Opioids

Opioids

Definition

Opioids are narcotic drugs that are generally prescribed to manage pain. The most commonly prescribed opioids are: buprenorphine, butorphanol, codeine, fentanyl, hydrocodone, hydromorphone, levorphanol, meperidine , methadone, morphine, nalbuphine, oxycodone, oxymorphone, pentazocine, and propoxyphene. These opioids are prescribed alone or in combination with aspirin or acetaminophen (Tylenol).

The most common brand names for these drugs are:

• Actiq
• Astramorph PF
• Buprenex
• Cotanal-65
• Darvon
• Demerol
• Dilaudid
• Dolophine
• Duragesic
• Duramorph
• Hydrostat IR
• Kadian
• Levo-Dromoran
• Methadose
• M S Contin
• MSIR
• MS/L
• MS/S
• Nubain
• Numorphan
• OMS
• Oramorph SR
• OxyContin
• PP-Cap
• Rescudose
• RMS Uniserts
• Roxanol
• Roxicodone
• Stadol
• Talwin

When combined with aspirin or acetaminophen, the most common brand names are:

• Allay
• Anexsia
• Anolor
• Bancap-HC
• Capital with Codeine
• Co-Gesic
• Damason-P
• Darvocet
• Darvon
• DHCplus
• Dolacet
• Dolagesic
• Duocet
• E-Lor
• Empirin with codeine
• Endocet
• Endodan
• EZ III
• Hycomed
• Hyco-Pap
• Hydrocet
• Hydrogesic
• HY-PHEN
• Lorcet
• Lortab
• Margesic
• Oncet
• Panacet
• Panasal
• Panlor
• Percocet
• Percodan
• Phenaphen with codeine
• Polygesic
• Propacet
• Propoxyphene Compound-65
• Pyregesic-C
• Roxicet
• Roxilox
• Roxiprin
• Stagesic
• Synalgos-DC
• Talacen
• Talwin compound
• T-Gesic
• Tylenol with codeine
• Tylox
• Ugesic
• Vanacet
• Vendone
• Vicodin
• Vicoprofen
• Wygesic
• Zydone

Purpose

Opioids are primarily used to manage pain. Some narcotics are also used just prior to, or during, surgery to increase the effectiveness of certain anesthetics. Codeine and hydrocodone are used to relieve coughing. Methadone is used to help people control their dependence on heroine or other narcotics.

Description

Opioids act on the central nervous system (CNS)to relieve pain. Many of these drugs are habit-forming and physical dependence may lead to withdrawal side effects when the medication is stopped. Because of the potential habit-forming nature of these drugs, most prescriptions cannot be refilled and a new prescription must be obtained after each preceding prescription runs out.

Recommended dosage

Opioids may be taken either orally (in pill or liquid form), by injection (or as part of an intravenous [IV]. line), as an anal suppository, or as a patch attached to the skin. The dosage prescribed may vary widely depending on the patient, the cancer being treated, and whether or not other medications are also being taken.

A typical adult dosage for buprenorphine is 0.3 mg injected into a muscle or vein every six hours as necessary. For children between the ages of two and twelve years, the dosage is typically 0.002 to 0.006 mg per kilogram (2.2 pounds) of body weight.

A typical adult dosage for butorphanol is 1-4 mg injected into a muscle or 0.5-2 mg injected into a vein every four hours as necessary. For children between the ages of two and twelve years, the dosage is typically based on the body weight of the child.

A typical adult dosage for codeine is 15-60 mg taken orally or injected into a muscle or vein every four to six hours as necessary for pain. This dosage is decreased to 10 to 20 mg when codeine is used to control coughing.

Fentanyl is most often used to manage pain in cancer patients who are already receiving and are tolerant to other opioids. This drug is available as a lozenge and as a skin patch. It is not used for the treatment of pain caused by injury or surgery. The dosage of fentanyl is determined on an individual patient basis by that patient's oncologist.

A typical adult dosage for hydrocodone is 5-10 mg taken orally every four to six hours as necessary for pain, 5 mg to control coughing.

A typical adult dosage for hydromorphone is 1-2 mg injected into a muscle, 2-2.5 mg taken orally, or 3 mg taken as a suppository every three to six hours as necessary.

A typical adult dosage for levorphanol is 2-4 mg taken orally or injected into a vein every four hours as necessary.

A typical adult dosage for meperidine is 100 mg taken orally or injected into a muscle or vein every four hours as necessary.

A typical adult dosage for methadone is 5-20 mg as an oral solution, 2.5-10 mg as an oral tablet or injection, every four to eight hours as necessary for pain. When used for detoxification, methadone is initially given in a dose of 15-40 mg per day as an oral solution. This dose is then decreased until the patient no longer requires the medication. The injection form of methadone is only used for detoxification in patients who are unable to take the medication by mouth.

Morphine is most often used to manage severe, chronic pain in patients who have already been receiving other narcotic pain relievers. The starting dose of morphine is generally determined based on the dosages of prior narcotic pain relievers the patient had been receiving. A typical starting dose is 5-30 mg every four hours.

A typical adult dosage for nalbuphine is 10 mg injected into a muscle or vein every three to six hours as necessary.

A typical adult dosage for oxycodone is 5 mg taken orally every three to six hours, or 10-40 mg taken as a suppository three to four times per day as necessary.

A typical adult dosage for oxymorphone is 1-1.5 mg injected into a muscle every three to six hours, or 5 mg taken as a suppository every four to six hours as necessary.

A typical adult dosage for pentazocine is 50 mg taken orally, or 30 mg injected into a muscle or vein every three to four hours as necessary.

Propoxyphene comes in two salt forms: propoxyphene hydrochloride and propoxyphene napsylate. The typical adult dosage for propoxyphene hydrochloride is 65 mg taken orally every four hours with a maximum daily dosage of 390 mg. The typical adult dosage for propoxyphene napsylate is 100 mg taken orally every four hours with a maximum daily dosage of 600 mg.

Precautions

Opioids magnify the effects of alcohol and other central nervous system depressants, such as antihistamines, cold medicines, sedatives, tranquilizers, other prescription and over-the-counter pain medications, barbiturates, seizure medications, muscle relaxants, and certain anesthetics including some dental anesthetics. Alcohol and other central nervous system depressants should not be taken or consumed while opioids are being taken.

Opioids are powerful narcotics. These drugs can cause some people to feel drowsy, dizzy, or lightheaded. People taking opioids should not drive a car or operate machinery.

Opioids can be habit-forming. Patients who have been taking these types of medication for a period of several weeks should not stop taking this type of medication all at once. The dosage should be slowly tapered off to avoid potential withdrawal side effects.

Intentional or accidental overdose of any of the opioids can lead to unconsciousness, coma, or death. The signs of opioid overdose include confusion, difficulty speaking, seizures, severe nervousness or restlessness, severe dizziness, severe drowsiness, and/or slow or troubled breathing. These symptoms are increased by alcohol or other central nervous system depressants. Anyone who feels that he or she, or someone else, may have overdosed on opioids, or a combination of opioids and other central nervous system depressants, should seek emergency medical attention for that person at once.

Opioids can interfere with or exacerbate certain medical conditions. For these reasons, it is important that the prescribing physician is aware of any current case, or history of:

• alcohol abuse
• brain disease or head injury
• colitis
• drug dependency, particularly of narcotics
• emotional problems;
• emphysema, asthma, or other chronic lung disease
• enlarged prostate
• gallstones or gallbladder disease
• heart disease
• kidney disease
• liver disease
• problems with urination
• seizures
• underactive thyroid

Side effects

The most common side effects of opioids include:

• constipation
• dizziness
• drowsiness
• itching
• nausea
• urine retention
• vomiting

Less common side effects of opioids include:

• abnormally fast or slow heartbeat
• blurred or double vision
• cold, clammy skin
• depression or other mood changes
• dry mouth
• fainting
• hallucinations
• hives
• loss of appetite (anorexia )
• nightmares or unusual dreams
• pinpoint pupils of the eyes
• redness or flushing of the face
• restlessness
• rigid muscles
• ringing or buzzing in the ears
• seizure
• severe drowsiness
• skin reaction at the site of injection
• stomach cramps or pain
• sweating
• trouble sleeping (insomnia)
• yellowing of the skin or whites of the eyes

Interactions

Opioids should not be taken in combination with any prescription drug, over-the-counter drug, or herbal remedy without prior consultation with a physician. It is particularly important that the prescribing physician be aware of the use of any of the following drugs:

• carbamazepine (Tegretol; antiepileptic)
• central nervous system depressants
• monoamine oxidase (MAO) inhibitors (a class of anti-depressants) such as furazolidone, isocarboxazid, pargyline, phenelzine, procarbazine , or tranylcypromine
• Naltrexone (opioid antagonist)
• Rifampin (antituberculosis drug)
• tricyclic antidepressants such as amitriptyline , amoxapine, clomipramine, desipramine, doxepin, imipramine, nortiptyline, protriptyline, or trimipramine
• Zidovudine (antiviral against aids virus)
• any radiation therapy or chemotherapy medicines

Paul A. Johnson, Ed.M.

KEY TERMS

Central nervous system depressant

—Any drug that tends to reduce the activity of the central nervous system. The major drug categories included in this classification are alcohol, anesthetics, antianxiety medications, antihistamines, antipsychotics, hypnotics, narcotics, sedatives, and tranquilizers.

Narcotic

—Any drug that produces insensibility or stupor and/or generally causes effects similar to those caused by morphine.