apomorphine

Absorption: Well absorbed (100%) following SUBQ administration; extent of absorption following SL administration unknown.

Distribution: Extensively distributed to extravascular tissues.

Metabolism/Excretion: Primarily metabolized by multiple routes to inactive metabolites.

Half-Life: SUBQ: 40 min; SL: 1.7 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
SUBQ	rapid	10–60 min	2 hr
SL	rapid	30–60 min	2 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to apomorphine or bisulfites;
Concurrent use of 5HT₃ antagonists (granisetron, ondansetron, palonosetron, alosetron);
Major psychotic disorder (may exacerbate condition).

Use Cautiously in:

Hypokalemia, hypomagnesemia, bradycardia, congenital QTc prolongation or concurrent use of drugs causing QTc prolongation (↑ risk of QT interval prolongation);
Mild to moderate renal impairment (↓ starting dose);
Mild to moderate hepatic impairment;
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children;
Geri: risk of confusion/hallucinations, falls, and cardiac, respiratory, and gastrointestinal events in older adults.

Cardiovascular or cerebrovascular disease (may exacerbate condition).

Adv. Reactions/Side Effects ⬆ ⬇

CV: chest pain, hypotension, HF, QT interval prolongation, angina, CARDIAC ARREST, hypotension, syncope

Derm: ↑sweating, flushing, pallor

EENT: rhinorrhea

GI: nausea, oral mucosal irritation/paresthesia/pain (SL only), vomiting, dry mouth (SL only), stomatitis(SL only)

GU: priapism

Hemat: hemolytic anemia

Local: injection site pain

MS: arthralgia, back pain, limb pain

Neuro: dizziness, hallucinations, somnolence, aggravation of Parkinson's disease, aggressive behavior, agitation, confusion, delirium, delusions, disorientation, drowsiness, dyskinesia, headache, paranoid ideation, urges (gambling, sexual)

Misc: yawning, falls, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

Profound hypotension or loss of consciousness may occur with 5-HT3 antagonists.
↑risk of hypotension with alcohol, antihypertensives, or vasodilators, especially nitrates; avoid concurrent use with alcohol; patients should lie down before and after taking SL nitroglycerin.
Dopamine antagonists, including antipsychotics and metoclopramide may ↓ efficacy.
QT interval prolonging medications may ↑ risk of QT interval prolongation.

Route/Dosage ⬆ ⬇

SC (Adults ): Initiate with test dose of 0.1 mL (1 mg)–0.2 mL (2 mg); if patient tolerates and responds to initial test dose, starting dose should be the same as the test dose, used on an as needed basis to treat recurring “off” episodes (may ↑ dose by 0.1 mL (1 mg) every few days as an outpatient). If more than 1 wk passes between doses, titration should be restarted at the 0.2 mL (2 mg) level. Doses should not exceed 0.6 mL (6 mg).
(Adults ): 10 mg every 2 hr as needed for “off” episodes. If dose is tolerated but response is insufficient, may ↑ dose in 5–mg increments every 3 days up to max dose of 30 mg. Only single doses should be used during a particular off period. Do not exceed 5 doses/day.
SC (Adults ): Mild or moderate renal impairment: Test dose and starting dose not to exceed 0.1 mL (1 mg)

Availability ⬆ ⬇

(Generic available)

Solution for injection (contains bisulfites): 10 mg/mL
Sublingual films: 10 mg; 15 mg; 20 mg; 25 mg; 30 mg

Assessment ⬆ ⬇

Assess for nausea and vomiting; severe with recommended doses.
Monitor BP standing and lying during dose titration. Orthostatic hypotension may occur any time during therapy but occurs more frequently during initial therapy or with a dose increase.

Implementation ⬆ ⬇

Administer antiemetic (trimethobenzamide 300 mg three times daily) beginning 3 days before starting apomorphine. Continue as long as necessary to control nausea and vomiting, but no longer than two months after starting therapy; >2 mo increases risk of somnolence, falls, and dizziness. Due to potential for profound hypotension and loss of consciousness, avoid use of 5–HT₃ antagonists (ondansetron, granisetron, palonosetron, alosetron).
Initial dose should be supervised by a health care professional. Administer SL film under tongue. Administer whole; do not cut, chew, or swallow. Will disintegrate in about 3 min.
SC: Always prime the pen before every injection and after loading a new cartridge.
- Never dial the dose or attempt to correct a dialing error with the BD pen needle in the skin, as this may result in an incorrect dose.
- Do not store or carry pen with a pen needle attached. Use a new sterile BD pen needle with each injection.
Administer SUBQ into stomach, upper arm, or upper leg. Pinch skin with finger and thumb and insert needle all the way into pinched skin. Push the injection button until a clicking sound is heard, and hold button for 5 min and gently rub injection site. Rotate site with each injection. Do not inject into skin that is red, sore, infected, or damaged. Solution should be clear and colorless; do not administer solution that is cloudy, green, or contains particles. Do not administer IV.
- Store apomorphine at room temperature. Syringes can be filled from ampules the night before and stored in the refrigerator until next day.

Patient/Family Teaching ⬆ ⬇

Provide patient and caregiver with detailed instructions on use of SL film and preparation and injection of dose, use of dosing pen, storage, and disposal of equipment. Advise patient to read the Patient Package Insert and Directions for Usebefore starting and with each Rx refill in case of changes. Medication is dosed in mL, not mg. A dose of 1 mg is represented on dosing pen as 0.1 mL (1.0 mL equals 10 mg). Caution patient that apomorphine is not used to prevent “off” episodes and does not take the place of other medications for Parkinson's disease. Advise patient to avoid rapid dose reduction or abrupt stopping of apomorphine; may cause symptoms similar to neuroleptic malignant syndrome (elevated temperature, muscular rigidity, altered consciousness, elevated creatine kinase, autonomic instability).
Advise patient to change positions slowly to prevent orthostatic hypotension. Caution patient to avoid drinking alcohol; will increase hypotensive effects of apomorphine.
May cause sudden bouts of falling asleep during activities of daily living. Advise patient to notify health care professional if daytime sleepiness occurs and to avoid other medications that cause drowsiness. May require discontinuation of apomorphine. Caution patients to avoid alcohol and other medications that cause sedation and to avoid driving and other activities requiring alertness until response to medication is known.
Caution patients that psychotic-like behavior including hallucinations (seeing or hearing things that are not real), confusion, excessive suspicion, aggressive behavior, agitation, delusional beliefs (believing things that are not real), and disorganized thinking may occur or worsen. Notify health care professional if this occurs.
Advise patient to notify health care professional if or new or increased gambling, sexual, or other intense urges occur.
Inform patient that apomorphine may cause prolonged painful erections and to notify health care professional immediately if this occurs.
Advise patient to notify health care professional if signs and symptoms of hypersensitivity reactions (urticaria, rash, pruritus, shortness of breath, facial swelling) occur.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆ ⬇

Canadian Brand Names ⬆ ⬇

Code ⬆