Isentress - Instructions For Use, Reviews, Price, Tablet Analogs

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Isentress

Isentress: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Isentress

ATX code: J05AX08

Active ingredient: raltegravir (Raltegravir)

Manufacturer: MSD International GmbH (Singapore Branch) [MSD International GmbH (Singapore Branch)] (Singapore); MSD International GmbH (Ireland / Netherlands); Pateon Pharmaceuticals Inc. (Patheon Pharmaceuticals Inc.) (USA); R-Pharm JSC (Russia)

Description and photo update: 2019-09-07

Prices in pharmacies: from 19,500 rubles.

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Isentress is an antiviral drug active against the human immunodeficiency virus (HIV).

Release form and composition

Dosage forms of the drug Isentress:

• film-coated tablets, dosage 400 mg: biconvex, oval, pink, engraved on one side with "227";
• film-coated tablets, dosage 600 mg: biconvex, oval, yellow, engraved with the Merck logo and 242 on one side;
• chewable tablets, dosage 25 mg: flat-cylindrical, with beveled edges, round, pale yellow interspersed with white, on one side engraved with the logo of the Merck company, and on the other - "473";
• chewable tablets, dosage 100 mg: biconvex, oval, pale orange interspersed with white, on one side there is a dividing line, and on the other there is an engraving of the Merck logo and "477", separated by a line.

Packaging: 60 pcs. in vials made of high density polyethylene, in a cardboard box 1 bottle and instructions for use of Isentress.

1 film-coated tablet contains:

• active substance: raltegravir potassium - 434.4 or 651.6 mg (equivalent to raltegravir in the amount of 400 and 600 mg);
• additional components: microcrystalline cellulose, magnesium stearate; additionally for 400 mg - hypromellose 2208, lactose monohydrate, calcium hydrogen phosphate, poloxamer 407 (includes 0.01% butylhydroxytoluene as an antioxidant), sodium stearyl fumarate; additionally for 600 mg - croscarmellose sodium, hypromellose 2910;
• film coat: 400 mg - Opadray II pink dye 85F94224 (macrogol, titanium dioxide, polyvinyl alcohol, talc, iron dye red oxide and black oxide); 600 mg - carnauba wax, Opadray II yellow 39K170005 (hypromellose 2910, lactose monohydrate, triacetin, titanium dioxide, iron dye yellow oxide and black oxide).

1 chewable tablet contains:

• active substance: raltegravir potassium - 27.16 or 108.6 mg (equivalent to raltegravir in the amount of 25 and 100 mg);
• additional components: sucralose, hyprolose, Opadry colorless YS-1-19025-A ^*, sodium saccharinate, Surelease E-7-19040 ^**, mannitol, sodium citrate dihydrate, ammonium glycyrrhizinate (Magnasweet 135 ^***), magnesium stearate, crospovidone, sodium stearyl fumarate, iron dye yellow oxide, natural and artificial orange flavor 501331 TP0551, natural banana flavor WONF Durarome 501392 TD0991, natural and artificial masking flavor 501482 TP0424 ^****; additionally for 100 mg - iron oxide red dye.

Notes

^* - contains hypromellose 2910 / 6cP and macrogol

^** - includes a 25% aqueous suspension of ethyl cellulose in purified water, ammonium hydroxide, ethyl cellulose 20cP, medium-chain triglycerides, oleic acid

^*** - consists of licorice extract, fructose and sorbitol

^**** - contains aspartame

Pharmacological properties

Pharmacodynamics

The active ingredient of Isentress, raltegravir, inhibits the catalytic activity of the enzyme involved in the multiplication (replication) of the HIV virus - HIV integrase. Inhibition of the latter prevents covalent introduction, or integration into the host cell genome of the HIV genome at the early stages of infection. HIV genomes that are not introduced into human DNA cannot produce new viral particles, thus, inhibition of the integration process blocks the further spread of viral infection in the body. In relation to human phosphotransferases, including DNA polymerases α, β, and γ, the inhibitory activity of raltegravir is weakly expressed.

At a plasma concentration of 31 ± 20 nmol / L, raltegravir inhibited viral replication by 95% (inhibitory concentration 95% - IC ₉₅) in cell cultures of human T-lymphocytes that were infected with the HIV-1 H9IIIB variant adapted to cell cultures, when compared with the control virus-infected cell culture. At concentrations of the active substance from 6 to 50 nmol / L, IC ₉₅ was achieved in cultures of human mitogen-activated peripheral blood mononuclear cells infected with various primary clinical strains of HIV-1, including strains of 5 non-B subtypes, as well as strains resistant to HIV protease inhibitors and reverse transcriptase inhibitors.

During the analysis of a single cycle of infection, raltegravir inhibited infection induced by 23 HIV strains, which are 5 non-B subtypes and 5 circulating recombinant forms with IC ₅₀ - 5–12 nmol / L. Mutations of HIV-1 integrase that contribute to the emergence of viral strains resistant to raltegravir (developed in patients treated with the drug, or in vitro), predominantly contain substitutions at positions 148 (Q148 is replaced by H, K or R), 143 (Y143 is replaced by C, H or R) or 155 (N155 substitution for H), in combination with at least one additional mutation (for example, T97A, E92Q, L74M, G140A / S, E138A / K, V151I, S230R, G163R).

Recombinant viruses with the inclusion of one primary mutation (Q148H, K or R, or N155H) were characterized by a reduced ability to replicate and poor sensitivity to raltegravir in vitro. Secondary mutations of the virus led to a further decrease in sensitivity to the active substance, in some cases compensating for the weakened ability of the virus to replicate.

Mutations associated with the emergence of resistance to raltegravir can also induce the formation of resistance to another integrase chain transfer inhibitor, elvitegravir.

In a placebo-controlled clinical study in which healthy volunteers took part, a single dose of Isentress at a dose of 1600 mg did not affect the duration of the QTc interval, despite the fact that its maximum concentration (C _max) in blood plasma was 4 times more than with a single dose of 400 mg.

Pharmacokinetics

In adult patients, raltegravir is rapidly absorbed after oral administration on an empty stomach, the plasma C _max in the blood is observed approximately 3 hours later. The area under the concentration-time curve (AUC) and C _{max of the} substance increase in proportion to the dose in the dose range from 100 to 1600 mg. Values raltegravir content in plasma 12 hours after administration (C _12h) increased proportionally with dose in the dose range from 100 to 800 mg, and increased slightly less in a range from 100 to 1600 mg.

When using Isentress 2 times a day, the equilibrium state is observed for about 2 days after the start of the course. The AUC and C _max values confirm the absence or minimal accumulation of the substance, and the C _{12 h} value indicates an insignificant accumulation. When used as a drug raltegravir monotherapy 2 times a day, 400 mg of the geometric mean value for AUC in the range from 0 to 12 hours (AUC _0-12ch) was 14.3 mol / l × h, the value of C _12h - 142 nmol / l … The absolute bioavailability of the product has not been determined.

On average, 83% of raltegravir binds to blood plasma proteins in the concentration range from 2 to 10 μmol. In the course of preclinical studies, it was found that the active substance easily penetrated the placental barrier in rats, but did not pass through the blood-brain barrier (BBB) to a noticeable extent.

In two clinical trials involving patients infected with HIV-1 who received Raltegravir at a dose of 400 mg twice a day, it was quickly fixed in the cerebrospinal fluid. In the first study in the cerebrospinal fluid, the mean raltegravir level was 5.8% (range from 1 to 53.5%) of the corresponding level in blood plasma, and in the second study - 3% (range from 1 to 61%) from corresponding level in blood plasma. The medians of the established values were approximately 3–6 times lower than the levels of the free fraction of raltegravir in blood plasma.

According to the results of studies that used selective inhibitors to the isoform of the enzyme uridine diphosphate glucuronyl transferase (UDFGT), produced by expression of complementary DNA, UDFGT1A1 belongs to the main enzymes responsible for the formation of raltegravir glucuronide. According to these results, in humans, the main pathway of metabolic transformation of raltegravir is the glucuronidation process mediated by UDPGT1A1. The duration of the final phase of the half-life (T _1/2) of the substance is approximately 9 hours, and most of the AUC corresponds to the shorter α-phase of the apparent T _{1/2 of the} active substance, averaging 1 hour.

After oral ingestion of radiolabeled raltegravir, approximately 32% of the dose received is excreted by the kidneys and 51% through the intestines. In the feces, only raltegravir was detected, probably formed by hydrolysis of raltegravir glucuronide, which was eliminated in the bile. Raltegravir and raltegravir-glucuronide were detected in urine at 9 and 23% of the initial dose, respectively. The main circulating radioactive ingredient in blood plasma was raltegravir, accounting for an average of 70% of the total radioactivity, the remaining 30% were raltegravir-glucuronide.

Gender, body mass index (BMI) and racial-ethnicity of patients do not have a clinically significant effect on the pharmacokinetic parameters of Isentress and do not require dose adjustment.

In children under 2 years of age, the pharmacokinetics of the drug has not been studied.

For adolescents and children over 2 years old (chewable tablets) and over 6 years old (film-coated tablets), doses of raltegravir for the treatment of HIV-1 infection are recommended on the basis that its main pharmacokinetic parameters are comparable to those in adult patients receiving 2 times per day film-coated tablets at a dose of 400 mg.

Indications for use

Isentress is recommended for the treatment of HIV-1 infection in combination with other antiretroviral drugs:

• film-coated tablets: in adults, adolescents and children from 6 years of age and older with a body weight of at least 25 kg (dosage 400 mg) or with a body weight of at least 40 kg (dosage 600 mg);
• chewable tablets: in children aged 2–11 years, both previously receiving and not receiving antiretroviral therapy (ART).

Contraindications

Absolute:

• pregnancy and lactation;
• age up to 6 years and body weight up to 25 kg (400 mg) or body weight up to 40 kg (600 mg) - for film-coated tablets; age up to 2 years and body weight up to 7 kg - for chewable tablets;
• deficiency of sucrase / isomaltase, fructose intolerance, glucose-galactose malabsorption - for chewable tablets (contain sorbitol and fructose);
• lactose intolerance, glucose / galactose malabsorption or lactase deficiency - for film-coated tablets (contain lactose);
• phenylketonuria - for chewable tablets because they contain phenylalanine as a component of aspartame (0.05 mg at a dose of 25 mg and about 0.1 mg at a dose of 100 mg);
• hypersensitivity to any component of the drug.

Relative (take Isentress tablets with caution):

• severe liver failure;
• myopathy and rhabdomyolysis (including data in anamnesis), as well as conditions and factors that predispose to their development;
• simultaneous use with strong inducers of UDFGT1A1 (including rifampicin) or with antacids containing magnesium / aluminum; additionally for 600 mg - with tipranavir / ritonavir, atazanavir;
• depression, including the presence of suicidal ideation and behavior (recorded mainly in patients with a history of depression or psychiatric illness);
• old age - for film-coated tablets.

Isentress, instructions for use: method and dosage

Isentress tablets are used orally, in combination with other antiretroviral drugs. The reception time does not depend on the diet.

A doctor with sufficient experience in treating HIV infection should prescribe and conduct treatment with the drug.

Film-coated tablets

Film-coated tablets should be swallowed whole without breaking, crushing or chewing.

For adults, adolescents and children with a body weight of at least 25 kg, Isentress in a dosage of 400 mg is recommended to be taken 2 times a day, 1 tablet, the daily dose is 800 mg. If it is necessary to further switch to taking tablets at a dosage of 600 mg, patients, including children with a body weight of at least 40 kg, are prescribed a drug at a dose of 1200 mg - 2 tablets of 600 mg, taken 1 time per day.

If pediatric patients have difficulty swallowing coated tablets, consider switching them to Isentress chewable tablets.

Chewable tablets

The maximum permissible daily dose of chewable tablets is 300 mg 2 times a day. There have been no studies of this form of antiviral therapy in HIV-infected adults and adolescents aged 12 to 18 years.

Since the dosage forms of Isentress are not bioequivalent, chewable tablets should not be replaced with film-coated tablets at a dosage of 400 mg.

Recommended single doses ^{* of} chewable tablets for children aged 2 to 11 years, depending on body weight (with a frequency of administration 2 times a day):

• > 7, but <10 kg: 50 mg - ½ 100 mg tablet ¹;
• ≥ 10 but <14 kg: 75 mg - 3 tablets of 25 mg;
• ≥ 14 but <20 kg: 100 mg - 1 tablet of 100 mg;
• ≥ 20 but <28 kg: 150 mg - 1½ 100 mg tablets;
• ≥ 28 but <40 kg: 200 mg - 2 tablets of 100 mg;
• ≥ 40 kg: 300 mg - 3 tablets of 100 mg.

Notes

^* - dose recommendations for body weight are based on approximately 6 mg / kg / dose 2 times daily

¹ - chewable tablets at a dosage of 100 mg can be divided into two halves, however, such division should be avoided if possible

Patients should strictly follow the dosing schedule, since the dose of raltegravir must be changed as the child grows.

Adults and adolescents aged 12 years and older with a body weight of at least 25 kg are recommended to take Isentress in the form of film-coated tablets at a dosage of 400 mg.

Side effects

The following adverse reactions have been reported in clinical trials and are associated with varying degrees of likelihood with the use of Isentress or in combination with another ART:

• infectious and parasitic diseases: infrequently - folliculitis, upper respiratory tract infection, nasopharyngitis, genital herpes, herpes simplex, shingles, herpes infection, gastroenteritis, lymph node abscess, influenza, molluscum contagiosum;
• immune system: infrequently - hypersensitivity to the drug, immune recovery syndrome, hypersensitivity reactions;
• hematopoietic system and lymphatic system: infrequently - anemia, soreness of the lymph nodes, iron deficiency anemia, neutropenia, lymphadenopathy, thrombocytopenia ¹;
• metabolism: often - decreased appetite; infrequently - increased appetite, hyperphagia, hyperlipidemia, hyperglycemia, hypercholesterolemia, dyslipidemia, diabetes mellitus, cachexia, impaired fat metabolism, polydipsia;
• unspecified, benign and malignant neoplasms (including polyps and cysts): infrequently - skin papillomatosis;
• nervous system: often - headache, psychomotor hyperreactivity ², dizziness; infrequently - decreased sleep quality, drowsiness, tremor, tension headache, migraine, hypersomnia, dysgeusia, postural dizziness, impaired attention, memory disorder, carpal tunnel syndrome, hypesthesia, lethargy, paresthesias, peripheral neuropathy, cognitive disorders, amnesia;
• mental disorders: often - insomnia, unusual dreams, nightmares, depression, behavior disorder ²; infrequently - sleep disturbances, insomnia in the middle of the night, mood changes, anxiety, depressed mood, mental disorders, major depressive disorder, panic attacks, suicidal attempts, suicidal behavior ¹, suicidal ideation ¹ (especially if there is a history of psychiatric illness);
• organ of hearing and labyrinthine disorders: often - vertigo; infrequently - tinnitus;
• organ of vision: infrequently - decreased visual acuity;
• respiratory system, chest and mediastinal organs: infrequently - nasal congestion, epistaxis, dysphonia;
• cardiovascular system: infrequently - flushes of blood to the skin of the face with a feeling of heat, palpitations, arterial hypertension, ventricular premature beats, sinus bradycardia;
• liver and biliary tract: infrequently - hepatic steatosis, hepatitis, liver failure ¹, alcoholic hepatitis;
• genitals and mammary gland: infrequently - symptoms of menopause, gynecomastia, erectile dysfunction;
• kidneys and urinary tract: infrequently - nocturia, nephrolithiasis, nephritis, renal dysfunction, kidney cyst, renal failure, tubulointerstitial nephritis;
• skin and subcutaneous tissue: often - skin rash; infrequently - dry skin, acne, acne rash, alopecia, facial lipoatrophy, erythema, acquired lipodystrophy, lipoatrophy, lipohypertrophy, night sweats, hyperhidrosis, pruritus (local and generalized), prurigo, urticaria, pruritic rash, macular rash / macular other skin lesions, drug rash with eosinophilia and systemic symptoms (DRESS syndrome) ¹, Stevens-Johnson syndrome ¹;
• musculoskeletal system: infrequently - pain in the side, back pain, pain in the extremities, arthritis, arthralgia, myalgia, osteopenia, pain in the neck, tendonitis, osteoporosis, myopathy, polyarthritis, rhabdomyolysis ¹;
• digestive system: often - dyspepsia, nausea, vomiting, bloating / abdominal pain, flatulence, diarrhea; infrequently - soreness when swallowing, dry mouth, belching, pain in the upper abdomen, discomfort in the epigastric region / abdomen, soreness in the abdomen, constipation, a feeling of discomfort in the anus, erosive duodenitis, glossitis, gingivitis, gastroesophageal reflux peptic ulcer, acute pancreatitis, rectal bleeding;
• intoxication, injury and complications of manipulation: infrequently - involuntary overdose;
• laboratory and instrumental data: often - an increase in the activity in plasma of aspartate aminotransferase (AST), alanine aminotransferase (ALT), pancreatic amylase and lipase, an increase in triglycerides and the number of atypical lymphocytes; infrequently - a decrease in the absolute number of plasma neutrophils; increased activity in plasma of creatine phosphokinase (CPK), alkaline phosphatase (ALP), decrease in albumin content; an increase in the level of bilirubin, creatinine, cholesterol (CS), urea nitrogen, glucose (including those determined on an empty stomach), low density lipoprotein cholesterol (LDL cholesterol), high density lipoprotein cholesterol (HDL cholesterol); an increase in the value of the international normalized ratio (INR), a decrease in the number of leukocytes and platelets in the blood, the presence of glucose and erythrocytes in the urine; increase / decrease in body weight,increase in waist circumference;
• general disorders: often - fever, asthenia, weakness; infrequently - chills, chest discomfort, malaise, anxiety, an increase in adipose tissue, facial edema, pain, peripheral edema, submandibular neoplasm.

Notes

¹ - side effects not caused by the use of Isentress, which were recorded in the post-registration period and were not detected during clinical trials

² - drug-related adverse events noted in one child: behavior disorder and psychomotor hyperreactivity of the III degree, insomnia

According to the data of clinical studies, when taking raltegravir in recommended doses in combination with other antiretroviral drugs in HIV-1 infected children and adolescents 2–18 years old, the severity, frequency and type of side effects caused by taking Isentress were the same as in adults.

Overdose

Against the background of an overdose of Isentress, no specific symptoms were recorded. When healthy volunteers were taking raltegravir in a regimen of 1600 mg once a day and 800 mg twice a day, the therapy was well tolerated without any signs of toxicity. During phase II / III studies, a single dose of the drug in a daily dose of 1800 mg did not show toxic effects. According to the available data, it can be concluded that the drug is well tolerated when used twice a day in doses up to 800 mg, as well as in combination with drugs that increase its exposure by 50–70% (atazanavir, tenofovir, etc.). Since raltegravir has a wide therapeutic range, its toxic potential is rather limited due to overdose.

If an overdose is suspected, standard supportive measures are recommended, such as evacuation of the unadsorbed drug from the digestive tract, monitoring of vital signs (including ECG), symptomatic therapy. The rate of excretion of raltegravir during dialysis has not been established.

special instructions

Patients should be made aware that current combination ART does not cure HIV infection and does not prevent HIV transmission through sexual contact or with blood to others. During the period of treatment with Isentress, appropriate safety measures must be continued to prevent transmission of the virus. During therapy, it is extremely important to be under the supervision of a specialist, since during this period infections or other undesirable conditions characteristic of HIV-infected patients (opportunistic infections) may still occur.

Raltegravir has a relatively low genetic barrier to the emergence of resistance, therefore, in order to enhance the effect of therapy and reduce the risk of developing resistance to Isentress, it should, if possible, be used in combination with two other active antiretroviral agents.

The physician is required to be informed of the occurrence of any unusual symptoms, as well as the persistence or aggravation of any known adverse reaction.

In HIV-infected patients with a severe form of immune deficiency, at the initial stage of combined ARVT, the so-called immune reconstitution syndrome may occur, which is an inflammatory reaction to asymptomatic current / residual opportunistic infections - disseminated / focal mycobacterial infections; Pneumocystis pneumonia caused by Pneumocystis jirovecii; cytomegalovirus retinitis and others. This complication can increase the severity of existing symptoms and lead to an aggravation of the clinical condition. As a rule, the appearance of such a reaction is possible during the first weeks or months after the start of combination treatment. Any inflammatory symptom should be assessed and treated if necessary.

Against the background of the development of the immune recovery syndrome, the appearance of such autoimmune disorders as Graves' disease is possible. However, the development of such phenomena can be recorded many months after the start of the course of treatment.

Despite the fact that the etiology of osteonecrosis is considered multifactorial (including severe immunodeficiency, alcohol consumption, GCS therapy, high BMI), there are reports of cases of this complication, especially with long-term combined ART and / or in the late stages of HIV infection. If you experience symptoms such as limited mobility, stiffness, or pain in your joints, you should consult your doctor immediately.

If signs / symptoms of a hypersensitivity reaction or severe dermatological reactions appear, which may include: weakness, general malaise, rash accompanied by fever or severe skin rash, blistering of the skin, muscle / joint pain, damage to the mouth, swelling of the face, conjunctivitis, eosinophilia, hepatitis, angioedema, it is necessary to urgently stop treatment with Isentress and other drugs that can cause such conditions. In such cases, it is required to carefully monitor the clinical status, including the level of hepatic aminotransferases, and conduct appropriate treatment. Untimely refusal of therapy with a drug or other means, presumably associated with these complications, after the onset of a severe rash, can lead to the development of life-threatening reactions.

Influence on the ability to drive vehicles and complex mechanisms

The influence of Isentress on the speed of psychomotor reactions and the ability to concentrate has not been studied. Since during therapy, blurred vision, drowsiness and dizziness may occur, patients should drive vehicles and work with other complex equipment with extreme caution.

Application during pregnancy and lactation

Controlled studies of the efficacy and safety of using Isentress in pregnant women have not been carried out, therefore, taking the drug during pregnancy is contraindicated.

There are no data on the intake of raltegravir in human breast milk. However, in the process of studies on animals, the penetration of the active substance into milk in lactating rats was revealed - when raltegravir was used in a daily dose of 600 mg / kg, its level in milk exceeded the plasma level by an average of 3 times.

Breastfeeding is not recommended for HIV-infected mothers to avoid transmission of the virus to babies, Isentress should not be used during lactation.

Pediatric use

Isentress chewable tablets are contraindicated for children under 2 years of age with a body weight of less than 7 kg. Taking film-coated tablets is contraindicated in children under 6 years of age: at a dose of 400 mg - with a child's body weight less than 25 kg, at a dose of 600 mg - less than 40 kg.

With impaired renal function

Patients with functional impairment of the kidneys do not need individual selection of Isentress doses. Due to the fact that the effectiveness of dialysis with raltegravir has not been established, it is not recommended to take the drug on the eve of a dialysis session.

For violations of liver function

The safety and efficacy of drug treatment in patients with severe concomitant liver diseases have not been established. In the presence of severe hepatic impairment, Isentress should be taken with extreme caution. In patients with liver dysfunction, including chronic hepatitis, against the background of combined ARVT, the incidence of liver dysfunction increases, as a result of which patients in this risk group should be monitored in accordance with standard practice. If they develop signs of worsening liver disease, it is necessary to consider temporarily interrupting or discontinuing the drug.

Patients with chronic hepatitis B or C who are also receiving combined ARVT have an increased risk of severe and potentially life-threatening adverse liver reactions.

With the presence of mild and moderate functional disorders of the liver, there is no need to adjust the dose of Isentress.

Use in the elderly

Since there is limited information on the use of raltegravir in patients over 65 years of age, treatment with the drug in patients of this age group should be carried out with caution (for doses of 400/600 mg). Elderly patients do not need to change the dose of Isentress.

Drug interactions

The effect of Isentress on the pharmacokinetic parameters of drugs that are substrates of P-glycoprotein or enzymes CYP2B6, CYP1A2, CYP2C8, CYP2D6, CYP2C9, CYP2C19, CYP3A or CYP3A4 is not detected, since raltegravir does not belong to the cytochrome ₄₅₀ system of substrates, as well as P-glycoprotein inhibitors. -glycoprotein-mediated transport.

Pharmacokinetic interaction of raltegravir with other drugs / substances:

• maraviroc, etravirine, tenofovir, hormonal contraceptives, midazolam, methadone: there is no clinically significant effect of raltegravir on the pharmacokinetics of these drugs; dose changes for these drugs are not required;
• Darunavir: there is a slight decrease in the plasma level of this substance in the blood, which is not considered clinically significant;
• rifampicin (strong inducers of UDPGT1A1): the concentration of raltegravir in the blood plasma decreases; at this concentration, care must be taken, since raltegravir is metabolized mainly with the participation of UDFGT1A1; the effect on the effectiveness of Isentress has not been established, if such a combination is necessary in adults, it is possible to increase the dose of raltegravir by 2 times, however, the combination of the latter in a daily dose of 1200 mg with rifampicin is not recommended; data on the combined use of raltegravir and rifampicin in patients under 18 years of age are not available;
• etravirine, nevirapine, efavirenz, GCS, rifabutin, pioglitazone, St. John's wort (inducers UDFGT1A1): it is possible to use these substances in combination with raltegravir in recommended doses;
• atazanavir, saquinavir, tenofovir, indinavir (inhibitors of UDFGT1A1): the plasma concentration of raltegravir in the blood increases; the combination of the latter at a dose of 1200 mg with atazanavir is not recommended; dose changes of Isentress are not required when combined with atazanavir and / or tenofovir;
• antacids containing bivalent metal ions (aluminum / magnesium): it is possible to reduce the absorption of raltegravir by chelation, which causes a decrease in the plasma concentration of the drug in the blood; these combinations are not recommended;
• antacids containing calcium carbonate: the plasma content of raltegravir decreases, but the interaction is not clinically significant; it is not recommended to take Isentress with these drugs at a dose of 1200 mg per day; when used in a daily dose of 800 mg, no correction is performed;
• famotidine, omeprazole, cimetidine, ranitidine (drugs that increase the pH of gastric juice, blockers of H ₂ -histamine receptors): the absorption rate of raltegravir and, as a consequence, the level of its concentration in blood plasma increases slightly; Isentress dose changes are not required.

Pharmacokinetic characteristics of raltegravir are distinguished by significant inter- and intraindividual variability. The information given on drug interactions with other agents is based on geometric averages. It is definitely impossible to foresee the reaction of an individual patient.

Analogs

Isentress's analogues are Abacavir, Darunavir, Atazanavir, Ziagen, Combivir, Zidovudine, Kemeruvir, Tenofovir, Nevirapine, Epivir, etc.

Terms and conditions of storage

Isentress tablets, film-coated, should be stored out of the reach of children, at temperatures up to 25 ° C.

The shelf life is 2.5 years.

Isentress chewable tablets should be stored with a moisture-absorbing agent in a tightly sealed original package, in a dry place out of the reach of children, at temperatures up to 30 ° C.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Isentress

According to a few reviews, Isentress, according to patients and specialists, is a fairly safe and effective antiviral drug used to treat HIV-1 infection as part of combination therapy. Isentress rapidly reduces viral load and increases the level of immunocompetent CD-4 cells.

The disadvantages of the drug include a low threshold of resistance, the development of side effects and its high cost.

The price of Isentress in pharmacies

Isentress price for 60 pcs. in the package can be:

• chewable tablets (100 mg) - 9,900 rubles;
• film-coated tablets (400 mg) - 13,500 rubles.

Isentress: prices in online pharmacies

Drug name Price Pharmacy

Isentress 400 mg film-coated tablets 60 pcs. 19500 RUB Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!