What is Ceftriaxone?

In recent years, the development of antibiotic drugs has become one of the essential factors in the control and treatment of infections. One of the important drugs in this field is ceftriaxone, which is an antibiotic with broad and effective effects in the treatment of various infections including respiratory, urinary, digestive and skin. Ceftriaxone has been introduced as a semi-synthetic cephalosporin with enhanced antibacterial properties. In addition to infection control, this drug also plays an important role in preventing the development of resistance in bacteria. This is a very important issue, because the resistance of bacteria to antibiotics is a serious challenge in treating patients and controlling epidemics.

Pharmaceutical forms of ceftriaxone

1. Injection solution: 1 g / 50 ml, 2 g / 50 ml
2. Powder for injection: 250 mg, 500 mg, 1 g, 2 g, 10 g, 100 g

Ceftriaxone uses

Ceftriaxone is used to treat a wide variety of bacterial infections. This drug belongs to a class of drugs called cephalosporin antibiotics, which work by stopping the growth of bacteria. The use of this drug in babies with high blood bilirubin levels and premature babies is not recommended due to the increased risk of side effects.

Uses of ceftriaxone in adults

1. Intra-abdominal infections
2. Acute bacterial otitis media
3. Pelvic inflammatory disease
4. Artificial joint infection
5. meningitis
6. Acute pyelonephritis without complications
7. Uncomplicated gonococcal infections
8. Surgical prophylaxis

Uses of ceftriaxone in children

1. Acute bacterial otitis media
2. Epiglottis (off label)
3. meningitis
4. Serious infections other than meningitis
5. Skin or skin structure infections
6. Gonococcal infections

Pharmacological effects and mechanism of action of ceftriaxone drug

The third generation cephalosporin is a broad-spectrum gram-negative activity that has less effect against gram-positive organisms, but is more effective against resistant organisms. It is very stable in the presence of beta-lactamases (penicillinase and cephalosporinase) of gram-negative and gram-positive bacteria. Bactericidal activity results from inhibition of cell wall synthesis by binding to 1 or more penicillin-binding proteins. It has an antimicrobial effect by interfering with the synthesis of peptidoglycan (the main structural component of the bacterial cell wall). Bacteria eventually lyse because the activity of cell wall autolytic enzymes continues while cell wall assembly ceases.

Distribution of the drug occurs throughout the body, including the gallbladder, lungs, bone, bile, and CSF (higher concentrations are obtained when the meninges are inflamed). It also passes through the placenta; It enters the amniotic fluid and breast milk. The half-life of this drug is 5-9 hours (normal liver and kidney function) and 12-16 hours (mild to severe renal failure) and excretion is through urine (33-67% as unchanged drug) and feces.

Ceftriaxone dosage

This drug is usually prescribed once or twice a day by injection into a muscle or vein. Dosage is based on your medical condition and response to treatment. Drink plenty of fluids while using this medication, unless your doctor tells you otherwise. Avoid mixing ceftriaxone with IV fluids that contain calcium (eg, Ringer’s solution, Hartmann’s solution, parenteral nutrition-TPN/PPN). Consult your pharmacist for more details about the safe use of IV calcium products in infants, children, and adults.

Ceftriaxone administration time in adults

1. For the treatment of complicated, mild to moderate intra-abdominal infections, use 1-2 g intravenously as a single daily dose or in divided doses every 12 hours for 4-7 days, with metronidazole.
2. Pelvic inflammatory disease, 250 mg intramuscularly as a single dose with doxycycline with or without metronidazole for 14 days.
3. Artificial joint infection, 2 grams per 24 hours as an intravenous injection for 2-6 weeks until clinical improvement is observed and the patient is afebrile for 48-72 hours.
4. Ceftriaxone is used for meningitis, 2 grams every 12 hours as an intravenous injection for 7-14 days.
5. Ceftriaxone is suitable for uncomplicated gonococcal infection of the pharynx, cervix, urethra or rectum. The dose used for a weight less than 150 kg is 500 mg daily as a muscle injection and for a weight greater than 150 kg 1000 mg is used as a muscle injection.
6. Of note, if chlamydial infection has not been ruled out, add doxycycline 100 mg BID every 7 days, or if pregnant, give azithromycin 1000 mg.
7. Necrotizing infection of the skin and soft tissues (due to Aeromonas hydrophilic), 1-2 g intravenously per day in combination with doxycycline and due to Vibrio vulnificus; Use 1 gram as an intravenous injection in combination with doxycycline.
8. Continue treatment until no further debridement is required, clinical improvement is observed, and the patient is afebrile for 48 to 72 hours.

How to use Ceftriaxone in children

1. The dosage for acute bacterial otitis media is 50 mg/kg by intramuscular injection, which should not exceed 1 gram per day.
2. For epiglottis treatment (off-label), continue 100 mg/kg on the first day, 50 mg/kg on the second day, 75 mg/kg on the third day as an intravenous injection daily for 10-14 days.
3. For the treatment of meningitis, a single dose of 100 mg/kg daily as an intravenous injection every 12 hours for 7-14 days is used.
4. For serious infections other than meningitis, 50-75 mg/kg is used as an intravenous and intramuscular injection every 12 hours for 7-14 days.
5. For the treatment of skin or skin structure infections in people over 12 years of age, 1-2 grams daily by intravenous and intramuscular injection in a single daily dose or divided every 12 hours for 7-14 days.

Precautions

Before taking ceftriaxone, if you are allergic to it or other antibiotics (such as penicillins and cephalosporins), avoid taking it. This medicine may contain inactive ingredients that can cause allergic reactions or other problems. Consult your doctor if you have medical history, including gallbladder disease, kidney disease, liver disease, stomach or intestinal diseases (such as colitis), etc. Intravenous calcium (including intravenous solutions such as Ringer’s solution, Hartmann’s solution, parenteral nutrition-TPN/PPN) should be used with caution in infants less than one month of age receiving this drug. Doing so can cause serious problems in vital organs.

1. Immune-mediated hemolytic anemia has been reported. If the patient develops anemia while taking ceftriaxone, discontinue the antibiotic until the cause is determined. Severe hemolytic anemia, including death, has been reported in both adults and children.
2. Ceftriaxone may increase the INR, especially in patients with malnutrition, liver or kidney disease, and long-term therapy should be used with caution.
3. Superinfections and promotion of nonsusceptible organisms occur with prolonged use or repeated treatment.
4. Abnormal ultrasound of the gallbladder has been reported, possibly as a result of ceftriaxone-calcium deposits. Discontinue use if signs or symptoms of gallbladder disease develop.
5. Ceftriaxone-calcium deposits in the urinary tract were observed in patients receiving ceftriaxone, which in some cases were diagnosed as ultrasound abnormalities. Some patients are asymptomatic and some may develop symptoms of calculi and ureteral obstruction and post-renal acute renal failure, which seems to be reversible after discontinuation of treatment and appropriate management. ensuring adequate hydration; Discontinue therapy in patients who develop signs and symptoms suggestive of kidney stones, oliguria, or renal failure and ultrasound findings.
6. Pancreatitis secondary to biliary obstruction has been rarely reported. It should be used with caution in patients with diseases of the gallbladder, bile ducts, liver or pancreas and patients with a history of penicillin allergy.
7. Clostridium difficile-associated diarrhea (CDAD) has been reported with the use of almost all antibacterial agents, including ceftriaxone.

Ceftriaxone contraindications

1. documented hypersensitivity; Hyperbilirubinemic infants, especially those who are preterm and infants less than 28 days old, if receiving calcium-containing IV products
2. Intravenous injection of ceftriaxone solutions containing lidocaine
3. Contraindications for lidocaine in case of using lidocaine solution as a solvent together with ceftriaxone for intramuscular injection

Ceftriaxone side effects

Inflammation at the injection site, diarrhea and vomiting, headache, pain, anemia, etc. are some of the side effects of ceftriaxone. If any of these effects persist or worsen, tell your doctor or pharmacist right away. Most people who use this drug do not experience serious side effects. Some serious side effects of this drug include easy bruising and bleeding, unusual tiredness, symptoms of gallbladder disease (such as stomach or abdominal pain, nausea, vomiting), symptoms of kidney problems (such as changes in the amount of urine), pink, bloody, and dark urine. Painful urination, back and side pain, yellow eyes and skin, uncontrollable movements, confusion, etc.

1. Eosinophilia
2. Thrombocytosis
3. diarrhea
4. Increased liver transaminases
5. Leukopenia
6. rush
7. Increased blood urea nitrogen
8. Strength in place
9. the pain
10. Agranulocytosis
11. anaphylaxis
12. Anemia

Drug interaction of ceftriaxone

1. Class X interactions (avoidance): B. G. (intravesical), cholera vaccine
2. Reducing the effects of drugs by ceftriaxone: aminoglycosides, BTH (intravesical), BTH vaccine (immunogenic), cholera vaccine, lactobacillus and sterol, sodium picosulfate, typhoid vaccine
3. Enhancement of drug effects by ceftriaxone: aminoglycosides, vitamin K antagonists
4. Enhancement of the effects of ceftriaxone by drugs: calcium salts (intravenous), probenecid, Ringer’s injection (lactated)

Ceftriaxone drug use during pregnancy and breastfeeding

Some reports and available data have not demonstrated an increased risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. The estimated background risk of birth defects and miscarriage for the specified population is unknown. All pregnancies have a background risk of birth defects, loss, or other adverse outcomes. Also, in animal reproduction studies, no adverse developmental effects were observed when ceftriaxone was administered to pregnant rats at doses approximately 2.8 times the clinical dose of 2 g/day.

The effect of ceftriaxone on breastfeeding

Some available data report that ceftriaxone is present in human milk. However, there is no information about the drug’s effects on a nursing baby or milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for medication and dextrose injection and any possible side effects on the breastfed child from injectable antibiotics and dextrose injection or the mother’s underlying disease.

Ceftriaxone storage conditions

Ceftriaxone should be stored at room temperature (less than 30 degrees Celsius) and away from light. Note that all chemical and herbal medicines should be kept out of the reach of animals and children.

The last word of ceftriaxone drug

The advantages and unique features of Ceftriaxone, including its use in the treatment of patients with multiple sensitivities to other antibiotics, show the capacity to quickly and effectively control infections and the possibility of preventing the development of bacterial resistance. However, as we said in this article from the online pharmacy magazine, it is always necessary to pay attention to the appropriate uses, recommended doses, and duration of treatment when using this drug. Also, reviewing new documents and advanced research in the field of this antibiotic is essential in order to benefit from its best and most effective use in the treatment and prevention of bacterial resistance.

Site source: Medscape