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Codeine codeine (Clinical Considerations (Drug interactions (Abitaterone…
Codeine
Clinical Considerations
General dosages
Solution
30 mg/5 mL
Discontinued in US for more than 1 year
Tablet
15 mg
30 mg
#
60 mg
Contraindications
Hypersensitivity to codeine or any component in formulation
Pediatric patients less than 12 years of age
Postoperative management in pediatric patients <18 years of age who have undergone tonsillectomy and/or adenoidectomy
Significant respiratory depression
Acute or severe bronchial asthma in an unmonitored setting or in the ansence of resucitative equipment
GI obstruction
Concurrent use with MAOIs or use of MAOIs within the last 14 days
Toxicities
Acute toxic effects
Miosis
Constipation
urinary retention
nausea
Vomiting
Hypothermia
Drowsiness
Dizziness
Apathy
Confusion
Respiratory depression
Hypotension
Pulmonary edema
Coma
Death
Lethal dose
Adult
0.5 - 1.0 g
Drug interactions
Abitaterone acetate
Ajmaline
Alizapride
Alvimopan
Amphetamines
Anticholinergic agents
Asunaprevir
Azelastine
Bionaserin
Brimonidine
Bromopride
Bromperidol
Cannabidiol
Cannabis
Chlormethiazole
Chlorphenesis carbamate
CNS depressants
Cobicstat
Darunavir
Desmopressin
Diuretics
Dronabinol
Flunitrazepam
GI agents
Hydrocodone
Imatinib
Kava kava
Lofexidine
Lumefantrine
Magnesium sulfate
Methotrimeprazine
Minocycline
MAOIs
Naltrexone
Opiod analgesics
Opiods
Oxycodone
Para;dehyde
Perampenel
Rufinamide
SSRIs
Somatostatin analogs
Tetrahydrocannabinol
Zolpidem
Controlled substance
Schedule II
Indications
Labeled indications
Management of mild to moderately severe pain
#
Limitations
Reserve for patients for whom alternative options (eg, nonopioid analgesics, opioid combination products) are ineffective, not tolerated, or would otherwise be inadequate
Off-label indications
Cough
Persistent diarrhea
#
Restless legs syndrome
Dental Applications
Treatment
Postoperative pain
Adults take 30 mg every 4 to 6 hours as needed
Prior opioid exposure may require higher initial doses
Usual range: 15 to 120 mg every 4 to 6 hours as needed
No local anesthesia / vasoconstrictor precautions
Considerations
Do not use as sole entity for analgesia
Moderate efficacy
High incidence of:
Nausea
Sedation
Constipation
#
Opioid addiction liability
Combine with acetaminophen / aspirin
No significant effects on dental treatment
Pharmacokinetics
Onset of action
Oral
0.5-1 hour
Injection
30-60 minutes
Peak effect
Oral
1-1.5 hours
Injection
30-60 minutes
Duration
Oral
4-6 hours
Injection
4-6 hours
Protein binding
~7% to 25%
Pharmacodynamics
General effects
Weak narcotic pain reliever
#
Cough suppressant
#
Small amount converted to morphine
Antitussive activity
Effective in cough secondary to:
Tuberculosis
Insomnia due to coughing
Intestinal motility
Reduces intestinal motility
Constipation
Chronic use
Obstructive bowel disease
CNS
Respiratory system depression
Activation of mu-type opioid receptors
#
Targets
Kappa-type opioid receptor
General function
Opioid receptor activity
Specific function
G-protein coupled opioid receptor
Delta-type opioid receptor
General function
Specific function
G-protein coupled receptor
Endogenous enkephalin and subset of opioids receptor
Mu-type opioid receptor
General function
Voltage-gated calcium channel
Specific function
Endogenous opioid receptor
Blood pressure
Increased risk of compromised ability to maintain blood pressure
Peripheral vasodilation
Sources:
Bolser DC, “Cough Suppressant and Pharmacologic Protussive Therapy: ACCP Evidence-Based Clinical Practice Guidelines,” Chest, 2006, 129(1 Suppl):238-48.
Earley CJ. Latest guidelines and advances for treatment of restless legs syndrome. J Clin Psychiatry. 2014;75(4):e08. doi: 10.4088/JCP.12074nr3c
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
