Coxerin

Cycloserine (cycloserine) instructions
Common name: cycloserine
Trade name: Seromycin
All names: cycloserine, cycloserine, seromycin, Coxerin

Indications:
For the treatment of active tuberculosis that is sensitive to this drug, but it needs to be used in conjunction with other effective anti-tuberculosis drugs. Because it may cause severe mental confusion, its clinical application is somewhat limited.

Usage and dosage:
. Adults take 0.5-1g per day, divided into 2 times. In the first 2 weeks, 0.25g each time, 2 times a day, the maximum dose is 1g per day.
Children take 5 to 20 mg/kg per day, divided into 2 to 4 times, half the amount for the first dose.

Adverse reactions:
Frequency undefined
Cardiovascular: arrhythmia, heart failure
Central nervous system: coma, confusion, dizziness, drowsiness, dysarthria, headache, hyperreflexia, mild paralysis, paresthesia, psychosis, agitation, epilepsy, vertigo.
Dermatology: Rash
Endocrine Metabolism: Cyanocobalamin deficiency, folate deficiency
Liver: Elevated liver enzymes
Allergy: Hypersensitivity
Neuromuscular and skeletal: Tremor

Contraindications:
Allergy to cycloserine or any component of the preparation.
Contraindicated for people with epilepsy, depression, severe anxiety or mental illness.
Contraindicated in patients with severe renal insufficiency.
Disabled for those who like to drink.

Precautions:
Central Nervous System Effects: Dose-related central nervous system toxicity, including seizures, psychosis, depression, and confusion; if occurs, reduce dose or discontinue use. Vitamin B6 can be administered in combination to prevent or treat central nervous system effects.
Skin Reactions: Allergic dermatitis may occur; if allergic dermatitis occurs, reduce dose or discontinue use.
Superinfections: Long-term use may result in fungal or bacterial superinfections, including Clostridium difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD is observed more than 2 months after antibiotic treatment.
Alcoholism: Use with caution in patients with a history of chronic alcoholism; increased risk of seizures.
Psychiatric Illness: Use with caution in patients with depression, severe anxiety, or psychosis.
Renal Impairment: Use with caution in patients with renal impairment; dose adjustment may be necessary. It is prohibited to use in patients with severe renal insufficiency.
Drug-Drug Interactions: Significant interactions may exist that may require dose or frequency adjustment, additional monitoring, or the selection of alternative therapies.
Patients who may be vitamin deficient: Use with caution in patients who may be deficient in vitamin B12 or folic acid (malnutrition, chronic anticonvulsant therapy, or the elderly).

Storage:
Sealed and placed in a cool place.

Mechanism of action:
This product is a second-line anti-tuberculosis drug that can inhibit the growth of Mycobacterium tuberculosis, but its effect is weaker than that of first-line drugs and its efficacy against tuberculosis is also lower. It can produce drug resistance when used alone, but drug resistance occurs more slowly than other anti-tuberculosis drugs, and there is no cross-resistance with other anti-tuberculosis drugs. Its antibacterial mechanism is to inhibit the synthesis of bacterial cell wall mucopeptides, thereby causing cell wall defects. The main structural component of the bacterial cell wall is cell wall mucopeptide, which is composed of N-acetylglucosamine (GNAc) and N-acetylmuramic acid (MNAc) linked to a pentapeptide. The formation of mucin precursors in the cytoplasm can be hindered by cycloserine, which can hinder the formation of N-acetylmuramic acid pentapeptide by inhibiting D-alanine racemase and synthase. It is absorbed quickly after oral administration and reaches blood concentration within 3-4 hours, and is widely distributed into body tissues and body fluids. The concentration of the drug in the cerebrospinal fluid is similar to that in the blood. Most of it is excreted unchanged in the urine, and about 35% is metabolized. The minimum inhibitory concentration is 25mg/L.

Safety and efficacy:
Clinical experiments have proven that the combination of cycloserine, isoniazid and rifampicin can improve patient survival rate. The efficacy of second-line drugs is relatively weak, and the treatment time is usually more than 2 years. 2033 sputum specimens (6099) from India were reviewed from 1991 to 1995. Of these, 521 (25.6%) patients (335 males and 186 females; aged 11 to 75 years) had positive sputum cultures and susceptibility to acid-fast bacilli (AFB) responses. Study on drug resistance patterns Formula: isoniazid 15%, rifampicin 66.8%, pyrazinamide 72.2%, ethambutol 8.4%, streptomycin 53.6%, cycloserine 39.2%, streptomycin 25.1% and ethionamide 65.3%. In 1998, the tuberculosis research department in India reported more than 200 cases of patients with isoniazid and rifampicin. Resistance to fupin and streptomycin was 72%, 49% and 37% respectively, while resistance to cycloserine and ethionamide was only 1%. Clinical experience has proven that chemotherapy for pediatric tuberculosis is effective.
In 2006, a tuberculosis research department in Osaka, Japan reported that second-line drugs cycloserine, ethambutol, pyrazinamide, etc. used by pregnant women were effective in treating multidrug-resistant tuberculosis (MDR-TB), and the newborn babies were healthy. In 2006, a hospital in the Spanish capital used levofloxacin and cycloserine to treat 17 non-HIV-infected multi-drug-resistant tuberculosis patients (68%) after 24 months of follow-up treatment. Cured, no recurrence or death occurred. Iran's Tuberculosis and Infectious Diseases Research Department reported in 2005 that the use of cycloserine in the treatment of MDR-TB can achieve a curative effect.
From May 2014 to April 2015, 48 patients with MDR-TB (Multi-drug-resistant tuberculosis) diagnosed in the tuberculosis prevention clinic and included in the treatment of the Global Fund's Multi-Drug-Resistant Tuberculosis Prevention and Treatment Project were selected as research subjects. They were randomly divided into the experimental group (n=24) and the control group (n=24). Both groups of patients received the WHO standard MDR-TB treatment regimen. The experimental group added cycloserine on this basis. The efficacy and drug differences of the two groups of patients during different treatment periods were observed. Good reaction. The results at the end of 24 months of treatment showed that the sputum bacterial negative conversion rates in the experimental group and the observation group were 87.5% and 62.5% respectively, and the lesion absorption improvement rates were 87.5% and 62.5% respectively. The difference between the two groups was statistically significant (all P<0.05); the incidence of central nervous system disease in the experimental group was higher than that in the observation group, and the incidence of drug-induced liver injury in the observation group was higher than that in the experimental group, and the differences were statistically significant (all P<0.05). Cycloserine combined with other anti-tuberculosis drugs in the treatment of multi-drug-resistant pulmonary tuberculosis can accelerate the conversion of acid-fast staining of sputum tuberculosis bacteria to negative, promote the absorption of lesions, and has no serious adverse reactions. It is safe and tolerable and deserves to be promoted.