upper & lower respiratory agents

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  1. 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)
  2. Antihistamines
    • Used to relieve symptoms of allergies
    • 1st Generation
    • * Diphenhydramine (Benedryl)
    • * Promethazine (Phenergan)
    • * Hydroxyzine (Vistaril, Atarax)
    • 2nd Generation
    • * Allegra
    • * Claritin
    • * Zyrtec
    • * Astelin
  3. 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
  4. Diphenhydramine (Benadryl): Side effects & interactions
    • S/E: sedation.. dizziness.. incoordination.. fatigue.. confusion.. paradoxal effect.. anticholinergic effects
    • Interactions: CNS depressants & anticholinergics
  5. 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 angioedema
    • Taken 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
  6. Fexofenadine (Allegra): Side effects & interactions
    • S/E: sedation... anticholinergic effects... bitter taste (nasal sprays)
    • Interactions: CNS depressants & anticholinergics
  7. 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
  8. 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
  9. 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
  10. 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]
  11. 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
  12. Oxymetazoline (Afrin): Side Effects
    • Rebound congestion
    • CNS stimulation
    • Vasoconstriction
  13. 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)
  14. 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)
  15. Dextromethorphan: Side effects & interactions
    • S/E: nausea... vomiting... drowsiness... dizziness... irritability... restlessness
    • Interactions: Opioids - enhanced effects
  16. 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
  17. 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
  18. Codeine: Side effects & interactions
    • S/E: sedation... dizziness... lighheadedness... dry mouth... nausea or vomiting... and constipation (mu*)
    • Interactions: ETOH & CNS depressants
  19. 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
  20. 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
  21. 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 tracheostomy
    • Acetylcysteine (Mucomyst)*, and Hypertonic saline
  22. 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)
  23. Acetylcystein (Mucomyst): Side effects & contraindications
    • Bronchospasm
    • Bronchoconstriction
    • Chest tightness
    • Burning feeling in the upper aitway
    • Rhinorrhea
    • Contraindications: respiratory disease & asthma
  24. 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)
  25. 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
  26. 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)
  27. 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
  28. 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
  29. 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)
  30. 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
  31. 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
  32. 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
  33. 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 death
    • Well absorbed when given orally
    • Cautious use: cardiac problems due to stimulatory effects, renal or hepatic disease
  34. 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
  35. 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
  36. 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
  37. 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
  38. 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
  39. 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
  40. 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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upper & lower respiratory agents
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