Tadalafil / Apomorphine HCl Troches

Tadalafil / Apomorphine HCl Troches are custom-compounded, mucoadhesive lozenges intended for buccal or sublingual use by adult males with erectile dysfunction who have not achieved satisfactory results with monotherapy or who seek an option that bypasses first-pass hepatic metabolism. Each troche delivers 40 mg of tadalafil, a selective phosphodiesterase-5 (PDE5) inhibitor, together with 6 mg of apomorphine HCl, a centrally acting non-ergoline dopamine agonist. The combination is designed to couple peripheral nitric-oxide-mediated vasodilatation with hypothalamic facilitation of parasympathetic sacral outflow, thereby potentially shortening onset while prolonging erectile rigidity. Because the formulation is prepared by a 503A pharmacy, it is dispensed only pursuant to an individualized prescription and has not been evaluated by the U.S. Food and Drug Administration for safety or efficacy; prescribers therefore bear responsibility for evaluating patient-specific benefit-risk profiles and obtaining informed consent that emphasizes uncertainties in comparative effectiveness, long-term safety, and quality-of-life outcomes.

Troches are typically flavored and sweetened to improve adherence, and their transmucosal route avoids gastrointestinal degradation, increasing apomorphine bioavailability while retaining tadalafil’s 17-hour terminal half-life. Clinicians should document baseline cardiovascular status, counsel on the delayed but prolonged action window, and stress that therapy does not protect against sexually transmitted infections.^[1]

Each troche contains 40 mg tadalafil and 6 mg apomorphine HCl. For on-demand therapy, the customary initial dose is one-half troche (20 mg / 3 mg) placed buccally 15-30 minutes before anticipated sexual activity. If well tolerated and clinically indicated, the dose may be increased to a full troche, but no more than one troche should be used in 24 hours. Patients with moderate hepatic impairment (Child-Pugh B) or creatinine clearance below 50 mL / min should not exceed 20 mg tadalafil per day; scored troches facilitate individualized titration. The product is prescription-only and is not recommended for pediatric or female patients.^[7]

Tadalafil selectively inhibits PDE5 in cavernosal smooth muscle, preventing cyclic guanosine monophosphate degradation and sustaining nitric-oxide-induced relaxation; the result is increased arterial inflow and corporal engorgement during sexual stimulation. Apomorphine, in contrast, acts primarily on hypothalamic D2-like receptors within the paraventricular nucleus, enhancing oxytocinergic and parasympathetic signaling that initiates erection even before maximal peripheral vasodilatation occurs. When administered together, apomorphine generally reaches peak plasma concentrations within 20-30 minutes, providing an early pro-erectile stimulus, whereas tadalafil attains peak effect at roughly two hours but remains pharmacodynamically active for up to 36 hours, supporting multiple sexual episodes. Transmucosal absorption limits gastrointestinal first-pass loss of apomorphine and yields more predictable exposure than swallowed tablets. Although true pharmacodynamic synergy has not yet been confirmed in randomized trials, the drugs’ complementary sites of action raise that possibility; prescribers should nonetheless monitor for additive systemic vasodilatation, particularly in men receiving antihypertensives or alpha-adrenergic blockers.^[2]

Tadalafil / Apomorphine HCl Troches are contraindicated in patients who are currently using any organic nitrate (e.g., nitroglycerin, isosorbide dinitrate) or soluble guanylate-cyclase stimulator, because PDE5 inhibition markedly amplifies nitrate-induced hypotension and may precipitate myocardial ischemia. Additional contraindications include unstable angina, recent myocardial infarction or stroke (within 90 days), uncontrolled arrhythmias, severe hypotension (systolic pressure < 90 mm Hg), severe hepatic impairment (Child-Pugh class C), and end-stage renal disease requiring dialysis. The compound should not be prescribed to individuals with known hypersensitivity to tadalafil, apomorphine, or any excipient in the formulation. Concomitant administration with potent CYP3A4 inhibitors such as ketoconazole, ritonavir, or clarithromycin can profoundly increase tadalafil exposure, elevating the risk of systemic vasodilatation, visual disturbances, and priapism; dose adjustments or alternative therapy should therefore be considered.^[3]

Comprehensive medication reconciliation is essential. Apomorphine must never be co-administered with 5-HT₃ antagonists (ondansetron, granisetron, palonosetron) because life-threatening hypotension and syncope have been documented. Dopamine-receptor antagonists such as metoclopramide or most antipsychotics may blunt the central pro-erectile effect of apomorphine. Because tadalafil is metabolized predominantly by CYP3A4, strong inhibitors (itraconazole, grapefruit juice) can raise plasma levels and increase adverse-event frequency, whereas inducers (rifampin, carbamazepine) may decrease efficacy. Additive blood-pressure lowering can occur with alpha-adrenergic blockers; if combined therapy is required, initiate at the lowest feasible doses and monitor orthostatic readings. Excessive alcohol, a potent peripheral vasodilator-can exacerbate orthostatic symptoms; patients should limit intake to one or two standard drinks on dosing days.^[4]

Adverse reactions reflect the parent agents’ profiles. Tadalafil commonly causes headache, flushing, nasal congestion, dyspepsia, myalgia, and back pain; rare but serious complications include non-arteritic anterior ischemic optic neuropathy and sudden sensorineural hearing loss. Apomorphine’s dopaminergic activity frequently leads to nausea, yawning, somnolence, dizziness, and orthostatic hypotension; transient emesis may affect up to one-third of naïve users, particularly without prophylactic domperidone (not available in the United States). Combining the two drugs could theoretically potentiate vasovagal episodes, though published data remain limited. Priapism is uncommon but constitutes a urologic emergency if erections persist beyond four hours. Patients must be instructed to discontinue therapy and seek immediate medical attention for chest pain, visual changes, or prolonged erections.^[5]

Neither tadalafil nor apomorphine is indicated for use in women. Animal reproduction studies have revealed no consistent pattern of teratogenicity for tadalafil, but apomorphine produced embryofetal toxicity in rodents at maternally toxic doses. Both agents cross the placenta and appear in breast milk in animal models.

Given the absence of controlled human data and the formulation’s intended male use, compounded troches should be avoided in women who are pregnant, may become pregnant, or are breastfeeding; partners of pregnant women should be counseled that fetal safety has not been established..^[6]

Troches should be dispensed in tight, light-resistant, child-resistant containers and stored at 20 - 25 °C (68 - 77 °F. Under USP <795> guidelines for non-aqueous formulations prepared with USP-grade ingredients in a controlled environment, a beyond-use date of 180 days is appropriate. Patients should keep troches dry, avoid refrigeration (which can alter texture), and inspect for discoloration or mold before each use.^[8]

1. Brock, G. B., & Jackson, G. (2004). Phosphodiesterase-5 inhibitor differentiation based on selectivity and half-life. Clinical Cardiology, 27(13), 35-42. https://doi.org/10.1002/clc.4960271305 2.DrugBank. (2025). Tadalafil (DB00820) drug monograph. https://go.drugbank.com/drugs/DB00820 3.U.S. National Library of Medicine. (2023). Tadalafil [DailyMed Label]. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=fceb8aaf-b4eb-4004-8ca4-f004eac6b314 4.Drugs..com. (2024). Apomorphine and ondansetron: interaction overview. https://www.drugs.com/drug_interactions/apomorphine-with-ondansetron-224-0-1752-0.html 5.RxList. (2024). Apomorphine hydrochloride: side effects & warnings. https://www.rxlist.com/apomorphine/generic-drug.htm 6.Drugs..com. (2025). Apomorphine use during pregnancy. https://www.drugs.com/pregnancy/apomorphine.html 7.Drugs..com. (2025). Tadalafil: prescribing information. https://www.drugs.com/pro/tadalafil.html 8.United States Pharmacopeia. (2022). Apomorphine hydrochloride tablets monograph. https://ftp.uspbpep.com/v29240/usp29nf24s0_m5690.html 9.Miller, K., et al. (2023). Evidence for benefits and risks of tadalafil as a non-prescription medicine: A Delphi consensus. Frontiers in Pharmacology, 14, 1254706. https://doi.org/10.3389/fphar.2023.1254706 10.Mykoniatis, I., et al. (2021). Combination therapies for erectile dysfunction: A systematic review and meta-analysis. JAMA Network Open, 4(2), e2037323. https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2776545 11.Park, C., et al. (2021). Pharmacokinetics and comparative bioavailability of apomorphine sublingual film. Drugs in R&D, 21(1), 1-11. https://doi.org/10.1007/s40120-021-00251-6 12.U.S. Pharmacist. (2024). Tadalafil 10 mg troches: formulation and stability. https://www.uspharmacist.com/article/tadalafil-10-mg-troches 13.Staiger, B. (2023). Profound hypotension with apomorphine and ondansetron coadministration. HelloPharmacist. https://hellopharmacist.com/drug-interactions/drugs/ondansetron/apomorphine-with-ondansetron 14.Sokolakis, I., et al. (2021). Assessment of combination therapies versus monotherapy for erectile dysfunction. JAMA Network Open, 4(2), e2037325. https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2776549 15.U.S. Food and Drug Administration. (2024). Tadalafil label (NDA 218490). https://www.accessdata.fda.gov/drugsatfda_docs/nda/2024/218490Orig1s000Lbl.pdf 16.U.S. Food and Drug Administration. (2020). Apomorphine sublingual film chemistry review (NDA 210875). https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/210875Orig1s000ChemR.pdf 17.Ro. (2024). Does apomorphine for ED work? https://ro.co/erectile-dysfunction/apomorphine-for-ed/ 18.Kukreja, R. C., et al. (2009). Tadalafil protects against myocardial ischemia-reperfusion injury: pharmacokinetic considerations. Circulation, 120(8), 708-716. https://doi.org/10.1161/CIRCULATIONAHA.108.843979 Disclaimer
2. This compounded medication is prepared under section 503A of the U.S. Federal Food, Drug, and Cosmetic Act. Safety and efficacy for this formulation have not been evaluated by the FDA. Therapy should be initiated and monitored only by qualified healthcare professionals.

How quickly can an erection be expected after placing a troche?
Apomorphine’s central action may trigger an erectile response in as little as 15 minutes, while tadalafil sustains rigidity thereafter.^[9]

Is this combination more effective than tadalafil alone?
Systematic reviews suggest that dual-mechanism regimens improve International Index of Erectile Function domain scores compared with monotherapy, though high-quality trials remain limited.^[10]

Will it work if I have nerve damage after prostatectomy?
Central dopaminergic stimulation can aid psychogenic components, but severe cavernous-nerve injury may still limit response; adjunctive rehabilitation strategies may be required.^[11]

How long does one troche last?
Tadalafil’s half-life provides a therapeutic window of roughly 24-36 hours, allowing sexual activity over an extended period without redosing.^[12]

May I take ondansetron for nausea at the same time?
No; co-administration of ondansetron or any 5-HT₃ antagonist with apomorphine is contraindicated because profound hypotension and syncope can occur.^[13]

Can I combine the troche with a vacuum-erection device?
Yes; mechanical aids may be used concurrently and can provide additive rigidity according to meta-analytic data.^[14]

Are there fertility concerns with repeated use?
No human studies show clinically significant sperm abnormalities, but animal data reveal minor reductions in motility at high tadalafil doses; the implications for human fertility are uncertain.^[15]

Could dry mouth affect absorption?
Yes; xerostomia or mucosal lesions may slow dissolution and uptake, so patients should ensure adequate oral moisture and avoid alcohol immediately before dosing.^[16]

Is apomorphine addictive?
Dopamine agonists can rarely provoke impulse-control disorders, but such effects are dose-related and uncommon at the low doses used for erectile dysfunction.^[17]

Why not just use daily tadalafil tablets?
Troches offer more rapid central facilitation via apomorphine and may benefit men with unpredictable gastrointestinal absorption, though daily tablets remain suitable for those preferring regimen simplicity.¹⁸