Smooth Muscle Drugs

Question 1

name the Short acting β2 agonists (SABA)

(“ROL call”)

Answer 1

Albuterol
(Salbutamol)

Terbutaline
(“do not distrub”)

Pirbuterol

Question 2

Inhaled corticosteroids

Answer 2

Beclomethasone

Budesonide

Fluticasone

-corticosteroids treat asthma by blocking inflammation and and cellular infiltration

*can cause oral candidiasis (“snow cone tongue”)

• treat with topical clopiprazole

Question 3

leukotrienes receptor antagonists

Answer 3

-AA turn to Leukotrienes by LOX
leukotrienes increase vascular permeability ,
increase mucus secretion and cause bronchoconstriction
(“lacrosse team constrict stick bronchi”)
——————————————————————————-
-CysLT1 is the receptor of LTD4 - the most potent leukotriene bronchocontrictor

–“kast” suffix

Montelukast (“monte the broadkaster”)

Zafirlukast

• cause bronchodilation (“dilated scarf”)
• taken orally“(monte opening his mouth”)

• *Zileuton** (“God_zile”_ above LOX Coach_)_

direct LOX inhibitor (“lipoxygenase inhibitor”)

-hepatotoxic

inhibition of COX shifts AA towards LOX ⇒ exacerbate bronchoconstriction therefore Zileuton is useful to prevent that

Question 4

Long acting β2 agonists

(LABA)

Answer 4

Salmeterol
(“salute formation”)

**Formoterol

-**
Long duration of action since highly lipophilic
(“long tapering flag”)

Question 5

methylxanthines

(“xanthine energy drinks”)

Answer 5

Theophylline (“you’ll be flyin”)

-related to caffeine (“energy drink says caffeine”)

-are phosphodiesterase inhibitors
(“don’t phoster disinterest” sign on shop)

-Increase cAMP
(“camping world” store)

-Adminstered orally
(“drinker open mouth”)

-can cause CNS side effects including Nervousness and tremor (“shaking kid”)

-can cause tachycardia
(“shaking kid has elevated heart wrist watch”)

-metabolized by CYP450
(“Chrome bumper hitting xanthine drink”)

Question 6

inhibitors of Histamine release

Answer 6

-mast cell degranulation of histamine causes asthma
(“Bee hive”)

-after first exposure mast cells are coated with IgE→second antigen exposure binds Fc portion of IgE →mast cell degranulation and release of histamine
(“IgE Gun shooting bee hive and making hole”)
——————————————————————————–
Omalizumab (“limousine driver stopping IgE gun”)
-is anti-IgE monoclonal antibody against Fc portion of IgE preventing mast cell sensitization

Chromolyn Na+ (“lynn’s bee control”)

-inhibits mast cell degranulation
(“bee sedating smoke”)

Question 7

treatment of acute exacerbation of Asthma

Answer 7

-albuterol (SABA)

-iv corticosteroids

• beclomethasone
• budesonide
• fluticasone

​-Ipratropium bromide (antimuscarinic)

• intramuscular Epinephrine (anaphylactic)
• oxygen ( in notes)

Question 8

H1 activation

Answer 8

is coupled to the Gq protein

• mediates allergic inflammation
  (“Q” dandelion”)

-increases nasal and bronchial mucus production
(“Dripping nose sap”)

-histamine increases vascular receptor permeability
(“Dripping vascular sap”)

-histamine causes constriction of bronchial smooth muscle
(“Constricted lung branch”)

-histamine functions as a neurotransmitter

• regulates sleep and arousal
  (“Brain tree”)

Question 9

H2 activation

Answer 9

coupled to Gs protein
(“Honeypot with 2”S””)

-mediates gastric acid secretion
(“Golden gastric honey”)

Question 10

Name 1st Generation Anti-Histamine drugs

Answer 10

Diphenhydramine
Dimenhydrinate
(“Dragonfly fairy”)

Chlorphenamine
(“Color fairy”)

Hydroxyzine
Meclizine
Promethazine
(“fairy cuiSINE”)

Question 11

H1 antagonists can treat …

Answer 11

-are 1st line therapy for type-1 allergic reaction􏰀 hives, allergic rhinitis
(“Fairy dust and dander”)

-treat vestibular nausea or motion sickness lipophilic􏰀 → enter CNS􏰀 → act on vestibular system and brainstem
(“Seasick fairy sailors”)

treat extrapyramidal side effects caused by antipsychotics (acute dystonia)
(“Falling “extra parking cone”)

• antimuscarinic effects re-establish dopaminergic- cholinergic balance

Question 12

H1 Antagonists Side Effects

Answer 12

-can cause drowsiness

• lipophilic􏰀 → cross BBB → 􏰀central effects
  (“Sleeping under brain tree”)

-antagonize peripheral and central muscarinic receptors

• pupillary dilation
• dry mouth
• urinary retention
• constipation
• exacerbation of glaucoma
• delirium
  ​(“Anti-muscarinic tea party”)

1st generation H1 blockers antagonize serotonin receptors in the CNS
(“Cut smiley face cake”)

• stimulate appetite and weight gain anti-serotonergic effects
  (“Stuffed fairy”)

-1st generation H1 blockers antagonize alpha-1 receptors􏰀 dizziness and hypotension

(“Extinguished single alpha candle”)
(“Fainted fairy”)

-cause cognitive impairment in the elderly (central antihistamine and antimuscarinic effects)
(“Delirious elderly man”)

​

Question 13

Name 2nd Generation H1 Antagonists

Answer 13

Fexofenadine
Loratidine
Cetirizine

(“Fox, satyr, and rat”)

Question 14

difference between 1st and 2nd Generation H1 antagonists

Answer 14

2nd generation H1 blockers are less lipophilic →􏰀do not cross BBB→ 􏰀less sedating

• also less antimuscarinic, antiserotonergic, or anti- alpha

(“Fox, satyr, and rat stand outside the brain tree”)