Cardiac toxicity of anthracycline-treated survivors of childhood cancer. Can J Clin Oncol, 1993, 11(10): 1906 (Received: 2002-10-10; Revised: 2003-09-27). Luo found that buprenorphine has far more applications in the treatment of opioid dependence cases compared to traditional methods.
Authors: Cuibao Qing, Wei Song, Teng Yanxia
Buprenorphine (hereinafter referred to as BUP), with its unique pharmacological properties, has proven effective in clinical practice for both moderate to severe pain relief and the treatment of opioid dependence, detoxification, and maintenance therapy. Extensive clinical practice has demonstrated that buprenorphine holds great promise as a treatment for opioid dependence and addiction.
### 1. Unique Pharmacological Properties of BUP
#### 1.1 Agonist-Antagonist Activity
BUP combines both agonistic and antagonistic activities. It has a high affinity for receptor recognition sites and other receptor agonists such as heroin, morphine, opium, and pethidine. When combined with brain receptors, it can produce analgesia, respiratory inhibition, bradycardia, euphoria, and addiction.
#### 1.2 Antagonistic Activity in Clinical Treatment
BUP's antagonistic activity is evident in its ability to precipitate withdrawal responses. According to literature, when administered within 4 hours after the last dose of morphine, BUP plays a competitive antagonistic role against morphine in animal experiments, inducing withdrawal responses in monkeys. If administered 8 hours after the last dose of morphine or close to the time of withdrawal symptoms, BUP excites and inhibits the occurrence of withdrawal reactions.
BUP is a typical biphasic opioid receptor drug, useful for treating opioid dependence and also for opioid overdose detoxification.
#### 1.3 Absorption and Long Duration of Action
BUP can be stored in fatty tissues, allowing for slow release. Due to its relatively slow interaction dynamics with opioid receptors, especially its very slow dissociation rate, it has a long duration of action. For example, sublingual tablets maintain effects for 8 to 12 hours, while injections last 6 to 8 hours.
#### 1.4 Euphoria and Respiratory Inhibition
BUP induces lighter euphoria and respiratory inhibition, with a ceiling effect.
#### 1.5 Inhibition of Opioid Euphoria Effects
A certain amount of BUP inhibits the euphoric effects of opioids due to its high affinity for opioid receptors, blocking the euphoric experiences of heroin addicts. Additionally, because BUP is a partial agonist, it metabolizes slowly, leading to low dependence and tolerance, much like naltrexone hydrochloride (NXT), which is also used for maintenance medication.
### 2. Application of BUP in Treating Opiate Dependence
Detoxification drug application should follow individual principles (age, body mass, drug abuse history, drug amount, type of poison, frequency of use, and BUP tolerance, etc.). It is necessary to understand the development process of heroin withdrawal symptoms.
Heroin dependence withdrawal syndrome is self-limiting, generally occurring 1 to 3 days after interrupting the drug, peaking on the fourth day, and gradually diminishing thereafter. If untreated, the entire withdrawal process lasts 10 to 14 days, with physical strength gradually recovering. The mechanism of opioid dependence is complex and not yet fully understood. However, since the discovery of opioid receptors, it is generally believed that endogenous opioid peptides (EOP) play a role in regulating systems such as the norepinephrine, histamine, pituitary-gonadal, thyroid, calcium ion channel, AC-cAMP system, and G protein family systems to maintain homeostasis. Opioid addicts taking substances like heroin disrupt this balance, causing negative feedback that inhibits the formation and release of normal EOPs. Once exogenous opioids are interrupted, EOC and EOP deficiencies lead to varying degrees of withdrawal syndrome.
Detoxification treatment involves using various medical measures to help dependent individuals alleviate physical pain and psychological stress, essentially treating anti-withdrawal symptoms.
#### 2.1 BUP Detoxification
① Generally, the first dose is: injection 0.3mg, 0.45 mg, or 0.6mg (intramuscular injection). The timing of the first dose: 4 to 8 hours after the last dose, or close to withdrawal reactions, or between doses, every six to eight hours, with appropriate dose adjustments as needed.
③ Daily dose ranges between 0.9 to 1.8mg.
① On the first day, serious withdrawal symptoms may require an increased dose.
⑤ After the fifth day, the daily dose delivery can be adjusted accordingly.
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