Table 1.
Daily dose ranges and selected physicochemical and pharmacokinetic properties of currently approved transdermally delivered drugs. (Reprinted from [34] with permission. Copyright 2014 Elsevier).
| Drug (Year of Approval) | Dose/Day (mg) | MW (Da) | Log P a | Cl (L/h) | T1/2 (h)b | F (%) c | Cp,eff (ng/mL) e |
|---|---|---|---|---|---|---|---|
| Scopolamine (1979) | 0.3 | 303 | 0.98 | 672 | 2.9 | 27 | 0.04 |
| Glyceryl trinitrate (1981) | 2.4–15 | 227 | 01.62 | 966 | 0.04 | <1 | 0.1–5 |
| Clonidine (1984) | 0.1–0.3 | 230 | 2.42 ± 0.52 | 13 | 6–20 | 95 | 0.2–2.0 |
| Estradiol (1986) | 0.025–0.1 | 272 | 4.01 | 615–790 | 0.05 | 3-5 | 0.04–0.06 |
| Fentanyl (1990) | 0.288–2.4 | 337 | 4.05 | 27–75 | 3–12 | 32 | 1.0 |
| Nicotine (1991) | 7–21 | 162 | 1.17 | 78 | 2 | 30 | 10–30 |
| Testosterone (1993) | 0.3–5 | 288 | 3.32 | 0.17–1.7 | <1 | 10–100 | |
| Estradiol & Norethisterone Acetate (1998) | 0.025–0.050 0.125–0.250 | 272 340 | 4.01 3.99 | 2–3 6–8 d | 3–5 64 | 0.04–0.07 0.8–1.1 | |
| Norelgestromin & EthinylEstradiol (2001) | 0.025–0.050 0.125–0.250 | 327 296 | 3.90 ± 0.47 3.67 | 28 17 d | 40 | 0.8 0.05 | |
| Estradiol & Levonorgestrel (2003) | 0.025–0.050 0.125–0.250 | 272 312 | 4.01 3.72 ± 0.49 | 3 28 d | 3-5 | 0.03–0.05 0.1–0.2 | |
| Oxybutynin (2003) | 3.9 | 357 | 4.02 ± 0.52 | 2 | 6 | 1.0–5.0 | |
| Selegeline (2006) | 6–12 | 187 | 2.90 | 84 | 10 | 10 | 2.0–3.0 |
| Methylphenidate (2006) | 26–80 | 233 | 2.15 ± 0.42 | 20 | 2–3 | 5–20 | 5.0–25 |
| Rotigotine (2007) | 1–3 | 315 | 4.58 ± 0.72 | 600 | 5–7 d | n/a | ~1.0 |
| Rivastigmine (2007) | 4.6–9.5 | 250 | 2.34 ± 0.16 | 108 | 1.5 | 40 | ~10 |
| Granisetron (2008) | 3.1 | 312 | 2.55 ± 0.28 | 33–76 healthy 15–34 patients |
4–6 healthy 9–12 patients |
60 | 0.7–9.5 |
| Buprenorphine (2010) | 0.12–1.68 | 468 | 4.98 | 55 | 22–36 d | n/a | 0.1–0.4 |
a Log{octanol-water partition coefficient (P)}: either experimental or calculated (mean ± SD) values; b Terminal half-life post-oral or IV dosing; c Oral bioavailability; d Terminal half-life following transdermal delivery; e Pharmacologically effective plasma concentration.