Efavirenz, Mechanism of Efavirenz, Metabolism ,side
Efavirenz is used to treat and prevent the growth of HIV virus .it comes under the category of antiretroviral medicine. This medicine is not cure the AIDS but it can stop the growth of virus. This is discrease the complication of HIV virus and helps to live to better life.
To prevent the spreading the deasease form you must take care by some rules
Don’t share your personal things to other person like razors , toothbrushes, needle and syringe , this things are may contact with your blood and having the chances of spreading of virus.
Use the condoms at the time of sex or any other activity.
Efavirenz Side effects
Side effect of this medicine is common like nausea , headache , feeling tired and sleeping troble. Some serious side effect like depression ,liver problems and seizures and sucide thought are come to the patients. During the pregnancy time this medicine is is avoided .
This medicine is approved by U.s in the 1998. And this medicine having more effective to combination of other regimen.
Efavirenz mechanism of action
Efavirenz directly inhibits HIV 1 virus . it is also noncompetitive inhibitor. But it is not inhibit the HIV 2 virus. This medicine is increase resistance power to NNRTIs (Non neucleoside reverse transcriptase ) which is a NNRTIs category medicine .
It is always given to combine medicine for the effective action . if the patient failing to treatment of HIV /AIDS with NNRTI category drug don’t give another medicine of NNRTI medicine .
When viral capsid enters into T-cell or other cell which is mainly containg CD4 substrate the viral capsids are collapsed . HIV Virus genetic material are enters in to host cell . this genetic material contain R-RNA of virus and some other enzyme .amoung this enzyme Reverse transcriptase is present which is helps to convert the R-RNA of virus to single strand DNA . so virus can replicate properly. In this stage Efaverinz are block the reverse transcriptase to attached the active side of Reverse transcriptase enzyme .so the enzyme don’t show the action of conversion of R-RNA to DNA. So growth of virus is gradually stop.
|Efavirenz 3D structure|
Oral absorption of efaverinz is aprox 50% . T1/2 of efaverinz is 48 hours. Efaverinz is metabolized by enzyme CYP2B6 and partially by the enzyme CYP3A4. Both the are cytochrome inducer category. Most interesting is this medicine induced the self metabolized enzyme. So the metabolism of this medicine is descrease when it take orally.
If the patients are treatment with nevirapin it may developed the tuberoculosis. So doctor advice to take Efaverinz instead of nevirapin.
Dose of efavirenz
Efavirenz is avalabile in the solid oral dosage form which is capsule and tablets. Capsule which is present 50 mg and 200 mg and in the tablet 600 mg content .
In the HIV 1 infection this medicine is use 600 mg for better effect with other medicine like protease inhibitor or NRTIs.
For mentenance dose you can take with voriconazole dose increase dose to 400 mg and descrease efavirenz to 300 mg per day.if you take the dose rifampicin then you take efavirenz 800 mg per day.
This medicine is show the better effect when you take I the empty stomach before 1 hour taking food in the night. If you forget to take medicine don’t take the extra dose I the next time .it produce the over dose effect.
Some codidition you don’t take efavirenz
If you are allergic reaction to efavirenz, you don’t take this medicine consult the doctor for this condition .
If you have any liver deasease you don’t take this medicine.
If you take the medicine like astemizole , terfenadine, bepridil, cisapride, cisapride , ergot alkaloids , midazolam ,triazolam , pimozide.
Efavirenz is taken if other medicine are not act against HIV virus, it ;can take with any other medicine which is act against HIV virus .
Most important thing which is discus with your doctor before taking EFAVIRENZ
If you have any metal illness , depression or any narcotic addition,if you fell any depression you can contact you doctor .
If you treated with anticonvunlsant treatment such as phenobarbital ,phenoytoin , carbamazipin etc.
If you have any liver problem you discuss with doctor before taking this medicine.
If you stop the this medicine discus with your doctor for any side effect.
Storage condition of efavirenz
This medicine is store in the room temperature, which is 20°C to 25°C. Keep this medicine away form the children for the safety purpose. If the medicine box or pack is unseal then don’t take this medicine . container pack is containing desiccant which is help prevent the moisture. Before taking this medicine check the expiry of box
Price of efavirenz
Efavirenz is present in the market in various brand name like sustiva, stocrin, fliginase , adiva , avifanz , efamat, Efavir , Efaverinz,Efcure, Efrin, Estiva.
In India EFAVIR 600 mg tablets price is 1854 rupees for 30 tablets manufacture by cipla ltd. And EFAMAT 600 MG tablet 1990 rupees for 30 tablet manufacture by mylan ltd.
Efavirenz is 14th approved medicine use for HIV 1 virus approved by FDA on September 21 1998. Mylan is manufacture generic tablets in feb 17 2016 approved by FDA.
Now a days efavirenz is marked by various company such as Aurobindo pharma ltd, Cipla ltd, hetero pharmaceutical , and mylan pharmaceutical.