SITI SUPARTIDepart.of Pharmacology & Therapy

Faculty Of Medicine – Padjadjaran University

DRUGS USED IN CHEMOTHERAPY OF

PROTOZOA INFECTION

CHEMOTHERAPY OF PARASITIC DISEASES

ANTI PROTOZOAL DRUGS

CHEMOTHERAPYOF AMOEBIASIS

* CHLOROQUINE* DILOXANIDE FUROATE* DEHYDROEMETINE* EMETINE* METRONIDAZOLE* DERIVATES OF 8 - HYDROXYQUINOLINES

CHEMOTHERAPYOF MALARIA

* PRIMAQUINE* CHLOROQUINE* QUININE* MEFLOQUINE* PYRIMETHAMINE* CHLOROGUANIDE

CHEMOTHERAPY OF PARASITIC DISEASES

CHEMOTHERAPY OF HELMINTHIASIS

CHEMOTHERAPYOF NEMATODES

* Mebendazole* Pyrantel pamoate* Thiabendazole* DEC

CHEMOTHERAPYOF TREMATODES

* Praziquantel

CHEMOTHERAPYOF CESTODES* Niclosamide

CHEMOTHERAPY OF AMOEBIASIS

AMOEBIASIS :CAUSED BY : Entamoeba histolyticaLocation : * Intestine ( Colon )

* Liver and other

CLASSIFICATION OF ANTIAMEBICIDES1. LUMINAL AMEBICIDES :

diloxanid furoate, tetracycline, paromomycin, iodoquinol

2. SYSTEMIC AMEBICIDES :Emetin, dehydroemetin, chloroquine

3. MIXED AMEBICIDES :metronidazol

I. LUMINAL AMEBICIDES : 1. Diloxanide furoate

* about 90 % absorbed. The unabsorbed drug is an active drug* Forintestinal amebiasis only* Side effects: flatulence, dryness of the mouth, pruritus urticaria* Contraindicated : pregnant women, children under 2 years of age

2. 8-hydroxyquinolines * Preparation : iodoquinol

Clioquinol ( iodochlor hydroxyquin ) * Significant risk of the clioquinol, 2 gr. per day for long periods is SMON ( subacute myelo-optic neuropathy ) * Not for routine use

3. Paromomycin

* an aminoglycoside antibiotic

* direct amebicid

* adverse effects :gastrointestinal distress, diarrhea

II. SYSTEMIC AMEBICIDE

1. Chloroquine * used in conjunction with metronidazole and diloxanid furoate * eliminates trophozoites in liver abscesses

2. Emetine, dehydroemetine * Their use is limited by their toxicities * Un toward effects :

- pain in site of injection- transient nausea- cardiotoxicity- neuromusscular weakness- dizzness- rashes

III. MIXED AMOEBICIDES Metro nidazole * Combination metronidazole plus a luminal amebicide/ difuloxanid furoate cure rates > 90 % * For treating infections caused by :

E.histolytica G.lamblia Trichomonas vaginalis

* For treating infections caused by : anaerobic cocci anaerobic gram-negative bacilli ( Bacteriades spp) anaerobic gram-positive bacilli ( Clostridia )

* Effective in the treatment of brain abscess ( caused by E.histolytica )Resistance :Strains of trichomonads resistent to metronidzol has been reported

Administration and Distribution* Oral administration, completely and rapidly absorbed* Usually administered with a luminal amebicide ( DF )* It distributes well through out body tissue and fluids* In vaginal and seminal fluids, saliva, CSF the drug can be found in therapeutic levels.

Fate :* metabolism in the liver by mixed function oxidase follow by glucuronidation* Phenobarbital enhance the rate metabolism

Adverse Effect :* Gastrointestinal effect : nausea, vomiting, epigastric distress, abdominal cramps* Neurotoxicological problems* Reversible neutropenia* Not recommended during the first trimester of pregnancy

Therapeutic Uses:1. In the treatment of infectious with

T.vaginalis:• Cures genital infectious in both female and

male• Dosage: 2 g single dose or 250 mg 3 times

daily for 7 days• Uncured or reccurent interval of 4 to 6

week between courses• Unsatisfactory response:

• Chronic infection of Skene’s and Bartholin’s glands

• Reinfection by partner 2 g to both sexual partner and given gel or vag

supp.

2. In the treatment of Amebiasis• Agent of choice for the treatment of all

symptomatic forms of amebiasis• Dosage: 750 mg, 3 times daily for 5 to 10

days• Least effective to an asymptomatic passer of

cyst in combination with diloxanide

3. Metronidazole is extremely useful for treatment of serious infection due to susceptible anaerobic bacteria: Bacteriodes, Clostridium, Fusobacterium, Peptococcus, Peptostreptococcus, Eubacterium and Helicobacter.