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Chapter 28 : Phototoxicity Due to Fluoroquinolones

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Phototoxicity Due to Fluoroquinolones, Page 1 of 2

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Abstract:

Particular culprits seen commonly in dermatology practice are the sulfonamide-based diuretics, antimalarials, amiodarone, major tranquillizers, the newer parenterally administered photodynamic therapy agents, and fluoroquinolone antimicrobials (FQs). The clinical presentation of phototoxicity is subdivided into five types: (i) a burning, painful, immediate skin reaction as seen with chlorpromazine and amiodarone; (ii) exaggerated sunburn response maximal at 24 h with thiazide diuretics; (iii) 72 to 96-hour delayed erythema and blistering seen with psoralens; (iv) telangiectatic response due to calcium channel antagonists; and (v) a pseudoporphyria response with skin fragility, pigmentation, and blistering induced by numerous agents. Enoxacin (a naphthyridine, like nalidixic acid) induced photosensitivity in Japanese patients, and pefloxacin, another early fluoroquinolone, appeared to have a phototoxic capacity. In addition, photoallergy is an idiosyncratic process that requires a sensitized immune system suggesting that in susceptible individuals repeated application/exposure to the drug is required. Clinical photosensitivity associated with FQs is dose related and phototoxic in origin, predominantly UVA dependent, and rapidly reversible after drug cessation. Although as a group FQs were initially thought to be mildly phototoxic, it is clear from controlled clinical trial data that some FQs are associated with levels of clinical photosensitivity that would be extremely difficult to prevent either in the hospital or the home environment. Due to the degree of phototoxicity, postphototoxic pigmentation, and photogenotoxicity appear linked, the development of highly phototoxic FQs should be discouraged. Identification of the phototoxic potential using in vitro and in vivo techniques in phase 1 of new FQ development is required.

Citation: Ferguson J. 2003. Phototoxicity Due to Fluoroquinolones, p 451-460. In Hooper D, Rubinstein E (ed), Quinolone Antimicrobial Agents, Third Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817817.ch28
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Figures

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Figure 1

Some members of the quinolone group.

Citation: Ferguson J. 2003. Phototoxicity Due to Fluoroquinolones, p 451-460. In Hooper D, Rubinstein E (ed), Quinolone Antimicrobial Agents, Third Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817817.ch28
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Figure 2

BAY y 3118. Severe photoxic blistering of the backs of hands in a South African Caucasian volunteer.

Citation: Ferguson J. 2003. Phototoxicity Due to Fluoroquinolones, p 451-460. In Hooper D, Rubinstein E (ed), Quinolone Antimicrobial Agents, Third Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817817.ch28
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Figure 3

Persistent abnormal pigmentation noted at monochromator phototest sites in a volunteer 3 months after phototesting on BAY y 3118, 2 00 mg/day.

Citation: Ferguson J. 2003. Phototoxicity Due to Fluoroquinolones, p 451-460. In Hooper D, Rubinstein E (ed), Quinolone Antimicrobial Agents, Third Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817817.ch28
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Figure 4

PI values for a range of FQs.* Sparfloxacin maximal phototoxicity was detected at 400 ± 30 nm. approaching the drug dose-dependent PI values for

Citation: Ferguson J. 2003. Phototoxicity Due to Fluoroquinolones, p 451-460. In Hooper D, Rubinstein E (ed), Quinolone Antimicrobial Agents, Third Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817817.ch28
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References

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Tables

Generic image for table
Table 1

Fluoroquinolone phototoxic index severity grading

Citation: Ferguson J. 2003. Phototoxicity Due to Fluoroquinolones, p 451-460. In Hooper D, Rubinstein E (ed), Quinolone Antimicrobial Agents, Third Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817817.ch28
Generic image for table
Table 2

Median PI estimations for BAY y 3118 (100 and 200 mg/day) and lomefloxacin (400 mg/day)

Citation: Ferguson J. 2003. Phototoxicity Due to Fluoroquinolones, p 451-460. In Hooper D, Rubinstein E (ed), Quinolone Antimicrobial Agents, Third Edition. ASM Press, Washington, DC. doi: 10.1128/9781555817817.ch28

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