3. In the early 20th century, it is invented by the German chemist Paul
Ehrlich while working on selective toxicity .
Dapsone (diamino-diphenyl sulfone)
is a medication most commonly used
in combination with rifampicin and
clofazimine as multidrug therapy
(MDT) for the treatment of
Mycobacterium leprae infections (leprosy).
Official in IP,BP,USP.
6. 1. Absorption
It is completely absorbed after oral administration
2. Distribution
Approximately 70% bound to plasma protein. The main
metabolite, monoacetyl dapsone, is nearly 100% protein
bound.
7. After oral administration the drug is mainly
eliminated by kidney.20 percent is excreted
unchanged while 80 percent as derivatives.
Only minor amount is excreted in faeces .
Bile: 10% of an oral dose was found in the bile
Breast-milk: Dapsone is excreted in breast milk
8. Plasma concentration of Dapsone is reduced by Rafampicin.
Plasma concentration of both drugs may increase when
Dapsone given with Trimethoprim.
This medication may decrease the effectiveness of combination-
type birth control pills.
This can result in pregnancy.
11. DISEASE ADULT CHILDREN DAYS
Leprosy - Lepromatous 50-100 mg/day 6-10 mg/day 2-5 years
Leprosy - Tuberculoid 100 mg/day NA 6 months
Dermatitis Herpetiformis 50-300 mg/day NA Life long basis
Pneumocystis Pneumonia 100 mg/day 2 mg/kg/day 14-21 days
Pneumocystis Pneumonia 100 mg/day 2 mg/kg/day Life long basis
Prophylaxis
Toxoplasmosis - Prophylaxis 100 mg/day 2 mg/kg/day Life long basis
12. TRANSDERMAL DOSE
Administered transdermally
As a gel 5% topical acne medication
available in 3-, 30-, and 60-gram tubes.
In normal use, 0.5 grams should be administered
to the face per application twice a day.
13. Mild haemolytic anaemia (decreases with
use of Vit C or Vit E ).
Gastric intolerance-nausea & anorexia
Methaemoglobinaemia (treated with Cemitidine) , headache,
paresthesias, mental symptoms & drug fever
allergic rashes, fixed drug eruption, hypermelanosis,
phototoxicity& rarely exfoliative dermatitis, steven Jhonsen
syndrome.
Hepatitis & agranulocytosis
14. Uncommonly weakness of the feet and
hands muscles with dose greater then
100 mg/day
It is tested by ability to walk on toes tip and to test
Hand grip.
Leucopenia presents with fever ,sore throat ,skin infections
and other common infections.
Bluish discoloration of lips and finger tips
Dapsone reaction/sulfone syndrome
15. Hypersensitivity
more frequent in patients receiving multiple-drug therapy.
The reaction involves a rash and may also include
fever, jaundice, and eosinophilia.
Swollen lymph glands and internal organ failure (Liver
, Lungs , Heart and Kidney).
In general, these symptoms will occur within the first six
weeks of therapy or not at all, and may be treated by
corticosteroid therapy.