Flexyx

Flexyx drugs: Lamprene

Lamprene - General Information:

A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Lamprene also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619)

Pharmacology:

Lamprene exerts a slow bactericidal effect on Mycobacterium leprae (Hansen's bacillus). Lamprene inhibits mycobacterial growth and binds preferentially to mycobacterial DNA. Lamprene also exerts antiinflammatory properties in controlling erythema nodosum leprosum reactions. Lamprene is highly lipophilic and tends to be deposited predominantly in fatty tissue and in cells of the reticuloendothelial system. It is taken up by macrophages throughout the body. Measurement of the minimum inhibitory concentration (MIC) of clofazimine against leprosy bacilli in vitro is not yet feasible. In the mouse footpad system, the multiplication of M.leprae is inhibited by introducing 0.0001%- 0.001% clofazimine in the diet. Although bacterial killing may begin shortly after starting the drug, it cannot be measured in biopsy tissues taken from patients for mouse footpad studies until approximately 50 days after the start of therapy.

Lamprene for patients

Patients should be warned that Lamprene may cause a discoloration of the skin from red to brownish-black, as well as discoloration of the conjunctivae, lacrimal fluid, sweat, sputum, urine, and feces. Patients should be advised that skin discoloration, although reversible, may take several months or years to disappear after the conclusion of therapy with Lamprene.

Patients should be told to take Lamprene with meals.

Lamprene Interactions

Preliminary data which suggest that dapsone may inhibit the anti-inflammatory activity of Lamprene have not been confirmed. If leprosy-associated inflammatory reactions develop in patients being treated with dapsone and clofazimine, it is still advisable to continue treatment with both drugs.

Lamprene Contraindications

There are no known contraindications.

Additional information about Lamprene

Lamprene Indication: For the treatment of lepromatous leprosy, including dapsone-resistant lepromatous leprosy and lepromatous leprosy complicated by erythema nodosum leprosum.
Mechanism Of Action: Appears to preferentially bind to mycobacterial DNA leading to disruption of the cell cycle and eventually kills the bacterium. It may also bind to bacterial potassium transporters, thereby inhibiting their function. Lysophospholipids have been found to mediate the activity of this drug.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Clofazimine
Synonyms: Clofazimina [INN-Spanish]; Chlofazimine; Clofaziminum [INN-Latin]
Drug Category: Antimycobacterials; Leprostatic Agents; Dyes; Anti-Inflammatory Agents, Non-Steroidal
Drug Type: Small Molecule; Approved
Other Brand Names containing Clofazimine: Lampren; Lamprene;
Absorption: Absorption varies from 45 to 62% following oral administration in leprosy patients. Bioavailability is approximately 70%. Food increases bioavailability and rate of absorption.
Toxicity (Overdose): Oral, rabbit: LD₅₀ = 3.3 g/kg; Oral, mouse: LD₅₀ = > 4 g/kg. Severe abdominal symptoms have necessitated exploratory laparotomies in some patients on clofazimine therapy. Rare reports have included splenic infarction, bowel obstruction, and gastrointestinal bleeding. Deaths have been reported, following severe abdominal symptoms.
Protein Binding: Not Available
Biotransformation: Hepatic. Three metabolites have been identified - two conjugated and one unconjugated, however, it is not yet known whether these metabolites are pharmacologically active. Metabolite I is formed by hydrolytic dehalogenation of clofazimine, metabolite II presumably is formed by a hydrolytic deamination reaction followed by glucuronidation, and metabolite III appears to be a hydrated clofazimine glucuronide.
Half Life: 10 days following a single dose, 70 days after long-term, high-dose therapy.
Dosage Forms of Lamprene: Capsule Oral
Chemical IUPAC Name: N,5-bis(4-chlorophenyl)-3-propan-2-yliminophenazin-2-amine
Chemical Formula: C27H22Cl2N4
Clofazimine on Wikipedia: http://en.wikipedia.org/wiki/Clofazimine
Organisms Affected: Mycobacteria