an early candidate for H2-blocking
action, and newer analogs with no effect on H1, H2, or
H3 receptors, have been shown to have significant
analgesic action in rodents when administered into the
central nervous system.
Burimamide,
The analgesia is said to be comparable to that produced
by
opioids
The analgesia is said to be comparable to that produced
by opioids, but tolerance, respiratory depression, and
constipation have not been reported. Although the
mechanism of this action is not known, these compounds
may represent an important new class of
analgesics
In pulmonary function laboratories, (blank) has been
used as a provocative test of bronchial hyperreactivity.
histamine aerosol
TOXICITV & CONTRAINDICATIONS of histamines
Flushing, hypotension, tachycardia, headache, wheals,
bronchoconstriction, and gastrointestinal upset
These effects are also observed after the ingestion of (blank)
(scombroid fish poisoning), and there is evidence that histamine
produced by bacterial action in the flesh of the fish is the major
causative agent.
spoiled fish
should not be given to patients with asthma
Histamine
Histamine antagonists
have smooth
muscle actions opposite to those of histamine, but they act at
different receptors.
Physiologic antagonists,
Physiologic antagonists,
especially epinephrine,
This is important clinically because injection of epinephrine can be
lifesaving in (blank) and in other conditions in which
massive release of(blank) – and other more important mediators
– occurs.
systemic anaphylaxis, histamine
reduce the degranulation of mast cells that
results from immunologic triggering by antigen-lgE interaction.
Release inhibitors
appear to have this effect and have
been used in the treatment of asthma, although the molecular
mechanism underlying their action is not fully understood.
Cromolyn and nedocromil
do not influence the formation or release
of histamine rather they block the receptor mediated response of a
target tissue
H1 receptor antagonist
can inhibit the release of histamine
from the mast cells.
Cromolyn
also appear capable of reducing
histamine release.
Beta 2-adrenoceptor agonists
was
described in 1972, its possible to antagonize the gastric acid-
stimulating activity of histamine. The development of selective H2-
receptor antagonists has led to more effective therapy for peptic
disease.
H2-receptor antagonist - burimamide
Compounds that competitively
block histamine or act as inverse agonists at H1 receptors have been
used in the treatment of allergic conditions for many years.
H1- RECEPTOR ANTAGONISTS
strong sedative effects
1st Generation H1 blockers,
are less sedating
2nd Generation H1 blockers,
readily cross the CNS or the blood-
brain barrier, it can cause sedation, impairment of performance (fine
motor skills, driving skills), anticholinergic/atropine like side effects (dry
mouth, diplopia, blurred vision).
1st generation H1 blockers