PROMETHAZINE HCL- promethazine hydrochloride injection
Wockhardt USA LLC.
Promethazine HCl Injection USP, is a sterile, pyrogen-free solution for deep intramuscular or intravenous administration. Promethazine HCl (10H -Phenothiazine-10 ethanamine,N ,N ,α-trimethyl-, monohydrochloride, (±)-) is a racemic compound and has the following structural formula:
Each mL contains Promethazine HCl, either 25 mg or 50 mg with 0.1 mg edetate disodium, 0.04 mg calcium chloride, 0.5 mg sodium metabisulfite in water for injection. The pH range is 4.0 to 5.5; buffered with acetic acid-sodium acetate, and it is sealed under nitrogen.
Promethazine HCl Injection is a clear, colorless solution. The product is light sensitive. It should be inspected before use and discarded if either color or particulate is observed.
Promethazine HCl is a phenothiazine derivative which possesses antihistaminic, sedative, antimotion-sickness, antiemetic, and anticholinergic effects. Promethazine is a competitive H1 receptor antagonist, but does not block the release of histamine. Structural differences from the neuroleptic phenothiazines result in its relative lack (1/10 that of chlorpromazine) of dopamine antagonist properties. Clinical effects are generally apparent within 5 minutes of an intravenous injection and within 20 minutes of an intramuscular injection. Duration of action is four to six hours, although effects may persist up to 12 hours. Promethazine HCl is metabolized in the liver, with the sulfoxides of promethazine and N-desmethylpromethazine being the predominant metabolites appearing in the urine. Following intravenous administration in healthy volunteers, the plasma half-life for promethazine has been reported to range from 9 to 16 hours. The mean plasma half-life for promethazine after intramuscular administration in healthy volunteers has been reported to be 9.8 ± 3.4 hours.
- Amelioration of allergic reactions to blood or plasma.
- In anaphylaxis as an adjunct to epinephrine and other standard measures after the acute symptoms have been controlled.
- For other uncomplicated allergic conditions of the immediate type when oral therapy is impossible or contraindicated.
- For sedation and relief of apprehension and to produce light sleep from which the patient can be easily aroused.
- Active treatment of motion sickness.
- Prevention and control of nausea and vomiting associated with certain types of anesthesia and surgery.
- As an adjunct to analgesics for the control of postoperative pain.
- Preoperative, postoperative, and obstetric (during labor) sedation.
- Intravenously in special surgical situations, such as repeated bronchoscopy, ophthalmic surgery, and poor-risk patients, with reduced amounts of meperidine or other narcotic analgesic as an adjunct to anesthesia and analgesia.
Promethazine HCl Injection is contraindicated in comatose states and in patients who have demonstrated an idiosyncratic reaction or hypersensitivity to promethazine or other phenothiazines.
Under no circumstances should Promethazine HCl Injection be given by intra-arterial injection due to the likelihood of severe arteriospasm and the possibility of resultant gangrene (see WARNINGS-Injection Site Reactions).
Promethazine HCl Injection should not be given by the subcutaneous route; evidence of chemical irritation has been noted, and necrotic lesions have resulted following subcutaneous injection. The preferred parenteral route of administration is by deep intramuscular injection.
| WARNING: PROMETHAZINE HCl INJECTION 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 INJECTION IN PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE. A WIDE RANGE OF WEIGHT-BASED DOSES OF PROMETHAZINE HCl INJECTION HAVE RESULTED IN RESPIRATORY DEPRESSION IN THESE PATIENTS.
CAUTION SHOULD BE EXERCISED WHEN ADMINISTERING PROMETHAZINE HCl INJECTION TO PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER. IT IS RECOMMENDED THAT THE LOWEST EFFECTIVE DOSE OF PROMETHAZINE HCl INJECTION BE USED IN PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER AND CONCOMITANT ADMINISTRATION OF OTHER DRUGS WITH RESPIRATORY DEPRESSANT EFFECTS BE AVOIDED.
Promethazine HCl Injection contains sodium metabisulfite, a sulfite that may cause allergic-type reactions, including anaphylactic symptoms and life-threatening or less severe asthma episodes, in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in nonasthmatic people.
Promethazine HCl Injection 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, sedative/hypnotics (including barbiturates), general anesthetics, narcotics, narcotic analgesics,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).
Use of Promethazine HCl Injection in patients with compromised respiratory function (e.g. COPD, sleep apnea) should be avoided.
Promethazine HCl Injection may lower seizure threshold and 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.
Promethazine HCl Injection 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.
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 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.
CAUTION SHOULD BE EXERCISE WHEN ADMINISTERING PROMETHAZINE HCl INJECTION 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 STRONLGY ASSOCIATED WITH PROMETHAZINE PRODUCTS AND NOT FIRMLY WIEGHT-RELATED , WHICH MIGHT OTHERWISE PERMIT SAFE ADMINISTRATION OF INDIVIDUALIZED DOSING. 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 INJECTION ADMINISTRATION MAY BE CONFUSED WITH THE CNS SIGNS OF UNDIAGNOSED PRIMARY DISEASE , E.G., ENCEPHALOPATHY OR REYE’S SYNDROME. THE USE OF PROMETHAZINE HCl INJECTION 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 Injection, 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 Injection.
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