Drug information of chlorcyclizine + pseudoephedrine

chlorcyclizine + pseudoephedrine

Drug group:

Chlorcyclizine and pseudoephedrine is a combination medicine used to treat runny or stuffy nose, sneezing, itching, watery eyes, sinus congestion, and other cold or allergy symptoms.

Mechanism of effect

Chlorcyclizine is an antihistamine that reduces the effects of natural chemical histamine in the body. Histamine can produce symptoms of sneezing, itching, watery eyes, and runny nose.

Pseudoephedrine is a decongestant that shrinks blood vessels in the nasal passages. Dilated blood vessels can cause nasal congestion (stuffy nose). Through direct action on alpha-adrenergic receptors in the mucosa of the respiratory tract, pseudoephedrine produces vasoconstriction. Pseudoephedrine relaxes bronchial smooth muscle by stimulating beta2-adrenergic receptors. Like ephedrine, pseudoephedrine releasing norepinephrine from its storage sites, an indirect effect. This is its main and direct mechanism of action. The displaced noradrenaline is released into the neuronal synapse where it is free to activate the postsynaptic adrenergic receptors.

Pharmacodynamic

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Pharmacokinetics

Chlorcyclizine

Absorption: Readily absorbed after oral administration and widely distributed throughout the body. Metabolised by N-demethylation to form norchlorcyclizine and by N-oxidation.

 

Volume of distribution: After a single oral dose of 2 mg/kg to 4 subjects, average peak plasma concentrations of about 0.05 mg/L and 0.03 mg/L were attained in 5 h for unchanged drug and norchlorcyclizine, respectively. After oral administration of 50 mg 3 times a day for 6 days, plasma concentrations of norchlorcyclizine of 0.05 to 0.11 mg/L were reported on the first day after the cessation of treatment and plasma concentrations of 0.02 to 0.04 mg/L were found on the 10th day after cessation of treatment.

 

Protein binding: about 85 to 90%.

 

Metabolism: High concentrations of the N-desmethyl metabolite are found in the liver, lungs, kidney, and spleen.

 

Route of elimination: urine

 

Half life: about 12 h

 

pseudoephedrine

Absorption: Pseudoephedrine is readily and almost completely absorbed from the GI tract and

 

there is no evidence of first-pass metabolism.

Protein binding: Pseudoephedrine does not bind to human plasma proteins over the concentration range of 50 to 2000 ng/mL

 

Metabolism: Hepatic.

 

Half life: 9-16 hours

Drug indications

nasal stuffiness

Dosage

Usual Adult Dose for Nasal Congestion

Chlorcyclizine-pseudoephedrine 25 mg-60 mg oral tablet:
1 tablet orally every 6 to 8 hours not to exceed 3 tablets daily.

Chlorcyclizine-pseudoephedrine 9.375 mg-30 mg/5 mL oral liquid:
10 mL orally every 6 hours not to exceed 40 mL daily.

Usual Pediatric Dose for Nasal Congestion

Chlorcyclizine-pseudoephedrine 25 mg-60 mg oral tablet:
6 to 11 years: 1/2 tablet orally every 6 to 8 hours not to exceed 1 1/2 tablets daily.
12 years or older: 1 tablet orally every 6 to 8 hours not to exceed 3 tablets daily.

Chlorcyclizine-pseudoephedrine 9.375 mg-30 mg/5 mL oral liquid:
6 to 11 years: 5 mL orally every 6 hours not to exceed 20 mL daily.
12 years or older: 10 mL orally every 6 hours not to exceed 40 mL daily.

Alerts

  • high blood pressure;
  • coronary artery disease (hardened arteries),
  • bladder obstruction or other urination problems; or
if you take potassium

Points of recommendation

Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Cold medicine is usually taken only for a short time until your symptoms clear up.

Do not give this medication to a child younger than 4 years old. Always ask a doctor before giving a cough or cold medicine to a child. Death can occur from the misuse of cough and cold medicines in very young children.

Measure liquid medicine with a special dose-measuring spoon or medicine cup.

Call your doctor if your symptoms do not improve after 7 days of treatment, or if you have a fever with a headache, cough, or skin rash.

If you need surgery or medical tests, tell the surgeon or doctor ahead of time if you have taken a cold medicine within the past few days.

Store at room temperature away from moisture and heat. Do not freeze.

 If you are taking the medication regularly, take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

chlorcyclizine and pseudoephedrine may cause blurred vision and may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly.

Drinking alcohol can increase certain side effects of this medication.

Ask a doctor or pharmacist before using any other cold, allergy, cough, or sleep medicine. Antihistamines and decongestants are contained in many combination medicines. Taking certain products together can cause you to get too much of a certain drug. Check the label to see if a medicine contains an antihistamine or decongestant.


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