DIFENGIDRAMIN (Diphenhydramine)

     Chemical name : 2 - (Difenilmetoksi) - N, N-dimetiletanamin (and as hydrochloride)

     Description : Difengidramina hydrochloride white powder melkokristallichesky bitter taste, is showing language. Gigroskopichen. Mg in water (1 g in 1 ml), the alcohol (1 g in 2 ml), chloroform (1 g in 2 ml), acetone (1 g in 50 ml). Very little is soluble in benzene, ether. pH 1% aqueous solution of about 5.5.

     Pharmacology : The drugs act-antigistaminnoe, anti, holinoliticheskoe, protivorvotnoe, sedative, sleeping pills, mestnoanesteziruyuschee.

Lock gistaminovye H1- receptors and eliminates the effects of histamine, oposreduemye through this type receptors. Decreases or prevents histamine cramps caused by smooth muscles, increased capillary permeability, tissue swelling, itching of the skin and hyperemia. Antagonism with histamine is more on local vascular reactions in allergy and pneumonia, compared with the system, ie down AD. It is a local anaesthetic (when administered there is a short feeling numb mucous membranes of the oral cavity), has spasmolytic effect, blocking holinoretseptory vegetative gangliev (lowers AD). Lock H3- gistaminovye brain receptors and oppressing central holinergicheskie structure. Has sedative, sleeping pills (more pronounced in Runoff receptions) and protivorvotnoe effect. When parenteral a patient with a deficit BCC adds hypotension. For patients with localized brain damage or epilepsy activates (even in low doses) apnoea level of EEG and can provoke epileptic attack. In more efficient at bronchospasm due liberatorami histamine (tubokurarin, morphine, sombrevin).

Difengidramin suppresses kashlevy reflex by direct action kashlevy Center suffering brain.

In causing the skin in the form of gel provides dermatotropnoe and chilling effect.

Long-term animal studies on the possible cancer-causing mutagennogo and Diphenhydramine not held. In experimental studies in rats and rabbits with Diphenhydramine in doses up to 5 times higher than the dose for a person who has identified effects on fertility and fetotoksicheskogo action.

When administered quickly and well absorbed, Cmax achieved through 1-4 hours Linking plasma proteins, 98-99%. Most metabolised in the liver, lower-output unchanged in the urine within 24 hours T1 / 2 hours at 1-4 Well distributed in the body, passes through the GEB. Excreted from the mother and can lead sedative effects in infants. Maximum activity develops in 1 hour, the duration of between 4 and 6 hours

     Application : Cold, pollinoz, vazomotorny rhinitis, zudyaschie Medicine, iridotsiklit severe, allergic conjunctivitis, swelling angionevrotichesky, kapillyarotoksikoz, whey disease, allergic complications of drug therapy, blood transfusions and blood fluids; Integrated anaphylactic shock therapy, radiation sickness, asthma, ulcerative stomach illness and giperatsidnogo gastritis; respiratory diseases, sleep disorders, sedation, extensive injuries skin and soft tissues (scorch razmozzheniya); parkinsonizm, trochaic, sea and air sickness, vomiting, incl. in pregnancy, Menera syndrome; local anaesthesia in patients with allergies to mestnoanesteziruyuschie drugs in history.

In a gel : sunburn, and I degree burns, insect bites, urticaria, skin lesions of various origins, itchy eczema, chickenpox, allergic skin irritation (except itching with cholestasis), contact dermatitis caused by contact with plants.

     Contraindications : Giperchuvstvitelnost, breastfeeding, child age (between birth and the state of prematurity).

     Restrictions : To Zakrytougolnaya glaucoma, prostate gland hypertrophy, stenoziruyuschaya stomach ulcer and duodenal ulcer, piloroduodenalnaya obstruction, stenoses neck of the bladder pregnancy.

     Application of pregnancy and breastfeeding : With caution, under strict medical supervision during pregnancy (adequate and well-controlled studies in pregnant women is not available). At the time of treatment should stop breastfeeding.

     Side Effects : From the nervous system and sensory organs : general weakness, fatigue, sedative effect, reduced attention, dizziness, drowsiness, headache, violation of traffic coordination, anxiety, heightened anxiety (especially in children), irritability, anxiety, insomnia, euphoria , sputannost consciousness, tremor, movement, convulsions, paresteziya; visual, diplopia, acute labirintit, noise in the head.

From the cardiovascular system and blood : hypotension, palpitations, tachycardia, arrythmia; Agranulotsitoz, thrombocytopenia, haemolytic anaemia.

For part of the digestive tract : dry mouth, swelling of mucous membrane of the mouth, anorexia, nausea, epigastralny distress, vomiting, diarrhea, constipation.

From the urogenital system : frequent and / or difficulty urinating, the delay mocheotdeleniya, early menstruation.

From the respiratory system : dry nose and throat, nose mortgage, get secret bronchi, tightening in the chest and heavy breathing.

Allergic reactions : rash, urticaria, anaphylactic shock.

Other : sweating, vomiting, photosensitization.

     Networking : hypnotics, sedatives, tranquilizers and alcohol increase (each) oppression CNS. MAO inhibitors increase holinoliticheskie effects Diphenhydramine. In a joint application with Psychostimulants been antagonistic interaction.

     Overdosing : Symptoms : dry mouth, difficulty breathing, persistent midriaz, Blush person, oppression or stir (more children), central nervous system, sputannost consciousness; Child-development convulsing and death.

Treatment : induction vomiting, gastric lavage, the appointment of activated carbon; Symptoms and maintenance therapy in the face of scrutiny of breath, and the level of AD.

     Dosing and Administration : inside in / m / w, rectally, nakozhno, route, in konyunktivalny bag. Inside, adults 30-50 mg 1-3 times a day to prevent motion for 30-60 minutes to travel. If insomnia is 50 mg before bedtime. The maximum single dose of 100 mg, 250 mg daily. V / m, 10-50 mg, the maximum single dose of 50 mg, 150 mg daily, in / in-drip 20-50 mg (75-100 ml isotonic sodium chloride solution). Children under 1 year-interference in the dose of 2-5 mg, 2-5 years, 5-15 mg, 6-12 years, 15-30 mg per reception. Suppository rectally 1-2 times a day (after purification intestines). Children under the age of 3 years clerical containing 5 mg Diphenhydramine, from 3 to 4 years to 10 mg, 5 to 7 years, 15 mg, 8-14 years, 20 mg. The course of treatment is 10-15 days. For the backfilling of konyunktivalny bag prepare 0,2-0,5% solutions (preferably in the 2% solution of boric acid) and instilliruyut to 1-2 drops 2-5 times a day. To local applications gel cause for the affected areas of skin, thin layer of 3-4 times per day may also manufacture and use of 3-10% creams or ointments. In rhinitis-route, in the form of sticks on 50 mg.

     Precautions : It is not recommended for S / to the introduction. Since difengidramin has atropinopodobnym action should be used with caution : in patients with respiratory infections in recent history (including asthma), increased inner pressure with Ray, Cardiovascular diseases, hypotension. Antihistamines can reduce LS liveliness of mind as an adult, and children, as well as the initiation and cause hallucinations, convulsions and death among infants and children, especially in cases of overdose. With careful use, aged 60 years and older, because a more likely development of dizziness, sedation and hypotension. During treatment difengidraminom should avoid sun exposure. It should not be used in conjunction with the drivers and people with occupations related to higher concentration. During treatment should avoid alcohol.

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