Peramivir Sodium Chloride Injection

Peramivir is a cyclopentane anti-influenza virus drug that can bind to the active site of influenza virus neuraminidase and has inhibitory activity against human influenza A and B viruses. Biochemical analysis showed that peramivir could inhibit the neuraminidase activity of several influenza A and B virus strains, with a median ICso value of 0.2nM (0.09~1.4nM, n=15) for influenza A virus strains, a median ICco value of 1.3nM (0.06~11nM, n=8) for influenza B virus strains, and an ICso value range of 0.06~0.26nM for 2009 HINIA influenza virus strains (swine flu). Antiviral activity: The antiviral activity of peramivir against laboratory virus strains and clinically isolated virus strains was investigated in cell culture experiments. The ECs0 value for seasonal influenza A HIN1 strains was 1μM (0.09~21μM, n=5), the ECso value for influenza A H3N2 strains was 0.07μM (0.01~0.16μM, n=12), and the ECso value for influenza B strains was 2.2μM (0.06~3.2uM, n=5). The relationship between antiviral activity in cell culture, neuraminidase inhibitory activity, and sustained influenza virus replication in humans has not been established. Limited biochemical analysis, cell culture, and animal model data show that the antiviral activity of peramivir and oseltamivir is synergistic. There are no data showing that peramivir has a synergistic effect with zanamivir. In the murine influenza A virus infection model, the combination of peramivir and oseltamivir showed enhanced antiviral activity, but its clinical significance is unclear. Resistance: There are no clinical data on peramivir resistance. In cell culture studies, peramivir-resistant influenza virus A/WSN/33 (HIN1) was characterized by the H275Y group, and clinical isolates of type A HIN1 expressing the oseltamivir-resistant H275Y group also showed resistance to peramivir. The H275Y group has been found in 2009 H1N1 in patients taking oseltamivir. As of September 5, 2009, the resistance rate of clinical isolates from treated and untreated patients was 1%. The resistance pathways of peramivir have not been fully clarified. Cross-resistance: Cross-resistance has been found among influenza virus neuraminidase inhibitors. In a neuraminidase assay, oseltamivir resistance groups E119V (A/H3N2), D198N (B), H275Y (A/HIN1), and R292K (H2N2) decreased susceptibility to peramivir by 1, 4, 8, 100, and 80-fold, respectively: zanamivir resistance groups E119A (H4N2), E119D (H4N2), E119G (H4N2), and R152K (B) decreased susceptibility to peramivir by 1, 33, 2, and 400-fold, respectively. The relationship between sensitivity to peramivir inhibition in biochemical assays and clinical effectiveness has not been established.

The main ingredient of this product is peramivir, and the excipients used are sodium chloride and dilute hydrochloric acid

This product is a colorless clear liquid.

For use with influenza A or B. Patients should use it within 48 hours of the first onset of symptoms.

Intravenous drip. Start treatment within 48 hours of the onset of flu symptoms. Adults: The general dosage is 300 mg, a single intravenous drip, and the drip time is not less than 30 minutes. For patients with severe complications, 600 mg can be used, a single intravenous drip, and the drip time is not less than 40 minutes. For patients with severe symptoms, it can be administered once a day, and repeated for 1 to 5 consecutive days. In addition, the dosage can be reduced as appropriate according to age and symptoms. Children: Under normal circumstances, peramivir can be used once a day, 10 mg/kg body weight each time, a single intravenous drip over 30 minutes, or repeated administration for several days according to the condition, not exceeding 5 days. The upper limit of a single dose is within 600 mg. Precautions for use and dosage: 1. Start administration as soon as possible after the onset of flu symptoms. There is no clinical effectiveness data for starting administration 48 hours after the onset of symptoms. 2. For repeated administration, it is necessary to determine whether to continue administration based on clinical symptoms such as body temperature, and do not blindly continue administration. 3. For patients with renal insufficiency, due to the risk of continued increase in plasma drug concentration, the dosage must be adjusted according to the degree of renal impairment. 4. This drug is limited to intravenous infusion.

Common adverse reactions include abnormal clinical test values and digestive system symptoms, and occasionally cardiovascular and nervous system reactions. Abnormal clinical test values are mainly manifested by decreased reticulocytes in the blood, decreased white blood cell count, decreased neutrophil ratio, increased lymphocyte ratio and increased triglycerides; common digestive system reactions include diarrhea, nausea, vomiting, stomach pain, etc. Some patients may experience chest tightness and abnormal electrocardiogram in the cardiovascular system. Some patients may experience dizziness and insomnia in the central nervous system. Occasionally, musculoskeletal system reactions may occur, with an incidence of 1.0%. The incidence of abnormal liver function after continuous administration is 4.44%. It usually recovers on its own after stopping the drug.

This product is contraindicated in patients with a history of hypersensitivity to any other neuraminidase inhibitor (oseltamivir phosphate or zanamivir) or the components of peramivir injection.

Precautions for children: The safety of the drug for low-birth-weight infants and newborns has not been determined. Precautions for pregnancy and lactation: For pregnant women and women who may become pregnant, the drug can only be used when the expected benefits outweigh the potential risks. The safety of the drug for pregnant women has not been established. This product did not show teratogenic effects in animal reproduction studies on rats and rabbits. The fetal rat reproductive toxicity phase II test study suggests that the drug may affect the skeletal development of the fetus, and the lowest adverse effect level (LOAEL) of developmental toxicity for Wistar rats is 30 mg/kg. The reproductive toxicity study of this product in rats showed that the drug can pass through the placenta; in the reproductive toxicity study of rabbits, there were reports of miscarriage and premature birth. The drug should be used with caution in lactating women. The safety of the drug for lactating women has not been studied yet. Studies on rats have shown that peramivir is secreted in breast milk, and its concentration is lower than the maternal blood drug concentration. It is not yet known whether this product is secreted in human breast milk. Precautions for the elderly: Due to the decline in liver, kidney or heart function in elderly patients, the probability of combining with other drugs to treat other complications is relatively high, so the drug should be used with caution in elderly patients.

Pharmacokinetic study data show that peramivir is not degraded in vivo and is excreted almost in its original form through the kidneys. It has a low protein binding rate, indicating that drug interactions related to protein binding are unlikely to occur. In vitro studies have shown that P450 enzymes are not involved in the metabolism of peramivir: peramivir does not inhibit the activity of hepatic cytochrome P450 drug metabolizing enzymes 3A4 and 2D6. Peramivir has a certain induction effect on the production of rat CYP3 enzymes, but the induction effect is not strong. At present, drug interaction studies of peramivir injection and co-administration trials with other drugs have not been carried out. Be cautious when used in combination with other drugs eliminated by the kidneys, and be cautious when used in combination with drugs that are also secreted by the kidneys and have a narrow safety range (such as chlorpropamide, methotrexate, and phenylbutazone), and monitor the patient's renal function appropriately. There is no evaluation of the interaction between peramivir and live attenuated influenza vaccines. However, due to the possible interaction between the two, unless clinically necessary, peramivir should not be used within two weeks of using live attenuated influenza vaccines, and live attenuated influenza vaccines should not be used within 48 hours after using peramivir. Because peramivir, as an antiviral drug, may inhibit the replication of live vaccine viruses, the trivalent inactivated influenza vaccine can be used at any time before or after the administration of peramivir.

Keep in a dark and airtight container below 25°C.

100ml: Peramivir (calculated as C15H28N4O4) 0.3g and sodium chloride 0.9g

36 months

Guangzhou Nucien Pharmaceutical Co., Ltd.

• Founded in:

  1993-09-17

• Address:

  Building 1-2, No. 196, Kaiyuan Avenue, Luogang District, Guangzhou

• Tax NO.:

  91440101618440809W

• Registered Funds:

  65.25 million yuan

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