Date of approval:
Date of revision:
Cefixime Capsules Instructions
Please read the instructions carefully and use under the guidance of a physician
Drug Name
Generic name: Cefixime Capsules
Trade name: Tepnin
English name: Cefixime Capsules
Hanyu Pinyin: Toubaokewo Jiaonang
Ingredients
The main ingredient of this product is cefixime.
Chemical name: (6R,7R)-7-[[(Z)-2-(2-amino-4-thiazolyl)-2-[(carboxymethoxy)imino]acetyl]amino]-3-vinyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid trihydrate.
The chemical structure formula is
Molecular formula: C16H15N5O7S2-3H2O
Molecular weight: 507.50
【Properties】.
The content of this product is white to light yellow powder or granule.
Indications]
This product is indicated for the following bacterial infectious diseases caused by Streptococcus spp. (except Enterococcus), Pneumococcus, Gonococcus, Cataplasma, Escherichia coli, Klebsiella, Serratia, Aspergillus and Haemophilus influenzae, which are sensitive to cefixime.
Acute bronchitis, pneumonia, secondary infection of chronic respiratory infectious diseases, cystitis, pyelonephritis, gonococcal urethritis, cholecystitis, cholangitis, otitis media, paranasal sinusitis, scarlet fever.
Specification】0.1g (according to C16H15N5O7S2)
Dosage
Adults and children over 30 kg in weight: 0.1g (1 capsule) orally, twice daily; in addition, it can be increased or decreased according to age, weight and symptoms.
[Adverse reactions].
Among the total 12,879 cases, a total of 294 cases (2.28%) of adverse reactions including abnormal clinical examination values were found. These adverse reactions included 112 cases (0.87%) of gastrointestinal symptoms such as diarrhea and 29 cases (0.23%) of skin symptoms such as rash. In addition, abnormal clinical examination values included 78 cases (0.61%) of increased ALT (GPT glutamate aminotransferase) AST (aspartate aminotransferase) increased in 58 cases (0.45%), and eosinophilia in 26 cases (0.20%).
(1) Serious adverse reactions.
(1) Shock: Due to the possibility of causing shock (<0.1%), close observation should be made, and if there is discomfort, abnormal sensation in the mouth, asthma, dizziness, dysgeusia, tinnitus, sweating, etc., drug administration should be stopped and appropriate disposition taken.
(2) Allergy-like symptoms: There is a possibility of allergy-like symptoms (including dyspnea, generalized flushing, angioneurotic edema, urticaria, etc.) (<0.1%), which should be closely observed, and if abnormalities occur, drug administration should be stopped and appropriate disposition taken.
(3) Skin lesions: there is a possibility of skin mucosal eye syndrome (Stevens-Johnson syndrome (0.1%)), toxic epidermal necrolysis (i.e. Lyell syndrome, <0.1%), which should be closely observed, and if fever, headache, arthralgia, skin or mucosal erythema, blistering, skin tension, burning sensation, pain, etc. occur, drug administration should be stopped and appropriate disposition taken. appropriate disposition.
(4) Blood disorders: there is a possibility of granulocyte deficiency (<0.1%, early symptoms: fever, sore throat, headache, tiredness, etc.), hemolytic anemia (<0.1%, early symptoms: fever, hemoglobinuria, anemia, etc.), thrombocytopenia (<0.1%, early symptoms: punctate bleeding, purple spots, etc.), etc., and there are also reports of complete blood cell reduction as with other cephalosporin antibiotics. Therefore, close observation should be made, such as regular examination, and when abnormalities occur, drug administration should be stopped and appropriate treatment should be taken.
(5) Renal dysfunction: There is a possibility of serious renal dysfunction (<0.1%), such as acute renal insufficiency, so it should be closely monitored, such as regular checkups, and if abnormalities occur, the drug should be stopped and appropriate treatment should be taken. (6) Colitis: It may cause severe colitis with bloody stools such as pseudomembranous colitis (<0.1%). If there is abdominal pain and recurrent diarrhea, the drug should be stopped immediately and appropriate treatment should be taken.
(7) Interstitial pneumonia (symptoms such as fever, cough, dyspnea, abnormal chest X-ray, eosinophilia, etc.) and PIE syndrome (all <0.1%) may occur.
(8) Liver dysfunction, jaundice: If AST (GOT), ALT (GPT) or ALP increase with liver dysfunction (less than 0.1%) or jaundice (less than 0.1%), close observation should be made, and if abnormalities are identified, drug administration should be discontinued and disposed of appropriately.
(2) Other adverse reactions.
0.1%~＜5%＜0.1% allergy rash, urticaria, erythema pruritus, fever, swelling blood eosinophilia granulocytopenia liver GOT elevation, GPT elevation, ALP elevation jaundice kidney BUN elevation digestive system diarrhea, stomach upset nausea, vomiting, abdominal pain, burning sensation in the chest, loss of appetite, abdominal fullness, constipation dysbiosis stomatitis, oral candidiasis Vitamin deficiency Vitamin K deficiency (hypoprothrombinemia, bleeding tendency, etc.), vitamin B deficiency (tongue inflammation, stomatitis, loss of appetite, neuritis, etc.) Other Headache, dizziness Note: When the above symptoms occur, stop administration and take appropriate treatment.
[Contraindication
It is prohibited for those who are allergic to this product and its components or other cephalosporins.
Caution】 1.
1. In order to prevent the emergence of drug-resistant strains, the sensitivity of this product should be confirmed in principle before use, and the dose should be controlled to the minimum dose required for disease control.
2. For patients with severe renal dysfunction, the dose should be reduced and the dosing interval should be increased according to the renal function, since the drug can be maintained in the blood.
3. The following patients should be administered with caution.
(1) Patients with a history of allergy to penicillins.
(2) Patients with allergic symptoms such as bronchial asthma, skin rash, urticaria, etc. in themselves or their parents or brothers.
(3) Patients with severe renal dysfunction.
(4) Patients with difficulty in oral administration or non-oral intake of nutrition, or patients with generalized hyperhydrosis. (Due to the presence of symptoms of vitamin K deficiency, it should be observed).
(5) Elderly patients (refer to [Geriatric Use])
4. Important precautions: Due to the possibility of shock, take a full medical history before administration.
5. Do not mix milk, juice, etc. with the drug and place it.
6. Effect on clinical test results.
In addition to test paper reactions, there is a possibility of false positives appearing in urine glucose tests performed with the Benedict’s (Benedict) reagent, Ferrous (Fehling) reagent, and urine glucose test pills (Clinitest), which should be noted.
The possibility of a positive direct Coombs test should be noted.
7. Other precautions.
In tests in juvenile rats, an inhibitory effect on sperm formation has been reported with oral administration of 1,000 mg/kg or more.
Pregnant women and nursing mothers
The safety and efficacy of this product in pregnant women have not been established and should be used only when the therapeutic benefit outweighs the risk; it is not known whether this product is secreted from breast milk and breastfeeding should be suspended if necessary.
Pediatric Use]
The safety of the drug in premature infants and neonates has not been established (no experience with its use).
Geriatric use]
According to the patient’s condition, pay attention to the dosage and interval time, and administer the drug carefully.
(1) The elderly have low physiological function and are prone to adverse reactions.
(2) Vitamin K deficiency in the elderly can easily lead to bleeding.
Drug Interactions]
When this product is combined with warfarin and anticoagulant drugs, it may enhance the effect of warfarin and anticoagulant drugs and increase the prothrombin time.
Drug name Clinical symptoms/measures Mechanism, risk factors Warfarin potassium has the potential to potentiate the effects of warfarin potassium.
However, there are no case reports on this preparation due to the possible disorder of intestinal bacteriocin, which can cause inhibition of vitamin K synthesis [drug overdose
Gastric lavage, no special antidote, hemodialysis and peritoneal dialysis cannot effectively remove this product.
Pharmacology and Toxicology
Pharmacological action
Mechanism of action: Cefixime exerts its bactericidal effect by preventing the synthesis of bacterial cell wall, and it has stability to certain β-lactamases. Therefore, some bacteria that are resistant to penicillin and cephalosporin due to the presence of β-lactamases may be sensitive to cefixime.
Resistance: Resistance to cefixime in Haemophilus influenzae and Neisseria gonorrhoeae isolates is usually associated with alterations in penicillin-binding proteins (PBPs). Cefixime may limit the activity of Enterobacter spp. in producing ultra broad-spectrum β-lactamases (ESBLs). Pseudomonas spp, Enterococcus spp, Group D Streptococcus, Listeria monocytogenes and most staphylococci (including methicillin-resistant strains), Enterobacter spp, Bacteroides fragilis, and Clostridium spp are resistant to cefixime.
Antibacterial spectrum: Cefixime is active against the following microbial isolates both in vitro and in clinical infections (see [Indications] section)
Gram-positive bacteria.
Streptococcus pneumoniae
Streptococcus pyogenes
Gram-negative bacteria.
Escherichia coli
Haemophilus influenzae
Moraxella mucosae
Neisseria gonorrhoeae
Aspergillus chimaericus
The following information was obtained in vitro, but its clinical significance is unclear. At least 90% of the following bacteria showed in vitro minimum inhibitory concentrations (MICs) below or equal to the cefixime susceptibility fold. However, the efficacy of cefixime in the treatment of clinical infections due to these bacteria has not been established in adequate, well-controlled clinical trials.
Gram-positive bacteria.
Streptococcus lactis-free
Gram-negative bacteria.
Citrobacter malonate free
Differential Citrobacter
Haemophilus parainfluenzae
Acid-producing Klebsiella
Klebsiella pneumoniae
Pasteurella multocida
Bacillus variegatus
Propionibacterium spp.
Salmonella spp.
Serratia marcescens
Shigella spp.
Toxicological studies
Genotoxicity
Cefixime did not show point mutations, DNA damage or chromosome damage in bacterial or mammalian cells in vitro, and no potential teratogenicity was seen in mouse micronucleus tests in vivo.
Reproductive toxicity
No effects on fertility or reproductive capacity were seen in rats (at doses up to 25 times the human dose). No fetal damage was observed in reproductive toxicity studies in mice and rats (at doses up to 40 times the human dose).
Carcinogenicity
Lifetime studies in animals have not been conducted to evaluate the potential carcinogenicity of cefixime.
Pharmacokinetic data]
In healthy adults, oral doses of 50, 100 and 200 mg of cefixime in a single dose on an empty stomach resulted in peak serum concentrations of 0.69, 1.13 and 1.95 µg/ml in about 4 hours, respectively, with a half-life of 2.3~2.5 h. In pediatric patients with normal renal function, oral doses of 1.5, 3.0 and 6.0 mg/kg of cefixime resulted in peak serum concentrations of 1.14 mg/kg in about 3~4 hours. The half-life of serum concentration was 3.2~3.7 hours.
In moderate renal impairment [30≤Creatinine clearance (Ccr) <60 ml/min, n=3] and severe renal impairment [10≤Ccr <30 ml/min, n=4], the peak value of cefixime 100 mg in a single oral dose was 2.04 µg/ml after 6 hours in moderate renal impairment and 2.27 µg/ml after 8 hours in severe renal impairment, respectively. The peak value was 2.27µg/ml after 8 hours for those with severe renal impairment and 0.71µg/ml and 1.83µg/ml after 12 hours, with half-lives of 4.15 hours and 11.05 hours, respectively, and delayed elimination for those with severe renal impairment.
Cefixime was well distributed in patients’ sputum, tonsils, mucosal tissue of epiglottis, middle ear secretion, bile and gallbladder tissue.
No antibacterial active metabolites were detected in human serum and urine.
Renal excretion was predominant. When cefixime 50mg, 100mg and 200mg were administered orally to healthy adults on an empty stomach, the urinary excretion rate (0-12 hours) was about 20-25%, and the highest urinary concentrations (4-6 hours) were 42.9, 62.2 and 82.7µg/ml, respectively.
In children with normal renal function, the urinary excretion rate (0~12 hours) is about 13~20% when cefixime 1.5mg, 3.0mg and 6.0mg/kg are administered orally.
Storage】Sealed and stored at room temperature.
Package】Polyvinyl chloride solid pharmaceutical hard tablets with pharmaceutical aluminum foil blister package, 6 capsules/plate, 3 plates/box.
Expiration date】12 months
【Execution standard
Approval Number】State Drug Administration H20041661
【Manufacturing Company】.
Company Name: Chengdu Bite Pharmaceutical Co.
Production Address: No. 1166, Airport Road 4, Southwest Airport Economic Development Zone, Shuangliu, Chengdu, China
Postal Code: 610207
Telephone number: 400-800-6276
Fax number: 028-85919027
Website: http://www.btyy.com