パロモマイシン 化学特性,用途語,生産方法
解説
パロモマイシンⅠ，アミノシジン，チゴマイシンともいう．種々のStreptomyces属菌が産生するアミノグリコシド系抗生物質．培養液より陽イオン交換膜樹脂Amberlite IRC-50に吸着させ，0.5 mol 塩酸で溶出すると得られる．カナマイシンAと同様の機作でグラム陽性菌，陰性菌を阻止する．白色の結晶．[α]25D＋65°(水)．水，メタノールに可溶．細菌性赤痢治療剤，また動物用抗生物質として細菌感染症治療に使用される．LD50 156 mg/kg(ラット，静注)， ＞ 1625 mg/kg(ラット，経口)．
効能
抗生物質, 抗アメーバ薬, タンパク質合成阻害薬
説明
Paromomycin is recommended
for treatment of acute and chronic forms of intestinal amobiasis, as well as for treating
intestinal bacteria Salmonella and Shigella. Synonyms of this drug are aminosidine, catenulin, crestomycin, hydroxymycin, monomycin, zygomycyn, and others.
適応症
The antibacterial activity and indications for using paromomycin are analogous to those of
neomycin. In addition, it is recommended for treating severe and chronic forms of gastric
amebiasis. Synonyms of this drug are aminosidine, catenulin, crestomycin, hydroxymycin,
monomycin, zygomycyn, and others.
世界保健機関（WHO）
Paromomycin, an aminoglycoside antibiotic was introduced into
medicine in 1959 for the treatment of protozoal, helminthic and bacterial infections.
It has been associated, particularly when used by parenteral route, with severe
adverse effects including renal damage, neuromuscular blockage and ototoxicity,
possibly leading to deafness in some patients. This route of administration is now
considered obsolete. However, parenteral dosage forms of paromomycin may still
remain available in certain countries.
抗菌性
A fermentation product of Streptomyces rimosus var. paromomycinus,
supplied as the sulfate. The commercial product is a
mixture of the two isomeric paromomycins I and II, which are
closely related to neomycin.
The antibacterial activity is almost identical to that of neomycin.
Since it differs from neomycin in having a hydroxyl
rather than an amino group at the 6′-position it is not sensitive
to AAC(6′) modifying enzymes. It is active against
M. tuberculosis, including multidrug-resistant strains, and the
M. avium complex.
Unlike other aminoglycosides, paromomycin is active
against some protozoa, including Entamoeba histolytica,
Cryptosporidium parvum, Leishmania spp., Giardia lamblia and
Trichomonas vaginalis. It also exhibits activity against the tapeworms
Taenia saginata, Taenia solium, Diphyllobothrium latum
and Hymenolepis nana.
It closely resembles neomycin in pharmacokinetic behavior
and liability to produce deafness and intestinal malabsorption.
臨床応用
Intestinal amebiasis (oral)
Cutaneous leishmaniasis (topical) and visceral leishmaniasis
(intramuscular)
Nitroimidazole-resistant trichomoniasis (topical)
Its antiprotozoal activity has attracted some attention, but it
has largely been superseded by more active and less toxic compounds.
Success in treating nitroimidazole-resistant trichomoniasis
with topical paromomycin has been reported. Trials in
India and East Africa of parenteral paromomycin alone, or
in combination with sodium stibogluconate, for treatment of
visceral
leishmaniasis have shown promising results.
パロモマイシン 上流と下流の製品情報
原材料
準備製品