Vivitrol

Vivitrol is a drug with a prolonged effect; it contains naltrexone, which is an opioid antagonist with the highest affinity for opioid mu-endings. Apart from the relatively opoidal mu-endings, naltrexone has almost no intrinsic effect. Also, naltrexone can constrict the pupils, but it has not yet been possible to determine the principle of the development of such an effect.

The use of drugs does not cause the appearance of tolerance, physical, mental or drug dependence. In people with opiate addiction, the use of the drug leads to the appearance of a withdrawal syndrome. [1]

Indications Vivitrol

It is used in persons with diagnosed alcohol dependence who are able to stop taking alcohol before starting treatment (it should be borne in mind that the medication does not weaken the intensity and does not eliminate the signs of ethyl alcohol withdrawal ).

Release form

The release of the medication is realized in the form of a lyophilisate for a prolonged-type suspension administered parenterally - inside bottles with a volume of 0.38 g (1 bottle with a solvent inside the box). The kit also contains a 1-time syringe, a medicine-making needle and 2 intramuscular injection needles.

Pharmacodynamics

The drug blocks the effect of opiates by competitively synthesizing with opiate endings within the central nervous system.

At the moment, it has not been possible to determine the exact principle of the development of the influence of drugs in people with alcohol dependence, but there are suggestions that the effect of naltrexone develops with the help of the internal opiate system. [2]

Naltrexone blockade disappears in the case of an increase in the portion of opiates, but at the same time, against the background of this effect, manifestations similar to those developing with increased release of histamine appear. [3]

The suspension of the medication is not used for aversive treatment and does not cause the appearance of disulfiram-like symptoms in the case of taking opiates and alcohol.

Pharmacokinetics

Vivitrol has a prolonged activity. When used intramuscularly, naltrexone is gradually released, showing an initial peak approximately 120 minutes after the injection; a repeated peak is observed after 2-3 days. After 2 weeks from the moment of the injection, there is a slow decrease in plasma levels of naltrexone. The substance is found inside the plasma after 1 month after the injection.

The main metabolic component of naltrexone is 6-β-naltrexone.

In the case of repeated injections, less than 15% of naltrexone with its active derivative accumulates.

In in vitro tests, a maximum of 21% of naltrexone is synthesized with plasma albumin. The medicine is actively transforming inside the body. Hemoprotein P450 is not involved in the metabolic processes of naltrexone. Together with the main derivative (6-β-naltrexone), a number of other derivatives are also formed, from which glucuronide conjugates are formed. After an i / m injection of naltrexone, the volume of 6-β-naltrexone formed is lower than in the case of oral administration.

The active element and its derivatives are excreted through the kidneys; a small amount of the administered portion is excreted unchanged.

The half-life is 5-10 days; this period is directly dependent on the severity of polymer degradation.

Dosing and administration

The medication in the form of a suspension is administered by the intramuscular route; the drug has a prolonged type of effect. Other methods of using drugs (in addition to the i / m injection) are strictly prohibited. Also, you can not drink alcohol at the beginning of treatment.

Vivitrol is used only as part of a systemic alcohol dependence therapy program, which also includes the mandatory provision of psychosocial support.

The drug can be used exclusively in a hospital. The suspension can only be made and administered by physicians with appropriate experience and qualifications.

During treatment, the medication is often used in a dosage of 0.38 g (the substance needs to be injected only intramuscularly), once a month. The suspension is injected deep into the muscles of the buttocks. The injection sites should be alternated, injecting them alternately into the left and right buttocks.

When you skip the next portion of the drug, you need to introduce it to the patient as quickly as possible.

Before the administration of the medication, naltrexone should not be taken orally.

The process of making a suspension for intramuscular injections.

During the manufacture of the drug, only the solvent provided in the kit is used. During the preparation and injection of drugs, you need to use only those needles that are also contained in the medication kit. It is forbidden to replace any elements of the medicine (the kit contains all the components required for the preparation and use of the medicine).

The medicine must be removed from the refrigerator 45-50 minutes before starting the preparation of the suspension. It is also necessary to ensure that the medication does not heat up above 25 ° C.

• Application for children

The medicine is not used in pediatrics (under the age of 18).

Use Vivitrol during pregnancy

No controlled drug tests have been performed during pregnancy. It is necessary to take into account the existing risks and do not use Vivitrol without medical supervision. During testing, drug administration was stopped in case of pregnancy.

Naltrexone together with 6-β-naltrexone are excreted in mother's milk. When breastfeeding, the medication is not used, because it can potentially cause a carcinogenic effect and the development of severe side signs of the drug in a newborn.

Contraindications

The main contraindications:

• hypersensitivity to naltrexone or other components of the drug;
• drug addiction or taking narcotic analgesics;
• active phase of opiate withdrawal syndrome;
• in case of failure to pass the provocative test (with the introduction of naloxone);
• persons who have a positive response to the analysis of opiates within the urine (the use of opiates, in order to avoid withdrawal syndrome, is stopped 7-10 days before the start of treatment with Vivitrol; despite the fact that the opiate analysis of urine cannot provide a 100% guarantee of accuracy, up to the initiation of therapy, it is necessary to perform a provocative test with the introduction of naloxone).

The medication is not used in people with active hepatopathologies (due to the potential hepatotoxicity of naltrexone (the proportion between the medicinal and hepatotoxic portion is less than 5)).

Caution is needed in such cases:

• severe stages of hepatic dysfunctions, in which the development of coagulation disorders and the appearance of complications when performing injections are possible;
• moderate or severe form of kidney failure (testing of the pharmacokinetic properties of drugs in such people has not been performed, but, taking into account the general pharmacokinetic parameters of the drug, such patients may need to change the dosage).

The drug is not used to block opiate activity or to treat opiate dependence, since in case of an increase in the portion of opiates, the blockade of the action of naltrexone disappears, which can provoke severe poisoning due to an increase in opiate levels. At the same time, naltrexone increases opiate sensitivity at the end of the drug use cycle, which can also cause poisoning (also potentially fatal) with the introduction of smaller portions of opiates. Patients should be warned against the use of opiates in combination with naltrexone.

Caution is also needed in the case of drug administration to people with various blood clotting disorders.

Side effects Vivitrol

Testing has identified the development of such side symptoms:

• dysfunction of the gastrointestinal tract: nausea, xerostomia, increased frequency of bowel movements, discomfort and pain in the epigastric zone, dyspepsia, appetite disorders (can reach anorexia) and vomiting. In addition, there may be a taste disturbance, GERD, bloating, various forms of stool disorders, hemorrhoids, gastroenteritis, colitis, bleeding inside the gastrointestinal tract, intestinal blockage and perirectal abscess;
• problems with the work of the hepatobiliary system: the active phase of cholecystitis, cholelithiasis and an increase in the values of intrahepatic enzymes;
• respiratory disorders: pharyngitis (may be associated with streptococcus) or nasopharyngitis, laryngitis with sinusitis and other infections of the respiratory tract, sore throat, dyspnea, difficulty breathing and obstruction of the respiratory ducts;
• lesions of the musculoskeletal structure: pain in the joints, muscles and limbs, joint stiffness, muscle twitching or spasm and arthritis;
• symptoms associated with the central nervous system: weakness, agitation, loss of consciousness, dizziness, sleep disturbances, headaches (including migraine), irritability and slowing down of reaction. In addition, euphoria, alcohol withdrawal syndrome, seizures, ischemic stroke, delirium, aneurysms associated with cerebral arteries and weakening of intellectual activity can be observed;
• disorders in the work of the CVS: myocardial infarction, CHF, increased blood pressure, thrombosis affecting the vessels of the lungs, DVT, angina pectoris, atherosclerosis affecting the coronary arteries, atrial fibrillation and heart rhythm disorders;
• lesions of the circulatory system: lymphadenopathy or increased leukocyte counts;
• change in test indications: an increase in the values of CPK or eosinophils (stabilized during subsequent treatment), a decrease in platelet counts and a false positive response in urine analysis for the presence of opiates and other individual drugs;
• signs of allergies: pustular rashes, anaphylactoid manifestations, itching, conjunctivitis and urticaria;
• local symptoms in the area of application of the suspension: swelling, pain and tissue induration, as well as itching and hematoma. Cases with the appearance of necrosis, abscess, as well as seals requiring surgery have been reported occasionally;
• other manifestations: asthenia, hyperthermia, toothache, anxiety, weight loss, tremors and lethargy. In addition, hypovolemia, urinary tract infection, libido disorder, hypercholesterolemia and heatstroke can occur.

Occasionally, hyperhidrosis (also nocturnal) and the development of cellulite were observed.

During testing, a case was noted with the development of eosinophilic type pneumonia, as well as a case with a suspicion of its development. The diseases were cured using corticosteroids and antibiotics. It was not possible to establish a direct connection between the action of naltrexone and the appearance of this disease, but in the case of dyspnea and progressive hypoxia, it is necessary to diagnose and carry out the required treatment.

The use of Vivitrol can provoke the appearance of suicidal thoughts (also after the completion of therapy) that accompany the emerging depression. Persons who are injected with the drug should be under the supervision of a doctor in order to timely detect suicidal thoughts and depression.

Overdose

There is only limited information regarding Vivitrol poisoning. In 5 volunteers, in the case of increasing the dosage to 784 mg, the development of toxic signs was not observed. An overdose should be expected to cause an increase in intensity and an increase in the likelihood of adverse symptoms.

Drug intoxication requires symptomatic and supportive action.

Taking into account the prolonged type of drug exposure, after exceeding the dosage, you need to monitor the patient for a long time.

Interactions with other drugs

The drug can fully block or weaken the activity that opioid-type analgesics demonstrate. If you need to perform anesthesia in people who use Vivitrol, you need to consider options with the introduction of non-narcotic analgesics, regional or local anesthesia, and in addition to benzodiazepines or general anesthesia.

If it is impossible to refuse the use of opiates, it is necessary to consider the option of increasing the dosage, which can provoke the prolongation and potentiation of respiratory suppression. In such situations, you need to make a choice in favor of drugs of a fast-acting type, minimally suppressing breathing, and also personally adjust the portion, taking into account the result obtained. In addition, it is necessary to take into account the increase in the likelihood of developing severe forms of allergy symptoms (arising from histamine release). Regardless of the type of medication selected, you need to carefully monitor the patient's condition.

Storage conditions

Vivitrol must be stored in the refrigerator (with temperature values in the range of 2-8 ° C). At a temperature of 25 ° C, the medication can be stored for a maximum of 1 week.

It is forbidden to keep the substance at a temperature of more than 25 ° C or freeze it.

Shelf life

Vivitrol in a completely sealed package can be used within 24 months from the date of manufacture of the drug. In case of violation of the tightness of the vials, it is prohibited to use the medication.

Analogs

The analogs of the drug are the substances Tison, Antabus, Beviplex with Glutargin Alkoklin, Galavit and Relium with Gepar Compositum, and besides this Muscomed, Vitanam, Sedalit and Prodetoxon. In addition, Tiaprid, Alkodez IC and Antaxon with Tazepam are on the list.

Reviews

Vivitrol is considered to be a very effective substance in helping with alcohol addiction. Reviews of patients show that the medication significantly weakens the manifestations of ethanol withdrawal. Due to this effect, mental dependence on alcohol is reduced, which increases the effectiveness of combination therapy.