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BY :- Shailja Sharma
M.Pharm
Pharmacology
• Leprosy is a chronic infectious disease caused by
Mycobacterium leprae. Host defenses are crucial in
determining the patient’s response to the disease,the
clinical presentation, and the bacillary load.
• Leprosy manifests in two forms
• Lepromatoid (the organism being localized to skin or
nerve)
• Lepromatous (a generalized bacteraemic disease that
effects many organs, analogous to miliary tuberculosis).
• The main drugs used to treat leprosy are dapsone,
rifampicin and clofazimin.
• The treatment of leprosy suggest multidrug regimens
rather than monotherapy because such a regimen has
proven to be more effective, delays the emergence of
resistance, prevents relapse, and shortens the duration
of therapy. Agents used in the treatment of leprosy are
dapsone,clofazimine,and rifampin.
• Treatment of tuberculoid leprosy is continued for at least
1 to 2 years,while patients with lepromatous leprosy are
generally treated for 5 years.
• In addition to chemotherapy, patients with leprosy need
psychosocial support, rehabilitation, and surgical repair of
any disfiguration.
• Sulfone: Dapsone
• Phenazine derivative: Clofazimine
• Antitubercular drugd : Rifampin
Ethionamide
• Other Antibiotics : Ofloxacin
Moxifloxacin
Minocycline
Clarithromycin
• The sulfones are structural analogues of PABA and are
competitive inhibitors of folic acid synthesis. Sulfones are
bacteriostatic and are used only in the treatment
ofleprosy.
• Dapsone (Avlosulfon) is the most widely used sulfone for
the long-term therapy of leprosy. Although the sulfones
are highly effective against most strains of M.leprae, a
small number of organisms,especially those found in
lepromatous leprosy patients,are less susceptible and
can persist for many years, resulting in relapse
• Sulfones, such as dapsone and sulfoxone (Diasone), are
well absorbed orally and are widely distributed
throughout body fluids and tissues.Peak concentrations
of dapsone are reached within 1 to 3 hours of oral
administration and have a half-life of 21 to 44
hours;about 50% of administered dapsone is bound to
serum proteins. The sulfones tend to remain in the skin,
muscle, kidney,and liver up to 3 weeks after therapy is
stopped. The concentration in inflamed skin is 10 to 15
times higher than that found in normal skin.The sulfones
are retained in the circulation for a long time (12–35
days) because of hepatobiliary drug recirculation. The
sulfones are acetylated in the liver,and 70 to 80% of drug
is excreted in the urine as metabolites.
• Dapsone, combined with other antileprosy
agents like rifampin and clofazimine, is used in
the treatment of both multibacillary and
paucibacillary M. leprae infections.
• Dapsone is also used in the treatment and
prevention of Pneumocystis carinii pneumonia in
AIDS patients who are allergic to or intolerant of
trimethoprim–sulfamethoxazole.
The sulfones can produce
• nonhemolytic anemia
• methemoglobinemia
• acute hemolytic anemia in persons
with a glucose-6-phosphate
dehydrogenase deficiency
• acute skin lesions
• Fever
• Pruritus
• Paresthesia
• Reversible neuropathy
• Hepatotoxicity
Pharmacology of Anti leprotic Agents

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Pharmacology of Anti leprotic Agents

  • 1. BY :- Shailja Sharma M.Pharm Pharmacology
  • 2. • Leprosy is a chronic infectious disease caused by Mycobacterium leprae. Host defenses are crucial in determining the patient’s response to the disease,the clinical presentation, and the bacillary load. • Leprosy manifests in two forms • Lepromatoid (the organism being localized to skin or nerve) • Lepromatous (a generalized bacteraemic disease that effects many organs, analogous to miliary tuberculosis). • The main drugs used to treat leprosy are dapsone, rifampicin and clofazimin.
  • 3. • The treatment of leprosy suggest multidrug regimens rather than monotherapy because such a regimen has proven to be more effective, delays the emergence of resistance, prevents relapse, and shortens the duration of therapy. Agents used in the treatment of leprosy are dapsone,clofazimine,and rifampin. • Treatment of tuberculoid leprosy is continued for at least 1 to 2 years,while patients with lepromatous leprosy are generally treated for 5 years. • In addition to chemotherapy, patients with leprosy need psychosocial support, rehabilitation, and surgical repair of any disfiguration.
  • 4. • Sulfone: Dapsone • Phenazine derivative: Clofazimine • Antitubercular drugd : Rifampin Ethionamide • Other Antibiotics : Ofloxacin Moxifloxacin Minocycline Clarithromycin
  • 5. • The sulfones are structural analogues of PABA and are competitive inhibitors of folic acid synthesis. Sulfones are bacteriostatic and are used only in the treatment ofleprosy. • Dapsone (Avlosulfon) is the most widely used sulfone for the long-term therapy of leprosy. Although the sulfones are highly effective against most strains of M.leprae, a small number of organisms,especially those found in lepromatous leprosy patients,are less susceptible and can persist for many years, resulting in relapse
  • 6. • Sulfones, such as dapsone and sulfoxone (Diasone), are well absorbed orally and are widely distributed throughout body fluids and tissues.Peak concentrations of dapsone are reached within 1 to 3 hours of oral administration and have a half-life of 21 to 44 hours;about 50% of administered dapsone is bound to serum proteins. The sulfones tend to remain in the skin, muscle, kidney,and liver up to 3 weeks after therapy is stopped. The concentration in inflamed skin is 10 to 15 times higher than that found in normal skin.The sulfones are retained in the circulation for a long time (12–35 days) because of hepatobiliary drug recirculation. The sulfones are acetylated in the liver,and 70 to 80% of drug is excreted in the urine as metabolites.
  • 7. • Dapsone, combined with other antileprosy agents like rifampin and clofazimine, is used in the treatment of both multibacillary and paucibacillary M. leprae infections. • Dapsone is also used in the treatment and prevention of Pneumocystis carinii pneumonia in AIDS patients who are allergic to or intolerant of trimethoprim–sulfamethoxazole.
  • 8. The sulfones can produce • nonhemolytic anemia • methemoglobinemia • acute hemolytic anemia in persons with a glucose-6-phosphate dehydrogenase deficiency • acute skin lesions
  • 9. • Fever • Pruritus • Paresthesia • Reversible neuropathy • Hepatotoxicity