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Apomorphine: Drug information

Apomorphine: Drug information
(For additional information see "Apomorphine: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Special Alerts
Health Canada Dopamine Agonists Safety Alert June 2021

Health Canada's review of the available information has established a link between use of the dopamine agonists pramipexole, quinagolide, or ropinirole and the risk of dopamine agonist withdrawal syndrome (DAWS). DAWS may occur after reducing the dose of or discontinuing dopamine agonists, and includes symptoms such as apathy, anxiety, depression, fatigue, sweating, panic attacks, insomnia, irritability, and pain. The Canadian product information for pramipexole has been updated to include a warning on the risk of DAWS. Health Canada will work with the manufacturers of quinagolide and ropinirole to update the product information to include a warning on the risk of DAWS. At this time, there is not enough information to establish a link between other dopamine agonists that were assessed as part of this safety review (ie, apomorphine, bromocriptine, cabergoline, pergolide [no longer marketed], and rotigotine) and DAWS. As a precaution, Health Canada will work with the manufacturers of these dopamine agonists to include the potential risk of DAWS in the product information.

Further information is available at https://hpr-rps.hres.ca/reg-content/summary-safety-review-detail.php?lang=en&linkID=SSR00269.

Brand Names: US
  • Apokyn;
  • Kynmobi;
  • Kynmobi Titration Kit
Brand Names: Canada
  • Kynmobi;
  • Movapo
Pharmacologic Category
  • Anti-Parkinson Agent, Dopamine Agonist
Dosing: Adult

Note: Beginning antiemetic therapy (eg, trimethobenzamide) is recommended 3 days prior to initiation; continue only as long as necessary, and generally no longer than 2 months, due to increased risk of adverse events. Apomorphine is intended to be used as adjunctive therapy with other anti-Parkinson agents.

Parkinson disease, "off" episode:

Sublingual film: Note: Determine starting dose when patient is in an "off" state and in a setting where a health care provider can monitor blood pressure and pulse. In clinical trials, to achieve an "off" state, the morning dose of carbidopa/levodopa (or any adjunctive Parkinson disease medications) was withheld and any Parkinson disease medications were avoided after midnight the night before. If response insufficient but dose tolerated, patient should resume usual Parkinson medications and return to health care provider in an "off" state to reinitiate at the next dose increment.

Initial: 10 mg as needed at intervals ≥2 hours for "off" episodes up to a maximum of 5 doses per day; may increase dose in 5 mg increments within 3 days based on response and tolerability up to a maximum single dose of 30 mg.

SUBQ: Initial test dose 0.2 mL (2 mg), medical supervision required; see "Note." Subsequent dosing is based on both tolerance and response to initial test dose.

If patient tolerates test dose and responds: Starting dose: 0.2 mL (2 mg) as needed; may increase dose in 0.1 mL (1 mg) increments every few days; maximum dose: 0.6 mL (6 mg)

If patient tolerates but does not respond to 0.2 mL (2 mg) test dose: Second test dose: 0.4 mL (4 mg)

If patient tolerates and responds to 0.4 mL (4 mg) test dose: Starting dose: 0.3 mL (3 mg), as needed for “off” episodes; may increase dose in 0.1 mL (1 mg) increments every few days; maximum dose: 0.6 mL (6 mg)

If patient does not tolerate 0.4 mL (4 mg) test dose: Third test dose: 0.3 mL (3 mg)

If patient tolerates 0.3 mL (3 mg) test dose: Starting dose: 0.2 mL (2 mg) as needed for “off” episodes; after a few days, may increase dose up to 0.3 mL (3 mg). Medically supervise for any subsequent dose increases >0.3 mL (3 mg).

If therapy is interrupted for >1 week, restart at 0.2 mL (2 mg) and gradually titrate dose.

Note: Medical supervision is required for all test doses with standing and supine blood pressure monitoring predose and 20-, 40-, and 60 minutes postdose (and after 60 minutes, if there is significant hypotension at 60 minutes). If subsequent test doses are required, wait >2 hours before another test dose is given; next test dose should be timed with another “off” episode. If a single dose is ineffective for a particular “off” episode, then a second dose should not be given. The average dosing frequency was 3 times/day in the development program with limited experience in dosing >5 times/day, single doses >0.6 mL (6 mg), and with total daily doses >2 mL (20 mg).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Sublingual film:

CrCl ≥30 mL/minute: No dosage adjustment necessary.

CrCl <30 mL/minute: Avoid use.

SUBQ:

Mild to moderate impairment: Initial test dose: 0.1 mL (1 mg); Starting dose: 0.1 mL (1 mg) as needed.

Severe impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Hepatic Impairment: Adult

Sublingual film:

Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary.

Severe impairment (Child-Pugh class C): Avoid use.

SUBQ:

Mild to moderate impairment: No dosage adjustment necessary; use caution.

Severe impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Older Adult

Use with caution; adverse effects (confusion and hallucinations), some serious, are reported more frequently in patients ≥65 years of age. Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Film, Sublingual, as hydrochloride:

Kynmobi: 10 mg (30 ea); 15 mg (30 ea); 20 mg (30 ea); 25 mg (30 ea); 30 mg (30 ea) [contains brilliant blue fcf (fd&c blue #1), edetate (edta) disodium dihydrate, levomenthol, sodium metabisulfite]

Kit, Sublingual, as hydrochloride:

Kynmobi Titration Kit: 10 mg (2s), 15 mg (2s), 20 mg (2s), 25 mg (2s), 30 mg (2s) [contains brilliant blue fcf (fd&c blue #1), edetate (edta) disodium dihydrate, levomenthol, sodium metabisulfite]

Solution Cartridge, Subcutaneous, as hydrochloride:

Apokyn: 30 mg/3 mL (3 mL) [contains benzyl alcohol, sodium metabisulfite]

Generic Equivalent Available: US

No

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Film, Sublingual, as hydrochloride:

Kynmobi: 10 mg (1 ea); 15 mg (1 ea); 20 mg (1 ea); 25 mg (1 ea); 30 mg (1 ea) [contains brilliant blue fcf (fd&c blue #1), edetate (edta) disodium dihydrate, levomenthol, sodium metabisulfite]

Solution Pen-injector, Subcutaneous:

Movapo: 10 mg/mL (3 mL)

Prescribing and Access Restrictions

Apokyn is only available through specialty pharmacies and cannot be obtained through a retail pharmacy. For more information, contact 1-877-7APOKYN (1-877-727-6596).

Administration: Adult

Sublingual film: Do not remove from pouch until immediately before use. Drink water to moisten mouth, then place film under the tongue and allow to dissolve (~3 minutes). Do not talk or swallow saliva while dissolving because this can impact absorption. Administer whole; do not cut, chew, or swallow.

SUBQ: For SUBQ administration only; do not administer IV (thrombus formation or pulmonary embolism may occur due to IV crystallization). Administer in abdomen, upper arm, or upper leg; change site with each injection. Three mL cartridges are used with a manual, reusable, multidose injector pen. Injector pen can deliver up to 1 mL (10 mg) in 0.02 mL (0.2 mg) increments.

Hazardous Drugs Handling Considerations

Hazardous agent (NIOSH 2016 [group 2]).

Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).

Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.

Use: Labeled Indications

Parkinson disease:

Sublingual film: Treatment of acute, intermittent "off" episodes in patients with Parkinson disease.

SUBQ: Treatment of acute, intermittent hypomobility "off" episodes in patients with advanced Parkinson disease.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported percentages are for the SUBQ product unless otherwise specified.

>10%:

Cardiovascular: Angina pectoris (≤15%), chest pain (≤15%), chest pressure (≤15%), hypotension (SUBQ: ≤11%; sublingual film: ≤4%), orthostatic hypotension (SUBQ: ≤20%; sublingual film: ≤4%), syncope (SUBQ: ≤11%; sublingual film: ≤4%)

Gastrointestinal: Nausea (SUBQ: ≤30%; sublingual film: 21% to 28%; can be severe nausea; can occur with antiemetic pretreatment), oral paresthesia (sublingual film: ≤13%), vomiting (SUBQ: ≤30%; sublingual film: 4% to 7%; can be severe vomiting; can occur with antiemetic pretreatment)

Local: Injection site reaction (5% to 26%; bruising at injection site [16%], injection site granuloma [4%], injection site pruritus [2%])

Nervous system: Dizziness (SUBQ: ≤20%; sublingual film: 9% to 11%), drowsiness (SUBQ: 35%; sublingual film: 11% to 13%), falling (SUBQ: 30%; sublingual film: 4% to 6%), hallucination (SUBQ: ≤14%, sublingual film: ≤6%), yawning (SUBQ: 40%; sublingual film: 4% to 12% [Olanow 2020])

Neuromuscular & skeletal: Dyskinesia (SUBQ: 24% to 35%; sublingual film: 1% [Olanow 2020])

Respiratory: Oropharyngeal edema (sublingual film: 1% to 15%), oropharyngeal pain (sublingual film: ≤13%), rhinorrhea (SUBQ: 20%; sublingual film: 6% to 7%)

1% to 10%:

Cardiovascular: Acute myocardial infarction (≤4%), cardiac failure (≥5%), edema (≤10%), presyncope (sublingual film: ≤4%)

Dermatologic: Diaphoresis (≥5%), ecchymoses (≥5%), facial swelling (sublingual film: ≤6%), hyperhidrosis (sublingual film: 4% to 6%), urticaria (sublingual film: ≤6%)

Endocrine & metabolic: Dehydration (≥5%)

Gastrointestinal: Constipation (≥5%), diarrhea (≥5%), oral mucosal erythema (sublingual film: 4% to 7%), oral mucosa ulcer (sublingual film: ≤7%), stomatitis (sublingual film: ≤7%), xerostomia (sublingual film: 1% to 6%)

Genitourinary: Urinary tract infection (≥5%)

Hypersensitivity: Hypersensitivity reaction (sublingual film: 6%)

Nervous system: Anxiety (≥5%), confusion (SUBQ: ≤10%; sublingual film: ≤6%), delusion (sublingual film: ≤6%), depression (≥5%), disorientation (sublingual film: ≤6%), exacerbation of Parkinson’s disease (≥5%), fatigue (SUBQ: ≥5%; sublingual film: 3% to 7%), headache (SUBQ: ≥5%; sublingual film: 6% to 8%), insomnia (≥5%)

Neuromuscular & skeletal: Arthralgia (≥5%), asthenia (≥5%), back pain (≥5%), limb pain (≥5%), swelling of extremities (≤10%)

Respiratory: Dyspnea (≥5%), pneumonia (≥5%)

Miscellaneous: Laceration (sublingual film: 1% to 6%)

<1%: Genitourinary: Priapism

Postmarketing:

Cardiovascular: Prolonged QT interval on ECG (dose related)

Hematologic & oncologic: Hemolytic anemia (combination therapy) (Colosimo 1994; Frankel 1990)

Nervous system: Aggressive behavior, agitation, behavioral changes, impulse control disorder (including pathological gambling, increased libido), mental status changes, paranoid ideation, psychosis (acute), sudden onset of sleep

Contraindications

Hypersensitivity to apomorphine, any component of the formulation, or to a sulfite; concomitant use with 5-HT3 antagonists.

Canadian labeling: Additional contraindications (not in US labeling): Concomitant use with antihypertensives or vasodilators (Movapo); severe hepatic or renal impairment.

Warnings/Precautions

Concerns related to adverse effects:

• GI effects: Severe nausea and vomiting may occur. Pretreatment with antiemetic (eg, trimethobenzamide) is necessary and should be started 3 days prior to initiation of therapy and continued only as long as necessary to control nausea/vomiting, and generally no longer than 2 months. Trimethobenzamide increases the risk of somnolence, dizziness, and falls. Avoid use of antidopaminergic antiemetic agents (eg, promethazine, prochlorperazine, chlorpromazine, metoclopramide, haloperidol).

• Hallucinations/psychosis: May cause hallucinations or psychotic-like behavior or thoughts (eg, paranoia, delusions, confusion, disorientation, aggression, agitation, delirium) which may be severe; avoid in patients with major psychotic disorders.

• Hypersensitivity: Hypersensitivity reactions (including angioedema or anaphylaxis) to apomorphine or its sulfite component may occur. If a hypersensitivity reaction to apomorphine occurs, discontinue and do not restart.

• Impulse control disorders: Has been associated with compulsive behaviors and/or loss of impulse control, which has manifested as pathological gambling, libido increases (hypersexuality), binge eating, and/or other intense urges. Dose reduction or discontinuation of therapy has been reported to reverse these behaviors in some, but not all cases.

• Orthostatic hypotension/syncope: May cause orthostatic hypotension, especially during dose escalation, and syncope. Parkinson disease patients appear to have an impaired capacity to respond to a postural challenge. The hypotensive effects of apomorphine are exacerbated by concomitant ethanol consumption and sublingual nitroglycerin use. Additional risk factors for hypotension may include concomitant use of other antihypertensive drugs or vasodilators or where transient hypotensive episodes would be poorly tolerated (cardiovascular disease or cerebrovascular disease). Carefully monitor for signs and symptoms of postural hypotension (especially during dose escalation). Avoid ethanol during therapy.

• Pleural/retroperitoneal fibrosis: Ergot-derived dopamine agonists have also been associated with fibrotic complications (eg, retroperitoneal fibrosis, pleural thickening, cardiac valvulopathy, and pulmonary infiltrates); monitor closely for signs and symptoms of fibrosis; effects may or may not be reversible.

• Priapism: Has been reported; severe priapism may require medical attention.

• Somnolence: Somnolence and falling asleep while engaging in activities of daily living, without prior warning signs, has been reported. Monitor for daytime somnolence or preexisting sleep disorder; caution with concomitant sedating medication; discontinue if significant daytime sleepiness or episodes of falling asleep occur. Patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Use with caution in patients receiving other CNS depressants or psychoactive agents. Effects with other sedative drugs or ethanol may be potentiated.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with cardiovascular disease; hypotension may cause coronary ischemia.

• Cerebrovascular disease: Use with caution in patients with cerebrovascular disease; hypotension may cause cerebral ischemia.

• Dyskinesias: Use with caution in patients with preexisting dyskinesias; may be exacerbated.

• Hepatic impairment: Use with caution in patients with hepatic impairment; avoid use in severe hepatic impairment (sublingual film).

• Renal impairment: Use with caution in patients with renal impairment; avoid use in severe renal impairment (sublingual film).

Special populations:

• Elderly: Adverse effects (confusion and hallucinations), some serious, are reported more frequently in patients ≥65 years; use with caution.

• Patients at risk for torsades de pointes: Use with caution in patients with risk factors for torsades de pointes (hypokalemia, hypomagnesemia, bradycardia, concurrent use of drugs that prolong QTc, or genetic predisposition).

Dosage form specific issues:

• Benzyl alcohol: Injection may contain benzyl alcohol which has been associated with "gasping syndrome" in neonates.

• Metabisulfite: Contains metabisulfite, which may cause hypersensitivity reactions. Sensitivity to sulfites is more common in patients with asthma and may cause hypersensitivity reactions (including anaphylaxis and life-threatening asthma exacerbations).

• Sublingual film: Mild to moderate oral mucosal irritation (ulceration, stomatitis, pain, paresthesia) has occurred; usually resolved after discontinuation (rechallenge is not recommended).

Other warnings/precautions:

• Abuse: Rare cases of abuse have been reported.

• Appropriate administration: Do not give SUBQ formulation IV; thrombus formation or pulmonary embolism may occur.

• Discontinuation of therapy: Dopaminergic agents have been associated with a syndrome resembling neuroleptic malignant syndrome (eg, hyperpyrexia, confusion) on abrupt withdrawal or significant dosage reduction after long-term use.

• Falling: Patients with Parkinson disease are at risk of falling; apomorphine may increase this risk.

Metabolism/Transport Effects

Substrate of CYP1A2 (minor), CYP2C19 (minor), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Alcohol (Ethyl): May enhance the hypotensive effect of Apomorphine. Risk X: Avoid combination

Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Alizapride: May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Risk X: Avoid combination

Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider therapy modification

Amisulpride (Injection): May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Risk X: Avoid combination

Amisulpride (Oral): Anti-Parkinson Agents (Dopamine Agonist) may diminish the therapeutic effect of Amisulpride (Oral). Amisulpride (Oral) may diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Risk X: Avoid combination

Antiemetics (5HT3 Antagonists): May enhance the hypotensive effect of Apomorphine. Risk X: Avoid combination

Antipsychotic Agents (First Generation [Typical]): Anti-Parkinson Agents (Dopamine Agonist) may diminish the therapeutic effect of Antipsychotic Agents (First Generation [Typical]). Antipsychotic Agents (First Generation [Typical]) may diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Management: Avoid concomitant therapy if possible. If antipsychotic use is necessary, consider using atypical antipsychotics such as clozapine, quetiapine, or ziprasidone at lower initial doses, or a non-dopamine antagonist (eg, pimavanserin). Risk D: Consider therapy modification

Antipsychotic Agents (Second Generation [Atypical]): May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Management: Consider avoiding atypical antipsychotic use in patients with Parkinson disease. If an atypical antipsychotic is necessary, consider using clozapine, quetiapine, or ziprasidone at lower initial doses, or a non-dopamine antagonist (eg, pimavanserin). Risk D: Consider therapy modification

Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Blood Pressure Lowering Agents: May enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy

Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Brivudine [INT]: May enhance the adverse/toxic effect of Anti-Parkinson Agents (Dopamine Agonist). Specifically, the risk of chorea may be increased. Risk C: Monitor therapy

Bromopride: May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Risk C: Monitor therapy

Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Risk X: Avoid combination

BuPROPion: Anti-Parkinson Agents (Dopamine Agonist) may enhance the adverse/toxic effect of BuPROPion. Risk C: Monitor therapy

Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Risk C: Monitor therapy

Herbal Products with Blood Pressure Lowering Effects: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy

Kava Kava: May enhance the adverse/toxic effect of Anti-Parkinson Agents (Dopamine Agonist). Kava Kava may diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Risk C: Monitor therapy

Levodopa-Containing Products: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. Risk C: Monitor therapy

Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Methotrimeprazine: May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Anti-Parkinson Agents (Dopamine Agonist) may diminish the therapeutic effect of Methotrimeprazine. Risk X: Avoid combination

Methylphenidate: May enhance the adverse/toxic effect of Anti-Parkinson Agents (Dopamine Agonist). Risk C: Monitor therapy

Metoclopramide: May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Risk X: Avoid combination

Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Nitroglycerin: May enhance the hypotensive effect of Apomorphine. Management: Patients taking apomorphine should lie down before and after taking sublingual nitroglycerin. Monitor blood pressure for hypotension and orthostatic hypotension when these agents are combined. Risk D: Consider therapy modification

Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Risk C: Monitor therapy

Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Risk D: Consider therapy modification

Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Risk C: Monitor therapy

Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy

Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Solriamfetol: May enhance the adverse/toxic effect of Anti-Parkinson Agents (Dopamine Agonist). Risk C: Monitor therapy

Sulpiride: May diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Risk X: Avoid combination

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Breastfeeding Considerations

It is not known if apomorphine is excreted in breast milk. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Monitoring Parameters

Supine and standing BP and pulse (for SUBQ, monitor predose and 20-, 40-, and 60 minutes postdose with each test dose); signs and symptoms of orthostatic hypotension; drowsiness or sleepiness; mental status and behavioral changes.

Mechanism of Action

Stimulates postsynaptic D2-type receptors within the caudate putamen in the brain.

Pharmacokinetics

Onset of action: SUBQ: Rapid.

Distribution: Vd: Sublingual: 3,630 L; SUBQ: 218 L.

Metabolism: Not established; potential routes of metabolism include sulfation, N-demethylation, glucuronidation, and oxidation.

Half-life elimination: Terminal: Sublingual: ~1.7 hours (range: 0.8 to 3 hours); SUBQ: ~40 minutes.

Time to peak, plasma: Sublingual: 0.5 to 1 hour; SUBQ: 10 to 60 minutes.

Pharmacokinetics: Additional Considerations

Renal function impairment: SUBQ: Cmax was increased by 50% in patients with moderate renal impairment.

Hepatic function impairment: SUBQ: Cmax was increased by 25% in patients with moderate hepatic impairment.

Pricing: US

Film (Kynmobi Sublingual)

10 mg (per each): $33.70

15 mg (per each): $33.70

20 mg (per each): $33.70

25 mg (per each): $33.70

30 mg (per each): $33.70

Kit (Kynmobi Titration Kit Sublingual)

10/15/20/25/30 mg (per each): $0.00

Solution Cartridge (Apokyn Subcutaneous)

30 mg/3 mL (per mL): $493.87

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Apo-Go (AT, CH, CL, CY, DK, EE, ES, FI, GR, HK, IE, IL, LV, NL, PT, RO, SE, SI, TH, TR, TW);
  • APO-go (GB, PL);
  • Apofin (IT);
  • Apokinon (AR);
  • Apomine (AU, NZ);
  • Apomorfin (IS);
  • Apowok (AU);
  • Apskyn (JP);
  • Britaject (HU, NO);
  • Britaject Pen (CZ);
  • Dacepton (AT, BG, CR, CZ, DE, DK, DO, EE, ES, FI, GB, GT, HN, HR, HU, LB, LV, NI, NL, NO, PA, PL, SK, SV);
  • Ixense (JP, TH);
  • Li Ke Ji (CN);
  • Movapo (AU);
  • Taluvian (HU);
  • Uprima (AE, BH, CY, EG, HU, IQ, IR, JO, KR, KW, LY, OM, PL, QA, SA, SY, TH, YE);
  • Zyprima (IN)


For country abbreviations used in Lexicomp (show table)

REFERENCES

  1. <800> Hazardous Drugs—Handling in Healthcare Settings. United States Pharmacopeia and National Formulary (USP 43-NF 38). Rockville, MD: United States Pharmacopeia Convention; 2020:74-92.
  2. Apokyn (apomorphine) [prescribing information]. Louisville, KY: US WorldMeds, LLC; April 2020.
  3. Colosimo C, Merello M, Albanese A. Clinical usefulness of apomorphine in movement disorders. Clin Neuropharmacol. 1994;17(3):243-259. doi:10.1097/00002826-199406000-00004 [PubMed 9316670]
  4. Factor SA, “Current Status of Symptomatic Medical Therapy in Parkinson's Disease,” Neurotherapeutics, 2008, 5(2):164-80. [PubMed 18394561]
  5. Frankel JP, Lees AJ, Kempster PA, Stern GM. Subcutaneous apomorphine in the treatment of Parkinson's disease. J Neurol Neurosurg Psychiatry. 1990;53(2):96-101. doi:10.1136/jnnp.53.2.96 [PubMed 2313313]
  6. Kynmobi (apomorphine) [prescribing information]. Marlborough, MA: Sunovion Pharmaceuticals Inc; August 2021.
  7. Kynmobi (apomorphine) [product monograph]. Mississauga, Ontario, Canada: Sunovion Pharmaceuticals Canada Inc; June 2020.
  8. Molina JA, Sàinz-Artiga MJ, Fraile A, et al, “Pathologic Gambling in Parkinson's Disease: A Behavioral Manifestation of Pharmacologic Treatment,” Mov Disord, 2000, 15(5):869-72. [PubMed 11009192]
  9. Movapo (apomorphine) [product monograph]. St. Laurent, Quebec, Canada: Paladin Labs Inc; November 2016.
  10. Olanow CW, Factor SA, Espay AJ, et al. Apomorphine sublingual film for off episodes in Parkinson's disease: a randomised, double-blind, placebo-controlled phase 3 study. Lancet Neurol. 2020;19(2):135-144. doi:10.1016/S1474-4422(19)30396-5 [PubMed 31818699]
  11. US Department of Health and Human Services; Centers for Disease Control and Prevention; National Institute for Occupational Safety and Health. NIOSH list of antineoplastic and other hazardous drugs in healthcare settings 2016. https://www.cdc.gov/niosh/docs/2016-161/. Updated September 2016. Accessed June 16, 2020.
  12. Weintraub D, Siderowf AD, Potenza MN, et al, “Association of Dopamine Agonist Use With Impulse Control Disorders in Parkinson Disease,” Arch Neurol, 2006, 63(7):969-73. [PubMed 16831966]
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