respiratory pharmacology

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RESPIRATORY RESPIRATORY PHARMACOLOGY PHARMACOLOGY

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Page 1: Respiratory Pharmacology

RESPIRATORY RESPIRATORY PHARMACOLOGYPHARMACOLOGY

Page 2: Respiratory Pharmacology

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.

Page 3: Respiratory Pharmacology

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.

Page 4: Respiratory Pharmacology

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.

Page 5: Respiratory Pharmacology

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.

Page 6: Respiratory Pharmacology

Bronchial Asthma Bronchial Asthma

Page 7: Respiratory Pharmacology

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.

Page 8: Respiratory Pharmacology

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.

Page 9: Respiratory Pharmacology

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.

Page 10: Respiratory Pharmacology

Bronchial AsthmaBronchial Asthma

Page 11: Respiratory Pharmacology

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.

Page 12: Respiratory Pharmacology

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).

Page 13: Respiratory Pharmacology

TERIMA KASIH

Page 14: Respiratory Pharmacology

Respiratory PharmacologyRespiratory Pharmacology

GENERIC:GENERIC: AlbuterolAlbuterol

BRAND:BRAND: Proventil, VentolinProventil, Ventolin

CLASS:CLASS: SympathomimeticSympathomimetic

Page 15: Respiratory Pharmacology

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

Page 16: Respiratory Pharmacology

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

Page 17: Respiratory Pharmacology

AlbuterolAlbuterol

Contraindications:Contraindications:1.1. Hypersensitivity to sympathomimeticsHypersensitivity to sympathomimetics

2.2. Cardiac dysrhythmiaCardiac dysrhythmia

3.3. Tachycardia and tachydysrhythmiasTachycardia and tachydysrhythmias

Page 18: Respiratory Pharmacology

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

Page 19: Respiratory Pharmacology

AlbuterolAlbuterol

Precautions:Precautions:1.1. DiabetesDiabetes

2.2. HyperthyroidismHyperthyroidism

3.3. Cerebrovascular diseaseCerebrovascular disease

4.4. Seizure disordersSeizure disorders

Page 20: Respiratory Pharmacology

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

Page 21: Respiratory Pharmacology

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

Page 22: Respiratory Pharmacology

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

Page 23: Respiratory Pharmacology

Respiratory PharmacologyRespiratory Pharmacology

GENERIC:GENERIC: EpinephrineEpinephrine

BRAND:BRAND: AdrenalinAdrenalin

CLASS:CLASS: Sympathomimetic/Sympathomimetic/CatecholamineCatecholamine

Page 24: Respiratory Pharmacology

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

Page 25: Respiratory Pharmacology

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

Page 26: Respiratory Pharmacology

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

Page 27: Respiratory Pharmacology

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

Page 28: Respiratory Pharmacology

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

Page 29: Respiratory Pharmacology

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

Page 30: Respiratory Pharmacology

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

Page 31: Respiratory Pharmacology

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

Page 32: Respiratory Pharmacology

EpinephrineEpinephrine

Notes:Notes:

ONSET:ONSET: ImmediateImmediate

PEAK:PEAK: MinutesMinutes

DURATION:DURATION: Several minutesSeveral minutes

Page 33: Respiratory Pharmacology

Respiratory PharmacologyRespiratory Pharmacology

GENERIC:GENERIC: IsoetharineIsoetharine

BRAND:BRAND: Bronkosol, BronkometerBronkosol, Bronkometer

CLASS:CLASS: SympathomimeticSympathomimetic

Page 34: Respiratory Pharmacology

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

Page 35: Respiratory Pharmacology

IsoetharineIsoetharine

Indications:Indications:

1. Relieve bronchospasm associated with asthma, chronic 1. Relieve bronchospasm associated with asthma, chronic bronchitis, and emphysemabronchitis, and emphysema

Page 36: Respiratory Pharmacology

IsoetharineIsoetharine

Contraindications:Contraindications:

1.1. Hypersensitivity to sympathomimeticsHypersensitivity to sympathomimetics

2.2. Cardiac dysrhythmiasCardiac dysrhythmias

3.3. Tachycardia and tachydysrhythmiasTachycardia and tachydysrhythmias

Page 37: Respiratory Pharmacology

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

Page 38: Respiratory Pharmacology

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

Page 39: Respiratory Pharmacology

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

Page 40: Respiratory Pharmacology

IsoetharineIsoetharine

Incompatible/Reactions:Incompatible/Reactions:

1. Additive adverse effects with other beta agonists1. Additive adverse effects with other beta agonists

Page 41: Respiratory Pharmacology

IsoetharineIsoetharine

Notes:Notes:

ONSET:ONSET: ImmediateImmediate

PEAK:PEAK: 5-15 minutes5-15 minutes

DURATION:DURATION: 1-4 hours1-4 hours

Page 42: Respiratory Pharmacology

Respiratory PharmacologyRespiratory Pharmacology

GENERIC:GENERIC: Metaproterenol SulfateMetaproterenol Sulfate

BRAND:BRAND: Alupent, MetaprelAlupent, Metaprel

CLASS:CLASS: SympathomimeticSympathomimetic

Page 43: Respiratory Pharmacology

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

Page 44: Respiratory Pharmacology

Metaproterenol SulfateMetaproterenol Sulfate

Indications:Indications:

1. Relieve bronchospasm of COPD and Asthma1. Relieve bronchospasm of COPD and Asthma

Page 45: Respiratory Pharmacology

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

Page 46: Respiratory Pharmacology

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

Page 47: Respiratory Pharmacology

Metaproterenol SulfateMetaproterenol Sulfate

Precautions:Precautions:

1.1. History of cardiovascular disease or hypertensionHistory of cardiovascular disease or hypertension

2.2. SeizuresSeizures

Page 48: Respiratory Pharmacology

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

Page 49: Respiratory Pharmacology

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

Page 50: Respiratory Pharmacology

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

Page 51: Respiratory Pharmacology

Respiratory PharmacologyRespiratory Pharmacology

GENERIC:GENERIC: Terbutaline SulfateTerbutaline Sulfate

BRAND:BRAND: Bricanyl, BrethineBricanyl, Brethine

CLASS:CLASS: SympathomimeticSympathomimetic

Page 52: Respiratory Pharmacology

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

Page 53: Respiratory Pharmacology

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

Page 54: Respiratory Pharmacology

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

Page 55: Respiratory Pharmacology

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

Page 56: Respiratory Pharmacology

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

Page 57: Respiratory Pharmacology

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

Page 58: Respiratory Pharmacology

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

Page 59: Respiratory Pharmacology

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

Page 60: Respiratory Pharmacology

Respiratory PharmacologyRespiratory Pharmacology

GENERIC:GENERIC: Theophylline EthylenediamineTheophylline Ethylenediamine

BRAND:BRAND: AminophyllineAminophylline

CLASS:CLASS: Methylxanthine SpasmolyticMethylxanthine Spasmolytic

Page 61: Respiratory Pharmacology

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

Page 62: Respiratory Pharmacology

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

Page 63: Respiratory Pharmacology

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

Page 64: Respiratory Pharmacology

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

Page 65: Respiratory Pharmacology

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

Page 66: Respiratory Pharmacology

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

Page 67: Respiratory Pharmacology

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

Page 68: Respiratory Pharmacology

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

Page 69: Respiratory Pharmacology

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

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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

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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.

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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.

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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.

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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

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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

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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.

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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.

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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.

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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

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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.

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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)

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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.

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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.

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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

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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])

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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.

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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.

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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

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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