Safety and efficacy of doxycycline in the treatment of rosacea

Figures & data

Figure 1 Chemical structure of tetracyclines.

Table 1 Anti-inflammatory effects of doxycycline⁷

Inhibition of mitogen-induced human lymphocytic proliferation by blockage of blast transformation^Citation21

Inhibition of phospholipase A2^Citation22

Inhibition of the expression of nitric oxide synthetase^Citation33,Citation34

Accelerated degradation of nitric oxide synthetase^Citation34

Table 2 Studies of doxycycline in rosacea

Study	No of subjects	Length of trial	Design	Results	Comments
Open-label^Citation24	50	8 weeks	Doxycycline hyclate 20 mg twice daily	80% to 100% clearance of inflammatory lesions and a 50% reduction in erythema	No adverse events reported
Multicenter, randomized, double-blind, placebo-controlled^Citation36	134	16 weeks	Doxycycline hyclate 20 mg twice daily vs placebo	Reduced lesion count (P = 0.009), and global severity score (P = 0.034)	No adverse events reported
Single-center, randomized, double-blind, placebo-controlled^Citation37	40	16 weeks	Doxycycline hyclate 20 mg twice daily plus metronidazole 0.75% lotion vs placebo plus metronidazole 0.75% lotion. Metronidazole discontinued in both groups at week 12	Reduced lesion count (P < 0.01) at week 12 that was maintained at week 16 after 4 weeks of doxycycline as monotherapy (P < 0.01) and decreased global severity score (P = 0.046)	Gastrointestinal events more common in the subantimicrobial-dose doxycycline/metronidazole group (5 vs 2). No cases of photosensitivity or vaginitis reported
Multicenter, randomized double-blind, placebo-controlled^Citation31	573	16 weeks	Doxycycline 40 mg once daily vs placebo	Reduced lesion count (P <.001), decreased erythema score (P = 0.017)	Adverse events were similar in both groups. No cases of photosensitivity or vaginitis reported
Multicenter, randomized double-blind, placebo-controlled^Citation38	72	16 weeks	Doxycycline 40 mg plus metronidazole gel 1% once daily vs metronidazole gel 1% and placebo. Metronidazole discontinued at week 12 in both groups	Reduced lesion count at week 4 (P = 0.008) and at week 12 (P = 0.002), decreased global severity score (P = 0.01) that was maintained through weeks 12 to 16	Improvement receded in the group that received only placebo from week 12 to 16
Multicenter, randomized, double-blind, active-control^Citation39	91	16 weeks	Doxycyline 40 mg plus metronidazole gel 1% once daily vs doxycycline 100 mg plus metronidazole gel 1% once daily	Similar mean change in inflammatory lesion count	Adverse events reported in 26 subjects in the 100 mg group versus 6 subjects in the 40 mg group

Table 3 Adverse events with doxycycline (100 to 200 mg daily)a

Digestive system
Esophageal erosion/ulcer
Heartburn/gastritis
Nausea/vomits
Skin (with/without multisystemic involvement)
Photosensitivity
Photo-onycholysis
Pruritus
Allergic skin symptoms
Acne
Fixed drug eruption
Acute generalized exanthematous eruption
Hypersensitivity reaction
Stevens-Johnson syndrome
Sweet’s syndrome
Rash
Central nervous system
Intracranial hypertension
Dizziness
Urogenital system
Vaginitis
Vaginal candidiasis
Vaginal dryness
Inflamed vulva/thick white discharge
Respiratory system
Rhinitis
Other
Hypoglycemia
Anosmia
Taste perversion
Thrombocytopenia
Minor laboratory abnormalities
Headache
Somnolence
Tooth discoloration
Temporary bone growth inhibition

a Based on case reports and clinical trials of Smith et al.⁵⁹

Table 4 Available formulations of doxycycline⁹²

Active ingredient	Dosage form	Strength	Proprietary name	Generic availability
Doxycycline	Capsule; delayed release	40 mg	Oracea	No
Doxycycline monohydrate	Capsule	50 mg, 75 mg, 100 mg	Monodox	Yes
Doxycycline hyclate	Capsule	50 mg, 100 mg	Vibramycin	Yes
Doxycycline monohydrate	Suspension	25 mg/5 mL	Vibramycin	Yes
Doxycycline calcium	Suspension	50 mg/5 mL	Vibramycin	No
Doxycycline hyclate	Capsule; delayed release	75 mg, 100 mg	N/A	Yes
Doxycycline hyclate	Tablet	20 mg	Periostat	Yes
Doxycycline hyclate	Tablet	100 mg	Vibra-tabs	Yes
Doxycycline hyclate	Tablet; delayed release	75 mg, 100 mg, 150 mg	Doryx	No

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