Introduction

Cefazolin sodium is a first-generation cephalosporin antibiotic used to treat a wide range of bacterial infections. It is commonly administered in hospital settings for its effectiveness against gram-positive bacteria and certain gram-negative bacteria. Cefazolin is available as an injectable medication, often used in surgical prophylaxis and treatment of infections such as skin and soft tissue infections, respiratory tract infections, and urinary tract infections.

Uses

Cefazolin sodium is used for:

  • Treatment of bacterial infections including skin and soft tissue infections, respiratory tract infections, bone and joint infections, and urinary tract infections.
  • Prophylaxis in surgical procedures to prevent postoperative infections.
  • Treatment of infections caused by susceptible strains of gram-positive bacteria and certain gram-negative bacteria.
Brand Name Cefazoline Panpharma
Type IM/IV Injection
Weight 1 gm/5 ml
Generic Cefazolin Sodium
Manufacturer City Overseas Ltd.
Available in English বাংলা

Mechanism of Action

Cefazolin sodium works by inhibiting bacterial cell wall synthesis. It binds to penicillin-binding proteins (PBPs) on the bacterial cell wall, interfering with the formation of peptidoglycan cross-links that are essential for cell wall integrity. This leads to cell lysis and death of the bacteria.

How Long Does It Take to Work?

The onset of action of cefazolin sodium is typically within 1 to 2 hours after administration. The therapeutic effects can be observed relatively quickly, but the full resolution of symptoms may take several days depending on the severity of the infection and the patient's overall health.

Absorption

Cefazolin sodium is not administered orally due to poor gastrointestinal absorption. Instead, it is given via intravenous (IV) or intramuscular (IM) injection, allowing for direct entry into the bloodstream.

Route of Elimination

Cefazolin sodium is primarily eliminated through the kidneys. It is excreted in the urine as unchanged drug, with approximately 60-70% of the dose being excreted in the urine within 24 hours.

Dosage

Adult Dose
  • Moderate to severe infection: 500 mg to 1 gm for every 6 to 8 hours
  • Mild infections caused by susceptible Gram-positive cocci: 250 mg to 500 mg for every 8 hours
  • Acute uncomplicated urinary tract infections: 1 gm for every 12 hours
  • Pneumococcal pneumonia: 500 mg for every 12 hours
  • Severe life-threatening infections (e.g. Endocarditis, Septicemia): 1 gm to 1.5 gm for every 6 hours. In rare instances, doses up to 12 gm per day can be used
Perioperative Prophylactic Use: To prevent postoperative infection in contaminated or potentially contaminated surgery, recommended doses are:
  • 1 gm IM or IV administered half hour to 1 hour prior to the start of surgery.
  • For lengthy operative procedures (e.g. 2 hours or more), 500 mg to 1 gm IM or IV during surgery.
  • 500 mg to 1 gm IM or IV every 6 to 8 hours for 24 hours postoperatively.
In surgery where the occurrence of infection may be particularly devastating (e.g. open-heart surgery and prosthetic arthroplasty), the prophylactic administration may be continued for 3 to 5 days following the completion of surgery.

The dosage of cefazolin sodium varies based on the type and severity of the infection, as well as patient factors such as renal function:

  • Adults: The typical dosage ranges from 1 to 2 grams every 8 hours, administered via IV or IM. For surgical prophylaxis, a single dose of 1 to 2 grams is usually given 30 minutes before surgery.
  • Pediatrics: Dosage is typically 25 to 50 mg/kg every 8 hours, not exceeding the adult maximum dose.

Administration

Cefazolin sodium is administered either intravenously or intramuscularly. For intravenous administration, the drug is usually diluted in a compatible fluid and given over a period of 3 to 5 minutes. For intramuscular administration, it is injected into a large muscle mass.

Side Effects

Common side effects of cefazolin sodium include:

  • Gastrointestinal disturbances such as nausea, vomiting, and diarrhea.
  • Local reactions at the injection site, including pain, redness, or swelling.
  • Allergic reactions, including rash, itching, and, rarely, anaphylaxis.

Toxicity

Toxicity is rare but can occur, particularly with overdose or rapid infusion. Symptoms of toxicity may include renal impairment, seizures, or gastrointestinal symptoms. Monitoring of renal function is recommended during prolonged therapy.

Precautions

Precautions for cefazolin sodium include:

  • Use with caution in patients with renal impairment, as dosage adjustments may be necessary.
  • Monitor for signs of anaphylaxis or severe allergic reactions, especially in patients with a history of penicillin allergy.
  • Periodic monitoring of renal function is advised during long-term therapy.

Interaction

Cefazolin sodium may interact with other medications, including:

  • Probenecid: Can increase cefazolin levels by inhibiting its renal excretion.
  • Anticoagulants: There may be an increased risk of bleeding, particularly if high doses are used.

Disease Interaction

Use cefazolin sodium with caution in patients with:

  • Renal disease, as dosage adjustments may be necessary.
  • History of severe allergic reactions to beta-lactam antibiotics.

Drug Interaction

Drug interactions with cefazolin sodium include:

  • Increased levels of cefazolin when used with probenecid.
  • Potential interactions with other antibiotics affecting gut flora or renal function.

Food Interactions

There are no significant food interactions with cefazolin sodium. However, it is advisable to follow general dietary recommendations and avoid excessive alcohol consumption, which can affect overall drug metabolism.

Pregnancy Use

Cefazolin sodium is classified as a Category B drug for pregnancy by the FDA, indicating that it is generally considered safe when used as directed. However, it should be used during pregnancy only if clearly needed and prescribed by a healthcare provider.

Lactation Use

Cefazolin sodium is excreted in breast milk in small amounts. It is generally considered safe for use during breastfeeding, but it is recommended to monitor the infant for any adverse effects.

Acute Overdose

In case of acute overdose, symptoms may include renal impairment or central nervous system effects such as seizures. Immediate medical attention should be sought if overdose is suspected.

Contraindication

Cefazolin sodium is contraindicated in patients with a known hypersensitivity to cephalosporins or penicillins. It should also be used with caution in individuals with a history of severe allergic reactions to beta-lactam antibiotics.

Use Direction

Follow the dosing instructions provided by the healthcare provider or included with the medication. Ensure proper administration technique and complete the full course of therapy to avoid recurrence of infection.

Storage Conditions

Cefazolin sodium should be stored at room temperature, away from light and moisture. Reconstituted solutions should be used promptly or stored according to the manufacturer's guidelines.

Volume of Distribution

The volume of distribution of cefazolin sodium is approximately 0.2 to 0.3 L/kg. It distributes well into body tissues and fluids, including skin, bone, and urine.

Half Life

The half-life of cefazolin sodium is approximately 1.8 to 2.5 hours in individuals with normal renal function. It may be prolonged in patients with renal impairment.

Clearance

The clearance of cefazolin sodium is primarily renal. Approximately 60-70% of the dose is excreted unchanged in the urine within 24 hours. Clearance may be reduced in patients with impaired renal function.

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Prof. Dr. Neyamat Ullah Khan

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Ear, Nose, Throat Specialist & Head Neck Surgeon

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