Apomorphine

Apomorphine Brand Name– Apokyn

What is Apomorphine

Apomorphine, a non-narcotic derivative of morphine, was first synthesized in 1869. Due to its potent emetic effects, apomorphine was used to treat acute poisonings in the early 1930s; however, safer alternatives (e.g., ipecac syrup) eventually became available.

In 1951 the drug was found beneficial in the treatment of Parkinson’s disease; however its significant emetic action precluded its usefulness at that time.

Research in the late 1960s led to the discovery that apomorphine possessed dopamine receptor agonist properties, confirming its potential as an anti-parkinson agent.

However, the simultaneous introduction of levodopa again diminished interest in the drug.

It was not until the 1980s that apomorphine’s intolerability was remedied by co-administration with domperidone, an anti-emetic. It was subsequently introduced into clinical practice in Canada and Europe, and was designated as an orphan drug for use in Parkinson’s disease by the FDA.

Apomorphine’s short duration of action, inconvenient drug delivery formulation (i.e. subcutaneous injection), and need for concomitant anti-emetic therapy have diminished its popularity in comparison to levodopa and other treatments for Parkinson’s disease.

Despite these drawbacks, the drug has several advantages including a quick onset of action, a significant effect on parkinsonian hypomobility (‘off’ episodes) unresponsive to oral medications, safety in those with a history of psychosis from other dopamine agonists, and a therapeutic effect comparable to levodopa.

Alternative formulations (e.g., transdermal, intranasal, rectal) have been investigated and may be potential delivery systems for apomorphine in the future.

Apomorphine has also been used as a diagnostic test for dopaminergic responsiveness in parkinsonian syndromes to determine whether a patient will respond or is still responsive to levodopa therapy. Limited data suggest apomorphine may be beneficial in restless leg syndrome, but further data are required.

One case report describes the successful treatment of neuroleptic malignant syndrome with subcutaneous apomorphine.

Apomorphine has been utilized in the management of erectile dysfunction (ED). In 2000, TAP Pharmaceuticals (now Takeda Pharmaceuticals) sought approval of Uprima, a sublingual formulation of apomorphine indicated for ED.

Although unpublished phase III data indicated that approximately 44—46% of men responded to the 2 mg SL dose compared to 32—38% of placebo patients, the NDA was withdrawn due to safety concerns which included fainting spells. Similar products have also been withdrawn from market in Europe.

Current guidelines for the treatment of erectile dysfunction do not advise on the role of apomorphine in the management of ED.

Apomorphine (Apokyn™ injection) was approved by the FDA as a subcutaneous injection for the rescue of ‘off’ episodes associated with advanced Parkinson’s disease on April 20, 2004.

Indications

  • Parkinson’s disease
  • parkinsonism

For use as acute, intermittent treatment of ‘off’ episodes (‘end-of-dose wearing off’ and unpredictable ‘on/off’ episodes) associated with advanced Parkinson’s disease

Side Effects

  1. agitation
  2. anaphylactoid reactions
  3. angina
  4. angioedema
  5. anxiety
  6. arthralgia
  7. back pain
  8. cardiac arrest
  9. chest pain (unspecified)
  10. confusion
  11. constipation
  12. contact dermatitis
  13. dehydration
  14. delirium
  15. depression
  16. diarrhea
  17. dizziness
  18. drowsiness
  19. dyskinesia
  20. dyspnea
  21. ecchymosis
  22. edema
  23. fatigue
  24. flushing
  25. hallucinations
  26. headache
  27. heart failure
  28. hyperhidrosis
  29. hypotension
  30. impulse control symptoms
  31. infection
  32. injection site reaction
  33. insomnia
  34. libido increase
  35. macular degeneration
  36. musculoskeletal pain
  37. myocardial infarction
  38. nausea
  39. orthostatic hypotension
  40. pallor
  41. palpitations
  42. paranoia
  43. peripheral edema
  44. priapism
  45. pruritus
  46. QT prolongation
  47. rash
  48. rhinorrhea
  49. stomatitis
  50. sudden sleep onset
  51. syncope
  52. torsade de pointes
  53. urticaria
  54. vomiting
  55. weakness
  56. yawning

Monitoring Parameters

  • blood pressure
  • neurologic function

Contraindications

  • abrupt discontinuation
  • acute myocardial infarction
  • alcoholism
  • angina
  • asthma
  • benzyl alcohol hypersensitivity
  • bradycardia
  • breast-feeding
  • cardiac arrhythmias
  • cardiac disease
  • cerebrovascular disease
  • children
  • CNS depression
  • coadministration with other CNS depressants
  • coronary artery disease
  • diabetes mellitus
  • driving or operating machinery
  • dyskinesia
  • ethanol ingestion
  • females
  • geriatric
  • heart failure
  • hepatic disease
  • hypertension
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • hypotension
  • impulse control symptoms
  • infants
  • intravenous administration
  • long QT syndrome
  • malnutrition
  • myocardial infarction
  • nausea/vomiting
  • nitrate/nitrite therapy
  • opiate agonist hypersensitivity
  • orthostatic hypotension
  • pregnancy
  • priapism
  • psychosis
  • QT prolongation
  • renal failure
  • renal impairment
  • retroperitoneal fibrosis
  • schizophrenia
  • substance abuse
  • sulfite hypersensitivity
  • syncope
  • thyroid disease

Interactions

  • Abarelix
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Codeine
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Propoxyphene
  • Acetaminophen; Tramadol
  • Aclidinium; Formoterol
  • Albuterol
  • Albuterol; Ipratropium
  • Alfentanil
  • Alfuzosin
  • Aliskiren
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Aliskiren; Hydrochlorothiazide, HCTZ
  • Aliskiren; Valsartan
  • Alprazolam
  • Amiodarone
  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Anagrelide
  • Angiotensin II receptor antagonists
  • Angiotensin-converting enzyme inhibitors
  • Anxiolytics; Sedatives; and Hypnotics
  • Arformoterol
  • Aripiprazole
  • Arsenic Trioxide
  • Artemether; Lumefantrine
  • Asenapine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atomoxetine
  • Azithromycin
  • Baclofen
  • Barbiturates
  • Bedaquiline
  • Belladonna; Opium
  • Benzhydrocodone; Acetaminophen
  • Benzodiazepines
  • Bepridil
  • Beta-adrenergic blockers
  • Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Brompheniramine
  • Brompheniramine; Carbetapentane; Phenylephrine
  • Brompheniramine; Dextromethorphan; Guaifenesin
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Brompheniramine; Pseudoephedrine
  • Budesonide; Formoterol
  • Buprenorphine
  • Buprenorphine; Naloxone
  • Buspirone
  • Calcium-channel blockers
  • Cannabidiol
  • Capsaicin; Metaxalone
  • Carbetapentane; Chlorpheniramine
  • Carbetapentane; Chlorpheniramine; Phenylephrine
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbidopa; Levodopa
  • Carbidopa; Levodopa; Entacapone
  • Carbinoxamine
  • Carbinoxamine; Dextromethorphan; Pseudoephedrine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Carbinoxamine; Phenylephrine
  • Carbinoxamine; Pseudoephedrine
  • Carisoprodol
  • Cenobamate
  • Central-acting adrenergic agents
  • Ceritinib
  • Cetirizine
  • Cetirizine; Pseudoephedrine
  • Chlophedianol; Dexchlorpheniramine; Pseudoephedrine
  • Chlorcyclizine
  • Chlordiazepoxide
  • Chlordiazepoxide; Clidinium
  • Chloroquine
  • Chlorpheniramine
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dextromethorphan
  • Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Phenylephrine
  • Chlorpheniramine; Pseudoephedrine
  • Chlorpromazine
  • Chlorzoxazone
  • Ciprofloxacin
  • Cisapride
  • Citalopram
  • Clarithromycin
  • Clemastine
  • Clofazimine
  • Clomipramine
  • Clonazepam
  • Clorazepate
  • Clozapine
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Crizotinib
  • Cyclobenzaprine
  • Cyproheptadine
  • Dantrolene
  • Dasatinib
  • Degarelix
  • Desflurane
  • Desipramine
  • Deutetrabenazine
  • Dexchlorpheniramine
  • Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Dexmethylphenidate
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Promethazine
  • Dextromethorphan; Quinidine
  • Diazepam
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Dimenhydrinate
  • Diphenhydramine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Diphenhydramine; Phenylephrine
  • Disopyramide
  • Dofetilide
  • Dolasetron
  • Dolutegravir; Rilpivirine
  • Donepezil
  • Donepezil; Memantine
  • Doxazosin
  • Doxepin
  • Doxylamine
  • Doxylamine; Pyridoxine
  • Dronabinol
  • Dronedarone
  • Droperidol
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Eliglustat
  • Emtricitabine; Rilpivirine; Tenofovir alafenamide
  • Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
  • Encorafenib
  • Enflurane
  • Entrectinib
  • Eplerenone
  • Eribulin
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Escitalopram
  • Esketamine
  • Estazolam
  • Ethanol
  • Etomidate
  • Ezogabine
  • Fentanyl
  • Fingolimod
  • Flecainide
  • Fluconazole
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluphenazine
  • Flurazepam
  • Fluticasone; Salmeterol
  • Fluticasone; Umeclidinium; Vilanterol
  • Fluticasone; Vilanterol
  • Fluvoxamine
  • Formoterol
  • Formoterol; Mometasone
  • Foscarnet
  • Gabapentin
  • Gemifloxacin
  • Gemtuzumab Ozogamicin
  • Gilteritinib
  • Glasdegib
  • Glycopyrrolate; Formoterol
  • Goserelin
  • Granisetron
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Halofantrine
  • Halogenated Anesthetics
  • Haloperidol
  • Halothane
  • Histrelin
  • Homatropine; Hydrocodone
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Hydroxychloroquine
  • Hydroxyzine
  • Ibuprofen; Oxycodone
  • Ibutilide
  • Iloperidone
  • Imipramine
  • Indacaterol
  • Indacaterol; Glycopyrrolate
  • Indapamide
  • Inotuzumab Ozogamicin
  • Isoflurane
  • Itraconazole
  • Ivosidenib
  • Ketamine
  • Ketoconazole
  • Lapatinib
  • Lasmiditan
  • Lefamulin
  • Lenvatinib
  • Leuprolide
  • Leuprolide; Norethindrone
  • Levalbuterol
  • Levocetirizine
  • Levodopa
  • Levofloxacin
  • Levomethadyl
  • Levorphanol
  • Lithium
  • Lofexidine
  • Long-acting beta-agonists
  • Loop diuretics
  • Loperamide
  • Loperamide; Simethicone
  • Lopinavir; Ritonavir
  • Lorazepam
  • Loxapine
  • Lumateperone
  • Lurasidone
  • Macimorelin
  • Maprotiline
  • Mecamylamine
  • Meclizine
  • Mefloquine
  • Meperidine
  • Meperidine; Promethazine
  • Metaproterenol
  • Metaxalone
  • Methadone
  • Methocarbamol
  • Methylphenidate
  • Metoclopramide
  • Metronidazole
  • Midazolam
  • Midostaurin
  • Mifepristone
  • Mirtazapine
  • Molindone
  • Morphine
  • Morphine; Naltrexone
  • Moxifloxacin
  • Nabilone
  • Nefazodone
  • Neuromuscular blockers
  • Nilotinib
  • Nitrates
  • Norfloxacin
  • Nortriptyline
  • Octreotide
  • Ofloxacin
  • Olanzapine
  • Olodaterol
  • Ondansetron
  • Orphenadrine
  • Osilodrostat
  • Osimertinib
  • Oxaliplatin
  • Oxazepam
  • Oxycodone
  • Oxymorphone
  • Paliperidone
  • Palonosetron
  • Panobinostat
  • Pasireotide
  • Pazopanib
  • Pentamidine
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenoxybenzamine
  • Phentolamine
  • Phenylephrine; Promethazine
  • Pimavanserin
  • Pimozide
  • Pirbuterol
  • Pitolisant
  • Posaconazole
  • Potassium-sparing diuretics
  • Pramipexole
  • Prazosin
  • Pregabalin
  • Primaquine
  • Procainamide
  • Prochlorperazine
  • Promethazine
  • Propafenone
  • Propofol
  • Propoxyphene
  • Protriptyline
  • Quazepam
  • Quetiapine
  • Quinidine
  • Quinine
  • Ranolazine
  • Remifentanil
  • Reserpine
  • Ribociclib
  • Ribociclib; Letrozole
  • Rilpivirine
  • Risperidone
  • Romidepsin
  • Ropinirole
  • Salmeterol
  • Saquinavir
  • Serotonin-Receptor Antagonists
  • Sertraline
  • Sevoflurane
  • Short-acting beta-agonists
  • Siponimod
  • Solifenacin
  • Solriamfetol
  • Sorafenib
  • Sotalol
  • Sparfloxacin
  • Sufentanil
  • Sunitinib
  • Tacrolimus
  • Tamoxifen
  • Tapentadol
  • Telavancin
  • Telithromycin
  • Temazepam
  • Terazosin
  • Terbutaline
  • Tetrabenazine
  • Thiazide diuretics
  • Thioridazine
  • Thiothixene
  • Tiotropium; Olodaterol
  • Tolterodine
  • Toremifene
  • Tramadol
  • Trazodone
  • Triazolam
  • Tricyclic antidepressants
  • Trifluoperazine
  • Trimethobenzamide
  • Trimipramine
  • Triprolidine
  • Triptorelin
  • Umeclidinium; Vilanterol
  • Vandetanib
  • Vardenafil
  • Vasodilators
  • Vemurafenib
  • Venlafaxine
  • Voriconazole
  • Vorinostat
  • Ziprasidone
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