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Black Box Warning
WARNING
See full prescribing information for complete Boxed Warning.
PROMETHAZINE HCl 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 IN PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE. A WIDE RANGE OF WEIGHT-BASED DOSES OF PROMETHAZINE HCl 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.
The average oral 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 adults, dosage should be adjusted to the smallest amount adequate to relieve symptoms. The administration of promethazine HCl 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 eight to twelve 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.
Nausea and Vomiting
The average effective dose of promethazine HCl for the active therapy of nausea and vomiting in adults is 25 mg. When oral medication cannot be tolerated, the dose should be given parenterally (promethazine injection) or by rectal suppository. 12.5 mg to 25 mg doses may be repeated, as necessary, at four-to six-hour intervals.
For prophylaxis of nausea and vomiting, as during surgery and the postoperative period, the average dose is 25 mg repeated at four-to six-hour intervals, as necessary.
Sedation
This product relieves apprehension and induces a quiet sleep from which the patient can be easily aroused. Adults usually require 25 to 50 mg for nighttime, presurgical, or obstetrical sedation.
Pre- and Postoperative Use
Promethazine HCl 50 mg doses for adults the night before surgery relieves apprehension and produces a quiet sleep.
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 25 to 50 mg doses in adults.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Promethazine (oral) in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Promethazine (oral) in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Allergy
The average oral 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, dosage should be adjusted to the smallest amount adequate to relieve symptoms. The administration of promethazine HCl in 25 mg doses will control minor transfusion reactions of an allergic nature.
Motion Sickness
For children, promethazine hydrochloride tablets 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.
The average effective dose of promethazine HCl for the active therapy of nausea and vomiting in children is 25 mg. When oral medication cannot be tolerated, the dose should be given parenterally (promethazine injection) or by rectal suppository. 12.5 mg to 25 mg doses may be repeated, as necessary, at four-to six-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 four-to six-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 the oral route or by rectal suppository at bedtime will provide sedation in children.
Pre- and Postoperative Use
Promethazine HCl in 12.5 to 25 mg doses for children 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.
Postoperative sedation and adjunctive use with analgesics may be obtained by the administration of 12.5 to 25 mg in children.
Promethazine hydrochloride tablets are contraindicated for children under 2 years of age.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Promethazine (oral) in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Promethazine (oral) in pediatric patients.
Contraindications
Promethazine hydrochloride tablets are contraindicated for use in pediatric patients less than two years of age.
Promethazine hydrochloride tablets 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.
See full prescribing information for complete Boxed Warning.
PROMETHAZINE HCl 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 IN PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE. A WIDE RANGE OF WEIGHT-BASED DOSES OF PROMETHAZINE HCl 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 tablets 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.
Use of promethazine HCl tablets in patients with compromised respiratory function (e.g., COPD, sleep apnea) should be avoided.
Lower Seizure Threshold
Promethazine HCl tablets 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 tablets 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.
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 illness (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 tablets are contraindicated for the use in pediatric patients less than two years of age.
Caution should be exercised when administering promethazine hcl tablets 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 tablets administration may be confused with the CNS signs of undiagnosed primary disease, e.g., encephalopathy or Reye's syndrome. The use of promethazine hcl tablets 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 tablets in pediatric patients may cause sudden death. 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
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 tablets should be used cautiously in persons with cardiovascular disease or with impairment of liver function.
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.
Postmarketing Experience
There is limited information regarding Postmarketing Experience of Promethazine (oral) in the drug label.
Drug Interactions
CNS Depressants
Promethazine HCl tablets 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 tablets, 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.
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 tablets overdose.
Anticholinergics
Concomitant use of other agents with anticholinergic properties should be undertaken with caution.
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 tablets.
Teratogenic effects have not been demonstrated in rat-feeding studies at doses of 6.25 mg/kg and 12.5 mg/kg of promethazine HCl. 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 in pregnant women.
Promethazine HCl tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nonteratogenic Effects:
Promethazine administered to a pregnant women within two weeks of delivery may inhibit platelet aggregation in the newborn.
Australian Drug Evaluation Committee (ADEC) Pregnancy Category
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Promethazine (oral) in women who are pregnant.
Labor and Delivery
Promethazine HCl may be used alone or as an adjunct to narcotic analgesics during labor. 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.
Nursing Mothers
It is not known whether promethazine HCl is excreted in human milk. Because many drugs are excreted in human milk and because the potential for serious adverse reactions in nursing infants from promethazine HCl tablets 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 tablets should be used with caution in pediatric patients 2 years of age and older.
Geriatic Use
Clinical studies of promethazine HCl 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 tablets and observed closely.
Gender
There is no FDA guidance on the use of Promethazine (oral) with respect to specific gender populations.
Race
There is no FDA guidance on the use of Promethazine (oral) with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Promethazine (oral) in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Promethazine (oral) in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Promethazine (oral) in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Promethazine (oral) in patients who are immunocompromised.
Administration and Monitoring
Administration
Oral
Intravenous
Intramuscular
Monitoring
There is limited information regarding Monitoring of Promethazine (oral) in the drug label.
IV Compatibility
There is limited information regarding IV Compatibility of Promethazine (oral) in the drug label.
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.
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.
Promethazine is an H1 receptor blocking agent. In addition to its antihistaminic action, it provides clinically useful sedative and antiemetic effects.
Structure
Promethazine hydrochloride, a phenothiazine derivative, is designated chemically as 10H-Phenothiazine-10-ethanamine, N,N,α-trimethyl-,monohydrochloride, (±)- with the following structural formula:
Promethazine hydrochloride is a racemic compound; the molecular formula is C17H20N2S • HCl and its molecular weight is 320.88.
Promethazine hydrochloride occurs as a white to faint yellow, practically odorless, crystalline powder which slowly oxidizes and turns blue on prolonged exposure to air. It is freely soluble in water and soluble in alcohol.
Each tablet for oral administration contains 12.5 mg, 25 mg or 50 mg promethazine hydrochloride, USP. The inactive ingredients include: hypromellose, lactose monohydrate, magnesium stearate, and microcrystalline cellulose. The 12.5 mg contains FD&C Yellow No.6 aluminum lake. The 50 mg contains D&C Red Lake Blend No.27 aluminum lake and D & C Red No. 30 aluminum lake.
Pharmacodynamics
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.
Pharmacokinetics
Promethazine is well absorbed from the gastrointestinal tract. Clinical effects are apparent within 20 minutes after oral administration and generally last four to six hours, although they may persist as long as 12 hours. 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.
Nonclinical Toxicology
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.
Clinical Studies
There is limited information regarding Clinical Studies of Promethazine (oral) in the drug label.
How Supplied
Promethazine hydrochloride tablets, USP contains 12.5 mg, 25 mg or 50 mg as promethazine hydrochloride, USP and are supplied as follows:
12.5 mg: Light peach, round, biconvex, uncoated tablets, debossed “107” on one side and scored on the other side.
NDC 57664-107-83 Bottles of 30 CRC
NDC 57664-107-88 Bottles of 100 CRC
NDC 57664-107-08 Bottles of 100
NDC 57664-107-13 Bottles of 500
NDC 57664-107-18 Bottles of 1000
25 mg: White to off-white, round, flat face bevel edge, uncoated tablets, debossed “108” on one side and scored on the other side.
NDC 57664-108-83 Bottles of 30 CRC
NDC 57664-108-88 Bottles of 100 CRC
NDC 57664-108-08 Bottles of 100
NDC 57664-108-13 Bottles of 500
NDC 57664-108-18 Bottles of 1000
50 mg: Light pink, round, biconvex, uncoated tablets, debossed “109” on one side and plain on the other side.
NDC 57664-109-83 Bottles of 30 CRC
NDC 57664-109-88 Bottles of 100 CRC
NDC 57664-109-08 Bottles of 100
NDC 57664-109-13 Bottles of 500
NDC 57664-109-18 Bottles of 1000
Store at 20° - 25°C (68° - 77°F).
Dispense in tight, light-resistant container.
Storage
There is limited information regarding Promethazine (oral) Storage in the drug label.
Images
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Promethazine HCl tablets 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. Pediatric patients should be supervised to avoid potential harm in bike riding or in other hazardous activities.
Patients should be advised to report any involuntary muscle movements.
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