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Anyone ever switch from ranitidine to U-gard pellets?

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  • #21
    It would be like taking a tums twice a day. It would buffer acid for about 2 hours, then the horse would go back to having pain when the acidic stomach contents contacted his ulcers.

    Comment


    • #22
      And I don't think there are any long-term unwanted side effects from ranitidine. It works by binding to parietal cells in place of histamine. It un-blocks (leaves the receptor) after 4-6 hours. It should really be given 3-4 times a day to be most efficacious. It really doesn't change any underlying physiology, other than correcting for abnormal effects of human-induced physiologic changes.

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      • Original Poster

        #23
        Originally posted by Lauren12 View Post
        And I don't think there are any long-term unwanted side effects from ranitidine. It works by binding to parietal cells in place of histamine. It un-blocks (leaves the receptor) after 4-6 hours. It should really be given 3-4 times a day to be most efficacious. It really doesn't change any underlying physiology, other than correcting for abnormal effects of human-induced physiologic changes.
        Thanks! I wonder if it would have any sort of desensitization in regards to binding? I guess that's kind of a rhetorical question, lol. He's been on it for probably 3-4 years continuously. The other lingering thought was--I only give it 2x/day (as per my previous vet/trainer). I don't think I could ever afford to give it 3x/day+ forever. However, doing it twice a day did improve his appetite issues and mellowed him out. I guess I will just keep him on it. Maybe one day they will come out with something else!
        Originally posted by rustbreeches
        [George Morris] doesn't always drink beer, but when he does, he prefers Dos Equis

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        • #24
          How much does your ranitidine cost you per month? I have one of my mares on twice a day compounded omeprazole powder, and it does SO much more than the ranitidine did. The compounded powder can be a little sketchy (may not contain the exact concentration of drug promised according to research), but it is the ONLY thing I have seen make positive changes for this horse on my limited budget. It's about $1 a day from Precision pharmacy.

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          • #25
            Lauren - is the compounded omeprazole powder buffered so the drug can work as intended, and not get degraded in the stomach?
            "If you think nobody cares about you, try missing a couple payments..."

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            • Original Poster

              #26
              Originally posted by Lauren12 View Post
              How much does your ranitidine cost you per month? I have one of my mares on twice a day compounded omeprazole powder, and it does SO much more than the ranitidine did. The compounded powder can be a little sketchy (may not contain the exact concentration of drug promised according to research), but it is the ONLY thing I have seen make positive changes for this horse on my limited budget. It's about $1 a day from Precision pharmacy.
              The ranitidine is $65.90/month from Smartpak. I also have to grind it up into individual doses and add one peppermint so he'll eat it (he's a picky eater), which is tedious. I did the omeprazole for a month, and saw no real difference at all.

              I've always been a bit cautious at the thought of long term PPI use since in humans it has shown decreased Ca and Mg absorption over time. I know horses =/ humans, but between the two drugs (and since he didn't show any difference when using omeprazole), I might as well just stick with the ranitidine.
              Originally posted by rustbreeches
              [George Morris] doesn't always drink beer, but when he does, he prefers Dos Equis

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              • #27
                SuckerForHorses: Are you talking about enteric coating?

                The compounded omeprazole is intended for use on ulcers located in the stomach, not in the hindgut. The enteric coating is only necessary if you want the medication to reach further in the GI tract than the stomach. Most horses have stomach ulcers, not hindgut ones, so the enteric coating not only isn't necessary, but isn't particularly efficacious in cases of stomach ulcers.

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                • #28
                  Originally posted by Lauren12 View Post
                  so the enteric coating not only isn't necessary, but isn't particularly efficacious in cases of stomach ulcers.
                  This is completely untrue.

                  The gastric acid in the stomach WILL degrade the omeprazole in the stomach, and the omeprazole must reach the hind gut in order to work properly. The omeprazole will ONLY work on stomach ulcers IF it can successfully make it through the stomach, and the only way to do that is to have an enteric coating or a buffered paste (like UlcerGard or GastroGard).
                  "If you think nobody cares about you, try missing a couple payments..."

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                  • #29
                    The enteric coating is only necessary if you want the medication to reach further in the GI tract than the stomach.
                    The hind gut is where its absorbed to work properly to treat ulcers, its not absorbed in the stomach to treat the stomach. So, technically, yes, you do want the omeprazole to reach further than the stomach, and in order to do that successfully, it needs an enteric coating or buffered paste.
                    "If you think nobody cares about you, try missing a couple payments..."

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                    • #30
                      Omeprazole is absorbed in the 1st part of the small intestine, not the "hindgut" (although anatomically I'm not certain where the "hindgut" begins as this term had not been coined when I studied vertebrate anatomy!) It does not work directly in the stomach like an antacid--needs to be absorbed first.

                      But omeprazole cannot survive an acid environment so it needs protection if there is still stomach acid hanging around. That can be done with buffers or enteric coating.
                      Click here before you buy.

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                      • #31
                        Originally posted by SuckerForHorses View Post
                        The hind gut is where its absorbed to work properly to treat ulcers, its not absorbed in the stomach to treat the stomach. So, technically, yes, you do want the omeprazole to reach further than the stomach, and in order to do that successfully, it needs an enteric coating or buffered paste.
                        This is incorrect, and makes no sense.

                        Hind Gut = large intestine. Hind gut ulcers and stomach ulcers are totally different entities. Hindgut ulcers are most commonly caused by improper and prolonged NSAID usage (which can ADDITIONALLY cause stomach ulcers), but can also be caused by carb overload and endotoxemia, among various other causes. They typically respond best to diet change. Stomach ulcers (in addition to NSAID use) can be caused by exercise and stress and a zillion other things.

                        To clarify: the STOMACH is at the BEGINNING of the intestinal tract, after the esophagus and before the small intestine. The HINDGUT is at the END of the digestive tract, before the rectum, but after the small intestine and cecum.

                        STOMACH ulcers do NOT need an enteric coating in order for them to work. The enteric coating is designed to RESIST stomach acid in order for the drug to move further down the intestinal tract in the intact form, in an effort to treat HINDGUT ulcers (which, incidentally, has not proven terribly efficacious because they are broken down long before they reach the hindgut).

                        In any form, omeprazole inhibits the H-K ATP-ase pumps on the parietal cells of the stomach by binding irreversibly - meaning once the proton pump is out, it's out for good. More omeprazole = more pumps irreversibly bound (dose dependence). All a buffer does is enable more omeprazole molecules to bind more effectively by marginally circumverting the effects of physiologic stomach acidity. The drug is not as efficacious in the stomach without a buffer, but does the job just the same. It's really just a rat race between how quickly the body can produce new H-K ATP-ase pumps and how many omeprazole molecules can be bound to active pumps to inhibit them.

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                        • #32
                          Laurie, you are quite wrong in this statement although you seem to be speaking the language.
                          Do your homework. Omeprazole does nothing for non-acid-induced ulcers. It is degraded by acid, hence the need to protect the naked drug so it can make it to the site of absorption, the duodenum.

                          STOMACH ulcers do NOT need an enteric coating in order for them to work. The enteric coating is designed to RESIST stomach acid in order for the drug to move further down the intestinal tract in the intact form, in an effort to treat HINDGUT ulcers (which, incidentally, has not proven terribly efficacious because they are broken down long before they reach the hindgut).
                          Click here before you buy.

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                          • #33
                            And the MOUTH is the beginning of the GI tract, not the stomach. But what do I know?
                            Click here before you buy.

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                            • #34
                              Originally posted by deltawave View Post
                              Laurie, you are quite wrong in this statement although you seem to be speaking the language.
                              Do your homework. Omeprazole does nothing for non-acid-induced ulcers. It is degraded by acid, hence the need to protect the naked drug so it can make it to the site of absorption, the duodenum.
                              Horses almost always get ulcers caused by stomach acid, so I'm not sure what you are talking about by "non-acid induced" ulcers. Are you talking about H. pylori? Horses do not get ulcers from H. pylori like humans do (and potentially small animals).

                              Omeprazole binds to H-K ATPase pumps in the STOMACH. The stomach is where parietal cells are located. That is where omeprazole works. It is NOT absorbed in duodenum, although it can have some receptor binding there if ulcers are present. GastroGuard does NOT have an enteric coating, because it works in the STOMACH. Gastroguard has a mild alkaline buffer, which as I said before, works by mildly circumventing the physiologic effects of stomach acidity. Do any of you have a Plumb's Veterinary Drug Handbook? You may want to consult that.

                              And again, deltawave, I mentioned the stomach is after the esophagus and before the small intestine. Last time I checked, the mouth was attached the esophagus. Sorry for simplifying.
                              Last edited by Lauren12; Dec. 7, 2012, 08:08 PM.

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                              • #35
                                OK, I'll break it down more simply.

                                1. By "non acid ulcers" I meant hindgut ulcers. Which omeprazole is NOT used to treat. So your contention that enteric coating on omeprazole is used to get omeprazole to the hindgut is incorrect on multiple levels.

                                2. Omeprazole binds to parietal cells VIA THE BLOOD STREAM, not via the lumen of the stomach. In order to ENTER THE BLOOD STREAM, it is ABSORBED IN THE DUODENUM. Fact. Your explanation is incorrect that omeprazole gets to parietal cells by way of direct gastric absorption or exposure. Look it up. Even wikipedia has it correct.

                                3. Gastroguard is buffered because without the buffer the drug would be degraded by the stomach acid, rendering it useless by the time it reaches the small intestine.

                                I don't have Plumb's Veterinary Drug Handbook, but I have a degree in medicine and a whole pile of pharmacology books on hand. You can be sure I'll be checking out Plumb, however, and if the misinformation you're posting comes from that source I'll be sure not to use it as a reference! Maybe re-read the chapter on pharmacodynamics of PPIs?
                                Last edited by deltawave; Dec. 7, 2012, 09:00 PM. Reason: too grumpy :p
                                Click here before you buy.

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                                • #36
                                  Deltawave - I believe I've already said that omeprazole is not efficacious for hindgut ulcers, in my previous post. I'll remind you that GastroGard is NOT enteric coated, and I am FULLY aware that the drug must be transported through the bloodstream (of the stomach) - one has to simplify to some degree on a BB. I'll also remind you that horses and humans are VERY, VERY different physiologically! Below is an excerpt from the NIH Drug Label site: http://dailymed.nlm.nih.gov/dailymed...5-409826d8fd66

                                  Clinical Pharmacology
                                  Mechanism of Action: Omeprazole is a gastric acid pump inhibitor that regulates the final step in hydrogen ion production and blocks gastric acid secretion regardless of the stimulus. Omeprazole irreversibly binds to the stomach gastric parietal cell's H+, K+ ATPase enzyme which pumps hydrogen ions into the lumen of the stomach in exchange for potassium ions. Since omeprazole accumulates in the cell cannaliculi and is irreversibly bound to the effect site, the plasma concentration at steady state is not directly related to the amount that is bound to the enzyme. The relationship between omeprazole mucosal absorption and plasma concentration is a function of the rate-limiting process of H+, K+ ATPase activity/turnover. Once all of the enzyme becomes bound, acid secretion resumes only after new H+, K+ ATPase is synthesized in the parietal cell (i.e., the rate of new enzyme synthesis exceeds the rate of inhibition).
                                  Pharmacodynamics: In a study of pharmacodynamic effects using horses with gastric cannulae, secretion of gastric acid was inhibited in horses given 4 mg omeprazole/kg/day. After the expected maximum suppression of gastric acid secretion was reached (5 days), the actual secretion of gastric acid was reduced by 99%, 95% and 90% at 8, 16, and 24 hours, respectively.
                                  Pharmacokinetics: In a pharmacokinetic study involving thirteen healthy, mixed breed horses (8 female, 5 male) receiving multiple doses of omeprazole paste (1.8 mg/lb once daily for fifteen days) in either a fed or fasted state, there was no evidence of drug accumulation in the plasma when comparing the extent of systemic exposure (AUC0-∞). When comparing the individual bioavailability data (AUC0-∞, Cmax, and Tmax measurements) across the study days, there was great inter- and intrasubject variability in the rate and extent of product absorption. Also, the extent of omeprazole absorption in horses was reduced by approximately 67% in the presence of food. This is evidenced by the observation that the mean AUC0-∞ values measured during the fifth day of omeprazole therapy when the animals were fasted for 24 hours was approximately three times greater than the AUC estimated after the first and fifteenth doses when the horses were fed hay ad libitum and sweet feed (grain) twice daily. Prandial status did not affect the rate of drug elimination. The terminal half-life estimates (N=38) ranged from approximately one-half to eight hours.

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                                  • #37
                                    It's great to simplify for clarity, but not if the simplification causes one to make statements that are factually wrong. For example:

                                    STOMACH ulcers do NOT need an enteric coating in order for them to work. The enteric coating is designed to RESIST stomach acid in order for the drug to move further down the intestinal tract in the intact form, in an effort to treat HINDGUT ulcers (which, incidentally, has not proven terribly efficacious because they are broken down long before they reach the hindgut).
                                    Once again, omeprazole is protected (either by buffering or enteric coating) in order to get the drug past the stomach and into the duodenum, where it is absorbed. It is not absorbed anyplace else. It is not protected in order to "move it along . . . to the hindgut". It is protected so it SURVIVES STOMACH TRANSIT. And this goes for humans and horses. Physiology of different species can indeed vary a lot, but not in this particular case. The citation you posted supports the facts as stated. Omeprazole is NOT active via direct contact with the gastric mucosa, CANNOT survive naked in an acid environment, and MUST be delivered to the duodenum intact (or given IV) in order for it to work.

                                    Small human studies indicate that blood levels of omeprazole rise sharply after a few days of steady dosing. Probably this means that suppression of acid production allows even more omeprazole to get to the duodenum, even if it's enteric coated. Since horses secrete acid non-stop, however, I'd take a lot of convincing that it is ever a smart idea to give naked omeprazole to a horse.
                                    Click here before you buy.

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                                    • Original Poster

                                      #38
                                      I should mention that it's likely that the compounded omeprazole powder formulations most likely have sodium bicarbonate as a buffer added to it to prevent gastric acid degredation, similar to the OTC human formulation, Zegerid. This is used as an alternative the enteric coating.
                                      Originally posted by rustbreeches
                                      [George Morris] doesn't always drink beer, but when he does, he prefers Dos Equis

                                      Comment


                                      • #39
                                        Here's a couple more articles: I'm not sure if y'all can get the full text, but at least the abstracts are there:


                                        http://www.ncbi.nlm.nih.gov.libproxy...ubmed/12387383
                                        http://www.ncbi.nlm.nih.gov.libproxy...ubmed/10696296
                                        http://www.scopus.com.libproxy.svm.l...+omeprazole%29

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                                        • #40
                                          I asked my gastroenterology buddy about this topic months ago (there is a thread on it somewhere, it got to be VERY long and detailed!) and he said mixing naked omeprazole with sodium bicarbonate was perfect for humans. Again, though, horses' capacity to secrete gastric acid is MUCH higher than ours.

                                          Lauren, you need a login to view those articles. Try PubMed, maybe? What do the articles say, in a nutshell?
                                          Click here before you buy.

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