Buprenorphine-naloxone

Fukase, H. et al., Effects of morphine, naloxone, buprenorphine, butorphanol, haloperidol and imi-pramine on morphine withdrawal signs in cynomolgus monkeys, Psychopharmacology, 116, 396,1994. 

Alfentanil, codein, dihydromorphine, etor-phine, fentanyl, heroin, hydromorphone, levo-methadone, morphine, oxycodone, pethidine, piritramide, remifentanil, sufentanil, tilidine, tramadol Buprenorphine, pentazocine Naloxone, naltrexone... 

The initial dose of buprenorphine should be given at least 12-24 hours after the last heroin dose, 24 hours after the last methadone dose, or 48 hours after the last LAAM dose (see Table 2-3). The methadone dosage of methadone maintenance patients should be reduced to 30 mg/day before the transfer to buprenorphine is attempted. Ideally patients should show clear evidence of opiate withdrawal before receiving the first dose of buprenorphine, to avoid the risk that buprenorphine will precipitate more severe withdrawal. For the first day, sublingual buprenorphine/naloxone doses of 2/0.5-4/1 mg can be given every 2-4 hours, up to a maximum total dose of 8/2 mg/day. On the... 

Dose amounts consist of the buprenorphine dose (the number before the slash) and the naloxone dose (the number after the slash). Do not begin buprenorphine until patient shows evidence of opioid withdrawal. 

The approval of buprenorphine for the office-based treatment of opioid dependence represents a major departure from the earlier methadone clinic system. Physicians with addiction specialist credentials or those who have completed 8 hours of approved training can become qualified to treat up to 30 patients in their private offices. Stable patients may be given prescriptions for up to a month of medication. The combination buprenorphine/naloxone tablet is expected to have minimal risk for diversion. When taken subhnguaUy, as prescribed, naloxone has minimal biologic activity and does not interfere with the buprenorphine dose. However, if an attempt is made to inject the drug, the addict will experience the full antagonist effect of the naloxone. 

Sarton E, Teppema L, Dahan A (2008) Naloxone reversal of opioid-induced respiratory depression with special emphasis on the partial agonist/antagonist buprenorphine. Adv Exp Med Biol 605 486 91... 

Suboxone (buprenorphine and naloxone), is used in maintenance treatment of opiate addiction. 

There are two types of pharmaceutically important derivatives (a) Compounds with a hydroxyl substituent at position 14, such as in oxycodone and the antagonists naloxone and naltrexone, and (b) Diels-Alder adducts such as etorphine and buprenorphine, where the latter compounds are all derived from another opium alkaloid, (—)-thebaine (12) (Scheme 5.10). Because thebaine is a rather scarce alkaloid, several syntheses have been investigated. Quite recently, Australian scientists have been able to modify P. somniferum in such a way that thebaine is now a main alkaloid, so that it is becoming better available [28],... 

Opioid A recent study has shown activity of hypericum extracts at opioid receptors (Simmen et al. 1998). Extracts displace naloxone from p and x opioid receptors in the micromolar range (IC50 25 and 90 pg/ml, respectively). In contrast, extracts of the sedative herb Valeriana officinalis do not have this effect. This effect is due to unidentified constituents and not by the flavonoids quercetin or kaemferol. Opioids are known to have effects on emotion, so it is conceivable that activity of hypericum at p and k receptors contributes to its therapeutic effects (Gerra et al. 1998 Tejedor-Real et al. 1995 Walker and Zacny 1998). Although they are not conventional treatment for depression, opioids such as buprenorphine have been effective in treatment of refractory depression (Bodkin et a. 1995). However, for any further conclusions to be drawn, it would be necessary to further e uddate the opioid effects of hypericum to determine what functional effect, if any, hypericum has on the receptors. 

Q35 contains buprenorphine with naloxone Q36 contains caffeine... 

Suboxone contains buprenorphine, an opioid partial agonist used in opioid dependence in combination with naloxone. 

Voltarol is a brand-name preparation for diclofenac (NSAID) and modified-release tablets are available in 75 mg and 100 mg strength. Nu-seals is a proprietary preparation of enteric-coated aspirin 75 mg. Fentanyl, co-codamol and Suboxone (buprenorphine and naloxone) consist of opioid drugs. 

Suboxone is a combination of buprenorphine (opioid partial agonist) and naloxone. It is presented as sublingual tablets and is used as an adjunct in the treatment of opioid dependence and in premedication or perioperative analgesia. A side-effect of opioids is drowsiness. 

In October 2002, the FDA approved two new medications for treating opiate addiction, both developed by Reckitt Benckiser Pharmaceuticals. The new drugs, Subutex (buprenorphine hydrochloride) and Suboxone tablets (buprenorphine hydrochloride and naloxone hydrochloride) contain buprenorphine, a partial opioid agonist. Like methadone, buprenorphine binds to the brain s opioid receptors, but produces significantly reduced pleasurable effects than heroin. 

Suboxone tablets (buprenorphine hydrochloride and naloxone hydrochloride)... 

Endogenous opioids are peptides that are cleaved from the precursors proenkephalin, pro-opiomelanocortin, and prodynorphin. All contain the amino acid sequence of the pentapeptides [Met]- or [Leuj-enkephalin (A). The effects of the opioids can be abolished by antagonists (e.g., naloxone A), with the exception of buprenorphine. 

Tablets, sublingual 2 mg buprenorphine base/0.5 mg naloxone, 8 mg buprenorphine base/2 mg naloxone (C-/77) Suboxone (Reckitt Benckiser)...

Buprenorphine/Naloxone combination Treatment of opioid dependence. 

Tablets Administer sublingually as a single daily dose in the range of 12 to 16 mg/day. When taken sublingually, buprenorphine and buprenorphine/naloxone have similar clinical effects and are interchangeable. Buprenorphine tablets contain no naloxone and are preferred for use during induction.

Maintenance - Buprenorphine/Naloxone is the preferred medication for maintenance treatment because of the presence of naloxone in the formulation. 

Reducing dosage and stopping treatment - Make the decision to discontinue therapy with buprenorphine or buprenorphine/naloxone after a period of maintenance or brief stabilization as part of a comprehensive treatment plan. Gradual and abrupt discontinuation have been used but there is not a best method of tapering the dose at the end of treatment. 

Acute abdominai conditions As with other p-opioid receptor agonists, the administration of buprenorphine or buprenorphine/naloxone may obscure the diagnosis or clinical course of patients with acute abdominal conditions. 

The most known narcotics are the opium alkaloids such as morphine, codeine, thebaine, papaverine, noscapine and their derivatives and modified compounds such as nalmorphine, apomorphine, apomopholcodine, dihydrocodeine, hydro-morphone and heroine, also known as diamorphine. Synthetic narcotics share the structural skeleton of morphine and include dextromethorphan, pentazocine, phenazocine meperidine (pethidine), phentanyl, anfentaitil, remifentalin, methadone, dextropropoxyphene, levoproxyphene, dipipanone, dextromoramide, meptazinol and tramadol. Thebaine derivatives are also modified narcotics and include oxycodone, oxymorphone, etorphine, buprenorphine, nalbuphine, naloxone or naltrexone. Narcotics can be semi-synthesized or totally synthesized from the morphine and thebaine model. The compounds serve various purposes in clinical practise. 

Opioid dependence Sublingual Initially, 12-16 mg/day, beginning at least 4 hr after last use of heroin or short-acting opioid. Maintenance 16 mg/day. Range 4-24 mg/day. Patients should be switched to buprenorphine and naloxone combination, which is preferred for maintenance treatment. 

Contraindications Hypersensitivity to buprenorphine hypersensitivity to naloxone for those receiving the fixed combination product containing naloxone (Suboxone)... 

Castells X, Casas M, Vildal X, Bosch R, Roncero C, Ramos-Quiroga JA Capella D (2007) Efficacy of central nervous system stimulant treatment for cocaine dependence a systematic review and meta-analysis of randomized controlled clinical trials. Addiction, 102, 1871-87 Chaisson RE, Bacchetti P, Osmond D, Brodie B, Sande MA Moss AR (1989). Cocaine use and HIV infection in intravenous drug users in San Francisco. Journal of the American Medical Association, 261, 561-5 Chapleo CB Walter DS (1997). The bupre-norphine-naloxone combination product. Research and Clinical Forums, 19, 55-8 Cheskin LJ, Fudala PJ Johnson RE (1994). A controlled comparison of buprenorphine and clonidine for acute detoxification from opioids. Drug and Alcohol Dependence, 36, 115-21... 

Buprenorphine is a semi-synthetic derivative of thebaine, one of the opium alkaloids. It is approximately 30 times as potent as morphine. A dose of 0.3 mg intramuscularly has a duration of analgesic action of 6-18 h. Buprenorphine is also effective sublingually. The average bio-availability by this route is about 55%, but absorption is slow and the time to achieve peak plasma concentrations is variable, with a range of 90-360 min. The onset of action is rather slow (5-15 min) after both intramuscular and intravenous administration, possibly due to slow receptor association. Buprenorphine binds to and dissociates from the p receptor very slowly, which may account for its low potential for physical abuse. It also means that buprenorphine-induced respiratory depression is difficult to reverse with naloxone, even with very high doses. Doxapram may in these circumstances be useful. Drowsiness and dizziness are the most common side effects, although they rarely... 

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