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  • BDD Moderators: Keif’ Richards | negrogesic

A Question of The Opiates & Comparative Review of Various Opioids!

BlackWarGreymon

Greenlighter
Joined
Sep 16, 2015
Messages
22
Hello Everyone,


I have decided towrite a detailed comparison of opioids/opiates I have used for painrelief medically as well as side effects and dosage. I also have aquestion to ask concerning a switch of medication and would like toget other peoples opinions on this question particularly those whohave used the drugs in question. I appreciate all responses but Iwill only personally take into consideration those who actually havehad experience taking the medication.


My question concernsswitching from Hydrocodone/APAP 10mg/325mg to Codeine/APAP60mg/300mg. So from Norco to Tylenol 4. The question at hand is to dowith the affinity of Mu agonism of each drug. Hydrocodone ismetabolized into the active Norhydrocodone and Hydromorphonemetabolites. The metabolism to Hydromorphone from Hydrocodone is saidto be 5-6% from what I can find. Codeine is metabolized into theactive Codeine-6-Glucuronide and Morphine (Morphine-6-Glucuronide)metabolites. The Metabolism of Codeine to Morphine is said to be5-10% (10% being the acceptable rate in normal metabolisms)


According to myresearch Hydrocodone's metabolism to Hydromorphone is not the mainresponsible reason for its pain relief and effect profile. However Ibelieve this metabolism can play a minor role in added pain reliefand effects. Codeine's metabolism to Morphine is said to beresponsible for much of its pain relief and effect profile howeversome question this and say its the Codeine-6-Glucuronide that isresponsible. I think honestly its both, like Hydrocodone, however Ifeel Codeine's metabolism to Morphine is much more responsible forits effects. So now we get to the question at hand finally! So withthis knowledge at hand the effect of each drug is dependent upon howmuch of it reaches the blood and brain. I have taken into theconsiderations of equivalent exchange or conversion of each to matchan added equivalent dosage as follows:


100mg Codeine = 15mgHydrocodone


The above representsa crude conversion of Codeine to Hydrocodone orally. Now taking thisinto consideration lets introduce the bio-availability of theminor/major metabolites of the codones to morphones. I'm not going tofactor in Codeine-6-Glucuronide or Norhydrocodone since those are notthe target focus here. Instead I am focusing on Morphine andHydromorphone. So using the above conversion if I take 100mg ofCodeine I should get 5mg-10mg of Morphine. If I take 15mg HydrocodoneI should get 0.75mg-0.9mg of Hydromorphone.


Seeing howHydromorphone oral has a bio-availability of 30-35% and Morphine oralhas 20-40%, I have concluded a dosage of 15mg Morphine would be3mg-6mg (30% = 4.5mg) and 3.75mg Hydromorphone would be 1.1mg-1.3mg(4mg tablet = 1.2mg-1.4mg). Knowing the conversion is one thing onpaper but in real life its a lot different than that in myexperience.


Knowing that thebio-availability of Codeine is 90% and Hydrocodone is 70% - 80%, thiswould easily explain why these oral morphine derivatives are morepotent orally than either of parent compounds.


I have read a lot ofinformation on the net about varying degrees of bio-availability todose conversions from I.V. to Oral Routes and I think it really comesdown to the person. Every study I read it always seems to vary somuch there is really no general ideal factor in my opinion.


So my question hasto do with the agonism effects of the metabolized Morphine vsHydromorphone. Both are strong agonist at the Mu Receptor vsHydrocodone and Codeine metobolites being much weaker. So my questionis would going to Codeine give more pain relief and morphine likeeffects (stronger sedation, more complete pain relief) vs staying onHydrocodone? Would the Codeine 100mg or for this purpose 2 60mgtablets (120mg) of Codeine provide more pain relief and overallMorphine effects vs the Hydrocodone with minor Hydromorphone effects?To me its not so simple but I think honestly thinking long and hardon this taking 120mg of Codeine should be stronger for myself knowingthat I only take my medication as needed and not every day ormultiple times a day. I take pain medication because after so manysurgeries due to my acquired condition I have been told furthersurgery will result in further loss of my voice and airwaycollapse/failure resulting. I suffer from laryngotracheal stenonsisof all 3 levels of the airway and am fortunate to have a doctor whois willing to treat my pain!


Well anyone is freeto answer this or give their own experiences or recommendations!


I have also decidedto give a detailed report of my use of the following prescribedopioids/opiates. I have rated them based on 3 factors, the length ofduration of effects, the amount of pain analgesia it produced and theamount of therapeutic euphoric affect it provided as I believe thisis part of the pain mechanism as well. Any Opioid/Opiate should beused responsibly and when taken in the correct dosage for the use ofpain relief should not lead to addiction. Simply because you take apain medication daily does not mean one is addicted to it in myopinion. I also believe that tolerance can be kept in check if usingas needed. Chronic use would end up with slowly escalating thedosages over the years or opioid rotation approaches. I don't condonethe use of these drugs for pure recreational use or doctor shoppingbecause from my understanding its making it harder for everyone withreal pain issues to acquire relief. Yes I also will say I hear it alltoo often from a few doctors I been to over my life that thinkbecause you are on narcotic opioids pain killers your either a drugaddict or going to become one any second have not ever been in anyreal pain to understand why you take them.


Darvocet N-100
(100mgPropoxyphene/650APAP)


I have takenDarvocet for about a year when it was still on the market before theU.S. banned it due to heart issues and such. I found this opioid tobe very weak and while it did relieve some pain I usually had to takebetween 200mg-400mg. Yes this substance like all opioids does createthat sense of peace for those whom question its therapeutic euphoriceffect.


Dose: 1-2 100mgtablets per 4-6 hours
Pain Relief: 4
Duration: 5 hours
Euphoria: 5
Adverse Effects:When taking 400mg or 600mg (extreme dose NOT recommended) it causedmild to moderately noticeable numbness in the mouth and lips/facialarea not physical numbness but a sense of decreased feeling likeNovocaine wearing off.


Tramadol 50mg


One of thosestigmas; its a partial, no wait now its a full agonist opioid… YeahI don't buy the full agonist effect stated by packaging labelsperiod. To me this drug is very weak and I got no relief of pain andvery minor therapeutic euphoric effects. Its state its suppose to beequivalent to Codeine for pain relief, well I don't think so!


Dose: 1-2 50mgtablets per 6–8 hours
Pain Relief: 0
Duration: NullEffect
Euphoria: 1
Adverse Effects: Ihave taken up to 300mg to just see if it was too low a dosagecompared to the Hydrocodone I was to be alternating it with. I feltstill no effect at this dosage and I feel any higher would reach asafety hazard.


Tylenol 3
(Codeine Phosphate30mg/500mgAPAP)


I was prescribedthis for pain after a surgery on my airway many years ago. I foundthis drug to be unique in effect profile.


Dose: 2 tablets per4 hours
Pain Relief: 7
Duration: 5 hours
Euphoria: 8.5
Adverse Effects: Ihave taken up to 120mg of Codeine and found it produced intenseitching and an intense sedated warm relaxed state which it mentionsis due to histamine release and the general effect of Morphinecausing a relaxed state of warmth. I took this dose because I neededto get some rest and figured doubling the adult dosage of 60mg wouldnot be too dangerous considering I just been given I.V. Morphine inthe hospital a few days earlier and that the max dosage in 8 hours is120mg so I figured as long as I did not take anymore for 12 hours Iwould be fine. (I do NOT recommend this to Opioid/Opiate Naive)Yes Iwas young at this time so that is why I got 30mg not 60mg because itsmore common to get Tylenol 3 than Tylenol 4.


Norco/Lortab
(Hydrocodone10mg/325APAP)


The prototypical midrange class opioid! While Hydrocodone is said to be a weak agonist atthe MU receptor, I find it is an excellent pain killer and Ipersonally find it superior to Oxycodone while so many say it palesin comparison… I was prescribed this for my airway pain which seemsto work well!


Dose: 1-1.5 tabletsper 4-8 hours (AS NEED)
Pain Relief: 8
Duration: 5 Hours
Euphoria: 7.5
Adverse Effects: Ifind after consuming a 15mg dose it takes about 35 – 45 minutes towork on an empty stomach and sometimes up to an hour depending on howmuch I ate. It was not until I was on this medication I started tolook at taking it around or before meals vs after. I find it impactsthe strength a lot if taken 30 before or 4 hours after eating sodosing on a good schedule before meals is important because missing adose and eating means you may have to take a higher dose which is notgood! I find the max effect dosage for Hydrocodone to be 30mg.Anything higher is a pure waste for therapeutic effect of paincontrol. Compared to Codeine I feel this opioid causes less histaminerelease, less body warmth (a side effect of histamine release too)and not as much sedation. Euphoria effect is strong but fortherapeutic reasons I question if it is as strong as Codeine? Codeineis also said to not be effected by food intake both on duration andeffect. I wonder if this is really true?


Percocet
(Oxycodone10mg/325APAP)


Oxycodone is hailedall around as being the king of opioids in the codone class and Ithought wow this must be as strong as it gets, so I was expecting alot.. I was prescribed this due to escalating work hours and toalternate with Hydrocodone and as a possible replacement if it workedwell.


Dose: 1 tablet per4-6 hours
Pain Relief: 9
Duration: 4 hours
Euphoria: 6.5
Adverse Effects: Ifound being on Oxycodone long term was not good. I found that theeffects were not as good therapeutically at least not for myself.While I will say Oxycodone is about double the strength ofHydrocodone for myself at least in terms of pain relief, its thetolerance that builds rapidly. I also found that the duration ofeffect was rather short lived compared to Hydrocodone. It also had agreater incidence of causing me at dosing intervals of say 4 hoursthen another after 3.5 hours I found myself spacing off once. Itseems this is the nod everyone talks about but there is nothingeuphoric about it and its dangerous if this is the result of thisdrug long term… I find it also has strong kappa agonist effectssimilar to Butorphanol Tartrate. So that means in terms oftherapeutic euphoria it has limited use per dose. I found thatoverall Oxycodone controlled pain faster and stronger than anyprevious opioid, however it did not last long for me and the effectprofile of intense sedation, labored breathing, massive toleranceincrease and dysphoric mood make me place this opioid belowHydrocodone and Codeine. Max dose I once took was 20mg. I discussedthis with my doctor and switched back to Hydrocodone immediately.


Dilaudid
(Hydromorphone 2mg)


Hydromorphone I wasgiven in short supply after a major surgery I had which lasted hoursand was multiple procedures done at once. I found this opioid to bevery strong but not long lasting. Slight itching with lots ofrelaxation effects. Profile of effects generally identical toHydrocodone with minor Morphine sedation.


Dose: 1-2 tabletsper 6-8 hours
Pain Relief: 9
Euphoria: 8
Adverse Effects:NONE


Stadol NS
(ButorphanolTartrate 1mg Spray)


This was given to meonce for migraines due to taking Decadron long term. I tried it out afew times and this stuff is the best migraine medicine I have evertaken. Which is odd seeing how I normally would never use an opioidfor relief of a headache due to rebound effect such as withHydrocodone.


Dose: 1-2 sprays pernostril per 2-4 hours
Pain Relief: 10(migraine pain only)
Euphoria: 3
Adverse Effects: Badtaste in mouth and because its a partial mu and partial kappaagonist/full competitive antagonist at both receptor types, it causesa bad mood in therapeutic and super-therapeutic dosages.


Non Opioid PainKillers:


Decadron
(Dexamethasone 4mg)


I am usuallyprescribed this medication in conjunction with an opioid medicationfor pain due to the massive inflammation of tissue. This is no drugto want to take long term!


Dose: 2 tablets perday
Pain Relief: 10
Euphoria: It doescreate a euphoric effect somewhat but its mostly do to high releaseof adrenaline!
Adverse Effects: Alot of effects here including mood changes, weight gain, foodcravings, water retention, odd aches and pains, migraines, adrenalinesurges, trouble sleeping, immune system suppression.


Kratom
(Mitragyna Speciosa)


While Kratom mayhave opioid activity I did not find it had any real pain relievingeffects nor did it even create any additional opioid effects. I tookseveral strands of this plant even the EUI Gold and various othertypes from 3 separate companies and none produced any effectcomparable to even Darvocet!


Dose: Varied butfrom 4-16 grams ingested
Pain Relief: Null
Duration: 30 Minutes
Euphoria: Null
Adverse Effects:Taste so horrible I tried stuffing some in caplets and man it wasstill a chore to take all those too.. All I got was a feeling ofwarmth like an opioid but it faded after 30 minutes. I feel thisplant is just some phase in history… I don't recommend it forreplacement of a real opioid synthetic, semi-synthetic or natural!Like I always say, an opioid is an opioid is an opioid. Got it! Thereis no faking it! Is it possible what I got was not the substance itwas purported to be? Perhaps but I highly doubt it!
 
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