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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.

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.

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).

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.

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.

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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