Leukotriene Modifiers
Drug Examples (3) and Uses? NOT effective for?
- Montelukast, Zafirlukast, and Zileuton
- Use: Primarily to prevent and control asthma exacerbations
- NOT EFFECTIVE for acute attacks
- PREVENTION inflammation that causes asthma attacks
- Max effectiveness if med taken in evening
3 routes? Drug Examples?
1) Inhaled: Beclomethasone, Triamcinolone, Budesonide, Mometasone, Ciclesonide, Azelastine/fluticasone, and Fluticasone
2) Oral: Prednisolone and Prednisone
3) IV: Dexamethasone, Hydrocortisone, and Methylprednisolone
Long term systemic use can cause?
- Weight gain, Impaired wound healing, Swelling of the face (moon face), Hypertension, Buffalo hump (Fat behind neck), Personality changes, Hyperglycemia, Decreased immune response, Insomnia, Cataracts, Gastric ulcers, Hyperlipidemia, Stunted growth in children, and Osteoporosis
Example Drugs?
- Aminophylline, Theophylline, and Caffeine
Check ___ levels... ___ while taking this will decrease the half life of this drug
- Check Theophylline levels!!
- Smoking while taking Theophylline will decrease the half life
MOA?
- Leukotrienes are substances that are released from mast cells, eosinophils and basophils
- They can result in smooth muscle contraction of the airways, increased permeability of the vasculature, increased secretions and activation of other inflammatory mediators
Steroids MOA and Uses?
- Uses: Most effective agent for long term treatment and prevention of asthma exacerbation
- MOA: Inhibits production of cytokines, leukotrienes, and prostaglandins
Patients should NOT ___ systemic steroids ____! Why?
- Patients should NOT stop systemic steroids ABRUPTLY!
- This can cause adrenal insufficiency which can be fatal
Uses?
- Treats breathing disorders (asthma, COPD, bronchospasm, apnea of prematurity)
Avoid what drinks? and when do you take SR tablets
- Avoid food/drink with caffeine
- Sustained-release should be taken at night
- DO NOT crush, dissolve, or chew sustained- release
Side effects?
Inhaled Steroids are NOT for what?
- NOT FOR RESCUE
- Mainstay of therapy
Do you give with food?
Yes
- Give oral doses with food to minimize gastric distress
Has been used to treat neonatal ___ in the past, now ___ is the preferred choice
- Apnea
- Caffeine
Other teaching points?
- Monitor V/S and I/O
- Take after meals to avoid GI upset
- Slow position changes due to dizziness, especially in the elderly
- Check peak flow before treatment and periodically thereafter
Drug interactions (2)?
- Lots of drug interactions!
- Increased toxicity if used with warfarin or phenytoin!
Systemic Steroid?
- Systemic: Should be used for the SHORTEST period of time and at the LOWEST dose possible
- Many drug interactions with systemic steroids!
Cautious with who? Why?
- Cautious use with elderly AND with diabetics: will elevate blood sugars
- Caution pt about exposure to illness (steroids lower immune response)
Actions?
- Decreases airway reactivity and relaxes bronchial smooth muscles
- In non-reversible obstructive airway disease (like emphysema), it increases the sensitivity of the brain to CO2 and stimulates the respiratory drive
- Reduces fatigue of the diaphragm and improves cardiac ventricular function
What is the therapeutic index for Methylxanthine?
- Narrow therapeutic index: 5-15 mcg/m
- Toxicity likely to occur when the serum level is greater than 20 mcg/ml
All 3: Montelukast, Zafirlukast, and Zileuton in relation to the liver?
- Zileuton: Contraindicated with active liver disease
- Zafirlukast: Use with caution with impaired liver function
- Montelukast: Can elevate liver enzymes
SE: Oral and Inhaled?
- Inhaled: Mouth irritation, Oral candidiasis, Cough and Hoarseness
- Oral: Hyperglycemia, N/V, HA, Insomnia, and Growth suppression
Monitor what?
- Monitor growth in children; avoid prolonged use!
- Assess peak flow before therapy and then periodically thereafter
Side Effects?
- N/V/D, HA, Anxiety, Abd cramping, Epigastric Pain, Anorexia, Irritability, Restlessness, Insomnia, Dizziness, Tachycardia, Palpitations, and Arrhythmias
What are the signs of toxicity?
- Hyperglycemia, Metabolic acidosis, Nausea and vomiting, Seizures, Cardiac arrythmias, and Death