Autacoids Flashcards
What are the 4 autacoids
Histamine
Serotonin
Prostaglandins
Peptides
What drugs inhibit histamine release
Cromolyn sodium
Catecholamines
Phosphodiesterase inhibitors
Glucocorticoids
Major H1 Mediated Effects on Vessels and Smooth Muscle
Contraction of smooth muscles of: GI, bronchioles, uterus, Large blood vessels
Vasodilation followed by contraction leading to increased permeability, edema, hypotension and hypovolemic shock
Other H1 Mediated Effects
Stimulation of exocrine secretion
Positive inotropic effect
CNS stimulation, inhibition of appetite
Major H2 Mediated Effects
Gastric acid secretion
Positive inotropic effect and increased heart rate
H1 antagonists are __
Antihistamines
H1 Antagonists - First Generation Characteristics
Crosses BBB
Sedating
H1 Antagonists First Generation Drugs
Diphenydramine Promethazine Cyproheptadine Terfenadine Meclizine
H1 Antagonists Second Generation Characteristics
Non-sedating
Does not cross BBB
More receptor selectivity
What do some second generation antagonists exhibit
non-competitive antagonism
anti-inflammatory effects by stabilizing mast cells
Second generation drugs
Piperidines (Terfenadine, astemizole, loratadine)
Ketotifen (noncompetitive H1 agntagonist)
Do first or second generation drugs have a longer duration of action
Second generation (12-24 hrs)
**First generation is 3-12 hrs
H1 Antagonists are readily absorbed ___
Orally
H1 Antagonists are metabolized by ___ and excreted by ___
Metabolized by the liver and excreted in the urine
Which H1 drug is used as an antiemetic, antitussive and sedative
Diphenhydramine
Which H1 drug is available as opthalmic for treatment of allergic conjunctivitis and orally as adjunctive for asthma prevention
Ketotifen
Side effects of H1 Antagonists
Anticholinergic effect
GI irritation
Alpha adrenergic block (phenothiazines)
Which two H1 Antagonists are associated with Cardiac Arrhythmias
Terfenadine and Astemizole
What are the H2 Antagonist drugs
Cimetidine
Ranitidine
Famotidine
Nizatidine
Do H2 Antagonists cross the BBB
NO
Cimetidine effects
Immunomodulatory
Inhibits suppressor T cells
Enhances cell mediated immunity
Ranitidine and Nizatidine effects
Cholinergic activity by inhibiting acetyl cholinesterase –> stimulates GI motility
Uses for H2 Antagonists
Peptic Ulcer
Gastric erosive disease
Gastroesophageal reflux disease
Duodenal ulcer
Cimetidine is used in the treatment of equine ____
Melanoma
Ranitidine or Nizatidine can be used as a ___
Prokinetic