The medicine belongs to the subgroup of H1-histamine receptor blockers. Diphenhydramine has a sedative and hypnotic spectrum of action and is not a narcotic. Taking the medication in large dosages or together with alcoholic beverages can cause hallucinations. Diphenhydramine is addictive.
pharmachologic effect
First generation H1-histamine receptor blocker. The effect on the central nervous system is due to the blockade of H1-histamine receptors and m-cholinergic receptors in the brain. Reduces or prevents histamine-induced spasms of smooth muscles, increased capillary permeability, tissue swelling, itching and hyperemia, has local anesthetic, antiemetic, sedative effects, and has a hypnotic effect. Antagonism with histamine manifests itself to a greater extent in relation to local vascular reactions during inflammation and allergies than to systemic ones, that is, a decrease in blood pressure. However, when administered parenterally to patients with a deficiency in circulating blood volume, a decrease in blood pressure and an increase in existing hypotension are possible. In people with local brain damage and epilepsy, it activates (even in low doses) epileptic discharges on the electroencephalogram and can provoke an epileptic attack.
The action develops within a few minutes and lasts up to 12 hours.
Nuances of dosages from the instructions
The tablets are intended for oral administration. Doses depend on age and current pathology6
- for adults – from 30 to 50 mg, up to three times a day, therapy lasts two weeks;
- combat insomnia - in a similar volume before bedtime;
- warnings of seasickness or air sickness - in the same amount, half an hour before the trip;
- children from 6 to 12 years old - from 15 to 30 mg per procedure.
The maximum daily dose cannot exceed 250 mg, a single dose - 100 mg.
Accidentally exceeding the recommended amount of Diphenhydramine contributes to the development of an overdose. Intoxication is manifested by dryness of the oral mucosa, redness of the face, persistent mydriasis, and impaired clarity of consciousness. In children, excitement or depression of the central nervous system and convulsive syndrome may occur. A complex overdose can lead to death. Treatment of poisoning consists of gastric lavage, taking sorbents, supportive and symptomatic therapy, with constant monitoring of blood pressure and breathing.
Pharmacokinetics
Bioavailability - 50%. The time to reach maximum concentration is 20-40 minutes (the highest concentration is determined in the lungs, spleen, kidneys, liver, brain and muscles). Communication with plasma proteins - 98 - 99%. Penetrates the blood-brain barrier. Metabolized mainly in the liver, partially in the lungs and kidneys. Removed from tissues after 6 hours. The half-life is 4 - 10 hours. Within 24 hours, it is completely excreted by the kidneys in the form of metabolites conjugated with glucuronic acid. Significant amounts are excreted in milk and may cause sedation in breastfed infants (a paradoxical reaction characterized by excessive excitability may occur).
Contraindications
Hypersensitivity, lactation period, angle-closure glaucoma, prostatic hyperplasia, stenosing peptic ulcer of the stomach and duodenum, stenosis of the bladder neck, bronchial asthma, epilepsy, children under 7 months of age.
Carefully
Increased intraocular pressure, hyperthyroidism, arterial hypertension, diseases of the cardiovascular system, bronchopulmonary diseases.
Use during pregnancy and lactation
During pregnancy, it is used only if the expected benefit to the mother outweighs the potential risk to the fetus.
Breastfeeding should be stopped during treatment.
Indications for Diphenhydramine therapy and contraindications
The instructions recommend the use of the medicine for patients:
- with nettle fever, hay fever, vasomotor rhinitis;
- itchy dermatoses, acute iridocyclitis, conjunctivitis of allergic etiology;
- Quincke's edema, capillary toxicosis, reaction to vaccination;
- allergies caused by taking medications or blood transfusions;
- problems with sleep, colds;
- burns, violations of the integrity of the dermis or soft tissues;
- parkinsonism, chorea, Meniere's syndrome;
- air or sea sickness.
Diphenhydramine is prescribed for local anesthesia - in case of intolerance to other painkillers. The medication is included in the complex treatment of anaphylaxis, radiation sickness, and gastrointestinal ulcers.
The drug is contraindicated:
- in case of individual intolerance to the component composition;
- angle-closure glaucoma, enlargement (by weight and volume) of the prostate;
- stenosing gastrointestinal ulcer;
- Marion's disease;
- chronic inflammation of the respiratory tract;
- pyloroduodenal obstruction.
The medicine is not used for pregnant and lactating women, newborns and premature infants.
special instructions
Do not administer subcutaneously due to irritant effects.
During treatment with diphenhydramine, ultraviolet radiation and ethanol should be avoided.
It is necessary to inform your doctor about the use of this drug: the antiemetic effect may make it difficult to diagnose appendicitis and recognize symptoms of overdose of other drugs.
Impact on the ability to drive vehicles and operate machinery
Taking into account possible side effects, during the treatment period you should refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Features of interaction and application
Taking the drug together with tranquilizers, alcoholic beverages, sleeping pills or sedatives leads to central nervous system depression. Combination with MAO inhibitors causes activation and prolongation of anticholinergic effects.
Increased caution during therapy with Diphenhydramine is required for hyperthyroidism, increased IOP, and cardiovascular pathologies. Physician supervision is necessary for elderly patients. The medicine is not recommended for patients whose work requires constant concentration: when driving a car or operating complex moving mechanisms.
During therapy it is necessary to avoid drinking alcohol.
Side effect
From the cardiovascular system: decreased blood pressure, palpitations, tachycardia, extrasystole.
From the respiratory system: dryness of the mucous membrane of the nose and throat, increased viscosity of sputum, a feeling of constriction in the chest or throat, heavy breathing, sneezing, nasal congestion.
From the nervous system: headache, sedation, decreased attention, drowsiness, dizziness, impaired coordination of movements, general weakness, fatigue, confusion, anxiety, increased excitability, nervousness, tremor, irritability, insomnia, euphoria, paresthesia, neuritis, convulsions .
From the senses: impaired visual perception, diplopia, vertigo, tinnitus, acute labyrinthitis.
From the digestive system: dry mouth, epigastric pain, anorexia, nausea, vomiting, diarrhea, constipation.
From the genitourinary system: frequent and/or difficult urination, urinary retention, early menstruation.
From the hematopoietic organs: hemolytic anemia, thrombocytopenia, agranulocytosis.
Allergic reactions: urticaria, drug rash, anaphylactic shock.
Other: increased sweating, chills, photosensitivity.
Overdose
Symptoms: depression of the central nervous system, development of agitation (especially in children) or depression, dilated pupils, dry mouth, paresis of the gastrointestinal tract.
Treatment: there is no specific antidote, gastric lavage, if necessary, medications that increase blood pressure, oxygen, intravenous administration of plasma-substituting fluids.
Epinephrine and analeptics should not be used.
Diphenhydramine-Belmed solution for IV and IM administration 10 mg/ml in 1 ml ampoules No. 5x2
Product description
Diphenhydramine-Belmed.
Release forms
Solution.
INN
Diphenhydramine.
FTG
H1-histamine receptor blocker.
Description
Transparent colorless solution.
Compound
For one ampoule: active substance: diphenhydramine hydrochloride – 10 mg excipient: water for injection.
Pharmacotherapeutic group
Antihistamines for systemic use. Diphenhydramine. ATC code: R06AA02.
pharmachologic effect
The effect on the central nervous system is due to the blockade of H1-histamine receptors in the brain and the depressive central m-anticholinergic effect (can cause both depression and excitation of the central nervous system). It has pronounced H1-blocking activity, reduces or prevents histamine-induced smooth muscle spasms, increased capillary permeability, tissue swelling, itching and hyperemia. Causes local anesthesia (when taken orally, a short-term numbness of the mucous membranes of the oral cavity occurs) - only in high doses, blocks m-cholinergic receptors in the central nervous system, has sedative, hypnotic, antiparkinsonian and antiemetic effects. In people with local brain damage and epilepsy, it activates (even in low doses) epileptic discharges on the electroencephalogram and can provoke an epileptic attack. Sedative and hypnotic effects are more pronounced with repeated doses. The maximum effect develops 60 minutes after application, the duration of action is from 4 to 6 hours.
Indications for use
Diphenhydramine in injection form is effective in adults and in pediatric patients, except premature infants and newborns, for the following conditions when oral diphenhydramine is inappropriate. As an antihistamine: to reduce the intensity of allergic reactions to blood or plasma products, in anaphylaxis, as an adjunct to epinephrine and other standard measures after control of acute symptoms, in other uncomplicated immediate allergic conditions when oral therapy is not possible or contraindicated. As a hypnotic: insomnia (for short-term treatment of situational insomnia in patients who have difficulty falling asleep).
Directions for use and dosage regimen
Intravenously or intramuscularly. For adults and children over 14 years of age, 1-5 ml of solution (10-50 mg) intravenously or intramuscularly 1-3 times a day. The maximum daily dose is 200 mg. For children aged 7 months to 12 months, 0.3-0.5 ml (3-5 mg), from 1 year to 3 years, 0.5-1 ml (5-10 mg), from 4 to 6 years 1-1.5 ml (10-15 mg), from 7 to 14 years 1.5-3 ml (15-30 mg) if necessary every 6-8 hours. Diphenhydramine in injection form is indicated when oral administration is inappropriate. The parenteral dosage form should be inspected visually for particulate matter and discoloration prior to use whenever the package is opened. Dosage should be individualized according to the patient's needs and response.
Side effect
From the cardiovascular system: decreased blood pressure, palpitations, tachycardia, extrasystole. From the respiratory system: dryness of the mucous membrane of the nose and throat, increased viscosity of sputum, a feeling of constriction in the chest or throat, sneezing, nasal congestion. From the nervous system: headache, sedation, drowsiness, dizziness, loss of coordination, weakness, confusion, anxiety, agitation, nervousness, tremor, irritability, insomnia, euphoria, paresthesia, neuritis, convulsions. From the senses: impaired visual perception, diplopia, vertigo, tinnitus, acute labyrinthitis. From the digestive system: dryness of the oral mucosa, epigastric pain, anorexia, nausea, vomiting, diarrhea, constipation. From the genitourinary system: frequent or difficult urination, urinary retention, early menstruation. From the hematopoietic organs: hemolytic anemia, thrombocytopenia, agranulocytosis. Allergic reactions: urticaria, drug rash, anaphylactic shock, photosensitivity. If the above adverse reactions or adverse reactions not listed in these instructions for medical use of the drug occur, you should consult a doctor.
Contraindications
Hypersensitivity to diphenhydramine, other antihistamines with a similar chemical structure, breastfeeding, pregnancy, childhood (newborn period and prematurity), closed-angle glaucoma, prostatic hypertrophy, stenosing ulcer of the stomach and duodenum, pyloroduodenal obstruction, bladder neck stenosis, bronchial asthma, pheochromocytoma, epilepsy, congenital long QT syndrome or long-term use of drugs that can prolong the QT interval, bradycardia, cardiac arrhythmias, porphyria. Injections should not be used as a local anesthetic (risk of local necrosis). Concomitant use with other drugs containing diphenhydramine, including oral and topical drugs.
Overdose
Symptoms: dry mouth, respiratory depression, persistent mydriasis, increased intraocular pressure, facial flushing, depression or excitation of the central nervous system, depression, confusion, hyperkinesia, convulsions, delirium, tachycardia, including torsade de pointes, arrhythmia. A case of the development 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-substituting fluids, oxygen therapy. As an antidote for an overdose of diphenylhydramine hydrochloride, physostigmine (0.02-0.06 mg/kg body weight) can be prescribed if anticholinergic symptoms increase. In cases of physostigmine overdose, atropine is recommended. With the development of convulsions, hyperthermia and symptoms of central nervous system excitation, parenteral diazepam is prescribed.
Precautionary measures
With prolonged uncontrolled use of diphenhydramine, tolerance, physical and mental dependence develop. After discontinuation of the drug, withdrawal syndrome may develop with sleep disturbances, anxiety, and agitation. When treating insomnia, do not use for longer than 7-10 nights without consulting a doctor. UV radiation and ethanol should be avoided during treatment with diphenhydramine. It is necessary to inform your doctor about the use of this drug: the antiemetic effect may make it difficult to diagnose appendicitis and recognize symptoms of overdose with other drugs. Cases of local necrosis associated with the use of diphenhydramine injection solution subcutaneously or intravenously have been described. Do not administer subcutaneously due to irritant effects. Pediatric Use: Diphenhydramine should not be used in newborns or premature infants. In pediatric patients, antihistamines, especially in overdose, may cause hallucinations, convulsions, or death. As in adults, antihistamines can reduce mental alertness in children. In young children, diphenhydramine may cause agitation. The safety and effectiveness of diphenhydramine for the treatment of insomnia in children younger than 12 years of age have not been studied. There is a risk of overdose and toxicity (including death) in children younger than 2 years of age receiving concomitant medications containing antihistamines, antitussives, expectorants, and decongestants, alone or in combination, to relieve symptoms of an upper respiratory tract infection. Evidence of the effectiveness of these drugs in this age group is limited; appropriate doses have not been established. Therefore, it is not recommended to use such drugs in children under 2 years of age. Due to the high risk of overdose and toxicity, these drugs are not recommended for use in children under 4 years of age. If necessary, you should strictly adhere to the dosage of diphenhydramine and avoid the use of cold medications. Use in the elderly (around 60 years of age and older): Antihistamines are more likely to cause dizziness, sedation, and hypotension in older patients. Diphenhydramine has atropine-like effects and should therefore be used with caution in patients with asthma, increased intraocular pressure, hyperthyroidism, cardiovascular disease or a history of hypertension. Use with caution in patients with lower respiratory tract diseases, including asthma. Diphenhydramine may cause drowsiness and has additive effects with alcohol. Carcinogenesis, mutagenesis, effects on fertility: Long-term animal studies have not been conducted to determine mutagenic and carcinogenic potential.
Use during pregnancy and lactation
Pregnancy: category B (according to FDA classification). Reproducible studies were conducted in rats and rabbits at doses up to 5 times higher than human doses and found no evidence of impaired fertility or fetal harm associated with diphenhydramine hydrochloride. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproductive studies do not always predict human response, this drug should be used during pregnancy only if truly needed.
Impact on the ability to drive a car and potentially dangerous mechanisms
Patients should refrain from all activities that require increased attention, rapid mental and motor reactions.
Interaction with other drugs
Enhances the effect of ethanol and drugs that depress the central nervous system. Monoamine oxidase inhibitors enhance the anticholinergic activity of diphenhydramine. Antagonistic interactions are observed when co-administered with psychostimulants. Reduces the effectiveness of apomorphine as an emetic drug in the treatment of poisoning. Strengthens the anticholinergic effects of a drug with M-anticholinergic activity. Diphenhydramine potentiates the effects of local anesthetics. When used with analeptics, there is a risk of developing seizures. The use of diphenhydramine along with antihypertensive drugs may increase the feeling of fatigue. Concomitant use of drugs that prolong the QT interval and cause hypokalemia (for example, thiazide diuretics) should be avoided.
Storage conditions
In a place protected from light at a temperature not exceeding 25°C. Keep out of the reach of children.
Best before date
3 years. Do not use after the expiration date stated on the packaging.
Package
1 ml in USP-1 glass ampoules in package No. 10 or in blister packs No. 5×1, No. 5×2.
Release from pharmacies
On prescription.
Buy Diphenhydramine-Belmed solution for intravenous and intramuscular administration. 10 mg/ml in 1 ml amp in container. cell unitary enterprise No. 5x2 in the pharmacy
Price for Diphenhydramine-Belmed solution for IV and IM injection 10 mg/ml in 1 ml amp in contact. cell Pack No. 5x2
Instructions for use for Diphenhydramine-Belmed solution for IV and IM injection 10 mg/ml in amp 1 ml in cont. cell Pack No. 5x2
Interaction with other drugs
Enhances the effect of ethanol and drugs that depress the central nervous system.
Monoamine oxidase inhibitors enhance the anticholinergic activity of diphenhydramine.
Antagonistic interactions are observed when co-administered with psychostimulants.
Reduces the effectiveness of apomorphine as an emetic drug in the treatment of poisoning.
Strengthens the anticholinergic effects of drugs with m-anticholinergic activity.
