Ceftriaxone

Ceftriaxone is a broad-spectrum antibiotic from the cephalosporin group (3rd generation). It is used to treat various bacterial infections, including gonorrhea (the clap).

For gonorrhea, ceftriaxone is the drug of choice, as many gonococcal strains have become resistant to other antibiotics. Treatment is given as a single injection, often in combination with oral azithromycin.

Ceftriaxone must be administered by healthcare professionals.

Ceftriaxone has a bactericidal effect by inhibiting cell wall synthesis:

Mechanism of action:

• Binds to the penicillin-binding proteins (PBPs) of bacteria
• Inhibits the cross-linking of peptidoglycan
• The bacterial cell wall becomes unstable
• The bacteria burst and die

Advantages in gonorrhea:

• Single-dose treatment is sufficient
• Reaches high tissue concentrations
• Low resistance rates

Pharmacokinetics:

• Long half-life (approx. 8 hours)
• Good penetration into all tissues
• Partly renal, partly biliary excretion

Ceftriaxone is suitable for:

• Uncomplicated gonorrhea (genital, pharyngeal, rectal)
• Gonorrhea during pregnancy
• Disseminated gonococcal infection
• Other severe bacterial infections

Standard treatment for gonorrhea: Ceftriaxone 500 mg i.m. (intramuscular) once PLUS azithromycin 2 g orally once

Not suitable for:

• Severe penicillin allergy (cross-allergy possible)
• Newborns who need or are expected to need calcium infusions

Gonorrhea – uncomplicated:

• 500 mg intramuscularly as a single dose
• Plus azithromycin 2 g orally

Gonorrhea with complications:

• 1-2 g intravenously every 24 hours
• For 7-14 days

Available strengths:

• Powder for solution for injection: 250 mg, 500 mg, 1 g, 2 g

Note: The injection is given into a large muscle group (usually the buttock). For doses >1 g, divide between two injection sites.

Administration: Ceftriaxone is administered as an injection by healthcare professionals. It is not suitable for self-administration.

For gonorrhea:

• A single injection into the gluteal muscle
• Together with oral azithromycin (2 g single dose)
• Follow-up check after 2 weeks recommended

After treatment:

• Sexual abstinence for 7 days
• Inform and treat all sexual partners from the last 60 days
• Testing for other STIs recommended (HIV, syphilis, chlamydia)

Ceftriaxone must not be used in cases of:

• Severe hypersensitivity to cephalosporins
• Known severe hypersensitivity (e.g. anaphylactic reaction) to other beta-lactam antibiotics (penicillins, monobactams and carbapenems)
• Newborns with hyperbilirubinemia
• Newborns receiving calcium infusions

Caution in cases of:

• Penicillin allergy (approx. 10% cross-allergy)
• Renal insufficiency
• Liver disease
• Gallstone disease (may cause biliary sludge)

Pregnancy: Can be used when appropriately indicated. For gonorrhea during pregnancy, ceftriaxone is the drug of choice.

Breastfeeding: Passes into breast milk in small amounts. Use is possible.

Common (1-10%):

• Diarrhea
• Pain at the injection site
• Elevated liver enzymes
• Skin rash

Uncommon:

• Nausea, vomiting
• Headache
• Fungal infections (oral thrush, vaginal yeast infection)
• Changes in blood count

Rare:

• Allergic reactions
• Pseudomembranous colitis
• Gallstones/biliary sludge
• Kidney stones

Jarisch-Herxheimer reaction: When treating syphilis, fever and deterioration may occur.

Contraindicated in newborns:

• Calcium-containing infusion solutions (fatal precipitation possible)

Interactions:

• Anticoagulants – increased tendency to bleed
• Aminoglycosides – synergistic effect (desired in severe infections)

No interactions with:

• Hormonal contraception
• Most oral medications