Darunavir is a 1-type HIV protease inhibitor (HIV-1). The drug selectively inhibits the cleavage of polyproteins Gag-Pol HIV in virus-infected cells, preventing the formation of full-fledged viral particles. Darunavir strongly binds to HIV-1 protease, is resistant to mutations that cause resistance to protease inhibitors. Darunavir does not inhibit any of the 13 human cell proteases studied.
Darunavir user’s manual
The drug is taken orally during a meal. The drug should always be prescribed in combination with ritonavir at a dose of 100 mg as a remedy to improve its pharmacokinetic characteristics, as well as in combination with other antiretroviral drugs. For adults, the recommended dose is 600 mg 2 r/day in combination with ritonavir at a dose of 100 mg 2 times daily.
A combination with calyx (lopinavir + ritonavir) is not recommended because of a decrease in the concentration of darunavir in plasma by more than 50%. It should not be combined with rifampicin, carbamazepine, diphenin, and phenobarbital, amiodarone, lidocaine, is incompatible with rifampicin, terfenadine, cisapride, ergot alkaloids (especially ergotamine), St. John’s Wort preparations (neurastin, gellarium, deprim). It may be necessary to reduce the dose of ketoconazole and increase the dose of rifabutin. It is not prescribed together with statins (simvastatin, etc.)
There are no clinically relevant interactions with doltegravir. With simultaneous application of dolutegravir reciprocal changes in dose is not required.
From the nervous system: A headache.
Mental disorders: unusual dreams.
On the part of the digestive system: pain in the abdomen, acute pancreatitis, diarrhea, dyspepsia, flatulence, nausea, vomiting, increased activity of ALT, AST, APF, acute hepatitis.
From the musculoskeletal system: myalgia, in patients receiving protease inhibitors, especially in combination with non-nucleoside reverse transcriptase inhibitors, an increase in the level of CK, myositis; rarely rhabdomyolysis.
From the metabolism: anorexia, diabetes.
From the immune system: a syndrome of immune reactivation.
From the side of metabolism: increase in the content of TG, total cholesterol, LDL cholesterol, glucose, pancreatic lipase, pancreatic amylase.
Infections: In HIV-infected patients with severe immunodeficiency during the initial combination antiretroviral therapy, inflammatory responses to asymptomatic or residual opportunistic infections are possible.
Common reactions: asthenia, fatigue.
The combination of Darunavir/ritonavir can be given to pregnant women only when the expected benefit of therapy for the mother exceeds the potential risk to the fetus.
It is not known whether darunavir is excreted in human milk. Given the possibility of HIV transmission in breast milk, as well as the risk of serious side effects in infants related to the effects of darunavir, HIV-infected women receiving darunavir should refrain from breastfeeding. Use with caution in patients with impaired liver function, with allergies to sulfonamides (because darunavir contains a sulfonamide group).
Patients should be informed that modern antiretroviral drugs do not cure HIV infection and do not prevent the transmission of HIV. Patients should explain the need for appropriate precautions.
Keep the drug in a dry place, protected from sun and inaccessible to children, at a temperature of 15 to 30 ° C. Date of manufacture and shelf life are indicated on the packaging.