Codeine – action, indications, side effects and dosage

Proven content

Codeine is a component of drugs that primarily relieve pain and cough. Most often we find it in cough or cold syrups. Used in accordance with the doctor’s recommendations, it effectively reduces the symptoms of the disease, but overuse of drugs with codeine can lead to addiction. What is codeine and how does it work? What are the indications for its use? When should you not use codeine, and what side effects can it cause? Which drugs contain codeine?

What is codeine? General characteristics

Codeine is an organic chemical compound from the group of alkaloids, also known as methylmorphine or a methyl derivative of morphine.

Codeine occurs naturally in opium, i.e. the milky juice of unripe poppy seeds. Opium obtained from poppy seeds is a substance containing about 20 alkaloids, including: morphine, codeine (0,7-2,5%), thebaine, papaverine and narcotic drugs. Opium is a compound that has been used as a pain reliever since antiquity. The codeine content of opium is 07-2,5%.

Codeine was first identified and isolated in pure form in 1832 by the French chemist and pharmacist Pierre Jean Robiquet. It was introduced to the pharmaceutical market in 1950.

Codeine exists as a white to off-white crystalline powder or colorless crystals. This compound is easily dissolved in boiling water and 96% ethanol.

Codeine has an analgesic, antitussive and antidiarrheal effect. It causes euphoria, drowsiness, blissful apathy, makes us insensitive to unpleasant sensations, slows down the peristalsis of the stomach and intestines, and causes the loss of hunger.

Codeine is a component of medicinal products, most often in the form of syrup, tablets, coated or effervescent tablets.

Need an e-Prescription for painkillers urgently? Sign up for an online consultation and you will receive an e-Prescription even in 10 minutes.

Codeine – mechanism of action

Codeine is a drug classified as a drug. It works by affecting opioid receptors. The mechanism of the central analgesic effect of opioid drugs is related to the inhibition of the transmission of pain stimuli to the central nervous system.

Codeine’s mechanism of action is associated with its conversion to morphine. It is morphine that is responsible for the analgesic effect of codeine.

For some people, codeine is converted into morphine much faster, resulting in high levels of morphine in the body. Codeine is similar to morphine – it is primarily a pain reliever.

Additionally, codeine reduces the secretion of mucus in the respiratory tract and causes the secretion to thicken. It has an antitussive effect by inhibiting the cough reflex. Codeine depresses the respiratory center, which leads to slower and shallow breathing.

Codeine has also been shown to have a constrictive effect, slowing down intestinal peristalsis and gastric emptying, and at the same time contracting the sphincters. Its action causes the constriction of the pupils, the release of histamine from mast cells or an increase in the tone of smooth muscles. Codeine lowers the seizure threshold and affects the endocrine secretion of the hypothalamic-pituitary axis.

The duration of the action of codeine is 2 to 6 hours. This drug passes into the milk of nursing mothers in trace amounts.

What should you know about pain medications? Check: From Opium to Ibuprofen – The History of Painkillers

Codeine – absorption and metabolism

Codeine, like other drugs, is metabolized by a complex of liver enzymes. About 90% of the dose taken is excreted in the urine within the first 24 hours after taking codeine. The entire ingested dose of codeine is excreted within 48 hours.

Codeine metabolites are:

1. morphine – formed by the demethylation of codeine. It is morphine that is thought to be the metabolite responsible for the analgesic effect of codeine;
2. norcodeine.

Morphine and norcodeine are then further metabolised by glucuronidation.

Some people have the so-called ultrafast codeine metabolismwhich leads to significantly higher than normal levels of morphine in the blood after taking codeine.

What should I know about addictive pain medications? Check: These painkillers and sedatives are the fastest to addict

Codeine – indications for use

Codeine is a compound that is part of drugs with analgesic, antitussive and anti-diarrheal properties.

The indications for the use of codeine may be:

1. dry cough;
2. diarrhea;
3. strong pain;
4. arthralgia;
5. osteoarthritis;
6. post-traumatic pain;
7. irritable bowel syndrome.

What is chronic pain and how do I deal with it? Check: Chronic pain – what drugs should not be used? Paracetamol, ibuprofen, and aspirin are not suitable for treating chronic pain

Strengthen your body with natural supplements – try the dietary supplement with Chang Shan extract available on Medonet Market.

Codeine – contraindications to use

Codeine, despite its effectiveness in combating pain or cough, cannot be used by every patient struggling with this type of ailments.

Medicines with codeine can not be used:

1. children up to 12 years of age;
2. children from 12 to 18 years of age with breathing problems;
3. breastfeeding mothers as codeine is passed on to babies through their milk;
4. women in the first trimester of pregnancy;
5. people of all ages with known rapid conversion of codeine into morphine.

In addition, the following ailments are among the contraindications to the use of drugs with codeine:

1. bronchial asthma;
2. sleep apnea;
3. respiratory failure;
4. breathing disorders;
5. constipation;
6. cystic fibrosis;
7. opioid addiction;
8. tonsil removal procedure in children and adolescents;
9. coma.

Medicines with codeine should not be taken by patients who are hypersensitive to this compound.

Is the use of painkillers safe? Read on: Are you still taking your painkillers? It could end up with a heart attack

Codeine – precautions

When using codeine, the precautions contained in the package leaflets should be observed.

However, it is worth remembering that when using codeine, care should be taken in the following:

1. in patients with head injuries;
2. after surgery to remove the gallbladder;
3. in patients with diseases of the biliary tract;
4. in patients with an enlarged prostate or problems with the drainage of urine;
5. in patients with hypothyroidism;
6. in patients with adrenal insufficiency;
7. in patients coughing up mucus. 

What is pain and how to treat it? Check: Pain – types, mechanism of action, treatment

Codeine – proper dosage

The correct dose of codeine depends on the form that has been prescribed by your doctor. In medicine, the following substances are used: codeine, codeine phosphate sesquihydrate, codeine phosphate hemihydrate, codeine hydrochloride dihydrate, as substances with analgesic and antitussive properties. The form of codeine most commonly prescribed by doctors is phosphate.

The dosage of the above-mentioned forms is as follows:

1. codeine – the usual single dose is 0,01 g-0,02 g. The usual daily dose is 0,06 g. A single maximum dose is 0,04 g, and the maximum daily dose is 0,24 g;
2. codeine phosphate sesquihydrate – the usual single dose is 0,01g-0,03g. The usual daily dose is 0,06 g. A single maximum dose is 0,06 g, and the maximum daily dose is 0,24 g;
3. codeine hydrochloride dihydrate – the usual single dose is 0,01g-0,03g. The usual daily dose is 0,06 g. The maximum single dose is: 0,06 g, and the maximum daily dose is 0,24 g;
4. codeine phosphate hemihydrate – (used orally or rectally): the usual single dose is 0,03 g. The usual daily dose is 0,06 g. The maximum single dose is 0,06 g, while the maximum daily dose is 0,24 g.

How Can I Deal With Pain? Check: Pain Treatment

Codeine – misuse of the drug

Improper use of codeine is considered to be taking more than the recommended dose of the drug or omitting the indicated dose during the day.

Codeine overdose has been associated with unpleasant symptoms such as confusion, somnolence, shallow breathing, narrowed pupils, nausea, vomiting, constipation and loss of appetite. Very high doses of codeine can lead to severe cardio-respiratory depression and, ultimately, death.

How to take medication correctly? Check: How to take medications effectively?

Codeine – side effects

Codeine, like any other drug, can cause side effects in patients. It is important to report any suspected adverse reactions after authorization of the medicinal product so that the benefit / risk balance of the medicinal product can be monitored.

The frequency classification of adverse body reactions (ADRs) is based on the following principles: very common (≥1 / 10), common (≥1 / 100 to <1/10), uncommon (≥1 / 1 to <000/1), rare (≥ 100 / 1 to <10 / 000), very rare (<1 / 1), not known (cannot be estimated from the available data).

Side effects common to codeine use there are constipation, dizziness and drowsiness.

Uncommonly after using codeine headache, urinary retention, dry mouth, respiratory depression, confusion, tremor, euphoria, vomiting, restlessness, blurred vision, nausea, rash, fainting, changes in blood pressure, insomnia, laryngospasm, bronchospasm, hallucinations, double vision may occur , abnormal dreams, loss of appetite, weakness, constriction of the pupils, dysphoria, stomach cramps, abnormal heart rhythm, paralytic ileus, and toxic dilatation of the colon.

With an unknown frequency they may occur fatigue, visual disturbance, mood changes, bradycardia, decreased libido, diarrhea, excessive sweating, erectile dysfunction, anorexia, fever, sexual dysfunction, drug addiction, depression, hypothermia, potency disorders, dyspnoea, hyperglycaemia, edema, anorexia, palpitations, redness, circulatory depression, withdrawal symptoms, urticaria, biliary spasms, confusion, cardiac arrest, shock, drug tolerance, pruritus, hypotension, tachycardia, gastrointestinal disturbances, pancreatitis, malaise or respiratory arrest.

How to deal with pain without medication? Check: Five natural remedies for pain. You don’t have to take the pills

Codeine – interactions with other drugs

Before starting treatment with codeine, please inform your doctor or pharmacist about all medications you are taking or have recently taken. You should also inform what medications the patient plans to take in the near future.

Codeine should not be used simultaneously with:

1. MAO inhibitors – enhances the anticoagulant effect of anticoagulants;
2. anti-ulcer antacids – intensify the depressive effect of codeine;
3. with ethyl alcohol – enhances the sedative effect of codeine;
4. XNUMXst generation antihistamines – intensify the depressive effect of codeine on the central nervous system;
5. neuroleptics – intensify the depressive effect of codeine on the central nervous system;
6. benzodiazepines and barbiturates – to a large extent increase the overall effect of codeine on the central nervous system.

Which drugs should never be combined with each other? Check: Dangerous interactions

Codeine – similar active substances

There are substances known on the pharmaceutical market that exhibit a similar mechanism of action to codeine. These are:

1. difenoksylat – is a pethidine derivative with an agonist effect on opioid receptors located in the intestines. This substance is used in the symptomatic treatment of acute diarrhea as an agent for short-term use or for longer treatment of chronic diarrhea, e.g. in the course of ulcerative colitis or Crohn’s disease. Diphenoxylate is also used to reduce the amount of faecal fluid after an ileostomy or colostomy;
2. dihydrokodeina – is an opioid with analgesic and antitussive properties. The drug is used in the relief of severe anti-cancer pain and in the treatment of long-term pain of a different origin;
3. fentanyl – are strong painkillers that act on opioid receptors. It is used to treat short-term pain exacerbations due to cancer in people who are taking other opioid medicines before. It is a drug used to treat long-term severe pain;
4. lewometadon – is a synthetic opioid similar to morphine. Indicated for the treatment of opioid addiction in combination with appropriate psychotherapy;
5. methadone – is a synthetic opioid with a strong analgesic effect. It is used to treat severe pain associated with cancer and after surgery. In addition, methadone is used to relieve the symptoms of withdrawal syndrome that occurs after opiate and opioid withdrawal. The compound is also used in substitution treatment in addiction to heroin and morphine;
6. morphine – is a psychoactive substance contained in opium. It is used to treat moderate to severe pain that does not go away with less-effective drugs;
7. oxycodone – is a strong pain reliever from the group of opioids called narcotic pain relievers. The indication for use is the treatment of moderate to severe pain that requires opioid treatment, often in combination with other analgesics, e.g. paracetamol, ibuprofen, aspirin, naloxone and naltrexone;
8. if that – is an opioid medicine with a strong analgesic effect. It is used to treat severe pain of various origins. It is given, inter alia, in acute myocardial infarction, hepatic and renal colic or postoperative pain. The drug is also used in premedication before surgery;
9. remifentanyl – is a selective opioid agonist with a potency comparable to fentanyl. Used as an anesthetic in anesthesia to induce or maintain general anesthesia, and immediately after surgery to provide short-term anesthesia before taking other long-acting painkillers. Another indication is the anesthesia of mechanically ventilated persons in the intensive care unit;
10. tapentadol – is a modern pain reliever. The indication for the use of tapentadol is the alleviation of moderate to severe acute pain. Due to its long duration of action, it is used in the case of chronic pain as a XNUMX-hour pain reliever. Tapentadol is indicated in patients with a history of troublesome nausea and vomiting after using other opioid analgesics;
11. tramadol – is a strong pain reliever from the group of opioids called narcotic pain relievers. It is used in the treatment of acute or chronic pain, as well as post-traumatic, post-operative and neoplastic pain. It is also used in palliative care in the treatment of acute and chronic pain of moderate and severe intensity. 

What are opioids and how do they work? Check: Opioids

Codeine and addiction

Codeine is a compound that can cause addiction in patients, both psychologically and physically. First of all, it develops very quickly mental dependence on codeinebecause it is related to the desire to experience the state of codeine.

Physical dependence on codeine and it takes about 6-12 months to develop. Discontinuation of codeine after this time causes withdrawal symptoms, such as irritability, lack of willingness to act, flu-like symptoms, depressive symptoms, sleep problems, headaches and a strong need to take the drug.

However, it is worth remembering that codeine is safe if it is taken briefly, as directed, and preferably after consulting a doctor first.

In order to reduce the risk of codeine addiction, from January 1, 2017, patients can only buy one small package of the drug with codeine (up to 150 mg of the substance in the package) at a pharmacy without a prescription. We currently have a Psychoactive Substances Shipping Test – a semi-quantitative test that shows the presence of codeine in the blood. It can be performed, for example, on a control at the workplace.

How to recognize drug addiction? Read: Dependence on pain medications

Drugs with codeine

Codeine is usually a component of other analgesic, antitussive or anti-diarrheal drugs in the form of syrup or tablets: coated or effervescent:

1. Thiocodin – a drug in syrup or tablets available without a prescription. Codeine content: 15 mg / tablet. It’s a cough suppressant. Thiocodin contains two active substances: codeine and sulfowaacol. The former reduces the frequency of coughing, while the latter facilitates expectoration. The drug is used in a dry, persistent cough without expectoration;
2. Sirupus Pini compositus – drug in syrup available without a prescription. Codeine content: 50 mg / 100 mg. It is a reliever medicinal product used in dry, exhausting cough in the course of catarrh of the upper respiratory tract;
3. HerbaPini – a drug in syrup available without a prescription. Codeine content: 50 mg / 100 mg. It’s a cough suppressant. The syrup contains codeine phosphate, administered temporarily in dry, exhausting cough that accompanies catarrh of the upper respiratory tract; 
4. Aflofarm complex pine syrup – a medicine in syrup available without a prescription. Codeine content: 9,72 mg / 15ml. It’s a cough suppressant. The syrup is indicated for immediate use during tiring, dry cough occurring in the course of catarrh of the upper respiratory tract;
5. Nurofen Plus – a drug in coated tablets available without a prescription. Codeine content: 12,8 mg / tablet. It’s a pain reliever. The drug is indicated for use in rheumatic and muscle pain, back pain, neuralgia, migraine, headache, toothache, dysmenorrhea, fever in the course of a cold or flu;
6. Neoazarina – a drug in coated tablets available without a prescription. Codeine content: 10 mg / tablet. It’s a cough suppressant. The indication for the use of the drug is catarrh of the upper respiratory tract in severe paroxysmal coughing attacks, including nocturnal coughing attacks;
7. Antidol 15 – drug in tablets available without a prescription. Codeine content: 15 mg / tablet. It’s a pain reliever. Indicated for short-term use in pain of various origins, such as headache, tooth extraction, osteoarticular, menstrual pain;
8. Efferalgan Codeine – a drug in effervescent tablets available on prescription. Codeine content: 30 mg / tablet. It is an analgesic, antitussive and antipyretic drug. Indicated in pain of various origins, e.g. headache, toothache, joint pain, post-traumatic, postoperative, menstrual pain and pains accompanying cancer; in feverish conditions, colds and flu, especially with a dry, tiring cough;
9. Solpadeine – a drug in capsules, tablets and effervescent tablets available without a prescription. Codeine content: 8 mg / tablet. It is a pain reliever, antipyretic and antitussive drug. The indications are headache, toothache, rheumatic pain, throat pain, dysmenorrhea, neuralgia, migraine, cold and flu symptoms;
10. Solpadeine Max – a drug in effervescent tablets available without a prescription. Codeine content: 12,8 mg / tablet. It’s a pain reliever. It is used to relieve pain that requires a greater effect than over-the-counter painkillers such as migraine, sciatica, sprains;
11. Talvosilen – a drug in tablets available on prescription. Codeine content: 20 mg / tablet. It is an analgesic, antitussive and antipyretic drug. Indicated in fever, colds, flu, especially when accompanied by a dry cough. In the treatment of pain of various origins: head, joints, teeth, menstrual, radicular, after injuries and surgeries, in neoplastic diseases. The drug is recommended in the fight against pain in cancer;
12. Talvosilen forte – a drug in capsules available on prescription. Codeine content: 30 mg / tablet. It is an analgesic, antitussive and antipyretic drug. Indicated in fever, colds, flu, especially when accompanied by a dry cough. In the treatment of pain of various origins: head, joints, teeth, menstrual, radicular, after injuries and surgeries, in neoplastic diseases. The drug is recommended in the fight against pain in cancer;
13. Ultracod – a drug in tablets available on prescription. Codeine content: 30 mg / tablet. It is a pain reliever and antipyretic drug. The preparation is indicated in adults for the treatment of moderate to severe pain. The preparation is indicated in adolescents 12–18 years of age. for the treatment of moderate acute pain that is not relieved by other painkillers used on its own, such as paracetamol or ibuprofen.

What are anti-inflammatory drugs and which one to choose? Check: Anti-inflammatory drugs – which ones to choose for your ailment?