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Tolerable

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Tolerable

It is resistant (foscarnet sodium chloride injection), and the indication is 1. Cytomegalovirus retinitis in AIDS patients; 2. Acyclovir resistant herpes simplex virus skin mucosal infection in patients with immune function impairment.

Drug name: Tolerable

Drug type: Prescription drugs, medical insurance drugs for work-related injuries
Use classification: Reverse transcriptase inhibitor

catalog

six Adverse reactions
seven taboo
eight matters needing attention
nine Drugs for pregnant and lactating women

Composition

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The main component of this product is sodium phosphoformate, and its chemical name is trisodium phosphoformate hexahydrate. The chemical structure formula is as follows:

character

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This product is a colorless clear liquid.

indication

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1. Cytomegalovirus retinitis in AIDS patients;

2. Acyclovir resistant herpes simplex virus skin mucosal infection in patients with immune function impairment.

Specifications

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250ml：3.0g。

Usage and dosage

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Intravenous drip. Dose individualization.

1. Cytomegalovirus retinitis (normal renal function) in AIDS patients

Induction treatment: the recommended initial dose is 60mg/kg, once every 8 hours, the intravenous drip time shall not be less than 1 hour, and it shall be used continuously for 2 to 3 weeks according to the efficacy.

Maintenance treatment: the maintenance dose is 90~120mg/kg a day (the dose is adjusted according to the renal function), and the intravenous drip time shall not be less than 2 hours. During maintenance treatment, if the condition worsens, the induction treatment and maintenance treatment can be repeated.

2. Acyclovir resistant herpes simplex virus skin mucosal infection in patients with immune function impairment.

The recommended dose is 40mg/kg, once every 8 or 12 hours, the intravenous drip time shall not be less than 1 hour, and it shall be used continuously for 2-3 weeks or until cured.

During the use of this product, the renal function should be closely monitored and the dosage should be adjusted. See the following table for details:

HSV CMV

Creatinine clearance equivalent to 80mg/kg/day equivalent to 120mg/kg/day equivalent to 180mg/kg/day

（ml/min/kg）（40mg/kg q12h）（40mg/kg q8h）（60mg/kg q8h）

＞1.4 40 q12h 40 q8h 60 q8h

＞1.0-1.4 30 q12h 30 q8h 45 q8h

＞0.8-1.0 20 q12h 35 q12h 50 q12h

＞0.6-0.8 35 q24h 25 q12h 40 q12h

＞0.5-0.6 25 q24h 40 q24h 60 q24h

≥0.4-0.5 20 q24h 35 q24h 50 q24h

＜ 0.4 Not recommended Not recommended Not recommended

Maintenance treatment

CMV

Creatinine clearance equivalent to 90mg/kg/day equivalent to 120mg/kg/day

(ml/min/kg) (once a day) (once a day)

＞1.4 90 q24h 120 q24h

＞1.0-1.4 70 q24h 90 q24h

＞0.8-1.0 50 q24h 65 q24h

＞0.6-0.8 80 q48h 105 q48h

＞0.5-0.6 60 q48h 80 q48h

≥0.4-0.5 50 q48h 65 q48h

＜ 0.4 Not recommended Not recommended

When using the above table, the measured 24-hour creatinine clearance (ml/min) shall be divided by the body weight, or the creatinine clearance (ml/min/kg) shall be calculated according to the following formula.

140 - Age

Male: ---------

Serum creatinine × 72

140 - Age

Female: -------- × 0.85

Serum creatinine × 72

Adverse reactions

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According to literature reports, the prospective clinical trials of 188 AIDS patients and the adverse reactions related to this product, unrelated and unrecognizable after marketing are as follows:

Renal function damage: serum creatinine value increases, creatinine clearance rate decreases, renal function abnormalities, acute renal failure, uremia, polyuria, metabolic acidosis. The serum creatinine value can return to the level before treatment or normal within 1 to 10 weeks after discontinuation of medication.

Dielectric: hypocalcemia, hypomagnesemia, hypokalemia, hypophosphatemia, or hyperphosphatemia. This product can chelate divalent metal ions (Ca [sup] 2+[/sup], Mg [sup] 2+[/sup], Fe [sup] 2+[/sup], Zn [sup] 2+[/sup]). 30% of AIDS patients have reversible hypocalcemia after using this product, which shows a dose effect relationship.

Convulsion (including grand seizure): Although many patients may have convulsions due to hypocalcemia or original diseases (cryptococcal meningitis, space occupying lesions or other central nervous system tumors), the relationship with this product cannot be excluded.

Anemia or low hemoglobin: generally not accompanied by a decrease in white blood cell and platelet count. Many AIDS patients received AZT treatment at the same time and had anemia before receiving this product.

Local irritation: phlebitis at the injection site, genital and urinary tract irritation symptoms or ulcers.

Whole body: fatigue, discomfort, chills, fever, sepsis.

Gastrointestinal system: nausea, vomiting, diarrhea, abdominal pain, dyspepsia, constipation, and pancreatitis was reported in one case.

Metabolism and nutrition disorders: hyponatremia and edema of lower limbs, increase of lactate dehydrogenase, alkaline phosphatase or amylase.

Central and peripheral nervous system: Paraethesia, headache, dizziness, involuntary muscle contraction, tremor, ataxia, neuropathy.

Mental disorders: anorexia, anxiety, neuroticism, mental disorder, depression, psychosis, excitement, aggressive reaction.

Hepatobiliary system: abnormal ALT and AST.

Cardiovascular: ECG abnormality, hypertension or hypotension, ventricular arrhythmia.

Others: leukopenia, granulocytopenia, thrombocytopenia, rash, muscle weakness.

taboo

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Inhibit allergy to foscarnet sodium.

matters needing attention

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1. This product must be used by a specialist in strict accordance with the instructions.

2. During the use of this product, the renal function must be closely monitored, and the dosage should be adjusted according to the renal function to achieve individualized administration.

3. This product cannot be administered by rapid or pellet intravenous injection. The intravenous infusion rate shall not be greater than 1mg/kg per minute.

4. In order to reduce the nephrotoxicity of this product, patients should be hydrated before and during use. The amount of intravenous infusion (0.5% glucose or normal saline) is 2.5 liters/day, and thiazide diuretics can be used appropriately.

5. Avoid contact with skin and eyes. In case of accidental contact, wash with water immediately.

Drugs for pregnant and lactating women

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Unless necessary, pregnant women should not use this product. Breastfeeding women should stop breastfeeding when using this product.

Drug interaction

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1. This product cannot be mixed with other drugs for intravenous drip. This product can only be diluted with 5% glucose or normal saline.

2. This product cannot be used together with other nephrotoxic drugs such as aminoglycoside antibiotics, amphotericin B or vancomycin. This product cannot be used in combination with intravenous injection of pentamidine to avoid hypocalcemia.

Pharmacology and toxicology

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This product is a broad-spectrum antiviral drug. Its mechanism of action is to directly inhibit virus specific DNA polymerase and reverse transcriptase. This product has inhibitory effect on type I, type II herpes simplex virus, cytomegalovirus, etc.

Pharmacokinetics

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According to data reports, two clinical studies conducted in the United States to treat patients with normal renal function by intermittent intravenous drip at a dose of 60mg/kg/time (once every 8 hours) showed that Cmax was 573 μ M and 445 μ M respectively after the first administration, and Cmin was 28 μ M and 88 μ M respectively; Cmax and Cmin were 579 μ M and 517 μ M and 110 μ M and 105 μ M respectively on the 14th or 15th day of use; The mean plasma clearance rates were 178 ± 48ml/min and 130 ± 44/min, respectively. The study on the first or third day of intermittent infusion indicated that the average plasma half-life was about 3 hours, and 80~90% of the dosage was discharged from urine in the original form. This product can enter the patient's cerebrospinal fluid, and the drug concentration in the cerebrospinal fluid is related to the defect degree of the patient's blood brain barrier. This product can accumulate in human bones, but the accumulation degree has not been determined.