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Almitrine Dimesylate: A Multifaceted Journey From Discovery to Promise

Historical Development

Back in the latter half of the 20th century, respiratory medicine wrestled with the tough realities of treating chronic obstructive pulmonary disease (COPD) and related hypoxemic disorders. The introduction of Almitrine Dimesylate sparked genuine interest among clinicians and pharmaceutical researchers. Reports started trickling out of France as Laboratoires Servier filed for patents describing the unique action of this compound. At a time when oxygen therapy offered only modest relief, almitrine’s ability to stimulate peripheral chemoreceptors gave patients and doctors hope for non-invasive management of chronic respiratory failure. Decades later, the story of its discovery and incremental clinical trials reflects the slow but steady path from basic pharmacological findings to application in clinical settings, especially across Europe and parts of Asia where respiratory diseases create significant burden.

Product Overview

Almitrine Dimesylate emerged as an oral medication designed for chronic hypoxemia, marking itself out not only by purpose but also by its distinctive action on carotid body chemoreceptors. The drug fine-tuned the body’s natural drive to breathe, improving blood gas profiles where conventional bronchodilators stalled. Across pharmacies, it appeared in bright, compact tablet form. Unlike most bronchodilators or corticosteroids, its function gears directly toward enhancing oxygenation rather than just easing constrained airways. International brand names, like Vectarion, built a presence in specific markets, but global enthusiasm wavered as broader trials highlighted variable benefits in differing patient groups.

Physical & Chemical Properties

With a molecular formula of C26H34F2N4O2•2C2H6O4S, Almitrine Dimesylate presents as a white to off-white solid powder. Under lab scrutiny, its melting point sits comfortably above 170 °C, reflecting solid stability under ordinary room conditions. Given its moderate solubility in water and greater solubility in methanol and ethanol, chemists found handling and compounding relatively straightforward. One defining point: its two fluorine atoms contribute not only to biological activity but also to the spectrum of spectral analysis signatures used during quality control. Some of the earliest batch records describe odorless, tasteless crystals—a boon for oral therapy development.

Technical Specifications & Labeling

Pharmaceutical preparations of Almitrine Dimesylate usually arrive as 30 mg tablets, with packaging designed to restrict inadvertent exposure to moisture or light. A complete label highlights the active salt, recommended dosing, excipients, storage temperature ranges (generally under 25°C), and a batch-specific expiration date. Most manufacturers include clear pictogram warnings about storage away from children and direct sunlight. In clinical practice, dosing recommendations stem from body weight and arterial blood gas analysis, with patients receiving tailored regimens to avoid overstimulation of respiratory drive. Labels also note contraindications, focusing on individuals with severe liver disease or pulmonary hypertension, as these populations faced higher adverse event rates during post-marketing surveillance.

Preparation Method

The synthetic pathway to Almitrine Dimesylate traces back to established routes for assembling fluorinated aromatic amines and tertiary alcohols, joined through stepwise condensation. Most labs work with substituted benzyl bromides, fluoroaryl precursors, and isopropylamine derivatives, combining them under controlled temperature and pH regimes. After base catalyzed condensation, the crude almitrine undergoes neutralization and a series of solvent washes to achieve primary purity. Mesylation, the critical salt formation step, comes last. By treating the free base with methanesulfonic acid in non-aqueous conditions, chemists isolate Almitrine Dimesylate as the final salt. Filtration, washing, and vacuum drying remove impurities, with quality checks focusing on residual solvents, particle size, and specific optical activity—a requirement under international pharmacopoeia standards.

Chemical Reactions & Modifications

In research environments, Almitrine Dimesylate sometimes acts as a scaffold for new exploratory drugs, given its intrinsic fluorinated aromatic rings and tertiary amine side chains. The compound withstands mild acid and base hydrolysis, though exposure to concentrated acid can result in demethylation or decomposition. In simulated metabolic studies, N-dealkylation and aromatic hydroxylation lead to primary metabolites observed in patient urine. Chemists push the core structure through nucleophilic substitution, aiming to tune activity at the carotid bodies or mitigate off-target side effects. Some early-stage experiments swapped out the fluorine sides for triazole and isoxazole groups, with varying effects on receptor binding. The mesylate salt formation step also sets the stage for analogs produced as tosylates or hydrochlorides in attempt to shift pharmacokinetics.

Synonyms & Product Names

Almitrine Dimesylate pops up on chemical registries under CAS number 29638-49-1, recognized across various pharma markets as Vectarion, Almitrin, and by its IUPAC name N,N-Dipropyl-2-[6-(trifluoromethyl)-2-pyridyl]ethanamine methane sulfonate. Catalog listings by bulk suppliers sometimes use alternate spellings, but the unique dimesylate identifier distinguishes it from the free base and other salts. Despite limited generic alternatives on the global stage—a result of patchy regulatory approval—trade names maintain consistent content claims, simplifying identification in clinical settings.

Safety & Operational Standards

Handling Almitrine Dimesylate in a professional environment comes with strict expectations for safety. Technicians processing the powder use gloves, face masks, and dust extractors to prevent skin contact or accidental inhalation. Standard operating procedures require secure containment, readiness for accidental spills, and comprehensive documentation from batch synthesis through to final compounding. Pharmacists keep careful records on patient dispensing, especially since Almitrine intake affects gas exchange and can alter ongoing oxygen therapy requirements. Adverse effect panels flag early signs of peripheral neuropathy, weight loss, or liver enzyme shifts as signals for immediate dose review. Facilities storing the medication comply with regulations regarding controlled drug storage, disposal, and documentation of transfers, keeping misuse and environmental contamination risks to a minimum.

Application Area

Chronic obstructive pulmonary disease, sleep apnea, and hypoxemia linked to cardiac or neuromuscular causes dominate the list of indications for Almitrine Dimesylate. In clinical rounds, its role centers on patients with chronic low oxygen levels who cannot tolerate or do not respond well to invasive ventilation. Some intensivists in Europe added it to management plans for end-stage lung disease before the transition to palliative care or transplantation. During the COVID-19 pandemic, a handful of researchers revisited the compound, testing its potential to counteract severe hypoxemia in acute respiratory distress. Results proved mixed, held back mostly by limited trial sizes and lingering questions about neurological side effects. In the research realm, basic scientists still probe almitrine derivatives for mechanistic insights into carotid body stimulation, laying groundwork for newer molecules.

Research & Development

Academic groups and pharmaceutical companies circle Almitrine Dimesylate with ongoing curiosity. Chronic respiratory disease remains a rising global health challenge, particularly in countries facing air pollution and high smoking rates. Pharmacological stimulation of chemoreceptors promises an alternative path to managing chronic hypoxic symptoms, especially for patients where other interventions cannot reach deep tissue oxygenation demands. Research pursuits chase smaller, more selective molecules, aiming to keep the therapeutic benefits without drifting into side effect territory. Preclinical researchers dissect how molecular tweaks influence absorption, metabolism, and central nervous system penetration. Large data sets from European post-market surveillance keep feeding meta-analyses that refine guidelines for patient selection—after all, therapies like almitrine only show full value in the right clinical scenario.

Toxicity Research

Safety warnings around Almitrine Dimesylate did not appear out of thin air. Years of clinical monitoring and animal research brought to light the risk of dose-dependent peripheral neuropathy, especially with long courses or excess dosing. Early rat and dog studies exposed neurotoxic patterns at the highest doses, including sensory nerve degeneration and weight loss. Human case series registered similar patterns: numbness in fingers and toes, subtle gait changes, and sluggish reflexes signaled issues for neurologists and primary care teams. Elevated liver enzymes also turned up in blood panels, with rare cases leading to drug withdrawal. Regulatory authorities in several countries either suspended or limited wider use pending ongoing safety reviews, shining a light on the tricky tradeoff between clinical benefit and likelihood of harm. The safety profile of any respiratory stimulant, as clinicians stress, depends on close follow-up, patient education, and clear criteria for stopping therapy.

Future Prospects

Continued interest in Almitrine Dimesylate arises from persistent unmet needs in respiratory care. As populations age and environmental air quality wavers, more people find themselves living with chronic hypoxic symptoms that defy the best efforts of ventilators and oxygen tanks. Scientific teams hunt for ways to separate the therapeutic elements of almitrine from its neurotoxic baggage, combining modern molecular modeling with old-school bench chemistry. Digital health tools and wearable monitors now help identify patients who might get the greatest benefit from non-invasive respiratory stimulants, opening new windows for research trials. Even where regulators stalled or halted almitrine use, progress here often lays the stepping stones for the next class of chemoreceptor-targeted therapies. The broader lesson that comes from decades of almitrine research: clinical innovation never really ends, especially when stubborn medical challenges keep knocking at the door.




What is Almitrine Dimesylate used for?

Facing Breathing Problems Head-On

People who struggle to catch their breath, especially those with chronic lung diseases, understand how heavy each inhale can feel. Over the years, the medical community has hunted for solutions to help these individuals lead fuller lives. Almitrine dimesylate, a drug born from this pursuit, steps in to support breathing where lungs begin to lose strength.

How Almitrine Dimesylate Offers Support

Doctors reached for almitrine as a way to prop up oxygen levels in certain patients. The drug acts by sharpening the response of blood vessels in the lungs, nudging more blood toward healthy air sacs and away from damaged ones. This allows the body to grab more oxygen from each breath, especially in people with damaged lungs from illnesses like COPD or emphysema. In my own encounters with respiratory clinics, I saw exhausted patients—those fighting for each breath—find some relief with a medication like this.

Unique Place Among Treatments

Doctors haven’t always had perfect tools for chronic respiratory disease. Oxygen tanks, inhalers, and steroids all play their part, but sometimes the body needs a spark to use oxygen more effectively. Almitrine offers another approach, rarely discussed outside of specialist circles. In France, the drug found a home in treatment plans for people with advanced lung diseases. Its use was not just about bringing in more medications, but about targeting problems right at the micro-level in the lungs.

Risks and Concerns: A Balanced Outlook

With any medicine, especially those tinkering with blood flow, you have to watch for trouble. Side effects like nerve problems or weight loss sent up red flags and led some countries to put a stop to regular use. Personally, I remember sitting with clinicians debating if the benefits could ever outweigh these risks. Some felt desperate to give patients every scrap of help, especially when oxygen tanks and standard inhalers stopped making life easier.

Fact: Reports show that some people taking almitrine developed tingling or numbness in their feet after months on the drug. These stories matter, because the right treatment shouldn’t trade one health problem for another. France’s drug watchdog, for example, pressed for tighter controls on almitrine in the late 2000s, highlighting the pressure the medical world feels to balance harm and help.

Looking for the Best Way Forward

Almitrine caught some attention during the COVID-19 pandemic. Doctors, searching for ways to lift failing oxygen levels, looked again to this niche drug. A small number of patients found their oxygen readings improved, giving hope when hospital beds filled with people clinging to every breath. Still, these uses stay experimental and require careful monitoring.

To do better for people with hard-to-treat lung conditions, research must go deeper. Clinical trials that track not just oxygen numbers but truly meaningful outcomes—such as the ability to walk or sleep—would offer real answers. Safer alternatives or new versions of the drug may also open the door for more widespread use one day.

Staying Informed, Choosing Wisely

Anyone considering almitrine faces a real tradeoff. It’s a tool, forged out of patient need and medical innovation, but not without sharp edges. Honest conversations between patients and their care teams make the difference. Every new advance or setback with almitrine reminds us to keep the focus on improving daily life for those who fight for every breath.

What are the common side effects of Almitrine Dimesylate?

Understanding Almitrine Dimesylate

Almitrine dimesylate draws the attention of doctors for one main reason: it helps boost oxygen in the blood. This medicine enters the scene for people who struggle with low oxygen due to longstanding lung diseases. Doctors in Europe have tried it over the years, mostly for breathing problems tied to conditions such as COPD.

The Side Effects You Might Face

Even though doctors hope for better breathing, every pill carries a risk. My own experience working in clinical settings taught me that no patient truly has the same reaction to medicine, but some patterns come up again and again.

The side effects most often mentioned with almitrine are felt by a wide range of people. The big ones to watch out for involve numbness or tingling in fingers and toes—what doctors call “peripheral neuropathy.” A large French study tracked thousands of patients on this medicine, and over 1 in 5 reported some kind of nerve discomfort. Some described burning pain, others felt their grip weaken. These symptoms don’t vanish in a day. Stopping the medicine might help, but nerves heal slowly.

Stomach problems come up too. The gut shows its protest as nausea or pain. I’ve seen patients complain of bloating or a drop in appetite. These symptoms often build up without warning.

Leg swelling crops up for some. Fluid builds up, especially if the drug is taken for many months. This swelling might look harmless at a glance, but it can spiral into bigger issues, especially for older adults, who already face risks from less active muscles and weaker veins.

Weight loss sneaks up on some users. Doctors believe this might connect to both nausea and nerve damage. Weight loss that comes with a drug tends to run under the radar until someone steps on the scale, only to find their pants fit looser than before.

Why Recognizing These Matters So Much

If we ignore these warning signs, people can end up worse off than where they started. Nerve pain doesn’t just make daily life tougher—it can set someone up for falls or injuries, especially in older adults. Stomach symptoms leave them less likely to keep eating or taking other medicines. Swelling in the legs can hide clots or heart trouble. These connections matter in real life, not just in hospital wards. I’ve met too many people who chalked up numb toes to old age, only to learn months later that their medicine played a role.

Fact-Based Steps Toward Solutions

Doctors who prescribe almitrine run regular checks for symptoms, looking for changes in nerve sensation and weight trends. Blood tests and foot exams become part of the routine. Education stands out as a key part: patients need to know the earliest signs, so no one gets caught off guard if a side effect appears.

Researchers urge doctors to use almitrine only when alternative choices run out. The drug doesn’t appear in most treatment protocols except for specific, tightly controlled scenarios. If side effects show up, doctors typically start with a lower dose or look at safer alternatives.

Finally, families need to keep close watch. Noticing a limp, a loss of appetite, mood dips, or complaints about numb toes could be the nudge that gets someone back to their doctor before small problems get bigger. Medicines like almitrine open possibilities for breathing and activity, but only if paired with careful eyes and honest reporting.

How should Almitrine Dimesylate be taken or administered?

Understanding What’s at Stake

Almitrine dimesylate gets prescribed to people who struggle with getting enough oxygen into their blood, mostly because their lungs don’t do the job well anymore. As someone who’s spent time with patients managing long-term respiratory conditions, I know small mistakes in how medicine is taken can create big problems. People trust their doctors, but health risks don’t take a break just because something is “prescribed.”

Taking Almitrine Dimesylate — How Patients Really Use It

Doctors usually ask people to swallow this drug as a tablet. No fancy gadgets. Just a pill and a glass of water. Missing a dose poses risks, and doubling up on pills to “catch up” pushes oxygen levels dangerously high. This sort of error can land someone in the hospital. Dosing schedules call for discipline, and for good reason. Almitrine sticks around in the body for hours, so timing and dose both keep people out of trouble.

Unlike some medicines, you don’t chew or split the pill unless a medical professional says it’s safe. Mixing things up—chewing or crushing—can affect how the medicine gets absorbed, and that’s not just an academic point. Every single person processes drugs at their own speed. As a result, sticking close to the dose and timing picked by the doctor makes a real difference for how well the drug helps and how often people run into bad side effects.

Watching Out for Trouble

Almitrine can put stress on nerves, sometimes making hands and feet tingle or go numb. There’s also a risk for liver problems, so folks on this medicine need lab tests. Skipping the check-ups lets complications sneak up unchecked, and that’s never good.

Alcohol can take a bad situation and make it worse. It’s tough to ask people to change habits, especially when they’re already dealing with a disease. Speaking from experience, thoughtful conversations beat lectures every time. One woman I know kept ending up in the emergency room with sick liver numbers—her effort only started making a difference once her care team explained risks in terms that connected with her day-to-day life.

Small Steps, Big Safety

A printed schedule taped to the fridge works better for most people than memory alone. Reminders help. Caregivers and family play a huge role, sometimes just by asking if someone took their dose at dinner.

Doctors and pharmacists share responsibility here, too. If instructions aren’t crystal clear, patients can’t follow them. I’ve seen more than one patient end up confused because their bottle said “take twice a day,” but they weren’t told if that meant every 12 hours or just morning and night. Clear language and easy-to-read printouts from the pharmacy give people a fighting chance to avoid mistakes.

The Value of Real-World Support

Staying safe with any medicine isn’t just about knowledge. Support at home, access to a reliable pharmacy, insurance that covers the full prescription—these things add up. I’ve learned the people who ask the most questions at the pharmacy window tend to do best, not just with almitrine but with any pill they pick up.

It comes down to trust. When doctors, nurses, pharmacists, and families work together to support people using almitrine dimesylate, there’s less guesswork and fewer dangerous slip-ups. That’s what counts most.

Are there any contraindications for using Almitrine Dimesylate?

What People Get Wrong About Almitrine Dimesylate

Almitrine dimesylate draws interest in respiratory therapy circles for its effects on improving oxygenation. Some believe it’s a miracle answer for chronic respiratory conditions. Still, no drug comes without real risks. The reality with almitrine dimesylate is both simple and important: certain health conditions make its use a real danger.

Key Contraindications That Shouldn’t Be Overlooked

Liver problems top the list. If you’ve ever coped with liver disease or serious hepatic impairment, this compound could harm more than help. The liver plays a central role in breaking down almitrine, so any dysfunction there may quickly escalate side effects. In clinical practice and in reports, severe liver injury led doctors to take almitrine off the table for some people.

Peripheral neuropathy stands as another major barrier. People dealing with nerve damage in their arms or legs, whether from diabetes or another cause, might see their symptoms worsen with this drug. Years of medical literature highlight that almitrine’s most reported side effect is peripheral neuropathy. Once that starts, it can take months to recover—if at all.

Careful Use Beyond the Obvious Cases

Severe pulmonary hypertension can slip under the radar as a contraindication, but it deserves attention. If you struggle with dangerously high blood pressure in your lungs, almitrine might make things worse. Increased pulmonary vascular resistance can tip someone into heart failure. Early clinical trials flagged this, and the warning remains relevant.

Not everyone realizes that cardiac conditions—especially right-sided heart failure—can clash badly with this therapy as well. This connects to the way almitrine works, shifting more blood to certain areas and putting extra load on the heart’s right side.

Drug Interactions and Individual Differences

Almitrine never works in a vacuum. It can interact with other drugs, including some that patients might take for breathing issues or heart health. For example, pairing it with other agents that affect the nervous system might amplify negative effects. Many patients depend on polypharmacy, so every new addition to the medication list adds risk. Doctors need to consider the whole person, not just isolated diagnoses.

Personal Experience and What Needs to Change

I saw a family member take almitrine as part of a clinical trial after years with severe COPD. For a few weeks, breathing seemed easier. But the improvement didn’t last. Over several months, numbness and tingling developed—in feet, then hands. There was confusion over which drug was causing it, so the therapy continued too long. Only when walking became difficult did the care team suspect nerve toxicity. Recovery was slow and incomplete.

This taught me the vital need for patient education and close monitoring. Too often, people think side effects are either trivial or unavoidable, especially when desperation for relief enters the picture. The reality: with new or rarely used medicines, early warning signs shouldn’t ever be dismissed.

Smarter and Safer Pathways Forward

Offering almitrine only after a thorough review of existing health conditions should be standard practice. Regular, honest follow-up visits protect patients from long-term harm. Monitoring liver function and neurological symptoms, not just once but throughout treatment, can catch early signs of trouble. Honest conversations between doctors, patients, and families set realistic expectations and help everyone act fast if things go wrong.

Can Almitrine Dimesylate interact with other medications?

Drawing from Everyday Experience

Most people don’t go through life thinking about the tiny chemical clashes happening inside their bodies. Yet, the moment your doctor hands over a prescription, especially one for a drug like almitrine dimesylate, that invisible game of interactions begins. Almitrine’s primary claim to fame sits in its ability to help people breathe easier, mainly by tweaking how oxygen travels in the lungs. But, like many specialized medicines, it rarely comes alone in a patient’s regimen.

How Interaction Happens

Doctors and pharmacists spend half their careers looking out for “drug-drug interactions.” One mistake can mean trouble ranging from a mild bellyache to a trip to the ER. For almitrine dimesylate, the scenario isn’t much different. Mixing it with medications that affect the liver or heart can bring surprises nobody needs. Research shows almitrine gets broken down in the liver by certain enzymes. Medications like antifungals (such as ketoconazole), some antibiotics, or even popular heart drugs can slow or speed this process up. Suddenly, too much almitrine floods your system, or worse, it disappears before it gets the job done.

Everyday Risks That Get Overlooked

Personal experience and the stories from friends and family have taught countless people that stacking medications multiplies risks. Imagine someone prescribed almitrine for chronic lung problems who is also taking drugs to control blood pressure. Some antihypertensives affect liver enzymes, changing how fast the body chews through almitrine. Reports in medical journals have described cases where mixing calcium channel blockers raises blood almitrine levels, putting extra strain on the heart.

Why Over-the-Counter Medications and Supplements Matter

People often load up on vitamins or herbal remedies thinking they’re harmless. Ginkgo and St. John’s Wort, for instance, have been shown to influence liver enzymes. Toss them into the mix with a prescription drug like almitrine, and results could become unpredictable.

Spotting Problems Before They Go Too Far

Side effects rarely announce themselves politely. Headaches, tingling, or unexpected swelling might sneak in and seem random. Truth is, some of these signs come from drug interactions. Anyone starting a new medication would gain from jotting down any new symptoms. It helps paint a clearer picture for the doctor, especially if that doctor isn’t the one who started the prescription in the first place.

What Can Actually Help?

Too often, people trust a single list of medications without updates. Bringing every pill bottle (including supplements) to appointments gives healthcare professionals the full story. Electronic health records make this easier, but nothing beats a straightforward conversation about every substance being taken. Pharmacists often spot problems that busy doctors might miss, especially when prescription lists grow long.

Listening to Professionals and Staying Informed

Trust in your healthcare team should extend to honesty about everything you take, even the items that don’t seem like medicine. Anyone prescribed almitrine dimesylate should ask questions—not just at the beginning, but at every appointment, especially before starting anything new. Professional guidance and staying aware give the best shot at avoiding those tiny chemical clashes no one wants to deal with in the first place.

Almitrine Dimesylate
Names
Preferred IUPAC name bis(methanesulfonic acid);2-[bis(4-fluorophenyl)methylidene]-N,N-dipropylhydrazinecarboxamide
Other names Almitrine mesilate
Almitrine dimethanesulfonate
Pronunciation /ælˈmaɪtriːn daɪˈmɛsɪleɪt/
Identifiers
CAS Number [29650-13-9]
Beilstein Reference 1614103
ChEBI CHEBI:31211
ChEMBL CHEMBL2106666
ChemSpider 5012175
DrugBank DB01430
ECHA InfoCard echa.infoCard=100.114.472
EC Number 85441-67-2
Gmelin Reference 401732
KEGG D02616
MeSH Dimephosphone
PubChem CID 6918492
RTECS number VN8575000
UNII IN8IA8J14X
UN number UN2811
Properties
Chemical formula C26H28F2N4O6S2
Molar mass 738.8 g/mol
Appearance White or almost white crystalline powder
Odor Odorless
Density 1.31 g/cm³
Solubility in water Slightly soluble in water
log P 2.8
Acidity (pKa) 6.7
Basicity (pKb) 8.3
Magnetic susceptibility (χ) -63.0×10⁻⁶ cm³/mol
Refractive index (nD) 1.513
Dipole moment 3.42 D
Thermochemistry
Std molar entropy (S⦵298) 412.5 J·mol⁻¹·K⁻¹
Std enthalpy of combustion (ΔcH⦵298) Std enthalpy of combustion (ΔcH⦵298) of Almitrine Dimesylate: **"-9792 kJ/mol"**
Pharmacology
ATC code R07AB06
Hazards
Main hazards Harmful if swallowed. Causes serious eye irritation. Causes skin irritation. May cause respiratory irritation.
GHS labelling GHS02, GHS07
Pictograms SGE, WSG, SGH
Signal word Warning
Hazard statements Hazard statements for Almitrine Dimesylate: "H302: Harmful if swallowed. H315: Causes skin irritation. H319: Causes serious eye irritation. H335: May cause respiratory irritation.
Precautionary statements P264, P270, P273, P301+P312, P330, P501
NFPA 704 (fire diamond) 2-3-1
Flash point > 252.3 °C
Autoignition temperature 250°C
Lethal dose or concentration LD50 oral rat 112 mg/kg
LD50 (median dose) LD50 (median dose): Mouse intravenous 30 mg/kg
NIOSH Not Listed
PEL (Permissible) Not established
REL (Recommended) 2-8°C
IDLH (Immediate danger) Not Established
Related compounds
Related compounds Almitrine
Almitrine bismesylate
Dimesylate
Mesylates