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Codeine

Codeine, also known as 3-methylmorphine, is an opiate used to treat pain, as a cough medicine, and for diarrhea. It is typically used to treat mild to moderate degrees of pain. Greater benefit may occur when combined with paracetamol (acetaminophen) or aspirin. Evidence does not support its use for cough suppression. 

The relief of pain (analgesia) is a primary goal for enhancing the quality of life of patients and for increasing the ability of patients to engage in day to day activities. Codeine, an opioid analgesic, was originally approved in the US in 1950 and is a drug used to decrease pain by increasing the threshold for pain without impairing consciousness or altering other sensory functions. Opiates such as codeine are derived from the poppy plant, Papaver somniferum (Papaveraceae).

Codeine is utilized as a central analgesic, sedative, hypnotic, antinociceptive, and antiperistaltic agent, and is also recommended in certain diseases with incessant coughing.

In Europe it is not recommended as a cough medicine in those under twelve years of age. It is taken by mouth. It typically starts working after half an hour with maximum effect at two hours. Effects last for about four to six hours.

Codeine is used to relieve mild to moderate pain. It is also used, usually in combination with other medications, to reduce coughing. Combination products that contain codeine and promethazine should not be used in children younger than 16 years of age. Codeine will help relieve symptoms but will not treat the cause of symptoms or speed recovery. Codeine belongs to a class of medications called opiate (narcotic) analgesics and to a class of medications called antitussives. When codeine is used to treat pain, it works by changing the way the brain and nervous system respond to pain. When codeine is used to reduce coughing, it works by decreasing the activity in the part of the brain that causes coughing.

Codeine is also available in combination with acetaminophen (Capital and Codeine, Tylenol with Codeine); aspirin; and carisoprodol; and as an ingredient in many cough and cold medications. This monograph only includes information about the use of codeine. If you are taking a codeine combination product, be sure to read information about all the ingredients in the product you are taking and ask your doctor or pharmacist for more information.

DRUG CLASS AND MECHANISM: Codeine is a narcotic pain-reliever and cough suppressant similar to morphine and hydrocodone. Moreover, a small amount of codeine is converted to morphine in the body. The precise mechanism of action of codeine is not known; however, like morphine, codeine binds to receptors in the brain (opioid receptors) that are important for transmitting the sensation of pain throughout the body and brain. Codeine increases tolerance to pain, decreasing discomfort, but the pain still is apparent to the patient. In addition to reducing pain, codeine also causes sedation drowsiness and depresses breathing. Codeine frequently is combined with acetaminophen (Tylenol) or aspirin for more effective pain relief. The FDA approved codeine in 1950.

Codeine is habit forming. Mental and physical dependence can occur but are unlikely when used for short-term pain relief. If codeine is suddenly withdrawn after prolonged use, symptoms of withdrawal may develop. The dose of codeine should be reduced gradually in order to avoid withdrawal symptoms.

How should Codeine be used?

Codeine (alone or in combination with other medications) comes as a tablet, a capsule, and a solution (liquid) to take by mouth. It is usually taken every 4 to 6 hours as needed. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take codeine exactly as directed.

Codeine can be habit-forming. Do not take a larger dose, take it more often, or take it for a longer period of time than prescribed by your doctor. Do not stop taking codeine without talking to your doctor. Your doctor may decrease your dose gradually. If you suddenly stop taking codeine, you may experience withdrawal symptoms such as restlessness, widened pupils (black circles in the center of the eyes), teary eyes, irritability, anxiety, runny nose, difficulty falling asleep or staying asleep, yawning, sweating, fast breathing, fast heartbeat, chills, hair on your arms standing on end, nausea, loss of appetite, vomiting, diarrhea, stomach cramps, muscle aches, or backache.

If you are giving codeine to a child, give the medication only as needed. Do not give codeine on a regular (around-the-clock) schedule and do not give more than six doses in 24 hours.

Shake the solution well before each use to mix the medication evenly. Do not use a household spoon to measure your dose. Use the measuring cup or spoon that came with the medication or use a spoon that is made especially for measuring medication.

Why Codeine Is Abused:

  1. Euphoric Effects: Codeine is an opioid that, when taken in higher doses than prescribed, can induce feelings of euphoria and relaxation. These effects can make it attractive for recreational use.
  2. Accessibility: As codeine is found in many over-the-counter cough syrups and prescription pain medications, it is relatively easy to obtain compared to stronger opioids, leading to potential misuse.
  3. Tolerance Development: Like other opioids, codeine can lead to physical tolerance, meaning users may need increasing amounts to achieve the same effects, which can quickly lead to abuse.
  4. Dependence and Addiction: Prolonged use can lead to physical dependence, where the body requires the drug to function normally, and addiction, where individuals feel compelled to seek and use the drug despite harmful consequences.
  5. Perception of Safety: Since codeine is often prescribed by doctors, many people may perceive it as safer than illicit drugs, even though it carries similar risks of addiction and overdose when misused.

Other uses for this medicine

This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

What special precautions should I follow?

Before taking codeine,

  • tell your doctor and pharmacist if you are allergic to codeine, any other medications, or any of the ingredients in the codeine product you plan to take. Ask your doctor or pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: antidepressants; medications for cough, cold, or allergies; medications for anxiety, mental illness, nausea, or seizures; monoamine oxidase (MAO) inhibitors such as isocarboxazid (Marplan), phenelzine (Nardil), selegiline (Eldepryl, Emsam, Zelapar), and tranylcypromine (Parnate); sedatives; sleeping pills; and tranquilizers. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have slowed breathing, or have or have ever had asthma or paralytic ileus (condition in which digested food does not move through the intestines). Your doctor may tell you not to take codeine.
  • tell your doctor if you drink or have ever drunk large amounts of alcohol and if you have had recent abdominal or urinary tract surgery. Also tell your doctor if you have or have ever had a head injury; a brain tumor; any condition causing increased pressure in your brain; seizures; mental illness; lung disease such as asthma, chronic obstructive pulmonary disease (COPD, a group of diseases that cause gradual loss of lung function),obstructive sleep apnea, or other breathing problems; prostatic hypertrophy (enlargement of a male reproductive gland); urinary problems; low blood pressure; Addison’s disease (condition in which the body does not make enough of certain natural substances); allergies; or thyroid, pancreatic, intestinal, gallbladder, liver, or kidney disease.
  • tell your doctor if you are pregnant or plan to become pregnant. If you become pregnant while taking codeine, call your doctor.
  • tell your doctor if you are breast-feeding. Some women who take codeine may have increased amounts of the medication in their breast milk, which can cause serious or life-threatening side effects in their breast-fed babies. Call your doctor immediately or get emergency medical help if you become very sleepy and have difficulty caring for your baby. You should also call your baby’s doctor or get emergency help if your baby is sleepier than usual, has trouble breast-feeding or breathing, or becomes limp. If you breast-feed during your treatment and stop breast-feeding or stop taking codeine, your baby might experience withdrawal symptoms including irritability, being more active than usual, vomiting, problems sleeping, weight loss, high-pitched cry, fever, shaking, or diarrhea or more stools than usual. Call your baby’s doctor if your baby has any of these symptoms.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking codeine.
  • you should know that this medication may make you drowsy. Do not drive a car or operate machinery until you know how this medication affects you. If you are giving codeine to a child, watch the child to be sure he or she does not get hurt while riding a bike or participating in other activities that could be dangerous.
  • you should know that drinking alcohol during your treatment may increase the risk that you will experience serious or life-threatening side effects. Talk to your doctor about the risks of drinking alcohol during your treatment.
  • you should know that codeine may cause dizziness, lightheadedness, and fainting when you get up too quickly from a lying position. This is more common when you first start taking codeine. To avoid this problem, get out of bed slowly, resting your feet on the floor for a few minutes before standing up.
  • you should know that codeine may cause constipation. Talk to your doctor about changing your diet and using other medications to treat or prevent constipation.

What special dietary instructions should I follow?

Unless your doctor tells you otherwise, continue your normal diet.

What should I do if I forget a dose?

Codeine is usually taken as needed. If your doctor has told you to take codeine regularly, take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

What side effects can this medication cause?

Codeine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • dizziness
  • lightheadedness
  • headache
  • drowsiness
  • mood changes
  • nausea
  • vomiting
  • constipation
  • stomach pain
  • difficulty urinating

Some side effects can be serious. If you experience any of the following symptoms, stop taking codeine and call your doctor immediately or get emergency medical attention:

  • sleepiness
  • confusion
  • noisy or shallow breathing
  • difficulty breathing or swallowing
  • fast, pounding, or irregular heartbeat
  • rash
  • itching
  • hives
  • changes in vision
  • seizures

Codeine may cause other side effects. Call your doctor if you have any unusual problems while you are taking this medication.

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

What should I know about storage and disposal of this medication?

Keep this medication in the container it came in, tightly closed. at room temperature and away from excess heat and moisture (not in the bathroom). Keep it in a safe place where no one else can take it accidentally or on purpose. Be especially careful to keep codeine out of reach of children. If a child accidentally takes codeine, get emergency medical help right away. Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.

Is Codeine a Controlled Substance ?

Yes, codeine is a controlled substance in most countries due to its potential for abuse, addiction, and dependence.

In the United States, for example, codeine is classified under the Controlled Substances Act (CSA) by the Drug Enforcement Administration (DEA):

  • Schedule II: Codeine is classified as a Schedule II drug when it is found in high concentrations (such as in pure form or in certain prescription painkillers), indicating a high potential for abuse and dependence.
  • Schedule III or V: When codeine is combined with other medications in lower doses, such as in some prescription cough syrups or pain medications, it may be classified as a Schedule III or Schedule V drug, which reflects a lower potential for abuse but still requires regulation.

In many countries, codeine is also regulated to varying degrees. For instance, it may only be available by prescription or in limited quantities over the counter, with specific restrictions based on local laws.

What Happen if I Overdose Codeine ?

An overdose of codeine can be life-threatening and requires immediate medical attention. Here’s what can happen during a codeine overdose:

Signs and Symptoms of Codeine Overdose:

  1. Respiratory Depression: Codeine, like other opioids, can slow down breathing. In an overdose, breathing may become dangerously shallow, irregular, or even stop completely, which is the leading cause of death in opioid overdoses.
  2. Extreme Drowsiness or Unconsciousness: An overdose can cause intense drowsiness, confusion, or coma. The person may be difficult or impossible to wake up.
  3. Cyanosis: If breathing is compromised, the skin, lips, or fingernails may turn blue due to lack of oxygen.
  4. Low Blood Pressure: A severe drop in blood pressure can occur, leading to dizziness, fainting, or shock.
  5. Slow or Irregular Heartbeat: Codeine overdose can cause the heart to beat slower than normal, leading to heart failure or cardiac arrest.
  6. Pupil Constriction: The pupils may become very small, a common sign of opioid overdose.
  7. Seizures: Although rare, high doses of codeine can cause seizures.
  8. Gastrointestinal Issues: Nausea, vomiting, and severe constipation are common in codeine overdose, and vomiting can further complicate breathing if the person is unconscious.

Long-Term Effects of Overdose:

  • Brain Damage: Prolonged lack of oxygen due to respiratory depression can result in permanent brain damage.
  • Coma or Death: If not treated promptly, codeine overdose can lead to coma or death, primarily due to respiratory failure.

What to Do in Case of Codeine Overdose:

  1. Call Emergency Services Immediately: If you suspect someone has overdosed on codeine, call emergency services (911 in the U.S.) right away.
  2. Administer Naloxone (if available): Naloxone (Narcan) is an opioid antagonist that can reverse the effects of an overdose. It can temporarily restore normal breathing until professional help arrives.
  3. Perform CPR: If the person has stopped breathing, CPR may be necessary while waiting for emergency services.
  4. Stay With the Person: Try to keep the person awake and breathing if they are still conscious. Roll them on their side to prevent choking if they are unconscious.

Symptoms of Overdose May Also Include the Following:

  • difficulty breathing
  • excessive drowsiness
  • loss of consciousness
  • loss of muscle tone
  • cold and clammy skin
  • fainting
  • dizziness
  • slow heartbeat

What other information should I know?

Keep all appointments with your doctor.

Before having any laboratory test, tell your doctor and the laboratory personnel that you are taking codeine.

Do not let anyone else take your medication. Selling or giving away this medication may cause death or harm to others and is illegal. Your prescription might not be refillable. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

Brand names

  • Tuzistra XR® (as a combination product containing Chlorpheniramine, Codeine)

Brand names of combination products

  • Airacof® (containing Codeine, Diphenhydramine, Phenylephrine)
  • Ala-Hist AC® (containing Codeine, Phenylephrine)
  • Allfen CD® (containing Codeine, Guaifenesin)
  • Ambenyl® (containing Bromodiphenhydramine, Codeine)
  • Ambophen® (containing Bromodiphenhydramine, Codeine)
  • Antituss AC® (containing Codeine, Guaifenesin)
  • Bitex® (containing Codeine, Guaifenesin)
  • Bromanyl® (containing Bromodiphenhydramine, Codeine)
  • Bromotuss® with Codeine (containing Bromodiphenhydramine, Codeine)
  • Brontex® (containing Codeine, Guaifenesin)
  • Bron-Tuss® (containing Codeine, Guaifenesin)
  • Brovex CB® (containing Brompheniramine, Codeine)
  • Brovex PBC® (containing Brompheniramine, Codeine, Phenylephrine)
  • Calcidrine® (containing Anhydrous Calcium Iodide, Codeine)
  • Cheracol® with Codeine (containing Codeine, Guaifenesin)
  • Cheratussin® (containing Codeine, Guaifenesin)
  • Codafen® (containing Codeine, Guaifenesin)
  • Codimal PH® (containing Codeine, Phenylephrine, Pyrilamine)
  • Cotab A® (containing Chlorpheniramine, Codeine)
  • Demi-Cof® (containing Chlorpheniramine, Codeine, Phenylephrine, Potassium Iodide)
  • Dex-Tuss® (containing Codeine, Guaifenesin)
  • Diabetic Tussin C® (containing Codeine, Guaifenesin)
  • Dicomal-PH® (containing Codeine, Phenylephrine, Pyrilamine)
  • Duraganidin NR® (containing Codeine, Guaifenesin)
  • EndaCof AC® (containing Brompheniramine, Codeine)
  • Endal CD® (containing Codeine, Diphenhydramine, Phenylephrine)
  • ExeClear-C® (containing Codeine, Guaifenesin)
  • Gani-Tuss NR® (containing Codeine, Guaifenesin)
  • Giltuss Ped-C® (containing Codeine, Guaifenesin, Phenylephrine)
  • Glydeine® (containing Codeine, Guaifenesin)
  • Guaifen AC® (containing Codeine, Guaifenesin)
  • Guiatuss AC® (containing Codeine, Guaifenesin)
  • Guiatussin® with Codeine (containing Codeine, Guaifenesin)
  • Halotussin AC® (containing Codeine, Guaifenesin)
  • Iophen® (containing Codeine, Guaifenesin)
  • Mar-cof CG® (containing Codeine, Guaifenesin)
  • Maxiphen CD® (containing Codeine, Guaifenesin, Phenylephrine)
  • M-Clear WC® (containing Codeine, Guaifenesin)
  • M-End PE® (containing Brompheniramine, Codeine, Phenylephrine)
  • Mytussin AC® (containing Codeine, Guaifenesin)
  • Nalex® AC (containing Brompheniramine, Codeine)
  • Notuss AC® (containing Chlorpheniramine, Codeine)
  • Notuss PE® (containing Codeine, Phenylephrine)
  • Pediacof® (containing Chlorpheniramine, Codeine, Phenylephrine, Potassium Iodide)
  • Pedituss® (containing Chlorpheniramine, Codeine, Phenylephrine, Potassium Iodide)
  • Pentazine VC® (containing Codeine, Phenylephrine, Promethazine)
  • Pentazine® with Codeine (containing Codeine, Promethazine)
  • Phenergan® VC with Codeine (containing Codeine, Phenylephrine, Promethazine)
  • Phenergan® with Codeine (containing Codeine, Promethazine)
  • Poly-Tussin AC® (containing Brompheniramine, Codeine, Phenylephrine)
  • Prometh® with Codeine (containing Codeine, Guaifenesin, Promethazine)
  • Robafen AC® (containing Codeine, Guaifenesin)
  • Robichem AC® (containing Codeine, Guaifenesin)
  • Robitussin® AC (containing Codeine, Guaifenesin)
  • Rolatuss® (containing Ammonium Chloride, Chlorpheniramine, Codeine, Phenylephrine)
  • Romilar AC® (containing Codeine, Guaifenesin)
  • Tusnel C® (containing Brompheniramine, Codeine, Guaifenesin)
  • Tussi Organidin® (containing Codeine, Guaifenesin)
  • Tussiden C® (containing Codeine, Guaifenesin)
  • Tussirex® (containing Caffeine, Codeine, Pheniramine, Phenylephrine, Salicylic Acid)
  • Tusso-C® (containing Codeine, Guaifenesin)
  • Vanacof® (containing Codeine, Dexchlorpheniramine, Phenylephrine)
  • Z Tuss AC® (containing Chlorpheniramine, Codeine)
  • Zodryl AC® (containing Chlorpheniramine, Codeine)
  • Zotex C® (containing Codeine, Phenylephrine, Pyrilamine)

This branded product is no longer on the market. Generic alternatives may be available.

How to Prevent Codeine Abuse

  1. Education and Awareness: Raising awareness about the risks of codeine misuse and the signs of opioid addiction can help people make informed choices and recognize when they or others may be at risk.
  2. Prescription Monitoring: Healthcare providers should carefully monitor prescriptions, limiting the amount of codeine prescribed and tracking patient use through prescription drug monitoring programs (PDMPs).
  3. Proper Disposal of Medications: Patients should be educated about how to safely dispose of leftover codeine to prevent misuse by others.
  4. Regulation and Control: Governments can regulate the sale of codeine-containing products, making them available only by prescription or limiting quantities to reduce easy access.
  5. Screening and Support: Screening for substance abuse in healthcare settings and providing early interventions, including counseling or treatment for those at risk of misuse, can reduce the chances of addiction.
  6. Alternative Treatments: Physicians can explore non-opioid alternatives for managing pain or cough, reducing reliance on codeine-containing medications.

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