Apomorphine Hydrochloride

What it is and how it works

Mechanism of Action Apomorphine hydrocloride is a non-ergoline dopamine agonist with high in vitro binding affinity for the dopamine D 4 receptor, and moderate affinity for the dopamine D 2 , D 3 , and D 5 , and adrenergic α 1 D, α 2 B, α 2 C receptors. The precise mechanism of action of apomorphine hydrocloride as a treatment for Parkinson's disease is unknown, although it is believed to be due to stimulation of post-synaptic dopamine D 2 -type receptors within the caudate-putamen in the brain.

Indications

Apomorphine hydrochloride injection is indicated for the acute, intermittent treatment of hypomobility, "off" episodes ("end-of-dose wearing off" and unpredictable "on/off" episodes) in patients with advanced Parkinson's disease. Apomorphine hydrocloride inejction has been studied as an adjunct to other medications . Apomorphine hydrocloride injection is a non-ergoline dopamine agonist indicated for the acute, intermittent treatment of hypomobility, "off" episodes ("end-of-dose wearing off" and unpredictable "on/off" episodes) associated with advanced Parkinson's disease

Dosage and administration (summary)

For subcutaneous use only Always express apomorphine hydrocloride dose in mL to minimize dosing errors The starting dose of apomorphine hydrocloride is 0.2 mL (2 mg); give the first dose under medical supervision; titrate the dose to effect and tolerance; the maximum recommended dose is 0.6 mL Treatment with a concomitant antiemetic, e.g., trimethobenzamide, is recommended, starting 3 days prior to the first dose of apomorphine hydrocloride.

Contraindications

Apomorphine hydrocloride is contraindicated in patients: Using concomitant drugs of the 5HT 3 antagonist class including antiemetics (e.g., ondansetron, granisetron, dolasetron, palonosetron) and alosetron . There have been reports of profound hypotension and loss of consciousness when apomorphine hydrocloride was administered with ondansetron.

Warnings and precautions

For subcutaneous use only; thrombus formation and pulmonary embolism have followed intravenous administration of apomorphine hydrocloride Falling asleep during activities of daily living, and daytime somnolence may occur Syncope and hypotension/orthostatic hypotension may occur Falls may occur, or increase May cause hallucinations and psychotic-like behavior May cause dyskinesia or exacerbate pre-existing dyskinesia May cause problems with impulse control and impulsive behaviors May cause coronary events May prolong QTc and cause torsades de pointes or sudden death Serious Adverse Reactions Af…

Pregnancy

Pregnancy Risk Summary There are no adequate data on the developmental risk associated with use of apomorphine hydrocloride in pregnant women. In animal reproduction studies, apomorphine had adverse developmental effects in rats (increased neonatal deaths) and rabbits (increased incidence of malformation) when administered during pregnancy at clini…

Storage and supply

Store at 25°C (77°F). Excursions permitted between 15°C to 30°C (59°F to 86°F)

Source: Apomorphine Hydrochloride (Apomorphine Hydrocloride) — US FDA prescribing information, 2022-02-24, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.