Terminology
Natural Opiates |
Semi-Synthetic |
Synthetic Opioids |
Codeine |
Burprenorphine |
Fentanyl |
Morphine |
Heroin |
Meperidine |
| |
Hydrocodone |
Methadone |
| |
Hydromorphone |
Sufentanil |
| |
Oxycodone |
Sufentanil |
| |
Oxymorphone |
| |
Tramadol |
PATHOPHYSIOLOGY
Risk 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 Tools
Score |
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
NALOXONE
MOA |
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 WITHDRAWAL
Dysphoric mood |
Fever |
Lacrimation or Rhinorrhea |
Muscle aches |
Yawning |
Diarrhea |
N/V |
Insomnia |
Pupillary Dilartion |
Piloerection (goosebumps) |
Sweating |
WITHDRAWAL TIMELINE
Onset 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 treatment
Methadone |
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 |
|
|
Terms
Opioid 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 CRITERIA
A 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 TREATMENT
APA |
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)
Methadone
Brand |
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 INTOXICATION
Pulillary Constriction |
Slurred Speech |
Drowsiness |
Impaired attention or memory |
Signs and Sx of Opioid OVERDOSE
Pupillary constriction |
Shallow or slow respirations |
Stupor |
Coma |
Hypothermia |
Bradycardia |
Narcan Formulations
Naloxone |
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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