Amikoside
Amikoside Uses, Dosage, Side Effects, Food Interaction and all others data.
Amikoside Sulfate is a semi-synthetic aminoglycoside antibiotic. Amikoside is active in vitro against Pseudomonas species, Escherichia coli, Proteus species, Providencia species, Klebsiella-Enterobacter species, Acinetobacter species, and Citrobacter freundii. When strains of the above organisms are found to be resistant to other aminoglycosides, including Gentamicin, TobrAmykin and KanAmykin, many are susceptible to Amikoside. Amikoside sulfate is active in vitro against penicillinase and nonpenicillinase-producing Staphylococcus species including methicillin-resistant strains.
Amikoside is an aminoglycoside antibiotic. Aminoglycosides bind to the bacteria, causing misreading of t-RNA, leaving bacteria unable to synthesize proteins vital to their growth. Aminoglycosides are useful mainly in the treatment infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, however, other antibiotics may be more potent and less toxic to humans.
Trade Name | Amikoside |
Availability | Prescription only |
Generic | Amikacin |
Amikacin Other Names | Amikacin, Amikacina, Amikacine, Amikacinum |
Related Drugs | amoxicillin, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, levofloxacin, Augmentin |
Weight | 100mg, 250mg, 500mg |
Type | Injection |
Formula | C22H43N5O13 |
Weight | Average: 585.6025 Monoisotopic: 585.285736487 |
Protein binding | The protein binding of amikacin in serum is ≤ 10%. |
Groups | Approved, Investigational, Vet approved |
Therapeutic Class | Aminoglycosides |
Manufacturer | Jagsonpal Pharmaceuticals Ltd, P,d,h, Pharmaceuticals (pvt) Ltd, |
Available Country | India, Pakistan |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Amikoside is used for the short-term treatment of serious infections due to susceptible strains of Gram-negative bacteria. It is effective in bacterial septicemia (including neonatal sepsis); in serious infections of the respiratory tract, bones and joints, central nervous system (including meningitis) and skin and soft tissue; intra abdominal infections (including peritonitis); and in bums and post operative infections (including post-vascular surgery). Amikoside is also effective in serious complicated and recurrent urinary tract infections due to susceptible Gram-negative organisms. It may be considered as initial therapy in suspected Gram-negative infections and therapy may be instituted before obtaining the results of susceptibility. Amikoside is also effective in infections caused by Gentamycln and/or TobrAmykin resistant strains of Gram-negative organisms. Amikoside has also been shown to be effective in Staphylococcal infection and may be considered as initial therapy under certain condition in the treatment of known suspected Staphylococcal disease such as, severe infections where the causative organism may either a Gram-negative bacterium or Staphylococcus infection due to susceptible strains of Staphylococcal I Gram-negative infections. In certain severe infections such as neonatal sepsis, concomitant therapy with a penicillin type drug may be used because of the possibility of infections due to Gram positive organism such as streptococci or pneumococci.
Amikoside is also used to associated treatment for these conditions: Bacterial Peritonitis, Bacterial Sepsis, Bone and Joint Infections, Burns, Central Nervous System Infections, Endophthalmitis, Infection caused by staphylococci, Infective pulmonary exacerbation of cystic fibrosis, Intra-Abdominal Infections, Lung Infection, Meningitis, Bacterial, Mycobacterium avium complex infection, Neonatal Sepsis, Nosocomial Pneumonia, Postoperative Infections, Respiratory Tract Infection Bacterial, Skin and Subcutaneous Tissue Bacterial Infections, Tuberculosis (TB), Grade 1, grade 2, grade 3, grade 4 Urinary Tract Infection, Severe Bacterial Infections
How Amikoside works
The primary mechanism of action of amikacin is the same as that for all aminoglycosides. It binds to bacterial 30S ribosomal subunits and interferes with mRNA binding and tRNA acceptor sites, interfering with bacterial growth. This leads to disruption of normal protein synthesis and production of non-functional or toxic peptides. Other actions have been postulated for drugs of this class. Amikoside, as well as the rest of the aminoglycosides, are generally bacteriocidal against gram-positive and gram-negative bacteria.
Dosage
Amikoside dosage
Adults and children: 15mg/kg/day in two equally- divided doses (equivalent to 500 mg bid in adults). Use of the 100 mg/2 ml strength is recommended for children for the accurate measurement of the appropriate dose.
Neonates and premature children: An initial loading dose of 10 mg/kg followed by 15 mg/kg/day in two equally divided doses.
Elderly: Doses should be adjusted under impaired renal function in elderly.
Life-threatening infections and/or those caused by pseudomonas: The adult dose may be increased to 500 mg every eight hours but should neither exceed 1.5 gm/day nor be administered for a period longer than 10 days. A maximum total adult dose of 15 gm should not be exceeded.
Urinary tract infections (Other than pseudomonal infections): 7.5 mg/kg/day in two equally divided doses (equivalent to 250 mg bid in adults).
Impaired renal function: In patient with impaired renal function the daily dose should be reduced and/or the intervals between doses increased to avoid accumulation of the drug. Simple doses schedule for renal impairment is given below:
Renal function Dosage schedule
Mild impairment 500 mg every 18 hours
Moderate impairment 500 mg every 24 hours
Severe impairment 250 mg every 24 hours.
Administration:
Intramuscular or intravenous administration: For most infections the intramuscular route is preferred, but in life threatening infections, or in patients in whom intramuscular injection route is not feasible the intravenous route may be used.
Intraperitoneal use: Amikoside may be used as an irrigant after recovery from anesthesia in concentration of 0.25%.
Other routes of administration: Amikoside in concentration of 0.25% may be used satisfactorily as an irrigating solution in abscess cavities, the pleural space, the peritoneum and the cerebral ventricles.
Intramuscular or intravenous administration: For most infections the intramuscular route is preferred, but in life threatening infections, or in patients in whom intramuscular injection route is not feasible the intravenous route may be used.
Intraperitoneal use: Amikoside may be used as an irrigant after recovery from anesthesia in concentration of 0.25%.
Other routes of administration: Amikoside in concentration of 0.25% may be used satisfactorily as an irrigating solution in abscess cavities, the pleural space, the peritoneum and the cerebral ventricles.
Side Effects
When the recommended precautions and dosages are followed the incidence of toxic reactous, such as tinnitus vertigo, and partial reversible or irreversible deafness, skin rash, drug fever, headache, paraesthesia, nausea and vomiting is low. Urinary signs of renal irritation, azotaemia and oliguria have been reported.
Toxicity
Oral (LD50): 6000 mg/kg (Mouse) . No antidote for toxicity is currently available. This drug is only 20% dialyzable; however, this is variable based on the type hemodialysis filter used.
Nephrotoxicity
Mild and reversible nephrotoxicity may be observed in 5 - 25% of patients. Amikoside accumulates in the proximal renal tubular cells. Tubular cell regeneration occurs despite continued drug exposure. Toxicity most commonly occurs several days following initiation of therapy. Amikoside may exacerbate pre-existing renal disease.
Ototoxicity
May cause irreversible ototoxicity. Ototoxicity appears to be correlated to cumulative exposure. Drug accumulation in the endolymph and perilymph of the inner ear causes irreversible damage to hair cells of the cochlea or summit of ampullar cristae in the vestibular complex. High- frequency hearing is lost first with progression leading to loss of low-frequency hearing. Further toxicity may lead to retrograde degeneration of the 8th cranial (vestibulocochlear) nerve. Vestibular toxicity may cause vertigo, nausea, vomiting, dizziness, and loss of balance.
Neuromuscular blockade
In addition to the above, amikacin may exacerbate neuromuscular blockade, however, this is less common.
Use in Pregnancy
Category D. Gentamicin and other aminoglycosides are known to cross the placenta. There is evidence of selective uptake of gentamicin by the fetal kidney resulting in damage to immature nephrons. Eighth cranial nerve damage has also been reported after in-utero exposure to some of the aminoglycosides. Because of the chemical similarity, all aminoglycosides should be considered potentially nephrotoxic and ototoxic to the developing fetus. Therapeutic blood amikacin levels in the mother do not equate with safety for the fetus. In reproductive toxicity studies in mice and rats, no effects on fertility or fetal toxicity were observed.
Use in Lactation
It is not known whether amikacin is excreted in breast milk. Since the possible harmful effect on the infant is not known, it is recommended that if nursing mothers must be given amikacin, the infants should not be breastfed during therapy.
Precaution
Since Amikoside is present in high concentrations in the renal excretory system, patients should be well hydrated to minimize chemical irritation of the renal tubules. If azotemia increases, treatment should be stopped. Monitoring of renal function during treatment with aminoglycosides is particularly important.
Interaction
Concurrent administration of Amikoside with myorelaxants leads to potentiation of their effects and there is a possibility of cessation of the breathing. The combination with other Aminoglycoside antibiotics should be avoided because of the augmentation of their ototoxic and nephrotoxic effects. Concurrent administration of Amikoside with fast acting diuretics increases the risk of ototoxicity in patients with renal failure. Combination with Cephalosporins or Polymixins increases the risk of nephrotoxicity.
Food Interaction
No interactions found.Amikoside Drug Interaction
Moderate: aspirin, aspirinUnknown: charcoal, charcoal, epinephrine, epinephrine, amoxicillin / clavulanate, amoxicillin / clavulanate, ciprofloxacin, ciprofloxacin, albuterol / ipratropium, albuterol / ipratropium, acetaminophen, acetaminophen, valproic acid, valproic acid, ascorbic acid, ascorbic acid, phytonadione, phytonadione
Amikoside Disease Interaction
Major: dehydration, neuromuscular blockade, ototoxicity, renal dysfunction
Volume of Distribution
- 24 L (28% of body weight healthy adult subjects).
Following administration of usual dosages of amikacin, amikacin has been found in bone, heart, gallbladder, and lung tissue. Amikoside is also distributed into bile, sputum, bronchial secretions, and interstitial, pleural, and synovial fluids.
Elimination Route
Rapidly absorbed after intramuscular administration. Rapid absorption occurs from the peritoneum and pleura. Poor oral and topical absorption. Poorly absorbed from bladder irrigations and intrathecal administration.
The bioavailability of this drug is expected to vary primarily from individual differences in nebulizer efficiency and airway pathology.
Following IM administration of a single dose of amikacin of 7.5 mg/kg in adults with normal renal function, peak plasma amikacin concentrations of 17-25 micrograms/mL are attained within 45 minutes to 2 hours.
Following IV infusion of the same dose given over 1 hour peak plasma concentrations of the drug average 38 micrograms/mL immediately following the infusion, 5.5 micrograms/mL at 4 hours, and 1.3 micrograms/mL at 8 hours.
Half Life
The plasma elimination half-life of amikacin is usually 2-3 hours in adults with normal renal function and is reported to range from 30-86 hours in adults with severe renal impairment.
Clearance
The mean serum clearance rate is about 100 mL/min and the renal clearance rate is 94 mL/min in subjects with normal renal function.
Elimination Route
This drug is eliminated by the kidneys. In adults with normal renal function, 94-98% of a single IM or IV dose of amikacin is excreted unchanged by glomerular filtration in the kidney within 24 hours. Amikoside can be completely recovered within approximately 10-20 days in patients with normal, healthy renal function.
In patients with impaired renal function, the clearance of amikacin is found to be decreased; the more severe the impairment, the slower the clearance. The interval between doses of amikacin should be adjusted according to the level of renal impairment. Endogenous creatinine clearance rate and serum creatinine which have a high correlation with serum half-life of amikacin, may be used as a guide for dosing.
Pregnancy & Breastfeeding use
The safety of Amikoside in pregnancy has not yet been established.
Contraindication
Amikoside injection is contraindicated in patients with a known history of hypersensitivity to Amikoside.
Special Warning
Impaired renal function: In patient with impaired renal function the daily dose should be reduced and/or the intervals between doses increased to avoid accumulation of the drug. Simple doses schedule for renal impairment is given below:
- Mild impairment: 500 mg every 18 hours
- Moderate impairment: 500 mg every 24 hours
- Severe impairment: 250 mg every 24 hours.
Pediatric Use: Safety and effectiveness of Amikoside for injection in children or adolescents under 16 years have not been established
Acute Overdose
In the event of overdose or toxic reaction, peritoneal dialysis or hemodialysis will aid in the removal of Amikoside from the blood.
Interaction with other Medicine
No information regarding drug interaction of Amikoside is available.
Storage Condition
Store in a cool dry place protected from light. Keep out of reach of children.
Innovators Monograph
You find simplified version here Amikoside
Amikoside contains Amikacin see full prescribing information from innovator Amikoside Monograph, Amikoside MSDS, Amikoside FDA label
FAQ
What is Amikoside used to treat?
Amikoside is a semi-synthetic aminoglycoside antibiotic derived from Kanamycin.It is used to treat certain serious infections that are caused by bacteria such as meningitis and infections of the blood, abdomen (stomach area), lungs, skin, bones, joints, and urinary tract.
What are the common side effects of Amikoside?
Common side effects of Amikoside include:
- diarrhea,
- hearing loss,
- spinning sensation (vertigo),
- numbness,
- skin tingling,
- muscle twitching and convulsions,
- dizziness,
- ringing or roaring in the ears,
- allergic reactions,
- Clostridium difficile associated diarrhea (CDAD),
- skin rash,
- drug fever,
- headache,
- numbness and tingling,
- tremor,
- nausea,
- vomiting,
- increase in white blood cells (eosinophilia),
- joint pain,
- anemia,
- low blood pressure, and
- low blood magnesium.
Is Amikoside safe for pregnancy?
Amikoside is harmful to the fetus and should not be used during pregnancy unless there are not safer options.
Is Amikoside safe for breastfeeding?
brfand is poorly excreted into breastmilk. it is best to be cautious before using it while breastfeeding.
Can Amikoside damage kidneys?
Amikoside can harm your kidneys, and may also cause nerve damage or hearing loss, especially if you have kidney disease or use certain other medicines.
When should I take Amikoside?
You should take Amikoside if you are not allergic to amikacin or similar antibiotics such as gentamicin, kanamycin, neomycin, paromomycin, streptomycin, or tobramycin.
Is Amikoside toxic?
Amikoside can cause neurotoxicity if used at a higher dose or for longer than recommended.
How long is Amikoside used for?
The recommended dose in prematures is 7.5 mg/kg in every 12 hours .The usual duration of treatment is 7 to 10 days.The total daily dose by all routes of administration should not exceed 15-20 mg/kg/day.
Can Amikoside be given alone?
Amikoside is rarely used alone and often combined with other antimicrobials.
What is indication of Amikoside?
Amikoside sulfate injection is indicated in the short-term treatment of serious infections due to susceptible strains of Gram-negative bacteria including Pseudomonas species, Escherichia coli, species of indole-positive and indole-negative Proteus, Providencia species, Klebsiella-Enterobacter-Serratia species.
Can Amikoside cause hearing loss?
amikacin or kanamycin is likely to result in the development of permanent hearing loss
How long does it take for Amikoside to work?
recommended dosage level, uncomplicated infections due to sensitive organisms should respond to therapy within 24 to 48 hours.
Can Amikoside be given orally?
There is no oral form available, as Amikoside is not absorbed orally.
How long does Amikoside stay in the body?
In adults with normal renal function the plasma elimination half-life of amikacin is usually 2-3 hours.
Can I drink alcohol with Amikoside?
Using alcohol certain medicines may also cause interactions to occur.
Can I drive after taking Amikoside?
Do not drive, use machinery after taking Amikoside.You may get drowsy or dizzy.