Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
APOMORPHINE HYDROCHLORIDE vs ACTAHIST
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.
Antihistamine; binds to histamine H1 receptors, blocking the effects of histamine; also exhibits anticholinergic and mild sedative properties.
FDA: Acute treatment of hypomobility episodes ('off' episodes) in Parkinson disease,Off-label: Refractory erectile dysfunction, treatment of levodopa-induced dyskinesias, depression
Symptomatic relief of allergic rhinitis,Urticaria,Off-label: motion sickness,Off-label: insomnia
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.
1.34 mg (one capsule) orally twice daily.
Terminal elimination half-life is 40–60 minutes in adults with normal renal function; prolonged to 3–6 hours in end-stage renal disease.
6.9 ± 1.7 hours in adults; prolonged to 12-18 hours in elderly or patients with hepatic impairment, requiring dosing interval adjustment.
Hepatic via CYP3A4, CYP2C9, and CYP2C19; main metabolite is apomorphine-8-O-sulfate; first-pass effect with rapid clearance.
Hepatic metabolism via CYP450 enzymes (primarily CYP3A4 and CYP2D6); major metabolite is inactive.
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%).
Primarily renal (approximately 85% as unchanged drug and metabolites) and fecal (15%) via biliary elimination.
Approximately 90–99% bound, primarily to albumin.
92% bound to albumin.
1.8–2.5 L/kg, indicating extensive tissue distribution.
0.9 ± 0.3 L/kg, indicating extensive extravascular distribution.
Subcutaneous: 100% (absolute); sublingual: 16–18%; oral: <1% due to extensive first-pass metabolism.
Oral: 68% ± 12% 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.
No dose adjustment required for mild to moderate renal impairment. Safety not established for severe impairment (GFR <30 m L/min).
Child-Pugh A and B: no dose adjustment necessary. Child-Pugh C: pharmacokinetics not studied; use with caution and monitor closely.
No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not recommended for severe hepatic impairment (Child-Pugh C).
Safety and efficacy not established; no pediatric dosing recommendations.
Not indicated for pediatric patients under 12 years of age. Safety and efficacy not established.
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.
No specific dose adjustment recommended; monitor for increased anticholinergic effects and cognitive 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; caution when driving or operating machinery. Avoid alcohol. Use with caution in patients with narrow-angle glaucoma, prostatic hyperplasia, or urinary retention. Geriatric patients more sensitive to anticholinergic effects. Pediatric patients <6 years: not recommended.
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. Newborns or premature infants. Breastfeeding (contraindicated due to risk of adverse effects in infants). Concomitant use with MAOIs.
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.
Avoid high-tyramine foods (aged cheese, cured meats, fermented products) if taking MAOIs. Grapefruit juice may increase phenylephrine absorption; limit intake.
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.
ACTAHIST (brompheniramine/phenylephrine) pregnancy category C. Inadequate human data; animal studies show no malformations at therapeutic doses. First trimester: theoretical risk from vasoconstrictive effects (phenylephrine) possibly reducing uterine blood flow; avoid if possible. Second/third trimester: phenylephrine may cause fetal hypoxia via placental vasoconstriction; use only if benefit outweighs risk. No known structural teratogenicity.
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.
Brompheniramine is excreted in breast milk in small amounts; M/P ratio not established. Phenylephrine has minimal excretion. Due to anticholinergic effects, may reduce milk production or cause sedation in infants. Use caution; prefer non-sedating alternatives if possible.
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 pharmacokinetic studies. Increased plasma volume and renal clearance in pregnancy may reduce drug levels, but efficacy threshold remains. No dose adjustment recommended; use the lowest effective dose for shortest duration due to potential risks.
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.
Actahist is a combination antihistamine-decongestant (chlorpheniramine/phenylephrine). Avoid in patients with hypertension, severe coronary artery disease, or MAOI use. Monitor for sedation and urinary retention, especially in elderly males with BPH.
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.
Take with food or milk to reduce stomach upset.,Avoid alcohol and CNS depressants as they can increase drowsiness.,Do not drive or operate machinery until you know how this medication affects you.,Contact your doctor if you experience chest pain, rapid heartbeat, or difficulty urinating.
"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 ACTAHIST, 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.. ACTAHIST is a Antihistamine that works by Antihistamine; binds to histamine H1 receptors, blocking the effects of histamine; also exhibits anticholinergic and mild sedative properties.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between APOMORPHINE HYDROCHLORIDE and ACTAHIST 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 ACTAHIST is: 1.34 mg (one capsule) orally twice daily.. 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 ACTAHIST 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. ACTAHIST is classified as Category C. ACTAHIST (brompheniramine/phenylephrine) pregnancy category C. Inadequate human data; animal studies show no malformations at therapeutic doses. First trimester: theoretical risk f. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.