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acetaminophen/dextromethorphan/pseudoephedrine/guaifenesin (Tylenol Cold Severe Congestion)

 

Classes: Cough/Cold, Non-narcotic Combos; Analgesic/Antitussive/Decongestant/Expectorant Combos

Dosing and uses of Tylenol Cold Severe Congestion (acetaminophen/dextromethorphan/pseudoephedrine/guaifenesin)

 

Adult dosage forms and strengths

acetaminophen/dextromethorphan/pseudoephedrine/guaifenesin

tablet

  • 325mg/15mg/30mg/200mg

 

Symptomatic Relief of Cough & Congestion

2 tablets PO q6hr; not to exceed 8 tablets/day

 

Pediatric dosage forms and strengths

acetaminophen/dextromethorphan/pseudoephedrine/guaifenesin

tablet

  • 325mg/15mg/30mg/200mg

 

Symptomatic Relief of Cough & Congestion

<12 Years Old

  • Not recommended

>12 Years Old

  • 2 tablets PO q6hr; not to exceed 8 tablets/day

 

Tylenol Cold Severe Congestion (acetaminophen/dextromethorphan/pseudoephedrine/guaifenesin) adverse (side) effects

Frequency not defined

Arrhythmia

Palpitations

Convulsion

Dizziness

Drowsiness

Excitability

Headache

Tremor

Weakness

Dermatologic rash

GI disturbances

Nausea

Vomiting

Anemia blood dyscrasias (neutropenia, pancytopenia, leukopenia)

Bilirubin and alkaline phosphatase may increase

 

Warnings

Contraindications

Documented hypersensitivity to the drugs or within 14 days of MAO inhibitor therapy; known G-6-PD deficiency

 

Cautions

Caution in cardiovascular disease, diabetes mellitus, prostatic hypertrophy and increased intraocular pressure when taking pseudoephedrine

Acetaminophen hepatotoxicity possible in chronic alcoholics following various dose levels; severe or recurrent pain or high or continued fever may indicate a serious illness; contained in many OTC products and combined use with these products may result in toxicity due to cumulative doses exceeding recommended maximum dose

Do not take dextromethorphan for persistent or chronic cough associated with smoking, asthma, or emphysema, or if it is accompanied by excessive phlegm unless directed by a healthcare provider; dextromethorphan may slow the breathing

Guaifenesin is not for administration in persistent cough associated with chronic bronchitis, smoking, asthma, or accompanied with excessive secretions

Acetaminophen: Risk for rare, but serious skin reactions that can be fatal; these reactions include Stevens-Johnson Syndrome (SJS), toxic epidermal necrolysis (TEN), and acute generalized exanthematous pustulosis (AGEP); symptoms may include skin redness, blisters and rash

 

Pregnancy and lactation

Pregnant or breastfeeding patients should seek advice of health professional before using OTC drugs

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Tylenol Cold Severe Congestion (acetaminophen/dextromethorphan/pseudoephedrine/guaifenesin)

Mechanism of action

Acetaminophen blocks pain impulse generation peripherally and may inhibit the generation of prostaglandin in the CNS. Reduces fever by inhibiting the hypothalamic heat-regulating center.

Dextromethorphan is a cough suppressant that acts centrally on the cough center in the medulla.

Pseudoephedrine stimulates the alpha-adrenergic receptors causing bronchodilation and vasoconstriction.

Guaifenesin increases respiratory tract fluid secretions and helps to loosen phlegm and bronchial secretions.

 

Pharmacokinetics

Acetaminophen

  • Peak plasma time: 10-60 min (PO immediate release); 60-120 min (PO extended release); 6 hr (PO 500 mg tablet); 8 hr (PO 650 mg extended release tablet)
  • Vd: 1 L/kg
  • Protein binding: 10-25%
  • Metabolism: Liver (microsomal enzyme systems); conjugation (glucuronic acid)
  • Half-life: 1.25-3hr
  • Excretion: Urine

Dextromethorphan

  • Onset: 15-30 min
  • Duration: 3-6 hr
  • Metabolism: Hepatic P450 enzyme CYP2D6
  • Excretion: Urine
  • Half-life: 2-4 hr (extensive metabolizers); 24 hr (poor metabolizers)
  • Peak plasma time: 2-3 hr

Pseudoephedrine

  • Half-Life: 3 hr (children); 9-16 hr (adults)
  • Onset: 30 min (decongestant)
  • Duration: 3-8 hr  
  • Peak PlasmaTime: 1.97 hr
  • Concentration: 422 ng/mL
  • Metabolism: Liver, by N-demethylation
  • Metabolites: Inactive
  • Clearance: 7.3-7.6 mL/min/kg
  • Excretion: Urine (43-96%)

Guaifenesin

  • Half-Life: 1 hr
  • Onset: 30 min
  • Duration: 4-6 hr
  • Metabolism: Liver
  • Metabolite: b-(2-methoxyphenoxy) lactic acid
  • Excretion: Urine