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Dapsone

Most commonly used in combination with rifampicin and clofazimine as multidrug therapy for the treatment of Mycobacterium leprae infections.

A second-line treatment for prophylaxis against Pneumocystis pneumonia caused by Pneumocystis jiroveci in HIV patients in whom CD4 counts are below 200/mm3.

It is an antibiotic and an anti-inflammatory agent.

Dapsone is thought to cause inhibition of myeloperoxidase, thereby leading to an anti-inflammatory and immunomodulatory effect.

Dapsone is associated with hemolysis, methemoglobinemia, agranulocytosis, hepatitis, and dapsone hypersensitivity syndrome.

Its use is contraindicated in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency, since it can lead to severe hemolysis.

Serum G6PD measurement, a complete blood cell count, a reticulocyte count, and liver function tests are recommended prior to dapsone initiation and, with the exception of G6PD level, at various intervals during treatment.

Can be used alone or in combination for the prevention and treatment of infections including leprosy, malaria, actinomycetoma, Pneumocystis jiroveci pneumonia in patients with HIV infection and chronic inflammatory disease characterized by infiltration of neutrophils and eosinophils such as dermatitis herpetiformis, and IgA dermatitis.

First line treatment for Linear IgA dermatosis.

It is also used in combination with pyrimethamine in the treatment of malaria.

Available as a gel 5% topical acne medication and is used as an acne treatment for mild to moderate acne in teens and adults.

Orally it may be prescribed for extremely severe acne, if conventional treatments fail.

Half-life 20 to 30 hours.

Undergoes acetylation in the liver.

Inhibits bacterial synthesis of dihydrofolic acid, via competition with para-aminobenzoate for the active site of dihydropteroate synthetase.

Mechanism of action in skin conditions in which bacteria do not have a role is not understood.

Has anti-inflammatory and immunomodulatory effects.

Is an anti-mycobacterial drug that can be used as an alternative to trimethoprim-sulfamethoxazole in primary or secondary prophylaxis of Pneomocystis in immunosuppressed patients.

Blocks myeloperoxidase, which is the probable mechanism of action in treating dermatitis herpetiformis.

Reversibly inhibits myeloperoxidase activity by promoting the formation of an inactive intermediate of the enzyme, thus preventing the conversion of hydrogen peroxide to hypochlorous acid, an extremely potent neutrophil oxidant.

Myeloperoxidase inhibition may be the mechanism for a neuron-sparing effect in inflammatory neurodegenerative diseases such as Alzheimer disease and stroke.

Does not block cyclo-oxygenase.

Indications include leprosy, pemphigoid, an autoimmune blistering disease of skin and mucous membranes, dermatitis herpetiformis, immunoglobulin A dermatosis, as well as other skin conditions including lichen planus.

Has been used to treat ITP, Brown recluse spider bites.

Administration is administered orally as a 100 mg tablet or alternatively as 25 mg tablets.

Can be administered transdermally as a gel 5% topical acne medication.

Side effects include dose-related hemolysis and methemoglobinemia.

Approximately 20% of patients on dapsone have hemolysis.

Hemolysis more common and severe in patients with glucose-6-phosphate dehydrogenase deficiency.

Patients should be screened for G6PD deficiency before treatment.

Agranulocytosis may occur rarely, as may aplastic anemia.

Can inhibit the Cytochrome P450 system.

HLA-B13:01 is associated with the development of dapsone hypersensitivity syndrome among patients with leprosy.

About 0.5-3.6% have drug hypersensitivity syndrome, characterized by fever, rash and systemic abnormalities involving the hematologic and hepatic systems.

Dapsone hypersensitive syndrome manifests 4 to 6 weeks after the initiation of therapy.

In a Chinese population the incidence rate and mortality of the dapsone hypersensitive syndrome is 1% and 11.1% respectively.

Other adverse effects include nausea, headache, rash, insomnia, psychosis, and peripheral neuropathy.

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