Pharmacokinetics and Bioavailability of Hydromorphone Following Intravenous and Oral Administration to Human Subjects

Vallner, J.J.; Stewart, James T.; Kotzan, Jeffrey A.; Kirsten, Edward B.; Honigberg, I. L.

doi:10.1002/j.1552-4604.1981.tb05693.x

Cited by 118 publications

(59 citation statements)

References 6 publications

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“…Hydromorphone is absorbed by first-order kinetics after both oral and rectal administration with biphasic absorption; an initial phase (up to 2 h) of fast absorption, followed by a slower phase [80]. Absorption is mainly from the upper small intestine [107]. Peak plasma levels coincide with analgesia.…”

Section: Oralmentioning

confidence: 99%

“…The Council of the League of Nations appointed a committee to consider the advantages and disadvantages of hydromorphone compared with other opioids [29,66]. The pharmacokinetics in humans following intravenous and oral administration were first studied in 1981 [80,107]. This article is based on a review of the human and animal literature published in English (Medline search 1965-1999, using "hydromorphone" and a combination of "hydromorphone" and "cancer" and "hydromorphone" and "pain" as keywords).…”

Section: Introductionmentioning

confidence: 99%

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Hydromorphone: pharmacology and clinical applications in cancer patients

Sarhill

Walsh

Nelson

2001

Support Care Cancer

145

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Hydromorphone is a more potent opioid analgesic than morphine and is used for moderate to severe pain. It can be administered by injection, by infusion, by mouth, and rectally. Oral bioavailability is low. The kidney excretes hydromorphone and its metabolites. Some metabolites may have greater analgesic activity than hydromorphone itself but are unlikely to contribute to the pharmacological activity of hydromorphone. With the exception of pruritus, sedation and nausea and vomiting, which may occur less after hydromorphone than after morphine, the side-effects of these drugs are similar. On a milligram basis hydromorphone is five times as potent as morphine when given by the oral route, and 8.5 times as potent as morphine when given intravenously.

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Section: Oralmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Hydromorphone: pharmacology and clinical applications in cancer patients

Sarhill

Walsh

Nelson

2001

Support Care Cancer

145

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“…Oxycodone and hydromorphone have moderate intestinal permeabilities with a bioavailability of 60-87% and 62%, respectively, whereas oxymorphone has a low bioavailability of 10% (11,14,15). Atenolol and metoprolol experiments were carried out to evaluate alcohol effects on low and high permeability drugs, respectively (16).…”

Section: Introductionmentioning

confidence: 99%

Effect of Ethanol on Opioid Drug Permeability Through Caco-2 Cell Monolayers

Volpe

Asafu-Adjaye

Ellison

et al. 2008

AAPS J

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“…Although plasma concentrations of hydromorphone have been studied in humans using high performance liquid chromatography (HPLC) (7) and radioimmunoassay methods (12,20), little is reported about the relationship between concentrations and pharmacodynamic effects of the drug.…”

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confidence: 99%

Analgesic and Nonanalgesic Effects of Intravenous Hydromorphone ‐ Relation to Plasma Concentrations in Healthy Volunteers

Westerling¹,

Björk²,

Svedman³

et al. 1996

Pain Research and Management

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Analgesic and nonanalgesic effects ofintravenous hydromorphone -Relation to plasma concentrations in healthy volunteers. Pain Res Manage 1996;1(2):86-92.OBJECTIVE: To investigate the analgesic and nonanalgesic effects and the pharmacokinetics of an intravenous infusion of 2 mg hydromorphone over 20 mins. DESIGN: Open study. SUBJECTS: Twelve healthy volunteers. MEASUREMENTS: The analgesic effect of hydromorphone was evaluated serially using pressure pain thresholds (PPTs) measured on the third fingers and toes. The nonanalgesic effects of hydromorphone were measured as miosis, decrease of saliva production and central nervous effects such as euphoria/dysphoria, nausea, headache, fatigue and feeling of heaviness. Plasma concentration of hydromorphone was measured using high performance liquid chromatography. RES UL TS: PPTs were significantly increased compared with baseline levels for up to 2 h after the infusion of hydromorphone. Significant miosis and reduction of saliva production were registered up to 6 h after drug administration. Fatigue and heaviness were reported by all subjects. In the studied opioid-naive subjects, the hydromorphone-induced analgesic effect was of shorter duration than the studied nonanalgesic effects. The terminal elimination half-life of hydromorphone was 1.87±0.4 h (± SD) (95% CI 1.61 to 2.13), systemic clearance was 1.81±0.25 L/min (95% CI 1.65 to 1.97) and volume of distribution was 4.15±0.86 L/kg (95% CI 3.6 to 4.71). CONCLUSION: Analgesia and nonanalgesic effects appear to be well correlated with the plasma concentrations of the hydromorphone. MESURES : L' effet analgesique de l 'hydromorphone a ete evalue en series en utilisant les seuils de la douleur a la pression mesures sur le majeur et le gros orteil. Les effets non analgesiques de l 'hydromorphone ont ete mesures en tant que myosis, diminution de la production de salive et effets du systeme nerveux central tels I' euphorie ou la dysphorie, la nausee, les cephalees, la fatigue et la sensation de lourdeur. La concentration plasmatique d'hydromorphone a ete mesuree par chromatographie haute performance. RESULT A TS : Les seuils de la douleur a la pression augmentaient considerablement comparativement aux valeurs de base jusqu'a deux heures apres la perfusion d 'hydromorphone. Un myosis important ainsi qu'une diminution de la production de salive ont ete enregistres jusqu'a 6 h apres !'administration du medicament. La fatigue et la sensation de lourdeur ont ete rapportees par tous les sujets. Dans le groupe etudie de sujets naifs a l'opio"ide, l'effet analgesique induit par l'hydromorphone persistait moins longtemps que les effets non analgesiques etudies. La demi-vie d'elimination finale de l'hydromorphone etait de 1,87±0,4 h (±ecart-type) (IC 95 % 1,61-2,13), la clairance systemique etait de 1,81 ±0,25 L/minute (IC 95 % 1,65-1,97) et le volume de distribution de 4,15±0,86 L/kg (IC 95 % 3,71). CONCLUSION: L'analgesie et les effets non analgesiques semblent correler avec les concentrations plasmatiques de l'hydromorphone.

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Pharmacokinetics and Bioavailability of Hydromorphone Following Intravenous and Oral Administration to Human Subjects

Cited by 118 publications

References 6 publications

Hydromorphone: pharmacology and clinical applications in cancer patients

Hydromorphone: pharmacology and clinical applications in cancer patients

Effect of Ethanol on Opioid Drug Permeability Through Caco-2 Cell Monolayers

Analgesic and Nonanalgesic Effects of Intravenous Hydromorphone ‐ Relation to Plasma Concentrations in Healthy Volunteers

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