ÇÀËÀÈÍ: ÂÛÑÎÊÎÝÔÔÅÊÒÈÂÍÛÉ ÏÐÎÒÈÂÎÃÐÈÁÊÎÂÛÉ ÏÐÅÏÀÐÀÒ

ÎÃËßÄ
Èíôîðìàöèÿ êîìïàíèè
“ÑìèòÊëÿéí Áè÷åì
Ôàðìàñüþòèêàëç”
Êëþ÷åâûå ñëîâà: ìèêîçû, ëå÷åíèå,
ñåðòàêîíàçîë, ÇÀËÀÈÍ.
ÇÀËÀÈÍ:
ÂÛÑÎÊÎÝÔÔÅÊÒÈÂÍÛÉ
ÏÐÎÒÈÂÎÃÐÈÁÊÎÂÛÉ
ÏÐÅÏÀÐÀÒ
Ðåçþìå.  îáçîðå ïðåäñòàâëåíû ðåçóëüòàòû èññëåäîâàíèé ýôôåêòèâíîñòè ïðåïàðàòà ÇÀËÀÈÍ (ñåðòàêîíàçîë) â ëå÷åíèè áîëüíûõ ñ ðàçëè÷íûìè ôîðìàìè ìèêîçîâ. Äàííûå ñâèäåòåëüñòâóþò î âûñîêîé ýôôåêòèâíîñòè ïðåïàðàòà, øèðîêîì ñïåêòðå åãî äåéñòâèÿ, íåçíà÷èòåëüíîì êîëè÷åñòâå ïîáî÷íûõ ýôôåêòîâ.
 ïîñëåäíèå ãîäû îòìå÷åí ðîñò çàáîëåâàåìîñòè
ìèêîçàìè. Ïî ñòàòèñòèêå îêîëî1/5 âñåãî íàñåëåíèÿ çåìíîãî øàðà ñòðàäàåò òîé èëè èíîé ôîðìîé ìèêîçîâ.
Ðàçâèòèå ãðèáêîâîé èíôåêöèè îáû÷íî çàâèñèò
îò êîëè÷åñòâà ãðèáêîâûõ êëåòîê, âíåäðÿþùèõñÿ â
îðãàíèçì ÷åðåç ïîâðåæäåííóþ êîæó èëè ñëèçèñòûå
îáîëî÷êè, è îò åãî ðåçèñòåíòíîñòè. Òÿæåñòü èíôåêöèè îáóñëîâëåíà èììóííûì îòâåòîì îðãàíèçìà íà
âíåäðåíèå ïàòîãåííîãî àãåíòà.
Âëèÿíèå ìíîãèõ ñåíñèáèëèçèðóþùèõ ôàêòîðîâ è
íåîáîñíîâàííîå ïðèìåíåíèå àíòèñåïòè÷åñêèõ
ñðåäñòâ è àíòèáèîòèêîâ, êîòîðûå èçìåíÿþò íîðìàëüíûé ñîñòàâ ìèêðîôëîðû, ïðèâåëî ê òîìó, ÷òî ïàòîãåííîñòü ãðèáîâ èçìåíèëàñü. Íàëè÷èå ìèêîçîâ,
óñòîé÷èâûõ ê ëå÷åíèþ èçâåñòíûìè ïðîòèâîãðèáêîâûìè ïðåïàðàòàìè, à òàêæå ðàñïðîñòðàíåíèå ÑÏÈÄà
âíåñëî îïðåäåëåííûå èçìåíåíèÿ â ïîêàçàòåëè çàáîëåâàåìîñòè ãðèáêîâûìè èíôåêöèÿìè è èõ êëèíè÷åñêèå ïðîÿâëåíèÿ. Êðîìå òîãî, íåäàâíî áûëè âûäåëåíû íåèçâåñòíûå ðàíåå âèäû ãðèáîâ, ïàòîãåííûõ äëÿ
÷åëîâåêà: Scopulariopsis brevicaulis è Trichosporon beigelii.
 íàñòîÿùåå âðåìÿ âî âñåì ìèðå ïðîâîäÿòñÿ íàó÷íûå èññëåäîâàíèÿ, ïîñâÿùåííûå ðàçðàáîòêå áîëåå ýôôåêòèâíûõ è áåçîïàñíûõ ïðîòèâîãðèáêîâûõ
ïðåïàðàòîâ. Èññëåäîâàòåëè “Ferrer Group Research
Centre” (Èñïàíèÿ) ðàçðàáîòàëè âåùåñòâî, ñîäåðæàùåå 1-(2-àðèë-2-çàìåùåííóþ-ýòèë) àçîëîâóþ ãðóïïó ñ âûðàæåííûì ïðîòèâîãðèáêîâûì äåéñòâèåì è
áåíçî(b)òèîôåíîâóþ ãðóïïó. Ïîñëåäíÿÿ, îêàçûâàÿ
ôóíãèöèäíîå äåéñòâèå è ÿâëÿÿñü âûñîêîëèïîôèëüíûì ôðàãìåíòîì, óñèëèâàåò ìåñòíîå äåéñòâèå ýòèõ
êîìïîíåíòîâ, çíà÷èòåëüíî ïîâûøàÿ èõ ïðîíèêíîâåíèå â êîæó è åå ïðèäàòêè.
Íà îñíîâå ýòîãî âåùåñòâà áûë ñîçäàí ñåðòàêîíàçîë, ïðîäâèãàåìûé íà óêðàèíñêîì ðûíêå êîìïàíèåé “ÑìèòÊëÿéí Áè÷åì Ôàðìàñüþòèêàëç” (Âåëèêîáðèòàíèÿ) ïîä òîðãîâûì íàçâàíèåì ÇÀËÀÈÍ —
ïåðâûé â ìèðå ïðîòèâîãðèáêîâûé ïðåïàðàò — ïðîèçâîäíîå áåíçîòèîôåíà è èìèäàçîëà, îêàçûâàþùèé
êàê ôóíãèñòàòè÷åñêîå, òàê è ôóíãèöèäíîå äåéñòâèå
ïðè ïðèìåíåíèè â òåðàïåâòè÷åñêèõ äîçàõ. Ñåðòàêîíàçîë îáëàäàåò øèðîêèì ñïåêòðîì äåéñòâèÿ â
îòíîøåíèè âîçáóäèòåëåé, âûçûâàþùèõ èíôåêöèè
êîæè è ñëèçèñòûõ îáîëî÷åê: ïàòîãåííûõ äðîææåâûõ ãðèáîâ (Candida albicans, C. tropicalis, C. pseudotropicalis, C. krusei, C. parapsilosis, C. neoformans;
Torulopsis, Trichosporon è Malassezia), äåðìàòîôèòîâ
(Trichophyton, Microsporum è Epidermophyton), ôèëàìåíòíûõ ãðèáîâ-îïïîðòóíèñòîâ* (Scopulariopsis,
Altermania, Acremonium, Aspergillus è Fusarium), ãðàìïîëîæèòåëüíûõ (ñòàôèëîêîêêè è ñòðåïòîêîêêè,
L. monocytogenes) è ãðàìîòðèöàòåëüíûõ ìèêðîîðãàíèçìîâ (E. faecium, E. faecalis, Corynebacterium spp.,
Bacteroides spp., P. acnes), ïðåäñòàâèòåëåé ðîäà Trichomonas. ÇÀËÀÈÍ âûñîêîàêòèâåí â îòíîøåíèè øòàììîâ
C. albicans ñåðîòèïîâ A è B (ñðåäíèå çíà÷åíèÿ ìèíèìàëüíîé èíãèáèðóþùåé êîíöåíòðàöèè (ÌÈÊ):
0,21 è 0,65 ìêã/ìë ÷åðåç 24 è 48 ÷ ñîîòâåòñòâåííî), à
òàêæå â îòíîøåíèè óìåðåííî ÷óâñòâèòåëüíûõ è
ðåçèñòåíòíûõ ê ïðîèçâîäíûì èìèäàçîëà øòàììîâ.
 òàáë. 1 ïðåäñòàâëåíà ñðàâíèòåëüíàÿ õàðàêòåðèñòèêà àêòèâíîñòè ðàçëè÷íûõ êëàññîâ ïðîòèâîãðèáêîâûõ ñðåäñòâ è ñåðòàêîíàçîëà â îòíîøåíèè
âîçáóäèòåëåé, âûçûâàþùèõ èíôåêöèîííûå çàáîëåâàíèÿ êîæè è ñëèçèñòûõ îáîëî÷åê.
Òàáëèöà 1
Ñïåêòð àêòèâíîñòè ðàçëè÷íûõ êëàññîâ ïðîòèâîãðèáêîâûõ ñðåäñòâ
ÏðîòèâîÂîçáóäèòåëè
ãðèáêîâûå
Äåðìà- Äðîææå- Ïëåñíåâûå Áàêòå- Ðåçèñòåíòïðåïàðàòû
òîôèòû âûå ãðèáû
ãðèáû
ðèè íûå ãðèáû *
Ïîëèåíû
—
++
++
—
?
Òèîêàðáàìàòû
++
—
—
—
?
5-Ôòîðöèòîçèí
—
++
—
—
—
Èìèäàçîëû
+++
+++
—
±
±
Ïèðèäîíû
+++
+++
++
++
?
Àëëèëàìèíû
+++
—
?
±
±
Ñåðòàêîíàçîë
+++
+++
++
+++
+++
Ìîðôîëèíû
+++
+++
?
?
±
* Ãðèáû ñ ïåðåêðåñòíîé óñòîé÷èâîñòüþ ê èìèäàçîëàì è 5-ôòîðöèòîçèíó.
ÇÀËÀÈÍ èìååò äâîÿêèé ìåõàíèçì äåéñòâèÿ, ÷òî
îáóñëîâëåíî íàëè÷èåì â åãî ñòðóêòóðå êàê òðàäèöèîííîãî äëÿ èìèäàçîëîâ àçîëîâîãî êîëüöà, òàê è ïðèíöèïèàëüíî íîâîãî ñîåäèíåíèÿ — áåíçîòèîôåíà (ðèñ. 1).
* Ãðèáàìè-îïïîðòóíèñòàìè íàçûâàþòñÿ ñàïðîôèòíûå ãðèáû, êîòîðûå ïðîÿâëÿþò ïàòîãåííîñòü ïðè èììóíîêîìïðîìèññå.
Ó Ê Ð À ¯ Í Ñ Ü Ê È É Ì Å Ä È × Í È É × À Ñ Î Ï È Ñ – ¹ 4 (12) – VII/VIII 1 9 9 9
27
ÎÃËßÄ
ýôôåêòèâíîñòè ðàçëè÷íûõ ïðîòèâîãðèáêîâûõ
ñðåäñòâ è ñåðòàêîíàçîëà ïðåäñòàâëåíû íà ðèñ. 4.
Ðåçóëüòàòû ìíîãîöåíòðîâûõ ðàíäîìèçèðîâàííûõ èññëåäîâàíèé ïîêàçàëè, ÷òî ñåðòàêîíàçîë ïðîÿâëÿåò ìàêñèìàëüíóþ êëèíè÷åñêóþ ýôôåêòèâíîñòü: 100% — ïðè äåðìàòîôèòîçàõ (Pedragosa R.
et al., 1992) è îòðóáåâèäíîì (ðàçíîöâåòíîì) ëèøàå
(Nassare J. et al., 1992), 95% — ïðè êàíäèäîçå êîæè
(Umbert P. et al., 1992). Ïî íåêîòîðûì äàííûì
(Alomar C. et al., 1992), îáùàÿ êëèíè÷åñêàÿ ýôôåêòèâíîñòü ÇÀËÀÈÍÀ ñîñòàâëÿåò 98,6%.
Ðèñ. 1. Ñòðóêòóðíàÿ ôîðìóëà ñåðòàêîíàçîëà
Àçîëîâàÿ ñòðóêòóðà ïðåïÿòñòâóåò ñèíòåçó ýðãîñòåðèíà — îäíîãî èç îñíîâíûõ êîìïîíåíòîâ ìåìáðàíû ãðèáêîâîé êëåòêè (ôóíãèñòàòè÷åñêîå äåéñòâèå), à áåíçîòèîôåí ïðîâîöèðóåò ðàçðûâ ïëàçìàòè÷åñêîé ìåìáðàíû ãðèáêîâîé êëåòêè, ÷òî ïðèâîäèò
ê åå ãèáåëè (ôóíãèöèäíîå äåéñòâèå) (Agut J. et al.,
1992). Áëàãîäàðÿ âûñîêîé ëèïîôèëüíîñòè áåíçîòèîôåí ãëóáîêî ïðîíèêàåò â êîæó. ×åðåç 2–4 ÷ 59%
íàíåñåííîé äîçû ÇÀËÀÈÍÀ äîñòèãàåò ãëóáîêèõ
ñëîåâ ýïèäåðìèñà (Albert C. et al., 1991), ÷åðåç 24 ÷
72% íàíåñåííîãî ïðåïàðàòà ñîõðàíÿåò àêòèâíîñòü
â ãëóáîêèõ ñëîÿõ ýïèäåðìèñà, ïðè ýòîì äåéñòâèå
ïðåïàðàòà ïðîäîëæàåòñÿ â òå÷åíèå 48 ÷ (Farre M.
et al., 1992).
Ñåðòàêîíàçîë îáëàäàåò ïåðâè÷íîé ôóíãèöèäíîé
àêòèâíîñòüþ, òî åñòü ìèíèìàëüíàÿ ôóíãèöèäíàÿ
êîíöåíòðàöèÿ (ÌÔÊ) ïðèáëèæàåòñÿ ê ìèíèìàëüíîé èíãèáèðóþùåé êîíöåíòðàöèè (ÌÈÊ) (Agut J.
et al., 1992) (ðèñ. 2).
Ðèñ. 3. ÈÔ ðàçëè÷íûõ ïðîòèâîãðèáêîâûõ ïðåïàðàòîâ â îòíîøåíèè Candida
albicans (êîíöåíòðàöèÿ 16 ìêã/ìë)
Òåðàïåâòè÷åñêàÿ êîíöåíòðàöèÿ
Ðèñ. 4. Êëèíè÷åñêàÿ ýôôåêòèâíîñòü ðàçëè÷íûõ ïðîòèâîãðèáêîâûõ
ñðåäñòâ
Ðèñ. 2. ÌÔÊ È ÌÈÊ ñåðòàêîíàçîëà
×åì ìåíüøå èíäåêñ ôóíãèöèäíîñòè (ÈÔ)
(îòíîøåíèå ÌÔÊ ê ÌÈÊ), òåì âûøå ôóíãèöèäíàÿ àêòèâíîñòü ïðîòèâîãðèáêîâîãî ïðåïàðàòà.
Äëÿ ñåðòàêîíàçîëà ÈÔ ïðèáëèæàåòñÿ ê åäèíèöå
(ðèñ. 3).
Âûñîêàÿ êëèíè÷åñêàÿ ýôôåêòèâíîñòü ÇÀËÀÈÍÀ
ïîäòâåðæäåíà ðåçóëüòàòàìè ìèêîëîãè÷åñêèõ èññëåäîâàíèé (O’Neill et al., 1983; Cauwenberg G.F. et al.,
1984; Hay R.J. et al., 1988; Alomar A. et al., 1989). Ïîëíîå âûçäîðîâëåíèå ïîäðàçóìåâàåò êëèíè÷åñêîå èçëå÷åíèå ïðè îäíîâðåìåííîé ýðàäèêàöèè âîçáóäèòåëÿ. Ðåçóëüòàòû ñðàâíèòåëüíûõ èññëåäîâàíèé
28
ÇÀËÀÈÍ îêàçûâàåò âûðàæåííîå ôóíãèöèäíîå
äåéñòâèå, ÷òî ñâîäèò ê ìèíèìóìó ðèñê ðàçâèòèÿ ðåöèäèâîâ ïîñëå ïðîâåäåííîãî êóðñà ëå÷åíèÿ (Alomar C. et al., 1992) (ðèñ. 5).
Ïðèìåíåíèå ïðåïàðàòà ÇÀËÀÈÍ ïðèâîäèò ê
ýðàäèêàöèè ðàçëè÷íûõ âèäîâ ãðèáîâ, â òîì ÷èñëå
ðîäà Candida è Trichophyton rubrum — âèäà, ÷àñòî ðåçèñòåíòíîãî ê ïðîòèâîãðèáêîâîé òåðàïèè (Raga M.
et al., 1986; Multicenter double-blind trial on the efficacy
and safety of sertaconazole 2% cream in comparison with
miconazole 2% cream in patients suffering from cutaneous mycoses, 1989) (ðèñ. 6).
Íåðåäêî ïîâåðõíîñòíûå ìèêîçû îñëîæíÿþòñÿ
âòîðè÷íîé áàêòåðèàëüíîé èíôåêöèåé. Êðîìå âûðàæåííîãî ïðîòèâîãðèáêîâîãî äåéñòâèÿ ÇÀËÀÈÍ
Ó Ê Ð À ¯ Í Ñ Ü Ê È É Ì Å Ä È × Í È É × À Ñ Î Ï È Ñ – ¹ 4 (12) – VII/VIII 1 9 9 9
ÎÃËßÄ
Ðèñ. 5. ×àñòîòà ðàçâèòèÿ ðåöèäèâîâ ïðè ïðèìåíåíèè ñåðòàêîíàçîëà è
ìèêîíàçîëà
ÇÀËÀÈÍ îêàçûâàåò òàêæå ïðîòèâîâîñïàëèòåëüíîå äåéñòâèå. Â îäíîì èç èññëåäîâàíèé, â êîòîðîì
àñåïòè÷åñêîå âîñïàëåíèå èíäóöèðîâàëè êðîòîíîâûì ìàñëîì, áûëî ïðîäåìîíñòðèðîâàíî, ÷òî ïðèìåíåíèå ÇÀËÀÈÍÀ â ôîðìå êðåìà óìåíüøàåò îòåê
íà 39,8% (Agut J. et al., 1996).
Ëå÷åíèå ïðîòèâîãðèáêîâûìè ïðåïàðàòàìè äëÿ
ìåñòíîãî ïðèìåíåíèÿ íåðåäêî ñîïðîâîæäàåòñÿ
ðàçëè÷íûìè ïîáî÷íûìè ýôôåêòàìè, ñâÿçàííûìè
â îñíîâíîì ñ àëëåðãè÷åñêèìè ðåàêöèÿìè è íåïåðåíîñèìîñòüþ ïðåïàðàòà.  îòíîøåíèè áåçîïàñíîñòè è ïåðåíîñèìîñòè ÇÀËÀÈÍ ïðåâîñõîäèò ëþáîé
äðóãîé ïðåïàðàò äëÿ ìåñòíîãî ïðèìåíåíèÿ (O’Neill
et al., 1983; Cauwenberg G.F. et al., 1984; Hay R.J. et al.,
1988; Multicenter double-blind trial on the efficacy and
safety of sertaconazole 2% cream in comparison with
miconazole 2% cream in patients suffering from
cutaneous mycoses, 1989). Ðåçóëüòàòû ñðàâíèòåëüíîãî èññëåäîâàíèÿ ïîáî÷íûõ ýôôåêòîâ ðàçëè÷íûõ
ïðîòèâîãðèáêîâûõ ïðåïàðàòîâ ïðåäñòàâëåíû íà
ðèñ. 7.
Ðèñ. 6. Ýðàäèêàöèÿ ðàçëè÷íûõ âîçáóäèòåëåé ïðè ïðèìåíåíèè ñåðòàêîíàçîëà, %
îáëàäàåò àíòèáàêòåðèàëüíûì ñâîéñòâîì. Ïðåïàðàò
àêòèâåí êàê â îòíîøåíèè ïåðâè÷íûõ âîçáóäèòåëåé
èíôåêöèè êîæè (S. aureus, S. pyogenes), òàê è âîçáóäèòåëåé-îïïîðòóíèñòîâ (Staphylococcus epidermidis,
Corynebacterium è Bacteroides), à òàêæå ïðîñòåéøèõ
ðîäà Trichomonas (Prats G. et al., 1995). ÌÈÊ ðàçëè÷íûõ ïðîòèâîãðèáêîâûõ ïðåïàðàòîâ â îòíîøåíèè
íåêîòîðûõ ãðàìïîëîæèòåëüíûõ è ãðàìîòðèöàòåëüíûõ ìèêðîîðãàíèçìîâ ïðåäñòàâëåíû â òàáë. 2.
Òàáëèöà 2
ÌÈÊ ðàçëè÷íûõ ïðîòèâîãðèáêîâûõ ïðåïàðàòîâ
Âîçáóäèòåëü
ÌÈÊ, ìã/ë
Áèôîíàçîë Êåòîêîíàçîë Ñåðòàêîíàçîë
ÃÐÀÌÏÎËÎÆÈÒÅËÜÍÛÅ ÁÀÊÒÅÐÈÈ
4–16
Íå àêòèâåí
4
S. aureus
4–16
Íå àêòèâåí
4
S. epidermidis
4–16
Íå àêòèâåí
1
S. pyogenes
4–16
Íå àêòèâåí
4
S. agalactiae
—
—
8
L. monocytogenes
ÃÐÀÌÎÒÐÈÖÀÒÅËÜÍÛÅ ÁÀÊÒÅÐÈÈ
—
—
2
E. faecium
—
—
8
E. faecalis
—
—
0,5
Corynebacterium spp.
—
—
8
Bacteroides spp.
—
—
4
P. acnes
Ðèñ. 7. Ðàçâèòèå ïîáî÷íûõ ýôôåêòîâ ïðè ïðèìåíåíèè ðàçëè÷íûõ ïðîòèâîãðèáêîâûõ ïðåïàðàòîâ, %
Ïðè ïðèìåíåíèè ÇÀËÀÈÍÀ íå çàðåãèñòðèðîâàíî ñëó÷àåâ êîíòàêòíîãî äåðìàòèòà (Alomar C. et al.,
1992), ïðåïàðàò íå âûçûâàåò ðàçâèòèÿ ðåàêöèé ôîòîñåíñèáèëèçàöèè (Grau M.T. et al., 1992) è íå îêàçûâàåò ñèñòåìíîãî äåéñòâèÿ (Farre M. et al., 1992).
Íåñìîòðÿ íà ãëóáîêîå ïðîíèêíîâåíèå ïðåïàðàòà â
êîæó è åå ïðèäàòêè, à òàêæå äëèòåëüíîå ñîõðàíåíèå àêòèâíîñòè, óðîâåíü ñèñòåìíîé àáñîðáöèè ÇÀËÀÈÍÀ íàñòîëüêî íèçêèé, ÷òî ïîñëå íàðóæíîãî
ïðèìåíåíèÿ ñåðòàêîíàçîë íå îïðåäåëÿåòñÿ â êðîâè
÷åëîâåêà (Farre M. et al., 1992). Ðåçóëüòàòû òîêñèêîëîãè÷åñêèõ èññëåäîâàíèé ïîêàçàëè, ÷òî ñåðòàêîíàçîë áåçîïàñåí â ñëó÷àå ïåðåäîçèðîâêè, åãî ìîæíî
ïðèìåíÿòü äëèòåëüíî áåç íåãàòèâíûõ ïîñëåäñòâèé
äëÿ îðãàíèçìà.
 1993 ã. çà ñîçäàíèå ïðåïàðàòà ÇÀËÀÈÍ èññëåäîâàòåëÿì “Ferrer Group Research Centre” áûëà ïðèñóæäåíà ïðåìèÿ Ãàëåíà â îáëàñòè èññëåäîâàíèÿ è ðàçðàáîòêè ëåêàðñòâåííûõ ñðåäñòâ.  1995 ã. ÇÀËÀÈÍ
áûë âêëþ÷åí â Åâðîïåéñêóþ Ôàðìàêîïåþ.
Ó Ê Ð À ¯ Í Ñ Ü Ê È É Ì Å Ä È × Í È É × À Ñ Î Ï È Ñ – ¹ 4 (12) – VII/VIII 1 9 9 9
29
ÎÃËßÄ
ËÈÒÅÐÀÒÓÐÀ
Agut J. et al. (1992) Direct membrane damaging effect of
Sertaconazole on Candida albicans as a mechanism of its fungicidal
activity. Arzneim.-Forsch. Drug Res., 42 (5à): 721–724.
Agut J. et al. (1996) Centro de Investigacion Grupo Ferrer,
Barcelona. Methods Findings Exp. Clin. Pharmacol., 18(4); 233–234.
Albert C. et al. (1991) Propiedades fisico-quimicas, determinaciones analiticas y estabilidad de nitrato de Sertaconazol. Centro
de Investigacion grupo Ferrer. Barcelona.
Alomar A. et al. (1989) Multicenter Phase III study to evaluate
the efficacy and safety of sertaconazole 2% cream as compared to
miconazole 2% cream in patients with cutaneous mycoses. XVIII
Cong. Nac. Acad. Esp. Dermatol., p. 97.
Alomar C. et al. (1992) Multi-centre double-blind trial on the
efficacy and safety of Sertaconazole 2% cream in comparison with
Miconazole 2% cream in patients suffering from cutaneous mycoses.
Arzneim.-Forsch. Drug Res., 42 (5a): 767–773.
Cauwenberg G.F. et al. (1984) Topical ketoconazole in
dermatology: A pharmacological and clinical review. Mykosen,
27(8): 395–401.
Farre M. et al. (1992) Pharmacokinetics and tolerance of
Sertaconazole in man after repeated percutaneous administration.
Arzneim.-Forsch. Drug Res., 42(5a): 752–754.
Grau M.T. et al. (1992) Dermal tolerance and phototoxicity
studies of Sertaconazole. Arzneim.-Forsch. Drug Res., 42(5a):
746–747.
Hay R.J. et al. (1988) Avances en el tratamiento topico de las
micosis. Springer-Verlag.
Multicenter double-blind trial on the efficacy and safety of
sertoconazole 2% cream in comparison with miconazole 2% cream
in patients suffering from cutaneous mycoses (1989) XVIII Cong.
Nac. Acad. Espan. Dermatol. (June 1–3, 1989, Sevilla), p. 97.
Nassare J. et al. (1992) Therapeutic efficacy and safety of the
new antimycotic Sertaconazole in the treatment of Pityriasis
versicolor. Arzneim.-Forsch. Drug Res., 42(5a): 764–767.
O’Neill et al. (1983) Tioconazole in the treatment of fungal
infections of the skin. An International Clinical Research Program.
Dermatologia, 166: 20–33.
Pedragosa R. et al. (1992) Therapeutic efficacy and safety of
the new antimycotic Sertaconazole in the treatment of cutaneous
dermatophytosis. Arzneim.-Forsch. Drug Res.
Prats G. et al. (1995) Servicio de microbiologia, Hosptal de la Sta.
Creu I Saint Pau, Barcelona, Rev. Esp. Quimoiterap., 8(4): 325–326.
ÐÅÔÅÐÀÒÈÂÍÀ
Ìíîãîöåíòðîâîå äâîéíîå ñëåïîå èññëåäîâàíèå
ýôôåêòèâíîñòè è áåçîïàñíîñòè ïðèìåíåíèÿ
2% êðåìà ñåðòàêîíàçîëà â ñðàâíåíèè ñ 2% êðåìîì
ìèêîíàçîëà ó ïàöèåíòîâ ñ ìèêîçàìè êîæè
Alomar C., Bassas S., Casas M., Crespo V., Fonseca E., et al.
(1992) Multicentre double-blind triàl on efficacy and safety of
sertaconazole 2% cream in comparison with miconasol 2% cream in
patients suffering from cutaneous mycoses [published erratum appears
in Arzneimittelforschung 1992 Jun;42(6):884]. Arzneimittelforschung,
42(5A):767-773.
Ýôôåêòèâíîñòü è ïåðåíîñèìîñòü 2 % êðåìà (7õëîðî-3-[1-2,4- äèõëîðîôåíèë- 1- èë)ýòîêñèìåòèë]
áåíçî[b] òèîôåíà (ñåðòàêîíàçîë, FI-7045, CAS
99592-32,2)), íàíîñèìîãî 2 ðàçà â äåíü, è 2% êðåìà
ìèêîíàçîëà, íàíîñèìîãî 2 ðàçà â äåíü, èçó÷åíà ó 631
ïàöèåíòà ñ ïîâåðõíîñòíûìè ìèêîçàìè êîæè (ñåðòàêîíàçîë — ó 317, ìèêîíàçîë — ó 314) â äâîéíîì
ñëåïîì êîíòðîëèðóåìîì ìíîãîöåíòðîâîì èññëåäîâàíèè ñ ïàðàëëåëüíûìè ãðóïïàìè. Òåðàïåâòè÷åñêóþ ýôôåêòèâíîñòü ïðåïàðàòîâ îöåíèâàëè ïî êëèíè÷åñêè îïðåäåëÿåìîìó óëó÷øåíèþ êëèíè÷åñêîãî
ñîñòîÿíèÿ ïàöèåíòîâ è óìåíüøåíèþ âûðàæåííîñòè ñèìïòîìîâ, äàííûì ìèêðîñêîïè÷åñêîãî èññëå30
Raga M. et al. (1986) New imidazole antifungal agents, derived
from Benzo(b)thiophene. European Journal of Medicinal Chemistry, 21(4).
Umbert P. et al. (1992) Phase II study of the therapeutic efficacy
and safety of the new antimycotic Sertaconazole in the treatment
of superficial mycoses caused by Candida albicans. Arzneim.Forsch. Drug Res., 42(5a): 757–760.
ÇÀËÀ¯Í: ÂÈÑÎÊÎÅÔÅÊÒÈÂÍÈÉ
ÏÐÎÒÈÃÐÈÁÊÎÂÈÉ ÏÐÅÏÀÐÀÒ
Ðåçþìå.  îãëÿä³ íàâåäåí³ ðåçóëüòàòè äîñë³äæåíü ç
âèâ÷åííÿ åôåêòèâíîñò³ ïðåïàðàòó ÇÀËÀ¯Í (ñåðòàêîíàçîë) ó ë³êóâàíí³ õâîðèõ ç ð³çíèìè ôîðìàìè
ì³êîç³â. Äàí³ ñâ³ä÷àòü ïðî âèñîêó åôåêòèâí³ñòü ïðåïàðàòó, øèðîêèé ñïåêòð éîãî 䳿, íåçíà÷íó ê³ëüê³ñòü
ïîá³÷íèõ åôåêò³â.
Êëþ÷îâ³ ñëîâà: ì³êîçè, ë³êóâàííÿ, ñåðòàêîíàçîë,
ÇÀËÀ¯Í.
ZALAIN: HIGHLY EFFICACIOUS
ANTIMYCOTIC DRUG
Summary. Results of clinical trials of the drug ZALAIN
(sertaconazole) in patients with various forms of cutaneous
mycoses are presented in the review. Data demonstrate
high efficacy of the drug, wide spectrum of its action and
very few side effects.
Key words: mycosis, treatment, sertaconazole,
ZALAIN.
Ïóáëèêàöèÿ ïîäãîòîâëåíà
ïî ìàòåðèàëàì, ïðåäîñòàâëåííûì
ïðåäñòàâèòåëüñòâîì êîìïàíèè
”ÑìèòÊëÿéí Áè÷åì Ôàðìàñüþòèêàëç”
â Óêðàèíå. Àäðåñ ïðåäñòàâèòåëüñòâà:
Êèåâ, Êîíòðàêòîâàÿ ïë., 10À, 3-é ýòàæ
Òåë.: (044) 462–59–47, 490–66–85
²ÍÔÎÐÌÀÖ²ß
äîâàíèÿ íà íàëè÷èå ãèô èëè ìèöåëèÿ â çîíå ïîðàæåíèÿ, êóëüòóðèðîâàíèÿ â öåëÿõ âûÿâëåíèÿ àêòèâíîé èíôåêöèè. Ïåðåíîñèìîñòü è áåçîïàñíîñòü îöåíèâàëè íà îñíîâàíèè äàííûõ îáùåãî àíàëèçà êðîâè, îïðîñà ïàöèåíòîâ íà ïðåäìåò íàëè÷èÿ ïîáî÷íûõ
ýôôåêòîâ. Ñòåïåíü êëèíè÷åñêîãî èçëå÷åíèÿ â îáåèõ òåðàïåâòè÷åñêèõ ãðóïïàõ ïî îêîí÷àíèè ëå÷åíèÿ
ñîñòàâèëà 95,6% ó ïàöèåíòîâ, ïðèìåíÿâøèõ ñåðòàêîíàçîë, è 88,1% — ìèêîíàçîë, ðàçëè÷èÿ áûëè ñòàòèñòè÷åñêè äîñòîâåðíû. Ïðè ñðàâíèòåëüíîì àíàëèçå ñòàòèñòè÷åñêèõ êðèâûõ âûÿâëåíî, ÷òî ïðè ëå÷åíèè ñåðòàêîíàçîëîì ïàöèåíòû èçëå÷èâàëèñü
áûñòðåå, ÷åì ïðè ëå÷åíèè ìèêîíàçîëîì, ðàçëè÷èÿ
áûëè äîñòîâåðíûìè. Íåãàòèâíûå ðåçóëüòàòû ïðè
ìèêðîñêîïè÷åñêîì èññëåäîâàíèè è êóëüòóðèðîâàíèè ïîäòâåðäèëè áîëåå âûñîêóþ ýôôåêòèâíîñòü
ñåðòàêîíàçîëà ïî ñðàâíåíèþ ñ ìèêîíàçîëîì óæå
÷åðåç 14 äíåé ïîñëå íà÷àëà òåðàïèè. Îòðèöàòåëüíûå
ðåçóëüòàòû ìèêðîáèîëîãè÷åñêèõ èññëåäîâàíèé ïîëó÷åíû ó 98,6% ïàöèåíòîâ, ïðèíèìàâøèõ ñåðòàêîíàçîë, è ó 91,7% — ìèêîíàçîë; ðàçëè÷èÿ áûëè äîñòîâåðíû.
Ó Ê Ð À ¯ Í Ñ Ü Ê È É Ì Å Ä È × Í È É × À Ñ Î Ï È Ñ – ¹ 4 (12) – VII/VIII 1 9 9 9