Oxytocin 50iu | PT-141 1mg | Tadalafil 5mg
Oxytocin 50iu | PT-141 1mg | Tadalafil 5mg is a prescriber-directed troche prepared or dispensed for patient-specific use within the Weight Management therapy area. Genesis should dispense this medication only pursuant to a valid prescription and the prescriber's clinical judgment.
This compounded troche or oral/sublingual preparation combines three active ingredients—oxytocin 50 IU, bremelanotide (PT-141) 1 mg, and tadalafil 5 mg—into a single patient-specific dosage form. Each ingredient addresses a distinct aspect of sexual function and intimacy: oxytocin modulates social bonding and arousal, PT-141 stimulates central melanocortin pathways to enhance sexual desire, and tadalafil inhibits PDE5 to promote vascular-mediated erectile or arousal response. Genesis Compounding prepares this as a prescription-only 503A compounded preparation that is not FDA-approved as a combined product.
| Active Ingredient | Pharmacologic Role |
|---|---|
| Oxytocin 50 IU | Posterior pituitary neuropeptide that, via central and peripheral oxytocin receptor activation, modulates social bonding, trust, and pro-sexual behaviors. |
| PT-141 (Bremelanotide) 1 mg | Melanocortin receptor 4 (MC4R) agonist that activates central dopaminergic pathways in the hypothalamus to enhance sexual desire and arousal independent of vascular mechanisms. |
| Tadalafil 5 mg | Selective phosphodiesterase type 5 (PDE5) inhibitor that increases cyclic GMP in vascular smooth muscle, promoting penile erection in men and enhanced genital blood flow in women. |
Route: Sublingual or buccal troche (dissolve under the tongue or between cheek and gum).
- Place the troche under the tongue or between the cheek and gum. Allow it to dissolve completely—do not chew or swallow whole.
- Avoid eating, drinking, or rinsing the mouth until the troche is fully dissolved (typically 10–20 minutes).
- Onset of systemic absorption begins with the sublingual/buccal mucosa, bypassing first-pass hepatic metabolism for the peptide components.
- Timing before anticipated sexual activity should be individualized per prescriber instructions.
Dosing is entirely prescriber-determined and patient-specific. General principles based on individual ingredient pharmacology:
- Oxytocin (intranasal/sublingual): Doses used in behavioral/sexual health research have ranged from 24–40 IU intranasally; exact sublingual troche equivalence requires prescriber judgment.
- PT-141: Approved subcutaneous dose is 1.75 mg; compounded sublingual bioavailability differs and dosing must be titrated by the prescriber.
- Tadalafil: FDA-approved PDE5-inhibitor dose for erectile dysfunction ranges from 5–20 mg; 5 mg is consistent with daily low-dose or on-demand use.
- Do not exceed one troche per 24 hours without explicit prescriber direction. Final dosing schedule is determined by the prescribing clinician.
- Oxytocin: Activates hypothalamic and limbic oxytocin receptors (OTRs) to release dopamine in reward circuitry, facilitating social bonding and pro-sexual motivation; also modulates parasympathetic tone.
- PT-141 (Bremelanotide): Agonizes MC4Rs in the medial preoptic area and paraventricular nucleus, activating central dopaminergic reward pathways that increase sexual arousal and desire independent of genital vascular effects.
- Tadalafil: Inhibits PDE5, the enzyme that degrades cGMP in corpus cavernosum and genital vasculature smooth muscle; elevated cGMP causes smooth muscle relaxation and vasodilation in response to nitric oxide (NO) released during sexual stimulation.
Indication context: This multi-ingredient troche is prescribed for individuals with hypoactive sexual desire, arousal disorders, or erectile dysfunction where a combination central and peripheral approach is clinically indicated. Each component is rooted in established pharmacology; however, the combined preparation has not been studied as a fixed combination in prospective clinical trials.
Monitoring considerations:
- Blood pressure monitoring—both PT-141 and tadalafil can affect blood pressure (PT-141 may transiently increase BP; tadalafil may lower BP, especially with nitrates).
- Assess for nausea, flushing, or headache at initiation.
- Tadalafil is contraindicated with nitrate-containing medications; prescribers must complete a thorough medication reconciliation before prescribing.
- Skin hyperpigmentation has been noted with extended daily PT-141 use; reassess at follow-up.
Contraindications:
- Concurrent use of organic nitrates or nitric oxide donors in any form (due to tadalafil)—risk of severe hypotension.
- Tadalafil is also contraindicated with guanylate cyclase stimulators (riociguat).
- Uncontrolled hypertension or cardiovascular disease (due to tadalafil and PT-141 hemodynamic effects).
- Hypersensitivity to any ingredient in the formulation.
Warnings & Precautions:
- PT-141 may cause transient blood pressure increases (~3 mmHg SBP/DBP) and small decreases in heart rate in the first 4 hours post-dose.
- Tadalafil potentiates hypotensive effects of antihypertensives and alpha-blockers; use caution and allow appropriate interval from alpha-blocker dose.
- PT-141 may cause focal skin hyperpigmentation (especially face, gums) with repeated use—more pronounced in patients with darker skin tones.
- Oxytocin may cause nausea or uterine cramping in some women; use in pregnant patients requires careful clinical consideration.
Drug Interactions:
- Nitrates, nitric oxide donors, riociguat: absolute contraindication with tadalafil.
- Alpha-blockers and antihypertensives: enhanced hypotension with tadalafil.
- Strong CYP3A4 inhibitors (ketoconazole, ritonavir): increase tadalafil plasma levels; dose reduction may be needed.
Common Side Effects: Nausea, flushing, headache (PT-141 and tadalafil); transient hypertension (PT-141); injection-site or mucosal irritation; back pain, myalgia (tadalafil).
Store troches in a cool, dry location away from direct light and heat (room temperature, 15–25°C is typical for troche formulations). Do not freeze. Keep in original dispensing container with lid tightly closed. Use within the beyond-use date assigned by Genesis Compounding per USP <795> or <797> standards as applicable. Keep out of reach of children.
Why are three medications combined in one troche?
Each ingredient targets a different mechanism in sexual function: oxytocin supports the social-bonding and motivational component, PT-141 activates central brain pathways that generate sexual desire, and tadalafil facilitates the peripheral vascular response to arousal. Combining them in one convenient troche allows a prescriber to address multiple pathways simultaneously.
Is this combination FDA-approved?
No. Each individual active ingredient has established pharmacology and, in some cases, FDA approval in specific formulations, but this three-ingredient combination is not FDA-approved as a fixed product. It is prepared by Genesis Compounding as a patient-specific 503A compounded preparation under a valid prescriber order.
How long before sexual activity should I take it?
Timing is prescriber-directed. PT-141 subcutaneous injection is typically taken at least 45 minutes prior; sublingual absorption may differ. Tadalafil has a prolonged half-life (~17.5 hours), so it may be taken more than an hour before. Follow your prescriber's specific instructions.
Can I take this if I use blood pressure medication?
Tadalafil may lower blood pressure and can interact with certain antihypertensive medications. PT-141 may transiently raise blood pressure. Inform your prescriber of all current medications before starting this preparation.
Can nitrates be used with this preparation?
No. The tadalafil component is absolutely contraindicated with nitrate-containing medications (e.g., nitroglycerin, isosorbide mononitrate) in any form. The combination can cause severe and potentially life-threatening hypotension.
Clinical References
Authoritative sources reviewed in preparing this clinical summary. Provided for prescriber reference; not a substitute for the prescriber’s clinical judgment.