EMTRICITABINE-RILPIVIRINE-TENOFOVIR



Complera


Indication:


This medicine is used to help control HIV infection. It helps to decrease the amount of HIV in your body so your immune system can work better. This lowers your chance of getting HIV complications (such as new infections, cancer) and improves your quality of life. Emtricitabine and tenofovir belong to a class of drugs known as nucleoside reverse transcriptase inhibitors (NRTIs). Rilpivirine belongs to a class of drugs known as non-nucleoside reverse transcriptase inhibitors (NNRTIs).



Brand name:Complera

Active Ingeridents:Emtricitabine-Rilpivirine-Tenofovir

Company Name: Gilead

Package:30 Tablets

Strength :Emtricitabine 200mg + Rilpivirine 25mg + Tenofovir 300mg

Mechanism of action:


Rilpivirine:

Rilpivirine is an NNRTI which binds to reverse transcriptase which results in a block in RNA and DNA- dependent DNA polymerase activities. One such activity is HIV-1 replication. Intracellular phosphorylation is not necessary for its antiviral activity. Because of the structure of rilpivirine is flexible around the aromatic rings, the molecule can have multiple conformations so that can bind to residues in the reverse transcriptase enzyme which have a lower mutation rate.

Emtricitabine

Emtricitabine works by inhibiting reverse transcriptase, the enzyme that copies HIV RNA into new viral DNA. Emtricitabine is a synthetic nucleoside analogue of cytidine. It is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate, which is responsible for the inhibition of HIV-1 reverse transcriptase. It competes with the natural substrate deoxycytidine 5'-triphosphate and incorporates into nascent viral DNA, resulting in early chain termination. Therefore emtricitabine inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate deoxycytidine 5'-triphosphate and by its incorporation into viral DNA. By inhibiting HIV-1 reverse transcriptase, emtricitabine can help to lower the amount of HIV, or "viral load", in a patient's body and can indirectly increase the number of immune system cells (called T cells or CD4+ T-cells). Both of these changes are associated with healthier immune systems and decreased likelihood of serious illness.

Tenofovir:

Tenofovir inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination. Specifically, the drugs are analogues of the naturally occurring deoxynucleotides needed to synthesize the viral DNA and they compete with the natural deoxynucleotides for incorporation into the growing viral DNA chain. However, unlike the natural deoxynucleotides substrates, NRTIs and NTRTIs (nucleoside/tide reverse transcriptase inhibitors) lack a 3'-hydroxyl group on the deoxyribose moiety. As a result, following incorporation of an NRTI or an NtRTI, the next incoming deoxynucleotide cannot form the next 5'-3' phosphodiester bond needed to extend the DNA chain. Thus, when an NRTI or NtRTI is incorporated, viral DNA synthesis is halted, a process known as chain termination. All NRTIs and NtRTIs are classified as competitive substrate inhibitors.


Dosage and Administration:


Use Complera (Emtricitabine/ Rilpivirine/ Tenofovir) as directed by your doctor. Check the label on the medicine for exact dosing instructions.

  • An extra patient leaflet is available with Complera (Emtricitabine/ Rilpivirine/ Tenofovir). Talk to your pharmacist if you have questions about this information.

  • Take Genvoya Complera (Emtricitabine/ Rilpivirine/ Tenofovir)by mouth with food.

  • If you are also taking an antacid (eg, that contains magnesium, aluminum, calcium), take it at least 2 hours before or 4 hours after you take Complera (Emtricitabine/ Rilpivirine/ Tenofovir).

  • Ask your health care provider any questions you may have about how to use Complera (Emtricitabine/ Rilpivirine/ Tenofovir).


Side effects:


All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Back pain; cough; darkened skin color on the palms of hands or soles of feet; diarrhea; dizziness; headache; indigestion; joint pain; loss of appetite; mild stomach pain or discomfort; nausea; nose or throat irritation; skin discoloration (small spots or freckles); strange dreams; tiredness; trouble sleeping; vomiting; weakness.


Precaution:


Before taking this medication, tell your doctor or pharmacist if you are allergic to emtricitabine, rilpivirine, or tenofovir; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.


Store:


Store Complera (Emtricitabine/ Rilpivirine/ Tenofovir) at 77 degrees F (25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store away from heat, moisture, and light.Do not use Complera (Emtricitabine/ Rilpivirine/ Tenofovir) if the seal over the bottle opening is broken or missing. Keep Complera (Emtricitabine/ Rilpivirine/ Tenofovir) in its original container and keep the container tightly closed. Keep Complera (Emtricitabine/ Rilpivirine/ Tenofovir) out of the reach of children and away from pets.



WARNING:


Complera (Emtricitabine/ Rilpivirine/ Tenofovir) is a prescription drug and should be used under proper medical guidance and advice. The information provided here is for general educational purposes only and does not constitute medical or pharmaceutical advice which should be sought from qualified medical and pharmaceutical advisers.