Cefirat Cefixime Anhydrous Caplet and Dispersible Tablet

Cefirat® Cefixime USP

 

COMPOSITION

Cefirat 400: Each film coated tablet contains cefixime USP as Trihydrate equivalent to cefixime Anhydrous 400mg.

Cefirat Dispersible Tablet 200mg/5ml: Each re-constituted tablet contains cefixime USP as Triydrate equivalent to cefixime Anhydrous 200mg.

Cefirat Dispersible Tablet 100mg/5ml: Each re-constituted tablet contains cefixime USP as Triydrate equivalent to cefixime Anhydrous 100mg.

 

Description

Cefirat 400mg is a white to off-white capsule shaped film-coated tablet engrave with NEMEL on one side and plain on the other side.

Cefirat Dispersible Tablet is an off-white round shaped uncoated tablet engrave with NEMEL on one side and plain on the other side.

 

Properties

Cefirat (Cefixim) belongs to the group of medicines called Cephalosporins. As with other Cephalosporins bactericidal action for cefixime result from inhibition of cell-wall synthesis, Cefixime is highly stable in the presence of beta-lactamase enzynies. As a result, many organism susceptible to cefixime has been shown to be active against most of the following organism both in vitro and in clinical infection.

 

Susceptibility of Pathogen Is As Follows

Streptococcus pneumonia, Streptococcus pathogens, Heamophilus influenza (beta-lactamase-positive and negative strains), Moraxella (Brahamella) catarrhalis (most of which are beta-lactamase positive). Eschericha coli, proteus mirabilis, Neisseri gononrrhoae (including penicllinase producing strain).

Cefixime has been shown to be active in vitro against most strain of the following organism; however, clinical efficiency has not been established.

Streptoccoccus agalactiae, Heamophilus paranfluenzae (beta-lactamase positive and negative strains), proteus vulgaris, Klebsiella pneumoniea, Klebsiella oxytoca, pasteurella multocida, providencia species, salmonella species. Shegella species citrobacter amalonaticus diversus, serratia marcescens.

Note: Pseudomonas species, strain of group D Streptococcus (including enteroccoci), listeria monocytogenes, most strain of Staphylococci (including methicilln – resistance strain) and most strain of Enterobacter are resistance to cefixime. In addition, most strain are bacterides fraglills and clostridia are resistance to confixime.

 

Pharmacokinetics

Cefirat (Cefixime) given orally is about 40% – 50% absorbed whether administered with or without food. However time to maximal absorption is increased by approximately 8 hours when administered with food. Peak serum concentration occur between 2 to 6 hours following a single 400mg tablet or 400mg suspension of cefixime.

Peak serum concentration occurs between 2 to 5 hours following oral administration. Half life is about 3 to 4 hours and is not dose dependent. Cefixime is excreted by renal and billiary mechanism. Approximately 50% of the absorbed dose is excreted unchanged in the urine in 24hours, in animal studies. It was noted that Cefixime is also excreted in the bile in excess of 10% of the administered dose. Serum protein binding is concentration independent with a bound fraction of approximately 65%.

In subject with moderate impairment of renal functions (20 to 40ml/min creatinine clearance), the average serum half life of Cefixime is prolonged to 64 hours. In severe renal impairment (5 to 20 ml/min creatinine clearance) the half-life is increased to as indicated with doses of 400mg, patient undergoing hemodialysis or peritoneal dialysis. However, a study clearance of 21- Adequate data on CSF level of cefixime are not available).

 

Indications and Usage

Cefirat (Cefixime) is indicated in the treatment of the following infection when caused by susceptible strain of the designated microorganism. Uncomplicated Urinary Tract infection caused by Eschercia coli and prateus mirabilis. Otitis Media caused by Haemophilus Influenza (beta-lactamase positive and negative strains), Morazella (Brahamella) catarrhalis ( most of which are beta-lactamase positive), and S. Pyogenes.

Acute Bronchitis and acute Exacerbation of chronic Bronchitis caused by streptococcus pneumonia and heamophilus influenza (beta-Iactamase positive and negative strains). Uncomplicated gonorrhea (cervical/urethral), cause by Neisseria gonorrhea (penicillinase and non penicillinase producing strain).

Appropriate culture and susceptibility studies, thereby should be performed to determine the causative organism and susceptibility to cefixime. However, therapy may be started while awaiting result of these studies. Therapy should be adjusted if necessary once these results are known.

Cefirat (Cefixime) may be use as empiric treatment for susceptible microorganism but when culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data local epidemiology and susceptibility pattern may contribute to the empiric selection of therapy.

 

Dosage and Administration

Adult

The recommended dose of Cefixime is 400mg once daily. This may be given as a single dose or as 200mg tablet every 12hours. For the treatment of uncomplicated cervical/urethral gonococcal infection, a single oral dose of 400mg tablet is recommended. Duration of administration should be between 6 to 14days.

Children

The recommended dosage is 8mg/kg/day as a single dose or in divided doses of 4mg/kg 12hourly of the reconstituted suspension. Duration of treatment is usually between 5-14 days. Below is the general guide for treatment in children above 2 years for Cefixime dispersible tablet 200mg/5ml.

Age Dosage Strength Age Dosage Strength
100mg/5ml 200mg/5ml 100mg/5ml 200mg/5ml
2-4 years 5ml daily 2.5ml daily 9-12 years 15ml daily 7.5ml daily
5-8 years 10ml daily 5ml daily Above 12 years >50kg Adult Dose of 400mg (single or divided dose)

Efficacy and safety infant less than 6 months have not been established.

 

Direction for re-constitution

According to prescribed dose, place tablet in a calibrated cap and add already boiled cooled water slowly to the desired calibrated mark and give to the child.

 

Renal impairment

Cefirat may be administered in the presence of impaired renal function. Normal dose and schedule may be employed in patients with creatinine clearance of 60ml/min or greater. Patient whose clearance is between 21 and 60ml/min or patient who are on renal hemodialysis may be given 75% of the standard dosing interval (i.e. 300mg daily).

Patient whose clearance is 20ml/min or patient who are on continuous ambulatory peritoneal diaslysis may be given half the standard dosage at the standard dosing interval (i.e. 200mg daily). Neither hemodialysis nor peritoneal dialysis removes significant amount of drug from the body.

 

Side Effects

Most adverse reaction observed in clinical trial were of mild and transient. The most commonly seen adverse reaction ware gastrointestinal event. Clinically mild gastrointestinal side effect occurred in 20% in all patient. Moderate event, occurred in 9% of all patients and severe adverse reaction occurred in 2% of all patient, individual event rates included diarrhea 16% loose or frequent stool, 6% abdominal pain 3%, nausea 7%, dyspepsia 3% and flatulence 4% these symptoms usually responded to symptomatic therapy or ceased when Cefixime was discontinued. Several patient developed severe diarrhea and/or documented pseudomembranous colitis and a few required hospitalization. Other adverse reaction (incident rate <20%) are Hypersensitivity reaction, Hepatic (transient elevation in SGOT alkaline phosphatase, hepatitis jaundice) renal (transient elevation in BUN or creatinine acute renal failure). Central nervous system (Headaches, dizziness, seizures). Haemic and Lymphatic system (Transient thrombocytopenia, eucopenial and eossinophillia) e.t.c.

 

Drug interaction

Carbamazepine: Elevated carbamazepine level has been reported in post marketing experience with concomitant administration of Cefixime. Drug monitoring may be of assistance in detecting alterations in Carbamazopine plasma concentration.

Warfarin and Anticoagulants: Increased Prothrombin time with or without bleeding has been shown with concomitant administration with Cefixime.

Aminoglycosides: Concomitant administration with Cefirat increases risk of kidney damage.

Probenecid: There is reduced body’s ability to remove cefixime in the blood if observed when given concomitantly with Probenecid.

 

General Precaution

The dose of Cefixime should be adjusted in patient with renal impairment as well as those undergoing continuous ambulatory peritoneal dialysis (CAPD) and (HD). Patient on dialysis should be monitored carefully. Cephalosporins may be associated with a fall in production activity.

 

Pregnancy

There are no data on the excretion of Cefirat into human milk. Consideration should be made given temporary discontinuing of breastfeeding during treatment period.

 

Labour and delivery

Cefirat (cefixime) has not been studied for use during labour and delivery.

Consideration should be given to discontinuing nursing temporarily during treatment with this drug.

 

Breast feeding

It is not known whether Cefirat (Cefixime) is excreted in human milk. Consideration should be given to discontinuing nursing temporarily during treatment with this drug.

 

Pediatric use

Safety and effectiveness of Cefirat (Cefixime) in children aged less than six month old have not been established. The incident of gastrointestinal adverse reaction including diarrhea and loose stools in the pediatric patient receiving the suspension was comparable to the incident seen in adult patients.

 

Overdose

Some of the possible effect of Cefirat overdose are:

Seizures.

Unusual muscle movement/hyperactivity.

Coma.

Brain Problems.

In cases of overdose, gastric lavage may be induced; otherwise, there is no specific, antidote for Cefirat poisoning/overdose.

Cefirat (Cefixime) is not removed in significant quantities from the circulation by hemodialysis or peritoneal dialysis. Adverse reactions in small numbers of healthy adult volunteers receiving single dose up to 2kg of Cefixime did not differ from the profile seen in patient treated at the recommended doses.

 

Contraindications

Cefixime is contraindicated in patient with known allergy to the cephalosporin group of antibiotics.

 

Presentation

Cefirat 400 is available in alu-alu blister pack of 10 caplets, each blister pack insert with leaflet in a pack.

Cefirat 200/100 dispersible tablets is available in alu-alu blister pack of 10 tablets, each blister inserted with leaflet in a pack.

 

Storage

Keep blister in the outer carton.

Store in cool dry place, away from direct heat and light below 30°C.

Do not take Cefirat after expiry date stated on the blister which is the last day of that month.

Keep out of the reach of Children.

 

Manufactured by

Nemel Pharmaceutical Nig. Ltd.

Head office: Plot 35 Emene Industrial Layout, Enugu, Nigeria.

Branch Office: 4A/4B Medical Road, Phase VI, Trans-Ekulu, Enugu, Nigeria.

nemelpharm@gmail.com

Advertisements

Leave a Reply