Autocoids (Ex2) Flashcards
1
Q
What are four autocoids?
A
Histamine
Serotonin
Prostaglandins
Peptides
2
Q
What induces histamine release?
A
- physical injury
- insect stings and reptile venom
- allergy and anaphylaxis
- disease
- drugs and chemicals
3
Q
What are four drugs that inhibit histamine release?
A
- Cromolyn sodium
- Catecholamines
- Phosphodiesterase inhibitors
- Glucocorticoids
4
Q
Major H1-Mediated Effects
A
- contraction of smooth muscles of GI, bronchioles, uterus, and large blood vessels
- vasodilation of vessels, then contraction, leading to increased permeability, edema, hypotension, and hypovolemic shock
- stimulation of exocrine secretion
- positive inotropic effect
- CNS stimulation, inhibition of appetite
5
Q
Major H2-Mediated Effects
A
- gastric acid secretion
- positive inotropic effect and increased heart rate
6
Q
Major H3-Mediated Effects
A
- inhibiting release of histamine, serotonin, norepinephrine, and acetylcholine
7
Q
First Generation H1-Antagonists
effects, examples
A
- cross blood-brain barrier, so cause sedation
- anti-cholinergic effects
- Ehylenediamines, Ethanolamines, Alkylamines, Piperazines, Phenothiazines, Methyl piperidines
8
Q
Second Generation H1-Antagonists
features, effects, examples
A
- non-sedating, do not cross BBB
- more receptor selectivity
- anti-inflammatory effects by stabilizing mast cells
- less anti-cholinergic
- piperidines, ketotifen
9
Q
Pharmacokinetics of H1-Antagonists
A
- readily absorbed orally
- wide distribution
- duration is 3-12 hours
- metabolized by liver
- excreted in urine
- most are enzyme inducers
10
Q
Therapeutic uses of H1-Antagonists
A
- allergy and anaphylaxis (not effective if histamine is already released, more preventative)
- anti-motion sickness (only 1st gen)
- Ketotifen used to treat allergic conjunctivitis, and prevention of asthma
- Not effective in bronchial asthma (must use beta-2 agonist)
11
Q
Side Effects of H1-Antagonists
A
- first gen causes sedation
- anticholinergic effect (atropine-like)
- GI irritation
- alpha adrenergic blocking effect
- cardiac arrhythmias
12
Q
What are 4 H2-Antagonist Drugs?
A
- Cimetidine
- Ranitidine
- Famotidine
- Nizatidine
13
Q
H2-Antagonist MOA
A
- competitive antagonist to H2 receptors (reduces gastric acid output)
- Cimetidine has immunomodulatory effects: inhibits suppressor T cells and enhances cell-mediated immunity
- Ranitidine and Nizatidine inhibit acetyl cholinesterase, stimulating GI motility
- do not cross BBB
14
Q
Therapeutic uses of H2-Antagonists
A
- peptic or duodenal ulcer
- gastric erosive disease
- gastroesophageal relfux disease
- Cimetidine: equine melanoma
- Ran or Niz: use as prokinetic (stimulate GI motility)
15
Q
Cisapride
classification, uses
A
- 5-HT4 receptor agonist in enteric neurons
- stimulates GI motility and secretions
- used as a prokinetic