Respiratory/HEENT Flashcards
In what drug class does Albuterol (ProAir) belong?
SABA - short-acting beta-2 receptor agonist
Albuterol (SABAs) Pharmacodynamics
- acts on the smooth muscle of the bronchi to reverse bronchospasm by activating beta 2 receptors in the lungs increasing vital capacity and airflow
- also has some effect on beta 1 receptors in the heart - causes side effects tachycardia, nervousness, etc.
Albuterol cautions/contraindications
- avoid in arrhythmias that cause tachycardia and pheochromocytoma (adrenal tumor- increased sympathetic response)
- can cause HTN
- caution in pts with CV disease (CHF, HTN), diabetes, glaucoma, and hyperthyroidism
Albuterol/SABA ADRs (usually transient)
tachycardia, dizziness, palpitations, tremors, nervousness, headache - ** due to effect on beta 1 receptors in the heart**
Examples of other SABAs
- terbutaline (Brethine, Brethaire)
- metaproterenol (Alupent)
- pirbuterol (Maxair)
- levalbuterol (Xopenex)
Three drug classes used for asthma
SABA - short-acting Beta 2 receptor antagonists
LABA - long-acting Beta 2 receptor antagonists **not as monotherapy in asthma**
ICS - inhaled corticosteroids
Salmeterol (Serevent) [LABA] MOA
- relaxes bronchial smooth muscle by selective action on beta 2 receptors
3 advantanges:
- Quick onset of action
- Long MOA- last longer
- More selective to Beta-2 receptors which decreases the prevalence of side effects
Salmeterol (Serevent) drug class
Long-acting beta 2 receptor agonist (LABA)
Other examples of LABA medications
- formoterol (Foradil) - taken Q 12 hrs
- vilanterol (Breo Ellipta) - Ultra long acting - taken QD “Very easy to take”
LABA cautions/contraindications
- NOT to be used as mono-therapy in patients with asthma (Serevent and Foradil) - causes downregulation of beta-2 receptors if used alone so in emergencies, short-acting beta-2 receptor antagonist medications (Albuterol) will not work - leads to increase in asthma intubations and death
- caution in pts with cardiovascular dz, diabetes, hyperthyroidism, glaucoma
What drug class contains Theophylline?
Xanthine dervatives
Theophylline/xanthine dervatives MOA
- general bronchodilator - leads to relaxation of smooth muscle
- sympathamometic - works on the sympathetic nervous system: CNS stim., CV effects, increased fight/flight - has similar chemical structure to caffeine
Theophylline/Xanthine derivatives cautions/ contraindications
- monitor closely in cardiovascular disease
- avoid in pts w/ hx of seizures, peptic ulcer dz
- educate patient to avoid smoking and caffeine
- educate pt on the signs of toxicity
- educate pt to maintain a steady diet
Ipratropium bromide (Atrovent) / SAMA MOA
selectively blocks M3 receptors in the lungs causing bronchodilation - muscarinic receptor antagonist
SAMA “-tropium” indictations and MOA
Mostly used for COPD - may be used in asthma exacerbation with albuterol (DuoNeb)
- selectively block the muscarinic 3 receptors in bronchial smooth muscle causing bronchodilation
- also have anticholinergic effects because muscarinic receptors are cholinergic receptors
Ipratropium bromide (Atrovent) = Immediate effects
Atrovent/Ipratropium bromide cautions/ contraindications
- not used alone for acute bronchospasm
- due to anticholinergic effects: avoid in pts with urinary retention, BPH, and closed-angle glaucoma
(Anticholinergic effects: patients can’t see, pee, spit, shit, or think)
Atrovent / SAMA adverse drug effects
cough, dry mouth, mouth and throat irritation, dyspepsia, nausea and vomiting
Atrovent/SAMA patient education
- after use, rinse mouth and spit it out
Tiotropium bromide (Spiriva) Indications for use and MOA - LAMAs
Used primarily for COPD to control symptoms
Selectively block the muscarinic 3 receptors (muscarinic 3 receptor antagonist) in the lungs leading to smooth muscle bronchodilation
- long acting anticholinergic/muscarinic agent
Tiotropium bromide (Spiriva) cautions/ contraindications
- due to anticholinergic effects: avoid in pts with urinary retention, BPH, and closed-angle glaucoma
LAMA Adverse Drug Reactions
- dry mouth, pharyngitis, upper respiratory infection, headache, mouth irritation - not approved for children < 12 years old
LAMA patient education
- Rinse mouth after inhaling medication
Leukotriene Modifiers Indication and Examples
Allergies/allergic rhinitis with asthma - if pt is not well controlled during times when seasonal allergies are worse
Montelukast (Singular)
Zafirlukast (Accolate)
Zileuton (Zyflo)
Montelukast and Zafirlukast MOA
Leukotriene receptor antagonist (LTRAs) - blocks the cysteinyl leukotriene (CysLT1) receptor and decreases the inflammatory response in the lungs
Zileuton (Zyflo) MOA
- prevents the synthesis of leukotrienes - inhibits 5-lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid
Leukotriene Modifiers cautions/contraindications
- Zafirlukast and Zileuton- use with caution in patients with hepatic disease
- Not to be used in acute asthma exacerbation
Leukotriene Modifiers ADRs
- headache, GI upset, myalgias
- Neuropsychiatric: hallucinations, agitation, aggression, suicidal ideations and behavior, insomnia, depression
- Zafirlukast and Zileuton/Zyflo: can cause hepatotoxicity
Clinical use of LTRAs
- Montelukast - persistent asthma in patients 1 year old and older -
- Zafirlukast - chronic asthma in patients 5 years old and older
- Zileuton - persistent asthma in patients 12 years old and older
*** needs to be taken daily - takes 3-5 days to reach full effect
Fluticasone (Flovent/Flonase) drug class
Inhaled corticosteroids (ICSs) - pulmonary inhalers and intranasal
Budesonide - another example of an ICS medication
ICSs indications
- Primarily used in asthma (2nd line if pt is using SABAs more than 2x/week)
- can also be used in COPD to reduce exacerbations - keep pts out of the hospital
ICSs MOA
- potent anti-inflammatory and vasoconstriction action
- inhaled: inhibit IgE in mast cell migration of inflammatory cells into the bronchioles - used in all ages
- intranasal: focuses on inflammation in the nasal mucosa alone
- used in patients 2 years and older
ICSs cautions/ contraindications
- NOT for asthma exacerbation
- use caution in active infection
- watch potassium levels, glucose, bone density, growth (high doses for a long time)
Avoid in: Cushing syndrome, herpes, tuberculosis, nasal trauma or ulcers, untreated respiratory infection
ICSs ADRs
-dry mouth (xerostomia), hoarseness, mouth and throat irriation, flushing, bad taste, oral candidiasis, rash, urticaria (rare)
ICS Patient education
- rinse mouth and spit after use
- keep taking as directed - the only way you know this is working is by less use of SABAs
- if using the a bronchodilator - use the bronchodilator 1st and then after a few minutes use the ICS inhaler
- nasal: blow nose prior to application
- effects are not immediate - takes 3-7 days to see full effect
Cromolyn sodium drug class
Mast Cell stabilizers - decrease bronchi hyperactivity to stimuli such as allergies
Cromolyn sodium Indication
Exercise induced bronchospasm (EIB) - asthma - allergic rhinitis
Cromolyn sodium MOA
- inhibits antigen-induced bronchospasm and blocks the release of histamine by inhibiting mast cell degranulation
- has no effect of beta receptors, but can help reduce the need for Albuterol - good for patients that have a need to SABA prior to athletics more than 2 times a week - use this instead
Cromolyn sodium cautions/contraindications
- not to be used for asthma exacerbation
Cromolyn sodium ADRs
- throat irritation, cough, drowsiness, bronchospasm (rare)
- nasal irritation and burning sensation in the nose
Examples of Inhaled Antihistamines (intranasal)
- Azelastine (Astepro)
- Olopatadine (Patanase)
Azelastine and Olopatadine indication for use
- seasonal allergies - allergic rhinitis and vasomotor rhinitis
Inhaled Antihistamines (Azelastine/Olopatadine) MOA
H1 blocker - Inhibit the release of histamine by competing with histamine at H1 receptor sites
Inhaled antihistamines cautions/contraindications
- do not combine w/ CNS depressants
- approved in pediatrics
Inhaled antihistamines (Azelastine/Olopatadine) ADRs
- somnolence (greater with azelastine)
- bitter taste
- headache
- nasal irritation - burning sensation
Leukotriene Modifiers Indication and Examples
Allergies/allergic rhinitis with asthma - if pt is not well controlled during times when seasonal allergies are worse
Montelukast (Singular)
Zafirlukast
Zileuton (Zyflo)
Decongestant oral and nasal examples
Oral: Phenylephrine HCL, Pseudoephedrine (Sudafed) Nasal: Afrin
Oral decongestants MOA
Alpha 1 agonists (sympathomimetics) - they mimic the endogenous catecholamines of the sympathetic nervous system
- produces vasoconstriction by stimulating the Alpha 1 receptors in the mucosa of the resp. tract, thus temporarily reducing swelling and inflammation
**used to treat symptoms
Decongestants cautions and ontraindications
- avoid in HTN and CAD
- oral not recommended in children < 4 years old - not recommended in pregnancy and lactation
- avoid in combination with beta blockers - potentiate CV issues
- topical/nasal: do not use for longer than 3 days (can cause rebound congestion)
Decongestants ADRs
- anxiety, restlessness, headache, insomnia, psychological disturbances, tremors, HTN, tachycardia (fight or flight symptoms) - topical: nasal irritation and rebound congestions with prolonged use
Examples of Antitussive medications
- Dextromethorphan
- Codeine
- Benzonatate
Dextromethorphan and Codeine MOA
-acts centrally in the medulla to elevate the threshold for coughing - affects serotonin - suppresses the cough reflex - risk for abuse
Benzonatate MOA
- thought to anesthetize the stretch receptors in the respiratory passages, calming the cough - numbs the lungs - makes lungs more relaxed - does cross blood-brain barrier
Antitussive medications cautions/ contraindications
- avoid in persistent/chronic cough caused by smoking, asthma, or emphysema
- additive CNS depression when dextromethorphan or codeine is used with CNS depressants - can decrease respiratory drive
- do not self-medicate for more than 7 days
Antitussive ADRs
- dextromethorphan and codeine - drowsiness, dizziness, and GI upset
- benxonatate - chest numbness, dizziness, GI upset, headache, and “chilly” sensation
Expectorant / Mucinex MOA
- decreases the surface tension of mucus making the mucus more thin and loose for clearance
Expectorant/Mucinex indication for use
- for cough due to common cold or upper respiratory infections
Expectorant/Mucinex ADRs
- GI upset - diarrhea - nausea - vomiting
- drowsiness - dizziness
Expectorant/Mucinex cautions/ contraindications
- do not use for persistent cough
- do not use for cough r/t heart failure or ACE inhibitor therapy
Diphenhydramine (Benadryl) indications
- allergic rhinitis
- hypersensitivity reactions
- urticaria and angioedema
- insomnia
Diphenhydramine Drug Class
1st Generation Antihistamine
Diphenhydramine MOA
- competitively antagonized the effects of histamine at the H1 receptor sites - has anticholinergic effects
Diphenhydramine Cautions/ Contraindications
- crosses the blood-brain barrier
- not to be combined with CNS depressants
- avoid in patients with glaucoma, BPH d/t anticholinergic effects
- avoid in infants, newborns, elderly
- Safe in pregnancy
- avoid in lactation (dries up milk production)
1st Generation Antihistamines (Benadryl) ADRs
- sedation - dizziness - confusion - ataxia - urinary retention - paradoxical excitation - dry mouth - tremor - blurred vision - constipation (think anticholinergic effects and CNS effects)
***cross the blood-brain barrier***
2nd Generation Antihistamines Examples
Cetirizine (Zyrtec) Loratadine Fexofenadine
2nd Generation Antihistamine (Zyrtec/ Loratadine/ Fexofenadine) indications
- respiratory allergies - urticaria
2nd Generation Antihistamine MOA (Zyrtec/ Loratadine/ Fexofenadine)
- competitively antagonizes the effects of histamine at the peripheral H1 receptor sites in the GI tract, blood vessels, and repiratory tract - in general- avoids crossing the blood-brain barrier - no anticholinergic effects
2nd Generation Antihistamines - Cetirizine, Loratadine, Fexofenadine cautions/ contraindications
- safe in pregnancy and lactation
- may have some CNS effects and can cause drowsiness - not as much as with 1st gen.
- Cetirizine ok for 6mo and older
- Loratadine ok for > 2 year olds
- Fexofenadine ok for > 6 year olds