Description

Simple

A strong painkiller that treats moderate to severe pain when appropriate.

Clinical

An opioid analgesic used to treat moderate to severe pain when the use of an opioid is indicated.

Overview

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).[4]

Codeine is utilized as a central analgesic, sedative, hypnotic, antinociceptive, and antiperistaltic agent, and is also recommended in certain diseases with incessant coughing.[LABEL,4]

Pharmacology

Indication

Codeine sulfate is a form of this drug that is commonly used. It is available in tablet form [FDA label] and indicated for the relief of mild to moderately severe pain, where the use of an opioid analgesic is appropriate [FDA label].

The solution form is used by itself or combined in a syrup with... Read more

Pharmacodynamic

**General effects**

Codeine is a weak narcotic pain reliever and cough suppressant that is similar to morphine and hydrocodone. A small amount of ingested codeine is converted to morphine in the body. Codeine increases tolerance to pain, reducing existing discomfort. In addition to decreasing pai... Read more

Mechanism of action

Codeine is a selective agonist for the mu opioid receptor, but with a much weaker affinity to this receptor than morphine, a more potent opioid drug. Codeine binds to mu-opioid receptors, which are involved in the transmission of pain throughout the body and central nervous system [FDA label], [ Read more

Absorption

**Absorption**

Codeine is absorbed from the gastrointestinal tract. The maximum plasma concentration occurs 60 minutes after administration [FDA label].

**Food Effects**

When 60 mg codeine sulfate was given 30 minutes post-ingestion of a high high-calorie meal, there was no significant cha... Read more

Protein binding

7-25% bound to plasma proteins [FDA label].

Volume of distribution

Apparent volume of distribution: about 3-6 L/kg, showing an extensive distribution of the drug into tissues [FDA label].

Clearance

Renal clearance of codeine was 183 +/- 59 ml min-1 in a clinical study [ Read more

Half life

Plasma half-lives of codeine and its metabolites have been reported to be approximately 3 hours [FDA label].

Route of elimination

About 90% of the total dose of codeine is excreted by the kidneys. Approximately 10% of the drug excreted by the kidneys is unchanged codeine [FDA label].

The majority of the excretion products can be found in the urine within 6 hours of ingestion, and 40-60 % of the codeine is excreted free or... Read more

Toxicity

**Oral LD50**: 427 mg kg-1 (rat) [MSDS].

**Overdose/toxicity**

Symptoms of opioid toxicity may include confusion, somnolence, shallow breathing, constricted pupils, nausea, vomiting, constipation and a lack of appetite. In severe cases, symptoms of circulatory and respiratory depression may e... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Above Age:
    • Amount: 12
    • Unit: year
  • Below Age:
    • Amount: 18
    • Unit: year
  • Patient Conditions:
      • Name: Obese or have conditions such as obstructive sleep apnea or severe lung disease, which may increase the risk of serious breathing problems
      • Drugbank Id: DBCOND0117809
  • Regions: US
  • Patient Conditions:
      • Name: To treat cough in patients younger than 18 years old
      • Drugbank Id: DBCOND0117808
  • Regions: US
  • Patient Conditions:
      • Name: Post Operative Pain Management in Children With Tonsillectomy/Adenoidectomy
      • Drugbank Id: DBCOND0059908
  • Regions: US
  • Patient Conditions:
      • Name: Pain
      • Drugbank Id: DBCOND0012160
  • Patient Conditions Associated With:
      • Name: Patients under 12 years old
      • Drugbank Id: DBCOND0116942
  • Regions: US
  • Patient Conditions:
      • Name: Paralytic Ileus
      • Drugbank Id: DBCOND0047064
  • Regions: US
  • Patient Conditions:
      • Name: Hypersensitivity to codeine or any component of the product
      • Drugbank Id: DBCOND0117801
  • Regions: US
  • Patient Conditions:
      • Name: Hypercarbia
      • Drugbank Id: DBCOND0063116
  • Regions: US
  • Patient Conditions:
      • Name: Acute or severe bronchial asthma
      • Drugbank Id: DBCOND0107797
  • Regions: US
  • Patient Conditions:
      • Name: Respiratory depression in the absence of resuscitative equipment
      • Drugbank Id: DBCOND0117800

Food Interactions

  • Avoid alcohol.
  • Take with food. Food reduces irritation.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Codeine can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may increase the analgesic activities of Codeine.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may increase the analgesic activities of Codeine.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may increase the analgesic activities of Codeine.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Codeine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Codeine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Codeine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Codeine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Abacavir
Abacavir may decrease the excretion rate of Codeine which could result in a higher serum level.
Abatacept
The metabolism of Codeine can be increased when combined with Abatacept.
Abiraterone
The metabolism of Codeine can be decreased when combined with Abiraterone.
Acarbose
Acarbose may decrease the excretion rate of Codeine which could result in a higher serum level.
Acebutolol
The metabolism of Codeine can be decreased when combined with Acebutolol.
Aceclofenac
Aceclofenac may decrease the excretion rate of Codeine which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Codeine which could result in a higher serum level.
Acepromazine
The risk or severity of hypotension and CNS depression can be increased when Acepromazine is combined with Codeine.
Aceprometazine
The risk or severity of hypotension and CNS depression can be increased when Aceprometazine is combined with Codeine.
Acetazolamide
The risk or severity of adverse effects can be increased when Codeine is combined with Acetazolamide.
Acetophenazine
The risk or severity of hypotension and CNS depression can be increased when Acetophenazine is combined with Codeine.
Acetylcholine
The risk or severity of adverse effects can be increased when Codeine is combined with Acetylcholine.
14 References
  1. 1 . Schroeder K, Fahey T: Over-the-counter medications for acute cough in children and adults in ambulatory settings. Cochrane Database Syst Rev. 2004 Oct 18;(4):CD001831.PubMed: 15495019
  2. 2 . Vree TB, van Dongen RT, Koopman-Kimenai PM: Codeine analgesia is due to codeine-6-glucuronide, not morphine. Int J Clin Pract. 2000 Jul-Aug;54(6):395-8.PubMed: 11092114
  3. 3 . Srinivasan V, Wielbo D, Tebbett IR: Analgesic effects of codeine-6-glucuronide after intravenous administration. Eur J Pain. 1997;1(3):185-90.PubMed: 15102399
  4. 4 . Bhandari M, Bhandari A, Bhandari A: Recent updates on codeine. Pharm Methods. 2011 Jan;2(1):3-8. doi: 10.4103/2229-4708.81082.PubMed: 23781422
  5. 5 . Chen ZR, Somogyi AA, Reynolds G, Bochner F: Disposition and metabolism of codeine after single and chronic doses in one poor and seven extensive metabolisers. Br J Clin Pharmacol. 1991 Apr;31(4):381-90.PubMed: 2049245
  6. 6 . Takahama K, Wakuda I, Fukushima H, Isohama Y, Kai H, Miyata T: Differential effect of codeine on coughs caused by mechanical stimulation of two different sites in the airway of guinea pigs. Eur J Pharmacol. 1997 Jun 18;329(1):93-7.PubMed: 9218689
  7. 7 . Straube C, Derry S, Jackson KC, Wiffen PJ, Bell RF, Strassels S, Straube S: Codeine, alone and with paracetamol (acetaminophen), for cancer pain. Cochrane Database Syst Rev. 2014 Sep 19;(9):CD006601. doi: 10.1002/14651858.CD006601.pub4.PubMed: 25234029
  8. 8 . Boom M, Niesters M, Sarton E, Aarts L, Smith TW, Dahan A: Non-analgesic effects of opioids: opioid-induced respiratory depression. Curr Pharm Des. 2012;18(37):5994-6004. doi: 10.2174/138161212803582469.PubMed: 22747535
  9. 9 . Prommer E: Role of codeine in palliative care. J Opioid Manag. 2011 Sep-Oct;7(5):401-6.PubMed: 22165039
  10. 10 . Codeine phosphate tablets, 30mg Link
  11. 11 . DailyMed: Codeine and promethazine syrup Link
  12. 12 . Codittusin, DailyMed Link
  13. 13 . EPAR, Codeine File
  14. 14 . Codeine, MedSafe NZ document File