Naltrexone - instructions for use, reviews, analogs and formulations (tablets and capsules 50 mg) of the drug for the treatment of withdrawal from alcoholism and drug addiction, reducing craving for alcohol in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Naltrexone. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Naltrexone in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Naltrexone in the presence of existing structural analogues.Use to treat withdrawal from alcoholism and drug addiction, reduce craving for alcohol in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Naltrexone - a competitive antagonist of opioid receptors. Eliminates the central and peripheral effects of opioids, including endogenous endorphins. Acts more intensively and more durable than naloxone.

Composition

Naltrexone hydrochloride + excipients.

Pharmacokinetics

After ingestion, naltrexone is almost completely absorbed from the digestive tract. Cmax naltrexone and its active metabolite 6-beta-naltrexol in blood plasma is achieved after 1 h. For prolonged use, naltrexone is not cumulated in the body, while the concentration of 6-beta-naltrexol in plasma reaches 40%. This is because the half-life of the metabolite is longer than that of naltrexone. 95% of the dose of naltrexone is biotransformed in the liver into pharmacologically active metabolites, the main of which is 6-beta-naltrexol is also an opioid antagonist. The second metabolite is 2-hydroxy-3-methoxy-6-beta-naltrexol. Naltrexone and its metabolites undergo intrahepatic recirculation.Naltrexone and its metabolites are excreted mainly by the kidneys. The amount of free naltrexone that is excreted in the urine is less than 1%, and the amount of free and bound 6-beta-naltrexol is about 38%.

Indications

opioid addiction (as an adjuvant for abstinence after the abolition of opioid analgesics);
alcoholism.

Forms of release

Tablets 50 mg.

Capsules 50 mg.

The dosage form in the form of implants for sewing and coding, as well as injections or injections, is not recorded.

Instructions for use and reception scheme

Inside. Treatment of alcoholism: 50 mg once a day for 12 weeks.

Therapy of drug dependence begins only after a 7-10-day abstinence from the use of opioids, confirmed by a provocative test and urinalysis. The initial dose is 25 mg, for 1 hour the patient's condition should be monitored, in the absence of the withdrawal syndrome, the remainder of the daily dose is administered. Naltrexone is prescribed at 50 mg every 24 hours (this dose is sufficient to prevent the effect of intravenously injected heroin at a dose of 25 mg). Alternative treatment regimens:

50 mg every weekday and 100 mg on a Saturday;
100 mg every other day;
150 mg after 2 days;
100 mg on Monday, 100 mg on Wednesday and 150 mg on Friday.

It should be borne in mind that the use of these regimens increases the risk of hepatotoxicity. The minimum course is 3 months, the recommended course is 6 months.

Side effect

excitation;
state of prostration;
irritability;
dizziness;
depression;
paranoia;
feeling tired;
confusion of consciousness;
disorientation in time and space;
hallucinations;
nightmarish dreams;
drowsiness;
decreased visual acuity;
pain and burning sensation in the eyes;
photophobia;
pain and a feeling of stuffiness in the ears;
noise in ears;
decreased appetite;
diarrhea, constipation;
dry mouth;
flatulence;
aggravation of hemorrhoid symptoms;
erosive and ulcerative lesions of the gastrointestinal tract;
increased activity of hepatic transaminases;
increased frequency or impaired urination;
slow ejaculation;
decreased sexual potency;
increased or decreased libido;
rash;
increased secretion of sebaceous glands;
epidermophytia of the feet;
skin changes corresponding to the 1st stage of frostbite;
hyperemia of the vessels of the nasal cavity;
nose bleed;
rhinorrhea;
sneeze;
dryness in the throat;
increased mucus;
sinusitis;
labored breathing;
tracheophophy;
cough;
dyspnea;
phlebitis;
edema;
increased blood pressure;
nonspecific changes in the cardiogram;
tachycardia;
a feeling of heat in the limbs;
sensation of a sudden surge of blood to the face;
a feeling of chills;
increased or loss of appetite;
increase in body weight;
pathological yawning;
fever;
pain in the groin;
enlarged lymph nodes;
lymphocytosis.

Contraindications

acute hepatitis;
liver failure;
children and adolescence (up to 18 years).

Application in pregnancy and lactation

The use of naltrexone in pregnancy is possible only if the potential benefit to the mother exceeds the potential risk to the fetus.

When naltrexone was orally taken, naltrexone and 6-beta-naltrexol were isolated from breast milk. Because of potential carcinogenicity and the likelihood of serious side effects in infants, a decision should be made to discontinue therapy with the drug during lactation or stop lactation, the time of treatment with the drug, depending on the importance of therapy for the mother.

Use in children

Contraindicated in children and adolescents under the age of 18 years.

special instructions

Naltrexone can be used only in cases where the patient does not take opioid analgesics for at least 7-10 days.

Naltrexone can be effective in the treatment of chronic alcoholism and reducing craving for alcohol.

Use with caution in patients with impaired liver and / or kidney function. During the treatment period, regular monitoring of liver function is recommended.

Naltrexone should be discontinued at least 48 hours before surgery, requiring the use of opioid analgesics.

Against the backdrop of naltrexone, in case of emergency analgesia, only narcotics with caution are prescribed opioids in a higher dosage (to overcome antagonism), because the respiratory depression will be deeper and more prolonged.

Patients should be warned that:

when seeking medical help, they are obliged to inform medical workers about treatment with naltrexone;
in the case of abdominal pain, darkening of the urine, yellowing of the sclera, it is necessary to stop taking the medicine and consult a doctor;
with independent use of heroin and other drugs in small doses, the effect of their use will not be, and further increase in the dose of drugs will lead to death (stopping breathing).

It should be borne in mind that with the use of naltrexone the probability of complete recovery from opioid dependence is variable.

Drug Interactions

With simultaneous use with naltrexone, the effectiveness of opioid receptor agonists (antitussives, analgesics) decreases.

Increases (mutually) the risk of liver damage when combined with hepatotoxic drugs. Possible lethargy or increased drowsiness when combined with thioridazine.

Analogues of the drug Naltrexone

Structural analogs for the active substance:

Antakson;
Vivitrol;
Naltrexone FV;
Naltrexone hydrochloride.

Analogues for the pharmacological group (detoxifying agents, including antidotes):

Anexam;
Antakson;
Artamine;
Acisol;
Bianodine;
Brydan;
Hemolactol;
Gepa Merz;
Gluconeodes;
Glutamic acid;
Dalizol;
Desferal;
Dianil;
Zorex;
Ionostigmine;
Calcium folinate;
Carbactin;
Carboxym;
Carbopect;
Carbosorb;
Cardiosan;
Diethylenetriamine pentaacetic acid;
Kuprenil;
Lamisplat;
Larnamine;
Levulose;
Leucovorin calcium;
Lignin;
Meglumine sodium succinate;
The mukonist;
MultiBeek;
MultiLuck;
Naloxone;
Naltrexone hydrochloride;
Sodium thiosulfate;
Ornilatex;
Ornitsetil;
Pelixim;
Pentacin;
Povidone;
Polyphane;
Polyphepan;
Solution for peritoneal dialysis with glucose;
Reamberin;
Sorbeks;
Trekrezan;
Activated carbon;
Uni thiol;
Uromitexan;
Ferrocin;
Sti Filter;
Ceruloplasmin;
Cystamine;
Eksidzhad;
Extranil;
Entereroz;
Epilapton;
Ethyl.

If there are no analogues of the medication for the active substance, you can go to the links below for diseases, from which the corresponding drug helps, and to look at the available analogs for therapeutic effects.

Used for the treatment of diseases: alcoholism, addiction, abstinence syndrome, alcohol abstinence