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DRUG FOR LESHIMANIA AND
TRYPANASOMIASIS
SALUM MKATA
CSEE,ACSEE,B.pharm.
AMPHOTERICIN
an alternative therapy for visceral
leishmaniasis, especially in parts of India with
high-level resistance to...
AMPHOTERICIN
Amphotericin B
(Fungilin, Fungizone, Abelcet, AmBisome, Fungisome,
Amphocil, Amphotec) is a polyene antifunga...
ORINICO RIVER
Cont.
Two amphotericins, amphotericin A and
amphotericin B are known, but only B is used
clinically, because it is signifi...
CONT.
Uses
Antifungal
Oral preparations of amphotericin B are used to
treat thrush; these are virtually non-toxic, in
contrast t...
MOA
• The primary site of action of amphotericin B on L. donovani
promastigote cells appears to be membrane sterols that
r...
Interactions
• Flucytosine: Toxicity of flucytosine is increased
and allows a lower dose of amphotericin B.
Amphotericin B...
Side-effects
Amphotericin B is well known for its severe
and potentially lethal side effects. Very often,
a serious acute ...
MILTEFOSINE
• It has shown efficacy for the treatment of
visceral leishmaniasis.
• Given in a dose of 2.5 mg/Kg for 28 day...
Cont.
• Transient elevations in liver enzymes are also
seen.
• The drug should be avoided in pregnancy
because of its tera...
DRUGS FOR TOXOPLASMOSIS
• Pyrimethamine plus sulphadiazine plus folinic
acid.
Why folic acid?
• Folinic acid (Leucovorin) ...
Can be used in pregnacy?
Cont.
• Management of maternal and fetal infection
varies depending on the treatment center. In
general, spiramycin is rec...
Drug for leshimania and trypanasomiasis
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Drug for leshimania and trypanasomiasis

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Drug for leshimania and trypanasomiasis

  1. 1. DRUG FOR LESHIMANIA AND TRYPANASOMIASIS SALUM MKATA CSEE,ACSEE,B.pharm.
  2. 2. AMPHOTERICIN an alternative therapy for visceral leishmaniasis, especially in parts of India with high-level resistance to sodium stibogluconate, but its use is limited in developing countries by difficulty of administration, cost and toxicity.
  3. 3. AMPHOTERICIN Amphotericin B (Fungilin, Fungizone, Abelcet, AmBisome, Fungisome, Amphocil, Amphotec) is a polyene antifungal drug, often used intravenously for systemic fungal infections. It was originally extracted from Streptomyces nodosus, a filamentous bacterium, in 1955 at the Squibb Institute for Medical Research from cultures of an undescribed streptomycete isolated from the soil collected in the Orinoco River region of Venezuela. Its name originates from the chemical's amphoteric properties.
  4. 4. ORINICO RIVER
  5. 5. Cont. Two amphotericins, amphotericin A and amphotericin B are known, but only B is used clinically, because it is significantly more active in vivo. Amphotericin A is almost identical to amphotericin B (having a double C=C bond between the 27th and 28th carbons), but has little antifungal activity.
  6. 6. CONT.
  7. 7. Uses Antifungal Oral preparations of amphotericin B are used to treat thrush; these are virtually non-toxic, in contrast to typical intravenous therapy (IV) doses. Antiprotozoan use as a drug of last resort in otherwiseuntreatable parasitic protozoan infections such as visceral leishmaniasis and primary amoebic meningoencephalitis.
  8. 8. MOA • The primary site of action of amphotericin B on L. donovani promastigote cells appears to be membrane sterols that result in a loss of the permeability barrier to small metabolites • Amphotericin B is highly lipophilic and easily absorbs into membrane lipids where it interacts with membrane sterols(cholesterol in mammals and ergosterol in fungi) to create channels in the membrane, which allows small molecules to be lost, eventually leading to cell death • Inhibition of respiration by the drug was a comparatively slower process
  9. 9. Interactions • Flucytosine: Toxicity of flucytosine is increased and allows a lower dose of amphotericin B. Amphotericin B may also facilitate entry of flucystosine into the fungal cell by interfering with the permeability of the fungal cell membrane. • Diuretics : Increased renal toxicity and increased risk of hypokalemia • Corticosteroids: Increased risk of hypokalemia
  10. 10. Side-effects Amphotericin B is well known for its severe and potentially lethal side effects. Very often, a serious acute reaction after the infusion (1 to 3 hours later) is noted, consisting of high fever, shaking chills, hypotension, anorexia, nausea, vomiting, headache, dyspnea and tachypnea, drowsiness, and generalized weakness
  11. 11. MILTEFOSINE • It has shown efficacy for the treatment of visceral leishmaniasis. • Given in a dose of 2.5 mg/Kg for 28 days it provided excellent clinical results. • A 100 mg daily dose is recommended in adults, • Vomiting and diarrhea are common but generally short-lived toxicities.
  12. 12. Cont. • Transient elevations in liver enzymes are also seen. • The drug should be avoided in pregnancy because of its teratogenic effects.
  13. 13. DRUGS FOR TOXOPLASMOSIS • Pyrimethamine plus sulphadiazine plus folinic acid. Why folic acid? • Folinic acid (Leucovorin) protects the bone marrow from the toxic effects of pyrimethamine. What for those with sulfa allergy? • If the patient has a hypersensitivity reaction to sulfa drugs, pyrimethamine plus clindamycin can be used instead.
  14. 14. Can be used in pregnacy?
  15. 15. Cont. • Management of maternal and fetal infection varies depending on the treatment center. In general, spiramycin is recommended (for the first and early second trimesters) or pyrimethamine/sulfadiazine and leucovorin (for late second and third trimesters) for women with acute T. gondii infection diagnosed at a reference laboratory during gestation.

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