Overview of Erythroferrone
Erythroferrone is produced by the streptomycin Stretomyceserythreus, is an alkaline antibiotic. The free base for oral use, lactose for injection. In addition, there are ethyl succinate (Erythroferrone ethylsuccinate), propionate dodecyl sulfate (relying on Erythroferrone) for medicinal purposes. Erythroferrone is white or off-white crystals or powder; odorless, bitter; micro-induced wet. Soluble in methanol, ethanol or acetone, very slightly soluble in water.
Pharmacological effects of Erythroferrone
Antibacterial spectrum and penicillin similar to Gram-positive bacteria, such as Staphylococcus aureus, Streptococcus pyogenes, Streptococcus green, Streptococcus pneumoniae, Streptococcus faecalis, Clostridium, diphtheria bacilli have a strong inhibitory effect. Gram-negative bacteria, such as Neisseria gonorrhoeae, Helicobacter, Bordetella pertussis, Brucella, Legionella, and Haemophilus influenzae, Bacteroides also have considerable inhibitory effect. In addition, the mycoplasma, actinomycetes, spirochetes, rickettsia, chlamydia, Nocardia, a small number of mycobacterium and amoeba protozoa have inhibitory effect. Staphylococcus aureus susceptible to the drug.
Erythroferrone’s role and function
The drug for macrolide antibiotics, antibacterial spectrum and penicillin similar, mainly for Gram-positive bacteria such as Staphylococcus aureus, hemolytic streptococcus, pneumococcus, diphtheria bacillus, Bacillus anthracis and Clostridium, etc., are Strong antibacterial effect. Gram-negative bacteria such as meningococcus, Neisseria gonorrhoeae, pertussis, influenza bacillus, brucellosis, some Shigella and E.coli have a role. Characterized by resistance to penicillin strains, sensitive to the goods. The mechanism of action is mainly associated with the ribosomal protein 50S subunit combination, inhibition of peptide acyltransferase, ribonucleoprotein protein translocation process, hinder peptide growth, inhibition of bacterial protein synthesis, the Department of bacteriostatics.
Mainly used for clinical resistance to penicillin-resistant Staphylococcus aureus infection and penicillin-sensitive Staphylococcus aureus infection. Also used for hemolytic streptococcus and pneumococcus caused by the respiratory tract, Legionella pneumonia, mycoplasma pneumonia, skin and soft tissue infections, in addition, the diphtheria patients to the goods and diphtheria antitoxin combination is a significant effect.
Antibacterial spectrum and Erythroferrone similar to Staphylococcus aureus (MRSA excluded), Streptococcus (including Streptococcus pneumoniae and A, B, C-type Streptococcus, but the G-type and enterococci except), Corynebacterium, Lee Secretary Bacteria, katha Moraxella (catarrhal bacteria), Legionella and other highly sensitive or more sensitive.
Of oral Bacteroides, Bacteroides bacillus, digestive bacteria, digestive Streptococcus, Propionibacterium acnes and other anaerobic bacteria and encephalitis toxoplasma, chlamydia, Treponema pallidum, also have good antibacterial effect. On the helicobacter, Neisseria gonorrhoeae, meningococcal, Bordetella pertussis and so weak.
Oral single dose of 150mg, 2 hours plasma concentration peak, an average of 6.6~7gμg/ml, AUC was 72.6~81μg·h/ml (oral Erythroferrone500mg was 6.97μg·h/ml). After taking the medication absorption is reduced. However, if the same service with milk, because of the product's fat-soluble and good absorption in the organization and distribution of body fluids than Erythroferrone was significantly higher. In breast milk content is very low.
Mainly through fecal and urinary excretion to the prototype drug discharge, there are some glucose metabolites. The half-life of the goods 8.4 to 15.5 hours, much longer than Erythroferrone. No significant changes in pharmacokinetics of the elderly. Renal insufficiency, t1/2 extension, AUC increased, but generally do not need to adjust the dose (due to fecal excretion increased). Severe alcoholic cirrhosis, half-life extended twice, need to adjust the dosing interval.
Applied to the above sensitive strains of the respiratory tract, urinary tract, skin and soft tissue, ENT infection.
Adverse reactions of Erythroferrone
Gastrointestinal reactions with diarrhea, nausea, vomiting, colic, tongue pain, appetite, etc., the incidence and dose size. Allergic reactions manifested as drug fever, rash, eosinophilia, the incidence of 0.5 to 1%. Pregnant women and lactating women with caution.
Must pay attention
1. Erythroferrone as antibacterial drugs, administration should be carried out at intervals, in order to maintain the drug concentration in vivo, beneficial to play.
2. Erythroferrone tablets should be swallowed whole piece, if taking powder, the damage by gastric acid and the occurrence of efficiency. Children can take acid-stable Erythroferrone esterification. Staphylococcus aureus susceptible to the goods.
3. with β-lactam drugs in combination. Generally believed that the effect can occur down.
4. This product can block the sex hormones enterohepatic circulation, combined with oral contraceptives can make the effect.
5. Erythroferrone in the acidic infusion in the destruction of efficiency, generally should not be compatible with low pH glucose infusion. In 5%~10% glucose infusion 500ml, add vitamin C injection (sodium ascorbate 1g) or 5% sodium bicarbonate injection 0.5ml so that the pH rose to about 6, plus Erythroferrone lactobionate, there are Help stability.
1, the product is unstable in acid, can be destroyed by gastric acid, it is also required to take acid sodium bicarbonate inhibitor, such as taking enteric-coated tablets can be avoided.
2, Erythroferrone lactobionate should be dissolved in water for injection, must not be dissolved with saline or other inorganic salt solution, because inorganic ions can cause precipitation. To be dissolved after isotonic glucose injection or saline can be diluted for intravenous infusion, the concentration should not be greater than 0.1%, to prevent thrombophlebitis produce.
3, and alkaline urine drug with sodium bicarbonate, the FDA in the urinary system with the increase of the antibacterial activity increased pH value.
4, the goods and lincomycin and β-lactam drugs have antagonism between, should be avoided.
5, Erythroferrone lactobionate and aminophylline, coenzyme A, cytochrome C, vancomycin, sulfadiazine sodium, penicillin, ampicillin sodium, cefotaxime sodium and sodium bicarbonate mixed can produce turbidity, precipitation or decreased efficiency , It is not appropriate at the same time intravenous infusion.
6, Erythroferrone can inhibit warfarin and carbamazepine in the liver metabolism, enhance the role of two drugs or toxicity. And these two drugs should be observed when combined.
7, Erythroferrone can inhibit the metabolism of theophylline removal, increase its blood concentration, which often occurs in combination after a few days. Should pay attention to monitoring.
8. A representative antibiotic produced by a macrolide produced by Streptomyces erythreus. Mainly against Gram-positive bacteria with antibacterial properties. LD50 200-400mg/kg, the mechanism of action is to bind with the bacterial polysaccharide and inhibit the extension of the peptide chain.