Prescription Drugs

DESCRIPTION Loracarbef is a synthetic b-lactam antibiotic of the carbacephem class for oral administration. Chemically, carbacephems differ from cephalosporin-class antibiotics in the dihydrothiazine ring where a methylene group has been substituted for a sulfur atom. The chemical name for loracarbef is: (6R,7S)-7-[(R)-2-amino-2-phenylacetamido]-3-chloro-8-oxo-1-azabicyclo[4.2.0]oct-2-ene-2- carboxylic acid, monohydrate. It is a white to off-white solid with a molecular weight of 367.8. The empirical formula is C16H16ClN3O4·H2O. Lorabid (loracarbef) Pulvules and Lorabid (loracarbef) for Oral Suspension are intended for oral administration only. Each Pulvule contains loracarbef equivalent to 200 mg (0.57 mmol) or 400 mg (1.14 mmol) anhydrous loracarbef activity. They also contain cornstarch, dimethicone, F Dy & C blue No. 2, gelatin, iron oxides, magnesium stearate, titanium dioxide, and other inactive ingredients. After reconstitution, each 5 ml of Lorabid for Oral Suspension contains loracarbef equivalent to 100 mg (0.286 mmol) or 200 mg (0.57 mmol) anhydrous loracarbef activity. The suspensions also contain cellulose, F Dy & C red No. 40, flavors, methylparaben, propylparaben, simethicone emulsion, sodium carboxymethylcellulose, sucrose, and xanthan gum.

INDICATIONS Loracarbef is indicated in the treatment of patients with mild to moderate infections caused by susceptible strains of the designated microorganisms in the conditions listed below. (As recommended dosages, durations of therapy, and applicable patient populations vary among these infections, please see DOSAGE AND ADMINISTRATION for specific recommendations.) Lower Respiratory Tract: Secondary Bacterial Infection of Acute Bronchitis caused by S. pneumoniae, H. influenzae(including b-lactamase-producing strains), or M. catarrhalis (including b-lactamase-producing strains). Acute Bacterial Exacerbations of Chronic Bronchitis: caused by S. pneumoniae, H. influenzae (including b-lactamase-producing strains), or M. catarrhalis (including b-lactamase-producing strains). Pneumonia: caused by S. pneumoniae or H. influenzae (non-b-lactamase-producing strains only). Data are insufficient at this time to establish efficacy in patients with pneumonia caused by b-lactamase-producing strains of H. influenzae. Upper Respiratory Tract: Otitis Media† caused by S. pneumoniae, H. influenzae (including b-lactamase-producing strains), M. catarrhalis (including b-lactamase-producing strains), or S. pyogenes. Acute Maxillary Sinusitis:† caused by S. pneumoniae, H. influenzae (non-b-lactamase-producing strains only), or M. catarrhalis (including b-lactamase-producing strains). Data are insufficient at this time to establish efficacy in patients with acute maxillary sinusitis caused by b-lactamase-producing strains of H. influenzae. † NOTE: In a patient population with significant numbers of b-lactamase-producing organisms, loracarbef's clinical cure and bacteriological eradication rates were somewhat less than those observed with a product containing a b-lactamase inhibitor. Loracarbef's decreased potential for toxicity compared to products containing b-lactamase inhibitors along with the susceptibility patterns of the common microbes in a given geographic area should be taken into account when considering the use of an antimicrobial (see CLINICAL STUDIES.) Pharyngitis and Tonsillitis: caused by S. pyogenes. (The usual drug of choice in the treatment and prevention of streptococcal infections, including the prophylaxis of rheumatic fever, is penicillin administered by the intramuscular route. Loracarbef is generally effective in the eradication of S. pyogenes from the nasopharynx; however, data establishing the efficacy of loracarbef in the subsequent prevention of rheumatic fever are not available at present.) For information on use in pediatric patients, see PRECAUTIONS, Pediatric Use. Skin and Skin Structure: Uncomplicated Skin and Skin Structure Infections caused by S. aureus (including penicillinase-producing strains) or S. pyogenes. Abscesses should be surgically drained as clinically indicated. Urinary Tract: Uncomplicated Urinary Tract Infections (cystitis) caused by E. coli or S. saprophyticus*. NOTE: In considering the use of loracarbef in the treatment of cystitis, loracarbef's lower bacterial eradication rates and lower potential for toxicity should be weighed against the increased eradication rates and increased potential for toxicity demonstrated by some other classes of approved agents (see CLINICAL STUDIES.) Uncomplicated Pyelonephritis: caused by E. coli. *Although treatment of infections due to this organism in this organ system demonstrated a clinically acceptable overall outcome, efficacy was studied in fewer than 10 infections. Culture and susceptibility testing should be performed when appropriate to determine the causative organism and its susceptibility to loracarbef. Therapy may be started while awaiting the results of these studies. Once these results become available, antimicrobial therapy should be adjusted accordingly. DOSAGE AND ADMINISTRATION Loracarbef is administered orally either at least 1 hour prior to eating or at least 2 hours after eating. The recommended dosages, durations of treatment, and applicable patient populations are described in TABLE 13. TABLE 13 Population/ Infection Dosage (mg) Duration (days) Adults (13 years and older) Lower Respiratory Tract Secondary Bacterial Infection of Acute Bronchitis 200-400 q12h 7 Acute Bacterial Exacerbation of Chronic Bronchitis 400 q12h 7 Pneumonia 400 q12h 14 Upper Respiratory Tract Pharyngitis/Tonsillitis 200 q12h 10* Sinusitis‡ 400 q12h 10 Skin and Skin Structure Uncomplicated Skin and Skin Structure Infections 200 q12h 7 Urinary Tract Uncomplicated cystitis‡ 200 q24h 7 Uncomplicated pyelonephritis 400 q12h 14 Pediatric Patients (6 months to 12 years) Upper Respiratory Tract Acute Otitis Media†‡ 30 mg/kg/day in divided doses q12h 10 Acute maxillary sinusitis‡ 30 mg/kg/day in divided doses q12h 10 Pharyngitis/Tonsillitis 15 mg/kg/day in divided doses q12h 10* Skin and Skin Structure Impetigo 15 mg/kg/day in divided doses q12h 7 * In the treatment of infections due to S. pyogenes, Lorabid should be administered for at least 10 days. † Otitis media should be treated with the suspension. Clinical studies of otitis media were conducted with the suspension formulation only. The suspension is more rapidly absorbed than the capsules, resulting in higher peak plasma concentrations when administered at the same dose. Therefore, the capsule should not be substituted for the suspension in the treatment of otitis media (see CLINICAL PHARMACOLOGY). ‡ (See CLINICAL STUDIES and INDICATIONS AND USAGE for further information.) TABLE 14 Pediatric Dosage Chart Daily Dose 15 mg/kg/day 100 mg/5 ml Suspension 200 mg/5 ml Suspension Weight Dose given twice daily Dose given twice daily lb kg ml tsp ml tsp 15 7 2.6 0.5 --- --- 29 13 4.9 1.0 2.5 0.5 44 20 7.5 1.5 3.8 0.75 57 26 9.8 2.0 4.9 1.0 TABLE 15 Pediatric Dosage Chart Daily Dose 30 mg/kg/day 100 mg/5 ml Suspension 200 mg/5 ml Suspension Weight Dose given twice daily Dose given twice daily lb kg ml tsp ml tsp 15 7 5.2 1.0 2.6 0.5 29 13 9.8 2.0 4.9 1.0 44 20 --- --- 7.5 1.5 57 26 --- --- 9.8 2.0 Renal Impairment: Loracarbef may be administered to patients with impaired renal function. The usual dose and schedule may be employed in patients with creatinine clearance levels of 50 ml/min or greater. Patients with creatinine clearance between 10 and 49 ml/min may be given half of the recommended dose at the usual dosage interval, or the normal recommended dose at twice the usual dosage interval. Patients with creatinine clearance levels less than 10 ml/min may be treated with the recommended dose given every 3 to 5 days; patients on hemodialysis should receive another dose following dialysis. When only the serum creatinine is available, the following formula (based on sex, weight, and age of the patient) may be used to convert this value into creatinine clearance (CLcr, ml/min). The equation assumes the patient's renal function is stable. Males = [(weight in kg) ´ (140 - age)] ¸ [72 ´ serum creatinine (mg/100 ml)] Females = (0.85) ´ (above value) Reconstitution Directions for Oral Suspension 50 ml: Add 30 ml of water in 2 portion to the dry mixture in the bottle. Shake well after each addition. 75 ml: Add 45 ml of water in 2 portions to the dry mixture in the bottle. Shake well after each addition. 100 ml: Add 60 ml of water in 2 portions to the dry mixture in the bottle. Shake well after each addition. After mixing, the suspension may be kept at room temperature, 59° to 86°F (15° to 30°C), for 14 days without significant loss of potency. Keep tightly closed. Discard unused portion after 14 days. HOW SUPPLIED Lorabid (loracarbef) Pulvules: 200 mg, is blue and gray with 3170. Lorabid (loracarbef) Pulvules: 400 mg, is blue and pink with 3171. Keep tightly closed. Store at controlled room temperature, 59° to 86°F (15° to 30°C). Protect from heat. Pulves oral suspension is strawberry bubble gum flavor. PRODUCT LISTING Capsule - Oral - 200 mg 30's $94.35 Lorabid (loracarbef) Pulvules, Lilly 00002-3170-30 Capsule - Oral - 400 mg 30's $121.46 Lorabid (loracarbef) Pulvules, Lilly 00002-3171-30 Powder For Reconstitution - Oral - 100 mg/5 ml 50 ml $15.07 Lorabid (loracarbef) , Lilly 00002-5135-87 100 ml $26.84 Lorabid (loracarbef) , Lilly 00002-5135-48 Powder For Reconstitution - Oral - 200 mg/5 ml 50 ml $25.16 Lorabid (loracarbef) , Lilly 00002-5136-87 75 ml $35.22 Lorabid (loracarbef) , Lilly 00002-5136-18 100 ml $40.28 Lorabid (loracarbef) , Lilly 00002-5136-48 REFERENCES 1. National Committee for Clinical Laboratory Standards, M2-A4 performance standards for antimicrobial disk susceptibility tests. ed 4, Villanova, PA, April, 1990. 2. National Committee for Clinical Laboratory Standards, M7-A2 methods for dilution antimicrobial susceptibility tests for bacteria that grow aerobically, ed 2, Villanova, PA, April, 1990.

PATIENT INFORMATION Loracarbef is an antibiotic used to treat infections such as bronchitis, sinusitis, pneumonia and tonsillitis. This drug should not be used by those with allergies to the cephalosporin antibiotics. You should also consult with your pharmacist or physician if you are allergic to penicillin before taking this medication. This medication shold be taken at least one hour prior to eating or at least 2 hours after eating. The most common side effects are rash, diarrhea and abdominal pain. You should discontinue the medication if you develop a skin rash.