PROMETHAZINE HYDROCHLORIDE suppository

United States - English - NLM (National Library of Medicine)

Buy It Now

Active ingredient:
PROMETHAZINE HYDROCHLORIDE (UNII: R61ZEH7I1I) (PROMETHAZINE - UNII:FF28EJQ494)
Available from:
A-S Medication Solutions
Administration route:
RECTAL
Prescription type:
PRESCRIPTION DRUG
Therapeutic indications:
Promethazine HCl Suppositories, USP are useful for: Perennial and seasonal allergic rhinitis. Vasomotor rhinitis. Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Amelioration of allergic reactions to blood or plasma. Dermographism. Anaphylactic reactions, as adjunctive therapy to epinephrine and other standard measures, after the acute manifestations have been controlled. Preoperative, postoperative, or obstetric sedation. Prevention and control of nausea and vomiting associated with certain types of anesthesia and surgery. Therapy adjunctive to meperidine or other analgesics for control of postoperative pain. Sedation in both children and adults, as well as relief of apprehension and production of light sleep from which the patient can be easily aroused. Active and prophylactic treatment of motion sickness. Antiemetic therapy in postoperative patients. Promethazine HCl Suppositories are contraindicated for
Product summary:
Product: 50090-5362 NDC: 50090-5362-1 1 SUPPOSITORY in a BLISTER PACK / 4 in a CARTON NDC: 50090-5362-2 1 SUPPOSITORY in a BLISTER PACK / 12 in a CARTON
Authorization status:
Abbreviated New Drug Application
Authorization number:
50090-5362-1, 50090-5362-2

Read the complete document

PROMETHAZINE HYDROCHLORIDE- promethazine hydrochloride suppository

A-S Medication Solutions

----------

PROMETHAZINE HYDROCHLORIDE

SUPPOSITORIES, USP

Rx Only

DESCRIPTION

Each rectal suppository contains 12.5 mg or 25 mg promethazine HCl with ascorbyl

palmitate, colloidal silicon dioxide, glyceryl monostearate, hard fat, and white wax.

Promethazine HCl Suppositories, USP are for rectal administration only.

Promethazine HCl is a racemic compound; the empirical formula is C

N S∙HCl and

its molecular weight is 320.88.

Promethazine HCl, a phenothiazine derivative, is designated chemically as 10H-

Phenothiazine, 10-ethanamine, N,N, α-trimethyl-, monohydrochloride, (±)- with the

following structural formula:

Promethazine HCl occurs as a white to faint yellow, practically odorless, crystalline

powder, which slowly oxidizes and turns blue on prolonged exposure to air. It is soluble

in water and freely soluble in alcohol.

CLINICAL PHARMACOLOGY

Promethazine is a phenothiazine derivative, which differs structurally from the

antipsychotic phenothiazines by the presence of a branched side chain and no ring

substitution. It is thought that this configuration is responsible for its relative lack (1/10

that of chlorpromazine) of dopamine antagonist properties.

Promethazine is an H receptor blocking agent. In addition to its antihistaminic action, it

provides clinically useful sedative and antiemetic effects.

Promethazine is metabolized by the liver to a variety of compounds; the sulfoxides of

promethazine and N-demethylpromethazine are the predominant metabolites appearing

in the urine.

INDICATIONS AND USAGE

Promethazine HCl Suppositories, USP are useful for:

Perennial and seasonal allergic rhinitis.

Vasomotor rhinitis.

Allergic conjunctivitis due to inhalant allergens and foods.

Mild, uncomplicated allergic skin manifestations of urticaria and angioedema.

Amelioration of allergic reactions to blood or plasma.

Dermographism.

Anaphylactic reactions, as adjunctive therapy to epinephrine and other standard

measures, after the acute manifestations have been controlled.

Preoperative, postoperative, or obstetric sedation.

Prevention and control of nausea and vomiting associated with certain types of

anesthesia and surgery.

Therapy adjunctive to meperidine or other analgesics for control of postoperative pain.

Sedation in both children and adults, as well as relief of apprehension and production of

light sleep from which the patient can be easily aroused.

Active and prophylactic treatment of motion sickness.

Antiemetic therapy in postoperative patients.

CONTRAINDICATIONS

Promethazine HCl Suppositories are contraindicated for use in pediatric patients less

than two years of age.

Promethazine HCl Suppositories are contraindicated in comatose states, and in

individuals known to be hypersensitive or to have had an idiosyncratic reaction to

promethazine or to other phenothiazines.

Antihistamines are contraindicated for use in the treatment of lower respiratory tract

symptoms including asthma.

WARNINGS

WARNING

PROMETHAZINE HCL SUPPOSITORIES SHOULD NOT BE USED IN

PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE BECAUSE OF THE

POTENTIAL FOR FATAL RESPIRATORY DEPRESSION.

POSTMARKETING CASES OF RESPIRATORY DEPRESSION, INCLUDING

FATALITIES, HAVE BEEN REPORTED WITH USE OF PROMETHAZINE HCL

SUPPOSITORIES IN PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE. A

WIDE RANGE OF WEIGHT-BASED DOSES OF PROMETHAZINE HCL

SUPPOSITORIES HAVE RESULTED IN RESPIRATORY DEPRESSION IN THESE

PATIENTS.

CAUTION SHOULD BE EXERCISED WHEN ADMINISTERING PROMETHAZINE

HCL TO PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER.

IT IS RECOMMENDED THAT THE LOWEST EFFECTIVE DOSE OF

PROMETHAZINE HCL BE USED IN PEDIATRIC PATIENTS 2 YEARS OF AGE

AND OLDER AND CONCOMITANT ADMINISTRATION OF OTHER DRUGS

WITH RESPIRATORY DEPRESSANT EFFECTS BE AVOIDED.

CNS Depression

Promethazine HCl Suppositories may impair the mental and/or physical abilities required

for the performance of potentially hazardous tasks, such as driving a vehicle or

operating machinery. The impairment may be amplified by concomitant use of other

central-nervous-system depressants such as alcohol, sedatives/ hypnotics (including

barbiturates), narcotics, narcotic analgesics, general anesthetics, tricyclic

antidepressants, and tranquilizers; therefore, such agents should either be eliminated or

given in reduced dosage in the presence of promethazine HCl (see PRECAUTIONS-

Information for Patients and Drug Interactions).

Respiratory Depression

Promethazine HCl Suppositories may lead to potentially fatal respiratory depression.

Use of Promethazine HCl Suppositories in patients with compromised respiratory

function (e.g., COPD, sleep apnea) should be avoided.

Lower Seizure Threshold

Promethazine HCl Suppositories may lower seizure threshold. It should be used with

caution in persons with seizure disorders or in persons who are using concomitant

medications, such as narcotics or local anesthetics, which may also affect seizure

threshold.

Bone-Marrow Depression

Promethazine HCl Suppositories should be used with caution in patients with bone-

marrow depression. Leukopenia and agranulocytosis have been reported, usually when

promethazine HCl has been used in association with other known marrow-toxic agents.

Neuroleptic Malignant Syndrome

A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant

Syndrome (NMS) has been reported in association with promethazine HCl alone or in

combination with antipsychotic drugs. Clinical manifestations of NMS are hyperpyrexia,

muscle rigidity, altered mental status and evidence of autonomic instability (irregular

pulse or blood pressure, tachycardia, diaphoresis and cardiac dysrhythmias).

The diagnostic evaluation of patients with this syndrome is complicated. In arriving at a

diagnosis, it is important to identify cases where the clinical presentation includes both

serious medical illnesses (e.g., pneumonia, systemic infection, etc.) and untreated or

inadequately treated extrapyramidal signs and symptoms (EPS). Other important

considerations in the differential diagnosis include central anticholinergic toxicity, heat

stroke, drug fever and primary central nervous system (CNS) pathology.

The management of NMS should include 1) immediate discontinuation of promethazine

HCl, antipsychotic drugs, if any, and other drugs not essential to concurrent therapy, 2)

intensive symptomatic treatment and medical monitoring, and 3) treatment of any

concomitant serious medical problems for which specific treatments are available. There

is no general agreement about specific pharmacological treatment regimens for

uncomplicated NMS.

Since recurrences of NMS have been reported with phenothiazines, the reintroduction of

promethazine HCl should be carefully considered.

Use in Pediatric Patients

PROMETHAZINE HCL SUPPOSITORIES ARE CONTRAINDICATED FOR THE USE IN

PEDIATRIC PATIENTS LESS THAN TWO YEARS OF AGE.

CAUTION SHOULD BE EXERCISED WHEN ADMINISTERING PROMETHAZINE HCL

SUPPOSITORIES TO PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER

BECAUSE OF THE POTENTIAL FOR FATAL RESPIRATORY DEPRESSION.

RESPIRATORY DEPRESSION AND APNEA, SOMETIMES ASSOCIATED WITH

DEATH, ARE STRONGLY ASSOCIATED WITH PROMETHAZINE PRODUCTS AND

ARE NOT DIRECTLY RELATED TO INDIVIDUALIZED WEIGHT-BASED DOSING,

WHICH MIGHT OTHERWISE PERMIT SAFE ADMINISTRATION. CONCOMITANT

ADMINISTRATION OF PROMETHAZINE PRODUCTS WITH OTHER RESPIRATORY

DEPRESSANTS HAS AN ASSOCIATION WITH RESPIRATORY DEPRESSION, AND

SOMETIMES DEATH, IN PEDIATRIC PATIENTS.

ANTIEMETICS ARE NOT RECOMMENDED FOR TREATMENT OF UNCOMPLICATED

VOMITING IN PEDIATRIC PATIENTS, AND THEIR USE SHOULD BE LIMITED TO

PROLONGED VOMITING OF KNOWN ETIOLOGY. THE EXTRAPYRAMIDAL

SYMPTOMS WHICH CAN OCCUR SECONDARY TO PROMETHAZINE HCL

SUPPOSITORIES ADMINISTRATION MAY BE CONFUSED WITH THE CNS SIGNS

OF UNDIAGNOSED PRIMARY DISEASE, E.G., ENCEPHALOPATHY OR REYE'S

SYNDROME. THE USE OF PROMETHAZINE HCL SUPPOSITORIES SHOULD BE

AVOIDED IN PEDIATRIC PATIENTS WHOSE SIGNS AND SYMPTOMS MAY

SUGGEST REYE'S SYNDROME OR OTHER HEPATIC DISEASES.

Excessively large dosages of antihistamines, including Promethazine HCl Suppositories,

in pediatric patients may cause sudden death (see OVERDOSAGE). Hallucinations and

convulsions have occurred with therapeutic doses and overdoses of promethazine HCl

in pediatric patients. In pediatric patients who are acutely ill associated with dehydration,

there is an increased susceptibility to dystonias with the use of promethazine HCl.

Other Considerations

Administration of promethazine HCl has been associated with reported cholestatic

jaundice.

PRECAUTIONS

General

Drugs having anticholinergic properties should be used with caution in patients with

narrow-angle glaucoma, prostatic hypertrophy, stenosing peptic ulcer, pyloroduodenal

obstruction, and bladder-neck obstruction.

Promethazine HCl Suppositories should be used cautiously in persons with

cardiovascular disease or with impairment of liver function.

Information for Patients

Promethazine HCl Suppositories may cause marked drowsiness or impair the mental

and/or physical abilities required for the performance of potentially hazardous tasks,

such as driving a vehicle or operating machinery. The use of alcohol or other central-

nervous-system depressants such as sedatives/hypnotics (including barbiturates),

narcotics, narcotic analgesics, general anesthetics, tricyclic antidepressants, and

tranquilizers, may enhance impairment (see WARNINGS–CNS Depression and

PRECAUTIONS–Drug Interactions). Pediatric patients should be supervised to avoid

potential harm in bike riding or other hazardous activities.

The concomitant use of alcohol or other central nervous system depressants, including

narcotic analgesics, sedatives, hypnotics, and tranquilizers, may have an additive effect

and should be avoided or their dosage reduced.

Patients should be advised to report any involuntary muscle movements.

Avoid prolonged exposure to the sun.

Drug Interactions

CNS Depressants

Promethazine HCl Suppositories may increase, prolong, or intensify the sedative action

of other central-nervous-system depressants, such as alcohol, sedatives/hypnotics

(including barbiturates), narcotics, narcotic analgesics, general anesthetics, tricyclic

antidepressants, and tranquilizers; therefore, such agents should be avoided or

administered in reduced dosage to patients receiving promethazine HCl. When given

concomitantly with Promethazine HCl Suppositories, the dose of barbiturates should be

reduced by at least one-half, and the dose of narcotics should be reduced by one-

quarter to one-half. Dosage must be individualized. Excessive amounts of promethazine

HCl relative to a narcotic may lead to restlessness and motor hyperactivity in the patient

with pain; these symptoms usually disappear with adequate control of the pain.

Epinephrine

Because of the potential for promethazine HCl to reverse epinephrine's vasopressor

effect, epinephrine should NOT be used to treat hypotension associated with

Promethazine HCl Suppositories overdose.

Anticholinergics

Concomitant use of other agents with anticholinergic properties should be undertaken

with caution.

Monoamine Oxidase Inhibitors (MAOI)

Drug interactions, including an increased incidence of extrapyramidal effects, have been

reported when some MAOI and phenothiazines are used concomitantly. This possibility

should be considered with Promethazine HCl Suppositories.

Drug/Laboratory Test Interactions

The following laboratory tests may be affected in patients who are receiving therapy with

promethazine HCl:

Pregnancy Tests

Diagnostic pregnancy tests based on immunological reactions between HCG and anti-

HCG may result in false-negative or false-positive interpretations.

Glucose Tolerance Test

An increase in blood glucose has been reported in patients receiving promethazine HCl.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term animal studies have not been performed to assess the carcinogenic potential

of promethazine, nor are there other animal or human data concerning carcinogenicity,

mutagenicity, or impairment of fertility with this drug. Promethazine was nonmutagenic

in the Salmonella test system of Ames.

Pregnancy

Teratogenic Effects

Pregnancy Category C

Teratogenic effects have not been demonstrated in rat-feeding studies at doses of 6.25

and 12.5 mg/kg of promethazine. These doses are from approximately 2.1 to 4.2 times

the maximum recommended total daily dose of promethazine for a 50-kg subject,

depending upon the indication for which the drug is prescribed. Daily doses of 25 mg/kg

intraperitoneally have been found to produce fetal mortality in rats.

Specific studies to test the action of the drug on parturition, lactation, and development

of the animal neonate were not done, but a general preliminary study in rats indicated no

effect on these parameters. Although antihistamines have been found to produce fetal

mortality in rodents, the pharmacological effects of histamine in the rodent do not

parallel those in man. There are no adequate and well-controlled studies of Promethazine

HCl Suppositories in pregnant women.

Promethazine HCl Suppositories should be used during pregnancy only if the potential

benefit justifies the potential risk to the fetus.

Nonteratogenic Effects

Promethazine HCl Suppositories administered to a pregnant woman within two weeks of

delivery may inhibit platelet aggregation in the newborn.

Labor and Delivery

Promethazine HCl may be used alone or as an adjunct to narcotic analgesics during

labor and delivery. (See "DOSAGE AND ADMINISTRATION"). Limited data suggest

that use of promethazine HCl during labor and delivery does not have an appreciable

effect on the duration of labor or delivery and does not increase the risk of need for

intervention in the newborn. The effect on later growth and development of the newborn

is unknown. (See also Nonteratogenic Effects.)

Nursing Mothers

It is not known whether promethazine HCl is excreted in human milk. Because many

drugs are excreted in human milk and because of the potential for serious adverse

reactions in nursing infants from Promethazine HCl Suppositories, a decision should be

made whether to discontinue nursing or to discontinue the drug, taking into account the

importance of the drug to the mother.

Pediatric Use

PROMETHAZINE HCL SUPPOSITORIES ARE CONTRAINDICATED FOR USE IN

PEDIATRIC PATIENTS LESS THAN TWO YEARS OF AGE (see WARNINGS-Black

Box Warning and Use in Pediatric Patients).

Promethazine HCl Suppositories should be used with caution in pediatric patients 2 years

of age and older (see WARNINGS – Use in Pediatric Patients).

Geriatric Use

Clinical studies of promethazine formulations did not include sufficient numbers of

subjects aged 65 and over to determine whether they respond differently from younger

subjects. Other reported clinical experience has not identified differences in responses

between the elderly and younger patients. In general, dose selection for an elderly

patient should be cautious, usually starting at the low end of the dosing range, reflecting

the greater frequency of decreased hepatic, renal or cardiac function, and of

concomitant disease or other drug therapy.

Sedating drugs may cause confusion and over-sedation in the elderly; elderly patients

generally should be started on low doses of promethazine HCl suppositories and

observed closely.

ADVERSE REACTIONS

Central Nervous System

Drowsiness is the most prominent CNS effect of this drug. Sedation, somnolence,

blurred vision, dizziness; confusion, disorientation, and extrapyramidal symptoms such

as oculogyric crisis, torticollis, and tongue protrusion; lassitude, tinnitus, incoordination,

fatigue, euphoria, nervousness, diplopia, insomnia, tremors, convulsive seizures,

excitation, catatonic-like states, hysteria. Hallucinations have also been reported.

Cardiovascular – Increased or decreased blood pressure, tachycardia, bradycardia,

faintness.

Dermatologic – Dermatitis, photosensitivity, urticaria.

Hematologic – Leukopenia, thrombocytopenia, thrombocytopenic purpura,

agranulocytosis.

Gastrointestinal – Dry mouth, nausea, vomiting, jaundice.

Respiratory – Asthma, nasal stuffiness, respiratory depression (potentially fatal) and

apnea (potentially fatal). (See WARNINGS–Respiratory Depression).

Other – Angioneurotic edema. Neuroleptic malignant syndrome (potentially fatal) has

also been reported (See WARNINGS–Neuroleptic Malignant Syndrome).

Paradoxical Reactions

Hyperexcitability and abnormal movements have been reported in patients following a

single administration of promethazine HCl. Consideration should be given to the

discontinuation of promethazine HCl and to the use of other drugs if these reactions

occur. Respiratory depression, nightmares, delirium, and agitated behavior have also

been reported in some of these patients.

To report SUSPECTED ADVERSE REACTIONS, contact G&W Laboratories, Inc.

at 1-800-922-1038 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

OVERDOSAGE

Signs and symptoms of overdosage with promethazine HCl range from mild depression

of the central nervous system and cardiovascular system to profound hypotension,

respiratory depression, and unconsciousness, and sudden death. Other reported

reactions include hyperreflexia, hypertonia, ataxia, athetosis, and extensor-plantar

reflexes (Babinski reflex).

Stimulation may be evident, especially in children and geriatric patients. Convulsions may

rarely occur. A paradoxical-type reaction has been reported in children receiving single

doses of 75 mg to 125 mg orally, characterized by hyperexcitability and nightmares.

Atropine-like signs and symptoms-dry mouth, fixed, dilated pupils, flushing, as well as

gastrointestinal symptoms-may occur.

Treatment

Treatment of overdosage is essentially symptomatic and supportive. Only in cases of

extreme overdosage or individual sensitivity do vital signs, including respiration, pulse,

blood pressure, temperature, and EKG, need to be monitored. Activated charcoal orally

or by lavage may be given, or sodium or magnesium sulfate orally as a cathartic.

Attention should be given to the reestablishment of adequate respiratory exchange

through provision of a patent airway and institution of assisted or controlled ventilation.

Diazepam may be used to control convulsions. Acidosis and electrolyte losses should be

corrected. Note that any depressant effects of promethazine HCl are not reversed by

naloxone. Avoid analeptics, which may cause convulsions.

The treatment of choice for resulting hypotension is administration of intravenous fluids,

accompanied by repositioning if indicated. In the event that vasopressors are

considered for the management of severe hypotension that does not respond to

intravenous fluids and repositioning, the administration of norepinephrine or

phenylephrine should be considered. EPINEPHRINE SHOULD NOT BE USED, since its use

in patients with partial adrenergic blockade may further lower the blood pressure.

Extrapyramidal reactions may be treated with anticholinergic antiparkinsonian agents,

diphenhydramine, or barbiturates. Oxygen may also be administered.

Limited experience with dialysis indicates that it is not helpful.

DOSAGE AND ADMINISTRATION

Promethazine HCl Rectal Suppositories are contraindicated for children under

2 years of age (see WARNINGS–Black Box Warning and Use in Pediatric

Patients).

Promethazine HCl Suppositories are for rectal administration only.

Allergy

The average dose is 25 mg taken before retiring; however, 12.5 mg may be taken

before meals and on retiring, if necessary. Single 25-mg doses at bedtime or 6.25 to

12.5 mg taken three times daily will usually suffice. After initiation of treatment in children

or adults, dosage should be adjusted to the smallest amount adequate to relieve

symptoms. The administration of promethazine hydrochloride in 25-mg doses will

control minor transfusion reactions of an allergic nature.

Motion Sickness

The average adult dose is 25 mg taken twice daily. The initial dose should be taken one-

half to one hour before anticipated travel and be repeated 8 to 12 hours later, if

necessary. On succeeding days of travel, it is recommended that 25 mg be given on

arising and again before the evening meal. For children, Promethazine HCl Rectal

Suppositories, 12.5 to 25 mg, twice daily, may be administered.

Nausea and Vomiting

Antiemetics should not be used in vomiting of unknown etiology in children and

adolescents (see WARNINGS– Use in Pediatric Patients).

The average effective dose of promethazine HCl for the active therapy of nausea and

vomiting in children or adults is 25 mg. 12.5- to 25-mg doses may be repeated, as

necessary, at 4- to 6-hour intervals.

For nausea and vomiting in children, the usual dose is 0.5 mg per pound of body weight,

and the dose should be adjusted to the age and weight of the patient and the severity of

the condition being treated.

For prophylaxis of nausea and vomiting, as during surgery and the postoperative

period, the average dose is 25 mg repeated at 4- to 6-hour intervals, as necessary.

Sedation

This product relieves apprehension and induces a quiet sleep from which the patient can

be easily aroused. Administration of 12.5 to 25 mg promethazine HCl by rectal

suppository at bedtime will provide sedation in children. Adults usually require 25 to 50

mg for nighttime, presurgical, or obstetrical sedation.

Pre- and Postopertive Use

Promethazine HCl in 12.5- to 25-mg doses for children and 50-mg doses for adults the

night before surgery relieves apprehension and produces a quiet sleep.

For preoperative medication children require doses of 0.5 mg per pound of body weight

in combination with an appropriately reduced dose of narcotic or barbiturate and the

appropriate dose of an atropine-like drug. Usual adult dosage is 50 mg promethazine

HCl with an appropriately reduced dose of narcotic or barbiturate and the required

amount of a belladonna alkaloid.

Postoperative sedation and adjunctive use with analgesics may be obtained by the

administration of 12.5 to 25 mg in children and 25- to 50-mg doses in adults.

Promethazine HCl Rectal Suppositories are not recommended for children under 2 years

of age.

HOW SUPPLIED

Product: 50090-5362

NDC: 50090-5362-1 1 SUPPOSITORY in a BLISTER PACK / 4 in a CARTON

NDC: 50090-5362-2 1 SUPPOSITORY in a BLISTER PACK / 12 in a CARTON

Mfd. by: Cosette Pharmaceuticals, Inc.

111 Coolidge Street, South Plainfield, NJ 07080

Dist. by: Taro Pharmaceuticals U.S.A., Inc., Hawthorne, NY 10532

8-PROMTRO2

Rev. 11/2019

Promethazine Hydrochloride

Similar products

Search alerts related to this product

View documents history

Share this information