ANTHELMINTIC DRUGS

M.Djamaludin.MG
Departement of
Parma!olo"#
A!mad $ani S!ool of
Medi!ine
AL%ENDA&'LE
INDICATI'N
1.Ascaris lumbricoides
2.Trichuris trichura
3.Necator americanus
4.Strongilodes stercoralis
5.Enterobius vermicularis
D'SE

Adults and children over 2 years : Single

dose 4 mg! orally re"eated 2#3 $ee%s

Taenia(i( : 4 #12 mg &or 3 days

Entero)ia(i(: 4 mg ingle dose.

'e"eated a&ter 2 ( 4 $ee%s to "revent
rein&ection

)isceral larva migrans

Trichinella s"iralis

*uchereria bancro&ti

+a"illaria "hili"inensis

+lonorchis sinensis
Cutaneou( lar*a mi"ran( :
4 mg,day!&or 5 days! ca"illariasis
intestinal 1 days! trichuriasis 15 days
C'NTRAINDICATI'NI:
-regnancy
.reast &eeding
CAUTI'NS: /e"atic and renal dys&unction
SIDE E++ECT ,
Abdominal discom&ort
0i11iness
/eadache
PREP:
+a"let 4 mg
+he$ ca"tab 1 mg
Siru& 2 mg,5 cc!1 cc
ME%ENDA&'LE
INDICATI'N:
Ascariasis!23yuriasisAn%ylosttomiasis!trich
uraisis!strongiloides stercoralis
D'SE:
23yuriasis : Single dose 1 mg
Ascariasis :T$ice 1 mg,day &or 3 days
Taenia (a"inata: T$ice 3 mg,day!&or 3
days
Tri!uria(i(: T$ice 1 mg,day! &or3#4
days
An-ilo(tomia(i(: T$ice 1mg ,day!&or 3
days
C'NTRAINDICATI'N:
-regnancy
PIPERA&IN HE.AH$DRAT
INDICATI'N: Ascariasis!o3yuriasis!
D'SE:
'/#uri(: Adult and children over 4 years! 1
measure s"oon!3 times ,day
+hildren: 3#4 year: 1 measure s"oon
t$ice,day
+hildren 1#2 years: 5 measure s"oon!
t$ice,day! &or 4 days
C'NTRAINDICATI'N,
/e"atic and renal dys&unction! e"ile"tic
CAUTI'N : 64-0 0e&
SIDE E++ECT:
67T synndrome!headache! hy"ersensitivity
DRUG INTERACT'NI:
-irantel dan "henothia1in
LE0AMIS'L 12onime/3
INDICATI'N:

Ascaris lumbricoides!An%ylostoma
duodenale
SIDE E++ECT

67T syndrome!di11iness!headache.
D'SE:

Adult and children over 15 years! 4#4 tablet

+hildren:12#15 years 3#4 tablet

8#12 years 3 tablet

+hildren: 4#8 years :2 tablet

3#4 years :1 5 tablet

1#3 years : 1 tablet

Single dose

-re": Tablet 25 mg: 4 tablet,stri"

DIETH$LCAR%AMA&INE
9:ilar1an;
CHEMISTR$: 7t is a "i"era1ine
derivated
M'A,
7mobili1ation and change sur&ace
structure o& micro<laria ! to
micro<laria &rom tissue! &acilitates
the destruction o& micro<laria by
host defense mechanism
INDICATI'N,
*uchereria bancro&ti! .rugia malayi!
.rugia Timori dan =oa>=oa
D'SE
3 times,day 2 mg,%g.. concommitent
$ith meal! 1#3 days.
SIDE E++ECT,
/eadache! malaise! anore3ia! $ea%ness!
nausea! vomitus
I0ERMECTIN
INDICATI'N:
7vermectin is the drug o& choice in
strongiloidosis and onchoceciasis. 7t is
also an alternative drug &or other
helminthic in&ectioni.e. ? *uchereria
bancro&ti! .rugia malayi! tro"ical
eosino<lia! and =oa#=oa.
SIDE E++ECT,
:ever! headache! nausea! vomitus
abdominal "ain! and rash
D'SE,
Single dose: 15 ug,%g.*! e@ectivity
"ro"ortional $ith 0E+ to micro<laria
o& tissue! s%in! and anterior chamber
o& eye.
C'NTRAINDICATI'N,

-re gnancy

+hildren under 5 years 9Sa&ety is not

established;

7t is not administered $ith barbiturat!

ben1odia1e"ine! or val"roac acid
PRA&I4UANTHEL
INDICATI'N , Taenia solium
Single dose : 1 mg,%g.*

NICL'SAMIDE
INDICATI'N ,Taenia solium
D'SE : T$ice a day A 1 gram
+hildren a hal& dose
THIA%ENDA&'LE
INDICATI'N : 0rug o& +hoice &or
S.stercoralis! cutaneous larva migrans. Not
recomended &or: As%ariasis! trichuriasis!
an%ylostomiasis and o3yuriasis D'SE:
2325 mg,%g.* &or 2 day.

:or hy"erin&ection syndrome 2325

mg,%g.*! 5#B days

:or cutaneous larva migrans 2325

mg,%g.$! 2#5 days
TREATMENT '+ SPECI+I2
+'RM '+ AME%IASIS
A. AS$MPT'MATIC INTESTINAL
IN+ECTI'N
Asym"tomatic carriers generally are not
treated in endemic areas but in
nonendemic area they are treated $ith
luminal amebicides
A tissue amebicides drug is
unnecessary. Standard luminal
amebicides are dilo3anide &uroate!
iodoCuinol! and "aramomycin.
Thera"y $ith luminal amebicides is
also reCuire in all other &orms o&
amebiasis
%.AME%IC C'LITIS

Detronida1ole "lus a luminal

amebicide is the treatment o& choice
&or colitis and dycentry

Tetracyclines and erythromycin are

alternative drugs &or moderate colitis
but are not e@ective against
e3traintestinal disease.
0ehydroemetine or emetinne can
also be used! but these agents are
best avoided! because o& their
to3icity
C.E.TRINTESTINAL
IN+ECTI'NS
The treatment o& choice is metronida1ole
"lus a luminal amebicide. A 1#day course
o& metronida1ole cures over E5F o&
uncom"licated liver abscesses. :or unusual
cases $here initial thera"y $ith
metronida1ole has &ailed! as"iration o& the
abscess and the addition o& chloroCuine to
a re"eat course o& metronida1ole should be
considered. 0ehydroemetine and emetine
are to3ic alternative drugs.
METR'NIDA&'LE

Detronida1ole nitroimida1ole is the

drug o& choice &or the treatment o&
e3traluminal amebicides. 7t %ills
tro"ho1oites but not cyst o&
E.hystolytica and e@ectively
erradicates intestinal and
e3traintestinal tissues
+hemistry and
-harmaco%inetics

Absorbed a&ter oral adminitration

"ermeates all tissues by sim"le
di@usion. =o$ binding $ith "rotein.
The drug and its metabolites are
e3creted mainly in the urine
Me!ani(m of A!tion

The nitro grou" o& metronida1ole is

chemically reduced in anaerobic
bacteria and sensitive "roto1oans.

'eactive reduction "roducts a""ear

to be res"onsible &or antimicrobial
activity.
Clini!al u(e(
1. Amebiasis
2. 6iardiasis
3. Trichomoniasis
0. Adverse E@ects and +autions

Nausea! headache! dry mouth! or metallic

taste occurs commonly.

7n&reCuent adverse e@ects include and

vomiting! diarrhea! insomnia! $ea%ness!
di11iness! thrush! rash! dysuria! dar% urine!
vertigo! "aresthesia!and neutro"enia.
Ta%ing the drugs $ith meals lessens git
irritation

The rare e@ects "ancreatitis! severe +NS

to3icity

Detronida1ole has a disul<ram#li%e

e@ect! so that nausea and vomiting
can occur i& alcohol ingested during
thera"y. The drug should be used
$ith caution in "atients $ith +NS
disease.

Detronida1ole has been re"orted to

"otentiate the anticoagulant e@ect o&
coumarin#ty"e anticoagulant.
I'D'4UIN'L

7odoCuinol 9iodohydro3yCuin; is a
halogenated hydro3yCuinoline. The D2A
o& iodoCuinol against tro"ho1oites is
un%no$n.

7t is an e@ective luminal amebicide. .ut

not against tro"ho1aotes in the intestinal
$all or e3traintestinal tissues.
7n&reCuent adverse e@ects include
diarrhea! $hich usually sto" a&ter
several days#anore3ia!
nausea!vomitus! abdominal "ain!
headache! rash! and "ruritus.
07=2GAN70E :H'2ATE

0ilo3anide &uroate is a
dichloroacetamide derivate. 7t as an
e@ective luminal amebicide but si not
active against tissue tro"ho1oites.

7n the gut dilo3anide &uroate is s"lit

into dilo3anide and &uroic acid! about
EF o& the dilo3anide is absorbed.
The unabsorbedis active antiamebic
substance. The D2A o& dilo3anide
&uroate is un%no$n. 7t is used$ith a
tissue amebicide! usually
metronida1ole to treat serious inestinal
and e3traintestinal in&ection.
SIDE E++ECTS,
:latulence
Nausea
'ash
C'NTRAINDICATI'N,
-regnancy
EMETINE 5
DEH$DR'EMETINE

Emetin is an al%aloid derived &rom

i"ecac! and dehydroemetine!
synhhetic analog! are e@ective
against tissue tro"ho1oites o&
hystolytica. The drug administered
"arenterally because oral
"re"aration are absorbed erraticaly.

0ehydroemetine is "re@ered over

emetine because o& its some$hat
better to3icity "ro<le

R'A:
S.+ or 7.D but never intravenously.
.ecause o& adverse e@ects it should
not be used more than 1 days.
Serious side e@ect is cardiac
arrythmias! heart &ailure! and
hy"ertension.
C'NTRAINDICATI'N,
1. +ardiac disease
2. 'enal disease
3. Ioung children
4. -regnancy
AME%IASIS TREATMENT

IN+ECTI'N D'C
ALTERNATI0E DRUGS
Asm",carier 7odoC.
0ilo%s.&ur,-ar
7nt mild#mod Detr...J7odoC AA
lumKT,0E,E
7nt sev. Detr....J7odoC AA
lumKT,0E,E
Absces Detr....J7odoC
0E,E....%loKAA lum
D'C 6 Dru" of !oi!e
ALTERN. DRUGS 6 Alternati*e Dru"(
Asm" L Asym"tomatic
7odoC. L 7odoCuinolon
0ilocs.&ur L 0ilocsanide &uroate

-ar L -aramomycin


7nt mild#mod L 7ntestinal mild#moderate
Detr L Detronida1ole
AA lum L Anti amebic luuminal
T L Tetracycline
0E L dehydro emetine
E L emetine
7nt sev. L 7nitestinal severe

'THER ANTIPR'T'&'AL
DRUGS
PENTAMIDINE
+linical uses
1. -neumocystosis
2. A&rican Try"anosomiasis 9Slee"ing
Sic%ness;
3. =eishmaniasis
TR$PAN'S'MIASIS 1SLEEPING
SIC2NESS3
Pentamidine

/as been used since 1E4 as an alternative

to suramin.

The drug can be used $ith suramin

-entamidine should not be used to treat late

try"anosomiasis $ith +NS involvement

D'SE: 2#4 mg,%g daily or on alternate days

&or a total o& 1#5 doses.

As chemo"ro"hylacti3is:v4 mg,%g every 3#4

months
S'DIUM
STI%'GLUC'NATE
:irst line agents &or cutaneous and visceral
leishmaniasis
R'A : 7.) or 7.D.
D'SE : 2nce daily!2 mg,Mg.* &or 2
days cutaneous and 28 days in visceral
leishmaniasis
M'A : N
SE : 67T! &ever! headache! myalgia!
arthralgia! rash
NITA&'.ANIDE

Nito1o3anide a""ears to have activity

against metronida1ole resistent "roto1o al
strains and is $ell tolerated.

:ree o& mutagen e@ect 9not as

metronida1ole;

2ther suce"tible to! nita1o3anide:

E.hystolytica! /."ylori! A.lumbricoides!

several ta"e$orms! and :. he"atica
'THER DRUGS +'R
TR$PAN'S'MIASIS 5 LEISHMANIASIS

SH'AD7N

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