Accolate (Zafirlukast) is a leukotriene receptor antagonist that has anti-inflammatory effects, relaxes the smooth muscles, and relieves airway edema. It is used to treat the following conditions:

• Prophylaxis and treatment of asthma in adults and children older than 5 years of age

• Chronic urticaria

Accolate (Zafirlukast) Dose in Adults

Dose in the treatment of Asthma:

• 20 mg orally two times a day

Off-label use in the treatment of Chronic urticaria:

• 20 mg orally two times a day

Accolate (Zafirlukast) Dose in Children

Dose in the treatment of Chronic Asthma:

• Children 5 - 11 years:
  • 10 mg orally two times a day
• Children older than 12 years and Adolescents:
  • 20 mg orally two times a day.

Pregnancy Risk Factor B

• Patients using zafirlukast during pregnancy have not experienced any adverse events, including teratogenic effects.
• It shouldn't be used as a first-line therapy for pregnant women. However, it can be continued if the patient is currently taking it.

Use of Accolate (Zafirlukast), during breast-feeding:

• It is excreted in breast milk.
• The manufacturer doesn't recommend that you continue breastfeeding while using it 

Accolate (Zafirlukast) Dose in Renal Disease:

Dose adjustment in patients with renal disease is not required.

Accolate (Zafirlukast) Dose in Liver Disease:

It is contraindicated in patients with liver disease

Common Side Effects of Accolate (Zafirlukast) Include:

• Central nervous system:
  • Headache

Less Common Side Effects of Accolate (Zafirlukast) Include:

• Central nervous system:
  • Dizziness
  • Pain
• Gastrointestinal:
  • Nausea
  • Diarrhea
  • Abdominal pain
  • Vomiting
  • Dyspepsia
• Hepatic:
  • Increased serum ALT
• Infection:
  • Infection
• Neuromuscular & skeletal:
  • Back pain
  • Myalgia
  • Weakness
• Miscellaneous:
  • Fever

Contraindication to Accolate (Zafirlukast) Include:

• Allergy to Accolate (zafirlukast), or any component of this formulation
• Hepatic impairment (liver cirrhosis)

Warnings and Precautions

• Eosinophilia, vasculitis:
  • Patients might present with systemic Eosinophilia or clinical vasculitis, which could be consistent with Churg Strauss syndrome or eosinophilic Granulomatosis with Polyangiitis.
  • Patients should be checked for eosinophilia and vasculitic skin rash, worsening of pulmonary symptoms, cardiac complications, neuropathy, and worsening of pulmonary symptoms.
• Hepatotoxicity:
  • It may lead to liver dysfunction, such as hyperbilirubinemia and hepatic failure.
  • It is important to periodically assess the liver and educate the patient about the signs and symptoms of hepatotoxicity such as anorexia and nausea.
  • If hepatotoxicity has been confirmed biochemically, treatment should be stopped immediately
  • Preexisting hepatic impairments should be avoided when prescribing the drug.
• Infections
  • Patients on zafirlukast are more likely to get infected, especially those over 55.
  • The respiratory tract is the most common area of infection.
• Events in neuropsychiatrics:
  • It is associated with behavioral changes like depression and insomnia.
  • It is important that patients are instructed to report any neuropsychiatric symptoms and behavioral changes.

Zafirlukast: Drug Interaction

Monitor:

• For improvements in the symptoms of asthma
• Clinical features liver injury. (Periodic monitoring of liver function tests may be considered)

How to take (Accolate) Zafirlukast?

•  It should be administered at least one hour before or two hours after a meal.

Mechanism of action of Accolate (Zafirlukast):

• It is a leukotriene receptor antagonist (LTRA) that competitively and selectively inhibits leukotriene D4 and E4 components of slow-reacting substance of anaphylaxis.
• Leukotriene is produced and activated by its receptors.
• This causes smooth muscle constriction and airway edema.
• It also activates the inflammatory process. It is used to treat asthma and allergic airway diseases.

Thepeak effectIt is usually seen in 2 to 6 weeks

Duration of the actionIt takes approximately 12 hours. 

It can be done quicklyabsorbedIt is primarily bound by albumin.

It isHighly metabolizedby the liver via CYP2C9,

it has ahalf-life eliminationBetween 8 and 16 hours, it takes approximately 10 hours.

Time to get therepeak serum concentrationChildren spend 2 - 2.5 hours, while adults take 3 hours.

It is primarilyexcretedIn the feces (90%).

International Brands of Zafirlukast:

• Accolate
• Accoleit
• Alukast
• Ventair
• Zafir
• Zaft
• Zukast
• Zuvair

Zafirlukast (Accolate) in Pakistan: