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Tralokinumab
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Montelukast Sodium
Brand Name: Singulair
Generic Available
Common Dosage Forms:
Tablets, chewable: 4 mg, 5 mg
Tablets: 10 mg
Granules: 4 mg per foil packet
FDA Indications/Dosages:
For the prophylaxis and chronic treatment of asthma in adults and children 2 years of age and older: The dosage for adolescents and adults 15 years of age and older is one 10 mg tablet daily to be taken in the morning. The dosage for pediatric patients 6-14 years of age is one 5 mg tablet daily to be taken in the evening. The dosage for pediatric patients 2-5 years of age is one 4 mg tablet daily to be taken in the evening.
For the relief of symptoms of seasonal allergic rhinitis for adults and pediatric patients 6 months of age and older: The dosage for adolescents and adults 15 years of age and older is one 10 mg tablet daily. The dosage for pediatric patients 6-14 years of age is one 5 mg tablet daily. The dosage for pediatric patients 6 months to 5 years of age is 4 mg daily.
For the prevention of exercise-induced bronchoconstriction in patients 15 years of age and older: One 10 mg tablet daily taken at least 2 hours prior to exercise. Wait 24 hours before taking another dose.
Pharmacology/Pharmacokinetics: Asthma pathophysiology, including airway edema, bronchospasm, and altered cellular activity, has been correlated to the presence of cysteinyl leukotrienes (LTC4, LTD4, LTE4) in the lungs. Mast cells and eosinophils release cysteinyl leukotrienes upon metabolism of arachidonic acid where they bind to specific receptors (CysLT). Montelukast binds with high affinity and selectively to the CysLT1 receptor where it inhibits physiologic actions of LTD4 without any agonist activity. After an oral dose, peak plasma levels are reached in 2-4 hours and the mean plasma half-life ranges between 2.7-5.5 hours. Metabolism occurs via cytochromes P450, 3A4, and 2C9. Food does not alter the availability of an oral dose.
Drug Interactions: Phenobarbital may increase metabolism of montelukast. May decrease the metabolism (via inhibition of P450 2C8) of paclitaxel, rosiglitazone, and repaglinide.
Contraindications/Precautions: Montelukast is not indicated for reversal of bronchospasm in acute asthmatic attacks, including status asthmaticus. Do not replace oral or inhaled steroids with montelukast without tapering steroid dose. Montelukast for inhalation should not be used as monotherapy for exercise induced asthma. Rare cases of systemic eosinophilia have been documented during therapy usually after the reduction or stopping of oral corticosteroids. Use with caution in nursing mothers. Pregnancy Category B.
Adverse Effects: Adverse effects closely resemble those found with placebo and include headache (18%), influenza (4%), cough (3%), abdominal pain (3%), dyspepsia (2%), and dizziness (2%). Rare cases of psychiatric disorders including agitation, aggressive behavior, abnormal dreams, depression, and suicidal thinking have been reported.
Patient Consultation:
This medication should be taken regularly even when the patient is asymptomatic.
This is not intended to treat asthmatic attacks and patients should have appropriate measures at hand to treat attacks.
Phenylketonurics should be aware that chewable tablets contain phenylalanine.
If a dose is missed, take it as soon as possible and return to normal dosing schedule.
Store in a cool, dry place away from sunlight and children.
Contact a physician if the above side effects are severe or persistent.
Granules can be given either directly in the mouth or mixed with a spoonful of soft food (applesauce, carrots, rice, or ice cream).
Fluticasone Propionate with Salmeterol Xinafoate
Brand Name: Advair
Generic Available
Common Dosage Forms:
Advair Diskus 100/50, 250/50, 500/50: Each dose contains 50 mcg salmeterol (as 72.5 mcg salmeterol xinafoate) and either 100, 250, or 500 mcg of microfine fluticasone propionate.
Advair HFA 45/21, 115/21, 230/21: Each dose contains 21 mcg salmeterol (as 30.45 mcg salmeterol xinafoate) and either 45, 115, or 230 mcg of fluticasone propionate.
FDA Interactions/Dosages:
For the long-term maintenance treatment of asthma (in patients 4 years of age and older for Advair Diskus and 12 years and older for Advair HFA): One diskus inhalation or 2 HFA inhalations twice daily, approximately 12 hours apart.
For the maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis: One inhalation of Advair 250/50 twice daily (morning and evening).
For patients who are not currently on an inhaled corticosteroid, whose disease severity warrants treatment with 2 maintenance therapies, including patients on non-corticosteroid maintenance therapy: The recommended starting dose is Advair Diskus 100/50 twice daily.
For patients on an inhaled corticosteroid, the recommended starting dose depends on the current corticosteroid and the current daily dose.
Monitor: BMD, IOP, FEV
Pharmacology/Pharmacokinetics: Fluticasone propionate is a synthetic, triflurinated corticosteroid. Corticosteroids bind to certain receptor proteins found in the cytoplasm of sensitive cells to form a steroid-receptor complex. This steroid-receptor complex enters the nucleus of the cell where it reacts with chromatin, or DNA. The steroid, or possibly the receptor, then uses stored information to stimulate, or in some cases inhibit, the transcription of mRNA. The stimulation of mRNA results in the synthesis of specific proteins and ultimately specific enzymes that carry out its anti-allergy and anti-inflammatory actions. Fluticasone propionate’s glucocorticoid receptor agonist affinity is 18 times greater than dexamethasone and twice that of beclomethasone. Salmeterol stimulates adenyl cyclase, the enzyme which catalyzes the formation of cAMP (cyclic 3′5′ adenosine monophosphate) from ATP (adenosine triphosphate). Increased cAMP is associated with relaxation of bronchial, uterine, and vascular smooth muscle through stimulation of beta-2-adrenergic receptors. In addition, increased cAMP levels inhibit the release of mediators of immediate hypersensitivity from cells, especially from mast cells. Onset of action occurs in 20 minutes with a duration of action of 12 hours.
Drug Interactions: Additive effects occur with systemic corticosteroids. Other sympathomimetics, tricyclic antidepressants, and monoamine oxidase inhibitors may increase the toxicity of this medication. Beta-blockers may decrease the effectiveness of salmeterol.
Contraindications/Precautions: Use is contraindicated in the primary treatment of status asthmaticus. LONG-ACTING BETA-2-ADRENERGIC AGONISTS INCREASE THE RISK OF ASTHMA-RELATED DEATH. Use caution in patients who are being transferred from systemic corticosteroids to Advair because deaths due to adrenal insufficiency have occurred during and after transfer to aerosolized steroids. Systemic steroids should be administered to these patients during periods of stress or during an acute asthmatic attack. Advair is not to be regarded as a bronchodilator and should not be given for rapid relief of bronchospasm. Secondary fungal infections of the oral cavity may occur and may require antifungal treatment. Response of the hypothalamic-pituitary-adrenal (HPA) function is highly individualized. Use caution in patients with cardiovascular disorders, hypertension, hyperthyroidism, diabetes mellitus, in nursing mothers, or pregnancy. Pregnancy Category C.
Adverse Effects: Adverse effects are usually mild to moderate in severity and include upper respiratory tract infection, pharyngitis, headache, nausea or vomiting, sinusitis, bronchitis, cough, RASH, and ANGIOEDEMA.
Patient Consultation:
Avoid contact with the eyes.
Rinse mouth after each use.
Contact a physician if the above side effects are severe or persistent.
Contact a physician if symptoms worsen or if the effectiveness of short-acting beta-2-agonists decrease.
If a dose is missed, skip it and return to normal dosing schedule.
Not intended to provide immediate relief of bronchospasm.
To receive the full benefits of therapy, use on a regular basis. Although benefits can be seen after 2 days of treatment, up to 4 weeks may be needed to observe benefits.
It is important that the patient understands how to use the Diskus device and the HFA inhaler appropriately.
Fluticasone Propionate (Inhalation)
Brand Name: Flovent
Common Dosage Forms:
Inhalation Aerosol in a Metered Dose Inhaler (MDI): Each canister contains a microcrystalline suspension of fluticasone propionate. Each actuation releases either 44 mcg (Flovent 44), 110 mcg (Flovent 110), or 220 (Flovent 220) from the actuator. Flovent 44 contains 60 actuations and Flovent 110 and Flovent 220 contain 120 actuation.
Diskus: Each inhalation delivers wither 50 mcg, 100 mcg, or 250 mcg.
FDA Indications/Precautions:
For the maintenance treatment of asthma as prophylactic therapy: For the MDI, start with 2 puffs of the 44 mcg inhaler twice a day. For the diskus, start with one inhalation of the 50 mcg inhaler. Normal dose is two puffs of the 110 or 220 MDI twice a day or one inhalation of the 100 or 250 mcg Diskus twice a day. The highest recommended dose is 440 mcg of the MDI given twice a day.
In children ages 4 to 11: Start with 44 mcg twice a day. The highest recommended dose in this population is 110 mcg twice a day.
Patients receiving systemic steroids: The patient’s asthma should be reasonably stable before treatment is started. After approximately one week, gradual withdrawal of the systemic steroid is started by reducing the daily dose. Subsequent reductions should be tried no sooner than every 1-2 weeks. These decrements should not exceed 2.5 mg prednisone or its equivalent. During periods of stress or a severe asthma attack, transfer patients will require supplementary treatment with systemic steroids.
Monitor: FEV, IOP, BMD
Pharmacology/Pharmacokinetics: Adrenocorticoids bind to certain receptor proteins found in the cytoplasm of sensitive cells to form a steroid-receptor complex. This steroid-receptor complex enters the nucleus of the cell where it reacts to chromatin, or DNA. The steroid (or possibly the receptor) then uses stored information to stimulate, or in some cases inhibit, the transcription the mRNA. The stimulation of mRNA results in the synthesis of specific proteins and ultimately specific enzymes that carry out its anti-allergy and anti-inflammatory actions. Fluticasone propionate’s glucocorticoid receptor agonist affinity is 18 times greater than dexamethasone and twice that of beclomethasone.
Drug Interactions: Additive effects occur with systemic corticosteroids.
Contraindications/Precautions: Use is contraindicated in the primary treatment of status asthmaticus. Use with caution in patients who are being transferred from systemic corticosteroids to this drug because deaths due to adrenal insufficiency have occurred during and after treatments to aerosolized steroids. Systemic steroids should be administered to these patients during periods of stress or during an acute asthmatic attack. This is not to be regarded as a bronchodilator and should not be given for rapid relief of bronchospasm. Secondary fungal infections of the oral cavity may occur and may require antifungal treatment. Response of the hypothalamic-pituitary-adrenal (HPA) function is highly individualized. Use with extreme caution during pregnancy. Pregnancy Category C.
Adverse Effects: Pharyngitis, nasal congestion, and upper respiratory infection.
Patient Consultation:
Avoid contact with the eyes.
Contact a physician if the above side effects are severe or persistent.
If a dose is missed, skip it and return to normal dosing schedule.
No intended to provide immediate relief of bronchospasm. To receive the full benefits of therapy, use on a regular basis. Although benefits can be seen after 2 days of treatment, up to 4 weeks may needed to observe benefits.
Use any prescribed bronchodilator a few minutes prior to using.
Follow enclosed instructions for aerosol inhalation technique:
Shake the inhaler well and move into inhaler position,
Breathe out as fully as you comfortably can. Hold the inhaler upright, place mouthpiece in the mouth, close lips tightly around the mouthpiece,
While breathing in deeply in deeply, press down on the cartridge and hold your breath as long as you can while the inhaler is still in your mouth,
Take your finger off the cartridge, remove the mouthpiece from your mouth, and breathe out gently. Wait one minute between puffs and repeat steps 2-4 if indicated,
Rinse your mouth or gargle after the dose is complete,
Clean the inhaler at least once a day by removing the cartridge and rinsing the plastic case in warm running water. Dry the case and replace the cartridge, and
Discard the inhaler after the date calculated by your physician or pharmacist.
Budesonide
Brand Name: Pulmicort
Common Dosage Forms:
Suspension for Inhalation: Each Respule (vial) contains 2 mL of sterile liquid budesonide suspension in either a 0.25 mg, 0.5 mg, or 1 mg strength. Supplied in foil envelopes each containing five Respules with 30 Respules per carton.
Metered Dose Inhaler (Flexhaler): 90 mcg (80 mcg budesonide) per actuation or 180 mcg (160 mcg budesonide) per actuation.
FDA Indications/Dosages:
For the maintenance treatment of asthma and as prophylactic therapy in children 12 months to 8 years of age: Respules should be administered via jet nebulizer. In patients currently taking bronchodilators alone, start with 0.5 mcg once or twice a day (max of 0.5 mg per day). In patients taking inhaled corticosteroids, start with 0.5 mg once or twice a day (max of 1 mg per day). In patients taking oral corticosteroids, start with 1 mg daily, given in one or two divided doses (max 1 mg per day).
For the maintenance treatment of asthma and as prophylactic therapy in adults and pediatric patients 6 years of age or older: Use the Flexhaler as directed. The recommended starting dose is 180 mcg (children) or 360 mcg (adults) twice a day. The maximum dosage should not exceed 360 mcg (children) or 720 mcg (adults) twice a day. A slow withdrawal of oral corticosteroids should be made after the patient is maintained on inhaled Pulmicort. *In patients with mild to moderate asthma who are well controlled on inhaled corticosteroids, once a day dose may be considered.
Monitor: FEV, BMD, IOP.
Pharmacology/Pharmacokinetics: Adrenocorticoids bind to certain receptor proteins found in the cytoplasm of sensitive cells to form a steroid-receptor complex. This steroid-receptor complex enters the nucleus of the cell where it reacts with chromatin, or DNA. The steroid (or possibly the receptor) then uses stored information to stimulate, or in some cases inhibit, the transcription of mRNA. The stimulation of mRNA results in the synthesis of specific proteins and ultimately specific proteins enzymes that carry out its anti-allergy and anti-inflammatory actions. Budesonide has strong glucocorticoid and weak mineralocorticoid activity. ALmost all of an inhaled dose is absorbed systemically with peak plasma concentrations occurring within 30 minutes of an inhaled dose. Metabolism occurs via cytochrome P450 3A to inactive metabolism.
Drug Interactions: Ketoconazole may increase plasma levels.
Contraindications/Precautions: Use is contraindicated in the primary treatment of status asthmaticus. LONG-ACTING BETA-2-ADRENERGIC AGONISTS INCREASE THE RISK OF ASTHMA-RELATED DEATH. Use in caution in patients who are being transferred from systemic corticosteroids to Pulmicort because deaths due to adrenal insufficiency have occurred during and after transfer to aerosolized steroids. Systemic steroids should be administered to these patients during periods of stress or during an acute asthma attack. Pulmicort is not to be regarded as a bronchodilator and should not be given for rapid relief of bronchospasm. Secondary fungal infections of the oral cavity may occur and may require antifungal treatment. Response of the hypothalamic-pituitary-adrenal (HPA) function is highly individualized. Pregnancy Category B.
Adverse Effects: Adverse effects with the Turbohaler include headache, asthenia, pain, dyspepsia, nausea, oral candidiasis, arthralgia, cough, respiratory infection, rhinitis, and sinusitis. Adverse effects from Respules include respiratory infection, rhinitis, cough, otitis media, vomiting, diarrhea, abdominal pain, and rash.
Patient Consultation:
Avoid contact with the eyes.
Contact a physician if the above side effects are severe or persistent.
If a dose is missed, skip it and return to normal dosing schedule.
Pulmicort is not intended to provide immediate relief of bronchospasm. To receive the full benefits of therapy, use on a regular basis. Although benefits can be seen after 2 days of treatment, up to four weeks may be needed to observe benefits.
Use any prescribed bronchodilators a few minutes prior to using Pulmicort.
Follow enclosed instructions for inhalation technique of the Turbohaler: (1) prime the inhaler the first time it is used by holding it in an upright position (mouthpiece up), turn the brown grip fully to the right and then to the left until it clicks, (2) to load a dose, hold it in an upright position (mouthpiece up), turn the brown grip fully to the right and then to the left until it clicks, and (3) Hold the Turbohaler in the upright or horizontal position, place the mouthpiece between the lips and inhale forcefully and deeply. Exhale through the nose and do not shake in inhaler.
The Respules should be gently shaken before use in an approved jet nebulizer and should not be mixed with other solutions.
Rise the mouth out without swallowing after each use.
A red mark will appear in the indicator window when there is 20 or fewer doses left in the Turbohaler.
Patients should avoid exposure to chickenpox or measles and if they are exposed promptly notify their physician.
Pulmicort Turbohaler should not be used with a spacer.
TABLETING AND COMPACTION PROPERTIES OF ANOGEISSUS LEIOCARPUS AND PROSOPIS AFRICAN A EXTRACT SCREENED AS AN ANTIASTHMATIC.
TABLETING AND COMPACTION PROPERTIES OF ANOGEISSUS LEIOCARPUS AND PROSOPIS AFRICAN A EXTRACT SCREENED AS AN ANTIASTHMATIC.
TABLETING AND COMPACTION PROPERTIES OF ANOGEISSUS LEIOCARPUS AND PROSOPIS AFRICAN A EXTRACT SCREENED AS AN ANTIASTHMATIC.
Abstract:
Anogeissus leiocarpus and Prosopis africana are popular herbal antiasthmatic drugs used in Northern Nigeria. However there is always the problem of standardisation. This can be over come by formulating the plant extract into a pharmaceutical dosage form. Tablets…
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