Darunavir is a drug sold under the trade name Danavir 300mg and which evacuate anti-retroviral activity. Depends upon appearance of anti-viral medicine resistance that occurred during single use of Danavir, the drug administered by consolidated with other anti-retroviral drugs. Danavir 300mg is belongs to HIV protease inhibitor, required for the treatment of AIDS & HIV infections.
Danavir 300mg concomitant use with Cobicistate or Ritonavir or other antiretroviral indicated for the treatment of HIV-1 infection in adult patients. The Danavir 300mg uses is based on two criteria,
- The levels of Analyzing of Plasma HIV-1 RNA
- The count of CD4+cells
Danavir 300mg with Ritonavir consolidation is indicated for the treatment of HIV-1 infection in pediatric patients.
MECHANISM OF ACTION
Darunavir is drive out an anti-retroviral effect by prohibiting the protease enzyme which is needed for HIV viral multiplication, Dimerization and catalytic effect of HIV-1 protease also forbidden.
In virus infected cells, darunavir includes in inhibits the separation of HIV encoded Gag-pol polyproteins, thus the prevention which blocks the production of mature infectious virus particle.
Darunavir has molecular affability, so it can easily adapt for changing shape of protease enzymes.
While Danavir combine with Ritonavir will produce Tmaxof approx. 2.5-4 hrs The drug bioavailability is 37% and 82% of Danavir 300mg and ritonavir 100mg.
The human plasma protein bound is 95%.
Moreover, Danavir 300mg go through oxidative metabolism by CYP3A.
After monotherapy or Co administration with Ritonavir will eliminated approx. feces79.5% and in urine 13.9%
DOSAGE AND ADMINISTRATION
In general dose 600mg (2 dose of 300mg) taken twice in a day (BD) with food in oral administration. In adult patients the treatment for no Danavirresistance along withsubstitutions is 800mg DanavirOD with Ritonavir OD (once daily) with food. Danavir 600mg combination with Ritonavir 100mg BD with food provide treatment for at least one Danavirresistance associated substitution is.
Pediatric age of 3 to less than 18 years
In pediatric patients, Danavirshould not be used as single dosing for daily.
Dose recommendation should be based on weighing at least 10kg but less than 15 kg;
Greater or equal to 10kg to less than 11kg: The prescribed dose is 200mg of Danavirwith 32mg of ritonavir
Greater or equal to 11kg to less than 12 kg: The prescribed dose is 220mg of Danavirwith 32mg of ritonavir
Greater or equal to 12kg to less than 13kg: The prescribed dose is 240mg of Danavirwith 40mg of ritonavir
Greater or equal to 13kg to less than 14kg: The prescribed dose is 260mg of Danavirwith 40mg of ritonavir
Greater or equal to 14kg to less than 15kg: The prescribed dose is 280mg of Danavirwith 48mg of ritonavir.
Dose recommendation for weighing at least 15kg
≥ 15kg to <30kg: 375mg of Danavirwith 50mg ritonavir
≥30kg to <40kg: 450mg of Danavirwith 60mg of ritonavir
≥40kg: 600mg of Danavirwith 100mg of ritonavir
Common side effects
Mild nausea, Stomach ache, Insomnia, Itching and rashes, Change in body shape (fat).
Serious side effects
Signs of allergic reaction like Hives, Dyspnea, Swelling of (face,lips,throat,tongue), Severe hepatomegaly with steatosis, Chest discomfort, Wheezing, Cold sore, increased heart rate, Lumbar pain
Darunavir is a sulfonamide moiety, use with cautiously if patients are allergy to sulfonamide.
Due to Drug interactions
Some drug – drug interaction may cause severe life threatening conditions. Avoid the combinational therapy.
In protease inhibitor therapies, there is a chance of getting increased bleeding condition leads to skin hematomas & hemarthrosis in patients suffered with hemophilia type A or B Diabetes
Increasing blood glucose level during the Danavir 300mg therapy is a major adverse effect. Monitor the patient’s glucose level during the treatment periodically.
Redistribution of fat
The major adverse risk of this condition is obesity. This may generally occur in anti-retroviral treatments.
Immune reconstitution syndrome
This may occur in Danavir 300mg therapy; to overcome the problem therapy should be discontinued.
Combination of Danavirwith ritonavir are mostly based on CYP3A for clearance and increased plasma concentration causes life threatening reactions similarly with interaction with Alfuzosin cause hypotension
Concomitant use with Dihydroergotamine causes peripheral vasospasm sand ischemia.
Danavir combination withCisapride andpimozide causes cardiac arrhythmias Interaction of Midazolam and triazolam causes respiratory depression.