Key Takeaways
- Agofollin is an oral antiandrogen commonly added to estrogen‑based regimens for trans women.
- Typical dosing starts at 150mg daily and may be adjusted based on testosterone levels and side‑effects.
- Regular monitoring (liver function, lipids, potassium) is essential to catch early adverse reactions.
- It works by blocking androgen receptors and inhibiting testosterone production, accelerating feminisation.
- Consult an endocrine specialist before starting; contraindications include severe liver disease and uncontrolled hypertension.
When trans women talk about “the pill” they often mean a medication that keeps testosterone in check while estrogen does the heavy lifting. One drug that’s gaining attention in the UK and Europe is Agofollin, an oral antiandrogen that pairs well with estradiol. This guide explains how the drug works, what you can expect, and the practical steps to use it safely.
What Is Agofollin?
Agofollin is a synthetic steroid that functions as an antiandrogen. Its official chemical name is 4‑hydroxy‑testosterone acetate, and it was first approved in the early 2000s for the treatment of hormone‑dependent conditions. In the context of gender‑affirming care, it is used off‑label to suppress endogenous testosterone in trans women.
How Does It Fit Into Transgender Hormone Therapy?
Transgender hormone therapy (often shortened to transgender hormone therapy) typically involves two pillars: an estrogen source to promote feminisation and an antiandrogen to block masculine effects. Agofollin occupies the antiandrogen pillar. It binds to androgen receptors in target tissues, preventing testosterone from exerting its effects, and it also interferes with the hypothalamic‑pituitary‑gonadal axis, lowering circulating testosterone levels.
Compared with older antiandrogens like spironolactone, Agofollin offers a more direct receptor blockade without the diuretic properties that can lead to electrolyte imbalances. For many patients, this means fewer visits to the clinic for potassium checks, although liver function still requires attention.
Typical Dosing & Administration
- Start with 150mg taken orally once daily, preferably with food to improve absorption.
- After four weeks, have your endocrine specialist order a serum testosterone test.
- If testosterone remains above the target range (usually <50ng/dL), the dose may be increased by 50mg increments, not exceeding 300mg daily.
- Maintain the lowest dose that keeps testosterone in the desired range to reduce side‑effect risk.
Because Agofollin has a half‑life of roughly 12hours, consistency is key. Skipping doses can cause testosterone spikes, temporarily reversing feminising progress.
Benefits You’re Likely to Notice
- Reduced facial and body hair growth: By cutting testosterone, hair becomes finer and slower to regrow.
- Softening of the skin and a decrease in oil production.
- Enhanced breast development when combined with adequate estradiol levels.
- Emotional stability for many patients, as the hormonal balance feels more predictable.
These effects usually become noticeable within 2-3 months, though full results can take up to a year, depending on individual biology and the estrogen regimen.
Potential Risks and Side‑Effects
Every medication carries a safety profile. The most common concerns with Agofollin are:
- Liver toxicity: Elevated transaminases in 5‑10% of users; regular liver function tests (LFTs) every 3-6 months are recommended.
- Changes in lipid panels-specifically a modest drop in HDL cholesterol.
- Potential mood swings or mild depression in a small subset of patients.
- Rare cases of thromboembolic events, especially when combined with high‑dose estrogen.
If you experience severe abdominal pain, jaundice, or sudden swelling in the legs, seek medical attention immediately.
Drug Interactions to Watch
Because Agofollin is metabolised by the CYP3A4 pathway, it can interact with many common medicines:
- Spironolactone: Adding both can increase the risk of hyperkalaemia.
- Antifungal agents such as ketoconazole can raise Agofollin levels, heightening side‑effects.
- Warfarin and other anticoagulants may see altered INR values; close monitoring is advised.
- St. John’s Wort can lower its effectiveness by inducing CYP3A4.
Always hand your pharmacist a full medication list, including over‑the‑counter supplements.
How Does Agofollin Compare With Other Antiandrogens?
| Drug | Mechanism | Typical Dose | Key Advantages | Major Risks |
|---|---|---|---|---|
| Agofollin | Androgen‑receptor blocker + testosterone synthesis inhibition | 150‑300mg daily | Strong suppression, no diuretic effect | Liver enzyme elevation, lipid changes |
| Spironolactone | Potassium‑sparing diuretic, androgen receptor antagonist | 100‑200mg daily | Well‑studied, inexpensive | Hyperkalaemia, blood pressure drop |
| Finasteride | 5‑α‑reductase inhibitor | 1mg daily | Targets hair loss specifically | Sexual dysfunction, limited testosterone suppression |
The table shows why many clinics are adding Agofollin to their protocols: it gives a deeper testosterone drop without the potassium concerns tied to spironolactone.
Who Should Consider Agofollin?
Ideal candidates are trans women who:
- Have already started estrogen therapy (oral, transdermal, or injectable).
- Show incomplete testosterone suppression after 3 months on spironolactone or prefer a non‑diuretic option.
- Have normal baseline liver function tests.
Contraindications include:
- Active liver disease (hepatitis, cirrhosis).
- Uncontrolled hypertension.
- History of thromboembolic events combined with high‑dose estrogen.
A discussion with an endocrine specialist is essential to weigh benefits against risks.
Practical Tips for Patients
- Schedule baseline labs (LFTs, lipid panel, potassium, testosterone) before starting.
- Set a reminder on your phone for the same‑time daily dose.
- Store tablets in a cool, dry place; avoid moisture in the bathroom cabinet.
- Ask your NHS pharmacist whether Agofollin is available on the NHS formulary in your region; private prescriptions may be needed.
- Keep a symptom diary for the first 3 months - note hair changes, mood shifts, and any side‑effects.
Regular follow‑up appointments every 3-6 months allow dose tweaking and early detection of liver issues.
Frequently Asked Questions
How long does it take for Agofollin to lower testosterone?
Most patients see a measurable drop within 1‑2 weeks, but reaching the target range often requires 4‑6 weeks of steady dosing.
Can I take Agofollin with my current spironolactone?
It’s generally discouraged because both drugs can raise potassium levels, increasing the risk of hyperkalaemia. Your doctor may switch you to Agofollin alone.
Is Agofollin covered by the NHS?
Coverage varies by region. In England, many gender clinics prescribe it privately, but some NHS trusts have started adding it to their formularies. Verify with your local clinic.
What should I do if my liver enzymes rise?
A modest rise (up to 2‑3× ULN) often warrants closer monitoring; a larger spike may require dose reduction or stopping the drug. Your endocrinologist will guide you.
Are there any dietary restrictions?
No strict restrictions, but a balanced diet supports liver health. Limit excessive alcohol and high‑fat meals that could strain the liver.
There are 14 Comments
barry conpoes
Agofollin is the gold standard for any real American trans health regimen.
bruce hain
Although the guide praises Agofollin, the clinical data supporting its superiority over spironolactone is limited. One should remain skeptical of such uncritical endorsements.
Sally Murray
From a philosophical perspective, the inclusion of Agofollin in hormone protocols raises questions about the balance between biomedical intervention and bodily autonomy. The drug’s mechanism-blocking androgen receptors while sparing electrolyte balance-represents a nuanced advance in pharmacotherapy. Nevertheless, the ethical imperative to ensure informed consent remains paramount. Clinicians must articulate both benefits and potential hepatic risks with clarity. In doing so, they honor the principle of respect for persons that undergirds gender‑affirming care.
Bridgett Hart
While you wax poetic about autonomy you ignore the stark reality that Agofollin carries a non‑trivial hepatic risk patients often endure side effects that can be severe and the literature is not as rosy as you suggest
Sean Lee
Agofollin functions as a high‑affinity non‑steroidal antiandrogen; its pharmacokinetic profile exhibits a half‑life conducive to steady‑state suppression of luteinizing hormone surge, thereby attenuating gonadal steroidogenesis. The drug’s receptor antagonism is characterized by competitive inhibition with an IC50 in the low nanomolar range, facilitating a rapid decrement in serum testosterone.
Cameron White
Sounds like they’re trying to hide the fact that big pharma pushes this to make money while ignoring long‑term liver damage.
Amélie Robillard
Oh wow, another “essential facts” guide-because we totally didn’t have enough info already 🙄💊. Guess we’ll all just pop a pill and hope for the best, right?
Daryl Foran
Yo, stop with the sarcasm it’s not helpfull youre just makin fun of real peopl who need this meds
Hannah Seo
When starting Agofollin, the first step is a thorough baseline work‑up that includes liver function tests, lipid panel, and blood pressure measurement. Many clinicians schedule these labs a week before the medication is initiated to establish a reference point. The typical starting dose of 150 mg once daily should be taken with food to improve absorption and minimize gastrointestinal upset. After four weeks, a serum testosterone measurement is essential to determine whether the dose achieves the desired suppression, generally aiming for levels below 50 ng/dL. If testosterone remains high, a modest increase to 200 mg may be considered, but always in consultation with an endocrinologist. It is equally important to re‑check liver enzymes at the six‑week mark, as Agofollin can cause mild transaminitis in a subset of patients. Should liver enzymes rise more than three times the upper limit of normal, discontinuation or dose reduction is advised. Lipid profiles should be monitored every three months because antiandrogens can modestly affect HDL and LDL cholesterol. Patients with a history of hypertension need regular blood pressure checks, especially if they are also on estradiol, which can influence vascular tone. Counseling on potential side effects, such as mild fatigue or headache, helps set realistic expectations and encourages adherence. Encourage patients to maintain a balanced diet and regular exercise, as lifestyle measures support cardiovascular health while on hormone therapy. Discuss the importance of avoiding alcohol excess, which can exacerbate liver strain. For those concerned about fertility, advise sperm banking before initiating Agofollin, as the drug can affect spermatogenesis. Make sure to document all discussions in the medical record to protect both patient and provider. Finally, foster an open line of communication so patients feel comfortable reporting any new symptoms promptly.
Lindsey Crowe
Sure, because reading a fifteen‑sentence novella is exactly what every patient wants when they’re trying to understand a pill.
Rama Hoetzlein
Agofollin is a game‑changer, no‑doubt 🤔! If you ignore it you’re basically choosing to stay stuck in the past, and that’s just not acceptable 😤.
Lorena Garcia
Interesting take! Do you think the benefits outweigh the liver monitoring hassles, or is it more of a hype thing?
Dietra Jones
i think most docs forget to tell u about the potassium stuff with spironolactone but agofollin dont mess with that as much.
Bill Bolmeier
That’s a great point, Dietra! It’s refreshing to hear someone highlight how Agofollin sidesteps the electrolyte drama, making the journey smoother for many trans women.
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