Antimicotice

→ atb: amfotericina ambele L → alialmine – inhiba selectiv scualen 2,3 epoxidaza

Griseofulvina sistemic ingust fungica → ↓ sinteza ergosterol
Nistatin ambele ingust Terbinafina ambele L
Natamicin ambele L Naftifina local L

→ azoli bifonazol local → alte structuri

Clotrimazol ambele ingust sau L Amarolfina local L
Econazol local L Ciclopirox local L
Fluconazol sistemic L Flucitozina ambele ingust
Fenticonazol -5FdUMP este puternic inhibitor al timidilat
Flutrimazol local L sintetazei, enzima in sinteza ARN
Isoconazol local Haloprogin local ingust
Itraconazol sistemic L Nifuratel
Ketoconazol ambele L Tolnafat local ingust
Miconazol ambele L Tolciclat local
Posaconazol sistemic
Sertaconazol local → alte structuri - inhiba selectiv 1,3 β D glucan
Tioconazol local ingust sintetaza → ↓ sinteza peretelui celular
Terconazol local ingust Caspofungin
Variconazol sistemic Micafungin
anidulafungin
→ Imidazoli
Clotrimazol ambele
Econazol local L
Flutrimazol local L
Isoconazol local
Sertaconazol local
Ketoconazol ambele L
Miconazol ambele L
Tioconazol local ingust
→ Triazoli
Fluconazol sistemic L
Itraconazol sistemic L
Posaconazol sistemic
Terconazol local ingust
Variconazol sistemic

Agenti patogeni
-superficiale -Trichophyton (herpes circinat, tinea unguium, pilomicoze uscate si supurate)
-Malassesia (pitiriazis)
-Epidermophyton (tinea cruris, tinea pedis, tinea manum)
-Corynebacterium minutissimum (eritrasma)
-Microsporium (pilomicoze uscate)
-Candida albicans

-sistemice -sporotricum schenckii (sporotricoza)

-Nocardia brasiliensis, N. asteroides,
-Streptomyces madurae, S. albus
-Abscheria boydii,
-Madurella mycetomatis,
-Aspergillus fumigatus,
-Cephalosporium falciforme,
-Geotrichum candidum

Micoze -superficiale -dermatofiti

-onicomicoze
-pilomicoze uscate / supurate
-candidoze

-sistemie -sporotricoza
-micetom (piciorul de Madura)
Amfotericina L Griseofulvina
-macrolid polienic
-toxic renal peste 3g/cura
Asociere flucitozina, rifampicina, minociclina
-Adm i.v, absorbtie p.o neglijabila
-Actiune: fungistatic-fungicid + imunostimulator
-Mecanism: legare ireversibila de structurile sterolice
(ergosterol) ale mb → ↑ permeabilitatea, eflux K, influx atb,
fungistatice (sinergism)
ingust (Microsporium, Epidermophyton, Trichophyton)
-Adm p.o variabila, grasimile ↑ abs
-Actiune: fungistatic, inductor enzimatic ↓ anticoagulante,
anticonceptionale
-Mecanism: patrunde in celule prin proces dependent de energie
→ pertubarea fusului de diviziune → inhiba mitoza
(rezistenta)
-R adv: boala serului, r de tip estrogenic, r disulfiram, ↑
protoporfirinelor in fecale
Penicillium griseofulvum

Nistatin (pag 92) Natamicin L (+ Trichomonas) (pag 393)

ingust (Trichophyton, Microsporium, Epidermophyton, -Adm p.o, absorbtie ↓, crème suspensii, inhalatii
Cryptococus, Candida)
≠ actinomicete, bacterii

-atb polienic
-Adm p.o, absorbtie ↓, vaginal (cpr, unguente)
-Actiune: fungistatic-fungicid
-Mecanism: legare ireversibila de structurile sterolice
(ergosterol) ale mb → ↑ permeabilitatea, eflux K, influx atb,
fungistatice (sinergism)
-PF Pimafucin
Streptomices nourei Streptomyces natalensis

Clotrimazol L Econazol L
Asociere cortizon local -Spectru + bacterii G+
-Mecanism: inhiba C 14 α sterol-demetilaza (CYP 450) →
-Spectru CCM d + blocheaza transf lanosterol in ergosterol
-Mecanism: inhiba C 14 α sterol-demetilaza (CYP 450) → ↑ permeabilitatea mb
blocheaza transf lanosterol in ergosterol Inhiba sinteza h steroidieni
↑ permeabilitatea mb
Inhiba sinteza h steroidieni

Ketoconazol L
-Actiune: fungistatic-fungicid
-Mecanism: inhiba C 14 α sterol-demetilaza (CYP 450) → blocheaza transf lanosterol in ergosterol
↑ permeabilitatea mb
Inhiba sinteza h steroidieni
Tulb endocrine ↓ libidou, ginecomastie, oligospermie, impotenta, tulb menstruale
-R adv: inhib CYP 450
↑ toxicitatea ciclosporinei, fenitoinei, terfenadinei, astemizol
↑ Cp antidiabetice → ↓ glicemia
↑ Cp anticoagulante → hemoragii
+ rifampicina (inductor) → ↓ Cp ketoconazol
+ amfotericina → ↓ actiunea ketoconazol
+ antiacide → ↓ absorbtia ketoconazol

Miconazol L Tioconazol ingust

-Spectru + bacterii G+ -Spectru: Nocardia, Malassesia
-Mecanism: inhiba C 14 α sterol-demetilaza (CYP 450) → -Mecanism: inhiba C 14 α sterol-demetilaza (CYP 450) →
blocheaza transf lanosterol in ergosterol blocheaza transf lanosterol in ergosterol
↑ permeabilitatea mb ↑ permeabilitatea mb
Inhiba sinteza h steroidieni Inhiba sinteza h steroidieni
 Fluconazol L Itraconazol L
-Mecanism: inhiba C 14 α sterol-demetilaza (CYP → hidroxi-itraconazol activ
450) → blocheaza transf lanosterol in ergosterol -Mecanism: inhiba C 14 α sterol-demetilaza (CYP
↑ permeabilitatea mb 450) → blocheaza transf lanosterol in ergosterol
≠ Inhiba sinteza h steroidieni ↑ permeabilitatea mb
≠ Tulb endocrine ≠ Inhiba sinteza h steroidieni
-PF Omicral cp, Orungal cps

Terbinafina L Naftifina L
-Adm local si oral -Adm local
-Mecanism: inhibă selectiv scualen-2,3-epoxidaza fungică -Mecanism: inhibă selectiv scualen-2,3-epoxidaza fungică
→ blocheaza biosinteza ergosterol → blocheaza biosinteza ergosterol

Amarolfina local L -derivat de morfolina

Ciclopirox local L -structura heterociclu

-fol ca sare olamina

Flucitozina ambele ingust

Patrunde in celula → dezaminare la 5-fluoro-uracil → 5-fluoro-uracil-ribozo-monofosfat → 5 FUDP si 5 FUTP ↓ sinteza proteica (ARN)
cu ajutorul unei (5-FU) antimetabolit (acid 5-fluoro-uridilic) → 5 FdUMP inhiba timidilat sintetaza
permeaze citozin-sensibile 5 FUMP (dUMP → dTMP component ARN)

Haloprogin local ingust -struct eter fenolic halogenat,

-fungicid-fungistatic + bactericid coci G+
Nifuratel
Tolnafat local ingust -tiocarbamati
Tolciclat local -fungicid
Trichomonas, giardia, amebiaza

5-nitro-imidazoli 5-nitro-tiazol Chinoline

Metronidazol Emetina Tenonitrazol Clorochina

-electie in amebioza hepatica si -alternativa a metronidazolului -4-amino-chinolina
dizenterie amebioza acuta -se acumuleaza -antimalaric
-se concentreaza in ficat -acumulare in ficat
Tinidazol -alternativa a metronidazolului in
Dehidro-emetina amebiaza hepatica
Nimorazol
+ metronidazol/ paromomicina
Ornidazol Mepacrina (quinacrina)
in dizenterie
Secnidazol + clorochina in amebiaza -colorant acridinic
hepatica -antimalaric
-acumulare
Diloxanid furoat
-diclor-acetamida-ester furonic Clorchinaldol
-activ pe chisturi -8-hidroxi-chinolina
-antiseptice intestinale
Paromomicina -abs p.o ↓
-absorbtie p.o ↓
-utilizat amebiaza intestinala
-lezeaza mb parazitului +
antibacterian asupra microO
normale si patogene (substart
nutritiv)