Komiskey: Anti-asthmatics, Antihistamine, and COPD Flashcards

1
Q

Synthesis of histamine occurs primarily in which two cell types?

A

mast cells and basophils

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2
Q

Histamine receptor H1 is found on smooth muscle, endothelium, and CNS tissue. Its activation results in?

A

vasodilatation, bronchoconstriction, smooth muscle activation, and separation of endothelial cells

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3
Q

Which histamine receptor regulates the release of other neurotransmitters?

A

H3

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4
Q

Stimulation of which cranial nerve causes bronchoconstriction and leads to cough?

A

Vagus

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5
Q

What type of receptor is H1?

A

G-protein coupled, linked to intercellular Gq, which activates phospholipase C

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6
Q

6 common first generation anti-histamines?

A
Diphenhydramine (Benadryl®)
Chlorpheniramine (Chlor-Trimeton®)
Brompheniramine (Dimetane®)
Hydroxyzine (Atarax®)
Cyproheptadine (Periactin®)
Promethazine (Phenergan®)
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7
Q

Second generation anti-histamines? (unlikely to cause drowsiness)

A
Fexofenadine (Allegra®) (14h)
 Cetirizine (Zyrtec®) (8h) (kids metabolize faster)
 Levocetirizine (Xyzal®)
 Loratadine (Claritin®) (up to 28h)
 Desloratadine (Clarinex®)

LEVOcetirizine:
This drug is the active enantiomer of cetirizine and is believed to be more effective and have fewer adverse side effects.
Also it is not metabolized and is likely to be safer than other drugs due to a lack of possible drug interactions (Tillement).
It does not cross the BBB and does not cause significant drowsiness

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8
Q

Intranasal anti-histamines?

A

Azelastine, Olopatadine (better SE)

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9
Q

Antagonists of H1 receptor?

A

Mepyramine, triprolidine, cetirizine

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10
Q

Agonist of H1?

A

Histaprodifen

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11
Q

Antihistamines are_______ ________ _________, meaning that they shift the equilibrium of the receptor configuration to the inactive state and thus block histamine effects.

A

competitive inverse agonists

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12
Q

What could be a later development of asthma? What cell type will show up?

A

COPD, neutrophils

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13
Q

What is the early phase reaction of asthma?

A

bronchoconstriction

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14
Q

What is the late phase reaction of asthma?

A

inflammation, mucus hypersecretion, hyperresponsiveness

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15
Q

List “relievers” of asthma

A

SABAs:
Salbutamol
Fenoterol

Anti-Cholinergics:
Ipratropium Bromide
Tiotropium

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16
Q

List “controllers” of asthma

A

LABAs (bronchodilation lasts >12h; good for EIB prevention):
Formoterol (***onset in 5-10m)
Salmeterol (onset in 30-40m)

ICSs (used more as prophylaxis):
Ciclesonide (**a PROdrug)
Flunisolide (MDI, BID)
Beclomethasone (MDI, BID)
Triamcinolone (MDI, BID)
Memotasone (MDI, BID)
Budesonide (breath-activated powder delivery)
Fluticasone (breath-activated powder delivery)

Oral CS (when ICS no longer work):
Prednisone
Prednilosone

(IV CS: Methylpredisolone, for untreatable asthma)

Leukotriene receptor agonist:
Monteluksat

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17
Q

What are combos of asthma drugs?

A

Budesonide + Formeterol

Fluticasone + Salmeterol

18
Q

Which B2 adrenergic agent (specific SABA) is safe in pregnancy?

A

albuterol

19
Q

What is the mechanism of albuterol?

A

stimulate AdCyl, increase cAMP, decrease Ca

20
Q

How does Methylxanthine work? (& theophylline)

A

Blocks PDE (phosphodiesterase)

21
Q

LABAs will dilate for at least how long?

A

6h

22
Q

How do corticosteroids work in the prevention or fix of asthma attacks?

A
  1. block phospholipase A and thus decrease PGs
  2. decrease cytokine/chemokine produciton
  3. inhibit the accumulation of basophils, eosinophils
  4. decrease vascular permeability
  5. enhance responsiveness of B2 receptors (thus decrease tolerance risk of SABAs, LABAs)

Overall, you see less leakage out of endothelial cells, improved airway smooth muscle, and decrease in mucus secretion.

23
Q

For MDI that is delivering and ICS, the patient should always use a _______.

A

Spacer

24
Q

List three common second=line therapy for asthma

A

Mast cell inhibitors: cromolyn/nedocromil (EIB)
Theophylline (if SABA/LABA fail)
Albuterol-Ipratropium combo (Combivent, DuoNeb)

25
Q

How do mast cell inhibitors work?

A

(think crumbs - degranulation. sounds like crom)
(cromolyn, nedocromil)
Mech is unknown but it inhibits release of cell mediators from eosinophils and lung mast cells, inhibits IgE synthesis and activation of inflammatory cells and promotes relaxation by interfering with Ca influx; given by inhalation. must be taken several times a day or BEFORE AN ATTACK

NEDOcromil is approved for patients 12 and older; Cromolyn for ALL AGES

26
Q

What drug blocks arachidonic acid from becoming 5-HPETE and thus blocks leukotriene synthesis?

A

Zileuton (lipo-oxygenase inhibitor). Can be used to treat aspirin allergy.

Other leukotriene pathway inhibitors (leukotriene receptor antagonists):

  • Montelukast (good for EIB. mountain) (ok for 6yo and older)
  • Zafirlukast (Liver test needed) (ok for 12yo and older)
27
Q

List three muscarinic antagonists used to calm the vagus nerve.

A
  • ipratropium bromide (short-acting)
  • tiotropium (24 hr duration of action; Slow dissociation from receptor) (long-acting)
  • aclidinium (long-acting)
28
Q

If your patient reports that s/he is using their SABA more than twice a week, what is your new plan of tx?

A
Start:
1. ICS
If needed add
2.     LABA
Other options:
3. Cromolyn sodium or Nedocromil
4. Leukotriene inhibitors
29
Q

Drug that binds IgE?

A

Omazilumab

30
Q

What drug is a PDE4 inhibitor and is used to reduce COPD exacerbations?

A

Roflumilast

31
Q

After how many months of controlled asthma can you consider stepping down treatment?

A

3 months

32
Q

What cells are active in asthma versus COPD?

A

Asthma: mast cells, eosinophils, CD4 T cells, MPs
COPD: Neutrophils, CD8 T cells, MPs

33
Q

Does COPD show a response to steroids like asthma does?

A

No

34
Q

In COPD, what is the preferred tx if your patient has few sx and a low risk of exacerbation?

A

Short-acting anticholingergic or SABA as needed

35
Q

In COPD, what is the preferred tx if your patient has more sx and a low risk of exacerbation?

A

Long-acting anticholingergic or LABA

36
Q

In COPD, what is the preferred tx if your patient has few sx and a high risk of exacerbation?

A

ICS + Long-acting anti-choligergic OR LABA

37
Q

In COPD, what is the preferred tx if your patient has many sx and a high risk of exacerbation?

A

ICS + Long-acting anti-choligergic &/OR LABA

38
Q

What is a new LABA on the market for tx in COPD but has insane SE?

A

Striverdi Respimat

39
Q

What can help reverse corticosteroid in COPD patients?

A

Theophylline

40
Q

What drugs may work in ACOS (asthma-COPD overlap syndrome)?

A

anticholinergics