Description

Hydromorphone is a potent opioid medication for managing moderate-to-severe acute and severe chronic pain in patients. Hydromorphone is prescribed only when initial treatments have proven ineffective, primarily due to the drug’s elevated potency, potential for abuse, and risk of overdose.[1] Moreover, this medication can also be prescribed off-label for refractory cough suppression.

The use of hydromorphone is limited to individuals who have either poorly tolerated alternative treatment regimens, such as nonopioid analgesics or combinations of opioids, or are anticipated to tolerate them poorly. Moreover, this drug is prescribed only to those without adequate pain relief from other treatment options.

Hydromorphone hydrochloride injection (high potency formulation) is exclusively intended for use in opioid-tolerant patients necessitating elevated opioid dosages to effectively manage severe pain, warranting opioid analgesia or when other available medications prove insufficient.

Hydromorphone functions as an opioid agonist by binding to various opioid receptors. The analgesic properties of the drug primarily stem from its interaction with the mu-opioid receptors. Moreover, hydromorphone also exerts its effects centrally at the medulla level, leading to respiratory depression and cough suppression.

Pharmacokinetics

The immediate-release oral formulations of hydromorphone have an onset of action within 15 to 30 minutes, reach peak levels between 30 and 60 minutes, and maintain their effectiveness for 3 to 4 hours. The drug’s half-life spans from 2 to 3 hours.

The extended-release formulations of hydromorphone have an onset of action within 6 hours, reach peak levels at 9 hours, and maintain their effectiveness for 13 hours. The drug’s half-life typically ranges around 11 hours, although it can vary between 8 and 15 hours.

The volume of distribution of hydromorphone is 4 L/kg, with 8% to 19% of the drug being bound to proteins. Hydromorphone is metabolized in the liver through glucuronidation, with the majority of the drug being transformed into hydromorphone-3-glucuronide.

Hydromorphone is primarily excreted through the urine in its glucuronidated form. The residual unchanged form gets excreted in both the urine (7%) and feces (1%)