Naloxone combinations

Rabinowitz J, Cohen H, Kotler M Outcomes of ultrarapid opiate detoxification combined with naltrexone maintenance and counseling. Psychiatr Serv 49 831—833, 1998 Reed PA, Schnoll SH Abuse of pentazocine-naloxone combination. JAMA 256 2562— 2564, 1986... 

Buprenorphine/Naloxone combination Treatment of opioid dependence. 

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. 

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... 

Mendelson J, Jones RT, Welm S, Baggott M, Fernandez I, Melby AK, Nath RP. Buprenorphine and naloxone combinations the effects of three dose ratios in... 

The combination of prolonged-release oxycodone 40, 60, or 80 mg/day and prolonged-release naloxone has been studied in 202 patients with chronic pain [143, 144 ]. Naloxone 20 and 40 mg significantly improved bowel function. A 2 1 oxycodone naloxone combination ratio was identified as most suitable and there were no unexpected adverse events. With the higher doses... 

A 10 1 methadone naloxone combination evaluated In man provoked few side effects,° advancing to clinical trials the previously described concept of using a parenterally effective antagonist combined with an oredly active narcotic to prevent abuse of oral medication. ... 

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. 

Holtzman, S.G. Behavioral effects of separate and combined administration of naloxone and J-amphetamine. J Pharmacol Exp Ther 189 51-60. 1974. 

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

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. 

Children (younger than 12 years ofagej- Clinical experience is limited use is not recommended.Pentazocine tablets are intended for oral use only. Severe, potentially lethal reactions may result from misuse by injection or when combined with other substances. Oral pentazocine tablets contain 0.5 mg naloxone, a narcotic antagonist, to aid in elimination of the abuse potential. 

Pentazocine (Talwin) (see also page 252) Street Names Crackers, poor man s h oin, T s and R s> Ts and Rits (all refer to combinations w/ Ritalin) (brands Talwin, Talwin Nx [CIV]) Use Medically used as opioid analgesic euphoria similar to heroin when mixed w/antihistamines combined w/ methylphenidate (Ritalin) is new abuse combination Actions Agonist-antagonist narcotic naloxone, a narcotic antagonist added to Talwin (Talwin NX) has reduced incidence of abuse Effects Euphoria, hallucinations, skin necrosis w/ illicit injection route... 

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

The combination preparation with naloxone ingeniously deters injected abuse... 

Receptor interactions are those where two chemicals both interact with the same receptor to change (usually decrease) the toxic effect of the combination. For example, naloxone binds to the same receptor as morphine and other opiates and so can be used as an antidote to excessive doses of opiates (antagonism). In other cases, such as when two organo phosphates are used together, both acting on acetylcholinesterase, the combined effect would be as expected (additive). 

The compound has a relevant abuse potential (Reed and Scholl, 1986) and high doses may produce dependence of the morphine type. Pentazocine effects can be antagonized with naloxone and combinations with naloxone are available to discourage parenteral misuse (Baum et al., 1987). 

Side-effects Tilidine has a morphine-like side-effect and abuse potential (Trojan and Beil, 1978 Jasinski and Preston, 1986). To inhibit parenteral abuse of oral formulations, a small amount of naloxone is added. Naloxone is completely inactivated after oral administration and does not impede analgesia, whereas after parenteral administration the naloxone component is active and blocks the tilidine effect and can induce withdrawal reactions (Vollmer, 1988). The combination with naloxone, in contrast to pure tildine, is available under normal prescription. 

In the tail flick assay -conotoxin GVIA in combination with morphine leads to an additive effect similar to the combination of morphine with SNX-111 in the formalin test. But when -conotoxin GVIA was applied 24 h before morphine, antinociception was greatly reduced. In morphine-dependent rats, w-conotoxin GVIA given i.c.v. 15 min before naloxone challenge (2 mg/kg i.p.), significantly attenuated the withdrawal symptoms (Table 4, Basilico et al., 1992). 

Buprenorphine is derived from thebaine. It is a partial mu agonist with kappa antagonist activity. Buprenorphine has 25 to 50 times the potency of morphine. It is used to produce a longer-lasting analgesia than morphine. Effects of buprenorphine last longer because it is released more slowly from mu receptors than morphine. It is available as an injectable for intramuscular (IM) or intravenous administration in a 1-ml solution containing 0.3 mg buprenorphine (as buprenorphine HC1) for the relief of moderate to severe pain. It is also available to treat opioid dependence in the formulation of a tablet,51 alone or in combination with naloxone, in 2- or 8-mg... 

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