Description: On February 5, 2002, the State Pharmaceutical Products Supervision and Administration issued the instructions for etimicin sulfate for injection in the Notice on Publishing the Catalogue of Instructions for the Second Batch of Chemicals. The instructions published by the State Administration of Pharmaceutical Products are reference samples for revising the specifications. In case of doubt, the enterprise may propose amendments. Indications should be consistent with the original approval; Adverse reactions, drug interactions and other contents, the instructions provided by the enterprise can not be less than those listed in the sample draft. For empty or incomplete items in the sample manual, enterprises should be required to fill in according to the actual situation, such as product name and specifications.
Drug name
Generic name: etimicin sulfate for injection
Former name:
Commodity name:
Etimicin sulfate for injection
Chinese Pinyin: Zhusheyonɡ ? Yitimixinɡ ?.
The main component of this product is etimicin sulfate. Its chemical name is: O2 amino 2,3,4,6 tetradeoxy 6 (amino) a D erythro hexopyranosyl (1→4)O[3 deoxy 4C methyl 3 (methylamino) b L arabinopyranosyl (1→6)2 deoxy N ethyl L- streptavidin 5/2 sulfuric acid.
Structural formula:
Molecular formula: C2 1H43N5O7.5/2H2SO4.
Molecular weight: 722
Character; Role; letter
This product is white or white-like powder or loose block.
Pharmacology and toxicology
This product is a semi-synthetic water-soluble antibiotic, belonging to aminoglycosides. In vitro antibacterial activity study shows that this product has a wide antibacterial spectrum and good antibacterial effect on a variety of pathogenic bacteria, including Escherichia coli, Klebsiella pneumoniae, Enterobacter, Serratia, Proteus mirabilis, Salmonella, Haemophilus influenzae and Staphylococcus. It has certain antibacterial activity against some Pseudomonas and Acinetobacter, as well as some staphylococcus aureus resistant to gentamicin, micronomicin and cefazolin. It also has certain antibacterial activity against some penicillin-producing staphylococci and some low-level methicillin-resistant staphylococci (MRSA). The mechanism of this product is to inhibit the normal protein synthesis of sensitive bacteria.
The results of animal ototoxicity test showed that the ototoxicity of intramuscular injection of this product was lower than that of other aminoglycoside antibiotics. Similar to netilmicin.
pharmacokinetics
The plasma concentrations of etimicin sulfate after intravenous infusion of 0. 1, 0. 15 and 0.2g were 1 1.30, 14.6 and 19.79 mg/L, respectively. The elimination half-life (tl/2b) of blood is about 65438 0.5 hours, and the excretion of prototype in urine is about 80% within 24 hours. Healthy adults were given the drug twice a day with an interval of 12 hours for 7 consecutive days, and there was no obvious accumulation in the blood. The binding rate of this product with serum protein is about 25%.
indicate
It is suitable for various infections caused by sensitive Escherichia coli, Klebsiella pneumoniae, Serratia, Acinetobacter, Enterobacter, Acinetobacter, Proteus, Haemophilus influenzae, Pseudomonas aeruginosa and Staphylococcus.
Clinical research shows that this product has a good curative effect on the following infections:
Respiratory tract infection: such as acute bronchitis, acute attack of chronic bronchitis, community lung infection, etc.
Infection of kidney and genitourinary system: such as acute nephritis, cystitis, chronic pyelonephritis or acute attack of chronic cystitis.
Skin and soft tissue infections: such as skin and soft tissue infections, trauma, trauma and postoperative infections and other sensitive bacterial infections.
dosage
Intravenous drip
Recommended dose for adults: patients with urinary tract infection or systemic infection with normal renal function, 0. L ~ 0. 15g daily 1 time (1 time 12 hours), diluted in l00ml sodium chloride injection or 5% glucose injection, and intravenously dropped 1 hour. The course of treatment is 5 ~ 10 days.
counteraction
This product is a semi-synthetic aminoglycoside antibiotic, and its adverse reactions are ears and kidneys, and the incidence and severity are similar to those of netilmicin. In some cases, the indexes of liver and kidney function such as urea nitrogen (BUN), SCr or alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) increased slightly, but they returned to normal after stopping taking drugs. Otototoxicity and vestibular toxicity of this product mainly occur in patients with renal insufficiency and patients with excessive or excessive dose, which are manifested as dizziness and tinnitus. Some patients have less hearing loss.
Other rare reactions include nausea, rash, phlebitis, palpitation, chest tightness and itchy skin.
taboo
Those who are allergic to this product and other aminoglycoside antibiotics are prohibited.
Matters needing attention
1. Patients with impaired renal function should not use this product. If necessary, the dosage should be adjusted and the concentration of etimicin sulfate in serum should be monitored. In addition, serum creatinine level and creatinine clearance rate are also the most suitable indicators to observe the degree of renal function. When adjusting the dose, one of the following two schemes can be adopted.
(1) Changing the times of administration: One way to adjust the dosage is to extend the interval between two routine administrations. Because the serum creatinine level is highly correlated with the blood elimination half-life (t 1/2b) of etimicin sulfate, laboratory examination can provide an index to adjust the administration interval. The interval between two doses (hours) is roughly equal to the serum creatinine level (mg/l00ml) multiplied by 8; For example, if a patient weighing 60kg has a serum creatinine level of 3.0 mg/100ml, then the treatment scheme of etimicin sulfate for this patient should be: 2mg/(kg×60kg) per dose, that is, 120mg, and the second interval should be calculated according to the serum creatinine level of 3.0(mg/ 100ml)×8.
(2) Changing the therapeutic dose: For patients with severe systemic infection and renal insufficiency, the frequency of etimicin sulfate administration can be increased, but the therapeutic dose should be reduced. For such patients, the serum concentration of etimicin sulfate should be determined. The recommended method is:
After the routine first dose, it is changed to every 8 hours: divide the routine recommended dose by the serum creatinine level; For example, for a patient weighing 60kg, the first dose is 120mg, and the serum creatinine concentration is 3.0 mg/ 100ml. The treatment scheme of etimicin sulfate for this patient is: one dose is (120÷3), that is, 40mg, 1 time, once every 8 hours.
If the creatinine clearance rate is known, the maintenance dose used every 8 hours can be calculated by the following formula:
Maintenance dose × routine maintenance dose
Creatinine clearance rate, ml/(min1.73m2)
The above recommended dose calculation method is only used when the serum etimicin sulfate level cannot be monitored. Because renal function can be changed at any time during infection, the dose of etimicin sulfate should be adjusted at any time.
2. During the treatment with this product, the changes of renal function and the function of the eighth cranial nerve should be closely observed, and the blood drug concentration should be detected as much as possible, especially for patients with renal insufficiency or failure, patients with extensive burns, newborns, premature infants, infants and elderly patients, patients with shock, heart failure, ascites, patients with severe dehydration and those with normal renal function who have moved in a short time.
3. This product belongs to aminoglycoside antibiotics, which may cause neuromuscular block. Therefore, special attention should be paid to patients with hematological diseases who receive anesthetics, succinylcholine, Tobalin or a large amount of citric acid anticoagulation. Once neuromuscular block occurs, this product should be stopped and treated with intravenous calcium salt.
Medication for pregnant and lactating women
Pregnant women must fully weigh the pros and cons before using this product. Lactating women need to temporarily stop breastfeeding during medication.
Children's medication
This product belongs to aminoglycoside antibiotics and should be used with caution by children.
Medication for elderly patients
Due to the decline of physiological renal function, it is necessary to adjust the dose and interval of this product.
drug interaction
This product should be avoided to be combined with other drugs with potential ototoxicity, such as polymyxin, other aminoglycosides and other antibiotics, strong uric acid and furosemide (furosemide), so as not to increase nephrotoxicity and ototoxicity.
excessive
standard
(1) 50mg (50,000 units) (2)0. 1 g (65,438+million units)
store
Sealed and stored in a cool and dark place.
parcel
term of validity
Registration authentication number
Production enterprise
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