CEFSPAN®

CEFSPAN®
Cefixime
Structural Formula
Non-proprietary name: Cefixime.
Chemical name: (5 R, 7R)-7-[(Z)-2-(2-Amino-4-thiazolyl)-2-(carboxymethoxyimino)
acetamido]-8-oxo-3-vinyl-5-thia-1-azabicyclo (4.2.0) oct-2-ene-2-carboxylic acid.
Molecular formula: CioH15N507S2; Molecular weight: 453.46
Description: Cefixime is a white to light yellowish crystalline powder, with little or a slight
distinctive odor.
Cefixime is freely soluble in methanol and dimethyl sulfoxide, sparingly soluble in
acetone, slightly soluble in ethanol, and practically insoluble in water, ethyl acetate,
ether and hexane.
Composition
Each capsule contains:
Cefixime.................................................................50 mg (potency) or 100 mg (potency).
Each teaspoon (5 ml) of suspension contains:
Cefixime.................................................................................................100 mg (potency).
Each film coated tablet contains:
Cefixime.............................................................................................200 mg (potency).
Pharmacology Antibacterial activity
Cefixime has broad-spectrum activity against gram-positive and negative microorganisms. In particular, in comparison with the other oral cephalosporins, it has potent activity against such gram-positive organisms as Streptococcus sp., Streptococcuspneumoniae, and such gram-negatives as Branhamella catarrhalis, Escherichia coli, Proteus sp., Haemophillus influenzae, Neisseria gonorrhoeae. Its mode of action is bactericidal. It is extremely stable to p-lactamase produced by many organisms, and has good activity against p-lactamase producing organism.
Mode of action
Its mode of action is inhibition of cell wall synthesis. It has high affinity for penicillin binding proteins (PBP) 1 (1 a, 1 b and 1 c) and 3, with the site of activity varying according to organism.
Pharmacokinetics Serum concentration
Following a single oral dose of 50, 100 or 200 mg (potency) of Cefixime in healthy, fasted adults, maximum serum concentrations at 4 hours were, respectively, 0.69, 1.13 and 1.95 pg/ml. The serum half-life was 2.3 - 2.5 hours.
Following a single oral dose of 1.5, 3.0 or 6.0 mg (potency)/kg of Cefixime in pediatric patients with normal renal function, maximum serum concentrations at 3 - 4 hours were,
respectively, 1.14, 2.01 and 3.97 ug/ml. The serum half-life was 3.2 - 3.7 hours.
Tissue penetration (distribution)
Penetration into sputum, tonsiis, maxillary sinus mucosal tissue, otorrhea, biliary fluid and gall-bladder tissue is good.
Metabolism
No antibacterially active metabolites are found in the human serum or urine.
Excretion
Cefixime is excreted primarily renally. The extent of urinary excretion (up to 12 hours) after oral administration of 50, 100 or 200 mg (potency) in healthy, fasted adults was about 20-25%. Maximum urine concentrations were, respectively, 42.9, 62.2 and 82.7 pg/ml at 4-6 hours. The extent of urinary excretion (up to 12 hours) after oral administration of 1.5, 3.0 or 6.0 mg (potency)/kg in pediatric patients with normal renal function was about 13-20%.
Indications
Cefixime is indicated in the treatment of the following infections when caused by
susceptible strains of the designated microorganisms:
Uncomplicated Urinary Tract Infections caused by Escherichia coli and Proteus mirabilis.
Otitis media caused by Haemophillus influenzae (Beta-lactamase positive and negative strains), Moraxella (Branhamella) catarrhalis (most of which are beta-lactamase positive), and Streptococcus pyogenes.
Pharyngitis and Tonsillitis, caused by Streptococcus pyogenes. Acute Bronchitis and Acute Exacerbations of Chronic Bronchitis, caused by Streptococcus pneumoniae and Haemophillus influenzae (beta-lactamase positive and negative strains).
Treatment of typhoid fever in children, with multi-resistant to the standard drug regiments.
Uncomplicated gonorrhoeae (cervical/urethral) which caused by Neisseria gonorrhoeae (penicilinase-and non penicilinase-producing strains).
Contraindications
Patients with a history of shock or hypersensitivity caused by any ingredient of this product.
Precautions
1. General Precautions: Careful inquiry about any form of hypersensitivity should be made, since reactions such as shock may occur.
2. This product should not be administered to the following patients as a general rule. If necessary, however, it can be administered with care.
Patients with a past history of hypersensitivity to any of ingredients in this product or any other cephem antibiotics.
3. Careful Administration:
a. Patients with a history of hypersensitivity to penicilins.
b. Patients with a personal or familial history of some form of allergy such as bronchial asthma, rash, urticaria.
c. Patients with serious renal functions disorder.
d. Patients with poor oral nutrition, patients receiving parenteral nutrition, elderly patients or patients in a debilitated state; Careful observation is essential
in these patients as vitamin K deficiency symptoms may develop.
4. Use during Pregnancy
Safety during pregnancy has not been established. This product should be administered to pregnant patients or women suspected of being pregnant, only if the expected therapeutic benefit is thought to outweigh any possible risk.
5. Use in Nursing Mother
It is not known whether Cefixime is excreted in human milk. Consideration should be given to discontinuing nursing temporarily during treatment with this drug.
6. Use in Newborns or Prematures
Efficacy and safety in children aged less than 6 months have not been established (including in newborn and prematures).
Adverse Reactions
1. Shock
Adequate caution in administration should be used as shock symptoms may rarely S, h3"y'e d !lgnS 0r sVmPtoms s"ch as feeling unwell, oral cavity discomfort, strrctor dizziness abnormal urge to defecate, tinnitus or diaphoresis occur, this product must be discontinued immediately.
2. Hypersensitivity
If signs of hypersensitivity reactions such as rash, urticaria, erythema, pruritus or Le taken ' be discontinued and appropriate measures should
3. Hematologic
Granulocytopenia or eosinophilia infrequently may occur. Rarely thrombocytopenia SnL S ! Pr°dUCti?h0uld be disc°"tinued if any of these abnormalities is found. It has been reported that hemolytic anemia has occurred with other oephems.
4. Hepatic
Infrequently an increase in GOT, GPT or alkaline phosphatase may occur.
5. Renal
Periodic monitoring of renal function is recommended as serious renal impairment
?™?nrfa h£ ,•rena.' lnsufiSency may rareli'occur-lf anV °f »ese abnormalities is found, discontinuation of this product and other appropriate measures should be
6. Digestive
In rare instances a serious colitis, such as pseudomembranous colitis, manifested by blood in stools, may occur. Abdominal pain or frequent diarrhoea requires appropriate measures including prompt withdrawal of this product infrequently vomiting diarrhoea, abdominal pain, stomach discomfort, heartburn or anorexia and rarely nausea, feeling of enlarged abdomen or constipation may occur!
7. Respiratory
In rare instances, interstitial pneumoniae or PIE syndrome, manifested by fever cough, dyspnea, abnormal chest x-ray or eosinophilia, may occur. If any such' symptoms occur this product should be immediately discontinued and appropriate measures such as giving adrenocortical hormones should be taken.
8. Alteration in bacterial flora
Rarely stomatitis or candidiasis may occur.
9 Vitamin deficiencies
Rarely vitamin K deficiencies (such as hypothrombinemia or bleeding tendencies) ma rT 9r°JP deflclsncles (such as Qlossitis, stomatitis, anorexia or neuritis)
10. Others
• Rarely headache or dizziness may occur.
. In studies where infants rats were given 1.000 mg/kg/day orally, a reduced spermatogenesis was reported. '
11. Influences on laboratory values
a. False-positive results may occur with urine sugar tests using Benedict's solution Testa lS S° and C"niteSt' Fa'Se positives nave not been ^Ported with
b. A positive direct Coombs test may occur.
Dosage and Administration
' weLSWnnt°^le,h 5° T°° mg and tablet 200 m9: For adults and children weighing > 30 kg, he usual recommended daily dose is 50-100 mg (potency) of cefixime given orally twice daily. Dosage should be adjusted according to the age body weight and condition of the patient. For more severe or intractable infections rS.™ I99 may' '"creased JP t0 200 mg (potency) given twice daily.
■ Cefspan® suspension 100 mg: The usual pediatric daily dose is 1.5 - 3 mg (potency)Ao given orally twice daily. Dosage should be adjusted according to the condition of the
ton ™ fr?„rtm°rewfV8re °r int'ac,able infections, the dosage may be increased up to 6 mg (potency)/kg given orally twice daily . I" children, otitis media should be treated with suspension. Clinical studies of otitis medtewera-oondi^ad with the suspension and the suspension results in higher peak blood levels than the tablet when administered at the same dose Therefore S„™l0n sh°u!d not be substituted in the treatment of otitis media!
• Typhoid fever in children: 10 -15 mg/kg/day for 2 weeks
' th.'^ Withrimpaired r9nral ,unction re<'uire modification of dosage depending on he degree of impairment. The recommended dosage is 75% of the standard dosage n»«;n( 9 VJ 1" creatlnine clearance is between 21 and 60 ml/min or for patients on renal hemodialysis, and 50% of the standard dosage (i.e. 200 mg daily)
^huif, me dearan?e is lsss than 20 ml/min or for patients on continuous ambulatory peritoneal dialysis.
• In case of over dosage:
Sfrl™ 'aVa?e m^,be indicated; otherwise, no specific antidote exists. Cefixime is diatyS '" S'gnlflCant 1uantlties from the circulation by hemodialysis or peritoneal
• For uncomplicated cervical/urethral gonorrhoeae, a single dose of 400 mg is recommended. M
Presentation
naS!,Smg: Box of 3 strips x 10 capsules Reg. No. DKL9211616501A1
S Inn m° : n™ ° ? S'ripS X 1 ° CapSUleS Re9- N0- DKL 9211616501B1
Filcotab 200 mg : Box of 1 strip x 10 tablets Reg. No. DKL 0311636517A1
Dry Syrup : Bottle of 30 ml Reg. No. DKL9211616738A1
nrlZC°"fitM°?' *e s,u„sPension maV be kePt 'or 7 days either at room temperature SlSaSvC S'9nifiCant '0SS °' P°,enCy- Keep «gh«V ciosedPDiscard Add 20 ml of water, shake for 60 seconds m
Q Capsules : Store below 25°C. Dry Syrup and Tablet: Store below 30°C.
HARUS DENGAN RESEP DOKTER On medical prescription only.