Antiinflammatory And Autacoids Flashcards
Excess production of histamines is measured in the urine by
Imidazole acetic acid
H3 antagonist
Clobenpropit
Classic demonstration of histamine effect
Triple response
Wheal
Flush
Flare
The triple response is mediated primarily by which H receptor type? How many histamine receptors are there?
H1
4
Describe all histamine receptor, distribution, and effect
H1 smooth muscle - pain itching bronchoconstriction, vasodilation, local edema
H2 stomach heart mast cells - gastric acid secretion, cardiac stimulation
H3 nerve endings - modulation of other NTs
H4 leukocytes - leukocyte chemotaxis
Most important amine autacoids
Histamine and serotonin
First generation antihistamines
Diphenhydramine
Chlorpheniramine Cyclizine Meclizine Promethazine Hydroxyzine
Similarities and differences in the MOA of first generation and second generation antihistamines
Similarities: both on H1 receptor
Differences: 1st gen: CNS and peripheral with anti motion sickness effect
2nd gen: peripheral only
_________ from interaction between azoles/erythromycin and terfenadine/astemizole
Fatal arrythmias
2nd gen antihistamines
Cetirizine Levocetirizine Loratidine Deslora Fexofenadine Terfenadine Astemizol
H2 receptor antagonist
Cimetidine, ranitidine, famotidine, nizatidine
H2 antagonist that causes gynecomastia
Cimetidine
Chemical name of serotonin
5 hydroxytryptamine or 5-HT
Excess production of serotonin is detected by _____ in the urine
5 hydroxy indole acetic acid (5-HIAA)
Serotonin receptor found in the brain
5 HT1D
5HT2 receptors are found in the
Smooth muscle and platelets
5 HT3 is found in the
Area postrema, sensory and enteric nerves
Prototype antagonis of 5HT2
Ketanserin
Secondary messenger of 5HT3
Ligand gated ion channel
5HT4 prototype antagonist
Tegaserod (partial agonist)
3 things that cause platelet aggregation.
TXA2
Serotonin
ADP
3 things that inhibit plateley aggregation
PGI2
cAMP
Adenosine
DOC for acute migraine, cluster headache
Sumatriptan
Moa of sumatriptan
5HT 1D/1B receptor agonists
MOA of ondansetron
5HT3 receptor antagonist
5HT3 receptor antagonist user for irritable bowel disease
Alosetron
5HT3 receptor antagonist that cause QRS and QT prolongation? Constipation?
Dolasetron
Alosetron
Complex molecules are produced by a fungus found in wet or spoiled grain
Ergot alkaloids
Ergotism
Hallucinations and psychotic like symptoms
Classification of ergot alkaloids
Vasoselective
Uteroaelective
CNS selective
5HT2 antagonist ergot alkaloid that is vasoselective
Ergotamine
Dihydroergotamine
Methysergide
5Ht2 antagonist ergot alkaloid that is uteroselective
Ergonovine
Methylergonovine
antidote for ergotamine is
Nitroprusside
Histamine is metabolized by the enzymes
MAO and DAO
Potent leukotriene bronchdilators for asthma
LTC4
LTD4
LTE4
Leukotriene mediator for chemotaxis
LTB4
Eicosanoid responsible for plateley aggregation
TXA2
Eicosanoid responsible for maintaining PDA
PGE1
Eicosanoid responsible for vascular smooth muscle relaxation particularly peripheral, coronary, and pulmonary blood vessels.
PGI2
Eicosanoid responsible for increasing uterine tone (uterotonic)
PGE2