Hydromorphone Hydrochloride

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Cat Number

API0232183

CAS Number

71-68-1

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CAS Number

71-68-1

EINECS

200-762-6

Synonyms

Hydromorphone HCl

Molecular Formula

C17H20ClNO3

Molecular Weight

321.8

Smiles

CN1CC[C@]23[C@@H]4[C@H]1CC5=C2C(=C(C=C5)O)O[C@H]3C(=O)CC4.Cl

Appearance

White or almost white crystalline powder

General Description

Hydromorphone hydrochloride is the hydrochloride salt form of hydromorphone, a semi-synthetic opioid agonist derived from morphine and classified as a Schedule II controlled substance. It is available in multiple formulations including immediate-release and extended-release oral tablets, oral solution, injectable solutions, and rectal suppositories. It is approximately five times more potent than morphine and is characterized by rapid onset and predictable duration of action.

Mechanism of Action

Hydromorphone exerts its analgesic effects primarily through selective agonist activity at the mu-opioid receptor, which is coupled to G-proteins and linked to intracellular signaling pathways. Receptor binding stimulates GTP exchange for GDP on the G-protein complex and inhibits adenylate cyclase, reducing intracellular cAMP levels. This leads to activation of voltage-gated potassium channels causing neuronal hyperpolarization, inhibition of voltage-gated calcium channels reducing neurotransmitter release, and modulation of nociceptive pathways in the central nervous system.

Application

Hydromorphone hydrochloride is indicated for the management of moderate-to-severe acute pain and severe chronic pain requiring around-the-clock opioid therapy in patients for whom alternative treatment options are inadequate. Due to significant risks of respiratory depression, addiction, abuse, and neonatal withdrawal syndrome, therapy requires careful patient selection, gradual tapering upon discontinuation, and availability of naloxone for overdose reversal.

Kolli S, et al. conducted a randomized comparative effectiveness trial enrolled 162 emergency department patients aged ≥65 years with acute severe pain (median baseline pain score 10/10) to receive either 1,000 mg intravenous acetaminophen or 0.5 mg intravenous hydromorphone. At 60 minutes, pain improvement was 3.6 points with acetaminophen and 4.6 points with hydromorphone (difference 1.0; 95% CI 0.1–2.0). Although statistically superior, this difference did not meet the predefined minimum clinically important difference of 1.3 points.

Fig. 1 Graphical depiction of participant-level pain scores at baseline and 60 minutes (Kolli S, et al., 2022)

References

Kolli S, et al. A Randomized Study of Intravenous Hydromorphone Versus Intravenous Acetaminophen for Older Adult Patients with Acute Severe Pain. Ann Emerg Med. 2022;80(5):432-439.

Shi J, et al. investigated the protective effects of hydromorphone pretreatment against lung injury caused by CO₂ pneumoperitoneum in mouse models and in patients undergoing laparoscopic gynecological surgery. In mice, hydromorphone alleviated lung injury, reduced oxidative stress markers (myeloperoxidase, total oxidant status), increased antioxidant capacity, upregulated heme oxygenase-1 (HO-1) expression, and improved mitochondrial morphology and dynamics. These protective effects were abrogated by HO-1 siRNA, confirming the essential role of HO-1. In clinical patients, hydromorphone pretreatment resulted in lower serum levels of lung injury markers (CC-16, ICAM-1), a reduced prooxidant-antioxidant balance, and higher HO-1 activity compared to morphine.

Fig. 2 Hydromorphone alleviates pneumoperitoneum-induced lung injury in mice. (Shi J, et al, 2021)

References

Shi J, et al. Hydromorphone Protects against CO2 Pneumoperitoneum-Induced Lung Injury via Heme Oxygenase-1-Regulated Mitochondrial Dynamics. Oxid Med Cell Longev. 2021;2021:9034376.

Does Hydromorphone Hydrochloride discolor upon prolonged light exposure?

Yes, it is photosensitive and may darken over time if exposed to light. We recommend storage in light-resistant, amber glass or opaque containers to maintain its appearance and purity.

What are the security requirements for shipping Hydromorphone Hydrochloride?

As a Schedule II controlled substance, it must be shipped via secure, traceable couriers with tamper-evident seals and chain-of-custody documentation at every transfer point.

Is Hydromorphone Hydrochloride hygroscopic, and how does this affect stability?

It is slightly hygroscopic. While not highly moisture-sensitive, excessive humidity can cause caking and potential degradation. We package it with desiccant in sealed containers.

How is the impurity hydromorphone dimer controlled during storage?

We monitor the dimer formation using a specific HPLC method during stability studies, ensuring it remains below the established qualification threshold throughout the shelf life.