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Riviamycin (Ridomycin, Liviomycin, Lividomycin) and antibacterial spectrum are similar to kanamycin, and it works well on Gram-negative bacteria such as E. coli, Klebsiella pneumoniae, dysentery bacillus and proteus It also has a good effect on Staphylococcus aureus. It is mainly used for urinary tract, thoracic and abdominal cavity and intestinal infections caused by sensitive bacteria. Agent

Riviamycin (Ridomycin, Liviomycin, Lividomycin) and antibacterial spectrum are similar to kanamycin, and it works well on Gram-negative bacteria such as E. coli, Klebsiella pneumoniae, dysentery bacillus and proteus It also has a good effect on Staphylococcus aureus. It is mainly used for urinary tract, thoracic and abdominal cavity and intestinal infections caused by sensitive bacteria. Agent
Chinese name
Rifamycin
Foreign name
Lividomycin
Alias
Lidunomycin, Lidomycin, Penicillin
Field
biological
CAS number
36019-37-1
Molecular formula
C29H55N5O19
Molecular weight
777.76900
Exact mass
777.34900
PSA
426.47000

Introduction of rifamycin compounds

Rividin Basic Information

Chinese name nomycin
Chinese aliases: Lidumycin; Lidumycin; Penicillin; Lidumycin A; Rividomycin A
English name: Lividomycin
English alias: Antibiotic 503-1; 2230C; 4) -2,6-diamino-2,6-dideoxyhexopyranosyl- (1- & 3) pentofuranosyl] oxy} -3-hydroxycyclohexyl 2-amino-2-deoxyhexopyranoside; Antibiotic 2230C; Mannosylparomomycin ; 2- [5-amino-2- (aminomethyl) -6- [5- [3,5-diamino-2- [3-amino-4,5-dihydroxy-6- (hydroxymethyl) oxan-2-yl] oxy-6-hydroxycyclohexyl] oxy-4-hydroxy-2- (hydroxymethyl) oxolan-3-yl] oxy-4-hydroxyoxan-3-yl] oxy-6- (hydroxymethyl) oxane-3,4,5-triol
CAS number: 36019-37-1
Molecular formula: C 29 H 55 N 5 O 19
Molecular weight: 777.76900
Exact mass: 777.34900
PSA: 426.47000

Physiochemical properties of rifamycin

Density: 1.69g / cm 3
Boiling point: 1094.3ºC at 760 mmHg
Flash point: 615.6ºC
Refractive index: 1.687 [1]

Rivetomycin Drug Description

Riviamycin pharmacological action

Treponema pallidum, Treponema pallidum, Treponema pectoralis, and Leptospira are all sensitive to this product. With the widespread clinical application, the resistance of bacteria to this product has become increasingly serious. Among them, Gram-positive cocci have been reported more frequently. The common strains include Staphylococcus aureus, Streptococcus aureus, and Diplococcus pneumoniae. The mechanisms of bacteria's resistance to this class of antibiotics are: 1. Bacteria produce -lactamase, which decomposes and inactivates antibiotics, such as enzyme-producing Staphylococcus aureus, etc. This is the most common clinical drug resistance mechanism. Deeper and broader,
Rifamycin
2. The bacterial cell penicillin-binding egg changes automatically, which reduces the antibiotic binding ability or cannot bind, such as methicillin-resistant Staphylococcus aureus (MRSA), etc .;
3. Changes in the bacterial cell wall and reduced permeability, making antibiotics less or unable to reach the site of action, such as drug-resistant gonococci;
4. Bacteria develop tolerance, which seems to be related to the lack of autolytic enzymes. Of course, there may be other mechanisms.

Rifamycin pharmacokinetics

This product is easily destroyed by gastric acid, and absorbed quickly by intramuscular injection, reaching peak plasma concentration in 15-30 minutes.
Rifamycin
This product is widely distributed in tissues, body fluids and body cavities after absorption. The drug concentration in the thoracic, abdominal and joint cavity fluids is about 50% of the blood concentration. This product does not easily enter the eyes, bone tissue, no blood supply area and abscess cavity, and easily penetrates into tissues with inflammation. This product is difficult to penetrate the blood-brain barrier. The concentration of drugs in the cerebrospinal fluid is 1% to 3% of blood concentration. Meninges The drug concentration in the cerebrospinal fluid of patients with inflammation can reach 10% to 30% of the blood concentration, so large-dose intravenous administration can still reach an effective therapeutic concentration. The plasma protein binding rate of this product is about 60%. It is mainly metabolized by the kidneys and has normal renal function. The half-life is about 0.5h. Patients with renal failure can reach 7-10 hours. Those with liver dysfunction can be delayed.

Rifamycin indications

This product is mainly used for various infections caused by sensitive bacteria, such as respiratory infections, pneumonia: bronchitis, meningitis, endocarditis, abdominal pain, abscess, otitis media, sepsis, gonorrhea, syphilis, self-throat, rat bite Heat, gas gangrene, anthrax, etc.

Riviamycin Usage and Dosage

Usual dose for adults, intramuscular injection, 800,000 to 2 million U per day, divided into 2 to 3 doses; intravenously
Rifamycin
Infusion, 2 million to 10 million U per day, divided into 2 to 4 times. Common dosage for children: intramuscular injection, 30,000 to 50,000 U per kilogram of body weight, divided into 2 to 3 times; intravenous drip, 50,000 to 200,000 U per kilogram of body weight, divided into 2 to 4 times medicine. In severe cases, the dose can be appropriately increased, and the dose and the administration interval can be adjusted in time according to renal function.

Rifamycin adverse reactions

1. Allergic reactions. The incidence is estimated to be 1% to 10%, ranging from rashes to allergies such as skin allergies,
Rifamycin
Organ allergies vary in severity, the most serious of which is anaphylactic shock, which can be life-threatening. If anaphylactic shock occurs, the drug should be discontinued immediately, and subcutaneous or intramuscular injection of epinephrine 0.5-10 mg, and those with cardiac arrest can be injected intracardially ( Young children cut).
2. Give oxygen and use antihistamines and adrenocortical hormones at the same time. If the clinical symptoms do not improve, repeat the administration after 30 minutes. Before applying this product, you must ask in detail whether there is a history of drug allergies and allergies. For those who use penicillin for the first time or stop using it for more than 72 hours, perform an intradermal sensitivity test. The skin test solution is a solution prepared by penicillin sodium and sodium chloride injection, containing 500U per penicillin.
Precautions
1. Treatment contradiction, Herxheimer reaction. When using this product to treat syphilis or other infections, there may be contradictions such as fever, sweating, headache, and reaction to the injured part. It is called Herzheimer reaction. The reason may be
Rifamycin
It can be caused by the endotoxin released by the killed pathogens, or the lesions can be anti-inflammatory too quickly, the tissues can be repaired late, and the organ function can be hindered.
2. A double infection may occur during treatment. Common infections include penicillin-resistant Staphylococcus aureus, Gram-negative bacilli, or Candida albicans.
3. Intramuscular injection of penicillin potassium salt has obvious local pain, and 0.2% lidocaine hydrochloride and 0.8% sodium chloride injection can be used as a diluent to reduce pain.
4. During the application of this product, it may interfere with some diagnoses, which can cause false positives in the determination of urine sugar by the ketone sulfate method.
5. In patients with tetanus and diphtheria, penicillin should be used to kill pathogens and prevent the production of toxins, but it cannot replace antitoxin treatment.

Leviamycin Expert Reviews

Lidomycin Lidomycin has been used to treat urinary tract infections, pelvic infections, bacillary dysentery, acute lymphadenitis, cellulitis, ridges, perianal abscesses, cholangitis, respiratory infections; eyes, ears, nose, throat, etc. There were 642 cases of purulent infection, peritonitis, prostatitis, paratestitis, and other infections, with a total effective rate of 72.6%. Rivitomycin has a good effect on acute urinary tract infections, with an effective rate of 90%, and a poor effect on chronic urinary tract infections. Oral rifamycin has a positive effect on infant bacillary dysentery. It also has a good effect in treating various eye, ear, nose and throat infections. Patients with otitis media can use local infusion. For skin purulent diseases and respiratory infections, the effect is not outstanding, and it should not be preferred [2] .

Rifamycin granules

Pharmacological action
Staphylococcus is a propionate derivative of macrolide antibiotic josamycin produced by Streptomycesnarbonensisvar.Josamyceticus. Its antibacterial spectrum is similar to that of erythromycin. It has antibacterial properties against Staphylococcus and Streptococcus. The effect is slightly worse than erythromycin, but it still has antibacterial activity against inducible drug-resistant strains; Neisseria meningitidis and Pertussis
Rifamycin
Sensitive; Good antibacterial effect against anaerobic bacteria such as pneumococcus, peptococcus, propionibacterium and Eubacteria; intracellular pathogens such as Mycoplasma, Chlamydia, Legionella are also sensitive to this product. This product does not induce resistance of Staphylococcus to macrolides and is a non-inducing antibiotic. This product is pink suspended particles.
dynamics
Eight healthy male volunteers took 1 g (potency) of this product orally, the average peak time (tmax) was 2.19 hours, the peak plasma concentration (Cmax) was 4.51 (g / ml, and the blood elimination half-life (t1 / 2 () was 1.75 hours, relative bioavailability is 117.4 (29.2. According to clinical reports, children take this product orally at a weight of 0.02 g / kg, and the blood concentration is 2.6 to 8.0 (g / ml for 1 hour, 0.66 to 4.4 (g / for 6 hours) ml, the blood concentration is higher than that of adults and it lasts for a long time. This product is an ester of josamycin, which is not easily affected by gastric acid and loses its potency. It is mainly excreted in the form of josamycin and its metabolites through urine. After pediatric oral administration of 0.02g / kg body weight, the urine excretion rate within 24 hours is 6.6 to 12.5%.
Indication
This product is suitable for pharyngitis and tonsillitis caused by Streptococcus pyogenes, sinusitis, otitis media, acute bronchitis and oral abscess caused by sensitive bacteria, pneumonia caused by Mycoplasma pneumonia, skin and soft tissue infection caused by sensitive bacteria, and can also be used for Staphylococcal infections resistant to penicillin and erythromycin.
Dosage
Take it orally. Children take 30mg / kg a day, divided into 3 to 4 times.
Adverse reactions
1. Gastrointestinal reactions include diarrhea, nausea, vomiting, upper and middle abdominal pain, mouth and tongue pain, and decreased gastric appetite. The incidence is related to dose. The incidence of gastrointestinal reactions of this product is significantly lower than that of erythromycin.
2. Hepatotoxic symptoms such as fatigue, nausea, vomiting, abdominal pain, fever and abnormal liver function are rare, and jaundice is occasionally seen.
3. Taking this product in large doses may cause hearing loss, and most of them can recover after stopping the medicine.
4, occasional allergic reactions, manifested by drug fever, rash, eosinophilia and so on.
Rifamycin
5, occasional arrhythmia, oral or vaginal candida infection.
Taboo
Those who are allergic to this product, erythromycin or other macrolide antibiotics are contraindicated.
Precautions
1. When the patient is allergic or intolerant to one of the macrolides (such as erythromycin), the other macrolide (such as this product) may also be allergic or intolerant.
2. Patients with hemolytic streptococcal infection should be treated with this product for at least 10 days to prevent the occurrence of acute rheumatic fever.
3. Patients with impaired renal function generally do not need to reduce the dosage.
4. Liver function should be regularly followed during taking this product. The dose for patients with liver disease and severe renal impairment should be appropriately reduced.
5. Interference to laboratory inspection indicators: This product can interfere with the fluorescence measurement of the Higerty method, which makes the measured value of urinary catecholamines falsely increase. Measurements of serum alkaline phosphatase, bilirubin, alanine aminotransferase, and aspartate aminotransferase may all increase.
6. Due to the differences in the sensitivity of different bacteria to this product, it is advisable to make a drug sensitivity test.
interaction
1. This product should be used in combination with preparations containing ergotamine drugs, or use ergotamine drugs in a reduced amount.
2, this product does not affect the role of liver drug metabolism enzymes, no compatibility with theophylline, oral contraceptives and cyclosporine.
3. When combined with penicillin, this product may interfere with the bactericidal activity of the latter.
4. This product has no significant effect on the metabolism of drugs such as aminophylline.

A brief case of rifamycin treatment

General information: The 120 patients in this group were all from urology clinics. They were all males, aged 20 to 51 years, 102 married, 18 unmarried, and had a history of unclean sex from 7 days to 1.5 years, including trachoma Chlamydia fluorescent antibody test was positive in 64 cases, ureaplasma urealyticum culture in 29 cases, and dual infection in 27 cases.
Clinical manifestations All patients have varying degrees of urethral discomfort and a small amount of thin secretions, and some patients have urethral pain and flushing of the urethra.
treatment method
Chlamydia-positive patients take oral rifamycin 0.5g twice daily for 2 weeks; Mycoplasma-positive patients take oral rifamycin 0.5g twice daily for 20 days; patients with dual infection take oral rifamycin 0.5g twice daily for 20 days. During the treatment of all patients, other antibiotics are prohibited. Avoid eating spicy, spicy, irritating food and alcohol. After the treatment was stopped, the drug was rechecked for 1 week to determine the efficacy and side effects were recorded.
result
Efficacy criteria for recovery: clinical symptoms and signs disappeared, pathogen examination turned negative for cure, otherwise it was invalid.
Results 86 cases of Chlamydia infection were cured, 5 cases were ineffective, the cure rate was 94.5%; 48 cases of Mycoplasma infection were cured, 8 cases were ineffective, the cure rate was 85.7%.
After taking the drug, 12 patients complained of dizziness and mouth pain, and 8 patients had gastric discomfort. The symptoms were mild and did not affect the treatment.
discuss
Rivitromycin is a new type of macrolide antibiotic, which is substituted by methyl group at the 6th hydroxy group on the macrolide ring of erythromycin. Antibacterial effect is produced mainly by blocking the connection of nuclear protein 50S subunits and inhibiting protein synthesis. Its efficacy is 7 to 10 times that of erythromycin and 4 times that of doxycycline. The drug has strong antibacterial activity against chlamydia and mycoplasma. Clinical reports have reported satisfactory results with imported rifamycin in the treatment of this disease. We use domestic rifamycin to treat the disease. The cure rates are 94.5% and 85.7%, The curative effect is close to that of domestic rifamycin, which shows that the curative effect of domestic rifamycin is reliable, and the price is cheap. It is an effective drug for the treatment of non-gonococcal urethritis, and it is available for clinical selection.

Levimycin reaction case

Clarithromycin dispersible tablets cause severe allergic reactions
A 28-year-old woman with antibiotics weighed 66 kg and had a history of penicillin allergy. He came to our hospital for red pimples on his face. After examination, he was diagnosed with acne vulgaris. He was given oral clarithromycin dispersible tablets, 250 mg / tablet twice a day, and applied compound sulfur yellow cream and compound chloramphenicol lotion. (All preparations made by our hospital). About 2-3 hours after taking the clarithromycin dispersible tablet for the first time, the patient developed chest tightness, palpitations, sweating, and weakness throughout his body. He felt anxiety and fear for several hours. Patients have since discontinued oral medication.
Discussion: Clarithromycin is a macrolide antibiotic. It is reported in the literature that the drug has low toxicity and is well tolerated by the body. The main adverse reactions were gastrointestinal reactions such as loss of appetite, nausea, vomiting, and diarrhea, and they mostly occurred in long-term large doses (2g / d), which had a lower incidence than erythromycin and roxithromycin. Individual patients may develop neurological symptoms such as headache and tinnitus, as well as allergic reactions such as rash. The adverse reactions reported so far are mostly such mild reactions. The drug has almost no cross-allergic reactions with other drugs, so it is widely used in clinical practice.
This patient's severe allergic reaction is rare. The time of its occurrence is 2-3 hours after taking the drug. It is the peak time of clarithromycin in the body. Is there a relationship between dose and adverse reactions or does the patient have The history of penicillin allergy is susceptible. The constitution is also sensitive to the semi-synthetic antibiotic clarithromycin, which deserves further analysis.
In short, this case report once again reminded the clinic of other antibiotics that do not require skin tests. Even if it is administered orally, do not ignore the patient's serious history of allergies to previous medications in order to remind patients to take good self-monitoring of medications and reduce seriousness. Occurrence of adverse reactions
A case of delayed allergy caused by intravenous drip of rifamycin?
Allergies caused by rifamycin are mostly slow, and delayed allergies caused by injection are rare in clinical practice. ?
1 Case introduction patient, male, 59 years old, suffering from osteoarthritis of the lower limbs. He was treated at the local health center all year round. Because the patient is allergic and allergic to penicillin and amikacin injection, he took oral diclofenac, inflammation Tongxikang tablets, Shujin Huoxue tablets, topical bone spurs a tea spirit, zhefeng cream, musk analgesic cream and other treatments, but the effect is not good. Multiple injections of Fengshenning injection and Xuelian injection have satisfactory results. On March 21, 2002, the patient went to the hospital again. We used 600,000 leucomycin injection and added 5% glucose injection to 250ml by intravenous drip. After 50 minutes, the patient described: skin on the top of the head, neck, and hands. Itching, scleral flushing, redness and swelling around the face, severe headache. Later, the patient reported chest tightness and discomfort. She checked T36.8 , P60 times / min, and blood pressure 11.2 / 8kpa. Consider levamycin allergy, then use: cedar Misong injection was given 10 mg intravenously, and phenagen injection was given 25 mg intramuscularly. After 30 minutes, severe headaches, itching, and chest tightness were alleviated and gradually improved, and the symptoms completely disappeared after 2 hours. ?
2 Discussion The antibacterial spectrum of rifamycin is similar to that of erythromycin, and its effect on gram-positive cocci is slightly weaker than that of erythromycin, but it is more effective against erythromycin-resistant Staphylococcus aureus due to drug resistance It appears slowly, this product has low toxicity, and is safe for intravenous injection. The main adverse reactions include nausea, vomiting, loss of appetite, abdominal pain and diarrhea. Severe headache, head itch, neck itching, chest tightness and discomfort are less common. This patient is allergic and has an allergic reaction to penicillin and amikacin injection. The skin appears to be pushed for 50 minutes with levamycin injection 600,000. Limb itching, facial swelling, severe headache, chest tightness and other reactions should attract the attention of medical staff. When using drugs for patients with allergies, you should closely observe the reaction to the drug, and immediately stop the drug for rescue treatment when abnormal reactions are found [3] .

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