Neostigmine (proserinum)
PROZERIN (Proserinum).
N - (meta Dimetilkarbamoiloksifenil) - trimetilammony metilsulfate.
Synonyms : Eustigmin, Metastigmin, Miostin, Muastigmine, Neoeserin, Neostigmani Methylsulfas, Neostigmine Methyisulfate, Prostigmin methylsulfate. Stigmosan, Syntostigmin, Vagostigmin and others.
The white crystalline powder odourless, bitter taste. Gigroskopichen. In light of a rosy tint. Very easily soluble in water (1 : 10), easy-to alcohol (1 : 5). Aqueous solutions (pH 5, 9, 7, 5) 100 + sterilized with 'C for 30 min.
Neostigmine is anticholinesterase synthetic substances. On chemical structure can be seen as a simple analogue fizostigmina containing N-alkilzameschennuyu karbamoiloksifenilnuyu part. However feature prozerina (as oksazila and Mestinon) is a molecule in the quaternary ammonium group. It differs from alkaloids fizostigmina and galantamina that do not contain quaternary nitrogen atoms.
Neostigmine has strong reversible anticholinesterase activity. For peripheral effects similar to fizostigminu and galantaminu. Like other quarternary ammonium compounds has predominant influence on peripheral systems and difficult to penetrate through the blood-brain barrier.
Applied in infants, motor violations after brain injury, paralysis, the reconstruction period after the forward meningitis polimielita, encephalitis etc., with visual nerve atrophy, neuritis, for the prevention and treatment atony bowel and bladder. In ophthalmic practice Neostigmine sometimes appointed to narrow down and missed inner pressure of open glaucoma.
Neostigmine is antidepolyarizuyuschih kurarepodobnyh antagonist drugs. However, large doses can be very nerve-muscle disturbance conductivity as a result of the accumulation of acetylcholine and resistant depolarization in the synapses. As Antidote muscle Neostigmine used in muscle weakness and oppression of breath after using antidepolyarizuyuschih anesthesia, as well as in the case of depolyarizuyuschih muscle (see Ditilin) when they begin type antidepolyarizuyushih (dual unit).
Neostigmine usually applied inside or under the skin.
Inside (for 30 minutes before eating) designate in powders or tablets for adults 0.01 - 0,015 grams (10 - 15 mg) 2 - 3 times a day; Children up to 10 years of 0,001 grams (1 mg) of one year of daily life; children over 10 years - not more than the total daily dose of 0.01 g (10 mg).
Children easily assign Neostigmine pellets.
Granules prozerina for children (Granulae Rgo serini pro infantibus) pink-white or pink-cream-coloured water soluble. Issued in vials of a capacity of 150 ml. Before use in the mouth svezheprokipyachennuyu warm water bottle labels to <100 ml>. The resulting solution with 0.02% solution prozerina contains one teaspoonful (5 ml) 0,001 g, and 1 dessert spoon (10 ml) 0,002 g prozerina.
Под кожу взрослым вводят по 0,0005 г (0,5 мг = 1 мл 0,05 % раствора) 1 - 2 раза в день; детям назначают по 0,1 мл 0,05 % раствора на 1 год жизни, но не более 0.75 mL of 1 injection. Applied children in the United States.
Doing miastenicheskogo Stroke adults Neostigmine injected 0.5--1 ml of 0.05% solution, then under the skin in normal doses with small intervals. For potentiation of prozerina sometimes enter into the skin more ephedrine-1 ml of 5% solution.
Treatment prozerinom a long-term infants. In other diseases treatment lasted 25 to 30 days; If necessary, repeat the treatment after 3 - 4-week break.
Doses for the treatment of infants should be collected individually. При недостаточной дозировке может наступить ухудшение состояния, а избыточные дозы могут привести к развитию холинергических кризов и стойкого нарушения нервно-мышечной проводимости с расстройствами дыхания . Neostigmine and other anticholinesterase drugs for the treatment of myasthenia used when necessary in conjunction with aldosterone antagonists (see Spironolakton), corticosteroid and anabolic hormones. The main tools pathogenetic therapy infants remain anticholinesterase drugs (Neostigmine, oksazil, Mestinon bromide, etc.).
Sometimes designate Neostigmine weakness in the labor activity; Give the interior of 0,003 grams (3 mg) in the reception 4 to 6 times at intervals of 40 minutes between appointments. To encourage childbirth can be injected under the skin on Neostigmine 1 ml 0.05% solution of 1 - 2 times to 1 hour intervals, in conjunction with the first injection under the skin once impose 1 ml of 0.1% solution of atropine. In recent years, with new tools and techniques stimulation of labor activity Neostigmine for this purpose are rarely used.
Higher doses for adults inside : single 0,015 g (15 mg), daily 0.05 g (50 mg); Under the Skin : single 0,002 grams (2 mg), 0,006 g daily (6 mg).
In ophthalmology practice to reduce the inner pressure in glaucoma using 0.5% solution : give konyuktivalny bag for 1 to 2 drops of 1 to 4 times a day.
When applying for prozerina edema of the muscle to impose pre atropine sulfate intravenously in doze0, 5 -0.7 mg (0.5 mL 0.7 0.1% solution), expect an increase in heart rate and through 1/2-2 minutes injected 1 , 5 mg (3 ml of 0.05% solution) prozerina. If the effect is insufficient, put repeat the same dose prozerina (regardless of the aetiology make more atropine injections). Total is a 5 - 6 mg (10 - 12 ml of 0.05% solution) prozerina for 20 to 30 minutes.
In prozerina overdose or sensitivity to the side effects may be associated with perevozbuzhdeniem holinoretseptorov (holinergichesky Stroke) : gipersalivatsiya, cramps, nausea, enhancing peristalsis, diarrhea, frequent urination, muscle car and foot muscles language, the gradual development of weakness. To remove the side effects reduce the dose or stop receiving the drug, atropine, if necessary, lead or other holinoliticheskie drugs.
Neostigmine is not suitable for epilepsy, giperkinezah, bronchial asthma, strokes, expressed atherosclerosis. In overdose and bad Portability used as antagonist atropine, metacin holinoliticheskie or other drugs.
Method of issuance : powder; Pills to 0,015 g; 0.05% solution of 1 ml ampoules; Granules for children (in vials of 60 granules).
Storage : A. In a list ukuporennyh banks orange glass or glass ampoules in the dark spot.
Rp. : Tab. Proserini 0,015 N.20
D.S. At one pill two times a day (adult)
Rp. : Sol. Proserini 0,05% 1 ml
D.t.d. N. in ampull 6.
S. At 1 ml 1 - 2 times a day, adults; 0.4 ml for children under 5 years old skin
Rp. : Granulae Proserini pro infntibus 60.0
D.S. Wrap in svezheprokipyachennoy hot water up to 100 ml.
Take 1 dessert spoon (10 ml), a child 2 years
M and P r h e and h is finished solution granules can be stored in the refrigerator up to 10 days.
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