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RT Program > CH.6 Pharmacology > Flashcards

CH.6 Pharmacology Flashcards

1
Q

Adrenergic (Sympathomimetic)

A

–Cardiopulmonary system
—increase in HR, BP, and RR
—Bronchodilation
–Eye
—Mydriasis (dilation)
–GI Tract
—Decreased motility
–Insulin secretion
—decreased

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2
Q

Sympathetic Nervous System

A

–When stimulated:
—relaxes the bronchial smooth muscle
—dilate the airways
—lowers airway resistance
– 3 Types of Receptors
—Alpha, beta 1 in heart, and beta 2 in the lungs

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3
Q

Airway Anatomy

A

-Thress layers of the airway
–Mucosa: innermost layer
—has goblet cells that produce sticky mucus to catch and debris
—ciliated cells
–Submucosa
—Bronchial glands
—smooth muscle
—capillary network
—elastic tissue
–Adventitia
—Support of airways

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4
Q

Bronchoconstriction

A

–reduction of the inner diameter of airway
–Bronchospasm: contraction of smooth muscle. Airway diameter is reduced, caused reduction in airflow
–Inflammation (Airway Edema): injury to mucous membranes causes dilation of the blood vessels, Swollen tissue reduces the diameter of the lumen of the airway.
–Secretions: impairment of the normal mucociliary clearance mechanism of the lungs. Secretions in the airway reduce the airway diameter.

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5
Q

Development of Beta Agonists: Catecholamines

A

–catechol nucleus and an amine side chain
–Not very Beta 2 specific
–Degraded by enzymes COMT and MAO, not given orally
–All sympathomimetic bronchodilators are either catecholamines or derivatives of catecholamines

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6
Q

Development of Beta Agonists: Resorcinols

A

–short duration of action
–resistant to breakdown by enzymes
–can be given orally
–derive from the catecholamines

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7
Q

Development of Beta Agonists: Saligenins

A

–most widely prescribed
–Most Beta 2 specific
–Rapid onset
—-derive from the catecholamines

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8
Q

Adrenergic Bronchodilators as Stereoisomers

A

–catecholamines and derivatives
– similar physical and chemical properties
–different physiological effects
–example: Levalbuterol

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9
Q

Nonsuperimposable Molecular Mirror images

A

–(R)-Isomer (right isomer) (levo), active on airway beta receptors producing bronchodilation
–(S)-Isomer (left isomer) (dextro), not active on adrenergic receptors
–Natural epinephrine from the adrenal gland occurs only in the R-isomer
–Racemic mixture have an S and R isomer
–example: Levalbuterol

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10
Q

Clinical Indications for Adrenergic Bronchodilators

A

–Relaxation of smooth airway muscle in the presence of reversible obstruction
–Can be short-acting or long-acting
–Asthma: acute, chronic, exercise-induced
–Bronchitis
–Emphysema
–Bronchiectasis
–Other obstructive airway disease

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11
Q

Indication for Short-Acting Agents

A

–Acute reversible airflow obstruction
–“rescue” agents or “ relievers”
–Albuterol
–Levalbuterol
–Metaproterenol

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12
Q

Indication for Long-Acting Agents

A

–maintenance bronchodilation, control of bronchospasm, and control of nocturnal symptoms
–“controllers”
–Salmeterol
–Formoterol
–Arformoterol
–Indacaterol
–Olodaterol
–Vilanterol

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13
Q

Bronchodilators’ Classification

A

–Ultrashort acting: duration less than 3 hours
—example: racemic epinephrine
–Short acting: duration of 4 to 6 hours
—examples: albuterol, levalbuterol, metaproterenol
–Long acting: duration of 12 to 24 hours
—examples: salmeterol, formoterol, arformoterol, indacaterol, olodaterol, vilanterol

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14
Q

Catecholamine

A

–Racemic Epinephrine: nebulized
–Control airway bleeding during endoscopy
–Reduce upper airway swelling: Postextubation stridor, Epiglottis, Croup, Bronchiolitis
–Allergic Reactions
–Decongestant
–Alpha-adrenergic vasoconstricting effect

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15
Q

Catecholamine: Racemic Epinephrine (Racemic Epi)

A

–Ultra-short acting
–Trade name: Asthmanefrin
–Mode of action: a and B receptors
–Method of administration: SVN 2.25%, 0.25-0.5 mL QID
–Onset: 3-5 mins
–Peak: 5-20 mins
–Duration: 0.5-2 hrs

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16
Q

Catecholamine: Epinephrine

A

–Potent catecholamine bronchodilator
–Stimulates both a- and B- receptors
–High prevalence of side effects: tachycardia, increased BP, Tremor, Headache, Insomnia

17
Q

Metabolism of Catecholamines

A

–Rapidly inactivated by COMT
–Duration of action is limited
–1.5 to 3 hrs
–Unsuitable for oral administration: inactivated in gut and liver
–Also inactivated by: heat, light, air

18
Q

Resorcinol Agents

A

–Better for maintenance therapy
–Significantly longer duration of action: 4-6hr
-Slower peak effect: 30-60 minutes
–Examples: Terbutaline (IV), Metaproterenol

19
Q

Resorcinols: Metaproterenol

A

–PO-tablet or syrup
–More Beta- 2 specific than catecholamines
–Treats bronchospasm, has many cardiac effects
–Onset: 1-5 min
–Peak: 60 minutes
–Duration: 2-6 hrs

20
Q

Resorcinols: Terbutaline (IV)

A

–parenteral
–treats bronchospasm and stops premature labor by relaxing smooth muscle

21
Q

Saligenin Agents

A

– B2 Preference
–Effective by mouth
–Peak effect in 30-60 minutes
–Duration: 4-6 hrs
–Examples: albuterol, levalbuterol

22
Q

Albuterol

A

– Tade Names: Proventil HFA, Ventolin HFA, ProAir HFA, AccuNeb
–Available as:
—MDI: 2 puffs, tid, qid
–Nebulizers: 0.5% (5mg/ml), 0.5ml, tid, qid
–Syrup: 2mg/5ml, 1-2 tsp tid, qid
–Extended release oral tablets: 2,4, and 8mg, bid, tid, qid
–given continuously for severe asthma
–Short acting
–Onset: 15 min
–Peak: 30-60 min
–Duration: 5- 12 hrs
–for lower airways

23
Q

Levalbuterol (Xopenex): The (R)- Isomer of Albuterol

A

–released in 1999 as the first synthetic inhaled solution available as a pure (R)-isomer of racemic albuterol
–Trade name: Xopenex
–Available as HFA MDI and nebulizer
–Available in four nebulizer does:
—0.31mg/ 3mL
—0.63mg/3 mL
–1.25mg/3 mL
–1.25mg/05 mL concentrated

24
Q

Single (R)- Isomer Formulation of Albuterol

A

–side effects of tremor and heart rate changes were less
–more potent that Albuterol with less side effects
–1.25 mg Levalbuterol dose showed higher peak effect on FEV1, than racemic albuterol

25
Q

Nebulization of Albuterol

A

–used for management of severe asthma
–reduces need for frequent therapist attendance
–generally, 10 to 15 mg/hour for adult
–or 2.5mg to 5 mg, Q20 minutes, three times
–If MD orders 10mg/hour of ).5% Albuterol, how many mls should be given 2 hours

26
Q

Nebulization of Albuterol

A

–Delivery Methods:
—refilling SVN
—Volumetric infusion pump
—Large-volume nebulizer
–Toxicity and monitoring:
—Potential complications: cardiac arrhythmias, hypokalemia, hyperglycemia, tremor

27
Q

Long-Acting B-Adrenergic Agents

A

–offer less frequent dosing and nocturnal
–Extended-release albuterol
–Salmeterol
–Formoterol
–Arformoterol
–Indacaterol
–Olodaterol
–Vilanterol

28
Q

Extended-Release Albuterol

A

–Available as Vospire ER
–4-mg or 8-mg oral tablet
–Activity time, 8-12 hrs

29
Q

Salmeterol (Serevent Diskus)

A

–Available as DPI
–Bronchodilator effect:
–Onset: 20 min
–Peak 3-5 hrs
–Duration: 12 hrs
–Long-acting
– take BID

30
Q

Formoterol (Performist, Foradil)

A

–B2- Selective agonist
–Onset: 15 min
–Peak: 30-60 min
–Duration: 12 hrs
–Available as an SVN and a DPI
Used for:
—Maintenance of asthma
—Asthma (5 year+)
—Exercise-induced bronchospasm (5+ years)
—COPD
–Long-acting
–Use BID

31
Q

Arformoterol (Brovana)

A

–B2- Selective agonist
–Single isomer of formoterol
–Onset: 15 min
–Peak: 30-60 min
–Duration: 12 hrs
–Available as nebulizer solution
Approved for:
–Maintenance treatment of COPD
–Maintenance therapy of asthma not controlled by inhaled corticosteroids
–Pt uses MDI

32
Q

Indacaterol (Arcapta Neohaler

A

–B2- Selective agonist
–Available as a DPI
–Onset: 5 min
–Peak: 30 min
–Duration: 24 hrs
–Ultra-long lasting
-Approved for
–Maintenance treatment of COPD

33
Q

Olodaterol (Striverdi Respimat)

A

–B2-Selective agonist
–Ultra-long lasting
–Onset: 5 min
–Peak: 30-60 min
–Duration: 24 hrs
-Approved for:
–maintenance treatment of COPD

34
Q

Vilanterol

A

–Not available as monotherapy
–B2- selective agonist approved in fixed combination agents will:
—Fluticasone (Breo Ellipta)
—Umeclidinuim (Anoro Ellipta)
–Ultra-long lasting

35
Q

Safety Concerns with Long-Acting B2 Agonists (LABAs)

A

-Not to used:
–without a controller medication
–by patients who are controlled on low-dose or medium-dose inhaled Corticosteroids (ICS)
–by patients on beta blocker drugs (for SABAs)
-Should be used:
–Only if patients are not controlled with ICS
–For short term only
–Children must use in conjunction with a corticosteroid

36
Q

Mechanism of Action: a-Receptor stimulation

A

–vasoconstriction effect
–Examples: phenylephrine, epinephrine

37
Q

Mechanism of Action: B1- receptor stimulation

A

–increased HR and contractile force

38
Q

Mechanism of Action: B2-Receptor Stimulation

A

–relaxation of bronchial smooth muscle

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