Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
APOMORPHINE HYDROCHLORIDE vs ACTIDIL
Clinician-reviewed, head-to-head comparison of mechanism, dosing, pharmacokinetics, and safety profiles.
Last clinically reviewed: July 2026 · OpiCalc Medical Review Team
Non-ergoline dopamine agonist with high affinity for D2 and D3 receptors, moderate affinity for D4, D5, and adrenergic receptors; activates striatal dopamine receptors to improve motor function.
H1-receptor antagonist; competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract, blocking histamine-induced bronchoconstriction, vasodilation, and increased capillary permeability.
FDA: Acute treatment of hypomobility episodes ('off' episodes) in Parkinson disease,Off-label: Refractory erectile dysfunction, treatment of levodopa-induced dyskinesias, depression
Allergic rhinitis,Allergic conjunctivitis,Urticaria,Angioedema
Subcutaneous injection: 0.2 m L (2 mg) test dose, then 0.2-0.6 m L (2-6 mg) as needed for acute hypomobility episodes; maximum single dose 0.6 m L (6 mg). Sublingual: 2-10 mg sublingually as needed, not more than every 2 hours, maximum 30 mg/day. Continuous subcutaneous infusion: 0.5-2.0 mg/hour via infusion pump.
2.5 mg orally every 4 to 6 hours as needed; maximum 10 mg per day.
Terminal elimination half-life is 40–60 minutes in adults with normal renal function; prolonged to 3–6 hours in end-stage renal disease.
Terminal elimination half-life is approximately 20-25 hours in healthy adults; may be prolonged in elderly or patients with hepatic impairment.
Hepatic via CYP3A4, CYP2C9, and CYP2C19; main metabolite is apomorphine-8-O-sulfate; first-pass effect with rapid clearance.
Hepatic via CYP450 isoenzymes (primarily CYP3A4 and CYP2D6); undergoes N-demethylation and N-oxidation.
Approximately 90% of an intravenous dose is excreted in urine within 24 hours, primarily as unchanged drug and sulfate conjugates. Biliary/fecal excretion is minimal (<5%).
Renal excretion of unchanged drug and metabolites accounts for approximately 60-80% of the administered dose; biliary/fecal elimination comprises the remainder (20-40%).
Approximately 90–99% bound, primarily to albumin.
Approximately 90% bound to plasma proteins, primarily albumin.
1.8–2.5 L/kg, indicating extensive tissue distribution.
2.5-4.0 L/kg, indicating extensive tissue distribution.
Subcutaneous: 100% (absolute); sublingual: 16–18%; oral: <1% due to extensive first-pass metabolism.
Oral bioavailability is approximately 50-60% due to first-pass metabolism.
No dose adjustment for mild to moderate impairment. Severe impairment (GFR <15 m L/min): avoid use as apomorphine is renally eliminated and accumulation may occur; use with caution and reduce dose if necessary at GFR 15-29 m L/min.
GFR 10-50 m L/min: 2.5 mg every 6-8 hours; GFR <10 m L/min: 2.5 mg every 8-12 hours.
Child-Pugh A and B: no dose adjustment necessary. Child-Pugh C: pharmacokinetics not studied; use with caution and monitor closely.
Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: contraindicated.
Safety and efficacy not established; no pediatric dosing recommendations.
Children 2-5 years: 1.25 mg orally every 4-6 hours (max 5 mg/day); Children 6-12 years: 1.25-2.5 mg every 4-6 hours (max 7.5 mg/day).
Elderly patients may be more sensitive to neuropsychiatric effects; initiate at low end of dosing range (e.g., 1-2 mg subcutaneously) and titrate slowly; monitor for hypotension and falls.
Initiate at 1.25 mg orally every 6-8 hours; maximum 5 mg per day due to increased risk of anticholinergic effects and renal impairment.
None.
None
Risk of hypotension, syncope, and orthostatic hypotension,Severe nausea and vomiting (pretreat with antiemetic),Potential for hallucination, dyskinesia, and impulse control disorders,Do not mix with serotonin 5-HT3 antagonists (e.g., ondansetron) due to severe hypotension,Use caution in patients with cardiovascular disease, hypotension, or renal impairment
May cause drowsiness and impair mental alertness,Avoid alcohol and other CNS depressants,Use with caution in patients with narrow-angle glaucoma, prostatic hypertrophy, or urinary retention,Elderly patients are more susceptible to anticholinergic effects
Concurrent use with serotonin 5-HT3 antagonists (e.g., ondansetron),Hypersensitivity to apomorphine or sulfite-containing products,Severe asthma or sulfite allergy
Hypersensitivity to any component,Concurrent use with monoamine oxidase inhibitors
Avoid alcohol: may increase drowsiness and hypotension. Grapefruit juice: may increase risk of QT prolongation. No specific food interactions; maintain normal diet but monitor for changes in blood pressure.
No specific food interactions, but taking with food may reduce GI side effects. Alcohol should be strictly avoided due to additive CNS depression. Grapefruit juice is not documented to interact.
Apomorphine hydrochloride is a dopamine agonist indicated for Parkinson's disease. Limited human pregnancy data; animal studies show fetotoxicity and teratogenicity at doses near maternal toxic doses. FDA Pregnancy Category C. First trimester: Avoid use unless benefit outweighs risk. Second/third trimester: No established safety; potential fetal effects include altered dopamine receptor development. Postnatal: Risk of neonatal withdrawal if used near term.
First trimester: Limited human data; animal studies show no teratogenicity. Second and third trimesters: Not associated with major congenital malformations. However, anticholinergic effects may cause neonatal tachycardia, irritability, and withdrawal symptoms if used near term.
No data on apomorphine excretion in human milk. M/P ratio unknown. Due to potential for serious adverse reactions in breastfeeding infants (e.g., somnolence, hypotension, dyskinesia), breastfeeding is not recommended during therapy.
Excretion into breast milk likely but negligible amounts; no adverse effects reported in infants. M/P ratio not established. Considered compatible with breastfeeding; monitor for sedation or irritability in neonate.
Pregnancy can alter apomorphine pharmacokinetics due to increased plasma volume, renal blood flow, and hepatic metabolism. No specific dose adjustment guidelines exist. Use lowest effective dose with careful titration. Monitor for reduced efficacy or increased adverse effects (e.g., hypotension, nausea).
No specific dose adjustments required in pregnancy; however, use lowest effective dose due to potential anticholinergic effects. Pharmacokinetics may be altered (increased volume of distribution), but no dose adjustment recommended.
Administer subcutaneously; avoid intravenous use due to risk of hemolytic anemia and hypotension. Onset is rapid (5-15 minutes) with short duration (1 hour). Use an antiemetic (e.g., domperidone or trimethobenzamide) for 3 days before starting to prevent nausea. Do not use with 5-HT3 antagonists (e.g., ondansetron) due to profound hypotension. Monitor for dyskinesia, orthostatic hypotension, and QT prolongation. Avoid in patients with dementia, psychosis, or severe respiratory depression; caution in hepatic/renal impairment. Test dose (0.2-0.5 m L) is required before first prescription.
ACTIDIL (triprolidine) is a first-generation antihistamine with sedative properties. Use cautiously in elderly due to risk of confusion, urinary retention, and falls. Avoid in patients with narrow-angle glaucoma, BPH, or asthma. Administer with food if GI upset occurs. Onset of action is 30-60 minutes; duration 4-6 hours.
Take this medication exactly as prescribed; it is for on-demand treatment of 'off' episodes.,Inject under the skin (subcutaneous) as directed; do not inject into a vein or muscle.,You may feel dizzy or lightheaded when standing up; rise slowly from sitting or lying down.,Nausea is common; your doctor may prescribe an anti-nausea medicine to take before each dose.,Report any chest pain, fainting, or severe dizziness immediately.,Avoid alcohol and grapefruit juice while using this medication.,Do not change your dose or frequency without consulting your doctor.,Keep this medication away from children and pets.
Do not drive or operate heavy machinery until you know how this medication affects you; it can cause drowsiness.,Avoid alcohol and other CNS depressants, as they may increase sedation.,Take exactly as prescribed; do not exceed recommended dose.,If you miss a dose, skip it; do not double the next dose.,Notify your doctor if you experience blurred vision, difficulty urinating, or severe drowsiness.,Do not use for prolonged periods without medical advice.
"Coadministration of morphine with palbociclib may increase plasma concentrations of palbociclib due to morphine-induced inhibition of intestinal P-glycoprotein (P-gp) efflux transporter and potential competition for CYP3A4 metabolism. This elevation can heighten the risk of palbociclib-related toxicities, including myelosuppression (neutropenia, leukopenia, anemia), hepatotoxicity, and gastrointestinal adverse effects (e.g., diarrhea, nausea). Patients should be monitored for signs of excessive palbociclib exposure and dose reductions considered if toxicity occurs."
"Morphine, a potent opioid analgesic, can inhibit the metabolism of sulfisoxazole, a sulfonamide antibiotic, by competing for hepatic glucuronidation pathways. This pharmacokinetic interaction leads to increased plasma concentrations of sulfisoxazole, potentially elevating the risk of dose-dependent adverse effects such as crystalluria, hypersensitivity reactions, and bone marrow suppression. Co-administration requires careful monitoring for sulfonamide toxicity, especially in patients with renal impairment or those receiving high-dose morphine."
"Morphine is a potent opioid analgesic that can inhibit the metabolism of isavuconazonium (prodrug of isavuconazole) via competitive inhibition of CYP3A4, the primary enzyme responsible for its activation. This leads to reduced conversion to the active antifungal isavuconazole, potentially decreasing its efficacy against invasive fungal infections. Conversely, isavuconazonium may also inhibit morphine metabolism, increasing opioid side effects such as respiratory depression, sedation, and constipation."
No interactions on record
Explore head-to-head clinical comparisons of other medications in the same therapeutic classes.
Common clinical questions about APOMORPHINE HYDROCHLORIDE vs ACTIDIL, answered by our medical review team.
APOMORPHINE HYDROCHLORIDE is a Opioid Agonist that works by Non-ergoline dopamine agonist with high affinity for D2 and D3 receptors, moderate affinity for D4, D5, and adrenergic receptors; activates striatal dopamine receptors to improve motor function.. ACTIDIL is a Antihistamine that works by H1-receptor antagonist; competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract, blocking histamine-induced bronchoconstriction, vasodilation, and increased capillary permeability.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between APOMORPHINE HYDROCHLORIDE and ACTIDIL depend on the specific clinical indication. These are agents from distinct pharmacological classes and are not directly interchangeable by dose. A physician or clinical pharmacist should guide any therapeutic switching decisions.
The standard adult dose of APOMORPHINE HYDROCHLORIDE is: Subcutaneous injection: 0.2 m L (2 mg) test dose, then 0.2-0.6 m L (2-6 mg) as needed for acute hypomobility episodes; maximum single dose 0.6 m L (6 mg). Sublingual: 2-10 mg sublingually as needed, not more than every 2 hours, maximum 30 mg/day. Continuous subcutaneous infusion: 0.5-2.0 mg/hour via infusion pump.. The standard adult dose of ACTIDIL is: 2.5 mg orally every 4 to 6 hours as needed; maximum 10 mg per day.. Dosing should always be individualized based on indication, renal and hepatic function, age, and other patient factors.
No direct drug-drug interaction has been formally documented between APOMORPHINE HYDROCHLORIDE and ACTIDIL in current clinical databases. However, individual patient risk factors including other medications, organ function, and comorbidities should always be evaluated by a qualified healthcare provider.
The maternal-fetal safety profiles differ. APOMORPHINE HYDROCHLORIDE is classified as Category D/X. Apomorphine hydrochloride is a dopamine agonist indicated for Parkinson's disease. Limited human pregnancy data; animal studies show fetotoxicity and teratogenicity at doses near m. ACTIDIL is classified as Category C. First trimester: Limited human data; animal studies show no teratogenicity. Second and third trimesters: Not associated with major congenital malformations. However, anticholinergi. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.