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Pharm test 4 part deux
Lara & Beth
54
Pharmacology
Undergraduate 4
07/20/2012

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Term
Cyclooxygenase Inhibitors
Definition
Anti-Inflammatorhy Drugs and Acetaminophen
Uses(block Cox-2): suppress inflammation, relieve pain, reduce fever
adverse(also blocks Cox-1, bad): gastric ulcer, bleeding, renal impairment
Term
Classification of COX Inhibitors
Definition
*Drugs with anti-inflammatory properties: NSAIDS
*Drugs without anti-inflammatory properties: acetaminophen
Term
Aspirin
Definition
First generation NSAID, bark of willow tree, arthritis pain
Term
Celecoxib
Definition
Second generation NSAID
Term
acetaminophen
Definition
NOT and NSAID: good for fever and pain, NOT inflammation
Term
Aspirin
Definition
-Nonselective COX inhibitor
-analgesic, antipyretic, anti-inflamm.
-suppression of platelet aggregation
-dysmenorrhea
-AD and cancer prevention (colorectal)
-
Term
Aspirin: adverse effects
Definition
GI, bleeding, renal impairment, salicylism, Reye's syndrome (encephalopathy), anaphylaxis
Term
Ibuprofen (Advil, Motrin)
Definition
1st Gen, NSAID. Propionic Acid derivative. Less effective against fever, less GI bleeding, inhibit platelets vs. aspirin
Term
Naproxen (Naprosyn)
Naproxen Sodium (Alleve)
Definition
1st gen. NSAID: very well tolerated, multiple indications
Term
Celecoxib (Celebrex)
Definition
NSAID: 2nd gen. Fewer adverse effects than 1st gen.
uses: osteoarthritis, RA, acute pain, dysmenorrhea, familial adenomatous polyposis (no benefit in preventing colorectal cancer)
Term
Celecoxib (Celebrex) adverse effects
Definition
GI ulceration, CV events, renal tox: sulfonamide allergy, contra-indicated in 3rd trimester, Warfarin, increase risk of bleeding (recent 2 minute commercials re: safety concerns, only 2nd gen NSAID left standing)
Term
Valdecoxib (Bextra)
Definition
2nd Gen NSAID: withdrawn in US following CABG. Hypersensitivity rxn: Steven-Johnson syndrome (fatality risk, black skin), Toxic Epidermal Necrolysis (fatality risk); no demonstrated advantage over other NSAIDS: Pfizer asked to suspend sales
Term
Rofecoxib (Vioxx)
Definition
NSAID: 2nd gen NSAID. Compare to Celebrex COX-2 inhib. VIGOR: Vioxx GI Outcomes Research. More CV w/ high dosage. Compared to Naproxen. Pulled in 2004.
Term
Acetaminophen (Tylenol)
Definition
Uses: analgesic, antipyretic, NOT ANTI-INFLAMMATORY.
Action: inhibits prostaglandin synthesis in CNS
Term
Acetaminophen (Tylenol): adverse effects
Definition
-Hepatotoxicity: 4gm/day=max adult dose
-OD: hepatic necrosis
-Acetylcysteine (Mucomyst, Acetadote) = antidote. Substitutes for glutathione. Mucomyst=oral, unpleasant-vomiting!!!
Term
Metabolism of acetaminophen
Definition
toxic metabolite build-up in liver due to glutathione depletion by ETOH and Acetaminophen OD. CHRONIC (alcoholic + >4g/day)
Term
Glucocorticoid Physiology
Definition
-metabolic effects: inc. glucose
-CV effects: need glu. to maintain BP
-stress effects: fight or flight
-maintain H2O and Na
-Lungs in neonates
Term
Glucocorticoids: therapeutic uses in non-endocrine disorders
Definition
-allergic rxn: inhaled
-asthma: inhaled
-dematologic disorder: cream
-neoplasms: paired w/ something else
-suppression of allograft rejection
-prevention of respiratory distress synd. in neonates
Term
Feedback regulation of glucocorticoid synthesis and secretion
Definition
(can shut down after medicated)
**see p. 3 diagram**
Term
Glucocorticoids: adverse effects
Definition
**adrenal insufficiency: life threatening
*osteoporosis
*cataracts and glaucoma (excess glu)
*PID
***adrenal suppression after weeks of oral glucocorticoids
*infection
*glucose intolerance
*myopathy
*fluid and electrolyte disturbance
*growth retardation
*psychologic disturbances
Term
Glucocorticoid drug interactions
Definition
interactions related to potassium loss, NSAIDs inc. PID, insulin and oral hypoglycemics (T2DM), vaccines(can get disease)************
Term
Glucocorticoid withdrawal
Definition
taper dosage over 7 days, switch from multiple to single doses, taper to 50% physiologic values, monitor for signs of insufficientcy
Term
Rheumatoid Arthritis (RA) treatment
Definition
Autoimmune inflammatory disorder: pannus (loss of cartilage that leads to bone fusion)
Tx: relieve symptoms, maintain joint fx, minimize systemic involvement, delay (not cure) progression of disease
Term
Classes of Antiarthritic Drugs
Definition
NSAIDs: Nonsteroidal anti-inflammatory drugs
DMARDs: Disease-Modifying Antirheumatic Drugs (immune system)
Glucocorticoids: adrenal corticosteroids (don't like to use long term)
Term
Drug Selection for RA
Definition
1) NSAIDs (Celebrex)
2)DMARDs (Methotrexate)
3) Glucocorticoids may be added until DMARDs take effect
Term
Methotrexate (Rheumatrex)
Definition
Antiarthritic drug: inhibits folic acid synthesis
-most rapid-acting DMARD (80% improve)
-adverse: hepatic fibrosis, bone marrow suppression, GI ulcers, fetal death or abnormalities
-anticancer drug
Term
Etanercept (Enbrel)
Definition
Antiarthritic and spine and skin disorders: $$$, new DMARD, TNF blocker
adverse: inc. risk of infection, injection site rxn., heart failure
Term
Disease-Modifying Antirheumatic Drugs
Definition
*Methotrexate: folic acid inhibition
*Entanercept (Enbrel): TNF blocker
*Infliximab (Remicade): TNF antibody
*Adalimumab (Humira): monoclon. to TNF
*Anakinra (Kineret): IL-1 receptor antag.
Term
GOUT
Definition
-recurrent inflammatory disorder
-hyperuricemia
-severe joint pain, large toe
-Tophi=gritty deposits in joints
Causes: excessive prod. of uric acid, impaired renal excretion of uric acid
Term
Drug therapy for Gout
Definition
-NSAIDs (Indomethacin, Indocin)
-Glucocorticoids (prednisone)
-Colchicine
Term
Indomethacin (Indocin)
Definition
NSAID for gout, 1st choice, minimal GI effects, headache
Term
**Colchicine
Definition
GOUT-specific drug: Anti-inflammatory
-leukocyte migration and infiltration inhibited by microtubule disruption
-GI side effects
-preferred oral not IV
Term
Drugs for Hypereuricemia
Definition
-Allopurinol (Zyloprim)
-Fevuxostat (Uloric)
-Probenecid
**Sufinpyrazone (Anturane): inc. renal secretion of uric acid, oral, used in chronic gout
Term
Allopurinol (Zyloprim)
Definition
-GOUT: reduces blood levels of uric acid
-uses: chronic tophaceous gout, hyperuricemia due to chemo
-adverse: well tolerated, rash, fever, GI, drowsiness
Term
Febuxostat (Uloric)
Definition
GOUT: NEW
-first new in 40 yrs.
-MOA: inhibit XO, same as allopurinol
-adverse effects uncommon
-GOOD DRUG
Term
Basic Priciples of Antimicrobial Therapy
Definition
-Chemo=use of chem to destroy invading org
-Antibiotic=one microbe destroys another
-Antimicrobial=natural or synthetic
-selective tox=no injury to host (cell wall)
-Narrow vs. broad spectrum
Term
Drugable targets of antibiotics
Definition
-cell wall synthesis
-cell membrane permeability
-protein synthesis (prefer non-lethal so memory cells form)
-nucleic acid synthesis
-antimetabolites (sulfa drugs)
-viral enzyme inhibitors (reverse transcriptase inhibitors)
Term
Mechanisms of microbial drug resistance
Definition
***Staphylococcus aureus
-spontaneous mutation
-conjugation (gram- bacteria, resistance factor, multiple drug resistance)
Term
Delaying Emergence of Drug Resistance
Definition
-vaccinate
-get the catheters out
-target the pathogen
-access the experts
-practice antimicrobial control
-use local data
-use Vanco as last resort
Term
Selection of Antibiotic
Definition
-match bug to drug
-ID organism
-drug sensitivity of org: gram + or -
-host factors: age
-allergy: penicillin
-patient variables: pathology
-penetration to site of infection (BBB)
Term
Misuses of Antimicrobial Drugs
Definition
-untreatable infection; common cold
-fever of unknown origin
-improper dosage: TB, dosage + length of time
-unidentified organism
-omission of surgical drainage: catheters
Term
Penicillins
Definition
Antibiotics that weaken the cell wall, causing bacteria to take up H2O and burst
-bactericidal
-bacterial resistance: drug can't reach target, or inactivation by bacterial penicillinase (enz. that breaks down penicillin)
Term
Penicillins (MOA)
Definition
Inhibition of transpeptidase, which makes strong cell walls in bacteria
Term
Gram + vs. Gram - bacteria: the bacterial cell envelope
Definition
*Gram + = thick peptidoglycan in cell wall
*Gram - = thin peptidoglycan in cell wall + outer membrane
(both have inner cytoplasmic membrane)
Term
Beta-lactamase
Definition
Penicillins are comprised of a Beta-lactam ring. Many bacteria make beta-lactamase that inactivates the drug by breaking a N-C bond
Term
Classifications of Penicillins
(-cillin=beta-lactam ring)
Definition
*narrow spectrum: penicillinase sensitive
*narrow spectrum: penicillinase resistant
*broad spectrum
*extended spectrum
Term
Penicillin G (Benzylpenicillin)
Definition
4 forms of penicillin salts:
-Sodium penicillin
-Potassium penicillin
-Procaine penicillin
-Benzathine penicillin
Term
Penicillin allergy
Definition
Types:
-Immediate (2-30 minutes)
-Accelerated (1-72 hours)
-Late (days to weeks)
Anaphylaxis: laryngeal edema, bronchoconstriction, severe hypotension
Tx: epinephrine, resp support
Prevention: skin test, have resp support ready
Term
Penicillinase-resistant penicillins, anti-staph
Definition
*Nafcillin
*Oxacillin
***Dicloxacillin-oral
Term
Amoxicillin (Amoxil, oral)
Definition
Broad spectrum penicillin (aminopenicillin)
also in this class: Ampicillin (Principen)
adverse: rash, diarrhea
Term
Ticarcillin (Ticar, IV)
Carbenicillin indanyl (Geocillin, oral)
Definition
Extended spectrum penicillins (antipseudomonal penicillins)
also in this class: Piperacillin
Term
Augmentin
Definition
Penicillin/Beta-Lactamase Inhibitor Combinations, only available in fixed-dose combos:
-Augmentin=Amoxicillin/Clavulanic acid
Term
Cephalosporins
Definition
*most widely used group of antibiotics
-"ceph"=beta-lactam
-similar to penicillin structure
-bactericidal
-given parenterally
adverse: less than cillins, bleeding, thrombophlebitis
Term
Classification of cephalosporins
Definition
Get better @ act. against gram-, resistance to B-lactase, into cerebrospinal fluid:
1st: Cephalexiin (Keflex): oral
2nd: Cefaclor (Ceclor): oral
3rd: Cefpodoxime (Vantin): oral
4th: Cefepime (Maxipime): IM/IV
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