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Doxycycline

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From Pharmacopedia
Doxycycline
Vibramycin, Doryx, Oracea, Adoxa, Monodox, Acticlate

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Summary
Common uses
Community-acquired pneumonia (atypical coverage)0, Inflammatory acne0, Rosacea0, Rickettsial infections including Rocky Mountain spotted fever0, Lyme disease0, Malaria prophylaxis0, Post-exposure prophylaxis for bacterial STIs (doxy-PEP)0, Chlamydia infections0
Pharmacy
Starting dose
100 mg PO BID; rickettsial 200 mg/d; doxy-PEP 200 mg within 72 hours after condomless sex
Preparations
50 mg, 75 mg, 100 mg, 150 mg tablets and capsules; delayed-release; suspension; IV
US FDA Max
~200 mg/d for most indications; higher doses for severe infections
Pharmacology
Routes
Oral, IV
Onset
Hours
Duration
12 hours
Half-life
16-22 hours[1]
Bioavailability
~95% (oral; reduced by dairy, antacids, iron via divalent-cation chelation, though less than for tetracycline itself)[1]
Pregnancy
Avoid in pregnancy and in children <8 years where alternatives exist (dental staining, possible effect on developing bone); life-threatening rickettsial disease is the recognized exception where benefit outweighs.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Doxycycline binds reversibly to the 30S bacterial ribosomal subunit and blocks aminoacyl-tRNA from accessing the A site, inhibiting protein synthesis; the resulting effect is bacteriostatic against a broad range of gram-positives, atypicals, spirochetes, and intracellular organisms.0 Pleiotropic non-antibiotic effects (matrix metalloproteinase inhibition) underlie efficacy in rosacea and the periodontitis-adjuvant indication at sub-antimicrobial doses. Photosensitivity, pill-induced esophagitis (take with water, remain upright), and esophageal/oral candidiasis are characteristic adverse effects[1].

References

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  1. 1.0 1.1 1.2 FDA Prescribing Information, Vibramycin (doxycycline), Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/050006s083lbl.pdf