Endogenous Opioids

October 4, 2014

Endogenous Opioids and Opioid Receptors

The term opioids are not new to many, it has been heard as the media is always abreast with all information about these opioid drugs which to the public are known mostly for the wrong reasons. People have got misinformed about these drugs so much that when you tell a layman that these drugs are used in hospital then to him you will something much worse than an alien. However to the medical fraternity these opioids are essentials that are hard to survive without. That said and left, back to the topic; Endogenous Opioids is a new term to many and if your prediction is as right as mine then you are hearing it for the first time. What does it really mean? The endogenous opioids are opiate-like substance, such as an endorphin, produced by the body. If you thought that you can live without these endogenous opioids then you need to wake up from your momentary slumber. Every day of our lives we face pain of all sorts even the most insignificant pains needs the actions of these opioids to give you peace.

Today, the endogenous opioid system is one of the most studied innate pain-relieving systems. The endogenous opioid system consists of widely scattered neurons that produce three opioids: beta-endorphin, the met- and leu-enkephalins, and the dynorphins. These opioids act as neurotransmitters and neuromodulators at three major classes of receptors, termed mu, delta, and kappa, and produce analgesia. The endogenous opioids works in the same manner as the narcotic opioids in that they bind to the same receptors and they also have both good and negative effects. There might be all sorts of information out there that you can lay your hands that may speak well of the opioids but the bitter truth is we all depend on despite the negative light they have been portrayed in.We are all naturally dependent on opioids for our emotional health. Both narcotics and internally generated endogenous opioids exert their action on the body by interacting with specific membrane receptor-proteins on our nerve cells.

There are three large pro-compounds that are produced by the body and these are: proenkephalin, prodynorphin, and pro-opiomelanocortin. However, endorphins can further decompose to small fragments, oligomers, which are still active. Oligomers pass the blood-brain barrier more readily. Enzymatic degradation of small-chain endorphins is accomplished by dipeptidyl carboxypeptidase, enkephalinases, angiotensinases, and other enzymes. This limits their lifetime in the unbound state.

Presynaptically opioid receptors inhibit transmission of excitatory pathways. These pathways include acetylcholine, the catecholamines, serotonin, and substance P. Substance P is a neuropeptide active in neurons that mediate our sense of pain. Endogenous opioids are also involved in glucose regulation. Opioid receptors are functionally designated as mu, delta, kappa among others. These categories can be further sub-classified by function or structure. Decoding the human genome has allowed the genetic switching-mechanisms that control the expression of each opioid receptor to be determined at the transcriptional and post-transcriptional level.

Opioid-driven inhibition of neuronal excitability is mediated by the activation of a variety of potassium channels in the plasma membrane. The disparate subjective and behavioral effects evoked by activation of the different categories of opioid receptor are typically not the outcome of different cellular responses, but reflect the different anatomical distributions of each receptor. Unlike kappa opioid receptors, however, both mu and delta opioid receptors internalize on exposure to agonists. Activation of any type of opioid receptor inhibits adenylate cyclase, resulting in a fall in intracellular cAMP and diminished action potential firing. This causes a reduced flow of nociceptive information to the brain. Conversely, opioid addicts undergoing withdrawal suffer elevated cAMP levels and enhanced protein kinase A activity, resulting in increased neurotransmitter release.

Role of Mu receptors in addiction

The Mu opioid receptors are the gateway to addiction. This is because they mediate positive reinforcement following direct or indirect activation. In an experiment where mice without mu receptors were used, it was found that the morphine’s analgesic and addictive properties are abolished in these mice. This shows that mu receptors mediate both the therapeutic and the adverse activities of opioids. The mice that were lacking mu receptors were found to lack of morphine-induced analgesia, reward, and dependence. The mice had increased sensitivity to pain. This shows that the mu receptors play a critical role in addiction. These mu receptors function as switches upon direct or indirect reinforcement of opioid abuse. Mu-opioid receptors are a key molecular switch triggering brain reward systems and potentially initiating addictive behaviors. The lack of mu-receptors abolishes the analgesic effect of morphine, as well as place-preference activity and physical dependence. This receptor therefore mediates therapeutic analgesia and adverse activities of morphine.

Opioid withdrawal symptom

endogenous opioids When a person has been using the opioids for some time, he will become physically adapted to the drugs so much that when he stops abruptly he will experience the symptoms of withdrawal. Withdrawal is not only faced by opioid user only but also other sick people who are on other drugs as well. However to limit the withdrawal symptoms, there are some factors that come in handy. One of these factors is the pace and how you exit from using these drugs. Your doctor will be of help in helping you by developing safe exit strategies that will limit the withdrawal symptoms.

Finally, you need more information to stay away from dependence on alcohol and drugs as these have crippled societies and that is why here at AWAREmed we are dedicated to finding the best solutions to addiction and dependence on substances. Dr. Dalal Akoury (MD) is always in the mood of helping any patient to be addiction free. Do not hesitate to call on her for help in managing any sort of chronic pain or any type of addiction as well as other diseases.

Endogenous Opioids and Opioid Receptors

Types of Opioids and Their Uses

October 4, 2014

Type of Opioids, Their Uses and Side Effects

Opioids are drugs that many people cannot do without. They are essential in hospitals as they are the most effective drugs that can be used to aid the pain patients. Diseases such as cancer are synonymous to pain and in some situations going through the treatments will be very painful and therefore there is need for a drug that will work in different ways to curb the pain that may be disabling to the patient. Chronic pain in itself presents a torture to the patient and without pain relievers, such pain may cripple a patient. The opioids are not news to many years; people know them some as dangerous drugs that should never have been created in the first place. While to many they has become very valuable essentials that they cannot survive without- the pain patients (and even addicts). However, people are not always informed about the given types of opioids. The opioids are mostly classified according to their source. There are opioids that are naturally extracted from the poppy plant and used without designing or any other further processing. These will fall under natural opioids. Opioids may be extracted from the poppy plant but then is further processed. This group is referred to use semi-synthetic opioids while there are some that are some opioids that are processed in the labs. The opioids falling in this group are known as synthetic opioids.

The naturally sourced opioids

The natural opioids are those that are naturally available from the poppy plant. After extraction they are not further processed in a manner that will deplete their contents. Some of these natural opioids are used as pain relievers in hospitals.

Here are examples of the opioids;

Morphine

Morphine is naturally extracted from poppy plant. It is the most dominant opiate in the poppy plant. It was the first active ingredient that was extracted from the poppy plant. Apart from morphine there are also other alkanoids of different types that are found in the opium. The major source of morphine is a chemical extraction from opium.

Despite its use in hospitals for pain relief in patients with intense pain, morphine has a high potential of addiction, tolerance and psychological dependence which develops very rapidly. However psychological dependence takes a little bit longer to develop and may take several months. With morphine, tolerance to respiratory depression and euphoria develops more rapidly than tolerance to analgesia.

Thebaine

Thebaine is naturally available in small quantities in opium. It is also known as Paramorphine. It is white, crystalline, slightly water-soluble and poisonous alkaloid. The Thebaine-Constituent of Raw-Opium is normally between 0.2% and 1.5%. However higher amounts have been reported. It is not used for therapeutic or recreational purposes, but is converted industrially into a variety of compounds such as oxycodone, oxymorphone, nalbuphine, naloxone, naltrexone, buprenorphine and etorphine.

In the past thabaine was believed to have no properties that were like those of morphine. However there are many studies that have found that thebaine has a considerable potential for dependence both psychological and physical when used in large doses for a long period of time.

Codeine

Naturally extracted from the poppy plant, codeine is used in hospitals as a narcotic pain-reliever and cough suppressant. It functions similar to morphine and hydrocodone. Moreover, when taken a small amount of codeine is converted to morphine in the body. However the mechanism of action of codeine is not known but just like morphine, codeine binds to opioid receptors in the brain. These receptors are important for transmitting the sensation of pain throughout the body and brain. Codeine increases tolerance to pain, decreasing discomfort, but the pain still is apparent to the patient. Despite its ability to suppress coughs and enable pain tolerance, it has the following side effects, noisy breathing, sighing, slow breathing with long pauses between breaths, drowsiness and blue colored lips.

Semi-synthetic opioids

This is a group of drugs that are naturally extracted from the poppy plant but are further processed before they are used. An example is heroine.

Heroine

Comes from the opium poppy but is further processed. When pure it is a white powder that has a bad taste. Some heroin is dark brown, and black tar heroin is either sticky or hard and looks like roofing tar. It has pain relieving properties. Unlike most pain relieving narcotics that are accepted in most states when prescribed by doctors, heroin is illegal in most countries basically because it is highly addictive and has quite grave side effects. Some of the withdrawal symptoms include; sleeplessness, bad chills and sweats, muscle pain, stomach cramps, nausea, vomiting, and diarrhea.

Synthetic opioids

These are opioids that are made in laboratories. They include;

Methadone

Methadone is used as a pain reliever and as part of drug addiction detoxification and maintenance programs and is only available from certified pharmacies. This drug helps reduce the severity of withdrawal symptoms that are suffered by heroin addicts when they stop using heroin. Some of its side effects include; rapid heart rhythm, severe dizziness and chest pain among others.

Oxycodone

This is an FDA approved drug for use in pain relief as well as suppressing coughs. This drug is a strong pain reliever and works better for both opioids moderate and severe pain. It increases tolerance to pain hence eliminating discomfort. It also causes sedation. May cause very severe side effects when mixed with alcohol. Cases of death have been reported.

Fentanyl

Fentanyl is an opioid medication that is used for anesthesia to help prevent pain after surgery or any other medical procedure that may result in moderate or severe pain. It is injected in the muscle or in the vain through IV. It is mostly used before surgery. Side effects include severe dizziness, drowsiness and impaired reactions.

Finally, you need more information to stay away from dependence on alcohol and drugs as these have crippled societies and that is why here at AWAREmed we are dedicated to finding the best solutions to addiction and dependence on substances. Dr. Dalal Akoury (MD) is always in the mood of helping any patient to be addiction free. Do not hesitate to call on her for help in managing any sort of chronic pain or any type of addiction as well as other diseases.

Type of Opioids, Their Uses and Side Effects

Benzodiazepine Withdrawal

October 3, 2014

Benzodiazepine Withdrawal and How to Help the Patient

Benzodiazepine The use of any other drug of abuse comes with some of the most undesired side effects. Before we go deep into this topic we should have at least a basic understanding of these terms.

Withdrawal- This term may have different meanings but to many it is associated with getting money from your bank account. That is right but here it means something completely different. Withdrawal in relation to drugs is a term that refers to the feelings of discomfort, distress, and uncontrolled desire for a substance that takes place when a person stops using the substance. For there to be withdrawal, a person must have used a certain substance for quite a good time that his entire body had become adapted to the substance. When a person has used a certain substance for a long time his body may become dependent on the substance to accomplish some critical functions of the body. When a body is metabolically adapted to the use of a certain drug, when a person stops using that drug he will suffer some defects. He will have physical symptoms of withdrawal and these may differ in severity. Some may be mild and flu like while some symptoms of withdrawal might be so severe and life threatening.

What is Benzodiazepine?

Benzodiazepine’s parent compound of several psychoactive drugs (e.g. nitrazepam, temazepam and diazepam) used as anxiolytics,sedatives and hypnotics; they do not specifically contraindicate local anaesthetics, but as they can cause drowsiness, ataxia, dysarthria andimpaired consciousness, their concomitant use could mask early signs of toxic effects of local anesthetics.

This drug was used in clinics mostly as a tranquilizer. However this drug has potential to be abused. These medicines should be used in a hospital setting or better yet with directions from a physician. However other people are using these drugs for their sedative and intoxicating purposes. Benzodiazepine are addictive drugs and when a person uses them for so long he may reach dependence, it is attempts to stop using these drugs after dependence that results in withdrawal. Just like with any other drug of abuse physical symptoms of withdrawal will appear when you stop using Benzodiazepine after using it for quite along time. There are myriads of symptoms that occur while you stop using these drugs but for this article we will handle just a few.

Some of the Withdrawal symptoms when one stops using Benzodiazepine

Seizure

Seizures are caused by abnormal electrical activity in the brain. However a people who have epilepsy are often considered having a seizure disorder this will require medication. Other factors that may cause seizures are low blood sugar level which is common in diabetic patients. Patients suffering from meningitis often suffer seizures as well. However using some drugs may lead to some dependence of brain cells on the drugs so much that when a person stops using the drugs then it may beckon abnormal electrical activity in the brain thereby causing seizures.

The outward effect of seizures can vary from uncontrolled jerking movement (tonic-clonic seizure) to as subtle as a momentary loss of awareness (absence seizure) in this state the patient may lay flat without even moving an inch.

Rebound Anxiety

When a person suffers anxiety disorders and walks into the hospital, the most likely drug that he will be prescribed will be the benzodiazepine. These drugs are known to work well in addressing anxiety disorders however these drugs have a share of the darker world too. They have other side effects that are quite serious. One of these serious side effects includes the rebound effect. When these drugs were used to cure anxiety disorders and then stopped the patient will become even more anxious which may in itself lead to even more problems. The disadvantage of using these drugs for anxiety is that you will become dependent on them so much as to cause rebound anxiety.

Insomnia

Typically insomnia is the lack of sleep. Insomnia is a symptom of a disease and not a disease in itself. Insomnia is often defined as inability to either initiate or maintain sleep or both. For anybody to have a sound sleep there are hormones that work. These hormones are subject to drug activities and this explains why Benzodiazepine may cause insomnia.

Intravenous Amino Acid Therapy for Benzodiazepine Withdrawal

What happens during addiction is that Neurotransmitters are damaged. There is need to restore the neurotransmitters if the normal functions of the body are to be reached. One fact however is that these neurotransmitters are made from amino acids and these amino acids control nearly every aspect of the neurotransmitters. Dependence or addiction on benzodiazepine destroys these neurotransmitters hence to help person overcome cravings for more of benzodiazepine among other withdrawal symptoms there is need to restore the neurotransmitters. Amino acid can be given intravenously to the patient, this is effective as IV delivery bypasses the digestive system hence effective in restoring the neurotransmitters. IV delivery of the amino acids helps even patients whose digestive systems have been affected by addiction to drugs, alcohol and other substances.

NAD and Intravenous Amino Acid Therapy for Benzodiazepine Withdrawal

Benzodiazepine Nicotinamide adenine dinucleotide (NAD) is a coenzyme derivative of vitamin B3 – otherwise known as niacin. This coenzyme is found in all living cells. It is a key metabolism agent as well as many other basic cellular processes. Addicts are often low in energy and because NAD is essential in energy production its supplementation can be of benefit to the addicts. When used in mega doses it helps in making detoxification more rapid. It is given in IV form to reduce the cravings for addictive substances in addicts without exploring replacement therapies. This method of treatment has been used for quite a good time and has been very successful especially on those addicted to prescription drugs like opiates, benzodiazepines and even on cocaine, alcohol and other drugs.

Drug Addiction is a vice that should be fought by all means that is why we at AWAREmed Health and Wellness Resource Center are committed to availing help to addicts and offering them a place to call home. It does not matter what kind of addiction you are wrestling with right now, just call on Dr. Dalal Akoury (MD) today and begin your journey to victory against addiction.

Benzodiazepine Withdrawal and How to Help the Patient

Proper use Opioids to Curb Addiction and Dependence

October 1, 2014

Better Use of Opioids to Curb Addiction and Dependence

opioids The opioid drugs have brought relief to many people that were suffering severe pain enough to even disable them. The use of these drugs however should be done with extreme caution as this is like a double aged knife. We talk of collateral damage here with this I mean that these drugs should be used in a manner that they are safe enough not to cause myriad problem such as addiction and dependence on these records. Today there are millions of Americans who depend on these opioid drugs to overcome what might otherwise be agonizing, crippling pain. However, each year, the numbers of people who have become addicted to these drugs rise. The very same drugs that help them to overcome the pain are poising a great danger in their lives needless to mention the use of these drugs has led to death of many Americans. The main cause of these deaths is overdose. Prescription opioid overdoses caused more than 16,000 deaths in the United States in the year 2010 alone. This is for times the number of deaths that were recorded in 1999 to have been caused by prescription opioid overdose. In the past it was not easy for both private and public health facilities to act on these unpleasant statistics but slowly they seem to lay strategies to curb the use of these opioid drugs and so far these strategies have shown positive results as very many lives have been saved not only in America but also in other continents.

The Centers for Disease Control and Prevention has cited Florida as one of the cities where the deaths have dropped owing to these strategies that have been employed by the health sector. The deaths dropped from 3201 as was in 2010 to 2666 in 2012. The report clarifies that most of these deaths were reduced due to reduction in prescription of these drugs to pain patients. There were fewer prescriptions to these opioid drugs as a result of in the policy that regulated the flow of these drugs. These policy changes led to a close of 250 of the state’s pill mills that were considered high volume pain medication dispensaries.

The United States remains far and away the world’s largest user of prescription opioids, with 259 million prescriptions written in 2012, according to the CDC — twice as many, per capita, as the next-largest consumer, Canada. A separate CDC report issued the same day as the Florida update showed that prescription rates vary widely among states. Now, when we take America out of the picture and we begin to find reasons why there are problems with the opioid medications we learn that one of the causes of these problems is;

Irresponsible prescription

Every patient entrusts his with the doctor, however in some situations this dependence may be abused either intentionally or unintentionally. Some doctors are opiophobiac and hence reluctant to give right doses to the patients while in some scenarios a patient may be handled by a doctor who is not experienced in pain treatment hence may either overdose or under dose the patient. Cases of overdose are a major cause of deaths from use of these pain drugs.

Another source of complication is, the patient may be afraid of these drugs as they are often portrayed negatively by the media. The fear of addiction and dependence may make a patient not to use the drugs as prescribed.

Due to the problems that were faced by both doctors and patients in dealing with the opioid medications, the universal precautions were developed to offer a structured rational approach to pain patients and serve “as a guide to start a discussion within the pain management and addictions communities. They are not promoted as complete precautionary measures but as a guide to opioid medications.

The difference between physical dependence, addiction and PSEUDO-ADDICTION

These three have different meanings. However they have always been confused causing fear among patients using these drugs. Physical dependence is the case that arises when a person has been using these drugs for some time. The body physically becomes dependent on these drugs so much that when you stop using them you will show signs of withdrawal. This is normal and happens with other medications not only with opiates.

Addiction on the other hand is a case when a person losses control of the drugs. He no longer can maintain the doses as prescribed but begins to take much more than the prescribed doses. In most cases those addicted to a drug will not accept that they are but will go through all hustles to satisfy their craving for the drug.

What is pseudo-addiction?

opioids When a pain patient on opioids begins behaving in a manner that most addicts do but in real sense he is not addicted, this is called pseudo-addiction. The patient will demand for more drugs because the doses he got have not settled the pain. They will even use more than the prescribed doses in a bid to cool the pain and are often early to request for more drugs since they overused the ones they were given to cool the pain . The difference between pseudo-addiction and addiction is the reason behind the need for more drugs; an addict needs more drugs to satisfy his craving while in pseudo-addiction a patient needs more drugs because of the pain.

You need more information to stay away from dependence on alcohol and drugs as these have crippled societies and that is why here at AWAREmed we are dedicated to finding the best solutions to addiction and dependence on substances. Dr. Dalal Akoury (MD) is always in the mood of helping any patient to be addiction free. Do not hesitate to call on her for help in managing any sort of chronic pain or any type of addiction as well as other diseases.

Better Use of Opioids to Curb Addiction and Dependence

Opiophilia Replaced By Opiophobia

October 1, 2014

Opiophilia Replaced By Opiophobia the Pendulum Is Again In Motion

Opiophobia There are certain phenomena in the medical field that are rather hard to understand. We were brought up knowing that opioids and like substances were bad and should be avoided at all costs and we did that but as we grew and each of us went his way in matters there are mysteries that we met. As everybody else chose careers I chose to be here practicing medicine and I tell here my perception of opiates and like substances were changed here we use them as drugs especially as pain management drugs. To many people this may sound irrational. How do you use a drug that has dangerous effects to treat an illness? Don’t worry we had the same questions and curiously we waited to have these mysteries unraveled. We use these drugs in doses that are only able to address the pain and for a time that may not cause any serious health problems. However as patients were put on these drugs the whole medical industry work up to the realization that the use of these drugs in most cases resulted in the patients being addicted to the drugs and hence demanded more and more of these drugs. These drugs are rewarding in nature and so patients that are put on these drugs will automatically tend to crave for them. That is when opiophilia became a disease to be fought from all corners to help patients on these drugs to evade addiction and dependence on these drugs.

What is Opiophilia?

Opiophilia is a love of opioids, the love for opioids may not begin as a choice but may begin gradually when a patient is prescribed opiates to help him in pain management. In the past the doctors had given a blind to the possibility of pain patients under opiate drugs to be addicted on these drugs as they believed that the dosage was not enough to make the develop dependence on these drugs. However as patients take these drugs they will become addicted as the drugs are rewarding in nature. This therefore means that before a doctor prescribes opiate to a chronic pain patient he should assess the patient and develop exit strategies that will help these patients avoid addiction.

Fortunately, the medical industry has fought opiophilia and better strategies have been put in place to ensure that patients on these drugs are safe. Opiophilia seems an already won battle. Apart from proper pain management by use of these drugs other natural ways of pain management have been embraced to help patients where necessary. These natural pain cures include Prolozone therapy, PRP and prolotherapy. These natural pain cures are now used worldwide to help patients with chronic pain.

The fight against opiophilia was won but that did not end all the problems associated with the use of opiates in managing pain in patients. Another disease came and replaced opiophilia and this is opiophobia.

Opiophobia is a disorder or affliction, so named because people affected have a great aversion to the use of prescription opioids for the treatment of pain, to the point where they will actually refuse to take or administer it. This is rather new disease in field of drugs and addiction. This term is also used to refer to instances when doctors fear or are unwilling to prescribe opioid medication to patients.

In most cases doctors who have had unwillingness to prescribe opioid medications are often counseled and so they go back to administer the drugs. Opiophobia should be addressed just as much as opiophilia since it is the opioid that goes deep in managing pain. This is because the only direct biologic pain-relief system in the human body is the endogenous opioid receptor system, consisting of endorphins and their tissue based action sites, or receptors. Using opioid based drug in pain offers instant relief and so the opiates still remain to be the best pain relief medication. The public as well as the doctors may be subject to opiophobia owing to the negative information that are spreading concerning the use of opiates in dealing with pain. The major concern of these groups is that they know that when a patient has used the opiates for a short term or long-term pain then he becomes addicted and will show symptoms of withdrawal once he stops using the drugs. This may be true but this is also true with other medications doesn’t a diabetic patient become dependent on insulin? Needless to mention several strategies have been put in place to ensure safe exit from the use of these drugs. When you are dependent on any drug for medical purposes. That is not abuse.

Because of opiophobia and opiophilia State regulators have been introducing legislation to severely curtail availability of opioid class of medication this unfortunately may be a disadvantage rather than an advantage as there are patients that are already dependent on these drugs needless to mention there is no alternative that has been put in place that can work effectively enough to replace opioid class of drugs in managing pain.

Exit strategy from opioid therapy

There is need for a safe exit strategy to help the patients evade any possible danger that may come from using the drug. However it is better for a doctor to formulate a safe exit strategy. He will be able to do so depending on such factors as; consistence of a patient’s behavior with drug addiction, patient’s willingness to cooperate with an outpatient-based opioid analgesic tapering plan, patient’s history with substances disorders. All these assessments will help the doctor to formulate a safer exit plan for the patient.

Here at AWAREmed we are dedicated to finding the best solutions to chronic illnesses and that is why Dr. Dalal Akoury (MD) is always in the forefront advocating for integrative medicine since it is only through integrative medicine that a person can be healed wholly. Do not hesitate to call on her for help in managing any sort of chronic pain as well as other diseases.

Opiophilia Replaced By Opiophobia the Pendulum Is Again In Motion

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