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.
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. |
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. |
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 |