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85 Cards in this Set
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- Back
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salicyclic acid derivative that irreversibly acetylated and inactivates Cox 1(inhibits prostaglandin synthesis)
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Acetylsalicylic Acid (Aspririn)
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What is an antithrombotic effect of Acetylsalicylic acid (Aspirin)
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irreversible acetylation and inactivation of the COX enzyme in platelets
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What is the rate limiting step of aspirin and is it absorbed rapidly or slowly?
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Dissolution and rapidly
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in the small intestine, what pH increases dissolution
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Increased pH (Alkalyne)
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absoroption of salicylate(aspirin) is not limited because.
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the large surface area of the small intestine
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Is aspirin poorly distributed or rapidly distributed?
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Rapidly and widely distributed
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is aspirin highly bound or not? can it cross the placental and blood brain barriers?
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Aspirin is highly bound and can cross both barriers
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what changes so that the renal clearance of free ionized salicylate increases from 3% to about 80%>
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urinary pH changes from 5 to 8 (becomes more alkalyne)
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Common adverse effects of aspirin?
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GI disturbances, tinnitus and hearing loss, renal medullary ischemia, pulmonary edema, reduction of erythrocyte life span,
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misoprostol (cytotec) is...
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a prostaglandin analogue that has anti-ulcer effects
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a common adverse effect that is also a sign that indicates adequate plasma concentrations of aspirin
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Tinnitus
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Why should Aspirin be discontinued 5-7 days before surgery
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to prevent excessive perioperative bleeding
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What type of hypersensitivity occurs with Aspirin
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Type 1, IgE antibodies are involved
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What is the Aspirin Triad in asthma patients
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Aspirin sensitivity, asthma, and nasal polyps
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Using salicylates (especially aspirin) in children with varicella infections and flu like illnesses leads to increased risk of what?
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Reye's Syndrome
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Can acetaminophen be used as an antipyretic in kids?
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Yes
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When can salicylates be used in pregnancy?
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only when benefits justify the risks and always avoided in last 3 months of pregnancy
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Salicylism is what?
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chronic salicylate intoxication. high dosages or prolonged therapy with high dosages
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What has happened when adults ingest 10-30g doss of aspirin or children have taken 4g
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Death
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most common manifestations in salicylate overdosage?
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acid-base and electrolyte disturbances, dehydration, hyperpyrexia, and hyperglycemia
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most common manifestations of chronic intoxication in adults? in children?
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adults-tinnitus and hearing loss
children-hyperventilation and CNS effects |
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to treat salicylic overdosages
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supportive therapy, remove the drug(ipecac syrup), prevent further absorption(activated charcoal), correct the disturbances, and ENHANCE SALICYLATE ELIMINATION(urine pH to 7.5 or higher)
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Major drug interactions with Aspirin (salicylic acid)
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1. protein-bound drugs(oral anticoagulants, sulfonylureas, penicillins)
2. anticoagulants-increases risk of bleeding 3.Corticosteroids-corticosteroids increase renal clearance 4. NSAIDS-potential GI effects |
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Main use and dosage for aspirin?
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use-mild to moderate pain, fever, inflammatory disease
dose-adults: 2.4-3.6g daily children: 3.6-5.4g daily |
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salicylic acid derivative that works as an analgesic and antiinflammatory, has little antipyretic effect
Works by reversibly inhibiting Cox enzyme |
Diflusinal (dolobid)
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Diflusinal is contraindicated in...
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those with history of hypersensitivity to aspririn and other NSAIDS
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Diflusinal is used for:
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acute or long term relief of mild to moderate pain
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Is Diflusinal recommended as an antipyretic?
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No
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NSAIDS inhibit COX1, COX2, or both pathways? and what are NSAIDS?
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Both COX1 and COX2.
analgesic and antipyretic but mostly anti-inflammatory |
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Main uses of NSAIDS
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Rheumatoid arthritis
Osteoarthritis Juvenile rheumatoid arthritis |
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What drugs cannot be used for rheumatoid arthritis
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Ketorolac, Meloxicam, and Mefenamic acid
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What drugs cannot be used for Osteoarthritis?
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Ketorlac and Mefenamic Acid
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Drugs that can be used for Juvenile Rheumatoid Arthritis?
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Tolmetin and Naproxen
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Are NSAIDS rapidly or poorly absorbed? What is the pKa of NSAIDS?
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rapidly and completely absorbed
pKa is ACIDIC |
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NSAIDS should be used with caution in patients with...
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compromised cardiac function, HTN, and other condition that predispose to fluid retention
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Which NSAID medications have a possibly of Strong Headaches, dizziness, and somnolescence/drowsiness
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INDOMETHACIN, fenoprofen, and ketorolac
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This increases the adverse reactions to NSAIDS so it must be used with care
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Age. Caution in the elderly
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Major problems with NSAIDS:
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1. Gastric/duodenal ulcers, intestinal ulceration, gingival ulcer
2. Autoimmune hemolytic Anemia(Type 2)-reversible 3. Hepatitis, jaundice |
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Asthma, anaphylaxis, acute respiratory distress, rapid fall in blood pressure, angioedema, dyspnea are signs of what? and which NSAID has shown this?
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Hypersensitivity ; Ibuprofen
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Should NSAIDS be avoided in nursing mothers?
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Yes. Can cause cardiovascular events in the infant
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NSAIDs should be avoided in the 3rd trimester of pregnancy? True or false?
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True
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NSAIDS inhibit the prostaglandin synthesis which can induce the closure of what during pregnancy?
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the fetal ductus arteriosus
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Major uses of NSAIDS?
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rheumatoid arthritis, osteoarthritis, juvenile rheumatoid arthritis, closure of persisitent patent ductus arteriosus
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the only COX2 inhibitor still on the market is?
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Celecoxib (celebrex)
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How does celebrex work?
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as an antiinflammatory, analgesic, antipyretic
Inhibits the COX2 but not the COX1 |
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Celecoxib should not be given to patients who have allergic type reactions to?
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Sulfonamides
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Main uses of Celecoxib(Celebrex)
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Osteoarthritis, Rheumatoid Arthritis, acute pain
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Acetaminophen weakly inhibits
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COX1 and COX2 enzymes
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What is the toxic level of acetaminophen?
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4000mg per day
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When acetaminophen is broken down by CYP P450 it is:
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highly reactive and toxic to the liver and the kidney
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The most serious adverse reaction to acetaminophen is
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hepatotoxicity
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A medication that restores glutathione levels and is a specific antidote for APAP toxicity? and when must it be given?
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Oral N-acetylcysteine (Mucomyst) must be given within 8 hours of ingestion
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Main use of APAP?
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Analgesic, antipyretic
Anti-inflammatory effects are much weaker |
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NSAID: Enolic Acid Derivatives: Oxicams
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1. Piroxicam (Feldene)
2. Meloxicam (Mobic) |
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NSAIDS: Non-acidic Compound(Alkanones)
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Nabumetone
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How does cyclosporine work?
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inhibits SIGNAL 1 by inhibiting calcineurin phosphatases
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How does Cyclosporine effect the cell cycle?
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reversibly inhibits lymphocytes in the G0 and G1 phase
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Most common adverse reaction of cyclosporine?
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Nephrotoxicity
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Main uses of cyclosporine?
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allogeneic transplants: prevent rejection in kidney, liver, and heart transplants
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Hydrolyzed to MPA which inhibits SIGNAL 3
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Mycophenolate (Cellcept)
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Adverse Reactions of Mycophenolate(Cellcept)?
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SEVERE NEUTROPENIA, vomiting, diarrhea, infections
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Main uses for mycophenolate(cellcept)
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allogeneic transplants: prevent rejection in renal, hepatic, and cardiac transplants
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What is Muromonab-CD3
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Murine monoclonal antibody blocks T-cell receptor
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Only adverse reaction to Muromonab?
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Hypersensitivity to murine products
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Serum Ig of horses reduces T-cells in the blood and affects SIGNAL 1
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Lymphocyte immune globulin (Atgam)
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What are common adverse reactions of Lymphocyte immune globulin?
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sensitivity for equine serum, chills, fever, vertigo, leukopenia, systemic infections
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What pregnancy category is lymphocyte immune globulin?
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Category C
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What are the uses of Lymphocyte Immune Globulin
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minimize rejection in renal transplant patients
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humanized IgG1 monoclonal antibody
Blocks SIGNAL 3, inhibits IL-2 binding |
Daclizumab (Zenepax)
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Adverse reactions of Daclizumab? Uses?
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ADR: GI disorders
Uses: minimize allograft rejection of renal and cardiac transplant patients |
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What is Rho Immune Globulin (RhoGAM) and what does it do?
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sterile, concentrated solution of immune globulin
Effects SIGNAL 1, produces high levels of Rho antibodies |
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Rho Immune Globulin (RhoGAM) is contraindicated in?
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Rho-positive patients and in Rho-negative patients who have already developed Rho antibodies
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Uses of Rho Immune Globulin (RhoGAM)
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prevent Rho hemolytic disease of the newborn (Erythroblastosis fetalis) administer in 72 hrs
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Human plasma that supplies a broad spectrum of IgG antibodies against antigens
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Immune Globulin (Gammagard)
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Systemic Allergic reactions and the possibility for transmission of bloodborne pathogenic agents are adverse reactions of what medication?
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Immune Globulin (Gammagard)
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Uses of Immune Globulin(Gammagard)
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Hypogammaglobulinemia, idiopathic thrombocytopenic purpura, Guillain-Barre syndrome, prevent infection in HIV patients
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3 major classes of interferons are:
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Alpha, Beta, Gama
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What is Interferon Beta-1b (Betaseron)
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works as an antiproliferative and immunoregulator
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Most serious adverse reactions of Interferon Beta-1b (Betaseron)
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depression, suicidal ideation, injection site reactions
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What are ADRs of Gamma-1B(Actimmune)? and What is its use?
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ADR: flu-like symptoms
USE: chronic granulomatous disease |
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IgE antibodies fix to mast cells and blood basophils. release of histamine and leukotrienes
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Type 1 or anaphylactic reaction
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Antagonists of Type 1 reactions
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Prednisone, isoproterenol, epinephrine, theophylline
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IgG and IgM antibodies target cells in circulatory system
Manifestions: Rho hemolytic disease of the newborn, autoimmune hemolytic anemia |
Type 2 or Cytotoxic reactions
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Most common reaction. IgM and IgG generate drug-antibody complexes that deposit in blood vessel walls, increase vascular permeability
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Type 3 or Serum Sickness or Arthus Reactions
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Mediated by sensitized T lymphocytes and macrophages e.g. Contact dermatitis
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Type 4 or Cell-Mediated reactions
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