Home Drugs Zafirlukast (Accolate) Uses, Side Effects, Interactions, Dosing Detailed 2020

Zafirlukast (Accolate) Uses, Side Effects, Interactions, Dosing Detailed 2020

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Zafirlukast (Accolate) Uses, Side Effects, Interactions, Dosing Detailed 2020

In this article, we will define Zafirlukast Uses that Where to Use of Zafirlukast, Accolate Side Effects and Zafirlukast Interaction with Other Drugs in details.

Zafirlukast is indicated for the prevention and chronic treatment of asthma in adults and in children five years old or older. 

It is a leukotriene receptor antagonist so actually it is used to control the symptoms of your asthma it is also used to prevent your asthma from getting worse so I can eat lock certain chemicals called leukotriene which causes narrowing and inflammation of the airways and also cause allergy symptoms. 

Like montelukast, zafirlukast is a selective, potent and competitive antagonist of the CysLT1.

 It antagonized the binding of LTD4 to CysLT1 with an IC50 ranging from 1.9 to 4.4 nM (Lynch et al. 1999; Sarau et al. 1999). When an in vitro comparison it was about 90-fold more potent than its metabolites in receptor antagonist activity (Accolate Label 2011).

Uses

It is used for preventions, control and chronic asthma especially in children. It is used to reduce bronchoconstriction induced by several stimuli, including

LTD4, allergens, exercise, and cold air, sulfur oxide or platelet-activating factor. When we compare inhalers of corticosteroids, zafirlukast is, like montelukast, less effective.

   However,  the addition of zafirlukast to inhaled corticosteroid therapy has been at least as effective as doubling of the corticosteroid doses. When we compare it to fluticasone, fluticasone was significantly superior to zafirlukast ineffectiveness.

It can be administered orally or by IV injection. It is taken before a meal when the stomach is empty, i.e before meal about 1 to 2 hours before a meal. The dosage of the drug depends upon age.

Side Effects

Doctors always prescribed drugs according to patients’ health and keeping the side effects of the drugs in mind. Although all drugs have side effects doctors suggest those drugs which have less impact on the patient.

The most frequent adverse effects include Headache, then a few common side effects i.e Nausea, Diarrhea, and infection.

Zafirlukast has been associated with Churg-Strauss syndrome, which is a rare form of vasculitis characterized by the presence of at least four of the following: asthma, eosinophilia, pulmonary infiltration, polyneuropathy, sinusitis, and extravascular eosinophils.

Mentally effects include 

  • Hallucinations 
  • Depression 
  • Loss of sleep
  • Anxiety 
  • Thoughts for suicide

Other rare adverse effects include hepatitis, yellowing of eyes, Darkening of Urine, sore throat.

Allergic reactions are rare in it but can cause skin rashes, itching, swelling of mouth, tongue, Dizziness, Breathlessness.

Other adverse effects include

  • Hyperbilirubinemia i.e increase in blood bilirubin
  • GIT disturbance 
  • Respiratory tract infection
  • Myalgia  

Precautions:

Before using any drug tell the doctor about allergy or any hereditary disease.

Before using a dication, tell about the disease you have, especially diseases associated with the liver.

Before using medication give all details about medication that you are using for any disease like diabetes, hypertension for any other disease.

If a woman is pregnant, use it by prescription of a doctor i.e by a gynecologist.

The drug can transfer to the baby through Breastfeeding. So patients must give a detailed family history to the doctor before using it.

Drug Interactions:

It inhibits the enzyme CYP3A4 as a result of this the plasma concentration of drugs increase as CYP3A4 metabolize some drugs such as Warfarin etc,

Coadministration of aspirin (2600 mg daily) with zafirlukast has resulted in a mean increase of

45% in its plasma concentrations i.e it increases the efficacy of the Zafirlukast.

When in turn single dose of zafirlukast was administered with erythromycin (500 mg three times daily to steady-state), the plasma concentrations of zafirlukast decreased by about 40%, presumably due to decreased bioavailability of zafirlukast, as a result, the efficacy of the Zafirlukast is decreased. Theophylline also decreases the effect of the zafirlukast.

Contraindications:

It is contraindicated in:

  • Liver diseases such as cirrhosis of the r
  • Renal Impairment such as Renal failure
  • Also due to Hypersensitivity
  • In children below 5 years

Dosage:

It is in the market in two dosage forms orally i.e is 10mg and 20mg.
For Children over 12 year and adults

20mg twice a day
For Below 12 to 5 Years

10 mg twice a day
Zafirlukast is generally not prescribed to patients above 50 years.

Dosage adjustment is not necessary.

Overdose:

The overdose of zafirlukast has no life-threatening effects up to 200mg overdose. There has not been any severe damage to the body.

It can cause stomach upset and rashes on overdose.

Brand Names:

  • Accolate was the first brand for the Zafirlukast in the USA.
  • Other includes 
  • Benalucost
  • Z-kast

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