Codeine

Trade Names:
Codeine
- Tablets 15 mg (as sulfate)
- Tablets 30 mg (as sulfate)
- Tablets 60 mg (as sulfate)
- Soluble Tablets for Injection 30 mg (as phosphate)
- Soluble Tablets for Injection 60 mg (as phosphate)
- Injection 15 mg/mL (as phosphate)
- Injection 30 mg/mL (as phosphate)

Pharmacology

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Stimulates opiate receptors in the CNS; also causes respiratory depression, peripheral vasodilation, inhibition of intestinal peristalsis, stimulation of the chemoreceptors that cause vomiting, increased bladder tone, and suppression of cough reflex.

Pharmacokinetics

Metabolism

Metabolized in the liver by undergoing O-demethylation, N-demethylation, and partial conjugation.

Elimination

Excreted in the urine, largely as inactive metabolites, and small amounts of free and conjugated morphine. The t _½ is 3 h.

Onset

15 to 30 min.

Peak

60 min.

Duration

4 to 6 h.

Indications and Usage

Relief of mild to moderate pain.

Contraindications

Hypersensitivity to opiates; upper airway obstruction; respiratory compromise; acute asthma; diarrhea caused by poisoning or toxins.

Dosage and Administration

IM / Slow IV / PO / Subcutaneous 15 to 60 mg every 4 to 6 h.

IM / PO / Subcutaneous 0.5 mg/kg every 4 to 6 h.

General Advice

• Incompatible with soluble barbiturates.
• Do not administer parenteral form if it is discolored or contains particulate matter.

Storage/Stability

Store below 104°F. Protect from light. Do not freeze.

Store at 59° to 86°F. Protect from moisture.

Store at 68° to 77°F.

Drug Interactions

Cause additive CNS depression.

May decrease the analgesic effect of codeine by interference with metabolism of codeine to morphine.

Laboratory Test Interactions

Amylase and lipase determination: Increased levels for up to 24 h after administration.

Adverse Reactions

Cardiovascular

Bradycardia, cardiac arrest, circulatory depression, fainting, orthostatic hypotension, palpitation, shock, syncope, tachycardia.

CNS

Agitation, anxiety, convulsions, disorientation, dizziness, drowsiness, dysphoria, euphoria, fear, headache, impaired mental and physical performance, insomnia, lethargy, lightheadedness, mental clouding, mood changes, psychic dependence, reduced libido, sedation, weakness.

Dermatologic

Flushing, hemorrhagic urticaria, pruritus, rash, sweating, urticaria.

EENT

Miosis, visual disturbances.

GI

Anorexia, constipation, dry mouth, increased biliary tract pressure and spasm, nausea, vomiting.

Genitourinary

Antidiuretic effect, reduced libido or potency, spasm of vesicle sphincter, ureteral spasm, urinary retention or hesitancy.

Respiratory

Respiratory depression, suppressed cough reflex.

Miscellaneous

Allergic reactions, edema.

Precautions

Pregnancy

Category C . Therapeutic doses of codeine have increased duration of labor.

Lactation

Excreted in breast milk.

Children

Do not give IV to children younger than 12 yr of age. Children are more sensitive to effects of drug. Safety and efficacy not established in newborns.

Safety and efficacy not established in children younger than 3 yr of age.

Elderly

More sensitive to effects of drug.

Renal Function

Duration of action may be prolonged; may need to reduce dose.

Hepatic Function

Duration of action may be prolonged; may need to reduce dose.

Special Risk Patients

Use with caution in patients with acute abdominal conditions, acute alcoholism, circulatory shock, decreased respiratory reserve, depleted blood volume, head injury or increased intracranial pressure, history of drug abuse potential, hypothyroidism, hypoxia, myxedema, supraventricular tachycardia, ulcerative colitis, and urinary/bowel elimination problems. Use with caution in elderly or debilitated patients and in patients with impaired renal or hepatic function, hypothyroidism, Addison disease, prostatic hypertrophy, or urethral stricture.

Acute abdominal conditions

Diagnosis or clinical course of acute abdominal conditions may be obscured.

Asthma or pulmonary emphysema

In asthma and pulmonary emphysema, the indiscriminate use of codeine may, because of its drying action upon the mucosa of the respiratory tract, precipitate severe respiratory insufficiency resulting from increased viscosity of the bronchial secretions and suppression of the cough reflex.

Drug dependency

Codeine has abuse potential.

Head injury

The presence of head injury, other intracranial lesions, or a preexisting increase in intracranial pressure may be exaggerated because of the respiratory depressant effects and the capacity of codeine to elevate cerebrospinal pressure.

Respiratory depression

Dose-related respiratory depression occurs.

Overdosage

Symptoms

Apnea, bradycardia, cardiac arrest, circulatory collapse, cold and clammy skin, death, extreme somnolence progressing to stupor or coma, hypotension, miosis, respiratory depression, skeletal muscle flaccidity.

Patient Information

• Instruct patient on self-assessment of pain and on how and when to administer medication.
• Advise patient to increase fluid intake to relieve constipation and to take stool softener or mild laxative as needed.
• Advise patient to take medication with food if GI upset occurs and to monitor for GI irritation.
• Explain that codeine may be habit forming.
• Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
• Instruct patient to avoid intake of alcoholic beverages or other CNS depressants.
• Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.

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