Nafcilline

Uses

Nafcilline is a penicillin derivative antibiotic used to treat susceptible staphylococcal infections.

Indicated in the treatment of infections caused by penicillinase-producing staphylococci which have demonstrated susceptibility to the drug.

Nafcilline is also used to associated treatment for these conditions: Bacterial Infections

How Nafcilline works

Like other penicillins, nafcillin exerts a bactericidal action against penicillin-susceptible microorganisms during the state of active multiplication in the bacterial cell wall synthesis . It inhibits the biosynthesis of the bacterial cell wall by forming covalent bonds with penicillin-binding proteins that play a critical role in the final transpeptidation process. Binding to penicillin-binding proteins inhibits the transpeptidase and carboxypeptidase activities conferred by these proteins and prevents the formation of the crosslinks .

Toxicity

Serious toxicity is unlikely following large doses of nafcillin. Acute ingestion of large doses of nafcillin may cause nausea, vomiting, diarrhea and abdominal pain. Acute oliguric renal failure and hematuria may occur following large doses. The oral LD50 in rats is >5000mg/kg and the intravenous LD50 in rats is >1000mg/kg .

Food Interaction

• Take on an empty stomach. Food may make the absorption of oral nafcillin unpredictable.

[Moderate] ADJUST DOSING INTERVAL: Certain penicillins may exhibit reduced gastrointestinal absorption in the presence of food.

The therapeutic effect of the antimicrobial may be reduced.

MANAGEMENT: The interacting penicillin should be administered one hour before or two hours after meals.

Penicillin V and amoxicillin are not affected by food and may be given without regard to meals.

Nafcilline Hypertension interaction

[Moderate] Each gram of parenteral nafcillin sodium contains approximately 67 mg (2.9 mEq) of sodium and is buffered with 40 mg of sodium citrate.

Each 250 mg capsule of nafcillin sodium contains approximately 17 mg (0.7 mEq) of sodium buffered with calcium carbonate.

The sodium content should be considered in patients with conditions that may require sodium restriction, such as congestive heart failure, hypertension, and fluid retention.

In addition, hypokalemia has been reported rarely during therapy with the penicillinase-resistant penicillins, which may be particularly important to bear in mind when treating patients with low potassium reserves or fluid and electrolyte imbalance.

Clinical monitoring of electrolytes is recommended if these agents are used for prolonged periods.

Nafcilline Drug Interaction

Major: warfarin, warfarinUnknown: amoxicillin / clavulanate, amoxicillin / clavulanate, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, meperidine, meperidine, insulin lispro, insulin lispro, insulin glargine, insulin glargine, furosemide, furosemide, escitalopram, escitalopram, esomeprazole, esomeprazole, sodium chloride, sodium chloride

Nafcilline Disease Interaction

Major: colitis, marrow toxicityModerate: renal/liver disease, sodium/potassium

Volume of Distribution

Nafcilline is reported to be widely distributed in various body fluids, including bile, pleural, amniotic and synovial fluids .

Elimination Route

Following intravenous administration of 500mg nafcillin, the mean plasma concentration was approximately 30 µg/mL. This value was reached after 5 minutes of injection .

Half Life

The serum half-life of nafcillin administered by the intravenous route ranged from 33 to 61 minutes as measured in three separate studies.

Elimination Route

Nafcilline is primarily eliminated by non-renal routes, namely hepatic inactivation and excretion in the bile.

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