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Codeine Abuse and Addiction

How Long Does Codeine Stay in Your System?

Codeine belongs to the class of opioids, a common prescription medicine used as an antitussive and analgesic. Sometimes it is also used to control severe diarrhea. Codeine is composed of methylated morphine, which is a significant alkaloid found in opium. Codeine is available as Codeine Phosphate and Codeine Sulphate in the United States. The specific Pharmacodynamics are still unknown but they carry out almost a similar mechanism of action as morphine. The drug acts on the mu-receptors in the brain. Feelings of euphoria, pain relief, and relaxation get elicited within few minutes of administration. Codeine carries a high potential for abuse and addiction. It is classified as Schedule II drug. The chronic use of the drug impairs physical and mental functions. To avoid detrimental effects, it is necessary to know the mechanisms and time durations of Codeine elimination from the body.

How long does Codeine stay in your system?

After stopping the drug usage, it takes some time to have it completely eliminated from the system. A time gap is present between the ingestion and full clearance of drug from the body. The half-life of Codeine ranges from 2.4 hours to 2.9 hours. Most of the sources have reported the half-life to be 2.9 hours. It means the consumed drug will get removed within 3 hours. For 100% clearance, the drug will take nearly 16 hours. In cases of fast metabolizers, the drug will take about 13.2 hours.

The metabolites of Codeine include codeine-6-glucuronide and morphine-3-glucuronide. They take more time for elimination than Codeine. The metabolites can take up to 24 hours to get removed from the body. Mostly after 24 hours, none of the remnants of drug can be detected in the body.

Factors that influence how long Codeine stays in your system:

There are many factors that influence the metabolism and excretion of drug. In some people, the process is more rapid than others while some take a much longer duration to eliminate the drug. This is due to certain variables that act to discriminate the time intervals.

Individual Factors:

Two individuals taking the same amount of drug may eliminate at different time intervals. It is due to the following factors.

  • Age:A young individual has a better physiological health, liver, and kidney functioning so he is capable of metabolizing and excreting at faster rates as compared to elderly people.
  • Body parameters:The height and weight of a person also alter the rate of drug elimination. The larger an individual, the more efficient and faster is the metabolism as compared to a smaller individual in terms of height and weight.
  • Genetics:The genetics play an important role in regulating the enzymes of the body. People exhibiting the alleles for CYP2D6 gene are called as rapid metabolizers as their metabolism is faster than other people.
  • Liver and kidney function: They are the organs directly involved in the various processes to excrete the drug out of the system. Optimum functioning is necessary for a faster rate. Any malfunctioning due to a disease process or trauma can slow down the rate. The prolonging of clearance time is further dependant on the degree of impairment.
  • Basal Metabolic Rate (BMR): Though BMR plays a significant role in the clearance process. However, people having a faster BMR tend to eliminate the drug more rapidly than other people.
  • Urinary pH: It plays a major role as the drug gets absorbed from the kidney tubules and keeps circulating in the system before it can be finally excreted out of the system. Acidic pH prevents the recirculation and excretes maximum drug at each time. Care should be taken while taking acidifying agents as they can lead towards acidosis, which can be a harmful condition.

Frequency of drug ingestion:

The more frequently the drug is consumed, more it has the chances to get accumulated in the body. The body has a certain capacity to metabolize drug at a single time. Taking the drug over and over again will slow down the metabolism and excretion of Codeine.

Co-administration of medicines:

Some drugs act as the inducers of hepatic enzymes and many drugs act as inhibitors. Rifampicin and Dexamethasone can expedite the metabolism of Codeine. Amiodarone, Clomipramine, Celecoxib, Haldol, and Diltiazem act as CYP2D6 inhibitors and slow down the metabolism of Codeine.

Dosages of Codeine:

Higher doses require more time to get cleared from the system. This results due to storage of Codeine inside the body.

Duration of use:

The longer durations of abuse lead to a slower metabolism and excretion process of Codeine.

Codeine absorption, metabolism, and excretion:

Codeine is a pro-drug, which means it stays inactive unless metabolized and broken down into active ingredients. Codeine is absorbed through the gastrointestinal tract into the portal circulation. The maximum concentration of Codeine is attained within 1 hour of ingestion. About 7-25 % of drug binds to the plasma proteins and doesn’t accumulate in the body tissues.

There are a variety of enzymes that act on Codeine like UGT2B7, CYP3A4, and CYP2D6. The UGT2B7/UGT2B4 performs 70-80% of the conjugation with the glucuronic acid to form metabolite such as codeine-6-glucuronide (C6G). The CYP2D6 converts 5-10% of Codeine through O-demethylation into morphine and the same enzyme converts 15 percent of Codeine into Narcodeine through N-demethylation.  The codeine-6-glucuronide (C6G) and morphine are the major metabolites that act on the mu-opioid receptors to elicit the analgesic effects. Narcodeine and morphine undergo further conjugation to form morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G).

The excretion of 90% of codeine takes place through kidneys within 24 hours of the last ingestion. The 10% is the unchanged drug and rest 80% is due to the metabolites; codeine-6-glucuornide (C6G) makes up the greatest percentage (70%) of metabolites. A little amount of drug also gets excreted through feces.

Different types of Codeine drug tests:

There are different ways for the detection of Codeine in the body. The variety of test includes urine tests, blood tests, hair analysis, and salivary tests.

  • Urine Tests:

The fresh urine samples are collected from the patient and tested in laboratory for the detection of codeine metabolites. Urine tests are non-invasive and provide a longer duration of stay of drug particles in the samples. The body should have 2000 ng/ml of Codeine in order to avoid the false positive results. Codeine and its metabolites appear in urine within few hours of ingestion and stay up to 24 hours. After 1 day, it is highly unlikely to detect Codeine in urine. Some tests like EMIT (enzyme multiplied immunoassay technique) and GC/MS (gas chromatography/mass spectrometry) can detect Codeine even up to 52 hours after the last ingestion of drug.  The cases of renal impairment may lead to slow excretion, taking up more time.

  • Hair Tests:

It is a less commonly used modality for identification of drug. Hair follicles from the head are plucked and sent for laboratory analysis. The research studies have confirmed the presence of Codeine within 15 minutes of 120 mg administered dose. A one cm new hair growth can show the traces of Codeine. The detection period stays for as many as ten weeks or 70 days, making it a useful test for various purposes. The hair color affects the detection with a lesser probability in cases of red or blonde hair. Moreover, the metabolites like glucuronides and morphine are not detectable in hair.

  • Salivary Tests:

These tests are quick to perform and are non-invasive. Saliva tests are a preferred modality in many circumstances. Codeine concentrations peak at 30 minutes to 2 hours after administration of drug. The test can detect the drug within 15 minutes and up to 24 hours after consumption. A drawback associated with it is that other substances in the saliva can interfere with the test results.

  • Blood Tests:

They are the less performed tests due to a short window period of detection and invasive nature. However, they become useful in cases of overdose and cases of Codeine-related complications. After collection of the blood sample, it is quickly analyzed to generate the results.  Codeine can be detected within minutes of ingestion. Peak levels are attained in 1 to 2 hours. The blood tests can detect the drug within 16 hours of the final dose.

Tips to clear Codeine from the system faster:

There are many methods that can expedite the process of drug clearance from the body. It is important to discuss with a doctor before practicing these tips.

  • The first step is to stop the use of Codeine. Some people have a misconception that small doses will not affect the clearance. To fully eliminate the drug, a person has to completely stop the use.
  • Many medicines and supplements can enhance the rate of metabolism.  Such substances act as the ‘enzymatic inducers’.
  • Change urinary pH to make it more acidic. This leads to a rapid clearance.
  • Stay hydrated as it allows the proper urinary flow and thus enough excretion of the drug.
  • Regular exercise improves the circulation and speeds up the clearance.