Cefpoprime

Uses

Cefpoprime is used for the treatment of patients infected with susceptible strains of micro-organisms which include a wide range of gram-positive & gram-negative bacteria. As it is highly stable in presence of b-lactamase enzyme, so it is more effective against gram-positive bacteria than other 3rd generation oral Cephalosporins.

The susceptible organisms include gram-positive bacteria eg. S. aureus (including penicillinase producing strains), S. saprophyticus, S. pneumoniae, S. pyogenes, S. agalactiae, P. magnus and gram-negative bacteria eg. E. coli, K. pneumoniae, H. influenzae (including b-lactamase producer & Ampicillin resistant strains), M. catarrhalis, N. gonorrhoeae (including penicillinase producing strains), P. mirabillis, C. diversus, H. parainfluenzae, K. oxytoca, P. vulgaris, P. rettgeri.

Ximeprox is used for the following diseases:-

(1) Lower respiratory tract infection: Acute community-acquired pneumonia, Acute bacterial exacerbation of chronic bronchitis; (2) Upper respiratory tract infection: Acute otitis media, Acute maxillary sinusitis, Pharyngitis, Tonsillitis; (3) Sexually transmitted diseases: Acute uncomplicated urethral & cervical gonorrhea, Acute ano-rectal infection in woman caused by N. gonorrhoeae; (4) Uncomplicated urinary tract infection: Cystitis, Pyuria; (5) Skin & soft tissue infections: Furuncle, Cellulitis, Subcutaneous abscess, infectious atheroma & periproctal abscess (6) Enteric fever.

Cefpoprime is also used to associated treatment for these conditions: Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB), Acute Otitis Media, Acute Sinusitis, Acute Tracheobronchitis, Acute maxillary sinusitis, Bacterial Infections, Bacterial Pneumonia, Community Acquired Pneumonia (CAP), Gonorrhea, Lower Respiratory Tract Infection (LRTI), Otitis Media (OM), Pharyngitis, Skin and Soft Tissue Infections, Streptococcal Pharyngitis, Streptococcal tonsillitis, Superinfection bacterial, Tonsillitis, Uncomplicated Urinary Tract Infections, Upper Respiratory Tract Infection, Uncomplicated Lower Respiratory Tract Infection (LRTI), Uncomplicated Upper Respiratory Tract Infection, Uncomplicated Urethritis gonococcal, Uncomplicated skin and subcutaneous tissue bacterial infections

How Cefpoprime works

Cefpoprime is active against a wide spectrum of Gram-positive and Gram-negative bacteria. Cefpoprime is stable in the presence of beta-lactamase enzymes. As a result, many organisms resistant to penicillins and cephalosporins, due to their production of beta-lactamase, may be susceptible to cefpodoxime. Cefpoprime is inactivated by certain extended spectrum beta-lactamases. The bactericidal activity of cefpodoxime results from its inhibition of cell wall synthesis. The active metabolite of cefpodoxime binds preferentially to penicillin binding protein 3, which inhibits production of peptidoglycan, the primary constituent of bacterial cell walls.

Dosage

Cefpoprime dosage

Ximeprox should be administered orally with food to enhance absorption. Ximeprox suspension may be given without regard to food.

Child :

15 days - 6 months : 4 mg/kg every 12 hours

6 months - 2 years : 40 mg every 12 hours

3 - 8 years : 80 mg every 12 hours

over 9 years : 100 mg every 12 hours

Patients with renal dysfunction: For patients with severe renal impairment (creatinine clearance <30 ml/min) the dosing intervals should be increased to 24 hourly.

Patients with liver cirrhosis: Cefpoprime proxetil pharmacokinetics in cirrhotic patients are similar to those in healthy subjects. Dose adjustment is not necessary in this population.

Direction for Reconstitution of suspension:

For 100 ml suspension : Add 50 ml (10 measuring spoonful) of boiled and cooled water to the dry mixture in the bottle. For ease of preparation add water to the bottle in two portions. Shake well after each addition until all the powder is in suspension.

For 50 ml suspension : Add 25 ml (5 measuring spoonful) of boiled and cooled water to the dry mixture in the bottle. For ease of preparation add water to the bottle in two portions. Shake well after each addition until all the powder is in suspension.

For 50 ml DS suspension : Add 25 ml (5 measuring spoonful) of boiled and cooled water to the dry mixture in the bottle. For ease of preparation add water to the bottle in two portions. Shake well after each addition until all the powder is in suspension.

Note: Shake the suspension well before each use. Keep the bottle tightly closed. The reconstituted suspension should be stored in a cool and dry place, preferably in refrigerator and unused portion should be discarded after 10 days.

Side Effects

Cefpoprime has very few side effects. The side effects include diarrhea, nausea, skin & vaginal fungal infection, abdominal pain, headache, chest pain, myalgia, dyspepsia, dizziness, vertigo, cough etc. In children incidence of fungal skin rash is more than adults.

Precaution

In patients with transient or persistent reduction in urinary output due to renal insufficiency, the total daily dose of cefpodoxime proxetil should be reduced. Cefpoprime, like other cephalosporins, should be administered with caution to patients receiving concurrent treatment with potent diuretics. As with other broad spectrum antibiotics, prolonged use of cefpodoxime proxetil may result in overgrowth of non-susceptible organisms. Repeated evaluation of the patient's condition is essential.

Interaction

Antacids or H2-blockers may decrease the absorption of cefpodoxime. Reduced renal excretion with probenecid.

Food Interaction

• Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.

[Moderate] ADJUST DOSING INTERVAL: Food enhances the oral bioavailability of cefpodoxime proxetil tablets.

Following a 200 mg dose taken with food, the extent of absorption (mean AUC) was 21% to 33% higher and the mean peak plasma concentration (Cmax) 19% higher than under fasting conditions.

Time to peak concentration (Tmax) was not significantly different between fed and fasted states.

On the contrary, when a 200 mg dose of the suspension was taken with food, the mean AUC and Cmax were not significantly different than those under fasting conditions, although the rate of absorption was slower with food (48% increase in Tmax ).br>
MANAGEMENT: To ensure maximal oral absorption, cefpodoxime proxetil tablets should be administered with or immediately after a meal.

Cefpoprime Drug Interaction

Moderate: furosemide, furosemideUnknown: aspirin, aspirin, ciprofloxacin, ciprofloxacin, docusate, docusate, polyethylene glycol 3350, polyethylene glycol 3350, acetaminophen, acetaminophen, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Cefpoprime Disease Interaction

Major: colitisModerate: renal dysfunction, dialysis, liver disease, seizure disorders

Elimination Route

Cefpoprime proxetil is a prodrug that is absorbed from the gastrointestinal tract and de-esterified to its active metabolite, cefpodoxime. Following oral administration of 100 mg of cefpodoxime proxetil to fasting subjects, approximately 50% of the administered cefpodoxime dose was absorbed systemically.

Half Life

2.09 to 2.84 hours

Elimination Route

Over the recommended dosing range (100 to 400 mg), approximately 29 to 33% of the administered cefpodoxime dose was excreted unchanged in the urine in 12 hours.

Pregnancy & Breastfeeding use

There are no adequate and well-controlled studies on Cefpoprime proxetil use in pregnant woman, but it was found neither teratogenic nor embryocidal in animal trial. However, the drug should be used during pregnancy only if clearly needed. In nursing mother, Cefpoprime is excreted in breast milk & there is potential risk of serious reactions in nursing infants, so a decision should be made whether to discontinue breast feeding or to discontinue the drug.

Contraindication

Cefpoprime is contraindicated in patients with known allergy to the cephalosporin class of antibiotics.

Renal Impairment: Patients with renal dysfunction: For patients with severe renal impairment (creatinine clearance <30 ml/min) the dosing intervals should be increased to 24 hourly.

Hepatic Impairment: The dosage does not require modification in cases of hepatic impairment.

Acute Overdose

Symptoms: Nausea, vomiting, epigastric distress and diarrhoea.

Management: Haemodialysis or peritoneal dialysis may be useful in the event of a serious toxic reaction particularly if renal function is compromised.

Interaction with other Medicine

Antacids: Concomitant administration of high doses of antacids (sodium bicarbonate and aluminum hydroxide) or H2 blockers reduces peak plasma level by 24% to 42% and the extent of absorption by 27% to 32% respectively.

Probenecid: Renal excretion of Cefpoprime proxetil was inhibited by Probenecid and resulted in an approximately 31% increase in AUC.

Nephrotoxic drugs: Close monitoring of renal function is advised when Cefpoprime proxetil is administered concomitantly with compounds of known Nephrotoxic potential.

Storage Condition

Capsule: Store below 30° C, protected from light and moisture.

Powder for suspension: Store below 25° C, protected from light and moisture.

After reconstitution: The suspension can be used within 7 days if be kept at room temperature and within 14 days if be kept in refrigerator (2° to 8° C). Always keep the bottle tightly closed.

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