Codeine, Chlorpheniramine, Phenylephrine, and Phenylpropanolamine

  • Generic Name or Active Ingridient: Codeine
Drug Class: Codeine, Chlorpheniramine, Phenylephrine, And Phenylpropanolamine > Codeine, Chlorpheniramine, And Phenylephrine > Codeine > Opiate > Opioids > Opioid Agonist > Analgesic.

Uses

Doctors prescribe products containing codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine to relieve symptoms caused by allergies and upper respiratory infections like the common cold. This combination product relieves cough and a stuffy or runny nose.

General Drug Information

Small doses of codeine suppress the cough reflex; larger doses relieve pain and cause other neurological effects including sedation, relaxation, and euphoria. These effects make codeine an attractive target for recreational drug abusers.

Pharmaceutical companies extract codeine from the opium poppy plant. Scientists classify opium as an opioid drug because of the way it binds to opioid receptors in the nervous system. Chlorpheniramine, phenylephrine, and phenylpropanolamine are decongestants.

Administration/Dosage

Drug manufacturers usually combine codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine into a syrup form for oral use. The consumer can take this product with food to avoid stomach upset.

Consumers should take codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine preparations exactly as prescribed and dispose of any unused doses after they no longer need it to control symptoms. Patients should take the smallest dose possible stop using codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine as soon as symptoms ease to avoid growing dependent on opioids.

Codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine may cause breathing problems in children and elderly patients. Prescribing physicians should monitor these patients closely, especially in the early stages of treatment and after increasing dosages.

Caregivers should use an approved measuring device when administering codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine products to children. Caregivers should never administer more than the prescribed dosage to a child.

Action

Codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine work in different ways to relieve multiple symptoms. Chlorpheniramine, phenylephrine, and phenylpropanolamine are decongestants that work by shrinking blood vessels in the nasal passage, allowing more room for air to flow inside the nose.

Codeine and other opioids depress the central nervous system, or CNS, to cause various effects. Opioids depress the hypothalamus, which serves as the breathing center of the brain. Codeine and other opioids make the brain apathetic about the need to cough phlegm and debris from the lungs and airway. At higher doses, opioids can slow breathing to the point of apnea, or stopped breathing.

Strong opioids cause other effects through CNS depression. Codeine binds to opioid pain receptors in the central nervous system to change the way the brain interprets pain messages it receives from various places in the body. Sedation, relaxation, and euphoria are immediately evident but codeine causes other CNS reactions that may not be apparent right away, including changes in the way a person thinks, feels, and behaves. These neurological actions can have a long-lasting, detrimental effect on the chronic codeine consumer, including the development of chemical dependence and addiction.

Chlorpheniramine, phenylephrine, and phenylpropanolamine are CNS stimulants that do not produce dependence and addiction, but these drugs can cause other effects such as increased blood pressure, nervousness, and anxiety.

Warnings

Researchers have associated phenylpropanolamine with an increased risk for hemorrhagic stroke, a serious condition marked by bleeding in the brain or in the tissue surrounding the brain, in women. While this risk is low for both men and women, the FDA suggests avoiding products containing phenylpropanolamine.

Consumers should not stop taking codeine abruptly, especially if the individual has used codeine regularly for more than a few weeks. Sudden cessation may cause unpleasant withdrawal symptoms. Patients should instead taper codeine use by taking a smaller dose each day.

Precautions

Codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine products can make the consumer feel dizzy, drowsy, or impair his ability to make decisions. Using this product with other opioids or alcohol enhances these effects. A consumer should not drive or operate heavy machinery until he determines how this product affects him.

Contraindications

Products containing codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine may be not be appropriate for all patients.

Doctors should exercise caution when prescribing chlorpheniramine to patients suffering from bone marrow depression, urinary retention, asthma, or thyroid, liver, or heart problems. Patients, especially children, with chronic breathing problems should use this product with care.

Phenylephrine may not be appropriate for patients suffering from high blood pressure, glaucoma, or diabetes.

Phenylpropanolamine is not for patients with high blood pressure, heart disease, diabetes, or some types of thyroid problems.

People with a history of hypersensitivity to codeine or other opioids should not use this product. Individuals with severe breathing problems should avoid codeine, especially those with asthma. Patients with a history of the serious digestive problem, paralytic ileus, should not use codeine products.

Pregnancy, Labor and Delivery, Breastfeeding

Codeine is an FDA Pregnancy Category C, which means scientists do not yet know how codeine affects reproductive capabilities of men or women, or how it might affect an unborn baby. A baby born to a woman who takes codeine regularly in the last three months of pregnancy may experience withdrawal symptoms after delivery. Pregnant women should only use codeine products when the benefits to the mother clearly outweigh the potential risk to the fetus.

Codeine passes into breast milk. Women should discontinue breastfeeding or choose another cough suppressant to reduce the risk of passing codeine onto a nursing baby.

Drug Interactions

Codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine preparations can interact with other medications to cause unsafe or unwanted effects. Prescribing physicians should ask patients for a complete list of all prescription and non-prescription drugs to avoid dangerous drug interactions. Patients should never change the way they take any medications while taking codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine without first consulting a doctor or pharmacist.

In general, products containing codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine can interact poorly with the following drugs:

  • Antidepressants
  • Aspirin or salicylates
  • Beta-blockers
  • Bladder or urinary medications
  • Blood pressure medication
  • Cimetidine, known as the brand name drug Tagamet
  • Diuretics, sometimes known as “water pills”
  • Irritable bowel syndrome medications
  • Medicines to treat psychiatric disorder
  • Rifampin
  • Seizure drugs
  • Zidovudine

Codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine combination products are not appropriate for patients who have taken an MAO inhibitor within 14 days. Patients sometimes take MAO inhibitors to control blood pressure or depression. Taking this combination product while MAO inhibitors are still present in the body can cause dangerous drug interaction or even death. Furazolidone, sodium oxybate and some antidepressants may increase side effects associated chlorpheniramine and phenylephrine combination drugs.

Physicians have reported cases of adverse interactions between the popular anti-depressant, Cymbalta and products containing codeine and phenylpropanolamine. Patients should not take Cymbalta while taking codeine and phenylpropanolamine products.

Side effects

All drugs can cause side effects, including preparations containing codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine. Most side effects are not serious and disappear with continued use at therapeutic doses. Non-serious side effects can include:

  • A warm or tingling feeling, or redness under the skin
  • Blurred vision
  • Constipation
  • Dizziness or drowsiness
  • Dry mouth
  • Insomnia
  • Itching
  • Memory or concentration problems
  • Ringing in the ears
  • Skin rash
  • Upset stomach
  • Vomiting

Some side effects can be serious. Consumers should contact a doctor right away if he experiences adverse reactions such as:

  • Anxiety, restlessness, nervousness
  • Clay-colored stools
  • Confusion, hallucinations
  • Dangerously high blood pressure
  • Dark urine
  • Easy bruising or bleeding
  • Fast, slow, pounding, or uneven heartbeats
  • Fever, chills, body aches, flu symptoms
  • Lightheadedness
  • Loss of appetite
  • Severe dizziness
  • Severe itching
  • Shallow breathing
  • Unusual thoughts or behavior
  • Unusual weakness
  • Upper abdominal pain
  • Urinating less than usual or not at all
  • Yellowing of the skin or eyes

Overdose

Allergy and cold preparations usually contain doses of codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine too low to cause overdose easily but it is possible for someone to take a toxic dose. Serious drug overdose can cause death. Each year, about 15,000 people die from overdoses of prescription drugs, especially painkillers like codeine and other opioids.

Prescription overdose death is an increasing problem in the United States, with death rates more than tripling in the decade between 1999 and 2008. In 2008, for the first time in the nation’s history, the number of prescription drug overdose deaths eclipsed the number of deaths from heroin and cocaine combined.

Anyone who has possibly taken an overdose should poison control center at 1-800-222-1222 or go to the nearest emergency room without waiting for overdose symptoms to appear. The individual should take the container with the remaining codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine product to help doctors determine how much medication the victim consumed.

Overdose symptoms include:

  • Abdominal pain
  • Cold, clammy skin
  • Confusion
  • Extreme drowsiness
  • Fainting
  • Feelings of warmth or tingling
  • Pinpoint pupils
  • Restlessness or nervousness
  • Seizure
  • Shallow or stopped breathing
  • Vomiting
  • Weak pulse

Abuse

Some people use codeine products to get high. The United States DEA classifies most codeine products as schedule II narcotics, meaning they pose a relatively high risk for abuse. Some codeine products, especially those intended to relieve cough, are DEA schedule III drugs because their weak doses pose less of a threat for abuse.

Codeine abuse increases the risk for developing opioid dependence that causes uncomfortable withdrawal symptoms when the individual stops using opioids. The U.S. Drug Enforcement Agency hopes to reduce the problems of abuse and dependence by restricting all schedule II drugs to sale by prescription only. Many drug abusers get around this law by “doctor shopping” to get as many prescriptions as possible, presenting phony or altered prescriptions at pharmacies, stealing from friends or pharmacies, or by purchasing illegal drugs.

Chlorpheniramine, phenylephrine, and phenylpropanolamine do not produce euphoria and are therefore rarely target of recreational drug abuse.

Withdrawal

Anyone who uses codeine products regularly for a long time can become physically dependent and suffer uncomfortable withdrawal symptoms when they stop using codeine. These withdrawal symptoms tend to appear in two waves, with the first set of symptoms beginning a few hours after the last dose of codeine.

At first, the patient will feel:

  • Agitation
  • Anxiety
  • Muscle aches
  • Increased tearing
  • Insomnia
  • Runny nose
  • Sweating
  • Yawning

Later, other symptoms may develop, including:

  • Abdominal cramps
  • Diarrhea
  • Dilated pupils
  • Goose bumps
  • Nausea and vomiting

Some patients experience increased blood pressure and rapid pulse during detoxification. These withdrawal symptoms can worsen some types of heart conditions. Other underlying conditions can worsen withdrawal symptoms or become aggravated by the detoxification process.

Chlorpheniramine, phenylephrine, and phenylpropanolamine do not cause physical dependence resulting in withdrawal symptoms but chronic use of preparations containing these drugs may complicate the detoxification process to alter or worsen withdrawal symptoms.

Unless interrupted, codeine withdrawal symptoms fade after five or more days as the body completes the detoxification process. Withdrawal symptoms do not return unless the individual starts taking codeine again and returns to an opioid-dependent state.

The patient can use non-opioid drugs to reduce the severity of withdrawal symptoms. He may use, for example, Imodium to slow diarrhea and ibuprofen for body aches. He could stop withdrawal symptoms completely by taking more codeine but this would return him to an opioid-dependent state and reverse the positive effects of detoxification.

Detox

Detoxification refers to the process of lowering opioid levels and relieving withdrawal symptoms. Detoxification can occur at home, with the help of an outpatient clinic, at a hospital, or in a specialized detoxification facility.

About 2 million Americans are physically dependent on opioids like codeine. Each of these individuals must participate in some form of detoxification to achieve an opioid-free state and cleanse their bodies of the toxic effects of chronic codeine use.

Detoxification does occur naturally: someone can detoxify at home, without the use of anti-withdrawal drugs or professional guidance. Outpatient clinics typically offer opioid replacement drugs that mimic the effects of codeine to reduce withdrawal symptoms while the patient tapers from opioid use. Inpatient clinics usually administer potent detoxification drugs to lower opioids along with medical grade anti-withdrawal drugs.

Rapid detox is an effective and humane approach to detoxification. During rapid detox, board-certified anesthesiologists sedate and anesthetize patients so they doze in a pleasant “twilight sleep” during detoxification. Patients awaken a few hours later, cleansed of the toxic effects of codeine and unaware of unpleasant withdrawal symptoms. Rapid detox patients feel renewed, refreshed, and ready for rehabilitation.

Storage

Consumers and caregivers should store codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine at room temperatures between 59 and 86 degrees Fahrenheit. This medication should be kept away from excessive heat and humidity.

Consumers and administrators should keep this and all medications out of the reach of children and pets. Physicians and pharmacists should remind patients never to share this medication with others. Consumers should keep track of codeine, chlorpheniramine, phenylephrine, and phenylpropanolamine doses and investigate any missing medication from the container.