Specificity Of Transdermal Buprenorphine

Buprenorphine is an opioid analgesic administered sublingually or by injection for the treatment of moderate to severe pain. Transdermal buprenorphine (BuTrans®, Napp Pharmaceuticals) is formulated as a matrix patch and is licensed for the treatment of moderate to severe cancer pain and severe pain not responding

Passive TDS

1st genera!:

backing layer drug reservoir rate-controlling membrane adhesive layer release liner

Figure IV-14. Composition of the two transdermal opioid systems (TDS) used in chronic pain therapy, the former Ravioli type and the available matrix type, both of which are marketed as fentanyl TTS and buprenorphine TDS

to non-opioid analgesics. BuTrans® ptaches (Napp Pharmaceuticals-UK; Purdue Pharma-USA) are available in three different strengths delivering 5, 10, 20 ^g/hr over 96 h. The starting dose is determined by the dose and type of previous analgesic. Patients not previously taking an analgesic, or taking a non-opioid analgesic, should begin with a dose of 10 ^g/hr. The patch should be replaced every 96 h and at least 7 days should elapse before a new patch is applied to the same area of skin. Sublingual buprenorphine should be available to treat breakthrough pain; if 0.4-0.6 mg/day is regularly required, the next patch strength should be used. Blood levels of buprenorphine increase slowly after application of the first patch. Therefore, additional analgesia may be required for the first 24-48 h. The commonest adverse events reported in clinical trials were nausea (17% of patients), erythema (17%), pruritus (15%), vomiting (9%), dizziness (7%), tiredness (6%) and constipation (5%).

The use of any transdermal systems is limited by the cost, the difficulties involved in delivering high doses, and the need for an alternative route to provide supplemental doses for breakthrough pain. In addition, these delivery systems are not preferred for therapy titration of opioid doses in the setting of severe pain since there is a lag of up to 14 h until sufficient high concentration of the opioid have been attained in the plasma (Fig. IV-15). Also, fever spikes, a problem affecting some patients with AIDS, and heat sources potentially may lead to an unstable or

Figure IV-15. Representative example of increasing plasma concentrations over time using a buprenor-phine patch with a concentration of 35 (n = 11) or 70 (n = 17)/u,g/h respectively. Note, after patch removal there is a gradual decay of plasma concentration because of the opioid depot still being present in the skin

Figure IV-15. Representative example of increasing plasma concentrations over time using a buprenor-phine patch with a concentration of 35 (n = 11) or 70 (n = 17)/u,g/h respectively. Note, after patch removal there is a gradual decay of plasma concentration because of the opioid depot still being present in the skin an increase of absorption from the transdermal system, resulting in higher concentrations than necessary. It is important to follow carefully the instructions that have been given with this medicine.

1. BuTrans® patches should be applied to a clean, dry, non-hairy, non-irritated area of skin, preferably on the upper outer arm, upper chest, upper back, or the side of the chest. Avoid areas with large scars. If you need to clean the skin before sticking on the patch use only water, not soap or other cleansers. If hair needs to be removed before applying the patch it should be cut with scissors, not shaved. The patch should not be stuck on immediately after a hot bath or shower, one should wait for the skin to cool down first, and not use talc, creams or moisturisers before applying the patch as they may prevent it sticking. The patch is stuck on immediately after removing it from the pouch and pressed firmly into place with the palm of the hand for 30 s.

2. The patches should not be divided, cut or damaged in any way.

3. One should not wear more patches than told by the physician. No more than two patches should be worn at any one time.

4. While wearing a patch one can swim, bathe and shower as normal, but one should avoid exposing the patch to excessive heat sources, such as hot water bottles, electric blankets, heat lamps, sunbeds, saunas or hot spa baths, as heat can increase the absorption of the active ingredient into the body, resulting in a greater risk of side effects.

5. The patient should tell his doctor once he got a fever while wearing the patch, as this might also increase the absorption of medicine through the skin.

6. Each patch should be worn for 7 days and then removed. New patches should be applied to a different area of skin, and one should avoid using the same area for the next 3-4 weeks. If a patch falls off before it needs changing, one should use a new one immediately, remembering that this patch should be replaced after 7 days.

7. Removed patches should be folded in half, sticky side innermost, and placed inside the open pouch or a piece of tin foil, for careful disposal away from children or animals. This is because used patches may still contain some active ingredient that may be harmful to children or animals.

8. The active ingredient of the patch, buprenoprhine, may cause drowsiness. One should not drive or operate machinery while wearing a patch, or for at least 24 h after removing the last patch. Alcohol should be avoided, as this may increase drowsiness.

9. The effect of buprenoprhine (including any side effects) can last for up to 30 h after removal of the last patch. If the physician is changing from this analgesic to another opioid painkiller, the new opioid, as a general rule, should not be administered within 24 h after removing the BuTran®s patch.

10. With prolonged use, the body may become dependent on this medicine. As a result, withdrawal symptoms such as feeling agitated, anxious, nervous or shaky, or having difficulty sleeping, may occur after the patient stops using the medicine. This is rare, and if they occur, these effects usually disappear after a couple of weeks.

11. BuTrans® patches are not recommended for children and adolescents under 18 years of age, as they have not been studied in this age group.

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