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28 Cards in this Set
- Front
- Back
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504-2 PHARM: ANTI-INFLAMMATORY DRUGS
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504-2 PHARM: ANTI-INFLAMMATORY DRUGS
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Histidine
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1. Created inside mast cell and basophils
2. Created from a.a. histidine 3. Also found in CNS as neurotransmitter. |
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H1 histamine receptors
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1. Linked to Gq/11
2. stimulation of PLC 3. mediates most allergic rxns |
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H2 histamine receptors
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1. linked to Gs
2. stimulation of of adenylyl cyclase 3. present on gastric parietal cells 4. mediates gastric acid secretion |
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What causes the release of histimine?
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1. released from mast cells and basophils as part of the inflammatory response.
2. also released in response to IgE as part of allergic rxn and anaphylaxis rxn. |
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Histidine's effect on CV
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1. relaxes smooth muscle to decrease BP
2. increase vascular permeability in venules--> edema. |
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Histidine's effect on smooth muscles
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Contracts bronchial and most intestinal smooth muscles.
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Histidine's effect on stomach parietal cells
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Stimulates gastric acid secretion, contributing to ulcers.
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Effect on skin?
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"Wheal" or hives due to edema from increased permeability.
Bright red due to vasodilation. |
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Drugs that affect histamine actions?
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H1 receptor antagonists:
1. benadryl 2. zyrtec 3. claritin 4. allegra H2 receptor antagonists 1. tagamet 2. zantac 3. pepcid |
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Benadryl
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First generation sedating
Competitive reversible blockade of H1 receptors. |
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Clinical uses of benadryl
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Tx allergic rxn and bronchospasms due to anaphylaxis.
Also act as secondary antiemetic and antivertigo actions. For sleep |
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Dramamine
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Tx motion sickness and vertigo
A salt of benadryl |
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"Second generation" Non-sedating Histamine H1 receptor antagonists are?
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1. zyrtec
2. claritin 3. allegra |
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What is mechanism for the drugs above?
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They DO NOT cross blood brain barrier.
No recognition of muscarinic receptors. Prevents action on CNS muscarinic and dopamine receptors. Selective, competitive reversible blockade of H1 receptors. |
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Side effects of First generation vs. Second generation?
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First generation: Penetrates CNS and cross reactivity of muscarinic cholinergic receptors.
Second generation: side effects greatly reduced due to no CNS penetration and limited cross reactivity of muscarinic receptors. |
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What are some examples of H2 Histamine receptor antagonists of first and second generation?
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First generation: Tagamet
Second generation: Zantac and Pepcid |
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Mechanism of pepcid and zantac?
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Selective, competitive reversible blockade of H2 receptors.
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Clinical uses of pepcid and zantac?
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1. Tx of ulcers
2. Tx of immediate hypersensitivity rxn |
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Side effects of G1 or Tagamet?
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Inhibits P450s, therefore affects clearance of drugs.
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Mechanism of Prednisone
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A glucocorticoid
Bind to glucocorticoid receptor leading to transcriptional regulation of genes. Basically, its effects are inside the nucleus. |
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Clinical uses of prednisone
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1. allergy
2. bronchial asthma 3. inflammation 4. autoimmune diseases |
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Side effects of prednisone or glucocorticoids in general?
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1. Cushing's syndrome
2. acute adrenal insufficiency due to abrupt withdrawal |
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Examples of immunomodulary agents?
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1. Interferon Beta-1a (avonex)
2. Interferon Beta-1b (betaseron) |
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Mechanism of action of immunomodulary agents
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Bind to cell surface receptor
Induces a cascade of signaling pathways Causes production of IFN stimulated gene products |
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What are the functions of IFN stimulated gene products?
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1. antiviral
2. antiproliferative 3. causes anti-inflammatory effects 4. reduction in T cell activation 5. decreases cytokines 6. decreases T cells entry into CNS |
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Clinical uses of immunomodulary agents?
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Multiple sclerosis
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Side effects of immunomodulatory agents?
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Generation of neutralizing antibodies
NOTE: IFN beta-1a is glycosylated while 1b is not. |
