Oral Tetracycline-Class Drugs in Dermatology: Impact of Food Intake on Absorption and Efficacy
Abstract
:1. Introduction
2. Results
2.1. Tetracycline
2.2. Doxycycline
2.3. Minocycline
2.4. Sarecycline
2.5. Low-Dose Doxycycline and Minocycline Efficacy Data
3. Discussion
4. Conclusions
5. Materials and Methods
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
Correction Statement
References
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Brand and Generic Name/Formulation | Dosage | Half-Life | Package Insert Recommendations Regarding Food | Evidence for Decreased Absorption with Food Intake | Approved Dermatology Indication |
---|---|---|---|---|---|
Tetracycline hydrochloride [12]. | 250 and 500 mg capsules [12]. | - | Food and some dairy products interfere with absorption [12]. | Serum concentrations decreased by approximately 50% [24,25]. | Adjunctive therapy for severe acne [12]. |
Doryx, Doxycycline hyclate delayed-release [22,23]. | 75, 80, 100, 150, 200 mg tablets [22,23]. | - | If gastric irritation occurs, may be administered with food or milk [22,23]. | The mean Cmax was 24% lower (100 mg tablet) [22,23]. The mean AUC was 13% lower (100 mg tablet) [22,23]. The mean Cmax was 19% lower (150 mg tablet) (unknown clinical significance) [22,23]. The AUC was unchanged (150 mg tablet) (unknown clinical significance) [22,23]. Bioavailability was unaffected by food (200 mg tablet) [22]. | Adjunctive therapy for severe acne [22,23]. |
Acticlate, doxycycline hyclate [26]. | 150 mg tablets and capsules [26]. | Range 18–22 h [26]. | If gastric irritation occurs, may be given with food or milk [26]. | The mean Cmax was 24% lower (tablet) (unknown clinical significance) [26]. The mean AUC was 15% lower (tablet) (unknown clinical significance) [26]. The mean Cmax was 20% lower (capsule) (unknown clinical significance [26]. The AUC was unchanged (capsule) [26]. | Adjunctive therapy for severe acne [26]. |
Monodox, doxycycline monohydrate [27]. | 50, 75, and 100 mg capsules [27]. | 16.33 h [27]. | If gastric irritation occurs, may be given with food [27]. | Ingestion of a high-fat meal delayed the Tmax by an average of 1 h and 20 min. However, in the same study, food enhanced the average Cmax by 7.5% and the AUC by 5.7% [27]. | Adjunctive therapy for severe acne [27]. |
Oracea, Doxycycline [28]. | 40 mg capsule [28]. | 21.2 h [28]. | Take at least 1 h prior to or 2 h after meals [28]. | The Cmax decreased by 45% (40 mg dose) [28]. The AUC decreased by 22% (40 mg dose) [28]. | Inflammatory lesions (papules and pustules) of rosacea in adult patients [28]. |
Dynacin, Minocycline hydrochloride [29]. | 50, 75, and 100 mg tablets [29]. | 11.38 to 24.31 h (average 17.03 h) [29]. | May be taken with or without food [29]. | Extent of absorption was decreased by 6% [29]. The Cmax decreased by 12% and was delayed by 1.09 h when administered with food, compared to dosing under fasting conditions [29]. | Adjunctive therapy of severe acne [29]. |
Minocin, Minocycline hydrochloride [14]. | 50 and 100 mg capsules [14]. | 11.1 to 22.1 h (average 15.5 h) [14]. | May be administered with or without food [14]. | Extent of absorption was unchanged compared with dosing under fasting conditions [14]. The mean Tmax was delayed by 1 h when administered with food, compared to dosing under fasting conditions [14]. | Adjunctive therapy for severe acne [14]. |
Minolira, Minocycline hydrochloride extended-release [30]. | 105 and 135 mg tablets [30]. | 15.6 h under fasting conditions and 17.1 h under fed conditions [30]. | May be taken with or without food [30]. Ingestion with food may reduce risk of esophageal irritation and ulceration [30]. | The Cmax was 700 ng/mL under fasting conditions and 707 ng/mL under fed conditions [30]. The Tmax was 2.0 h under fasting conditions and 3.5 h under fed conditions [30]. The AUC was 10,874 ng.hmL under fasting conditions and 12,000 ng.h/mL under fed conditions [30]. | Inflammatory lesions of non-nodular moderate-to-severe acne vulgaris in patients 12 years of age and older [30]. |
Solodyn, Minocycline hydrochloride extended-release [31]. | 45, 55, 65, 80, 90, 105, 115, and 135 mg tablets [31]. | - | May be taken with or without food [31]. Ingestion with food may reduce risk of esophageal irritation and ulceration [31]. | Extent and timing of absorption when administered with a meal that contained dairy products did not differ from that of administration under fasting conditions [31]. | Inflammatory lesions of non-nodular moderate-to-severe acne vulgaris in patients 12 years of age and older [31]. |
Ximino, Minocycline hydrochloride extended-release [32]. | 45, 90, and 135 mg capsules [32]. | - | May be taken with or without food [32]. Ingestion with food may reduce risk of esophageal irritation and ulceration [32]. | The AUC was 17.90 (5.56) mcg × h/mL under fasting conditions and 17.16 (3.19) mcg × h/mL when administered with a high-fat meal [32]. The Cmax was 0.96 (0.32) mcg/mL under fasting conditions and 0.97 (0.25) mcg/mL when administered with a high-fat meal [32]. | Inflammatory lesions of non-nodular moderate-to-severe acne vulgaris in patients 12 years of age and older [32]. |
SEYSARA, Sarecycline [15]. | 60, 100, and 150 mg tablets [15]. | 21–22 h [15]. | May be administered with or without food [15]. | The Cmax decreased by 31% [15]. The AUC decreased by 27% [15]. | Inflammatory lesions of non-nodular moderate-to-severe acne vulgaris in patients 9 years of age and older [15]. |
Treatment | Duration | Patient Population | Efficacy | Other Considerations |
---|---|---|---|---|
Doxycycline hyclate 20 mg tablets BID [35]. | 6 months [35]. | Adults with moderate facial acne [35]. | At 6 months: | - |
Doxycycline hyclate 20 mg tablets BID [36]. | 3 months [36]. | Adults with moderate facial acne [36]. | At 3 months: | Low-dose 20 mg doxycycline treatment was well tolerated [36]. One patient in the low-dose 20 mg doxycycline group dropped out due to nausea and vomiting [36]. Five patients in the antimicrobial dose 100 mg doxycycline group developed esophagitis [36]. |
Doxycycline 40 mg controlled-release capsules once daily [37]. | 16 weeks [37]. | Adults with moderate-to-severe rosacea [37]. | At 16 weeks:
| - |
Doxycycline monohydrate 40 mg capsules once daily [38]. | 16 weeks [38]. | Adults with rosacea [38]. | At 16 weeks:
| - |
Doxycycline 40 mg delayed-release once daily [39]. | 16 weeks [39]. | Adults with moderate-to-severe rosacea [39]. | Both anti-inflammatory 40 mg delayed-release doxycycline and 100 mg doxycycline are equally effective once daily treatments for moderate-to-severe rosacea for up to 16 weeks [39]. | 5% of the subjects receiving 40 mg delayed-release doxycycline exhibited gastrointestinal symptoms compared to 26% of those receiving the 100 mg doxycycline dose [39]. |
Doxycycline 40 mg modified-release once daily [6,9,10]. | 12 weeks [6,9,10]. | Adults with HS [6,9,10]. | HiSCR was achieved in 64% of patients receiving doxycycline 40 mg and 60% of patients receiving doxycycline 100 mg [6,9,10]. | - |
Minocycline 20 mg extended-release capsule once daily and 40 mg extended-release capsule once daily [40]. | 16 weeks [40]. | Adults with mild-to-severe papulopustular rosacea [40]. | A higher proportion of patients who received the minocycline 40 mg ER formulation achieved IGA treatment success (defined as an IGA grade 0 or 1 and ≥2-grade improvement) compared with placebo (66.04% vs. 11.54%; p < 0.0001), doxycycline 40 mg (66.04% vs. 33.33%; p = 0.0010), and minocycline 20 mg ER (66.04% vs. 31.91%; p = 0.007) [40]. Patients who received 40 mg minocycline ER formulation had a greater reduction in inflammatory lesions compared with placebo (−19.2 vs. −7.3; p < 0.0001), doxycycline 40 mg (−19.2 vs. −10.5; p = 0.0004), and minocycline 20 mg ER (−19.2 vs. −12.6 p = 0.0070) [40]. | - |
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Tao, R.E.; Prajapati, S.; Pixley, J.N.; Grada, A.; Feldman, S.R. Oral Tetracycline-Class Drugs in Dermatology: Impact of Food Intake on Absorption and Efficacy. Antibiotics 2023, 12, 1152. https://doi.org/10.3390/antibiotics12071152
Tao RE, Prajapati S, Pixley JN, Grada A, Feldman SR. Oral Tetracycline-Class Drugs in Dermatology: Impact of Food Intake on Absorption and Efficacy. Antibiotics. 2023; 12(7):1152. https://doi.org/10.3390/antibiotics12071152
Chicago/Turabian StyleTao, Rachel E., Stuti Prajapati, Jessica N. Pixley, Ayman Grada, and Steven R. Feldman. 2023. "Oral Tetracycline-Class Drugs in Dermatology: Impact of Food Intake on Absorption and Efficacy" Antibiotics 12, no. 7: 1152. https://doi.org/10.3390/antibiotics12071152