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62 Cards in this Set
- Front
- Back
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What is dimenhydrinate?
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1st generation H1 blocker
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What is diphenhydramine?
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1st generation H1 blocker
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What is doxylamine?
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1st generation H1 blocker
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What is hydroxyzine?
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1st generation H1 blocker
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What is cyclizine?
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1st generation H1 blocker
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What is meclizine?
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1st generation H1 blocker
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What is promethazine?
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1st generation H1 blocker
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What is fexofenadine?
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2nd generation H1 blocker
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What is loratadine?
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2nd generation H1 blocker
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What is desloratadine?
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2nd generation H1 blocker
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What is cetirizine?
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2nd generation H1 blocker
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What is cimetidine?
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H2 blocker
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What is nizatidine?
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H2 blocker
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What is famotidine?
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H2 blocker
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What is ranitidine?
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H2 blocker
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What is histamine?
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an autocoid, an important mediator of immediate allergic and inflammatory reactions (type 1 HS) and a NT in the brain and gut
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As a NT, is histamine excitatory or inhibitory?
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generally excitatory (NT in the brain and gut)
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what are the 4 ways histamine is released?
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immunologic, chemical, mechanical and by gastric stimulation
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Where are H1 receptors found?
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smooth muscle, endothelium and the brain
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Where are H2 receptors found?
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gastric mucosa, cardiac muscle, mast cells, the brain
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Where are H3 receptors found?
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presynaptic in the brian and myenteric plexus - modulates the release of other NTs
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Where are H4 receptors found?
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eosinophils, neutrophils and T cells
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What are the effects of histamine on the CV system?
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decreases systolic and diastolic BP, increases vascular permeability (H1), decreases atrial concratactility, directly increases contractility and pacemaker activity; indireclty causes reflex tachycardia
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What are the effects of histamine on the GI?
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smooth muscle contractionan dgastric acid secretion by increasing cAMP and thus protien kinase
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What is the effect of histamine on bronchiolar smooth muscle?
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constriction - problematic in patients with bronchial asthma or CF
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What is the effect of histamine on the uterus (in women)?
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susceptible to anaphylactic reactions
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What are the effects of histamine on nerve endings?
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pain and itching, modulates NT release - plays a role in alertness and attentiveness, presynaptic (H3) plays a role in HT release in the CNS and ENS
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what is the "triple response"
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1. localized red spot after histamine injection followed by 2. wheal (edema) and 3. flare (vasodilation)
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what is the physiological antagonist of histamine?
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epinephrine
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What inhibits the release of histamine?
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cromolyn -reduces mast cell degranulation; and nedocromil
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What are H1 blockers used for?
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to treat allergic reactions - rhinits, urtircaria; and motion sickness
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Are H1 blockers reversible or irreversible and competitive or non-competitive?
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reversible and competitive
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What are the adverse effects of H1 blockers?
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1. sedation and antimuscarinic effects (1st gen > 2nd gen), 2. paradoxical excitation and convulsions in kids with high doses, 3. poastural hypotension (elderly) due to cross reaction with alpha receptors, 4. allergic responses, 5. cardiac arrhythmias (2nd generations) 6. teratogenic effects
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What are the drugs interactions of H1 blockers?
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terfenadine and astemizole + ketoconazole, itraconazole or erythromycin = cardiac arrhythmias and inhibition of P450s
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Are 1st or 2nd generation H1 blockers more effective at treating motion sickness?
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1st generation H1 blockers
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What is diphenhydramine used for?
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to treat motion sickness, hay fever, urticaria and chemo induced vomiting
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What are the major adverse effects of diphenhydramine?
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VERY SEDATING and strong anti-cholinergic effects
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What is dimenhydrinate used for?
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motion sickness
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What is doxylamine used for?
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a sleep aid due to the marked sedation
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What is cyclizine used for?
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to treat motion sickness
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What is meclizine used for?
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to treat motion sickness and vertigo (it is slightly sedating)
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What is promethazine used for?
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to treat motion sickness and as an antiemetic
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What are the adverse effects of promethazine?
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marked sedation and orthostatic hypotension
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Which H1 blockers,1st or 2nd generation, enter the CNS more readily?
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1st generation, 2nd are less lipid soluble
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what is fexofenadine used for?
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seasonal allergies and urticaria
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When is fexofenadine contraindicated?
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when used with Al or Mg antacids due to a 41% increase in bioavailability
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What are the adverse effects of fexofenadine?
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little to no sedation = peripherially selective; no serious abnormal heart effects
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what is fexofenadine a product of?
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terfenadine
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what is loratadine used for?
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allergies and urticaria
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what is the duration of action and adverse effect of loratadine?
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long duration of action, mild sedative effect but available OTC (claritin)
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What is desloratadine used for?
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allergic rhinitis and chronic urticaria
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what is desloratadine an active product of?
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it is an active metabolite of loratadine, but has no advantages over loratadine
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what is cetirizine used for?
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seasonal allergies and urticaria
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What are H2 blockers used for?
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to treat GERD, peptic ulcer disease and non-ulcer dyspepsia
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are H2 blockers seletive?
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Yes, they are highly selective; they are revesible and competitive inhibitors
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what is the action of H2 blockers?
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bind to gastric parietal cells and reduces gastric acid secretion
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what is the potency of cimetidine, ranitdine, nizatidine and famotidine compared to each other?
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most to least potent: famotidine > ranitidine and nizatidine > cimetidine
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what are the adverse effects of cimetidine?
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CNS dysfunciton, blood dyscrasias, gynecomastia, galactorrhea, decreased sperm count, reversible impotence; reversible liver toxicity and it inhibits P450s - increases effects/toxicities of other drugs
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what are the adverse effects of ranitidine?
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headache and mild diarrhea, reversible hepatitis
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What are the adverse effects of famotidine?
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reversible abnormalities of liver enzymes
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what are the adverse effects of nizatidine?
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reversible abnormalities of liver enzymes
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Of the H2 blockers which is the only one that does NOT inhibit 1st pass gastric metabolism of alcohol?
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famotidine
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