Опіоїдні анальгетики
Drug | Adult Dose* | Pediatric Dose† | Comments | |||
|---|---|---|---|---|---|---|
Opioid agonists in combination products‡ for moderate pain | ||||||
Codeine | Oral: 30–60 mg every 4–6 hours as needed | — | Less potent than morphine | |||
Hydrocodone | Oral: 5–10 mg every 4–6 hours as needed | — | More potent than codeine | |||
Opioid agonists for moderate-to-severe pain | ||||||
Fentanyl | Transdermal: 12 or 25 mcg/hour every 3 days Transmucosal: 100–200 mcg every 2–4 hours Intranasal: 100–200 mcg every 2–4 hours Parenteral: 25–100 mcg every 30–60 minutes IV or as patient-controlled analgesia | Parenteral: 1–2 mcg/kg/dose IV; may be repeated in 2–4 hours as needed | 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 | |||
Hydromorphone | Oral immediate release: 2–4 mg every 4–6 hours Oral extended-release: 8–32 mg every 24 hours Oral liquid: 2.5–10 mg every 4–6 hours Parenteral: 0.2–1 mg every 4–6 hours or as patient-controlled analgesia Rectal: 3 mg every 6–8 hours | — | Short half-life Rectal form: Used at bedtime | |||
Levorphanol | Oral: 2 mg every 6–8 hours Parenteral: 1–2 mg IM or subcutaneously every 6–8 hours; 1 mg IV every 3–6 hours | — | Long half-life | |||
Meperidine | Oral: 50–300 mg every 4 hours Parenteral: 50–150 mg IV or IM every 4 hours as needed | — | 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 practices | |||
Methadone | Oral: 2.5–10 mg every 8–12 hours Parenteral: 2.5–10 mg IM or IV every 8–12 hours | — | 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 | |||
Morphine | Oral immediate-release: 5–30 mg every 4 hours Oral controlled-release: 15 mg every 12 hours Oral sustained-release: 30 mg every 24 hours Parenteral: 2–5 mg IV or IM every 2–4 hours as needed | > 6 months old and < 50 kg:
> 6 months old and ≥ 50 kg:
| Standard of comparison Triggers histamine release more often than other opioids, causing itching | |||
Oxycodone‡ | Oral: 5–10 mg every 6 hours Oral controlled-release: 10–20 mg every 12 hours | — | Also in combination products containing acetaminophen or aspirin | |||
Oxymorphone | Oral: 5 mg every 4 hours Oral controlled-release: 5–10 mg every 12 hours IM : 1–1.5 mg every 4 hours IV: 0.5 mg every 4 hours Rectal: 5 mg every 4–6 hours | — | May trigger less histamine release than other opioids | |||
Opioid agonist-antagonists§ | ||||||
Buprenorphine | IV or IM: 0.3 mg every 6 hours Sublingual: 75 mcg once a day or, if tolerated, every 12 hours for ≥ 4 days, then increased to 150 mcg every 12 hours Transdermal patch: initially 5mcg/hour applied once a week; may be titrated to 20 mcg/hour once a week | Use only in patients > 13 years (same as adult dose) | Psychotomimetic effects (eg, delirium, sedation) less prominent than those of other agonist-antagonists, but other effects similar Lower risk of respiratory depression with buprenorphine than with traditional analgesics (eg, morphine, fentanyl) but not fully reversible with naloxone Higher affinity for mu receptors than traditional analgesics May induce acute withdrawal if added to long-term opioid therapy Analgesic effect of traditional analgesics possibly limited when they are added to long-term therapy with buprenorphine Sublingual and transdermal buprenorphine used occasionally for chronic pain May be used as agonist therapy in opioid use disorder but requires special licensure | |||
Butorphanol | IV: Initially 1 mg, may be repeated every 3–4 hours as needed; usual range: 0.52 mg every 3–4 hours as needed IM: Initially 2 mg, may be repeated every 3–4 hours as needed; usual range: 1–4 mg every 3–4 hours as needed. Nasal: Initially1 mg (1 spray in one nostril); if adequate relief is not achieved, may be repeated in 60–90 minutes; after the second dose, may be repeated every 3–4 hours as needed | Not recommended | — | |||
Nalbuphine | Parenteral: 10 mg IM, IV, subcutaneous every 3–6 hours | Not recommended | Psychotomimetic effects less prominent than those of pentazocine but more prominent than those of morphine; 2.5–5 mg IV (lower dose) possibly useful for opioid-induced pruritus (may repeat dose once) | |||
Pentazocine | Oral: 50–100 mg every 3–4 hours Parenteral: 30 mg IV, IM, every 3–4 hours (not to exceed 360 mg/day) | Not recommended | Usefulness limited by the following:
Available in tablets combined with naloxone, aspirin, or acetaminophen Can cause confusion and anxiety, especially in older patients | |||
Mu-opioid agonists/norepinephrine reuptake inhibitors | ||||||
Tapentadol | Oral immediate-release: 50–100 mg every 4–6 hours, a second dose ≥ 1 hour later (≤ 700 mg total dose on 1st day); after 1st day, 50–100 mg every 4–6 hours (≤ 600 mg total daily dose) Oral extended-release: 50 mg every 12 hours (usual therapeutic dose of 100–250 mg every 12 hours; maximum 500 mg/day) | — | 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, | |||
Tramadol | Oral immediate-release: 50–100 mg every 4–6 hours; maximum 400 mg/day Oral extended-release: 100 mg once a day; increase by ≤ 100 mg/day every 5 days to a dose of ≤ 300 mg total daily dose | Not recommended | Less potential for abuse than with other opioids Not as potent as other opioid analgesics | |||
* Starting doses are for opioid-naive patients. Patients with opioid tolerance or severe pain may require higher doses. | ||||||
† Not all drugs are appropriate for analgesia in children. | ||||||
‡ 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 drugs of choice for older patients. | ||||||