Term
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Definition
| -formed from L-tryptophan (hydroxylated and decaroxylated |
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Term
| Where is serotonin found in the body? |
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Definition
-GI (90%) in enterochromaffin cells
-platelets: homeostasis
-CNS is found regionally (neurotransmitter, sleep, sensory perception, and behaviour |
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Term
| What agents are used for migraines? |
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Definition
-"triptans"
-5-HT 1D,ab agonists
-used for ACUTE control of migraines
-C/I in pts with hx of CHD |
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Term
| What drugs have an effect on emesis? |
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Definition
-5-HT 3 antagonists
-ondansetron, granisetron, and butanopride
-useful in chemo emesis
-blocks 5-HT 3 receptors on GI afferents and CTZ |
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Term
|
Definition
-cyproheptadine
-5-HT1A anatagonist
-moderate anticholinergic effects
-used for skin allergies; GI hypermotill |
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Term
|
Definition
-5-HT2A and 5-HT2C antagonist
-reduces platlet aggregation and blood pressure |
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Term
|
Definition
-Buspar
-5-HT1A agonists
-only non-benzo/barb used for anxiety
-not as effective as benzos/barbs |
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Term
| What is the location(s) and effects of H1 histamine receptors? |
|
Definition
-Blood vessels, smooth muscle, heart, CNS
-increase vascular permeability, airway smooth mus contraction, vasodilation and flushing, mucus secretion, pruritus, and neurotransmission in CNS |
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Term
| What are the location(s) and effects of H2 histamine receptors? |
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Definition
-Gastric mucosa, heart, uterus, CNS
-increase gastric acid secretion, respiratory mucus secretion, nasal airway resistance, smooth mus relaxation in lower airways |
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Term
| What are the location(s) and effects of H3 histamine receptors? |
|
Definition
-airways, GI tract, CNS
-decrease histamine synthesis and release from nerve tissue
-decrease neurotransmitter release |
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Term
| What are ethanolamines and what are the applications? |
|
Definition
-1st generation H1-antihistamines
-allergic rhinitis, analphylaxis, insomnia ,motion sickness, parkinsonism, urticaria |
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Term
| What are piperazines and what is there applications? |
|
Definition
-1st generation H1 antihistamines
-hydroxyzine, cyclizine, meclizine
-pruritus, etoh withdrawal, anxiety, vomitting (hydroxyzine)
-motion sickness, vertigo (meclizine) |
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Term
| What is the difference between 1st and 2nd generation H1 antihistamines? |
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Definition
-1st gen are able to cross BBB which explains their sedative effects
-2nd gen are unable to cross BBB hence why they have little or no sedative effects |
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Term
| What anti-histamies were pulled off the market and why? |
|
Definition
-terfenadine (Seldane) and astemizole (hismanal)
-caused QT prolongation
-this may precipitate ventricular tachycardias
--affects CYP3A4 system |
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Term
| What are the common uses of H1 antagonists? |
|
Definition
-Allergies (early phase not late phase)
-Motion sickness
-Emesis (promethazine) |
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Term
| What is the general mechanism for H2 antagonists? |
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Definition
| They reversibly compete with histamine for H2 receptors found on the basolateral membrane of parietal cells. |
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Term
| What is the parietal cell and what is its function? |
|
Definition
-found on the lumen of the stomach
-responsible for secreting acid
-controlled by histamine, ACh, and gastrin |
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Term
| What are the drugs that effect acid production? |
|
Definition
-H2 antagonists compete reversibly with histamine for histamine 2 receptors on basolateral side of parietal cells
-PPI's inhibit the last step in acid production. H/ K ATPase pump |
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Term
| What is the role of protaglandins in GI physiology? |
|
Definition
-Misoprostol (PGE1 meth ester analog)
-Suppresses acid secretion
-stimulates muscuss secretion
-DO NOT USE IN PREGNANCY (oxytocic) |
|
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Term
|
Definition
-complex Al-hydroxide gel of sucrose
- gel binds to ulcer bes
-no GI absorption, constipation possible
-30 min. prior to meals |
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Term
| What are antacids and how do they work? |
|
Definition
-goal is to increase pH >4.0
-neutralize acid
-improves healing
-can cause alkalosis
*Mg (catharsis) Al (constipation) |
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Term
| What are the difference between different antacids? |
|
Definition
|
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Term
| What is peptic ulcer disease and what is the tx goals? |
|
Definition
-H. pylori manifestation
-gaol to relief pain, accel. healing, and irradicate H. Pylori
-use anatcids for systomatic relief prn
-use PPI's and H2 for acid supression with abx (&bismuth) to eradicate H.pylor |
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Term
| How do NSAIDS damage the GI system? |
|
Definition
-Dual effect sytemically
-inhibits COX-->decrese PG's-->inc. acid secretion, lower HCO3+mucus, de. blood flow
-ionization of aspirin in GI epithelial cell causes damage |
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Term
| What is zollinger ellison syndrome? |
|
Definition
-excessive secretion from gastric tumors
-high doses of PPI's for tx |
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