Asthma Flashcards
Class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Counseling on a Dry Powder Inhaler
Counseling on a Meter Dosed Inhaler
Asthma
Background:
- is a disease that affects the airways (bronchi) of the lungs.
- two different processes are going on:
1) Inflammation
- a thickening of the lining of the airway
- so, the diameter of the airway is much smaller due to the inflammation.
- making it harder to breath
2) Bronchoconstriction
- narrowing of the airway is called bronchoconstriction
The inflammation AND bronchoconstriction cause airflow obstruction, which results in expiratory airflow limitation (difficulty with exhalation).
Classic symptoms:
- wheezing
- breathlessness
- chest tightness
- cough
———————————————————————————————————————- characterized by chronic airway inflammation and bronchoconstriction (narrowed airways).
Asthma Diagnosis and Assessment:
- an asthma diagnosis is confirmed with Spirometry * and pulmonary function tests.
- this is going to test your lung function with a couple different parameters, to see how well you are able to exhale and exhale over time.
- ## these should be measured at baseline and after use of a short acting bronchodilator to test for reversibility.Spirometry: Tests Lung Function (How Well The Longs Work)
FEV1:_________________
FVC:___________________
FEV1/FVC:______________
FEV1 [Forced Expiratory Volume 1 second]: How much air can be forcefully exhaled in one second.
FVC [Forced Vital Capacity]: The maximum volume of air that is exhaled after taking a deep breath.
FEV1/FVC: The percentage of total air capacity (vital capacity) that can be forcefully exhaled in 1 second from the lungs.
—————————————————————————————————————————————————————————————————————————————-Specifically, when you run this Spirometry test
- you measure FEV1
- then give a bronchodilator (albuterol) to patient
- measure FEV1 again (assessing for reversibility)
- **If FEV1increases greater than > 12%, Symptoms are reversible with bronchodilator medication*
Diagnosis of Asthma confirmed.
- genetics
- pollution
- cigarettes
- cold air/changes in weather
- pets
- dust, pollen, cockroaches
- perfume & cosmetics
- drugs, aspirin, NSAIDs,
- non-selective beta-blockers:
Comorbid conditions that can worsen asthma or trigger an exacerbation:
——————————————————————————————————————– Infections (Colds and Viruses), Allergic Rhinitis, GERD, Obesity, Obstructive Sleep Apnea, Anxiety, Stress and Depression
Nonmodifiable:
- genetics
- pollution
- weather- can’t control but limit exposure
————————
Modifiable:
Classification of Asthma Severity-
1) Intermittent (comes and goes): less than or equal to 2 times a week]
2) Persistent (a more chronic form of asthma where they have symptoms everyday)
- How do we determine what category a patient falls into? There are a lot of characteristics.
Includes:
Rescue Inhaler Use**
[Persistent Categories] - If patient is using inhaler more than 2 times per week, then is in one of these categories**
- - Mild:
- - Moderate:
- - Severe:
Daytime symptoms:
Nighttime awakenings:
**Rescue inhaler use:
*Intermittent: less than or equal to 2 days/week of use of rescue inhaler.
*MILD- greater than 2 days per week, BUT NOT daily or greater than 1x / day
*MODERATE- daily
*SEVERE- Several times per day
Activity limitations:
Lung function FEV1 (%predicted) & FEV1/FVC*:
exacerbations requiring oral systemic steroids:
Why do we do this?
It is going to help us understand the patient and Guide the level of treatment the patient needs.
So if a patient is classified as having Intermittent asthma, then we are going to start in the algorithm at an earlier step in the process.
Treatment Principles:
General Approach
Controlling risk Factors
——————————————————————————————————
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-
-
-
-
-
-
Diagnosis
- symptom control and risk factors (including lung function)
- Inhaler technique and adherence
- patient preference
Asthma medications
- non-pharmacological strategies
- treat modifiable risk factors
Symptoms
Exacerbations
Side-effects
Patient Satisfaction
Lung Function
Drug Treatment:
Inhaled delivery preferred.
[Rescue Drugs (Relievers)]**
—————————————————————————————————————-
1)
2)
3)
4)
Relievers or rescue inhalers, rapidly open airways within minutes of inhalation to treat acute symptoms (they make breathing easier).
1) Low-dose ICS + formoterol (LABA) [preferred*]
2) (SABAs)- Short-acting beta-2 agonist- - - [no longer 1st line]
3) systemic steroids (injection or oral)
- more for an exacerbation or someone with very advanced asthma
4) (SAMA)- Inhaled short acting muscarinic antagonist
[also called Anticholinergics]
- not very common
- would be for add on therapy or during an exacerbation if not getting the control we need with a rescue inhaler
Reliever or rescue inhalers:
- patients use these when they are having symptoms or getting into an exacerbation
- these are quick acting medications
- they rapidly open airways within minutes of inhalation to treat acute symptoms
- they make breathing easier
we want a medication to help control inflammation.
Low-dose ICS + formoterol is the preferred rescue medication in patients with asthma.
Controllers (Maintenance drugs)
- these are used daily to help control symptoms more long term.
- they reduce inflammation and help maintain asthma control
- ICS are the mainstay of treatment
Drug Treatment:
Maintenance Drugs (Controllers): Taken DAILY
- to help prevent a worsening or control symptoms long term**
—————————————————————————————————————–
1)
2)
—————————————————————————————————————-
3)
4)
5)
6)
1) Inhaled Corticosteroids (ICS)**
**- First Line for all patients
**- most effective anti-inflammatory
—————————————————————————————————————
2) Long-Acting Beta-2 Agonists (LABA)
**- Never would use by itself [for ASTHMA]
**- used by themselves, we see increased risk of death if NOT combined with an ICS to decrease the inflammation.
**- bronchodilators: there going to allow the airway to open
- They can be used ALONE in COPD
——————————————————————————————————————
[These are going to be ADD on therapies a little later down in the process or alternative treatments for special situations]
3) Leukotriene receptor Antagonists (LTRAs)
4) Theophylline
5) Inhaled Long-Acting Muscarinic Antagonists (LAMA)
aka also called Anticholinergics.
**- only one we use in ASTHMA
-Spiriva Respimat
6) Monoclonal antibodies
Asthma Treatment Algorithm:
**Each patient with Asthma:
- needs a Reliever medication. They need that Acute medication for when they have symptoms.
- Low-dose ICS + formoterol combination (preferred reliver medication)
OR
- Low-dose ICS
“One of these options has to be present so that the patient can have a treatment for when they have symptoms acutely.”
Asthma Treatment Algorithm:
After Initial Step, now we are looking to see if patients asthma is controlled?
remember- we are looking at patients Rescue Inhaler Use to help Guide us.
If Well controlled? ————> Maintain current treatment
[Low-dose ICS + formoterol] options:
- Symbicort
- Dulera
[Low-dose ICS] options: [Low dose ICS strength]
-
- (QVAR RediHaler) beclomethasone [100-200mcg daily]
breath-actuated inhalation aerosol
40 or 80 mcg/inhaler
- (Pulmicort Flexhaler) budesonide [200-400mcg daily]
DPI- dry powder inhaler
90 or 180mcg/inhaler - (Flovent HFA) fluticasone [100-250 mcg]
MDI- meter dose inhaler
44/110/220mcg inhaler - (Flovent Diskus) fluticasone [100-250 mcg]
DPI - dry powder inhaler
50/100/250mcg inhaler - (Arnuity Ellipta) fluticasone [100-250 mcg]
DPI - dry powder inhaler
50/100/200mcg inhaler - (ArmonAir Digihaler) fluticasone [ 55mcg]
-inhalation powder - 55/113/232mcg inhaler
- (Alvesco) ciclesonide [80-160mcg]
MDI- meter dose inhaler
80/160mcg inhalers - (Asmanex HFA) mometasone [200-400mcg]
MDI- meter dose inhaler
50/100/200mcg inhalers - (Asmanex Twisthaler) mometasone [110-220mcg]
DPI- dry powder inhaler
110/220mcg inhaler
Asthma Treatment Algorithm:
After Initial Step, now we are looking to see if patients asthma is controlled?
remember- we are looking at patients Rescue Inhaler Use to help Guide us.
If Not well controlled—————–> Step up 1 step
- Symptom/rescue inhaler use:
Rescue inhaler use is > greater than 2 days of the week
[patient NOT well controlled]
—————————————————————————————- - night awakenings 1-3 times/week
- some limitations to normal activity
Asthma Treatment Algorithm:
After Initial Step, now we are looking to see if patients asthma is controlled?
remember- we are looking at patients Rescue Inhaler Use to help Guide us.
If Poorly controlled———————> step up 1-2 steps (consider short course of oral steroids)
Asthma Treatment Algorithm:
remember- we are looking at patients Rescue Inhaler Use to help Guide us.
- Symptom/rescue inhaler use:
- Uses Rescue inhaler less than or equal to 2 days/week**
Step 1 (Intermittent Asthma):
- asthma that comes and goes.
- if you have intermittent asthma, this is when you can use a RELIEVER (rescue medication) by itself.
Remember- in general, First line is an ICS. So we are looking to see if patient has this first. If someone is not well controlled on ICS, then we can either increase dose on ICS or add on LABA.
For someone with intermittent asthma we would want to have them on an
1) PRN low-dose ICS + formoterol [preferred]
- Symbicort
- Dulera
OR
2) [low-dose ICS + SABA]
Asthma Treatment Algorithm:
remember- we are looking at patients Rescue Inhaler Use to help Guide us.
- Symptom/rescue inhaler use:
- Uses rescue inhaler greater than > 2 days per week but not daily OR greater than 1 time per day. **
Step 2 (Mild persistent Asthma)
For someone with Mild Persistent Asthma, we would want to treat them daily with something now.
[Controller/Maintenance]
1) Low-dose ICS daily
OR
2) Low-dose ICS + formoterol PRN
Asthma Treatment Algorithm:
remember- we are looking at patients Rescue Inhaler Use to help Guide us.
- Symptom/rescue inhaler use:
- Uses rescue inhaler daily**
Step 3 (Moderate persistent Asthma)
For someone with Moderate Persistent Asthma, we would want them on a daily
Low dose inhaled ICS + LABA.
Asthma Treatment Algorithm:
remember- we are looking at patients Rescue Inhaler Use to help Guide us.
- Symptom/rescue inhaler use:
- Uses rescue inhaler several times per day.**
Step 4 (Severe persistent Asthma)
For someone with Severe Persistent Asthma, we would want them on a
Medium-dose ICS + LABA
Asthma Treatment Algorithm:
remember- we are looking at patients Rescue Inhaler Use to help Guide us.
- Symptom/rescue inhaler use:
Step 5 (Severe persistent Asthma)
High-dose ICS + LABA
Beta-2 Agonists:
- these medications bind to the Beta-2 receptors, causing relaxation of bronchial smooth muscle, which leads to bronchodilation.
- NOT FOR MONOTHERAPY
- Should only be used in combination with ICS (either taken as needed or with ICS or daily)
PO formulations are available but NOT RECOMMENDED.
Beta-2 Agonists:
- (SABAs) Short Acting Beta-2 Agonists:
- includes: (albuterol, levalbuterol)
- PRN as needed only, NOT RECOMMENDED to use SABA alone**
- 200 inhalations/canister
- ## levalbuterol is R-isomer of albuterol
- 90 mcg/inhalation (albuterol)
- ## 45 mcg/inhalation (levalbuterol)Primatene Mist - OTC epinephrine - is a SABA.
[Asthmanefrin] - FDA approved for mild symptoms in intermittent asthma only.
- SIDE EFFCTS: nervousness/tremor, tachycardia, palpitations, cough, increased blood glucose, decreased potassium
ProAir RespiClick - dry powder inhaler albuterol
ProAir HFA - meter dosed inhaler albuterol
Ventolin HFA - meter dosed inhalers albuterol
- also comes in 60 inhalations per canister
Proventil HFA - meter dosed inhalers albuterol
ProAir Digihaler -
Xopenex-
Xopenex Concentrate-
Xopenex HFA-
**MDI/DRI: 1-2 inhalations every 4-6 hours as needed
- Shake well before use (HFA products) MDIs
Counseling points:
Beta-2 Agonists:
LABA Long-Acting Beta-2 Agonists:
-includes: [formoterol, salmeterol]
- are used as part of rescue therapy (e.g. ICS + formoterol) OR as maintenance therapy beginning in Step 3 of treatment with the ICS.
- BOXED WARNING: Increased risk of asthma related death when used as monotherapy
- ONLY USE AS ADD ON to ICS therapy
- NOT FOR MONOTHERAPY
- Formoterol used for rescue WITH ICS [Symbicort, Dulera]
- SIDE EFFCTS: nervousness/tremor, tachycardia, palpitations, cough, increased blood glucose, decreased potassium
(Serevent Diskus) - salmeterol- DPI: 1 inhalation BID
- 50mcg/inhalation
-Is the only single product FDA approved for Asthma - REMEMBER we would NEVER want to use MONOTHERAPY, NEEDS to be in combination with ICS**
- Maintenance inhaler only; not for acute bronchospasms
BOXED WARNING: INCREASED RISK OF ASTHMA RELATED DEATHS; Should only be used in asthma patients who are currently receiving but are not adequately controlled on an inhaled corticosteroid.
- Increased risk of asthma-related hospitalizations in pediatric and adolescent patients
Inhaled Corticosteroids:
- First line therapy for Persistent Asthma for all patients, even children
- Low, Medium, High
- Used PRN with formoterol or SABA for rescue
Warning: adrenal suppression with prolonged use of High doses —-> growth retardation in children.
Side effects: dysphonia (difficulty speaking), oral candidiasis (thrush), cough, increased blood glucose
oral thrush, whitish plaques on the tongue and on the mouth.
Whenever we use a steroid have to rinse your mouth and spit it out.
Inhaled Corticosteroids:
Contraindications:
Warnings:
Side effects:
Monitoring:
Notes:
Contraindications:
- primary treatment of status asthmaticus or acute episodes of asthma.
Warnings:
- High doses for prolonged periods of time can cause adrenal suppression, *Increased risk of fractures, growth retardation (in children) and immunosuppression.
Side effects:
- dysphonia (difficulty speaking), oral candidiasis (thrush), cough, headache, hoarseness, URTIs, hyperglycemia
Monitoring:
Use of SABA/rescue inhaler, symptoms frequency, peak flow; growth (children/adolescents), s/sx adrenal insufficiency; s/sx of thrush; bone mineral density
- ## Rinse mouth with water and spit out after each use to prevent thrush; can use a spacer device with an MDI to decrease risk.
- ## Alvesco: MDI that does not need to be shaken before use
- ## Budesonide: only ICS available as a nebulized solution; used commonly in young children
- ## Pulmicort Respules: only use with a jet nebulizer connected to an air compressor; Do Not Use an ultrasonic nebulizer.
- ## QVAR RediHaler: breath-activated aerosol with characteristics of a DPI and MDI; DO NOT SHAKE or use with a spacer; Does Not Need priming or activation.
- Aron Air and AirDuo Digihalers: contain a built-in electronic module that detects, records and stores data (detects when the inhaler is used and measures inspiratory flow).
Inhaled Corticosteroids:
No
LAMA/LABA
or
LAMA/LABA/ICS combinations FDA approved for asthma.
(QVAR RediHaler) beclomethasone: MDI 1-4 inhalations BID
40, 80 mcg/inhalation
(Pulmicort Flexhaler) budesonide: DPI 1-4 inhalations BID
90, 180 mcg/inhalation
(Pulmicort Respules)budesonide nebulizer suspension:
0.25-0.5 md daily or BID in children aged 1-8 years.
———————————————
(Flovent HFA) fluticasone: MDI 2 inhalations BID
44, 110, 220 mcg/inhalation
(Flovent Diskus) fluticasone: DPI 1-2 inhalations BID
50, 100, 250 mcg/inhalation
(Arnuity Ellipta) fluticasone: DPI 1-2 inhalations daily
100, 200 mcg/inhalation
(ArmonAir Digihaler) fluticasone: DPI 1 inhalation BID
55, 113, 232 mcg/inhalation
——————————————————————————————————————
(Asmanex HFA) mometasone: MDI 1-2 inhalations BID
100, 200 mcg/inhalation
(Asmanex) mometasone: DPI 1-2 inhalations daily
110, 220 mcg/inhalation
——————————————————————————————————————-
(Alvesco) ciclesonide: MDI 1-2 inhalations BID
80, 160 mcg/inhalation
——————————————————————————————————————–
(Symbicort): budesonide + formoterol
(Dulera): mometasone + formoterol
————————————————————————————————–
(Advair Diskus): fluticasone + salmeterol [NOT for RESCUE]
(Advair HFA): fluticasone + salmeterol [NOT for RESCUE]
(AirDuo Digihaler): fluticasone + salmeterol DPI [NOT for RESCUE]
(AirDuo RespiClick): fluticasone + salmeterol MDPI [NOT for RESCUE]
(Wixela Inhub): fluticasone + salmeterol DPI
(Breo Ellipta): fluticasone + vilanterol [NOT for RESCUE]
** the onset of LABA is longer and so would NOT be appropriate for short acting use**
Recognizing & Understanding inhaled delivery devices
MDIs - meter dosed inhaler
*[How you know which type of device you are dealing with is the SECOND 2nd part of the name]
————————————————————————————————————
- (Brand name identifiers): HFA, Respimat or no suffix (e.g. Alvesco)
-
- Deliver aerosolized liquid medication
- some use propellant (HFA)
-
- administration: slow, deep inhalation while pressing canister
- SPACER CAN BE USED (to increase the time you have to breath in the medication), so when you press down, it releases the medication into a camber, and gives you more time to breath in the medication
-.
- shake well, remember it is a medication suspended in a liquid EXCEPT for
[QVAR RediHaler, Alvesco, Respimat products]
——————————————————————————————————————– have to press and breath in at the same time
- need to have hand-breath coordination
Recognizing & Understanding inhaled delivery devices
DPIs - dry powder inhaler
*[How you know which type of device you are dealing with is the SECOND 2nd part of the name]
—————————————————————————————————————–
- (Brand name identifiers): Diskus, Ellipta, Pressair, Handihaler, Neohaler, RespiClick, Flexhaler
-
- delivers fine powder medication
- no propellant
- administration: quick, forceful inhalation (nothing to press)
- CANNOT USE A SPACER (will be harder to inhale)
- Do NOT shake (powder will get spilled everywhere)
——————————————————————————————————————— NEED to have a FAST, FORCEFUL inhale to get it to the site of action.
- Do NOT want a slow deep breath. Want a fast sharp deep inhale.
- Don’t need to press anything, just need to forcefully get powder into lungs.
- Need to activate dose before you take it.
- Do NOT want to exhale into device, powder goes into the air everywhere, EXHALE AWAY FROM DEVICE.
- Do NOT want to TIP Device. Powder is a solid and will go all over the ground.
Inhaled Corticosteroids:
Recognizing & Understanding inhaled delivery devices
MDIs - meter dosed inhaler
*[How you know which type of device you are dealing with is the SECOND 2nd part of the name]
- (Brand name identifiers): HFA, Respimat or no suffix (e.g. Alvesco)
——————————————————————————————————————– - - - - - ** Counseling Points**:
- ## if someone struggles to do a Deep Fast Inhale and needs more time, then maybe a MDI is a better choice
Inhaled Corticosteroids:
Recognizing & Understanding inhaled delivery devices
DPIs - dry powder inhaler
*[How you know which type of device you are dealing with is the SECOND 2nd part of the name]
- (Brand name identifiers): Diskus, Ellipta, Pressair, Handihaler, Neohaler, RespiClick, Flexhaler
——————————————————————————————————————-
- - - - - - ** Counseling Points**:
- ## if you geta case and the patient has (RA) rheumatoid arthritis and patient has difficulty using hands, think about what inhaler would be better for them. It would be hard for them to press on a canister and breath in at same time. Might be easier to use a DPI where it is just the force of the inhale that they need.
LAMA
(Spiriva Respimat) tiotropium
Leukotriene Modifying Agents:
- (Singulair) montelukast:
- age 1 year old and older
- take in the evening
- neuropsychiatric events
- Granules: instructions for use
- (Accolate) zafirlukast:
- (Zyflo) zileuton:
- Not first line treatment
- add on adjunctive therapy or alternative for special situations
- leukotrienes are mediators of airway inflammation
- leukotriene receptor antagonists (LTRAs) reduce airway edema, constriction and inflammation.
(Singulair)
Class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
montelukast
Class: Leukotriene receptor Antagonists (LTRA)
- approved in Allergic Rhinitis
- exercise-Induced Bronchoconstriction (EIB)
MOA: drug works at receptor (LTD4) leukotriene D4 receptor and inhibits it.
Dosage forms: tablet. chewable, packet (granules).
Dosing: daily
10mg by mouth daily in the evening
Age 1-5 years: 4mg daily in the evening
Age 6-14 years: 5mg daily in the evening
EIB:
- Age 6-14 years old: 5mg daily
- Age 15 years old or older: 10mg 2 hours before exercise
Max dose:
Boxed Warnings:
** Neuropsychiatric events (e.g. serious behavior and mood-related changes, including suicidal thoughts or actions).
Warnings:
*Neuropsychiatric events: monitor for signs of aggressive behavior, hostility, agitation, hallucinations, depression, suicidal thinking.
Systemic eosinophilia, sometimes presenting with features of vasculitis consistent with Churg-Strauss syndrome (rare).
Side Effects:
headache, dizziness, abdominal pain, increased LFTs, URTIs
Monitoring:
mood and behavior changes (montellukast)
Pearls/Notes:
- comes in kid friendly formulations
- Remember: Granules can ONLY be mixed in certain things.
- **Granules can be administered DIRECTLY IN THE MOUTH, dissolved in a small amount (5mL) of BREASTMILK OR FORMULA or mixed with a spoonful of APPLESAUCE, CARROTS, RICE, ICECREAM (Do NOT mix with anything else); Use within 15 minutes of opening the packet. **
Drug-Drug/Food interactions:
(Accolate)
Class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
zafirlukast
Class: Leukotriene receptor Antagonists (LTRA)
Indications:
MOA: drug works at receptors (LTD4 and LTD5) and inhibits it.
Dosage forms:
Dosing: BID
20mg BID
Age 5-11: 10mg BID
Take 1 hour before or 2 hours after meals (empty stomach)
Max dose:
Contraindications:
** Hepatic Impairment**
Warnings:
Side Effects:
headache, dizziness, abdominal pain, increased LFTs, URTIs
Monitoring:
LFTs
Pearls/Notes:
- PROTECT from moisture and light; DISPENSE IN ORIGINAL CONTAINER
- Is a major substrate of CYP2C9 AND it inhibits CYP2C9 (moderate)
Drug-Drug/Food interactions:
- can increase levels of theophylline and CYP2C9 substrates (e.g. warfarin)
-
- erythromycin and theophylline decrease levels of zafirlukast.
(Zyflo)
Class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
zileuton
Class: 5-lipoxygenase inhibitor
Indications:
MOA: drug inhibits leukotriene formation blocking their production, so works a little earlier in the process.
Dosage forms:
Dosing: QID
Zyflo: 600mg QID
ER tablet: 1200mg BID within one hour after morning and evening meals
Age less than 12 years < NOT recommended
Max dose:
Contraindications:
** Hepatic Impairment**
Warnings:
Side Effects:
headache, dizziness, abdominal pain, increased LFTs, URTIs
Monitoring:
LFTs
Pearls/Notes:
Drug-Drug/Food interactions:
Theophylline
- dosed using IBW (so if patient is normal weight or obese we USE IBW)
- IF TBW is less than < IBW, then use TBW
- ## side effects: Nausea, headache, tachycardia, insomnia, tremor/nervousness
- ## toxicity: arrhythmias, seizures
- ## **therapeutic range: 5-15 mcg/mL
- ## conversion to aminophylline and caffeine
- Many Drug Interactions:
thee-off-ah-linn
- narrow therapeutic index drug
- has a lot of side effects
- ## broken down into caffeine.so think about side effects of drinking too much coffee/caffeine.
Many drug interactions
- - - CYP1A2 and CYP3A4
- - - Michaelis-Menten Kinetics: (a saturable form of kinetics)
- saturable kinetics (1st order kinetics followed by zero-order kinetics)
- so at low doses can increase the dose ok but as you get close to therapeutic range, a small dose change can lead to a really high increase rate.
- so small changes can have a big impact
Theo-24
Class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
theophylline
Class:
Indications: Asthma- adjunct last line
MOA: blocks phosphodiesterase, causing an increase in cyclic adenosine monophosphate (cAMP) and release of epinephrine from adrenal medulla cells. This results in bronchodilation, but is also causes diuresis, CNS and cardiac stimulation and gastric acid secretion.
Dosage forms: ER capsule, ER tablet, elixir, oral solution, injection
Dosing:
Oral loading dose: 5mg/kg IBW (or TBW if < IBW)
Oral maintenance dose 300-600 mg daily
**Therapeutic range: 5-15 mcg/mL
Measure peak level at steady state, after 3 days or oral dosing.
Max dose:
Contraindications:
Warnings:
Can exacerbate cardiovascular arrhythmias, peptic ulcer disease and seizure disorders.
Side Effects:
Nausea, Vomiting, headache, insomnia, Increased heart rate, nervousness
-
**Toxicity: persistent vomiting, arrhythmias, seizures
Monitoring:
Theophylline levels, HR, CNS effects (insomnia, irritability), use of rescue inhaler
Pearls/Notes:
-** To Convert aminophylline to theophylline, multiply by 0.8
-** To convert theophylline to aminophylline, divide by 0.8
- Use of theophylline is Limited by decreased effectiveness, drug interactions and adverse effects.
- Active metabolites of theophylline are CAFFEINE and 3-methylxanthine
- Michaelis-Menten Kinetics [1st order kinetics followed by zero-order kinetics]
-
- major substrate of CYP1A2 & CYP3A4
- CYP1A2 inhibitors that increase levels of Theophylline: cimetidine, ciprofloxacin, fluvoxamine, propranolol, zileuton
- CYP3A4 inhibitors that increase theophylline levels: clarithromycin and erythromycin
- Other drugs that increase theophylline levels: zafirlukast, alcohol, allopurinol, disulfiram, estrogen-containing oral contraceptives, methotrexate
Drugs that decrease theophylline levels: carbamazepine, fosphenytoin, phenobarbital, phenytoin, primidone, rifampin, ritonavir
- Theophylline can decrease lithium levels (via increased renal excretion) and zafirlukast.
Elixophyllin
Class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
theophylline
Class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
Other Asthma Medications:
- Anticholinergics (inhaled muscarinic antagonists) *
tiotropium (Spiriva Respimat) for patients 6 years and older
-
———————————————————————————————————— - Monoclonal Antibodies (parenteral products)
omalizumab (Xolair) blocks IgE binding to the IgE receptors on mast cells
Boxed Warning: anaphylaxis - must be given in healthcare setting.
Indicated for moderate to severe allergic asthma. - ## only for ALLERGIC Type Asthma
- Interleukin receptor antagonists
Indicated for Severe asthma with an EOSINOPHILIC phenotype.
- - mepolizumab (Nucala): SC every 4 weeks
- reslizumab (Cinqair): IV every 4 weeks
- benralizumab (Fasenra): SC every 8 weeks
- duplimumab (Dupixent): SC every 2 weeks
- ## inhibit muscarinic cholinergic receptors and reduce the intrinsic vagal tone of the airway, leading to bronchodilation. Short-acting anticholinergics (e.g. ipratropium) are sometimes used in combination with SABAs in hospitalized patients experiencing an acute exacerbation.
- ** a long-acting anticholinergic, tiotropium (Spiriva Respimat), is FDA-approved for asthma in patients 6 years and older with a history of exacerbation despite ICS/LABA therapy.
Xolair
Class:
Indications:
MOA:
Dosage forms:
Dosing:
Max dose:
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
Drug-Drug/Food interactions:
omalizumab
Class: monoclonal antibody
Indications: moderate-severe Allergic Asthma in patients 6 years and older who have a positive skin test to a perennial aeroallergen and inadequate symptom control on strep 5 treatment.
MOA: antibody inhibits IgE binding to the Ige receptor on mast cells and basophils.
Dosage forms:
Dosing:
Administer SC every 2 or 4 weeks
Max dose:
Boxed Warning: Anaphylaxis- has occurred as early as after the first dose and has occurred beyond 1 year after beginning treatment; closely observe patients after administration and be prepared to manage anaphylaxis that can be life threatening.
Contraindications:
Warnings:
Side Effects:
Monitoring:
Pearls/Notes:
- every single dose has to be given in a healthcare setting, due to the risk of anaphylaxis.
Drug-Drug/Food interactions:
Special Situations:
Exercise-Induced Bronchospasm (EIB): prevent it
- - - rescue inhaler 5-15 minutes before exercise
Pregnancy: Keep Control
- down titration of medications NOT necessary
- rescue inhaler is a must
- preferred controllers: ICS (typically budesonide)
Patient Self-Management and Education:
Inhalers
- days supply
- general guidance
Nebulizers
- fine mist delivered via a mouthpiece or face mask
- **medications may need to be FURTHER DILUTED before being put in the device (0.5% albuterol solution)
- these are a great option for young patients or patients that are in an exacerbation and are really struggling to breath.
Spacers
- can improve coordination of MDI technique
- decrease thrush incidence
- allows a little more time to breath and helps get more medication into the lungs
Patient Self-Management and Education:
- if using a SABA, it would be best to use that medication first. It quickly opens up the airways and allows other medications to get to the site of action better.
- then would want to add on or take the LAMA or LABA
- Last inhaler patient would want to use in sequence would be the ICS
“if they are using sperate inhalers for each”
- ## patient should be waiting about 1 minute (60 seconds) between each inhale. So, they can get their full lung capacity and get the medication in as much as possible.
With
With a Spacer, More drug gets into the lungs.
- spacers are helpful for children and anyone that has difficulty with hand-breath coordination (e.g. pressing down on the inhaler while breathing in at the same time) with an MDI. Plus, spacers reduce the risk of thrush from inhaled corticosteroids.
Common spacers include:
Aerochamber, OptiHaler, OptiChamber
*Peak Flow Meters:
- are a tool for someone to use at home, to evaluate their symptoms and help recognize when they might be getting into trouble, to keep them out of the hospital, and keep them out of an exacerbation.
How do we use these devices?
So it is a device at home that patient will exhale into and it tells them, based on their personal PEFR, what zone they are in.
- these handheld devices measure the (PEFR) Peak Expiratory Flow Rate.
Personal Best (PB)- measured in office with Spirometry.
Red zone (less than < 50% PB) - - - DANGER- - - need to get help
Yellow zone (50-80% PB)
Green zone (greater than > 80% PB)
- Not for every patient with asthma
- for patients struggling to understand when they have symptoms
- ## also for those newly diagnosed that are not well controlled yet
- measure PEFR in the morning when patient wakes
- before asthma medications
- have to do it from standing
- from fully inflated lungs
- have to do 3 tests, and you take best of those 3
**This information goes into the patients Asthma Action Plan which is specific for every individual patient.
albuterol (MDI) meter dosed inhaler:
- has a metal canister which contains the medication
- plastic actuator (canister goes inside)
- dusk cap to protect the mouthpiece of inhaler from dust (remember dust is a trigger for asthma)
- whenever you take off the cap, you want to inspect mouthpiece.
- most have a suspended liquid with drug in it. So, prior to using each time for inhalation, you want to shake it up first for about 5 seconds.
- ## when you first get the product from a pharmacy, you need to prime device.
- requires good hand and breath coordination
- ## closed seal mouth technique-slow inhalation and press and continue inhalation.
- hold breath for about 10 seconds
- ## then slowly exhale
- there is a counter on the inhaler. With each inhalation it will count down.
- ## wait 60 seconds between inhalations
-
- may look like a traditional dose meter dose inhaler BUT its different
- taking off or opening the cap ACTIVATES the DOSE
- INSTRUCT patients NOT to keep opening and closing the cap. Can damage inhaler and waste a lot of doses.
- exhale away from device
- Do NOT shake device, will spill powder everywhere. Hold in a specific position.
- Quick FORCEFUL inhalation in
- Hold breath for up to 10 seconds then exhale
- - remember cannot be used with a spacer
no as much coordination needed as with the MDI
- to load dose, Twist the bottom in one direction until you here a click, then turn back in the opposite direction until you hear click again. Then the dose is ready.
- exhale away from device
- quick forceful inhalation
- rinse mouth with water after each use and spit out water to prevent thrush.
- remember cannot be used with a spacer
no as much coordination needed as with the MDI
- hold device flat like a hamburger
- device has a thumb grip
- once you push to the side you expose the mouth piece
- there is a lever that you push back to load the dose
- exhale away from device
- quick forceful inhale
- rinse mouth and spit out water after each use
- close after use using thumb grip
- remember cannot be used with a spacer
no as much coordination needed as with the MDI