posted
I want to know if anyone has seen any research on this.
I've seen it said over and over on this site and others that Mepron is best absorbed when taken with a meal with a high fat content.
But the actual insert that comes with Mepron doesn't actually say that. What it does say is:
Administering atovaquone with food enhances its absorption by approximately 2 fold. In one study, 16 healthy volunteers received a single dose of 750 mg MEPRON Suspension after an overnight fast and following a standard breakfast -23 g fat: 610 kCal-.
So I would interpret this as a standard meal vs an empty stomach. There is no more emphasis on fat content than the 610Kcal. No where does it say that Mepron particularly binds with fat.
Maybe it's more the size of the meal that matters than the amount of fat [23 grams is a LOT].
Can anyone shed light on this?
James
Below is the full section on Mepron and absorption.
Pharmacokinetics
Absorption: Atovaquone is a highly li pophilic compound with low aqueous solubility. The bioavailability of atovaquone is highly dependent on formulation and diet. The suspension formulation provides an approximately 2-fold increase in atovaquone bioavailability in the fasting or fed state compared to the previously marketed tablet formulation. The absolute bioavailability of a 750-mg dose of MEPRON Suspension administered under fed conditions in 9 HIV-infected [CD4 > 100 cells/mm3] volunteers was 47% � 15%. In the same study, the bioavailability of a 750-mg dose of the previously marketed tablet formulation was 23% � 11%.
Administering atovaquone with food enhances its absorption by approximately 2 fold. In one study, 16 healthy volunteers received a single dose of 750 mg MEPRON Suspension after an overnight fast and following a standard breakfast [23 g fat: 610 kCal]. The mean [� SD] area under the concentration-time curve [AUC] values were 324 � 115 and 801 � 320 hr*mcg/mL under fasting and fed conditions, respectively, representing a 2.6 � 1.0-fold increase. The effect of food [23 g fat: 400 kCal] on plasma atovaquone concentrations was also evaluated in a multiple-dose, randomized, crossover study in 19 HIV-infected volunteers [CD4 < 200 cells/mm3] receiving daily doses of 500 mg MEPRON Suspension. AUC was 280 � 114 hr*mcg/mL when atovaquone was administered with food as compared to 169 � 77 hr*mcg/mL under fasting conditions. Maximum plasma atovaquone concentration [Cmax] was 15.1 � 6.1 and 8.8 � 3.7 mcg/mL when atovaquone was administered with food and under fasting conditions, respectively.
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Hoosiers51
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There have been studies done on it. This paragraph from www.drugs.com lists two of them.
I found this by clicking the Interactions Checker on drugs.com, and then when you scroll down, you see the "food-drug" interactions. That is a great way to see if any of your meds need to be taken with food, or without calcium, etc.
But otherwise, your pharmacy should have put one of those stickers on the box your Mepron bottle came in, or on the bottle itself, that says, "Take with a fatty meal" You know how they have those little stickers with important tidbits?
Here is the info from drugs.com:
"Interactions between your selected drugs and food
Moderate Drug-Food Interaction atovaquone (Moderate Drug-Food) ADJUST DOSING INTERVAL: Food, particularly high-fat food, significantly enhances the oral absorption and bioavailability of atovaquone. In 16 healthy volunteers, administration of a single 750 mg dose of atovaquone suspension following a standard breakfast (23 g fat: 610 kCal) resulted in an approximately 3.4-fold increase in the mean peak plasma concentration (Cmax) and a 2.5-fold increase in the mean area under the plasma concentration-time curve (AUC) of atovaquone compared to administration following an overnight fast. In a study consisting of 19 HIV-infected volunteers receiving atovaquone suspension 500 mg/day, Cmax and AUC of atovaquone increased by 72% and 66%, respectively, in the fed state relative to the fasting state.
MANAGEMENT: To ensure maximal oral absorption, atovaquone products (suspension, tablet, or in combination with proguanil) should be administered with a meal or milky drink at the same time(s) each day. Because plasma atovaquone concentrations have been shown to correlate with the likelihood of successful treatment and in some cases, survival, alternative therapies may be appropriate for patients who have difficulty taking atovaquone with food."
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Hoosiers51
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Okay, I see that what you actually posted has similar numbers. I didn't read it before I posted. But read what I posted, because it says it more in plain English. I actually understood what I posted, and what you posted is more confusing because it's using medical abbreviations that I don't know.
The first study mentioned is where the "23 g of fat" comes from, that you hear people referring to.
So if you do that, you're getting 3.4 TIMES more out of the Mepron. That is HUGE.
What I would like to know is how much that 3.4 drops off when the levels of fat go down, like say 17 grams, 13 grams, 7 grams, etc.
I'm guessing you'll still be getting a lot out of the Mepron even if your meal has 16 or 17 grams. I at least goal for that, if 23 is unrealistic.
Then in the HIV study, they had 72% greater concentration than without food.
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springshowers
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I also read somewhere and can not find it that the 23 grams of fat rule was for an older version of Mepron and they have changed it somehow now to not need as much.. Hence the full stomach as opposed to empty but no mention of 23 grams. I do not know now where I read that and if it is true either.
Maybe a clue to look into?
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Hoosiers51
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Did you guys read the two long paragraphs I posted? 23 grams of fat is the amount used in the study with the 16 healthy participants. It resulted in 3.4 TIMES the amount of Mepron concentration.
The second study mentioned in that same paragraph was among people immunocompromised with HIV.
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Hoosiers51
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springshowers,
I might have misread what you are saying.
There were problems with the old Mepron tablets that they had, and the problems were that it wasn't well-absorbed, and the absorption was very finicky among different people, or it would absorb at different times.
With the suspension, they did not have those problems. That is why you can't get the tablets in the US anymore.
BUT....if you read what I posted, it says "atovaquone suspension" which is the liquid form of Mepron that we take. Suspension=a solid suspended in a liquid. (that's why Mepron is so thick). I'm assuming it is not water-soluble (like salt or sugar), so they just really blended the heck out of it, or maybe they add some chemical to keep it "suspended" in the liquid.
So the 23 grams of fat came from a study using our version of Mepron.
Unless they had two different liquid versions. In that case, I would have though they'd add some kind of suffix to it, like "Mepron XR" so people would know if they were getting the good or bad stuff.
But I do know the liquid (suspension) is absorbed better than the tablets were.
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springshowers
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H51
Yeah that must have been it. Your right. It must have been that old tablet form. So the studies showing the liquid suspension and the 23 grams is what you posted and is most current.
And I was just not sure is all.. either.. And you clarified it >> Thanks.
I tried making sure I got 23 grams but it is near impossible without some substantial weight gain and nausea that kills.
So for me so I do make sure I ate and add something like olive oil or omega 3 oil supplements or such.
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You didn't read my first post. It DOESN'T SPECIFICALLY CREDIT FAT CONTENT AS THE REASON FOR BETTER ABSORPTION.
It simply mentions that the MEAL the volunteers ate had 23g of fat and 610Kcal. It doesn't say FAT per se is important, just that a meal is better than a fast.
Read it carefully. No specific reference to fat.
So again, why does everyone think it's fat that's important?
I do not see a reference to fat specifically. Maybe you only need a 610Kcal meal and fat is not that important.
It does NOT say "take with 23g of fat" anywhere that I can find.
James
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MariaA
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I'm pretty sure I read that there was a separate study that looked at fat. I would have found that in Schaller's book on babesia, which tends to cite references, I just can't look it up right now.
I think also that Mepron absorption varies drastically among different patients, which is why some LLMD's like Burrascano recommended testing Mepron levels iwth a blood test, to see if you needed to adjust dosing. So if one of us needs 23 grams, another might absorb it with less, so I doubt a study has really said that 'absorption decreases x percent with x reduction in the fat'
-------------------- Symptom Free!!! Thank you all!!!!
Hoosiers51
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posted
James,
Sorry, I must have misread what you were asking.
I want to say there had to be some kind of correlation with the "fat" issue, because doctors also say to avoid taking it with fat soluble vitamins, like Vitamin E, or fat soluble supplements like CoQ10.
Singleton is the one that has written about that in his book, so I will check the book and see if he references any studies, on the page that he says the fat soluble supplements need to be avoided.
I find it hard to believe they would say that about the vitamins/supplements without knowing that these substances decrease atovaquone concentration. But maybe I'm giving them too much credit.
But, there are a small number of LLMD's that do let their patients take milk thistle with Mepron, regardless of the so-called warnings out there about absorption....so maybe they know that no such studies exist. Dunno.
Now I'm just reading Momfromtexas' post, and that does seem to indicate there were other studies showing specifically that fat was a factor.
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Hoosiers51
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Also, I downloaded the file that Momfromtexas pulled that quote from, and after that quote, they have (9, 26, 102). Which means if you look at the "References" section on pages 8-11 of that document, you will see 3 studies (numbered #9, #26, #102) of where the info for that quote came from.
So if you are really interested, you could try to find those 3 studies online, or through a medical student or doctor you know that has free access to some of those published articles from those online medical databases.
They could be on PubMed, dunno. You'd just have to google it.
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