Autocoids and therapy of migraines Flashcards
histamine releasers
Morphine, d-tubocurarine, vancomycin, succinylcholine
Heat, cold, exposure to sunlight & X-rays
Insect bites/ stings, venoms
*** may lead to anaphylaxis, side effects, allergies
anaphylactic shock
bronchospasms, angioneurotic edema, and hypotension (due to release, and effects of histamine)
drug of choice against anaphylactic shock
epinephrine
Histamine release inhibitors
β2 agonist- Albuterol, Epinephrine
Mast cell membrane stabilizers- sodium cromoglycate
***Used in bronchial asthma
H1 blockers are used in
allergic conditions
H2 blockers are used in
peptic ulcer
H1 receptor mediated actions
Smooth muscles: bronchoconstriction
Exocrine glands: ↑ secretion
** Postsynaptic H1 in CNS: maintenance of wakefulness
H1 & H2 receptor mediated actions
fall i BP, ↑ cap permeability, headache: due to release of EDRF (NO)**
flush, wheel, flare
H2 receptor mediated actions
H2 receptor on gastric parietal cells
H3 receptor mediated actions
feedback inhibitors
release of histamine, NE & Ach
First generation H1 receptor antagonists
High permeability to BBB
More sedating
antimuscarinic side effects (dry mouth, urinary retention, constipation)
Second generation H1 receptor antagonists
selective H1 antagonism
Poor permeability to BBB (non-/less sedating)
First generation H1 receptor antagonist examples
Dimenhydrinate Diphenhydramine
HIGHLY SEDATIVE, antimotion sickness, antiemetic, sleep aid
Second generation H1 receptor antagonist examples
Fexofenadine
Cetrizine
Loratadine Desloratadine
(NON-SEDATING, more potent, longer acting, no/minimal anticholinergic effects )
Vertigo (Meniere’s disease)
cinnarizine
COX 1
constitutive
COX 2
inducible
PGI2 causes
vasodilation and inhibits platelet aggregation