chlorpheniramine polistirex/codeine polistrirex

General

Genetic Implications: Genetic Implications

Pronunciation:
klor-fen-ir-a-meen pol-is-ty-rex /koe-deen pol-is-ty-rex


Trade Name(s)

  • Tuzistra XR

Ther. Class.
allergy, cold and cough remedies
antitussives

Pharm. Class.
antihistamines
opioid agonists

Controlled Substance Schedule: III

Indications

For the relief of cough associated with upper respiratory allergies or common cold.

Action

  • Chlorpheniramine–Antagonizes the effects of histamine at H2-receptor sites; does not bind to or inactivate histamine.
  • Codeine–suppresses the cough reflex.

Therapeutic Effect(s):

Decreased cough due to allergy or common cold.

Pharmacokinetics

Codeine

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

Distribution: Widely distributed. Minimal amounts excreted in breast milk. Crosses the blood-brain barrier.

Metabolism and 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. Crosses the placenta; enters breast milk.

Protein Binding: 7%.

Metabolism and Excretion: Mostly metabolized by the liver (primarily via CYP2D6); 10% converted to morphine;Genetic implicationthe 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.

TIME/ACTION PROFILE (cough suppression)

ROUTEONSETPEAKDURATION
POunknownunknown12 hr

Contraindication/Precautions

Contraindicated in:

  • Hypersensitivity to chlorpheniramine, codeine or any other components of the formulation
  • Genetic implication Ultra-rapid metabolizers of codeine;
  • Pedi: Children <12 yr and children <18 yr following tonsillectomy and/or adenoidectomy (↑ risk of respiratory depression and death).

Use Cautiously in:

  • Head injury /↑ intracranial pressure (avoid use);
  • Severe renal, hepatic, or pulmonary disease;
  • Hypothyroidism;
  • Adrenal insufficiency;
  • Alcoholism/history of substance abuse;
  • Prostatic hyperplasia
  • Undiagnosed abdominal pain;
  • Angle-closure glaucoma
  • Geri: Geriatric or debilitated patients (appears on Beers list, dose ↓ recommended; ↑ risk of CNS depression, constipation);
  • OB: Has been used during labor; respiratory depression may occur in the newborn;
  • Lactation: Avoid use in breastfeeding (↑ risk of drowsiness and respiratory difficulty in infant);
  • Pedi: Children 12–18 yr who are postoperative; have obstructive sleep apnea, obesity, or severe pulmonary disease, neuromuscular disease; or are taking other medications that cause respiratory depression (↑ risk of respiratory depression).

Adverse Reactions/Side Effects

Chlorpheniramine

CNS: drowsiness, dizziness, excitation (in children)

EENT: blurred vision

CV: hypertension, arrhythmias, hypotension, palpitations

GI: dry mouth, constipation, obstruction

GU: urinary retention, urinary hesitancy

codeine

CNS: confusion, sedation, dysphoria, euphoria, floating feeling, hallucinations, headache, unusual dreams

EENT: blurred vision, diplopia, miosis

Resp: respiratory depression

CV: hypotension, bradycardia

GI: constipation, nausea, vomiting

GU: urinary retention

Derm: flushing, sweating

Misc: physical dependence, psychological dependence, tolerance

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

  • ↑ risk of CNS depression (including respiratory depression) may occur with anti-anxiety agents, other antihistamines, antipsychotics, other opioids, sedative hypnotics and should be undertaken with caution.
  • CYP3A4 inhibitors, inclulding erythromycin, clarithromycin, ketoconazole, itraconazole, protease inhibitors may ↑ levels and risk of respiratory depression.
  • CYP3A4 inducers may ↓ levels.
  • CYP2D6 inhibitors, including amiodarone and quinidine may ↓ analgesic effects.
  • Concurrent use with MAOIs or tricyclic antidepressants may result in ↑ the effect of codeine or the tricyclic antidepressant; monitor for excess effect.
  • ↑ risk of anticholinergic side effects (dry mouth, blurred vision, constipation) with other anticholinergics.
  • Phenytoin levels may be ↑ by chlorpheniramine.

Route/Dosage

PO: (Adults) 10 mL (29.4 mg codeine [equivalent to 40 mg codeine phosphate] and 5.6 mg chlorpheniramine [equivalent to 8 mg chlorpheniramine maleate]) every 12 hr; not to exceed 2 doses/24 hr.

Availability

Extended-release oral suspension (cherry): 14.7 mg codeine (equivalent to 20 mg codeine phosphate) and 2.8 mg chlorpheniramine (equivalent to 4 mg chlorpheniramine maleate) per 5 mL

Assessment

  • Assess cough periodically during therapy.

Potential Diagnoses

Implementation

  • PO: May be administered without regard to food. Shake well. Use accurate mL measuring device; do not use household teaspoon to measure dose. Oral solution is pink to reddish pink, and cherry-flavored. Do not dilute with fluids or mix with other drugs.

Patient/Family Teaching

  • Instruct patient to take medication as directed. Emphasize importance of using an accurate measuring device and not using household teaspoon.
  • 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 while taking this medication.
  • May cause drowsiness and dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known
  • Advise female patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding

Evaluation/Desired Outcomes

Relief of cough.

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