Is Ilosone Safe for Use?

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Is Ilosone Safe for Use?

Updated February 12, 2011

3 minute read

Studies reveal that the erythromycin estolate causes hepatotoxicity or liver damage. The textbook Pharmacognosy 9th edition cites that the high incidence of cholestatic jaundice in adults taking erythromycin with the estolate salt had made some doctors limit the use of this antibiotic for young children.

Ilosone, originally manufactured by Eli Lilly but now under GlaxoSmithKline, is a brand name of erythromycin estolate. It is available in liquid form designed for kids. Ilosone’s leaflet or insert include a contraindication for cholestatic hepatitis, jaundice and pre-existing liver disease but not a mention that Ilosone can cause hepatotoxicity as a side effect. We may wonder if the manufacturer could be covering up for their product.

Erythromycin formulations

Erythromycin has various dosage forms and salts. It can be in tablet, capsule, suspension, drops, as an injection (parenteral) and in eye (ophthalmic)/ ear (otic) solution types. Each dosage form has its own salt.

The erythromycin with the salt stearate for instance is usually in tablet form; the succinate in suspension oral liquid types; while the erythromycin gluceptate and lactobionate for parenteral use.

Ilosone formulation

Unlike the stearate salt that is normally in film coated tablet form, estolate is acid stable. The acidity in the stomach cannot affect it. Thus, erythromycin estolate can be in capsule or in simple tablet type. On the contrary, Ilosone is only available in liquid form- in a 100mg drops, 125mg and 250 suspension. There are no Ilosone available in tablet or capsule types.

Image by the author

There are some manufacturers who produce estolates in capsule and tablet forms though. Some of these are YSP industries, Schwitz Biotech and Taj Pharmaceuticals Ltd.

Among the three manufacturers, YSP industries mentioned hepatotoxicity as one of the adverse reactions of their product which is in capsule form.

So does this means, erythromycin estolate is safer in children than in adults? Is the manufacturer of Ilosone merely playing safe?

Macrolides and hepatotoxicity

In majority, macrolides have a special precaution with liver diseases. Listed below are the different macrolides- those that cite special precaution with liver damage and the ones giving a warning about it. The erythromycin is included as it is also categorized as a macrolide.

With a special precaution to liver damage:

Erythromycin stearate

Erthromycin ethylsuccinate

Eythromycin estolate

Josamycin

Roxithromycin

With a warning about liver toxicity:

Azithromycin

Clarithromycin

Erythromycin ethylsuccinate

Erythromycin estolate and drug induced cholestasis

Unfortunately, estolate is the only erythromycin salt and the only macrolide that can cause drug induced cholestasis - a slowing of the flow of bile from the liver that result from medication use. Other drugs that can slow or stop the flow of bile from the liver to the gallbladder and gut, which may damage the liver, are the following: Ampicillin and other penicillin-based antibiotics, anabolic steroids, chlorpromazine, cimetidine, estradiol, gold salts, imipramine, nitrofurantoin, oral contraceptives, prochlorperazine, sulindac, terbinafine and tolbutamide.

Drug recalls

Erythromycin estolate was noted as a dangerous antibiotic but why hasn’t been it recalled?

Drug recalls have two basic considerations:

(1) If it has been found to be unsafe for the consumers.

(2) If it had violations to some drug authority requirements.

However, drugs may remain in the market based upon the negotiation between the manufacturers and the drug authority.

So, is Ilosone safe for use?

Ilosone has been in the market for decades and till now, still under the name of a reliable manufacturer. The danger of estolate still remains same as other antibiotics. The liver can be damaged for prolonged use. Erythromycin estolate should not be used for more than ten days and if an individual has a liver problem, this antibiotic is definitely not for him.

References:

Pharmacognosy 9th edition

Philippine Pharmaceutical Directory 5th edition

Wilson and Gisvold’s Textbook of Organic Medicinal and Pharmaceutical Chemistry 4th edition

MIMS Philippines

http://www.nlm.nih.gov/medlineplus/ency/article/000218.htm

http://www.mims.com/Page.aspx?menuid=mng&name=Erythromycin+YSP+cap&brief=true&h=erythromycin,estolate&CTRY=MY&searchstring=erythromycin+estolate

http://heinonline.org/HOL/LandingPage?collection=journals&handle=hein.journals/foodlj27&div=90&id=&page=

http://books.google.com.ph/books?id=6m6GsOiiXWUC&pg=PA290&lpg=PA290&dq=what+are+the+basis+for+drug+recalls&source=bl&ots=NS0tWXaGbH&sig=MNG2ytaeb8nV7DJbhHjn94zxyRU&hl=tl&ei=XKdOTfSYNoykvgOFncDXDw&sa=X&oi=book_result&ct=result&resnum=7&ved=0CE4Q6AEwBg#v=onepage&q=what%20are%20the%20basis%20for%20drug%20recalls&f=false

http://www.suddenlysenior.com/braunblackbox.html

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