November 2008 

What is opioid dependence/addiction? 

Taking strong opioid painkillers, in large doses, for an extended period of time, can cause physical dependence in humans.

This means when the medication is discontinued abruptly, withdrawal symptoms occur. This is normal physiology and does not require addiction treatment.

However, if an uncontrollable compulsion develops and is accompanied by an increased quantity of drug to achieve the same effect, and opioid use continues despite negative consequences, such as loss of a job, then these conditions may be considered addiction and may require treatment. 

Opioid addiction is a brain disease 

Opioid addiction is a treatable chronic brain disease precipitated by fundamental, long-term, changes to the structure and functioning of this organ. Once someone becomes addicted, areas of the brain are altered from the normal healthy state. This is why addiction is classified as a disease. These are physical changes to the brain – not caused by lack of morals, controlled by willpower, nor cured by good advice. It’s a disease as is diabetes or cancer, and it is treatable. 

The Drug Addiction Treatment Act of 2000 (DATA 2000) 

The Act enables qualified physicians to prescribe and/or dispense opioid medications for the purpose of treating opioid dependency (addiction).

For the first time in over 30 years, physicians are able to treat this disease from their private offices or other clinical settings.

This presents a very desirable treatment option for those who are unwilling or unable to seek help in drug treatment clinics. Patients can now be treated in the privacy of their doctor’s office. One medication doctors may now prescribe is buprenorphine.

What is Buprenorphine? 

Buprenorphine (Byoo-pre-nor-feen) has been used in the U.S. to treat pain and in Europe to treat opioid dependence (addiction) for over 10 years. Buprenorphine is a semi-synthetic opioid and is a partial agonist. 

• Opioid Agonists are drugs that cause an opioid effect like heroin, oxycodone, hydrocodone, and methadone. 

• Opioid Antagonists are drugs that block and reverse the effects of agonist drugs. Narcan® is an antagonist and is used to reverse heroin overdoses.

Buprenorphine acts like both an agonist and antagonist. Buprenorphine attaches to the opioid receptors but only activates them partially. Even when all available receptors are occupied with buprenorphine the total opioid effect is relatively low. This is observed as a ceiling effect.

Beyond a certain dose, effects of more buprenorphine are not detected by the patient. The antagonist property of the medication “kicks off” and blocks other opioids from the opioid receptor sites.

Therefore, even if the patient decides to misuse opioid drugs after taking buprenorphine, the effects can be blocked, depending on dosage. Other opioids continue to provide more effect as more is taken, eventually leading to respiratory depression and death.

Buprenorphine is different; its effects level off at a relatively low dose. That is, even if more is taken, there are no significant increased effects. This helps lower the risk of overdose and misuse.