Medications for Respiratory Alterations

Asthma

Chronic inflamatory disorder of the airway

Immune-mediated airway inflammation created by an allergen or irritant

cause of asthma

Allergen

A substance that can produce a hypersensitive reaction in the body bu not necessarily intrisically harmful

chronic cough and excessive sputum production

S+S of chronic bronchitis

from hypertrophy of mucous secreting glands in the epithelium of the large airways

Emphysema cause

1. chronic bronchitis

2. emphysemaASt

Two COPD disease processes:

1. sense of breathlessness

2. chest tightening

3. wheezing

4. dyspnea

5. cough

S+S of asthma [5]

1. ihalation of allergens or pollutants

2. infection

3. cold air

4. vigorous exercise

5. emotional stress

triggers of asthma: [5]

1. regulate air humidit

2. dry clothes in the drier

3. avoid carpets

4. encase mattresses and pillow cases

5. regularly change air exchanger and air conditioner filters

6. avoid housing pets

7. stay inside on high pollen days

Non-pharm interentions for asthma control [7]

50%Clas

Want to keep air humidity less than how much with asthma?

1. beta-2 andrenergic agonists

2. glucocorticoids

3. cromolyn

4. methylxanthines

5. Ipratropium

6. Leukotriene modifiers

Different classes of asthma medications(5)

1. therapeutic effects delivered directly ot site of action

2. systemic effects are minimized

3. rapid onset of actionSmall,

Benefits of inhaled asthma medication

MDI (metered dose inhaler

Small, pressurized devices (aerosol canisters) at measured doses. Inhale prior to activating the device,

10%. Most gets lost in oropharynx, swallowed etc.

How much drug reaches the lungs with MDI?

Dry powder inhaler

Inhaler that gets more drug to lung (20%), activated by inhalation and does not require hand lung coordination

Nebulizer

Small machine used to convert drug solution into a mist. Finer particles are easily absorbed. Takes longer to administer dose

acute bronchospasm and exercised induced bronchospasm

Indications for beta-2 adrenergic agonists [2]

Drug acts like epinephrine

What does it mean that Beta-2 andrenergic agonists are “Sympathomimetic”

Ventolin (Albuterol)

“rescue” Beta-2 andrenergic agonist inhaler that is short acting, 2 puffs q-4-6h PRN

Serevent (Salmeterol)

Long acting beta-2 adrenergic agonist inhaler for bad asthma

Terbutaline (Brethine)

Oral, long acting beta-2 adrenergic agonist medication (5mg po tid)

1. selectively activates beta-2 andrenergic receptors

2. acts on smooth muscle in the lungs causing bronchodilation

3. Suppresses histamine

4. increases ciliary action and motility

Beta-2 andrenergic agonist MOA

When binds to beta-1, cases vascular contraction and increased BP

effect of Beta-2 andrenergic agonists on vascular smooth muscle

They have a higher affinity for beta-2, but still attaches to beta-1.

What does it mean by “selectivity is relative, not absolute”

Attaching to Beta-1 (located in heart vessels)Vent

Side effects of Beta-2 adrenergic agonists (ventolin) come from:

1. tachycardia

2. increased FOC

3. Vasoconstrictoin

4. Agina

5. tremors, sweating, agitation

Ventolin side effects:

1. decreases deposition in oropharynx

2. need to wait one minute between pumps

Benefits of using a spacer

Chronic asthma as maintenance therapy

Methylxanthines are used for what?

Theophilline (Theodur)

Methylxanthine prototype drug

1. CNS exciteation

2. bronchodilation

3. diuresis

Effects of Theophylline (Theodur) [3]

1. Produces bronchodilation by relaxing bronchial smooth muscle

2. inhibits the enzyme that increases intracellular levels of cyclic AMP

3. Binds to adenosine receptors, blocks their activation by adenosine

Methylxanthines MOA

1. has a narrow therapeutic range

2. metabolized in the liver (age, disease and drug considerations

3. formulation contains large amounts of drug

Why is Theophylline dangerous? [3]

PO only

Theophylline route

1. caffeine

2. cigarettes

Theophylline interactions (non-med) [2]

1. antibiotics

2. anticonvulsants

Theophylline decreases the effects of: [2]

1. nausea

2. vomiting

3. diarrhea

4. insomnia

5. restlessness

Mild toxicity effects of theophylline

in the morning because mild toicity can cause restlessness and insomnia

When to take theophylline and why?

1. severe dysthrymias (little to no cardiac output)

2. convulsions

3. death

Adverse effects of Theophylline (toxicity)

suppresses inflammation

End result of glucocorticoids

binds to and stabilizes mast cells to decrease synthesis of histamine and leukotrienes

blocks ensyme that is the first step in the synthesis of prostaglandins and leukotrienes from phospholipids

• decreased infiltration and activity of inflammatory cells

• decreased edema and airway of mucosa

Glucocorticoid MOA

1. Pulmicort

2. flovent

Glucocorticoid protoype drugs: [2]

Prophylaxis of chronic asthma, used regularly (very safe)

Primary use of Flovent and Pulmicort

1. Adrenal suppression (adrenals get lazy)

2. osteoporosis

3. thrush

4. Dysphonia

5. PUD (increased gastric secretions

6. Cataracts and glaucoma

7. Temporarily stunts growth

Adverse effects of glucocorticoids

Rinse and gargle afterwards. Thrush

How to prevent oropharyngeal candidiasis with glucocorticoids

temporarily slows frowth, reserved for adults unless asthma is severe

Why are glucocorticoids reserved for adults

1. infection

2. fluid and electrolyte imbalances

3. hyperglycemia

Adverse effects of glucocorticoids

interruption of inflammation and immune response

How do glucocorticoids for asthma cause infection

effects on sodium and water retention

How do glucocorticoids for asthma cause fluid and electrolyte imbalance

Affects glucose production

How do glucocorticoids for asthma cause hyperglycemia

Intal (inhalation only, regular basis prior to attack)

Cromolyn drug prototype

Prophylactic treatment of asthma

Primary use of intal

1. exercise induced bronchospasm

2. allergic rhinitis

Other uses of intal besides prophylaxis of asthma [2]

1. suppresses inflammation (not a bronchodilator)

2. Stabilizes the cytoplasmic membrane of mast cells

3. prevents release of histamine and other mediators

4. inhibits other inflammatory cells (eosinophils, macrophages)

Cromolyn MOA

Suppresses the effects of leukotrienes

Decreases bronchocontriction and inflammatory responses such as edema and mucous secretion

Leukotriene modifier MOA

Montelukast (Singulair)

Leukotriene modifier prototype

1. prophylaxisand maintenance of asthma in patients at least one year old

2. prevention of exercised induced bronchospasm in patient at least 15 years old

3. Relief of allergic rhinitis

Three indications of singulair

Suicidal ideation

Side effect of Singulair in pre-teens

tablets, chewables, and oral granules (PO, rapidly absortbed, highly bound to plasma proteins)

Singulair route

Leukotriene receptor blockers

Singulair MOA

Umeclidinium

incruse ellipta prototype

Long-acting muscarinic antagonist. bronchodilator, used for COPD

incruse ellipta MOA

Dry powder for inhalation, use one puff daily to treat COPD

Incruse ellipta dosing

Combination of fluticasone (Steroid) and vilanterol (bronchodilator)

Breo ellipta is a combination of what medications to treat asthma and COPD?

1. allergic reaction

2. regulation of gastric secretions

Histamine plays an important role in:

mast cells and basophils

histamine is stored where?

Neurons

histmamine is produced by what?

Certain agents can act directly on mast cells to trigger histamine release. Cell injury can also cause direct release

when is histamine release triggered (non-allergic)

1. Vasodilation

2. increased vascular pereability

3. bronchoconstriction

4. stimulation of goblet cells

5. chemotaxis

H1 receptor stimulation causes [5]

1. secretion of gastric acid

2. act directly on parietal cells to promote acid release

H2 receptor stimulation causes [2]

Caused largely by histamine acting on H1 receptors

Role of histamine in mild/moderate allergy:

Some histamine but mainly lukotrienes

Role of histamine is severe anaphylactic reacitons:

Epinephrine

Drug of choice when histamine plays less of a role in allergic reactions (severe)

1. H1 antagonists

2. H2 antagonists

Two types of antihistamines

1. blocks the actions of histamine at H1 receptors

2. No blockage of H2 receptors

3. Some binding to muscarinic receptors

H1 antagonist MOA [3]

1. first generation H1 antagonists

2. second generation H1 antagonistsPer

Two major groups of H1 antagonists

1. Reduce local flshing

2. reduce itching and pain

Peripheral effects of H1 antagonists [2]

1. Can have CNS depression (sedation) at therapeutic doses.

2. Second generation has less sedation

3. Overdose can have CNS stimulation, convulsions

CNS effects of H1 antagonists [3]

Very young children Ad

What population are highly sensitibe to CNS stimulation from H1 antagonists?

1. sedation

2. other CNS effects: (dizziness, fatigue, coordination problems, confusion)

3. GI effects (N+V, loss of appetite, constipation)

4. Anticolinergic effects (weak atropine like effects)

Adverse effects of H1 antagonists:

With food because of all GI effects.

When to give H1 antagonists?

CNS depressants

H1 antagonists interact with:

crosses the placenta, contraindicated in the third trimester and during lactation.

When are H1 antagonists contraindicated in pregnancy?

CNS and anticholinergic reactions

1. dilated pupils

2. flushed face

3. hyperpyrexia

4. tachycardia

5. dry mouth

6. urinary retention

H1 antagonist acute toxicity S+S:

Hyperpyrexia

High temp

1. Activated charcoal (induces vomiting)

2. IV benzos (convulsions)

3. Ice packs/sponge baths (hyperthermia)

Treatments for H1 antagonist acute toxicity [3]

Diphendydramine (Benadryl)

Hydroxyzine (vistaril)

First gen h1 antagonist prototype

1. dry mouth

2. urinary hesitancy

Anticholinergic properties of first gen H1 antagonists [2]

1. cetirizine (reactine)

2. Fexofenadie (allegra)

Second generation H1 antagonist prototypes

ON an empty stomach. Food delays absorption

Important to take reactine when?

1. allergic rhinitis

2. Chronic idiopathic urticaria (Hives)

uses for Reactine [2]

Cetirizine (Reactine)

Second generation H1 antagonist that is more sedating

Fexofenadine (allegra)

Second generation H1 antagonist that should not be taken with fruitjuice, and used cautiously with people with renal impairment

Loratadine (Claritin)

Second gen H1 antagonist that should be used cautiously in people with significant hepatic and renal impairment and food delays absorption

Desloratadine (Aerius)

second gen H1 antagonist that can be taken with or without food and may cause some minor anticholinergic effects (dry mouth and mucous membranes, etc.)