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Prescription medications such as pain relievers, central nervous system (CNS) depressants (tranquilizers and sedatives), and stimulants are highly beneficial treatments for a variety of health conditions. Pain relievers enable individuals with chronic pain to lead productive lives; tranquilizers can reduce anxiety and help patients with sleep disorders; and stimulants help people with attention-deficit hyperactivity disorder (ADHD) focus their attention. Most people who take prescription medications use them responsibly. But when abused—that is, taken by someone other than the patient for whom the medication was prescribed, or taken in a manner or dosage other than what was prescribed—prescription medications can produce serious adverse health effects, including addiction.

Patients, health care professionals, and pharmacists all have roles in preventing the abuse¹ of and addiction to prescription medications. For example, patients should follow the directions for use carefully; learn what effects and side effects the medication could have; and inform their doctor/pharmacist whether they are taking other medications [including over-the-counter (OTC) medications or health supplements], since these could potentially interact with the prescribed medication. The patient should read all information provided by the pharmacist. Physicians and other health care providers should screen for past or current substance abuse in the patient during routine examination, including asking questions about what other medications the patient is taking and why. Providers should note any rapid increases in the amount of a medication needed or frequent requests for refills before the quantity prescribed should have been finished, as these may be indicators of abuse.1

Similarly, some OTC medications, such as cough and cold medicines containing dextromethorphan, have beneficial effects when taken as recommended; but they can also be abused and lead to serious adverse health consequences. Parents should be aware of the potential for abuse of these medications, especially when consumed in large quantities, which should signal concern and the possible need for intervention.

Commonly Abused Prescription Medications

Although many prescription medications can be abused, the following three classes are most commonly abused:

• Opioids—usually prescribed to treat pain.
• CNS depressants—used to treat anxiety and sleep disorders.
• Stimulants—prescribed to treat ADHD and narcolepsy.

Opioids

What Are Opioids?

Opioids are analgesic, or pain-relieving, medications. Studies have shown that properly managed medical use (taken exactly as prescribed) of opioid analgesics is safe, can manage pain effectively, and rarely causes addiction.

Among the compounds that fall within this class are hydrocodone (e.g., Vicodin), oxycodone (e.g., OxyContin—an oral, controlled-release form of the drug), morphine, fentanyl, codeine, and related medications. Morphine and fentanyl are often used to alleviate severe pain, while codeine is used for milder pain. Other examples of opioids prescribed to relieve pain include propoxyphene (Darvon); hydromorphone (Dilaudid); and meperidine (Demerol), which is used less often because of its side effects. In addition to their effective pain-relieving properties, some of these medications can be used to relieve severe diarrhea (for example, Lomotil, also known as diphenoxylate) or severe coughs (codeine).

How Are Opioids Abused?

Opioids can be taken orally, or the pills may be crushed and the powder snorted or injected. A number of overdose deaths have resulted from the latter routes of administration, particularly with the drug OxyContin, which was designed to be a slow-release formulation. Snorting or injecting opioids results in the rapid release of the drug into the bloodstream, exposing the person to high doses and causing many of the reported overdose reactions.

How Do Opioids Affect the Brain?

Opioids act by attaching to specific proteins called opioid receptors, which are found in the brain, spinal cord, and gastrointestinal tract. When these compounds attach to certain opioid receptors in the brain and spinal cord, they can effectively change the way a person experiences pain.

In addition, opioid medications can affect regions of the brain that mediate what one perceives as pleasure, resulting in the initial euphoria or sense of well-being that many opioids produce. Repeated abuse of opioids can lead to addiction—a chronic, relapsing disease characterized by compulsive drug seeking and abuse despite its known harmful consequences.

What Adverse Effects Can Be Associated With Opioids?

Opioids can produce drowsiness, cause constipation, and, depending upon the amount taken, depress breathing. Taking a large single dose could cause severe respiratory depression or death.

These medications are only safe to use with other substances under a physician’s supervision. Typically, they should not be used with alcohol, antihistamines, barbiturates, or benzodiazepines. Because these other substances slow breathing, their effects in combination with opioids could lead to life-threatening respiratory depression.

What Happens When You Stop Taking Opioids?

Patients who are prescribed opioids for a period of time may develop a physical dependence on them, which is not the same as addiction. Repeated exposure to opioids causes the body to adapt, sometimes resulting in tolerance (that is, more of the drug is needed to achieve the desired effect compared with when it was first prescribed) and in withdrawal symptoms upon abrupt cessation of drug use. Thus, individuals taking prescribed opioid medications should not only be given these medications under appropriate medical supervision, but they should also be medically supervised when stopping use in order to reduce or avoid withdrawal symptoms. Symptoms of withdrawal can include restlessness, muscle and bone pain, insomnia, diarrhea, vomiting, cold flashes with goose bumps (“cold turkey”), and involuntary leg movements.

Are There Treatments for Opioid Addiction?

Individuals who abuse or are addicted to prescription opioid medications can be treated. Initially, they may need to undergo medically supervised detoxification to help reduce withdrawal symptoms; however, that is just the first step. Options for effectively treating addiction to prescription opioids are drawn from research on treating heroin addiction. Behavioral treatments, usually combined with medications, have also been proven effective. Currently used medications are—

• Methadone, a synthetic opioid that eliminates withdrawal symptoms and relieves craving, has been used successfully for more than 30 years to treat people addicted to heroin as well as opiates.
• Buprenorphine, another synthetic opioid, is a more recently approved medication for treating addiction to heroin and other opiates. It can be prescribed in a physician’s office.
• Naltrexone is a long-acting opioid receptor blocker that can be employed to help prevent relapse. It is not widely used, however, because of poor compliance, except by highly motivated individuals (e.g., physicians at risk of losing their medical license). It should be noted that this medication can only be used for someone who has already been detoxified, since it can produce severe withdrawal symptoms in a person continuing to abuse opioids.
• Naloxone is a short-acting opioid receptor blocker that counteracts the effects of opioids and can be used to treat overdoses.

CNS Depressants

What Are CNS Depressants?

CNS depressants (e.g., tranquilizers, sedatives) are medications that slow normal brain function. In higher doses, some CNS depressants can be used as general anesthetics or preanesthetics.

CNS depressants can be divided into three groups, based on their chemistry and pharmacology:

• Barbiturates, such as mephobarbital (Mebaral) and sodium pentobarbital (Nembutal), are used as preanesthetics, promoting sleep.
• Benzodiazepines, such as diazepam (Valium), alprazolam (Xanax), and estazolam (ProSom), can be prescribed to treat anxiety, acute stress reactions, panic attacks, convulsions, and sleep disorders. For the latter, benzodiazepines are usually prescribed only for short-term relief of sleep problems because of the development of tolerance and risk of addiction.
• Newer sleep medications, such as zolpidem (Ambien), zaleplon (Sonata), and eszopiclone (Lunesta), are now more commonly prescribed to treat sleep disorders. These medications are nonbenzodiazepines that act at a subset of the benzodiazepine receptors and appear to have a lower risk for abuse and addiction.

How Are CNS Depressants Abused?

CNS depressants are usually taken orally, sometimes in combination with other drugs or to counteract the effects of other licit or illicit drugs (e.g., stimulants).

How Do CNS Depressants Affect the Brain?

Most of the CNS depressants have similar actions in the brain: they enhance the actions of the neurotransmitter gamma-aminobutyric acid (GABA)—neurotransmitters are brain chemicals that facilitate communication between brain cells. GABA works by decreasing brain activity. Although different classes of CNS depressants work in unique ways, it is ultimately their common ability to increase GABA activity that produces a drowsy or calming effect.

What Adverse Effects Can Be Associated With CNS Depressants?

Despite their beneficial effects for people suffering from anxiety or sleep disorders, barbiturates and benzodiazepines can be addictive and should be used only as prescribed.

CNS depressants should not be combined with any medication or substance that causes drowsiness, including prescription pain medicines, certain OTC cold and allergy medications, and alcohol. If combined, they can slow both heart rate and respiration, which can be fatal.

What Happens When You Stop Taking CNS Depressants?

Discontinuing prolonged use or abuse of high doses of CNS depressants can lead to serious withdrawal symptoms. Because the drug works by slowing the brain’s activity, when one stops taking a CNS depressant, this activity can rebound to the point that seizures can occur. Someone who is either thinking about ending use of a CNS depressant, or who has stopped and is suffering withdrawal should seek medical treatment.

Are There Treatments for Addiction to CNS Depressants?

In addition to medical supervision during withdrawal, counseling in an inpatient or outpatient setting can help people who are overcoming addiction to CNS depressants. For example, cognitive-behavioral therapy has been used successfully to help individuals in treatment for abuse of benzodiazepines. This type of therapy focuses on modifying a patient’s thinking, expectations, and behaviors while simultaneously increasing his or her skills for coping with various life stressors.

Stimulants

What Are Stimulants?

Stimulants (amphetamines [Adderall, Dexedrine] and methylphenidate [Concerta, Ritalin]) increase alertness, attention, and energy. They also increase blood pressure and heart rate, constrict blood vessels, increase blood glucose, and open up the pathways of the respiratory system. Historically, stimulants were prescribed to treat asthma and other respiratory problems, obesity, neurological disorders, and a variety of other ailments. As their potential for abuse and addiction became apparent, the prescribing of stimulants by physicians began to wane. Now, stimulants are prescribed for treating only a few health conditions, most notably ADHD, narcolepsy, and, in some instances, depression that has not responded to other treatments.

How Are Stimulants Abused?

Stimulants may be taken orally, but some abusers crush the tablets, dissolve them in water, and then inject the mixture; complications can arise from this because insoluble fillers in the tablets can block small blood vessels. Stimulants have been abused for both “performance enhancement” and recreational purposes (i.e., to get high).

How Do Prescription Stimulants Affect the Brain?

Stimulants have chemical structures that are similar to key brain neurotransmitters called monoamines, including dopamine and norepinephrine. Their therapeutic effect is achieved by slow and steady increases of dopamine that are similar to the natural production of this chemical by the brain. The doses prescribed by physicians start low and increase gradually until a therapeutic effect is reached. However, when taken in doses and routes other than those prescribed, stimulants can increase the brain’s dopamine levels in a rapid and highly amplified manner—as do most other drugs of abuse—disrupting normal communication between brain cells, producing euphoria, and increasing the risk of addiction.

What Adverse Effects Are Associated With Stimulant Abuse?

Taking high doses of a stimulant can result in an irregular heartbeat, dangerously high body temperatures, and/or the potential for cardiovascular failure or seizures. Taking some stimulants in high doses or repeatedly can lead to hostility or feelings of paranoia in some individuals.

Stimulants should not be mixed with antidepressants, which may enhance the effects of a stimulant; or with OTC cold medicines containing decongestants, which may cause blood pressure to become dangerously high or may lead to irregular heart rhythms.

Are There Treatments for Stimulant Addiction?

Treatment of addiction to prescription stimulants is based on behavioral therapies proven effective for treating cocaine or methamphetamine addiction. At this time, there are no proven medications for the treatment of stimulant addiction.

Depending on the patient’s situation, the first step in treating prescription stimulant addiction may be to decrease the drug’s dose slowly and attempt to treat withdrawal symptoms (mood changes, sleep and appetite disturbances). This process of detoxification could then be followed with one of many behavioral therapies: contingency management, for example, improves treatment outcomes by enabling patients to earn vouchers for drug-free urine tests; the vouchers can be exchanged for items that promote healthy living. Cognitive-behavioral therapies—which teach patients skills to recognize risky situations, avoid drug use, and cope more effectively with problems—are proving beneficial. Recovery support groups may also be effective in conjunction with a behavioral therapy.