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

Effect Regions Age Groups Incidences Evidence Type
Dry Eyes US
Literature
Urticaria US
Varying Reports
Weakness US
Varying Reports
Visual Disturbance US
Varying Reports
Vertigo US
Varying Reports
Somnolence US
Varying Reports
Shakiness US
Varying Reports
Nervousness US
Varying Reports
Insomnia US
Varying Reports
Headache US
Varying Reports
Fatigue US
Varying Reports
Anxiety US
Varying Reports
Pancreatitis US
Varying Reports
Gastrointestinal distress US
Varying Reports
Dry Mouth US
Varying Reports
Anorexia US
Varying Reports
Diarhhea US
Varying Reports
Abdominal Cramps US
Varying Reports
Flushing US
Varying Reports
Palpitations US
Varying Reports
Syncope US
Varying Reports
Hypotension US
Varying Reports
Feeling of faintness US
Varying Reports
Dysphoria US
Varying Reports
Euphoria US
Varying Reports
Circulatory depression US
Varying Reports
Shock US
Varying Reports
Cardiac Arrest US
Varying Reports
Respiratory Arrest US
Sweating US
Varying Reports
Respiratory Depression US
Varying Reports
Rash US
Varying Reports
Pruritus US
Varying Reports
Agranulocytosis US
Varying Reports
Thrombocytopenia US
Varying Reports
Dysphoria US
Varying Reports
Euphoria US
Varying Reports
Abdominal Pain US
Varying Reports
Constipation US
Varying Reports
Nausea US
Varying Reports
Shortness of Breath US
Varying Reports
Allergic Reactions US
Varying Reports
Vomiting US
Varying Reports
Lightheadedness US
Varying Reports
Drowsiness US
Varying Reports
Sedation US
Varying Reports
Dizziness US
Varying Reports

Contraindications

  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: Turkey
  • Patient Conditions:
      • Name: Ultrarapid Metabolizer Due to Cytochrome P450 CYP2D6 Variant
      • Drugbank Id: DBCOND0061597
  • Route:
    • Oral
  • Hypersensitivity:
    • true
  • Regions: US
  • 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: 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.