Properties
What is it?
Zinnat Cefuroxime Qualitative and Quantitative Composition: Zinnat tablets contain 125, 250 or 500 mg of cefuroxime (as cefuroxime axetil) Pharmaceutical Form Film-coated tablets Clinical Features Indications Cefuroxime axetil is an oral prodrug of the bactericidal cephalosporin antibiotic cefuroxime, which is resistant to beta-lactamases and has broad-spectrum gram-positive and gram-negative activity. It is indicated for the treatment of infection caused by susceptible bacteria. Indications include: • Upper respiratory tract infections (e.g., ear, nose, and throat infections such as otitis media, sinusitis, tonsillitis, and pharyngitis). • Lower respiratory tract infections. (e.g., pneumonia, acute bronchitis, and exacerbations of chronic bronchitis). • Urinary tract infections (e.g., pyelonephritis, cystitis, and urethritis), gonorrhea, acute uncomplicated gonococcal urethritis, and cervicitis. • Skin and soft tissue infections, e.g., furunculosis, pyoderma, and impetigo). • Gonorrhea, acute uncomplicated gonococcal urethritis, and cervicitis. • Treatment of early Lyme disease and prevention of later Lyme disease in adults and children over 12 years of age. Cefuroxime is also available as a sodium salt (Zinacef) for parenteral use. This allows for subsequent treatment with the same drug when clinically indicated to switch from parenteral therapy to oral. When necessary, Zinnat is effective for initial parenteral Zinacef (cefuroxime sodium) in the treatment of pneumonia and exacerbations of chronic bronchitis. See blog: Zinnat – an effective antibiotic in combating various types of infections Dosage and Administration The usual course of treatment lasts for 7 days (within 5-10 days). Cefuroxime axetil should be taken after meals for optimal absorption. Dosage in Adults Most infections 250 mg twice daily Urinary tract infections 125 mg twice daily Mild to moderate lower respiratory tract infections 250 mg twice daily More severe respiratory tract infections, or suspected pneumonia 500 mg twice daily Pyelonephritis 250 mg twice daily Uncomplicated gonorrhea 1 g single dose Lyme disease in adults and children over 12 years of age 500 mg twice daily for 20 days Subsequent therapy; Pneumonia: 1.5 g Zinacef (IV or IM) for 48-72 hours, then 500 mg twice daily oral therapy with Zinnat (cefuroxime axetil) for 7-10 days. Acute exacerbation of chronic bronchitis: 750 mg Zinacef (IV or IM) for 48-72 hours, then 500 mg twice daily oral therapy with Zinnat (cefuroxime axetil) for 5-10 days. The duration of both parenteral and enteral therapy is determined by the severity of the infection and the patient's clinical status. Dosage in Children Most infections 125 mg (1 x 125 mg tablet) twice daily, up to a maximum of 250 mg daily Children aged 2 years or older with otitis media or, when indicated, more severe infections 250 mg (1 x 250 mg tablet or 2 x 125 mg tablets) twice daily, up to a maximum of 500 mg daily Zinnat tablets cannot be divided, therefore they are not suitable for treating patients who cannot swallow them, such as young children. Zinnat oral suspension may be used in children. There is no data on the use of Zinnat in children under 3 months of age. Contraindications The drug should not be used in patients with known hypersensitivity to cephalosporin antibiotics Special Precautions Particular caution is indicated in patients who have had allergic reactions to penicillin or beta-lactams. As with all antibiotics, prolonged use of cefuroxime axetil may cause overgrowth of Candida. Prolonged use may lead to overgrowth of non-susceptible organisms (e.g., enterococci and Clostridium difficile), which may necessitate discontinuation of treatment. The use of broad-spectrum antibiotics may cause pseudomembranous colitis, so this must be considered in patients who develop severe diarrhea during or after antibiotic use. Jarisch-Herxheimer type reaction has been observed following treatment of Lyme disease with Zinnat. It is due to the bactericidal activity of Zinnat against the causative organism of Lyme disease – Spirochaeta Borrelia burgdorferi. Patients should be reassured that this is a usual and self-limiting feature of antibiotic treatment of Lyme disease. The timing of the switch to oral therapy during the post-treatment regimen is determined by the severity of the infection, the patient's clinical status, and the susceptibility of the involved pathogens. If no clinical improvement is observed within 72 hours, the parenteral course of treatment should be continued. Therefore, the patient should be informed about the relevant information on cefuroxime sodium before starting subsequent therapy. Interactions with Other Medicinal Products Drugs that reduce gastric acidity may cause relatively lower bioavailability of Zinnat compared to fasting intake and may abolish the enhanced postprandial effect. Like other antibiotics, Zinnat affects the intestinal flora. This leads to reduced estrogen reabsorption and reduced efficacy of combined oral contraceptives. Insofar as a false-negative result may occur in the ferricyanide test, it is recommended to use either glucose oxidase or hexokinase methods for determining blood/plasma glucose levels in patients receiving cefuroxime axetil. This antibiotic does not affect creatinine in the alkaline picrate assay. Pregnancy and Lactation Although there is no experimental confirmation of any embryopathic and teratogenic effects associated with cefuroxime axetil, like other drugs, it may be prescribed with particular necessity and great caution in the first months of pregnancy. Cefuroxime is excreted in breast milk during lactation; its administration should be done with great caution. Effect on Ability to Drive and Use Machines Since this medication may cause dizziness, patients should be warned to exercise caution when driving or operating machinery. Adverse Reactions Adverse effects caused by cefuroxime axetil are usually mild and transient in nature. Frequently occurring effects listed below, as well as for most reactions, (e.g., for placebo-controlled studies) calculated levels are not available. In addition, the number of adverse reactions associated with cefuroxime axetil may vary according to indications. Data from numerous clinical trials were used to determine very common and rare adverse effects. These effects were mainly determined from post-marketing studies. Data from placebo-controlled studies are not available. Side effects that occur more often than isolated cases are listed with the following gradations: Very common ≥1/10; Common ≥1/100, <1/10; Uncommon ≥1/1000, <1/100); Rare ≥1/10,000, <1/1000); Very rare <1/10,000); Infections and Infestations Common: Overgrowth of Candida Blood and Lymphatic System Disorders Common: Eosinophilia Uncommon: Coombs' positive test, thrombocytopenia, leukopenia (sometimes absolute) Very rare: Hemolytic anemia The cephalosporin group has the property of adsorbing onto the surface of red blood cell membranes and reacting with antibodies directed against the drug to produce a positive Coombs' test (which may affect blood cross-compatibility) and very rarely hemolytic anemia. Immune System Disorders: Hypersensitivity reactions including Uncommon: Skin rash Rare: Urticaria, itching Very rare; Drug fever, serum sickness, anaphylactic reactions Nervous System Disorders Common: Headache, dizziness Gastrointestinal Disorders Common: Gastrointestinal disturbances, including diarrhea, nausea, abdominal pain Uncommon: Vomiting Rare: Pseudomembranous colitis Hepatobiliary Disorders Often: Transient increase in liver enzyme levels (ALT(SGPT), AST (SGOT) LDH) Very rare: Jaundice (predominantly cholestatic), hepatitis Skin and Subcutaneous Tissue Disorders Very rare: Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (exanthematous necrolysis) See also Immune System Disorders. Overdose Overdosage of cephalosporins may cause cerebral irritation accompanied by convulsions. Certain levels of cefuroxime can be reduced by hemodialysis and peritoneal dialysis. Pharmacological Properties Pharmacodynamics Bacteriology: The in vitro bactericidal activity of cefuroxime axetil is due to its parent compound cefuroxime. Cefuroxime is a well-described and effective antibacterial substance with bactericidal activity against a broad range of commonly occurring bacteria, including beta-lactamase producing strains. Cefuroxime has high resistance to beta-lactamase, and therefore is active against many ampicillin-resistant or amoxicillin-resistant strains. The bactericidal activity of cefuroxime stems from the inhibition of cell wall synthesis by binding to essential target proteins. Cefuroxime is usually active in vitro against the following organisms: Aerobic Gram-negative: Haemophilus influenzae (including ampicillin-resistant strains) Haemophilus parainfluenzae Moraxella (Branhamella) catarrhalis Neisseria gonorrhoeae (including penicillinase and non-penicillinase producing strains) Escherichia coli Klebsiela spp. Proteus mirabilis Providencia spp. proteus rettgeri Aerobic Gram-positive: Staphylococcus aureus and Staphylococcus epidermidis (including penicillinase producing strains, but not methicillin-resistant strains) Streptococcus pyogenes (and other beta-hemolytic streptococci) Streptococcus pneumoniae Streptococcus Group B (Streptococcus agalactiae) Anaerobes: Gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus species) Gram-positive bacilli (including Clostridium species) and gram-negative bacilli (Bacteroides and Fusobacterium species) Propionbacterium spp. Other organisms: Borrelia burgdorferi The following organisms are not susceptible to cefuroxime: Clostridium difficile Pseudomonas spp. Campylobacter spp. Acinetobacter calcoaceticus Listeria monocytogenes Staphylococcus aureus and Staphylococcus epidermidis methicillin-resistant strains Legionella spp. Enterococcus (Streptococcus) faecalis Morganella morganii Proteus vulgaris Enterobacter spp. Citrobacter spp. Serratia spp. Bacteroides fragilis Pharmacokinetic Properties Following oral administration, cefuroxime axetil is slowly absorbed from the gastrointestinal tract and rapidly hydrolyzed in the intestinal mucosa and blood to deliver cefuroxime into circulation. Optimal absorption is achieved when taken as soon as possible after a meal. Peak serum levels (2-3 mg/L for 125 mg, 4-6 mg for 250 mg, 5-8 mg/L for 500 mg dose, and 9-14 mg/L for 1 g dose) are observed approximately 2-3 hours after administration following a meal, unlike intravenous dosing which reaches peak concentration immediately. Absorption of cefuroxime from suspension is considerably longer than from tablets, resulting in later lower serum levels and slightly reduced systemic bioavailability (4-17% less) after reaching peak levels. The serum half-life is 1-1.5 hours. Protein binding varies from 33-50% depending on the methodology used. Cefuroxime is not metabolized and is excreted by glomerular filtration or tubular secretion. Concurrent administration of probenecid increases the area under the serum concentration-time curve by 50%. Serum levels of cefuroxime are reduced by dialysis. Pre-clinical Safety Data There are no significant data Pharmaceutical Properties List of Excipients: Microcrystalline cellulose Croscarmellose sodium Hypromellose Sodium lauryl sulfate Hydrogenated vegetable oil Silicon dioxide Propylene glycol Methylhydroxybenzoate (E 218) Propylhydroxybenzoate (E 216) Titanium dioxide (E 171) Sodium benzoate (E 211) Incompatibility Not specified Shelf Life Shelf life is indicated on the packaging Special Storage Conditions Zinnat tablets should not be stored above 30°C. Container Nature and Composition According to local registration Instructions for use/handling are not provided All descriptions are not available in all countries
