Case 27: Case 29

1. Give the synthesis and MOA of Histamine 1. MOA of Ergot Alkaloids

-Synthesis:
Histamine is formed by decarboxylation of the amino acid
l-histidine, a reaction catalyzed in mammalian tissues by the
enzyme histidine decarboxylase. Once formed, histamine is
either stored or rapidly inactivated. Very little histamine is
excreted unchanged. The major metabolic pathways involve
conversion to N-methylhistamine, methylimidazoleacetic acid, The ergot alkaloids act on several types of receptors . As
and imidazoleacetic acid (IAA). shown by the color outlines in Table 16–7, the nuclei of both
catecholamines (phenylethylamine, left panel) and 5-HT
(indolethylamine, right panel) can be discerned in the ergoline
nucleus. Their effects include agonist, partial agonist, and
antagonist actions at α adrenoceptors and serotonin receptors
(especially 5-HT1A and 5-HT1D; less for 5-HT2 and 5-HT3); and
agonist or partial agonist actions at central nervous system
dopamine receptors (Table 16–8). Furthermore, some
members of the ergot family have a high affinity for
presynaptic receptors, whereas others are more selective for
postjunctional receptors. There is a powerful stimulant effect
on the uterus that seems to be most closely associated with
agonist or partial agonist effects at 5-HT2 receptors. Structural
variations increase the selectivity of certain members of the
- MOA: family for specific receptor types.
Histamine exerts its biologic actions by combining
with specific receptors located on the cell membrane. Four
different histamine receptors have been characterized and are Case 31:
designated H1–H4; they are described in Table 16–1. Unlike 3. therapeutic uses of, AE, and CI to the use of
the other amine transmitter receptors discussed previously, no eicosanoids
subfamilies have been found within these major types,
although different splice variants of several receptor types
have been described
Case 32:
All four receptor types have been cloned and belong 2. Give the classification of asthma according to
to the large superfamily of G protein-coupled receptors
(GPCR). The structures of the H1 and H2 receptors differ
severity. How would you classify the patient’s
significantly and appear to be more closely related to asthma. Give your basis.
muscarinic and 5-HT1 receptors, respectively, than to each
other. The H4 receptor has about 40% homology with the H 3
receptor but does not seem to be closely related to any other
histamine receptor. All four histamine receptors have been
shown to have constitutive activity in some systems; thus,
some antihistamines previously considered to be traditional
pharmacologic antagonists must now be considered to be
inverse agonists

Case 33
Case 28: 7. Differentiate the different long acting beta-2
7. What is the advantage of ranitidine over agonist use in the treatment of asthma
cemitidine

Case 34:
C3:1. How do you classify ambroxol and
guaiafenisin asa cough medication? Explain the
difference between MOA of a mucolytic and and
expectorant?