This slides are prepared for undergraduate medical (MBBS) class for teaching pharmacology. Materials for slides are taken from Essentials of Pharmacology, KD Tripathi 7th ed, Medical Pharmacology, SK Shrivastav and Sharma & Sharma. Pictures are obtained from google.
6. Dapsone
Oldest, Cheapest and Most Effective
Diamino diphenyl Sulfone (DDS)
Inhibit conversion of PABA to folic acid – Leprostatic
Spectrum same as sulfonamides but
Effective against M.leprae at lower doses
Resistance may develop if used as monotherapy
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7. Dapsone: Pharmacokinetics
Complete and Rapid absorption
Peak Conc. In 5 hours and t1/2 24 hours
Wide Distribution, Concentrated in Skin, Muscle, Liver and
Kidney
Metabolized by Acetylation
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10. Rifampicin
Antitubercular, Potent Cidal drug for M.leprae
Rapidly renders leprosy patient non contagious
99.99% bacilli killed with in 3-7 days, Lesions start regressing in 2 months
Used in Multidrug therapy
Shortens duration of treatment
600mg monthly dose given
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11. Clofazimine
Dye with Leprostatic and anti-inflammatory property
Acts by interference with template function of DNA
Alteration of membrane structure and transport function
Disrupts mitochondrial electron transport chain
M.leprae resistant to Dapsone respond to Clofazimine
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13. Adverse Effects
• Reddish Black Discoloration of skin, Hair and body secretions
• Dryness of skin and itching, Acneform eruptions, Photo toxicity
• Conjunctival pigmentation
• Nausea, anorexia, abdominal pain, weight loss.
• Avoid in pregnancy and renal and liver disease
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14. Ofloxacin
FQ are highly active against M.leprae
Hasten Bacteriological and clinical response
Used in alternate regimens instead of rifampicin
Reduces duration of treatment
Reduces chances of development of resistance
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15. Minocycline
High lipophilicity helps to penetrate M.leprae
Efficacy in-between clarithromycin and rifampicin
Rapid relief from lepromatous symptoms
Vertigo on long term use
Used in alternate regimes
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19. NLEP Classification
Paucibacillary
1-5 skin lesions
No/one nerve
involvement
Skin smear negative
TT and BT
Multibacillary
6 or more lesions
>1 nerve involvement
Skin smear positive
LL, BL and BB
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20. MultidrugTherapy of Leprosy (MDT)
Effective in cases with primary Dapsone resistance
Prevent emergence of resistance
Quick symptomatic relief, Make patient noncontagious
Reduces total duration of therapy
Highly effective with reduced relapse and good patient compliance
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21. Multibacillary Leprosy
Rifampicin – 600mg once a month Supervised
Dapsone – 100 mg daily self administered
Clofazimine – 300 mg once a month supervised 50 mg daily self
administered
Duration – 12 months
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23. Alternative regimen
Intermittent ROM : Rifampicin 600 mg + Ofloxacin 400 mg+
Minocycline 100 mg once a month. PBL – 3-6 months, MBL- 12-
24 months.
Clofazimine 50mg+ 2 of O/M/Clar for 6 months f/b Clo+ O.M for
18 months
If Clofazimine is not tolerated than substitute with O or M in
standard MDT
Intermittent RMMx – Moxi 400mg+ Mino 200 mg+ Rifampicin
600 mg once a month. PBL – 6 months . MBL – 12 months
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24. Reactions in Leprosy
Reversal reaction
Seen inTT and BL due to delayed hypersensitivity to antigen of M.leprae
Cutaneous ulceration, Multiple nerve involvement with Swollen, painful
and tender nerves.
Prednisolone – 4-60mg daily till reaction subside and tapered gradually
Clofazimine is effective
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25. Lepra reaction type 2 ( Erythema
nodosum leprosum)
Occur in LL Arthus type of reaction (JH reaction)
Mild , severe or life threatening
Existing lesions enlarges, become red, swollen and painful.
Malaise, fever and other constitutional symptoms
Appearance of newer lesions
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26. Lepra reaction
Temporary discontinuation of Dapsone in severe cases
Clofazimine 200 mg
Prednisolone 40-60 mg/day
Thalidomide – 100-300 mg OD alternate to prednisolone
Chloroquine
Analgesics, antipyretics and antibiotics
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