Apomorphine

FDA label

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Titration Increase in 0.1 mL (1 mg) increments every few days (outpatient); supervised re-test doses at least 2 hours after the previous dose at the next observed "off" period.

Renal Mild or moderate: reduce test dose and starting dose to 0.1 mL (1 mg). Severe: not studied.

Hepatic Mild or moderate: use caution and monitor closely (increased Cmax/AUC); no dose given. Severe: not studied.

Doses above 0.6 mL (6 mg) are not recommended (no added effect; QTc). Average dosing frequency in trials was 3 times per day.

Instructions

• SC only, with the multiple-dose APOKYN Pen and supplied cartridges — never IV (thrombus/pulmonary embolism from IV crystallization).
• Always prescribe and express the dose in mL (pen is marked in mL).
• Initial dose and titrations by a healthcare provider; check supine and standing BP/pulse pre-dose and at 20, 40 and 60 min post-dose; clinically significant orthostatic hypotension on the test dose = not a candidate.
• Test-dose ladder: tolerates 0.2 mL but inadequate response → 0.4 mL test; tolerates/responds to 0.4 mL → maintenance 0.3 mL (3 mg) PRN; not tolerating 0.4 mL → 0.3 mL test, maintenance 0.2 mL (2 mg), may increase to 0.3 mL, ordinarily not to 0.4 mL as outpatient.
• Premedicate with trimethobenzamide 300 mg TID starting 3 days before the first dose (or start at 0.1 mL (1 mg) without it); continue only as long as needed, generally no longer than two months.
• Do not give a second dose for the same "off" episode; never repeat sooner than 2 hours after the last dose.
• Interruption of more than a week: restart at 0.2 mL (2 mg) and titrate gradually.
• Inspect solution (colorless, clear); rotate injection sites; aseptic technique.
• Avoid alcohol; lie down before and after sublingual nitroglycerin.

Available strengths

• inj 4.9 mg/mL

Contraindications

• Concomitant 5HT3 antagonists — ondansetron, granisetron, dolasetron, palonosetron, alosetron (profound hypotension and loss of consciousness reported).

Cautions

• IV administration — thrombus and pulmonary embolism; SC only
• Nausea and vomiting (may be severe); avoid antidopaminergic antiemetics
• Falling asleep during activities of daily living; somnolence
• Syncope / hypotension / orthostatic hypotension (alcohol, nitroglycerin, antihypertensives)
• Falls
• Hallucinations / psychotic-like behavior
• Dyskinesias
• Hemolytic anemia
• Impulse control / compulsive behaviors
• Coronary events
• QTc prolongation / proarrhythmia
• Withdrawal-emergent hyperpyrexia and confusion
• Hypersensitivity (contains sodium metabisulfite)
• Fibrotic complications
• Priapism
• Retinal pathology in albino rats

Adverse reactions

• Yawning (40%)
• Dyskinesias (35%)
• Drowsiness or somnolence (35%)
• Nausea and/or vomiting (30%)
• Dizziness or postural hypotension (20%)
• Rhinorrhea (20%)
• Chest pain/pressure/angina (15%)
• Hallucination or confusion (10%)
• Edema/swelling of extremities (10%)
• Injection site reactions (26%)

Pregnancy No adequate human data; animal studies showed increased neonatal deaths (rats) and heart/great-vessel malformations (rabbits) at clinically relevant doses — may cause fetal harm.

Lactation No data on presence in human milk, effects on the breastfed infant, or milk production; weigh breastfeeding benefits against maternal need.