SUBOXONE - the key to freeing your life from addictionSUBOXONE - the key to freeing your life from addiction

FACTSFACTS

• Suboxone is not a new medication; it has been used in other countries since 1975

• Suboxone is similar to Subutex, which is used as a pain drug

• In 2002, the FDA approved Suboxone for opioid addiction

• Suboxone is a sublingual medication that comes in two strengths: 2mg and 8mg tablets

STATISTICSSTATISTICS

9.8 % of hospitalizations in 2008 were due to painkillers

The largest age group of opioid use is 15 years – 24 years

Girls are more likely than boys to abuse painkillers

OUTLINEOUTLINE• Opioids

– Dependence– Definition– Effects on the brain– Abuse– Mechanism of

analgesia• Addiction, Tolerance, and

Dependence• Opioid Dependence• Opioid Addiction• Opioid Addiction

Treatment • Suboxone• bupenorphine• Naloxone• Partial versus Full Opiate

Agonist

• Suboxone Treatment- step-wise therapy

- precautions

- example treatment regimen

• Precautions • Basic Treatment Regimens • Conclusion

OPIOID DEPENDENCEOPIOID DEPENDENCE

• Chronic medical condition

• Specific physiological characteristics– changes in the central nervous system– physiological adaptation to the effects of the opioid– progressive desensitization to the opioid– development of various signs and symptoms that

appear when opioid is withdrawn

OPIOID DEFINITIONOPIOID DEFINITION

Opioid: any compound related to opuimOpiate: drug derived from opium

Opioids are analgesic, or pain-relieving medications▪ oxycodone/Oxycontin ▪ propoxyphene (Darvon)

▪ morphine ▪ hydromorphone (Dilaudid)

▪ fentanyl ▪ meperidine (Demerol) ▪ codeine ▪ Methadone

Opioids exert their effect by mimicking naturally occurring endogenous opioid peptides or endorphins

▪ enkephalin ▪ dynorphins

▪ endorphins

EFFECT OF OPIOIDS ON THE BRAINEFFECT OF OPIOIDS ON THE BRAIN

• Opioids act by attaching opioid receptors

– Brain

– Spinal cord

– Gastrointestinal tract

• When these compounds attach they can effectively change the way a person experiences pain

• Opioid medications can affect regions of the brain that mediate pleasure

– results in initial euphoria

ABUSE OF OPIOIDSABUSE OF OPIOIDS

• Opioids can be taken:– orally– pills may be

• crushed • snorted or • injected

► Dealths due to overdose have resulted from snorting or injecting opioids, particularly OxyContin

- was designed to be a slow-release formulation - Snorting or injecting opioids results in the rapid

release of the drug into the bloodstream, exposing the person to high doses and

causing many of the reported overdose reactions.

MECHANISMS OF OPIOIOD ANALGESICS AND ANTAGONISTSMECHANISMS OF OPIOIOD ANALGESICS AND ANTAGONISTS

Opioid analgesics and antagonists. In: Basic and clinical pharmacology, 8th edition. Katzung BG. USA: The McGraw Hill Companies, Inc, 2001:512–531.

MECHANISM OF DRUGS AFFECTING THE BRAINMECHANISM OF DRUGS AFFECTING THE BRAIN

DEPENDENCE, TOLERANCE, AND ADDICTIONDEPENDENCE, TOLERANCE, AND ADDICTION

• Dependence: a characteristic set of withdraw symptoms occur upon reduction or cessation of the active compound at cell receptors• Chronic use of opioids may cause development of physical

and psychological dependence

• Tolerance: higher and higher doses are needed to achieve the same effect

• Addiction: a chronic, relapsing disease characterized by compulsive drug seeking and abuse despite its known harmful consequences

• May involve physical dependence and tolerance

DEPENDENCE DEPENDENCE

Physical dependence involves two related occurrences:

1. tolerance ` 2. withdrawal

• Tolerance occurs when patients must take more of the drug over time to achieve the same effect

• Physical symptoms of withdrawal:- myalgia- cramps - diarrhea

• Psychological symptoms of withdraw: - anxiety,- craving- insomnia

OPIOID ADDICTIONOPIOID ADDICTION

• Addiction: occurs when patients find the psychoactive effects of a drug so emphasized that it results in difficultly controlling use of the drug

• Addiction is characterized by the four Cs: – loss of Control over use– continued use despite

knowledge of harmful

Consequences

– Compulsion to use

– Craving

OPIOID ADDICTION TREATMENTOPIOID ADDICTION TREATMENT

• Medically supervised detoxification may need to be performed to help reduce withdrawal symptoms

• Behavioral treatments in addition to medications, have also been proven effective

• Currently used medications in opiod addiction are—

- Methadone, a synthetic opioid that eliminates withdrawal symptoms and relieves craving, has been used successfully in treatment for heroin addiction as well as opiates

- Buprenorphine, another synthetic opioid, is a more recently approved medication for treating addiction to heroin and other opiates.

- Naltrexone is a long-acting opioid receptor blocker that can be used to help prevent relapse. It is not widely used because of poor compliance, except by highly motivated individuals (e.g., physicians at risk of losing their medical license). It should be noted that this medication can only be used for someone who has already been detoxified, since it can produce severe withdrawal symptoms in a person continuing to abuse opioids.

- Naloxone is a short-acting opioid receptor blocker that counteracts the effects of opioids and can be used to treat overdoses

SUBOXONESUBOXONE

• Mixture of 2 agents combined into one pill– buprenorphine:naloxone 4:1

preparation

• Hexagonal orange tablets in 2 dosage strengths

• Taken sublingually Buprenophine

- antagonist at the mu-opioid receptor Naloxone

- Opioid receptor antagonist

BUPRENOPHINE – (SUBUTEX) BUPRENOPHINE – (SUBUTEX) • Partial agonist at the mu opioid receptor

• High binding affinity at this receptor

• MOA:- acts on the brain’s opiate receptors to relieve withdrawal and cravings without stimulating the same intense high or dangerous side effects as other opioids

• USES:- treats opioid addition at higher doses (< 2mg)- controls moderate pain in non-opioid tolerant patients in

- lower dosages (~200 µg). - indicated for the use of opioiod dependence

• At adequate doses,buprenophine prevents other opioids from attaching to those receptors, blocking their effects.

NALOXONE NALOXONE

• Opioid Antagonist – Competitive agonists– bind to the opioid receptors with higher affinity than

agonists but do not activate receptors– This effectively blocks the receptor, preventing the

body from responding to opiates and endorphins

• Naloxone is present in Suboxone to help deter diversion/misuse– When suboxone is crushed or injected by individuals

dependent upon the drug or who have recently used a full opioid agonist or heroin, the naloxone component causes immediate withdrawal symptoms

SUBOXONE TREATMENTSUBOXONE TREATMENT

• 5-Steps of Suboxone Treatment1. Intake

► Seen by physician

2. Induction

► Inpatient, in office, or at home

3. Stabilization

► First week determines dose

4. Maintenance

► Typically from 6-12 months

5. Medically supervised withdraw

PRECAUTIONSPRECAUTIONS

• Need stable living situation• Need support system

– Support group recommended• Avoid benzodiazepines • Avoid alcohol• Cost of medication• Avoid Pregnancy

– Use Subutex• Limit filling prescription to• Drug Interactions• Has potential to cause

– Liver, Kidney, and Lung Impairment– Brain functioning depression– Blood pressure abnormalities

BASIC TREATMENT REGIMENBASIC TREATMENT REGIMEN

• Day 1– Depending on the individulized

patient as well as the doctor, starting doses may range substantiall

• Day 2– The dose regimen that the patient was

on (successfully) plus 2 mg should be used as a day 2 regimen

• Maintainance Dose– The dose the patient ended up taking

on day two will become their maintainence dose

• PRN Doses– Incase of cravings

• Suboxone provides an easy way to detox from opioids for both physicians and patients. It minimizes undesirable withdraw effects for the patient and is easy to take.

• This drug is essentially harmless and can greatly improve lives of those addicted to opioids!

• Questions?