Instructions Diphenhydramine 1% solution for injection ampoule 1 ml No. 10
Composition
active ingredient: 1 ml of solution contains diphenhydramine hydrochloride 10 mg;
excipient: water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: clear colorless liquid.
Pharmacotherapeutic group
Antihistamines for systemic use. ATX code R06A A02.
Pharmacological properties
Pharmacodynamics
The first-generation H1-histamine receptor blocker eliminates the effects of histamine that manifest through this type of receptor. The effect on the central nervous system (CNS) is due to the blockade of H3-histamine receptors in the brain and the suppression of central cholinergic structures. It has pronounced antihistamine activity, reduces or prevents histamine-induced smooth muscle spasms, increased capillary permeability, tissue edema, itching and hyperemia. It causes the effect of local anesthesia (when taken orally, short-term numbness of the mucous membranes of the oral cavity occurs), blocks ganglion cholinergic receptors (reduces blood pressure (BP)) and the CNS, has sedative, hypnotic, antiparkinsonian and antiemetic effects. Antagonism with histamine is manifested to a greater extent in relation to local vascular reactions in inflammation and allergies than to systemic ones, i.e. a decrease in blood pressure. However, when administered parenterally to patients with a deficit in circulating blood volume, a decrease in blood pressure and an increase in existing hypotension due to ganglion-blocking action may occur. In patients with local brain damage and epilepsy, Diphenhydramine activates (even in low doses) epileptic discharges on the EEG and can provoke an epileptic seizure. It is more effective in bronchospasm caused by histamine liberators (tubocurarine, morphine), and to a lesser extent - in bronchospasm of an allergic nature. Sedative and hypnotic effects are more pronounced with repeated administration.
Pharmacokinetics
Plasma protein binding is 98-99%. Most of it is metabolized in the liver, the smaller part is excreted unchanged in the urine within 24 hours. The half-life (T1/2) is 1-4 hours. It is well distributed in the body, penetrates the blood-brain barrier.
Metabolized mainly in the liver by hydroxylation and conjugation to glucuronides; biotransformation products are eliminated in the urine. Excreted in breast milk and may cause sedation in breastfed infants. Maximum activity develops after 1 hour, duration of action - from 4 to 6 hours.
Indication
Anaphylactic shock, urticaria, hay fever, serum sickness, hemorrhagic vasculitis (capillary toxicosis), polymorphic exudative erythema, angioedema, pruritic dermatoses, itching, allergic conjunctivitis and allergic eye diseases, allergic reactions associated with taking medications, chorea, Meniere's disease, postoperative vomiting.
Contraindication
Hypersensitivity to the drug. Bronchial asthma attack, pheochromocytoma, epilepsy, congenital long QT syndrome or long-term use of drugs that can prolong the QT interval, angle-closure glaucoma, prostatic hyperplasia, stenosing gastric and duodenal ulcers, bladder neck stenosis, bradycardia, cardiac arrhythmias. Porphyria.
Interaction with other medicinal products and other types of interactions
Diphenhydramine potentiates the effects of anesthetics, hypnotics, sedatives, narcotic analgesics and local anesthetics. When used with tricyclic antidepressants, the anticholinergic effect and CNS depressant effects may be enhanced. There is a risk of convulsions when used simultaneously with analeptics. Simultaneous administration of MAO inhibitors and Diphenhydramine may lead to an increase in blood pressure, as well as an effect on the central nervous and respiratory systems. The use of Diphenhydramine together with antihypertensive drugs may increase the feeling of fatigue. The drug enhances the effect of ethanol, reduces the effectiveness of apomorphine as an emetic in the treatment of poisoning. It should not be prescribed together with drugs containing diphenhydramine, including those for topical use.
Application features
Not recommended for subcutaneous administration. Since Diphenhydramine has an atropine-like effect, it should be used with caution in patients with a recent history of respiratory diseases (including asthma), increased intraocular pressure, hyperthyroidism, cardiovascular diseases, arterial hypotension. May worsen obstructive pulmonary diseases, severe cardiovascular diseases, ileus, conditions with biliary obstruction. Diphenhydramine may cause drowsiness, as well as cause excitement and hallucinations, convulsions, especially in case of overdose. Use with caution in patients over 60 years of age due to a higher likelihood of dizziness, sedation and arterial hypotension.
During treatment with the drug, UV radiation and alcohol consumption should be avoided. Patients should inform their doctor about the use of this drug: the antiemetic effect may complicate the diagnosis of appendicitis and the recognition of symptoms of overdose with other drugs.
Ability to influence reaction speed when driving vehicles or other mechanisms
Since Diphenhydramine has sedative and hypnotic effects, during treatment with the drug, one should refrain from potentially hazardous activities that require increased attention and speed of psychomotor reactions.
Use during pregnancy or breastfeeding
Diphenhydramine is contraindicated during pregnancy, as there is no adequate data on the safety and effectiveness of its use.
If necessary, use of the drug should stop breastfeeding.
Method of administration and doses
The drug is administered to adults intramuscularly and intravenously by drip. The drug should not be administered subcutaneously due to its irritating effect.
For intramuscular administration, a single dose is 10-50 mg (1-5 ml); the maximum single dose is 50 mg (5 ml), the maximum daily dose is 150 mg (15 ml). Intravenously, the drug is administered dropwise in a dose of 20-50 mg (2-5 ml) of Diphenhydramine in 100 ml of 0.9% sodium chloride solution. The duration of treatment depends on the achieved effect and tolerability of the drug.
Children
The drug should not be used in pediatric practice.
Overdose
Symptoms: dry mouth, respiratory depression, persistent mydriasis, facial flushing, central nervous system depression or excitation, depression, confusion, hyperkinesia, convulsions, delirium, tachycardia, arrhythmia. A case of rhabdomyolysis after an overdose of Diphenhydramine has been described.
Treatment: symptomatic and supportive therapy with careful monitoring of respiratory function and blood pressure. Epinephrine and analeptics are not allowed. Intravenous drip administration of plasma-replacing fluids, oxygen therapy. As an antidote for diphenylhydramine hydrochloride overdose, physostigmine (0.02-0.06 mg/kg body weight intravenously) can be administered several times if anticholinergic symptoms increase. In cases of physostigmine overdose, atropine is recommended. In case of convulsions and symptoms of CNS excitation, diazepam should be administered parenterally.
Adverse reactions
From the nervous system and sensory organs: general weakness, fatigue, sedative effect, decreased attention, dizziness, drowsiness, headache, impaired coordination of movements, decreased speed of psychomotor reactions, anxiety, increased excitability, fear of death, irritability, nervousness, insomnia, euphoria, confusion, tremor, neuritis, convulsions, paresthesias, dilated pupils, increased intraocular pressure, visual impairment, diplopia, acute labyrinthitis, tinnitus. In patients with local lesions or epilepsy, convulsive discharges on the EEG are activated (even when using low doses of Diphenhydramine) and the drug can provoke an epileptic seizure.
From the cardiovascular system: arterial hypotension, palpitations, tachycardia, extrasystole.
From the blood system: agranulocytosis, thrombocytopenia, hemolytic anemia.
On the part of the digestive tract: dry mouth, short-term numbness of the oral mucosa, anorexia, nausea, epigastric pain, vomiting, diarrhea, constipation.
On the part of the genitourinary system: frequent and/or difficult urination, urinary retention, early menstruation.
On the part of the respiratory system: dryness of the mucous membrane of the nose and throat, nasal congestion, thickening of bronchial secretions, feeling of tightness in the chest, difficulty breathing, shortness of breath.
On the part of the skin and its derivatives: hyperemia, itching, polymorphic rashes, cyanosis of the skin and mucous membranes.
Allergic reactions: rash, urticaria, anaphylactic shock.
Injection site reactions: local necrosis with subcutaneous and intradermal administration.
Others: increased sweating, chills, fever, hyperthermic syndrome, photosensitivity.
Expiration date
4 years.
Storage conditions
Store in original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Packaging
10 ampoules in a box, 1 ml in an ampoule, 10 ampoules in a contour blister pack, 1 contour blister pack in a pack.
Vacation category
According to the recipe.
Producer
PJSC "Galychpharm".
Location of the manufacturer and its business address
79024, Ukraine, Lviv, Opryshkivska St., 6/8.
