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Allergic Rhinitis
- Inflammatory disorder that affects the upper airway, lower airway and eyes
- Symptoms: Sneezing.. Rhinorrhea.. Pruritis.. and Nasal Congestion
- Triggered by allergens; bind to IgE mast cells
- Release of histamine, leukotrienes, and prostaglandins
- Treatment: oral antihistamines, intranasal gluccocorticoids, sympahomimetics (decongestants)
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Antihistamines
- Used to relieve symptoms of allergies
- 1st Generation
- * Diphenhydramine (Benedryl)* Promethazine (Phenergan)
- * Hydroxyzine (Vistaril, Atarax)
- 2nd Generation
- * Allegra
- * Claritin
- * Zyrtec
- * Astelin
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Diphenhydramine (Benadry)
- Blocks the release of histamine
- Therapeutic uses: relieves symptoms of allergic rhinitis; motion sickness: used to relieve nausea, vomiting, and vertigo; treatment of extrapyramidal symptoms (EPS)
- 1st generation antihistamine: signigicant antimuscarinis activity and produce marked sedation in most patients
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Diphenhydramine (Benadryl): Side effects & interactions
- S/E: sedation.. dizziness.. incoordination.. fatigue.. confusion.. paradoxal effect.. anticholinergic effects
- Interactions: CNS depressants & anticholinergics
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Fexofenadine (Allegra)
- Selectively blocks the effects of histamines and the H1-receptor sites
- Has some anticholinergic & antipruitic effects
- 2nd generation antihistamine:
less sadation and anticholinergic effects - Therapeutic uses: relief of symptoms associated with seasonal and perennial rhinitis; allergic conjunctivitis; uncomplicated urticaria; and angioedemaTaken orally and absorbed rapidly; slightly metabolized in the liver; excreted in feces mostly
- Contraindications: hypersensitivity, children under 12, pregnant/lactating women, pts with renal failure, use with othr CNS depressants
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Fexofenadine (Allegra): Side effects & interactions
- S/E: sedation... anticholinergic effects... bitter taste (nasal sprays)
- Interactions: CNS depressants & anticholinergics
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Itranasal glococorticoids: Beclometasone (Beconase)
- Most effective drugs for the prevention and treatment of seasonal and perennial rhinitis
- Treatment of all major symptoms; decrease inflammation
- Adverse effects: drying, burning, itching of nasal muscosa, sore throat, epistaxis, HA
- Systemic effects possible: adrenal suppression & slowing of growth in children
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Decongestant Drugs
- Sympathomimetic agent used to decrease nasal congestion
- Activates alpha-1 adrenergic receptors on nasal blood vessels (alpha-1 stimulation = fight-or-flight)
- Can be administered orally or topically
- * Sudafed & Afrin
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Pseudoephedrine (Sudafed)
- Mimics the actions of the sympathetic nervous system
- Constriction of vasculature to promote drainage
- Therapeutic uses: reduces the volume of nasal mucus; relieves pressure of ottitis media by promoting drainage
- Absorbed readily from the GI tract
- Duration: 4 - 6 hours for regular formulations; 8-12 hours XR preparations
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Pseudoephedrine (Sudafed): Side effects & contraindications
- S/E: (related to sympathomimetic effects): CNS, CV
- Contraindications: severe HTN & CAD
- * Special caution: diabetes, thyrotoxicosis, BPH, and increased intraocular pressure (IOP) [Glaucoma - cautious use - causes pupil dilation = angle of the pupil tightend with the cornea and does not facillitate aqeous humor drainage]
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Oxymetazoline (Afrin)
- Powerful alpha-adrenergic stimulant
- Stimulates alpha-1 adrenergic receptors causing reduction of inflammation
- Therapeutic uses: Relieves nasal stuffiness caused by allergic rhinitis, URI, sinusitis
- Found in many OTC topical preparations
- Avoid use in abraded nasal membranes
- Can cause serious effects when absorbed systemically
Caution: coronary heart disease & HTN- Topical and oral formulations
Limit topical use to 3 - 5 days
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Oxymetazoline (Afrin): Side Effects
- Rebound congestion
- CNS stimulation
- Vasoconstriction
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Antitussive Drugs
- Drugs that suppress the cough reflex
- Coughing is reflexive but persistent coughing can be exhausting, cause muscle strain, and further irritate the repiratory tract.
- Nonopiod: Dextromethorphan (e.g., Robitussin-DM)
- Opioid: Codeine and hydrocodone (Vicotuss & others)
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Dextromethorphan
- Mainly works by affecting the cough center in the medulla
- Therapeutic uses: treatment of chronic, nonproductive cough;
not for treating chronic coughs resulting from emphysema and asthma - Absorbed rapidly from the GI tract; undergoes extensive hepatic metabolism
- Nonopioid antitussive (Robitussin-DM & many more)
- Related to opiates (but do not have opioid actions)
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Dextromethorphan: Side effects & interactions
- S/E: nausea... vomiting... drowsiness... dizziness... irritability... restlessness
- Interactions: Opioids - enhanced effects
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Benzoatate (Tessalon Perles)
- Nonopioid antitussive drug
- Works by numbing the stretch receptors in the lungs, that during breathing, elicit a cough
- Not recommended for people at increased risk for choking (may be unaware of feeling at the back of their throat, avoid use in elderly adults & children)
- Local anesthetic
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Codeine
- Opioid antitussive [others: hydrocodone (more sedating than codeine)]
- Works directly on the medullary center to suppress the cough reflex
- Therapeutic uses: suppress chronic non-productive cough
- Controlled substance used in treating cough: schedule II
- More sedating than dextromethorphan and also may induce repiratory depression
- Patient education: avoid driving, change position slowly
- Cautious use: pregnant/breast-feeding, head injuries (drug will decrease respiratory drive = CO2 retention, cerebral vessel diation & increased intracranial pressure), asthma, liver & renal dysfunction, chronic cough, addictions
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Codeine: Side effects & interactions
- S/E: sedation... dizziness... lighheadedness... dry mouth... nausea or vomiting... and constipation (mu*)
- Interactions: ETOH & CNS depressants
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Guaifenesin (Robitussin, Mucinex, Humabid, Tussin)
- * Expectorant
- Enhances the output of respiratory tract fluids by reducing the adhesiveness and surface tension of the respiratory fluids; the result of thinning secretions is a more productive cough; may be used for treatment of infertility
- Therapeutic uses: treatment of cough
- Taken orally and absorbed readily from the GI tract
- Duration of action: 4 to 6 hours
- Eliminated by the kidneys
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Iodine preparations
- * Expectorant
- Used for many years to stimulate an increase in the fluid produced by the lungs
- Are used as an adjunctive treatment in respiratory tract conditions such as CF, chronic sinusitis
- Bitter flavor limits their popularity
- Must be used with caution because of their effect on the thyroid gland
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Mucolytic drugs
- Break down mucus to help the high-risk respiratory patient cough up thick, tenacious secretions to improve breathing and air flow
- Administered by a nebulizer or through and endotracheal tube or tracheostomyAcetylcysteine (Mucomyst)*, and Hypertonic saline
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Acetylcystein (Mucomyst)
- * Mucolytic
- Reacts with mucus to make it more watery
- Therapeutic uses: COPD, CF, pneumonia, TB, development of atelectasis, diagnostic bronchoscopy, acetaminophen OD (* must be given within 24 hours of acetaminophen OD to prevent hepatotoxicity)
- Onset: occurs within 1 minute, peak effect occuring within 5 to 10 minutes
- Keep suction equipment available
- (Mucomyst - smells like rotten eggs)
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Acetylcystein (Mucomyst): Side effects & contraindications
- Bronchospasm
- Bronchoconstriction
- Chest tightness
- Burning feeling in the upper aitway
- Rhinorrhea
- Contraindications: respiratory disease & asthma
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Asthma
- Common, chronic, inflammatory, immune mediated respiratory condition
- S/S: dyspnea, chest tightness, wheezing, cough
- Treatment aimed at controlling bronchoconstriction & inflammation * Beta-2 agonists * Glucocorticoids * Cromolyn (coming off the market)
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Bronchodilator classes
- Sympathomimetics - beta-2 adrenergic agonists: albuterol (Ventolin, Proventil)
- Anticholinergics: ipratropiuim bromide (Atrovent)
- Xanthine derivatives - theophylline (Theodur)
* steroids and beta agonists frequently combined together
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Beta-2 Agonists
- Beta-2 receptors more predominant in the lungs (Beta-1 more predominant in the heart)
- Formulations: short-acting & long-acting inhalers, oral
- Levalbuterol (Xopenex)
- Pirbuterol (Maxair)
- Salmeterol (Serevent)
- Terbutaline (Breathine)
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Beta-2 Agonist drugs
- Activate beta-2 adrenergic receptors in smooth muscle of the lung, promote bronchodilation
- Therapeutic uses: COPD & asthma
- Bronchodilation occurs within 5 to 15 minutes (inhalation); within 30 minutes (tablet or liquid)
- S/E: related to sympathomimetic activity - tachycardia, dysrhythmias, angina pectoris, tremor
- Labs/monitoring: HR, BP, RR, pulse ox, peak flow
- Patient education: rescue drug, proper use of inhaler, frequency of inhaler use, limit caffeine, and refrain from certain OTC medications
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Beta-2 Agonists: Contraindications & precautions
- Hypersensitivity and HTN, cardiac disease, cardiac arrhythmias, ischemic heart disease, hyperthyroidism, DM, and seizures
- Overuse of albuterol may induce rebound bronchoconstriction
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Respiratory Anticholinergic Agents
- Diminish the effect of acetylcholine, their terminal neurotransmitter in the parasympathetic nervous system
- Use of inhaled anticholinergic drugs stops the bronchoconstriction that is caused by stimulation of the parasympathetic nervous system
- * Ipratropium Bromide (Atrovent, Combivent, Duoneb); Tiotropim (Spiriva)
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Ipratropium Bromide (Atrovent, Combivent, Duoneb)
- * Bronchodilator
- Antagonizes the action of acetylcholine by blocking muscarinic cholinergic receptors
- Therapeutic uses: maintenance treatment of bronchospasm associated with bronchitis, pulmonary emphysema, COPD; off-label use with asthma
- Administered through oral inhalation or intranasal spray
- Pt teaching: will not abort an asthma attack is progress
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Ipratropium Bromide (Atrovent, Combivent, Duoneb): Side effects & precautions
- S/E: rare, paradoxic bronchospasm - usually see with the first inhalation from a newly opened MDI -- patients should "prime" the canister with three pumps before using a new MDI for the first time
- Cautious use: (becuase parasympathetic opposition of the sympatheric nervous system is opposed) bladder obstruction.. BPH.. closed-angle glaucoma
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Xanthine Derivatives
- * Bronchodilators
- Come frome a variety of naturally occuring sources
- Theophylline
- Aminophylline (breaks down to theophyllin and is usually used as IV)
- Diphylline
- Oxytriphylline
- Caffeine
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Theophylline (Theodur)
- Directly relaxes the smooth muscle of the respiratory tract
- Therapeutic uses: symptomatic relief or prevention of bronchial asthma and reversal of bronchospasm associated with COPD; Unlabeled us: treatment of apnea and bradycardia in premature infants
- Labs & monitoring: normal serum level 10-20 mcg/mL - greater than 30 mcg/mL may result in deathWell absorbed when given orally
- Cautious use: cardiac problems due to stimulatory effects, renal or hepatic disease
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Theophylline (Theodur): Side effects, interactions & contraindications
- S/E: related to serum level
- Interactions:
- * Lowers levels: phenobarbital, phenytoin, rifampin
- * Raises levels: H2 blockers (cimetidine/Tagamet or rantidine/Zantac) and antibiotics
- Smoking cigarettes may decrease serum theophylline levels, requiring dosages of up to 50% more (smoking causes the drug to break down more rapidly)
- Contraindications: Hypersensitivity, status asthmaticus (asthma attack that you cannot break), peptic ulcer
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Anti-inflammatory: Glucocorticoid Steroids
- The most effective anti-inflammatory drugs available for the management of respiratory disorders
- May be given orally, paraenterally, or by inhalation
- Peak effect in 1 to 2 weeks of regular use
- Use as a maintenance drug, not for acute respiratory symptoms
- Cautious use: active infection
- Adverse effects: sore throat.. hoarseness.. coughing.. dry mouth.. pharyngeal and laryngeal fungal infections (thrush)
- Pt teaching: Rinse mouth after use; use spacer; use daily
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Cromolyn Sodium (Intal)
- * Mast cell stabilizer [others in class: Nedrocromil (Tilade) which was removed from market]
- Prevents the breakdown of mast cells which prevents the release of histamine
- Therapeutic uses: prophylactic agent in the treatment of mild to moderate asthma; nasal inhaler to treat seasonal allergic rhinitis; as an opthalmic solution to treat allergic conjuctivitis
- * Improvement of syptoms takes several weeks of therapy
- Pt teaching: use 15 to 20 minutes prior to engaging in precipitant to bronchospasm
- * Being taken off the market - unable to find a company willing to change clorofluorocarbone propellent inhaler to a hydrofluoralkane inhaler (HFA) inhaler
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Cromolyn Sodium (Intal): side effects & contraindications
- S/E: bronchospasm, throat irritation, and cough; lactose intolerance symptoms in oral preparations
- Contraindications: aerosol preparations in those with CAD or cardiac dysrhythmias
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Leukotriene Receptor Antagonists: Montelukast (Singulair)
- [others: Zileuton (Zyflo), Zafirlukast (Accolate)]
- Thereapeutic uses: have been identified as important mediators in the pathology and symptomatology of both acute and chronic asthma; prophylaxis treatment of chronic asthma
- Labs & monitoring: LFTs (AST, ALT), other drug levels
- Zileuton inhibits leukotriene synthesis
- Zafirlukast and montelukast block leukotriene receptors
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Leukotriene Receptor Antagonists: Montelukast (Singulair) - Side effects & interactions
- S/E: Zileuton and Zafirlukast may cause liver failure and hepatitis..
- S/E of all agents in class: HA.. GI disturbances.. arthralgias.. myalgias
- Interactions: metabolized through cytochrome P540.. Increases levels of: theophyllin, warfarin, and propanolol
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Leukotriene Receptor Antagonists: Montelukast (Singulair) - Physiologic Action
- Prevents the formation of potent leukotrienes; this mechanism may be beneficial to disorders such as asthma, rheumatoid arthritis, and ulcerative colitis; but at this time is only approved for the management of asthma
- Decreases inflammation
- Decreases bronchoconstriction
- Decreases edema
- Decreases mucus production
- Decreases recruitment of inflammatory cells
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