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Guy sitting on a weight benchDISCLAIMER: Morphine and all opiate-based medication is dangerous and can be highly habit- forming, even lethal. I do not condone the use of medication used to treat post-operative and severe pain for ‘cranking out a few extra sets’. However I know there are those of you out there using morphine and many of its derivatives for this or similar purposes. The article is titled “morphine” because she is the mother of all opiates. I offer this article as an educational tool. If you do find yourself sinking into the dark abyss of addiction, help is available; you just need to take the first step and ask for it. There are also those of you who won’t develop an addiction or even an affinity for opiates. You’ll use them legally and responsibly… good for you. However you could probably learn a thing or two from this article as well.

Morphine is a naturally occurring alkaloid found in the sap of the opium poppy (Papaver somniferum) pod. Among many other medicinal alkaloids found in this particular species of poppy such as: codeine, papervine, and narcotine to name a few, morphine is the principal alkaloid of interest found in opium. It also causes the most euphoria, and is the most habit-forming. It was first synthesized in 1804 by the German pharmacist Friedrich Wilhelm Adam Sertürner. He named the drug “morphium” after Morpheus, the Greek god of dreams (14). In 1806 the drug was being used regularly to treat pain, coughs, and diarrhea (3). Exactly 100 years after its acceptance into the medical community, The Pure Food and Drug Act was passed, regulating labels of patent medicines containing any ‘narcotics’’, including alcohol, cocaine, marijuana, and opiates (1).
Pharmacology & Availability

Morphine is also known as “7,8-didehydro-4,5 -epoxy-17-mtehyl-morphinian-3, 6 -diol sulfate,” and has an empirical formula is C17H19NO3 (1,2,14). Morphine primarily activates the mu-opioid receptors in the Central Nervous System (CNS). Mu-opioid receptors are the receptors most responsible for causing the euphoric ‘high’ associated with opiates, hence the drug’s reputation for being one of the most euphoric of opiates; many believe even more so than heroin, although it is shorter acting with a half-life of only two to three hours (1,2). Morphine also agonizes the Kappa-opioid receptors of the CNS, which gives the drug its pain-dulling properties. According to RxList.com, “Morphine has a pKa of 7.9, with an octanol/water partition coefficient of 1.42 at pH 7.4. At this pH, the tertiary amino group is mostly ionized, making the molecule water-soluble. Morphine is significantly more water-soluble than any other opioid in clinical use.” Oral morphine has only 30% – 40% bioavailability compared to injectable preparations, which range in dose from .25 to 3 mg (2). Sustained release morphine tablets come in doses ranging from 15 to 200 mg, while the instant-release tablets are available in doses of 15 and 30 mg/tablet.

Both preparations can be abused in many ways. Yet surprisingly the drug has avoided media scrutiny in terms of its abuse potential. Unlike its synthetic cousin Oxycontin, which some pharmaceutical companies reformulated to prevent people from insulfating or injecting the drug (15), morphine has ‘flown under the radar’, so to speak. The instant release pills basically melt as soon as they touch water, and can be insulfated or made into an intra-nasal solution, even smoked. In terms of legality, don’t expect to find any ‘research chem’ suppliers carrying it, as straight morphine, or morphine preparations containing more than 50 mg per 100 ml or per 100 grams, are Schedule II in the United States. However products containing less than 50 mg per 100 ml, or per 100 grams, and which contain one or more active, non-narcotic ingredients in “recognized therapeutic amounts” are Schedule III in the United States (2). The Schedule III products are usually cough syrups, or diarrhea medications such as Paregoric, which contains 2mg/5ml of anhydrous morphine (3). In fact, a few trips to a G.I. specialist after mega-dosing magnesium or cheap creatine may yield a script for Paregoric, especially if you’ve been self-medicating your chronic diarrhea with Imodium (loperamide) for years… but that’s your call.

Why would athletes take narcotics such as morphine? Side effects such as lethargy and a decrease in motor skills dissipate within a few days of oral dosing (15). Unfortunately, so does the euphoria. A responsible athlete looking for a drug that won’t block prostaglandin secretion (more on that later), will increase pain threshold to exponential levels, and kill the appetite (1,14,15,) does sound like a performance-enhancing substance. An athlete can compete and train longer and harder, while reducing or eliminating pain, allowing optimal performance despite injury or illness. Although morphine wasn’t isolated until 1804, the use of opiates by athletes throughout antiquity is more than well documented. The extraction of opium, and the compounding of various tinctures and preparations is well documented among manuscripts from ancient Egypt, Greece, and even Minoan civilizations. The first written documentation of its use dates back to 800 BCE (7). Morphine, while highly sedating in most of the population, has an opposite effect on many people, causing some to become ‘wired’, especially opiate-tolerant individuals. One interesting fact about morphine is that it actually increases smooth muscle tone in the gastrointestinal tract, while decreasing contractions, causing constipation.

Perhaps, in addition to its ability to increase the pain threshold, morphine also exerts an increase in the tone of skeletal muscle. However, the only studies that support this theory were performed on rats and forced swim tests (8,9). For those of you not ‘in the loop’, forced swim tests are when creepy old men in lab coats make rats swim until they nearly drown, then pull them out by their tails once their rat bodies give out. Although many an athlete has been suspended from his or her organization after testing positive for morphine metabolites. Vaclav Drobny, a Czech soccer player tested positive for morphine following a game in 2003 but was later cleared of any wrongdoing, and no punitive action was taken (11). In an ironic addition to human athletes using horse drugs, in 2002 twenty British racehorses tested positive for morphine, however trainers blamed “contaminated feed” for the positive results (11). I wish I had known at the time, I would’ve bought British horse-feed by the ton.

Drug Testing, Clearance Time & Miscellaneous Info

Drug testing and doping among athletes and their governing bodies is a constant cat and mouse game (in case any of you bodybuilders are unaware), and here’s where it gets a bit tricky. Every naturally occurring and many synthetic opiates/opioid convert to morphine metabolites, specifically, glucuronide metabolites, the most prevalent being morphine-3-glucuronide (15). It is these metabolites that trigger a positive test result for opiates, as the tests (for the most part) are actually looking for morphine metabolites under the broad spectrum of ‘opiates’. However, certain compounds known as “partial opiate agonists” do not convert to morphine, so no morphine metabolites are produced. Therefore certain opiates/opioids don’t show up on a standard opiate test, but can be tested for separately, and sometimes are. Athletes use such compounds as: methadone (not common, but used as it is seldom tested for), nalbuphine (Nubain), buprenex (Subutex, Suboxone, Temegesic), and propoxyphene (Darvon, Darvocet), in hopes of avoiding a positive test result, in addition to the other advantages of using certain compounds.

Nubain, for example is rumored to lower cortisol levels, and definitely regulates mood and hunger while dieting. The Nubain craze over the past 15 years or so can be attributed to the late, great Dan Duchaine, who advocated its use in the 1980’s, when the drug developed a strong following among bodybuilders up until the proverbial well ran dry with the crack-down on certain chemical supply houses nearly three years ago during the DEA’s ‘Operation Web-Slinger’. In addition, the carnage of Mexican veterinary pharmacies and anabolic-androgenic steroid (AAS) production brought the availability of Ketamine, another popular anesthetic, euphoriant (pain killer), and recreational drugs among bodybuilders to a screeching halt. However certain bodybuilders favor morphine in its many forms: MS-Contin, MS-IR, and Paregoric. Hell even Poppy-Tea is growing in popularity due to the availability of P. somniferum pods on the Internet. Close one door, another opens sooner or later. I should mention, even something as benign-sounding as ‘poppy tea’ can contain hepatoxic alkaloids if made from other species of poppy, used excessively, or brewed from chemically treated plants.

Why morphine? Why not ibuprofen, acetaminophen, or naproxen? Should every-day aches and pains associated with bodybuilding and strict, contest-prep dieting be treated with one of the most potent and most habit forming pain medications known to modern pharmacopoeia? Of course not, but many of you are using some type of narcotic painkiller for just this purpose. And in terms of toxicity, and hindering muscle gain and/or fat-loss, common OTC painkillers, even Rx narcotics such as Vicodin, and Percocet are most likely far worse. The reason is that all contain Non-Steroidal Anti-Inflammatory Drugs (NSAID’s), either as pure preparations or mixed with an opiate. Even COX-2 inhibitors such as Viox can be detrimental to recovery from a weight training session (4,5). When an individual trains with weights, hypoxia of the endothelium (4) is the main cause for prostaglandin release, which as anyone who’s used PGF2-A (Lutylyse) can attest to, causes muscles to grow. While Lutylyse has been marginally effective at causing muscle growth, so far synthetic prostaglandins are no match for the endogenous kind. While morphine was shown in one study to inhibit endothelial hypoxia (6), NSAID’s and COX-2 inhibitors have a much more pronounced effect on inflammation and blocking prostaglandin release (4,5). That being said, the old adage: “no pain, no gain,” proves true once again.

No painkillers will yield the most gain, however if you believe you need to push through the pain killing ability of your natural endorphins, opiates/opioids, and morphine in particular would be your best bet. Another important aspect to note is that morphine may be toxic to the liver or kidneys with prolonged use and excessive dosing. As a tolerance develops, and the euphoric effects of the drug dissipate, it will become tempting to increase the dose, however even with a tolerance morphine still lessens awareness of pain (2), so just as in the case of methylated, oral AAS, more, wile often better at first, is always worse in the long run. Unlike NSAID’s and COX-2 inhibitors, opiates do not ‘remove’ or ‘kill’ pain, they simply increase a person’s pain threshold ad-infinitum, depending on the dose and the particular drug. Just as someone in a car wreck can walk around with broken bones and serious injuries thinking their fine (due to endogenous endorphins), an individual under the influence of a potent opiate such as morphine could probably drill a hole in his or her head, literally… if he or she had enough of the drug.

Dosing Info & Precautions

So clearly, caution needs to be exercised in many areas when working out under the influence of opiates. Take extra care to warm up, stretch, and most importantly, stay aware of pain. A 200 lb. Bodybuilder taking a twice-daily dose of 60 mg MS-Contin would be able to function at 100% intensity in the gym within four or five days of drug therapy. However a muscle tear might feel like a bad cramp, so constant vigilance with regards to hydration and proper electrolyte levels is a must. In addition, an athlete who decides to use morphine absolutely must not ‘chase the high’, by increasing the dose. Euphoria from morphine is only a side effect, just like the lethargy, circulatory/respiratory depression, and edema (water retention).

Although I can find no studies to support the following statement, some people claim that chronic use of certain synthetic opiates actually causes muscle spasms and cramps during exercise, although, this is no more than hear-say. Another interesting fact with regards to morphine is that it appears if one is actually in pain (be it from training through an injury), training with a nerve or muscular disorder, or any medical condition that would cause severe pain, morphine does not cause euphoria or a pronounced ‘high’. According to one recent study, those who are actually in pain feel no need to increase their dose once proper analgesia was achieved, and only 9.5% reported withdrawal symptoms, as opposed to 89.5% of recreational users reporting withdrawal symptoms (11). This is something to keep in mind should you decide to use morphine to ‘train through pain’.

Effects on Glucose Metabolism

In addition to addiction, possible liver and/or kidney impairment, and, reduced prostaglandin release during exercise, opiates interfere with the insulin receptor, over time leading to defective glucose recognition by pancreatic beta-cells. So if you for example maintain a state of addiction for a significant period, your pancreas won’t respond to glucose as well as they should (12). However, that particular study was done with diabetic heroin addicts, not nearly healthy individuals. One nutrition book actually states that short-term administration of opiate medication, “heightens and delays glucose response to insulin,” (13) which at least sounds good. I know from personal experience, that the ‘carb-coma’ I get from a post-workout drink consisting of 75g high-GI carbs and 45g. of protein is significantly more intense when on an opiate.

Bullet Points & Things To Keep in Mind

    • Constipation: a side effect of morphine that will not go away; particularly important for pre-contest dieters.  Supplement with ground flax seeds, psyllium husks (colon-cleanse products).  Keep fiber and distilled water intake high.
    • ‘Chasing the high’: opiate euphoria will go away, while the desired analgesic effects will remain despite a tolerance.  Find the dose that works for you and stick with it.
    • Supplement with liver and kidney cleansing products, especially if combining with AAS.
    • Supplement with a ‘pre-workout energy’ product until the sleepiness and lethargy pass.  Also, use caution when operating a motor vehicle.
    • If you find that, despite your best efforts, you’ve developed a physical addiction to the drug, seek professional assistance from a doctor.
    • If you opt for a professional detox (expensive and unnecessary in my opinion), the following links will point you in the right direction. Subutex/Suboxone Doctor Locator.  Subutex is a much better alternative to methadone for detoxing from opiates.  If you’ve got the money, the “Rapid Opiate Detox” procedure is king: 24 hours and you’re good as new.
    • Ibogaine therapy is one way to make detoxing from opiates fun! While some clinics are extremely expensive, Eric Taub’s “I Begin Again” clinics, located around the world, are not.
    • If for some reason rehab or Ibogaine are not viable options, go to your local pharmacy.  Buy the following in order of importance:

– Blood-pressure monitor & batteries
– Enough loperamide (anti-diarrhea pills) to last for 3-5 days.
– Ibuprofen- not acetaminophen, naproxen, or any other OTC pain med.  Enough to last for a week.
– Benadryl (a more potent anti-histamine such as phenagran would be better) –enough to last a week.

– Epsom salts for baths.
– Chocolate and sugary candies.
– Gatorade & distilled water
– Some sort of ‘detox tea’ or herbal diuretic to help flush yourself out.

  • Have someone stay with you, and remember that what you’re about to go through is no different from the flu.  Tell yourself that repeatedly.  Your mind will fuck with you during the withdrawal period.
  • Depending on what opiate your coming off and how much you’ve been taking, withdrawal can last anywhere from two days to six months (six months if you’ve been on methadone for years).  Expect the hard part of a morphine withdrawal to last 48 hours once you start feeling ‘sick’.
  • Before you get sick, go online and do your research, I’m not a medical professional and can’t tell you how to combine the above drugs for optimal benefits.  I can tell you to check your BP regularly and take hot baths w/ Epsom salts once the leg cramps start.

Summary

As I advise towards the end of any article dealing with a potentially life-ruining substance, moderation is the key to using morphine or your opiate/opioid of choice. If you go chasing the euphoria and increasing your dose, you’ll pay a hefty price. Treat the drug with respect, and the benefits will outweigh the risks. Just keep in mind that morphine, like any performance-enhancing drug, is a double-edged sword. However unlike AAS, in terms of safety, morphine is probably right up there with DNP, insulin, and diuretics in that it has the ability to kill you instantly if you take too much or mix it with other CNS depressants. Yet I’d even place it one tier higher on the ‘dange-o-meter’, due to the added component of withdrawal effects.

Any questions regarding this article can be posted in the “Mind & Muscle Magazine” forum. Any questions regarding personal matters can be emailed to me at: [email protected], or PM’d to username: Viator at the Mind & Muscle forums.

References

1. “Morphine Vault” The Vaults of Erowid. Online 17 March, 2006. Available: www.erowid.org
2. “MS Contin Online: Description…” Rx List. Online 17 March, 2006. Available: www.rxlist.com
3. “Paregoric.” Drug Store Dot Com. Online 17 March, 2006. Available: www.drugstore.com/pharmacy/prices
4. Winn, TS, & Marshall JM. “Contribution of prostaglandins to the dilation that follows isometric forearm contraction in human subjects: effects of aspirin and hyperoxia.” Journal of Applied Physiology. 2005 Jul;99(1):45-52. Epub 2005 Mar 3. Available: PubMed
5. “Stretch Induced Myoblast Proliferation is Dependant on the COX2 Pathway.” . Experimental Cell Research. 2005 Nov 1;310(2):417-25. Epub 2005 Sep 15.. PubMed.
6. “Morphine Sulfate Inhibits Hypoxia-Induced Vascular Endothelial Growth Factor Expression in Endothelial Cells and Cardiac Myocytes.” Journal of Molecular and Cellular Cardiology. 2001 Dec;33(12):2179-87. Available PubMed.
7. P.G. Kritikos & S.P. Papadaki. “The history of the poppy and of opium and their expansion in antiquity in the eastern Mediterranean area.” United Nations Office on Drugs & Crime. Online 14 March, 2006. Available: www.unodc.org
8. Smith, M.A. and Yancy, D.L. “Sensitivity to the effects of opioids in rats with free access to exercise wheels: mu-opioid tolerance and physical dependence.” Psychopharmacology. 2003 Aug;168(4):426-34. Epub 2003 Apr 23.
9. Broom, D.C., Et. al. “Nonpeptidic delta-opioid receptor agonists reduce immobility in the forced swim assay in rats.” Neuropsychopharmacology. 2002 Jun;26(6):744-55.
10. “Guide to Drugs in Sport.” News24.com. Online: 19 March 2006. Available :http://www.news24.com/News24/Olympics2004/
11. Cowan, DT, Et. al. “Opioid Drugs: a Comparative Survey of Therapeutic and “Street” Use.” Pain Medicine. 2001 Sep;2(3):193-203 Available: PubMed.
12. Giugliano, D. “Morphine, Opioid Peptides, and Pancreatic Islet Function. Diabetes Care. 1984 Jan-Feb;7(1):92-8.
13. Coon, Julius Et. al. Nutrition and Drug Interrelations. Academic Press. May 1978. pp. 627.
14. “Morphine.” Wikipedia. Online 20 March, 2006. Available: http://en.wikipedia.org/wiki/Morphine.
15. Physicians’ Desk Reference (PDR) 2003. Ed: Medical Economics Staff. Pp: 2810 & 2812.

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