Opioid Analgesics
Medication* | Route of Administration | Comments* |
|---|---|---|
Opioid agonists in combination products† for moderate pain | ||
CodeineCodeine | Oral | Less potent than morphineLess potent than morphine Metabolized to morphine by CYP2D6 and due to its pharmacogenomic variability, not recommended in children and breastfeeding patients Metabolized to morphine by CYP2D6 and due to its pharmacogenomic variability, not recommended in children and breastfeeding patients Found in combination products with acetaminophen, aspirin, ibuprofen, guaifenesin, promethazine, and others and used for cough suppression.Found in combination products with acetaminophen, aspirin, ibuprofen, guaifenesin, promethazine, and others and used for cough suppression. |
HydrocodoneHydrocodone | Oral | More potent than codeineMore potent than codeine Found in combination with acetaminophen, ibuprofen and other medications. Found in combination with acetaminophen, ibuprofen and other medications. |
Opioid agonists for moderate-to-severe pain | ||
FentanylFentanyl | Transdermal, transmucosal, intranasal, IV | May trigger less histamine release and thus may cause less hypotension than other opioids Transdermal: When used in cachectic patients, may result in erratic absorption and blood levels Supplemental analgesia required at first because peak analgesia does not occur until 18–24 hours after application May take many hours for adverse effects to resolve after removing patch Short-acting transmucosal and intranasal forms: Used for breakthrough pain in opioid-tolerant adults and for conscious sedation in children IV form: Sometimes used for procedural sedation |
HydromorphoneHydromorphone | Oral, IV, IM, subcutaneous, rectal | Short half-life Rectal form: Used at bedtime |
LevorphanolLevorphanol | Oral, IV, IM | Long half-life |
MeperidineMeperidine | Oral, IV, IM | Not preferred because its active metabolite (normeperidine) causes dysphoria and central nervous system excitation (eg, myoclonus, tremulousness, seizures) and accumulates for days after dosing is begun, particularly in patients with renal failure Because of these risks, use of meperidine for pain management discouraged and meperidine no longer used in some practicesBecause of these risks, use of meperidine for pain management discouraged and meperidine no longer used in some practices Has anticholinergic properties which can cause tachycardia as well as pupillary dilation |
MethadoneMethadone | Oral, IV, IM | Used for treatment of heroin withdrawal, long-term maintenance treatment of opioid use disorder, and analgesia for chronic pain Establishment of a safe, effective dose for analgesia complicated by its long half-life (usually much longer than duration of analgesia) Requires close monitoring for several days or more after amount or frequency of dose is increased because serious toxicity can occur as the plasma level rises to steady state Risk of QT-interval prolongation; ECG monitoring recommended |
MorphineMorphine | Oral, IV, IM | Standard of comparison Triggers histamine release more often than other opioids, can cause itching; all opioids can cause pruritis by direct opioid agonist action independent of histamine release Can cause respiratory depression, sedation, and central nervous system excitation (eg, myoclonus) in renal failure due to accumulation of its active metabolites (morphine-6-glucuronide and morphine-3-glucuronide) Can cause respiratory depression, sedation, and central nervous system excitation (eg, myoclonus) in renal failure due to accumulation of its active metabolites (morphine-6-glucuronide and morphine-3-glucuronide) |
Oxycodone†Oxycodone† | Oral | Also in combination products containing acetaminophen or aspirinAlso in combination products containing acetaminophen or aspirin |
OxymorphoneOxymorphone | Oral, IV, IM, rectal | May trigger less histamine release than other opioids |
Opioid agonist-antagonists‡ | ||
BuprenorphineBuprenorphine | IV, IM, sublingual, transdermal patch | Lower risk of psychotomimetic effects (eg, delirium, sedation) compared with other agonist-antagonists, but other side effects are similar Higher affinity for mu receptors than most other opioids but similar mu receptor affinity as hydromorphone and sufentanil. Higher affinity for mu receptors than most other opioids but similar mu receptor affinity as hydromorphone and sufentanil. Requires higher dosing for reversal with naloxone and may not be fully reversible. Requires higher dosing for reversal with naloxone and may not be fully reversible. May induce acute withdrawal if administered to patients on full agonist therapy. Analgesic effect of other opioids possibly limited when they are added to long-term therapy with buprenorphineAnalgesic effect of other opioids possibly limited when they are added to long-term therapy with buprenorphine Sublingual, buccal and transdermal buprenorphine used occasionally for Sublingual, buccal and transdermal buprenorphine used occasionally forchronic pain (intradermal available for opioid use disorder). May be used as opioid replacement therapy in opioid use disorder |
ButorphanolButorphanol | IV, IM, intranasal | — |
NalbuphineNalbuphine | IM, IV, subcutaneous | Psychotomimetic effects less prominent than those of pentazocine but more prominent than those of morphine; lower dose (eg, 2.5–5 mg IV) possibly useful for opioid-induced pruritusPsychotomimetic effects less prominent than those of pentazocine but more prominent than those of morphine; lower dose (eg, 2.5–5 mg IV) possibly useful for opioid-induced pruritus |
Pentazocine | Oral, IV, IM | Usefulness limited by the following:
Available in tablets combined with naloxone, aspirin, or acetaminophenAvailable in tablets combined with naloxone, aspirin, or acetaminophen Can cause confusion and anxiety, especially in older patients |
Mu-opioid agonists/norepinephrine reuptake inhibitorsMu-opioid agonists/norepinephrine reuptake inhibitors | ||
TapentadolTapentadol | Oral | Used to treat neuropathic pain due to diabetes, moderate to severe acute pain, and moderate to severe chronic pain Reported to have fewer frequent adverse effects (eg, constipation) than other opioids. Very weak serotonin reuptake inhibition |
TramadolTramadol | Oral | Less potential for abuse than with other opioids Not as potent as other opioid analgesics Inhibits serotonin reuptake and may cause serotonin syndrome in combination with other medications |
* Not all medications are appropriate for analgesia in children (eg, tramadol, codeine, buprenorphine, butorphanol, nalbuphine, pentazocine).* Not all medications are appropriate for analgesia in children (eg, tramadol, codeine, buprenorphine, butorphanol, nalbuphine, pentazocine). | ||
† These opioid agonists may be combined into a single pill with acetaminophen, aspirin, or ibuprofen. They are often used alone so that acetaminophen, aspirin, or ibuprofen dosing limits do not limit opioid dosing. If combination therapy is desired, acetaminophen, aspirin, or ibuprofen can be added separately while maximizing flexibility in dosing the opioid agonist.† These opioid agonists may be combined into a single pill with acetaminophen, aspirin, or ibuprofen. They are often used alone so that acetaminophen, aspirin, or ibuprofen dosing limits do not limit opioid dosing. If combination therapy is desired, acetaminophen, aspirin, or ibuprofen can be added separately while maximizing flexibility in dosing the opioid agonist. | ||
‡ Opioid agonist-antagonists are not usually used for chronic pain and are rarely analgesics of choice for older patients. | ||