Antiamebic drugs

z Luminal amebicides: act in the bowel lumen

{ Direct amebicides
1. Diloxanide
2. Iodoquinol
3. Paromomycin
{ Indirect amebicides
1. Erythromycin & tetracyclinesÆ⇓flora Æstarvation of ameba
z Tissue amebicides: effective against trophozoites in tissues
{ Emetine & dehydroemetine
{ ChloroquineÆ effective against trophozoites in liver only

z Mixed (luminal & tissue amebicides)

Metronidazole & tinidazole

Treatment of amebiasis
z Aim of treatment:
z Eradication of tissue invading trophozoites
z Eradication of the cyst in intestinal lumen
Clinical setting Drugs of choice Alternative drugs

Asymptomatic Luminal agents

carrier 1. diloxanide 3 times daily for
10 days
2. Iodoquinol 3 times daily for
21 days
3. Paromomycin 3 times daily
for 7days
Mild intestinal Metronidazole (10days therapy) Erythromycin or tetracycline (10days
infection + luminal agent therapy)
+luminal agent
Severe intestinal Metronidazole (10days therapy) Emetine or dehdroemetine
infection + luminal agent (10days therapy)
+luminal agents
Hepatic & extra- Metronidazole (10days therapy) Emetine or dehdroemetine+
intestinal abscess + luminal agent chloroquine (liver abscess only)
(10days therapy)
+luminal agents
 Metronidazole
z Action:
1. Activity against protozoa
a. Anti-amebic activity: mixed luminal & tissue amebicidal
b. Less effect as lumen amebicidal .It is rapidly absorbed ◊ low intra-
intestial concentration
c. Anti-giardiasis
d. Antitrichomoniasis
2. Powerful activity against anerobic bacteria: e.g. Bacteroids fragilis &
Clostridium difficile
z Uses
1. Amebiasis
Drug of choice for :Entamoeba Histolytica
i. Intestinal amebiasis
ii. Hepatic amebic abscess
iii. Extra-intestinal amebic disease
2. Trichomoniasis
3. Giardiasis
4. Anaerobic infection
a. Pseudomembranous colitis: clostridium difficile
b. Sepsis caused by anerobic bacteria: e.g. intraabdominal infection
caused by bacteroids fragilis
c. Bacterial vaginosis
What are the adverse effects of metronidazole ?
• GI irritation :cramps ,nausea & vomiting
• Metallic taste
• Dark coloration of urine
• Disulfiram –like reaction with ethanol
• CNS disturbances : Dizziness & ataxia
•
Emetine & Dehydroemetine
z It is used for severe intestinal amebiasis and extra-intestinal amebiasis
z It is alternative to metronidazole
z It is given Sc or IM
z Never given IV ◊ cardiotoxicity
z Not used more than 10 days
z Adverse effects
1. CVS toxicity: arrhythmia & hypotension
2. GIT toxicity: nausea& vomiting
3. Local pain and tenderness at site of injection
4. Muscle weakness & peripheral neuritis
z Dehydroemetine is less toxic
Leishmaniais
Visceral leishmaniasis
Drug of choice :Sodium stibogluconate
Alternative drugs:
 1. Pentamidine
2. Amphotericin B
3. Meltefosine
Cutaneous leishmaniasis
Drug of choice :Sodium stibogluconate
Alternative drugs:
1. Pentamidine
2. Ketoconazole

Sodium stibogluconate
z Pentavalent antimonials
z 1st line drug for cutaneous and visceral leishmaniasis
z It is given IV or IM once daily for 20days for cutaneous leishmaniasis and for 28
days for visceral leishmaniasis
z Resistance stat to appear in certain endemia areas
z Adverse effects
1. Nausea & vomiting
2. Fever, headache, arthralgia & mylagia
3. ECG changes: prolongation of Q-T interval. Continued treatment Æ
serious arrhythmia. Monitor ECG during therapy
Pentamidine
1. It is effective for cutaneous leishmaniasis caused by some species of leishmania
2. It is given IM or IV daily or every other day for 15 doses
3. Rapid intravenous administration Æ severe hypotension & tachycardia
4. IV pentamidine should be given while the patient in supine position ,slowly over
60min. with close monitoring of blood pressure and ECG monitor during and
several times after administration
5. Adverse effects
a. Hypotension and cardiac arrhythmia
b. Pain and tenderness at site of IM injections
c. Hypoglycemia & diabetogenic effects: may occur during
therapy or after drug discontinuation (days or months)
d. Nephrotoxicity: reversible on discontinuation
e. Leucopenia
f. GIT toxicity: nausea, vomiting & diarrhea
g. Elevated AST and ALT concentrations
N.B(immmmmmp).
z Parenteral pentamidine is used for treatment of pneumocystis carnii
pneumonia in immuno-suppressed patients
z Inhaled pentamidine powder is used for prophylaxis against pneumocystis
carnii pneumonia in immuno-suppressed patients
Miltefosine
z Effective for treatment of visceral leishmaniasis
z It is given orally
z Adverse effects
{ Vomiting & diarhea
 { Transient elevation of liver enzymes
Giardiasis
z Giardia lamblia: cause an infection of the small intestine
z 1st line drug is metronidazole or tinidazole
z Metronidazole is given orally 3 times daily for 5days
z Tinidazole is given as a single oral dose
z Alternative drugs :
{ Furazolidone
{ Albendazole
z Furzolidone
{ It has activity against gram+ve & gram-ve enteric bacteria
{ It has activity against giardia lamblia
{ Adverse effects
i. Nausea, vomiting & diarrhea
ii. Hypersensitivity reactions

Trichomoniasis
z The causative organism is Trichomonas vaginalis
z It is sexually transmitted disease may be symptomatic or asymptomatic
z Symptomatic women complain from yellowish green malodorous genital
discharge with vulvular irritation
z Most infected men are asymptomatic
z There is association between vaginal trichomoniasis and adverse pregnancy
outcome
z Metronidazole is given orally for treatment of trichomoniasis
z Both partners should be treated
z Pregnant women can be treated with metronidazole only during second and third
trimesters
z During pregnancy: Single oral 2g dose is used instead of 7 days therapy
z For lactating mother : a single oral 2 g dose is used and breast feeding is
interrupted for 12-24hrs to allow clearance of the drug