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Pronunciation |
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(KOE
deen) |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Codeine Contin®; Linctus Codeine Blac;
Linctus With Codeine Phosphate; Paveral Stanley Syrup With Codeine
Phosphate |
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Synonyms |
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Codeine Phosphate; Codeine Sulfate; Methylmorphine |
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Pharmacological Index |
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Analgesic, Narcotic; Antitussive |
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Use |
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Dental: Treatment of postoperative pain
Medical: Treatment of mild to moderate pain; antitussive in lower doses;
dextromethorphan has equivalent antitussive activity but has much lower toxicity
in accidental overdose |
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Restrictions |
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C-II |
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Pregnancy Risk
Factor |
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C/D (if used for prolonged periods or in high doses at
term) |
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Contraindications |
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Hypersensitivity to codeine or any component |
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Warnings/Precautions |
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Use with caution in patients with hypersensitivity reactions to other
phenanthrene derivative opioid agonists (morphine, hydrocodone, hydromorphone,
levorphanol, oxycodone, oxymorphone); respiratory diseases including asthma,
emphysema, COPD, or severe liver or renal insufficiency; some preparations
contain sulfites which may cause allergic reactions; tolerance or drug
dependence may result from extended use |
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Adverse
Reactions |
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Percentage unknown: Increased AST, ALT
>10%:
Central nervous system: Drowsiness
Gastrointestinal: Constipation
1% to 10%:
Cardiovascular: Tachycardia or bradycardia, hypotension
Central nervous system: Dizziness, lightheadedness, false feeling of well
being, malaise, headache, restlessness, paradoxical CNS stimulation, confusion
Dermatologic: Rash, urticaria
Gastrointestinal: Xerostomia, anorexia, nausea, vomiting,
Genitourinary: Decreased urination, ureteral spasm
Hepatic: Increased LFTs
Local: Burning at injection site
Ocular: Blurred vision
Neuromuscular & skeletal: Weakness
Respiratory: Shortness of breath, dyspnea
Miscellaneous: Histamine release
<1%: Convulsions, hallucinations, mental depression, nightmares, insomnia,
paralytic ileus, biliary spasm, stomach cramps, muscle rigidity, trembling
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Overdosage/Toxicology |
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Symptoms of overdose include CNS and respiratory depression, gastrointestinal
cramping, constipation
Naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as
necessary up to a total of 10 mg |
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Drug
Interactions |
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CYP2D6 and 3A3/4 enzyme substrate; CYP2D6 enzyme inhibitor
Increased toxicity: CNS depressants, phenothiazines, TCAs, other narcotic
analgesics, guanabenz, MAO inhibitors, neuromuscular blockers
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Stability |
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Store injection between 15°C to
30°C, avoid freezing; do not use if injection is
discolored or contains a precipitate; protect injection from
light |
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Mechanism of
Action |
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Binds to opiate receptors in the CNS, causing inhibition of ascending pain
pathways, altering the perception of and response to pain; causes cough
supression by direct central action in the medulla; produces generalized CNS
depression |
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Pharmacodynamics/Kinetics |
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Onset of action: Oral: 0.5-1 hour; I.M.: 10-30 minutes
Peak action: Oral: 1-1.5 hours; I.M.: 0.5-1 hour
Duration of action: 4-6 hours
Absorption: Oral: Adequate
Distribution: Crosses the placenta; appears in breast milk
Protein binding: 7%
Metabolism: Hepatic to morphine (active)
Half-life: 2.5-3.5 hours
Elimination: 3% to 16% excreted in urine as unchanged drug, norcodeine, and
free and conjugated morphine |
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Usual Dosage |
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Doses should be titrated to appropriate analgesic effect; when changing
routes of administration, note that oral dose is
2/3
as effective as parenteral dose
Children: Oral, I.M., S.C.: 0.5-1 mg/kg/dose every 4-6 hours as needed;
maximum: 60 mg/dose
Adults: Oral, I.M., I.V., S.C.: 30 mg/dose; range: 15-60 mg every 4-6 hours
as needed
Antitussive: Oral (for nonproductive cough):
Children: 1-1.5 mg/kg/day in divided doses every 4-6 hours as needed:
Alternative dose according to age:
2-6 years: 2.5-5 mg every 4-6 hours as needed; maximum: 30 mg/day
6-12 years: 5-10 mg every 4-6 hours as needed; maximum: 60 mg/day
Adults: 10-20 mg/dose every 4-6 hours as needed; maximum: 120 mg/day
Dosing adjustment in renal impairment:
Clcr 10-50 mL/minute: Administer 75% of dose
Clcr <10 mL/minute: Administer 50% of dose
Dosing adjustment in hepatic impairment: Probably necessary in
hepatic insufficiency |
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Dietary
Considerations |
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Alcohol: Additive CNS effects, avoid or limit alcohol; watch for sedation
Food: Glucose may cause hyperglycemia; monitor blood glucose concentrations
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Administration |
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Not intended for I.V. use due to large histamine release and cardiovascular
effects |
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Monitoring
Parameters |
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Pain relief, respiratory and mental status, blood pressure, heart
rate |
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Reference Range |
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Therapeutic: Not established; Toxic: >1.1
mg/mL |
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Mental Health: Effects
on Mental Status |
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Drowsiness is common; may cause euphoria, confusion, insomnia,
hallucinations, or depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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Concurrent use with psychotropics may produce additive toxicity; concurrent
use with fluoxetine or paroxetine may result in loss of pain
control |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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<1% of patients experience dry mouth |
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Patient
Information |
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If self-administered, use exactly as directed (do not increase dose or
frequency); may cause physical and/or psychological dependence. While using this
medication, do not use alcohol and other prescription or OTC medications
(especially sedatives, tranquilizers, antihistamines, or pain medications)
without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids
unless instructed to restrict fluid intake). May cause dizziness, drowsiness,
confusion, agitation, impaired coordination, or blurred vision (use caution when
driving, climbing stairs, or changing position - rising from sitting or lying to
standing, or when engaging in tasks requiring alertness until response to drug
is known); nausea or vomiting, or loss of appetite (frequent mouth care, small
frequent meals, sucking lozenges, or chewing gum may help); constipation
(increased exercise, fluids, or dietary fruit and fiber may help - if
constipation remains an unresolved problem, consult prescriber about use of
stool softeners). Report confusion, insomnia, excessive nervousness, excessive
sedation or drowsiness, or shakiness; acute GI upset; difficulty breathing or
shortness of breath; facial flushing, rapid heartbeat or palpitations; urinary
difficulty; unusual muscle weakness; or vision changes.
Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend
to be pregnant. If you are breast-feeding, take medication immediately after
breast-feeding or 3-4 hours prior to next feeding. |
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Nursing
Implications |
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Observe patient for excessive sedation, respiratory depression, implement
safety measures, assist with ambulation |
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Dosage Forms |
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Injection, as phosphate: 30 mg (1 mL, 2 mL); 60 mg (1 mL, 2 mL)
Solution, oral: 15 mg/5 mL
Tablet, as sulfate: 15 mg, 30 mg, 60 mg
Tablet, as phosphate, soluble: 30 mg, 60 mg
Tablet, as sulfate, soluble: 15 mg, 30 mg, 60 mg |
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References |
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Cardan E, "Fatal Case of Codeine Poisoning," Lancet, 1981,
1(8233):1313.
de Groot AC and Conemans J, "Allergic Urticarial Rash From Oral Codeine,"
Contact Dermatitis, 1986, 14(4):209-14.
Desjardins PJ, Cooper SA, Gallegos TL, et al,
"The Relative Analgesic Efficacy of Propiram Fumarate, Codeine, Aspirin, and Placebo in Postimpaction Dental Pain,"
J Clin Pharmacol, 1984, 24(1):35-42.
"Drugs for Pain," Med Lett Drugs Ther, 1998, 40(1033):79-84.
Ferrell BA, "Pain Management in Elderly People," J Am Geriatr Soc,
1991, 39(1):64-73.
Forbes JA, Keller CK, Smith JW, et al,
"Analgesic Effect of Naproxen Sodium, Codeine, a Naproxen-Codeine Combination and Aspirin on the Postoperative Pain of Oral Surgery,"
Pharmacotherapy, 1986, 6(5):211-8.
Ivey HH and Kattwinkel J, "Danger of Actifed-C," Pediatrics, 1976,
57(1):164-5.
Kaiko RF, Wallenstein SL, Rogers AG, et al, "Narcotics in the Elderly,"
Med Clin North Am, 1982, 66(5):1079-89.
Wilkins D, Rollins DE, Seaman J, et al,
"Quantitative Determination of Codeine and Its Major Metabolites in Human Hair by Gas Chromatography - Positive Ion Chemical Ionization Mass Spectrometry: A Clinical Application,"
J Anal Toxicol, 1995, 19(5):269-74.
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