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地红霉素肠溶胶囊2
地红霉素肠溶胶囊
  • 地红霉素肠溶胶囊2
  • 地红霉素肠溶胶囊
ENGLISH NAME: Dirithromycin Enteric-coated Capsules
SPECIFICATIONS: (1) 0.125 g; (2) 0.25 g
LICENSE NUMBER: (1) 0.125 g  H2005161; (2) 0.25 g  H20061219
PRODUCT PACKAGING: Aluminium Plastic Composite Panel, 4 capsules/box, 6 capsules/box, 8 capsules/box, 12 capsules/box, 24 capsules/box, 48 capsules/box
FORMULATION: Capsule
STORAGE CONDITION: Shading, Closed, Preservation of the Shade
SHELF LIFE: 24 Months
Description: Dirithromycin Enteric-coated Capsules is in a class of drugs called macrolide antibiotics. Dirithromycin fights bacteria in your body. Dirithromycin Enteric-coated Capsules is used to treat many different types of bacterial infections, such as bronchitis, pneumonia, tonsillitis, and skin infections. Dirithromycin Enteric-coated Capsules may also be used for purposes other than those listed in this medication guide.  Dirithromycin has the chemical name (2R,3R,6R,7S,8S,9R,10R,12R,13S,15R,17S)-9-{[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy}-3-ethyl-2,10-dihydroxy-7-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy}-15-[(2-methoxyethoxy)methyl]-2,6,8,10,12,17-hexamethyl-4,16-dioxa-14-azabicyclo[11.3.1]heptadecan-5-one.

Pharmacological effects: Dirithromycin is a macrolide glycopeptide antibiotic. It is used to treat many different types of bacterial infections, such as bronchitis, pneumonia, tonsillitis, and even skin infections. Pharmacology: Dirithromycin is a pro-drug which is converted non-enzymatically during intestinal absorption into the microbiologically active moiety erythromycylamine. Erythromycylamine exerts its activity by binding to the 50S ribosomal subunits of susceptible mircoorganisms resulting in inhibition of protein synthesis. Dirithromycin/erythromycylamine has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections: Staphylococcus aureus (methicillin-susceptible strains only), Streptococcus pneumoniae, Streptococcus pyogenes, Haemophilus influenzae, Legionella pneumophila, Moraxella catarrhalis, and Mycoplasma pneumoniae. Mechanism of action: Dirithromycin prevents bacteria from growing, by interfering with their protein synthesis. Dirithromycin binds to the 50S subunit of the 70S bacterial ribosome, and thus inhibits the translocation of peptides. Dirithromycin has over 10 times higher affinity to the subunit 50S than erythromycin. In addition, dirithromycin binds simultaneously in to two domains of 23S RNA of the ribosomal subunit 50S, where older macrolides bind only in one. Dirithromycin can also inhibit the formation of ribosomal subunits 50S and 30S. Drug type: Approved. Small Molecule. Drug category: Anti-Bacterial Agents. Anti-Infectives. Macrolides.

Pharmacokinetics: Dirithromycin is a 14-membered lactone ring macrolide and is the C9-oxazine derivative of erythromycylamine. The human pharmacokinetics and clinical pharmacology of dirithromycin have been studied. Dirithromycin has unique pharmacokinetics which distinguish it from erythromycin. In man, following an oral 500 mg dose of dirithromycin, a mean peak plasma concentration (Cmax) of 0.48 mg/L (range 0.1-1.97) was observed at 4 h. The mean area under the plasma concentration versus time curve (AUC0-24h) measured 3.37 mg.h/L (range 0.39-17.16). No plasma accumulation was observed with multiple-dose administration. Dirithromycin may be taken without regard to meals, although food and H2-receptor antagonists may increase the systemic bioavailability in some patients. Based upon drug interaction studies performed with antipyrine and theophylline, dirithromycin has shown less potential to interact with other drugs metabolized by the cytochrome P450 system that does erythromycin. Plasma concentrations and AUCs were low due to rapid movement of the drug from the vascular space to the extravascular compartment, as reflected by tissue concentrations, which exceeded plasma concentrations 4 h after dosing. Dirithromycin achieves relatively high tissue concentrations (approximately 0.8-5.0 mg/kg) 4-24 h after dosing. The extensive tissue penetration is reflected in a large mean apparent volume of distribution of 800 L (range 504-1041). Dirithromycin is rapidly converted by non-enzymatic hydrolysis during absorption to erythromycylamine, which is microbiologically active. In a 14C-radiolabelled study, 60-90% of the administered dose was hydrolysed to erythromycylamine within 35 min of infusion. After 1.5 h, conversion to erythromycylamine in serum was virtually complete. Plasma protein binding was determined to be 15-30% by ultracentrifugation. Dirithromycin is characterized by a plasma elimination half-life of 44 h (range 16-65 h) that permits once-daily administration. Total body clearance was 226-1040 mL/min in the 14C-radiolabelled study. The primary route of elimination of dirithromycin/erythromycylamine was faecal/hepatic. Following intravenous administration, approximately 17-25% of the radioactivity appeared in the urine and 62-81% appeared in the stool, indicating predominantly hepatic excretion. With oral administration 1.2-2.9% of the radioactivity appeared in the urine and 81-97% in the stool. The major part of urinary excretion occurs within the first 48 h post-administration; however, urinary excretion of radioactivity lasted longer than 240 h. The absolute bioavailability calculated from dose-corrected urinary excretion data was 10% (6-14%).


Indications:  Applicable to the treatment of individuals age 12 years and older with mild-to-moderate infections caused by susceptible strains of the designated microorganisms in the specific conditions listed below: Acute Bacterial Exacerbations of Chronic Bronchitis due to Haemophilus influenzae, Moraxella catarrhalis, orStreptococcus pneumoniae. Secondary Bacterial Infection of Acute Bronchitis due to Moraxella catarrhalis or Streptococcus pneumoniae. Community-Acquired Pneumonia due to Legionella pneumophila, Mycoplasma pneumoniae, or Streptococcus pneumoniae. Pharyngitis/Tonsilitis due to Streptococcus pyogenes Uncomplicated Skin and Skin Structure Infections due to Staphylococcus aureus or Streptococcus pyogenes .

Precautions: Hepatic Insufficiency: No dosage adjustment should be necessary in patients with mildly impaired hepatic function. Renal insufficiency: No dosage adjustment should be necessary in patients with impaired renal function. Pseudomembranous colitis has been reported with nearly all antibacterial agents, including dirithromycin, and may range in severity from mild to life-threatening. Therefore, it is important to consider this diagnosis in patients who suffer of diarrheasubsequent to the administration of antibacterial agents. After the diagnosis of pseudomembranous colitis has been established, therapeutic measures should be initiated. Mild cases of pseudomembranous colitis usually respond to discontinuation of the drug alone. In moderate-to-severe cases, consideration should be given to management with fluids and electrolytes, protein supplementation, and treatment with an antibacterial drug clinically effective against C. difficile colitis.

Adverse reaction:  In clinical trials, 3299 patients were treated with dirithromycin 500 mg q.d. P.O. for approximately 7 to 14 days. There were no deaths or permanent disabilities thought related directly to drug toxicity. Eighty-seven (2.6%) patients discontinued medicationdue to adverse reactions. Thirty-five (40%) of the 87 patients who discontinued therapy did so because of nausea or abdominal pain. In additional clinical trials, patients were treated with dirithromycin 500 mg q.d. for 5 days. Thirty-five (3.8%) patients discontinued medication due to adverse reactions. Fifteen (43%) of the 35 patients who discontinued therapy did so because of nausea or abdominal pain. The following adverse reactions were reported during the dirithromycin clinical trials: headache 7.7%, abdominal pain 7.1%, diarrhea 6.7%, nausea 5.9%, gastrointestinal disorder 2.6%, dizziness/vertigo 2.1%, rash 1.4%, vomiting 1.1% etc. Platelet count increased 3.8%, potassium increased 2.6%, bicarbonate decreased 1.4%, CPK  increased 1.2%, eosinophils increased 1.2%, seg neutrophils increased 1.2%, leucocytes increased etc.  1% to 10%: Central nervous system: Headache, dizziness, vertigo, insomnia Dermatologic: Rash, pruritus, urticaria Endocrine & metabolic: Hyperkalemia. Gastrointestinal: Abdominal pain, nausea, diarrhea, vomiting, dyspepsia, flatulence. Hematologic: Thrombocytosis, eosinophilia, segmented neutrophils. Neuromuscular & skeletal: Weakness, pain, increased CPK. Respiratory: Increased cough, dyspnea<1%: Palpitations, vasodilation, syncope, edema, anxiety, depression, somnolence, fever, malaise, dysmenorrhea, hypochloremia, hypophosphatemia, increased uric acid, dehydration, abnormal stools, anorexia, gastritis, constipation, abnormal taste, xerostomia, abdominal pain, mouth ulceration, polyuria, vaginitis, neutropenia, thrombocytopenia, decreased hemoglobin/hematocrit; increased alkaline phosphatase, bands, basophils; leukocytosis, monocytosis, Increased ALT/AST, GGT; hyperbilirubinemia, paresthesia, tremor, myalgia, amblyopia, tinnitus, increased creatinine, phosphorus, epistaxis, hemoptysis, hyperventilation, hypoalbuminemia, flu-like syndrome, diaphoresis, thirst.
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