Pantrixon

Pantrixon

ceftriaxone

Manufacturer:

Panpharma Healthcare

Distributor:

Panpharma Healthcare
Full Prescribing Info
Contents
Ceftriaxone sodium.
Description
Each 10-mL vial contains ceftriaxone (as sodium) 1 g.
Action
Antibacterial.
Pharmacology: Ceftriaxone sodium is a β-lactam antibiotic from the 3rd generation cephalosporin group.
Ceftriaxone is a broad-spectrum cephalosporin antibiotic resistant to β-lactamases. It is active against gram-positive aerobes (Staphylococcus metis, Streptococcus, Streptococcus pneumoniae), gram-negative aerobes (Borrelia burgdorferi, Branhamella catarrhalis, Citrobacter freundii, Citrobacter koseri, Enterobacter, Escherichia coli, Haemophilus influenzae, Klebsiella, Morganella morganii, Neisseria including N. meningitidis and N. gonorrheae, Proteus mirabilis, Proteus multocida, Proteus vulgaris, Providencia, Salmonella, Serratia, Shigella, Yersinia) and anaerobes (Clostridium perfringens, Fusobacterium, Peptostreptococcus, Prevotella).
Pharmacokinetics: Distribution: After IV infusion of a single dosage of 1 g, the maximum serum concentration is in average about 168 mg/L after 30 min. After IM injection of the same dosage, a serum peak of 80 mg/L is reached within 2 or 3 hrs.
The IM and IV routes are bioequivalent (similar areas under the curve). Ceftriaxone administered by IM route has an absolute bioavailability near 100%. The distribution volume of ceftriaxone is 7-12 L. The diffusion of ceftriaxone is good in the interstitial liquid, the tissues and the organic liquids (especially the cerebrospinal fluid, bile, bones, bronchial secretions, infectious areas of the ENT sphere).
Protein-Binding: The binding of ceftriaxone to serum proteins (albumin) is reversible and saturable. It may vary from 80-95% in the range of therapeutic concentrations. As the albumin rate is lower, the proportion of free ceftriaxone in the interstitial liquid is consequently higher than in the plasma.
Metabolism: Ceftriaxone is very poorly metabolized. The intestinal flora only transforms it to inactive metabolites.
Excretion: Ceftriaxone is excreted by urinary and biliary routes. The total serum clearance is 10-22 mL/min. The renal clearance is 5-12 mL/min. Fifty to 60% of ceftriaxone is excreted as unchanged form in the urine whereas around 40-50% is excreted in the bile. In adults, the elimination t½ is about 8 hrs long.
Pharmacokinetics in Particular Clinical Conditions: In newborns, the quantity of ceftriaxone remaining in the urine corresponds to about 70% of the administered dosage.
In newborns <8 days, the average elimination t½ is generally 2 or 3 times higher than in young adults; it is shorter in newborns 3-12 months.
In children and newborns, after a single IM injection of 50 mg/kg, the peak serum concentration of ceftriaxone is reached after 5.4 hrs (192±135mg/L).
In children and newborns, after a single IM injection, the diffusion in the middle ear is good with rates higher than the MIC of main bacillus responsible for middle ear acute disease during at least 48 hrs. After a single injection of 50 mg/kg, the total concentration of ceftriaxone in the middle ear liquid is about 5 mg/L after 1.5 hrs (33±20 mg/L), after the 15th hr, stable on the 24th hr (35±12 mg/L) and is still about 19±7mg/L after 48 hrs.
In patients with renal or hepatic insufficiency, ceftriaxone pharmacokinetics is very much different and the elimination t½ is only very poorly increased. If only the renal function is concerned, then the ceftriaxone biliary elimination is increased. If only the hepatic function is concerned, the renal elimination is increased.
Indications/Uses
Treatment of infections due to susceptible organisms. They include: Chancroid, endocarditis, gastroenteritis (invasive salmonellosis, shigellosis), gonorrhea, meningitis (including meningococcal meningitis prophylaxis except those due to Listeria monocytogenes), septicemia, syphilis, typhoid fever and Whipple's disease.
Lyme disease disseminated during the early stage with meningitis (secondary stage) and the delayed stage with neurological and articular systemic manifestations (tertiary stage).
Surgical infection prophylaxis for prostate transurethral resection.
Dosage/Direction for Use
Adults: Usual Dosage: 1 g/day as a single injection and up to 2 g/day as once-daily dose according to the severity of the infection and the patient's body weight.
Lyme Disease: 2 g/day as a single injection. Usual therapy is 14 days long and can be up to 21 days long in severe or delayed forms of the disease.
Prophylaxis of Postsurgical Infections: IV/IM injection of 1 g as a single dose when inducing anesthesia. The antibioprophylaxis must be of short duration and most often limited to the preoperative period, sometimes over 24 hrs. It shall never exceed 48 hrs.
Susceptibility to Purpura fulminans: The 1st dose should be administered via IV route if possible, otherwise by IM route 1-2 g.
Children and Infants: Usual Dosage: 50 mg/kg/day as a single injection.
Lyme Disease: 50-100 mg/day as a single injection. Usual therapy is 14 days long and can be up to 21 days long in severe or delayed forms of the disease.
Meningitis: The dosage may vary from 50-100 mg/kg/day as a single injection, the dosage at 100 mg/kg is only justified as attack treatment. However, in the newborn from 3-12 months, injections every 12 hrs may be recommended because of a shorter plasma t½.
Susceptibility to Purpura fulminans: The 1st dose should be administered if possible through IV route, otherwise via IM route 50-100 mg/kg without exceeding 1 g.
Acute Otitis Media: In case of therapeutic failure: 50 mg/kg/day for 3 days. In case of alternative treatment to oral treatment: 50 mg/kg as a single injection.
Neonates: 50 mg/kg as a single injection whatever the indication.
Elderly: Recommended dosages are the same in elderly patients as in adults.
Administration: Ceftriaxone may be administered through IM or IV route: Reconstitute the solution with the appropriate diluent (water for injection for IV use, lidocaine for IM use) as given in the dilution table. Shake well until dissolved and then withdraw the entire contents of the vial into the syringe and use immediately. (See table.)

Click on icon to see table/diagram/image

Use the preparation immediately after reconstitution or dilution. Do not use lidocaine in case of allergy to lidocaine. Do not use lidocaine for IV administration.
IM Injection: The IV form may be used IM but the lidocaine solution is absolutely contraindicated through IV route. IM injection for babies is carried out in the antero-lateral part of the thigh. Do not inject >1 g at the same body site. The reconstituted solutions maintain potency for at least 6 hrs at room temperature (25±2°C) or at 24 hrs between 2-8°C.
IV Injection: Inject slowly over 2-4 min in the vein or through the tubing of an infusion. The reconstituted solutions maintain potency for at least 6 hrs at room temperature (25±2°C) or at 24 hrs between 2-8°C.
Infusion: The infusion is about 30 min long. Two grams of ceftriaxone is dissolved in 40 mL of water for injection or in 40 mL of the following fluids commonly used for IV infusion: sodium chloride injection 0.9%, sodium chloride 0.45% + dextrose 2.5% solution, dextrose 5% solution, dextrose 10% solution, dextran 6% in dextrose 5% solution, hydroxyethylstarch 6-10%.
Overdosage
Ceftriaxone is poorly dialyzable. In case of overdosage, treatment must be symptomatic.
Contraindications
Allergy to penicillins and cephalosporins. The use of ceftriaxone with lidocaine is contraindicated in the following situations: Allergy to lidocaine or any other local anaesthetic product of the amide type, porphyria, unapplianced auriculo-ventricular block and cardiogenic shock.
Special Precautions
Treatment should be discontinued immediately should any sign of allergy appear. Prescribing cephalosporins requires the patient's preliminary inquiry as allergy to penicillins is crossed with allergy to cephalosporins in 5-10% of the cases.
Cephalosporins must be used with caution in penicillin-sensitive patients; a medical monitoring is necessary after the first administration.
Cephalosporins must not be prescribed in patients with a history of immediate allergy to cephalosporins. In case of any doubt, physician must monitor the patient on the 1st administration so as to treat any possible anaphylactic shock.
Hypersensitivity reactions (anaphylaxis) to cephalosporins and penicillins may be serious and even fatal.
In case of pain in the right side of hypochondrium, an echography should be carried out to look for an eventual biliary precipitate (see Adverse Reactions).
Studies indicate that ceftriaxone, just like other cephalosporins, may displace bilirubin from serum albumin. That is why newborns with hyperbilirubinemia and who receive ceftriaxone must be carefully monitored. Ceftriaxone must not be used in newborns (and particularly in premature babies) liable to develop an encephalopathy with bilirubin.
In case of prolonged treatment, regular control of the blood formula is necessary.
In case of severe renal insufficiency or renal and hepatic-associated insufficiencies, dosages should be adapted according to creatinine clearance.
Ceftriaxone must not be mixed with solutions containing calcium. When calcium-containing solutions are administered, it is recommended to infuse ceftriaxone through another route and at a period of time different from that on which calcium is infused even if the administration routes are different. When a risk of physical or chemical incompatibility with medicines other than calcium cannot be prevented, ceftriaxone must be administered exclusively; it can only be mixed with the solutions and substances mentioned in Dosage & Administration.
Concomitant use of ceftriaxone with oral anticlotting agents may increase anticlotting effect and hemorrhage risk.
Use in pregnancy & lactation: The studies carried out in animals did not reveal any teratogenic effect. Given the absence of teratogenic effects in animals, malformation in humans is not expected. In studies carried out on both species, substances responsible for malformation in the human species proved to be teratogenic in animals.
So far, ceftriaxone has been used on a limited number of pregnant women in hospitals and clinics. Seemingly, this use has revealed no malformation of fetotoxical particular effect. Nevertheless, additional studies are necessary to evaluate the consequences of such use during pregnancy. Therefore, ceftriaxone will only be used during pregnancy if absolutely necessary.
Ceftriaxone diffusion in the mother's milk is low (<5%); the ingested quantities are far inferior to therapeutic dosages. Consequently, nursing is possible during treatment with Pantrixon. Nevertheless, should diarrhea, candida or skin rash appear, nursing (or treatment with Pantrixon) shall be stopped.
Use In Pregnancy & Lactation
The studies carried out in animals did not reveal any teratogenic effect. Given the absence of teratogenic effects in animals, malformation in humans is not expected. In studies carried out on both species, substances responsible for malformation in the human species proved to be teratogenic in animals.
So far, ceftriaxone has been used on a limited number of pregnant women in hospitals and clinics. Seemingly, this use has revealed no malformation of fetotoxical particular effect. Nevertheless, additional studies are necessary to evaluate the consequences of such use during pregnancy. Therefore, ceftriaxone will only be used during pregnancy if absolutely necessary.
Ceftriaxone diffusion in the mother's milk is low (<5%); the ingested quantities are far inferior to therapeutic dosages. Consequently, nursing is possible during treatment with Pantrixon. Nevertheless, should diarrhea, candida or skin rash appear, nursing (or treatment with Pantrixon) shall be stopped.
Adverse Reactions
Skin Reactions: Allergic skin rash, urticaria. As with other cephalosporins, a few cases of severe mucocutaneous reactions were reported (erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome).
General Hypersensitivity Reactions: Fever, anaphylactic reactions.
Digestive Reactions: Stomatitis, diarrhea, nausea, vomiting, pseudomembranous colitis (rare).
Hepatobiliary Disorders: Echographic pictures of vascular sedimentations (precipitation of ceftriaxone calcium salts in the gallbladder) have been reported, and particularly in children. They are associated or not with a clinical symptomatology. Ceftriaxone therapy must be discontinued so that signs decrease; rare cases of hepatic enzymes increase.
Pancreatic Disorders: Exceptional cases of pancreatitis have been reported, they decreased on interrupting the therapy.
Hematological Reactions: Moderated hypereosinophilia, leuko-neutropenia, thrombocytopenia, hemolytic anemia (rare), isolated cases of agranulocytosis, very rare cases of coagulation disorders.
Renal Disorders: Some alterations of the renal function have been reported with antibiotics of the same group, and particularly in case of treatment associated with aminoglycosides and diuretics; rare cases of oliguria and of increase in the serum creatinine.
Some exceptional cases of renal precipitations have been reported, mainly in children >3 years receiving high daily dosages (eg, ≥80 mg/kg/day), or receiving total doses >10 g and having other risk factors (eg, hydric restriction, confinement to bed). This effect may be symptomatic or not, and may lead to a renal insufficiency; it is reversible at the end of the treatment.
Central Nervous System Disorders: Very few cases of headache and dizziness. The administration of high doses of β-lactams particularly in patients with renal impairment may lead to encephalopathies (consciousness disorders, abnormal movements, convulsive crises).
Exceptional severe accidents, some of them fatal, have been reported in premature or newborn infants, who were simultaneously administered both ceftriaxone and calcium salt (sodium gluconate) through IV route (see Cautions for Usage).
Local Manifestations: IM injections without lidocaine are painful. Local phlebitis has sometimes been observed after IV injection.
Drug Interactions
Drug-Laboratory Interactions: Positive results of Coombs' tests have been reported during treatment with the cephalosporins.
Some false-positive results of galactosemia may appear with ceftriaxone.
Non-enzymatic methods for the glucose determination in the urine may give false-positive results. This is the reason why it is necessary to use enzymatic methods for the urine-glucose determination during therapy with ceftriaxone.
Take into account the sodium content (83 mg/g vial) in patients with a strict poor-sodium diet.
Lidocaine may cause a false-positive reaction on anti-doping tests.
Incompatibilities: Do not mix ceftriaxone with solutions containing calcium. As long as a risk of physical or chemical incompatibility with medicines other than calcium cannot be prevented, ceftriaxone must be administered alone. It must be mixed only with solutions and substances mentioned in Dosage & Administration.
Precipitates have been observed with solutions containing calcium, and particularly in newborns.
Do not mix ceftriaxone sodium with solutions containing calcium, and particularly Hartmann's solution or Ringer's solution.
Ceftriaxone sodium is not compatible with amsacrine, vancomycin, fluconazole and aminoglycosides.
Storage
Store at temperatures not exceeding 25°C.
Shelf-Life: 3 years.
MIMS Class
ATC Classification
J01DD04 - ceftriaxone ; Belongs to the class of third-generation cephalosporins. Used in the systemic treatment of infections.
Presentation/Packing
Powd for inj (vial) 1 g x 1's, 10's, 50's.
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