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Dexchlorpheniramine Maleate


Dexchlorpheniramine Maleate

is an

antihistamine

. It blocks the effects of the naturally occurring chemical histamine in your body.

Dexchlorpheniramine Maleate

is used to treat sneezing; runny nose; itching, watery eyes; hives; rashes; itching; and other symptoms of allergies and the

Common cold

.
Dosing
Adult dosing of

Dexchlorpheniramine Maleate

:

Important Note:
  • Beers Criteria:

    Use

    caution or
    avoid

    use

    as potentially inappropriate in older adults

  • Allergic

    conjunctivitis:

    Syrup:
  • 2 mg
    ORALLY
    every 4 to 6 hours

  • Extended-release tablets
    :
  • 4 to
    6 mg
    ORALLY
    at
    bedtime
    or every 8 to 10 hours during the day

  • Allergic

    rhinitis

    , Anaphylaxis; Adjunct, Blood transfusion reaction, cutaneous hypersensitivity:

    Syrup:
  • 2 mg
    ORALLY
    every 4 to 6 hours

  • Extended-release tablets
    :
  • 4 to
    6 mg
    ORALLY
    at
    bedtime
    or every 8 to 10 hours during the day

  • Common cold

    :

  • 2 mg
    ORALLY
    every 46
    hours
  • 4 to
    6 mg
    ORALLY
    at
    bedtime
    or every 810 hours

  • Dermatographic urticaria, vasomotor

    rhinitis

    :

    Syrup:
  • 2 mg
    ORALLY
    every 4 to 6 hours

  • Extended-release tablets
    :
  • 4 to
    6 mg
    ORALLY
    at
    bedtime
    or every 8 to 10 hours during the day

  • Pediatric dosing of

    Dexchlorpheniramine Maleate

    :

    Important Note:
  • Beers Criteria:

    Use

    caution or
    avoid

    use

    as potentially inappropriate in older adults.

  • Allergic

    conjunctivitis,

    Allergic

    rhinitis

    , Anaphylaxis; Adjunct, Blood transfusion reaction:

    Syrup:
  • Ages
    12 years and older:
    2 mg
    ORALLY
    every 4 to 6 hours
  • Ages
    6 to 11 years: 1

    mg

    ORALLY
    every 4 to 6 hours
  • Ages
    2 to 6 years: 0.5

    mg

    ORALLY
    every 4 to 6 hours

  • Extended-release tablets
    :
  • Ages
    12 years and older: 4 to
    6 mg
    ORALLY
    at
    bedtime
    or every 8 to 10 hours during the day
  • Ages
    6 to 12 years: 4

    mg

    ORALLY
    once daily at
    bedtime

  • Common cold

    :

    2-5 years:
  • 0.5

    mg

    ORALLY
    every 46 hours

  • 6-11 years:
  • 1

    mg

    ORALLY
    every 46 hours

  • 6-12 years:
  • 4

    mg

    ORALLY
    at
    bedtime

  • Cutaneous hypersensitivity, Dermatographic urticaria, vasomotor

    rhinitis

    :

    Syrup:
  • Ages
    12 years and older:
    2 mg
    ORALLY
    every 4 to 6 hours
  • Ages
    6 to 11 years: 1

    mg

    ORALLY
    every 4 to 6 hours
  • Ages
    2 to 6 years: 0.5

    mg

    ORALLY
    every 4 to 6 hours

  • Extended-release tablets
    :
  • Ages
    12 years and older: 4 to
    6 mg
    ORALLY
    at
    bedtime
    or every 8 to 10 hours during the day
  • Ages
    6 to 12 years: 4

    mg

    ORALLY
    once daily at
    bedtime

  • Indications
    FDA-Labeled Indications of

    Dexchlorpheniramine Maleate

    :

  • Allergic

    conjunctivitis
  • Allergic

    rhinitis

  • Anaphylaxis; Adjunct
  • Blood transfusion reaction
  • Common cold

  • Cutaneous hypersensitivity
  • Dermatographic urticaria
  • Vasomotor

    rhinitis


  • Mechanism of Action
  • Dexchlorpheniramine maleate

    ; an

    antihistamine

    with anticholinergic properties; competes with histamine for receptor sites on effector cells in the control of

    allergic

    reaction; aside from inducing slight to moderate sedation.
  • Adverse Effect
    Common Adverse effect of

    Dexchlorpheniramine Maleate

    :

    Gastrointestinal:
  • Diarrhea
  • Epigastric discomfort
  • Nausea
  • Vomiting
  • Xerostomia

  • Neurologic:
  • Somnolence

  • Respiratory:
  • Nasal mucosa dry

  • Contraindication
  • Hypersensitivity to

    dexchlorpheniramine

    products; including racemic chlorpheniramine
  • Interaction
    Major:
  • Bupropion (theoretical)
  • Donepezil (theoretical)

  • Contraindication:
  • Tranylcypromine (theoretical)

  • Phamacokinetics
    Absorption of

    Dexchlorpheniramine Maleate

    :

    Time for Maximum Plasma Concentration (Tmax):
  • Oral: 3 hours

  • Distribution of

    Dexchlorpheniramine Maleate

    :

  • Plasma Protein binding: 69% to 72%

  • Metabolism of

    Dexchlorpheniramine Maleate

    :

  • Extensively metabolized

  • Excretion of

    Dexchlorpheniramine Maleate

    :

  • Renal: 19% in 24 hours and 34% in 48 hours
  • Dialyzable: little value

  • Elimination of

    Dexchlorpheniramine Maleate

    :

  • 20 hours to 24 hours

  • Precaution
    Beers Criteria:
  • Avoid

    use

    in elderly patients as the highly anticholinergic effects and reduced clearance with advanced age increase the risk of anticholinergic effects and toxicity. Tolerance develops when used as a hypnotic. In men with lower urinary tract symptoms or benign prostatic hyperplasia; decreased urinary flow and urinary retention may occur.
  • Bladder neck obstruction
  • Bronchial asthma
  • Narrow angle glaucoma
  • Prostatic hypertrophy; symptomatic
  • Pyloroduodenal obstruction
  • Stenosing peptic ulcer
  • Pregnancy Category
  • B (FDA)
  • A (AUS)
  • Breast Feeding
  • Infant Risk Cannot be Ruled out.
  • Monitoring
  • Improvement in

    rhinitis

    symptoms
  • Improved skin manifestations of urticaria or angioedema
  • CNS effects
  • How to Take or Administration
    Oral:
    Extended release tablet:
  • Do not crush or chew, swallow whole
  • Treatment
    Management of Mild to Moderate Toxicity:
  • The majority of

    antihistamine

    overdoses require only supportive care
  • Give activated charcoal if

    patient

    presents shortly after ingestion
  • Sedate with

    benzodiazepines

    for agitation and delirium.
  • Hypertension and tachycardia are generally mild and well tolerated; and do not require specific treatment.
  • Physostigmine can be used to establish a diagnosis; it may also help
    avoid
    an invasive; costly workup; but should only be given in a setting where intensive monitoring and resuscitation are available.
  • It should NOT be given if there is a history or ECG (QRS widening) evidence that suggests a tricyclic antidepressant poisoning.

  • Management of Severe Toxicity:
  • Orotracheal intubation for airway protection should be performed early.
  • Gastric lavage may be of benefit; if the

    patient

    presents soon after a large ingestion; administer activated charcoal as well.
  • GI decontamination should be performed only in patients who can protect their airway or who are intubated.
  • Severe delirium may develop and require large doses of benzodiazepines for sedation.
  • Seizures (may rarely progress to status epilepticus) may require aggressive

    use

    of benzodiazepines; propofol and/or barbiturates.
  • Monitor for QRS widening and ventricular dysrhythmias; treat with intravenous sodium bicarbonate (1 to 2 mEq/kg IV bolus starting dose; titrate to blood pH 7.45 to 7.55); or lidocaine if sodium bicarbonate unsuccessful.
  • Monitor core temperature and treat hyperthermia with aggressive benzodiazepine sedation to control agitation and external cooling.
  • Clinical manifestations may be prolonged due to delayed absorption in the setting of an anticholinergic ileus.
  • Toxicology
  • Depends on the specific

    antihistamine

    ; assessment of

    patient

    signs and symptoms are generally more important than attempting to determine
  • Patient Counselling or Clinical Teaching
  • Patient

    should
    avoid
    activities requiring mental alertness until drug effects are realized; as drug may cause somnolence.
  • This drug may cause anticholinergic effects; diarrhea; epigastric discomfort; nausea; vomiting; or dry nasal mucosa.
  • Patient

    should
    avoid
    alcohol and other CNS depressants while taking this drug.












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