PHARM Flashcards
What is the MOA of first generation antihistamines?
They DOWNREGULATE constitutive H1 receptor activity, not antagonists but INVERSE AGONISTS
What are the adverse effects of first generation antihistamines in adults?
They have a sedative effect b/c lipophilic and cross the BBB
What paradoxical effect may first generation antihistamines have in children?
Paradoxical agitation
Below what age is it the use of first generation antihistamines contraindicated? Why?
Below the age of 2 because there have been a small number of deaths associated
Why were second generation antihistamines developed? When is the onset of action? Peak serum level?
Developed LIPOPHOBICALLY to avoid the sedative effects of Gen1. Onset is in one hour and peaks at 2-3 hours.
How are third generation antihistamines similar to second generation?
3rd generations are METABOLITES of second generation
What are the antiinflammatory properties of 3rd generation antihistamines?
1) They decrease release of mast cell mediators 2) they downregulate adhesion molecules and 3) they inhibit the production of IL-4 and IL-13
What receptor do beta agonists for asthma act on? What is the route of administration?
Relative affinity for beta 2 (though they can cause tachycardia and tremors) and they are inhaled
What is an MDI?
Metered Dose inhaler
What is the problem with chronic use of a beta agonist for asthma?
It may 1) Increase mortality and 2) It may lead to tolerance
Is it best to use a beta agonist daily or PRN? Why?
PRN because daily use is associated with increased death and tolerance
Why was salmeterol better than other beta-agonists? What was the problem and how is it circumvented?
Because it was long-acting but it was associated with INCREASED DEATH; however, co-administration with an inhaled steroid was not associated with increased death
Why might the fact that corticosteroids reverse B-2 downregulation be important?
Because they improve mortality in ppl who use Beta-agonists chronically; probably because they decrease tolerance
Why do people get a first pass effect from inhaled corticosteroids? What pathology in GI is associated?
Because they swallow their inhalations! Candida esophagitis
A pregnant asthmatic in need of an inhaled corticosteroid should be given:
Budenoside
Why would a person on inhaled steroids have a scratchy throat? What other oral pathology may present?
Because the steroid can deposit on the oropharynx and larynx; they can get oral thrush
Which types of inhaled steroid devices have reduced risk of dysphonia?
Those with dry powder
How can a person asthma medications reduce the risk for thrush?
Rinsing of the mouth after administration
What are 4 systemic side effects of corticosteroids?
Osteoporosis, adrenal suppression, and ocular effects. In children it can cause short-term growth deceleration.
What are the two types of leukotriene modifying drugs?
1) 5-lipooxygenase enzyme inhibitor 2) Leukotriene receptor antagonist
Name a 5-lipoxygenase inhibitor
Zileuton
Name 2 LTD4 receptor antagonists:
Zafirlukast and Montelukast
What is the MOA of theophylline? Safe for pregnancy?
It is similar to caffeine and prevents the breakdown of cAMP which allows for increased calcium and bronchodilation; YES it is safe in pregnancy
Why would coffee help ameliorate Sx of asthma?
It would act like theophylline by decreasing breakdown of cAMP
