Darunavir - instructions for use, dose, side effects, contraindications

Competitively inhibits the protease of human immunodeficiency virus, in connection with which the formation of inactive virus particles that are not capable of infection of new cells.

Pharmacokinetics:

Bioavailability is 37%. It binds to plasma proteins by 82%. Biotransformation occurs in the liver, the half-life of 15 hours, is eliminated through the gastrointestinal tract - 79.5% (41.2% - in unchanged form), kidneys - 13.9% (7.7% - unchanged).

Indications:

Human immunodeficiency virus of the first and second types (in combination with low-dose ritonavir and other antiretroviral drugs).

ICD-10

I.B20-B24.B24 Disease caused by human immunodeficiency virus [HIV], unspecified

Contraindications:

Age under 18, hypersensitivity, severe hepatic insufficiency, simultaneous use with drugs, the clearance of which is predominantly determined CYP3A4, and an increase in plasma concentration is associated with the occurrence of serious and life-threatening side effects (narrow therapeutic range). These drugs include astemizole, alfuzosin, sildenafil (used for the therapy of pulmonary arterial hypertension), terfenadine, midazolam (orally), rifampicin, triazolam, cisapride, pimozide, sertindole, preparations containing ergot alkaloids (ergotamine, dihydroergotamine), preparations containing St. John's wort extract, a combination lopinavir + ritonavir, simvastatin, lovastatin, quetiapine.

Carefully:

Chronic liver diseases (mild and moderate), hypersensitivity to sulfonamides, simultaneous administration with quinidine, amiodarone, lidocaine, bepridilom, dexamethasone. Pregnancy and lactation.

Pregnancy and lactation:

Category FDA - B. Adequate and well-controlled studies on humans have not been conducted. The combination darunavir + ritonavir can be given to pregnant women only in cases where the expected benefit of therapy for the mother exceeds the potential risk to the fetus. It is not known whether darunavir with human breast milk. Given the possibility of transferring human immunodeficiency virus with breast milk, as well as the risk of serious side effects in infants, associated with exposure to darunavir, HIV-infected women receiving darunavir, should refrain from breastfeeding.

Dosing and Administration:

Orally. Admission 600 mg 2 times a day, with a joint admission with other drugs, the dose needs to be adjusted.

Side effects:

From the musculoskeletal system: pain in the extremities, arthralgia, myalgia, osteoporosis, osteopenia, rhabdomyolysis.

From the side of the urinary system: polyuria, nephrolithiasis.

From the skin: lipoatrophy, drug dermatitis, eczema, folliculitis, hyperhidrosis, alopecia, allergic dermatitis, erythema multiforme, toxicermia, rash.

From the cardiovascular system: myocardial infarction, increased blood pressure, tachycardia.

From the respiratory system: hiccough, shortness of breath, cough.

From the nervous system: anxiety, hypesthesia, paresthesia, transient ischemic attack, nightmares, disorientation, confusion, dizziness, emotional lability.

Other: gynecomastia, fever, chills, night sweats, asthenia, peripheral edema, opportunistic infections, changes in blood counts.

Overdose:

Not described, treatment is symptomatic.

Interaction:

Simultaneous reception with such drugs as disopyramide, quinine, fentanyl, alfentanil - increases the concentration in the blood of the latter.

Simultaneous reception with antiarrhythmic drugs is contraindicated.

Simultaneous reception with cisapride, astemisole, ergot derivatives, pimozide, triazolam, terfenadine, midazolam leads to inhibition of the metabolism of the latter.

Simultaneous reception with benzodiazepines leads to an increase in their concentration in the blood.

Simultaneous reception with blockers of slow calcium channels leads to an increase in the concentration of these drugs in the blood.

Simultaneous reception with zalcitabine and zidovudine leads to a change in their pharmacokinetic parameters.

Simultaneous reception with delavirdine leads to a fivefold increase in the concentration of the latter.

With simultaneous administration with warfarin, there is a violation of the concentration of warfarin.

Simultaneous administration with inhibitors of HMG-CoA reductase leads to a risk of myopathy and rhabdomyolysis.

Special instructions:

During treatment, careful monitoring of all clinical blood counts, including quantities Cd4 + lymphocytes, blood glucose concentrations, control of viral load and triglyceride concentration.

Influence on the ability to drive a car and drive machinery.

Studies of the effect of the drug on the ability to drive vehicles and work with mechanisms have not been conducted. Some of the side effects of the drug, such as dizziness, can adversely affect the ability to drive and perform potentially dangerous activities requiring increased concentration and speed of psychomotor reactions. When dizziness occurs, you should refrain from performing these activities.

Instructions

Darunavir (Darunavirum)