Amikacin – Dosing

Background

Amikacin is a semi-synthetic aminoglycoside antibiotic that is derived from kanamycin A. Amikacin is synthesized by acylation with the l-(-)-γ-amino-α-hydroxybutyryl side chain at the C-1 amino group of the deoxystreptamine moiety of kanamycin A.

Amikacin’s unique property is that it exerts activity against more resistant gram-negative bacilli such as Acinetobacter baumanii and Pseudomonas aeruginosa. Amikacin also exerts excellent activity against most aerobic gram-negative bacilli from the Enterobacteriaceae family, including Nocardia and some Mycobacterium (M. avium-intracellulare, M. chelonae, and M. fortuitum). M. avium-intracellulare (MAC) is a type of nontuberculous mycobacteria (NTM) found in water and soil. Symptoms of this disease include a persistent cough, fatigue, weight loss, night sweats, and shortness of breath and the coughing up of blood.

Several forms of amikacin are used currently, including an intravenous (IV) or intramuscular (IM) injection. In September 2018, a liposomal inhalation suspension of this drug was approved by the FDA for the treatment of lung disease caused by Mycobacterium avium complex (MAC) bacteria in a small population of patients with the disease who do not respond to traditional treatment.

Brand names

Amikin, Amiglyde-V, Arikayce, Amikin Pediatric

amikacin-sulfate-injection vial.jpg

Storage of Amikacin

Store at controlled room temperature 15°-30°C (59°-86°F).

Identity of Amikacin

Type of medicine Aminoglycosides
Synonyms Amikin, Amikin Pediatric
Molecular Formula C22H43N5O13
Molecular Weight 585.6 g/mol
IUPAC Names (2S)-4-amino-N-[(1R,2S,3S,4R,5S)-5-amino-2-[(2S,3R,4S,5S,6R)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4-[(2R,3R,4S,5S,6R)-6-(aminomethyl)-3,4,5-trihydroxyoxan-2-yl]oxy-3-hydroxycyclohexyl]-2-hydroxybutanamide
Structural formula of main components Amikacin structural image.png
Pure active ingredient Amikacin sulfate
Appearance White crystalline powder
Melting point 203-204 °C
Available as Tablets and Injectable solution
Prescription Doctor prescription is required

What is Amikacin (Amikin) used for?

  • Bacteremia
  • Intraabdominal Infection
  • Joint Infection
  • Meningitis
  • Mycobacterium avium-intracellulare — Treatment
  • Osteomyelitis
  • Peritonitis
  • Pneumonia
  • Skin or Soft Tissue Infection
  • Bacterial Infection
  • Tuberculosis — Active
  • Urinary Tract Infection
  • Tuberculosis – Urinary Tract
  • Tuberculous Esophagitis
  • Ocular Tuberculosis
  • Infection – Bacterial/Fungal/Protozoal/Viral
  • Adrenal Tuberculosis
  • Tuberculous Pleurisy
  • CNS Tuberculosis
  • Pulmonary Tuberculosis

Possible side effects of Amikacin

  • Decreased kidney function
  • Feeling dizzy
  • Trouble standing
  • Hearing a roaring noise
  • Loss of hearing
  • Muscle twitching or feeling weak
  • Need to urinate less
  • Diarrhea
  • Nausea
  • Vomiting
  • Upset stomach
  • Allergic reaction with these symptoms: rash, hives, itching, chills, fever, short of breath, muscle aches, swelling of the face or neck, headache, tight feeling in throat, or coughing

These are the most common side effects, but there may be others. Please report all side effects to the doctor or nurse. In case of a severe side effect or reaction, call the doctor, nurse, or pharmacist

Mechanism of Action

Amikacin binds to the 30 S bacterial ribosome subunit, resulting in interference with a reading of the genetic code and inhibition of protein synthesis, e.g., elicits premature protein termination and incorporation of incorrect amino acid.  Amikacin, as well as the rest of the aminoglycosides, are generally bacteriocidal and probably have an additional mechanism of action, which as yet remains undetermined. Aminoglycosides demonstrate bacterial killing that is concentration-dependent and also have a post-antibiotic effect.

Amikacin, when combined with penicillins, can have an additive effect on specific microorganisms.

Amikacin, when combined with carbapenems, can have a synergistic effect against some gram-positive organisms.

Amikacin may retain activity against tobramycin- and gentamicin-resistant strains because of reduced inactivation by bacterial acetylase, adenylase, and phosphorylase. Thus, its routine clinical use should be reserved for difficult to treat serious nosocomial infections.

Interaction

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

Other medications that may affect the kidneys or hearing may increase the risk of kidney damage or hearing loss if taken with amikacin. Some examples include: amphotericin B, cidofovir, cisplatin, polymyxin B, tobramycin, cephalosporins such as cephaloridine, nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen, among others.

Dosage Forms & Strengths

Injectable solution

  • 50mg/mL
  • 250mg/mL

General Dosing: 15 mg/kg/day divided IV/IM q8-12hr

Urinary Tract Infection: 250 mg IV/IM q12hr

Extended Interval Dosing (q24 Hours)

First dose: 15 mg/kg IV based on lean body weight

Subsequent doses: consult pharmacist

Hospital Acquired Pneumonia

20 mg/kg/day IV; may administer with antipseudomonal beta-lactam or carbapenem

Dosage Modifications

Renal impairment

  • CrCl >90 mL/min and aged <60 yr: q8hr
  • CrCl 60-90 mL/min OR aged ≥60 yr: q12hr
  • CrCl 25-60 mL/min: q24hr
  • CrCl 10-25 mL/min: q48hr
  • CrCl <10 mL/min: q72hr
  • Administer after dialysis in ESRD

Overdose

In the event of overdosage or toxic reaction, peritoneal dialysis or hemodialysis will aid in the removal of amikacin from the blood. In the newborn infant, exchange transfusion may also be considered.

Precautions

Your doctor will check your progress closely while you or your child are receiving this medicine. This will allow your doctor to see if the medicine is working properly and to decide if you or your child should continue to receive it. Blood, urine, hearing, and nerve tests may be needed to check for unwanted effects.

If your or your child’s symptoms do not improve within a few days, or if they become worse, check with your doctor.

Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant. If you think you have become pregnant while using the medicine, tell your doctor right away.

This medicine may cause serious allergic reactions, including anaphylaxis, which can be life-threatening and require immediate medical attention. Call your doctor right away if you or your child have itching; hives; hoarseness; shortness of breath; trouble breathing; trouble swallowing; or any swelling of your hands, face, or mouth after you receive this medicine.

Stop using this medicine and check with your doctor right away if you or your child have sudden decrease in hearing or loss of hearing, which may be accompanied by dizziness and ringing in the ears. Tell your doctor if you or your child have dizziness or lightheadedness; feeling of constant movement of self or surroundings; or sensation of spinning. These may be symptoms of a damage to your hearing or sense of balance.

Tell your doctor right away if you have trouble using your muscles or trouble breathing while receiving this medicine.

Check with your doctor right away if you or your child have blood in the urine, change in frequency of urination or amount of urine, difficulty with breathing, drowsiness, increased thirst, loss of appetite, nausea or vomiting, swelling of feet or lower legs, or weakness. These may be symptoms of a serious kidney problem.

This medicine may cause nerve problems. Check with your doctor right away if you or your child have numbness, skin tingling, muscle twitching, or seizures.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Is amikacin safe to take if I’m pregnant or breastfeeding?

Amikacin is harmful to the fetus and should not be used during pregnancy unless there are not safer options.

It is not known whether Amikacin enters breast milk; therefore, it is best to be cautious before using it while breastfeeding.

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