Codeine is an opiate used to treat pain, coughing, and diarrhea. It is typically used to treat mild to moderate degrees of pain. Greater benefit may occur when combined with paracetamol or a nonsteroidal anti-inflammatory drug such as aspirin or ibuprofen. Wikipedia
IUPAC ID: (5α,6α)-7,8-didehydro-4,5-epoxy- 3-methoxy-17-methylmorphinan-6-ol
Other names: 3-Methylmorphine
Onset of action: 15–30 minutes
Elimination half-life: 2.5–3 hours
Duration of action: 4–6 hours
- It can treat pain and cough.
- Controlled substance
- High risk for addiction and dependence (which may lead do Codeine withdrawal). Can cause respiratory distress and death when taken in high doses or when combined with other substances, especially alcohol.
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- Availability: Prescription needed
- Pregnancy: Consult a doctor
- Alcohol: Avoid. Very serious interactions can occur
- Drug class: Opiate, Opioid
Codeine or 3-methylmorphine is an opiate used to treat pain, as a cough medicine, and for diarrhea. It is often sold as a salt in the form of either codeine sulfate or codeine phosphate in the United States and Australia; codeine hydrochloride is more common worldwide and the citrate, hydroiodide, hydrobromide, tartrate, and other salts are also seen. Codeine is the second-most predominant alkaloid in opium, at up to three percent. Although codeine can be extracted from natural sources, a semi-synthetic process is the primary source of codeine for pharmaceutical use. It is considered the prototype of the weak to midrange opioids. In 2013 about 361,000 kilograms of codeine were produced while 249,000 kilograms were used. It is the most commonly taken opiate. It is on the WHO Model List of Essential Medicines, a list of the most important medication needed in a basic health system.
- Codeine anhydrous
- Morphine monomethyl ether
- Morphine 3-methyl ether
- Morphine-3-methyl ether
- Norcodine, N-methyl
- Norcodeine, N-methyl
- CODEINE BASE
- Codeine polistirex
- CCRIS 7555
- Morphine-3-methyl ester
- HSDB 3043
- EINECS 200-969-1
- Morphinan-6-ol, 7,8-didehydro-4,5-epoxy-3-methoxy-17-methyl-, (5alpha,6alpha)-
- Codeine Anhydrate
- Morphinan-6alpha-ol, 7,8-didehydro-4,5alpha-epoxy-3-methoxy-17-methyl-
- Morphinan-6-alpha-ol, 7,8-didehydro-4,5-alpha-epoxy-3-methoxy-17-methyl-
- Codeine [INN:BAN]
- Novahistine DH
- Codeine Alkaloid
- Codeine USP
- N-methyl norcodine
- Codeine (anhydrous)
- Codalgin Forte Codate
- morphine monomethy l ether
- Epitope ID:120369
- Codeine polistirex [USAN]
- 3-o-methylmorphine monohydrate
- Codeine 0.1 mg/ml in Methanol
- Codeine 1.0 mg/ml in Methanol
- Codeine, European Pharmacopoeia (EP) Reference Standard
- 7,8-didehydro-4,5-ep oxy-3-methoxy-17-methylmorphinan-6-ol
- CODEINE (SEE ALSO: CODEINE PHOSPHATE (CAS 52-28-8))
- 7,8-didehydro-4,5-epoxy-3-methoxy-17-methyl-(5alpha, 6alpha)-morphinan 6-ol
- Codeine solution, 1 mg/mL in methanol, ampule of 1 mL, certified reference material
- Codeine solution, analytical standard, for drug analysis, 1.0 mg/mL in methanol
- Morphinan-6-ol, 7,8-didehydro-4,5-epoxy-3-methoxy-17-methyl-, (5-alpha,6-alpha)-
- Morphinan-6-ol, 7,8-didehydro-4,5-epoxy-3-methoxy-17-methyl-, (5-alpha,6-alpha)- (9CI)
- Morphinan-6-ol, 7,8-didehydro-4,5-epoxy-3-methoxy-17-methyl-, (5alpha,6alpha)- (9CI)
- Morphinan-6alpha-ol, 7,8-didehydro-4,5alpha-epoxy-3-methoxy-17-methyl- (8CI)
- 10-methoxy-4-methyl-(1S,5R,13R,14S,17R)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10,15-tetraen-14-ol phosphate(codeine)
- 10-methoxy-4-methyl-(1S,5R,13R,14S,17R)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10,15-tetraen-14-ol(codeine (H3PO4))
- 10-methoxy-4-methyl-(1S,5R,13R,14S,17R)-12-oxa-4-azapentacyclo[9.6.1.01,13.05,17.07,18]octadeca-7(18),8,10,15-tetraen-14-ol(codeine phosphate)
Codeine may be habit forming. Take codeine exactly as directed. Do not take more of it, take it more often, or take it in a different way than directed by your doctor. While taking codeine, discuss with your healthcare provider your pain treatment goals, length of treatment, and other ways to manage your pain. Tell your doctor if you or anyone in your family drinks or has ever drunk large amounts of alcohol, uses or has ever used street drugs, or has overused prescription medications, or if you have or have ever had depression or another mental illness. There is a greater risk that you will overuse codeine if you have or have ever had any of these conditions. Talk to your healthcare provider immediately and ask for guidance if you think that you have an opioid addiction or call the U.S. Substance Abuse and Mental Health Services Administration (SAMHSA) National Helpline at 1-800-662-HELP.
Codeine may cause serious or life-threatening breathing problems, especially during the first 24 to 72 hours of your treatment and any time your dose is increased. Your doctor will monitor you carefully during your treatment. Tell your doctor if you have or have ever had slowed breathing or asthma. Your doctor will probably tell you not to take codeine. Also tell your doctor if you have or have ever had lung disease such as chronic obstructive pulmonary disease (COPD; a group of diseases that affect the lungs and airways), a head injury or any condition that increases the amount of pressure in your brain. The risk that you will develop breathing problems may be higher if you are an older adult or are weak or malnourished due to disease. If you experience any of the following symptoms, call your doctor immediately or get emergency medical treatment: slowed breathing, long pauses between breaths, or shortness of breath.
When codeine was used in children, serious and life-threatening breathing problems such as slow or difficulty breathing and deaths were reported. Codeine should never be used to treat pain or a cough in children younger than 18 years of age. If your child is currently prescribed a cough and cold medicine containing codeine, talk to your child’s doctor about other treatments.
Taking certain medications during your treatment with codeine may increase the risk that you will experience breathing problems or other serious, life-threatening breathing problems, sedation, or coma. Tell your doctor if you are taking or plan to take any of the following medications: certain antibiotics such as erythromycin (Erytab, Erythrocin); certain antifungal medications including ketoconazole; benzodiazepines such as alprazolam (Xanax), diazepam (Diastat, Valium), estazolam, flurazepam, lorazepam (Ativan), and triazolam (Halcion); carbamazepine (Carbatrol, Epitol, Equetro, Tegretol, Teril); certain medications for human immunodeficiency virus (HIV) including indinavir (Crixivan), nelfinavir (Viracept), and ritonavir (Norvir, in Kaletra); medications for mental illness or nausea; other medications for pain; muscle relaxants; phenytoin (Dilantin, Phenytek); rifampin (Rifadin, Rimactane, in Rifamate); sedatives; sleeping pills; or tranquilizers. Your doctor may need to change the dosages of your medications and will monitor you carefully. If you take codeine with any of these medications and you develop any of the following symptoms, call your doctor immediately or seek emergency medical care: unusual dizziness, lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness. Be sure that your caregiver or family members know which symptoms may be serious so they can call the doctor or emergency medical care if you are unable to seek treatment on your own.
Drinking alcohol or using street drugs during your treatment with codeine also increases the risk that you will experience these serious, life-threatening side effects. Do not drink alcohol, take prescription or nonprescription medications that contain alcohol, or use street drugs during your treatment.
Tell your doctor if you are pregnant or plan to become pregnant. If you take codeine regularly during your pregnancy, your baby may experience life-threatening withdrawal symptoms after birth. Tell your baby’s doctor right away if your baby experiences any of the following symptoms: irritability, hyperactivity, abnormal sleep, high-pitched cry, uncontrollable shaking of a part of the body, vomiting, diarrhea, or failure to gain weight.
Do not allow anyone else to take your medication. Codeine may harm or cause death to other people who take your medication, especially children.
Your doctor or pharmacist will give you the manufacturer’s patient information sheet (Medication Guide) when you begin treatment with codeine and each time you refill your prescription. Read the information carefully and ask your doctor or pharmacist if you have any questions. You can also visit the Food and Drug Administration (FDA) website (http://www.fda.gov/Drugs/DrugSafety/ucm085729.htm) or the manufacturer’s website to obtain the Medication Guide.
Codeine side effects
The most frequently observed adverse reactions with codeine administration include drowsiness, lightheadedness, dizziness, sedation, shortness of breath, nausea, vomiting, sweating, and constipation. Other adverse reactions include allergic reactions, euphoria, dysphoria, abdominal pain, and pruritis.(source)
Concurrent use of other opioids, antihistamines, antipsychotics, antianxiety agents, or other CNS depressants (including sedatives, hypnotics, general anesthetics, antiemetics, phenothiazines, or other tranquilizers or alcohol) concomitantly with codeine sulfate tablets may result in additive CNS depression, respiratory depression, hypotension, profound sedation, or coma. Use codeine sulfate with caution and in reduced dosages in patients taking these agents.
Side effects of codeine include:
- low blood pressure
- irregular heart beat
- false feeling of well-being
- a general feeling of discomfort (malaise)
- contradictory (paradoxical) central nervous system stimulation
- rash or hives
- loss of appetite
- dry mouth
- bladder spasm with decreased urination
- increased liver function tests
- burning at injection site
- blurred vision
- difficulty breathing
- histamine release
- low blood pressure with IV use
- seizures with excessive doses
- respiratory depression
Rare side effects of Codeine include:
- severe allergic (anaphlactoid) reaction
Postmarketing side effects of Codeine reported include:
- severe low blood pressure
- life-threatening respiratory depression
- neonatal opioid withdrawal syndrome
- death related to ultra-rapid metabolizers of codeine
- adrenal insufficiency
- gastrointestinal adverse reactions
- feeling of excitement or happiness
- feeling of unease or dissatisfaction
- abdominal pain
- serotonin syndrome
- acute allergic reaction
- androgen deficiency
In case of emergency/overdose
In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.
While you are taking codeine, you may be told to always have a rescue medication called naloxone available (e.g., home, office). Naloxone is used to reverse the life-threatening effects of an overdose. It works by blocking the effects of opiates to relieve dangerous symptoms caused by high levels of opiates in the blood. You will probably be unable to treat yourself if you experience an opiate overdose. You should make sure that your family members, caregivers, or the people who spend time with you know how to tell if you are experiencing an overdose, how to use naloxone, and what to do until emergency medical help arrives. Your doctor or pharmacist will show you and your family members how to use the medication. Ask your pharmacist for the instructions or visit the manufacturer’s website to get the instructions. If someone sees that you are experiencing symptoms of an overdose, he or she should give you your first dose of naloxone, call 911 immediately, and stay with you and watch you closely until emergency medical help arrives. Your symptoms may return within a few minutes after you receive naloxone. If your symptoms return, the person should give you another dose of naloxone. Additional doses may be given every 2 to 3 minutes, if symptoms return before medical help arrives.
Symptoms of overdose may include the following:
- difficulty breathing
- excessive drowsiness
- loss of consciousness
- loss of muscle tone
- cold and clammy skin
- slow heartbeat
- 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.
Acetaminophen AND Codeine
acetaminophen and codeine phosphate tablet
Acetaminophen and codeine is supplied in tablet form for oral administration.
Acetaminophen, 4′-hydroxyacetanilide, a slightly bitter, white, odorless, crystalline powder, is a non-opiate, non-salicylate analgesic and antipyretic. It has the following structural formula:
Codeine phosphate, 7,8-didehydro-4,5α-epoxy-3-methoxy-17methylmorphinan-6α-ol phosphate (1:1) (salt) hemihydrate, a white crystalline powder, is a narcotic analgesic and antitussive. It has the following structural formula:
Each 300 mg/30 mg Acetaminophen and Codeine Phosphate Tablet contains:
Acetaminophen …………………………………………………………………………………………300 mg
Codeine Phosphate ……………………………………………………………………………………..30 mg
In addition each tablet contains the following inactive ingredients: magnesium stearate, microcrystalline cellulose, povidone, pregelatinized corn starch, sodium metabisulfite, sodium starch glycolate and stearic acid.
Acetaminophen has been associated with cases of acute liver failure, at times resulting in liver transplant and death. Most of the cases of liver injury are associated with the use of acetaminophen at doses that exceed 4000 milligrams per day, and often involve more than one acetaminophen-containing product. The excessive intake of acetaminophen may be intentional to cause self-harm or unintentional as patients attempt to obtain more pain relief or unknowingly take other acetaminophen-containing products.
The risk of acute liver failure is higher in individuals with underlying liver disease and in individuals who ingest alcohol while taking acetaminophen.
Instruct patients to look for acetaminophen or APAP on package labels and not to use more than one product that contains acetaminophen. Instruct patients to seek medical attention immediately upon ingestion of more than 4000 milligrams of acetaminophen per day, even if they feel well.
There have been post-marketing reports of hypersensitivity and anaphylaxis associated with use of acetaminophen. Clinical signs included swelling of the face, mouth, and throat, respiratory distress, urticaria, rash, pruritus, and vomiting. There were infrequent reports of life-threatening anaphylaxis requiring emergency medical attention. Instruct patients to discontinue Acetaminophen and Codeine Phosphate Tablets, USP immediately and seek medical care if they experience these symptoms. Do not prescribe Acetaminophen and Codeine Phosphate Tablets, USP for patients with acetaminophen allergy.
In the presence of head injury or other intracranial lesions, the respiratory depressant effects of codeine and other narcotics may be markedly enhanced, as well as their capacity for elevating cerebrospinal fluid pressure. Narcotics also produce other CNS depressant effects such as drowsiness, that may further obscure the clinical course of the patients with head injuries.
Codeine or other narcotics may obscure signs on which to judge the diagnosis or clinical course of patients with acute abdominal conditions.
Codeine is habit-forming and potentially abusable. Consequently, the extended use of this product is not recommended.
Acetaminophen and codeine phosphate tablets contain sodium metabisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in nonasthmatic people.
Drug Abuse and Dependence
Acetaminophen and Codeine Phosphate tablets are classified as a Schedule III controlled substance.
Abuse and Dependence:
Codeine can produce drug dependence of the morphine type and, therefore, has the potential for being abused. Psychological dependence, physical dependence, and tolerance may develop upon repeated administration, and it should be prescribed and administered with the same degree of caution appropriate to the use of other oral narcotic medications.
Following an acute overdosage, toxicity may result from codeine or acetaminophen.
Signs and Symptoms:
Toxicity from codeine poisoning includes the opioid triad of: pinpoint pupils, depression of respiration, and loss of consciousness. Convulsions may occur.
In acetaminophen overdosage: dose-dependent, potentially fatal hepatic necrosis is the most serious adverse effect. Renal tubular necrosis, hypoglycemic coma and coagulation defects may also occur. Early symptoms following a potentially hepatotoxic overdose may include: nausea, vomiting, diaphoresis and general malaise. Clinical and laboratory evidence of hepatic toxicity may not be apparent until 48 to 72 hours post-ingestion.
A single or multiple drug overdose with acetaminophen and codeine is a potentially lethal polydrug overdose, and consultation with a regional poison control center is recommended. Immediate treatment includes support of cardiorespiratory function and measures to reduce drug absorption.
Oxygen, intravenous fluids, vasopressors, and other supportive measures should be employed as indicated. Assisted or controlled ventilation should also be considered. For respiratory depression due to overdosage or unusual sensitivity to codeine, parenteral naloxone is a specific and effective antagonist.
Gastric decontamination with activated charcoal should be administered just prior to N-acetylcysteine (NAC) to decrease systemic absorption if acetaminophen ingestion is known or suspected to have occurred within a few hours of presentation. Serum acetaminophen levels should be obtained immediately if the patient presents 4 hours or more after ingestion to assess potential risk of hepatotoxicity; acetaminophen levels drawn less than 4 hours post-ingestion may be misleading. To obtain the best possible outcome, NAC should be administered as soon as possible where impending or evolving liver injury is suspected. Intravenous NAC may be administered when circumstances preclude oral administration.
Vigorous supportive therapy is required in severe intoxication. Procedures to limit the continuing absorption of the drug must be readily performed since the hepatic injury is dose dependent and occurs early in the course of intoxication.
In The News
UK medicines regulator ‘will consider’ ban on over-the-counter codeine
Over-the-counter codeine could be banned as fears of UK opioid addiction crisis grow
Codeine may be taken off shelf to avoid opioids crisis
What is codeine used for?
Codeine is used to relieve mild to moderate pain. It is also used, usually in combination with other medications, to reduce coughing. Codeine will help relieve symptoms but will not treat the cause of symptoms or speed recovery
How much codeine is too much?
The recommended dose of Codeine phosphate tablets (PSM) is: Adults: Given orally in divided doses of 15 mg to 60 mg, as prescribed by your doctor. The maximum recommended daily dose should not exceed 300 mg.
Is codeine and codeine the same thing?
Codeine and hydrocodone are prescribed for different types of pain. Codeine is typically used for mild to moderate pain, while hydrocodone is more potent and used for more severe pain.
Is Codeine a narcotic?
Codeine is a narcotic cough suppressant. It affects the signals in the brain that trigger cough reflex.
Is codeine a safe drug?
There is no safe level of drug use. Codeine affects everyone differently, based on: the person’s size, weight and health. whether the person is used to taking it. whether other drugs are taken around the same time.