What Is Lincomycin?

Lincomycin, a drug, is a 50S subunit that acts on the ribosomes of sensitive bacteria, preventing the peptide chain from elongating, thereby inhibiting protein synthesis in bacterial cells.

(1) The infrared absorption spectrum of this product should be consistent with the control spectrum. (2) Take this product and lincomycin reference substance, add mobile phase separately to make a solution containing about 2mg per 1ml, and perform the test according to the HPLC conditions under the content determination item. The retention time of the main peak of the test product It should be consistent with the retention time of the main peak of the reference. (3) The identification of chlorides in aqueous solution of this product. ^[1]

English name LincomycinHydrochlorideOralSolution, Western medicine.

Pharmacological action

1. Pharmacology This product is a lincomycin antibiotic. The antibacterial spectrum is similar but narrower than that of erythromycin. It has high antibacterial activity against Gram-positive bacteria such as Staphylococcus (including penicillin-resistant strains), Streptococcus, Diphtheria, Anthracis and so on. It also has good antibacterial activity against Gram-negative anaerobic bacteria. Bacteroides, including Bacteroides fragile, Fusobacterium, Peptococcus, Peptostreptococcus, and Perfringens are most highly sensitive to this product. Gram-negative aerobic bacteria, including Haemophilus influenzae, Neisseria and Mycoplasma, are resistant to this product. This product has no cross-resistance with penicillin, chloramphenicol, cephalosporins and tetracyclines, has partial cross-resistance with macrolides, and completely cross-resistance with lincomycin. The mechanism of action of this product is that it binds to the bacterial ribosomal 50S subunit, preventing the extension of the peptide chain, thereby inhibiting the protein synthesis of bacterial cells. This strain is a bacteriostatic drug, but it also has a bactericidal effect on certain bacteria at high concentrations.

2. Toxicology: The LD50 of this product: 214 mg / kg for mice intravenously, 4000 mg / kg for oral administration; 4000 mg / kg for rats. This product is a red-brown transparent liquid with a sweet taste.

dynamics

This product enters the fetal circulation through the placenta

This product is quickly absorbed in the gastrointestinal tract after oral administration and is not damaged by gastric acid. This product is taken orally on an empty stomach, and only 20% to 30% is absorbed, and less absorbed after eating. Oral 0.5g of this product, peak blood concentration (Cmax) within 2 to 4 hours, can maintain the minimum inhibitory concentration (MIC) for most Gram-positive bacteria for 6 to 8 hours. Except for cerebrospinal fluid, it is widely and rapidly given to various body fluids and tissues

English name LincomycinHydrochlorideTablets, western medicine.

Pharmacological action

This product has high antibacterial activity against common aerobic gram-positive bacteria, such as Staphylococcus aureus (including those who are resistant to penicillin G), Staphylococcus epidermidis, -hemolytic streptococcus, Streptococcus green and Streptococcus pneumoniae. Good antibacterial effects on anaerobic bacteria include tetanus, corynebacterium diphtheria, and perfringens. Inactive against gram-negative bacteria such as enterococci, meningococci, Neisseria gonorrhoeae, and Haemophilus influenzae, as well as fungi. This product has no cross-resistance with penicillin, chloramphenicol, cephalosporins and tetracyclines, and it is partially cross-resistant with macrolides. This product acts on the 50S subunit of the ribosomes of sensitive bacteria, prevents the extension of the peptide chain, and thus inhibits the protein synthesis of bacterial cells. Generally, it is a bacteriostatic agent, but at high concentrations, it also has a bactericidal effect on some bacteria. This product's LD50 is given intravenously at 214 mg / kg in mice and 4000 mg / kg in oral; rats are given 4000 mg / kg in oral. This product is a white tablet or sugar-coated tablet; it appears white after removing the coating.

dynamics

Oral is not inactivated by gastric acid and can be absorbed from the gastrointestinal tract. Only 20% to 30% of it is absorbed on an empty stomach, and less absorbed after taking it. Adults take 0.5g on an empty stomach or after eating, reaching peak plasma concentrations (Cmax) 2 at 2 and 4 hours, respectively

Lincomycin side reaction case

Lincomycin, also known as jiemycin, can inhibit bacterial protein synthesis,

Occasional urticaria

Positive bacteria and some anaerobic bacteria have antibacterial effects. Because of its low price and no skin test, it is widely used in clinical applications, especially in small and medium-sized hospitals. It has become one of the most commonly used antibiotics. With the expansion of clinical application scope and people's emphasis on adverse drug reactions, In recent years, there have been increasing reports of adverse reactions to lincomycin, which should be paid attention to.

1. Gastrointestinal reactions Gastrointestinal reactions can occur either orally or by injection, and can be manifested as anorexia, nausea, vomiting, upset stomach, gastritis, glossitis, itching of the anus, and diarrhea. Diarrhea occurs more than 3-10 days after administration.

2. Liver damage It has been reported that high-dose medications can cause elevated aminotransferases and elevated bilirubin with pathological changes in the liver. Therefore, those with liver dysfunction should be used with caution.

3. Allergic reactions include drug rash, dermatitis, mucosal ulcers, angioedema, serum disease, and solar allergy. Sometimes it can also cause allergic asthma, eosinophilia, thrombocytopenic purpura and so on. There have even been reports of anaphylactic shock.

4. Cardiovascular response High-dose rapid intravenous injection can cause blood pressure drop, electrocardiogram changes, flushing and fever, etc., and even cause cardiac arrest. Therefore, this product can not be injected directly intravenously, it should be intravenously dripped after dilution. And the drip rate should be slow.

5. Others According to reports, lincomycin can also cause numbness, tinnitus, and dizziness in the mouth. Because lincomycin can enter the fetal circulation, pregnant women and lactating women should be used with caution. Newborn disabled. ^[2]

Lincomycin suppurative otitis media case

normal information

All patients were simple chronic suppurative otitis media with a total of 50 cases, including 27 males and 23 females. The maximum age is 70 years and the minimum is 1 year. Middle ear exudates were purulent or mucopurulent.

Methods and results

Treatment method Use a 20ml disposable sterile syringe, take 1ml (0.6g / 2ml) of lincomycin injection, and then draw 0.9% sodium chloride injection or 9ml of sterilized injection water to make it 3% lincomycin Solution. Ear drops, 3 to 4 times / day, continuous medication for 3 to 7 days.

Efficacy standard cure: After treatment, no purulent or mucus in the middle ear flows from the tympanic membrane perforation, and the external auditory canal is dry. Significant effect: The pus discharged from the middle ear is significantly less than that before treatment, but the ear is not dry. No significant reduction.

Results 39 cases (78%) were cured, and 11 cases (22%) were markedly effective. The total effective rate is 100%.

discuss

Lincomycin injection is effective against most Gram-positive bacteria and most anaerobic bacteria. The most common pathogenic bacteria of this disease are Staphylococcus aureus, Streptococcus and Pseudomonas aeruginosa, which are in line with the antibiotic range of lincomycin. The author used 3% lincomycin solution to treat chronic suppurative otitis media with satisfactory results and low price, which is suitable for grassroots and remote areas. ^[2]

Clinical analysis of lincomycin costal chondritis

clinical information

General Information This group of 49 cases, 7 males and 42 females, 33 cases aged 20-30 years, 16 cases over 30 years old, 5 cases with a course of 30 days.

Treatment method: 2.4 g of lincomycin was added to 250 ml of 0.9% physiological saline, once a day and the quiescent point. 7 days was a course of treatment.

The treatment results were cured: 39 cases (79.6%) of local pain disappeared after treatment; improvement: 8 cases (16.3%) of local pain reduced after treatment; ineffective: 2 cases (4.1%) had no significant change after treatment.

Typical cases

Patient, female, 33 years old, suffered from osteochondritis for 2 months. The second and third costal cartilage on the left side were significantly thickened and raised, and the surface was smooth. After oral painkillers, topical procaine closure, hot compress and other methods, the symptoms can be temporarily relieved, but they will soon recur and gradually worsen, which can cause local pain during dressing and seriously affect rest. After admission to the hospital for 3 days, the symptoms were alleviated. The symptoms disappeared after 1 week of treatment, and the thickened rib cartilage obviously recovered. No relapse occurred after stopping the treatment.

Expert discussion

Costal chondritis is characterized by single or multiple thickening of the costal cartilage, bulging accompanied by significant pain and tenderness. The second to fourth costal cartilage is more common, occurring in young people (67.3%), and more women (85.7%) . At present, the cause is not clear, and some patients have influenza osteomyelitis.

A case of lethal intravenous lincomycin

Case information

Male, 36 years old. She could not turn up for 2 days due to swelling of the foreskin. She went to the outpatient clinic of this hospital on April 11, 1998 and was diagnosed with foreskin. Previous history of sulfa allergy. 250 ml of 10% glucose injection was added with 1.2 g of lincomycin and 10 mg of dexamethasone intravenously. When about 100ml was instilled, the patient experienced a short chill phenomenon, which was not paid attention at that time, and continued the infusion for 45 minutes. When the patient was ready to get up and leave after the instillation, he suddenly fell to the ground, and then convulsed, and his heartbeat breathing stopped, that is, chest chest compressions, tracheal intubation, artificially assisted breathing, intravenous epinephrine, dexamethasone, etc., a total of 4 rescued Hours, heartbeat breathing did not recover.

Expert discussion

Lincomycin hydrochloride is a widely used antibiotic in clinical practice, and its side effects are mainly gastrointestinal reactions. A few can appear transient leukocytes and thrombocytopenia. There have been clinical reports of large-dose rapid intravenous infusion causing blood pressure drop. . The "new edition of pharmacology" (14th edition) stipulates that when intravenous administration of lincomycin, it should be diluted with more than 100ml of liquid for every 0.6 to 1.0g, and the infusion time should not be less than 1 hour. In this case, the drip was completed in 45 minutes. Whether the cause of death was related to the rapid drip infusion was worth discussing. In addition, whether the infusion of lincomycin and dexamethasone is reasonable is worthy of further discussion. The patient had chills and convulsions during the application of this drug, combined with a history of allergy to other drugs. The author believes that the cause of death is likely to be anaphylactic shock caused by lincomycin. Therefore, before using lincomycin in patients with a history of drug allergy, it is best to conduct an allergy test, pay attention to the drip rate, and observe closely to avoid similar phenomena. ^[2]