amikacin sulfate

amikacin sulfate

[am′ikā′sin]

an aminoglycoside antibiotic.

indication It is prescribed in the treatment of various severe infections caused by susceptible strains of gram-negative bacteria.

contraindications Concurrent use of certain diuretics or known hypersensitivity to this or other aminoglycosides prohibits its use. The drug is used with caution in patients who have impaired renal function or myasthenia gravis and those under the influence of neuromuscular blocking agents or other nephrotoxins.

adverse effects Among the most serious adverse reactions are nephrotoxicity, auditory and vestibular ototoxicity, and neuromuscular blockade. GI disturbances, pain at the site of injection, and hypersensitivity reactions may occur.

---

amikacin sulfate

a semisynthetic aminoglycoside antibiotic derived from kanamycin, used parenterally in the treatment of bacterial infections, particularly those caused by gram-negative organisms.

---

antibiotic 

1. Pertaining to the ability to destroy or inhibit other living organisms.

2. A substance derived from a mould or bacterium, or produced synthetically, that destroys (bactericidal) or inhibits the growth (bacteriostatic) of other microorganisms and is thus used to treat infections. Some substances have a narrow spectrum of activity whereas others act against a wide range of both gram-positive and gram-negative organisms (broad-spectrum antibiotics). Antibiotics can be classified into several groups according to their mode of action on or within bacteria: (1) Drugs inhibiting bacterial cell wall synthesis, such as bacitracin, vancomycin and the β-lactams based agents (e.g. penicillin, cephalosporins (e.g. ceftazidime, ceftriaxone, cefuroxime). (2) Drugs affecting the bacterial cytoplasmic membrane, such as polymyxin B sulfate and gramicidin. (3) Drugs inhibiting bacterial protein synthesis, such as aminoglycosides (e.g. amikacin sulfate, framycetin sulfate, gentamicin, neomycin sulfate and tobramycin), tetracyclines, macrolides (e.g. erythromycin and azithromycin) and chloramphenicol. (4) Drugs inhibiting the intermediate metabolism of bacteria, such as sulfonamides (e.g. sulfacetamide sodium) and trimethoprim. (5) Drugs inhibiting bacterial DNA synthesis, such as nalixidic acid and fluoroquinolones (e.g. ciprofloxacin, levofloxacin, moxifloxacin, norfloxacin and ofloxacin). (6) Other antibiotics such as fusidic acid, the diamidines, such as propamidine isethionate and dibrompropamidine. Syn. antibacterial. See antiinflammatory drug; fusidic acid.

---

amikacin sulfate

Amikin

Pharmacologic class: Aminoglycoside

Therapeutic class: Anti-infective

Pregnancy risk category D

FDA Boxed Warning

• Observe patient closely because of potential ototoxicity and nephrotoxicity. Safety isn't established for treatment exceeding 14 days.
• Neuromuscular blockade and respiratory paralysis have occurred after parenteral injection, topical use (as in orthopedic and abdominal irrigation), and oral use.
• Monitor renal function and eighth-nerve function closely, especially in patients with known or suspected renal impairment at onset of therapy, as well as those with initially normal renal function who develop signs of renal dysfunction during therapy.
• Avoid concurrent use with potent diuretics (such as furosemide and ethacrynic acid) because diuretics may cause ototoxicity. Also, I.V. diuretics may increase aminoglycoside toxicity by altering antibiotic serum and tissue levels.
• Avoid concurrent and sequential systemic, oral, or topical use of other neurotoxic or nephrotoxic products and other aminoglycosides. Advanced age and dehydration also may increase toxicity risk.

Action

Interferes with protein synthesis in bacterial cells by binding to 30S ribosomal subunit, leading to bacterial cell death

Availability

Injection: 50 mg/ml, 250 mg/ml

⊘Indications and dosages

➣ Severe systemic infections caused by sensitive strains of Pseudomonas aeruginosa, Escherichia coli, or Proteus, Klebsiella, Serratia, Enterobacter, Actinobacter, Providencia, Citrobacter, or Staphylococcus species

Adults, children, and older infants: 15 mg/kg/day I.V. or I.M. in two to three divided doses q 8 to 12 hours in 100 to 200 ml of dextrose 5% in water (D₅W) over 30 to 60 minutes. Maximum dosage is 1.5 g/day.

Neonates: Initially, 10 mg/kg I.M., then 7.5 mg/kg I.M. q 12 hours

➣ Uncomplicated urinary tract infections caused by susceptible organisms

Adults, children, and older infants: 250 mg I.M. or I.V. twice daily

Dosage adjustment

• Renal impairment (adults)
• Patients undergoing hemodialysis

Off-label uses

• Mycobacterium avium-intracellulare infection

Contraindications

• Hypersensitivity to aminoglycosides
• Parkinsonism
• Breastfeeding

Precautions

Use cautiously in:
• decreased renal function, neuromuscular disorders
• parkinsonism, myasthenia gravis
• elderly patients
• pregnant patients.

Administration

• Don't physically mix amikacin with other drugs. Administer separately.
• For I.V. use, dilute in 100 to 200 ml of normal saline solution or D₅W and give over 30 to 60 minutes.
• Ensure adequate fluid intake to avoid dehydration.
• Draw peak blood level 1 hour after I.M. infusion or 30 to 60 minutes after I.V. infusion.
• Draw trough blood level just before next dose.

Route	Onset	Peak	Duration
I.V.	Immediate	30 min	8-12 hr
I.M.	Variable	1 hr	8-12 hr

Adverse reactions

CNS: dizziness, vertigo, tremor, numbness, depression, confusion, lethargy, headache, paresthesia, ataxia, neuromuscular blockade, seizures, neurotoxicity

CV: hypotension, hypertension, palpitations

EENT: nystagmus and other visual disturbances, ototoxicity, hearing loss, tinnitus

GI: nausea, vomiting, splenomegaly, stomatitis, increased salivation, anorexia

GU: azotemia, increased urinary excretion of casts, polyuria, painful urination, impotence, nephrotoxicity

Hematologic: purpura, eosinophilia, leukemoid reaction, aplastic anemia, neutropenia, agranulocytosis, leukopenia, thrombocytopenia, pancytopenia, hemolytic anemia

Hepatic: hepatomegaly, hepatic necrosis, hepatotoxicity

Musculoskeletal: joint pain, muscle twitching

Respiratory: apnea

Skin: rash, alopecia, urticaria, itching, exfoliative dermatitis

Other: weight loss, superinfection, pain and irritation at I.M. site

Interactions

Drug-drug. Acyclovir, amphotericin B, cephalosporin, cisplatin, diuretics, vancomycin: increased risk of ototoxicity and nephrotoxicity

Depolarizing and nondepolarizing neuromuscular junction blockers, general anesthetics: increased amikacin effect, possibly leading to respiratory depression

Dimenhydrinate: masking of ototoxicity signs and symptoms

Indomethacin: increased trough and peak amikacin levels

Parenteral penicillin: amikacin inactivation

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, blood urea nitrogen, creatinine, lactate dehydrogenase, nonprotein nitrogen, nitrogen compounds (such as urea): increased levels

Calcium, potassium, magnesium, sodium: decreased levels

Reticulocytes: increased or decreased count

Patient monitoring

• Monitor kidney function test results and urine cultures, output, protein, and specific gravity.
• Monitor results of peak and trough drug blood levels.
• Evaluate for signs and symptoms of ototoxicity (hearing loss, tinnitus, ataxia, and vertigo).
• Assess for secondary superinfections, particularly upper respiratory tract infections.

Patient teaching

☞ Inform patient that drug may cause hearing loss, seizures, and other neurologic problems. Tell him to report these symptoms immediately.
• Instruct patient to immediately report fever, cough, breathing problems, sore throat, and other signs and symptoms of infection.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Instruct patient to notify prescriber if he's urinating much more or much less than normal.
• Advise patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.
• Inform patient that he'll undergo regular blood and urine testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.