Accolate (Zafirlukast) - Uses, Dose, Side effects, and Brands ...

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

Risk Factor C (Monitor therapy)

Alpelisib

May lower the serum level of CYP2C9 substrates (High risk with Inducers).

CYP2C9 Inducers (Moderate)

May lower the serum level of CYP2C9 substrates (High risk with Inducers).

Erythromycin (Systemic)

May lower the level of zafirlukast in the serum.

Lumacaftor

May decrease the serum concentration of CYP2C9 Substrates (High Risk with Inhibitors or Inducers). Lumacaftor may increase the serum concentration of CYP2C9 Substrates (High Risk with Inhibitors or Inducers).

Rifapentine

May decrease the serum concentration of CYP2C9 Substrates (High risk with Inducers).

Theophylline Derivatives

May lower the level of zafirlukast in the serum. Theophylline derivatives' serum levels may rise when zafirlukast is used. Dyphylline is an exception.

Vitamin K Antagonists (eg, warfarin)

The blood concentration of Vitamin K antagonists may rise when using zafirlukast.

Risk Factor D (Consider therapy modification)

Dabrafenib

May lower the serum level of CYP2C9 substrates (High risk with Inducers). Management: When possible, look for CYP2C9 substrate substitutes. If concurrent therapy cannot be avoided, pay special attention to the substrate's clinical consequences (particularly therapeutic effects).

Enzalutamide

May lower the serum level of CYP2C9 substrates (High risk with Inducers). Treatment: Enzalutamide should not be used concurrently with CYP2C9 substrates that have a limited therapeutic index. Enzalutamide use, like with the use of any other CYP2C9 substrate, should be done with caution and under close observation.

Risk Factor X (Avoid combination)

Loxapine

Agents to Treat Airway Disease may enhance the adverse/toxic effect of Loxapine. More specifically, the use of Agents to Treat Airway Disease is likely a marker of patients who are likely at a greater risk for experiencing significant bronchospasm from use of inhaled loxapine. Management: This is specific to the Adasuve brand of loxapine, which is an inhaled formulation. This does not apply to non-inhaled formulations of loxapine.

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:

Zafirlukast [Tabs 10 Mg]

Novilokast Novins International
Zafiro Scotmann Pharmaceuticals
Zair Wilshire Laboratories (Pvt) Ltd.
Zilesta Genix Pharma (Pvt) Ltd
Zukast Everest Pharmaceuticals

Zafirlukast [Tabs 20 Mg]

Accolate ICI Pakistan Ltd.
Benalucost Tg Pharma
Freair Medisure Laboratories Pakistan (Pvt.) Ltd.
Nefes Macter International (Pvt) Ltd.
Novilokast Novins International
Z-Kast Lowitt Pharmaceuticals (Pvt) Ltd
Z-Saf Saaaf Pharmaceuticals
Zafir Acme Laboratories Pakistan (Pvt) Ltd.
Zafiro Scotmann Pharmaceuticals
Zair Wilshire Laboratories (Pvt) Ltd.
Zakulate 3h Hamaz Pharmaceutical (Pvt) Ltd.
Zilesta Genix Pharma (Pvt) Ltd
Zukast Everest Pharmaceuticals