An Overview of the Effects and Pharmacology of the Opioid Drugs

Discussion in 'Opiates' started by etkearne, Jun 7, 2011.

  1. etkearne

    etkearne Resident Pharmacologist

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    Hi. I find many questions asked in this sub-forum pertaining to things such as "What does [insert opioid] make you act like?" or "What dose is good for [opioid] if I don't have any tolerance?"

    Well, I think that I will start a post that will be a bit like an encyclopedia for opioids. Unlike a purely academic venture, I will also include subjective effects and my own thoughts. More importantly, various users (no pun intended) can chime in on their Opioid of Choice to expand on my base information. So here it goes:

    Codeine: 60mg Codeine (orally) ~ 5mg Hydrocodone (Vicodin), brand names include Tylenol #3, Purple Drank, and others.

    This drug is a true opiate, right from the opium poppy. It is a common opioid for mild pain relief. It is actually the first opioid I ever encountered, from a prescription for a cough syrup as a 12- year-old.

    The way Codeine works is tricky. Codeine itself is a negligably weak opioid agonist (agonist: a drug that excites a neuro-receptor). The way it works, is that when taken orally, it is absorbed in the gut, and passed through the liver. In the liver, an enzyme actually transforms some of the Codeine into Morphine (a much more powerful opioid agonist). That is where Codeine gets it's umph. An immediate consequence of this is that it is best taken orally. Insufflation (snorting) will not produce much of an effect.

    Morphine: 5mg Morphine Sulphate (orally) ~ 5mg Hydrocodone, brands include MS Contin, Kadian, or just plain "M.S.". It is also a direct product from the opium poppy, and thus a true opiate.

    Morphine is indicated for moderate to moderately severe pain. The key to morphine is that it has a crappy oral bioavailability. So only around 20-30% of what you put into your mouth ever makes it to the blood-stream. So, that is why oral Morphine is often not prescribed (the doses can be in the 100's of milligrams for tolerant patients).

    This drug is dangerous and can easily kill a person not used to opioids. I would not suggest taking more than 25mg orally if you are not used to opioids. In hospital settings, morphine is much more useful, because it can simply be injected into the bloodstream, with a full, 100% bioavailability. Thus 5mg of injected Morphine is equal to wayyy more than 5mg of oral Hydrocodone. It is also common to insufflate and administer anally (into the rectum). Some squeamish homo-phobes are absolutely horrified about "plugging" Morphine, but, it really does increase bioavailability greatly.

    Hydrocodone: 5mg Hydrocodone orally = 5mg Hydrocodone orally (duh). Brands include Vicodin, Lortab, and Norco (all of which combine HC with Acetaminophen). There is also cough syrup preps. available.

    This drug is the most widely prescribed pharmaceutical in America. It is a perfect fit for moderate pain relief (especially for post-minor-surgery recovery). It is not particularly strong, so it is a good opioid to start using if you want to try an opioid.

    But, there is a catch! All common HC preparations compound it with Acetaminophen (Tylenol) or another OTC painkiller. This makes taking high doses of HC very dangerous. One's liver can be permanantly damaged by as little as 4,000mg of Acetaminophen taken in one day. So for Vicodin, which contains between 325 and 625mg Acet. per 5-10mg HC, you should not exceed 3,000mg of Acet. in one day IMO. That means, for regular 5mg HC/ 500mg Acet. Vicodin, that 6 pills is the daily limit. So, you can get 30mg of Hydrocodone into your system. For novices, this is a perfectly good high (it is actually a strong one and likely would make you vomit- start HC doses at 12.5mg or so), but for people tolerant to opioids, it precludes its use completely.

    The same caveat is involved with Lortabs or Norcos. They just contain different amounts of Acet. The "best" HC preparation for the opioid-tolerant is the Norco. All Norcos (including the 10mg HC pill) only contain 325mg Acetaminophen. So, that means that 10 pills (yes, 100mg HC) can be taken in one day, safely.

    So, please, proceed with caution with this stuff. The high is considered superior to other opioids by some (even seasoned users), due to its heavy body load and propensity towards nodding-out (something I'll explain later on...).

    Oxycodone: 3mg Oxycodone (oral) ~ 5mg Hydrocodone (oral), brands include Percocet (OC mixed with Acetaminophen), Roxycodone (Immediate release OC), and OxyContin (extended-release OC).

    This drug is notorious in the USA for being abused. Although only slightly stronger than Hydrocodone, it is NOT compounded with Acetaminophen in many cases (like Roxycodone or OxyContin). Thus, very high doses of "Pure Opioid" can be taken without risk of liver toxicity from the Acet.

    This, however, should ring some warning bells. One can EASILY O/D on this stuff if they don't know the proper dose. I have given the opinion so far that a novice should not take more than the equivalent of 30mg of Hydrocodone at once. That means, take no more than 20mg of OC if you aren't familiar with opioids. EVEN THIS dose can cause vomiting and a very bad time. I suggest starting with 10mg of Oxycodone. Seriously. You will likely have a great experience (or relieve pain adequately) on that dose if you are not used to opioids.

    Up until a year ago, OxyContin (which comes in doses as high as 80mg!!- they used to have a 160mg too...) could be easily crushed with a credit-card, then injected or insufflated. It was a drug-abuser's dream come true. But, last year, they remade the pill so that it gels-up when you try to crush it. Various methods can circumvent this, but I am a harm-reductionist, not a drug-abuse-advocate, so you can look that up somewhere ELSE.

    This is a hard-core opioid (if you want to call things 'hard-core') and I would caution its use by novices. Codeine or Hydrocodone are a better bet, but, if you really want to use Oxy, take ONE 10mg Percocet or cut a 15mg Roxycodone in half, and take that.

    The high is generally more lucid than HC or Morphine. You can take higher doses and function better. This is very good for pain patients, but some abusers dislike this. I personally like Oxycodone more than HC, Codeine, or Morphine. But, others will disagree.

    Fentanyl: 50 MICROgrams of Fentanyl ~ 5mg (oral) Hydrocodone, Brand names include Duragesic (extended release transdermal patch), Actiq and Fentora (immediate release high-dose buccal [mouth lining] lozenges).

    I spent some time trying to think of which opioid to add to the list next. I was tempted to continue adding opioids in terms of strength, which would have seen something like Hydromorphone next. But, since this is a harm-reduction thread as well as an informative one, I chose Fentanyl. The reason is that this is one of the most dangerous pharmaceutical agents known to man-kind and, unfortunately, is also readily available, and sadly leads to many overdoses in opioid abusers, even in the opioid-tolerant.

    Note that to get the buzz of a 5mg Hydrocodone, only 50 mcg (that is 0.050milligrams) of Fentanyl is needed. Now. Actiq, a common immediate release Fentanyl product comes in strengths varying from 200mcg to 1600mcg. So, even if you get your hands on the WEAKEST Actiq product, it is equivalent to 20mg of Hydrocodone- enough to make you throw up for hours if you aren't tolerant. But, if you are 'unlucky', and take the 1600mcg Actiq, you are essentially taking 160mg of Hydrocodone AT ONCE. That has a good chance of killing you, even if you have a bit of an opioid tolerance. You have to be used to taking MASSIVE amounts of opioids for at least 6 months or more to even think about messing with Fentanyl.

    There is almost NOTHING I can write that would condone recreational use of this drug. It is notorious for causing unpleasant side effects even in the most hard-core opioid users, and is generally passed up when it comes to recreational use. However, if you are a chronic pain patient, CONSIDER USING this drug if your current regimen is not helping enough. This drug could, potentially, give you the pain relief that is right up your alley.

    That is all I am writing about Fentanyl. Simply put: If you are trying to get high, and haven't been ADDICTED to opioids for some time, don't even mess with it.

    Hydromorphone: 1.5mg (oral) Hydromorphone ~ 5mg (oral) Hydrocodone, brands include Dilaudid and is known as "Dillies". It is used out-patient in moderately severe pain relief and in the hospital both orally and intravenously for surgical pain relief and palliative care.

    Unlike Fentanyl, this drug is commonly used by recreational users and pain patients alike. It is most commonly encountered in 2,4, and 8mg oral tablets in the USA. They are immediate release and used mainly for breakthrough pain relief. Doing the math, an 8mg HM tablet ~ 32mg Hydrocodone. So, this drug is dangerous, but less likely to cause accidental O/D's compared with Fentanyl. It was very popular in the past decade, but now, OxyContin has almost completely taken over its place in recreational use.

    The reason is that HM is poorly absorbed orally. It has a low oral bioavailability. However, it is 5 times more potent if given IV and 3 times as potent if "plugged". So, recreational users often use this drug in IV form as a substitute to heroin. This is dangerous because of the fillers in the pills, which can cause infectious problems if they are not filtered out prior to injection. Plugging is less prone to danger, but the risk of O/D is heightened due to the higher bioavailability. Keep this in mind if you are planning on doing this.

    The drug is known for giving highly variable results patient to patient. Some people get amazing highs from this drug (and, in turn, amazing analgesia). Other people barely feel the stuff. So it is not that popular amongst newbie opioid abusers. Also worth noting, is that there is no extended release version in the USA, but in other countries there exist preps. such as Palladone that come up to 64mg of Extended-Release HM. THESE can easily cause O/D's in abusers. So, if you are an international HipForumer, be careful if you encounter those pills.

    Oxymorphone: 1.25-1.75mg Oxymorphone (oral)~5mg Hydrocodone (oral), brands include Opana (both Extended and Immediate release). It has hit the US market within the last five years as a viable alternative to Oxycodone in the management of chronic moderately severe to severe pain, especially with the introduction of Opana ER (which comes in doses from 5mg up to 40mg).

    OM is an interesting opioid in that it is extremely strong, but at the same time, is much better tolerated compared with even weaker opioids. Patients who are strongly dependent on opioids who can't handle Fentanyl and who are pushing the upper limits on Oxycodone (say, taking 2 80mg pills a day), are increasingly being switched to this medication.

    It is highly abuseable, and the risk of O/D is very real. Being around the same strength (some say a tad stronger, some say a tad weaker) as Hydromorphone, one can imagine that it is a hot item illicitly. One 40mg ER pill, crushed and taken at once will flood you with the equivalent of about 100mg of Oxycodone (at once). So, if you are thinking about using these pills for recreation, be aware of the dosing conversion. I would not recommend this drug for first-time opioid dabblers. Even the 5mg tablet is enough to give the user some serious nausea and unpleasantness. However, if you are experienced with opioids, this is a viable alternative to Oxycodone or Hydromorphone. It should be noted that the Opana ER tablets resist being crushed into a powder, making snorting and injection problematic. I would not recommend injecting this drug, and if you want to snort it, look elsewhere for tips! It is meant to be taken orally in the Opana ER preparation.

    I have not taken this opiod, but all reports I have read indicate that it is not as sedating as Morphine and Hydromorphone, and allows the user (especially if you are a legitimate patient trying to live a normal life) to go about daily business pain-free, but not overwhelmed by opioid side-effects. Euphoria is strong and clean. This med and another (Buprenorphine) have been studied as novel treatments for severe, refractory depression (but don't expect your family doc to give it to you for that- maybe hit up Johns Hopkins' Psych. ward).

    Methadone: The dosing for methadone is special: For less than 200mg of Hydrocodone, the methadone dose is 20% of the Hydrocodone equivalent dose. For between 200 and 500mg of (equivalant) HC, the methadone dose is only 10% of the (equiv.) HC dose. This same scheme follows for higher doses. Essentially, this means that methadone becomes STRONGER at EQUIVALENT higher doses of another drug. It is known as Methadone everywhere. It is used for severe refractory pain management and for a replacement-medication in opioid dependent people (be it addicts or simply legitimate pain patients getting off of their drug regimen). Because of its (almost miraculous) fact that you need LESS of it as the amount of your previous drug was HIGHER, it is a god-send for the terribly addicted.

    As an example, a person taking 1,000mg of Hydrocodone (or, 650mg Oxycodone, or 150mg Opana, etc.- any equivalent will work for the example), requires 50mg of methadone to relieve withdrawal. However, this is not much more than the amount of methadone needed to adequetely switch from 200mg Hydrocodone (or 130mg Oxycodone, etc.). What an amazing concept! Even the most opioid-dependent folks can seek solace in this drug.

    However, there is a catch. It's use for illicit addicts is HIGHLY regulated. For the first year (in many cases), you are required to go to a special dispensary DAILY to recieve your dose. Random drug screens are common-place, and unforuntately, many un-informed members of society look down upon the users of this drug.

    Abusing methadone is common, as people recieving "take-home" doses can divert them. However, it is very strong and has prominent morphine-like side-effects which generally only limit illicit use to people who are already addicted to strong opioids, including Heroin (a pro-drug to Morphine that is injected).

    That is all I will say about Methadone. If you are thinking about abusing it, find something else to get your hands on. If you are SEVERELY addicted to opioids, read more about this amazing drug.

    Buprenorphine: 0.25mg (or 250 micrograms) ~ 5mg Hydrocodone (oral). However, their exists a CEILING DOSE at which increasing doses beyond such a dose will NOT yield more opioid effects. The ceiling dose is between 6 and 8 milligrams of Buprenorphine. This is equivalent to 160mg of Hydrocodone, or about 100mg of Oxycodone. It is sold as a sublingual tablet called Subutex and as sublingual film-strips and tablets (compounded with a drug Naloxone) called Suboxone. It also has been seen in lower doses for pain management in transdermal forms. Naloxone, contrary to popular belief DOES NOT lower the effectiveness of Suboxone. It is ONLY there in case a person injects a LARGE dose of Suboxone, in which case the Naloxone will cause precipitated withdrawal. Thus, it is only a deterrent to excessive IV abuse.

    This strange drug was made popular in the 1990s as an alternative to methadone in treating opioid dependence in patients who may not have hit 'rock-bottom' but who still wanted off opioids. Like I mentioned, the highest attainable opioid effect from this drug is the equivalent of about 100mg of Oxycodone, so some addicts can benefit from it. However, for some, Methadone is a more rational choice. Many methadone users switch to this drug when they lower their dose (to around 25mg methadone per day).

    It produces a very clean-clear, euphoric effect devoid of typical opioid sedation and mental fogginess. However, it is still highly abuse-able, especially given that it can be taken anytime, enjoyed for its euphoria, without sedating the user to the point of not being able to function. I will disclose, here, that I personally take this drug both as an opioid-replacement-maintenance drug AND as a novel treatment for severe, refractory depression. I find it a miraculous agent, especially given that tolerance build up is VERY slow compared to other opioids. I have only had to slightly 'up' my dose ONCE in eight months of taking the drug. Since then, I have LOWERED it again without losing any euphoria or anti-depressant effects.

    Abusing this drug is not a good idea since in order to take an amount low enough to not cause severe vomiting and possible O/D, you need to take something the size of a crumb (or if using the film strip, the size of about 1/8 inch by 1/8 inch). I know from experience that it rarely produces good effects in the opioid naive, simply because of how little room for error there is in dosing it. Simply put: Don't look to Suboxone to get high if you aren't dependent on opioids already.
    I AM ENDING THIS HERE FOR NOW. I STILL PLAN ON ABOUT FOUR MORE OPIOIDS, INCLUDING HEROIN AND TRAMADOL. STAY TUNED!.
     
    1 person likes this.
  2. BottleFED

    BottleFED Member

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    ETK, thats an excellent guide for the three most used opiates today. Thanks for writing that up, Hopfully we can get the MODS to STCIKY this.

    Perfect material for the new person considering trying an opiate for the first time. All the info doesnt get lost in discussing ROAs and other stuff like CWE or prepping for other things.
     
  3. etkearne

    etkearne Resident Pharmacologist

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    Thank you, sir. Don't worry, though, the fun is just beginning. I am not even to the -morphones or the crazy-strong synthetics yet.

    I figured, when it comes to things about "What is the best way to abuse a certain pill" there are countless threads, but a frightening LACK of threads on basic things like proper dosing, etc.
     
  4. EggoKiller

    EggoKiller Member

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    Nice job, rather informative. Hopefully first timers read it before they take something. You might even want to add the "psuedo opioid" tramadol, it's use has become much more prevalant in my neck of the woods.
     
  5. etkearne

    etkearne Resident Pharmacologist

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    I am definitely going to add Tramadol. I really hope to get at least 10 opioids up by the end of the day tomorrow. I might have to take some opioids to motivate myself to do it...
     
  6. BottleFED

    BottleFED Member

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    Damn it would be great to have a MOD that frequesnts our section and we may I just dont know who it is and our little piece of the world doesnt have the traffic most other sections do. But after reading your plans for this thread, We should really get this stickied.

    MODS CAN WE GET THIS PUT UP AS A STICKY, PRETTY PLEASE!!!! (also willing to volunteer to Moderate this sub-forum if the site needs the help.)
     
  7. ness33

    ness33 Member

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    I second the sticky... even though i don't post on here much. I read almost every post.
     
  8. p0rkch0p

    p0rkch0p Member

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    thirded, even tho it appears to have been moved. Who is the mod for this section? if i may ask?
     
  9. deleted

    deleted Visitor

    http://www.hipforums.com/newforums/showgroups.php?

    can we discuss drugs and less the other stuff..

    I didn't sticky it at first, as I was waiting to see what the OP wanted to do.. It is his thread after all.

    9 times out of 10 asking to be a mod isnt going to happen..
    The cloud people know who they want to place here, should they decide.. :sunny:

    Now I have to go in and remove all the Off topic discussion. See how this works, Ima leave the Off topic discussion in for the time being.. :(

    etkearne you can use this one til you finish and then copy to a updated version. :2thumbsup:
    Sticky now for easier access... :love:
     
  10. BottleFED

    BottleFED Member

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    Thanks for the Sticky Orison......
     
  11. etkearne

    etkearne Resident Pharmacologist

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    Note to viewers: I added three or four new opioids that I suggest checking out (including Opana- our forum's favorite, and Buprenorphine- the forum's runner-up HAHA!).
     
  12. etkearne

    etkearne Resident Pharmacologist

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    Tramadol: 50mg-75mg Tramadol (oral) ~ 5mg Hydrocodone (oral), brands include Ultram, Ultram ER, Ulracet, etc. This drug is considered by some to not be a real opioid. It is used as an analgesic for mild pain, having a strength similar to codeine.

    Pharmacologically, Tramadol itself is not an active opioid. It is an active Serotonin-Norepinephrine Reuptake Inhibitor (like the drugs Effexor and Cymbalta for depression). However, when metabolized in the liver, into O-Desmethyltramadol, it becomes a mu-opioid agonist (and, a 'real opioid').

    It is popular with doctors who are treating minor pains and don't want to get involved with scripting scheduled narcotics. That is important to note: Tramadol, in the federal level of the USA, is NOT scheduled. However, some states scheduled it (look them up before trying "something" possibly illegal). It is not as sedating as the traditional opioids (likely due to its inherent weakness AND its Norepinephrine enhancement- NOR agonists are stimulants).

    Due to its ease of availability (I won't tell you how most people get their hands on it. You can figure that out.) and lack of being scheduled, it is used to get a 'high' by thousands of people. I personally have much experience with this drug. Taking two 50mg tablets gives a good opioid buzz in the beginning, but, let me tell you- a tolerance builds up VERY quickly. At one point (only 4 months after starting to take the drug daily), I was up to 10 50mg tablets a day, often taking 15 tablets to get really stoned. This is dangerous, however. If you are taking Ultracet, it is dangerous because of the Acetaminophen compounding (see: Hydrocodone- Vicodin). And even without the Acet., it is dangerous because it lowers one's seizure threshold, known to invoke seizures in some at as low as what would be 7 50mg tablets. I played with fire with this drug, and luckily, escaped without harm. However, I would not risk it!

    Be cautious of this purportedly 'safe' 'un-abuseable' drug. It has a tolerance build up more rapidly than some of the harder opioids, and the seizure risk makes it dicey as well.

    Diamorphine (Heroin): 0.5mg-0.75mg Heroin (IV/IM) ~ 5mg Hydrocodone (oral). This drug is not used in medicine in the USA, thus I don't know any brand names besides Heroin. It used to be used for severe pain, given intravenously. However, most countries banned it due to severe addiction risks. However, it is not inherently more addictive than some of its cousin strong opioids mentioned above. Thus, treat them with the same fear and respect as you would Heroin!

    Heroin taken orally simply converts to morphine (it is a pro-drug like Codeine). It is therefore taken either by snorting, smoking, or injecting it. Snorting is not popular, smoking has mixed results (and is terrible for your lungs), so most people end up injecting it. When injected, Diamorphine is metabolized not into morphine, BUT into a very powerful opioid called 6-MAM. It is one of the most itchy, raw, nodding-out type opioids known to man (along with Hydromorphone IV and Fentanyl). So when people get high on heroin, they really are getting high on 6-MAM. Thus, black tar heroin is actually just already manufactured 6-MAM mixed with god-knows-what!

    Unlike the pharmaceuticals above, heroin is not regulated for purity. Street heroin is not just animal feces with a little morphine for kicks like some want you to believe, BUT it certainly isn't 100% Diamorphine. Thus, I advise no one here to begin their journey into opioids with Heroin products. Not only is it risky in terms of dosing (and overdosing subsequently), but the risk of transmission of disease and foreign particulate matter from improper hygienic technique with needles and preparation of the injectable solution itself, is very high. Hepatitis C is a common heroin-user ailment, and even HIV/AIDS has been known to spread amongst users. So, please, don't use this drug. That is all I am saying about it.

    Miscellaneous Opioids/ Conclusion: There are literally 100s of opioid compounds out there, mostly synthetic. Most aren't even used in medicine, but sit on some pharmaceutical company's shelf waiting for a use to come up. We currently (in the US at least) have a wide array of useful opioids to treat all sorts of pain. However, the basic problems of tolerance and addiction still haunt every opioid put on the market. New research will focus on finding opioids that don't build tolerance (or are like Methadone and Buprenorphine and only slowly build tolerance over years and years of use) and cannot easily be diverted to the black market.

    Also, hopefully the government will continue research into the use of opioids for treatment resistant mental illness. I, personally, am a part of this experiment. I now take Suboxone only for its antidepressant properties. I have been on at least 15-20 other antidepressant agents (not just including things labeled as antidepressants by the FDA), and Suboxone is the only one that 'really' works. Seriously. But I won't go on about that, as I want to keep this article objective.

    Just for fun, here are some more opioids out there you might encounter. If you want to know about one of them, send me a PM, or just reply in this thread requesting its addition to the other ones with articles.

    Nucynta (Tapentadol), Darvon (Propoxyphene), Levorphanol, Meperidine, 7-Hydroxymitragynine (in the Kratom plant), Salvinorin A (a kappa-opioid agonist in the Salvia D. plant)...

    Those are some of the more popular ones. Most are dangerous (like Darvon-products, which were withdrawn last year from the market), and others don't even produce euphoria because they act more on the delta or kappa opioid receptors and not the mu opioid receptors.

    I will finish by describing the opioid 'high' (which is the same mechanism for the analgesia) pharmacologically, but very rapidly:

    The opioid binds to the mu-opioid receptor in the brain and spinal horn. It causes the retention of the neurotransmitter associated with the neuron it attaches to. Luckily, in the spinal horn, this means lack of transmission of Substance P, the transmitter of pain. It also prohibits the release of hormones, including cortisol stress hormones, giving content peace to the user. And, finally, in the Nucleus Accumbens, it prohibits GABA from STOPPING the transmission of dopamine at that site. This, in turn, means that dopamine FLOODS the Nucleus Accumbens and subsequent mesolimbic pathway in amazingly abnormally high amounts, causing intense euphoria. All of these things together give that un-replicate-able opioid high.
     
  13. p0rkch0p

    p0rkch0p Member

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    i recently found out there are opiates that are like 3000% more potent than moraphine, if i can find the link again ill post it, its scary that shit is out there, lol obviously its not for human use, or may not be used at all, lol....ill look for it again.
     
  14. p0rkch0p

    p0rkch0p Member

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    Introduction.
    Sufentanil is a highly lipophilic synthetic opioid analgesic chemically
    similar to fentanyl. It is thought to be 10 times more potent than
    fentanyl
    1,2
    although this has not been tested within the subcutaneous
    infusion model. It is used widely in anaesthetics but has had limited use
    to date within palliative care .
    Aim
    To describe the use of sufentanil in palliative care patients under the care
    of the palliative care team at the Mater Hospital.
    Methods
    Patients who had received the drug were identified from pharmacy held
    SAS forms. Patient characteristics were obtained from hospital records.
    Case notes were searched for opioid use prior to, or following sufentanil,
    and the clinical outcome.
    Findings
    Over the 5 months August to December 2003, 16 patients received
    sufentanil by continuous subcutaneous infusion (csci) during the course
    of their treatment as inpatients in the Mater Misericordae Hospital,
    Brisbane. Four patients had received csci morphine, 3 csci fentanyl, 3
    transdermal fentanyl, 2 oral SR morphine, 2 oral SR oxycodone and 2 had
    not been on opioids prior to the sufentanil.
    Sufentanil was used on its own in the syringe driver in 4 patients and in
    combination with midazolam (3), methotrimeprazine (2), clonazepam (1),
    haloperidol (1), midazolam and methotrimeprazine (2), clonazepam and
    methotrimeprazine (1), haloperidol and ketamine (1), haloperidol and
    metoclopramide (1) and haloperidol, midazolam and glycopyrrolate (1).
    No problem with drug compatibility was noted by visual inspection.
    The mean starting dose of sufentanil was 189.4mcg/day. The mean dose
    of fentanyl equivalent dose prior to conversion was 3083mcg/day; a dose
    ratio of 1:16.3.
    Sufentanil was given for a mean of 6 days (range 1-17 days).
    The mean dose of sufentanil on completion of the infusion was
    258mcg/day.
    Six patients died whilst receiving csci sufentanil (1 at home). Five patients switched to another opioid following sufentanil; to fentanyl
    transdermal patches (2), methadone (1) hydromorphone (1) and an
    intrathecal regimen of bupivicaine and morphine (1).
    Six patients remain alive at the time of audit; on fentanyl transdermal
    patches (3), SR oxycodone (2). One patient remains on sufentanil at time
    of evaluation. The duration of survival for these patients is a mean period
    of 22 days (3-56).
    Conclusion
    Only one paper
    3
    describing 2 patients who received sufentanil by csci
    have been found on literature review.
    Sufentanil is a suitable opioid analgesic for substitution for fentanyl
    where the dose volume exceeds that deliverable by Graseby MS16 driver.
    The potency of sufentanil allows reduction in the volume of injection.
    There is controversy as to the exact dose equivalence between fentanyl
    and sufentanil with relative potencies of between 24:1 and 16:1 being
    reported by Paix et al
    3
    In our series, sufentanil was found to be .
    approximately 16 times more potent than fentanyl, which is at odds with
    the ratio quoted by others
    1,2
    but identical to at least one patient in the
    series of Paix et al
    3
    .
    Some concerns exist that the extreme lipophicity of sufentanil may
    produce a depot effect within subcutaneous fat producing significant
    accumulation of drug that is slowly released into the systemic circulation
    following termination of the infusion. Great caution should be taken
    when converting from sufentanil to another opioid. Further research in
    the use of this drug is warranted.
     
  15. EggoKiller

    EggoKiller Member

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    Sounds like Fentanyl for elephants...

    And nice work by the way, it turned out great.
     
  16. etkearne

    etkearne Resident Pharmacologist

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    Thank you. I really hope that both new and senior members will at least take a LOOK at this thread to either keep themselves from accidentally killing themselves, or just to become more knowledgeable about their drugs of choice.
     
  17. BiggJimm

    BiggJimm Guest

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    Yes I agree that is very informative & much needed thread. Hopefully those who truly need it can find the information before the do harm to themselves. Where I'm at we need something like that printed up and put in the newspaper or something as we have a lot of young people ODing because they are not aware of the dosing conversion between the hydros they find in the med cabinet at home & the OC's they're getting off the street. Oxicontin are very plentiful around here in pretty high strengths so it is kind of a problem in my area. And another thing is a lot of people are not familiar with the difference between instant and extended release and the dangers of taking an ER and not feeling anything right away so they take a couple more and then run into trouble. Kudos to you for putting all the right information together and posting somewhere it can be accessed in a manner that doesn't necessarily "glorify" the abuse of but instead "informs" one to the safe use of a said opiate. Have a wonderful and "pain free"'day to all.
     
  18. EggoKiller

    EggoKiller Member

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    I just noticed you put a brand name for codeine as "Purple Drank", that made me laugh.
     
  19. etkearne

    etkearne Resident Pharmacologist

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    Oh, believe me, it made ME laugh when I typed it too!! But, regretfully, I have to admit that I HAVE seen people using such a elementary-school-level slang term here before!
     
  20. bluedragonfly

    bluedragonfly Member

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    This is such an informative post. Thank you so much for posting it.
     

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