Download - Respiratory Pharmacology
RESPIRATORY RESPIRATORY PHARMACOLOGYPHARMACOLOGY
Bronchial Asthma Bronchial Asthma (Long term respiratory dysfunction)(Long term respiratory dysfunction)
Definition:Definition:
A chronic inflammatory disorder of the A chronic inflammatory disorder of the
airway airway (trachea, bronchi, & bronchioles)(trachea, bronchi, & bronchioles)
characterized bycharacterized by attacks of wheezy attacks of wheezy
breathlessness, sometimes on exertion, breathlessness, sometimes on exertion,
sometimes at rest, sometimes mild, sometimes at rest, sometimes mild,
sometimes severe.sometimes severe.
Bronchial Asthma Bronchial Asthma
Etiology:Etiology:
Triggers factors tend to Triggers factors tend to participate and/or aggravate asthma participate and/or aggravate asthma exacerbation.exacerbation.
1.1. Allergens e.g: pollens,air pollution, dust.Allergens e.g: pollens,air pollution, dust.
2.2. Irritants e.g: Tobacco smoke, sprays.Irritants e.g: Tobacco smoke, sprays.
3.3. Exercise.Exercise.
4.4. Temperature or weather changes.Temperature or weather changes.
5.5. Exposure to infection.Exposure to infection.
6.6. Animals: e.g: cats, dogs, rodents, horses.Animals: e.g: cats, dogs, rodents, horses.
Bronchial AsthmaBronchial Asthma
7.7. Strong emotions: e.g: fear, laughing.Strong emotions: e.g: fear, laughing.
8. Food: e.g: Nuts, chocolate, milk.8. Food: e.g: Nuts, chocolate, milk.
9. 9. Medication: e.g: Aspirin.Medication: e.g: Aspirin.
Bronchial AsthmaBronchial Asthma
Pathophysiology:Pathophysiology:
Asthma triggerAsthma trigger
- Inflammation & edema of the mucous Inflammation & edema of the mucous membranes.membranes.
- Accumulation of tenacious secretions from Accumulation of tenacious secretions from mucous glands.mucous glands.
- Spasm of the smooth muscle of the bronchi & Spasm of the smooth muscle of the bronchi & bronchioles decreases the caliber of the bronchioles decreases the caliber of the bronchioles.bronchioles.
Bronchial Asthma Bronchial Asthma
Bronchial Asthma Bronchial Asthma
Clinical manifestations:Clinical manifestations:
A) A) General manifestations:General manifestations:
1.1. The classical manifestationsThe classical manifestations are: dyspnea, are: dyspnea,
wheezing, & cough.wheezing, & cough.
2.2. The episode of asthmaThe episode of asthma is usually begins with is usually begins with
the child feeling irritable & increasingly the child feeling irritable & increasingly
restless. Asthmatic child may complain restless. Asthmatic child may complain
headache, feeling tired, & chest tightness.headache, feeling tired, & chest tightness.
Bronchial AsthmaBronchial Asthma
Clinical manifestations:Clinical manifestations:
B) B) Respiratory symptoms:Respiratory symptoms:- Hacking, paroxysmal, irritating and non productive - Hacking, paroxysmal, irritating and non productive
coughcough (( جافه متقطعه كحه جافه نوبات متقطعه كحه due to bronchial due to bronchial ((نوباتedema.edema.
Accumulation of secretion stimulate cough that becomes Accumulation of secretion stimulate cough that becomes rattlingrattling((مجلجلهمجلجله) ) & productive (frothy, clear, & productive (frothy, clear, gelatinous sputum).gelatinous sputum).
- Shortness of breath, prolonged expiration, wheezy - Shortness of breath, prolonged expiration, wheezy chest, cyanosed nail beds, & dark red color lips that chest, cyanosed nail beds, & dark red color lips that
may progress by time to blue.may progress by time to blue.
Bronchial AsthmaBronchial Asthma
C) C) On chest examination:On chest examination:- InspectionInspection reveals major changes in the form reveals major changes in the form
of supraclavicular, intercostals, subcostal, & of supraclavicular, intercostals, subcostal, & sternal retractionssternal retractions due to the frequent use of due to the frequent use of accessory muscles of respiration.accessory muscles of respiration.
With repeated episodes:With repeated episodes: chest shape is changed chest shape is changed toto barrel chest, & elevated shoulder. barrel chest, & elevated shoulder.
- Auscultation Auscultation reveals loud breath sounds in reveals loud breath sounds in the form of the form of course crackle, grunting, wheezescourse crackle, grunting, wheezes throughout the lung region.throughout the lung region.
Bronchial AsthmaBronchial Asthma
Bronchial AsthmaBronchial Asthma
Diagnostic evaluation:Diagnostic evaluation:
1.1. Clinical manifestations, history, physical Clinical manifestations, history, physical
examination, & Lab tests.examination, & Lab tests.
2.2. Radiographic examination.Radiographic examination.
3.3. Pulmonary function tests provide an Pulmonary function tests provide an
objective method of evaluating the degree objective method of evaluating the degree
of lung disease. of lung disease.
Bronchial AsthmaBronchial Asthma
Therapeutic management:Therapeutic management:
- Allergic control to prevent attacks.Allergic control to prevent attacks.
- Drug therapy:Drug therapy:
B- adrenergic, Theophyllin, & corticosteroids B- adrenergic, Theophyllin, & corticosteroids
preparations + chest physiotherapy (only in preparations + chest physiotherapy (only in
between attacks).between attacks).
TERIMA KASIH
Respiratory PharmacologyRespiratory Pharmacology
GENERIC:GENERIC: AlbuterolAlbuterol
BRAND:BRAND: Proventil, VentolinProventil, Ventolin
CLASS:CLASS: SympathomimeticSympathomimetic
AlbuterolAlbuterol
ActionsActions1.1. Agonist for Beta 2 adrenergic receptors; relaxing Agonist for Beta 2 adrenergic receptors; relaxing
bronchial smooth muscle which results in bronchial smooth muscle which results in bronchodilationbronchodilation
2.2. Minimal cardiac side effectsMinimal cardiac side effects
AlbuterolAlbuterol
Indications:Indications:1.1. Treatment of bronchospasm associated with asthma, Treatment of bronchospasm associated with asthma,
chronic bronchitis and emphysemachronic bronchitis and emphysema
2.2. Prevention of exercise-induced bronchospasmPrevention of exercise-induced bronchospasm
AlbuterolAlbuterol
Contraindications:Contraindications:1.1. Hypersensitivity to sympathomimeticsHypersensitivity to sympathomimetics
2.2. Cardiac dysrhythmiaCardiac dysrhythmia
3.3. Tachycardia and tachydysrhythmiasTachycardia and tachydysrhythmias
AlbuterolAlbuterol
Adverse Reactions:Adverse Reactions:1.1. Excessive use may cause paradoxical bronchospasm Excessive use may cause paradoxical bronchospasm
and arrhythmiasand arrhythmias
2.2. Tachycardia, palpitations, angina, PVCs, hypotension, Tachycardia, palpitations, angina, PVCs, hypotension, and hypertensionand hypertension
3.3. TremorsTremors
4.4. HyperglycemiaHyperglycemia
5.5. Peripheral vasodilationPeripheral vasodilation
6.6. NervousnessNervousness
7.7. Nausea/VomitingNausea/Vomiting
AlbuterolAlbuterol
Precautions:Precautions:1.1. DiabetesDiabetes
2.2. HyperthyroidismHyperthyroidism
3.3. Cerebrovascular diseaseCerebrovascular disease
4.4. Seizure disordersSeizure disorders
AlbuterolAlbuterol
Dose:Dose:1.1. 2 inhalations with metered-dose inhaler, q 4-6 hours2 inhalations with metered-dose inhaler, q 4-6 hours
2.2. 3 ml premixed bullet in nebulizer3 ml premixed bullet in nebulizer
AlbuterolAlbuterol
Incompatible/Reactions:Incompatible/Reactions:1.1. Tricyclic antidepressants/monoamine oxidase Tricyclic antidepressants/monoamine oxidase
inhibitors (MAOIs), may increase the effect of this druginhibitors (MAOIs), may increase the effect of this drug
2.2. Other sympathomimeticsOther sympathomimetics
3.3. Beta blockers inhibit the effectsBeta blockers inhibit the effects
AlbuterolAlbuterol
Notes:Notes:
Onset:Onset: 5-15 minutes5-15 minutes
Peak:Peak: 30 minutes – 2 hours30 minutes – 2 hours
Duration:Duration: 3-4 hours3-4 hours
1.1. Can be delivered by inhaler and nebulizerCan be delivered by inhaler and nebulizer
2.2. Metabolized in the liver and excreted in the urineMetabolized in the liver and excreted in the urine
Respiratory PharmacologyRespiratory Pharmacology
GENERIC:GENERIC: EpinephrineEpinephrine
BRAND:BRAND: AdrenalinAdrenalin
CLASS:CLASS: Sympathomimetic/Sympathomimetic/CatecholamineCatecholamine
EpinephrineEpinephrine
Action:Action:1.1. Direct effect on Direct effect on alphaalpha and and betabeta adrenergic receptor adrenergic receptor
sitessites
2.2. Effects include:Effects include:
Alpha:Alpha: bronchial, cutaneous, renal and visceral bronchial, cutaneous, renal and visceral arteriolar constrictionarteriolar constriction
Beta 1:Beta 1: positive inotropic and chronotropic actions, positive inotropic and chronotropic actions, increases automaticityincreases automaticity
Beta 2:Beta 2: bronchial smooth muscle relaxation and bronchial smooth muscle relaxation and dilation of skeletal vasculaturedilation of skeletal vasculature
3. Inhibits the release of histamine3. Inhibits the release of histamine
EpinephrineEpinephrine
Indications:Indications:1.1. Cardiac arrest in generalCardiac arrest in general
2.2. Ventricular fibrillationVentricular fibrillation
3.3. AsystoleAsystole
4.4. Pulseless electrical activityPulseless electrical activity
5.5. Infusion for profound hypotension associated with Infusion for profound hypotension associated with bradycardias, in combination with other pressorsbradycardias, in combination with other pressors
6.6. Bronchospasm and bronchoconstriction of bronchial Bronchospasm and bronchoconstriction of bronchial asthma and some forms of COPDasthma and some forms of COPD
7.7. AnaphylaxisAnaphylaxis
EpinephrineEpinephrine
Contraindications:Contraindications:
1.1. Uncorrected tachydysrhythmiasUncorrected tachydysrhythmias
2.2. Underlying cardiovascular disease or hypertensionUnderlying cardiovascular disease or hypertension
3.3. GlaucomaGlaucoma
4.4. Hypersensitivity to catecholaminesHypersensitivity to catecholamines
5.5. HypothermiaHypothermia
Epinephrine/Adverse ReactionsEpinephrine/Adverse Reactions
HypertensionHypertension
Ventricular arrhythmiasVentricular arrhythmias
Pulmonary edemaPulmonary edema
TachycardiaTachycardia
PalpitationsPalpitations
AnxietyAnxiety
Psychomotor agitationPsychomotor agitation
Nausea/VomitingNausea/Vomiting
Pupil dilationPupil dilation
AnginaAngina
NervousnessNervousness
HeadacheHeadache
DizzinessDizziness
TremorsTremors
HallucinationsHallucinations
Cerebral hemorrhageCerebral hemorrhage
AnorexiaAnorexia
EpinephrineEpinephrine
Precautions:Precautions:1.1. Due to the possibility of cardiovascular disease, Due to the possibility of cardiovascular disease,
epinephrine should be administered with caution in epinephrine should be administered with caution in patients over 35 years of age (with respiratory patients over 35 years of age (with respiratory problems or if they are conscious)problems or if they are conscious)
2.2. The patient should be carefully monitored for changes The patient should be carefully monitored for changes in pulse, blood pressure, and ECG after administration in pulse, blood pressure, and ECG after administration of epinephrine.of epinephrine.
3.3. Because of its strong inotropic and chronotropic Because of its strong inotropic and chronotropic effects, epinephrine causes an increased myocardial effects, epinephrine causes an increased myocardial O2 demandO2 demand
EpinephrineEpinephrine
Precautions:Precautions:4.4. Hypovolemia (replenish volume first)Hypovolemia (replenish volume first)
5.5. Diabetes mellitusDiabetes mellitus
6.6. HyperthyroidismHyperthyroidism
7.7. Prostatic hypertrophyProstatic hypertrophy
8.8. Must be protected from lightMust be protected from light
9.9. Tends to be deactivated by alkaline solutions (sodium Tends to be deactivated by alkaline solutions (sodium bicarbonate)bicarbonate)
10.10. Do not use with MAOIs or tricyclic antidepressants due Do not use with MAOIs or tricyclic antidepressants due to the danger of hypertensive crisisto the danger of hypertensive crisis
EpinephrineEpinephrine
Dose:Dose:1.1. Cardiac dosage: 1:10,000Cardiac dosage: 1:10,000
a. 1 mg q 3-5 minutes (until the heart restarts)a. 1 mg q 3-5 minutes (until the heart restarts)
b. Intermediate: 2-5 mg q 3-5 minutesb. Intermediate: 2-5 mg q 3-5 minutes
c. Escalating: 1 mg – 3 mg – 5 mg; 3 minutes apartc. Escalating: 1 mg – 3 mg – 5 mg; 3 minutes apart
d. High: 0.1 mg/kg q 3-5 minutesd. High: 0.1 mg/kg q 3-5 minutes
2.2. Infusion: Mix 1 mg in 250 ml and run at 2-10 mcg/minInfusion: Mix 1 mg in 250 ml and run at 2-10 mcg/min
3.3. Anaphylaxis and Asthma: .1-.5 mg (1:1,000) SQ or IMAnaphylaxis and Asthma: .1-.5 mg (1:1,000) SQ or IM
EpinephrineEpinephrine
Incompatible/Reactions:Incompatible/Reactions:1.1. Potentiates other sympathomimeticsPotentiates other sympathomimetics2.2. Patients on MAOIs, antihistamines, and tricyclic Patients on MAOIs, antihistamines, and tricyclic
antidepressants may have heightened effectsantidepressants may have heightened effects3.3. Sodium bicarbonate – deactivates epinephrineSodium bicarbonate – deactivates epinephrine4.4. NitratesNitrates5.5. LidocaineLidocaine6.6. AminophyllineAminophylline7.7. Don’t mix the above drugs in the same syringe with Don’t mix the above drugs in the same syringe with
epi; but can use in the same IV line – just flush epi; but can use in the same IV line – just flush between medsbetween meds
EpinephrineEpinephrine
Notes:Notes:
ONSET:ONSET: ImmediateImmediate
PEAK:PEAK: MinutesMinutes
DURATION:DURATION: Several minutesSeveral minutes
Respiratory PharmacologyRespiratory Pharmacology
GENERIC:GENERIC: IsoetharineIsoetharine
BRAND:BRAND: Bronkosol, BronkometerBronkosol, Bronkometer
CLASS:CLASS: SympathomimeticSympathomimetic
IsoetharineIsoetharine
Actions:Actions:
1. Beta 2 agonist (slight specificity); relaxes smooth 1. Beta 2 agonist (slight specificity); relaxes smooth muscle of bronchioles, vasculature, uterusmuscle of bronchioles, vasculature, uterus
IsoetharineIsoetharine
Indications:Indications:
1. Relieve bronchospasm associated with asthma, chronic 1. Relieve bronchospasm associated with asthma, chronic bronchitis, and emphysemabronchitis, and emphysema
IsoetharineIsoetharine
Contraindications:Contraindications:
1.1. Hypersensitivity to sympathomimeticsHypersensitivity to sympathomimetics
2.2. Cardiac dysrhythmiasCardiac dysrhythmias
3.3. Tachycardia and tachydysrhythmiasTachycardia and tachydysrhythmias
IsoetharineIsoetharine
Adverse Reactions:Adverse Reactions:1.1. Dose-related tachycardia, palpitations, tremors, Dose-related tachycardia, palpitations, tremors,
nervousness, peripheral vasodilation, nausea/vomiting, nervousness, peripheral vasodilation, nausea/vomiting, transient hyperglycemia, life-threatening arrhythmias; transient hyperglycemia, life-threatening arrhythmias; multiple excessive doses can cause paradoxical multiple excessive doses can cause paradoxical bronchoconstrictionbronchoconstriction
2.2. AnginaAngina
3.3. HypertensionHypertension
4.4. Headache, dizziness, anxiety, restlessness, Headache, dizziness, anxiety, restlessness, hallucinationshallucinations
IsoetharineIsoetharine
Precautions:Precautions:1.1. Use with caution in patients with diabetes, Use with caution in patients with diabetes,
hyperthyroidism, cardiovascular and cerebrovascular hyperthyroidism, cardiovascular and cerebrovascular diseasedisease
2.2. Seizure disordersSeizure disorders
3.3. Isoetharine contains acetone sodium bisulfite; a sulfite Isoetharine contains acetone sodium bisulfite; a sulfite that may cause allergic-type reactions, including that may cause allergic-type reactions, including anaphylactic symptoms in certain susceptible anaphylactic symptoms in certain susceptible individualsindividuals
IsoetharineIsoetharine
Dose:Dose:
ADULTADULT
1-2 inhalations with metered-dose inhaler1-2 inhalations with metered-dose inhaler
3-7 inhalations, via hand nebulizer q 4 hours3-7 inhalations, via hand nebulizer q 4 hours
PEDIATRICPEDIATRIC
Not recommended in children less than 12 yearsNot recommended in children less than 12 years
IsoetharineIsoetharine
Incompatible/Reactions:Incompatible/Reactions:
1. Additive adverse effects with other beta agonists1. Additive adverse effects with other beta agonists
IsoetharineIsoetharine
Notes:Notes:
ONSET:ONSET: ImmediateImmediate
PEAK:PEAK: 5-15 minutes5-15 minutes
DURATION:DURATION: 1-4 hours1-4 hours
Respiratory PharmacologyRespiratory Pharmacology
GENERIC:GENERIC: Metaproterenol SulfateMetaproterenol Sulfate
BRAND:BRAND: Alupent, MetaprelAlupent, Metaprel
CLASS:CLASS: SympathomimeticSympathomimetic
Metaproterenol SulfateMetaproterenol Sulfate
Actions:Actions:
1. Agonist for Beta 2 adrenergic receptors – acts directly 1. Agonist for Beta 2 adrenergic receptors – acts directly on smooth muscleon smooth muscle
Metaproterenol SulfateMetaproterenol Sulfate
Indications:Indications:
1. Relieve bronchospasm of COPD and Asthma1. Relieve bronchospasm of COPD and Asthma
Metaproterenol SulfateMetaproterenol Sulfate
Contraindications:Contraindications:
1.1. Hypersensitivity to sympathomimeticsHypersensitivity to sympathomimetics
2.2. HyperthyroidismHyperthyroidism
3.3. Cerebrovascular or cardiovascular disordersCerebrovascular or cardiovascular disorders
4.4. Tachycardia and tachydysrhythmiasTachycardia and tachydysrhythmias
Metaproterenol SulfateMetaproterenol SulfateAdverse ReactionsAdverse Reactions
Dose-related tachycardiaDose-related tachycardia
PalpitationsPalpitations
NervousnessNervousness
Peripheral vasodilationPeripheral vasodilation
Excessive use – lethal Excessive use – lethal arrhythmias, paradoxical arrhythmias, paradoxical bronchospasmbronchospasm
HypertensionHypertension
Tremors, headache, Tremors, headache, dizziness, anxiety, dizziness, anxiety, hallucinationshallucinations
Nausea/vomitingNausea/vomiting
Metaproterenol SulfateMetaproterenol Sulfate
Precautions:Precautions:
1.1. History of cardiovascular disease or hypertensionHistory of cardiovascular disease or hypertension
2.2. SeizuresSeizures
Metaproterenol SulfateMetaproterenol Sulfate
Dose:Dose:
ADULT:ADULT:
2-3 inhalations, q 3-4 hours2-3 inhalations, q 3-4 hours
Metered-dose inhaler or nebulizerMetered-dose inhaler or nebulizer
PEDIATRICS:PEDIATRICS:
Not recommended in children under 12 yearsNot recommended in children under 12 years
Metaproterenol SulfateMetaproterenol Sulfate
Incompatible/Reactions:Incompatible/Reactions:
1.1. Beta blockersBeta blockers
2.2. MAOIs, tricyclic antidepressantsMAOIs, tricyclic antidepressants
3.3. Potentiates other beta agonistsPotentiates other beta agonists
Metaproterenol SulfateMetaproterenol Sulfate
Notes:Notes:
ONSET:ONSET: 1 minute1 minute
PEAK:PEAK: 1 hour1 hour
DURATION:DURATION: 1-5 hours with single dose1-5 hours with single dose
2-5 hours with repeated dose2-5 hours with repeated dose
Respiratory PharmacologyRespiratory Pharmacology
GENERIC:GENERIC: Terbutaline SulfateTerbutaline Sulfate
BRAND:BRAND: Bricanyl, BrethineBricanyl, Brethine
CLASS:CLASS: SympathomimeticSympathomimetic
Terbutaline SulfateTerbutaline Sulfate
Actions:Actions:
1.1. Beta 2 agonist – has an affinity for beta 2 receptors of Beta 2 agonist – has an affinity for beta 2 receptors of bronchial, vascular, and uterine smooth musclebronchial, vascular, and uterine smooth muscle
2.2. At increased doses, beta 1 effects may occurAt increased doses, beta 1 effects may occur
Terbutaline SulfateTerbutaline Sulfate
Indications:Indications:
1.1. Relieve bronchospasm associated with asthma, Relieve bronchospasm associated with asthma, chronic bronchitis and emphysema (prevalent in chronic bronchitis and emphysema (prevalent in patients over the age of 40 or with coronary artery patients over the age of 40 or with coronary artery disease)disease)
2.2. Used in-hospital to stop pre-term laborUsed in-hospital to stop pre-term labor
Terbutaline SulfateTerbutaline Sulfate
Contraindications:Contraindications:
1.1. Hypersensitivity to sympathomimeticsHypersensitivity to sympathomimetics
2.2. Cardiac dysrhythmiasCardiac dysrhythmias
3.3. Tachycardia and tachydysrhythmiasTachycardia and tachydysrhythmias
4.4. GlaucomaGlaucoma
Terbutaline SulfateTerbutaline Sulfate
Adverse Reactions:Adverse Reactions:
1.1. Tachycardia, tremors, palpitations, nervousness and Tachycardia, tremors, palpitations, nervousness and dizzinessdizziness
2.2. Angina, PVCs, hypotension, and hypertensionAngina, PVCs, hypotension, and hypertension
3.3. Headache, anxiety, hallucinationsHeadache, anxiety, hallucinations
4.4. Nausea, vomitingNausea, vomiting
5.5. BronchospasmBronchospasm
Terbutaline SulfateTerbutaline Sulfate
Precautions:Precautions:
1.1. Used with caution to patients with a history of Used with caution to patients with a history of cardiovascular disease or hypertensioncardiovascular disease or hypertension
2.2. Seizure disordersSeizure disorders
3.3. Thyroid diseaseThyroid disease
4.4. DiabetesDiabetes
Terbutaline SulfateTerbutaline Sulfate
Dose:Dose:
ADULT:ADULT:
0.25 mg SQ; repeat in 15-20 minutes0.25 mg SQ; repeat in 15-20 minutes
2 inhalations separated by a 60 second interval with a 2 inhalations separated by a 60 second interval with a metered dose inhalermetered dose inhaler
4mg/7ml nebulizer mix4mg/7ml nebulizer mix
Terbutaline SulfateTerbutaline Sulfate
Incompatible/Reactions:Incompatible/Reactions:
1.1. Alkaline solutionsAlkaline solutions
2.2. Degrades when exposed to light for long periods of Degrades when exposed to light for long periods of timetime
Terbutaline SulfateTerbutaline Sulfate
Notes:Notes:
ONSET:ONSET: 15 minutes15 minutes
PEAK:PEAK: 30-60 minutes30-60 minutes
DURATION:DURATION: 90 minutes – 4 hours90 minutes – 4 hours
Respiratory PharmacologyRespiratory Pharmacology
GENERIC:GENERIC: Theophylline EthylenediamineTheophylline Ethylenediamine
BRAND:BRAND: AminophyllineAminophylline
CLASS:CLASS: Methylxanthine SpasmolyticMethylxanthine Spasmolytic
TheophyllineTheophylline
Actions:Actions:1.1. Beta 2 agonist; directly relaxes bronchial smooth Beta 2 agonist; directly relaxes bronchial smooth
musclemuscle
2.2. Dilates pulmonary and coronary arterioles, decreasing Dilates pulmonary and coronary arterioles, decreasing pulmonary hypertension and increasing coronary blood pulmonary hypertension and increasing coronary blood flowflow
3.3. Slight positive chronotropic and inotropic effectsSlight positive chronotropic and inotropic effects
4.4. Strengthens diaphragmatic contractions by affecting Strengthens diaphragmatic contractions by affecting intracellular calciumintracellular calcium
5.5. Mild diureticMild diuretic
TheophyllineTheophylline
Actions:Actions:6.6. Stimulates CNS vomiting centersStimulates CNS vomiting centers
7.7. Respiratory center stimulantRespiratory center stimulant
8.8. Stimulates vagal and vasomotor centers in the brain – Stimulates vagal and vasomotor centers in the brain – can lead to decreased heart rate, vasoconstriction in can lead to decreased heart rate, vasoconstriction in the brain – depends on CNS or peripheral the brain – depends on CNS or peripheral predominancepredominance
TheophyllineTheophylline
Indications:Indications:
1.1. Relieve bronchospasm associated with asthma, Relieve bronchospasm associated with asthma, chronic bronchitis, emphysema, and pulmonary edemachronic bronchitis, emphysema, and pulmonary edema
2.2. Management of CHF and pulmonary edemaManagement of CHF and pulmonary edema
TheophyllineTheophylline
Contraindications:Contraindications:
1.1. Hypersensitivity to xanthene compounds (e.g. caffeine)Hypersensitivity to xanthene compounds (e.g. caffeine)
2.2. Cardiac dysrhythmiasCardiac dysrhythmias
3.3. Tachycardia and tachydysrhythmiasTachycardia and tachydysrhythmias
TheophyllineTheophyllineAdverse ReactionsAdverse Reactions
Nausea/vomitingNausea/vomiting
HypotensionHypotension
IrritabilityIrritability
TachycardiaTachycardia
AnginaAngina
FlushingFlushing
DiarrheaDiarrhea
Increased respiratory rateIncreased respiratory rate
Cardiac arrhythmiasCardiac arrhythmias
TremorsTremors
SeizuresSeizures
PalpitationsPalpitations
HypertensionHypertension
AnorexiaAnorexia
TheophyllineTheophylline
Precautions:Precautions:1.1. Caution if patient is already taking theophylline-Caution if patient is already taking theophylline-
containing medicationscontaining medications
2.2. Caution to patients with a history of cardiovascular Caution to patients with a history of cardiovascular disease or hypertensiondisease or hypertension
3.3. Thyroid diseaseThyroid disease
4.4. Active peptic ulcerActive peptic ulcer
5.5. Hypotension may occur following rapid administrationHypotension may occur following rapid administration
6.6. May oppose the effects of beta blockersMay oppose the effects of beta blockers
TheophyllineTheophylline
Dose:Dose:
ADULT:ADULT:
Loading dose of 6 mg/kg IV infusion over 20 minutesLoading dose of 6 mg/kg IV infusion over 20 minutes
Loading dose of 1 mg/kg IV infusion over 20 minutes if the Loading dose of 1 mg/kg IV infusion over 20 minutes if the patient has had theophylline products in the last 35 patient has had theophylline products in the last 35 hourshours
TheophyllineTheophylline
Incompatible/Reactions:Incompatible/Reactions:
1.1. Incompatible with most drugsIncompatible with most drugs
2.2. Simetidine, propranolol, erythromycin, and Simetidine, propranolol, erythromycin, and troleandomycin may increase the effects of the drugtroleandomycin may increase the effects of the drug
3.3. Barbiturates, phenytoin, and smoking may decrease Barbiturates, phenytoin, and smoking may decrease blood levelsblood levels
4.4. May increase the effects of anticoagulantsMay increase the effects of anticoagulants
TheophyllineTheophylline
Notes:Notes:ONSET:ONSET: 15 minutes:15 minutes:PEAK:PEAK: 30 minutes – 1 hour30 minutes – 1 hourDURATION:DURATION: Averages 5 hoursAverages 5 hours
1.1. Common forms or oral aminophylline include:Common forms or oral aminophylline include:* Marax* Marax * Primatene* Primatene* Quibron* Quibron * Slo-Phyllin* Slo-Phyllin* Slobid* Slobid * Somophyllin* Somophyllin* Tedral* Tedral * Theo-Dur* Theo-Dur
Respiratory PharmacologyRespiratory Pharmacology
Respiratory meds are used for several Respiratory meds are used for several purposes, the most obvious is the treatment of purposes, the most obvious is the treatment of asthma.asthma.
Class includes:Class includes:1.1. Cough suppressantsCough suppressants
2.2. Nasal decongestantsNasal decongestants
3.3. AntihistaminesAntihistamines
Antiasthmatic MedicationsAntiasthmatic Medications
Asthma has two basic pathophysiologies:Asthma has two basic pathophysiologies:1.1. BronchoconstrictionBronchoconstriction2.2. InflammationInflammation
Treatment is aimed to relieve bronchospasm Treatment is aimed to relieve bronchospasm and decrease inflammation.and decrease inflammation.Specific approaches are categorized as beta 2 Specific approaches are categorized as beta 2 selective sympathomimetics, nonselective selective sympathomimetics, nonselective sympathomimetics, methylxanthines, sympathomimetics, methylxanthines, anticholinergics, glucocorticoids and anticholinergics, glucocorticoids and leukotriene antagonists.leukotriene antagonists.
Beta 2 Specific AgentsBeta 2 Specific Agents
Albuterol (Proventil, Ventolin) is the prototype of this Albuterol (Proventil, Ventolin) is the prototype of this class.class.
1.1. These agents relax bronchial smooth muscle, resulting These agents relax bronchial smooth muscle, resulting in bronchodilation and relief from bronchospasm.in bronchodilation and relief from bronchospasm.
2.2. These agents are first line therapy for acute shortness These agents are first line therapy for acute shortness of breath.of breath.
3.3. Administered via metered dose inhaler or nebulizer.Administered via metered dose inhaler or nebulizer.
4.4. Overall, these agents are very safe.Overall, these agents are very safe.
Nonselective Nonselective SympathomimeticsSympathomimetics
Stimulate both beta 1 and beta 2 receptors, as well as Stimulate both beta 1 and beta 2 receptors, as well as alpha receptors.alpha receptors.
Rarely used to treat asthma because they have the Rarely used to treat asthma because they have the undesired effects of increased peripheral vascular undesired effects of increased peripheral vascular resistance and increased risks for tachycardias and resistance and increased risks for tachycardias and other dysrhythmias.other dysrhythmias.
Agents include: epinephrine, ephedrine, and Agents include: epinephrine, ephedrine, and isoproterenolisoproterenol
Epinephrine is the only nonselective sympathomimetic in Epinephrine is the only nonselective sympathomimetic in common use today.common use today.
MethylxanthinesMethylxanthines
CNS stimulants that have additional bronchodilatory CNS stimulants that have additional bronchodilatory properties.properties.
Used only when other drugs such as beta 2 specific Used only when other drugs such as beta 2 specific agents are ineffective.agents are ineffective.
Possibly block adenosine receptors.Possibly block adenosine receptors.
Prototype is theophylline, taken orally.Prototype is theophylline, taken orally.
Aminophylline, an IV medication, is rapidly metabolized Aminophylline, an IV medication, is rapidly metabolized into theophylline and, therefore, has identical effects.into theophylline and, therefore, has identical effects.
Chief side effects: nausea/vomiting, insomnia, Chief side effects: nausea/vomiting, insomnia, restlessness, and dysrhythmiasrestlessness, and dysrhythmias
AnticholinergicsAnticholinergics
Ipratropium (Atrovent) is an atropine derivative given by Ipratropium (Atrovent) is an atropine derivative given by nebulizer.nebulizer.
Because stimulating the muscarinic receptors in the Because stimulating the muscarinic receptors in the lungs results in constriction of bronchial smooth muscle, lungs results in constriction of bronchial smooth muscle, ipratropium, a muscarinic antagonist, causes ipratropium, a muscarinic antagonist, causes bronchodilation.bronchodilation.
Ipratropium is inhaled, and has no systemic effects.Ipratropium is inhaled, and has no systemic effects.
Has an additive effect when used with beta 2 agonists.Has an additive effect when used with beta 2 agonists.
Most common side effect is dry mouthMost common side effect is dry mouth
GlucocorticoidsGlucocorticoids
Anti-inflammatory properties.Anti-inflammatory properties.
Lower the production and release of inflammatory Lower the production and release of inflammatory substances such as histamine, prostaglandins, and substances such as histamine, prostaglandins, and leukotrienes, and reduce mucus and edema secondary leukotrienes, and reduce mucus and edema secondary to decreasing vascular permeability.to decreasing vascular permeability.
May be inhaled or taken orally, as well as IV.May be inhaled or taken orally, as well as IV.
Prototype of inhaled glucocorticoid is beclomethasone.Prototype of inhaled glucocorticoid is beclomethasone.
Prototype of oral glucocorticoid is prednisone.Prototype of oral glucocorticoid is prednisone.
Administered as preventative care.Administered as preventative care.
GlucocorticoidsGlucocorticoids
When inhaled they cause few side effects.When inhaled they cause few side effects.
Side effects are due mostly to direct exposure on the Side effects are due mostly to direct exposure on the oropharynx, and gargling after taking the drug can oropharynx, and gargling after taking the drug can decrease the side effects.decrease the side effects.
Side effects from the IV administrations of Side effects from the IV administrations of methylprednisolone in emergencies are not likelymethylprednisolone in emergencies are not likely
Long periods of administration can lead to adrenal Long periods of administration can lead to adrenal suppression and hyperglycemia.suppression and hyperglycemia.
Another anti-inflammatory agent used is cromolyn (Intal), Another anti-inflammatory agent used is cromolyn (Intal), an inhaled powder.an inhaled powder.
GlucocorticoidsGlucocorticoids
Cromolyn is the safest of all antiasthma agents.Cromolyn is the safest of all antiasthma agents.
Only side effects are coughing or wheezing due to local Only side effects are coughing or wheezing due to local irritation caused by the powder.irritation caused by the powder.
Often used for preventing asthma in adults and children.Often used for preventing asthma in adults and children.
Leukotriene AntagonistsLeukotriene Antagonists
Leukotrienes are mediators released from mast cells Leukotrienes are mediators released from mast cells upon contact with allergens.upon contact with allergens.
Contribute powerfully to both inflammation and Contribute powerfully to both inflammation and bronchoconstrictionbronchoconstriction
Can either block the synthesis of leukotrienes or block Can either block the synthesis of leukotrienes or block their receptors.their receptors.
Zileuton (Zyflo) is the prototype of those that block the Zileuton (Zyflo) is the prototype of those that block the synthesis of leukotrienessynthesis of leukotrienes
Zafirlukast (Accolate) is the prototype of those that block Zafirlukast (Accolate) is the prototype of those that block their receptorstheir receptors
DRUGS USED FOR RHINITIS DRUGS USED FOR RHINITIS AND COUGHAND COUGH
Rhinitis: (inflammation of the nasal lining) Rhinitis: (inflammation of the nasal lining) comprises a group of symptoms including nasal comprises a group of symptoms including nasal congestion, itching, redness, sneezing, and congestion, itching, redness, sneezing, and rhinorrhea (runny nose).rhinorrhea (runny nose).Allergic reactions or viral infections may cause itAllergic reactions or viral infections may cause itDrugs that treat the symptoms of rhinitis and Drugs that treat the symptoms of rhinitis and cold are commonly found in over-the-counter cold are commonly found in over-the-counter remedies.remedies.Nasal decongestants, antihistamines, and cough Nasal decongestants, antihistamines, and cough suppressants are available in prescription suppressants are available in prescription medications.medications.
Nasal DecongestantsNasal Decongestants
Nasal congestion is caused by dilated and engorged Nasal congestion is caused by dilated and engorged nasal capillaries.nasal capillaries.
Drugs that constrict these capillaries are effective nasal Drugs that constrict these capillaries are effective nasal decongestants.decongestants.
Main pharmacologic classification in this functional Main pharmacologic classification in this functional category is alpha 1 agonistscategory is alpha 1 agonists
Alpha 1 agonists may be given either topically or orallyAlpha 1 agonists may be given either topically or orally
Examples of agents: phenylephrine, pseudoephedrine, Examples of agents: phenylephrine, pseudoephedrine, and phenylpropanolamine, (administered in drops or and phenylpropanolamine, (administered in drops or mist)mist)
AntihistaminesAntihistamines
Arrest the effects of histamine by blocking its receptors.Arrest the effects of histamine by blocking its receptors.
HistamineHistamine is an endogenous substance that affects a is an endogenous substance that affects a wide variety of organs systems.wide variety of organs systems.
Noted for its role in allergic reaction.Noted for its role in allergic reaction.
Histamine binds with H1 receptors to cause vasodilation Histamine binds with H1 receptors to cause vasodilation and increased capillary permeability (vasculature)and increased capillary permeability (vasculature)
In the lungs, H1 receptors cause bronchoconstrictionIn the lungs, H1 receptors cause bronchoconstriction
In the gut, H2 receptors cause an increase in gastric acid In the gut, H2 receptors cause an increase in gastric acid releaserelease
Histamine also acts as a neurotransmitter in the CNS.Histamine also acts as a neurotransmitter in the CNS.
AntihistaminesAntihistamines
Histamine is synthesized and stored in two types of Histamine is synthesized and stored in two types of granulocytes; tissue-bound mast cells and plasma-granulocytes; tissue-bound mast cells and plasma-bound basophilsbound basophils
Both types are full of secretory granules, which are Both types are full of secretory granules, which are vesicles containing inflammatory mediators such as vesicles containing inflammatory mediators such as histamine, leukotrienes, and prostaglandins, among histamine, leukotrienes, and prostaglandins, among others.others.
When cells are exposed to allergens, they develop When cells are exposed to allergens, they develop antibodies on their surfaces.antibodies on their surfaces.
On subsequent exposures, the antibodies bind with their On subsequent exposures, the antibodies bind with their specific allergen.specific allergen.
AntihistaminesAntihistamines
Secretory granules then migrate towards the cell’s Secretory granules then migrate towards the cell’s exterior and fuse with the cell membrane. Causing them exterior and fuse with the cell membrane. Causing them to release their contents.to release their contents.
Histamines are useful in our immune systems.Histamines are useful in our immune systems.
When our immune systems overreact do allergies such When our immune systems overreact do allergies such as hay fever or cedar fever send us running for the as hay fever or cedar fever send us running for the antihistaminesantihistamines
Typical symptoms of allergic reaction include most of Typical symptoms of allergic reaction include most of those associated with rhinitis.those associated with rhinitis.
Severe allergic reactions (anaphylaxis) may cause Severe allergic reactions (anaphylaxis) may cause hypotensionhypotension
AntihistaminesAntihistamines
Antihistamines are at best only a secondary drug for Antihistamines are at best only a secondary drug for treating anaphylaxis.treating anaphylaxis.
Just as there are H1 and H2 histamine receptors, there Just as there are H1 and H2 histamine receptors, there are H1 and H2 histamine receptor antagonists.are H1 and H2 histamine receptor antagonists.
Most old antihistamines were H1 receptor antagonists, Most old antihistamines were H1 receptor antagonists, newer antihistamines are H2 receptor antagonists.newer antihistamines are H2 receptor antagonists.
Chief side effect is sedation (H1), newer generation do Chief side effect is sedation (H1), newer generation do not cause this sedation effect (H2).not cause this sedation effect (H2).
First generation medications: alkylamines First generation medications: alkylamines (chlorpheniramine [Chlor-Trimeton]), ethanolamines (chlorpheniramine [Chlor-Trimeton]), ethanolamines (diphenhydramine [Benadryl])(diphenhydramine [Benadryl])
AntihistaminesAntihistamines
Other first generation antihistamines: clemastine Other first generation antihistamines: clemastine (Tavist), and phenothiazines (promethazine (Tavist), and phenothiazines (promethazine [Phenergan]).[Phenergan]).
Some antihistamines also have significant anticholinergic Some antihistamines also have significant anticholinergic properties: promethazine and dimenhydrinate properties: promethazine and dimenhydrinate (Dramamine), used for motion sickness.(Dramamine), used for motion sickness.
Second generation antihistamines include: terfenadine Second generation antihistamines include: terfenadine (Seldane), loratadine (Claritine), cetirizine (Zyrtec, and (Seldane), loratadine (Claritine), cetirizine (Zyrtec, and fexofenadine (Allegra).fexofenadine (Allegra).
These agents do not cross the blood-brain barrier and These agents do not cross the blood-brain barrier and therefore do not cause sedation.therefore do not cause sedation.
Cough SuppressantsCough Suppressants
Coughing is a complex reflex that depends on functions Coughing is a complex reflex that depends on functions in the CNS, the PNS, and the respiratory muscles.in the CNS, the PNS, and the respiratory muscles.
It is a defense mechanism that aids the removal of It is a defense mechanism that aids the removal of foreign particles like smoke and dust.foreign particles like smoke and dust.
In general, treating a productive cough is not In general, treating a productive cough is not appropriate, as it is performing a useful function.appropriate, as it is performing a useful function.
An unproductive cough, usually results from an irritated An unproductive cough, usually results from an irritated oropharynx and can be troublesome.oropharynx and can be troublesome.
The three classifications of cough suppressants include The three classifications of cough suppressants include one that is supported by evidence and two that are not.one that is supported by evidence and two that are not.
Cough SuppressantsCough Suppressants
AntitussivesAntitussives1.1. Suppress the stimulus to cough in the CNS.Suppress the stimulus to cough in the CNS.
2.2. This functional class includes two specific This functional class includes two specific pharmacologic types:pharmacologic types:
a. Opioidsa. Opioids
b. Nonopioidsb. Nonopioids
3.3. Two most common opioid antitussives are codeine and Two most common opioid antitussives are codeine and hydrocodonehydrocodone
4.4. Both inhibit the stimulus for coughing in the brain but Both inhibit the stimulus for coughing in the brain but also produce varying degrees of euphoriaalso produce varying degrees of euphoria
Cough SuppressantsCough Suppressants
5.5. The nonopioid antitussives do not have the potential The nonopioid antitussives do not have the potential for abuse.for abuse.a. Dextromethoraphan a. Dextromethoraphan b. Diphenhydramineb. Diphenhydraminec. Benzonatate (Tessalon)c. Benzonatate (Tessalon)Expectorants:Expectorants: intended to increase the productivity of intended to increase the productivity of coughcoughMucolytics:Mucolytics: make mucus more watery and easier to make mucus more watery and easier to cough upcough upLittle data supports the effectiveness of either of these Little data supports the effectiveness of either of these approaches to cough suppressionapproaches to cough suppression