ROCEFIN ® Ceftriaxone

ROCEFIN ® is a drug based on Ceftriaxone disodium

THERAPEUTIC GROUP: General antimicrobials for systemic use - Cephalosporins

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications ROCEFIN ® Ceftriaxone

ROCEFIN ® is selectively indicated in the treatment of infections due to Gram negative bacteria, generally resistant to antibiotic therapy, in patients who are defected or after surgery.

Mechanism of action ROCEFIN ® Ceftriaxone

Ceftriaxone, active ingredient of ROCEFIN ®, is a beta-lactam antibiotic belonging to the category of third-generation cephalosporins that can be taken parenterally, characterized by a wide spectrum of action including both Gram positive and negative bacteria, even when resistant to antibiotic therapy penicillin base.

The bactericidal activity, like other beta-lactams, is realized through the inhibition of transpeptidase, an enzyme involved in the formation of cross-linkages between peptidoglycan molecules and in the structuring of the bacterial wall, thus determining the lysis of the microorganism by osmotic shock .

However, the presence of the methoximinic group gives Ceftriaxone a natural resistance to the action of bacterial beta-lactamases, preserving its antibiotic activity even for penicillin-resistant species.

Staphylococci, Streptococci, E.Coli, Haemophilus influenzae, Klebsielle, Proteus, Neisserie and Enterobacteriacee are some of the organisms to which ceftriaxone has been shown to be effective both in vitro and in vivo.

The inability to absorb ceftriaxone via the gastrointestinal tract makes it necessary to take ROCEFIN ® intramuscularly or intravenously, but still allowing for the maintenance of a very high bioavailability and a therapeutic action prolonged over time for about 8 hours.

Studies carried out and clinical efficacy

1. THE EFFECTIVENESS OF CEFTRIAXONE IN THE TREATMENT OF THE GONORREA

Int J STD AIDS. 2012 Feb; 23 (2): 126-32.

Interesting meta-analysis study, which after evaluating different studies for over 2500 enrolled patients, demonstrated the high efficacy of ceftriaxone taken at doses of 250 mg daily in the treatment of gonorrhea, even in patients with defects.

2 . EFFECTIVENESS OF CEFTRIAXONE IN THE TREATMENT OF Syphilis IN HIV-POSITIVE PATIENTS

Med Mal Infect. 2012 Jan; 42 (1): 15-9.

Study conducted on 116 patients with syphilis, of which 80% HIV-positive, demonstrating that treatment with ceftriaxone -doxicilicna may be effective in the treatment of primary syphilis and in some cases also secondary syphilis characterized by neurological symptoms and ophthalmic.

3. THE CEFTRIAXONE IN PEDIATRIC AGE

J Pharm Pharmacol. 2011 Jan; 63 (1): 65-72.

Pharmacokinetic study aimed at defining the optimal dosage of ceftriaxone in pediatric patients. Unfortunately, the potential side effects greatly limit the use of this antibiotic, although particularly effective, in the neonatal population.

Method of use and dosage

ROCEFIN ®

Powder and solvent for solution for injection of 250 mg of ceftriaxone for 2 ml of solution;

Powder and solvent for solution for injection of 500 mg ceftriaxone for 2 ml of solution;

Powder and solvent for solution for injection of 1 g of ceftriaxone for 3.5 ml of solution.

Although the standard dosage for adults involves taking 1 g of ceftriaxone a day in a single administration, it is up to the doctor to define the appropriate therapeutic scheme based on the patient's physiopathological characteristics, the severity of the clinical picture and the goals therapeutic to achieve.

An adjustment of the doses used would be necessary for patients in pediatric and geriatric age, or contextually affected by renal pathologies.

Before taking ROCEFIN ® it would be advisable to carefully check the chemical-physical properties of the preparation, avoiding taking it in the presence of precipitates or after 6 hours from its reconstitution.

Warnings ROCEFIN ® Ceftriaxone

Given the potential side effects and the selectivity of the therapeutic indications envisaged for the use of ROCEFIN ®, it would be appropriate for the doctor to carefully assess the patient's state of health, making sure:

The absence of previous hypersensitivity reactions to antibiotics and lidocaine;
The absence of conditions incompatible with cephalosporin therapy;
Of prescriptive correctness;
Renal and hepatic function.

Periodic monitoring of the patient's state of health would also be necessary in order to avoid the possible appearance of adverse reactions.

In this regard, the patient should immediately inform his or her doctor following the onset of any undesirable effect, and consider the possibility of suspending the therapy in progress.

Antibiotic therapies prolonged over time, besides favoring the onset of resistant microbial strains, could seriously alter the intestinal microflora, facilitating the appearance of adverse reactions and compromising the absorption of other active ingredients.

It would therefore be important to consider reducing the contraceptive efficacy of oral contraceptives, taken during antibiotic therapy.

PREGNANCY AND BREASTFEEDING

ROCEFIN ® should be prescribed, during pregnancy and in the subsequent breastfeeding period, with particular caution and only in cases where it is necessary therapeutically.

These limitations are justified by the absence of studies able to characterize the safety profile of this antibiotic for fetal health.

Interactions

In order to avoid unpleasant side effects, sometimes even clinically relevant, it would be advisable to avoid reconstitution of the powder with calcium-containing solvents, given the high tendency to form precipitates.

Studies have shown the synergistic action between aminoglycosides and ceftriaxone in countering bacterial growth, although it cannot be administered simultaneously due to physical incompatibility.

Contraindications ROCEFIN ® Ceftriaxone

The use of ROCEFIN ® is contraindicated in patients who are hypersensitive to penicillins and cephalosporins or their excipients, premature infants, full-term infants up to the 28th day of age, patients suffering from jaundice or diseases characterized by hyperbilirubinemia.

The presence of lidocaine in the solvent intended for intramuscular use extends the aforementioned contraindications even to patients hypersensitive to lidocaine.

Undesirable effects - Side effects

Different clinical trials and careful post-marketing monitoring assessed all possible side effects associated with therapy with injectable cephalosporins.

In addition to local reactions characterized by edema, pain, redness and itching, the patient receiving ROCEFIN ® may develop adverse reactions in character:

Gastrointestinal with nausea, vomiting, diarrhea and widespread abdominal pain;
Dermal with rash, hives and dermatitis;
Neurological with headache and vertigo;
Systemic with leukopenia, thrombocytosis, anemia, hypertransaminasemia and hyperbilirubinemia.

Particularly serious from the clinical point of view would also result the possible adverse reactions of an allergic nature such as to determine in the worst cases bronchospasm, laryngospasm, hypotension and anaphylactic shock.

Prolonged use over time could, albeit very rarely, facilitate the growth of resistant microorganisms such as Clostridium Difficile, the etiological agent of pseudo-membranous colitis.