Amikacin Sulfate Injection
Amikacin Sulfate Injection

[Indications] 1. Typhoid fever and other Salmonella infections: choice of drug sensitive strains caused by typhoid paratyphoid, infected by Salmonella gastroenteritis is generally not used this product, such as a serious condition, there is septicemia can use whenever possible. 2. Ampicillin resistant Haemophilus influenzae type B meningitis or in patients allergic to penicillin, Streptococcus pneumoniae, Neisseria meningitidis meningitis and sensitive gram negative bacilli meningitis, this product can be used as a selection of drugs. 3. Brain abscess, especially of the ear, often mixed with aerobic and anaerobic bacteria. 4. Serious anaerobic infections, such as Bacteroides fragilis infection, especially for lesions involving the central nervous system, combined with aminoglycoside antibiotics for the treatment of abdominal infection and pelvic infection, to control and aerobic and anaerobic bacteria infection. 5. No alternative to other antibacterial drugs with low toxicity when treating serious infections caused by sensitive bacteria, such as Haemophilus influenzae, Salmonella and other gram negative bacteria due to sepsis and pulmonary infection, often combined with aminoglycosides. 6. Rickettsia infection can be used for Q fever, Rocky Mountain spotted fever, endemic typhus and so on.

[Name of drug]
Amikacin Sulfate Injection

Chinese Name: 硫酸阿米卡星注射液

Chinese Pinyin: Liusuan A'mikaxing Zhusheye

 

[Ingredients] Amikacin sulfate

Chemical name: O-3- amino -3- deoxy -D- alpha - - -O-[6- () - amino group -6- deoxy -D- - -2- - - glycosyl - - (1 to 4)]-N- (4- amino, -2- hydroxy, -1-, oxygen butyl), deoxy, deoxy, -D-, trans amine sulfate.

Chemical formula:

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Molecular formula: C22H43N5O13. NH2SO4 (n=1.8 or 2)

Molecular weight: 762.15(n=1.8)or781.76(n=2)

All auxiliary components: Sodium citrate, Sodium sulfite.

[Character] This product is colorless to slightly yellow transparent liquid.

[Indications]

This product is suitable for Pseudomonas aeruginosa and other Pseudomonas, Escherichia coli, proteus sp., Kleber, Sarre, Enterobacter sp., Acinetobacter and other sensitive gram negative bacilli and Staphylococcus (methicillin sensitive strains) caused by severe infection, such as bacteremia or sepsis bacterial endocarditis, and lower respiratory tract infection, bone and joint infections, biliary tract infection and abdominal infection and complicated urinary tract infections, skin and soft tissue infection.Because of this product for most carbepenems stability, it is especially suitable for the treatment of coused by gram negative bacilli and kanamycin and gentamicin or tobramycin resistant strains .

[Specification] 2ml:0.2g

 

[Usage and Dosage]

1. Adults were injected intramuscularly or intravenously. Simple urinary tract infections are resistant to commonly used antimicrobial agents, every 12 hours 0.2g (1 branches); for other systemic infections every 12 hours 7.5mg/kg, or 24 15mg/kg every hour. Adults are not more than 1.5g a day, the course of treatment is not more than 10 days.

2. Intramuscular injection or intravenous drip of children. The first dose is 10mg/Kg by weight, followed by 7.5mg/kg per 12 hours or 15mg/kg every 24 hours.

3. Patients with renal dysfunction: creatinine clearance rate >50 to 90ml/min per 12 hours to normal doses (7.5mg/Kg) of 60 to 90%; creatinine clearance rate of 10 to 50ml/min, every 24~48 hours with 7.5mg/kg of 20 ~ 30%. Creatinine clearance rate can be measured directly or calculated from the value of blood creatinine:

 

                                                                                                                  (140- age) * standard body weight (kg)
                                         Adult male creatinine clearance rate=----------------------------------------------------------------------------
                                                                                                                72 * Serum creatinine concentration (mg/dl)
                                                                                                                    (140- age) * standard body weight (kg)
                                                                                             Or-------------------------------------------------------------------------------
                                                                                                                50 * Serum creatinine concentration (mol/L)
                                                                                                                    (140- age) * standard body weight (kg)
                                         Adult female creatinine clearance rate=-------------------------------------------------------------------------*0.85
                                                                                                                72 * Serum creatinine concentration  (mg/dl)
                                                                                                                     (140- age) * standard body weight (kg)
                                                                                             Or------------------------------------------------------------------------------ * 0.85
                                                                                                                50 * Serum creatinine concentration (mol/L)

 

[Adverse Effects]

1. Patients may suffer from hearing loss, tinnitus or fullness of the ear, and a small number of patients may also suffer from dizziness, unstable gait and other symptoms. Hearing loss is usually no longer aggravated after withdrawal, but may continue to develop after deafness.
2. This product has certain kidney toxicity, patients can appear hematuria, micturition frequency decrease or urine quantity decrease, blood
The value of urea nitrogen and serum creatinine increased. Most of them were reversible, but they were relieved after discontinuation. However, there were some reports of renal failure.
3. Weak muscle, lethargy, dyspnea and other neuromuscular blocking effects are rare.
4. Other adverse reactions are headache, numbness, acupuncture, infection, tremors, convulsions, arthralgia, fever of drugs, eosinophilia, abnormal liver function, blurred vision, etc.

[Contraindicated] Disable Amikacin or other aminoglycosides allergic patients.

[Matters Needing Attention]

1. Cross allergic, an allergic to aminoglycosides may be allergic to other aminoglycosides.
2. In the course of medication, should pay attention to the following inspection:
   (1) Routine urinalysis and renal function tests were performed to prevent severe nephrotoxicity.
   (2) Hearing test or electro acoustic examination, especially pay attention to high-frequency hearing impairment, which is particularly important for elderly patients.
3. In the course of treatment, the serum concentration should be monitored, especially in the newborns, the elderly and the patients with renal hypofunction. The serum peak concentration (Cmax) should be kept at 15~30 g/ml per 12 hours for 7.5mg/kg and the trough concentration is 5~10 g/ml; 1 times a day for 15mg/kg, the peak concentration of serum should be maintained at 56~64 g/ml, and the trough concentration should be <1 mu g/ml.

4. The following should be used with caution:
   (1) Dehydration can increase the serum concentration and cause toxic reaction;
   (2) Eighth nerve damage to the brain, because this product can cause vestibular and auditory nerve damage;
   (3) Myasthenia gravis or Parkinson's disease, because this disease can cause neuromuscular block effect, leading to skeletal muscle weakness;
   (4) The renal function impairment is due to nephrotoxicity.
5. For the diagnosis of interference: This product can make the alanine aminotransferase (ALT), aspartate aminotransferase (AST), serum bilirubin concentration and lactate dehydrogenase concentration increased; calcium, magnesium, potassium and sodium concentration might decrease.

6. Aminoglycosides can be inactivated when mixed with beta lactams (cephalosporins and penicillins). When combined with these antibiotics, the product must be divided into bottles. Amikacin should not be given the same bottle as other drugs.
7. Patients should be given adequate water to reduce renal tubular damage.
8. When preparing intravenous medication, add Sodium Chloride Injection or 5% Glucose Injection or other sterile diluent every 100 500mg to 200ML. Adults should be given a slow infusion within 30~60 minutes, reducing the amount of diluted fluid in infants.

[Medication for pregnant women and lactating women]

This product belongs to the D class used by pregnant women, which has certain harm to human beings, but it may be more beneficial than disadvantages after drug use. This product may pass through the placenta to the fetal tissues and may cause fetal hearing impairment. Pregnant women before using this product must be fully cons. Lactating women should be temporarily suspended from breast-feeding.

[Child Medication] Aminoglycosides should be used cautiously in pediatrics, especially in premature infants and neonates. The renal tissue has not yet been fully developed, so that the half-life of this kind of medicine is prolonged, and the drugs are easy to accumulate in the body and produce toxic reactions.

[Senile Medication] The renal function of the elderly patients has a certain degree of physiological decline, even if the renal function measured in the normal range, should still use a smaller amount of treatment. It is easy for elderly patients to produce various toxic reactions after the use of this product. It is necessary to monitor the concentration of serum during the course of treatment.

 

[Drug Interactions]

1. This product with other aminoglycosides combined or successively local or systemic application, can increase the ototoxicity and nephrotoxicity and neuromuscular blockade.
2. This product is combined with neuromuscular blocking drugs, can aggravate the neuromuscular block effect, leading to muscle weakness, respiratory depression and other symptoms. This product with capreomycin, cisplatin, ethacrynic acid, furosemide (or vancomycin or norvancomycin) combination, or successively local or systemic application may increase ototoxicity and renal toxicity.
3. This product with cephalothin or local or systemic cefazolin combination may increase renal toxicity. This product should not be compatible with amphotericin B, cefoxitin, sulfadiazine and tetracycline injections, not drip in the same bottle.
4. This product has been combined with polymyxin B injections or has been applied continuously, locally or systemically. It can increase nephrotoxicity and neuromuscular block.
5. Other nephrotoxic drugs and drugs are not in combination with the product or has applied, so as not to aggravate renal toxicity or ototoxicity.

[Overdose] Due to the lack of specific antagonists, this product overdose or cause toxicity, mainly with symptomatic treatment and supportive therapy, while adding large amounts of water. Hemodialysis or peritoneal dialysis can help clear Amikacin from the blood.

[Pharmacology and Toxicology]

Amikacin sulfate is an aminoglycoside antibiotic. The product of the Enterobacteriaceae, such as Escherichia coli, Klebsiella, enterobacter, proteus, Shigella, Salmonella spp., Citrobacter spp., Sarre etc with good effect on Pseudomonas aeruginosa and some other Pseudomonas, Acinetobacter bar sp., Alcaligenes etc. also have a good effect; of gonococcus, meningitis, influenza bacillus, Salmonella, Campylobacter fetus Jerson, Mycobacterium tuberculosis and Mycobacterium has better certain antibacterial effect, the antibacterial activity of gentamicin was slightly lower. The most outstanding advantage of this product is that it is stable against aminoglycoside inactive enzymes produced by many gram negative bacilli and will not be inactive because of the inactivation of this enzyme. Of the 12 enzymes currently isolated, the product can only be passivated by AAC (6'); moreover, AAD (4') and APH (3') - III can sometimes cause bacteria to be moderately resistant to this product. Clinical isolates of Enterobacteriaceae to gentamicin, tobramycin and netilmicin magnitude of aminoglycoside resistance in about 60 ~ 70% of the goods are still sensitive. In recent years, the number of Amikacin resistant strains in gram negative bacilli has also increased. Among the gram positive cocci, Streptococcus pneumoniae, each group of Streptococcus and Enterococcus were mostly resistant to Staphylococcus aureus sensitive strains. This product is ineffective against anaerobic bacteria. The mechanism of action is the 3OS subunit, which acts on bacterial ribosomes, inhibits the synthesis of proteins by bacteria. Amikacin is often synergistic with semisynthetic penicillins or cephalosporins.

[Pharmacokinetics]

Amikacin is rarely absorbed orally. It is absorbed rapidly after intramuscular injection. Mainly distributed in the extracellular fluid, some drugs can be distributed to the various organizations, and can accumulate in renal cortical cells and inner ear fluid; but in the heart, pericardial fluid, auricle muscle, fat and fluid in low concentration. Low concentrations of bronchial secretions, bile, and aqueous humor. Protein binding rate is low. Non metabolism in vivo. The half-life of adult blood elimination (t1/2 beta) ranged from 2 to 2.5 hours. Through the placenta into the fetal tissue. Low CSF concentration. Excreted mainly by glomerular filtration and excreted more than 90% within 24 hours after administration. Hemodialysis and peritoneal dialysis remove considerable amounts of blood from the blood, thereby significantly reducing the half-life.

 

[Storage] Keep in a cool place (keep out of light for no more than 20 degrees).

[Packing] Ampoule packing, 10 pcs / boxes

[Validity]  24 months

[Implementation Criteria] Chinese Pharmacopoeia, 2010 edition, two parts

[Approval Number] SFDA approval number H33021538

[Production Enterprise]

Name of enterprise: Zhejiang Chengyi Pharmaceutical Co., Ltd.
Production address: No. 118, Chemical Road, Dongtou District, Wenzhou city,Zhejiang province,China.

Phone number: 86-577-6348-3979

Fax number: 86-577-6348-5135

URL:http://en.chengyipharma.com

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