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196 Cards in this Set

  • Front
  • Back
Cor pulmonale
right ventricle failure
Hyperpnea
abnormally deep breathing
Hypopnea
shallow breathing
Orthopnea
difficulty breathing in supine position
Dyspnea
difficulty breathing
Hypoxemia
deficiency of O2 conc. in the blood
Hypercapnia
greater than normal amts. of CO2 in the blood
Acidosis
inc. conc. of H+ ions & retention of CO2 (pH < 7.35)
Alkalosis – excess of bicarbonate ions (pH > 7.45). Loss of CO2 & hyperventilation.
excess of bicarbonate ions (pH > 7.45). Loss of CO2 & hyperventilation.
Hematocrit
A measure of the packed cell volume of red cells expressed as a percentage of the total blood volume
Hemoglobin
carries O2 to the cells from the lungs and CO2 away from the cells to the lungs
Upper Respiratory Tract Contains
Nose
Nasal cavity
Paranasal sinuses
Pharynx
The Pharynx..
*Conducts air to the lower respiratory tract
*Conveys food to the esophagus
Lower Respiratory Tract Contains
Larynx (voice box)
Trachea (windpipe)
Bronchi
Bronchioles
Alveoli of the lungs
The right lung has..
3 lobes and is higher than the left due to the liver
The left lung has....
2 lobes because of the heart
Goals of COPD
1.) Smoking cessation
2.) Treatment & Prevention of acute exacerbations
3.) Reduction in rate of progression of disease (stop smoking)
4.) Should receive influenza and pneumococcal vaccinations as standard-of-care
What is Chronic Bronchitis
* Chronic or recurrent excess mucous production with cough
* Cough occurs most days during a 3 month period for at least 2 consecutive years.
* < o2 Blue Bloater
* Always have condition but symptoms may get better
* Acute exacerbations is usually due to an infection
What is Emphysema
* Abnormal Permanent enlargement of the air spaces distal to the terminal bronchiole with destruction of their wall and without obvious fibrosis (loss of elasticity)
* Normal inhalation, difficult exhalation
* < CO2 Pink Puffer
Age of Emphysema
60+
Dyspnea with Emphysema
Severe
Cough with Emphysema
After dyspnea
Sputum with Emphysema
Scanty, Mucoid
Infection with Emphysema
Less Common
Resp Episode with Emphysema
Often terminal
Chest Film with Emphysema
Increase in diameter
PaCO2 with Emphysema
35-40
PaO2 with Emphysema
65-75
Hct% with Emphysema
35-45
Age with Bronchitis
50+
Dyspnea with Bronchitis
Mild
Cough with Bronchitis
Before Dyspnea
Sputum with Bronchitis
Copious
Infection with Bronchitis
Frequent
Resp Episode
Repeated
Chest Film
Large Heart
PaCO2
50-60
PaO2
45-60
Hct%
50-60
Rest with Emphysema
None or Mild
Cor Pulmonale with Emphysema
Rare
Diffusion Cap with Emphysema
Decreased
Classification with Emphysema
Pink Puffers
Rest with Bronchitis
Mod-Severe
Cor Pulmonale with Bronchitis
Common
Diffusion Cap with Bronchitis
Slightly Decreased
Classification with Bronchitis
Blue Bloaters
Acute Respiratory Failure
* Change in arterial blood gases
* PaO2 < 50mm Hg or a PaO2 dec of 10-15 mm Hg that dec. serum pH to 7.3 or less
Most common cause of acute respiratory failure
acute exacerbation of bronchioles with inc. in volume and viscosity of sputum
Pathophysiology of Chronic Bronchitis
1 - Continual Bronchial Irritation

2 - Hyperplasia/Hypertrophy

3 - Tracheobronchial Mucus Secretion

4 - Inflammation, narrowing of lumen, fibrosis

5 - Obstruction (small airway changes)

6 - Hypoxemia

which leads to Pulmonary HTN OR Erythropoiesis

and Pulmonary HTN leads to Cor Pulmonale
Pathophysiology of Emphysema
1 - Smoking

2 - Macrophage alveolitis which leads to Inc. neutrophils

3 - Dec. Protease inh., Inc. Proteases (elastase)

4 - Lung destruction loss of elastic recoil
What happens in the early stages of COPD? (6 things)
1) Wheezing at rest and prolonged expiratory phase
2) Diminished breath sounds
3) Reduced rib cage expansion
4) Hyperresonance of the lungs
5) Breathlessness
6) Cough (Usually productive of purulent sputum)
What happens in the advanced stages of COPD? (7 things)
1) Pulmonary circulation
2) Right heart (Right ventricular dilation and enlargement may occur resulting in cor pulmonale)
3) Respiratory muscles
4) Persistent alveolar hypoxia
5) Barrel chest
6) Weight loss
7) Hypercapnia
Force Expiratory Volume (FEV1) in NONSMOKERS Begins...
FEV1 in nonsmokers without respiratory disease begins an annual decline at about age 35
Force Expiratory Volume (FEV1) - rate of loss in non smokers
normally is about 25-35 ml each year.
Force Expiratory Volume (FEV1) in smokers...
* Annual decline in heavy smokers or susceptible people can be up to 100 ml annually
* Although lung function occurs rapidly there is a reserve which delays the onset of symptoms
* Symptoms may not occur until age 50
* Dypsnea with effort may not occur until age 60
Diagnosis of COPD - Spirometry
Involves the measurement of lung volumes and capacities or pulmonary function test.
Diagnosis of COPD - Chest radiographs
Not sensitive to detect mild COPD
Diagnosis of COPD -Arterial blood gases
Not necessary if stable with no apparent distress (monitor in patients with stage I-II COPD because of hypoxemia)
Hallmark of COPD &
Severity of COPD
Hallmark of COPD is a decrease in FEV1 in forced vital capacity (FVC) ratio to below 75% on spirometry
Severity of COPD is usually based on FEV1 findings alone
Drugs used in COPD
* Anticholinergics (Ipatropium, Tiotropium, Atropine)
* Via nebulizer or MDI
* Less systemic side effects than that of beta agonist and has greater improvement on PFT’s.
anticholinergics used in COPD have a
Slower onset of action than beta agonist.
Do NOT use anticholinergics as...
PRN use as schedule dosing .
For an acute COPD attack use...
beta2 agonist (Xopenex has only R isomer which helps avoid heart issues esp. in children).
For a chronic COPD use...
Ipatropium and a short acting beta2 agonist as a rescue inhaler.
If COPD is still not under control use....
Ipatropium with long acting beta2 agonist (Salmeterol) and a short acting rescue (Albuterol).
1st drug used in acute COPD attacks
Beta2 Agonist (Albuterol, Levalbuterol, Salmeterol)

* Use levalbuterol because only has R isomer
Another COPD drug
Methylxanthines (Theophylline)
Lastly you can also use _________ for COPD
Glucocorticoids (IV, or inhaled)
Glucocorticoids used IV
Methylprednisolone, hydrocortisone, cortisone, dexamethasone
Glucocorticoids used PO for COPD
Hydrocortisone, prednisone, methylprednisolone, triamcinolone & dexamethasone
Glucocorticoids used Inhaled for COPD
Triamcinolone, beclomethasone & Flunisolide
Leukotriene Antagonist
– block the release of leukotrienes in the lungs. Inflammation causes an inc. in leukotrienes, substances that constitute the slow-reacting substance of anaphylaxis (SRS-A)
Methylxanthines (Theophylline) –
inc. cyclic AMP to inhibit breakdown of sensitized mast cells that stimulate the release of histamine, serotonin and SRS-A
Mast Cell Stabilizers –
inhibit the release of histamine from mast cells to reduce allergic effects
Sympathetic Agonist –
stimulate sympathetic systems to decrease mucus secretions & relax bronchial muscle spasms
Corticosteroids –
produce an anti-inflammatory effect and reduce mucus secretions & tissue histamine
Anticholinergic –
reverse effects of ANS on pulmonary tree and smooth muscle
Symptoms of Asthma
1) Breathlessness and tightness of chest
2) Wheezing
3) Dypsnea
4) Cough
Test for lung function in Asthma
1) Forced expiratory volume (FEV)
2) Peak expiratory flow rate (PEFR)
Exercise Induced Bronchospasm
1) Starts immediately after exercise
2) Peaks in 5-10 minutes
3) Resolves in 20-30 minutes
4) Use beta2 agonist immed. Before exercise or Cromolyn inhaled 15 min. before exercise prophylacticly.
Step 1 Mild Intermittent Asthma
1) Treated on a PRN basis. No long term meds are needed.
2) Acute attacks treated with a short acting beta2 agonist.
3) If needed < twice weekly; nocturnal sx < 2 x mo; PEF/FEV > 80% predicted, PEF variability < 20% go to step 2
Step 2 Mild Persistent Asthma
1) Long term control
2) Quick-relief
a. 1st Long term control low dose with glucocort. and with beta2 agonist.
b. 2nd cromolyn and leukotriene rec. antagonist
3) Sx > 2 x wk, nocturnal sx > 2 x mo, PEF/FEV > 80% predicted, PEF variability 20-30%
Step 3 Moderate Persistent Asthma
1) Inhale medium dose glucocort or low dose glucocort with long-acting inhaled beta2 agonist (Salmeterol) with short acting beta2 agonist
2) Low dose glucocorticoid
a. Leukotriene receptor antagonist
b. Theophylline SR
c. Long-acting beta2 agonist
3) Sx daily, nocturnal awakenings at least 1 x wk, PEF/FEV > 80% of predicted PEF variability > 30%

If pt is using short acting beta2 agonist once daily move to step 4
Step 4 Severe Persistent Asthma
1) High dose inhaled glucocort. w/ long-acting beta2 agonist. If needed an oral glucocort. can be added and for breakthrough add short acting beta2 agonist
2) May try step down tx once sx are managed
3) Continuous sx, frequent nocturnal awakenings and exacerbations, PEF/FEV < 60% predicted PEF variability > 30%
Acute Severe Exacerbations in Asthma
1) Hospitalization may be required. Use nebulizer or mdi beta2 agonist
2) If pt. is unconscious or cannot generate PEFR SQ Epi should be given
3) If no response to beta2 agonist a glucocort (IV methylprednisolone or PO prednisone) should be given
4) Maintain O2 saturation above 95%
Zone System for Monitoring Tx
Green, Yellow and Red zone
Green Zone
Pt has no Sx and has a PEFR greater than 80% of their personal best. Control is good
Yellow Zone
Beta2 agonist if this does not work use a short course (4 days) of oral glucocorticoid.
Red Zone
Sx occur at rest or interfere with activities and PEFR is less than 50% of personal best.
Beta2 agonist inhaled immed. if remains below 50% seek medical attention.
Most asthma drugs are given...
via inhalation
1) Delivers drug directly to site
2) Systemic effects are minimized
3) Relief of acute attack is rapid.
3 kinds of inhalation devices
Inhalation Devices
1) Metered-dose inhalers
a. Chlorofluorocarbons (CFC’s)
b. Hydrofluoalkane (HFA’s)
2) Dry-powder inhalers
3) Nebulizers
Metered-dose inhalers (MDI)–
Releases a fixed amount of drug with each actuation
Only 10% reaches the lungs (use spacers esp. with glucocorticoids)
Chlorofluocarbons (CFC’s)
Hydrofluoralkane (HFA’s)
Dry-powder inhalers (DPI)
Delivers dry micronized powder directly into the lungs
No propellant is employed
Delivers more drug into the lung 20%
Nebulizers
– Converts drug soln. into a mist much finer than produced with inhalers
Some beta2 agonist may not work as an inhaler because drug will be delivered slower, bronchioles dilate slowly and gains deeper access.
Drugs for Asthma - 2 main classes
1) Anti-inflammatory agents (glucocort. & Cromolyn)
2) Bronchodilators (beta2 agonist)
Drugs for Asthma - other classes
1) Methylxanthines
2) Anticholinergic
3) Leukotriene modifiers
4) Monoclonal antibody
Glucocorticoids for Asthma
Most effective (inhalation, PO, IV)
Used on a fixed schedule not PRN
Glucocorticoids for Asthma (what do they do to inflammation, synthesis & Infiltration)
* Suppresses inflammation reducing bronchial activity
* Decreases synthesis and the release of inflammatory mediators (leukotrienes, histamine, prostaglandins)
* Decreased infiltration & activity of inflammatory cells (eosinophils, leukocytes)
Glucocorticoids for Asthma (what do they do to edema & airway mucus)
* Decreased edema of the airway mucosa (secondary to a dec. in vascular permeability)
* Decrease airway mucus production and inc. the number of beta2 rec. as well as their responsiveness to beta2 agonist.
Inhaled Glucocorticoids
1st line Tx used in pts. w/ moderate-severe asthma used daily not PRN.
6 glucocorticoids for Asthma
1) Beclomethasone (QVAR, Beconase) HFA
2) Budesonide (Pulmicort) Nebulizer and DPI
3) Flunisolide (Aerobid) *CFC
4) Fluticasone (Flovent) HFA
5) Mometasone (Asmanex) DPI
6) Triamcinolone (Azmacort) *CFC
If it is a CFC...
use a spacer device
A) Increased amount of drug delivered to site
B) Reduce amt. deposited in oropharynx
C) HFA do not need spacer b/c the drops deposited are much smaller
What should you use before a glucocorticoid?
****Using Beta-2 agonist 5 min. BEFORE using a glucocort so it can penetrate deeper into the lungs.****
Precautions/Adverse Effects of Glucocorticoids... ( 7 things)
Even at high doses adverse effects are minimal but watch for adrenal suppression and bone loss.
1) Use lowest dose possible
2) Intake adequate amount of Ca+ & Vit D
3) Participate in weight bearing exercise
4) May slow growth in children
5) Prolonged use can cause glaucoma and cataracts
6) Gargle after use and/or use spacer to avoid oropharryngeal candidiasis & dysphonia.
7) Hyperglycemia
Oral Glucocorticoids
1) Prednisone, Prednisolone, Fludrocortisone (Florinef)
Reserve oral glucocorticoids for...
pts. w/ severe asthma
Use briefly...
for acute uncontrolled asthma at high doses for short periods of time.

Withdraw tx use tapering dose
May retard bone growth. Caution in pts. with diabetes (esp. during long term use)
Increased risk for peptic ulcer disease
Adverse effects of oral glucocorticoids
1) Adrenal suppression
2) Sodium retention and potassium loss (Florinef)
3) Osteoporosis
4) Hyperglycemia
5) Peptic ulcer dz.
6) Suppression of growth in young people
Prednisone MOA
Decreased inflammation by suppression of migration of leukocytes and reversal of increased capillary permeability
Prednisone Pharmacokinetics
Hepatically metabolized
Half-life 2.5-3.5 h
Inhalation only for chronic use not PRN
Taper oral dose if use for longer than 2 weeks
Take in the morning with food
Prednisone > effect toxicity
Use of NSAIDS may increase GI ulceration
Prednisone < effect toxicity
Barbiturates
Phenobarbital
Rifampin
Salicylates
Vaccines
Bronchodilators
Albuterol, Epinephrine, Formoterol, Isoetherine, Isoproterenol, Levalbuterol, Metaproterenol, Pirbuterol, Salmeterol, Terbutaline
Albuterol: Adrenergic rc, Isoproterenol
(min), DOA (hours)
Beta 1 < Beta 2, < 5, 3-8
Epinephrine: Adrenergic rc, Isoproterenol (min), DOA (hours)
Alpha, Beta 1 & 2, 1-5, 1-3
Formoterol: Adrenergic rc, Isoproterenol (min), DOA (hours)
Beta 1 < Beta 2, 3-5, 12
Isoetherine: Adrenergic rc, Isoproterenol (min), DOA (hours)
Beta 1 < Beta 2, < 5, 1-3
Levalbuterol: Adrenergic rc, Isoproterenol (min), DOA (hours)
Beta 1 < Beta 2, 10-17, 5-6
Metaproterenol: Adrenergic rc, Isoproterenol (min), DOA (hours)
Beta 1 < Beta 2, 5-30, 2-6
Pirbuterol: Adrenergic rc, Isoproterenol (min), DOA (hours)
Beta 1 < Beta 2, < 5, 5
Salmeterol: Adrenergic rc, Isoproterenol (min), DOA (hours)
Beta 1 < Beta 2, 5-14, 12
Terbutaline: Adrenergic rc, Isoproterenol (min), DOA (hours)
Beta 1 < Beta 2, 5-30, 3-6
What does a Beta2 Agonist do?
* > Heart rate (esp. if non-selective beta agonist)
* > Blood pressure (esp. if non-selective beta agonist)
* RBC’s pour into the circulation from the spleen
* Blood flow shifts to skeletal muscle
* > Blood glucose
* Bronchioles and pupils dilate
Nonselective Epinephrine
* Bronkaid Mist, Primatene Mist
* Bronchial asthma, bronchitis, prevention of bronchospasm
Nonselective Epinephrine - Pharmacokinetics
* Inhalation onset 3-5 min, SQ 6-15 min, IM variable
* Duration 1-3 hours
* Maximum 12 inhalations/24 hours
* Metabolized at sympathetic nerve endings
* Excreted in kidneys
Nonselective Epinephrine Important info for person taking..
* Do not administer epi. and other beta adrenergic agents concurrently, allow 4 h between doses
* Teach pt. to take pulse rate before inhalation tx
* Relief within 20 min.
* Emergency self inject with epi. SQ
Nonselective Beta Agonist Isoproterenol
Bronchial asthma, bronchitis, emphysema, (cardiac arrest, AV block)
Nonselective Beta Agonist Isoproterenol - Pharmacokinetics
* inhalation onset 2-5 min., SL 15-30 min, IV immediate
* Duration 0.5-2 hours
* Metabolized in the liver, lungs
* Excreted by the kidneys
Nonselective Beta Agonist Isoproterenol - Pharmacodynamics
* beta 1 and beta 2 agonist, main action on bronchial smooth muscle and heart,
* > blood glucose
Isoproterenol - CAUTION
* arrhythmias, coronary insufficiency, HTN, hyperthyroidism, diabetes
* Allow 1-5 min between inhalations
* Rinse mouth after use
* Do not use if a precipitate or discoloration occurs in vial.
Inhaled Short Acting Beta2 Agonist - 4 kinds
* Albuterol (Proventil HFA, Ventolin HFA, ProAir HFA)
* Bitolterol (Tornalate)
* Levalbuterol (Xopenex nebules, Xopenex HFA)
* Pirbuterol (Maxair)
Inhaled Short Acting Beta2 Agonist (3 things)
1) Effect almost immed. & persist up to3-5 hours. Long acting persist up to 12 hours.
2) Taken PRN or for exercise induced asthma
3) For severe acute attack use a nebulizer (MDI can still be very effective)
Inhaled Short Acting Beta2 Agonist - Adverse Effects
Generally well tolerated (tachycardia, angina & tremor)
Albuterol - MOA
* Beta 2 specific
* Stimulates enzyme adenyl cyclase to produce cyclic 3’5’ AMP relaxing smooth muscle of bonchi, uterus and blood vessels.
Albuterol - Pharmacokinetics
* 1-2 puffs q 4-6 hours
* Inhalation onset 5-15 min, PO 15-30 min
* Duration 3-6 hours
* Hepatically metabolized
* Excreted kidneys, feces
Albuterol - Drug Interactions
* Similar to Isoproterinol
* MOAI
* Epinephrine
* Other inhaled sympathomimetics
* Tricyclic antidepressants
Albuterol Management
* Smoking cessation
* Avoid caffeine
* Foul taste will gradually disappear
* Rinse mouth after inhalation
* Excessive use may cause paradoxical bronchospasm
* Do NOT add OTC drugs to regimen, NO OTC (Primatine Mist, Bronkaid Mist)
* Report: chest pain, extreme dizziness, severe headache, palpitations, tachycardia, HTN
Inhaled Long Acting Beta2 Agonist (2 kinds)
* Formoterol (Foradil Aerolizer) – Works w/n 1-3 min.
*Salmeterol (Servent Diskus) – Works w/n 10-30 min.

1) Dosing done on a fixed schedule not PRN.
2) They are NOT 1st line of tx and should NOT be given alone but given in combo with glucocorticoid
Oral Beta2 Agonist (2 kinds)
* Albuterol (Proventil, Volmax)
* Terbutaline (Brethine)
Only used for long term control because effects are too slow.
Are NOT 1st line tx
Should not be used alone
Oral Beta2 Agonist - Adverse Effects
1) Selectivity is not 100% and will still activate some beta1 rec. in the heart. Pt. should ALWAYS report chest pain and inc. heart rate.
2) Can cause tremor by stimulating beta2 rec. in skeletal muscle and will dec. with inc. use.
Combo Glucocort/Beta2 Agonist
* Fluticasone (glucocort) & Salmeterol (long-acting beta2 agonist) is in Advair Diskus (DPI)
* Approved for maintenance in adult and children at least 12 years of age.
* Make sure pt. understands how to use
* Make sure to tell pt. that there is no taste (Some pts. will continue activating device because they think they are not receiving medication because there is no taste)
Cromolyn (Mast Cell Stabilizer)
Cromolyn (Intal), Nedocromil (Tilade MDI), Nasalcrom nasal spray
Cromolyn (Mast Cell Stabilizer) - MOA
* Inhibits release of mediators from mast cells including histamine and < number of eosinophils
* Prophylactic use not acute attack. Reduces frequency/severity of attacks.
* It suppresses inflammation by stabilizing the mast cell cytoplasmic membrane preventing the release of histamine, eosinophils, macrophages & other inflammatory cells
* It is NOT a bronchodilator
Cromolyn Sodium - Pharmacokinetics
* Only 8% absorbed by the lungs, no systemic effects & unchanged in the urine.
* Onset of action 15 minutes
* Duration 4-6 hours
Cromolyn Sodium - Contraindications
* Do not use in acute attacks
* Impaired hepatic/renal function
Cromolyn Sodium Management
* > fluid intake
* Take at regular intervals
* Takes 2-4 weeks for full effect
* Not for acute attack
* Use with steroid inhaler
Anticholinergics ( 2 kinds)
* Ipratropium (Atrovent HFA, Combivent & DuoNeb)
* Tiotropium (Spiriva) Long acting
* Act through blockade of muscarinic receptors in the bronchi causing bronchodilation. ACh antagonist
Ipatropium Pharmacokinetics
* 2 puff qid (max 12 puffs/24 h)
* Inhalation onset 15 min, peak 1-2 h
* Not for occasional use; do not change dose
* Duration 3-6 h
* Half-life 2 h
Ipatropium Bromide - Adverse Effects
Cough, Nervousness, dry mouth, hoarseness
Ipatropium Bromide - Contraindications
* Hypersensitivity to atropine and peanuts
* Glaucoma
* Bladder neck obstruction
* Pedi safety < 12 y/o not established
Metylxanthines ( 2 kinds)
1) Theophylline (Theo-24, Uniphyl)
2) Aminophylline (Truphylline)
Asthma, chronic bronchitis, emphysema
Metylxanthine - MOA
* Blocks phosphodiesterase which inc. tissue concentrations of cAMP which stimulates catecholamine stimulation of lipolysis, glycogenolysis and gluconeogenesis and induces release of epi.
Theophylline has a....
narrow Tx range, given orally, NO effect by inhalation
Theophylline - Pharmacokinetics
* onset 30-60 min.
* Half-life adults 8 h, pedi 4 h
* Duration 24 h
* Hepatically metabolized to caffeine
* Excreted by kidneys
Theophylline - Adverse Effects
* Life threatening – respiratory arrest, ventricular tachycardia
* Common – tachypnea, palpitations, sinus tachycardia, nervousness, restlessness, insomnia, anorexia
Theophyllilne Factors > therapeutic effect
* Age
* Erythromycin, cimetidine, ciprofloxacin
* Disease – cirrhosis, pulmonary edema, CHF, severe COPD
Theophyllilne Factors < therapeutic effect
* Adolescence
* Phenobarbital, phenytoin, tobacco, marijuana
* High protein diet
Theophylline - Contraindications
* Hypersensitivity
* Peptic ulcer disease
* Cardiovascular disease
* Seizure disorder
Theophylline - management
* > Fluid intake to < secretion viscosity
* Smoking cessation
* Serum drug levels q 6-12 mo if asymptomatic
Theophylline - overdose
* No known antidote
* < drug absorption, activated charcoal, gastric lavage
Leukotriene Modifiers
Suppress effects of leukotriene and decrease bronchoconstriction, inflammation, edema, mucus secretion and recruitment of eosinophils.

1) Zileuton (Zyflo)
2) Zafirlukast (Accolate)
3) Montelukast (Singulair)
4) Amalizumab (Xolair)
Zileuton (Zyflo)
* Blocks leukotriene synthesis
* Prophylactic tx not for acute attack
* Is metabolized by CYTP450 so if combined with theophylline can increase theophylline levels (can also inc levels of warfarin & propranolol)
* Use in adjunct with glucocort. or beta2 agonist
* Can cause liver damage and inc levels of alanine aminyltransferase (ALT) activity
Zafirlukast (Accolate)
– Anti-inflammatory leukotriene rec. antagonist which dec. bronchoconstriction but is less effective than beclomethasone
* Approved for maintenance tx for asthma for children 5 yr. and older.
* Food reduces absorption by 40% give 1 hr. AC or 2 hr. PC.
* Hepatic metabolism so check LFT’s and ALT.
* Inhibits CYTP450 (watch theophylline and warfarin levels)
Montelukast (Singulair)
* (tabs, chewable, granules)
* MOA same as Zarfirlukast
* Not for quick relief. Taken HS
* Approved for pts. over 1 yr. of age
* Less effective than inhaled glucocort.
* Protein bound and metabolized by CYTP450
* No liver damage, no serious drug interactions (does NOT inc. levels of warfarin or theophylline)
Amalizumab (Xolair)
* Monoclonal antibody
* Rarely used because of anaphylaxis and cancer
* Given SQ and may cost $10,000/yr
Tuberculosis
2 billion people infected and kills more people than AIDS and malaria combined.
Tuberculosis is cause by
Mycobacterium tuberculosis and may have no sx.. However, when the disease is active morbidity can be high.
Tuberculosis is transmitted by
by aerosol taken into the lungs by phagocytic cells and can be transmitted via lymphatic circulation.
Tuberculosis - the bodies immune system can
get infection under control but unless receive proper medication can harbor lifelong infection.
Tuberculosis treatment
* divided into 2 phases and is long so adherence is a problem.
* 1st the induction phase which renders sputum non-infectious, then last 2 months tx with 4 drugs 1-3 x’s/week
Tuberculin Skin Test (TST)
* Intradermal injection of Purified Protein Derivative (PPD)
* If pt. is exposed to tuberculosis the immune system elicits a response in 48-72 hours
* Hardness around injection site and size will determine how aggressive tx should be.
* Smaller the size the more aggressive the tx.
* 2 or more drugs are used to kill active and resting tubercle bacilli.
Tuberculosis Treatment Regimens
* Drug susceptibility tests on first isolation
* Monitor closely for compliance, adverse rxn, progress or tx program.
* Chemoprophylaxis: INH qd x 6 mo; HIV INH qd x 12 mo.
* Begin 4 drug regimen
4 drug regimen for treatment of tuberculosis
1) Isoniazid (INH)
2) Rifampin
3) Pyrazinamine (PZA)
4) Ethambutol or Streptomycin
Treatment Guidelines - Tuberculosis
* Multidrug regimens and completion of full course of tx
* Single daily dose preferred
* Prolonged tx necessary
* Supervised, twice-weekly regimens reasonable alternative for noncompliant
* Follow closely to ensure compliance and monitor for efficacy and toxicity
* Elaborate programs of rest and diet no longer applicable.
Drugs used in Tuberculosis - 1st line drugs
1) Isoniazid (INZ)
2) Rifampin
3) Rifapentin
4) Rifabutin
5) Pyrazinamide
6) Ethambutol
Drugs used in Tuberculosis - 2nd line drugs
1) Strptomycin
2) Para-aminosalcylic acid
3) Kanamycin
4) Amikacin
5) Capreomycin
6) Ethionamide
7) Cycloserine
8) Levofloxacin, moxifloxacin and Gatifloxacin
Isoniazid
* Highly selective for M. tuberculosis.
* Bacterialcidal to actively dividing mycobacteria.
* Bacterialstatic to mycobacteria that are resting.
* Drugs that are resistant to INZ are also resistant to ethionamide.
* Preferred tx for latent and prophylaxis tb
* Single agent for prophylaxis or with other agents against active tb
* Tx given over 6-9 months given daily or twice weekly.
* PO or IM
Isoniazid - how to take
* Take on an empty stomach
* Encourage compliance
Isoniazid - Pharmacokinetics
* PO, IM; dose 5 mg/kg (300 mg): Pedi 10 mg/kg (300 mg)
* Hepatically metabolized
* Excreted by the kidneys
Isoniazid - Adverse Effects
1) Depletes Pyridoxine (B6) causing peripheral neuropathy. So give B6 in conjunction with isoniazid
2) Hepatoxicity- monitor AST and ALT q month (jaundice)
3) Burning dark urine, jaundice, tingling
Isoniazid Drug Interactions
* ETOH > INH metabolism which > risk of hepatoxicity
* Antacids < INH absorption
* Disulfiram (Antabuse) so do not drink alcohol while taking Isoniazid
Rifampin MOA
* Broad spectrum antibiotic against tb and N. meningitis
* Bacterialcidal blocks RNA transcription
Rifampin Pharmacokinetics
* PO 600 mg/d; Pedi serum 10-20 mg/kg/day
* Peak serum 1.5 – 4 h
* Half-life – 5 h
* Hepatically metabolized
* Excreted in feces
Rifampin Adverse Effects
* Anorexia, discoloration of body fluids
* Pruritus, rash, mouth/tongue soreness
* Chills, respiratory difficulty, shivers, fever, H/A, b0ne/muscle pain
Rifampin Drug Interactions
* ETOH > hepatotoxicity risk
* < Corticosteroids effectiveness
* HIV protease inhibitors
* INH > hepatotoxicity risk.
Rifampin Nursing Management
* Baseline and periodic hepatic function
* Give with 240 ml water on empty stomach
* Given concurrently with other antitubercular drugs x 6 mo- 2yr
* Alert client of reddish-brown discoloration of body fluids
* Alternate form of contraception
* Avoid ETOH
Pyrazinamide Pharmacokinetics
* dose: 5-8.75 mg/kg q 6 h (max 3 g/d): Pedi 5.t-15 mg/kg bid (max 1.5 g)
* Peak serum 1-2 h
* Half-life – 9-10 h
* Hepatically metabolized
* Excreted by kidneys
Pyrazinamide Adverse Effects
Urination difficulties, Pruritus, rash, photosensitivity, jaundice, joint pain and swelling.
Ethambutol MOA
* Bacteriostatic suppresses RNA synthesis
* Effective ONLY against actively dividing mycobacterium
Ethambutol Pharmacokinetics
dose: PO 15 mg/kg/day
* Take with food
* Do not use in children < 13 y/o
* Peak serum 2-4 hours
* Half-life – 3-4 hours
* Heapatically metabolized
* Excreted by kidney
Ethambutol Adverse Effects
* Caution: Optic neuritis and renal impairment
* Optic neuritis – blurred vision, loss of red-green perception
* Chills, joint pain/swelling
Streptomycin (Aminoglycoside) Pharmacokinetics
15 mg/kg/day or up to 1 g biw-tiw pedi 20 mg/kg/day
Streptomycin Adverse Effects
* Tinnitus
* Nephrotoxicity
* Hepatotoxicity
Tuberculosis Management
* Give INH, ethambutol, rifampin single OBSERVED dose qd
* Give rifampin 1 h before or 2 h after meal
* Streptomycin deep IM, rotate sites
* Report severe GI problems, yellow sclera, dark urine, clay-colored stool, vision, hearing changes, numbness or tingling
Expectorants (Guaifenesin) MOA
* Irritates the gastric mucosa and stimulates respiratory tract secretions.
* Take with a lot of water
* Sugar and alcohol content