Naltrexone

Chemical name

(5альфа)-17-(Циклопропил метил)-4,5-эпокси-3,14-диг идроксиморфинан-6-он

Gross

C20-H23-N-O4

Characteristics

White TNT substance soluble in water.

Of drugs

Drugs, the blocking Waismann receptors. Competitive blocks agonist binding or replacing them with opioid receptors. Decreases or eliminates symptoms caused in / with the introduction of opiates. The affinity is to mu- and каппа-рецепторам.Эффе ктивен when administered in blood absorbed by 96%. The liver almost entirely (95%) becoming a pharmacologically active metabolites, incl. in 6-beta-naltrekson. T_1/2 extended 3.9 hour 6-beta-naltrekson - 12.9 hours; Average T_1/2 depends on the dose and increases in long-term use. Naltrexone and its metabolites derived mainly kidneys and excreted (at kishechno-pechenocna circulation). The Cl is 1.5 l / Min.nacinet act in 1-2 hours If you are a long-term warns physical dependency to morfinu, heroin and other opiates. The dose of 50 mg blocks pharmacological effects 25 mg in / on by heroin in a 24-hour double dose (100 mg) for a period of 48 h, and 150 mg-3 Sutok.dlitelnoe appointment is tolerance and dependence. The combination of high doses of opioids leads to the release of increased gistamina with typical clinical picture (reddening of skin, rashes). In patients with opioid dependence is fit enough. When alcoholism is associated with opioidnami receptors and blocks the effects endorfinov. Reduces alcohol and prevent relapse within six months after the twelfth week of therapy (the success of the treatment depended on the consent of the patient and his interaction with the doctor).

Indications

Alcohol dependence (with the consent of the patient and in combination with психотерапевтическим и and social practices), the prevention of pharmacological effects of exogenous opioids to maintain clean of the opioids in patients with opioid dependence upon prior detoxification (as part of the psychological and vocational rehabilitation).

Contraindications

Гиперчувствительност ь (incl. to nalokson), opioid dependence, a positive test for opiodov in urine, the withdrawal syndrome, acute hepatitis, liver failure, pregnancy, breast-feeding (at the time of treatment excluded), Children and Youth age (up to 18 years).

Side-Effects

The decline of appetite, nausea, vomiting, diarrhoea or constipation, pain in the abdomen, violations of the liver, headache, weakness, sleep disturbance, anxiety, dizziness, depression, paranoia, hallucinations, reddening of bronhoobstrukcia weakening potency, shivers, zalojennosti nose, rinorea, cough, difficulty in breathing, facial bleeding, flebita, oedema, the AD tachycardia, pain in joints and muscles, gemorroy, tremor, acne, alopecia, itching, generalized erythema.

Patient interaction

Increases (mutually), the risk of liver damage when combined with gepatotoksicnami drugs. There may be lethargic or increased sleepiness when combined with tioridazinom.

Precautions

The application should be deleted subklinicescuu liver failure during treatment should periodically monitor the level transaminaz; Can be combined with drugs that have gepatotoksicskimi properties. To prevent the development of acute withdrawal syndrome patients should be at least 10 days the deadline for the opioids and preparations containing them with the required definition of opioids in the urine and provocative test with naloxone; in the absence of these requirements, the withdrawal syndrome can occur in five minutes after and continue for 48 C.na against drugs in the case of an emergency analgesia only drugs with caution appoint opiates in the high dosage (to overcome antagonism), as respiratory depression there is a deeper, продолжительное.След��ет warn patients that : when applying for medical assistance they have an obligation to inform medical personnel for the treatment prescribed; , 2a4 in the case of pain in the abdomen, dark urine, yellowing skler must stop reception and to see a doctor; - through home use of heroin and other drugs in small doses, the effect of their use is not, and a further increase in drug overdose leading to death (stopping breathing).

Dosing and Administration

Treatment of Alcoholism : inside of 50 mg once a day for 12 Ned.terapiu addiction begin only after 7-10-dnevnogo refraining from the use of opioids, confirmed provocative test and the analysis of urine. Initial dose of 25 mg, for 1 hour to monitor the status of the patient, in the absence of abstinence syndrome, a 50 mg once a day. Alternative regimens : 1. 50 mg budnyi every day, and 100 mg on Saturday; 2. 100 mg a day; 3. 150 mg in 2 days; 4. 100 mg on Monday, 100 mg on Wednesday, and 150 mg in Piatnytu.sleduet aware that the application of the treatment increases the risk of hepatotoxicity.

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