section name header

Pronunciation ⬇

klor-fen-IR-a-meen pol-is-TY-rex /KOE-deen pol-is-TY-rex

Classifications ⬆ ⬇

Therapeutic Classification: allergy, cold and cough remedies, antitussives

Pharmacologic Classification: antihistamines, opioid agonists

Indications ⬆ ⬇

BEERS REMS

Action ⬆ ⬇

  • Chlorpheniramine: Antagonizes the effects of histamine at H2-receptor sites; does not bind to or inactivate histamine.
  • Codeine: suppresses the cough reflex.
Therapeutic effects:
  • Decreased cough due to allergy or common cold.

Pharmacokinetics ⬆ ⬇

Chlorpheniramine

Absorption: Well absorbed following oral administration; polistirex delays absorption, prolonging action.

Distribution: Widely distributed. Crosses the blood-brain barrier.

Metabolism/Excretion: Extensively metabolized by the liver.

Half-Life: 12–15 hr.

Codeine

Absorption: 50% absorbed from the GI tract; polistirex delays absorption, prolonging action.

Distribution: Widely distributed.

Protein Binding: 7%.

Metabolism/Excretion: Mostly metabolized by the liver (primarily via the CYP2D6 isoenzyme); 10% converted to morphine;the CYP2D6 isoenzyme exhibits genetic polymorphism (some patients [1–10% Whites, 3% African Americans, 16–28% North Africans/Ethiopians/Arabs] may be ultra-rapid metabolizers and may have ↑ morphine concentrations and an ↑ risk of adverse effects); 5–15% excreted unchanged in urine.

Half-Life: 2.5–4 hr.

Time/Action Profile ⬆ ⬇

(cough suppression)

ROUTEONSETPEAKDURATION
POunknownunknown12 hr



Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

Chlorpheniramine

CV: hypertension, arrhythmias, hypotension, palpitations

EENT: blurred vision

GI: dry mouth, GI obstruction, constipation

GU: urinary hesitancy, urinary retention

Neuro: confusion, drowsiness, sedation, dizziness, dysphoria, euphoria, excitation (in children), floating feeling, hallucinations, headache, unusual dreams

Codeine

CV: hypotension, bradycardia

Derm: flushing, sweating

EENT: blurred vision, diplopia, miosis

GI: constipation, nausea, vomiting

GU: urinary retention

Resp: RESPIRATORY DEPRESSION

Misc: allodynia, opioid-induced hyperalgesia, physical dependence, psychological dependence, tolerance

Interactions ⬆ ⬇

Drug-drug:

Route/Dosage ⬆ ⬇

  • PO (Adults ): 1 tablet every 12 hr as needed; not to exceed 2 tablets/24 hr.

Availability ⬆ ⬇

  • Extended-release tablets: codeine phosphate 54.3 mg/chlorpheniramine maleate 8 mg

Assessment ⬆ ⬇

  • Assess cough periodically during therapy.
  • Assess risk for opioid addiction, abuse, or misuse prior to administration.
  • Assess BP, pulse, and respirations before and periodically during administration. If respiratory rate is <10/min, assess level of sedation. Physical stimulation may be sufficient to prevent significant hypoventilation. Monitor for respiratory depression, especially during initiation or following dose increase; serious, life-threatening, or fatal respiratory depression may occur. May cause sleep-related breathing disorders (central sleep apnea, sleep-related hypoxemia).
    • Assess bowel function routinely. Prevention of constipation should be instituted with increased intake of fluids and bulk, and laxatives to minimize constipating effects. Stimulant laxatives should be administered routinely if opioid use exceeds 2–3 days, unless contraindicated.
    Assess risk for opioid addiction, abuse, or misuse prior to administration. Abuse or misuse of extended-release preparations by crushing, chewing, snorting, or injecting dissolved product will result in uncontrolled delivery of codeine and can result in overdose and death.

Toxicity and Overdose:

  • If an opioid antagonist is required to reverse respiratory depression or coma, naloxone is the antidote. Dilute the 0.4-mg ampule of naloxone in 10 mL of 0.9% NaCl and administer 0.5 mL (0.02 mg) by IV push every 2 min. For children and patients weighing <40 kg, dilute 0.1 mg of naloxone in 10 mL of 0.9% NaCl for a concentration of 10 mcg/mL and administer 0.5 mcg/kg every 2 min. Titrate dose to avoid withdrawal, seizures, and severe pain.

Implementation ⬆ ⬇

  • High Alert: Accidental overdose of opioid analgesics has resulted in fatalities. Before administering, clarify all ambiguous orders.
  • Discuss availability of naloxone for emergency treatment of opioid overdose with the patient and caregiver and assess the potential need for access to naloxone, both when initiating and renewing therapy, especially if patient has household members (including children) or other close contacts at risk for accidental exposure or overdose. Consider prescribing naloxone, based on the patient’s risk factors for overdose, such as concomitant use of CNS depressants, a history of opioid use disorder, or prior opioid overdose. However, the presence of risk factors for overdose should not prevent the proper management of pain in any patient.
  • PO: Administer 1 tablet twice daily; do not exceed 2 tablets in 24 hr. May be administered without regard to food.

Patient/Family Teaching ⬆ ⬇

  • Instruct patient to take medication as directed and not to take more than prescribed.
  • May cause drowsiness and dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known
  • Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose. Inform patients and caregivers about various ways to obtain naloxone as permitted by individual state naloxone dispensing and prescribing requirements or guidelines (by prescription, directly from a pharmacist, or as part of a community-based program).
  • Advise patient that codeine is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed. Store out of sight and reach of children and in a location not accessible by others.
  • Assess risk for opioid addiction, abuse, or misuse prior to administration. Abuse or misuse of extended-release preparations by crushing, chewing, snorting, or injecting dissolved product will result in uncontrolled delivery of codeine and can result in overdose and death.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications. Instruct patient to avoid alcohol and other CNS depressants, including opioids, while taking this medication.
  • Rep: May cause fetal harm. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. Advise patient to avoid use during pregnancy; may cause neonatal opioid withdrawal syndrome (irritability, hyperactivity and abnormal sleep pattern, high-pitched cry, tremor, vomiting, diarrhea, and failure to gain weight) shortly after birth. Monitor neonates exposed to opioids during labor or breastfeeding for signs of excess sedation and respiratory depression. Chronic use may impair fertility in females and males.

Evaluation/Desired Outcomes ⬆ ⬇

  • Relief of cough. Evaluate need for medication within 5 days of use.

US Brand Names ⬆ ⬇

Tuxarin ER

Contr. Subst. Schedule ⬆

Schedule III (C-III)