Cycloserine

Drug #1444

Cycloserine is a second-line, broad-spectrum antibiotic, produced by Streptococcus orchidaceus. In 1955, it was first isolated from a fermentation brew and was later synthesized. Cycloserine is used in the treatment of active pulmonary and extrapulmonary tuberculosis (TB), when primary agents have failed (such as INH, rifampin, streptomycin etc). When Cycloserine is employed to treat tuberculosis, it must be given together with other effective agents. Cycloserine is given orally. It was approved by the FDA in 1956.

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Primary Characteristics

It is of Natural/Synthetic origin and belongs to Aminoisoxazolidin.

Molecular Weight: 102.1 · pK_a: 4.4, 7.4 · Solubility in Water: 1 in 10 · Solubility in Alcohol: 1 in 50 · Non-proprietary name: Cycloserine.

Pharmacokinetics

Absorption: Cycloserine has an oral bioavailability is 50% (±50%), pre-systemic (first-pass) metabolism accounts for 5% (±5%).

Distribution: Cycloserine has a plasma protein binding is < 20%.

Elimination: it is metabolised via hepatic, plasma half-life is 10 hr, renal excretion is 50-70% (unchanged).

Indications

Cycloserine is primarily indicated in conditions like Mycobacterial infection, Pophylaxis of acute renal transplant rejection, Tuberculosis.

Cycloserine is also indicated for secondary conditions like Minor surgical and medical procedures.

Contraindications

Cycloserine is contraindicated in conditions like Epilepsy, Renal failure, Mental illness, Hypersensitivity.

Dosage

Cycloserine's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
0.75 g	0.75 g	—	PO	for divided doses.
250 mg	250 mg	Every 12h	PO	for two weeks.
Paediatric Dosage (20kg)
7.5 mg/kg	7.5 mg/kg	Every 12h		to maximum dose of 1g daily.
Neonatal Dosage (3kg)
No data.

Drug Interactions

2 interactions

Minor1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Cycloserine in overdosage may give rise to further complications which include Congestive heart failure , Psychiatric disturbances , Megaloblastic anemia, Excitement .

Cycloserine produces potentially life-threatening effects which include Convulsions , Nervous system manifestation. Careful monitoring is needed with proper medical management.

Cycloserine is known to cause more or less tolerable side effects which are usually transient. These include Aggression, Anxiety, Cardiac arrhythmias , Confusion, Depression, Disorientation, Drowsiness, Fever, Headache, Hyper-reflexia, Irritability, Nausea, Peripheral neuropathy, Photosensitivity, Rashes , Suicidal tendencies, Tremor, Vertigo.

Warnings / Precautions

It has a low therapeutic index and its dosage should be adjusted according to plasma concentration which should be monitored atleast weekly in patinet with renal impairment and in patients showing sings of neurological toxicity. Patients with renal impairment require lower doses.

Available Brands

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Single Ingredient

Caps

250 mg

Storage Conditions

Cycloserine should be stored Caps.

Drug Classification

1.6.2.4 — Anti-tuberculosis drugs

Manufacturers

Manufacturers of Cycloserine in Pakistan:

Century Hoffman Shrooq