ASTHMA DRUGS

General: ppl sensitive to ASPRIN get intense bronchoconstriction In response to allergens Asthma causes irreversible remodelling

BRONCHODILATORS

ANTI-INFLAMMATORY
MAST CELL STABILIZERS:

LEUKOTRIENE ANTAGONIST


SS2-AGONIST

ANTI- MUSCURANIC
Ipratropium Bromide:
• Orally and Nasal Spray

METHYLXANTHINE
Theophylline: • Long term prevention of bronchoconstriction in ptx w/asthma or emphysema • less CNS stimulation & more bronchodilation than caffeine.

↑ cAMP concentration in SM =

Stabilize plasma membrane of mast cells/eosinophils preventing degranulation = no release of histamine or leukotrines

prevent/relieve bronchospasm w/out cardiac stimulation (higher doses become non selective) only ones used to counteract acute asthma attack
LONG LASTING:

• • •

used in children; only prophylactically for prevention of attack efficacy is low, given several times daily via enabler do not cause bronchodilation (not used for relief)

useful in preventing Nocturnal Asthmatic Attacks (which are sometimes lifethreatening), and the prevention of Exercise-induced Asthma.

< effective than β2agonists but w/few A/E • Quaternary structure that is not absorbed well

• • •

inhibit late phase of Allergen-induced Bronchoconstriction, that occurs after bronchodilating effect of short-acting drugs wanes • never used for acute attacks

Tx ptx w/COPD (DOC) such as Emphysema, the bronchodilating effect develops slower than albuterol but it lasts longer, less useful in asthma

Inhibition of phosphodiesterase (PDE) isozymes, which catalyzes degradation of cAMP. • antagonism of adenosine receptors, inhibition of Ca 2= influx. Adenosine is a Theophylline antagonist. • enhancement of Catecholamine secretion In asthmatic patients, causes inhibition of T lymphocytes proliferation & cytokine production. It also ↓ # of eosinophils, lymphocytes, & monocytes that infiltrate the bronchial epithelium (basophils not involved) • well absorbed from the gut, is widely distributed & crosses the BBB to enter the CNS.

• efficacy low A/E: may cause irritation of throat, cough & bronchospasm Cromolyn sodium: • inhibits Ca influx into mast cells • does not interfere w/binding of IgE to mast cells of Ag

Mediators of inflammation that contributes to bronchospasm Compete w/leukotrines for receptors preventing airway inflammation, edema, bronchoconstriction, secretion of thick mucus Inhibit early/late phases of allergen induced bronchospasm Can Only Be Use as an ADJUNCT (w/steroids, not approved for monotherapy) Montelukast: leukotriene receptor blocker Zefilukast: hardly used b/c used 2x daily and has some DI Both contain sulfur moiety and resemble structures of sulfidopeptide, leukotrines or LTC4, LTD4 and LTE4 Ziluteon:

• •

inhibits 5-Lipoxygenase (enzyme responsible for catalyzing formation of leukotrienes from arachidonic acid) ORALLY 4x daily • Prevents synthesis of LTC during an asthmatic attack. Used for mild-moderate asthma A/E: flu-like syndrome, headache, drowsiness, & dyspepsia; ↑s serum transaminases (should watch for hepatitis) Shouldn’t give to ptx w/transaminases level 3X ULN.

Combined therapy w/albuterol = >er bronchodilating effect

Used for Systemic Mastocytosis. GLUCOCORTICOIDS: • most efficacious antiinflammatory drug • adverse effects ↓ when given by inhalation long term prevention rather then relief of acute attacks A/E: ICS = ↓er side effects Oral thrush prevented w/ spacers/mouth wash Long term use=osteoperosis, hypertension, diabetes (↑serum [glucose]), pituitary-adrenal axis suppression, obesity, skin thinning, muscle weakness Indications: all forms of asthma except mild-intermediate Inhaled: Beclomethasone: 3-4x daily Budesonide: 1-2x daily Flunisolide: 1-2x daily Fluticasone: coupled w/LABA (advil) Triamcinolone: 3-4x daily Oral: Prednisone, Prednisolone, Methylprednisolone

in the even of an acute attack, ptx taking these drugs do

• • •

narrow therapeutic index, more side effects and a greater potential for drug interactions. ↓ dyspnea,↑ diaphragmatic contractility, improves the exercise performance & sense of well being, & ↓ fatigue. ↑ central respiratory drive and has s favorable cardiovascular effects, including:

SHORT ACTING:
Prevent/treat acute bronchospasm Inhaled: Albuterol: some ptx have tachy. For children/adults who can’t use MDI (Terbutaline also) Bitolterol: solution Isotharine: generic solution Levalbuterol: solution Metaproterenol: MDI Tablet or Syrup Oral formulations have slower onset of action, may cause more systemic effects Pirbuterol: MDI Salbutamol: Terbutaline:

Inhibits CYP1A2 & CYP3A4 &

o o o

↓ pulmonary artery ed pressure & vascular resistance ↑ in rt & lt vent. ejection fractions. ↑ mucociliary clearance &↓ airway inflammation. Indications: Moderate to severe COPD, &Asthma

A/E: G.I.T.: Abdominal pain, Nausea & Vomiting.* CNS: Headache, Anxiety, Restlessness, Insomnia, Dizziness, & Seizures. Cardiovascular: HypoTN, Brady, Extrasystole, PVB (premature ventricular breaths) & Tachy. Seizures and

Recurrent Apnea in Premature Infants (adenosine antagonism). • Obstructive Sleep Apnea.

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