Pharmacology Flashcards

0
Q

Advantages of treatment of the respiratory tract with inhaled aerosols?

A
  • Aerosol doses are usually smaller than doses for system administration
  • Onset of drug action is rapid
  • Delivery is targeted to the organ requiring treatment
  • Less systemic side effects, or less often or less severe
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1
Q

Primary focus of respiratory care pharmacology…

A

The delivery of bronchoactive inhaled aerosols to the respiratory tract for the diagnosis and treatment of pulmonary diseases.

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2
Q

Pharmacokinetic phase of drug action

A

The time course and disposition of a drug in the body based on its absorption, distribution mechanism, and elimination.

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3
Q

Fully ionized vs. nonionized drugs

A

Fully ionized- not absorbed across a lipid membrane, effects are largely local. (Ipratropium)

Nonionized- lipid-soluble and diffuses across a cell membrane into the bloodstream, effects can be systemic. (Atropine)

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4
Q

Pharmacodynamic phase of drug action

A

the mechanisms of drug action by which a drug molecule causes its effects on the body

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5
Q

Types of receptors in the lungs

A

Sympathetic (adrenergic)

Parasympathetic (cholinergic)

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6
Q

Neurotransmitters of the sympathetic and parasympathetic systems

A

Sympathetic- Norepinephrine (adrenergic)
(similar to epinephrine or adrenaline)

Parasympathetic- Acetylcholine (cholinergic)

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7
Q

Adrenergic

A

-Drug that stimulates a receptor responding to norepinephrine or epinephrine

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8
Q

Antiadrenergic

A

Drug that blocks a receptor for norep. or epinephrine

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9
Q

Cholinergic

A

Drug that stimulates a receptor for acetylcholine (mimics acetylcholine)

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10
Q

Anticholinergic

A

drug that blocks a receptor for acetylcholine

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11
Q

Muscarinic

A

Drug that stimulates acetylcholine receptors specifically at parasympathetic nerve ending sites

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12
Q

Receptors in the heart and effects

A

Beta-1 adrenergic (increases rate and force)

M2-cholinergic (decreases rate)

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13
Q

Receptors in bronchiole smooth muscle

A

Beta-2 adrenergic (bronchodilation)

M3-cholinergic (bronchoconstriction)

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14
Q

Receptors in pulmonary blood vessels

A

Alpha-1 adrenergic (vasoconstriction)
Beta-2 adrenergic (vasodilation)
M3-cholinergic (vasodilation)

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15
Q

Receptors in bronchial blood vessels

A

Alpha-1 adrenergic (vasoconstriction)

Beta-2 adrenergic (vasodilation)

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16
Q

Receptors at submucosal glands

A

Alpha-1-adrenergic (increased fluid, mucin)
Beta-2-adrenergic (increased fluid, mucin)
M3-cholinergic (Exocytosis, secretion)

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17
Q

Most common use for adrenergic bronchodilators?

A

-to improve flow rates in asthma (including exercise induced asthma), acute and chronic bronchitis, emphysema, bronchiectasis, cystic fibrosis, and other OBSTRUCTIVE airway states.

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18
Q

Indications for short-acting bronchodilators… (beta-2 agonists like albuterol and levalbuterol)

A

-indicated for relief of acute reversible airflow obstruction in asthma or other obstructive airway diseases (termed “rescue agents”)

19
Q

Indications for long-acting bronchodilators… (salmeterol, formoterol, and arformoterol)

A

-indicated for maintenance bronchodilation and control of bronchospasm and nocturnal symptoms of asthma or other obstuctive diseases, such as COPD.

20
Q

Indication for racemic epinephrine

A

Often used by inhaled aerosol or by direct lung instillation for its strong beta-adrenergic vasoconstricting effect to reduce airway swelling after extubation or during epiglottitis, croup, or bronchiolitis or to control airway bleeding during endoscopy.

21
Q

Bronchodilator effects

Alpha stimulation, beta-1, and beta-2 stimulation

A

Alpha-1 receptor stimulation- vasoconstriction and a vasopressor effect (increased BP)

Beta-1 receptor stimulation- causes increased HR and myocardial contractility

Beta- 2 receptor stimulation- relaxes bronchial smooth muscle, stimulates mucociliary activity, inhibitory action on inflammatory mediator release

22
Q

Ultra-short-acting adrenergic bronchodilators (catecholamines)

A

Epinephrine (Adrenaline Chloride) (Alpha, beta)
-Onset 3-5 minutes, Duration 1-3 hours, peak 5-20 mins
-SVN, 1% solution, 0.25-0.5 ml 4 times daily
Racemic epinephrine (microNefrin) (Alpha, beta)
-Onset 3-5 mins, Duration 0.5-2 hrs, peak 5-20 mins
-SVN, 2.25% solution, 0.25-0.5ml 4 times daily

23
Q

Short-acting adrenergic bronchodilator agents (noncatecholamine)

A

Albuterol (Proventil HFA, Ventolin HFA) (beta-2)
-Onset 15 min, Duration 5-8 hours, peak 30-60 mins
-SVN- 0.5% solution, 0.5 ml (2.5mg), MDI: 200ug/puff, 2 puffs every 4-6hrs
Levalbuterol (Xopenex) (beta-2)
-Onset 15 min, Duration 5-8 hours, peak 30-60 mins
-SVN 0.31, 0.63, or 1.25 mg/3ml, 3 times daily

24
Q

Long-acting adrenergic bronchodilators

A

-Salmeterol (Servant Diskus) (beta-2 agonist)

Onset 20 mins, Duration is 12 hours, peak 3-5, DPI: 50ug/blister, twice daily.

25
Q

Adverse effects of adrenergic bronchodilator agents

A

-Dizziness, Hypokalemia, Loss of bronchoprotection (loss of ability of beta-2 agonists to prevent bronchoconstriction from a stimuli), Nausea, tolerance (tachyphylaxis-decrease in response to drug), Worsening ventilation/perfusion (V/Q) ratio (decrease in PaO2/SpO2).

26
Q

Assessment of bronchodilator therapy

A
  • Monitor flow rates and lab reports of PFT’s before and after
  • Access ABG’s or pulse ox. saturation
  • Note effect of beta agonist on blood glucose (increase) and K+ (decrease) lab values
  • Emphasize patient education that beta agonists do not treat underlying inflammation and don’t prevent progression of asthma
  • Instruct and then verify correct use of aerosol delivery device
  • Instruct patients on assembly and cleaning of inhalation devices
  • Long-acting beta agonist (assess ongoing lung function such as FEV1 and peak expiratory flows, assess amount of rescue beta agonist use, assess number of exacerbations, hospitalizations, days absent from school/work, and ability to reduce dose on concomitant corticosteroids
27
Q

Anticholinergic bronchodilators

as opposed to adrenergic

A

Produce airway relaxation by blocking cholinergic receptors that induce bronchoconstriction.

  • *Effective only if bronchoconstriction is secondary to cholinergic activity
  • Adrenergic actively stimulates and anticholinergic passively blocks
28
Q

Indications for use of anticholinergic bronchodilators

A

Indicated as bronchodilators for maintenance treatment in COPD, including chronic bronchitis and emphysema.

29
Q

Indications for both Adrenergic and Anticholinergic bronchodilators

A

For use in patients with COPD receiving regular treatment who require additional bronchodilation for relief of airflow obstruction.

Example: Ipratropium bromide and albuterol (Combivent; DuoNeb)

30
Q

Mode of action of Anticholinergic bronchodilators

A

Ipratropium bromide and tiotropium act as competitive antagonists for acetylcholine at M3 muscarinic receptors on airway smooth muscle

31
Q

Adverse effects of Anticholinergic bronchodilators

A

Ipratropium and tiotropium bromide have little side effects because they are fully ionized. Eyes should be protected during nebulization.

Atropine sulfate is nonionized and does cause a number of systemic side effects such as; dry mouth, pupillary dilation, lens paralysis, increases intraocular pressure, increases HR, urinary retention, and altered mental state. Not recommended by nebulization.

32
Q

Mucous-controlling agents

A

N-acetyl-cysteine (10 or 20%) (NAC) (Mucomyst) (*always given with bronchodilator)
-SVN (3-5ml) used for bronchitis (efficacy not proven)
Dornase alfa (Pulmozyme)
-SVN (2.5mg/ampule, x’s 1 a day) Cystic fibrosis

33
Q

Side effects of Mucus-controlling agents

A

NAC-
-Irritation of the airway and cause of bronchospasm, especially in subjects with hyperactive airways. Pretreatment with adgrenergic bronchodilator can reduce airway resistance with NAC.
-Airway obstruction secondary to rapid liquefaction of secretions
-Disagreeable odor secondary to hydrogen sulfide
-Incompatibility with certain antibiotics if mixed in solution
-increased concentration and toxicity towards end of nebulizer treatment
-Nausea, rhinorrhea
-Stomatitis
-Reactivity with rubber, copper, iron, cork
Dornase alfa
-Pharyngitis, laryngitis, voice alteration, chest pain, conjunctivitis,

34
Q

Mode of action of NAC and Dornase alfa

A

NAC- breaks disulfide bonds

Dornase alfa- proteolytic enzyme that breaks down DNA material from neutrophils found in purulent secretions

35
Q

Inhaled Corticosteroids

A

-Endogenous hormones produced in the adrenal cortex, regulate basic metabolic functions in the body and exert an antiinflammatory effect. Those used to treat Asthma and COPD are glucocorticoids.

36
Q

Indications for use of corticosteroids

A

For antiinflammatory maintenance therapy of persistent asthma and severe COPD.

37
Q

Mode of action of corticosteroids

A

Glucocorticoids are lipid-soluble drugs that act on intracellular receptors. Do not provide immediate relief as mechanism of action takes hours or days to have full effect.

38
Q

Types of inhaled corticosteroids available

A

Beclomethasone dipropionate HFA (QVAR)
-Dosage: MDI 40 and 80 ug/puff, adults and children >12, twice daily
Flunisolide hemihydrate HFA (AeroSpan)
-Dosage: MDI 80 ug/puff, adults and children>12, twice daily
Budesonide (Pulmicort Flexhaler or Respules)
-Dosage: Flexhaler (DPI, 90ug/actuation and 180ug/act. >12 yrs
Respules (SVN, 0.25mg, 0.5mg or 1mg/2ml, children 1-8yrs
Fluticasone propionate/salmeterol (Advair Diskus and HFA)
-Dosage: Diskus (DPI, 100ug, 250ug or 500ug fluticasone/50 ug salmeterol
HFA (100 ug/50ug, 1 inhalation twice daily, ~12hrs apart
Symbicort
-Dosage: MDI, 80ug or 1600ug budesonide/4.5 ug formoterol, >12 yrs take 320ug or 160ug/9ug twice daily.
Dulera
-Dosage: MDI, 100ug or 200ug mometasone/5ug formoterol, >12 yrs previously medium dose (400ug/20ug daily) previously high dose (800ug/20ug daily)

39
Q

Adverse effects of corticosteroids

A

Much less systemic effects than other classes of inhaled aerosolized drugs.
Systemic- adrenal insufficiency, extra-pulmonary allergy, acute asthma, HPA supression, Growth retardation (controversial), Osteoporosis (controversial)
Local- Oropharyngeal infections (most common side effect), dysphonia, cough, bronchoconstriction, incorrect use of MDI

40
Q

Nonsteroidal antiasthma drugs

A

Cromolyn sodium (NasalCrom)
-Dosage: Spray, 40mg/ml, 1 spray each nostril, 3-6x’s/ 4-6 hrs)
Montelukast (Singulair)
-Dosage: Tablets, 10, 5, or 4mg, >15yrs one10mg tablet daily, children 6-14yrs (one 5mg chewable daily, 2-5yrs (One 4mg chewable daily)
Omalizumab (Xolair)
-Dosage: >12yrs, one subcutaneous injection every 4wks

monoclonal antibodies or anti-IgE agents

41
Q

Indications for use of antiasthma drugs

A

Prophylactic management of persistent asthma (step 2 or greater)

Cromolyn sodium and antileukotrienes recommended as alternatives to inhaled corticosteroids in step 2 and step 3 asthma

Cromlyn sodium and montelukast are often used in infants as alternatives to steroids in step 2 asthma

Antileukotrienes can be useful in combination with corticosteroids to reduce the dose of the streroid in step 2 through step 4 asthma

Monoclonal antibodies considered in appropriate populations.

42
Q

Mode of action of antiasthma drugs (4 drugs)

A
  • Cromlyn sodium- degranulates mast cells in response to allergic and nonallergic stimuli preventing release of histamine, etc.
  • Zafirlukast and montelukast act as leukotriene receptor antagonists and are selective competitive antagonists of leukotriene receptors LTD4 and LTE4 (prevents bronchoconstriction)
  • Zileuton inhibits the 5-lipoxygenase enzyme that catalyzes the formation of leukotrienes form arachonidonic acid
  • Omalizumab inhibits attachment of IgE to mast cells, reducing inflammatory mediator response.
43
Q

Adverse effects of antiasthma drugs

A

Inappropriate use, controllers rather than relievers and so people tend to overuse them thinking they aren’t working.

-Headaches, liver enzyme changes, abdominal pain, dyspepsia

44
Q

Aerosolized antiinfective agents

A

Pentamidine isethionate (NebuPent)
-Dosage: 300mg powder in 6ml water, 300mg every 4 wks in treatment of PCP prophylaxis
Ribavirin (Virazole)
-Dosage: 6 g powder in 300ml water, given every 12-18 hours/day for 3-7 days by SPAG nebulizer for treatment of RSV
Tobramycin (TOBI)
-Dosage: 300mg/5ml ampule, >6yrs, 300mg 28 days on, 28 days off to treat P. aeruginosa infection in CF

45
Q

Adverse effects of antiinfective agents

A

Pentamidine- cough, bronchial irritation, bronchospasm, wheezing, fatigue, metallic taste in mouth, conjunctivitis, rash and chest pain, decreases appetite, nausea, night sweats, chills, pancreatitis, hypoglycemia, spontaneous pneumothoraces, neutropenia

Ribavirin- skin rash, eyelid erythema, and conjunctivitis

Tobramycin- possible auditory and vestibular damage with potential for deafness and nephrotoxicity, dysphonia, tinnitus