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Assessment 06
Pharm - NSAIDS, DMARDS, Analgesics, Asthma/COPD, Immuno-sup
125
Pharmacology
Professional
09/21/2010

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Term
Acetylsalicylic acid (Aspirin)
Definition
acetylation of COX (1&2) enzymes, irreversible inhibition;
inhibits platelet aggregation;
tx inflammation, fever, pain, HA, arthritis, dysmenorrhea, RA (large dose);
SE - GI ulcer, tinnitus, hearing loss, hepatic injufy, Reyes', asthma, inc bleeding time;
CI with bleeding disorders
Term
Acetaminophen (Tylenol)
Definition
NSAID - inhibitor of COX-1,2,(3);
analgesic and antipyretic;
NOT useful for anti-inflammatory;
SE - HEPATOTOXICITY;
No effects on platelets, NO GI IRRITATION
Term
Indomethacin (Indocin)
Definition
NSAID - POTENT;
anti-inflammatory, analgesic, antipyretic;
tx gout, arthritis;
Used to close Ductus Arteriosus;
SE - GI IRRITATION, CNS effects (HA, dizziness, depression), renal dysfxn;
CI in pregnancy
Term
Ibuprofen (Advil, Motrin)
Definition
NSAID - reversible COX inhibitor;
Alter platelet (prolonged bleeding), anti-inflamm, antipyretic, analgesic;
tx RA (3200mg), pain (400mg/6hrs);
SE- GI irritation (less than others);
CI in pregnancies
Term
Naproxen (Aleve)
Definition
NSAID - reversible COX inhibitor;
Alter platelet (prolonged bleeding), anti-inflamm, antipyretic, analgesic;
Long half-life - 14hrs, so 2xday dosing;
SE- GI irritation
Term
Oxaprozin (Daypro)
Definition
NSAID - reversible COX inhibitor;
Alter platelet (prolonged bleeding), anti-inflamm, antipyretic, analgesic;
LONG HALF-LIFE - 40hrs, once a day;
SE- GI irritation
Term
Ketorolac (Toradol)
Definition
NSAID - heteroaryl acetic acid deriv;
POTENT analgesic, moderate anti-inflamm;
IM, oral, parenteral admin;
SHORT-TERM USE ONLY;
tx post-op pain and inflamm, topical for eye inflamm (alergies or post-op);
Term
Diclofenac (Voltaren)
Definition
NSAID - heteroaryl acetic acid deriv;
potent COX inhibition;
tx RA, OA;
SE - GI, elevation of hepatic aminotransferase activities;
CI for pregnancy
Term
Anthrotec (trade name)
Diclofenac + Misoprostol
Definition
NSAID + PGE1 agonist - heteroaryl acetic acid deriv;
gastric protection
Term
Misoprostol (Cytotec)
Definition
PGE1 analog;
gastric protection
Term
Piroxicam (Feldene)
Definition
NSAID - Enolic Acid;
Anti-inflamm, antipyretic, analgesic;
Equiv w/ asprin, indo, naproxen;
LONG HALF-LIFE - 50hrs, one a day;
SE - GI, RENAL (high risk);
Drug interaction - lithium (reduce clearance)
Term
Meloxicam (Mobic)
Definition
NSAID - Enolic Acid;
More selective for COX2;
LONG HALF-LIFE - one a day;
tx OA, RA;
SE - GI (better than others)
Term
Celecoxib (Celebrex)
Definition
NSAID - selective COX2;
anti-inflamm, antipyretic, analgesic;
tx OA, RA, acute pain, dysmenorrhea;
SE - CV, some GI uleration, dyspepsia, inhibits labor, renal alteration, hypersensitivity rxns;
Drug interaction- "heart meds", diuretics, coumadin
Term
Methotrexate (*Rheumatrex*)
Definition
DMARD - inhibits DHFR to inhibit purine biosynth;
tx RA!, leukemias, psoriasis, immunosuppressor (dec Igs, TNF, IL-1,6);
SE - hepatotoxicity, infections, teratogenic;
CI - poor renal fxn, NSAIDs dec clearance, pregnancy (Cat X!)
Term
Leflunomide (Arava)
Definition
DMARD - inhibits pyrimidine synth;
tx mild RA;
SE - skin rash, hepatic toxicity (BLACK BOX!), long-term teratogen (1-2 yrs to clear, use cholestyramidine to conjugate), myelosuppression (bone marrow);
Term
Sulfasalazine (Azulfidine)
Definition
DMARD - prodrug;
met. to sulfapyridine (unknown benefit) and 5ASA (therapeutic);
tx RA, UC, Crohn's;
SE - GI, DEC. WBCs
Term
Hydroxychloroquine (Plaquenil)
Definition
DMARD - anti-malaria;
2nd line for mild RA;
long onset (3-4 mo.) but well tolerated;
SE - nausea, gastric pain, HEMOLYSIS, retinal damage (visual symptoms!)
Term
Gold (Myochrysine) (Aurolate)
Definition
DMARD - unknown mech;
tx. primarily for RA, once was 1st-line choice;
IM admin;
SE - skin, mucous membranes (mouth 15%), renal, blood dyscrasias
Term
Etanercept (Enbrel)
Definition
DMARD - TNF inhibitor;
Reduce circulating TNF-a and block action at receptor;
mech - fusion of 75 TNF receptor to human IgG;
produced in CHO cells (hamster);
admin SC injection 2x a week (3-4 day half life);
tx RA who don't respond to other DMARDs, psoriatic arth, AS, plaque psorisis;
SE - injection site rxn, infection, auto-Ab
Term
Infliximab (Remicade)
Definition
DMARD - TNF inhibitor;
Reduce circulating TNF-a and block action at receptor;
chimeric IgG1 monoclonal Ab, induces lysis of activated TNF-alpha expressing cells;
IV admin 0 and 2 weeks, every other month;
tx RA, Crohn's, psoriatic arth, AS, UC, plaque psoriasis;
SE - injection site rxn, infection, auto-Ab
Term
Adalimumab (Humira)
Definition
DMARD - TNF inhibitor;
Reduce circulating TNF-a and block action at receptor;
Human monoclonal anti-TNF-alpha Ab;
SC injection, every other week;
tx RA, AS, Crohn's, psoriatic arthritis, plaque psoriasis;
SE - injection site rxn, infection, auto-Ab
Term
Simponi (Golimumab)
Definition
DMARD - TNF inhibitor;
Reduce circulating TNF-a and block action at receptor;
Human monoclonal Ab;
tx RA and other arthritis;
SC admin, once per month
Term
Cimzia (Certolizumab Pegol)
Definition
DMARD - TNF inhibitor;
Reduce circulating TNF-a and block action at receptor;
Anti-TNF Ab conjugated to polyethylene glycol;
SC injection, once a month;
tx arthritis, Crohn's
Term
Anakinra (Kineret)
Definition
DMARD;
IL-1 receptor antagonist;
Competitively binding to IL-1 type I receptor;
tx - mod to severe RA, tried other DMARDs;
Use after failed TNF-inhibitor therapy;
SC injection;
SE - injection site rxns;
CI - w/ other TNF blocking agents
Term
Abatacept (Orencia)
Definition
DMARD;
T-cell costim blocker;
CTLA4 conjugated w/ IgG, binds CD28 on Tcell, blocks response and cytokines (TNF);
admin IV first 0,2,4 weeks then once a month;
Use after failed TNF-inhibitor therapy;
SE - inc infections (immunocompromised)
Term
Rituximab (Rituxan)
Definition
DMARD;
depletion of B cells;
monoclonal Ab against CD20 on Bcells, dec cytokine production;
tx RA who failed to respond to other TNF antagonists
Term
Salicylate drug interactions (3)
Definition
Oral hypoglycemic, phenytoin, uricosurics
Term
Morphine
Definition
MOR Agonist;
active but conv to M-6-glucaronide (100x potency);
tx mod/severe pain;
4 hr half life - accumulation;
extensive (70%) first pass metabolism;
Use in pts taking MAO-Is;
SE - tolerance, constipation, renal clearance
Term
Hydromorphone (Dilaudid)
Definition
MOR agonist (morphine-like);
oral and parenteral admin;
tx mod/SEVERE pain
Term
Oxycodone (OxyContin)
Definition
MOR agonist (morphine-like);
long acting;
tx mod/severe pain;
high abuse potential
Term
Meperidine (Demerol)
Definition
MOR agonist (morphine-like);
tx mod/severe pain;
50% inactivated, first pass;
less spasmogenic, no miosis, less constipation;
Toxic met. (normeperidine) can accumulate to produce seizure risk;
CI - lethal w/ MAO-inhibitors, CHILDREN
Term
Methadone (Dolophine)
Definition
MOR agonist (morphine-like);
po admin;
tx abuse withdrawl/cravings, dampen peaks/troughs of drug conc during weaning
Term
Fentanyl (Sublimaze)
Definition
MOR agonist (morphine-like);
tx mod/severe pain;
80x potency;
transdermal patch for chronic;
rapid onset, short duration - anesthesia IV;
Use in pts taking MAO-Is;
Term
Remifentanil (Ultiva)
Definition
MOR agonist (morphine-like);
tx mod/severe pain;
rapid onset, short duration - anesthesia IV
Term
Propoxyphene (Darvon)
Definition
MOR agonist (morphine-like);
tx mild pain;
dec efficacy;
renal clearance;
norproproxyphene (metabolite) produces cardiac toxicity;
Term
Codeine
Definition
MOR agonist (morphine-like);
Low affinity, 10% conv to morphine;
oral or parenteral admin;
renal clearance, resistance in 10% caucasians;
tx mild pain, cough suppressant (@brainstem)
Term
MS Contin
Definition
MOR agonist (morphine-like);
long duration (8-12 hrs);
tx severe pain
Term
LAAM
Definition
po admin;
very long half life;
PRODRUG - conv to 2 active metabolites;
tx abuse withdrawl/cravings, dampen peaks/troughs of drug conc during weaning
Term
Buprenorphine (Buprenex)(Subutex)
Definition
MOR partial agonist (low action), KOR antagonist;
dec abuse potential;
po admin;
tx addiction/abuse;
SE - abstinence syndrome (if morph-dependent)
Term
Butorphanol (Stadol)
Definition
opioid mixed agonist/antagonist;
bind and inactivates MOR;
activates KOR;
tx mod/severe pain, but analgesic effect is sl. dec;
no constipation, no respiratory depression;
SE - abstinence syndrome;
Term
Pentazocine (Talwin)
Definition
opioid mixed agonist/antagonist;
bind and inactivates MOR;
activates KOR;
tx mod/severe pain, but analgesic effect is sl. dec;
no constipation, no respiratory depression;
SE - abstinence syndrome;
Term
Naltrexone (ReVia)
Definition
opioid receptor antagonist;
LONG DURATION (24 hrs);
po admin, extensive first pass;
tx alcohol abuse (craving and relapse)
Term
Nalmefene (Revex)
Definition
opioid receptor antagonist;
long duration (4hr);
tx opioid OD
Term
Naloxone (Narcan)
Definition
opioid receptor antagonist;
IV only: rapid onset, short duration (esp compared to morhphine), dose accordingly;
EXTENSIVE P.O. FIRST PASS METABOLISM;
tx opioid OD, reverses respiratory depression;
can cause opioid withdrawal; start low, go slow
Term
Dextromethorphan
Definition
antitussive - cough suppression;
opiate derivative;
no analgesia;
acts on non-opioid receptors;
Term
Loperamide (Imodium)
Definition
opiate derivative;
dec GI motility, peristalsis and secretion = inc absorption;
tx diarrhea;
no CNS effects - doesn't cross BBB
Term
Mu opoid receptor
Definition
analgesia;
dec respiration;
dec GI activity
Term
Delta opioid receptor
Definition
analesia;
GI regulation;
autonomics
Term
Kappa opioid receptor
Definition
analgesia;
hallucinations
Term
CNS opioid effects (7)
Definition
dec respiration (RR and TV);
dec cough;
pupillary constriction/ miosis at high doses (NO TOLERANCE);
nausea and vomiting;
euphoria (bolus IV);
sedation;
seizures (high doses)
Term
Peripheral actions of opoids (5)
Definition
Constipation (dec motility and secretions)- NO TOLERANCE;
Vasodilation;
Urticaria;
Contraction of bladder and sphincter;
Dec uterine contraction
Term
Major drug interactions of Opiates (4)
Definition
Sedatives/hypnotics;
Sympathomimetics;
Antihistamines;
MAO inhibitor antidepressants
Term
MOR and KOR Actions (2)
Definition
inhibit ascending pain paths;
activate decending pain-suppression paths
Term
Diphenhydramine (Benadryl)
Definition
1st Gen antihistamine - ether deriv;
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma
Term
Dimenhydrinate (Dramamine)
Definition
1st Gen antihistamine - ether deriv;
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma
Term
Clemastine (Travist)
Definition
1st Gen antihistamine - ether deriv;
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma
Term
Chlorpheniramine (Chlor-Trimenton)
Definition
1st Gen antihistamine - Alkylamine deriv;
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma
Term
Brompheniramine (Dimentane)
Definition
1st Gen antihistamine - Alkylamine deriv;
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma
Term
Promethazine (Phenagren)
Definition
1st Gen antihistamine - Phenothiazine deriv;
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma
Term
Cyclizine (Marezine)
Definition
1st Gen antihistamine - Piperazine deriv;
Long lasting (4-24hrs);
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma
Term
Meclizine (Antivert)
Definition
1st Gen antihistamine - Piperazine deriv;
Long lasting (4-24hrs);
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma
Term
Hydroxyzine (Atarax)
Definition
1st Gen antihistamine - Piperazine deriv;
Long lasting (4-24hrs);
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma
Term
Triprolidine (Actidil)
Definition
1st Gen antihistamine - Alkylamine deriv;
Sedative, anti-emetic, GI cramps, anticholinergic;
tx allergies, hay fever, rhinitis, urticaria, insect bites, motion sickness & vertigo (antiemetic);
SE - sedation, dystonia, nasal congestion;
CI - asthma
Term
Loratadine (Claritin)
Definition
2nd Gen antihistamine - piperidine deriv;
Longer duration, non-sedating, no anticholinergic fxn, SAFE for asthmatics;
tx allergy, hayfever, rhintis, urticaria, insect bites, contact flora;
SE - mild congnitive disturance, some appetite stimulation
Term
Acrivastine (Semprex)
Definition
2nd Gen antihistamine - Alkylamine deriv.;
Longer duration, non-sedating, no anticholinergic fxn, SAFE for asthmatics;
tx allergy, hayfever, rhintis, urticaria, insect bites, contact flora;
SE - mild congnitive disturance, some appetite stimulation
Term
Cetirizine (Zyrtec)
Definition
2nd Gen antihistamine - piperazine deriv;
appetite stimulation, some sedation;
Longer duration, non-sedating, no anticholinergic fxn, SAFE for asthmatics;
tx allergy, hayfever, rhintis, urticaria, insect bites, contact flora;
SE - mild congnitive disturance, some appetite stimulation
Term
Desloratadine (Clarinex)
Definition
2nd/3rd Gen antihistamine;
high specificity for H1, some muscarinic activity;
LONG HALF LIFE (27hrs);
Term
Olopatadine (Patanol)
Definition
2nd/3rd Gen antihistamine;
INHIBITS RELEASE of histamine from mast cells;
more specific for H1;
tx ocular rhinitis
Term
Azelastine (Astelin)
Definition
2nd/3rd Gen antihistamine;
inhibits histamine, LTs, PAF activity;
LONG HALF LIFE;
tx rhinitis and hay fever;
can use in asthmatics;
SE - somnolence, taste, nasal burning, ST, dry mouth, TERATOGENIC
Term
Levocabastine (Livostin)
Definition
2nd/3rd Gen antihistamine;
MOST SPECIFIC FOR H1;
tx ocular rhinitis;
SE - generally none! (even at high dose)
Term
Mizolastine (Mizollen)
Definition
2nd/3rd Gen antihistamine;
antagonizes PAF and LTD4 bronchoconstriction;
tx allergic rhinitis (+ocular symtpm), urticaria;
non-sedative;
approved in EUROPE
Term
Emedastine (Emedine)
Definition
2nd/3rd Gen antihistamine;
anti-allergic, comp to 2nd gen;
inhibits histamine and LTC4 release (leukocytes);
tx asthma, ALLERGIC CONJUNCTIVITIS
Term
Ebastine (Kestine)
Definition
2nd/3rd Gen antihistamine;
hybrid of 1ST GEN AND 2ND GEN;
anti-LT and anti-bradykinin;
Term
Epinephrine
Definition
Adrenergic Agonist - Bronchodilator;
B1, [B2], a1, a2;
Stim AC to inc cAMP - bronch dilation;
tx asthma, COPD;
inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
Term
Ephedrine
Definition
Adrenergic Agonist - Bronchodilator;
B1, [B2], (some a);
Stim AC to inc cAMP - bronch dilation;
tx asthma, COPD;
inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
Term
Isoproterenol (Isuprel)
Definition
Adrenergic Agonist - Bronchodilator;
B1, [B2];
Stim AC to inc cAMP - bronch dilation;
tx asthma, COPD;
inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
Term
Metaproterenol (Alupent)
Definition
Adrenergic Agonist - Bronchodilator;
[B2] specific - FAST - reliever or rescue admin;
Stim AC to inc cAMP - bronch dilation;
tx asthma, COPD;
inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
Term
Albuterol (Proventil)
Definition
Adrenergic Agonist - Bronchodilator;
[B2] specific - FAST - reliever or rescue admin;
Stim AC to inc cAMP - bronch dilation;
tx asthma, COPD;
inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
Term
Terbutaline (Brethin)
Definition
Adrenergic Agonist - Bronchodilator;
[B2] specific - FAST - reliever or rescue admin;
Stim AC to inc cAMP - bronch dilation;
tx asthma, COPD;
inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
Term
Salmeterol (Serevent)
Definition
Adrenergic Agonist - Bronchodilator;
[B2]specific - SLOW - prevention (esp night-time, exercise use);
Stim AC to inc cAMP - bronch dilation;
tx asthma, COPD;
inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
Term
Formoterol (Foradil)
Definition
Adrenergic Agonist - Bronchodilator;
[B2]specific - SLOW - prevention (esp night-time, exercise use);
Stim AC to inc cAMP - bronch dilation;
tx asthma, COPD;
inhibit release of mediators from mast cells, inhib vasculature perm, promote mucociliary transport;
SE skeletal m. tremor, nausea, vomit, HA, dec BP, inc HR, arrhythmias, PAO2????? (on discussion board)
Term
Atropine
Definition
Cholinergic antagonist - Bronchodilator;
Competitive M blockade;
dec airway SM constriction, dec mucous secretion;
SE - pupillary dilation & cycloplegia (X ciliary m)
Term
Ipratropium (Atrovent)
Definition
Cholinergic antagonist - Bronchodilator;
Competitive M blockade;
short acting and no systemic functions;
dec airway SM constriction, dec mucous secretion;
SE - pupillary dilation & cycloplegia (X ciliary m)
Term
Tiotropium (Spiriva)
Definition
Cholinergic antagonist - Bronchodilator;
Competitive M blockade;
dec airway SM constriction, dec mucous secretion;
SE - pupillary dilation & cycloplegia (X ciliary m)
Term
Theophylline
Definition
Methylxanthine - Bronchodilator;
Inhibit PDE - inc cAMP - bronchodilation;
Block adenosine recept - bronchodilation;
Dec release of mediators - anti-inflamm;
tx asthma/COPD;
chronotropic, ionotropic, inc CNS act, gastric acid sec, inc SK muscle str (diaphragm);
SE - (10-20ug/mL)- nausea, vomit, HA, nervous, insomnia, (>20ug/mL)- hypoK, hyperglycemia, tachycardia, arrhy, NM irritability, seizures
Term
Aminophylline (Quibron)
Definition
Methylxanthine - Bronchodilator;
Inhibit PDE - inc cAMP - bronchodilation;
Block adenosine recept - bronchodilation;
Dec release of mediators - anti-inflamm;
tx asthma/COPD;
chronotropic, ionotropic, inc CNS act, gastric acid sec, inc SK muscle str (diaphragm);
SE - (10-20ug/mL)- nausea, vomit, HA, nervous, insomnia, (>20ug/mL)- hypoK, hyperglycemia, tachycardia, arrhy, NM irritability, seizures
Term
Cromolyn (Crolom)
Definition
Anti-inflamm;
Alt Cl- channel: mast cells (dec degran), eosinophils (dec inflamm), airway nn (inhibit cough), dec bronchial hyperactivity;
tx asthma,COPD;
SE - TASTE, irritation of trachea (cough/bronchospasm)
Term
Nedocromil (Tilade)
Definition
a Cromolyn - Anti-inflamm;
Alt Cl- channel: mast cells (dec degran), eosinophils (dec inflamm), airway nn (inhibit cough), dec bronchial hyperactivity;
tx asthma,COPD;
SE - TASTE, irritation of trachea (cough/bronchospasm)
Term
Beclomethasone (Beclovent)
Definition
Inhaled Glucocorticoid - Anti-inflamm;
Dec production of inflamm cytokines;
Inc prod of anti-inflamm proteins;
Dec mucus secretion, dec bronch hyperactivity;
tx asthma, COPD;
SE - candidiasis, hoarse, dry mouth, dec bone density, dec growth rate (kids), CUSHINGOID SYNDROME
Term
Budesonide (Pulmicort)
Definition
Inhaled Glucocorticoid - Anti-inflamm;
Dec production of inflamm cytokines;
Inc prod of anti-inflamm proteins;
Dec mucus secretion, dec bronch hyperactivity;
tx asthma, COPD;
SE - candidiasis, hoarse, dry mouth, dec bone density, dec growth rate (kids), CUSHINGOID SYNDROME
Term
Triamcinolone (Amcort)
Definition
Inhaled Glucocorticoid - Anti-inflamm;
Dec production of inflamm cytokines;
Inc prod of anti-inflamm proteins;
Dec mucus secretion, dec bronch hyperactivity;
tx asthma, COPD;
SE - candidiasis, hoarse, dry mouth, dec bone density, dec growth rate (kids), CUSHINGOID SYNDROME
Term
Fluticasone (Flonase)
Definition
Inhaled Glucocorticoid - Anti-inflamm;
Dec production of inflamm cytokines;
Inc prod of anti-inflamm proteins;
Dec mucus secretion, dec bronch hyperactivity;
tx asthma, COPD;
SE - candidiasis, hoarse, dry mouth, dec bone density, dec growth rate (kids), CUSHINGOID SYNDROME
Term
Ciclesonide (Omnaris)
Definition
Inhaled Glucocorticoid - Anti-inflamm;
Dec production of inflamm cytokines;
Inc prod of anti-inflamm proteins;
Dec mucus secretion, dec bronch hyperactivity;
tx asthma, COPD;
SE - candidiasis, hoarse, dry mouth, dec bone density, dec growth rate (kids), CUSHINGOID SYNDROME
Term
Prednisone (Deltasone)
Definition
Oral Glucocorticoid - Anti-inflamm;
Dec production of inflamm proteins;
Inc prod of anti-inflamm cytokines;
Dec mucus secretion, dec bronch hyperactivity;
tx asthma, COPD;
SE - glu intolerance, inc BP and weight, dec bone density, dec growth rate (kids), cataracts, immunosuppression, CUSHINGOID SYNDROME
Term
Prednisolone (Predacort)
Definition
Oral Glucocorticoid - Anti-inflamm;
Dec production of inflamm proteins;
Inc prod of anti-inflamm cytokines;
Dec mucus secretion, dec bronch hyperactivity;
tx asthma, COPD;
SE - glu intolerance, inc BP and weight, dec bone density, dec growth rate (kids), cataracts, immunosuppression, CUSHINGOID SYNDROME
Term
Monteleukast (Singulair)
Definition
Leukotriene receptor blocker - Anti-inflamm;
Block LTD4 - dec bronch reactivity/constriction, dec mucosal secretion, dec airway inflamm;
tx asthma (aspirin-induced);
SE - GI, URI, nausea, otitis
Term
Zafirlukast (Accolate)
Definition
Leukotriene receptor blocker - Anti-inflamm;
Block LTD4 - dec bronch reactivity/constriction, dec mucosal secretion, dec airway inflamm;
tx asthma (aspirin-induced);
SE - GI, HA, inc liver enzymes, CANCER RISK
Term
Zileuton (Zyflo)
Definition
Leukitriene Synth inhibitor - Anti-inflamm;
inhibits 5-lipoxygenase and LT formation (B,C,D,E -4);
dec SM contraction, dec blood vessel perm (leukocyte migration);
SE - inc hepatic enzymes (watch liver func tests), inhibits CYP1A2 (theophylline)
Term
Omalizumab (Xolair)
Definition
Anti-IgE - Humanized antibody;
Dec severity and freq of asthma attacks;
tx severe allergic asthma (step 5/6 treatment, slide 32);
SE - anaphylaxis, cold symptoms
Term
Horse [ATGAM]
Definition
Polyclonal Ab; (use rabbit more) - immunosup;
anti-thmocyte globulin;
Nonspecific binding to T-cells, lose 80-90%;
tx for bone marrow or organ transplant, aplastic anemia;
Neutralizing Abs dev = tolerance;
SE - fever, chills, hypoT, thrombocytopenia
Term
Rabbit [rATG]
Definition
Polyclonal Ab - immunosup;
anti-thmocyte globulin;
Nonspecific binding to T-cells, lose 80-90%;
tx for bone marrow or organ transplant, aplastic anemia;
Neutralizing Abs dev = tolerance;
SE - fever, chills, hypoT, thrombocytopenia
Term
Carimune
Definition
IV immunoglobulin - Immune boost;
tx immunodeficiency;
SE- renal failure
Term
Muromonab (Orthoclone)
Definition
Mouse anti-CD3 Ab - Immunosup;
Tcells in peripheral blood, reversible;
Neutralizing Abs can dev = TOLERANCE;
SE - acute hypersensitivity, systemic cytokine-med symp;
pretreat with high-dose steroids
Term
Abatacept (Orencia)
Definition
Co-stimulation blocker - Immunosup;
Fusion protein - blocks CD28 - dec Tcell prolif and apoptosis;
tx RA;
SE - HA, dizziness, HTN, GI, infections
Term
Belatacept
Definition
Co-stimulation blocker - Immunosup;
Fusion protein - blocks CD28 - dec Tcell prolif and apoptosis;
tx RA;
SE - HA, dizziness, HTN, GI, infections
Term
Alefacept (Amevive)
Definition
Co-stimulation blocker - Immunosup;
Fusion protein of LFA-3/ IgG1;
Binds Tcell CD2 (mostly memory T) - apoptosis;
IM admin;
tx Psoriasis;
SE - lymphopenia (@6-8weeks), secondary skin malignancies, SERIOUS infections, hypersensitivity and injection site rxns
Term
Efalizumab (Raptiva)
Definition
Co-stimulation blocker - Immunosup;
Monoclonal Ab, anti-LFA-1 preventing binding to ICAM-1;
Prevent binding Tcell migration thru endothelium;
SC admin;
tx Psoriasis;
SE - 1st dose rxn, pain, flu-like, periph edema, UTI
Term
Daclizumab (Zenapax)
Definition
CD25 inhibitor - Immunosup;
Block IL-2Ra/CD25 on Tcell;
Does not change lymphocyte #, just prevents prolif;
Long half life - weeks;
No neutralizing Abs develop;
SE - severe acute hypersensitivity
Term
Basiliximab (Simulect)
Definition
CD25 inhibitor - Immunosup;
Block IL-2Ra/CD25 on Tcell;
Does not change lymphocyte #, just prevents prolif;
Long half life - weeks;
No neutralizing Abs develop;
SE - severe acute hypersensitivity
Term
Cyclosporine (Sandimmune)
Definition
Calcineurin inhibitor - Immunosup;
inhibit 1st phase of Tcell activation (block NFAT prod) so no IL-2, IFN-gamma;
Subseq block of B cell act, no IL-4;
SE - Hirsuitism, gingivial hyperplasia, renal tox, HTN, infections, secondary malignancy
Term
Tacrolimus (FK506, Prograf)
Definition
Calcineurin inhibitor - Immunosup;
100X more potent than cyclo;
inhibit 1st phase of Tcell activation (block NFAT prod) so no IL-2, IFN-gamma;
Subseq block of B cell act, no IL-4;
SE - neurotox, CYP3A5 snps, renal tox, HTN, infections, secondary malignancy
Term
Pimecrolimus (Elidel)
Definition
Calcineurin inhibitor - Immunosup;
inhibit 1st phase of Tcell activation (block NFAT prod) so no IL-2, IFN-gamma;
Subseq block of B cell act, no IL-4;
SE - renal tox, HTN, infections, secondary malignancy
Term
Alemtuzumab
Definition
Humanized monoclonal Ab - Anti-CD52;
Immunosup;
Lysis of B&T cells in bone marrow and blood (less in spleen and lymph);
Profound, long-term lymphopenia;
SE - infusion rxn (chills, rigor, nausea, vomit)
Term
Methylprednisolone (Medrol)
Definition
Corticosteroid - Immunosup;
low dose- dec inflam cytokine,
high dose - inc anti-inflamm proteins;
Inhibits T&B cells;
Short-term use;
SE - CNS confusion, psychosis, HPA suppression, steroid withdrawal syndrome
Term
Sirolimus (Rapamune)
Definition
mTOR inhibitor - Immunosup;
Prevents 2nd phase of Tcell activation (G1 arrest);
Prevention of Bcell diff into plasma cell (dec Ig's);
Synergistic w/ cyclo;
SE - hyperlipid, azotemia (inc creatinine, dec GFR), TUMORS, HEPATOTOXICITY and necrosis
Term
Mycophenolate mofetil (CellCept)
Definition
Cell-cycle disrupt - Immunosup;
Inhibits IMPDH - dec purines, cGMP;
T and Bcells - selective to lymphocytes;
Blocks memory B cell response;
SE - GI, infections, tumors
Term
Azathioprine (Imuran)
Definition
Cell-cycle disrupt - Immunosup;
Blocks S phase purine formation;
Inhibits RAC1/CD28 costimulation = apoptosis of memory Tcells;
SE - skin cancer
CI - pregnancy cat D; low TPMT gene product (should genotype), Allopurinol
Term
Methotrexate (*Trexall*)
Definition
Cell-cycle disrupt - Immunosup;
Blocks S phase by inhibiting Dihydrofolate reductase;
SE - GI, severe nausea, vomit, pancytopenia, hepatotoxicity;
CI - pregnancy cat X!!
Pretreat w/ 5HT3-antag and corticosteroid;
Term
Cyclophosphamide (Cytoxan)
Definition
Cell-cycle disrupt - Immunosup;
Prodrug to phosphoramide mustard;
Produce lymphopenia in B cells > T (fewer B);
SE - pancytopenia (incl anemia), acrolein metabolite (hemorrhagic cystitis, tx w/ MENSA), amenorrhea, infertility
Term
Calcitonin (Miacalcin)
Definition
Adjuvant for analgesia/opioids;
esp. for bone metastasis
Term
Phenytoin (Dilantin)
Definition
Adjuvant for analgesia/opioids;
tx neuropathic pain (damage or infiltrate)
Term
Clonazepam (Klonopin)
Definition
Adjuvant for analgesia/opioids;
tx neuropathic pain (damage or infiltrate)
Term
Amitriptyline (Elavil)
Definition
Adjuvant for analgesia/opioids;
tx neuropathic pain (damage or infiltrate)
Term
Desipramine (Norpramin)
Definition
Adjuvant for analgesia/opioids;
tx neuropathic pain (damage or infiltrate)
Term
Clonidine (Catapres)
Definition
Adjuvant for analgesia/opioids;
enhance opioid analgesia
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