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[h=2]Oral steroids- Ways of Increasing Bioavailability[/h]
Unfortunately our oral steroids aren’t the only thing that grapefruit juice will have this effect on here is a direct copy of a list (even this is not complete) of things grapefruit juice will have the same effect on:
https://secure.pharmacytimes.com/lessons/200303-02.asp
Table 2. Potential Interactions Between Grapefruit Juice and CYP3A4 Substrates
Drug Class Drugs(s) with Significant Grapefruit Juice Interaction Drug(s) with Negligible Grapefruit Juice Interaction Findings with Significant Interaction Implications with Significant Interaction
Anti-arrhythmics Amiodarone Increases AUC by 50% and peak plasma concentration by 84%. Both PR and QRS intervals were not significantly altered and systolic arterial pressure decreased slightly.42 Watch for arrhythmias and toxicity.
Quinidine Delays absorption of quinidine and inhibits the metabolism of active metabolite.43 Clinical significance is unknown.
Anti-convulsant Carbamazepine Increases AUC, peak and trough concentrations by 40%.44 Watch for signs of toxicity such as dizziness, ataxia, drowsiness, nausea, vomiting, tremor, and agitation. Monitor blood levels.
Anti-depressant Sertraline Trazodone Nefazodone Clomipramine Increases plasma concentrations. Watch for increases in side effects.
Anti-histamine Fexofenadine Desloratadine May decrease oral absorption and blood levels by inhibiting the organic anion transporting polypeptide.24 Clinical significance is unknown.
Anti-hypertensive Carvedilol Increases bio-availability of a single dose by 16%. Clinical significance is unknown
Losartan May reduce the AUC of the major active metabolite. May reduce effectivness of losartan but further studies are needed to determine significance.
Anxiolytics & hypnotics Diazepam Midazolam Triazolam Buspirone Alprazolam Increased plasma concentrations. Watch for possible increase in sedation.
Caffeine Decreases caffeine clearance.45,46 Watch for possible increase in side effects such as nervousness or insomnia.
Calcium channel blockers Felodipine Nicardipine Nifedipine Nimodipine Isaradipine Verapamil Amlodipine Diltiazem Increased plasma concentrations.47 Watch for toxicity, such as flushing, headache,t achycardia, and hypotension.
Cortico-steroids Methylprednisolone, oral Prednisone Increased plasma concentrations. Consumption of large amounts of grapefruit juice may increase the risk of adverse effects.
Budesonide Increases ora absorption.l Watch for hypercorticism.
Estrogens Ethinyl estradiol Increased plasma concentration. Clinical significance is unknown.
HMG-CoA reductase inhibitors Atorvastatin Lovastatin Simvastatin Fluvastatin Pravastatin Increased plasma concentrations. Increased toxicity such as GI complaints and muscle pain.
Immune modulators (immuno-suppressants) Cyclosporine Increased plasma concentrations of cyclosporine.48 Watch for signs of toxicity such as hepatotoxicity, renal toxicity, and increased immunosuppression.
Tacrolimus Possible increases in plasma concentrations. Watch for signs of toxicity such as nephrotoxicity, and increased immunosuppression.
Macrolide antibiotics Erythromycin Increased plasma concentration. Clinical significance is unknown.
Protease inhibitors Ritonavir Nelfinavir Saquinavir Indinavir Amprenavir Increases plasma concentrations. Watch for possible increased side effects.
Others Sildenafil Increased bioavailability.49
AUC = area under the curve; PR = pulse rate; GI = gastrointestinal.
NOTE: This will increase the potential for side effects for serious medications from blood pressure lowering medications to mood stabilizers. It will also increase the potency of caffeine and the ED drugs Viagra and Cialis so something very important to keep in mind since Priapism can occur and while you may think it is funny to have an erection for longer than 4 hours it can cause serious nerve damage and be extremely painful. Also keep in mind liver toxicity so please remember to use ALA and NAC while attempting any of this.
And as usual for my writeups:
Now for the disclaimer: I am an MD, but I cannot and will not give medical advice. Any advice given is simply what I would do with the information I have on the situation, I do not pretend to have all the answers I am just a knowledgeable source who has done a LOT of research on many different topics. Any help I give directly or otherwise is just that, help from one person to another, if you want medical advice I ADVISE you as a PERSON who cares about other people to see your Doctor, as they will be able to perform the proper tests and deal with you face to face. It is unethical for me to think that I could help anyone without seeing them and I will not bend my rules no matter what the circumstances.
Some references for everyone since I have been better about posting them with my information these days, some of these were posted in the write up but I wanted to throw them on the end as well for easy reference:
http://www.sciencedirect.com/science...39128X9500008E
Metabolism of anabolic steroids in humans: synthesi... [Steroids. 1995] - PubMed - NCBI
https://secure.pharmacytimes.com/lessons/200303-02.asp
10. Enzymatic Reactions of Anabolic Steroids
Nutrition Journal | Full text | Medicinal importance of grapefruit juice and its interaction with various drugs
http://onlinelibrary.wiley.com/doi/1...C9179C1.d03t03
– Department of Medicine at Indiana University
Oral steroids- Ways of Increasing Bioavailability
Let’s start with the basics, this will help for anyone who wants to read about it more:
https://secure.pharmacytimes.com/lessons/200303-02.asp
Everyone knows that oral steroids are subjected to a ‘first-pass’ metabolism (first pass meaning before it reaches is a general term which refers to the metabolic reduction of a compound prior to reaching the general circulation). A lot of these metabolic reactions will take place in the liver and small intestine. The liver of course is known for being the drug metabolizing organ of the body but the enzymes are spread out throughout the body, not just with the liver.
Metabolic processes can lead to a deactivation and excretion, or the production of more potent metabolites. So metabolic transformation is not always a bad thing. For example, tamoxifen is converted into the vastly more potent compounds 4-hydroxytamoxifen and endoxifen, biologically-inactive prohormones are converted into active target hormones (Thank you Patrick Arnold for that discovery) and so on.
So knowing this, we know that orally taken steroids are subject to extensive first pass metabolism. Not only does this cause the bioavailability of the oral steroid to go down, but it always converts the active androgens to far weaker or inactive metabolites. This is where the science gets a little more complicated but it’s because of the names of what we will be talking about more than anything else. CYP3A4 (see what I mean) is mainly found in the liver, it is one of the most important enzymes involved in the metabolism of xenobiotics (any chemical which is found in an organism but which is not normally produced or expected to be present, like any sort of pharmaceuticals). CYP3A4 in the intestine plays an important role in the metabolism of certain drugs as well.
The next bit might go a little fast but I want to get this write up posted with as much information on the subject as possible.
So why are we talking about the CYP3A4 enzyme? Because CYP3A4-mediated first-pass hydroxylation tends to affect 17a-methylated and non-17a-methylated steroids in roughly the same manner, so CYP3A4 inhibitors also improve the bioavailability of most 'oral' androgens.
A comprehensive list of inhibitors can be found here:
– Department of Medicine at Indiana University
On this list is grapefruit juice, grapefruit juice contains Bergamottin which is a moderate inhibitor (it will increase the bioavailability and subsequently the circulating amount by anywhere from 20-40% as well as increase the clearance time (half life). This alone will help many of you who want to get the most out of your oral steroids. Keep in mind that this will also cause a harsher environment for your liver, so proper liver supports are not only a good idea but will also keep you healthy through all of this.
So how much should you drink? About 250ml (roughly 8 fl oz) or 1 small glass of grapefruit juice will have a lasting effect on the uptake of the orals you are taking. How long varies much like all the science I am pointing out but about 24 hours until you need to drink some more to get the effect, so basically before every time you take an oral take some grapefruit juice (or wash it down with some).
Want to up the stakes and increase the bioavailability even more? Well this can be done as well and relatively safely, take Cimetidine a stomach acid inhibitor (for acid reflux) also known as Tagamet, this is a weak inhibitor of the CYP3A4 enzyme and will increase your uptake on it’s own by about 10% and decrease the clearance time by 20-50%.
And for those of you who just want the cliff notes here is a list
Ways to increase bioavailability and clearance time of your oral steroids
- 250ml grapefruit juice (8 fl oz roughly) before or with your oral steroids will increase availability by 20-40%
- Cimetidine (Tagamet) will on its own increase the availability by about 10%
Want more, here is a list of other things that will do this as well:
– Department of Medicine at Indiana University
(same link as above)
Let’s start with the basics, this will help for anyone who wants to read about it more:
https://secure.pharmacytimes.com/lessons/200303-02.asp
Everyone knows that oral steroids are subjected to a ‘first-pass’ metabolism (first pass meaning before it reaches is a general term which refers to the metabolic reduction of a compound prior to reaching the general circulation). A lot of these metabolic reactions will take place in the liver and small intestine. The liver of course is known for being the drug metabolizing organ of the body but the enzymes are spread out throughout the body, not just with the liver.
Metabolic processes can lead to a deactivation and excretion, or the production of more potent metabolites. So metabolic transformation is not always a bad thing. For example, tamoxifen is converted into the vastly more potent compounds 4-hydroxytamoxifen and endoxifen, biologically-inactive prohormones are converted into active target hormones (Thank you Patrick Arnold for that discovery) and so on.
So knowing this, we know that orally taken steroids are subject to extensive first pass metabolism. Not only does this cause the bioavailability of the oral steroid to go down, but it always converts the active androgens to far weaker or inactive metabolites. This is where the science gets a little more complicated but it’s because of the names of what we will be talking about more than anything else. CYP3A4 (see what I mean) is mainly found in the liver, it is one of the most important enzymes involved in the metabolism of xenobiotics (any chemical which is found in an organism but which is not normally produced or expected to be present, like any sort of pharmaceuticals). CYP3A4 in the intestine plays an important role in the metabolism of certain drugs as well.
The next bit might go a little fast but I want to get this write up posted with as much information on the subject as possible.
So why are we talking about the CYP3A4 enzyme? Because CYP3A4-mediated first-pass hydroxylation tends to affect 17a-methylated and non-17a-methylated steroids in roughly the same manner, so CYP3A4 inhibitors also improve the bioavailability of most 'oral' androgens.
A comprehensive list of inhibitors can be found here:
– Department of Medicine at Indiana University
On this list is grapefruit juice, grapefruit juice contains Bergamottin which is a moderate inhibitor (it will increase the bioavailability and subsequently the circulating amount by anywhere from 20-40% as well as increase the clearance time (half life). This alone will help many of you who want to get the most out of your oral steroids. Keep in mind that this will also cause a harsher environment for your liver, so proper liver supports are not only a good idea but will also keep you healthy through all of this.
So how much should you drink? About 250ml (roughly 8 fl oz) or 1 small glass of grapefruit juice will have a lasting effect on the uptake of the orals you are taking. How long varies much like all the science I am pointing out but about 24 hours until you need to drink some more to get the effect, so basically before every time you take an oral take some grapefruit juice (or wash it down with some).
Want to up the stakes and increase the bioavailability even more? Well this can be done as well and relatively safely, take Cimetidine a stomach acid inhibitor (for acid reflux) also known as Tagamet, this is a weak inhibitor of the CYP3A4 enzyme and will increase your uptake on it’s own by about 10% and decrease the clearance time by 20-50%.
And for those of you who just want the cliff notes here is a list
Ways to increase bioavailability and clearance time of your oral steroids
- 250ml grapefruit juice (8 fl oz roughly) before or with your oral steroids will increase availability by 20-40%
- Cimetidine (Tagamet) will on its own increase the availability by about 10%
Want more, here is a list of other things that will do this as well:
– Department of Medicine at Indiana University
(same link as above)
Unfortunately our oral steroids aren’t the only thing that grapefruit juice will have this effect on here is a direct copy of a list (even this is not complete) of things grapefruit juice will have the same effect on:
https://secure.pharmacytimes.com/lessons/200303-02.asp
Table 2. Potential Interactions Between Grapefruit Juice and CYP3A4 Substrates
Drug Class Drugs(s) with Significant Grapefruit Juice Interaction Drug(s) with Negligible Grapefruit Juice Interaction Findings with Significant Interaction Implications with Significant Interaction
Anti-arrhythmics Amiodarone Increases AUC by 50% and peak plasma concentration by 84%. Both PR and QRS intervals were not significantly altered and systolic arterial pressure decreased slightly.42 Watch for arrhythmias and toxicity.
Quinidine Delays absorption of quinidine and inhibits the metabolism of active metabolite.43 Clinical significance is unknown.
Anti-convulsant Carbamazepine Increases AUC, peak and trough concentrations by 40%.44 Watch for signs of toxicity such as dizziness, ataxia, drowsiness, nausea, vomiting, tremor, and agitation. Monitor blood levels.
Anti-depressant Sertraline Trazodone Nefazodone Clomipramine Increases plasma concentrations. Watch for increases in side effects.
Anti-histamine Fexofenadine Desloratadine May decrease oral absorption and blood levels by inhibiting the organic anion transporting polypeptide.24 Clinical significance is unknown.
Anti-hypertensive Carvedilol Increases bio-availability of a single dose by 16%. Clinical significance is unknown
Losartan May reduce the AUC of the major active metabolite. May reduce effectivness of losartan but further studies are needed to determine significance.
Anxiolytics & hypnotics Diazepam Midazolam Triazolam Buspirone Alprazolam Increased plasma concentrations. Watch for possible increase in sedation.
Caffeine Decreases caffeine clearance.45,46 Watch for possible increase in side effects such as nervousness or insomnia.
Calcium channel blockers Felodipine Nicardipine Nifedipine Nimodipine Isaradipine Verapamil Amlodipine Diltiazem Increased plasma concentrations.47 Watch for toxicity, such as flushing, headache,t achycardia, and hypotension.
Cortico-steroids Methylprednisolone, oral Prednisone Increased plasma concentrations. Consumption of large amounts of grapefruit juice may increase the risk of adverse effects.
Budesonide Increases ora absorption.l Watch for hypercorticism.
Estrogens Ethinyl estradiol Increased plasma concentration. Clinical significance is unknown.
HMG-CoA reductase inhibitors Atorvastatin Lovastatin Simvastatin Fluvastatin Pravastatin Increased plasma concentrations. Increased toxicity such as GI complaints and muscle pain.
Immune modulators (immuno-suppressants) Cyclosporine Increased plasma concentrations of cyclosporine.48 Watch for signs of toxicity such as hepatotoxicity, renal toxicity, and increased immunosuppression.
Tacrolimus Possible increases in plasma concentrations. Watch for signs of toxicity such as nephrotoxicity, and increased immunosuppression.
Macrolide antibiotics Erythromycin Increased plasma concentration. Clinical significance is unknown.
Protease inhibitors Ritonavir Nelfinavir Saquinavir Indinavir Amprenavir Increases plasma concentrations. Watch for possible increased side effects.
Others Sildenafil Increased bioavailability.49
AUC = area under the curve; PR = pulse rate; GI = gastrointestinal.
NOTE: This will increase the potential for side effects for serious medications from blood pressure lowering medications to mood stabilizers. It will also increase the potency of caffeine and the ED drugs Viagra and Cialis so something very important to keep in mind since Priapism can occur and while you may think it is funny to have an erection for longer than 4 hours it can cause serious nerve damage and be extremely painful. Also keep in mind liver toxicity so please remember to use ALA and NAC while attempting any of this.
And as usual for my writeups:
Now for the disclaimer: I am an MD, but I cannot and will not give medical advice. Any advice given is simply what I would do with the information I have on the situation, I do not pretend to have all the answers I am just a knowledgeable source who has done a LOT of research on many different topics. Any help I give directly or otherwise is just that, help from one person to another, if you want medical advice I ADVISE you as a PERSON who cares about other people to see your Doctor, as they will be able to perform the proper tests and deal with you face to face. It is unethical for me to think that I could help anyone without seeing them and I will not bend my rules no matter what the circumstances.
Some references for everyone since I have been better about posting them with my information these days, some of these were posted in the write up but I wanted to throw them on the end as well for easy reference:
http://www.sciencedirect.com/science...39128X9500008E
Metabolism of anabolic steroids in humans: synthesi... [Steroids. 1995] - PubMed - NCBI
https://secure.pharmacytimes.com/lessons/200303-02.asp
10. Enzymatic Reactions of Anabolic Steroids
Nutrition Journal | Full text | Medicinal importance of grapefruit juice and its interaction with various drugs
http://onlinelibrary.wiley.com/doi/1...C9179C1.d03t03
– Department of Medicine at Indiana University
