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Short-acting beta agonists (SABA) medication
Albuterol (ProAir, Ventolin, Proventil)
used 2x max
used as a rescue inhaler
Long-acting beta agonists (LABA) medication
Salmeterol (Serevent)
Formoterol (Foradil)
vilanterol
Anticholinergics
Ipratropium
Tiotropium
Leukotriene Modifiers
Montelukast (singulair)
prevent histamine and bronchospasm for people with asthma
Albuterol
Selective beta2 agonist with minor beta1 activity
Relaxes bronchial smooth muscle and decrease the obstruction
“Rescue inhaler” for bronchospasm
Used in addition to other medication to maintain bronchodilation
Beta Agonist Side Effects
tachycardia
palpations
CNS excitation effects (tremors, dizziness, skakiness, nervousness, and restlessness)
headache
increase blood sugar
can developer tolerance
be careful with HTN and CAD
Long-Acting Beta Agonists
Typically 12 hour half-life
Very effective in COPD in reducing exacerbations
Often in combination with an inhaled steroid
Localized
LABA and Asthma
LABA must be used with steroid in asthmatic patients
Used in asthma when symptoms are not responding to steroids alone
Should not be used in children under age 4 and caution in children under 16
Muscarinic Receptors in healthy lungs
control smooth muscle tone, mucus secretion, vasodilation, and inflammation.
Muscarinic Receptors in COPD and asthma
cholinergic (parasympathetic) mechanisms contribute to increased bronchoconstriction and mucus secretion that limit airflow
Inhaled Anticholinergics
Promotes bronchodilation by blocking muscarinic cholinergic receptors by antagonizing acetylcholine → anticholinergic
Decreases amount of cellular energy which leads to decreased contractility of smooth muscle in the airway**.**
Effective only in mouth-airways
Inhaled Anticholinergics short acting medication
Ipratropium bromide (Atrovent)
Blocks the muscarinic cholinergic receptors
Inhaled Anticholinergics long acting medication
Tiotropium bromide (Spiriva)
Inhibits the muscarinic M3 receptors in the lungs
Ipratropium (SABA)
Blocks the muscarinic cholinergic receptors
Poorly absorbed so minimal systemic exposure (1-2%)
Watch for anticholinergic side effects: mainly dry mouth
May cause cough
NOT FOR ACUTE BRONCHOSPASM
Can not use if allergic to SOY
Tiotropium (LAMA)
Muscarinic Blocker
Dry powder inhaler:About 20% bioavailability- potential more side effects (urine retention, increased IOP)
Anticholinergic Side effects
skin
skin flushing
unable to sweat
overheating
Brain
drowsiness
dizziness
confusion
hallucinations
eyes
blurred vision
dry eyes
mouth
dry mouth
heart
rapid heart rate (Tachycardia)
bowel
constipation
bladder
urine retention
Bronchodilators
Beta Agonists (B2) work to dilate the airways to decrease resistance in improve airflow
Can be short acting for rescue or long acting for maintenance
Given as inhaler or in nebulized form
Rescue meds-should not be used more than 2x week; Use an indicator of therapy efficacy/failure
Exercise induced asthma
Anti-inflammatory medications can…
Block the inflammatory process which leads to the swelling, mucus and narrowing of the airway
Corticosteroids (SONE/NIDE)
Foundation of asthma care
Used in advanced COPD
Blocks components of the inflammatory process in the arachidonic pathway
Used when rapid decrease in inflammation is needed
Usually begin at a higher dose then taper
Coricosteriods Long term effects or overdose
Osteoporosis will develop in up to 20% of those treated with steroids for a year with decreased density in 3 months
Hyperglycemia
CNS
Delirium, agitation, panic and anxiety, mania
HTN
Thin skin
Bruising, purpura
Poor wound healing
Gastric ulceration
Sweating
Anxiety, insomnia, weakness, mood swings
Cushingoid Syndrome
Sensitizes blood vessels and heart to epinephrine and norepinephrine → increased BP and myocardial contractility
Increases glucose production in liver and increases free fatty acid formation for increased insulin production.
Blocks insulin effect in muscles to shunt glucose to brain
Bone is broken down to release calcium for muscle contraction and nerve conduction
Depressed T-Cell function, TNF, Ils and Interferons thus depressing inflammation to divert energy
Cushingoid Syndrome Symptoms
CNS irritability and emotional disturbances
red and round face
hypertension
cardiac hypertrophy
hyperplasia, tumor
purple striae
obesity (fat deposition on abdomen and back of neck)
osteoporosis
muscle wasting
skin ulcers
Females: amenorrhea, hirsutism
males: erectile dysfunction
Montelukast (Singulair)
Leukotriene receptor antagonist
Inhibits leukotriene receptor And blocks the actions of the leukotriene
Stops the allergic response which decreases the asthma and inflammatory response
Not used in primary treatment
Headache, GI symptoms. Generally well tolerated
Used in those age 2 and over
Taken at night
Actions of leukotriene
bronchospasm
bronchial edema
Montelukast (Singulair) Black box warning
psychiatric side effects such as aggression, depression, agitation, sleep disturbances, suicidal thoughts, and suicide.
Inhaled Steroids
Includes all three types of Medications: ICS, LAMA, LABA
Only 10-30% of the medication makes it to the lung
If not used with spacer up to 92% stays in the mouth.
Bioavailability depends on the medication
Fluticasone- has 30% of dose is absorbed
Not for relief of acute bronchospasm
More expensive as there are few generics
Intra nasal Steroid Allergic Rhinitis
Steroids work by inhibiting IgE and the mast cells into the tissues
Nasal sprays have local effect
Coricosteriod suffix
-sone
-lone
-ide
Antihistamines First generation
diphenhydramine
very effective
Often not tolerated because of side effects
Anticholinergic
Onset 15 minutes
Antihistamines Second generation
Loratidine, Cetirizine , Fexofenadine
Less effective
Less side effects
Half life 7 and 30 hours.
Onset in about an 1-2 hours
Decongestants
Pseudoephedrine (Sudafed)
Oxymetazoline
Pseudoephedrine (Sudafed)
a sympathomimetic with a mixed mechanism of action, direct and indirect.
It indirectly stimulates alpha-adrenergic receptors, causing the release of endogenous norepinephrine (NE) while it directly stimulates beta-adrenergic
OTC but must come from the pharmacist
Side Effects can be a problem
Phenylephrine: not as effective
Oxymetazoline
An alpha-1A adrenoceptor agonist used to treat nasal congestion
Afrin nose spray
Works great but can cause rhinitis medicamentosa
Antitussives medications
Dextromethorphan (DM)
Guaifenesin
Antitussives
Cough medicines
Very few are effective
Treat the cause of the cough
Nonopioid
Opioid
Combination
Dextromethorphan (DM):
complex mechanism of action.
Suppresses cough center in brain, blocks NMDA and agonist of Sigma-1 receptors.
A lot of side effects
Guaifenesin:
expectorant loosens secretions to eliminate by coughing by decreasing viscosity