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ceftriaxone sodium

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ceftriaxone sodium
[sef′trī·ak′sōn]
a parenteral third-generation cephalosporin antibiotic.
indications It is prescribed for infections of the lower respiratory tract, urinary tract, skin, abdomen, bones, and joints. It is also used to treat gonorrhea, septicemia, and meningitis and in surgical prophylaxis, particularly in coronary bypass operations. It has a comparatively long half-life and although its dosage must still be decreased with renal impairment, it is one of the few cephalosporins that is eliminated primarily by the liver.
contraindications It is contraindicated in patients who are hypersensitive to this product or to other cephalosporin antibiotics.
adverse effects Among reported adverse reactions are skin rash, diarrhea, eosinophilia, thrombocytosis, leukopenia, increased liver enzyme and blood urea nitrogen levels, and pain and tenderness at the site of injection.

ceftriaxone sodium

Rocephin

Pharmacologic class: Third-generation cephalosporin

Therapeutic class: Anti-infective

Pregnancy risk category B

Action

Interferes with bacterial cell-wall synthesis and division by binding to cell wall, causing cell to die. Active against gram-negative and gram-positive bacteria, with expanded activity against gram-negative bacteria. Exhibits minimal immunosuppressant activity.

Availability

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

Premixed containers: 1 g/50 ml, 2 g/50 ml

Indications and dosages

Infections of respiratory system, bones, joints, and skin; septicemia

Adults: 1 to 2 g/day I.M. or I.V. or in equally divided doses q 12 hours. Maximum daily dosage is 4 g.

Uncomplicated gonorrhea

Adults: 250 mg I.M. as a single dose

Surgical prophylaxis

Adults: 1 g I.V. as a single dose within 1 hour before start of surgical procedure

Meningitis

Adults: 1 g to 2 g I.V. q 12 hours for 10 to 14 days

Children: Initially, 100 mg/kg/day I.M. or I.V. (not to exceed 4 g). Then 100 mg/kg/day I.M. or I.V. once daily or in equally divided doses q 12 hours (not to exceed 4 g) for 7 to 14 days.

Otitis media

Children: 50 mg/kg I.M. as a single dose; maximum of 1 g/dose.

Skin and skin-structure infections

Children: 50 to 75 mg/kg/day I.V. or I.M. once or twice daily. Maximum dosage is 2 g daily.

Other serious infections

Children: 50 to 75 mg/kg/day I.V. or I.M. once or twice daily

Off-label uses

• Disseminated gonorrhea
• Endocarditis
• Epididymitis
• Gonorrhea-associated meningitis
• Lyme disease
Neisseria meningitides carriers
• Pelvic inflammatory disease

Contraindications

• Hypersensitivity to cephalosporins or penicillins

Precautions

Use cautiously in:
• renal impairment, hepatic disease, biliary obstruction, phenylketonuria
• history of GI disease
• elderly patients
• pregnant or breastfeeding patients.

Administration

• Obtain specimens for culture and sensitivity testing as necessary before starting therapy.
• Know that drug for I.V. injection is compatible with sterile water, normal saline solution, dextrose 5% in water (D5W), half-normal saline solution, and D5W and normal saline solution.
• After reconstituting, dilute further to desired concentration for intermittent I.V. infusion. Infuse over 30 minutes.
• For I.M. use, reconstitute powder for injection with compatible solution by adding 0.9 ml of diluent to 250-mg vial, 1.8 ml to 500-mg vial, 3.6 ml to 1-g vial, or 7.2 ml to 2-g vial, to yield a concentration averaging 250 mg/ml.
• Divide high I.M. doses equally and administer in two separate sites. Inject deep into large muscle mass.

RouteOnsetPeakDuration
I.V.RapidEnd of infusion12-24 hr
I.M.Rapid1-2 hr12-24 hr

Adverse reactions

CNS: headache, confusion, hemiparesis, lethargy, paresthesia, syncope, seizures

CV: hypotension, palpitations, chest pain, vasodilation

EENT: hearing loss

GI: nausea, vomiting, diarrhea, abdominal cramps, oral candidiasis, pseudomembranous colitis

GU: vaginal candidiasis

Hematologic: lymphocytosis, eosinophilia, bleeding tendency, hemolytic anemia, hypoprothrombinemia, neutropenia, thrombocytopenia, agranulocytosis, bone marrow depression

Hepatic: jaundice, hepatomegaly

Musculoskeletal: arthralgia

Respiratory: dyspnea

Skin: urticaria, maculopapular or erythematous rash

Other: chills, fever, superinfection, pain at I.M. injection site, anaphylaxis, serum sickness

Interactions

Drug-drug. Aminoglycosides, loop diuretics: increased risk of nephrotoxicity

Probenecid: decreased excretion and increased blood level of ceftriaxone

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, bilirubin, blood urea nitrogen, creatinine, eosinophils, gamma-glutamyltransferase, lactate dehydrogenase: increased levels

Coombs' test, urinary 17-ketosteroids, nonenzyme-based urine glucose tests (such as Clinitest): false-positive results

Hemoglobin, platelets, white blood cells: decreased values

Drug-herbs. Angelica, anise, arnica, asafetida, bogbean, boldo, celery, chamomile, clove, danshen, fenugreek, feverfew, garlic, ginger, ginkgo, ginseng, horse chestnut, horseradish, licorice, meadowsweet, onion, papain, passionflower, poplar, prickly ash, quassia, red clover, turmeric, wild carrot, wild lettuce, willow: increased risk of bleeding.

Patient monitoring

Monitor for extreme confusion, tonic-clonic seizures, and mild hemiparesis when giving high doses.
• Monitor coagulation studies.
• Assess CBC and kidney and liver function test results.
• Monitor for signs and symptoms of superinfection and other serious adverse reactions.
• Be aware that cross-sensitivity to penicillins and cephalosporins may occur.

Patient teaching

• Instruct patient to report persistent diarrhea, bruising, or bleeding.
• Caution patient not to use herbs unless prescriber approves.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.



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In 2008, China totally exported about 500 tons, in which ceftriaxone sodium accounted for 40%.
 
 
 
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