hypotension and electrocardiographic changes, particularly non-specific and usually reversible

Q and T wave distortions, have been associated with the administration of phenothiazines.

Therefore,

prochlorperazine

should

used

with

caution

patients

with

compensated

cardiovascular and cerebrovascular disorders.

Neuroleptic

phenothiazines

potentiate

interval

prolongation.

prolongation

exacerbated, in particular, in the presence of bradycardia, hypokalemia, and congenital or

acquired

(i.e.,

drug

induced)

prolongation.

(See

also

WARNINGS

ADVERSE

REACTIONS.)

Page 6 of 19

Unexpected, sudden deaths have occurred in hospitalized patients treated with phenothiazines.

Previous brain damage or seizures may predispose. High doses should be avoided in known

seizure patients. Sudden exacerbations of psychotic behavior patterns occurred in several patients

shortly before death. Acute fulminating pneumonia or pneumonitis and aspiration of gastric

contents also were observed. Therefore, the physician also should keep in mind the possible

development of “silent pneumonias”.

Neuroleptic drugs elevate prolactin levels; the elevation persists during chronic administration.

Tissue culture experiments indicate that approximately one-third of human breast cancers are

prolactin-dependent in vitro, a factor of potential importance if the prescription of these drugs is

contemplated in a patient with a previously detected breast cancer. Although disturbances such

as galactorrhea, amenorrhea, gynecomastia and impotence have been reported, the clinical

significance of elevated serum prolactin levels is unknown for most patients. An increase in

mammary neoplasms has been found in rodents after chronic administration of neuroleptic drugs.

Neither clinical studies, nor epidemiologic studies conducted to date, however, have shown an

association between chronic administration of these drugs and mammary tumorogenesis; the

available evidence is considered too limited to be conclusive at this time.

Withdrawal Emergent Neurological Signs: Abrupt withdrawal after short-term administration of

antipsychotic drugs does not generally pose problems. However, transient dyskinetic signs are

experienced by some patients on maintenance therapy after abrupt withdrawal. The signs are

very similar to those described under Tardive Dyskinesia, except for duration. Although it is not

known whether gradual withdrawal of antipsychotic drugs will decrease the incidence of

withdrawal emergent neurological signs, gradual withdrawal would appear to be advisable.

Older Patients: The incidence of adverse reactions may be greater in patients over 55 years of

age since the half-lives of antipsychotic drugs are often prolonged. To minimize this possibility,

the maintenance dosage should be reduced to the lowest effective level as soon as possible after

initial titration and periodically reviewed.

Since psychiatric syndromes in the elderly can be caused by drugs or organic disease, withdrawal

of the precipitating drug or treatment of the medical condition should supersede initiation of

antipsychotic medication. These agents should not be used for non-psychiatric conditions for

which other drugs are available, since the elderly are especially prone to develop adverse effects

from antipsychotic drugs.

Children: Children with an acute febrile illness or suffering from dehydration seem to be much

more susceptible than adults to neuromuscular reactions, particularly dystonias. In such patients,

the drug should be used under close supervision and at low doses.

Page 7 of 19

ADVERSE REACTIONS

Adverse reactions with different phenothiazines vary in type, frequency, and mechanism of

occurrence, i.e., some are dose-related, while others involve individual patient sensitivity. Some

adverse reactions may be more likely to occur with greater intensity, in patients with special

medical problems.

Not all of the following adverse reactions have been observed with every phenothiazine

derivative, but they have been reported with one or more and should be borne in mind when

drugs of this class are administered:

Neurological:

Extrapyramidal

reactions

including

tremor,

rigidity,

akathisia,

dystonia,

dyskinesia, oculogyric crises, opisthotonos, hyperreflexia and sialorrhea. EEG changes, disturbed

temperature regulation and seizures have also been encountered.

Persistent Tardive Dyskinesia: As with other antipsychotic agents, tardive dyskinesia may occur

in patients on long-term therapy or may be observed after drug therapy has been discontinued.

The risk seems to be greater in elderly patients on high doses, especially females. The symptoms

are persistent and in some patients appear to be irreversible. The syndrome is characterized by

rhythmical involuntary movements of the tongue, face, mouth or jaw (e.g., protrusion of tongue,

puffing of cheeks, puckering of mouth, chewing movements). Sometimes, these may be

accompanied by involuntary movements of the extremities.

There is no known effective treatment for tardive dyskinesia; antiparkinsonian agents usually do

not alleviate the symptoms of this syndrome. It is suggested that all antipsychotic agents be

discontinued if these symptoms appear. Should it be necessary to reinstitute treatment, or

increase the dosage of the agent, or switch to a different antipsychotic agent, the syndrome may

be masked. It has been reported that fine vermicular movements of the tongue may be an early

sign of the syndrome and, if the medication is stopped at that time, the syndrome may not

develop. The physician may be able to reduce the risk of this syndrome by minimizing the

unnecessary use of neuroleptic drugs and reducing the dose or discontinuing the drug, if possible,

when manifestations of this syndrome are recognized, particularly in patients over the age of 50.

Behavioral:

Sleep

disturbances,

drowsiness,

fatigue,

insomnia,

depression

have

been

reported and may, in severe cases, necessitate reduction in dosage. As with other phenothiazine

derivatives, reactivation or aggravation of psychotic processes may be encountered. Paradoxical

effects such as agitation, anxiety, restlessness, excitement and bizarre dreams, have been

observed.

Autonomic Nervous System: Dry mouth, nasal congestion, headache, nausea, constipation,

tachycardia,

hypotension,

syncope,

dizziness,

blurred

vision,

vomiting,

sweating,

nasal

congestion, and urinary incontinence have been observed.

Page 8 of 19

Patients with pheochromocytoma, cerebral vascular or renal insufficiency, or a severe cardiac

reserve deficiency such as mitral insufficiency appear to be particularly prone to hypotensive

reactions with phenothiazine compounds, and should therefore be observed closely when the

drug is administered. Should hypotension occur in patients receiving Stemetil (prochlorperazine)

and a vasopressor agent be required i.v. norepinephrine or phenylephrine should be used, and not

epinephrine, since phenothiazine derivatives can reverse the pressor effect of the latter drug.

Other autonomic reactions which have occurred with phenothiazines are salivation, polyuria,

glaucoma, bladder paralysis, adynamic ileus, and fecal compaction.

Metabolic and Endocrine: Anorexia, menstrual irregularities, impotence, and increased thirst,

weight changes, increased appetite, peripheral edema, galactorrhea, gynecomastia, and changes

in libido have also occurred in patients receiving phenothiazine therapy.

Allergic or Toxic: Pruritus, dermatitis, rash, erythema, urticaria, seborrhea, eczema, exfoliative

dermatitis, and photosensitivity. The possibility of an anaphylactoid reaction should be borne in

mind.

Blood dyscrasias including leukopenia, agranulocytosis, pancytopenia, thrombocytopenic or

non-

thrombocytopenic

purpura,

eosinophilia,

anemia,

have

been

associated

with

phenothiazine therapy. Routine blood counts are therefore advisable during prolonged therapy.

If any soreness of the mouth, gums or throat or any symptoms of upper respiratory infection

occur

confirmatory

leukocyte

count

indicates

cellular

depression,

therapy

should

discontinued and other appropriate measures instituted immediately.

Cholestatic jaundice and biliary stasis may be encountered, particularly during the first months of

therapy, and require immediate discontinuation of treatment.

Miscellaneous:

following

adverse

reactions

have

been

reported

patients

receiving

phenothiazine derivatives : headache, asthma, laryngeal, cerebral and angioneurotic edema,

altered cerebrospinal fluid proteins, systemic lupus erythematosus-like syndrome, hyperpyrexia,

ECG and WEG changes and hypotension severe enough to cause fatal cardiac arrest. Skin

pigmentation, epithelial keratopathy, lenticular, and corneal deposits have been associated with

long-term administration.

Very rare cases of QT interval prolongation have been reported. There have been isolated

reports

sudden

death,

with

possible

causes

cardiac

origin

(see

WARNINGS

PRECAUTIONS) as well as cases of unexplained sudden death, in patients receiving neuroleptic

phenothiazines.

Page 9 of 19

Sudden, unexpected and unexplained deaths have been reported in hospitalized psychotic

patients receiving phenothiazines. Previous brain damage or seizures may be predisposing

factors; high doses should be avoided in known seizure patients. Several patients have shown

flare-ups of psychotic behavior patterns shortly before deaths. Autopsy findings have usually

revealed

acute

fulminating

pneumonia

pneumonitis,

aspiration

gastric

contents

intramyocardial lesions.

Potentiation of CNS depressants (barbiturates, narcotics, analgesics, alcohol, antihistamines),

may occur.

SYMPTOMS AND TREATMENT OF OVERDOSAGE

Symptoms: Primarily extrapyramidal reactions, CNS depression which may vary from simple

lethargy to coma. Agitation and restlessness may also occur. Other possible manifestations

include convulsions, fever and autonomic reactions such as hypotension, dry mouth and ileus.

Treatment: Essentially symptomatic and supportive. Early gastric lavage may be helpful.

Maintain an open airway. If hypotension occurs, the standard measures for managing circulatory

shock should be initiated; if a pressor agent is required give norepinephrine or phenylephrine and

not epinephrine as it may further depress the blood pressure. Extrapyramidal reactions should be

treated with an antiparkinsonian agent.

Centrally, acting emetics will be ineffective because of prochlorperazine’s antiemetic action.

Limited experience indicates that phenothiazines are not dialyzable.

DOSAGE AND ADMINISTRATION

Begin with the lowest recommended dosage. Adjust to response of the individual.

ADULTS

Rectal route - To control nausea, vomiting or excessive anxiety : usually 5 to 10 mg, 3 or 4 times

daily; in mild cases, a single dose of 5 to 10 mg is often adequate.

Parenteral route - I.M. Dosage: The drug is given by deep intramuscular injection. Total daily

dosage rarely exceeds 40 mg, except in severe psychiatric cases. When control is achieved, the

oral route should be substituted. To control nausea, vomiting or excessive anxiety: 5 to 10 mg, 2

or 3 times a day. In psychiatry, for the immediate control of severely disturbed patients, 10 to 20

mg initially, repeated every 2 to 4 hours until control is obtained. More than 3 or 4 doses are

seldom necessary. The patients should be kept in bed and under medical supervision. In surgery :

5 to 10 mg I.M., 1 to 2 hours before anesthesia. Repeat once during surgery, if necessary. Post-

operatively, the same dose of 5 to 10 mg I.M. may be given to control acute symptoms and

Page 10 of 19

repeated, if necessary, every 3 to 4 hours (maximum, 40 mg daily).

I.V. Infusion: During and after surgery, Stemetil may be given I.V. in the infusion solution at a

concentration of 20 mg per liter. Total daily dose rarely exceeds 30 mg.

CHILDREN

Daily dosage, administered in divided doses, should be based on body weight rather than on age,

and should not be exceeded. Do not administer to children under 2 years of age or 9 kg of body

weight. Occasionally the patient may react to the drug with signs of restlessness and excitement;

if this occurs, treatment should be discontinued.

Parenteral route:

For severe nausea and vomiting, and in child psychiatry: calculate each dose on the basis of 0.13

mg/kg of body weight and give by deep I.M. injection. Control is usually obtained with one dose.

When further therapy is needed, transfer the patient to an oral form at an equal or higher dose.

Page 11 of 19

PHARMACEUTICAL INFORMATION

Drug substance

Proper name:

Prochlorperazine

Chemical name:

2-chloro-10[3-(4-methyl-1-piperazinyl)propyl]-10H-phenothiazine

Structural formula:

Molecular formula:

Molecular weight:

373.94

Physical form:

Clear, pale yellow, viscous liquid

Solubility:

Insoluble in water and freely soluble in alcohol, chloroform and ether.

Drug Substance

Proper name:

Prochlorperazine mesylate

Chemical name:

2-chloro-10[3-(4-methyl-1-piperazinyl)propyl]-10H-phenothiazine

mesylate

Structural Formula:

Molecular formula:

Molecular weight:

566.2

Physical form:

White or almost white powder

Solubility:

Very soluble in water; sparingly soluble in alcohol; slightly soluble in

chloroform; practically insoluble in ether.

2.0 to 3.0

Page 12 of 19

Composition

Injectable

: Each mL contains: prochlorperazine base 5 mg (as the mesylate). Non-medicinal

ingredients: sodium chloride, sodium citrate, sodium sulphite anhydrous and water for injection.

Suppositories

: Each rectal suppository contains: prochlorperazine base 10 mg. Non-medicinal

ingredients: hydrogenated vegetable glycerides.

Stability and storage recommendations:

Stemetil (prochlorperazine) suppositories and Stemetil (prochlorperazine mesylate) injectable

should be stored at 15

to 25

C. Protect from light.

AVAILABILITY OF DOSAGE FORMS

Stemetil (prochlorperazine base) 5 mg/mL (as mesylate) injectable is available in amber glass

ampoules of 2 mL in boxes of 10 ampoules.

Stemetil (prochlorperazine base) 10 mg suppositories are available in boxes of 10 suppositories.

PHARMACOLOGY

The pharmacologic profile of prochlorperazine in experimental animals is similar to that of other

phenothiazines. The following findings relate to animal studies in which prochlorperazine and

chlorpromazine

effects

were

compared

drug

weight

basis.

sedative

activity

prochlorperazine, based on the potentiating effects of ether anesthesia and morphine analgesia, is

approximately

half

that

chlorpromazine.

ability

prochlorperazine

block

conditioned avoidance in rats is approximately one and a half times greater than chlorpromazine.

The cataleptic effects of prochlorperazine are slightly greater than those of chlorpromazine but

both compounds appear to be equi-effective in reducing motor activity.

The antiemetic effect of prochlorperazine, determined by the apoamorphine-induced vomiting in

dogs, is four to six times greater than that of chlorpromazine. Chlorpromazine exerts more potent

adrenergic

serotonin

blocking

effects

anticholinergic

activity

than

does

prochlorperazine.

In rats, prochlorperazine administered intraperitoneally distributes in all body tissues. The liver

and spleen appear to store greater concentrations of the drug than other organs. Prochlorperazine

enters the entero-hepatic circulation and is excreted chiefly in the feces. Less than 25 % of an

intra peritoneal dose in rats is excreted in the urine.

Page 13 of 19

TOXICOLOGY

Acute Toxicity

The following LD

values have been obtained in mice for prochlorperazine.

- I.V.

- 90 mg/kg

- S.C.

- 400 mg/kg

- P.O. - 800 mg/kg

Subacute Toxicity

Administration of prochlorperazine to rats, 50 mg/kg P.O, daily for one month produced no

disturbances of liver or kidney functions and no blood or bone-marrow alterations. All the

animals survived without loss of weight, and appeared normal. Histological examination of

kidney, liver, lung, and spleen did not reveal any toxic lesions.

In the dog, daily doses of 30 mg/kg for one month produced no mortality and all the animals

appeared normal throughout treatment. They showed only a slight loss of weight, but no

disturbances of liver or kidney functions. Histological examination revealed no abnormalities.

Teratogenicity

Prochlorperazine administered to pregnant rabbits and rats at dosage levels approximately 80 to

100 times the human therapeutic dose, produced no teratogenic effects.

Page 14 of 19

REFERENCES

Baker FM, Cook P. Compazine complications; A review. J Natl Med Assoc 1981;73:409-

412.

Carter CH. Prochlorperazine in emotionally disturbed, mentally defective children. Southern

Med J

1959;52:174-8.

Courvoisier S, Ducrot R, Fournet J, Julou L. Proprietes pharmacodynamiques generales de la

prochlorpemazine (6140 R.P.). Cr Soc Biol 1957;41:1144-8.

Cubeddu LX. QT prolongation and fatal arrhythmias: a review of clinical implications and

effects of drugs. American Journal of Therapeutics 2003;10(6):452-7.

Fenichel RR, Malik M, Antzelevitch C, Sanguinetti M, Roden DM, Priori SG, et al. Drug-

induced torsades de pointes and implications for drug development. J Cardiovasc Electr

2004;15(4):475-95.

Frytak S, Moertel CG, O’Fallon JR, Rubin J, Creagan ET, O'Connell MJ, et al. Delta-9

tetrahydrocannabinol

antiemetic

for patients

receiving

cancer

chemotherapy.

comparison with prochlorperazine and a placebo. Ann Intern Med 1979;91:825-30.

Giffen MR. Emotional dysfunction and the use of psychopharmacological drugs in a military

theater. Mil Med 1961;126:199-203.

Goldberg HL, Finnerty RJ. Double-blind Study of prochlorperazine, oblordiazepoxide and

placebo

psychoneurotic

outpatients

with

dominant

symptoms

anxiety.

Pharmacopsychiat 1979;14:264-77.

Kenbubpha K, Silpakit C. Association between antipsychotics and sudden death in psychotic

in-patients. International Medical Journal 2002;9(1):27-31.

Lankamp DJ, Willemse J, Pikaar SA, van Heyst AN. Prochlorperazine in childhood : side

effects. Clin Neurol Neurosurg 1977;80:264-71.

Lapierre J, Amin M, Hattangadi S. Prochlorperazine - A review of the literature since 1956.

Can Psychiatr Assoc J 1969;14:267-74.

Loeser EA, Bennett G, Stanley TU, Machin R. Comparison of droperidol, haloperidol and

prochlorperazine as postoperative anti-emetics. Can Anaesth Soc J 1979;26:125-7.

Page 15 of 19

Mehtonen OP, Aranko K, Malkonen L, Vapaatalo H. A survey of sudden death associated

with the use of antipsycgotic or antidepressant drugs: 49 cases in Finland. Acta Psychiatr

Scand 1991;84:58-64.

Milkovich L, Van Den Berg BJ. An evaluation of the teratogenicity of certain antinauseant

drugs. Am J Obstet Gynecol 1976;125:244-8.

Peikes IL. Nausea and vomiting of pregnancy treated with a sustained-release form of

prochlorperazine. Clin Med 1957;4:1385-7.

Phillips

Miya

Disposition

S35-prochlorperazine

rat.

Pharm

1964;53:1098-101.

Ray WA, Meredith S, Thapa PB, Meador KG, Hall K, Mur

r

ay KT. Antipsychotics and the

risk of sudden cardiac death. Arch Gen Psychiat 2001;58(12):1161-7.

Reilly

Ayis

Ferrier

Jones

Thomas

SHL.

Thioridazine

sudden

unexplained death in psychiatric in-patients. Brit J Psychiat 2002;180:515-22.

Rickels

Russell

Csanalosi

Gingrich

Werblowsky

Schless

Prochlorperazine, chlordiazepoxide and placebo in anxious outpatients. Current Therapeutic

Research, Clinical & Experimental 1981;29:156-64.

Steele N, Gralla RJ, Braun DW, Young CW. Double-blind comparison of the antiemetic

effects of nabilone and prochlorperazine on chemotherapy-induced emesis. Cancer Treat Rep

1980;64:219-24.

Taylor DM. Antipsychotics and QT prolongation. Acta Psychiat Scand 2003;107(2):85-95.

Teal N. Maintenance therapy for mental patients. Postgrad Med 1958;24:638-47.

Ungerleider JT, Andrysiak T, Fairbanks L, Sarna G, Jamison K Cannabis and cancer

chemotherapy

comparison

oral

Delta-9-THC

prochlorperazine.

Cancer

1982;50:636-45.

Zeltser D, Justo D, Halkin A, Prokhorov V, Heller K, Viskin S. Torsade de pointes due to

noncardiac

drugs:

most

patients

have

easily

identifiable

risk

factors.

Medicine

2003;82(4):282-90.

IMPORTANT: PLEASE READ

Page 16 of 19

CONSUMER INFORMATION

Pr

STEMETIL

®

Prochlorperazine mesylate injection

Prochlorperazine Suppositories

This leaflet is designed specifically for Consumers. This

leaflet is a summary and will not tell you everything about

Stemetil

®

. Contact your doctor or pharmacist if you have

any questions about the drug.

ABOUT THIS MEDICATION

What the medication is used for:

Stemetil

is used to treat symptoms of psychotic disorders such

as agitation, confusion, delusion, tension and anxiety.

Stemetil

is also used for the control of nausea and vomiting.

Ask your doctor if you have any questions about why Stemetil

has been prescribed to you.

What it does:

Stemetil

helps to:

reduce and control psychotic symptoms

control nausea and vomiting

induce sleep

When it should not be used:

Do not use Stemetil

if you:

Are allergic to Stemetil

,

to phenothiazines (a type of

antipsychotic) or to any of the ingredients in the product

(see the section “

What the non-medicinal ingredients

are”

Have a sudden blood circulation failure or are in an altered

state of consciousness or coma, especially if these were

caused by alcohol or drugs

Suffer from severe depression

Have liver disease

Have a blood disorder

Have kidney problems

Have pheochromocytoma (a tumour of the adrenal gland)

Have severe heart or blood vessel disorders

Have or have had brain damage

Are taking high doses of drugs that cause you to sleep

Stemetil

is not indicated for use in children undergoing a

surgery.

What the medicinal ingredient is:

Suppositories: Prochlorperazine

Injection: Prochlorperazine

What the nonmedicinal ingredients are:

Suppositories: hydrogenated vegetable glycerides

Injection: Sodium chloride, sodium citrate, sodium sulphite

anhydrous and water for injection.

What dosage forms it comes in:

Suppositories 10 mg

Injection: 10 mg/2 mL prochlorperazine as prochlorperazine

mesylate

WARNINGS AND PRECAUTIONS

At the beginning of treatment, Stemetil

may cause some people

to become drowsy or less alert. You should not drive a car,

operate machinery or participate in activities requiring alertness

until you are sure Stemetil

does not affect you.

You should use

extra care not to be exposed to extreme heat or

some type of insecticides. Check with your doctor or pharmacist.

Children seem to be more susceptible than adult to some side

effects. Stemetil

should not be used in children under 2 years old

unless the doctor decides that Stemetil

is needed.

The incidence of adverse reactions may be greater in patients over

55 years of age. The lowest effective dose should be used to

reduce the risk of having adverse reactions.

If you experience severe constipation and you are elderly, please

consult your doctor as soon as possible.

Tardive dyskinesia, neuroleptic malignant syndrome cardiac, eye,

skin and respiratory problems may occur in some patients taking

Stemetil

(see the section

“SIDE EFFECTS AND WHAT TO

IMPORTANT: PLEASE READ

Page 17 of 19

DO ABOUT THEM”

.

Before using Stemetil

, tell your doctor if you:

Have heart or blood vessel disease

Have cerebrovascular (blood vessels of the brain) disorder

Have constipation or intestinal blockage

Have or have had a brain tumour or brain damage

Suffer from an enlarged prostate (Benign Prostatic

Hypertrophy)

Suffer from an increase pressure within the eyes

(glaucoma)

Have or have had seizure disorders (e.g. epilepsy or have

members of your family with seizure disorders)

Have or have had breast cancer

Plan to have surgery (or a procedure requiring

anaesthetics)

Are or are planning to become pregnant

Are breast-feeding

During long-term treatment, blood, liver, and kidney tests

should be done at regular intervals.

INTERACTIONS WITH THIS MEDICATION

Stemetil

can add to the effects of alcohol. You should avoid

consuming alcoholic beverages while on Stemetil

therapy.

Before using any prescription, over-the-counter medicines or

herbal products, check with your doctor or your pharmacist.

Stemetil

can add to the effects of other drugs that cause

drowsiness. Some examples of drugs that can cause drowsiness

are:

Drugs for allergies

Drugs for insomnia

Drugs for pain

Drugs for seizure

Drugs for depression

Drugs for mental illness

Stemetil

may cause a false pregnancy test result. Please check

with your doctor if this happens.

PROPER USE OF THIS MEDICATION

Usual dose:

Your doctor has decided the best dose for you based on your

individual situation and needs. It is important to take Stemetil

way your doctor told you. Your doctor may increase or decrease

your dose depending on your response.

You may experience side effects if the drug is stopped suddenly.

Contact your physician before stopping your drug.

Adults

Rectal route: To control nausea, vomiting or anxiety, the usual

dose is 5 to 10 mg, 3 or 4 times daily; in mild cases, a single dose

of 5 to 10 mg is often adequate.

Injection in the muscle: Total daily dose rarely exceeds 40 mg,

except in severe cases.

Injection in the vein: Stemetil

may be given as an injection in the

vein during and after surgery. The Stemetil

injection formulation

is diluted in a solution and injected slowly in a vein. Total daily

dose rarely exceeds 30 mg.

Children

Stemetil

should not be given to children under 2 years of age or 9

kg of body weight. Occasionally, the children may react to the

drug with signs of restlessness and excitement; if this occurs,

treatment should be stopped.

Injection in the muscle

Stemetil

may be given as an injection in the muscle to control

severe nausea and vomiting or in psychiatry. The dose is based on

the body weight

Overdose:

If you have taken too much Stemetil

, immediately see your

doctor or go to your nearest hospital emergency department. Do

this even if there are no signs of discomfort or poisoning. The

signs if you have taken too much Stemetil

may vary from

drowsiness to coma. Agitation and restlessness may also occur.

Other possible reactions include confusion, drowsiness, fever, low

blood pressure, dry mouth and intestinal obstruction.

IMPORTANT: PLEASE READ

Page 18 of 19

SIDE EFFECTS AND WHAT TO DO ABOUT

THEM

Stemetil®, like any medication, may cause some side effects.

Discuss with your doctor if you do experience side effects.

Side effects include:

Agitation, anxiety, bizarre dreams, dizziness, excitement,

restlessness.

Appetite changes, constipation, dizziness, dryness of the

mouth,

headache,

increased

thirst,

nasal

congestion,

nausea, vomiting, sweating, urinary incontinence, weight

changes.

Changes in libido, impotence, increase of the breast size in

men, lactation, menstrual irregularities, peripheral oedema

(swelling of the legs, ankles, and feet).

Your skin may be more sensitive to sunlight

Side effects that might need a reduction in your dose are:

Drowsiness, fatigue, insomnia, sad mood, sleep

disturbances.

SERIOUS SIDE EFFECTS, HOW OFTEN THEY HAPPEN

AND WHAT TO DO ABOUT THEM

Talk with your

doctor or

pharmacist

Symptom / effect

See text below for details

Only if

severe

In all

cases

Stop

taking

drug and

call your

doctor or

pharmacist

Common

Extrapyramidal

reactions

a)

Uncommon

Allergic

Reactions

b)

Blood disorders

c)

Cardiac

disorders

d)

Eye disorders

e)

Liver disorders

c)

Lung disorders

c)

SERIOUS SIDE EFFECTS, HOW OFTEN THEY HAPPEN

AND WHAT TO DO ABOUT THEM

Talk with your

doctor or

pharmacist

Neuroleptic

malignant

syndrome

f)

Tardive

dyskinesia

g)

a) Extrapyramidal reactions

. The signs and symptoms of

extrapyramidal reactions include tremor, muscle stiffness, body

spasm, impairment of voluntary movement, upward eye rolling,

exaggeration of reflexes or drooling. Tell your doctor if you

experience any of these side effects. Your medication might have

to be reduced.

b) Allergic Reactions

:: You may develop an allergy to Stemetil

for example skin rash, redness or itching. Consult your doctor

immediately if you develop an allergy to Stemetil

c) Blood, liver and lung disorders

have been associated with this

class of drug. It is important that you tell your doctor at once

about any unexplained symptom you might experience. Examples

of this are soreness of the mouth, gums or throat or any symptoms

of upper respiratory infection, unexplained fever, itching, flu-like

symptoms, coughing, abdominal pain, jaundice.

d) Cardiac disorders

: Low blood pressure and fainting have been

reported. Uncommonly, Stemetil

may cause the heartbeat to

become faster or irregular. Check immediately with your doctor if

these side effects occur.

e) Eye disorders:

Blurred vision has been observed. Other eye

disorders are reported, specifically after long-term administration.

Consult you doctor if you experience any vision problems.

f) Neuroleptic malignant syndrome

:Another possible serious

unwanted effect is the neuroleptic malignant syndrome. Signs and

symptoms of the neuroleptic malignant syndrome include severe

muscle stiffness, increased sweating, fever, fast or irregular

heartbeat, high or low blood pressure, difficult or fast breathing

and confusion. If any of the above side effects occur, consult your

doctor immediately.

g) Tardive dyskinesia

may occur in some patients on long-term

therapy or after they stop using Stemetil

. Signs of tardive

dyskinesia include muscle twitching or uncontrolled movements

of the mouth, tongue, face or jaw (e.g., protrusion of tongue,

IMPORTANT: PLEASE READ

Page 19 of 19

puffing of cheeks, puckering of mouth, chewing movements).

Sometimes, these may be accompanied by involuntary

movements of the extremities. In some patients, this side effect

may not go away after they stop using Stemetil

. These effects

are rare and usually appear only after long-term therapy at high

doses. Elderly patients may be at higher risk. Tell your doctor

immediately if you experience any muscle twitching or

abnormal body movements.

This is not a complete list of side effects. For any unexpected

effects while taking Stemetil

®

, contact your doctor or

pharmacist.

HOW TO STORE IT

Stemetil

suppositories and injection should be stored at room

temperature between 15°C and 25°C.

Protect from exposure to light.

Keep out of reach of children.

REPORTING SUSPECTED SIDE EFFECTS

To monitor drug safety, Health Canada collects information on

serious and unexpected effects of drugs . If you suspect you

have had a serious or unexpected reaction to this drug you may

notify Health Canada by:

toll-free telephone:

866-234-2345

toll-free fax

866-678-6789

By email: cadrmp@hc-sc.gc.ca

By regular mail:

National AR Centre

Marketed Health Products Safety and Effectiveness

Information Division

Marketed Health Products Directorate

Tunney’s Pasture, AL 0701C

Ottawa ON K1A 0K9

NOTE: Before contacting Health Canada, you should contact

your physician or pharmacist.

MORE INFORMATION

Your physician, nurse and pharmacist are always your best source

of information about your condition and treatment. If you have

additional questions or concerns, be sure

to ask them.

This document plus the full product monograph is available upon

request to the sponsor, sanofi-aventis Canada Inc., 2150 St Elzear

Blvd. West , Laval , Quebec H7L 4A8, at:

1-800-265-7927

This leaflet was prepared by sanofi-aventis Canada Inc..

Last revised: October 13, 2006

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