section name header

Indications ⬇

BEERS REMS

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: physical dependence, psychological dependence, tolerance

Interactions ⬆ ⬇

Drug-drug:

Availability ⬆ ⬇

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

Route/Dosage ⬆ ⬇

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

US Brand Names ⬆ ⬇

Tuxarin ER

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.

Classifications ⬆ ⬇

Therapeutic Classification: allergy, cold and cough remedies, antitussives

Pharmacologic Classification: antihistamines, opioid agonists

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 enzyme system 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.

Contr. Subst. Schedule ⬆ ⬇

Schedule III (C-III)

Time/Action Profile ⬆ ⬇

(cough suppression)

ROUTEONSETPEAKDURATION
POunknownunknown12 hr

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.

Pronunciation ⬆

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