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30 Cards in this Set

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  • Back
What is an autocoid
This word is derived from the Greek words autos (self) and akos (medicinal agent or remedy)—hence self agent. Autocoids can be thought of as locally acting hormones that involve a wide variety of pharmacological activities. These agents are not secreted into the systemic blood-stream as are true hormones
Name 4 of the principle autocoids within the body
Serotonin; Histamine; Bradykinins; Prostaglandins
What is serotonin
Serotonin is an indole ethylamine found in both plant and animal tissues
What is serotonin derived from
Where is most of the serotonin in the body found
The enterochromaffin cells of the GI tract contain approximately 90%, the CNS contains most of the remaining 10%
How does serotonin exert its actions
Through seven major 5-HT cell membrane receptor subtypes
How is serotonin metabolized
By monoamine oxidase
What are serotonin’s physiologic actions
Neurotransmission; Regulation of the pituitary gland; Vasoconstriction (except for skeletal muscle and heart, where it causes vasodilation); Contraction of GI smooth muscle; Stimulation of pain receptors; Precursor to melatonin
Name a serotonin agonist
What is sumatriptan used for
To treat migraine headaches
What are the adverse effects of sumatriptan
Dizziness and muscle weakness and neck pain
Name three serotonin inhibitors
Ketanserin; Ondansetron; Cyproheptadine
What is the clinical use of ketanserin
Lowers blood pressure
What is the clinical use of ondansetron
Treatment of nausea and vomiting associated with surgery and chemotherapy
What is the clinical use of cyproheptadine
Treatment of smooth muscle constriction in carcinoid tumor
Are ketanserin, ondansetron, and cyproheptadine selective serotonin inhibitors
No. They block 5-HT receptors, but they also inhibit H1 and α receptors
What is the mechanism of action of histamine
Histamine formed from the amino acid histidine exerts its effects by binding to H1 and H2 receptors which are located on cell surfaces and mediate a variety of physiological responses
Where is histamine found within the body
Within granules of mast cells and basophils
What is the physiologic role of histamine
Histamine when released from mast cells causes: Constriction of bronchioles (H. receptors); Constriction of intestinal smooth muscle (H. receptor); Stimulates sensory nerve endings mediating pain (H. receptors) and itching; Lowers blood pressure (H2 receptors); Stimulates gastric HCl secretion (H2 receptors); Increases permeability of skin capillaries (H2 receptors)
What are the clinical uses of histamine
Histamine itself is of no use clinically. However, histamine blockers are very important
Name some H1-receptors blockers and their clinical uses
Diphenhydramine—allergic reaction, motion sickness; Hydroxyzine—allergic reactions; Promethazine—motion sickness
Name a few H2-receptor blockers
Cimetidine; Ranitidine; Famotidine
What are ergot alkaloids
A group of compounds produced by the fungus Claviceps purpurea
What is the mechanism of action of the ergot alkaloids
The ergot alkaloids interact with adreno-receptors, 5-HT receptors, and dopamine receptors
What are the physiologic actions of the ergot alkaloids
Hallucinations and psychoses at high doses; Vasoconstriction; Stimulation of uterine muscle
Give some examples of ergot alkaloids
Bromocriptine; Ergonovine; Ergotamine
What is the clinical use of Bromocriptine
What is the clinical use of Ergonovine
Postpartum hemorrhage
What are the clinical uses of Ergotamine
Migraine—ergotamine diminishes cerebral vascular pulsations; Postpartum hemorrhage
What are the adverse effects of the ergot alkaloids
Prolonged vasoconstriction—may result in gangrene (Nitroprusside can be administered to treat ergotamine-induced vasoconstriction); Diarrhea; Nausea, vomiting; Unwanted uterine contraction; CNS psychosis