Lecture 77 - Non-Malignant Pain Part 3 Flashcards
Opioids
Uses: Acute and chronic pain
Side effects: Antitussive; Constipation; Nausea & vomiting; Itching; Orthostatic Hypotension; Urinary Retention; Sedation; Respiratory depression
Clinical pearls: Consider starting stool softener and/or stimulant laxative; Potential for tolerance, dependence and addiction; Schedule II controlled substances - Exceptions: tramadol, codeine
Opioids: Codeine (Tylenol #3)
Available formulations: Tablet; Cough syrup Clinical pearls: Schedule V, III or II controlled substance, depending on strength; Metabolized to morphine via CYP 2D6 - Poor metabolizers will get no effect from codeine, Ultra-rapid metabolizers can experience overdose resulting in respiratory depression and death, especially in children, Not recommended in breastfeeding mothers or children < 12
Opioids: Tramadol (Ultram- Discontinued, ConZip, Qdolo)
Available formulations: Capsule ER 24hr (Conzip); Tablet- IR and ER 24hr; Oral solution; Combination products with acetaminophen and celecoxib available
Clinical pearls: Risk of serotonin syndrome when used with other serotonergic medications; Renally dose adjusted; US Boxed Warning: Use of CYP 450 3A4 inducers, 3A4 inhibitors, and 2D6 inhibitors with tramadol requires careful consideration of the effects on the parent drug and metabolite; Schedule IV controlled substance
Opioids: Morphine
Available formulations: Capsule ER 24 hr; Tablet - IR and 12 hr ER (MS Contin®); Oral solution; Solution for injection (IM, IV, subQ); Suppository; Abuse-deterrent tablet - DISCONTINUED
Clinical pearls: Itching more prominent compared to other opioids; Morphine and its metabolites are renally excreted and accumulate in renal dysfunction - Avoid in patients with end stage renal disease or acute kidney injury; US Boxed Warning: Avoid alcohol while taking ER capsules- leads to increased morphine plasma levels and potentially fatal overdose.
Opioids: Hydromorphone (Dilaudid)
Available formulations: IR and ER tablets; Oral solution; Solution for injection; Suppository
Clinical pearls: US Boxed Warning about dosing errors when prescribing, dispensing an administering: Oral solution- do not confuse mg and mL, IV solution- do not confuse high potency solution (10mg/mL) with other solutions (1, 2 or 4mg/mL)
Opioids: Hydrocodone +/- Acetaminophen (Combination products are all generic- discontinued brands are Norco, Lortab, Vicodin)
Available formulations: Oral solution; ER tablet (Hysingla); Tablet - Norco 5/325mg, 7.5/325mg, 10/325mg
Clinical pearls: Counsel patients on acetaminophen use; US Boxed Warning: Use with CYP 3A4 inhibitors may increase hydrocodone plasma concentrations
Opioids: Oxycodone (Oxycontin, Xtampza) Oxycodone and Acetaminophen (Percocet)
Available formulations: Tablet (IR and ER 12 hr); Capsule (IR and ER 12 hr); Oral solution
Clinical pearls: Counsel patients on acetaminophen use with combination product
- Percocet 2.5/325mg, 5/325mg, 7.5/325mg, 10/325mg; ER capsule/tablets are abuse-deterrent; US Boxed Warning: Use with CYP 3A4 inhibitors may increase oxycodone plasma concentrations
Opioids: Fentanyl
Available formulations: Buccal tablet; Sublingual liquid; Lozenge; Injectable solution; Patch
Clinical pearls: US Boxed Warning: Monitor patients receiving CYP3A4 inhibitors or inducers; Can use in renal impairment; Less hypotension than morphine or hydromorphone at similar doses; Non-injectable forms are ONLY indicated for patients who are opioid tolerant - Opioid tolerant is defined as taking morphine 60mg per day (or equivalent) for at least 1 week, Doses are NOT converted from one fentanyl product to another on a mcg-per-mcg basis
Fentanyl (Duragesic) Patch Counselling
Apply one patch every 72 hours (3 days)
Apply the patch to the chest, back, flank, or
upper arm
Do not cut the patches or use a patch that is torn or damaged - This could cause an overdose
Do not use the patch over broken skin
Do not let the patch get too warm while wearing
- Avoid using heating pad, electric blanket, sauna, hot tub, heated waterbed, sunlight, or hot weather; Your body will absorb too much medication
Opioids: Methadone (Methadose)
Uses: Last line treatment of chronic pain; Opioid detoxification
Available formulations: Oral solution; Injectable solution; Tablet
Clinical pearls: US Boxed Warning: QTc prolongation - Check baseline ECG prior to initiation; US Boxed Warning: Monitor patients receiving CYP 3A4 inhibitors or inducers; Long half life (8-59 hours)
Opioids: Meperidine (Demerol)
Available formulations: Injectable solution; Oral solution; Tablet
Clinical pearls: Avoid in the elderly, avoid in renal impairment, caution use in hepatic impairment; US Boxed Warning: Monitor patients receiving CYP 3A4 inhibitors or inducers; US Boxed Warning: Do not use within 14 days of monoamine oxidase inhibitors (MAOI’s); Metabolized by the liver into an active metabolite - Accumulation of active metabolite can cause
delirium and seizures; Not commonly used due to adverse effects
Potential Side Effects
Several of the opioids have serotonergic activity and have potential to:
1. Lower seizure threshold
2. Cause serotonin syndrome when used with other agents with serotonergic activity
especially tramadol
Allergic Cross Reaction - natural opiates
Morphine, Codeine
Yes: Avoid in patients with allergy to other natural opiates and semi synthetic opioids
Allergic Cross Reaction - semi synthetic opioids
Hydromorphone, Oxycodone, Oxymorphone, Hydrocodone, Buprenorphine
Yes: Avoid in patients with allergy to other semi synthetic opioids and natural opiates
Allergic Cross Reaction - synthetic opioids
Fentanyl, Methadone, Meperidine, Tramadol
No: Can be used if patient has an allergy to another synthetic opioid, semi synthetic opioid or natural opiate
