Commonly used, oral and transdermal, long-acting pure mu-opioid agonists for chronic pain in adults (refer to notes)

Drug	Brand name (United States)	Sample initial dose in opioid-tolerant adults	Serum half-life (hours)	Duration of analgesic effect (hours)	Comments
Oral, long-acting preparations
Hydrocodone	Hysingla ER	20 mg orally every 24 hours	7 to 9	24	Use a reduced dose in kidney and/or hepatic impairment May interact with drugs that alter CYP3A4 and CYP2D6 metabolism* Converted to active metabolite by CYP2D6, which is subject to polymorphisms; individual effects vary Hysingla ER and Zohydro ER have abuse-deterrent^¶ properties
Hydrocodone	Zohydro ER (brand not available; generic only)	10 mg orally every 12 hours	13	≤12 in patients with non-cancer back pain
Hydromorphone	Exalgo	8 mg orally every 24 hours	11	24	Use a reduced dose in kidney and/or hepatic impairment Non-CYP metabolism (ie, glucuronidation) may be an advantage for patients receiving drugs that significantly alter CYP3A4 metabolism Exalgo has abuse-deterrent^¶ properties
Hydromorphone	Hydromorph Contin (available in Canada)	3 mg orally every 12 hours	Not specified	≥12
Morphine	MS Contin	15 mg orally every 8 or 12 hours	Not specified	8 to 12	Active metabolites are dependent on kidney function for clearance; avoid or use a reduced dose frequency in organ dysfunction Accumulation of metabolite may contribute to hyperalgesia or other neurotoxicity Non-CYP metabolism (ie, glucuronidation) may be an advantage for patients receiving drugs that significantly alter CYP3A4 metabolism May interact with drugs that inhibit P-glycoprotein (P-gp) efflux* Capsule (Kadian) may be opened and sprinkled on soft food for immediate swallowing
Morphine	Kadian (brand not available; generic only)	30 mg orally daily in 1 or 2 divided doses	11 to 13	12 to 24
Oxycodone	OxyContin	10 mg orally every 12 hours	4.5	8 to 12	Use a reduced dose in kidney and/or hepatic impairment. May interact with drugs that alter CYP3A4 metabolism. OxyContin has abuse-deterrent^¶ properties. Xtampza ER has abuse-deterrent^¶ properties; capsule may be opened and sprinkled on soft food for immediate swallowing. Xtampza ER doses are expressed as oxycodone base*. 9 mg oxycodone base is equivalent to 10 mg oxycodone hydrochloride (OxyContin).
Oxycodone	Xtampza ER	9 mg orally every 12 hours	5.6	≤12
Oxymorphone	Generic only	5 mg orally every 12 hours	9 to 11	12	Use a reduced dose in kidney and/or hepatic impairment Take on empty stomach Opana ER brand, an abuse-deterrent formulation, was withdrawn from the United States market in mid-2017 due to concerns related to IV injection abuse, including reports of thrombotic microangiopathy; generic extended-release preparations of oxymorphone remain available
Tapentadol	Nucynta ER	50 mg orally every 12 hours	5 to 6	12	Inhibits norepinephrine reuptake Avoid in patients with severe kidney impairment (CrCl <30 mL/minute) Use a reduced dose in moderate liver dysfunction, avoid use with severe hepatic dysfunction Risk for serotonin syndrome in patients using MAOI, SSRI, SNRI, and TCA medications Generally reserved for third-line use
Transdermal
Fentanyl	Duragesic	12 or 25 mcg per hour, patch applied every 72 hours	20 to 27 following patch removal	48 to 72 Some analgesic effect may persist following patch removal due to continued absorption from skin	Use a reduced dose in kidney and/or hepatic impairment May interact with drugs that alter CYP3A4 metabolism* Onset of analgesic effect is delayed 12 to 24 hours after initial application Approximate dose conversions for fentanyl transdermal and commonly used oral opioids are provided as a separate table in UpToDate

NOTES:

The total daily dose requirement for a long-acting opioid formulation should be established first with the use of an appropriate immediate-release opioid analgesic. Details for initiating and adjustment of dose vary by each agent. Refer to UpToDate reviews on chronic non-cancer and cancer pain management with opioids and individual drug monographs (ie, Lexicomp) for detailed information on individual agents.
Opioids have similar equianalgesic potency whether administered as an immediate-release form (ie, smaller, more frequently divided doses) or an extended-release preparation. To convert from an oral immediate-release to an extended-release preparation of the same opioid, use the sum of the doses of the immediate-release form administered during the usual interval of the extended-release form. As an example, morphine sulfate immediate-release 30 mg orally every 4 hours (total of 180 mg per day) may be converted to morphine sulfate extended-release 60 mg orally every 8 hours (total of 180 mg per day).
Approximate equianalgesic dose equivalents and information on oral immediate-release and parenteral pure mu-opioid agonists that are commonly used in management of chronic non-cancer and cancer-related pain are provided as separate tables within UpToDate.

CYP3A4: cytochrome P450 3A4; CYP2D6: cytochrome P450 2D6; IV: intravenous; mcg: microgram; ER: extended-release; P-gp: P-glycoprotein; MAOI: monoamine oxidase inhibitor; SSRI: selective serotonin reuptake inhibitor; SNRI: serotonin-norepinephrine reuptake inhibitor; TCA: tricyclic antidepressants; CrCl: creatinine clearance.

* Lists of drugs that alter CYP3A4 metabolism or P-gp multidrug efflux transporter (ie, inhibitors and inducers) are available as separate tables in UpToDate. To determine drug interactions and management suggestions for specific combinations, use the Lexicomp drug interactions program included within UpToDate.

¶ Abuse-deterrent formulations have 1 or more properties that make intentional manipulation of the dose form more difficult (eg, resistant to crushing and dissolution) or less likely to produce an opioid effect (eg, altered to minimize absorption through nasal mucosa). No oral opioid formulation prevents ingestion of an excessive dose.

Courtesy of Kathleen Broglio, DNP, MN, ANP-BC, ACHPN and Russell K Portenoy, MD.

Additional data from:

National Comprehensive Cancer Network. Adult Cancer Pain, Version 2.2016.

Graphic 111207 Version 18.0

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Commonly used, oral and transdermal, long-acting pure mu-opioid agonists for chronic pain in adults (refer to notes)