The main problem in overdose is brainstem respiratory CO2 sensitivity falls and the patient stops breathing. The purity of heroin on the streets is strong enough now that we’re seeing this even with inhaled and smoked heroin sometimes. Now, tolerance occurs rapidly particularly to the nausea and that kind of discomfort and it becomes purely pleasurable at that point but only one in ten people who try heroin tend to become addicted to it. So we have to be realistic about this and reasonable, not that heroin could ever be thought of as a legalized substance, but not everybody who walks in who says, you know, “I used heroin at a party” is a heroin addict and we have to do some work to tease out “Do we have a criteria of dysfunction being met?”
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What’s the withdrawal amount? Well, the locus caeruleus is suppressed by chronic heroin use and when that suppression is released we have up-regulation of noradrenerigic receptors and suddenly the adrenergic arousal goes wild. There isn’t up-regulation of the opioid receptors themselves but there is up-regulation in terms of dopamine activity and the two sides are the ventral tegmental area – VTM – and nucleus accumbens which we talked about before but both of these are involved. Heroin is not a one site reinforcer. It seems to involve this system.
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I’m not going to talk about the long term treatment, for instance methadone. Harm reduction is an important goal nowadays because it reduces HIV transmission. So needle exchange works. Even in areas with lots of severe heroin addicts, we see reduction in HIV transmission thanks to needle exchange regardless of what the government’s policy is. Generic viagra 100 mg online at cheap pharmacy mall. Rapid detox can be done in less than five days with a combination of either these two – clonidine or naltrexone – plus or minus buprenorphine which I think actually improves the experience and retention for the patients and the L Group published on this. I think it’s definitely better combined.
Anesthesia detox. You actually can get a full blown heroin addict onto full dose naltrexone totally blockaded at the mu-receptor – they can’t become high now – in five hours using anesthesia. The problem is you don’t know if the therapeutic change has happened so that the patient doesn’t go out and then try and overcome naltrexone and dose themselves so badly that they overshoot and go into coma which has happened now a few times.
LAM – levo acetyl methadone. LAM is now FDA approved. It’s just a long acting type of methadone. So you can dose 100 mg Monday, 100 mg Wednesday, 150 mg on Friday and the patient is covered in the intervening days. They have more freedom. They can return to a more normal life. The patients like it. They retain better on it. Not available in all states. Call for details.
Buprenorphine. I hope it’s going to come out this year from the FDA. I keep saying that. The slowdown has been that the FDA is being pushed to allow dispensing in physicians’ offices. Buprenorphine is another long acting opioid like LAM, like methadone, safer and we may get to use it in office practice.
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The dopamine agonists – bromocriptine, amantadine, mazindol – this is conclusively disproved now. Amantadine hasn’t done as well as bromocriptine and bromocriptine has had side effects and has had some negative trials now too. So the answer on do we have a treatment for cocaine? No. All we have is longitudinal treatment and then relapse prevention. Isolating from the cues. Reintroducing the cues as the patient succeeds to give them a chance to bolster their techniques of thinking about the consequences, reminding themselves of the spouse’s wishes to stay clean and various counseling techniques. Stress. Coping with stress, learning to pamper one’s self in ways other than the most immediate gratification. These are things our patients really don’t know how to do.
You probably are seeing all the advertisements for tramadol, Ultram. A new pain agent, nonsteroidal but it’s not one of the NSAIDs. It’s a nonopiate analgesic but there is some concern that it can trigger relapse so we have to be careful with it. I haven’t seen a big market in Ultram abuse but there is actually a study assessing that rationally. So far, so good. One of the physiologic effects of the opiates that is helpful to remember for the boards but also for looking at patients in emergency situations, remember that aside from the analgesia and the rush and the euphoria of opioids they also produce smooth muscle inhibition and that’s down at the bottom of page 284. You might just want to put a check mark or a star there. That helps you think of several other things without having to memorize all of them.
Tramadol online – Tramadol is a non-opioid pain relief medication that is meant to help alleviate moderate to moderately severe pain. Tramadol is a synthetic analgesic, not an anti-inflammatory, which means that people who cannot take anti-inflammatories due to the side effects can often take Tramadol to help relieve their pain.
Smooth muscle inhibition. So the pinpoint pupils in patient’s eyes when they’re intoxicated with heroin, that’s because the smooth muscle that opens the iris for a full pupil is being relaxed. So that smooth muscle inhibition allows the pupil to close down that tight. It’s also responsible for some of the initial nausea and vomiting that people have sometimes when they try codeine for the first time. Heroin does it too, by the way. The same thing is true of withdrawal. If smooth muscle inhibition is part of the intoxication what do you think happens in withdrawal? You get smooth muscle hyperactivation so you get all nausea and diarrhea and the loss of appetite and the pupils get enlarged.
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The mu-opioid receptor system is the primary analgesic receptor system. It’s anti nociception. Anti nociception means you don’t feel pain. You can feel pressure but you don’t feel pain when these sites are occupied. Heroin, morphine, methadone, the m’s go with mu. The delta receptors are also supportive for analgesia and the akephalines have the better binding for this. So we have these three major systems. The kappa system you know about. Talwin, pentazocine produces analgesia there but it is also associated with a risk for dysphoria and Talwin is contraindicated in a patient who has mu-opioid dependence – heroin, morphine or methadone. Contraindicated because it will trigger a dysphoric reaction.
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