Side effects of Hydromorphone that cannot be ignored

Narcotic or opioid medications always come with a lot of side effects that range from mild to severe. You cannot ignore even mild side effects that continue to exist for a long time. You should immediately call your health care provider if you notice any unusual side effects that bother you. This article will illustrate side effects of Hydromorphone that cannot be ignored and need immediate medical attention

Major – Less Common side effects

In case you notice the below given side effects,, call your medical help immediately.

  • Blurred vision
  • Dry mouth
  • behavioral changes
  • chest discomfort or pain
  • mental or mood changes
  • fainting, dizziness or lightheadedness
  • convulsions
  • decreased urination
  • irregular, pounding, fast pulse or heartbeat
  • stiff neck
  • breathing problems
  • irregular or slow heartbeat
  • rapid breathing
  • severe stomach burning, cramping or pain
  • sunken eyes
  • suicidal thoughts
  • unusual tiredness
  • wrinkled skin
  • severe and continuous vomiting

Occurrence not known

  • confusion
  • dizziness
  • headache
  • cough
  • clammy or cold skin
  • bluish skin or lips
  • change in vision to see colors like yellow and blue the most
  • heart stops
  • decreased urination
  • weak or fast pulse
  • noisy breathing
  • painful urination
  • not breathing
  • appetite loss
  • sweating
  • unconscious
  • sleeping problems
  • chest tightness
  • no pulse or no BP
  • shallow, slow, fast or irregular breathing

Get emergency medical help in case you notice any of these symptoms of overdose

Overdose symptoms

  • no muscle movement or muscle tone
  • increased eyes sensitivity to light
  • unusual drowsiness or sleepiness
  • decreased responsiveness or awareness


Minor side effects

Some of the Hydromorphone side effects that need no medical attention are some minor side effects which go away with time as your body gets used to the medicine.  You can speak to your physician to know how to prevent or reduce these minor side effects. If you notice any of the minor side effects continue to exist for a long time, then call your doctor immediately.

More Common

  • nausea
  • problems with moving
  • joint pain
  • muscle stiffness or pain
  • troublesome bowel movement

Less Common

  • belching
  • diarrhea
  • sour or acid stomach
  • discouragement
  • back pain
  • muscles spasms
  • irritability
  • pain in legs and arms
  • trouble concentrating
  • unusual weight loss or weight gain
  • tingling of feet and hands
  • stomach pain, upset or discomfort
  • indigestion
  • heartburn
  • loss of pleasure or interest
  • feeling empty or sad
  • bloating feet, legs, arms or face
  • irritability

Some rare side effects are

  • double vision
  • being forgetful
  • clumsiness
  • crying
  • full feeling
  • extra heartbeats
  • hearing loss
  • increased appetite
  • muscles aches
  • passing gas
  • shivering
  • week pulse

In case you notice any symptoms that are unusual, it is always better to speak to your doctor and your doctor can advice you how to prevent or treat the side effects safely.

Hydromorphone drug interactions elaborated

While taking Hydromorphone, you should speak to your doctor about drug interactions related to Hydromorphone. Knowing about various drug interactions can help you to be alert for any unusual side effects that you may experience because of drug interactions. This article will help you know the Hydromorphone drug interactions.

Hydromorphone with CNS depressants

Using CNS depressants like general anesthetics, tranquilizers, phenothiazines and alcohol parallel with opioids can lead to added depressant effects. Hypertension, respiratory depression, coma or profound sedation can occur. When the combination of medications is observed, the dose of one or other medication needs to be reduced. Hydromorphone tablets should not be taken with alcohol. Hydromorphone can increase the neuromuscular blocking action and create high level of respiratory depression.

Hydromorphone with Mixed Antagonist/Agonist opioid analgesics

Antagonist analegesic/Agonist like butorphanol, nalbuphine, buprenophine, pentazocine should be examined with caution to the patient who is receiving or has received a session of therapy using pure opioid agonist anlegesic like hydromorphone. In such instances mixed antagonist analgesic/agonist can decrease the hydromorphone effect or lead to withdrawal symptoms.

Hydromorphone oral – artemether-lumefantrine (oral)

Hydromorphone oral can enhance the effect of artemether-lumefantrine(oral) by changing drug metabolism

Hydromorphone oral- selegiline hcl (oral)

Hydromorphone oral can enhance the toxicity of selegiline hcl (oral) through unknown mechanism. There should be a gap of 14 days between halting the use of MAO inhibiting medication and beginning Hydromorphone.

Hydromorphone- Tramadol

Check with your doctor before you use the combination of Hydromorphone and tramadol. Taking these medications together can enhance the risk of breathing problems, seizures and other serious side effects. If your health care provider prescribes the combination of these two medicines, you might need dose adjustments or certain special tests in order to use both medications safely. Speak to your doctor, if you have tremors, seizures, shallow breathing, speech problems, problems with walking or balance. Avoid driving till the time you know how the medication works for you. Also let your doctor know about any other medication you use including herbs and vitamins.

Hydromorphone- Lorazepam

Using Hydromorphone and lorazepam together can enhance the side effects such as drowsiness, dizziness, confusion and difficulty in concentrating. Some elderly people also experience impairment in judgment, thinking and motor coordination. Try to avoid consuming alcohol or limit the use of alcohol when you are on these medications. Do not engage yourself in activities that  need extra alertness such as driving.  In case you have any questions, speak to your doctor  and also let him know about all other medications you are using currently.

Taking two medications together does not necessarily or always mean that you should discontinue taking either of them. Speak to your  health care provider so that the drug interactions are managed well by him. Apart from drugs some other things that can interact with the drug are caffeine, nicotine (through cigarettes), street drugs or supplements that you use for various purposes. Let your physician know about these medications as they can also affect how Hydromorphone works for you. You need to follow doctor’s instructions in order to use the drugs safely.

Hydromorphone dosage information and treating overdose

Use Hydromorphone as prescribed by the doctor. Do not use in large doses or for a longer period than recommended by the doctor. This is important for old patients, who are often very sensitive to pain medication effects. Taking the medication in large amounts can lead to habit-forming or drug dependency.

Dosing Information

For extended-release tablets or capsules

Extended-release tablets or capsule forms of Hydromorphone are recommended for patients who are opioid tolerant only. If you are not sure whether you are tolerant to opioids or not, discuss with your doctor before you start using this medication.

There is a medication guide that comes with the medicine. Read the instructions carefully and follow them. In case you have any queries speak to your doctor.

Take the medicine the same time every day, with food or without food. Swallow the tablet as whole and do not chew, break or crush it. When using this tablet some portion of tablet can pass into stools, which is normal and you need to worry about that.

Do not shift from extended release to immediate release tablets unless your physician asks you to do so.

The dose of this medication will vary from person to person. Follow the instructions of your doctor and read the label carefully. The information given below includes average doses of Hydromorphone. If doctor has prescribed you a different dose, do not try to change the dose without doctor’s consultation.

Oral dosage – extended release form- capsules – for moderate- severe pain

For patients shifting from other narcotic drugs


The capsule is recommended once in a day. The first dose entirely depends on the amount of narcotic medication you are taking on a daily basis. Your doctor will suggest you the right dose and can increase the dose if required. For patients who shift from fentanyl transdermal, this medication should be taken at least after 18 hours of fentanyl patch removal.


For right use and the right dose you should consult your doctor.

Oral dosage – extended release form- tablets – for moderate- severe pain

For patients shifting from regular forms of Hydromorphone


The tablet is recommended once in a day. The total quantity of mg (milligrams) each day is exactly same as quantity of Hydromorphone that is used per day.


For right use and the right dose you should consult your doctor.


For patients shifting from regular forms of Hydromorphone


The capsule is recommended once in a day. The first dose entirely depends on the amount of narcotic medication you are taking on a daily basis. Your doctor will suggest you the right dose and can increase the dose if required. For patients who shift from fentanyl transdermal, this medication should be taken at least after 18 hours of fentanyl patch removal.


For right use and the right dose you should consult your doctor.

Oral dosage- Liquid form

For pain


At first – 2.5-10ML or 1-1/2 – 2 teaspoonful after every 3-6 hours as required.


For right use and the right dose you should consult your doctor.

Hydromorphone overdose treatment

Overdose of Hydromorphone can be fatal and if you notice any unusual symptoms call poison centre for help.

How effective is Hydromorphone in treating pain?

Hydromorphone is an opioid medication used to treat mild to severe pain. It is also known as a narcotic. The generic name is Hydromorphone and brand name is Exalgo, Dilaudid-5 and Dilaudid.

This medication in its extended form is used as 24 hours treatment medicine to treat mild to severe pain.

Some important information

Hydromorphone can stop or slow your breathing.  do not use this  medication in excess amounts or for a longer period than prescribed. do not break, crush or open the pill available in extended release form. swallow the pill as whole to avoid life threatening complications. Hydromorphone can cause drug dependency even through regular doses. Do not share the medicine with others who have a history of drug addicition or drug abuse and store the medicine in a place where others cannot have access to the medicine.

Misuse of any narcotic drug can lead to overdose, death or addiction, especially in people who use the medication without doctor’s prescription or in children. If you are pregnant you should tell your doctor as Hydromorphone can lead to withdrawal symptoms in unborn baby, which can be fatal too.

Do not combine alcohol with Hydromorphone as it can even lead to death.

What should I ask my doctor before using Hydromorphone?

You should avoid taking this medicine if you are allergic to Hydromorphone or any other  narctotic medicine or if you have

  1. blockage in intestines or stomach
  2. severe breathing problems or asthma
  3. paralytic ileus or bowel problems

Avoid using Hydromorphone if you had used MAO inhibitor in last 14 days. There are chances of harmful drug interactions. Some medicines interact with Hydromorphone and lead to a serious medical condition known as serotonin syndrome. Make sure you inform your doctor if you are taking medicines for migraine, depression, Parkinson’s disease, infections, medicines for preventing vomiting or nausea, headaches or mental illness. Ask your doctor before making changes in dose and frequency of medciations you are taking.

Your doctor may not advice you to use Hydromorphone if you are not tolerant to the medication or never being treated with any other narcotic medicine for pain. Speak to your doctor if you are not tolerant to opioid medication.

To ensure that Hydromorphone is safe for you tell your physician if you have

  • lung disease or breathing problem
  • seizures, brain tumor, head injury in the past.
  • history of mental illness, addiction or drug abuse
  • kidney or liver disease
  • sulfite allergy
  • urination problems
  • disorders related to adrenal gland or Addison’s disease
  • problem with pancreas, gallbladder or thyroid

Is Hydromorphone addictive?

Hydromorphone is a common drug associated with drug abuse. Since it acts quite fast to treat pain, many people get addicited to the medicine easily. Many people who face addicition problem often visit rehabs meant for treating opiates addicition. This helps them get rid of the urge to use the medicine and eliminate addiction completely.

Taking the medicine in excess to get desired effect can cause drug addiction. Avoid taking medication in large amounts.

Effects of Hydromorphone on pregnancy and breastfeeding

Pregnancy and breastfeeding is a completely different phase wherein a woman not only takes good care of her, but also cares for her baby. During this phase, apart from healthy and nutritional diet, she should take care of medications that she is using and how the drugs going to affect her baby.

In this article we will discuss about the effects of hydromorphone on pregnancy and breastfeeding.

Hydromorphone and pregnancy

Hydromorphone intersect the placenta causing fetal exposure. If you are pregnant and using Hydromorphone, you should tell your doctor to know how this drug is going to affect your pregnancy. Hydromorphone should be used during pregnancy only if the possible benefits are higher than the risks. If you are using Hydromorphone regularly during your pregnancy, there are chances that your baby may experience harmful withdrawal symptoms post birth.

The expecting mothers who take Hydromorphone regularly before their delivery can become dependent on the drug and the withdrawal signs may include

  • Tremors
  • Hyperactive reflexes
  • Excessive crying
  • Sneezing
  • Yawning
  • Fever
  • Vomiting
  • Irritability
  • Increased stools

There are still no best methods discovered to manage withdrawal. To support treatment supportive care is given along with certain medications.

Hydromorphone and breastfeeding

Low levels of Hydromorphone are found in breast milk, which can lead to respiratory problems in new born babies. Hydromorphone should not be taken while breastfeeding as it is secreted in breast milk and can harm the baby. There is limited data available indicating that low doses of Hydromorphone are secreted in breast milk. Mothers using narcotic drugs during breastfeeding often results in infant death, drowsiness and depression of central nervous system. New born are sensitive to even low doses of narcotic drugs.

While breastfeeding it is better to manage pain using non narcotic medications and restrict the use of Hydromorphone for a couple of days to low doses and monitor the health of your baby closely.

If your baby shows some unusual signs like increased sleepiness, breathing problems, difficulty in breastfeeding or limpness, immediately contact your physician.

Sometimes nursing mothers have to undergo surgery after birth of their baby and they need narcotic analgesics during their surgery. They can arrange for nursing their new born prior to their surgery so that they can take some time to recover. They can consult their lactating consultant to help them suggest supplementary feedings or helping her arrange for a breast pump for temporary use. She can also opt to freeze supply of breast milk before undergoing a surgery.

Once the nursing mother recovers from surgery she can take care of her baby and be alert. She can also consult her doctor to prescribe her low doses of pain medications.

It is always better to be safe and not use narcotic medications during breastfeeding or pregnancy. You can also look for other alternative non narcotic drugs to treat pain. If you want to use narcotic drugs safely, consult your doctor for the right dosage. It will help you avoid complications that can be harmful for you and your baby.

Side effects of Dilaudid (hydromorphone)

Dilaudid( hydrochloride,hydromorphone) is an analgesic opioid and morphine’s hydrogenated ketone. The side effects of hydromorphone (Dilaudid) are as below

You should ask for emergency help if you notice the signs of allergic reactions like breathing problems, hives, swelling on tongue, lips, face or your throat.

Call your health care provider if notice side effects like

  1. Seizures
  2. Confusion, drowsiness, weakness
  3. Feel like urinating
  4. Fluttering in chest or pounding heartbeats

Some of the side effects that are less serious are

  • Itching
  • Sweating
  • Drowsiness
  • Dizziness
  • Double or blurred vision
  • Constipation, nausea, constipation, stomach pain, diarrhea
  • Dry mouth
  • Sleeping problems

The most important that you need to know about hydromorphone is that it is a habit forming drug and needs to be used by only those whom the doctor prescribes. Keep the medicine in a safe place so that others are not able to reach.

Avoid consuming alcohol as it can lead to dangerous side effects even death which occurs if you consume alcohol in combination with any narcotic medicine for pain. Also check the medicine labels that you are using other than hydromorphone and food that you are eating to make sure it doesn’t contain alcohol.

Avoid taking hydromorphone in higher doses or for a longer period than what your doctor has suggested. Let your doctor know if the medication isn’t working for you or stopped working. The medication can also impact your reaction or thinking. Do not drive or operate machinery as the hydromorphone can affect in many ways that you might not be aware of.

Dilaudid(hydromorphone)  some of the side effects like dizziness, swelling, drowsiness, dry mouth, flushing will decrease after using medication for a while. You can reduce the lightheadedness and dizziness by getting up slowly when you rise from lying, sitting position.

The side effects associated with dlaudid( oral tablets or liquid) include apnea and respiratory depression. to some extent, cardiac arrest, respiratory shock or respiratory arrest, circulatory depression etc., some side effects that are adverse can be dysphoria, pruritus euphoria etc.,

Some cardiovascular side effects are faintness, hypertension, chills, hypotension, tachycardia, bradycardia, syncope, palpitation etc., respiratory effects are laryngospasm and bronchospasm.

Gastrointestinal side effects are cramps, changes in taste, biliary tract spasm, constipation. Some genitourinary effects are ant diuretic effects, urinary retention, hesitancy etc., dermatologic effects include skin rashes, urticaria, and diaphoresis.

Some of the effects like constipation you can easily prevent by eating fiber rich diet, drink  a lot of water and exercise regularly. You can deal with some side effects which also go with time if you are using the medication for a short period. Still any other side effect which you feel is severe and needs medical help should immediately be taken care of.

We all are dependent on drugs and narcotic drugs need extra care, to get maximum benefit from these drugs we should avoid overdose and dependency on the drug. The drug can help if used in a right way.

How to use Hydromorphone Injection

Hydromorphone is useful in relieving moderate type of pain to severe pain. It is a narcotic pain reliever. It works on certain brain centers in order to provide you relief from pain.

Using hydromorphone injection

Depending on the specific product recommended to you, hydromorphone is given form of injection under your skin, through a muscle or slowly into your vein. You need to use exactly how your doctor has advised you to use. Learn the right way to give hydromorphone injections. In case of any queries you can speak to your pharmacist or doctor.

Before using, check the product for any discoloration or particles. If either of the two is present, avoid using the liquid. Before you inject each hydromorphone dose, clean injection site with the help of rubbing alcohol and if the medication is given under your skin or into your muscle, it is essential to change injection location with every dose in order to avoid problematic areas under your skin.

Use syringes or needles just once. Learn how to dispose medical supplies and needles safely. Some brands of hydromorphone medication comprise of more than one dose while some contain just one dose. Read about the usage of product that your pharmacist has prescribed and if the doctor has advised you to use brand containing only one dose, use the same for just single dose only. If there is any medication that remains in the package do not save it. Speak to your pharmacist to get more information.

The dosage solely depends on your response to the treatment and medical condition. Pain medications always work best if you use them, when initial sign of pain is noticed. If you do not take action till your pain worsens, the medications might not work well. Do not try to increase your dose than prescribed, do not use medication constantly or prolong the use of medication than your doctor has prescribed. Stop the medication properly as directed by the doctor.

If you are taking narcotic medications that are long-acting or using narcotic patches for pain that is ongoing, this medication needs to be used only for sudden pain and needs to be taken only as you need it. The medications also come with withdrawal reactions especially when you use the medication regularly for a prolonged period or take high doses of medication. The withdrawal symptoms include sweating, yawning, fast breathing, watering eyes, mood or mental changes or Goosebumps and these symptoms can occur in case you stop taking the medicine suddenly. To prevent these possible withdrawal reactions, speak to your doctor as he/she can reduce the dose slowly.

Apart from its benefits, the medication can rarely cause addiction. The risk can increase if you have history of drug or alcohol abuse. To reduce the risk of addiction, take this medicine as prescribed by your doctor.

Sometimes using this medication for long term also doesn’t work well for you. Your doctor may suggest increase in dose or change your current medication.

Treating Patients with Addictive Disorders

Safe and effective pain treatment is especially important for persons with a drug use history because inadequate treatment or lack of treatment for pain may have problematic consequences, such as illicit drug use (e.g., heroin), misuse of prescription opioids and other pain medications (e.g., benzodiazipines), psychiatric distress, functional impairment and a tendency for health providers to attribute pain complaints and requests for pain medication to an addictive disorder rather than to a pain disorder (Gureje, et al., 2001;Scimeca, Savage, Portenoy, & Lowinson, 2000).

Undertreatment of pain among addicted persons may lead to the adverse medical, social and personal consequences associated with continued drug-seeking behavior (Savage, 1996).

Pain complaints may be most problematic among persons with opioid addiction, as this group may have lower tolerance for pain than other addicted populations (Compton, 1994; Compton, Charuvastra, & Ling, 2001).

Pain and opioid addiction may be further intertwined among persons who have a history of abusing controlled opioid pain medications, such as oxycodone or hydrocodone.

Opioid Treatment for Chronic Pain

Opioid therapy is the mainstay approach for the treatment of moderate to severe pain associated with cancer or other serious medical illnesses (Patt & Burton, 1998; World Health Organization, 1996). Although the use of opioid analgesics for the treatment of CNMP has been increasing in recent years (Joranson, Ryan, Gilson & Dahl, 2000) and has been endorsed by numerous professional societies (AAPM, APS, 1997; American Geriatric Society, 1998; Pain Society, 2004), the use of opioids remains controversial due to concerns about side effects, long-term efficacy, functional outcomes, and the potential for drug abuse and addiction. The latter concerns are especially evident in the treatment of CNMP patients with substance use histories (Savage, 2003).

Other concerns that may contribute to the hesitancy to prescribe opioids may be related to perceived and real risks associated with regulatory and legal scrutiny during the prescribing of controlled substances (Office of Quality Performance, 2003). These concerns have propelled extensive work to develop predictors of problematic behaviors or frank substance abuse or addiction during opioid therapy. Questionnaires to assist in this prediction and monitoring have been developed and used in research and field trials. Examples include the Prescription Drug Use Questionnaire (PDUQ; Compton et al., 1998); the Pain Assessment and Documentation Tool (PADT; Passik et al., 2004) and the Current Opioid Misuse Measure (COMM; Butler et al., 2007). These instruments are not used in practice settings at this time.

Narrative reports on the use of opioids for CNMP have underscored the effectiveness of opioid therapy for selected populations of patients and there continues to be a consensus among pain specialists that some patients with CNMP can benefit greatly from long-term therapy (Ballantyne & Mao, 2003; Trescot et al., 2006). This consensus, however, has received little support in the literature. Systematic reviews on the use of opioids for diverse CNMP disorders report only modest evidence for the efficacy of this treatment (Trescot et al., 2006; 2008). For example, a review of 15 double-blind, randomized placebo-controlled trials reported a mean decrease in pain intensity of approximately 30% and a drop-out rate of 56% only three of eight studies that assessed functional disturbance found improvement (Kalso, Edwards, Moore, & McQuay, 2004).

A meta-analysis of 41 randomized trials involving 6,019 patients found reductions in pain severity and improvement in functional outcomes when opioids were compared with placebo (Furlan, Sandoval, Mailis-Gagnon, & Tunks, 2006). Among the 8 studies that compared opioids with non-opioid pain medication, the six studies that included so-called “weak” opioids (e.g., codeine, tramadol) did not demonstrate efficacy, while the two that included the so-called “strong” opioids (morphine, oxycodone) were associated with significant decreases in pain severity. The standardized mean difference (SMD) between opioid and comparison groups, although statistically significant, tended to be stronger when opioids were compared with placebo (SMD = 0.60) than when strong opioids where compared with non-opioid pain medications (SMD = 0.31). Other reviews have also found favorable evidence that opioid treatment for CNMP leads to reductions in pain severity, although evidence for increase in function is absent or less robust (Chou, Clark, & Helfand, 2003; Eisenberg, McNicol, & Carr, 2005).

Little or no support for the efficacy of opioid treatment was reported in two systematic reviews of chronic back pain (Deshpande, Furlan, Mailis-Gagnon, Atlas, & Turk, 2007; Martell, et al., 2007). Because patients with a history of substance abuse typically are excluded from these studies, they provide no guidance whatsoever about the effectiveness of opioids in these populations.

Adding further to the controversy over the utility of opioid analgesics for CNMP is the absence of epidemiological evidence that an increase in the medical use of opioids has resulted in a lower prevalence of chronic pain. Noteworthy is a Danish study of a national random sample of 10,066 respondents (Eriksen, Sjøgren, Bruera, Ekholm, & Rasmussen, 2006).

Denmark is known for having an extremely high national usage of opioids for CNMP and this use has increased by more than 600% during the past two decades (Eriksen, 2004). Among respondents reporting pain (1,906), 90% of opioid users reported moderate to very severe pain, compared with 46% of non-opioid users; opioid use was also associated with poor quality of life and functional disturbance (e.g., unemployment).

Although this epidemiological study may be interpreted as demonstrating that opioid treatment for CNMP has little benefit, the authors acknowledge that these disquieting findings do not indicate causality and could be influenced by the possibility of widespread undertreatment, leading to poorly managed pain.

This latter interpretation is supported by a commentary on the Ericksen et al. study (Keane, 2007). Keane notes that among the 228 pain patients receiving opioids only 57 (25%) were using strong opioids, while the remainder was using weak opioids. European (as well as United States) clinical guidelines generally recommend long-acting formulations of strong opioids for the treatment of chronic moderate to severe pain, which may be supplemented with short-acting opioids for breakthrough pain (Pain Society, 2004; OQP, 2003; Gourlay, 1998; Vallerand, 2003; Fine & Portenoy, 2007).

The possibility of inappropriate opioid treatment is further supported by another Danish study that assigned pain patients who were on opioid therapy to either a multidisciplinary pain center (MPC) or to general practitioners (GP) who had received initial supervision from the MPC staff (Eriksen, Becker, & Sjegren, 2002). At intake, a substantial number of patients in both groups were apparently receiving inappropriate opioid therapy for chronic pain (60% were being treated with short-acting opioids and 49% were taking opioids on demand). At the 12 month follow-up, 86% of MPC patients were receiving long-acting opioids and 11% took opioids on demand.

There was no change in the administration pattern in the GP group. These findings suggest that a significant proportion of opioid-treated CNMP patients may be receiving inappropriate opioid treatment and that educating general practitioners in pain medicine may require more than initial supervision.

It is generally acknowledged that there is a wide degree of variance in the prescribing patterns of opioids for chronic pain (Lin, Alfandre, & Moore, 2007; Trescot et al., 2006). Some opioid treatment practices persist despite evidence that they might be harmful or have little benefit, such as the over-prescribing of propoxyphene among the elderly (Barkin, Barkin, & Barkin, 2006; Singh, Sleeper, & Seifert, 2007). Nursing home patients being treated with opioids have been found to be inadequately assessed for pain and to be more likely treated with short-acting rather than long acting opioids (Fujimoto & Coluzzi, 2000). A substantial number of physicians are reluctant or unwilling to prescribe long-acting opioids to treat CNMP, even when it may be medically appropriate (Nwokeji, et al., 2007).

Controversy about the long-term effectiveness of opioid treatment also has focused on the potential clinical implications of opioid-induced hyperalgesia. As noted earlier, exposure to opioids can result in an increased sensitivity to noxious stimuli in animals, and an increased perception of some types of experimental pain in humans (c.f., Koppert & Schmeltz, 2007; Angst & Clark, 2006). Anecdotal reports of hyperalgesia occurring with very high or escalating doses of opioids (Angst & Clark, 2006) has been viewed as a clinical correlate of these experimental findings.

The extent to which this phenomenon is relevant to the long-term opioid therapy administered to most patients with chronic pain is unknown. Although experimental evidence suggests that opioid-induced hyperalgesia might limit the clinical utility of opioids in controlling chronic pain (Chu, Clark, & Angst., 2006), there have been no reports of observations in the clinical literature to suggest that it should be a prominent problem. More research is needed to determine whether the physiology underlying opioid-induced hyperalgesia may be involved in a subgroup of patients who develop problems during therapy, such as loss of efficacy (tolerance) or progressive pain in the absence of a well defined lesion.

Outcome studies of long term use of opioids are compromised by methodological limitations which make it difficult to acquire evidence of efficacy (Noble, Tregear, Treadwell, & Schoelles, 2007). Methodological limitations may be unavoidable because of the ethical and practical challenges associated rigorous studies such as randomized controlled trials. Guidelines for opioid therapy must now be based on limited evidence; future evidence may be acquired by utilizing other study designs (Noble et al., 2007) such as practical clinical trials (Tunis, Stryer, & Clancy, 2003). These studies should include at least three criteria to reflect a positive treatment response: i.e., reduction of pain severity (derived from subjective reports or scores on pain scales), recovery of function (improved scores on instruments that measure some aspect of function), and quality of life.

Guidelines for the use of opioids for the treatment of chronic pain have been published (AAFP et al., 1996–2002; OQP, 2003), and recent guidelines have emphasized the need to initiate, structure and monitor therapy in a manner that both optimizes the positive outcomes of opioid therapy (analgesia and functional restoration) and minimize the risks associated with abuse, addiction and diversion (Portenoy et al., 2004). These guidelines discuss patient selection (highlighting the likelihood of increased risk among patients with prior histories of substance use disorders), the structuring of therapy to provide an appropriate level of monitoring and a presumably lessened risk of aberrant drug-related behavior, the ongoing assessment of drug-related behaviors and the need to reassess and diagnose should these occur, and strategies that might be employed in restructuring therapy should aberrant behaviors occur and the clinician decide to continue treatment.

They also note that therapy should be undertaken initially as a trial, which could lead to the decision to forego more therapy, and that an “exit strategy” must be understood to exist should the benefits in the individual be outweighed by the burdens of treatment.

The relatively recent recognition that guidelines for the opioid treatment of chronic pain must incorporate both the principles of prescribing as well as approaches to risk assessment and management may represent an important turning point for this approach to pain management. Acknowledging that prescription drug abuse has increased during the past decade, a period during which the use of opioid therapy by primary care physicians and pain specialists has accelerated, pain specialists and addiction medicine specialists now must collaborate to refine guidelines, help physicians identify the subpopulations that can be managed by primary care providers, and discover safer strategies that may yield treatment opportunities to larger numbers of patients.

Terminology of Opioid Abuse: Dependence, Tolerance, Addiction

Concerns that addiction is a frequent iatrogenic consequence of the medical use of opioids may partially be attributed to confusion over terminology, as a well as failure to recognize that both addiction and chronic pain have a multifactorial etiology. In an effort to develop universal agreement on terminology related to addiction, the American Academy of Pain Medicine (AAPM), the American Pain Society (APS), and the American Society of Addiction Medicine (ASAM) approved a consensus document that clarified this terminology (ASAM, 2001; Savage, 2003).

According to the consensus document, tolerance is defined as a decreased subjective and objective effect of the same amount of opioids used over time, which concomitantly requires an increasing amount of the drug to achieve the same effect. Although tolerance to most of the side effects of opioids (e.g., respiratory depression, sedation, nausea) does appear to occur routinely, there is less evidence for clinically significant tolerance to opioids– analgesic effects (Collett, 1998; Portenoy et al., 2004). For example, there are numerous studies that have demonstrated stable opioid dosing for the treatment of chronic pain (e.g., Breitbart, et al., 1998; Portenoy et al., 2007) and methadone maintenance for the treatment of opioid dependence (addiction) for extended periods (Strain and Stitzer, 2006).

However, despite the observation that tolerance to the analgesic effects of opioid drugs may be an uncommon primary cause of declining analgesic effects in the clinical setting, there are reports (based on experimental studies) that some patients will experience worsening of their pain in the face of dose escalation (Ballantyne, 2006). It has been speculated that some of these patients are not experiencing more pain because of changes related to nociception (e.g. progression of a tissue-injuring process), but rather, may be manifesting an increase in pain as a result of the opioid-induced neurophysiological changes associated with central sensitization of neurons that have been demonstrated in preclinical models and designated opioid-induced hyperalgesia (Mao, 2002; Angst & Clark, 2006).

Analgesic tolerance and opioid-induced hyperalgesia are related phenomena, and just as the clinical impact of tolerance remains uncertain in most situations, the extent to which opioid-induced hyperalgesia is the cause of refractory or progressive pain remains to be more fully investigated. Physical dependence represents a characteristic set of signs and symptoms (opioid withdrawal) that occur with the abrupt cessation of an opioid (or rapid dose reduction and/or administration of an opioid antagonist). Physical dependence symptoms typically abate when an opioid is tapered under medical supervision. Unlike tolerance and physical dependence which appear to be predictable time-limited drug effects, addiction is a chronic disease that “represents an idiosyncratic adverse reaction in biologically and psychosocially vulnerable individuals” (ASAM, 2001).

The distinction between physical dependence and addiction is not always made clear in the pain literature (Ferrell, McCaffery, Rhiner, 1992). Most patients who are administered opioids for chronic pain behave differently from patients who abuse opioids and do not ever demonstrate behaviors consistent with craving, loss of control or compulsive use (e.g., Cowan et al., 2001). Of course, pain and addiction are not mutually exclusive and some patients who are treated for pain do develop severe behavioral disturbances indicative of a comorbid addictive disorder.

Some patients who are treated with opioids for pain display problematic behaviors that, on careful assessment, do not reflect addiction, but rather, appear to relate to a different process. This may be another psychiatric disorder associated with impulsive drug-taking, an unresolved family issue, a disorder of cognition, or criminal intention. In addition, there appear to be some patients who engage in problematic behaviors related specifically to desperation about unrelieved pain. The term pseudoaddiction was coined to describe the latter phenomenon (Weissman & Haddox, 1989).

Behaviors that may represent pseudoaddiction and behaviors that reflect addiction or some other serious psychopathology can occur simultaneously, and presumably, one type of phenomenon may incite the others. The diagnosis of these and other conditions may be challenging and requires a careful assessment of clinical phenomenology, specifically a range of drug-related behaviors during treatment with a potentially abusable drug (Portenoy, 1994, Lue, Passik, & Portenoy, 1998).

The term aberrant drug-related behaviors has been used to indicate the broad array of problematic nonadherence behaviors (Passik, Kirsh, Donaghy, & Portenoy, 2006), the nature of which is uncertain until a diagnosis can be developed based on astute clinical assessment. Some aberrant drug-related behavior strongly suggests the existence of addiction. These may include the use of alternative routes of administration of oral formulations (e.g., injection or sniffing), concurrent use of alcohol or illicit drugs, and repeated resistance to changes in therapy despite evidence of adverse effects; examples of aberrant behavior less suggestive of addiction are drug hoarding during periods of reduced symptoms, occasional unsanctioned dose escalation, and aggressive complaining about the need for more drugs (Portenoy, 1994).

How Opioids Work and what is Opioid receptors ?

Opioids are a type of narcotic pain medication. They can have serious side effects if you don’t use them correctly.

When you have a mild headache or muscle ache, an over-the-counter pain reliever is usually enough to make you feel better. But if your pain is more severe, your doctor might recommend something stronger — a prescription opioid.

Opioid receptors have been targeted for the treatment of pain and related disorders for thousands of years, and remain the most widely used analgesics in the clinic. Mu (μ), kappa (κ), and delta (δ) opioid receptors represent the originally classified receptor subtypes, with opioid receptor like-1 (ORL1) being the least characterized. All four receptors are G-protein coupled, and activate inhibitory G-proteins. These receptors form homo- and hetereodimeric complexes, signal to kinase cascades, and scaffold a variety of proteins.

Opioids look like chemicals in your brain and body that attach to tiny parts on nerve cells called opioid receptors. Scientists have found three types of opioid receptors: mu, delta, and kappa (named after letters in the Greek alphabet). Each of these receptors plays a different role. For example, mu receptors are responsible for opioids’ pleasurable effects and their ability to relieve pain.

Opioids act on many places in the brain and nervous system, including:

  • the limbic system, which controls emotions. Here, opioids can create feelings of pleasure, relaxation, and contentment.
  • the brainstem, which controls things your body does automatically, like breathing. Here, opioids can slow breathing, stop coughing, and reduce feelings of pain.the parts of the brain that are affected
  • the spinal cord, which receives sensations from the body before sending them to the brain. Here too, opioids decrease feelings of pain, even after serious injuries.

Whether it is a medication like Vicodin or a street drug like heroin, the effects of opioids (and many other drugs) depend on how much you take and how you take them. If they are injected, they act faster and more intensely. If opioids are swallowed as pills, they take longer to reach the brain and are much safer.

the parts of the brain that are affected

Opioids attach to receptors in the brain. Normally these opioids are the endogenous variety that are created naturally in the body. Once attached, they send signals to the brain of the “opioid effect” which blocks pain, slows breathing, and has a general calming and anti-depressing effect. The body cannot produce enough natural opioids to stop severe or chronic pain nor can it produce enough to cause an overdose.

opioids can activate receptors because their chemical structure mimics that of a natural neurotransmitter. This similarity in structure “fools” receptors and allows the drugs to lock onto and activate the nerve cells. Although these drugs mimic brain chemicals, they don’t activate nerve cells in the same way as a natural neurotransmitter, and they lead to abnormal messages being transmitted through the network.

Opioids target the brain’s reward system by flooding the circuit with dopamine. Dopamine is a neurotransmitter present in regions of the brain that regulate movement, emotion, cognition, motivation, and feelings of pleasure. The overstimulation of this system, which rewards our natural behaviors, produces the euphoric effects sought by people who misuse drugs and teaches them to repeat the behavior.

Our brains are wired to ensure that we will repeat life-sustaining activities by associating those activities with pleasure or reward. Whenever this reward circuit is activated, the brain notes that something important is happening that needs to be remembered, and teaches us to do it again and again, without thinking about it. Because drugs of abuse stimulate the same circuit, we learn to abuse drugs in the same way.

Opioid drugs work by binding to opioid receptors in the brain, spinal cord, and other areas of the body. They reduce the sending of pain messages to the brain and reduce feelings of pain.

Opioids are used to treat moderate to severe pain that may not respond well to other pain medications.

Some types of opioid drugs include:

  • codeine (only available in generic form)
  • fentanyl (Actiq, Duragesic, Fentora)
  • hydrocodone (Hysingla ER, Zohydro ER)
  • hydrocodone/acetaminophen (Lorcet, Lortab, Norco, Vicodin)
  • hydromorphone (Dilaudid, Exalgo)
  • meperidine (Demerol)
  • methadone (Dolophine, Methadose)
  • morphine (Astramorph, Avinza, Kadian, MS Contin, Ora-Morph SR)
  • oxycodone (OxyContin, Oxecta, Roxicodone)
  • oxycodone and acetaminophen (Percocet, Endocet, Roxicet)
  • oxycodone and naloxone (Targiniq ER)

Your doctor can prescribe most of these drugs to take by mouth. Fentanyl is available in a patch. A patch allows the medication to be absorbed through the skin.