DIPHENHYDRAMINE- diphenhydramine hydrochloride injection, solution
APP Pharmaceuticals, LLC
Diphenhydramine hydrochloride is an antihistamine drug having the chemical name 2-(Diphenylmethoxy)-N,N-dimethylethylamine hydrochloride. It occurs as a white, crystalline powder, is freely soluble in water and alcohol.
The structural formula is as follows:
C17 H21 NO•HCl M.W. 291.82
Diphenhydramine hydrochloride in the parenteral form is a sterile, pyrogen-free solution available in a concentration of 50 mg of diphenhydramine hydrochloride per mL. pH 4.0 to 6.5; sodium hydroxide and/or hydrochloric acid added, if needed, for pH adjustment.
Diphenhydramine hydrochloride is an antihistamine with anticholinergic (drying) and sedative side effects. Antihistamines appear to compete with histamine for cell receptor sites on effector cells.
Diphenhydramine hydrochloride in the injectable form has a rapid onset of action. Diphenhydramine hydrochloride is widely distributed throughout the body, including the CNS. A portion of the drug is excreted unchanged in the urine, while the rest is metabolized via the liver. Detailed information on the pharmacokinetics of diphenhydramine hydrochloride injection is not available.
Diphenhydramine hydrochloride in the injectable form is effective in adults and pediatric patients, other than premature infants and neonates, for the following conditions when diphenhydramine hydrochloride in the oral form is impractical.
For 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, and for other uncomplicated allergic conditions of the immediate type when oral therapy is impossible or contraindicated.
For active treatment of motion sickness.
For use in parkinsonism, when oral therapy is impossible or contraindicated, as follows: parkinsonism in the elderly who are unable to tolerate more potent agents; mild cases of parkinsonism in other age groups, and in other cases of parkinsonism in combination with centrally acting anticholinergic agents.
This drug should not be used in neonates or premature infants.
Because of the higher risk of antihistamines for infants generally, and for neonates and prematures in particular, antihistamine therapy is contraindicated in nursing mothers.
Because of the risk of local necrosis, this drug should not be used as a local anesthetic. Antihistamines are also contraindicated in the following conditions: Hypersensitivity to diphenhydramine hydrochloride and other antihistamines of similar chemical structure.
Antihistamines should be used with considerable caution in patients with narrow-angle glaucoma, stenosing peptic ulcer, pyloroduodenal obstruction, symptomatic prostatic hypertrophy, or bladder-neck obstruction.
Local necrosis has been associated with the use of subcutaneous or intradermal use of intravenous diphenhydramine hydrochloride.
In pediatric patients, especially, antihistamines in overdosage may cause hallucinations, convulsions, or death.
As in adults, antihistamines may diminish mental alertness in pediatric patients. In the young pediatric patient, particularly, they may produce excitation.
Antihistamines are more likely to cause dizziness, sedation, and hypotension in elderly patients.
Diphenhydramine hydrochloride has an atropine-like action and, therefore, should be used with caution in patients with a history of bronchial asthma, increased intraocular pressure, hyperthyroidism, cardiovascular disease or hypertension. Use with caution in patients with lower respiratory disease including asthma.
Patients taking diphenhydramine hydrochloride should be advised that this drug may cause drowsiness and has an additive effect with alcohol.
Patients should be warned about engaging in activities requiring mental alertness such as driving a car or operating appliances, machinery, etc.
Diphenhydramine hydrochloride has additive effects with alcohol and other CNS depressants (hypnotics, sedatives, tranquilizers, etc.).
MAO inhibitors prolong and intensify the anticholinergic (drying) effects of antihistamines.
Long-term studies in animals to determine mutagenic and carcinogenic potential have not been performed.
Pregnancy Category B. Reproduction studies have been performed in rats and rabbits at doses up to 5 times the human dose and have revealed no evidence of impaired fertility or harm to the fetus due to diphenhydramine hydrochloride. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Diphenhydramine hydrochloride should not be used in neonates and premature infants (see CONTRAINDICATIONS).
Diphenhydramine hydrochloride may diminish mental alertness, or, in the young pediatric patient, cause excitation. Overdosage may cause hallucinations, convulsions, or death (see WARNINGS and OVERDOSAGE).
See also DOSAGE AND ADMINISTRATION section.
The most frequent adverse reactions are underscored.
- General: Urticaria, drug rash, anaphylactic shock, photosensitivity, excessive perspiration, chills, dryness of mouth, nose and throat.
- Cardiovascular System: Hypotension, headache, palpitations, tachycardia, extrasystoles.
- Hematologic System: Hemolytic anemia, thrombocytopenia, agranulocytosis.
- Nervous System: Sedation, sleepiness, dizziness, disturbed coordination, fatigue, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, euphoria, paresthesia, blurred vision, diplopia, vertigo, tinnitus, acute labyrinthitis, neuritis, convulsions.
- GI System: Epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation.
- GU System: Urinary frequency, difficult urination, urinary retention, early menses.
- Respiratory System: Thickeningofbronchialsecretions, tightness of chest or throat and wheezing, nasal stuffiness.
All MedLibrary.org resources are included in as near-original form as possible, meaning that the information from the original provider has been rendered here with only typographical or stylistic modifications and not with any substantive alterations of content, meaning or intent.