Cefixime Granules Instruction
Please read the instruction manual carefully and use under the guidance of a physician
[Drug Name].
Generic Name: Cefixime Granules
Trade Name: Sefixu
English name: Cefixime Granules
Hanyu Pinyin: Toubaokewo Keli
[Ingredients
The main ingredient of this product is cefixime.
The chemical name is: (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] This product is a mixed suspension granule.
[Indications].
This product is indicated for the following bacterial infectious diseases caused by Streptococcus spp. (except Enterococcus spp.), Pneumococcus spp., Gonococcus spp., Cataplasma spp., Escherichia coli, Klebsiella spp., Serratia spp., Aspergillus spp. 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]50mg (based on C16H15N5O7S2)
[Dosage].
Adults and children over 30 kg in weight: 0.05g or 0.1g (1 or 2 sachets) orally twice daily; in addition, it can be increased or decreased according to age, weight and symptoms, and in severe cases, 0.2g (4 sachets) can be given orally twice daily. For children, 1.5 to 3 mg/kg (body weight) twice daily can be administered orally. Increase or decrease according to symptoms. For patients with severe disease, 6mg/kg can be given orally twice a day each time. Or as directed by a physician.
[Adverse Reactions
A total of 294 (2.28%) adverse reactions, including abnormal clinical test values, were identified in 12,879 total cases. These adverse reactions included 112 (0.87%) gastrointestinal symptoms such as diarrhea and 29 (0.23%) skin symptoms such as rash. ) increased in 78 cases (0.61%), AST (GOT aspartate aminotransferase) increased in 58 cases (0.45%), and eosinophilia increased in 26 cases (0.20%).
(1) Serious adverse reactions.
1) Shock: Because of the possibility of causing shock (<0.1%), close observation should be made, and if there is discomfort, abnormal feeling in the mouth, asthma, dizziness, stool, tinnitus, and sweating, drug administration should be stopped and appropriate disposition taken.
2) Allergy-like symptoms: The possibility of allergy-like symptoms (including dyspnea, generalized flushing, angioneurotic edema, urticaria, etc.) (<0.1%) should be closely observed, and if abnormalities occur, drug administration should be discontinued and appropriate disposition should be taken.
3) Skin lesions: The possibility of cutaneous mucocutaneous ophthalmic syndrome (Stevens-Johnson syndrome, 0.1%), toxic epidermal necrolysis (i.e., Lyell syndrome, <0.1%) should be monitored closely and if fever, headache, arthralgia, skin or mucosal erythema, blistering, skin tension, burning sensation, pain, etc. occur, the drug should be Discontinue drug administration and take 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 whole blood cytopenia as with other cephalosporin antibiotics. The drug should be closely monitored, for example, by regular checkups, and administration should be stopped and appropriate treatment taken if abnormalities occur.
5) Renal dysfunction: There is a potential for severe renal dysfunction ( 6) Colitis: it may cause severe colitis with bloody stools such as pseudomembranous colitis (<0.1%). If abdominal pain and recurrent diarrhea are present, stop administration immediately and take appropriate treatment.
7) Interstitial pneumonia (with symptoms such as fever, cough, dyspnea, abnormal chest X-ray, eosinophilia) and PIE syndrome (both <0.1%) may occur.
8) Liver dysfunction, jaundice: The presence of increased AST (GOT), ALT (GPT), ALP with liver dysfunction (less than 0.1%) and jaundice (less than 0.1%) should be closely monitored and when abnormalities are identified, dosing should be discontinued and disposed of appropriately.
(2) Other adverse reactions.
0.1% to AllergiesRash, hives, erythemaitching, fever, swellingBloodEosinophiliagranulocytopeniaLiverGOT elevation, GPT elevation, ALP elevationJaundiceKidney BUN elevatedBUN Elevated =”font-family:equine; font-size:10pt”>Digestive systemDiarrhea, upset stomachNausea, vomiting, abdominal pain, burning sensation in the chest, loss of appetite, abdominal fullness, constipationDysbiosis Stomatitis, oral candidiasisVitamin Deficiency Vitamin K deficiency (hypoprothrombinemia, bleeding tendency, etc.), vitamin B deficiency (tongue inflammation, stomatitis, loss of appetite, neuritis, etc.)Other Headache, dizzinessNote: Discontinue dosing and take appropriate disposition when above symptoms occur.
Post-marketing adverse reactions: serious adverse reactions seen in clinical use in China from April 2008 to April 2018 were psychiatric disorders, hematuria, and new general adverse reactions were white spots, dry mouth, belching, abnormal bowel sounds, tooth discoloration, chills, pallor, weakness, irritability, convulsions, local numbness, chest tightness, drowsiness, urinary urgency, urinary frequency, cardiac enzyme abnormalities, and palpitations.
[Contraindications
It is contraindicated in patients with hypersensitivity to this product, its components, or other cephalosporins.
[Precautions
1. To prevent the emergence of drug-resistant strains, confirm susceptibility in principle before using this product and control the dose to the minimum required for disease control.
2. In patients with severe renal dysfunction, the dose should be reduced appropriately based on renal function and the dosing interval should be increased appropriately because the drug can maintain concentrations in the blood.
3. Administer with caution in the following patients.
(1) Patients with a history of allergy to penicillins.
(2) Patients with allergic symptoms such as bronchial asthma, rash, or urticaria, either in themselves or in their parents or brothers.
(3) Patients with severe renal dysfunction.
(4) Patients with difficulty in trans-oral administration or non-oral nutritional intake, patients with systemic eosinophilic state. (Observe for signs of vitamin K deficiency when present).
(5) Elderly patients ([refer to Geriatric Dosing])
4. Important precautions:Due to the potential for shock, take an adequate history before administration. .
5. Do not mix milk, juice, etc. with the medication and leave it in.
6. Effects on clinical test results.
In addition to test paper reactions, there is a possibility of false positives for urine glucose testing with the Benedict’s ( Benedict’s) reagent, Fehling’s (Fehling’s) reagent, and urine glucose test pills (Clinitest), which should be noted.
The possibility of a positive direct Coomassie test should be noted.
7. Other considerations.
In tests in juvenile rats, inhibition of spermatogenesis has been reported with oral administration of 1,000 mg/kg or more.
[For pregnant and lactating women].
The safety and efficacy of this product in women during pregnancy have not been established and it should be used only when the benefit of treatment is judged to outweigh 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 preterm, neonatal infants has not been established (no experience with use).
[Geriatric Use
Dosage and intervals should be administered with caution depending on the patient’s status.
(1) The elderly have low physiological function and are prone to adverse reactions.
(2) In the elderly, vitamin K deficiency can easily lead to bleeding.
[Drug Interactions].
When this product is combined with warfarin and anticoagulant drugs, it may potentiate the effects of warfarin and anticoagulant drugs and increase the prothrombin time.
Drug NameClinical symptoms/measures approachmechanism, risk factorBenzylacetone Coumarin (Warfarin)There is a possibility that the effect of benzylacetone coumarin could be enhanced.
But no cases have been reported for this agent As this product may cause intestinal bacteriocin disorder, it may cause inhibition of vitamin K synthesis[Drug Overdose
Gastric lavage, no specific antidote, hemodialysis and peritoneal dialysis do not effectively remove this product.
[Pharmacology and Toxicology]
Pharmacological effects
This product is an oral third-generation cephalosporin with a broad antibacterial spectrum. It has antibacterial activity against some Gram-positive and negative bacteria, especially against Streptococcus spp. of Gram-positive bacteria (except Enterococcus spp.), Pneumococcus spp. Its mechanism of action is to prevent the synthesis of bacterial cell wall, its point of action varies according to the type of bacteria, and has high affinity with PBP1 (1a, 1b, 1c) and PBP3 in penicillin binding protein (PBP). It is highly stable to β-lactamases produced by various bacteria.
Toxicological studies
Reproductive toxicity: SD rats were given 100-1000 mg/kg orally before and during early gestation, and 320-3200 mg/kg orally during organogenesis, perinatal period, and lactation. No effect on fertility was observed, no teratogenic effect was observed, and no abnormalities in growth, development, and reproductive capacity of newborn pups were found.
[Pharmacokinetics].
1. Blood concentration
(1) In healthy adults, oral doses of 50, 100, and 200 mg on an empty stomach reached peak concentrations after approximately 4 hours, with maximum serum concentrations of 0.69, 1.13, and 1.95 μg/mL, respectively, and half-lives of 2.3 to 2.5 hours. When a single oral dose of 1.5, 3.0, and 6.0 mg/kg of drug is administered to a pediatric patient with normal renal function, peak concentrations are reached after approximately 3-4 hours at 1.14, 2.01, and 3.97 μg/ mL, respectively, with a half-life of 3.2 – 3.7 hours.
(2) Subjects with moderate kidney injury (30≦creatinine clearance<60 mL/min, N = 3) and subjects with severe kidney injury (10≦creatinine clearance& lt;30 mL/min, N = 4) were given a single dose of 100 mg cefixime pellets, respectively, with peak time of 2.04 μg/ mL at 6 hours post-dose in the moderate kidney injury group and 2.27 μg/ mL at 8 hours post-dose in the severe kidney injury group. serum levels were 0.71 μg/mL and 1.83 μg/mL at 12 hours, respectively. Elimination was significantly delayed in the severe kidney injury group, with half-lives of 4.15 and 11.05 hours, respectively.
2. Distribution
Distribution was observed in patients’ sputum, tonsil tissue, maxillary sinus mucosa, middle ear secretion, bile, and gallbladder tissue.
3. Metabolism
No active metabolites were found in human serum and urine.
4. Excretion
Primarily excreted renally, the urinary excretion rate (0-12 hours) in healthy adults at 50, 100, and 200 mg orally on an empty stomach was approximately 20-25%, with maximum urinary concentrations of 42.9 (4 to 6 hours), 62.2 (4 to 6 hours), and 82.7 (4 to 6 hours) μg/ mL, respectively. The urinary excretion rate (0 to 12 hours) at 6.0 mg/kg was approximately 13-20%.
[Storage] Store at room temperature.
[Packaging] Paper/aluminum/polyethylene pharmaceutical packaging laminate film. 6 bags/box; 8 bags/box; 10 bags/box; 12 bags/box.
[Executive Standard]
[Approval Number] State Drug Certificate H10940128
[Manufacturer]
Marketing license holder: Baiyunshan Pharmaceutical General Factory, Guangzhou Baiyunshan Pharmaceutical Group Co.
Registered Address: No. 88 Yunxiang Road, Tonghe Street, Baiyun District, Guangzhou
Postal code: 510515
Quality Service Tel: (020) 87063679
Sales service phone: (020) 87573176
Fax number: (020) 87061075
Website: http://www.byszc.com
Drug manufacturer: Baiyunshan Pharmaceutical General Factory, Guangzhou Baiyunshan Pharmaceutical Group Co.
Production Address: No. 88, Yunxiang Road, Tonghe Street, Baiyun District, Guangzhou