Active Pharmaceutical Ingredients

Molecular Formula: C22H47N5O21S2

Molecular Weight: 781.760

CAS No.: 39831-55-5

Amikacin sulfate is a semi-synthetic aminoglycoside antibiotic.

Description

It is a white, crystalline powder. Freely soluble in water.

Application

It is a semi-synthetic aminoglycoside antibiotic. Its antibacterial spectrum is similar to that of gentamicin. It is effective against Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Proteus. It is also effective against other resistant strains of aminoglycoside antibiotics.

It is an anti-infective drug used to treat urinary tract infections, sepsis, skin infections, bone and joint infections, pneumonia and lower respiratory tract infections caused by sensitive bacteria.

Packing

25Kg per drum

Storage：

Preserve in tight containers in a dry place.

Shelf Life :

36 months from date of production when stored in good condition.

Minimum Order

One package.

Amikacin Sulfate Introduction

Item	Details
Generic Name	Amikacin Sulfate
Trade Names	Amikin, etc.
Classification	Aminoglycoside antibiotic
Chemical Structure	Amikacin is derived from kanamycin A. It has a complex structure with multiple amino and hydroxyl groups. The sulfate salt form is used for pharmaceutical purposes. The molecular formula of amikacin sulfate is (C₂₂H₄₃N₅O₁₃)₂·3H₂SO₄, and it has a relatively high molecular weight. This structure enables it to bind to bacterial ribosomes.
Pharmacological Action	Amikacin sulfate binds to the 30S subunit of the bacterial ribosome. This binding interferes with the accuracy of translation during protein synthesis. It causes misreading of the genetic code, leading to the production of non – functional or toxic proteins. As a result, bacterial growth and survival are inhibited. It has a broad – spectrum antibacterial activity, being effective against many Gram – negative bacteria, including Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, and also has some activity against certain Gram – positive bacteria. It is particularly useful against bacteria that have developed resistance to other aminoglycosides due to its unique structure that is less affected by common resistance mechanisms.
Clinical Applications	1. Serious Gram – negative Bacterial Infections: – Used in the treatment of sepsis caused by Gram – negative bacteria, especially in cases where other antibiotics have failed or resistance is suspected. – Treats pneumonia, particularly when caused by Pseudomonas aeruginosa or other difficult – to – treat Gram – negative pathogens in immunocompromised patients or those with ventilator – associated pneumonia. – Effective against complicated urinary tract infections, such as those caused by multidrug – resistant Gram – negative bacteria. 2. Combination Therapy: Often used in combination with other antibiotics, such as beta – lactams, to provide broader coverage and enhance the antibacterial effect. This is especially important in the treatment of severe infections where a synergistic effect can improve patient outcomes.
Dosage and Administration	Adults: – The usual dosage is 15 mg/kg body weight per day, divided into 2 – 3 equal doses. For example, in less severe infections, it may be given as 7.5 mg/kg every 12 hours. In more severe cases, the dose may be adjusted according to the patient’s condition and renal function. – It is usually administered by intramuscular or intravenous injection. The intravenous infusion should be given slowly over 30 – 60 minutes to reduce the risk of adverse effects. Children: – The dose is also calculated based on body weight, typically 15 mg/kg body weight per day, divided into 2 – 3 doses. Neonates may require special dosing considerations based on their gestational age and post – natal age. Patients with Renal Impairment: Dosage adjustment is crucial. The dosing interval may need to be extended or the dose reduced depending on the degree of renal impairment. Regular monitoring of serum drug levels and renal function is necessary to ensure safe and effective treatment.
Adverse Reactions	1. Ototoxicity: This is a major concern. It can cause both cochlear and vestibular damage. Cochlear damage may lead to hearing loss, which can be permanent. Vestibular damage can result in dizziness, vertigo, and balance problems. The risk of ototoxicity increases with higher doses, longer treatment duration, and in patients with pre – existing hearing impairment or renal dysfunction. 2. Nephrotoxicity: Amikacin sulfate can cause damage to the kidneys, leading to acute tubular necrosis in severe cases. Symptoms may include increased blood urea nitrogen (BUN) and creatinine levels, decreased urine output, and electrolyte imbalances. Monitoring of renal function is essential during treatment. 3. Neuromuscular Blockade: Rarely, it can cause neuromuscular blockade, leading to muscle weakness, respiratory depression, and even paralysis. This is more likely to occur in patients with pre – existing neuromuscular disorders or when amikacin is used in combination with other drugs that affect neuromuscular transmission, such as neuromuscular blocking agents. 4. Allergic Reactions: Although less common, allergic reactions can occur, ranging from rashes, itching, and fever to more severe anaphylactic reactions.
Drug Interactions	1. With Loop Diuretics: Concurrent use with loop diuretics, such as furosemide, can increase the risk of ototoxicity. Loop diuretics can enhance the uptake of aminoglycosides into the inner ear, potentiating their ototoxic effects. 2. With Other Nephrotoxic Drugs: Using amikacin sulfate with other nephrotoxic drugs, like certain cephalosporins or vancomycin, increases the risk of nephrotoxicity. The combined effect on the kidneys can lead to more severe renal damage. 3. With Neuromuscular Blocking Agents: As mentioned, co – administration with neuromuscular blocking agents can potentiate neuromuscular blockade, increasing the risk of respiratory depression and muscle weakness. 4. With Penicillins: In some cases, the combination of amikacin with penicillins can result in chemical inactivation of amikacin when mixed in the same solution. However, when used separately but in combination therapy, they can have a synergistic antibacterial effect.
Special Population Considerations	1. Pregnant Women: Use during pregnancy is associated with a risk of ototoxicity to the fetus. It should be used only when the potential benefits outweigh the risks, and close monitoring of the mother and fetus is required. 2. Breastfeeding Women: Amikacin is excreted in breast milk in small amounts. Caution should be exercised, and in some cases, breastfeeding may need to be discontinued during treatment. 3. Patients with Renal Impairment: As mentioned, dosage adjustment is essential. Regular monitoring of renal function and serum drug levels is crucial to avoid toxicity. 4. Elderly Patients: Elderly patients are more prone to the adverse effects of amikacin, especially ototoxicity and nephrotoxicity. Close monitoring and careful dosing are required.
History and Development	Amikacin was developed as a semi – synthetic aminoglycoside antibiotic to address the issue of bacterial resistance to existing aminoglycosides. It was introduced in the 1970s and has since been an important drug in the treatment of serious Gram – negative bacterial infections. Its development was a significant step in expanding the options for treating infections caused by resistant bacteria.

 

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