Novilokast

Novilokast Uses, Dosage, Side Effects, Food Interaction and all others data.

Novilokast is a selective and competitive leukotriene-receptor antagonist (LTRA) of leukotriene D4 and E4 (LTD4 and LTE4), components of slow-reacting substance of anaphylaxis (SRSA). Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of asthma, including airway oedema, smooth muscle constriction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma.

Novilokast is a synthetic, selective peptide leukotriene receptor antagonist (LTRA) indicated for the prophylaxis and chronic treatment of asthma. Patients with asthma were found in one study to be 25-100 times more sensitive to the bronchoconstricting activity of inhaled LTD4 than nonasthmatic subjects. In vitro studies demonstrated that zafirlukast antagonized the contractile activity of three leukotrienes (LTC4, LTD4 and LTE4) in conducting airway smooth muscle from laboratory animals and humans. Novilokast prevented intradermal LTD4-induced increases in cutaneous vascular permeability and inhibited inhaled LTD4-induced influx of eosinophils into animal lungs.

Trade Name Novilokast
Availability Prescription only
Generic Zafirlukast
Zafirlukast Other Names Zafirlukast
Related Drugs Dupixent, Xolair, ProAir Digihaler, Symbicort, Breo Ellipta, Ventolin, Xopenex, Ventolin HFA
Weight 10mg, 20mg
Type Tablet
Formula C31H33N3O6S
Weight Average: 575.675
Monoisotopic: 575.209006493
Protein binding

99%

Groups Approved, Investigational
Therapeutic Class Leukotriene receptor antagonists
Manufacturer Novins International
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am
Novilokast
Novilokast

Uses

Zukast is used for the treatment of asthma.

Novilokast is also used to associated treatment for these conditions: Asthma, Chronic Urticaria

How Novilokast works

Novilokast is a selective and competitive receptor antagonist of leukotriene D4 and E4 (LTD4 and LTE4), components of slow-reacting substance of anaphylaxis (SRSA). Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle constriction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma.

Dosage

Novilokast dosage

Novilokast should be taken continuously. Children under 7 years of age: There is no clinical experience of the use of Novilokast in children under 7 years of age until safety information is available.Children over 7 years through 11 years of age: The recommended dose of Novilokast in this age group is 10 mg twice daily.Adult and children aged 12 years and over: The dosage is one 20 mg tablet twice daily. This dosage should not be exceeded. Higher doses may be associated with elevations of one or more liver enzymes consistent with hepatotoxicity. As food may reduce the bioavailability of Novilokast, Novilokast should not be taken with mealsElderly: The clearance of Novilokast is significantly reduced in elderly patients (over 65 years old), and Cmax and AUC are approximately double than those of younger adults. However, accumulation of Novilokast is not greater than that seen in multiple dose trials conducted in adult subjects with asthma and the consequences of the altered kinetic in the elderly are unknown. Clinical experience with Novilokast in the elderly (over 65 years) is limited and caution is recommended until further information is available.Renal impairment: No dosage adjustment is necessary in patients with mild renal impairment.

Side Effects

Effect on ability to drive or operate machinery: There is no evidence that Novilokast affects the ability to drive and use machinery. Administration of Novilokast in clinical trials against placebo has been associated with headache (9.9% vs. 9.0%) or gastrointestinal disturbance (nausea 2.6% vs. 2.2%, vomiting 1.2% vs. 1.0%, diarrhoea 2.3% vs. 1.8%, abdominal pain 1.6% vs. 1.2%). These symptoms are usually mild and do not necessitate withdrawal from therapy. During post-marketing experience, bruising, bleeding disorders, including menorrhagia (rare), thrombocytopaenia and agranulocytosis (very rare) have also been reported.Hypersensitivity reactions, including urticaria and angio-oedema have been reported. Rashes, including blistering, have also been reported. The above events have usually resolved during continued treatment or following cessation of therapy. Infrequently, elevated serum transaminase levels have been observed in clinical trials against placebo with Novilokast (increased AST 1.0% vs. 0.9%, increased AST 0.6% vs. 0.6%); at recommended doses the incidence was equivalent to placebo. Rarely the transaminase profile has been consistent with drug-induced hepatitis, which resolved following cessation of Novilokast therapy. During post-marketing experience there have been rare reports of hepatitis, with or without elevated bilirubin levels. These cases were usually reversible.In placebo controlled clinical trials, an increased incidence of infection has been observed in elderly patients given Novilokast (7.8% vs. 1.4%). Infections were usually mild, predominantly affecting the respiratory tract.

Toxicity

Side effects include rash and upset stomach.

Precaution

Novilokast should be taken regularly to achieve benefit, even during symptom free periods. Novilokast therapy should normally be continued during acute exacerbations of asthma. Novilokast does not allow a reduction in existing steroid treatment. As with inhaled steroids and hormones (disodium cromoglycate, nedocromil sodium), Novilokast is not indicated for use in the reversal of bronchospasm in acute asthma attacks. Novilokast has not been evaluated in the treatment of labile (brittle) or unstable asthma.Cases of Churg Strauss syndrome have been reported in association with Novilokast usage. A causal relationship has neither been confirmed nor refuted. If a patient develops a Churg Strauss syndrome type illness, Novilokast should be stopped, a re-challenge test should not be performed and treatment should not be restarted.Elevations in serum transaminases can occur during treatment with Novilokast. These are usually asymptomatic and transient but could represent early evidence of hepatotoxicity.If clinical symptoms or signs suggestive of liver dysfunction occur (e.g., nausea, vomiting, right upper quadrant pain, fatigue, lethargy, flu-like symptoms, enlarged liver, pruritus and jaundice), the serum transaminases, in particular serum ALT, should be measured and the patient managed accordingly. A decision to discontinue Novilokast should be individualized to the patient’s condition, weighing the risk of hepatic dysfunction against the clinical benefit of Novilokast to the patient.

Interaction

Novilokast may be administered with other therapies routinely used in the management of asthma and allergy. Inhaled steroids, inhaled and oral bronchodilator therapy, antibiotics and antihistamines are examples of agents which have been co-administered with Novilokast without adverse interaction.Novilokast may be administered with oral contraceptives without adverse interaction. Co-administration with Warfarin results in an increase in maximum prothrombin time by approximately 35%. It is therefore recommended that if Novilokast is co-administered with Warfarin, prothrombin time should be closely monitored. The interaction is probably due to an inhibition by Novilokast of the cytochrome P450 2C9 enzyme system. In clinical trials co-administration with Theophylline resulted in decreased plasma levels of Novilokast, by approximately 30%, but with no effect on plasma Theophylline levels. However, during postmarketing surveillance, there have been rare cases of patients experiencing increased Theophylline levels when co-administered with Novilokast.Co-administration with Terfenadine resulted in a 54% decrease in AUC for Novilokast, but with no effect on plasma Terfenadine levels. Coadministration with Acetylsalicylic acid (650 mg four times a day) may result in increased plasma levels of Novilokast, by approximately 45%.Co-administration with Erythromycin will result in decreased plasma levels of Novilokast, by approximately 40%. The clearance of Novilokast in smokers may be increased by approximately 20%

Food Interaction

  • Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.

[Moderate] ADJUST DOSING INTERVAL: Food may reduce the oral absorption and bioavailability of zafirlukast.

In two separate studies, one using a high-fat and the other a high-protein meal, administration of zafirlukast with food reduced the mean bioavailability by approximately 40%.

MANAGEMENT: To ensure maximal oral absorption, zafirlukast should be administered at least 1 hour before or 2 hours after meals.

Novilokast Disease Interaction

Major: liver disease

Volume of Distribution

  • 70 L

Elimination Route

Rapidly absorbed following oral administration, reduced following a high-fat or high-protein meal.

Half Life

10 hours

Clearance

  • apparent oral CL=20 L/h
  • 11.4 L/h [7-11 yrs]
  • 9.2 L/h [5-6 yrs]

Elimination Route

The most common metabolic products are hydroxylated metabolites which are excreted in the feces.

Pregnancy & Breastfeeding use

Pregnancy: The safety of Novilokast in human pregnancy has not been established. In animal studies, Novilokast did not have any apparent effect on fertility and did not appear to have any teratogenic or selective toxic effect on the foetus. The potential risks should be weighed against the benefits of continuing therapy during pregnancy and Novilokast should be used during pregnancy only if clearly needed.Lactation: Novilokast is excreted in human breast milk. Novilokast should not be administered to nursing mothers.

Contraindication

Novilokast should not be given to patients who have previously experienced hypersensitivity to the product or any of its ingredients. Novilokast is contraindicated in patients with a history of moderate or severe renal impairment. Novilokast is contraindicated in patients with hepatic impairment or cirrhosis; it has not been studied in patients with hepatitis or in long term studies of patients with cirrhosis. Novilokast is contraindicated in children under 7 years of age until safety information is available.

Storage Condition

Store between 20-25° C. Protect from light and moisture.

Innovators Monograph

You find simplified version here Novilokast

Novilokast contains Zafirlukast see full prescribing information from innovator Novilokast Monograph, Novilokast MSDS, Novilokast FDA label

FAQ

What is the Novilokast used for?

Brand is used to prevent asthma symptoms. Brand is in a class of medications called leukotriene receptor antagonists (LTRAs). It works by blocking the action of certain natural substances that cause swelling and tightening of the airways.

What is the mechanism of action of Novilokast?

Brand blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs and inflammation of the breathing passages.

Does Novilokast cause weight gain?

Weight gain is not a common side effect of Novilokast. Sometimes, people might have stomach issues, like diarrhea or nausea, when they start this medication, but they typically don't gain weight.

Does Novilokast cause depression?

This Novilokast may cause some people to be agitated, disoriented, irritable, or display other abnormal behaviors. It may also cause some people to have suicidal thoughts and tendencies or to become more depressed and have problems with sleep.

Is Novilokast an anti-inflammatory?

Brand also exhibited evidence of an anti-inflammatory effect in the lung in preliminary studies involving segmental antigen challenge. The results from these clinical trials demonstrate that Novilokast is effective and safe for the prophylactic treatment of asthma.

Does Novilokast require monitoring?

There are over 100 reported cases of severe hepatic failure with Novilokast. Signs of hepatitis, including right upper quadrant pain, jaundice, and pruritus, should warrant monitoring transaminases and discontinuation if clinical suspicion of hepatoxic effects occurs.

Is Novilokast a controlled substance?

Brand is used in the treatment of asthma, maintenance and belongs to the drug class leukotriene modifiers.Novilokast 20 mg is not a controlled substance under the Controlled Substances Act (CSA).

Do I take Novilokast with food?

Brand should be taken on an empty stomach, 1 hour before or 2 hours after a meal. To work properly, Novilokast must be taken every day at regularly spaced times, even if your asthma seems better.

What does Novilokast interact with?

Other medications can affect the removal of Novilokast from your body, which may affect how Novilokast works. An example is erythromycin, among others. This medication can slow down the removal of other medications from your body, which may affect how they work. An example is warfarin, among others.

Does Novilokast cause insomnia?

Neuropsychiatric adverse events, including insomnia and depression, have been reported in association with accolate therapy.

How long does it take for Novilokast to work?

It may take 1 to 2 weeks before you feel the full benefit of this medication. Inform your doctor if your condition (e.g., asthma symptoms, number of times you use your rescue inhaler) persists or worsens.

Can I crush Novilokast?

Brand comes as a pill and should be taken twice a day. If your child cannot swallow a pill, crush it between 2 spoons or inside a plastic bag or folded paper.

What are common side effects of Novilokast?

Common side effects may include:

  • nausea, diarrhea, stomach pain;
  • headache; or.
  • cold symptoms such as stuffy nose, sneezing, sore throat.


What does Novilokast do to the body?

Novilokast is used to prevent asthma symptoms.Novilokast is in a class of medications called leukotriene receptor antagonists (LTRAs). It works by blocking the action of certain natural substances that cause swelling and tightening of the airways.

Does Novilokast make me sleepy?

Headache, sore throat, trouble sleeping, malaise, and nausea may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Can I take Novilokast for a long time?

Long-term treatment with Novilokast was safe and well tolerated in asthmatic patients. Sustained efficacy and asthma control and good compliance were observed over extended treatment period. Results demonstrate long-term safety and effectiveness of and compliance with this anti-leukotriene agent.

Can I stop taking Novilokast?

Novilokast may help control asthma symptoms, but it does not cure asthma. Continue to take Novilokast even if you feel well. Do not stop taking Novilokast without talking to your doctor.

What is the mechanism of action of Novilokast?

Brand blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs and inflammation of the breathing passages.

Why was Novilokast discontinued?

Commercial reasons are cited for this decision and it is stressed that there were no safety concerns with this medicine.Brand is a leukotriene receptor antagonist and as such the closest available alternative is montelukast. Action: Clinicians should be aware of this product being discontinued.

Is Novilokast safe during pregnancy?

There is no proven risk in humans during pregnancy time.

Is Novilokast safe during breastfeeding?

If Novilokast is required by the mother, it is not a reason to discontinue breastfeeding. Because there is no published experience with Novilokast during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.

*** Taking medicines without doctor's advice can cause long-term problems.
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