Ceftriaxone
Encyclopedia
Ceftriaxone (icon) is a third-generation cephalosporin
antibiotic
. Like other third-generation cephalosporins, it has broad spectrum activity against Gram-positive and Gram-negative bacteria
. In most cases, it is considered to be equivalent to cefotaxime
in terms of safety and efficacy. Ceftriaxone sodium is marketed by Hoffman-La Roche under the trade name
Rocephin.
and/or aminoglycoside
antibiotics) for the treatment of community-acquired or mild to moderate health care-associated pneumonia
. It is also a choice drug for treatment of bacterial meningitis
. In pediatrics, it is commonly used in febrile infants between 4 and 8 weeks of age who are admitted to the hospital to exclude sepsis
.
The dosage for acute ear infection in the very young is 50 mg/kg IM, one dose only. It has also been used in the treatment of Lyme disease
, typhoid fever
and gonorrhea
.
Intravenous dosages may be adjusted for body mass in younger patients and is administered every 12–24 hours, at a dose that depends on the type and severity of the infection.
For the treatment of gonorrhea
, a single intramuscular injection is usually given. Treatment for chlamydia infection is also recommended (usually with azithromycin
) unless it is specifically ruled out.
It must not be mixed or administered simultaneously (within 48 hours) with calcium-containing solutions or products for patients younger than 28 days old, even via different infusion lines (rare fatal cases of calcium-ceftriaxone precipitates in lung and kidneys in neonates have been described).
To reduce the pain of intramuscular injection, ceftriaxone may be reconstituted with 1% lidocaine
.
Ceftriaxone has also been investigated for efficacy in preventing relapse to cocaine addiction.
Ceftriaxone seems to increase EAAT2 pump expression in central nervous system and has therefore a potential to reduce glutamatergic toxicity. Despite earlier negative results in 1990s, new, large clinical trials are underway to test its effacy in Amyotrophic lateral sclerosis
(ALS) patients.
of a 1% aqueous solution is approximately 6.7.
The syn-configuration of the methoxy
imino moiety confers stability to β-lactamase enzymes produced by many Gram-negative bacteria. Such stability to β-lactamases increases the activity of ceftriaxone against otherwise resistant Gram-negative bacteria. In place of the easily hydrolysed
acetyl
group of cefotaxime, ceftriaxone has a metabolically stable thiotriazinedione moiety.
and bleeding are specific side effects. Haemolysis is reported. Biliary sludging
is another known though rare adverse effect which occurs primarily in neonates.
Cephalosporin
The cephalosporins are a class of β-lactam antibiotics originally derived from Acremonium, which was previously known as "Cephalosporium".Together with cephamycins they constitute a subgroup of β-lactam antibiotics called cephems.-Medical use:...
antibiotic
Antibiotic
An antibacterial is a compound or substance that kills or slows down the growth of bacteria.The term is often used synonymously with the term antibiotic; today, however, with increased knowledge of the causative agents of various infectious diseases, antibiotic has come to denote a broader range of...
. Like other third-generation cephalosporins, it has broad spectrum activity against Gram-positive and Gram-negative bacteria
Bacteria
Bacteria are a large domain of prokaryotic microorganisms. Typically a few micrometres in length, bacteria have a wide range of shapes, ranging from spheres to rods and spirals...
. In most cases, it is considered to be equivalent to cefotaxime
Cefotaxime
Cefotaxime is a third-generation cephalosporin antibiotic. Like other third-generation cephalosporins, it has broad spectrum activity against Gram positive and Gram negative bacteria...
in terms of safety and efficacy. Ceftriaxone sodium is marketed by Hoffman-La Roche under the trade name
Trade name
A trade name, also known as a trading name or a business name, is the name which a business trades under for commercial purposes, although its registered, legal name, used for contracts and other formal situations, may be another....
Rocephin.
Clinical use
Ceftriaxone is often used (in combination, but not direct, with macrolideMacrolide
The macrolides are a group of drugs whose activity stems from the presence of a macrolide ring, a large macrocyclic lactone ring to which one or more deoxy sugars, usually cladinose and desosamine, may be attached. The lactone rings are usually 14-, 15-, or 16-membered...
and/or aminoglycoside
Aminoglycoside
An aminoglycoside is a molecule or a portion of a molecule composed of amino-modifiedsugars.Several aminoglycosides function as antibiotics that are effective against certain types of bacteria...
antibiotics) for the treatment of community-acquired or mild to moderate health care-associated pneumonia
Pneumonia
Pneumonia is an inflammatory condition of the lung—especially affecting the microscopic air sacs —associated with fever, chest symptoms, and a lack of air space on a chest X-ray. Pneumonia is typically caused by an infection but there are a number of other causes...
. It is also a choice drug for treatment of bacterial meningitis
Bacterial meningitis
Bacterial meningitis refers to meningitis that is caused by bacterial infection.-Signs and Symptoms:*Fever*Seizures*Meningismus*Headache*Vomiting*Photophobia*Altered mental status and coma*Anorexia...
. In pediatrics, it is commonly used in febrile infants between 4 and 8 weeks of age who are admitted to the hospital to exclude sepsis
Sepsis
Sepsis is a potentially deadly medical condition that is characterized by a whole-body inflammatory state and the presence of a known or suspected infection. The body may develop this inflammatory response by the immune system to microbes in the blood, urine, lungs, skin, or other tissues...
.
The dosage for acute ear infection in the very young is 50 mg/kg IM, one dose only. It has also been used in the treatment of Lyme disease
Lyme disease
Lyme disease, or Lyme borreliosis, is an emerging infectious disease caused by at least three species of bacteria belonging to the genus Borrelia. Borrelia burgdorferi sensu stricto is the main cause of Lyme disease in the United States, whereas Borrelia afzelii and Borrelia garinii cause most...
, typhoid fever
Typhoid fever
Typhoid fever, also known as Typhoid, is a common worldwide bacterial disease, transmitted by the ingestion of food or water contaminated with the feces of an infected person, which contain the bacterium Salmonella enterica, serovar Typhi...
and gonorrhea
Gonorrhea
Gonorrhea is a common sexually transmitted infection caused by the bacterium Neisseria gonorrhoeae. The usual symptoms in men are burning with urination and penile discharge. Women, on the other hand, are asymptomatic half the time or have vaginal discharge and pelvic pain...
.
Intravenous dosages may be adjusted for body mass in younger patients and is administered every 12–24 hours, at a dose that depends on the type and severity of the infection.
For the treatment of gonorrhea
Gonorrhea
Gonorrhea is a common sexually transmitted infection caused by the bacterium Neisseria gonorrhoeae. The usual symptoms in men are burning with urination and penile discharge. Women, on the other hand, are asymptomatic half the time or have vaginal discharge and pelvic pain...
, a single intramuscular injection is usually given. Treatment for chlamydia infection is also recommended (usually with azithromycin
Azithromycin
Azithromycin is an azalide, a subclass of macrolide antibiotics. Azithromycin is one of the world's best-selling antibiotics...
) unless it is specifically ruled out.
It must not be mixed or administered simultaneously (within 48 hours) with calcium-containing solutions or products for patients younger than 28 days old, even via different infusion lines (rare fatal cases of calcium-ceftriaxone precipitates in lung and kidneys in neonates have been described).
To reduce the pain of intramuscular injection, ceftriaxone may be reconstituted with 1% lidocaine
Lidocaine
Lidocaine , Xylocaine, or lignocaine is a common local anesthetic and antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery.- History :Lidocaine, the first amino...
.
Ceftriaxone has also been investigated for efficacy in preventing relapse to cocaine addiction.
Ceftriaxone seems to increase EAAT2 pump expression in central nervous system and has therefore a potential to reduce glutamatergic toxicity. Despite earlier negative results in 1990s, new, large clinical trials are underway to test its effacy in Amyotrophic lateral sclerosis
Amyotrophic lateral sclerosis
Amyotrophic lateral sclerosis , also referred to as Lou Gehrig's disease, is a form of motor neuron disease caused by the degeneration of upper and lower neurons, located in the ventral horn of the spinal cord and the cortical neurons that provide their efferent input...
(ALS) patients.
Chemistry
Ceftriaxone is a white crystalline powder which is readily soluble in water, sparingly soluble in methanol and very slightly soluble in ethanol. The pHPH
In chemistry, pH is a measure of the acidity or basicity of an aqueous solution. Pure water is said to be neutral, with a pH close to 7.0 at . Solutions with a pH less than 7 are said to be acidic and solutions with a pH greater than 7 are basic or alkaline...
of a 1% aqueous solution is approximately 6.7.
The syn-configuration of the methoxy
Methoxy
In chemistry , methoxy refers to the functional group consisting of a methyl group bound to oxygen. This alkoxy group has the formula O–CH3.The word is used in organic nomenclature usually to describe an ether...
imino moiety confers stability to β-lactamase enzymes produced by many Gram-negative bacteria. Such stability to β-lactamases increases the activity of ceftriaxone against otherwise resistant Gram-negative bacteria. In place of the easily hydrolysed
Hydrolysis
Hydrolysis is a chemical reaction during which molecules of water are split into hydrogen cations and hydroxide anions in the process of a chemical mechanism. It is the type of reaction that is used to break down certain polymers, especially those made by condensation polymerization...
acetyl
Acetyl
In organic chemistry, acetyl is a functional group, the acyl with chemical formula COCH3. It is sometimes represented by the symbol Ac . The acetyl group contains a methyl group single-bonded to a carbonyl...
group of cefotaxime, ceftriaxone has a metabolically stable thiotriazinedione moiety.
Adverse Effect
HypoprothombinaemiaHypoprothrombinemia
Hypoprothrombinemia is a blood disorder in which a deficiency of prothrombin results in impaired blood clotting, leading to an increased physiological risk for bleeding, especially in the gastrointestinal system, cranial vault, and superficial integumentary system.-Causes:Hypoprothrombinemia can...
and bleeding are specific side effects. Haemolysis is reported. Biliary sludging
Gallstone
A gallstone is a crystalline concretion formed within the gallbladder by accretion of bile components. These calculi are formed in the gallbladder, but may pass distally into other parts of the biliary tract such as the cystic duct, common bile duct, pancreatic duct, or the ampulla of...
is another known though rare adverse effect which occurs primarily in neonates.