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Thread: buprenorphine patches


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1. buprenorphine patches #1 leftwing

Bluelight Crew Join Date Oct 2005 Posts 17,411 04-03-2008 08:59 ive just been prescribed 10mg bupe patches (10mics/hr), leaving them on for a few days a time. before this i was still unsure what type of patches i would be recieving (for those who read my other thread a little while ago) but up until guessed it would be a fentanyl pacth. bupe never even passed my mine, because i wasnt aware of it being prescribed for pain on many ocassions. has anyone else had any experience with these for pain management? ive spondylosis, curvature to the back and neck pain which is all congenital...my blessed genes. ive just got off tramadol finally today 2 weeks before i was scheduled to. ive also now had the patch on for about 8 hours im guessing and am starting to feel some pain dissipate, until now ive knocked myself out with valium. which raises my next question. im fairly tolerant to valium (100mg+ as a start sometime) but only took 70 mgs around 6 hours ago and normally now i would still be hazed as shit and barely functional to perform out of the way tasks, but i now feel somewhat less buzzed from when id just before i dozed off and am feeling a little more alert. interactions with the bupe maybe?

im somewhat of an opiate lover and am a little disheartened ive been given bupe. given ill be wanting to dabble with other opiates at time, but i guess thats a second to my pain at the moment. Last edited by Captain.Heroin; 08-02-2010 at 08:59. Reason: added (bupe) title

2.

#2 phrozen

Bluelight Crew Join Date May 2004 Posts 15,902 04-03-2008 16:26 I'm guessing you're in Europe? Haven't heard of bupe patches here. Anyway, they seem unnecessary. Bupe has a long half-life, and most are fine dosing just once a day. As for giving it for pain, it's not that popular, since it's not a full agonist.

3.

#3 NickyBundles

Bluelighter Join Date May 2004 Location ny Posts 361 04-03-2008 18:59 i dont think bupe is that good of a pain killer, once your tollerant to it you berily feel it even at high doses not much happens, and the shitty part is if you have breakthru pain or just a bad day were the bupes not cuttin it your not gonna be able to take something that will really help.

4.

#4 'medicine cabinet'

Bluelighter Join Date Jun 2006 Location Baltimore Posts 4,389 04-03-2008 20:07

i was in a clinical trial for a bupe skin patch a few years ago at johns hopkins here in baltimore. i know they have them in europe already, i forget what they are called tho....the one that i got to try looked like a flying saucer, like it had a little dish on the inside with the bupe gel in it. it lasted for 2 days and after that i started to get sick. it didnt seem like it worked as well as sublingual bupe tho, i wouldnt be surpirsed if it never gets to market.

5.

#5 euphoricnod

Bluelight Crew Join Date Oct 2004 Posts 9,629 04-03-2008 20:31 i dislike drugs that absorb through the skin like fent or bupe for me it always felt like I got way less out of it.

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#6 rave23

Bluelighter Join Date Feb 2007 Location Canada / Germany Posts 1,622 04-03-2008 20:50 ^^ way less and usuall a lot longer, right?

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#7 jykkE

Bluelighter Join Date Jan 2007 Location Atlanta, GA Posts 961 04-03-2008 20:51 bupe patches...that would be awesome if they had them here. whats the price on them compared to the pills? especially since they are 10mg. of course it might not be as fun since its only 10mics/hr. That would kinda suck. since bupe seems to have a ceiling dose, what will you be prescribed once you reach that? especially since you are getting them for pain, it kinda seems pointless in that light since you will probably have to switch to opiates. then when you want to get off the opiates, what will there be

to goto if you become psychologically addicted, an extremely high dose of methadone?

8.

#8 leftwing

Bluelight Crew Join Date Oct 2005 Posts 17,411 04-03-2008 23:36 phrozen - no im in australia. my guess is he gave me them for abuse potential, plus theyre on the pbs here. to the other guys - they cost me $5 for 2 patches for 2 weeks. the brand name is norspan. they come in 5mg, 10mg and 20mg patches. ive had the patch on for just under 24 hrs now and am pretty much pain free with a nice little buzz going on. i read somewhere if your on a dose less than 2mg a day you can get away with taking other low doses of other opiates on top without going into withdrawal. it seemed to work last night when i dosed some codeine with it, ~240mg after a cwe. i talked to my dr about breakthrough pain but he gave me codeine for these first 2 weeks, but ill be asking me to either take me off patches and put me on a better pill or be asking for a higher dose.

9.

#9 NickyBundles

Bluelighter Join Date May 2004 Location ny Posts 361 05-03-2008 00:03 hmm, im pretty sure that no matter what dose of buprenorphine your takeing it will block other opiates from working, if your tollerant to the bupe and take codiene you wont get sic, you just wont feel the codiene, weird that he would even prescribe that with bupe.

10.

#10 leftwing

Bluelight Crew Join Date Oct 2005 Posts 17,411 05-03-2008 00:10

yer i was very suprise as well. im just going to get something good off him that makes me happy then move onto someone else whos not such a quack. heres what the patches are like

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#11 jykkE

Bluelighter Join Date Jan 2007 Location Atlanta, GA Posts 961 05-03-2008 00:25 when you need to switch meds will it be necessary to taper before the switch, or are you able to switch over without withdrawing? i would assume the latter as you are taking codeine without (obvious) problems. also, im guessing you have to take a high amount of a time release opiate (oxycontin, mscotton morphine, etc) when you do eventually switch to a different med since bupe has a ceiling dose, since your body is used to a constant supply of bupe that is in the patch?

12.

#12 leftwing

Bluelight Crew Join Date Oct 2005 Posts 17,411 05-03-2008 00:33 the withdrawals will depend how long im on them till i switch. this is only my 2nd day on it. so the sooner the better. i have and will be able to get more diazepam at the very least to help with withdrawals and other otc products. i have to admit theyre working great for the pain so far, as well me having a not too great of an opiate tolerance im getting a nice buzz with some cones and diazepam on top of it. im also feeling quite energetic as i did when i was using oxycontin

13.

#13 euphoricnod

Bluelight Crew Join Date Oct 2004 Posts 9,629 05-03-2008 01:07

How did you get those patches? That looks like a delightful alternative to taking a pill everyday twice a day... Are you in the United States?

14.

#14 leftwing

Bluelight Crew Join Date Oct 2005 Posts 17,411 05-03-2008 02:32 ^no im in australia. ive been on tramadol for the last 3 and a bit years for back pain. my dr then decided to switch me over to patches. hes dodgy on his information but is letting me give my say in what i want and letting me say my bit without acting like a prick. i went and tried to find a few water0proof patches for showering just before and they were all fucking fail. i think itll be glad wrap from now

15.

#15 nabollocks

Bluelighter Join Date Mar 2007 Posts 1,130 05-03-2008 03:23 Hey leftwing... I suggested these patches to you a while back... good to see you finally got them. You can still take your Tram while on the Bup patch which is a good thing ;-) The only thing that I dislike about the patch is the doctors are only aloud to prescribe 2 weeks worth at any 1 time... kind of a bugger when you havent the time to visit the doc every other week... Keep us posted on how they go, you can always ask for the next dose up if they are not cutting your pain... Can you let us know how they compare to your Tram SR? Both in terms of pain relief and antidepressant activity. I still taking the Tram SR as I can get 4 months prescribed at once...

16.

#16 swybs

Bluelighter Join Date Jan 2004 Location nyc area Posts 2,292

05-03-2008 05:08 Without getting into specifics, I will say that the united states is about to have 2 separate bupe patch products hit market very soon. They both seem very mild in dose and (as far as I know) are indicted for mild to moderate persistent pain (think half step between scehdule 3 and schedule 2 pain meds or, as one company is trying to market it as the safe alternative to the boogeyman slow-release opiates/oids). I reviewed the data for both-their landmark clinical trials that will get them approval and be in their PIs-and wasn't impressed. Further, I think the physician population is underestimating how difficult it is for longterm bupe users to quit-very few are sucessful. Swybs

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#17 leftwing

Bluelight Crew Join Date Oct 2005 Posts 17,411 05-03-2008 08:13 Originally Posted by nabollocks Hey leftwing... I suggested these patches to you a while back... good to see you finally got them. You can still take your Tram while on the Bup patch which is a good thing ;-) The only thing that I dislike about the patch is the doctors are only aloud to prescribe 2 weeks worth at any 1 time... kind of a bugger when you

havent the time to visit the doc every other week... Keep us posted on how they go, you can always ask for the next dose up if they are not cutting your pain... Can you let us know how they compare to your Tram SR? Both in terms of pain relief and antidepressant activity. I still taking the Tram SR as I can get 4 months prescribed at once... yer man i was quite suprised when he bought up the patch straight , though i didnt think it would be bupe, i was thinking fent. and yer it does suck only getting 2 at a time, but i have to go see my psych every week and hes at the same practice so its not a big hassle. ive had it on for nearly 2 days now and its been nothing but success. i had codeine earlier in the morning with a small dose of 30mg of valium and ive been more hazed than i should be. probably from the vodka still in my system. the antidepressant values have been the same if not better than tramadol so far, ive been f=more energetic and motivated Last edited by leftwing; 31-10-2009 at 00:16.

18.

#18 ifonly

Bluelighter Join Date Jun 2006 Posts 1,091 05-03-2008 09:51

Originally Posted by leftwing yer i was very suprise as well. im just going to get something good off him that makes me happy then move onto someone else whos not such a quack. heres what the patches are like

zoom:

good to see my msn window in the background my friend keep me updated on how u feel as the week contuinues im actually interested. i know a lot of people on bupe maintenence (8mb pills) but never the patches.

19.

#19 canj00feelit?

Bluelighter Join Date May 2004 Location Jersey Shore Posts 748 07-04-2008 08:25

Glad to hear they are workimg out for you man

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#20 nabollocks

Bluelighter Join Date Mar 2007 Posts 1,130 18-04-2008 06:49 In light of this article: Effectiveness and tolerance of tramadol in cancer pain. A comparative study with respect to buprenorphine by Bono AV, Cuffari S Service d'Urologie, Hopital di Circolo, Varese, Italie. Drugs 1997; 53 Suppl 2:40-9 ABSTRACT Opioid analgesics represent one of the most important tools in a sequential pharmacological approach to oncological pain relief. They are recommended by the WHO when nonsteroidal anti-inflammatory drugs (NSAIDs) no longer provide adequate analgesia. However, the use of opioids is limited because of their numerous and often severe adverse effects. This aspect of opioids has motivated continuous research projects aimed at discovering drugs that can provide maximum pain relief but with improved tolerability. Tramadol is a new, centrally acting analgesic with a dual mechanism of action. It shows a selective interaction with mu receptors, which are responsible for nociception, and has weak pharmacodynamic activity on other opioid receptors. At the same time, it acts synergistically on neuroamine transmission by inhibiting synaptic noradrenaline (norepinephrine) reuptake and inducing intrasynaptic serotonin (5-hydroxytryptamine; 5-HT) release. From a

pharmacokinetic standpoint, tramadol offers high bioavailability, with similar patterns after oral or parenteral administration (half-life 5 to 7 hours, time to peak plasma concentration 3.1 hours, and approximately 20% plasma protein binding). Although the efficacy of tramadol is comparable to that of other drugs with similar modes of action, the incidence of side effects such as constipation and respiratory depression is lower. The frequency of euphoria and dysphoria is negligible, resulting in little risk of abuse or dependence. It therefore seemed appropriate to further investigate the efficacy and tolerability of tramadol, defined as having only weak potency, in comparison with a widely used opioid, in oncological pain. Buprenorphine was selected as an opioid with a potency equivalent to half that of morphine, but with tolerability that is partially limited by the fact that it frequently gives rise to adverse reactions considered typical of stronger opioids. To compare the analgesic effect and tolerability of tramadol and buprenorphine, 60 patients (44 men, 16 women; average age 61.4 years), all presenting with advanced tumours, were treated orally in a controlled crossover trial with randomised sequences. Patients took both drugs, each for a week, with a 24-hour washout period between treatments. Tramadol was prescribed at the daily dose of 300mg, orally, and buprenorphine at 0.6 mg/day, as a sublingual preparation. Assessments were made of Karnofsky performance status and severity of pain before and during the 4 hours after taking the 2 drugs. Each patient also completed a daily diary recording the severity of pain 1 hour after the dose, the evolution of pain during the day and its severity compared with that on the previous day. They also assessed the duration and quality of sleep. The Karnofsky index changed little with either treatment, but all other variables showed worthwhile improvement, indicating the significant analgesic effect of both drugs. Buprenorphine and tramadol had a similar analgesic effect, although the improvement with the test drug was significant within 1 hour of administration (p < 0.05 compared with baseline) and more marked (p < 0.05 on day 2 compared with buprenorpine). At the end of tramadol treatment, sleep had also improved, both quantitatively and qualitatively (both p < 0.05). The final assessment was significantly in favour of tramadol as regards efficacy (p < 0.05) and patient acceptability (p < 0.01). Thus, tramadol was better tolerated than buprenorphine, and caused fewer and milder adverse reactions. Only 1 patient discontinued tramadol, compared with 18 using reference therapy. Tramadol, although theoretically less potent, nevertheless brought about as much pain relief as the comparator opioid. In conclusion, for this class of drug, tramadol provides an excellent balance between efficacy and tolerability, confirming preliminary studies. Would the OP still recommend the change from Tramadol to Bup? I know the MOA is different in the study above, but I am still considering the move due to drug drug interactions with Tramadol.

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#21 tadfish

Ex-Bluelighter Join Date Feb 2005 Posts 1,568 14-02-2009 00:35 Originally Posted by jykkE bupe patches...that would be awesome if they had them here. whats the price on them compared to the pills? especially since they are 10mg. of course it might not be as fun since its only 10mics/hr. That would kinda suck. since bupe seems to have a ceiling dose, what will you be prescribed once you reach that? especially since you are getting them for pain, it kinda seems pointless in that light since you will probably have to switch to opiates. then when you want to get off the opiates, what will there be to goto if you become psychologically addicted, an extremely high dose of methadone? Well i got patches but i wondering what is this about ceiling dose? How long does it take to work? I was thinking as long as it doesn't go over 2mg a day cause i gto 10mg patches which are costly can i have other opiates with it to potentiate or will they compete? Also wondering what happens if you mix kanna with bupe?

22.

#22 tadfish

Ex-Bluelighter Join Date Feb 2005 Posts 1,568 14-02-2009 00:37 This might help THose finding info on mixing it with kanna is hard. Anyone got any ideas? doc gave me stemzine wonder hgow that will add to the mix anyone? From MIMS: Uses/Indications: Partial opioid agonist. Mod to severe pain Contraindications: Severe respiratory impairment; nonselective MAOIs (within 14 days of stopping MAOI) Precautions: Not for narcotic dependence treatment, postop use, situations with a narrow therapeutic index, rapidly varying analgesia need; inflammatory bowel, convulsive disorders; head injury; impaired consciousness (undiagnosed); intracranial lesion; raised ICP; respiratory, hepatic, renal, biliary disease; hypotension, hypovolaemia, shock; pancreatitis; prostatic hypertrophy; adrenocortical insufficiency; debility; 24 hrs prior to pain relieving surgery incl cordotomy; after abdominal surgery; drug, alcohol abuse; serious mental illness; congenital QT prolongation; severe febrile illness; hypothyroidism; withdrawal; narcotic dependence; opioid naive; avoid excess heat to patch site; debility; pregnancy, lactation, children < 18 yrs Adverse Reactions: Respiratory depression; QT prolongation; euphoria; dependence; GI upset esp constipation; anorexia; sweating; dizziness; headache; somnolence; confusion; pruritus; erythema; rash; application site reaction; anxiety; insomnia; nervousness; paraesthesia; depression; vasodilation; oedema; dyspnoea; taste perversion; asthenia; pain; others, see full PI

Drug Interactions: Nonselective MAOIs (see Contra); selective MAOIs; CNS depressants (eg sedatives, hypnotics, general anaesthetics, other opioids, phenothiazines, centrally acting antiemetics, benzodiazepines, alcohol); drugs that prolong QT (eg antiarrhythmics), cause respiratory depression, hypotension; drugs affecting hepatic metabolism; CYP3A4 inhibitors (eg protease inhibitors, azole antimycotics, Ca channel antagonists, macrolides); enzyme inducers (eg phenobarbitone, carbamazepine, phenytoin, rifampicin); warfarin (poss) NORSPAN 5 TRANSDERMAL PATCH (Transdermal patch) Prescription required. S8 This product may cause drowsiness. Buprenorphine (equiv. 5 mcg/hr); gluten free; Dose: Apply patch every 7 days to intact skin (sites, skin prep, application, removal: see full PI); initially commence with Norspan 5. Titrate; incr at intervals greater than or equal to 3 days as needed by replacing or adding patch (max 2 concurrent patches). Give other analgesics during initiation, titration; change to other analgesic if analgesia inadequate on max Norspan dose. Rotate sites, avoid other opioids 24 hrs after patch removal (see full PI) Uses/Indications: Partial opioid agonist. Mod to severe pain Contraindications: Severe respiratory impairment; nonselective MAOIs (within 14 days of stopping MAOI) Precautions: Not for narcotic dependence treatment, postop use, situations with a narrow therapeutic index, rapidly varying analgesia need; inflammatory bowel, convulsive disorders; head injury; impaired consciousness (undiagnosed); intracranial lesion; raised ICP; respiratory, hepatic, renal, biliary disease; hypotension, hypovolaemia, shock; pancreatitis; prostatic hypertrophy; adrenocortical insufficiency; debility; 24 hrs prior to pain relieving surgery incl cordotomy; after abdominal surgery; drug, alcohol abuse; serious mental illness; congenital QT prolongation; severe febrile illness; hypothyroidism; withdrawal; narcotic dependence; opioid naive; avoid excess heat to patch site; debility; pregnancy, lactation, children < 18 yrs Adverse Reactions: Respiratory depression; QT prolongation; euphoria; dependence; GI upset esp constipation; anorexia; sweating; dizziness; headache; somnolence; confusion; pruritus; erythema; rash; application site reaction; anxiety; insomnia; nervousness; paraesthesia; depression; vasodilation; oedema; dyspnoea; taste perversion; asthenia; pain; others, see full PI

Drug Interactions: Nonselective MAOIs (see Contra); selective MAOIs; CNS depressants (eg sedatives, hypnotics, general anaesthetics, other opioids, phenothiazines, centrally acting antiemetics, benzodiazepines, alcohol); drugs that prolong QT (eg antiarrhythmics), cause respiratory depression, hypotension; drugs affecting hepatic metabolism; CYP3A4 inhibitors (eg protease inhibitors, azole antimycotics, Ca channel antagonists, macrolides); enzyme inducers (eg phenobarbitone, carbamazepine, phenytoin, rifampicin); warfarin (poss) NORSPAN 5 TRANSDERMAL PATCH (Transdermal patch) Prescription required. S8 This product may cause drowsiness. Buprenorphine (equiv. 5 mcg/hr); gluten free; Dose: Apply patch every 7 days to intact skin (sites, skin prep, application, removal: see full PI); initially commence with Norspan 5. Titrate; incr at intervals greater than or equal to 3 days as needed by replacing or adding patch (max 2 concurrent patches). Give other analgesics during initiation, titration; change to other analgesic if analgesia inadequate on max Norspan dose. Rotate sites, avoid other opioids 24 hrs after patch removal (see full PI) Chemical name: (2S)-2-[17-(cyclopropylmethyl)- 4, 5alpha-epoxy-3hydroxy-6-methoxy-6alpha, 14-ethano-14alpha- morphinan-7alpha-yl]3, 3-dimethylbutan-2-ol. Molecular formula: C29H41NO4. MW: 467.6. CAS: 52485-79-7. Buprenorphine is a white or almost white powder and is very slightly soluble in water, freely soluble in acetone, soluble in methanol and ether and slightly soluble in cyclohexane. The pKa is 8.5. Norspan Transdermal Patch is a rectangular (10 microgram/hour) or square (5 and 20 microgram/hour) beige coloured matrix patch with rounded corners, marked with the trade name and consisting of a protective liner and functional layers. Proceeding from the outer surface towards the surface adhering to the skin, the layers are (1) a beige coloured web backing layer of polyester material; (2) an adhesive matrix rim without buprenorphine; (3) a separating foil over the adhesive matrix; (4) the buprenorphine containing adhesive matrix; and (5) a release liner (see Figure 1). Before use the release liner covering the adhesive layer is removed and discarded. Please refer to figure 1. Norspan Transdermal Patch transdermal system is available in three different strengths: 5, 10 and 20 microgram/hour. The composition of all three strengths is identical except for size. The proportion of buprenorphine in the adhesive matrix is the same in each strength (10% by weight). The amount of buprenorphine released from each system per hour is proportional to the surface area of the system. The skin is the limiting barrier to diffusion from the system into the bloodstream. topActions

Pharmacology. Buprenorphine is a partial opioid agonist, acting at the mu-opioid receptor. It also has antagonistic activity at the kappa-opioid receptor. The opioid agonist activities of buprenorphine are dose related. Like other opioid agonists, buprenorphine produces dose related analgesia, however a ceiling effect to analgesia is well documented. Buprenorphine binds to and dissociates from the mu receptor slowly, which may account for the prolonged duration of analgesia and, in part, for the limited physical dependence potential observed with the drug. Buprenorphine produces similar effects to other opioids on the central nervous system, and the cardiovascular, respiratory and gastrointestinal systems, although the intensity and duration of the effects may vary when compared with other opioids. Opioids may also influence the hypothalamic pituitary adrenal or hypothalamic pituitary gonadal axes, including an increase in serum prolactin and decreases in plasma cortisol and testosterone, which can manifest in clinical symptoms. Since kappa receptor agonist activity is related to psychotomimetic and dysphoric effects, buprenorphine is expected to produce fewer psychotomimetic and dysphoric effects than drugs with kappa agonist activities. Like other opioid agonists, buprenorphine may produce increases in cerebrospinal fluid pressure, cause altered mentation, mental clouding or amnesia. Buprenorphine acts to reduce blood pressure in a manner similar to other opioids. Norspan Transdermal Patch application resulted in transient decreases in blood pressure in healthy young and elderly subjects, without clinical adverse events. Respiratory depression is less common than with full mu agonists, such as morphine, and there appears to be a ceiling effect. When respiratory depression occurs it appears to have a slower onset and longer duration compared to morphine. Like other opioids buprenorphine may cause nausea, vomiting, constipation and an increase in biliary tract pressure. Effects on the immune system were seen with natural opioids like morphine in in vitro and animal studies, although the clinical significance of these is unknown. It is not known whether buprenorphine, a semisynthetic opioid, has immunological effects similar to morphine. Buprenorphine can cause dose related miosis and urinary retention in some patients. Pharmacokinetics. Each Norspan Transdermal Patch provides a steady delivery of buprenorphine for up to seven days. Steady state is achieved by day 3 following the first application. After removal of the Norspan

Transdermal Patch, buprenorphine concentrations decline, decreasing approximately 50% in 12 hours (range 10 to 24 hours). Norspan Transdermal Patch 5, 10 and 20 microgram/hour provide dose proportional increases in total exposure (AUC (area under the curve)) over the seven day application period. Dose proportional increases in plasma concentrations occur at steady state with Norspan Transdermal Patch application for up to 60 days. Accumulation of plasma buprenorphine did not occur during the 60 days. The rate of buprenorphine release from each patch is proportional to the surface area. Each Norspan Transdermal Patch 5 microgram/hour releases buprenorphine 5 microgram per hour and contains a total of buprenorphine 5 mg. Each Norspan Transdermal Patch 10 microgram/hour releases buprenorphine 10 microgram per hour and contains a total of buprenorphine 10 mg. Each Norspan Transdermal Patch 20 microgram/hour releases buprenorphine 20 microgram per hour and contains a total of buprenorphine 20 mg. Absorption. Following Norspan Transdermal Patch application, buprenorphine diffuses from the patch through the skin. In clinical pharmacology studies, the median time for Norspan Transdermal Patch 10 microgram/hour to deliver detectable buprenorphine concentrations (25 picogram/mL) was approximately 17 hours. The bioavailability of buprenorphine from a Norspan Transdermal Patch relative to IV (intravenous) is 15% (for all three strengths). Accidental oral ingestion. Measurable systemic levels of buprenorphine were demonstrated in dogs given Norspan Transdermal Patch by oral administration. Distribution. Buprenorphine is approximately 96% bound to plasma proteins. In a study of IV buprenorphine in healthy subjects, the volume of distribution at steady state was 430 L, which is indicative of the high lipophilicity of the drug. Following IV administration, buprenorphine and its metabolites are secreted into bile, and within several minutes distribute into the cerebrospinal fluid (CSF). CSF concentrations appear to be approximately 15 to 25% of concurrent plasma concentrations. Metabolism and elimination. Buprenorphine metabolism in the skin following Norspan Transdermal Patch application is negligible. Buprenorphine is eliminated via hepatic metabolism, with subsequent biliary excretion and renal excretion of soluble metabolites. Hepatic metabolism through CYP3A4 and UGT1A1/1A3 enzymes results in two the primary metabolites, norbuprenorphine and buprenorphine 3-Oglucuronide, respectively. Norbuprenorphine is also glucuronidated prior

to elimination. Buprenorphine is also eliminated in the faeces within seven days. In a study in postoperative patients the total clearance of buprenorphine was 55 L/hour. Norbuprenorphine is the only known active metabolite of buprenorphine. It has been shown to be a respiratory depressant in rats at concentration at least 50-fold those seen following application of Norspan Transdermal Patch 20 microgram/hour. Specific inhibitors of CYP450 (e.g. ketoconazole, gestodene, nifedipine, norfluoxetine, ritonavir) inhibited formation of the buprenorphine metabolite norbuprenorphine in human microsomes. Application site. A study in healthy subjects demonstrated that the pharmacokinetic profile of buprenorphine delivered by Norspan Transdermal Patch is similar when applied to the upper outer arm, upper chest, upper back or the side of the chest (midaxillary line, 5th intercostal space). In a study of healthy subjects applying Norspan Transdermal Patch repeatedly to the same site, immediate reapplication caused increased absorption, without clinical adverse events. For this reason, rotation of application sites is recommended (see Dosage and Administration). In another study in healthy subjects application of a heating pad directly on the Norspan Transdermal Patch caused a transient 26 to 55% increase in blood concentrations of buprenorphine. Concentrations returned to normal within five hours after the heat was removed. For this reason, applying heat sources such as hot water bottles, heat pads or electric blankets directly to the Norspan Transdermal Patch is not recommended. A heating pad applied to a Norspan Transdermal Patch site directly after patch removal did not alter absorption from the skin depot.

23.

#23 cvillian

Bluelighter

Join Date Dec 2008 Location NoVA Posts 151 14-02-2009 01:54 Originally Posted by leftwing temgesics are something i would like to try before fentanyl. Temgesic are the sublingual version of buprenorphine in a pill form. I'm not sure if you knew that or not. I'm sure that you could put the patch under your tongue and it will absorb just like people do with the fentanyl patches by putting it against their cheeks and gums. I wouldn't advise you to do these since you seem to really need it for pain but it seems that you dabble in the abuse department of your meds, so you could give it a shot with the remainder of your bupe patches. I'm not sure if you will achieve a high of any sort though. It seems people get tolerant to buprenorphine pretty fast.

24.

#24 tadfish

Ex-Bluelighter Join Date Feb 2005 Posts 1,568 16-02-2009 07:43 i Meant having kratom with bupe. Had an 8 mg bupe sub with patch the other day. I think as long as as bupe dose below 2mg it doesn't compete as strongly for the position. Fuck it i going to put another patch on now.

I read tramadol mixes good with bupe. But i hate tramadol although i might try some tommorrow. it doesn't make sense this patch i only on 10mg ones that last a week 10 ug/h that doesn't make sense. i got 2 patches on. getting more soon i'll be covered in patches.

25.

#25 leftwing

Bluelight Crew Join Date Oct 2005 Posts 17,411 16-02-2009 07:55 ^an 8mg sub with a patch = 2 x doses of buprenorphine i cant really understand what you're trying to say but the patch has a total of 10mg of bupe on it. they transdermally release 10ug/h. 1 day worth of bupe = 24 hours x .01mg = 0.24mg/day. over a week = 7 x 0.24 = 1.68mg. is that what you meant by it not making sense? they actually put more drug in the patch than is released? with my 2 x 20mg patches on i absorb just under 8mg of buprenorphine a week

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