MINOCYCLINE Film-coated tablet Ref.[7903] Active ingredients: Minocycline

Source: Medicines & Healthcare Products Regulatory Agency (GB)  Revision Year: 2019  Publisher: Accord-UK Ltd (Trading style: Accord), Whiddon Valley, Barnstaple, Devon, EX32 8NS

Pharmacodynamic properties

ATC code: J01AA08

Mechanism of action

Minocycline hydrochloride has a spectrum of activity and mode of action similar to that of tetracycline hydrochloride, but it is more active against many species. In addition, it is reported to be effective in vitro, against some tetracycline resistant staphylococci, streptococci and certain strains of tetracycline-resistant Escherichia coli and Haemophilus influenzae.

Pharmacokinetic properties

Absorption

Minocycline is readily absorbed from the GI tract and is not significantly affected by the presence of food or moderate amounts of milk although absorption is impaired by the concomitant administration of iron salts or antacids containing calcium, magnesium or aluminium salts. Normal doses of 200mg followed by 100mg every 12 hours produced plasma concentrations within the range of 1-4μg/ml.

Distribution

It is more lipid-soluble than doxycycline and the other tetracyclines and is widely distributed in body tissues and fluids, including the cerebrospinal fluid. A higher ratio of CSF to blood concentrations has been reported with minocycline than with doxycycline. It crosses the placenta and diffuses into milk of nursing mothers. About 75% of minocycline in the circulation is bound to plasma proteins. The plasma half-life tends to be prolonged in patients with severe renal impairment. It has a lower renal clearance than doxycycline and its plasma half-life ranges from 11-23 hours. It penetrates well into thyroid, lung and liver tissues and in most instances tissue levels exceed serum levels. It also appears in tears and saliva.

Biotransformation

In contrast to most tetracyclines, minocycline appears to undergo some metabolism in the liver, mainly to 9-hydroxyminocycline. It is also excreted in bile.

Elimination

About a third of the drug may be excreted unchanged and although figures vary widely, about a third of this unchanged drug may appear in the urine and two thirds in the faeces.

Preclinical safety data

Not applicable.

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