Opioids: Uses, common brands, and safety info

Pain management is a topic receiving a lot of attention in today’s healthcare industry. One of the most common reasons people go to the drugstore is to get pain medicine. Drugs that alleviate pain are called analgesics. Analgesics are available over-the-counter and by prescription. So, how do you know which analgesic is appropriate for your pain? This is an important question for effective pain management.

For intense pain—after surgery or a traumatic injury, for example—opioids are the most effective analgesics for pain relief. If you have ever broken a bone or had your wisdom teeth removed, you may be familiar with some brand-name prescription opioids such as Percocet, Lortab, or Tylenol #3. In this article, we will review important details about opioid medications–including their properties, common brand names, and safe use.

What are opioids?

Opioids are a class of drugs used to relieve moderate to severe pain. Opioids are also called narcotics. The term “narcotic” is used by some people to refer to illicit drugs, but technically it refers to opioids. Opioids are legal when purchased with a prescription issued in accordance with federal and state laws.

Opioids are naturally occurring; opium, morphine, and codeine are derived from the Asian opium poppy plant. Synthetic opioids are modified in a lab. These include oxycodone, hydrocodone, fentanyl, and many others.

How do opioids work?

There are naturally occurring opioids found in our body called endorphins. Endorphins bind and activate certain receptors in the nervous system. Collectively, the different receptors are referred to as opioid receptors. When activated, the receptors block signals traveling to the brain that register pain. In addition to dulling pain, this can create a feeling of calmness and happiness. 

A common situation in which endorphins create this effect is during exercise. Opioid drugs mimic the body’s endorphins by activating the opioid receptors to an even greater degree. Some opioid drugs have their effect very quickly. These are used to treat breakthrough pain (severe pain that lasts for a relatively short time). 

Extended-release opioids work more slowly but for longer periods. These are often used to help lower pain scores throughout the day or night while decreasing the use of immediate-release opioids, which are more likely to be habit-forming.

What are opioids used for?

Opioids are used to treat moderate to severe pain. The following medical scenarios are commonly associated with opioid use:

• Cancer such as leukemia, prostate cancer, colon cancer, breast cancer, and others

• Palliative care

• Sickle cell crisis

• Arthritis (including psoriatic arthritis, rheumatoid arthritis, and osteoarthritis) 

• Opioid use disorder

• Sciatica

• Post-surgical pain

• Kidney stones

• Migraine headaches

• Musculoskeletal pain (such as lower back pain)

• Opioids in small doses are combined with other ingredients to treat cough or diarrhea.

Who can take opioids?

Infants, children, and adolescents

Opioids are prescribed for children and adolescents to relieve pain after surgery. Not all opioids are appropriate for this age group. Fentanyl, morphine, and methadone are used in all ages. Oxycodone and hydromorphone are not indicated for use in children younger than 6 months of age. Hydrocodone is not indicated for use in patients under 2 years of age. 

In 2017, the FDA placed a restriction on the use of codeine and tramadol in children, due to serious breathing complications. Specifically, codeine should not be used in children younger than 12 years, and tramadol should not be used in children younger than 18 years. Meperidine is not recommended for use in pediatric patients due to the accumulation of a toxic metabolite that can cause toxicity in seizures, particularly in those with poor kidney function. 

Adults

Opioids are safe to use in adults if they are taken for a short period and as prescribed by a healthcare provider. The most common side effects are the result of central nervous system (CNS) depression, which include drowsiness, sedation, and psychomotor impairment. Some patients may experience memory impairment or confusion. All people using opioids should understand the inherent risk for opioid dependence, addiction, and overdose. These risks are increased when opioids are misused.

Seniors

Opioid use should also be avoided when possible in the geriatric population. Using opioids in the elderly greatly increases the risk for falls, as they can cause ataxia, impaired psychomotor function, and syncope. If no safe alternatives are available, opioids may be prescribed at the lowest effective dose—typically 25% to 50% of the adult dose—and then adjusted based on tolerance.

Pets

Two opioids have FDA approval for use in animals; buprenorphine is approved for use in cats, while butorphanol is approved for use in cats, dogs, and horses. Veterinarians will commonly prescribe opioids ‘off-label’ for use in pets. For example, hydrocodone is used to treat pain and cough in dogs. Tramadol is frequently prescribed to manage pain in dogs and cats.

Are opioids safe?

All opioids carry some risk for opioid addiction, abuse, and misuse. The National Institute on Drug Abuse reports that more than 2 million Americans abuse opioids and that more than 90 opioid overdose deaths occur in America daily. Widespread opioid misuse and over-prescribing is a major public health crisis commonly referred to as the opioid epidemic. To minimize the risk of opioid abuse, the U.S. Food and Drug Administration (FDA) has taken many steps to guide patients and prescribers on their safe use.

In 2016, the FDA announced a new requirement that immediate-release opioids include a “black box” warning on their labeling, detailing their risk of misuse and abuse, which can lead to addiction, overdose, and death.

The same year, the FDA required a black box warning for opioids outlining the risk of using opioids with other central nervous system depressants, including benzodiazepines. These two separate classes of drug, when taken together, may result in profound sedation, respiratory depression, coma, and death.

In 2020, the FDA required that labeling for opioids include a recommendation to speak with a healthcare professional about the use of naloxone—an antidote used to treat opioid overdose.

Long-term use of opioids is no longer recommended for chronic pain other than cancer-related pain. In fact, long-term use of opioids can make some types of chronic pain worse and puts patients at greater risk for opioid dependence.

When used properly, short-term medical use of opioids can be safe and rarely results in dependence. To avoid overdose, always administer opioids as instructed on the package labeling.

Opioid recalls

Any marketed drug is liable to be recalled if the manufacturer or regulatory authorities become aware that it may be defective or potentially harmful. Below are recent recalls issued for opioid products:

Hospira, Inc. recalled their hydromorphone injection on April 13, 2020, due to the potential for empty or cracked glass vials. All affected products have since expired.

Alvogen recalled their fentanyl transdermal patches due to product mislabeling in July 2019. A small number of cartons contained fentanyl patches of the wrong strength. All affected products have since expired.

PharMEDium Services, LLC recalled their hydromorphone injection due to the presence of sulfite—labeling information for the product claimed the product was sulfite-free. Exposure to sulfite could result in serious adverse reactions in patients with a sulfite allergy. All affected products have since expired.

Opioids restrictions

Opioids should be avoided in patients with a history of substance use or prescription drug abuse as they have the potential to be habit-forming.

Use extreme caution when taking any opioid drug if you have ever had a severe hypersensitivity reaction to an opioid. It is common for opioids to cause the release of histamine, resulting in itching. This is not a true allergy. A true allergy to opioid agents includes anaphylaxis or angioedema. Because of similarities in their chemical structure, it is possible to experience cross-sensitivity with opioids other than the original offending agent.  

Opioids should not be used in patients with a respiratory condition as respiratory depression may be worsened by opioids. 

Opioids should not be used in patients with a known or suspected gastrointestinal (GI) obstruction, including paralytic ileus, as opioids can significantly reduce the motility of the GI tract.

Patients with liver or kidney disease should be monitored closely while on opioids. Their dosages likely need to be adjusted to avoid dangerous levels of CNS depression.

Can you take opioids while pregnant or breastfeeding?

The Centers for Disease Control and Prevention (CDC) recommends against opioid use while pregnant or breastfeeding if safer alternatives are possible. In addition to the risk for misuse (which may cause harm to the mother), prolonged use of opioids during pregnancy or while breastfeeding can harm the child. Opioids cross the placenta, so neonates are exposed to their effects. According to the CDC, this can result in preterm birth, poor fetal growth, and birth defects (including neural tube defects, glaucoma, stomach defects, and congenital heart defects). It is common for infants exposed to opioids during pregnancy to develop neonatal dependence and withdrawal. 

Symptoms of opioid withdrawal include vomiting, diarrhea, failure to gain weight, high-pitched cry, abnormal sleep patterns, irritability, hyperactivity, and tremors. This condition can be life-threatening without early treatment. The severity is dependent on the maternal dose and frequency.

Are opioids controlled substances?

Because of their potential for abuse and misuse, opioids are classified as controlled substances by the U.S. Drug Enforcement Agency (DEA). Nearly all opioids are listed as Schedule II controlled substances. Drugs in this category are the most highly regulated of all prescription drugs. There are a few exceptions, such as buprenorphine, tramadol, and acetaminophen-codeine. These are still controlled substances but have fewer restrictions on their use. The scheduling system, and specific drugs assigned to each schedule, can differ among states according to the state Controlled Substance Acts.

Common opioids side effects

There are multiple side effects common to all opioid medications. Many of these adverse effects are the result of CNS depression. These side effects can be increased by other substances that cause CNS depression, such as benzodiazepines, alcohol, and barbiturates. These include:

• Drowsiness

• Confusion

• Sleep disturbance

• Psychomotor impairment

• Dyspnea (difficulty breathing)

Opioid medications also slow down the gastrointestinal tract. This causes side effects such as:

• Nausea/vomiting

• Constipation

Opioids cause the release of histamine, which can result in:

• Pruritus (itching)

• Rash

• Flushing

If you have been taking an opioid medication for an extended period, you should not stop suddenly as you may experience withdrawal symptoms. Your physician should guide a slow titration to discontinue the drug safely.

How much do opioids cost?

Many opioids are available generically at an affordable price, typically less than $20 with a SingleCare coupon. Some common opioids in this price range include tramadol, oxycodone, buprenorphine tablets, and generic Percocet, Lortab, and Tylenol #3. Some opioids are much more costly. 

For example, oxymorphone typically costs more than $500 for the generic (or $111.81 with a SingleCare coupon). Some opioids—like Nucynta—are only marketed under the brand name, which makes them more expensive (Nucynta is around $274 for a 30-day supply at most retail pharmacies).

Insurance plans typically list most generic opioids in Tier 1, which is the lowest cost tier of prescription drugs.

Insurance plans will often limit how much of an opioid drug they will cover within a certain period. Doctors can submit a prior authorization form to the insurance company if the patient requires a higher dose than the plan typically allows. For example, many insurance plans will only cover a 7-day supply the first time a beneficiary receives an opioid prescription while using their health plan.

Other coverage limitations may apply depending on the condition being treated. For example, methadone is covered by a medical plan and not through pharmacy coverage if it is being used for addiction treatment, rather than pain.

Before you fill your opioid prescription, check with SingleCare to make sure you are paying the lowest possible price.

Resources:

• Opioid addiction, HelpGuide

• About opioid use during pregnancy, CDC

• Maternal treatment with opioid analgesics and risk for birth defects, CDC

• AGS Beers Criteria, Journal of the American Geriatrics Society

• Opioid abuse, American Society of Anesthesiologists

• Opioid use in children, The Journal of Pediatric Pharmacology and Therapeutics