leprosy by jitendra bhangale

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© 2010 Delmar, Cengage Learning1

By- Jitendra Bhangale

Assistant Professor & Head,

Department of Pharmacology,

Smt N. M. Padalia Pharmacy College,

Ahmedabad


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 thatwhich causes tuberculosis.

It attacks the nerves of thehands, feet and face.

If left untreated can take awaythe ability to move fingers, toesand eyelids.

It can also destroy the ability tofeel pain so those affected areprone to injuries and burns.

The longer the disease is leftundetected, the more likely it isthat the deformities, so oftenassociated with leprosy, will occur.



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



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



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



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



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.



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



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.


By Jitendra BhangaleAsst. Prof. Dept of Pharmacology, Smt N. M. Padalia Pharmacy College, Ahmedabad

leprosy by jitendra bhangale

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