Open classification: antibiotics, roxithromycin
Drug name
Generic name: English name: roxithromycin capsules
Main ingredients: roxithromycin
Chemical name: 9-[O-[(2- methoxyethoxy)-methyl] oxime] erythromycin.
Molecular formula: C4 1H76N2O 15.
Molecular weight: 837.03
Pharmacology and toxicology
This product is a semi-synthetic 14 macrolide antibiotic. The antibacterial spectrum and antibacterial effect are basically similar to erythromycin, but the effect on gram-positive bacteria is slightly worse than erythromycin, and the effect on Legionella pneumophila is stronger than erythromycin. The antibacterial effect on Chlamydia pneumoniae, Mycoplasma pneumoniae and Ureaplasma urealyticum is similar to or slightly stronger than erythromycin.
The product can penetrate bacterial cell membrane, reversibly bind to bacterial ribosome 50S subunit near the donor ("P" site), prevent t-RNA from binding to "P" site, and prevent polypeptide chain from transferring from the receptor ("A" site) to "P" site, thus inhibiting bacterial protein synthesis.
The natural products of 14 yuan macrolides used in clinic are erythromycin and oleanolic acid; Semi-synthetic products include erythromycin ethylsuccinate, erythromycin propionate, erythromycin estolate, formoterol and roxithromycin, clarithromycin and dirithromycin, which only came out in recent years.
pharmacokinetics
The binding rate of this product with albumin is15.6-26.7%; Take 0.3g of this product, which has good absorption and high peak concentration. The peak time is 1.30 1.00 hours, and the peak concentration is 6.32 1.45mg/l/L, which is widely distributed, with a high concentration in lung, tonsil and other tissues, and the elimination half-life is 7.3 1.65438.
indicate
1, suitable for the following infections caused by sensitive strains: (1) upper respiratory tract infection; (2) Lower respiratory tract infection; (3) Otolaryngology infection; (4) Infection of urogenital system; (5) Skin and soft tissue infection; (6) Pediatric infection.
2. It can also be used for infections caused by mycoplasma, chlamydia and Legionella.
dosage
Oral administration on an empty stomach, the general course of treatment is 5 ~ 12 days.
Adults 150mg once, twice a day; Or 300mg at a time, one day 1 time.
Children weigh 2.5 ~ 5 mg/kg once, twice a day.
counteraction
The main adverse reactions were abdominal pain, diarrhea, nausea, vomiting and other gastrointestinal reactions, but the incidence was significantly lower than erythromycin. Occasionally rash, itchy skin, dizziness, headache, abnormal liver function (elevated ALT and AST), and peripheral blood cell reduction.
taboo
It is forbidden for those who are allergic to this product, erythromycin or other macrolides.
Matters needing attention
1. Use with caution in patients with hepatic insufficiency. The blood elimination half-life (t 1/2b) of patients with severe liver cirrhosis was prolonged to more than twice the normal level. If it is really necessary to use it, it should be given 150mg once a day 1 time.
2. There is no need to adjust the dosage for patients with mild renal insufficiency, and the medication time for patients with severe renal insufficiency is doubled (150mg once,/kloc-0 once a day).
3. This product has cross resistance to erythromycin.
4. In order to obtain a higher plasma concentration, this product should be taken with water on an empty stomach (1 hour before meals or 3-4 hours after meals).
5. Follow up liver function regularly during medication.
Medication for pregnant and lactating women
Pregnant women and lactating women should use it with caution. Less than 0.05% of the dose is discharged into breast milk. Although there are reports that it has little effect on babies, it is still necessary to consider whether to stop breastfeeding.
Children's medication
Medication for elderly patients
If the pharmacokinetics of the elderly has not changed significantly, there is no need to adjust the dose.
drug interaction
1. Incompatible ergotamine, dihydroergotamine, bromocriptine, terfenadine, ketoconazole and cisapride.
2. It has little effect on aminophylline metabolism, and basically has no effect on antacids such as carbamazepine, warfarin and ranitidine.
excessive
Validity period: tentatively 1 year.
standard
50 mg (2)75 mg (3) 150 mg
Sustained-release preparation is a preparation that delays the release, absorption, distribution, metabolism and excretion of drugs in vivo by appropriate methods, thus prolonging the action of drugs. In addition to ibuprofen, aspirin and Tylenol all have sustained-release preparations.
Roxithromycin sustained-release capsules have the same effect as the former! !
Compared with common preparations, sustained-release preparations have three advantages:
1, easy to take. General preparations often need to be administered several times a day, while sustained-release preparations usually only need to be administered 1-2 times a day.
2. Slow-release drugs take effect more slowly than common preparations, which avoids the fluctuation of effective blood drug concentration caused by excessive fluctuation of blood drug concentration after frequent administration of common preparations.
3. The toxic and side effects are less than those of general preparations.