Table 1. Physicochemical, pharmacokinetic properties and indications of currently marketed transdermal drugs.
| Drug | Dose/day (mg) | MW (Da) |
MP
(°C) |
Log P | Saq (mg/mL) | Clearance (cl) L.h-1 | t1/2 (h) | Oral F (%) | Plasma Concentration | Estimated Jskin Required (µg/h) | In vivo J skin (µg/cm2/h) | Product name | Indication |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Buprenorphine | 0.12-1.68 | 468 | 209 | 3.8 | 0.047, 0.008 (32°C) | 77 i.v. 55 i.m. |
22-36 | 51 sI 28 bc |
0.1-0.4 | 7.7 | 0.8 | Butrans | Moderate to severe pain |
| Clonidine | 0.1-0.3 | 230 | 130 | 2.7 | 0.17, 13.58 | 15 | 6-20 | 95 | 0.2-2.0 | 3-30 | 1.2 | Catapres- TTS |
Hypertension |
| Ethinyl oestradiol | - | 296 | 141-146 | 4.3 | 0.039, 0.0092 (25°C) | 70 | 7.7 p.o, 17 t.d. | 55 | 0.025-0.075 | 1.75-5.25 | 0.07 | Ortho Evra | Female contraception |
| Fentanyl | 0.288-2.400 | 337 | 83-84 | 3.9 | 0.15, 0.2 (30°C), 0.2 (25°C) |
27-75 | 3-12 | 50 | 1-3 | 27-225 | 2.4 | Duragesic | Chronic pain |
| Granisetron | 3.1 | 312 | 152-154 | 2.6 | 0.017 | 33-76 | 4-6 | 60 | 3.9 (t.d. Mean C max) |
129-296 | 2.5 | Sancuso | Chemotherapy-induced emesis |
| Glyceryl trinitrate | 2.4-15.0 | 227 | 13, liquid | 1 | 0.66, 1.3 (30°C) | 216-3270 | 0.03-0.05 | < 1 | 0.1-5 | 4.32-1308 | 20,30 | Nitro-Dur | Angina |
| Estradiol and Levonorgesterel | 0.050, 0.0007-0.015 | 272, 312 | 173-179 235-237 |
4.2 3.8 |
0.003 (30°C) 0.0015 (25°C) 0.017 |
600-800 5.7 |
Approx. 1p.o. 28t.d19.3p.o. |
3-5 | 0.03-0.05 0.1-0.2 |
24-48 1 |
0.63, 0.09, 0.12, 0.18, 0.14, 0.23, 0.42, 0.17 0.2 0.03 |
Climara Pro | Female contraception |
| Methylphenidate | 26.0 - 80.0 | 233 | 74-75, liquid | 2.1 | 1.8 | 12(d); 21(1) (children 30kg) | 1.5-5 | 5-20 | 5-25 | 60-315 | 88 | Daytrana | ADHD |
| Nicotine | 7.0-21.0 | 162 | -79, liquid | 1.1 | 62,1085 (30°C) | 77 | 2 | 20-45 | 5-30 | 385-2310 | 29, 69, 31, 40 | Nicoderm | Smoking cessation |
| Norelgestromin | 0.2 | 327 | 110-130 | 3.67 | 0.0043 | - | 28 | - | 0.6-1.2 | - | 0.31 | Ortho Evra | Female contraception |
| Norethindrone acetate | 0.125-0.250 | 341 | 161-162 | 3.2 | 0.0065 | 20.6 | 6-8 | 60 | 0.5-0.8 | 10.3-16.5 | 0.65 | Combipatch | Female HRT |
| Oxybutynin | 3.9 | 358 | 56-58 | 4.3 | 10-64 | 2 | 6 | 0.5-5 | 5-192 | 4.2 | Oxytrol | Enuresis | |
| Oestradiol | 0.025-0.100 | 272 | 173-179 | 4.2 | 0.003 (30°C) 0.0015 (25°C) |
600-800 | 0.05 | 3-5 | 0.04-0.06 | 24-48 | 0.2,0.17,0.14, 0.12,0.42,0.18, 0.63,0.23, 0.09 |
VivelleDot | Female HRT |
| Rivastigmine | 4.6-9.5 | 250 | Oil at 25°C | 2.3 | 25 | 108 | 1.5 | 36 | 2.5-20 | 270-2160 | 39 | Exelon | Alzheimer’s disease |
| Rotigotine | 1.0-3.0 | 316 | 75-77 | 4.7 | 0.017 | 600 | 5-7 | - | 0.4-2 | 240-1200 | 8.3 | Neupro | Parkinson’s disease & restless leg syndrome |
| Scopolamine | 0.3 | 303 | 55, liquid | 0.8 | 1.8, 75 (30°C) | 65-121 | 1-5 | 4-27 | 0.04 | 3.25-6.05 | 5.6 | Transderm Scop | Travel sickness |
| Seligiline | 6.0-12.0 | 187 | Liquid at 25°C | 2.7 | 0.73 | 84 | 10 | 4,10 | 2 | 168 | 12.5 | Emsam | Depression |
| Testosterone | 0.3-5.0 | 288 | 155 | 3.6 | 0.02 | 41 | 0.17-1.7 | <1, 7 | 3-10.5 | 123-430.5 | 13.9 | Androderm | Hypogonadism |
Abbreviation: i.v. intravenous, i.m. intramuscular, p.o. per oral, t.d. transdermal, s.I. sublingual, bc buccal.