CICO works (with help from Contrave)
I'm never doing a fad diet again. Over the course of the past 5 months, I've slowly, but surely, lost a little over 30 lbs. How? CICO and contrave.
Contrave has changed my life. I know that sounds a little dramatic, but it's true. I can't believe it took me so long to get started on it. I'd had an almost-full bottle (120 pills) that Mom let me have last year when I visited for Christmas. She had gotten them prescribed because she wanted to try them out, but couldn't tolerate the side effects (she said they made her really irritable 😒).
Anyway, I was curious but skeptical. Contrave contains bupropion (antidepressant) and naltrexone (opioid antagonist), and not a single stimulant - or anything else that's been well-studied for weight loss. I'm not one to bother with OTC diet pills (they're pretty much all the same anyway) because they're unregulated and unproven, but I have been on phentermine a few times. Unfortunately, phentermine treatment is limited to 12 weeks at a time, and the awesome appetite suppressant effects diminishes quite a bit after the first few weeks, anyway.
I had a general idea of how contrave could work (background info: I have a formal education in human anatomy & physiology, biochemistry, introductory pharmacology, and human pathophysiology):
1. Naltrexone blocks endogenous opioids from attaching to opiate receptors, an action which mediates a dopamine response (dopamine is fundamental to the brain's reward center and the development of addiction). By blocking these receptors, one could theoretically reduce or eliminate the biochemical process that reinforces addictive behavior. This has already been extensively researched as a treatment for alcoholism.
2. Bupropion is an NE (aka adrenaline) and dopamine reuptake inhibitor. This means that bupropion prevents the "stop" of NE and dopamine activity, which leads to a whole bunch of other effects. Bupropion is chemically related to amphetamines, which explains this effect on certain neurotransmitters, but it also stimulates the release of 2 other molecules, alpha MSH and AGRP, which are involved in a lot of autonomic processes in the body, including regulation of appetite and energy expenditure. Most research that exists has focused on the psychological effects of bupropion as it is normally used to treat depression and to help people quit smoking.
So here's the interesting part:
Those 2 other molecules that are stimulated by bupropion? They each play a vital role in explaining how bupropion could be effective for weight loss:
a) alpha MSH does a lot of things, including appetite reduction and increases in energy expenditure (metabolism). Theoretically then, you could take just bupropion for weight loss right? Well, no. Like nearly every physiological process in our bodies, the cells that release a-MSH have a self-limiting feature to stop the whole process from going on indefinitely. Otherwise, humans could run out of energy needed to live.
b) This limiting feature works because cells release AGRP at the same time as a-MSH. AGRP's only function is to attach back to the cell that released it. When enough AGRP has attached, a signal is sent inside the cell telling it to stop producing both a-MSH and AGRP.
This basically means that no matter how much bupropion you take, its weight loss effects are going to be limited by your body's natural processes.
So back to my point, how does contrave work, exactly? I've already explained how it can help reduce appetite and increases metabolism via release of a-MSH, and how this process is self-limited by the concurrent release of AGRP. Theoretically, if we could find a way to eliminate or block AGRP without affecting a-MSH, then the potential of bupropion for weight control could be significant.
Well, here's the kicker... AGRP IS A TYPE OF BETA ENDORPHIN!
It's an endogenous opioid! This means that the sites AGRP attach to on a cell can be blocked by naltrexone without limiting a-MSH!
FYI, I didn't know any of this stuff until this past weekend, when I basically gave myself a mini neurochemistry lesson using articles available on PubMed. And sorry, I didn't bookmark any of them to use as references here.
When I began contrave, I wasn't expecting much of anything. The bottle sat in my kitchen for a few months before I gave it a go, and even then it wasn't for weight loss. My psych was planning on possibly adding bupropion to my regimen anyway, so I figured I may as well try it out. Here's how things went:
Side effects are minimal due to the titration (slow increase) in dose that is prescribed to most people. The only thing I noticed was a short period of GI discomfort (nausea mostly) a few hours after taking a pill, but this stopped happening after about a week. It's probably due to the opioid receptors found in intestinal walls (something new I learned from my weekend of "research" lol) which affect intestinal motility. This is why opioids cause constipation, while opioid withdrawal produces nausea and diarrhea.
Price: you can go to the contrave website and get connected to a teledoctor who can write you a Rx (I used this service when I ran out of the bottle my mom had given me; consultation was $45). You can choose to have it sent to a local pharmacy, or use their preferred mail pharmacy, which charges $99 total to ship you a month's worth of medication. I chose this option because retail pharmacy prices are much higher. Total price: $144.00 first month, $99 monthly afterwards.
Insurance: most plans do not cover weight loss medications; mine certainly doesn't. The teledoctors they use also do not accept any insurance.
Regimen: you titrate up every week, starting with 1 pill/day during the first week (90mg bupropion+8mg naltrexone) until you get to 4 pills a day (360mg bupropion + 32mg naltrexone, all extended release).
Weight loss: at first, I had almost no faith that contrave would be effective for weight loss. I started off eating a 1200 cal/day (loosely tracked) and working out 1x a week. I'm still doing that, actually. I should also add that I used to crash diet a lot, often restricting myself to 500 cal a day, so I honestly didn't believe that staying under 1200 cal a day would actually do anything. Because of this irrational belief, I avoided the scale a lot. At some point - when I was up to 2-3 pills/day - I began to notice that I could go long periods of time without wanting or needing food. Even when I was physically hungry, eating felt like more of a chore. A few weeks after that started happening, some coworkers began commenting on my weight loss, which totally surprised me. I finally got the courage to weigh myself, and I was DOWN. 15. POUNDS. This all over the course of about 3 months.
Obviously, I was very encouraged by that, so I decided to continue with it. I'm basically doing the same now as I was then - 1200 cal/day (loosely) plus 1-2 days/week intense workouts (mostly CrossFit). It's now been 5 months and I'm down 32.6 lbs, to be exact.
Contrave has changed my life. It's like my brain has been reset; the damage done by all those years of starving and bingeing has been reversed. I have a normal relationship with food now: I eat when I'm hungry and stop when I'm satiated. I prepare nearly every meal I eat, which has eliminated almost all unhealthy, overprocessed foods from my diet. I'm trying to up my activity level, but I'm extremely busy with a full time job and another degree that I'm pursuing, leaving me pretty sleep-deprived during the weekdays. But weight loss is mostly diet, anyway.
I am more hopeful now than ever that I can achieve lasting weight loss. And the best part is that there's really no reason I can't be on contrave indefinitely, or for at least a few years. Bupropion is a medication that's already taken on a long term basis without issue. Naltrexone can damage the liver so it is typically not used long term; however, this effect has mostly been observed in people taking much higher doses of naltrexone (300mg+). Contrave contains a much smaller, extended release dose (32mg in 4 pills) that is even less than the dose used to treat alcoholism (50mg).
I'll update again when I remember to, lol. Hopefully I'll be down another 30 lbs 😁