Hydromorphone hydrochloride

Description

Hydromorphone hydrochloride is a pure opioid agonist with the principal therapeutic activity of analgesia. It has an analgesic potency approximately two to eight times greater than that of morphine and has a rapid onset of action. A significant feature of the analgesia is that it can occur without loss of consciousness.

Chemical properties

White Solid

The Uses of Hydromorphone hydrochloride

Analgesic (narcotic). Preparation by electrolytic reduction of Morphine. Controlled substance (opiate).

Biochem/physiol Actions

Narcotic opiate analgesic; μ opioid receptor agonist.

Clinical Use

Hydromorphone is a potent μ agonist (eight times greater than morphine) that is used to treat severe pain. It is available in intramuscular, intravenous, subcutaneous, oral, and rectal dosage forms. Like all strong μ agonists, hydromorphone is addicting and is a Schedule II drug. Hydromorphone has an oral:parenteral potency ratio of 5:1. The plasma half-lives after parenteral and oral dosage are 2.5 and 4 hours, respectively.

Safety Profile

Poison by subcutaneous and intravenous routes. Experimental teratogenic effects. A powerful analgesic. When heated to decomposition it emits very toxic fumes of NOx and HCl. See also MORPHINE.

Drug interactions

Potentially hazardous interactions with other drugs
Alcohol: can cause dose dumping with sustained release preparations.
Analgesics: possible opioid withdrawal effects with buprenorphine and pentazocine.
Antidepressants: possible CNS excitation or depression with MAOIs - avoid concomitant use and for 2 weeks after stopping MAOI; possible CNS excitation or depression with moclobemide; increased sedative effects with tricyclics.
Antihistamines: increased sedative effects with sedating antihistamines.
Antipsychotics: enhanced hypotensive and sedative effects.
Dopaminergics: avoid with selegiline.
Nalmefene: avoid concomitant use.
Sodium oxybate: enhanced effect of sodium oxybate - avoid.

Metabolism

Hydromorphone undergoes extensive firstpass metabolism. It is extensively metabolised by glucuronidation in the liver and excreted in the urine mainly as conjugated hydromorphone, dihydroisomorphine, and dihydromorphine.