Tenofovir ester reports

- Dec 18, 2017 -

Tenofovir ester reports

basic situation 

This product is a new type of nucleotide reverse transcriptase inhibitors. The reverse transcriptase is inhibited in a manner similar to nucleoside reverse transcriptase inhibitors and therefore has potential anti-HIV-1 activity. Tenofovir disoproxil, the active ingredient of tenofovir, inhibits viral polymerase by binding directly and competitively to natural deoxyribose substrates and terminates the chain by inserting DNA.

Chinese common name: tenofovir dipivoxil

Alias: Tenofovir, Tenofovir disoproxil fumarate

English name: Tenofov ir Disoprox

The nature of the drug: prescription drug indications for the treatment of HIV, HBV infection.

This product and other reverse transcriptase inhibitors for HIV-1 infection, the therapeutic pharmacokinetics of hepatitis B Tenofovir hardly absorbed through the gastrointestinal tract, so the esterification, salt, become tenofovir disoproxil Magnesium acid salt. Tenofovir disoproxil is water-soluble and can be quickly absorbed and degraded to the active substance tenofovir, which is then converted to tenofovir disoproxil, the active metabolite of tenofovir. Ten to two hours after administration of tenofovir for blood peak. Tenofovir and food service bioavailability increased by about 40%.

 

Tenofovir disoproxil phosphate intracellular half-life of about 10h, can be administered once a day. Since this drug is not metabolized by the CYP450 enzyme system, there is little likelihood that the drug will interact with other drugs. The drug is mainly excreted through the glomerular filtration and active tubule transport system, about 70% to 80% of the prototype urine excreted. Usage and dosage Oral daily 1, each 300mg, and food with the service.

Adverse reactions 

1. General weakness

2. Gastrointestinal reactions Light to moderate gastrointestinal discomfort, common diarrhea, abdominal pain, loss of appetite, nausea, vomiting and flatulence, pancreatitis.

3. Metabolic hypophosphatemia (1% incidence); Fat accumulation and redistribution, including concentric obesity, buffalo back, peripheral thinning, breast enlargement, Cushing syndrome.

4. May cause lactic acidosis, hepatomegaly associated with steatosis and so on.

5. Nervous system dizziness, headache.

6.Breathing system breathing difficulties.