Overview
Amikacin sulfate is an aminoglycoside drug used in the short-term treatment of a wide range of serious bacterial infections for which other drugs may not be effective. It is used to manage meningitis, infections of the blood, lungs, skin, abdomen, etc. However, this drug may not be effective for cold, flu, or other viral infections. Amikacin sulfate must be administered only under the supervision of a doctor. It should be used only in the treatment or prevention of proven or strongly suspected infections caused by the bacteria in order to minimize drug resistance and maintain the effectiveness of the drug.
How Does Amikacin Sulfate Work?
Amikacin sulfate binds to the bacterial components, blocks protein synthesis, and produces important bacterial proteins that prevent further bacterial growth. It helps treat infections caused by Escherichia coli, Pseudomonas species, Klebsiella, Enterobacter, Serratia species, certain Staphylococcus species, etc.
What Are the Indications of Amikacin Sulfate?
Amikacin sulfate is used in the short-term treatment of serious infections caused by gram-negative bacteria.
What Are the Contraindications of Amikacin Sulfate?
Amikacin sulfate is contraindicated in patients with a history of hypersensitivity or serious toxic reactions to the drug.
What Is the Dosage of Amikacin Sulfate?
Amikacin sulfate is recommended at a dose of 15 mg/kg/day (milligram/kg/day), divided into two or three equal doses at 7.5 mg/kg every 12 hours or 5 mg/kg every eight hours for 7 to 10 days. If the treatment is continued beyond 10 days, Amikacin must be re-evaluated, and serum levels and also renal, auditory, and vestibular functions must be monitored. The total dose must not exceed 15 mg/kg/day; if Amikacin is indicated in newborns, a loading dose of 10 mg/kg is administered initially, followed by 7.5 mg/kg every 12 hours. A dose of 250 mg twice daily is indicated if Amikacin is recommended for uncomplicated urinary tract infections. Dose adjustments must be made for patients with renal function disorders based on the creatinine clearance or serum creatinine values, either by administration of normal doses at prolonged intervals or reduced doses at fixed intervals.
Uncomplicated infections usually respond to treatment in 24 to 48 hours; however, if a definite clinical response is not obtained within three to five days, the treatment must be stopped. The antibiotic susceptibility pattern of the organism must be checked, as failure may be due to resistance of the organism or presence of septic foci, which may require surgical drainage.
What Are the Drug Warnings and Precautions?
Drug Warnings:
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Patients treated with Amikacin sulfate in 0.9 % sodium chloride injection, must be closely monitored, as the drug has the potential to cause ototoxicity and nephrotoxicity, and the safe period for treatment is no longer than 14 days.
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Neurotoxicity may occur as a result of vestibular and permanent bilateral auditory ototoxicity and is associated with an increased risk in patients with a history of renal damage. Ototoxicity can also occur in patients with normal renal function but treated with high doses of Amikacin sulfate or for a prolonged duration than recommended. Neurotoxicity can be associated with numbness, tingling sensation, convulsions, and muscle twitching.
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Cochlear damage can occur but may not be associated with any symptoms during the treatment. However, it can lead to partial or complete bilateral deafness after the treatment with Amikacin sulfate is discontinued. Ototoxicity induced by the aminoglycoside group of drugs is usually irreversible.
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Amikacin sulfate has been known to be associated with a risk of nephrotoxicity, especially in patients with renal disorders, or in patients who receive high doses or prolonged treatment.
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Neuromuscular blockade and respiratory paralysis can occur following the injection of Amikacin sulfate.
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Serum creatinine, blood urea nitrogen, or creatinine clearance must be frequently checked during the treatment.
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In cases of symptoms of nephrotoxicity or ototoxicity such as dizziness, tinnitus, vertigo, roaring in the ears, or hearing loss is noticed, the dose must be modified or the drug must be discontinued.
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Drugs such as Bacitracin, Vancomycin, Colistin, Amphotericin B, or other aminoglycosides must be avoided in any form of administration, as it may increase the risk of toxicity.
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Amikacin sulfate must not be used along with diuretics such as Furosemide or Ethacrynic acid, as it may alter the antibiotic concentration in the serum and tissues and also increase toxicity.
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Aminoglycoside drugs may harm the fetus when administered to pregnant women, as the drug has the potential to cross the placental barrier or cause serious adverse effects such as bilateral congenital deafness.
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The majority of the antibacterial agents are associated with Clostridium difficile-associated diarrhea (CDAD), ranging from mild diarrhea to fatal colitis. If CDAD is suspected, the treatment must be discontinued, appropriate fluid and electrolyte administration must be done along with protein supplementation.
Precautions:
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Renal function must be assessed before the initiation of treatment and frequently monitored during the course of treatment.
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Administering or prescribing Amikacin without the confirmation of bacterial infection, or as a prophylactic indication may not benefit the patient, and it also increases the chance of the development of drug-resistant bacteria.
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Patients must be adequately hydrated during the treatment to reduce the risk of chemical irritation of renal tubules. Hydration must be increased in cases of symptoms of renal irritation, and reduction in the doses of Amikacin sulfate must be considered if symptoms of renal dysfunction are observed, and the treatment must be discontinued if urinary output decreases.
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Amikacin sulfate must be cautiously used in patients with muscle disorders, as it may affect the neuromuscular junction, and aggravate muscle weakness.
For Patients:
What Is Amikacin Sulfate?
Amikacin sulfate is a prescription medicine used to treat serious bacterial infections of the lungs, bones, joints, skin, meninges, blood, abdomen, and urinary tract. It works by destroying the bacteria and preventing their growth. However, this medicine is not effective for the common cold, flu, or other viral infections. Antibiotics must be taken only if the infection is proven or strongly suspected, to prevent the development of drug-resistant bacteria.
What Is the Most Important Information About Amikacin Sulfate?
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Amikacin sulfate must be taken under the supervision of the doctor; the patient may begin to feel better during the first few days of treatment, but the dose regimen must be taken completely; if the condition does not improve or worsen, the doctor must be immediately informed.
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In case the dose is stopped abruptly or skipped, the infection may not be completely cured, and the bacteria may become resistant to medications.
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Diarrhea is a common side effect associated with antibiotics and stops when the medicine is discontinued, if the symptoms persist for more than two months, the doctor must be informed.
What Should the Patients Inform the Doctor About Before Taking Amikacin Sulfate?
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Before taking Amikacin sulfate, the doctor must be informed if the patient is allergic to Amikacin or other aminoglycoside antibiotics such as Streptomycin, Gentamicin, Neomycin, etc., or any other medications.
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The doctor must be informed if the patient is taking any vitamin or herbal supplements, over-the-counter (OTC) medicines, or other antibiotics such as Ampicillin, Amoxicillin, Meclizine, etc., as many medicines may interact with Amikacin and the doctor might have to modify the doses and also monitor for any side effects.
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The doctor must be informed if the patient is suffering from muscle problems such as Parkinson’s disease, myasthenia gravis, etc., or has a history of cystic fibrosis or any other diseases.
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Female patients must inform the doctor if they are pregnant or planning to become pregnant, breastfeeding, or planning to breastfeed. If the patient becomes pregnant during the treatment, the doctor must be informed immediately, as Amikacin may cause fetal harm.
How Should Amikacin Sulfate Be Stored?
Amikacin sulfate must be stored at room temperature at around 20 to 25 degrees Celsius. Any unused medicine must be safely discarded.
How Should Amikacin Sulfate Be Taken?
Amikacin sulfate injection is administered by a healthcare professional or in a hospital. Amikacin sulfate injection is administered into a vein or into a muscle every 8 to 12 hours; the medicine is infused slowly over a period of 30 to 60 minutes. The duration of the treatment depends on the type of infection.
What Are Some of the Side Effects of Amikacin Sulfate?
Some serious side effects include;
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Amikacin can affect the nerves and cause loss of hearing, loss of balance, or both, or may cause damage to the cochlea (inner ear), causing high-frequency deafness.
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This group of drugs may cause muscle weakness or acute paralysis of the muscles.
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Changes in kidney functions can be observed during the treatment, but they may be reversible after the treatment is discontinued.
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According to post-marketing studies, Amikacin sulfate may cause acute renal failure or have toxic effects on the kidneys.
Some of the common side effects of Amikacin sulfate include;
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Nausea and vomiting.
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Headache.
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Fever.
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Diarrhea.
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Rash and itching.
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Peeling of the skin.
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Hives (itchy bumps on the skin).
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Swelling of the eyes, lips, tongue, face, and throat.
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Breathing difficulty.
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Severe diarrhea or bloody stools (occurring for more than two months after the treatment).
If the patients experience any serious side effects or other unusual symptoms, the doctor must be contacted immediately.
For Doctors:
Description-
Amikacin sulfate injection is derived from Kanamycin and is a semisynthetic aminoglycoside drug. It is available as a sterile colorless or a light straw-colored solution recommended for intramuscular or intravenous use. A 100 mg per 2 mL vial contains:
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50 mg Amikacin sulfate.
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0.13 percent Sodium metabisulfite.
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0.5 percent Sodium citrate dihydrate.
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Water for injection (pH adjusted to 4.5 with sulfuric acid).
Clinical Pharmacology-
Mechanism of Action: Amikacin acts by binding to the prokaryotic ribosome and inhibits protein synthesis in the bacteria, causing infection. It is bactericidal against both gram-positive and gram-negative bacteria. However, aminoglycoside drugs have low activity against gram-positive bacteria, except Staphylococcus species, and are ineffective against Salmonella and Shigella species.
Amikacin sulfate, in combination with beta-lactam antibiotics, is known to be highly effective against many gram-negative organisms.
Pharmacokinetics:
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Following an intramuscular administration, Amikacin sulfate gets rapidly absorbed and the average maximum serum concentration is obtained in one hour at about 12,16, and 21 mcg/mL (microgram per milliliter) at the single doses of 250 mg (milligram), 375 mg, and 500 mg respectively. It is well tolerated when administered at recommended doses, and no ototoxicity or nephrotoxicity was observed.
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Approximately 91.9 percent of the intramuscular dose is excreted in the first eight hours, and 98.2 percent within 24 hours, unchanged in the urine. Mean urine concentration was 563 mcg/mL, 697 mcg/mL, and 832 mcg/mL following 250 mg, 375 mg, and 500 mg doses respectively.
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Following a single dose intravenous administration of 500 mg Amikacin sulfate over a period of 30 minutes, as an infusion, maximum serum concentration was observed at 24 mcg/mL, 18 mcg/mL, and 0.75 mcg/mL at 30 minutes, one hour, and ten hours respectively. Repeated infusions were tolerated by normal adult patients every 12 hours at 7.5 g/kg, with no drug accumulation. The mean serum half-life is more than two hours, with an apparent volume of distribution of 24 liters.
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Amikacin is eliminated by glomerular filtration, and patients with impaired renal function, may excrete the drug more slowly than normal patients, and hence renal function must be frequently monitored and dose modifications must be done accordingly.
Drug Interactions:
Using Amikacin sulfate with the following medicines is not recommended, as it can cause a risk of adverse effects:
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Ibuprofen.
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Furosemide.
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Mannitol.
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Lysine.
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Succinylcholine.
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Vancomycin.
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Alcuronium.
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Live cholera vaccine.
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Decamethonium.
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Ethacrynic acid.
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Foscarnet.
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Gallamine.
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Cidofovir.
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Atracurium.
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Doxacurium.
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Hexafluronium.
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Pancuronium.
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Metocurine.
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Rapacuronium.
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Pipecuronium
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Tacrolimus.
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Rocuronium.
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Tubocurarine.
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Vecuronium.
Clinical Studies: Clinical studies have demonstrated that Amikacin sulfate is effective against gram-negative infections, and staphylococcal infections and may be considered as an initial therapy under certain conditions in serious infections of the respiratory tract, central nervous system, serious complicated and recurrent urinary tract infections (UTI), skin, soft tissues, bone, and joint infections. However, it may not be effective for uncomplicated, or initial episodes of UTI. Clinical trials have shown that Amikacin was effective against infections caused by gram-negative organisms, which were resistant to drugs such as Gentamycin, Tobramycin, etc.
Non-clinical Toxicology: Carcinogenicity and mutagenicity studies to evaluate the potential of Amikacin sulfate
have not been performed in animals. However, when Amikacin sulfate was administered daily to rats at four times the human dose, subcutaneously it did not cause any change in the male and female fertility.
Uses of Amikacin Sulfate in Specific Populations:
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Pregnancy: Amikacin sulfate belongs to aminoglycosides, and it has the potential to cause fetal harm or cause serious adverse effects to effects when administered to pregnant women. Female patients must use effective birth control measures during the treatment with Amikacin sulfate. If the patient becomes pregnant during the treatment, she should be informed of the potential risk to the fetus.
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Nursing Mothers: Adequate studies have not been conducted to determine the risk of using Amikacin sulfate during breastfeeding, however as most of the drugs have the potential to pass into the breast milk, this medication must be avoided during breastfeeding, or otherwise.
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Pediatric Use: Adequate studies have not been conducted in the pediatric population to demonstrate the use of Amikacin sulfate injection in children.
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Geriatric Use: Adequate data is not available to determine the effects of Amikacin sulfate injection in elderly people. However, patients with renal disorders may require dose modifications or the drug must be cautiously used with frequent monitoring.
