pharmacopeia
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/api/v1/drug/apomorphine

Mechanism of action

Sourced from openFDA

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.

Dopamine

Indications

Sourced from openFDA
  • 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 [see Clinical Studies (14) ] .ICD-10: G20

Contraindications

Sourced from openFDA
  • 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 [see Drug Interactions (7.1) ] . There have been reports of profound hypotension and loss of consciousness when apomorphine hydrocloride was administered with ondansetron.contraindicated

Dosage & administration

Sourced from openFDA

For subcutaneous use only ( 2.1 ) Always express apomorphine hydrocloride dose in mL to minimize dosing errors ( 2.1 ) 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 ( 2.3 ) Treatment with a concomitant antiemetic, e.g., trimethobenzamide, is recommended, starting 3 days prior to the first dose of apomorphine hydrocloride. Treatment with trimethobenzamide should only be continued as long as necessary to control nausea and vomiting, and generally no longer than two months ( 2.2 , 5.2 , 6.1 , 17 ) Apomorphine hydrocloride doses must be separated by at least 2 hours ( 2.5 ) Renal impairment: reduce test dose, and reduce starting dose to 0.1 mL (1 mg) ( 2.4 , 8.6 , 12.3 ) 2.1 Important Administration Instructions Apomorphine hydrocloride is indicated for subcutaneous administration only [see Warnings and Precautions (5.1) ] and only by a multiple-dose APOKYN ® Pen with supplied cartridges. The APOKYN ® Pen is supplied separately by a different manufacturer. The initial dose and dose titrations should be performed by a healthcare provider. Blood pressure and pulse should be measured in the supine and standing position before and after dosing. A caregiver or patient may administer apomorphine hydrocloride if a healthcare provider determines that it is appropriate. Instruct patients to follow the directions provided in the Patients Instructions For Use.

Warnings & precautions

Sourced from openFDA

For subcutaneous use only; thrombus formation and pulmonary embolism have followed intravenous administration of apomorphine hydrocloride ( 5.1 ) Falling asleep during activities of daily living, and daytime somnolence may occur ( 5.3 ) Syncope and hypotension/orthostatic hypotension may occur ( 5.4 ) Falls may occur, or increase ( 5.5 ) May cause hallucinations and psychotic-like behavior ( 5.6 ) May cause dyskinesia or exacerbate pre-existing dyskinesia ( 5.7 ) May cause problems with impulse control and impulsive behaviors ( 5.8 ) May cause coronary events ( 5.9 ) May prolong QTc and cause torsades de pointes or sudden death ( 5.10 ) 5.1 Serious Adverse Reactions After Intravenous Administration Following intravenous administration of apomorphine hydrocloride, serious adverse reactions including thrombus formation and pulmonary embolism due to intravenous crystallization of apomorphine have occurred. Consequently, apomorphine hydrocloride should not be administered intravenously. 5.2 Nausea and Vomiting Apomorphine hydrocloride causes severe nausea and vomiting when it is administered at recommended doses. Because of this, in domestic clinical studies, 98% of all patients were pre-medicated with trimethobenzamide, an antiemetic, for three days prior to study enrollment, and were then encouraged to continue trimethobenzamide for at least 6 weeks.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are discussed in more detail in the Warnings and Precautions section of labeling: Serious Adverse Reactions After Intravenous Administration [see Warnings and Precautions (5.1) ] Nausea and Vomiting [see Warnings and Precautions (5.2) ] Falling Asleep During Activities of Daily Living and Somnolence [see Warnings and Precautions (5.3) ] Syncope/Hypotension/Orthostatic Hypotension [see Warnings and Precautions (5.4) ] Falls [see Warnings and Precautions (5.5) ] Hallucinations/Psychotic-Like Behavior [see Warnings and Precautions (5.6) ] Dyskinesias [see Warnings and Precautions (5.7) ] Impulse Control/Compulsive Behaviors [see Warnings and Precautions (5.8) ] Coronary Events [see Warnings and Precautions (5.9) ] QTc Prolongation and Potential for Proarrhythymic Effects [see Warnings and Precautions (5.10) ] Withdrawal-Emergent Hyperpyrexia and Confusion [see Warnings and Precautions (5.11) ] Hypersensitivity [see Warnings and Precautions (5.12) ] Fibrotic Complications [see Warnings and Precautions (5.13) ] Priapism [see Warnings and Precautions (5.14) ] Most common adverse reactions (incidence at least 10% greater on apomorphine hydrocloride than on placebo) were yawning, drowsiness/somnolence, dyskinesias, dizziness/postural hypotension, rhinorrhea, nausea and/or vomiting, hallucination/confusion, and edema/swelling of extremities ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact TruPharma, LLC at 877-541-5504 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Use in specific populations

Sourced from openFDA

Pregnancy: Based on animal data, may cause fetal harm ( 8.1 ) Geriatric Use: In clinical trials, patients 65 years of age and older were more likely to experience certain adverse events ( 8.5 ) 8.1 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 clinically relevant doses. These doses were also associated with maternal toxicity [see Data ] . In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. The background risk of major birth defects and miscarriage for the indicated population is unknown. Data Animal Data No adverse developmental effects were observed when apomorphine (0.3, 1, or 3 mg/kg/day) was administered by subcutaneous injection to pregnant rats throughout organogenesis; the highest dose tested is 1.5 times the maximum recommended human dose (MRHD) of 20 mg/day on a mg/m 2 basis.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption Apomorphine hydrochloride is a lipophilic compound that is rapidly absorbed (time to peak concentration ranges from 10 minutes to 60 minutes) following subcutaneous administration into the abdominal wall. After subcutaneous administration, apomorphine appears to have bioavailability equal to that of an intravenous administration.

Overdosage

Sourced from openFDA

A 62-year-old man accidentally injected 25 mg of apomorphine hydrocloride subcutaneously. After 3 minutes, the patient felt nauseated and lost consciousness for 20 minutes. Afterwards, he was alert with a heart rate 40/minute and a supine blood pressure of 90/50. He recovered completely within an hour.

Approval history

Sourced from openFDA
  • Feb 23, 2022ANDAANDA212025Tp Anda Holdings
  • Feb 3, 2025NDANDA214056Mdd Us

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
1,672 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Nausea19211%
  2. 2Somnolence1498.9%
  3. 3Fall1418.4%
  4. 4Dizziness1378.2%
  5. 5Dyskinesia1277.6%
  6. 6Fatigue1177.0%
  7. 7Gait Disturbance965.7%
  8. 8Hypotension955.7%
  9. 9Hallucination915.4%
  10. 10Vomiting824.9%
  11. 11Headache764.5%
  12. 12Injection Site Nodule754.5%
  13. 13Constipation734.4%
  14. 14Speech Disorder724.3%
  15. 15Injection Site Erythema653.9%

Literature

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Recent PubMed references pinned to Apomorphine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 66 ClinicalTrials.gov registrations naming Apomorphine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Apomorphine work?
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.
What is Apomorphine used for?
According to FDA labeling, Apomorphine carries indications including: 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 [see Clinical Studies (14) ] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Apomorphine?
Apomorphine is classified as Dopamine agonists, Drugs used in erectile dysfunction, Dopaminergic Agonist, Dopamine Agonists.
What are the brand names for Apomorphine?
Apomorphine is marketed under brand names including Apokyn, Kynmobi, Onapgo.
What are the contraindications for Apomorphine?
Apomorphine labeling lists contraindications including: 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 [see Drug Interactions (7.1) ] . There have been reports of profound hypotension and loss of consciousness when apomorphine hydrocloride was administered with ondansetron.. Always consult the full prescribing information and a clinician.
Note. Data for apomorphine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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