TerminologyNatural Opiates | Semi-Synthetic | Synthetic Opioids | Codeine | Burprenorphine | Fentanyl | Morphine | Heroin | Meperidine | | | Hydrocodone | Methadone | | | Hydromorphone | Sufentanil | | | Oxycodone | Sufentanil | | | Oxymorphone | | | Tramadol |
PATHOPHYSIOLOGYRisk Factors: males, history of depression or anxiety, family history of alcohol or drug abuse, age ≤ 30, long-term opioid use
Involves the mesolimbic reward system |
Standardized Assessment ToolsScore | Severity | 5 to 12 | Mild | 13 to 24 | Moderate | 25 to 36 | Moderate to Severe | > 36 | Severe |
COWS: Clinical Opiate Withdrawal Scale
• used clinically to monitor withdrawal
• often utilized to determine when PRNs are needed NALOXONEMOA | Opioid Antagonist | Warnings/ADRs | Cardiac or respiratory effects associated with rapid reversal of opioids | | | Aggression (from immediate withdrawal) | Administration | Call 911 FIRST | | | Administer | | | If no response after 3 minutes, administer 2nd dose |
• It only works on opioid receptors!
• It will NOT affect someone (positively or negatively) if they do not have opioids in their system Opioid Use Disorder | TREATMENT| | FIRST LINE | SECOND LINE | APA: | | | Buprenorphine | Naltrexone PO | | | Methadone | BAP: | | | Buprenorphine | Naltrexone PO | | | Methadone | VA/DOD: | | | Suboxone | Naltrexone | | | Buprenorphine | | | Methadone |
Psychosocial treatment is also the first line in addition to pharmacotherapy Buprenorphine Formulations| | Buprenorphine | Buprenorphine-Naloxone | Brand | Subutex | Suboxone, Zubsolv | MOA | Mu opiate receptor - partial agonist | Mu-partial agonist and opioid antagonists | Formulation | SL tablet | SL tablet, SL film; (4:1 ratio of bupren. and naloxone) | Dosing range | 8 to 32 mg bupren./day | 8 to 32 mg bupren/day | Warnings | initiation should not begin until pt is experiencing withdrawal | same | | | respiratory depression | same | | | risk of abuse or dependence | same | DDIs | CYP3A4 inhibitors/inducers | same | | | CNS depresants | same | Monitoring | Tolerability, resp. depression, (LFTs), urine drug screening, PMP, urine buprenorphine | same | Clinical Pearls | Preferred in pregnancy; higher abuse potential | naloxone added as an abuse deterrent; preferred formulation in non-pregnant patients | | | partial agonist activity results in ceiling effect, higher binding affinity than other opioids, newer formulation include sub-dermal implant, and subcutaneous injection | same |
Prescribing Restrictions:
Schedule III
DATA waiver
Initial no. of pts is 30
May apply 1 year to increase no. of patients to 100, then 275
DEA number will begin with X Signs and Sx of opioid WITHDRAWALDysphoric mood | Fever | Lacrimation or Rhinorrhea | Muscle aches | Yawning | Diarrhea | N/V | Insomnia | Pupillary Dilartion | Piloerection (goosebumps) | Sweating |
WITHDRAWAL TIMELINEOnset of withdrawal will depend upon the half-life of the opioid used (normally within 36 to 72 hours) | Completed within 7 days for short acting opioids (heroin) and 14 days for long-acting opioids (buprenorphine, methadone) |
Preferred treatmentMethadone | buprenorphine | Chronic Pain | Prolonged QT interval | history or diversion or pilysubstance use | not able to attend daily clinic | requires closer monitoring | requires less monitoring and no untreated psychiatric comorbidities | pregnant women | dependent on lower doses of opioids (ceiling effect) | requires wide dosing range |
| | TermsOpioid Tolerance | Person using opioids begins to experience a reduced response to medication requiring more opioids to experience the same effect | Opioid Dependence | Occurs when the body adjusts its normal functioning around regular opioid use (unpleasant physical symptoms occurs when med is stopped) | Opioid Addiction | Occurs when attempts to cut down use are unsuccessful or when results insocial problems and a failure to fulfill obligations; often comes after person has developed opioid tolerance and dependence |
DSM-5 DIAGNOSTIC CRITERIAA problematic pattern of substance use leading to clinically significant impairment or distress, manifested by ≥ 2 of the following over a 12-month period | ⓵ Substance is taken in larger amounts or over a longer period than intended | ⓶ Persistent desire or unsuccessful efforts to reduce or control use | ⓷ A great deal of time is spent in activities necessary to obtain, use, or recover from effects | ⓸ Cravings or a strong desire to use | ⓹ Recurrent use resulting in a failure to fulfill major obligations | ⓺ Continued use despite having persistent social or interpersonal problems caused by the substance | ⓻ Important social, occupational, or recreational activities are given up or reduced | ⓼ Recurrent use in situations that are physically hazardous | ⓽ Recurrent use despite knowledge of having a persistent or recurrent physical or psychological problem due to use | ⓾ Tolerance | ⑪ Withdrawal |
FIRST - LINE TREATMENTAPA | British Association of Psychopharmacology | Buprenorphine | Alpha-2 agonist | Methadone | Buprenorphine | | | Methadone |
Targeted at individual symptoms of withdrawal
Common practice if an opioid treatment program (OTP) or bridging medication-assisted treatment (MAT) MethadoneBrand | METHADOSE | MOA | opioid agonist | Formulation | Liquid (opioid maintenance); tablets (pain only) | this is for pharmacies (methadone clinics do tabs) | Maintenance dose | 80 to 120 mg daily | Warnings | QTc prolongation, respiratory depression, risk of abuse or dependence | DDI | QTc prolongating meds, CYP3A4 inhibitors or inducers, Medications that induce hypokalemia, hypocalcemia, or hypomagnesemia; CNS depressants | Monitoring | Tolerability, respiratory depression, HR/BP, EKG, electrolytes, UDS, urine methadone, PMP | Clinical Pearls | prolonged or delayed withdrawal due to long half-life; overdose risk is highest during initial 2 weeks of treatment |
Prescribing restrictions:
- schedule II; restricted to certified opioid treatment program (OTP)
- it is not appropriate to dispense methadone from a community pharmacy for the purposes of opioid detox, withdrawal, or maintenance
- pts must be currently addicted and have opioid use disorder ≥ 1 year
- exceptions: pregnancy, recently released from correction, and previous treatment in OTP
know difference between prescribing of methadone and buprenorphine Signs and Sx of INTOXICATIONPulillary Constriction | Slurred Speech | Drowsiness | Impaired attention or memory |
Signs and Sx of Opioid OVERDOSEPupillary constriction | Shallow or slow respirations | Stupor | Coma | Hypothermia | Bradycardia |
Narcan FormulationsNaloxone | IM/IV/SQ | Naloxone | Intranasal | Evzio | IM auto-injector | Narcan | Intranasal |
SYMPTOMATIC TREATMENT (PRN)Medication | Class/MOA | Indication | Clonidine | Alpha-2 agonist reduced the noradrenergic hyperactivity associated with opioid withdrawal | Generalized Sx of opioid withdrawal | Loperamide | Anti-diarrheal | Diarrhea | Ondansetron | Antiemetic | N/V | Trazodone | Sedatine antidepressant | Insomnia | Hydroxyzine | Antihistamine/anxiolytic | Anxiety | Ibuprofen | NSAID | muscle pain | Cyclobenzaprine | skeletal muscle relaxant | muscle cramps |
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