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Active Ingredient: Naltrexone hydrochloride.

Indications for use:
👉Opioid addiction (as an auxiliary drug after the withdrawal of opioid analgesics);
👉Alcoholism (as part of a combination treatment).

Other names for this medication:
Nal trex own, Naltrexone oral.

Release form and composition

Dosage forms of Naltrexone:
Capsules: gelatinous with a white body and a dark green cap; contents – white or almost white powder (10 each in a blister pack; 2 or 5 packs in a carton; 100, 200 or 300 packs in a carton (for hospitals));
Tablets (10 pieces each in blister packs; 1, 2 or 5 packs in a cardboard box; 100, 200 or 300 packs in a cardboard box (for hospitals)). Active substance: naltrexone hydrochloride – 50 mg in 1 capsule / tablet.

Additional components:
Capsules: lactose monohydrate, magnesium stearate;
Tablets: potato starch, low molecular weight polyvinylpyrrolidone medical (povidone), milk sugar (lactose), aerosil (colloidal silicon dioxide), magnesium stearate, crospovidone; The composition of the capsule shell: titanium dioxide 1% and 2%, gelatin, dye indigo carmine, dye iron oxide yellow.

Contraindications
☞ Withdrawal syndrome;
☞ Taking opiates;
☞ Liver failure;
☞ Acute hepatitis;
☞ A positive test for the presence of opioids in the urine;
☞ Age to 18 years;
☞ Pregnancy;
☞ Period of breastfeeding;
☞ Hypersensitivity to the components of the product.

Mode of application

Dosage Inside.
Treatment for opioid addiction. The phase of introduction to the course of therapy with naltrexone.
Treatment with naltrexone is prescribed after the patient refrains from taking opioids for 7-10 days (in the absence of withdrawal symptoms).
Abstinence from the use of opioids is identified by indicators of laboratory tests of urine for the content of opioids. Treatment begins with a negative provocative test with 0.5 g of naltrexone . Description of the naltrexone test: the patient must be administered 0.2-0.4 mg of naltrexone intravenously for 5 minutes. or as an injection subcutaneously or intramuscularly. If there is no reaction to the administration of naloxone within 15-30 minutes, a second dose of 0.4 mg intravenously or 0.4-0.8 mg subcutaneously is administered and the reaction is monitored. The test is considered positive with severe mydriasis, a change in affect from complacently-drowsy to dysphoric, behavioral disorders, the appearance of signs of opium withdrawal. A naloxone test is not performed in patients with withdrawal symptoms and in the detection of opioids in the urine. The naloxone test can be repeated after 24 hours. Treatment with naltrexone is begun with caution, gradually increasing the dose. The contents of the capsule are dissolved in 50 ml of water. Initially, 25 mg of naltrexone is prescribed orally (contained in 25 ml of the stock solution). The doctor should monitor the act of swallowing the drug solution. Maintenance therapy with naltrexone. The next day after the initial dose is administered, 50 mg of naltrexone is started every 24 hours (the use of naltrexone at the indicated dose is sufficient to block the effects of parenteral opioids, for example, 25 mg of heroin injected intravenously). 100 mg of naltrexone is prescribed every 2 days or 150 mg every 3 days. Alcoholism treatment As part of combination therapy. Daily intake of 50 mg of naltrexone, the minimum course is 3 months. Treatment should be part of an appropriate alcohol dependence elimination program. Throughout the course of treatment, it is necessary to monitor adherence to all components of the treatment of alcoholism that affect a favorable outcome. Medication is recommended to be accompanied by a course of psychotherapy.
The criteria for selecting patients for the treatment of alcoholism are:
1) a positive attitude towards treatment;
2) the willingness to abandon the use of alcohol (psychoactive substances);
3) participation in rehabilitation programs;
4) the beginning of a healthy lifestyle after the end of the course of treatment.

Overdose
Naltrexone is a moderately safe drug. According to studies, even large doses do not cause serious symptoms. There is evidence of a clinical study during which patients took 800 mg per day of naltrexone for a week without signs of intoxication.
If intoxication is suspected, symptomatic treatment should be prescribed.
At the preclinical study stage, with repeated administration of naltrexone at a dose of 100 mg / kg exceeding the maximum daily dose for treating a person by approximately 35 times, no significant changes were found in hematological and biochemical parameters of blood, as well as in the structure of internal organs. Naltrexone also has no local irritant effect.

Side effects
Digestive system: abdominal pain, dry mouth, nausea and / or vomiting, constipation, diarrhea, gastrointestinal upset, frequent bowel movements, flatulence, anorexia, taste change, decreased / increased appetite, erosive and ulcerative defects of the gastrointestinal tract, increased activity of liver enzymes, increased symptoms of hemorrhoids;
Respiratory system: hoarseness, cough, hyperemia of the vessels of the nasal cavity (nasal congestion), bronchial obstruction, sneezing, rhinorrhea, shortness of breath, nosebleeds, difficulty breathing, dry throat, increased sputum mucosa, pharyngitis (including streptococcal), sinusitis, nasopharyngitis;
Nervous system and sensory organs: nightmares, fatigue, nervousness, general weakness, restless sleep, dizziness, headache, blurred visual perception, hallucinations, confusion, drowsiness, irritability, fainting, depression of the central nervous system, disorientation, congestion and ringing ears, photophobia, burning sensation and pain in the eyes;
Cardiovascular system and hemopoietic system: chest pain, nonspecific changes in the electrocardiogram, increased blood pressure, tachycardia, palpitations, lymphocytosis, phlebitis;
Genitourinary system: increased urination, discomfort during urination, edema syndrome (swelling of the legs, feet, fingers, face), sexual disorders in men (decreased potency, delayed ejaculation);
Musculoskeletal system: arthritis, stiffness in joints, back pain, pain in joints / limbs, spasm and stiffness of muscles, muscle pain, muscle twitching;
Allergic reactions: skin rash, itching, flushing of the skin (including flushing of the face);
Other: decrease or increase in body weight, thirst, chills, fever, lymphadenopathy (including cervical adenitis), increased sweating.

Special instructions
Before starting the Naltrexone course, you need to make sure that there is no subclinical liver failure, during the period of treatment it is necessary to periodically monitor the level of transaminases. You can not use the drug with drugs that have a hepatotoxic effect.
In order to avoid the development of acute withdrawal symptoms, patients should stop using opioids and drugs containing them at least 7–10 days before the start of therapy, and be sure to conduct a provocative test with naltrexone . If these requirements are not observed, the development of withdrawal symptoms can occur 5 minutes after taking the drug and continue for 48 hours.
Before surgery, in which opioid analgesics will be used, the drug must be canceled at least 48 hours before the operation.
The use of Naltrexone is ineffective in the treatment of cocaine as well as non-opioid drug dependence.
When observing a persistent decrease in appetite and progressive weight loss, therapy should be discontinued. In case of emergency analgesia with narcotic drugs, it is necessary to prescribe opiates with extreme caution in an increased dosage (to overcome antagonism), since this will cause a deeper and longer respiratory depression.

Patients should know what is needed:

  • To inform, on a mandatory basis, medical personnel about treatment with naltrexone when seeking medical help;
  • Stop taking the medicine and consult a doctor if you observe yellowing of the sclera, darkening of urine and abdominal pain.
    It is required to take into account that there will be no effect from the independent use of heroin and other drugs in small doses, and a further increase in the doses of narcotic drugs will lead to death (respiratory arrest).

Drug interaction
Naltrexone reduces the effectiveness of drugs that include opioids (analgesics, antitussive drugs). In combination with hepatotoxic drugs, the threat of liver damage is aggravated (mutually). When combined with thioridazine, the risk of developing increased drowsiness or lethargy increases. Terms and conditions of storage Store in a place protected from moisture and light, out of the reach of children, at a temperature not exceeding 25 ° C.

Shelf life is 36 months.

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Indinavir is an HIV protease inhibitor used in combination with other medicines to manage human immunodeficiency virus (HIV).

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Other names for this medication: Avirodin, Avural, Ciplaindivan, Cirixivan, Compound j,  Crixivan, Elvenavir, Flamind, Forli, Virixit, Virotec .

Pharmachologic effect:
Antiviral drug, a specific inhibitor of HIV proteases. Active against HIV – inhibits HIV replication, incl. with resistance to reverse transcriptase inhibitors. By binding to the active site, it inhibits the HIV-1 protease (and to a lesser extent the HIV-2 protease), which participates in the assembly of the viral virion (which is considered the transport form of the virus) at the exit from the affected cell. As a result of the inhibition of HIV protease activity, inactive virus particles are formed.

Pharmacokinetics:
After ingestion, the fasting is quickly absorbed (high-calorie foods, especially rich in fats and proteins, slow down absorption, reduce Cmax and AUC). TCmax – 45-50 min. Communication with plasma proteins – 60%. It is metabolized in the liver with the participation of cytochrome CYP3A4, CYP3A5 and CYP3A7 with the formation of 6 oxidation products and one conjugate with glucuronic acid. It is an inhibitor of isoenzymes CYP3A4, CYP3A5 and CYP3A7. T1 / 2 – 1.5-2 hours. Not cumulated. About 80% of the accepted dose is excreted as metabolites (approximately in the same ratio by the kidneys and with bile), and 20% is excreted by the kidneys unchanged. In patients with liver failure, an increase in T1 / 2 to 2.8 h.

Indications:
Diseases caused by HIV-1 in adult patients: not previously treated with antiretroviral drugs (in combination with antiretroviral drugs or as monotherapy at the beginning of treatment of patients who are clinically inappropriate to administer nucleoside analogues); previously received antiretroviral drugs and having contraindications or resistance to drugs – reverse transcriptase inhibitors (in combination with antiretroviral drugs or as monotherapy).

Contraindications:
Hypersensitivity, pregnancy, lactation period. C caution. Hemophilia, liver failure, children and old age (safety and efficacy have not been established).

Side effects:
On the part of the digestive system: aphthous stomatitis, abdominal pain, heartburn, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, taste disturbance, increased activity of liver transaminases, cholecystitis (including calculous), cholestatic hepatitis , hyperbilirubinemia (total bilirubin more than 2.5 mg / dL due to indirect bilirubin). Nervous system disorders: asthenia, dizziness, headache, hypoesthesia, sleep disturbances (drowsiness), nervousness, depression, paresthesias, tremor, peripheral polyneuropathy. On the part of the musculoskeletal system: arthralgia, myalgia, muscle cramps, stiff muscles, chest pain. On the part of the respiratory system: cough, respiratory failure, sinusitis, upper respiratory tract infections, pneumonia. On the part of the urinary system: dysuria, nocturia, nephrourolithiasis, pain in the kidney area, hematuria, proteinuria, hypercreatininemia. For the skin: dry skin, itching, dermatitis (including contact, seborrheic). From the side of blood-forming organs and the hemostatic system: spontaneous bleeding in patients with hemophilia A and B (who received protease inhibitors). Other: lymphadenopathy, fever, increased sweating, flu-like syndrome, hemolytic anemia.

Interaction:
Enhances (mutually) the effect of reverse transcriptase inhibitors. Increases rifabutin concentration. With the simultaneous appointment of zidovudine and indinavir, AUC indinavir increases by 13%, zidovudine – by 17%; with simultaneous use of indinavir, zidovudine and lamivudine, the AUC of indinavir does not change, the AUC of zidovudine is increased by 36%, and the AUC of lamivudine is reduced by 6% (dose adjustment is not required). Decreases the metabolic rate and increases the toxicity of terfenadine, astemizole and cisapride, midazolam and thiazolide, which can lead to the occurrence of cardiac arrhythmias (simultaneous administration of drugs is not recommended). Ketoconazole increases the concentration of indinavir, and rifampicin reduces. In combination therapy with didanosine, drugs are taken on an empty stomach with an interval between doses of 1 hour.

Special instructions:
To ensure adequate hydration and prevention of nephroluritiasis, 1.5-2 liters of fluid should be drunk per day. During treatment, it is recommended to control the activity of amylase, ALT, AST, the concentration of bilirubin and glucose in plasma. Care should be taken when prescribing to patients with hemophilia (isolated cases of spontaneous bleeding of unknown etiology have been reported).

The information provided in this section is intended for medical and pharmaceutical professionals and should not be used for self-medication. The information is given for familiarization and can not be considered as official.

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👉Active Ingredient: Tranexamic acid.

Cyklokapron (Tranexamic acid) is used for short-term control of bleeding in hemophiliacs, including dental extraction procedures.


⚛ Other names for this medication:
Acide tranexamique, Acido tranexamico, Acidum tranexamicum, Amchafibrin, Anvitoff, Asamnex, Azeptil, Ciclokapron, Cyklo-f, Cyklonova, Ditranex, Espercil, Ethinex, Exacyl, Examic, Hemlon, Hemotran, Hemotrex, Hemsamic, Hexakapron, Hexamic, Hexatron, Intermic, Kalnex, Keisamine, Lunex, Lysteda, Medisamin, Nexa, Nexitra, Nicolda, Plasminex, Pletasmin, Ranobis, Rikavarin, Ronex, Spotof, Tacid, Tracapmin, Tranarest, Trand, Tranex, Tranexamsyra, Tranexid, Tranon, Transabon, Transamin, Transamine, Transcam, Tranxa, Traxyl, Trexam, Ugurol, Vanarin top, Vasolamin, Xamic.

👉Pharmacotherapeutic group

Fibrinolysis inhibitors

👉Pharmacological properties
Antifibrinolytic, antiallergic, anti-inflammatory. Competitively inhibits plasminogen activator, in higher concentrations binds plasmin. Extends thrombin time. It inhibits the formation of kinins and other peptides involved in inflammatory and allergic reactions. When ingestion absorbed 30-50% of the dose. The maximum concentration is reached 3 hours after administration. The initial volume of distribution – 9-12 liters. Easily passes through histohematogenous barriers, including BBB, placental. Concentration in cerebrospinal fluid is 1/10 of plasma. It is found in seminal fluid, where it inhibits fibrinolytic activity, but does not affect sperm migration. The insignificant part undergoes biotransformation. The main route of excretion is glomerular filtration. Excreted with urine. Antifibrinolytic concentration in various tissues is maintained for 17 hours, in plasma – up to 7-8 hours.

👉Indications for use Cyklokapron
Bleeding due to increased general and local fibrinolysis (treatment and prevention): hemophilia, hemorrhagic complications of fibrinolytic therapy, thrombocytopenic purpura, aplastic anemia, leukemia, bleeding during surgery and in the postoperative period, uterine during childbirth, pulmonary, nasal, gastrointestinal, meno- and metrorrhagia, gross hematuria, caused by bleeding from the lower urinary tract; aphthous stomatitis, tonsillitis, laryngopharyngitis, hereditary angioedema, eczema, allergic dermatitis, urticaria, drug and toxic rash.

👉Contraindications
Hypersensitivity, subarachnoid hemorrhage, renal failure, thrombophilic conditions (deep vein thrombosis, thromboembolic syndrome, myocardial infarction), impaired color vision, pregnancy.

👉Cautions when using
In case of renal insufficiency (depending on the degree of increase in serum creatinine), the dose and frequency of administration is reduced. During and after treatment for several days, an ophthalmologist should be observed with a check of acuity, margins and color vision, and examination of the fundus. With caution used in combination with tissue hemostatic drugs, hemocoagulase (in large doses), heparin. When treating hematuria of renal genesis, the risk of mechanical anuria increases as a result of a clot in the urethra.

👉Interaction with drugs
Incompatible with urokinase, noradrenaline bitartrate, desoxyepinephrine hydrochloride, metarmine bitartrate, dipyridamole, diazepam. In a solution, tranexamic acid reacts (cannot be mixed) with antibiotics (benzylpenicillin, tetracyclines), blood proteins.

👉Side effects
Dyspeptic phenomena (anorexia, nausea, vomiting, diarrhea), dizziness, weakness, drowsiness, tachycardia, chest pain, hypotension (with rapid on / in the introduction), impaired color vision, skin allergic reactions.

👉Application and dosage

▫ Inside, regardless of the meal – 250-500 mg 3-4 times a day.

▫ With profuse uterine bleeding – 1-1.5 g 3-4 times a day for 3-4 days.

▫ With repeated nasal bleeding – 1 g 3 times a day for 7 days.

▫ After surgery, cervix conization – 1.5 g 3 times a day for 12-14 days.

▫ Patients with coagulopathy, before extraction of the tooth – at 25 mg / kg 3-4 times a day, starting 1 day before the upcoming surgery and continuing for 6-8 days after.

▫ For hereditary angioedema, by mouth, 1-1.5 g 2-3 times a day (constantly or intermittently, depending on the presence of prodromal symptoms).

▫ In case of violation of the excretory function of the kidneys, correction of the dosage regimen is necessary: ​​when the concentration of creatinine in the blood is 120-250 μmol / l, 15 mg / kg 2 times a day; 250-500 µmol / l – in the same single dose 1 time per day; more than 500 µmol / l – 7.5 mg / kg 1 time per day.

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