Leprosy by JITENDRA BHANGALE

9/2/2012

By- Jitendra Bhangale
Assistant Professor & Head,
Department of Pharmacology,
Smt N. M. Padalia Pharmacy College,
Ahmedabad
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© 2010 Delmar, Cengage Learning

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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By J. O. Bhangale, Head, Dept of Pharmacology, Smt N. M. Padalia Pharmacy College, A’bad

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9/2/2012

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 © 2010 Delmar, Cengage Learning
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9/2/2012

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 8

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Sulfones

Dapsone
Other
Phenazine derivative
Ofloxacin
Clofazimine
Minocycline
Anti TB agents
Clarithromycin
Rifampin

Ethionamide
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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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9/2/2012

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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9/2/2012

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
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Asst. Prof. Dept of Pharmacology, Delmar, Cengage Learning Pharmacy College, Ahmedabad
© 2010 Smt N. M. Padalia

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Leprosy by JITENDRA BHANGALE

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