Respiratory/HEENT Flashcards
Class of Albuterol (ProAir) is ____
SABA - selective short-acting beta-2 receptor agonist (some minor beta 1 activity)
Albuterol (SABAs) : Pharmacodynamics
- acts on beta 2 receptors of intracellular adenyl cyclase (thus increase cAMP conversation) in the lungs – increasing vital capacity and airflow –> Act on the smooth muscle of the bronchi to reverse bronchospasm and inhibit the release of hypersensitivity mediators from mast cell degranulation
- some effect on beta 1 receptors in the hear –> SE: tachycardia, nervousness, etc.
Albuterol : cautions/contraindications
-
avoid in arrhythmias that cause tachycardia or heart blocks and pheochromocytoma (adrenal tumor- increased sympathetic response)
- with pheochromocytoma –> severe HTN
-
caution in pts with CV disease (CHF, HTN), diabetes, glaucoma, and hyperthyroidism
- may need to increase insulin dose in DM (d/t drug-induced hyperglycemia)
- can decrease digoxin serum level
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 agonists
- LABA - long-acting Beta 2 receptor agonists **not as monotherapy in asthma**
- ICS - inhaled corticosteroids (take bronchodilator before ICS)
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
Other examples of LABA medications
- formoterol (Foradil) Q12h
- 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 an increase in asthma-related death
- caution in pts with CVD, diabetes, hyperthyroidism, glaucoma
What drug class contains Theophylline?
Xanthine dervatives
Theophylline/Xanthine derivatives MOA
- general bronchodilator –> inhibit PDE –> increase cAMP –> leads to relaxation of smooth muscle and pulmonary vessel relaxation
- sympathomimetic-–works on the sympathetic nervous system: CNS stim., CV effects, increased fight/flight
- has a 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/anticholinergic gent
-a bronchodilator
SAMA “-tropium”: indications and MOA
Mostly used for COPD - prevent bronchoconstriction
- may be used in asthma exacerbation with albuterol (DuoNeb)
- selectively block the muscarinic 3 receptors in the bronchial smooth muscle causing bronchodilation
- also have anticholinergic effects because muscarinic receptors are cholinergic receptors
- (drying, confusion in elders, dry eyes, urinary retention)
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)
Ipotropium [Atrovent]/ SAMA : ADR
cough, dry mouth, mouth and throat irritation, dyspepsia, n/v
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 antagonist 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 OR 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 (no mast cell degranulation)
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
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 to 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, TB, 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 and MOA
Mast Cell stabilizers (Inhaled Anti-inflammatory agents)
*no bronchodilating activity
MOA:
- Inhibit mast cell degranulation –> prevents the release of histamine and SRS-A
- Continues used – decreased bronchi hyperactivity to stimuli such as allergies
- 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: Indications
- Exercise induced bronchospasm (EIB) - prophylaxis
- asthma (alternative long-term control for mild persistent)
- allergic rhinitis (2nd line)
Cromolyn sodium cautions/contraindications
Contraindications:
- asthma exacerbation/acute bronchospasm
- hypersensitivity to cromolyn
Cautions
- breastfeeding
Safe for children as young as 2 yo (nebulizer)
Cromolyn sodium ADRs
Generally well-tolerated, but inhaled cromolyn may cause bronchospasm, which can be avoided by administering a beta-agonist bronchodilator
- 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
- 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
Decongestant oral and nasal examples
Oral: Phenylephrine HCL, Pseudoephedrine (Sudafed)
Nasal: Oxymetazoline [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 Contraindications
- avoid in HTN and CAD
- Oral (PO) 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 BBB
Antitussives: cautions/ contraindications
- avoid in persistent/chronic cough caused by smoking, asthma, or emphysema
- in asthma, antitussives may impair expectoration and thus cause increased airway resistance
- 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
- benzonatate [Tessalon] - peripherally acting; no risk of CNS sedation
- chest numbness,
- dizziness,
- GI upset,
- headache, and
- “chilly” sensation
Expectorant / Mucinex: MOA
- Thins respiratory secretions (decreases the surface tension of mucus) –> promotes ciliary action in the lungs
GUAIFENESIN
Expectorant/Mucinex: INDICATIONS
- for cough due to common cold or URI
- For congested feeling
Expectorant/Mucinex ADRs
- GI upset : n/v/d
- Drowsiness
- Dizziness
Expectorant/Mucinex: cautions/ contraindications
- do not use for a 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 BBB
- 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 respiratory 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
