91525876-52573816-antimicotice
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8/13/2019 91525876-52573816-Antimicotice
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I. Clasificare
1.mecanism de actiune si caracteristici structurale generale
A.ANTIMICOTICE CARE INHIBA BIOSINTEZA ERGOSTEROLULUI SI
INTERFERA FUNCTIILE ACESTUIA
A.1. Antibitice !acrli"e #lienice
A.$. A%li &i!i"a%li si tria%li' ( cna%li
A.). Ticarba!ati (Tolnaftat, Tolciclat)
A.*. Alila!ine si a!ine tertiare (Naftifina, Terbinafina)
A.+. ,eri-ati "e !rflina (Amorolfina)
B. INHIBITORI AI SINTEZEI ERETELUI CELULAR FUNGIC
B.1. Antibitice li##e#ti"ice/ Caspofungin
ANTIMICOTICE
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C. ANTIMICOTICE CARE INTERFERA FUNCTIILE ACIZILOR
NUCLEICI AI
CELULEI FUNGICE
(diviziune celulara, metabolismul bazelor azotate,
sinteza proteica)
C.1. Antibiotice cu structura spiro-benzouranica
!Griseofulvina)
C.". #eri$ati piri%i#inici (Flucitozina)
&. IN'I(ITORI AI TRAN)*ORTULUI MEM(RANAR AL
AMINOACIZILOR
(Ciclopirox olamina)
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ANTIMICOTICE. C+asiicare
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A. ANTIIC!TIC" CA#" IN$I%A %I!&INT"'A "#G!&T"#!I &IINT"#F"#A FNCTII" AC"&TIA
A.*. Antibiotice macrolide polienice
Nistatin
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&inonim+ StamicinStreptomyces noursei
rop. fizizo-cimice+
pulbere galbena sau galben-cafenie, miros slab
caracteristic (cereale), higroscopica; termolabila, sensibila
la lumina si umiditate conservare/
foarte 0reu solubil in apa si alcool, usor solubil in 1&!,
1FA
&pectru de activitate Nistatin
Fun,ici# Can#i#a sp. Asper0illus sp., Cr3ptococcus
neoformans
NI&TATIN. NI&TAT7N (1CI, F# 8)
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roduse farmaceutice
Nistatin + antibiotice + metronidazol +
glucocorticoizi
NI)TATIN compr. film. 566.666 I/ pulb pt suspensie orala
*,9:
)TAMICIN compr. film. 566.666 I
M/CO)TATIN compr. 566.666 I/
suspensie uz intern *66.666 I;ml/
ung., crema *66.666 I;0
TRICOMICON compr. vaginale (<etronidazol, <
Cloramfenicol)
MACMIROR COM*LE0 - ovule, ung. vaginal (<Nifuratel)
*OL/G/NA0 caps vagin. (<Neomicina <olimixina)
NI&OFLOR ung. (<Neomicina <Triamcinolon acetonid)
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&inonim+ Pimafucin, Pimaricin; Streptomyces natalensis
&pectru de activitateFun0i unicelulari+ Candida albicans
1ermatofiti+ "pidermop3ton, Tricop3ton, icrosporum
uce0aiuri+ Asper0illus
rotozoare+ Tricomonas va0inalis
Indicatii+ antimicotic exclusiv local candidoze locale
dermatomicoze ale pielii, un0iilor si patului un0ial/
intertri0o, micoze interdi0itale/ iritatia de scutec/ va0initecandidozice/ candidoze datorate antibioterapiei prelun0ite/
stomatite candidozice/ otomicoze/ candidoza larin0elui si
farin0elui
#eactii adverse+ bine tolerat , local si di0estiv
NATAMICINA. NATAM/CINUM !&CI2
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od de administrare
Crema *-4 aplicatii locale; zi/Lotiune =-> aplicatii;zi
Ovule * ovul;zi x 4-> zile (se reia dupa menstre)
1 Comr! oral x =;zi
• candidoza intestinala (timp de ?-*6 zile)/
•ca tratament ad"uvant celui toic, in+ candidoza
ung#iilor (timp de @-4 luni),candidoza extinsa a ielii
(inca * sapt. dupa disparitia simptomelor clinice) (Natamicina
se acumuleaza in conc. eficace terapeutic in tesuturile
eratinizate); vaginita candidozica rezistenta (timp de *6-
@6 zile/ <ovule)
roduse farmaceutice
*IMAFUCIN crema @:,lotiune; ovule *66 m0/
compr. enterosolubile *66 m0
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AF!T"#ICINA %. A$!T"#ICIN" % (1CI)
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AF!T"#ICINA %. A$!T"#ICIN" % (1CI)
roduse farmaceutice
AMFOTERICIN ( pulb sterila liofilizata de uz perfuzabil
(56 m0)
FUNGIZONE flac uz parenteral; susp. orala; crema,lotiune, ung.
A(ELCET complex lipidic (dimiristoilfosfatidil-colina,
-0licerol)
AM(I)OME amfotericina %lipozomica -suspensie
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benzil-imidazoli (Clotrimazol, %ifonazol, Flutrimazol)
fenil-etil-imidazoli (conazoli generatia I+
eteri - iconazol, Isoconazol, "conazol, Tioconazol/
tioeteri B &ulconazol
oxime B !xiconazol
imidazoli ! structuri varia+ %utoconazol, !moconazol
A.@. Azoli (imidazoli si triazoli) ; conazoli
A.".1. Azo+i #e ,eneratia I (imidazoli
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Azo+i #e ,eneratia I benzi+-i%i#azo+i.$erezentanti teraeutici
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.".1. Azo+i #e ,eneratia I (imidazoli
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C!T#IA'!. C!T#IA'! (1CI)
1enumire cimica+ *-D@-clorfenil)-difenil-metilE-*$-imidazol
scade actiunea altor antimicotice (antibiotice antimicotice
Contraind.+ alergie la clotrimazol; sarcina %trim!&'
roduse si forme farmaceutice+
CLOTRIMAZOL crema "#, sol ext. "# (@-4 aplic;zi x = sapt)
compr. vaginale *66 m0 (*-@;zi, >-*@ zile)
CANE)TEN crema, pudra, sol ext. "#
CANE)TEN 'G crema (Clotrimazol *: <$idrocortizon acetat *6 m0)
G/NO-CANE)TEN compr. vaginale "$$ mg, %$$ mg, &$$ mg
crema vaginala "# si %# cu aplicator
LOTRIMIN crema, lotiune "#
G/NE-LOTRIMIN compr. vagin. "$$ mg; crema vaginala "#
MECLOZOL compr. vagin. (<etronidazol<Neomicina<$exestrol
acetat)
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FT#IA'!. FT#IA'! (1CI)
<efect antiinflamator intrinsec dermatite
inflamatorii
MICETAL crema, gel "#; spray uz extern %IF!NA'!. %IF!NA'! (1CI)
enetrabilitate crescuta in straturi (eratinoase %ung#ii'
toleranta superioara
o sin0ura aplicatie zilnica (stabil si activ timp de @= )/
durata tratam. variaza in functie de afectiune
(candidoze >-9 zile/ dermatofitii *6-*@ zile/ pitiriazis @
sapt/
onicomicoze @ luni/ tricofitii > zile si repetare dupa * sapt
de pauza)
Contraind+ ipersensibilitate la bifonazol
roduse si forme farmaceutice+(IAZOL crema "#
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Azoli de 0eneratia I
fenil-etil-imidazoli
(conazoli 0eneratia I)
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osolo0ie
local
*comr! oral @56 m0 x 4 ori;zi, timp de *-@sapt in candidoza
orala si @-= sapt. in candidoza 0astro-intestin./ 5 zile;luna sau in
perioada de risc pt profilaxia candidozei la pacienti imunodeprimati,
cateterizati sau tratati cu antibiotice p.o./
@ comr! vaginale; zi x ? zile sau * compr. va0in, seara x *= zile
(si in trimpul menstrei, nu se fac spalaturi va0inale) compr. oral
x =;zi B va0inite micotice, va0inite mixte/
crema, solutie, sra), udra, lotiune B alicatii toice de @
ori;zi/
solutie erfuzabila*
menin0ite criptococice, candidoze sistemice B
*966-4>66 m0;zi divizat in 4 perfuzii lente, timp de 4-*@ sapt.
IC!NA'!.
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roduse si forme farmaceutice cu iconazol+
MICOTO* gel, crema %#
MICONAZOL compr orale %&$ mg; compr vaginale "&$ mg
MICONAL ECO(I
crema %#;
crema vaginala %#; ovule &$ mg; caps vaginale ",% g;
solutie pt spalaturi vaginale $,%#
MONI)TAT
crema %#, spray %#
supozitoare vaginale %$$ mg
solutie perfuzabila %#&A3TARIN gel oral %#
G/NO-&A3TARIN ovule '$$ mg
G/NOZOL caps vagin %$$ mg, '$$ mg
3LION compr. vagin. (iconazol) etronidazol
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"C!NA'!. "C!NA'!" NIT#AT" (1CI)
antimicotic de uz toic;
spectru similar isoconazolului ) germeni *ram-pozitivi de
suprainfectie
vulvo-vaginite candidozice* * ovul;zi x *5 zile
candidoze cutanate si dermatofitii (suprainfectate+
@ ori;zi x @-=sapt. < @ sapt dupa disparitia
simptomelor
pitiriazis+ spuma (cu un burete umed, seara, pe zona
afectata x 4 zile)
roduse si forme farmaceutice+
AMICEL ovule "&$ mg; crema vagin "#; crema si spuma
externa "#
*EAR/L crema "#
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&"#TAC!NA'!. &"#TAC!NA'!" NIT#AT" (1CI)
Anti%icotic #e uz topic
tinea interdigitale si candidoze vulvo-vaginale la
imunocompromisi
ZALAIN crema %#, @ aplic;zi
&C!NA'!. &C!NA'!" NIT#AT" (1CI)
derivat fenil-etil-imidazolic B inlocuire isosterica a ! din structura
econazolului cu &/
orme tinea nefoliculare (corporis, pedis, cruris, pitiriazis
dermatita seboreica, matreata
E0EL&ERM crema si lotiune "#
*-@ori;zi x @-= sapt. si inca @ sapt. dupa disparitia
simptomelor
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!8IC!NA'!. !8IC!NA'!" NIT#AT" (1CI)
enetrabilitate buna in tesuturile /eratinoase
tinea %inclusiv onicomicoze si itiriazis', candidoze
vulvo-vaginale
O0I)TAT crema, lotiune "#
M/FUNGAR crema "#
G/NO-M/FUNGAR compr vagin $$ mg
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Azoli de 0eneratia I B imidazoli cu structuri varia
%T!C!NA'!" NIT#AT" (1CI)Anti%icotic uz topic candidoze vulvo-vaginale
G/NAZOLE crema vagin unidoza %#
!!C!NA'!" NIT#AT" (1CI)
Candidoze, dermatofitii ale pielii 0labre, ale miinilor si picioarelor
FONGAMIL crema, solutie, pudra "#; @ aplic;zi x 4 sapt
FONGARE0 ovule 0$$ mg
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Azoli de 0eneratia a II-a (conazoli 0en. a II-a)
2lasificare
imidazoli3 Hetoconazol
triazoli+ Terconazol, Itraconazol
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H"T!C!NA'!. H"T!C!NA'!" (1CI)
4enumire chimica+
cis-*-acetil-=-D-=-DD@-(@,=-diclorofenil)-@-(*5-imidazol-*-il-metil)-*,4-
dioxolan-=-ilE-metiloxiEfenilEpiperazina
rop. fiz.-chimice+
pulbere alb sau 0 lbuie, lipsit de miros, insolubil n ap , solubil nă ă ă ă ă ă
acizi.
2onservare+ ferit de umiditate, flacoane bine ncise.
6c iune farmacologic ţ ă+
ntimicotic sectru larg* dermatofiti, levuri, fun0i dimorfici
ntirotozoaric (eismania sp.)
ntiinflamator
&n#ibitor al aromatazei (biosinteza $. sexuali)
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Indicatii terapeutice+ Anti%icotic #e uz siste%ic si +oca+
curativ3
micoze sistemice (>-*@ luni), subcutanate Ji oportuniste,
pitiriazis versicolor,
K forme tinea/ (! < local, @-= s pt mLni)ă ă
dermatite seboreice, m trea -ă ţă local
profilactic3 (!), candidoze la pacien i &I1A, transplanta i, boliţ ţ
autoimune,
neoplazici, care urmeaz antibioterapie cu antibioticeă
spectru lar0
6lte indica ii ţ
7eishmanioze cutaneomucoase - (!), tratam. de alternativă
2ancer de prostat recurentă
H"T!C!NA'!
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8eac ii adverse3 ţ
ulb! gastro-intestinale
(0rea , vom , anorexie, dureri abdomin.)ţă ă admin. n
timpul mesei
ulb! #eatice (icter colestatic),ulb! endocrine (0inecomastie, dureri ale sLnilor, menstre
nere0ulate,
oli0ospermie, impoten )ţă
metabolice (sc derea colesterolemiei, ipertri0liceridemie)ă
reac ii alergiceţ locale, Joc anafilactic (prima doz ).ă
rar3 tulb. nervoase (cefalee, ame eli, somnolen , fotofobie,ţ ţă
modific ri ale viselor) Jiă cardio-vasc. ($TA, aritmii).
H"T!C!NA'!
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H"T!C!NA'!
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IT#AC!NA'!. IT#AC!NA'!" (1CI)
antifun0ic, spectru analo0 Hetoconazol < tulpini Asper0illus/ ! Ji
/
antifun0ic de prim ale0ere n micoze profunde/ă
de alternativ n asper0iloze pulmonare Ji extrapulmonare laă
pacien i cu intoleran sau nonresponsivi laţ ţă 6mfotericină/
(eratofilic
conc. terapeutice n un0ii de 5 ori M plasmatice, remanente n
un0ie Ji piele un interval mare de timp (un0ie - > luni dup 4ă
luni tratam./ piele - @-= s pt. dup un tratam. de = s pt.)ă ă ă
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diferen e de biodisponibilitate ntre formele farm. orale+ţ
capsule Ji solu ie oralţ ă
biodisponibilitate oral maximă ă
capsule+ la administrare dup -mas Ji cu o b utură ă ă ă
acidulată
solu ie uz intern+ la admin. nainte de masţ ă
$eac ii adv!* bine tolerat ţ /
la tratam. de lun0 durat , pe cale i.v. reac ii adv. asem.ă ă ţ
Hetoconazolului+ tulb 0astro-intestin., sdr. 0ripal.
IT#AC!NA'!
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Contraind*
sarcină (terato0en),al tare,ă
aritmii cardiace,
afec iuni epatice.ţ
recau ii3 aclorhidrie, tulbur ri de ritm cardiac, edem ţ ă pulmonar
Interac iuni+ similare etoconazoluluiţ
roduse farm.
)*ORANO0 capsule *66 m0,solu ie uz intern ţ / flac
perfuzabile
ORUNGAL capsule *66 m0
IT#AC!NA'!
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$erezentanti teraeutici ai conazolilor de gener! a &&-a T"#C!NA'!. T"#C!NA'!" (1CI)
.ungicid Candida albicans vulvo-vaginite
orme farm3 crema, ovule * doza;zi, 4-? zile
#eactii adverse locale+ arsuri, iritatii vulvo-va0inale
generale+ cefalee, mial0ii, febra
Nu interfera cu contraceptivele orale
rodus farm.
TERAZOL crema vaginala $.'# si $.9#
supozitoare vaginale 9$ mg
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Azoli de 0eneratia a III-a (triazoli, conazoli 0en. a III-a)
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FLUCONAZOL.
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A.6. Tiocarba%ati + Tolnaftat , Tolciclat
$ela ii structur / ac iuneţ ă ţ
N #isubstituit !-C'6 -Ar2 7 esen ia+ţ
r-0, r-O0 sau r-OC0
(indiferent de pozi ia pe nucleul aromatic ţ
6r-substituen i electrono-atr g tori ţ ă ă
activit antimicotică
A 6 Ti b ti
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rop. fiz-chim. + ulberi microcristaline albe sau alb-cenuJii,
lipsite de miros, insolubile n ap , uJor solubile n alcool.ă
2onservare+ ferit de lumin Ji umiditateă
Indicatii terap. 3 E8c+usi$ +oca+ B #er%atoi ii pit9riazisţ
$ersico+or
O inactivi pe Candida albicans, micoze ale scalpului Ji
onicomicoze
8eac ii adverse rare ţ olnaftat
TINACTIN solu ie uz extern, crem ţ ă *:
MICONAFT cremă *:
AFTATE spray (pudr :i solu ie, gelă ţ *:
A.6. Tiocarba%ati +
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A.=. Alilamine si amine tertiare+
NAFTIFINA , T"#%INAFINA
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*ro#use ar%.
Natiina
23O42$&L
sol. uz extern,
crema "#
N.&.&N
crema, gel "#
Terbinaina
L5&S&L
crema "#
comprim. %&$ mg
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A 5 1 i ti d f li A lfi
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A.5. 1erivati de morfolina + Amorolfina
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%.*. Antibiotice lipopeptidice+ CA&!FNGIN
%. IN$I%IT!#I AI &INT"'"I "#"T"I C"A# FNGIC
CA)*OFUNGIN ACETAT !&CI2
Indicatii terapeutice+
candidemie siabcese intra-abdominale, eritoneale si
leurale cu Candida/
candidoze esofagiene
asergiloze invazive la pacienti refractari sau intoleranti
la alte antimicotice (amfotericina, itraconazol)
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CA)*OFUNGIN .
#eactii adverse+
tromboflebite, iritatii venoase/
cauzate de eliberarea #istaminei (ras, prurit, edem facial,
anafilaxie)
tulb! #eato-biliare (in special, la pacienti tratati
concomitent cu 2iclosporina)
&pecialitati
CANCI&A) flac cu pulb liofilizata 56 m0, ?6 m0
&olutia perfuzabila se prepara prin dizolvare in ser fiziolo0ic sau
apa distilata/
nu se asociaza in perfuzie cu alte subst. medicam.
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C. ANTIIC!TIC" CA#" INT"#F"#A FNCTII"
ACI'I!# NC"ICI AI C""I FNGIC"
(diviziune celulara, metabolismul bazelor azotate, sinteza proteica)
C.*. Antibiotice cu structura spiro-benzofuranica
G#I&"!FPINA. G#I&"!FPIN (1CI, F# 8)
enicillium griseofulvum; izomerul dextrogir activ biologic
G#I&"!FPINA
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G#I&"!FPINA
rop fiz-chim3
ulbere crist alba sau alb-0albuie, lipsita de miros si de
0ust.
ractic insolubila in apa, 0reu solubila in etanol si metanol/
solubila in 1FA si 1&!, propilen0licol.stabila in stare solida si in solutii la p$4-9
ec de actiune si spectru de activitate antifungica
.ungistatic prin blocarea diviziunii celulare (mitoza), fiind
activa numai pe
fungii-dermatofitii aflati in faza de crestere
%multilicare'*
"pidermop3ton sp., Tricop3ton sp.,
G#I&"!FPINA
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G#I&"!FPINA
G#I&"!FPINA
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G#I&"!FPINA
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&pecialitati+
GRI)EOFULIN compr. "%& mg griseofulvina
micronizata
FULICIN compr. %&$ mg, &$$ mg griseofulvina
micronizata
GRI)ACTIN caps. %&$ mg, &$$ mg griseofulvina
micronizata
GRIFULIN susp. uz oral
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C.@. 4erivati pirimidinici+
FCIT!'INA. FCIT!&IN" (1CI)
&-luorocitozina (&-2
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FCIT!'INA
ecanism si spectru de activitate
sectru ingust* Candida albicans, Cr)tococcus
neoformans
fungistatic, rin interferarea metabolismului bazelor
irimidinice
si sintezei proteice+•conversia 5-FC la 5-Fluorouracil, sub actiunea citozin-dezaminazei/•conversia 5-Fluorouracil la acid 5-Fluorouridilic, care va fiincorporat in locul uridinei in structura A#N proteineanormale
selectivitate entru celula fungica
(absenta citozin-dezaminazei din celula umana)
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CIT!'INA
eactii adverse+ doze mari, tratam. indelun0ate
0astro-intestinale, disfunctii epatice, ematolo0ice, reactii aler0i
ontraind.3 sarcina, alaptare, copii
pecialitati+
ANCO(ON caps. %&$ mg, &$$ mg
ANCOT/L caps &$$ mg; sol perfuzabila
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1 IN$I%IT!#I AI T#AN&!#TI
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1. IN$I%IT!#I AI T#AN&!#TI
"%#ANA#
A AIN!ACI'I!# + CIC!I#!8 !AINA
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