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Fusidic acid (Systemic)


VA CLASSIFICATION
Primary: AM900

Commonly used brand name(s): Fucidin Leo.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).

*Not commercially available in the U.S.



Category:


Antibacterial (systemic) —

Indications

Note: Bracketed information in the Indications section refers to uses that are not included in U.S. product labeling.

General considerations
Fusidic acid is active against a wide variety of gram positive organisms especially staphylococci, Streptococci (including Pneumococci), and Corynebacteria. Fusidic acid is inactive against most gram negative bacteria.{01}


Accepted

[Bone and joint infections (treatment) or]
[skin and soft tissue infections (treatment)]—Fusidic acid is indicated for the treatment of infections due to penicillinase–producing and non-penicillinase-producing strains of Staphylococcus aureus{01}


Pharmacology/Pharmacokinetics

Mechanism of action/Effect:

Fusidic acid inhibits bacterial protein synthesis by interfering with amino acid transfer from aminoacyl-tRNA to protein on the ribosomes.{01}

Absorption:

Oral sodium fusidate tablets have a 91% bioavailability. Absorption of the film-coated tablets is complete when compared to a solution, however oral absorption is variable.{02} Oral fusidic acid hemihydrate (suspension) achieved a 22.5% bioavailability in pediatric patients following a 20 milligram/kilogram dose.{03}

Protein binding:

Very high (97 to 99%){04}

Biotransformation:

Metabolites include dicarboxylic ester/acid, 3-keto fusidic acid, hydroxy fusidic acid, glucuronide fusidic acid and a glycol metabolite.{05}


Elimination half-life:

Adults: approximately 5 to 6 hours{05}{06}

Time to peak concentration:

Oral tablets: 1.9 to 3 hours{06}

Peak plasma concentration:

Following an intravenous dose of 500 mg fusidic acid, a mean peak plasma level of 52.4 milligrams/liter (mg/L) was produced. Repeated doses of 500 mg every 8 hours for 3 days produced a mean peak plasma level of 123.1 mg/L.{02}

Following oral doses of sodium fusidate of 250, 500, 750, and 1000 mg blood levels of 11.6, 30.6, 48.1, and 65.2 mg/L respectively were obtained.{06}

Elimination:
    Fusidic acid is extensively excreted in the bile; 0.3% is present as the unmetabolized drug, 15% is the glucuronide conjugate, 10% is the dicarboxylic metabolite and 3% is the hydroxy metabolite. Fusidic acid is excreted 20% in the feces.{05}


Precautions to Consider

Carcinogenicity/Mutagenicity

Long-term studies in animals have not been done to evaluate the carcinogenic or mutagenic potential of fusidic acid.

Pregnancy/Reproduction

Pregnancy—
Problems in humans have not been documented.{01}

Breast-feeding

Fusidic acid is distributed into breast milk.{01}

Pediatrics

Studies performed to date have not demonstrated pediatrics-specific problems that would limit the usefulness of fusidic acid in children.{01}


Geriatrics


No information is available on the relationship of age to the effects of fusidic acid in geriatric patients.

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

» Lincomycin or
» Rifampin    (may interfere due to a similar biliary excretion pathway)

{01}
» Aminosol infusion solution or
whole blood    (may increase the risk of hemolysis of the erythrocytes)

{01}

Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With physiology/laboratory test values
Increased hepatic function tests
Increased bilirubin or transaminases
Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Except under special circumstances, this medication should not be used when the following medical problem exists:
» Previous allergic/anaphylactic reaction to fusidic acid{01}
Risk-benefit should be considered when the following medical problems exist
» Hepatic function impairment    (fusidic acid is metabolized in the liver; patients with impaired or immature hepatic or renal function, especially neonates and infants, or adults with impaired hepatic function, may require a reduction in dose; serum concentrations should be monitored{01})



Patient monitoring
The following may be especially important in patient monitoring (other tests may be warranted in some patients, depending on condition; » = major clinical significance):

» Hepatic function tests    (fusidic acid may cause an increase in serum transaminases, and rarely, may cause jaundice; periodic assessment of hepatic function is recommended{01})

    (If elevated serum bilirubin level is detected, hepatic function should be closely monitored until the serum bilirubin concentration has returned to a satisfcatory level; If an elevated bilirubin level persists, administration of fusidic acid should be discontinued)




Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence less frequent
    
Jaundice (itching; loss of appetite; nausea ; abdominal or stomach pain; unusual tiredness or weakness; yellow eyes or skin)
    
thrombophlebitis or
venospasm (bluish color; changes in skin color; pain; tenderness; swelling of foot or leg)—observed with intravenous administration

Note: Cases of jaundice rarely have developed during treatment, usually following a rapid infusion or an excessive intravenous dose. The jaundice is usually accompanied by an elevated serum bilirubin level. Occasionally, serum transaminases may also be elevated. Alteration of the administration procedure by lengthening the infusion period or changing to oral treatment may help control this side effect. {01}


Incidence rare
    
Pruritis (skin rash)



Those indicating need for medical attention only if they continue or are bothersome
Incidence less frequent
    
Anorexia
dyspepsia (stomach pain; loss of appetite; acid or sour stomach; belching; heartburn; indigestion ), nausea
vomiting

Incidence rare
    
Pruritis (skin rash)



Those not indicating need for medical attention
Incidence rare
    
Blurred vision
dizziness
    
headache
{01}




Overdose
For more information on the management of overdose or unintentional ingestion, contact a poison control center (see Poison Control Center Listing).

Clinical effects of overdose
The following effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:
Acute
    
Diarrhea or (increase in bowel movements; loose stools; soft stools), epigastric or gastric discomfort

Chronic
    
Abnormal liver biochemistry
jaundice ( itching; loss of appetite; nausea; abdominal or stomach pain; unusual tiredness or weakness; yellow eyes or skin)


Treatment of overdose


Monitoring:
Excessive intravenous doses of fusidic acid may result in hypocalcemia due to the amount of phosphate buffer administered (each 10 milliliters of phosphate/citrate buffer for intravenous infusion contains 196 milligrams disodium hydrogen phosphate equivalent to 1.1 millimols of phosphate){01} Patient monitoring including serum calcium determinations and possible treatments may be required with intravenous overdoses of fusidic acid.{01}

Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric consultation.



Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Fusidic Acid (Systemic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Other medications, especially other antibiotics such as lincomycin, rifampin which have a similar biliary pathway. Aminosol infusion solution or whole blood should also be avoided during intravenous infusion of fusidic acid due to the increased risk of hemolysis.{01}
Other medical problems, especially previous allergic/anaphylactic reaction to fusidic acid or liver function impairment{01}

Proper use of this medication
» Not giving to infants up to 1 year of age

Proper administration technique for oral liquid
Shaking well before each dose

Using a specially marked measuring spoon or other device

Storing out of direct sunlight

» Proper dosing
Taking as soon as possible; not taking if almost time for next scheduled dose; not doubling doses


Side/adverse effects
Signs of potential side effects, especially jaundice, thrombophlebitis or venospasm


General Dosing Information
Fusidic acid should not be administered either by intramuscular or subcutaneous injection, since it has been demonstrated that local tissue injury occurs. It should not be infused with amino acid solutions or with whole blood because of the risk of hemolysis of the erythrocytes.{01}

Fusidic acid displaces bilirubin from its albumin binding site in vitro. The clinical significance of this finding is uncertain and kernicterus has not been observed in neonates receiving fusidic acid. However, this observation should be borne in mind when fusidic acid is given to preterm, jaundice, acidotic, or seriously ill patients.{01}

The total duration of treatment should be dictated by the patient's clinical condition and the results of bacteriological monitoring. For skin and soft tissue infections, the minimum duration of treatment should be 1 to 2 weeks. For acute osteomyelitis a minimum of 2 to 4 weeks is recommended; however, the treatment of chronic osteomyelitis may require several months. For more deep seated infections where other antibiotics have failed, a minimum of 2 to 4 weeks is recommended for septicemia, pneumonia and burns; and 1 to 2 months for endocarditis.{01}

For parenteral dosing forms:
Fusidic acid should be administered slowly over 2 hours or more.Total daily dosages should be administered in 3 separate equally divided doses at 8 hour intervals. Infusions should be made into a wide bore vein with good flow or a central venous catheter to minimize the risk of venospasms or thrombophlebitis.

For oral dosing forms:
Fusidic acid oral tablets or suspension may be administered with food to lessen possible gastrointestinal adverse reaction.{01}

For treatment of adverse effects
Lengthening the rate of intravenous administration may lessen the risk of venospasm and thrombophlebitis.{01}


Oral Dosage Forms

Note: Bracketed information in the Indications section refers to uses that are not included in U.S. product labeling.

FUSIDIC ACID HEMIHYDRATE SUSPENSION

Usual Adult Dose
[Skin and soft tissue infections or]
[bone and joint infections]
Oral, 15 milliliters (738 mg fusidic acid) three times daily{01}


Usual adult prescribing limits
Dose may be doubled to 30 milliliters for the treatment of fulminating infections.{01}

Usual Pediatric dose
[Skin and soft tissue infections or]
[ bone and joint infections]
Up to 1 year of age: 1 milliliter (49 mg fusidic acid) per kilogram body weight daily, divided into three equal doses
Age 1 to 5 years: 5 milliliters (246 mg fusidic acid) three times daily
Age 6 to 12 years: 10 milliliters (492 mg fusidic acid) three times daily


Usual pediatric prescribing limits
Doses may be doubled for fulminating infections.{01}

Strength(s) usually available
U.S.—

Canada—


246 mg fusidic acid per 5 milliliters (Rx) [Fucidin Leo]

Packaging and storage:
Store between 15 and 30 °C (59 and 82 °F).{01}

Auxiliary labeling:
   • Shake well.
   • Protect from light.
   • Do not dilute suspension.
   • Continue medicine for full time of treatment.


SODIUM FUSIDATE TABLETS

Usual Adult Dose
[Skin and soft tissue infections or]
[ bone and joint infections]
Oral, 500 mg sodium fusidate three times daily{01}


Usual adult prescribing limits
Up to 1 gram three times daily for fulminating infections.{01}

Strength(s) usually available
U.S.—

Canada—


250 mg sodium fusidate (240 milligrams fusidic acid) (Rx) [Fucidin Leo]

Packaging and storage:
Store between 15 and 25 °C (59 and 77 °F).{01}

Auxiliary labeling:
   • Continue medicine for full time of treatment.



Parenteral Dosage Forms

Note: Bracketed information in the Indications section refers to uses that are not included in U.S. product labeling.

SODIUM FUSIDATE INJECTION

Usual Adult Dose
[Skin and soft tissue infections or]
[ bone and joint infections]
Intravenous 500 mg sodium fusidate (480 mg fusidic acid) three times daily infused over at least 2 hours{01}


Usual adult prescribing limits
Total daily dose should not exceed 2 grams{01}

Usual pediatric dose
[Skin and soft tissue infections or]
[ bone and joint infections]
1 to 12 years of age: 20 milligrams sodium fusidate (19.2 mg fusidic acid) per kilogram body weight daily, divided into three equal doses and each of which should be infused over a period not less than 2 hours{01}


Strength(s) usually available
U.S.—

Canada—


500 mg sterile sodium fusidate (480 milligrams fusidic acid) (Rx) [Fucidin Leo]

Packaging and storage:
Store between 15 and 30 °C (59 and 82 °F).{01}

Incompatibilities:
Infusion solutions containig sodium fusidate are incompatible with kanamycin, gentamicin, vancomycin, cephaloridine, carbenicillin, whole blood, amino acid solutions and clacium containig solutions{01}. If these medications are to be concurrently administered, they should be administered in separate sites{01}.



Developed: 05/04/2000



References
  1. Product Information: Fucidin Leo ®, Fusidic acid. Leo Pharma Inc., Ajax, Ontario, Canada, reviewed 4/2000.
  1. Taburet AM, Guibert J, Kitzis MD et al: Pharmacokinetics of sodium fusidate after single and repeated infusions and oral administration of a new formulation. J Antimicrob Chemother 1990; 25(suppl B):23-31.
  1. Bourget P, Duhamel JF, Sorensen H et al: Pharmacokinetics of fusidic acid after a single dose of a new paediatric suspension. J Clin Pharm Ther 1993; 18:171-177.
  1. Bannatyne RM & Cheung R: Protein binding of fusidic acid. Curr Ther Res 1982; 31:159-161.
  1. Reeves DS: Review: the pharmacokinetics of fusidic acid. J Antimicrob Chemther 1987; 20:467-476.
  1. MacGowan AP, Greig MA, Andrews JM et al: Pharmacokinetics and tolerance of a new film-coated tablet of sodium fusidate administered as a single oral dose to healthy volunteers. J Antimicrob Chemother 1989; 23:409-415.
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