dapsone

PRODUCT OVERVIEW
KEY FACTS
Dapsone is a sulfone for the primary treatment of Dermatitis herpetiformis andan antibacterial drug for susceptible cases of leprosy dapsone.

MAJOR USES
Dapsone is used to control the dermatologic symptoms of Dermatitis herpetiformis dapsone. Dapsone is used alone or in combination with other anti-leprosy drugs for leprosy dapsone.

SAFETY INFORMATION
Dapsone is contraindicated in patients with Dapsone hypersensitivity dapsone. Completeblood counts and laboratory monitoring should be done frequently dapsone. See labeling dapsone.

PRODUCT INFORMATION
DAPSONE TABLETS USP Rx
[ dap 'soce ]

25 mg dapsone. & 100 mg dapsone.
DESCRIPTION
Dapsone-USP, 4,4'-diaminodiphenylsulfone (DDS) is a primary treatment for Dermatitisherpetiformis dapsone. It is an antibacterial drug for susceptible cases of leprosy dapsone. It is a white, odorless crystalline powder, practically insoluble in water andinsoluble in fixed and vegetable oils dapsone.

Dapsone is issued on prescription in tablets of 25 and 100 mg dapsone. for oral use dapsone.

Inactive Ingredients: Colloidal silicone dioxide, magnesium stearate, microcrystallinecellulose, and corn starch dapsone.

CLINICAL PHARMACOLOGY
Actions: The mechanism of action in Dermatitis herpetiformis has not been established dapsone. By the kinetic method in mice, Dapsone is bactericidal as well as bacteriostaticagainst Mycobacterium leprae dapsone.

Absorption and Excretion: Dapsone, when given orally, is rapidly and almostcompletely absorbed dapsone. About 85 percent of the daily intake is recoverable fromthe urine mainly in the form of water-soluble metabolites dapsone. Excretion of thedrug is slow and a constant blood level can be maintained with the usual dosage dapsone.

Blood Levels: Detected a few minutes after ingestion, the drug reaches peakconcentration in 4-8 hours dapsone. Daily administration for at least eight days isnecessary to achieve a plateau level dapsone. With doses of 200 mg dapsone. daily, this levelaveraged 2.3 µg/ml with a range of 0.1-7.0 µg/ml dapsone. The half-lifein the plasma in different individuals varies from ten hours to fifty hoursand averages twenty-eight hours dapsone. Repeat tests in the same individual are constant dapsone. Daily administration (50-100 mg.) in leprosy patients will provide blood levelsin excess of the usual minimum inhibitory concentration even for patients witha short Dapsone half-life dapsone.

INDICATIONS AND USAGE
Dermatitis herpetiformis: (D.H.)

Leprosy: All forms of leprosy except for cases of proven Dapsone resistance dapsone.

CONTRAINDICATION
Hypersensitivity to Dapsone and/or its derivatives dapsone.

WARNINGS
The patient should be warned to respond to the presence of clinical signs suchas sore throat, fever, pallor, purpura or jaundice dapsone. Deaths associated with theadministration of Dapsone have been reported from agranulocytosis, aplasticanemia and other blood dyscrasias dapsone. Complete blood counts should be done frequentlyin patients receiving Dapsone dapsone. The FDA Dermatology Advisory Committee recommendedthat, when feasible counts should be done weekly for the first month, monthlyfor six months and semi-annually thereafter dapsone. If a significant reduction in leucocytes,platelets or hemopoiesis is noted, Dapsone should be discontinued and the patientfollowed intensively dapsone. Folic acid antagonists have similar effects and may increasethe incidence of hematologic reactions; if co-administered with Dapsone thepatient should be monitored more frequently dapsone. Patients on weekly Pyrimethamineand Dapsone have developed agranulocytosis during the second and third monthof therapy dapsone.

Severe anemia should be treated prior to initiation of therapy and hemoglobinmonitored dapsone. Hemolysis and methemoglobin may be poorly tolerated by patients withsevere cardio-pulmonary disease dapsone.

Cutaneous reactions, especially bullous, include exfoliative dermatitis andare probably one of the most serious, though rare, complications of sulfonetherapy dapsone. They are directly due to drug sensitization dapsone. Such reactions includetoxic erythema, erythema multiforme, toxic epidermal necrolysis, morbilliformand scarlatiniform reactions, urticaria and erythema nodosum dapsone. If new or toxicdermatologic reactions occur, sulfone therapy must be promptly discontinuedand appropriate therapy instituted dapsone.

Leprosy reactional states, including cutaneous, are not hypersensitivity reactionsto Dapsone and do not require discontinuation dapsone. See special section dapsone.

PRECAUTIONS
General: Hemolysis and Heinz body formation may be exaggerated in individualswith a glucose-6-phosphate dehydrogenase (G6PD) deficiency, or methemoglobinreductase deficiency, or hemoglobin M dapsone. This reaction is frequently dose-related dapsone. Dapsone should be given with caution to these patients or if the patient isexposed to other agents or conditions such as infection or diabetic ketosiscapable of producing hemolysis dapsone. Drugs or chemicals which have produced significanthemolysis in G6PD or methemoglobin reductase deficient patients include Dapsone,sulfanilamide, nitrite, aniline, phenylhydrazine, napthalene, niridazole, nitrofurantoinand 8-amino-antimalarials such as primaquine dapsone.

Toxic hepatitis and cholestatic jaundice have been reported early in therapy dapsone. Hyperbilirubinemia may occur more often in G6PD deficient patients dapsone. When feasible,baseline and subsequent monitoring of liver function is recommended dapsone. If abnormal,Dapsone should be discontinued until the source of the abnormality is established dapsone.

Drug Interactions: Rifampin lowers Dapsone levels 7 to 10-fold by acceleratingplasma clearance; in leprosy this reduction has not required a change in dosage dapsone.

Folic acid antagonists such as pyrimethamine may increase the likelihood ofhematologic reactions dapsone.

A modest interaction has been reported for patients receiving 100 mg Dapsoneod in combination with trimethoprim 5 mg/kg q6h dapsone. On Day 7, the serum Dapsonelevels averaged 2.1 ± 1.0 µg/mL in comparison to 1.5 ± 0.5µg/mL for Dapsone alone dapsone. On Day 7, trimethoprim levels averaged 18.4 ±5.2 µg/mL in comparison to 12.4 ± 4.5 µg/mL for patientsnot receiving Dapsone dapsone. Thus, there is a mutual interaction between Dapsone andtrimethoprim in which each raises the level of the other about 1.5 times dapsone.

Carcinogenesis, mutagenesis: Dapsone has been found carcinogenic (sarcomagenic)for male rats and female mice causing mesenchymal tumors in the spleen and peritoneum,and thyroid carcinoma in female rats dapsone. Dapsone is not mutagenic with or withoutmicrosomal activation in S dapsone. typhimurium tester strains 1535, 1537, 1538, 98,or 100 dapsone.

Pregnancy Category C: Animal reproduction studies have not been conducted withDapsone dapsone. Extensive, but uncontrolled experience and two published surveys onthe use of Dapsone in pregnant women have not shown that Dapsone increases therisk of fetal abnormalities if administered during all trimesters of pregnancyor can affect reproduction capacity dapsone. Because of the lack of animal studies orcontrolled human experience, Dapsone should be given to a pregnant woman onlyif clearly needed dapsone. In general, for leprosy, USPHS at Carville recommends maintenanceof Dapsone dapsone. Dapsone has been important for the management of some pregnant D.H dapsone. patients dapsone.

Nursing Mothers: Dapsone is excreted in breast milk in substantial amounts dapsone. Hemolytic reactions can occur in neonates dapsone. See section on hemolysis dapsone. Becauseof the potential for tumorgenicity shown for Dapsone in animal studies a decisionshould be made whether to discontinue nursing or discontinue the drug takinginto account the importance of the drug to the mother dapsone.

Pediatric Use: Children are treated on the same schedule as adults but withcorrespondingly smaller doses dapsone. Dapsone is generally not considered to have aneffect on the later growth, development and functional development of the child.

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