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© 2010 Delmar, Cengage Learning
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By- Jitendra Bhangale
Assistant Professor & Head,
Department of Pharmacology,
Smt N. M. Padalia Pharmacy College,
Ahmedabad
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By J. O. Bhangale, Head, Dept of Pharmacology, Smt N. M. Padalia Pharmacy College, A’bad
It is a chronic infectious disease caused by M.leprae, an
acid fast, rod shaped bacillus.
It mainly affects the skin, peripheral nerves, and mucosa of
the respiratory tract etc.,
It has left behind a terrifying image in history and human
memory of mutilation, rejection and exclusion from society.

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Caused by a germ similar to that
which causes tuberculosis.
It attacks the nerves of the
hands, feet and face.
If left untreated can take away
the ability to move fingers, toes
and eyelids.
It can also destroy the ability to
feel pain so those affected are
prone to injuries and burns.
The longer the disease is left
undetected, the more likely it is
that the deformities, so often
associated with leprosy, will occur.
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Lepromatous: damages respiration, eyes, and skin
Tuberculoid: affects nerves in fingers and toes, and
surrounding skin
Borderline: has effects of both types

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Examine skin
Check for patches
Test for sensation
Count the number of patches
Look for damage to nerves
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Test for sensation
Take a pointed soft object (feather, cotton wick)
Lightly touch alternately the patch & normal skin
Ask the person to point where they were touched
Ask them to close their eyes and repeat the procedure
In case of loss of sensation the person will be able to
point to where they were touched on the normal skin but
not on the patch

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The diagnosis is made based on finding definite loss of
sensation in one or more patches.
When you have examined the whole body, count the number
of patches.
1-5 patches is paucibacillary (PB), more than 5 patches is
multibacillary (MB) leprosy
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PB Adult
(6 blister packs)
Rifampicin 600 mg once a month
Dapsone 100 mg every day
MB Adult
(12 blister packs)
Rifampicin 600 mg once a month
Clofazimine 300 mg once a month
Clofazimine 50 mg and dapsone 100 mg every day

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Sulfones
Dapsone
Phenazine derivative
Clofazimine
Anti TB agents
Rifampin
Ethionamide
Other
Ofloxacin
Minocycline
Clarithromycin
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The sulfones are derivatives of 4,4-diaminodiphenylsulfone
(dapsone).
Dapsone is bacteriostatic, but not bactericidal.
Mechanism of action:-
They are competitive inhibitors of dihydropteroate synthase and
prevent the normal bacterial utilization of para-amino-benzoic acid.
Both possess approximately the same range of antibacterial activity
and both are antagonized by para-aminobenzoic acid.

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Untoward Effects
Methemoglobinemia, Anorexia, nausea, and vomiting,
headache, nervousness, insomnia, blurred vision,
paresthesias, reversible peripheral neuropathy
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The rifamycins (rifampin, rifabutin, rifapentine) are a group of
structurally similar, complex macrocyclic antibiotics produced by
Streptomyces mediterranei .
Antibacterial Activity:- Rifampin inhibits the growth of most
gram-positive bacteria as well as many gram-negative
microorganisms such as Escherichia coli, Pseudomonas, indole-
positive and indole-negative Proteus, and Klebsiella. Rifampin is very
active against Staphylococcus aureus and coagulase-negative
staphylococci.

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Mechanism of Action:-
Rifampin inhibits DNA-dependent RNA polymerase of mycobacteria
and other microorganisms by forming a stable drug-enzyme
complex, leading to suppression of initiation of chain formation in
RNA synthesis.
More specifically, the β subunit of this complex enzyme is the site
of action of the drug, although rifampin binds only to the
holoenzyme.
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Nuclear RNA polymerases from a variety of eukaryotic cells do not
bind rifampin, and RNA synthesis is correspondingly unaffected in
eukaryotic cells.
High concentrations of rifamycin antibiotics can inhibit RNA
synthesis in mammalian mitochondria, viral DNA-dependent RNA
polymerases, and reverse transcriptases.
Rifampin is bactericidal for both intracellular and extracellular
microorganisms.

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Adverse effect:-
Hepatitis and deaths
Chronic liver disease
Alcoholism
Respiratory syndrome
Cutaneous syndrome
Flu syndrome
Abdominal syndrome
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Clofazimine appears to preferentially bind to GC-rich
mycobacterial DNA and also increase mycobacterial
phospholipase A2 activity and inhibit microbial K+ transport.
It is weakly bactericidal against M. intracellulare.
The drug also exerts an antiinflammatory effect and prevents the
development of erythema nodosum leprosum.
The compound also is useful for treatment of chronic skin ulcers
produced by Mycobacterium ulcerans.

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Thalidomide has been shown effective for the treatment of
erythema nodosum leprosum.
It has immunomodulatory actions and inhibits tumor necrosis
factor-a.
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By Jitendra Bhangale
Asst. Prof. Dept of Pharmacology, Smt N. M. Padalia Pharmacy College, Ahmedabad

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