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ANTIPARASIT
Protozoal infections
Amebiasis
Protozoal infections
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Amebiasis
Amebiasis is a protozoal infection of the
intestinal tract that occurs due to ingestion
of foods or water contaminated with
Entameba Histolytica cysts
LIFE CYCLE
Clinical Presentations
Asymptomatic Intestinal infection
ANTIAMOEBIC DRUGS
LUMEN AMOEBICIDES
Acts
Mixed amoebicides
Metronidazol
Tinidazole
METRONIDAZOLE
Mixed amoebicide.
Drug of choice for intestinal
&
extraintestinal amoebiasis.
Acts on trophozoites.
Has no effect on cysts.
Nitro group of metronidazole is reduced by
protozoan leading to cytotoxic reduced product
that binds to DNA and proteins resulting into
parasite death.
Pharmacokinetics
Given orally or IV.
Absorption is rapid and complete.
Due to rapid absorption from GIT, not reliably
effective against luminal parasites.
Wide distribution to all tissues and body fluids
(CSF, saliva, milk).
Plasma protein binding is low ( < 20%).
Plasma half life is 8 h
Pharmacokinetics
Metabolized in liver by mixed function
oxidase followed by glucouroidation.
Excreted in urine as unchanged drug plus
metabolites.
Clearance is decreased in liver impairment.
Tinidazole has longer duration, simpler
dosing regimen, less toxicity, than
metronidazole, but is equally active.
Clinical Uses
Extraluminal
Adverse effects
1. GIT:
Nausea
Vomiting
Dry mouth
Metallic taste
Diarrhoea
Oral Thrush (Moniliasis, yeast infection).
Adverse effects
2. CNS: Neurotoxicological effect
Insomnia, dizziness
peripheral neuropathy, paresthesia
encphalopathy, convulsion ( IV infusion, rare).
3. Dysuria, dark urine.
4. Neutropenia
5. Disulfiram-like effect if taken with alcohol.
aldehyde
dehydrogenase
Acetaldehyde
Acetate
Adverse effects of
metronidazole
Drug interactions:
Enzyme
CONTRAINDICATIONS / PRECAUTIONS:
Pregnancy and nursing women
Alcohol intake
CNS diseases
Severe hepatic disease
Severe renal disease
Anthelmintic Drugs
Anthelmintics
The major
Benzimidazoles (BZAs)
thiabendazole, mebendazole, and albendazole
Mechanism of action
inhibition of microtubule polymerization by
binding to -tubulin
Drug resistance in nematodes may involve
expression of a mutated -tubulin
PK/PD
Thiabendazole
Absorbed rapidly after oral ingestion. A
fatty meal enhances absorption
Reaches peak plasma concentrations
after 1 hour
Excreted in the urine within 24 hours as 5hydroxythiabendazole, conjugated either
as the glucuronide or the sulfate
Mebendazole
Tablet formulations of mebendazole are poorly
and erratically absorbed, and plasma
concentrations are low
The low systemic bioavailability (22%) of
mebendazole results from a combination of poor
absorption and rapid first-pass hepatic
metabolism
THERAPEUTIC USES
Thiabendazole generally has been replaced by
newer agents
Mebendazole always is taken orally, and the same
dosage schedule applies to adults and children >2
years of age. For treatment of enterobiasis, a
single 100-mg tablet is taken, repeated after 2
weeks
For
Albendazole
Use in Pregnancy
Both
Praziquantel
a
pyrazinoisoquinoline derivative
Mechanism of Action
low concentrations, it causes increased muscular
activity, followed by contraction and spastic
paralysis
At slightly higher concentrations, praziquantel
causes tegumental damage, which exposes a
number of tegumental antigens. The tegument of
schistosomes seems to be the primary site of
action; the drug causes an influx of Ca2+ across
the tegument via unknown mechanisms
PK/PD
Readily
THERAPEUTIC USES
FDA approved
kontraindikasi
Praziquantel
Pyrantel Pamoate
a
PK/PD
DIETHYLCARBAMAZINE
Diethylcarbamazine
PK/PD
Absorbed
THERAPEUTIC USES
W. Bancrofti, B. Malayi, and B. Timori
The standard regimen for LF has been a 12-day, 72mg/kg
(6 mg/kg/day) course of diethylcarbamazine. A single dose
of 6 mg/kg had comparable macrofilaricidal and
microfilaricidal efficacy to previous regimens. Single-dose
therapy may be repeated every 612 months, as necessary.
Diethylcarbamazine remains the best drug for therapy of
loiasis. Treatment is initiated with test doses of 50 mg (1
mg/kg in children) daily for 23 days, escalating as tolerated
to daily doses of 9 mg/kg in Three doses for a total of 23
weeks.
<810 mg/kg/daycarbamazine,
including anorexia, nausea, headache,
and vomiting, are rarely severe and
usually disappear within a few days
despite continued therapy
Ivermectin
Mechanism of action :
Avermectins affect a group of glutamategated Cl channels found in nematode
nerve or muscle cells, causing
hyperpolarization and paralysis by
increasing Cl permeability of the cell
membrane
PK/PD
Peak
THERAPEUTIC USES
Onchocerciasis
Single oral doses of ivermectin (150 g/kg) given every
612 months are considered effective, safe, and practical
for reducing the number of circulating microfilariae in
adults and children 5 years of age or older
Lymphatic Filariasis
Single annual doses of ivermectin (400 g/kg) are
effective and safe for mass therapy of infections with W.
bancrofti and B. malayi.
Ivermectin is as effective as diethylcarbamazine for
controlling lymphatic filariasis and can be used in regions
where onchocerciasis, loiasis, or both are endemic.
Infecting Organism
Drug of Choice
Alternative Drugs
Ascaris lumbricoides
(roundworm)
Albendazole or pyrantel
pamoate or mebendazole
Ivermectin, piperazine
Trichuris trichiura
(whipworm)
Mebendazole or
albendazole
Ivermectin
Necator americanus
(hookworm); Ancylostoma
duodenale (hookworm)
Albendazole or
mebendazole or pyrantel
pamoate
Strongyloides stercoralis
(threadworm)
Ivermectin
Albendazole or
thiabendazole
Enterobius vermicularis
(pinworm)
Mebendazole or pyrantel
pamoate
Albendazole
Trichinella spiralis
(trichinosis)
Mebendazole or
albendazole; add
corticosteroids for severe
infection
Roundworms
(nematodes)
Infecting Organism
Drug of Choice
Alternative Drugs
Roundworms
(nematodes)
Albendazole
Trichostrongylus species
Pyrantel pamoate or
mebendazole
Albendazole
Albendazole or ivermectin
Thiabendazole (topical)
Albendazole
Mebendazole
Angiostrongylus
cantonensis
Albendazole or
mebendazole
Wuchereria bancrofti
(filariasis); Brugia malayi
(filariasis); tropical
eosinophilia; Loa loa
(loiasis)
Diethylcarbamazine
Onchocerca volvulus
(onchocerciasis)
Ivermectin
Dracunculus medinensis
(guinea worm)
Metronidazole
Thiabendazole or
mebendazole
Capillaria philippinensis
(intestinal capillariasis)
Albendazole
Mebendazole
Ivermectin
Infecting Organism
Drug of Choice
Alternative Drugs
Schistosoma haematobium
(bilharziasis)
Praziquantel
Metrifonate
Schistosoma mansoni
Praziquantel
Oxamniquine
Schistosoma japonicum
Praziquantel
Praziquantel
Albendazole
Paragonimus westermani
(lung fluke)
Praziquantel
Bithionol
Bithionol or triclabendazole
Praziquantel or niclosamide
Heterophyes heterophyes;
Metagonimus yokogawai
(small intestinal flukes)
Praziquantel or niclosamide
Flukes (trematodes)
Infecting Organism
Drug of Choice
Alternative Drugs
Praziquantel or niclosamide
Mebendazole
Praziquantel or niclosamide
Praziquantel or niclosamide
Cysticercosis (pork
tapeworm larval stage)
Albendazole
Praziquantel
Praziquantel
Niclosamide, nitazoxanide
Echinococcus granulosus
(hydatid disease);
Echinococcus multilocularis
Albendazole
Tapeworms (cestodes)
TRIMETHOPRIM
SULFAMETHOXAZOLE
ANTIBACTERIAL SPECTRUM
ABSORPTION,DISTRIBUTION,AND
EXCRETION
After
About
Gastrointestinal Infections
Drug interactions:
Prolonged
Fluoroquinolon
Adverse reactions to
SEKIAN
TERIMA KASIH !!
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