Promethazine

Chemical name

N,N,альфа-Триметил-10Н-ф��нотиазин-10-этанамин (and as hydrochloride or kamsilata)

Gross

C17-H20-N2-S

Characteristics

Derived fenotiazina. Crystalline powder white or nejno-jeltogo colors, odourless. Slowly oxidized in the air, with the blue. Very easily soluble in water, it is readily soluble in alcohol.

Of drugs

The drugs-antigistaminnoe, protiwallergicescoe, sedative, sleeping, protivorvotnoe, mestnoanestezirutee, protivozudnoe. Competitive H_1-gistaminove blocks receptors to antiekssoudativoe, protiwallergicescoe, antiinflammatory, mestnoanestezirutee effect. Decreases capillary permeability, swollen mucous membranes, skin. Provides adrainoliticescoe, moderate force on the central and holinoliticescoe effect. Ingibiruet Gistamin-n-metiltransferzu, blocking central gistaminove H_3-retseptora. Oppressing CNS has sedative, anxiolytic, and antipsihoticescoe pills act lowers body temperature. Decreases anxiety vestibular receptors inhibits the maze eliminates dizziness. Protivorvotny effect of the blockade was receptors hemoretseptorna zone oblong brain. Penetrates the GEB. In appointing the two weeks before the birth can oppress agregatia platelets in newborns. In experimental studies have been found mutagennogo effects and the adverse effects on the development of Ploda.bystro and completely absorbed from the digestive tract. The ingestion effects are manifested through 15-60 minutes, with the / m introduction-after 20 minutes, when in / in-five minutes. The duration of 4-6 hours (after intake of up to 12h). Associated with blood plasma proteins at 65%. Metabolised in the liver and parts of the kidneys, with the formation of sulfoxidov prometazina, N-desmetilprometazina and other derivatives. T_1/2 - 7-14 hours Write mainly urine, including in the form of metabolites.

Indications

Allergodermatozy, prurigo, eczema, ekssoudativei diates, urticaria, rash and other allergic skin reactions to drugs and chemicals, itching, allergic conjunctivitis, rhinitis, pollinoz, running dogs, bees, scorpions, bumblebees, savorotocnaya disease angioneuroticeski swelling, false croup, bronchitis asthma, atopical bronchial asthma, and anaphylacticskie anaphylactoidnye reaction (in the complex therapy), suffer from allergic expressed component; Ménière syndrome, dizziness, nausea and vomiting, sickness syndrome; anxiety, neuroses, and neurozopodobne state, psychosis, insomnia, ekstrapiramidnye disorders (in the background reception doses), nevralgia troinicnogo nerve, migraine, trochaic, hyperthermia; premedikation and posleoperazionny period (as a sedative, to artificially gibernation, potenzirovania narcosis and local anaesthesia) Study stomach secretions (using as a catalyst gistamina secreta).

Pregnancy and lactation

Contraindicated. At the time of treatment should stop breastfeeding.

Contraindications

Гиперчувствительност ь (incl. to fenotiazinam etc.), coma, alcohol intoxication, liver failure, jaundice, Denmark prostate, predisposition to delay urine, stenoses neck bladder zakratougolnaya glaucoma, a disease hospital with piloroduodenalna obstruction, disease divisions lower respiratory tract disease, epilepsy, AIDS patients in a dream, Ray syndrome, pregnancy, breast-feeding, Children (up to 2 years) and old age.

Side-Effects

From the nervous system and sensory organs : sedative effect, dizziness, drowsiness, anxiety, arousal, bad dreams, frequent night ventricle; Rarely disorientation, sputannosti consciousness ekstrapiramidnye disorders, the sudorojna activity (children); Ccomodation violation and view noise or sound in Ushah.so the circulatory system and blood (blood, gemostaz) : ortostatical gipotenzia (with on / in the introduction), hypertension, tachycardia, or aetiology; rarely lakopenia, thrombocytopenia, Agranulozitoz.so part of the intestine : anaesthesia and dry mouth, nausea, vomiting, holetaz, Zapor.so the respiratory system : dryness in the nose, Glotke.so the urogenital system : rarely difficulty or pain �очеиспускание.Аллерг ические reactions : urticaria, dermatitis, Astma.prochie : increased sweating, photosensitization.

Specific guidance

The solution is not intended for in / a and d / to the introduction. Some pharmaceutical forms prometazina metabisulfit contain sodium, which can cause allergic reactions, including anaphylactoidnye and asthmatic. To prevent distortion of the skin skarifikih samples for allergens, it is necessary to cancel 72 hours before the allergologicaki testing. During treatment possible absorption tests of pregnancy.

Patient interaction

Do effects of analgesics, hypnotics, tranquilizers, neitroleptikov, anaesthesia of local anaesthetics m-holinoblokatorov, gipotenziveh funds (a correction doses). Ters of amphetamine derivatives, m-holinomimetikov, antiholinesteraznah drugs ephedrine, guanetidina, levodopa, dopamine. Barbiturates eliminatiu accelerate and reduce the activity. Beta-adrenoblokatora increase (each) concentration in plasma (possible sharp gipotenzia, adults, irreversible retinopathy diskinesia later). Ters of bromokriptina and increases prolactin concentration in the serum. Tricyclic antidepressants and antiholinergicakie means potenziruut m-holinoblokirutuyu activity, ethanol, klofelin, противоэпилептически е Vehicles - CNS oppression. MAO inhibitors (simultaneous use is not recommended), and derivatives fenotiazina the risk of hypotension and extrapiramidale disorders. Quinidine increases the likelihood cardiodepressivnogo action.

Overdosing

Symptoms : hyperemia skin, shortness of breath, dry mucous membranes, midriaz, anxiety, hyperactivity engine, causing deliri (children), ekstrapiramidnye disorder, tremor, epileptiformnye seizures (rare), gipotenzia, respiratory depression, loss Soznaniya.lechenie : induction vomiting, stomach wash, the appointment of activated carbon plant laxatives (to the inside), in / in a liquid; Monitoring and maintaining vital functions; symptomatic therapy : sossoudossoujiwate (and hypotension), oxygen (to maintain adequate oksigenation). We do not recommend the use of analeptikov (can cause convulsions), and epinephrine (possibly increased hypotension). In developing extrapiramidale reactions using antiholinergicakie means to be used in the treatment parkinsonizma, difengidramin or barbiturates. Dialysis ineffective.

Precautions

Can suppress kashleva reflex, there is a need for caution in patients (particularly children) with the increase of chronic respiratory disease. The caution should be applied to people with impaired liver, cardiovascular disease and oppression kostnomozgovy blood. In old age caution is needed when Injecting the high doses, it ekstrapiramidnye possible violations and acute urine retention. With long-term use should be periodically monitored across the peripheral blood. As protivorvotny is to be used only when running vomit known etiology. To prevent oppression central to the appointment of caffeine. With long-term use increases the risk of dental diseases (caries, parodontit, candidiasis) due to a decrease slunootdelenia. Can mask ototoksicescoe Effects (uproar in the head and dizziness), in conjunction drugs. Increases need for riboflavine. It should not be used in conjunction with the drivers of vehicles and people skills relate to the high concentration of attention (especially at the beginning of the course). There should be no alcohol at the time of treatment.

Dosing and Administration

Inside (after delivery), rektalno in / m, / 386/1989 Adults : on 12,5-25 mg 3-4 times during daylight hours and 25-50 mg per night (maximum dose : single 75 mg, daily-500 mg). In kinetozah - 12,5-25 mg 3-4 times a day inside. When nausea and vomit at the beginning of 25 mg, then 12,5-25 mg every 4 to 6 hours Children : at the age of 2-6 years, 12.5 mg, 14 years, 25 mg 3-4 times a day. Parenteral (emergency cases anesteziological practice) : the / m (deep in the muscle) in the dose of 0.5-1 mg / kg 3-5 times a day (in the most severe cases, the primary dose of 1-2 mg / kg), the maximum daily dose is 250 mg; In / in (for gibernation) 0,15-0,3 mg / kg (maximum), 25 mg / ml, the rate of 25 mg / min). To prepare for the operation, the previous evening 25-50 mg inside conjunction with other drugs; On the day of operation for 2.5 hours before it is 50 mg in / m (in conjunction with analgesic and holinoliticom) may re-introduction of a one hour; Children, the dose of 1.1 mg / kg To prevent sickness syndrome once for 1 h to visit adult-25-50 mg, children between 10 and 20 mg. For adjuvant therapy anaphylacticski shock-10-20 mg in / in slowly (after injection of epinephrine), and further in the next 24 to 48 hours to prevent recurrence.

Literature

Saeed R. Diagnosis and treatment of Meniere's disease / / Br. Med. J.-1998-V. 316-N-7128 P. 368.

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