Alright, buddy, let’s break this down like we’re ripping apart a set of deadlifts.
We’ve got these things called Selective Androgen Receptor Modulators, or SARMs for short. They’re basically muscle-building compounds that latch onto androgen receptors, sort of like how you grip a barbell when you’re lifting.
Originally, they were being researched as possible solutions for some heavy hitters like cancer, osteoporosis, sexual issues, multiple sclerosis, Alzheimer’s, and muscle wasting – pretty serious stuff. But recently, these SARMs have started popping up in supplements that are being sold to people who are into fitness, just like us.
However, these things aren’t all protein shakes and post-workout recovery, my friend. SARMs have been seen to mess with your natural testosterone levels, play around with your cholesterol levels, and even tinker with how your liver functions.
Some gym rats have started taking different SARMs together, sort of like mixing up a crazy cocktail, and they’re doing it in cycles. In between these cycles, they’re practicing something called post-cycle therapy. This involves using SERMs, which are different kinds of compounds, to try and get their hormone balance back to normal.
But here’s the kicker, bro: pharmacists need to be on top of this SARMs business. They need to understand the not-so-great side effects so they can educate people about the potential risks. It’s kind of like a personal trainer needs to know what exercises can hurt their clients if not done correctly.
Now, pharmacists – those are the guys and gals that are the crucial link between the white coats and us, the patients. They gotta realize that folks might not be straight-up with them about everything they’re taking. SARMs, for instance, are gaining serious popularity as supplements that enhance performance. Why? Because they build lean muscle mass, cut fat, boost endurance, and help with recovery. Sounds like a magic potion, right?
Who’s popping these bad boys? Fitness junkies, bodybuilders, and those with jobs that are physically tough. But here’s the thing, SARMs got a red card from the sports world by the World Anti-Doping Agency in 2008. A few years later, in 2017, the FDA came out swinging, saying that these compounds were sneaking into bodybuilding products, and that they were upping the risk of serious stuff like heart attacks, strokes, and liver damage.
The Council for Responsible Nutrition, which is like the team captain for the supplement industry, put out guidelines suggesting that SARMs shouldn’t be in dietary supplements. Even the Department of Defense’s (DOD) chimed in, warning their military folks, healthcare providers, and civilians that SARMs might artificially lower natural testosterone and mess up liver function and cholesterol levels.
This recent study took a deep dive into dietary supplements sold online that were labeled as SARMs. They analyzed what was actually in these supplements versus what was on their labels. Out of 44 products tested, only about half actually had SARMs in them. Around 39% had some other drug that wasn’t approved, and 9% had no active compound at all. About 25% contained substances not listed on the label. Only 41% of the products had the amount of active compound that matched what was on the label, and in 59% of them, there was a big difference between what was listed and what was found. This tells us there’s a real issue with oversight and regulation, and raises big safety concerns.
Now, the hot-ticket SARMs out there right now include Ostarine (MK-2866), Ligandrol (LGD-4033), Testolone (RAD-140), and Andarine (GTx-007, S-4). Despite the buzz and the so-called safety of these compounds in the fitness world, there aren’t many studies actually looking at their effects, their potential dangers, and how they might interact with other drugs. Their long-term impact on our bodies is pretty much an unknown. The experience we do have with SARMs comes mostly from illegal use, not from clinical studies. Plus, in the fitness world, people are often taking SARMs in doses and for durations that exceed what’s been tested.
Right now, you can legally sell and buy SARMs that are marketed as “research chemicals”, which usually happens online. But it’s illegal to sell and buy those packaged in capsules for human consumption or labeled as dietary supplements. They can’t be marketed to the public as supplements, and no claims can be made about their benefits. Here, we’re gonna review what’s out there in the clinical literature to weigh up the pros and cons of using SARMs to up your game.
Nonsteroidal SARMs: Alternative to Androgenic-Anabolic Steroids
SARMs were discovered in the late ’90s, and they’re these performance-enhancing agents that turn up the volume on anabolism – that’s the process that increases muscle mass and strength – and help speed up recovery after your workout. They’re not anabolic steroids though, they’re synthetic ligands that hook onto androgen receptors.
Based on their chemical structure, they can act as full agonists, partial agonists, or antagonists. Think of them like workout buddies that either fully motivate you, sort of motivate you, or hold you back. Each SARM-androgen receptor combo has a different shape, and different tissues like muscles, bones, the prostate, brain, skin, and liver show different patterns of these receptor expressions.
What makes SARMs stand out is how they work selectively in tissues to promote anabolic activity. They’re seen as a pretty tempting alternative to anabolic-androgenic steroids, mostly because they come with fewer restrictions. Unlike their steroid pals, SARMs are easy for the body to absorb when taken orally. Plus, they exhibit less androgenic activity because they’re not broken down to dihydrotestosterone, or DHT, by an enzyme that’s present in high amounts in androgenic tissues. They also don’t get broken down to estrogen. All these factors combined give nonsteroidal SARMs an edge over their steroid counterparts.
Believe it or not, SARMs have shown a lot of promise as potential treatments for stuff like male contraception, osteoporosis, prostate cancer, sexual dysfunction, Alzheimer’s disease, muscle diseases, breast cancer, and muscle wasting conditions. A part of this is because people believe that SARMs are safer than anabolic steroids.
Now, for the recreational users – folks like us – they’re leveraging the different anabolic profiles of various SARMs to selectively bulk or cut. Bulking is when you’re in a phase to gain muscle, combining a diet designed for weight gain with heavy weight lifting. Cutting, on the other hand, is when you’re shedding fat, sticking to a strict weight-loss diet, doing aerobic exercises, and some lighter weight training. The word on the street is that different SARMs can give different results when it comes to bulking and cutting, which is why bodybuilders and fitness fans often use them together, or ‘stack’ them.
Ostarine/Enobosarm/GTx-024/MK-2866/S-22
Ostarine is this orally bioavailable, nonsteroidal SARM that was developed by Gtx, Inc. in the late ’90s. Its main goal was to help treat muscle wasting and osteoporosis. Among all SARMs, Ostarine is like the gym rat who’s always there – it’s the best clinically characterized SARM.
Clinical trials have looked at its potential for treating muscle loss seen with stress urinary incontinence, breast cancer, a type of lung cancer, and cancer-related muscle wasting. The trials thus far have shown a significant increase in total lean body mass, even in cancer patients. Some studies also saw a decrease in total fat mass without any change in total body weight.
But like any heavy workout, there can be side effects – common low-grade ones include headache, nausea, fatigue, and back pain. Other observed effects were a temporary spike in an enzyme called alanine transaminase, reductions in good cholesterol, blood glucose, insulin, and insulin resistance. The good news is, these issues typically return to normal after stopping treatment.
Now, if you cruise around personal blogs and commercial websites, you’ll find advice suggesting fitness and bodybuilding enthusiasts to supplement with ostarine at doses ranging from 10 mg to 30 mg for at least 12 weeks. These doses are like trying to lift ten times your weight – they’re 10 times higher than what’s been studied clinically. Word on the street suggests that taking ostarine at these high doses for this long can lead to lower testosterone levels. This can mean a lower sex drive, erectile dysfunction, infertility, muscle weakness, bone density loss, weight gain with more body fat, insomnia, and even depression.
There’s been some research into potential interactions between ostarine and certain drugs, like itraconazole, probenecid, celecoxib, and rosuvastatin, but there’s little evidence of any serious interactions.
Still, you’ll find some websites promoting SARMs that recommend ‘stacking’ them for better and different benefits. Whether taking higher doses of multiple SARMs over time can lead to adverse drug interactions is still a mystery, though.
Ligandrol/LGD-4033/VK5211
Let’s move on to Ligandrol, another orally available SARM. This bad boy was developed by Ligand Pharmaceuticals. There’s only been one clinical trial involving this power-lifter of a drug. In this trial, 76 healthy dudes were given either a placebo or 0.1 mg, 0.3 mg, or 1.0 mg of LGD-4033 daily for 3 weeks.
This powerhouse of a drug was well tolerated, with no major bad reactions. Various blood measures like hemoglobin, a prostate-specific antigen, aspartate aminotransferase, and alanine transaminase didn’t show any changes at any dose. At the highest dose, though, two hormones related to your fertility – follicle-stimulating hormone and free testosterone – were significantly suppressed. But don’t sweat, champ, these hormone levels went back to normal once the guys stopped the treatment.
Lean body mass increased depending on the dose, but there were no significant changes in fat or appendicular skeletal muscle mass. There were some improvements in strength and stair-climbing speed and power, but they were like trying to spot the difference between two almost identical barbell plates – not significant.
Total and bad cholesterol didn’t change much from baseline at any dose. Good cholesterol went up at the 0.3 and 1.0 mg doses, but returned to normal once the treatment stopped. Triglyceride levels, a type of fat in your blood, dropped from baseline at all doses. Most common side effects were a headache and dry mouth. In a recent case, a healthy 24-year-old guy showed signs of liver injury, and these symptoms popped up a week after he stopped the drug. This is a concern, as this type of liver damage is associated with androgenic anabolic steroids.
Online blogs are full of praises for Ligandrol, calling it a beast for performance enhancement, bulking up, muscle hardening, increasing vascularity, gaining size, and speeding up recovery. Fitness buffs are recommended to take between 5 mg and 10 mg daily for 6 to 10 weeks. But it’s worth noting that there’s a risk of testosterone suppression at doses greater than 10 mg. Just like ostarine, Ligandrol is often stacked with other SARMs for even greater gains. Side effects reported in the fitness and bodybuilding community include nausea, fatigue, headaches, and low libido, all of which might be due to lower testosterone levels.
Testolone/RAD-140
Testolone is a SARM that’s used mainly to tackle muscle wasting and breast cancer. This contender was brought to the stage by Radius Health, Inc. As of now, Testolone is still in its baby steps of first-stage clinical trials, and we’re all eagerly waiting for the results expected later this year. So, there’s not a ton of info on its safety yet.
That said, there’s one recent case report that’s worth paying attention to. It describes a pretty significant liver injury in a 49-year-old guy who had been taking Testolone. The amount he was taking wasn’t reported, but the signs pointed to some serious liver damage – there were increases in his bilirubin, AST, ALT, and creatinine levels, which are all markers for liver injury. When the docs took a look at his liver, they also found inflammation. But hey, don’t freak out – all his liver tests were back to normal 12 months after his initial visit.
Looking for some serious gains? Word on the street is that Testolone should be taken at 5 mg to 30 mg daily for 8 to 16 weeks for maxing out lean muscle mass and strength in the gym. There have also been some reports of side effects like sleeplessness and feeling wiped out. But remember, bro, that’s all anecdotal, so take it with a grain of salt.
Andarine/GTx-007/S-4
It’s time to talk about Andarine. As of now, there’s a gap in the weight rack because no human clinical studies have been done with this guy. But that doesn’t mean it’s not talked about in our iron paradise. On the web and in gyms everywhere, it’s known as a supplement that can get you shredded and pump up your muscle game.
Just a heads up, it’s seen as a bit of a lightweight compared to some of the other heavy-hitting SARMs, so it’s usually teamed up with others to get that sweet spot of performance. Pop 25 mg of Andarine daily, and it’s said to amp up your mood and overall wellness. Push that dose up to 50 mg per day, and you might see a modest jump in your strength, lean mass, and fat torching ability.
Got your eyes set on bulking up? Stack 50 mg of Andarine with 10 mg of Testolone every day for 8 to 12 weeks, and you could be flexing some serious muscle. If you’re chasing strength, try 50 mg of Andarine with 10 mg of Ligandrol daily for a 2 to 3-week cycle. For the guys wanting to cut, consider stacking 25 mg of it with 20 mg of Cardarine, which ain’t a SARM but a paroxisome proliferator-activated receptor-delta agonist, daily for a 12-week stretch.
But let’s say you want the best of both worlds – lose fat and gain muscle at the same time, right? Try stacking 50 mg of Andarine with 25 mg of Ostarine and 20 mg of Cardarine daily for 9 to 12 weeks.
But remember, every rep has its toll. The main side effects reported with Andarine include a change in vision, like seeing things with a yellow tint, and testosterone suppression.
SARMs and Postcycle Therapy
Now we’re going to dig into something important – post-cycle therapy, or PCT. Look, in the muscle world, we all understand that a few weeks of a SARM cycle can likely drop your testosterone levels. So, to keep those hard-earned gains, balance your hormones, and get your testosterone back to its prime levels, you need some downtime with PCT between your SARM cycles. This ain’t medical advice, just wisdom passed around in our iron sanctuary and on various online forums.
There are plenty of PCT options out there, each promising to naturally crank up your testosterone, keep estrogen in check, balance your cortisol, and give your liver a health boost. You’ll see a mix of ingredients in these guys, like the aromatase inhibitor arimistane, an anti-estrogen supplement, and D-aspartic acid or DAA. Then you have the prescription-grade stuff, Clomid and Nolvadex, which you might find online from overseas sources.
Clomid, or clomiphene citrate, is a selective estrogen receptor modulator, or SERM. It gives your testosterone production a kick and wards off ‘moobs’ or gynecomastia. If you’ve been on a heavy SARM cycle, Clomid’s your strongman PCT. But remember, every supplement has its price – Clomid’s known for side effects like mood swings, headaches, and vision changes at high dosages.
Nolvadex is a gentler SERM but works the same way. While there are PCT options with natural extracts and non-SERM ingredients that are theoretically safer than Clomid and Nolvadex, their effectiveness hasn’t been tested in the lab.
The gym gurus suggest starting PCT with a higher dosage when testosterone levels are at their lowest, then tapering down as levels get back to normal. Start your PCT the day after your SARM cycle ends, and keep it going for about 4 weeks. Remember though, the length and even the need for PCT can vary based on the strength and dose of the SARM you used.
Without solid scientific research, we can’t fully know the potential risks of cycling SARMs with PCT supplements.
Conclusion
SARMs, despite over 20 years of research, still don’t have the green light from the FDA. Not even for conditions where their benefits could outmuscle any significant risks. Most of what we know about their performance-enhancing benefits and overall safety is gym-talk, not hard scientific evidence. What we do know from the limited clinical studies is that there are some big health risks involved like heart attacks, strokes, and liver damage.
Those most likely to try SARMs for fun or to gain a performance edge are your fellow bodybuilders, fitness enthusiasts, or those in physically tough jobs like cops or firefighters. Beyond the stuff you can find online, there are also SARMs products like SARM-X and Osta-Plex available in some supplement stores.
Now, here’s where your friendly neighborhood pharmacist comes in. They have a duty to pump you full of knowledge about the potential health risks associated with SARMs use. They should dig deep to find out about all the supplements you’re taking, as you might not tell them everything or even know everything that’s in them. They need to remind you that supplements aren’t as tightly regulated as prescription drugs, so the quality and safety can be hit or miss. If you mention a health issue, it’s their job to be a detective and find all the possible causes. If your profile fits a typical SARMs user, or you’re having side effects that match those associated with SARMs or PCT, they should be on high alert for potential SARMs use.
Just remember, bro, this info is just for your knowledge. It’s not meant to replace professional advice. You’re responsible for any decisions you make based on this information.
REFERENCES
- The World Anti-Doping Agency: www.wada-ama.org/en/content/what-is-prohibited/search/Sarms.
- The FDA: www.fda.gov/news-events/fda-brief/fda-brief-fda-warns-against-using-sarms-body-building-products.
- The Council for Responsible Nutrition: www.crnusa.org/self-regulation/voluntary-guidelines-best-practices/crn-recommended-guidelines-sarms-containing.
- Operation Supplement Safety: www.opss.org/infographic/sarms-dietary-supplements.
- A study on the chemical composition and labeling of SARMs sold online: JAMA. 2017;318(20):2004-2010.
- A review of the best SARMs for sale in 2020: www.provhosp.org/best-sarms-for-sale/.
- A mini-review on SARMs: Open Access Journal of Reproductive System and Sexual Disorders. 2018;1(1).
- A warning about SARMs from the United States Antidoping Agency: www.usada.org/dietary-supplements/usada-supplement-groups-support-action-on-dangerous-sarms/.
- A study on SARMs and their clinical applications: Sex Med Rev. 2019;7: 84-94.
- A detailed overview of the discovery and therapeutic promise of SARMs: Mol Interv. 2005;5:173-188.
- A review of the best SARMs for bodybuilding: www.nfsmi.org/best-sarms/.
- An article on the best SARMs stacks: www.sciencescape.org/best-sarms-stacks/.
- A study on the effects of enobosarm on muscle wasting and physical function in cancer patients: Lancet Oncol. 2013;14:335-345.
- A study on drug-induced liver injury by SARMs: Hepatol Comm. 2020;4:450-452.
- A review of Testolone (RAD140): www.psychonomic-journals.org/testolone-rad140-review/.
- A review of Andarine (S4): www.psychonomic-journals.org/andarine-s4-review/.
- An article on post cycle therapy for SARMs: https://ishib.org/post-cycle-therapy/.
- A study on adverse effects of sports supplements in men: Aust Prescr. 2018;41:10-13.