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Total Categories: 6
Zafirlukast functions by directly relaxing the smooth muscles in the airways to improve airflow.
Answer: False
Zafirlukast functions by blocking the action of cysteinyl leukotrienes on CysLT1 receptors, which reduces airway inflammation and bronchoconstriction, rather than by directly relaxing smooth muscles.
Zafirlukast's pharmacodynamic action involves blocking the effects of cysteinyl leukotrienes on specific receptors.
Answer: True
Pharmacodynamically, Zafirlukast acts as an antagonist of the cysteinyl leukotriene receptor 1 (CysLT1), blocking the effects of cysteinyl leukotrienes.
Cysteinyl leukotrienes contribute to asthma symptoms by causing vasodilation and reducing mucus secretion.
Answer: False
Cysteinyl leukotrienes contribute to asthma symptoms by causing bronchoconstriction, increasing mucus secretion, and promoting airway edema, not vasodilation.
Zafirlukast antagonizes cysteinyl leukotrienes, including LTC4, LTD4, and LTE4.
Answer: True
Zafirlukast acts as an antagonist to cysteinyl leukotrienes, specifically Leukotriene C4 (LTC4), Leukotriene D4 (LTD4), and Leukotriene E4 (LTE4).
Research suggests Zafirlukast may act as a partial inverse agonist at the CysLT1 receptor, though its primary role is antagonist.
Answer: True
Some research indicates Zafirlukast might function as a partial inverse agonist at the CysLT1 receptor, in addition to its primary role as an antagonist.
What is the primary classification of Zafirlukast?
Answer: A leukotriene receptor antagonist (LTRA)
Zafirlukast is primarily classified as an orally administered leukotriene receptor antagonist (LTRA).
How does Zafirlukast exert its therapeutic effect in asthma?
Answer: By blocking the action of cysteinyl leukotrienes on CysLT1 receptors
Zafirlukast exerts its therapeutic effect by competitively inhibiting the binding of cysteinyl leukotrienes (LTC4, LTD4, LTE4) to their CysLT1 receptors on airway cells.
What is the primary role of cysteinyl leukotrienes in asthma, according to the source?
Answer: To cause bronchoconstriction, mucus secretion, and edema
Cysteinyl leukotrienes play a primary role in asthma by inducing bronchoconstriction, increasing mucus secretion, and contributing to airway edema.
Zafirlukast is primarily prescribed for the immediate relief of acute asthma attacks.
Answer: False
Zafirlukast is indicated for the chronic management of asthma and is not designed for the immediate relief of acute asthma attacks.
Zafirlukast is considered more effective than inhaled glucocorticoids when used as the sole treatment for asthma.
Answer: False
Zafirlukast is generally considered less effective than inhaled glucocorticoids when used as monotherapy for asthma management.
Zafirlukast is recommended for patients with a known hypersensitivity to the drug.
Answer: False
Zafirlukast is contraindicated in individuals who have a known hypersensitivity or allergic reaction to the medication.
Zafirlukast has demonstrated clear cost-effectiveness in managing asthma.
Answer: False
While some preliminary evidence suggests potential cost savings, the overall cost-effectiveness of Zafirlukast in asthma management has not been definitively established.
Zafirlukast has been investigated for potential benefits in treating chronic urticaria and COPD.
Answer: True
Research has explored Zafirlukast's potential therapeutic benefits beyond asthma, including its investigation for treating chronic urticaria and improving lung function in patients with Chronic Obstructive Pulmonary Disease (COPD).
For which condition is Zafirlukast primarily indicated?
Answer: Chronic management of asthma in adults and children over five years old
Zafirlukast is primarily indicated for the chronic management of asthma in adults and children aged five years and older.
Zafirlukast is generally considered less effective than which other class of asthma medications when used alone?
Answer: Inhaled glucocorticoids
When used as monotherapy for asthma, Zafirlukast is generally considered less effective than inhaled glucocorticoids.
Zafirlukast is contraindicated in patients with:
Answer: Known hypersensitivity to the medication
Zafirlukast is contraindicated in patients who exhibit known hypersensitivity or allergic reactions to the drug itself.
Which of the following is NOT mentioned as an investigated or suggested indication for Zafirlukast besides asthma?
Answer: Hypertension
While Zafirlukast has been investigated for chronic urticaria and COPD, hypertension is not mentioned as an investigated or suggested indication.
Kidney impairment significantly affects the way Zafirlukast is absorbed and eliminated by the body.
Answer: False
Renal impairment does not appear to significantly alter the pharmacokinetic profile of Zafirlukast, meaning its absorption, distribution, metabolism, and excretion are not notably affected by kidney issues.
Significant liver damage can lead to increased clearance of Zafirlukast from the body.
Answer: False
Significant hepatic impairment can impair the clearance of Zafirlukast, potentially leading to increased plasma concentrations and drug exposure, rather than increased clearance.
Zafirlukast is extensively metabolized in the liver by the enzyme CYP2C9 into active metabolites.
Answer: False
Zafirlukast is extensively metabolized in the liver by CYP2C9, but its metabolites are considered inactive.
The primary route of elimination for Zafirlukast from the body is through urine.
Answer: False
The primary route of elimination for Zafirlukast is through biliary excretion, leading to fecal elimination; it is not significantly excreted via urine.
Genetic variations in the LTC4 synthase gene are linked to a potentially better response to Zafirlukast.
Answer: False
Genetic polymorphisms in the LTC4 synthase gene have been associated with a decreased clinical response to Zafirlukast, particularly in individuals with severe asthma phenotypes.
Individuals with genetic variations that reduce CYP2C9 function may experience lower Zafirlukast levels.
Answer: False
Genetic variations that reduce CYP2C9 function can lead to decreased clearance of Zafirlukast, consequently resulting in higher plasma levels and increased drug exposure.
Zafirlukast's interaction with CYP2C9 primarily involves its inhibition of this enzyme, thereby affecting the metabolism of other drugs.
Answer: False
Zafirlukast is primarily metabolized by CYP2C9, meaning it is a substrate for this enzyme. Its primary interaction affecting other drugs involves the inhibition of CYP3A4, not CYP2C9.
The bioavailability of Zafirlukast is well-documented and known to be high.
Answer: False
The bioavailability of Zafirlukast is listed as unknown in the provided source material.
Zafirlukast is highly bound to plasma proteins, primarily albumin, exceeding 99% binding.
Answer: True
Zafirlukast exhibits high protein binding in plasma, with over 99% bound to albumin.
The primary metabolites of Zafirlukast are pharmacologically active and contribute to its therapeutic effect.
Answer: False
The primary metabolites of Zafirlukast are hydroxylated and considered pharmacologically inactive.
Zafirlukast has an elimination half-life of approximately 24 hours.
Answer: False
The elimination half-life of Zafirlukast is approximately 10 hours, not 24 hours.
Fecal excretion is the main pathway for Zafirlukast elimination from the body.
Answer: True
Zafirlukast is primarily eliminated through biliary excretion, which results in fecal excretion being the main pathway from the body.
Albumin's role concerning Zafirlukast is primarily related to its metabolism in the liver.
Answer: False
Albumin's primary role concerning Zafirlukast is its high protein binding, facilitating transport throughout the body, not its metabolism in the liver.
How does hepatic impairment affect Zafirlukast pharmacokinetics?
Answer: It can impair clearance, leading to increased plasma concentration.
Significant hepatic impairment can impair the clearance of Zafirlukast, leading to an increase in its plasma concentration and overall drug exposure.
Which enzyme is primarily responsible for the metabolism of Zafirlukast?
Answer: CYP2C9
Zafirlukast undergoes extensive metabolism in the liver, primarily mediated by the cytochrome P450 enzyme CYP2C9.
What is the primary route of elimination for Zafirlukast?
Answer: Biliary excretion
The primary route of elimination for Zafirlukast from the body is through biliary excretion, leading to its presence in feces.
Zafirlukast is highly bound to which plasma protein?
Answer: Albumin
Zafirlukast is highly bound to plasma proteins, predominantly albumin, with binding exceeding 99%.
The source states that Zafirlukast's bioavailability is:
Answer: Unknown
According to the provided source material, the bioavailability of Zafirlukast is listed as unknown.
Headaches and nausea are the most frequently reported side effects of Zafirlukast.
Answer: True
Headaches and gastrointestinal upset, including nausea, are among the most frequently reported side effects associated with Zafirlukast use.
Hallucinations and insomnia are considered rare side effects of Zafirlukast.
Answer: False
While hallucinations and insomnia are potential neuropsychiatric side effects associated with Zafirlukast and other leukotriene receptor antagonists, they are not exclusively classified as rare. They are part of a spectrum of potential neuropsychiatric effects identified through post-marketing surveillance.
Neuropsychiatric side effects associated with Zafirlukast were primarily identified during initial clinical trials.
Answer: False
Neuropsychiatric side effects associated with Zafirlukast were primarily identified through post-marketing surveillance, as initial clinical trials were not specifically designed to detect these effects.
Hepatotoxicity, or liver damage, from Zafirlukast typically occurs within the first month of treatment.
Answer: False
Zafirlukast-induced hepatotoxicity typically occurs within 2 to 6 months of initiating treatment, not usually within the first month.
The exact mechanism causing Zafirlukast-induced hepatotoxicity is well understood and confirmed.
Answer: False
The precise mechanism underlying Zafirlukast-induced hepatotoxicity remains unclear and is hypothesized to involve a metabolic intermediate.
Eosinophilic Granulomatosis with Polyangiitis (EGPA) is directly caused by Zafirlukast treatment.
Answer: False
While cases of EGPA have been reported in patients using Zafirlukast, it is not believed to be directly causative but rather associated with underlying conditions and treatment changes in asthma management.
Overdoses of Zafirlukast, even up to 200 mg, have consistently resulted in fatalities.
Answer: False
The highest reported overdose amount for Zafirlukast was 200 mg, and all patients who experienced overdoses survived, reporting symptoms such as rash and upset stomach.
Zafirlukast can increase the concentration of drugs metabolized by CYP3A4, such as warfarin.
Answer: True
Zafirlukast inhibits the cytochrome P450 enzyme CYP3A4, which can lead to increased concentrations of other drugs metabolized by this enzyme, such as warfarin.
Zafirlukast-induced hepatotoxicity predominantly affects males and is usually mild.
Answer: False
Zafirlukast-induced hepatotoxicity predominantly affects females and can range from mild to fatal, posing a significant risk.
Which of the following is a common side effect of Zafirlukast?
Answer: Headaches and gastrointestinal upset
Headaches and gastrointestinal upset, such as nausea and stomach discomfort, are among the most frequently reported side effects of Zafirlukast.
Which of the following is a potential serious adverse effect associated with Zafirlukast?
Answer: Acute liver injury (hepatotoxicity)
Acute liver injury, or hepatotoxicity, is a potential serious adverse effect associated with Zafirlukast treatment.
What effect does Zafirlukast have on drugs metabolized by CYP3A4?
Answer: It decreases their metabolism, potentially increasing their levels.
Zafirlukast inhibits CYP3A4, which can decrease the metabolism of drugs processed by this enzyme, potentially leading to elevated plasma concentrations of those drugs.
Which of the following is a potential neuropsychiatric side effect reported with Zafirlukast?
Answer: Auditory hallucinations
Auditory hallucinations are among the potential neuropsychiatric side effects that have been reported in association with Zafirlukast use.
Adults and children aged 5 to 12 years old should both take the 20 mg dosage of Zafirlukast.
Answer: False
The recommended dosage for Zafirlukast differs by age group; adults and children over 12 years typically take 20 mg, while children aged 5 to 12 years are prescribed 10 mg.
Zafirlukast tablets should be stored in a cool, damp place to maintain their stability.
Answer: False
Zafirlukast tablets should be stored at room temperature, protected from direct sunlight and moisture, not in a damp environment.
Older adults (65+) taking Zafirlukast may experience increased plasma concentrations of the drug due to impaired hepatic clearance.
Answer: True
In individuals aged 65 and older, Zafirlukast's hepatic clearance is impaired, leading to higher plasma concentrations and increased drug exposure.
Zafirlukast is classified as a pregnancy category C drug, indicating potential risks to the fetus.
Answer: False
Zafirlukast is classified as pregnancy category B. Animal studies did not demonstrate teratogenicity at doses up to 20 times the maximum recommended human dose.
There is extensive data available on the effects of Zafirlukast use during lactation.
Answer: False
Data regarding the effects of Zafirlukast use during lactation is limited, with only a small percentage of the maternal dose expected to transfer to the infant via breast milk.
Taking Zafirlukast with a high-fat meal enhances its oral absorption.
Answer: False
The oral absorption of Zafirlukast is reduced by approximately 40% when taken with meals high in fat or protein; it should be taken on an empty stomach.
The effectiveness of Zafirlukast in pediatric asthma is generally higher in children with more severe, atopic asthma.
Answer: False
Research suggests that Zafirlukast may be more effective in younger children with less atopic asthma, rather than those with more severe, atopic asthma.
What dosage strength of Zafirlukast is recommended for children aged 5 to 12 years?
Answer: 10 mg
For pediatric patients aged 5 to 12 years, the recommended dosage strength of Zafirlukast is 10 mg.
What is the recommended way to take Zafirlukast concerning meals?
Answer: Take on an empty stomach, one hour before or two hours after meals.
To maximize absorption, Zafirlukast should be taken on an empty stomach, defined as one hour before or two hours after a meal, as food intake reduces absorption.
What is the reported pregnancy category for Zafirlukast?
Answer: Category B
Zafirlukast is classified under pregnancy category B, indicating that animal reproduction studies have not demonstrated a risk to the fetus, and there are no adequate studies in pregnant women.
How does Zafirlukast's absorption change when taken with a meal high in fat?
Answer: Absorption decreases by approximately 40%.
Taking Zafirlukast with a meal high in fat or protein reduces its oral absorption by approximately 40%.
Accolate is the brand name for Zafirlukast in the United States and was the first drug of its kind approved by the FDA.
Answer: True
Accolate is the United States brand name for Zafirlukast, and it holds historical significance as the first cysteinyl leukotriene receptor antagonist approved by the FDA.
Zafirlukast is practically insoluble in water but soluble in organic solvents like methanol.
Answer: False
Zafirlukast is practically insoluble in water but shows slight solubility in methanol; it is freely soluble in other organic solvents like tetrahydrofuran and acetone.
Zafirlukast was approved in the US in 1996, marking it as the first leukotriene receptor antagonist.
Answer: True
Zafirlukast received US FDA approval in 1996, signifying its status as the first approved cysteinyl leukotriene receptor antagonist.
Zafirlukast is exclusively used in human medicine and has no applications in veterinary care.
Answer: False
Zafirlukast does have applications in veterinary medicine, notably for the treatment of bronchial asthma in cats.
The IUPAC name for Zafirlukast includes the term 'carbamate'.
Answer: True
The IUPAC name for Zafirlukast, Cyclopentyl 3-{2-methoxy-4-[(o-tolylsulfonyl)carbamoyl]benzyl}-1-methyl-1H-indol-5-ylcarbamate, indeed includes the term 'carbamate'.
Zafirlukast's chemical formula is C31H33N3O6S, corresponding to a molar mass of approximately 575.68 g/mol.
Answer: True
The chemical formula for Zafirlukast is C31H33N3O6S, and its molar mass is approximately 575.68 g/mol.
Zafirlukast has a melting point significantly above 200 degrees Celsius.
Answer: False
Zafirlukast has a melting point range of 138 to 140 degrees Celsius, which is not significantly above 200 degrees Celsius.
Zafirlukast is classified under the ATC code R03DC01.
Answer: True
Zafirlukast is classified under the Anatomical Therapeutic Chemical (ATC) Classification System with the code R03DC01.
In the United Kingdom, Zafirlukast is available over-the-counter without a prescription.
Answer: False
In the United Kingdom, Zafirlukast is classified as POM (Prescription Only), meaning it is not available over-the-counter.
What is the significance of Zafirlukast (Accolate) in the history of asthma medication?
Answer: It was the first cysteinyl leukotriene receptor antagonist approved by the FDA.
Zafirlukast, marketed as Accolate, holds historical significance as it was the first cysteinyl leukotriene receptor antagonist approved by the U.S. Food and Drug Administration (FDA).
The source lists Zafirlukast's chemical formula as:
Answer: C31H33N3O6S
The chemical formula for Zafirlukast is C31H33N3O6S.
What is the approximate molar mass of Zafirlukast?
Answer: 575.68 g/mol
The molar mass of Zafirlukast is approximately 575.68 g/mol.
What is the ATC code for Zafirlukast?
Answer: R03DC01
The ATC code assigned to Zafirlukast is R03DC01.
The source indicates that Zafirlukast is used in veterinary medicine for which condition?
Answer: Bronchial asthma in cats
Zafirlukast finds application in veterinary medicine, specifically for the treatment of bronchial asthma in feline patients.
What is the approximate melting point range for Zafirlukast?
Answer: 138-140 °C
Zafirlukast exhibits a melting point range of approximately 138 to 140 degrees Celsius.
According to the source, Zafirlukast is practically insoluble in:
Answer: Water
Zafirlukast is characterized as being practically insoluble in water.