APOMORFIN (Apomorphinum).

     Apomorphine is a semisynthetic pygmy derived from morphine when exposed to hydrochloric acid. It is characteristic of the alkaloid removed morphine oxygen bridge and the molecular rearrangements of the newly chetyrehtsiklicheskoe connection.

     Apomorphine still some pharmacological properties of morphine. He has a weak analgeziruyuschey activity, has a dampening effect on the respiratory center. Especially expressed impact on apomorfina hemoretseptornuyu launcher (Trigger) zone suffering brain excitation which makes it a strong emetic effect. Immediately emetic center Apomorphine, like morphine, oppressing. If the first dose apomorfina vomitoxin not provided, then reintroducing it is ineffective. Application apomorfina no effect as if overwhelmed by anxiety vomitoxin centre (for example, deep anaesthesia) or hemoretseptornoy trigger zone (for example, under the influence neyrolepticheskih substances).

     Neuroleptics antagonism against vomitoxin apomorfina so typical that in the experiment, this phenomenon is often used to detect new substances neyrolepticheskih.

     In recent years, attracted the attention of the ability apomorfina dofaminergicheskie stimulate brain structure. It has now been determined that Apomorphine is a specific agonist for D receptors (see Dopamine).

     Several behavioral reactions that occur in experimental animals when the apomorfina (stereotypes, aggressiveness, etc.), explains its stimulant effect on dofamine receptors. In effect on dofamine receptors linked to a certain extent and emetic effect apomorfina. Neuroleptic and some other drugs with protivorvotnoy activity (for example, Metoclopramide) are antagonists dofamine receptors.

     In connection with the ability to penetrate the blood-brain barrier and provide a central dofaminergicheskoe tried to apply for Apomorphine treatment parkinsonizma (see Tools for treatment parkinsonizma). Apomorphine is antiparkinsonichesky curative effect, but has not been included for this purpose in the practice of medicine because of vomitoxin, nefrotoksichnosti and other side effects.

     It is estimated that violation of dofaminergicheskih plays an important role in the pathogenesis of chronic alcoholism. The relation between cravings syndrome with blood accumulation in the release.

     Apomorfinom widely used for experimental purposes in pharmacological research and the search for new, more effective psychotropic drugs.

     It is possible that the ability to interact with apomorfina dofamine receptors linked to the similarity of its molecule structure something.

     For medical applications issued apomorfina hydrochloride (Apomorphini hydrochloridum, Apomorphine hydrochloride).

     White, light grey or slightly yellow crystalline powder and odourless. In the air and on the light turns green. It is soluble in water (1:60) and alcohol (1:50). Aqueous solutions under the influence of light and air zeleneyut quickly and lose activity.

     Injectable Solution (pH 2, 3, 3, 0) are plus stabilizer.

     As emetic means apomorfina hydrochloride used in the rapid removal of the stomach for Toxic Substances and unsound food, especially when it is not possible to make washing stomach. STEP is a few minutes after subcutaneous injection. Enter into the skin of adult 0,002 - 0,005 grams (0.2 - 0.5 ml of 1% solution), children (over 2 years of age) for the 0,001 - 0,003 g.

     How rare is rarely used because of the short duration of action. Usually designated for that purpose in adult medicine for 0,001 - 0,005 grams, children 2 to 5 years - 0.0005 - 0.001 g, 6-12 years - to 0,001 - 0,0025 city

     Higher doses for adults : single inside 0,01 g, 0,005 g of the skin; Daily inside 0.03 g, 0.01 g. under the skin

     Children under the age of 2 years Apomorphine not appointed.

     In practice apomorfinom drug used to treat alcoholism.

     For the uslovnoreflektornoy negative reactions to alcohol impose apomorfina hydrochloride under the skin of a single dose of 0,002 g to 0.01 g (0.2 to 1 ml 1% solution), individually choosing the dose which causes a particular patient vomiting. After 3 to 4 minutes after apomorfina provide patient in the hands of flowers from 30-50 ml of alcohol, which he exploits. In early nausea offer drink a sip of the drink, followed by his bicycle and poloskat his mouth. When nausea and dramatically increase the patient feel approaching vomiting, he should drink even a sip of alcohol. Typically 1 to 15 minutes after the nausea vomiting develops. Showtimes are 1 to 2 times a day.

     For a permanent adverse reaction to alcohol requires 15 to 30 sessions.

     To treat alcohol cravings, and pathological attraction to alcohol abstinence outside Apomorphine to apply to the following method : drug are in gelatine capsules (to avoid irritation of mucous membrane of the mouth), starting with a single dose of 10 mg; Later in the day every 2 h gradually increase the dose of 10 mg up to a sense of nausea or vomiting. Previous dose not cause nausea or vomiting, is therapeutic for the patient. This daily dose designate every 2 h (except at night) for 5 to 7 days. To improve the intake to give consent after food, rich in protein and fat, and to increase drug resistance in the capsule add ascorbic acid.

     Sometimes the solution apomorfina enter into the skin for acute alcohol intoxication; Apomorphine often causes vomiting before comfort, then (after 5 to 30 minutes) sleep.

     Apply Apomorphine should be cautious; For some patients can develop collapse, have visual hallucinations (especially for persons who are in the past white runs), those with traumatic encephalopathy may be neurological disorders. Possible allergic reactions (skin rashes, itching of the skin, etc.).

     With the dramatic drop in blood pressure, to appoint cardiovascular funds to the patient horizontal position.

     Apomorphine is not suitable for serious heart disease, atherosclerosis, open forms of pulmonary tuberculosis and other diseases tend to pulmonary bleeding, stomach ulcers and duodenal ulcers in the stomach burns strong acids and alkalis, and organic diseases, central nervous system, in old age.

     In applying apomorfina should guard against falling keep the masses in the respiratory tract.

     Method of issuance : powder; 1% solution in 1 ml ampoules in a package of 5 or 10 vials.

     For use with alcohol packed powder pharmacies specialized facilities in gelatine capsules to 10; 20; 30; 40; 60 and 80 mg, with the addition of a drug to enhance the resilience ascorbic acid powder up to a total mass of 200 mg (0.2 g).

     Storage : List A.

     Powder contain well ukuporennyh banks orange glass ampules, in the dark place.

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