Cycloserine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Second line drug in tuberculosis
Adult: In combination with other anti-TB agents for the treatment of pulmonary and extrapulmonary TB: Initially, 250 mg 12 hourly for the 1st 2 weeks, followed by 500-1,000 mg daily in equally divided doses. Adjust dose based on blood concentration and response. Max: 1,000 mg daily.
Child: In combination with other anti-TB agents for the treatment of pulmonary and extrapulmonary TB: Initially, 10 mg/kg daily. Adjust dose based on blood concentration and therapeutic response. Max: 1,000 mg daily. Dosage and treatment recommendations may vary among countries and individual products (refer to latest local or specific product guidelines).

Oral
Urinary tract infection
Adult: Usual dose: 250 mg 12 hourly for 2 weeks. Use must only be considered when the organism has been demonstrated to be susceptible and when more conventional therapy has failed. Dosage and treatment recommendations may vary among countries and individual products (refer to latest local or specific product guidelines).
Suy thận
Mild to moderate: Dose reduction may be needed. Severe: Contraindicated.
Cách dùng
May be taken with or without food. May be taken after meals if GI discomfort occurs.
Chống chỉ định
Hypersensitivity. Epilepsy, mental depression, severe anxiety, psychosis, alcohol abuse or alcoholism. Severe renal impairment.
Thận trọng
Patient with porphyria, history of chronic alcoholism; potential vitamin B12 and/or folate deficiency (e.g. malnutrition, chronic use of antiseizure medications). Patient receiving >500 mg daily dose. Mild to moderate renal impairment. Children and elderly. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Vitamin B12 or folate deficiency, megaloblastic anaemia, sideroblastic anaemia; exacerbations of porphyria, allergic dermatitis, CNS toxicity (e.g. psychoses possibly with suicidal tendencies; depression, somnolence, confusion, hyperreflexia, headache, tremor, vertigo, paresis, dysarthria, seizures). Rarely, heart failure (in patients receiving daily dose of 1,000-1,500 mg); hypersensitivity reactions (including rash and photosensitivity).
Investigations: Increased serum aminotransferases.
Nervous system disorders: Disorientation with loss of memory; paraesthesia, dizziness, coma.
Psychiatric disorders: Personality changes, hyperirritability, aggression.
Chỉ số theo dõi
Perform culture and susceptibility tests; consult local institutional recommendations before treatment initiation due to antibiotic resistance risks. Monitor plasma cycloserine concentrations (at least weekly for patients with renal impairment, taking doses >500 mg daily, or with signs and symptoms of neurotoxicity); renal, hepatic, and haematological functions periodically. Evaluate neuropsychiatric status every month or more frequently if symptoms occur.
Quá liều
Symptoms: Headache, vertigo, confusion, drowsiness, hyperirritability, paraesthesias, dysarthria, and psychosis; in larger doses, paresis, convulsions, and coma may occur. Management: Symptomatic and supportive treatment. Airway of the patient must be protected and ventilation and perfusion supported. Monitor vital signs, serum electrolytes, and blood gases and maintain them within acceptable limits. Activated charcoal may be more effective than emesis or gastric lavage in reducing absorption. May give 200-300 mg of pyridoxine daily to treat and prevent neurotoxic events in adults. Haemodialysis may remove the drug from the bloodstream but must be reserved for life-threatening toxicity which is unresponsive to less invasive treatment.
Tương tác
Increased neurotoxic side effects with ethionamide. Enhanced CNS toxicity (e.g. dizziness, drowsiness) with isoniazid.
Tương tác với thức ăn
Increased risk of seizures with alcohol.
Tác dụng
Description:
Mechanism of Action: Cycloserine is a broad-spectrum antibiotic that inhibits cell wall synthesis in susceptible bacteria by competing with the amino acid, D-alanine, for incorporation into the bacterial cell wall. It may be bacteriostatic or bactericidal in action depending on the drug concentration at the site of infection and susceptibility of the organism.
Pharmacokinetics:
Absorption: Readily and almost completely absorbed from the gastrointestinal tract. Time to peak plasma concentration: 3-4 hours.
Distribution: Widely distributed into body tissues and fluids, including the CSF, lungs, bile, sputum, lymph tissue, and ascitic, pleural, or synovial fluids. Crosses the placenta and enters breast milk.
Metabolism: Metabolised in the liver.
Excretion: Via urine (approx 65% as unchanged drug within 72 hours); faeces (small amounts). Elimination half-life: 12 hours.
Đặc tính

Chemical Structure Image
Cycloserine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6234, Cycloserine. https://pubchem.ncbi.nlm.nih.gov/compound/Cycloserine. Accessed Oct. 26, 2023.

Bảo quản
Store between 20-25°C.
Phân loại MIMS
Thuốc kháng lao
Phân loại ATC
J04AB01 - cycloserine ; Belongs to the class of antibiotics. Used in the systemic treatment of tuberculosis.
Tài liệu tham khảo
Anon. Cycloserine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 27/07/2023.

Anon. Cycloserine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/07/2023.

Buckingham R (ed). Cycloserine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/07/2023.

Coxerin Capsules 250 mg (Zulat Pharmacy Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 27/07/2023.

Cycloserine 250 mg Hard Capsules (Neon Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 27/07/2023.

Cycloserine Capsule (Dr. Reddy's Laboratories, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 27/07/2023.

Cycloserine. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 28/09/2023.

Joint Formulary Committee. Cycloserine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/07/2023.

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