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Flashcards in Asthma Drugs Deck (19):
1

Albuterol (Proventil)

- short acting beta2 adrenergic agonist
- relief of symptoms
- inhaler
- hit maximal effect at 30 min; lasts several hours
- adverse effects minimal due to low systemic absorption. may see tachycardia or muscle tremors in increased doses

2

Salmeterol (Serevent)

- long acting beta2 adrenergic agonist
- long duration (12+ hours)
- not for acute attacks - 2 puffs daily - hits maximal effect at 2 weeks
- inhaler
- must be used with corticosteroids (long acting beta agonists should NOT be used without corticosteroids)
- adverse effects minimal due to low systemic absorption. may see tachycardia or muscle tremors in increased doses

3

Epinephrine

- non-selective beta agonist
- drug of choice for anaphylaxis
- rapid action (given IV or IM)
- severe CV side effects

4

Isoproterenol

- non-selective beta agonist
- very potent and fast acting: greater effect on breathing than epinephrine, so used if the patient is suffering mainly from bronchoconstriction
- inhaled
- cardiac arrhythmias

5

Ipratropium Bromide

- muscarinic antagonist
- not acute; hits peak effect at 1-2 hours
- does not work for non-muscarinic bronchospasm
- inhaled, minimal side effects; may see drying of the mouth/upper airways - can alleviate with spacer

6

Caffeine (coffee)

- methylxanthine

7

Theobromine (cocoa)

- methylxanthine

8

Theophylline (tea)

- methylxanthine
- narrow therapeutic range: 5-15 micrograms/mL
staying in this range is hard
- oral (tablet) - not for acute bronchospasm
- mechanism of action:
1. phosphodiesterase inhibitor --> increases production of cAMP, which leads to bronchodilation
2. adenosine antagonist (adenosine = bronchoconstrictor)
- side effects at therapeutic doses: headaches, nervousness, insomnia, nausea/vomiting, epigastric pain
- side effects at greater than therapeutic doses:
> 30 micrograms/mL --> hypokalemia, cardiac dysfunction
> 40 micrograms/mL --> seizures
- metabolism: liver cytochrome P450 --> many drug interactions which increase theophylline in the blood
- drugs that may increase serum theophylline levels: erythromycin, oral contraceptives, zileuton
- drugs that may decrease serum theophylline levels: barbiturates, carbamazepine, cigarette smoke (chemicals, not nicotine)
- disease states that may result in increased serum concentrations: liver disease, febrile illnesses like pneumonia or influenza
--> reduce the dose 50% in children with fever
- disease states that may result in decreased serum concentrations: CF

9

Flunisolide (Flovent)

- anti-inflammatory agent
- corticosteroid
- inhaled
- mechanisms: controls eosinophils, reduce mucosal edema, potentiate beta-adrenergics, inhibit transcription of inflammatory agents
- side effects: minimal since inhaled; can see oropharyngeal candidiasis (solution = gargle and spit after inhaling)
- corticosteroids work on everyone

10

Fluticasone (in Advair, a combination drug)

- anti-inflammatory agent
- corticosteroid
- inhaled
- mechanisms: controls eosinophils, reduce mucosal edema, potentiate beta-adrenergics, inhibit transcription of inflammatory agents
- side effects: minimal since inhaled; can see oropharyngeal candidiasis (solution = gargle and spit after inhaling)
- corticosteroids work on everyone

11

Prednisone

- anti-inflammatory agent
- corticosteroid
- systemic
- mechanisms: controls eosinophils, reduce mucosal edema, potentiate beta-adrenergics, inhibit transcription of inflammatory agents
- side effects: HTN, diabetes, iatrogenic cushings (hyper secretion of adrenal steroids --> change in fat distribution from extremities to midsections), adrenal suppression (adrenal fatigue), peptic ulcers
- corticosteroids work on everyone

12

Fluticasone and Salmeterol (Advair)

- Fluticasone = corticosteroid; Salmeterol = long acting beta2 adrenergic agonist
- inhaler with internal blister pack (no spacer needed)
- one puff twice a day
- dosing: mg Fluticasone/mg Salmeterol
500/50 = systemic corticosteroid effects with extended use
250/50 or 100/50 = more common, no systemic effects
- must use long acting beta2 adrenergic agonist like Salmeterol with a corticosteroid
- corticosteroids work on everyone

13

LTB4

- leukotriene
- attracts neutrophils

- plasma LT's may be a marker for asthma in humans
- blood leukocytes from asthmatics release more
- urine LTE4 correlates with the severity of spontaneous bronchoconstrictive attacks
- 5-lipooxygenase activity is stimulated by antigen challenge of sensitized tissues

14

LTC4, LTD4 (SRS-A)

- leukotriene
- SRS-A = slow reacting substance of anaphylaxis
- causes bronchoconstriction, hyperreactivity, mucosal edema, and mucus secretion

- plasma LT's may be a marker for asthma in humans
- blood leukocytes from asthmatics release more
- urine LTE4 correlates with the severity of spontaneous bronchoconstrictive attacks
- 5-lipooxygenase activity is stimulated by antigen challenge of sensitized tissues

15

Zileutin

- anti-LT
- inhibits 5-lipoxygenase
- oral --> systemic
- metabolism: liver cytochrome P450
--> drug interactions: increase theophylline levels, decrease warfarin clearance (increased prothrombin time), increase carbamazepine effect
- side effects: abnormal liver function tests, tachycardia, alopecia, rash, fibromyalgia-like symptoms, churg-strauss syndrome (rebound eosinophilia which can be life-threatening)
- anti-LT are good for exercise and aspirin-induced asthma; used to decrease dose of inhaled corticosteroids

16

Zafirlukast

- anti-LT
- LT receptor antagonist
- oral --> systemic
- metabolism: liver cytochrome P450
--> drug interactions: increase theophylline levels, decrease warfarin clearance (increased prothrombin time), increase carbamazepine effect, erythromycin use decreases Zafirlukast
- side effects: abnormal liver function tests, tachycardia, alopecia, rash, fibromyalgia-like symptoms, churg-strauss syndrome (rebound eosinophilia which can be life-threatening)
- anti-LT are good for exercise and aspirin-induced asthma; used to decrease dose of inhaled corticosteroids

17

Cromolyn

- inhibits mediator release from mast cells, neutrophils, eosinophils
- causes an interaction between secretory vesicles and the cytoskeleton (increased binding of moesin-like mast cell protein with actin)
- may suppress calcium and chloride channel activity
- chronic, prophylactic use
- inhaler
- don't work on all mast cells or everyone
- no effect on skin mast cells
- side effects: minimal (poor absorption), localized to site: throat irritation, cough, mouth dryness (alleviated by using a spacer or gargling/spitting after)

18

Nedrocromil

- inhibits mediator release from mast cells, neutrophils, eosinophils
- causes an interaction between secretory vesicles and the cytoskeleton (increased binding of moesin-like mast cell protein with actin)
- may suppress calcium and chloride channel activity
- chronic, prophylactic use
- inhaler
- don't work on all mast cells or everyone - like anti-LT, used to decrease dose of corticosteroids
- no effect on skin mast cells
- works on conjunctiva only *specific for Nedrocromil
- side effects: minimal (poor absorption), localized to site: throat irritation, cough, mouth dryness (alleviated by using a spacer or gargling/spitting after)

19

Omalizumab

- anti-IgE
- monoclonal antibody against IgE; binds circulating IgE regardless of specificity; forms small, biologically inert Omalizumab:IgE complexes (goal: decrease IgE levels to