The History of Bethanechol: A Timeline of Its Development and Use

Barbara Lalicki October 30, 2025 Medications 11 Comments
The History of Bethanechol: A Timeline of Its Development and Use

Bethanechol isn’t a household name, but for decades it’s been quietly helping people who struggle to empty their bladders after surgery, nerve damage, or childbirth. It doesn’t cure anything. It doesn’t make you feel better instantly. But it does something simple and powerful: it tells your bladder to contract. And that’s made all the difference for millions.

Origins in the 1930s: A Drug Born from Nerve Research

In the early 1930s, scientists were digging into how nerves control organs. They knew acetylcholine was the main chemical messenger for the parasympathetic nervous system - the part that slows your heart, boosts digestion, and makes your bladder squeeze. But acetylcholine itself couldn’t be used as a drug. It broke down too fast in the body, lasting only seconds.

Researchers at the University of Chicago, led by pharmacologist Henry Dale and later expanded by others, started testing synthetic versions. They wanted something that mimicked acetylcholine but lasted longer. That’s when they created bethanechol - a molecule designed to resist breakdown by cholinesterase, the enzyme that normally destroys acetylcholine.

By 1934, they had a stable compound. It was called carbamoyl-β-methylcholine chloride. Later, it got the simpler name: bethanechol chloride. It wasn’t flashy. It didn’t cure cancer or kill bacteria. But it was precise. It acted only on muscarinic receptors - the ones in the bladder, gut, and salivary glands - not on the ones in the heart or blood vessels. That made it safer than earlier drugs.

1940s-1950s: First Medical Use in Hospitals

Bethanechol hit the market in the late 1940s. It was initially used in hospitals to treat postoperative urinary retention. After major surgeries - especially pelvic or spinal procedures - many patients couldn’t urinate. Catheters were common, but they carried infection risks. Bethanechol offered a non-invasive alternative.

By the 1950s, doctors were using it for neurogenic bladder, a condition where nerve damage from diabetes, multiple sclerosis, or spinal injuries weakens bladder control. It was also tried for ileus - when the intestines stop moving after surgery. Some studies showed it helped restore gut motility faster than waiting it out.

One 1953 study in the Journal of the American Medical Association tracked 87 patients with urinary retention after hysterectomy. Nearly 70% passed urine naturally within two hours of a 10 mg dose. That was a big deal back then. Catheters were messy. Infections were common. Bethanechol gave doctors a tool that worked without cutting or inserting anything.

1960s-1980s: Widespread Use and Side Effects

By the 1970s, bethanechol was in most hospital pharmacies. It came in tablets and injections. The typical dose was 5-10 mg, taken three or four times a day. Doctors prescribed it for chronic urinary retention, especially in older women after childbirth or men with enlarged prostates who couldn’t tolerate surgery.

But side effects were hard to ignore. Because bethanechol affects all muscarinic receptors, it triggered sweating, salivation, stomach cramps, diarrhea, and blurred vision. Some patients felt their heart race or drop too low. That’s why it wasn’t used for heart conditions - it was too unpredictable. Still, for many, the trade-off was worth it.

By the 1980s, newer drugs like oxybutynin and tolterodine started appearing. These targeted the bladder more directly and had fewer systemic side effects. Bethanechol began to fade from first-line use. But it never disappeared. In nursing homes, rehab centers, and outpatient clinics, it remained a go-to for patients who didn’t respond to newer options.

Happy patient receiving bethanechol pill as their bladder contracts in cartoon style.

1990s-2010s: Niche Role and Regulatory Scrutiny

The 1990s brought stricter FDA guidelines. Drug companies had to prove long-term safety and effectiveness. Bethanechol, a cheap, old drug with no patent, didn’t get the funding for big trials. But smaller studies kept showing its value.

A 2002 study in Neurourology and Urodynamics looked at 120 patients with spinal cord injuries. Those who took bethanechol had significantly fewer urinary tract infections and less residual urine than those who didn’t. Another 2010 review in The Journal of Urology confirmed it was still effective for neurogenic bladder when other drugs failed.

Insurance companies started pushing back. Bethanechol was inexpensive - often under $10 for a month’s supply - but some insurers labeled it “outdated.” That didn’t stop doctors. In rural clinics and Veterans Affairs hospitals, it remained a staple. It didn’t need refrigeration. It didn’t require complex monitoring. It worked when you needed it.

2020s: Still in Use, Still Important

Today, bethanechol is still on the World Health Organization’s List of Essential Medicines. It’s available in the U.S., U.K., Canada, Australia, and many European countries. Generic versions are sold under names like Urecholine and Bethanechol Chloride.

It’s not the first choice anymore. But it’s still the last resort for many. Elderly patients with dementia who can’t take newer drugs because of confusion or dry mouth? Bethanechol. Patients with spinal cord injuries who can’t afford expensive bladder implants? Bethanechol. People in low-income countries with no access to advanced urology care? Bethanechol.

It’s also used off-label for gastroparesis - when the stomach doesn’t empty properly. While metoclopramide is more common, some patients who can’t tolerate it find relief with bethanechol. A 2021 case series from the University of Manchester reported three elderly patients with diabetic gastroparesis who regained normal eating habits after adding low-dose bethanechol.

Elderly person with glowing bethanechol pill and happy bladder icon in cozy setting.

How It Works - Simply

Bethanechol doesn’t trick your body. It doesn’t mask symptoms. It directly stimulates the muscarinic receptors in the detrusor muscle of the bladder. That muscle is what squeezes to empty your bladder. When it’s weak or inactive, bethanechol gives it a nudge. Within 30 to 60 minutes, you feel the urge to go. The effect lasts about an hour.

It’s not magic. It doesn’t fix nerve damage. But it restores function. For someone who’s been catheterized for weeks, that’s everything.

Why It Still Matters

Modern medicine loves new gadgets and expensive pills. But bethanechol reminds us that sometimes, the best tools are the oldest ones. It’s cheap. It’s reliable. It doesn’t need a smartphone app or a complex algorithm to work.

It’s also a lesson in precision. It targets one system - the parasympathetic nervous system - without wrecking others. That’s why it survived when other drugs failed. It didn’t try to do too much. It just did one thing well.

Today, as healthcare costs climb and access narrows, bethanechol’s role is growing again. In places with limited resources, it’s often the only option. Even in wealthy countries, it’s a lifeline for people who can’t tolerate newer drugs or can’t afford them.

It’s not glamorous. But for the millions who’ve peed on their own again because of it - it’s everything.

Is bethanechol still prescribed today?

Yes, bethanechol is still prescribed, though less often than in the past. It’s mainly used for urinary retention caused by nerve damage, surgery, or childbirth, especially when newer drugs don’t work or aren’t affordable. It’s also used off-label for gastroparesis in some cases. Generic versions are widely available and cost under $10 per month in many countries.

What are the main side effects of bethanechol?

Common side effects include sweating, increased saliva, stomach cramps, nausea, diarrhea, flushing, and blurred vision. Less common but serious effects are low blood pressure, slow heart rate, and bronchospasm in people with asthma. It’s not recommended for people with ulcers, intestinal blockages, or severe heart conditions.

How does bethanechol compare to oxybutynin?

Bethanechol makes the bladder contract to help empty it. Oxybutynin relaxes the bladder to reduce urgency and frequency. They treat different problems. Bethanechol is for retention - when you can’t pee. Oxybutynin is for overactive bladder - when you pee too often or too urgently. They’re not interchangeable.

Can you take bethanechol long-term?

Yes, many patients take bethanechol for months or years with no major issues, especially under medical supervision. Long-term use requires monitoring for side effects like low blood pressure or digestive problems. It’s often used in combination with pelvic floor therapy or intermittent catheterization for best results.

Why isn’t bethanechol used more often?

It’s not used as often because newer drugs like tolterodine and mirabegron have fewer side effects and are easier to tolerate. Also, since bethanechol is generic and cheap, drug companies haven’t invested in large marketing campaigns or new studies. But it remains a critical option for patients who don’t respond to other treatments.

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11 Comments

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    Katie Ring

    October 31, 2025 AT 11:37

    Bethanechol is the quiet hero of urology-no hype, no patent, no fancy marketing. Just a molecule that says, 'I see you struggling, and I’m here to help.' Modern medicine forgets that sometimes the best solutions aren’t the newest ones-they’re the ones that just work.

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    Adarsha Foundation

    November 1, 2025 AT 23:28

    This is beautiful. In India, we still use this in rural clinics where nothing else is available. It’s not glamorous, but it saves dignity. Thank you for writing this.

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    Alex Sherman

    November 2, 2025 AT 15:08

    Oh please. This is just a 1930s relic that’s kept alive by nostalgia and poor prescribing habits. We have better drugs now. Why are we still clinging to this like it’s some kind of sacred text?

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    Oliver Myers

    November 3, 2025 AT 23:54

    I just want to say how much I appreciate this thoughtful, well-researched piece. It’s rare to see a drug get the respect it deserves-not because it’s trendy, but because it’s reliable. Thank you for highlighting the quiet heroes of medicine.

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    John Concepcion

    November 4, 2025 AT 11:22

    Wow, someone actually wrote a whole essay about a drug that makes you sweat and cramp? Congrats, you just turned a side effect list into a TED Talk. Next up: ‘The Emotional Journey of Laxatives’?

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    Caitlin Stewart

    November 5, 2025 AT 19:45

    My mom took this after her hysterectomy. She cried when she peed on her own for the first time in weeks. Not because it was perfect-but because it gave her back a part of her body they told her was broken. This isn’t just pharmacology. It’s humanity.

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    Emmalee Amthor

    November 5, 2025 AT 22:39

    It’s wild how we’ve forgotten that medicine doesn’t have to be complicated to be powerful… bethanechol is like a whisper in a world that screams for innovation… it doesn’t fix the nerve… it just gives the muscle a nudge… and somehow… that’s enough…

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    Marcia Facundo

    November 6, 2025 AT 12:44

    Ugh. I hate when people romanticize old drugs. It’s just a crutch. People should get real treatment-not this outdated junk.

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    Ajay Kumar

    November 7, 2025 AT 21:28

    You know what’s really funny? In India, we use this because we can’t afford fancy bladder implants, but in the U.S., people use it because they think it’s ‘natural’ or ‘holistic’-like it’s some kind of herbal tea. Meanwhile, the WHO lists it as essential, but you guys treat it like a relic from the dinosaur age. Hypocrisy much?

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    Joseph Kiser

    November 8, 2025 AT 05:59

    THIS. This right here. 🙌 I’ve seen patients on catheters for months… then one dose of bethanechol… and they walk out of the clinic smiling. No tech. No app. Just chemistry and care. This is why I became a doctor. Not for the hype. For the quiet wins.

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    Pradeep Kumar

    November 8, 2025 AT 20:15

    So simple, so powerful 😊 In my village, we call it 'the pee pill' and it’s more trusted than any new medicine. No need for fancy machines. Just one tablet. One hope. One chance to feel normal again.

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