LEPROSY AND LEPROTIC DRUG

CLASSIFICATION
BY SHIKHAR SRIVASTAVA

BATCH 2K19
RDASMC AYODHYA
INTRODUCTION
• LEPROSY IS A CHRONIC INFECTIOUS DISEASE CAUSED BY SLOW GROWING
TYPE OF BACTERIA CALLED MYCOBACTERIUM LEPRAE.
• ALSO KNOWN AS HENSON’S DISEASE AFTER THE NAME OF THE SCIENTIST
WHO DISCOVERED M. LEPRAE IN 1873.
• IT PRIMARILY AFFECTS THE SKIN AND THE PERIPHERAL NERVES.
• IT HAS LONG INCUBATION PERIOD OF 3-5 YEARS.
TYPES OF LEPROSY
• WHO DIVIDED LEPROSY INTO
PAUCIBACILLARY LEPROSY-
- IN THIS CASE THE PATIENT HAVE 1-5 SKIN LESIONS.
- NO NERVE OR ONLY ONE NERVE INVOLVEMENT.
- SKIN SMEAR –VE AT ALL SITES .

MULTIBACILLARY LEPROSY-
- IN THIS CASE THE PATIENT HAVE 6 OR MORE SKIN LESIONS.
- MORE THAN ONE NERVE INVOLVEMENT IRRESPECTIVE OF NO. OF SKIN LESIONS.
- SKIN SMEAR POSITIVE AT ONE SITE.
CLASSIFICATION OF ANTILEPROTIC DRUGS
DAPSONE
- IT IS DIAMINO DIPHENYL SULFONE.
- IT IS SIMPLEST OLDEST & CHEAPEST DRUG OF ITS CLASS.

MODE OF ACTION-
- PRODUCES LEPROSTATIC ACTION EVEN AT LOW CONCENTRATION.
- CHEMICALLY RELATED TO SULPHONAMIDES AS IT PRODUCES SAME MECHANISM FOR THE INHIBITION
OF PABA INCORPORATION INTO FOLIC ACID BY FOLATE SYNTHASE.
- ITS SPECIFICITY FOR M. LEPRAE MAY BE DUE TO DIFFERENCE IN THE FOLATE SYNTHASE ENZYME.
- DAPSONE MAY DEVELOP RESISTANCE WHEN USED ALONE DUE TO MUTATED FOLATE SYNTHASE
WHICH LOWERS THE AFFINITY OF FOLATE SYNTHASE FOR DAPSONE.
PHARMACOKINETICS:

-DAPSONE IS GIVEN ORALLY AND IS ALMOST COMPLETELY ABSORBED FROM THE GUT.
-70% BOUND TO THE PLASMA PROTEIN, AND IS WIDELY DISTRIBUTED IN THE BODY.
-GETS CONCENTRATED MAINLY IN LIVER, SKIN, MUSCLE KIDNEY ETC.
-SECRETED IN BILE AND UNDERGOES ENTEROHEPATIC CYCLING.
-METABOLISED BY ACETYLATION AND THE METABOLITE IS EXCRETED THROUGH URINE.

ADVERSE EFFECTS:
- PRODUCES HEMOLYTIC ANEMIA, G6PD PATIENTS ARE MORE SUSCEPTIBLE.
- OTHER SIDE EFFECTS ARE ANOREXIA, NAUSEA, VOMITING, FEVER, HEADACHE, ALLERGIC DERMATITIS,
ITCHING & PERIPHERAL NEUROPATHY.
- METHAEMOGLOBINEMIA CAN ALSO OCCUR.
SULPHONE SYNDROME
- STARTS AFTER 4-6 WEEKS OF THERAPY MORE COMMON WITH MDT.

SYMPTOMS- FEVER, MALAISE, LYMPHADENOPATHY, SKIN EXFOLIATION,

JAUNDICE & ANEMIA.

MANAGEMENT-
STOPPING OF DAPSONE, CORTICOSTEROID THERAPY.

DAPSONE IS CONTRAINDICATED IN SEVERE ANEMIA & G6PD DEFICIENT PATIENTS.

CLOFAZIMINE
- IT IS A PHENAZINE DYE AND HAS ANTILEPROTIC, ANTI-INFLAMMATORY, AND
BACTERIOSTATIC ACTIVITY.
MODE OF ACTION-
- CLOFAZIMINE BINDS TO MYCOBACTERIAL DNA TO INHIBITS ITS TEMPLATE
FUNCTION.
- MONOTHERAPY CAUSES RESISTANCE IN 1-3 YEARS.
- DAPSONE RESISTANT RESPOND TO IT.
PHARMACOKINETICS:
- ABSORBED ORALLY AND GET ACCUMULATED IN SUB CUTANEOUS TISSUES AS
CRYSTALS
- HALF LIFE 70 DAYS.
- FATTY MEAL INCREASES ITS ABSORPTION.
ADVERSE DRUG REACTION:
- IT CAUSES REDDISH BLACK DISCOLORATION OF SKIN OF EXPOSED PART.

- IT CAUSES PIGMENTATION OF THE CONJUNCTIVA AND CORNEA AND DISCOLORATION OF THE HAIR, TEAR,
SWEAT, URINE, ETC.
OTHER SIDE EFFECTS ARE –
NAUSEA
VOMITING
DIARRHOEA
ABDOMINAL PAIN

IT IS CONTRAINDICATED IN EARLY PREGNANCY, LIVER & KIDNEY DISEASES.

RIFAMPICIN:
- IT IS THE MOST EFFECTIVE AND RAPIDLY ACTING BACTERICIDAL DRUG.
- SKIN SYMPTOMS REGRESS WITHIN 2 MONTHS.
- INCLUDED IN MDT TO SHORTEN THE DURATION OF TREATMENT AND ALSO
TO PREVENT RESISTANCE.

OFLOXACIN:
- ALL FLOROQUINOLONES EXCEPT CIPROFLOXACIN ARE ACTIVE.

- USED AS ALTERNATIVE TO RIFAMPICIN.

ETHIONAMIDE:
- IT IS 2ND LINE ANTITUBERCULAR DRUG AND IS ALSO EFFECTIVE AGAINST
LEPRA BACILLI.
- IT IS FAST ACTING DRUG THAN DAPSONE.
- IT CAN BE USED AS AN ALTERNATIVE DRUG WHEN THERE IS C/I FOR THE
USE OF CLOFAZIMINE OR IF IT IS UNACCEPTABLE.
- IT MAY CAUSE HEPATOTOXICITY.
CLARITHROMYCIN:
- ONLY MACROLIDE WITH ACTIVITY AGAINST M. LEPRAE.
- LESS BACTERICIDAL ACTIVITY THAN RIFAMPICIN.
- SYNERGISTIC ACTION WITH MINOCYCLINE.
- USED IN ALTERNATIVE MDT REGIMENS

MINOCYCLINE:
- ONLY TETRACYCLINE THAT HAS ANTILEPROTIC ACTIVITY.
- B/C OF HIGH LIPOPHILICITY THIS TETRACYCLINE PENETRATES INTO M. LEPRAE AND IS ACTIVE
AGAINST THEM.
ANTILEPROTIC ACTIVITY;
RIFAMPICIN > MINOCYCLINE > CLARITHROMYCIN

“THE BIGGEST DISEASE IS TODAY IS NOT LEPROSY OR

TUBERCULOSIS BUT RATHER THE FEELING OF BEING
UNWANTED, UNCARED FOR & DESERTED BY EVERY BODY.”—
MOTHER TERESA
THANKYOU