Pharmacology Exam 3

Front 1

H1 histamine receptor

Back 1

vasodilation, bronchoconstriction, increased capillary leakage

Front 2

H1 antihistamines

Back 2

end in "ine"

Front 3

epinephrine

Back 3

life-saving drug in systemic anaphylaxis;

Front 4

first generation vs. second generation H1 antagonists

Back 4

first gen have strong sedative effects; second not as strong

Front 5

Ethanolamines

Back 5

Carbinoxamine, Dimenhydrinate, Diphenhydramine, Doxylamine

Front 6

Ethylaminediamines

Back 6

pyrilamine, tripelennamine

Front 7

Piperazine derivs

Back 7

hydroxyzine, cyclizine, meclizine

Front 8

Alkylamines

Back 8

brompheniramine, chlorpheniramine

Front 9

promethazine

Back 9

a phenothiazine H1 antagonist; also an anti-emetic

Front 10

cyproheptadine

Back 10

H1 antag that also induces appetite; antagonist of histamine and serotonin

Front 11

terfenadine

Back 11

a second generation drug that was with drawn b/c it caused lethal arrhythmias

Front 12

fexofenadine (Allegra)

Back 12

carboxylated version of terfenadine; a piperidine second gen H1 blocker

Front 13

other second generation H1 antagonists

Back 13

loratadine (Claritin), cetrizine (Zyrtec), desloratadine (Clarinex);
all OTC; can still cause sedation but not as much as first gen.
certirizine is the most sedating

Front 14

kinetics of second generation H1 antagonists

Back 14

oral admin; peak 1-2 hours; metabolized by liver; can have duration of about 12-24 hrs

Front 15

mechanism of second gen

Back 15

carboxyl group makes them less lipid soluble (more polar); does not cross BBB --- no CNS penetration

Front 16

mechanism of H1 blockers

Back 16

resemble muscarininc and alpha adrenergic receptor blockers; some also block serotonin receptors; do not really affect H2 receptors

Front 17

CNS effects of H1 blockers

Back 17

sedation, anti motion sickness;

Front 18

Diphenhydramine

Back 18

used for atopic dermatitis; sedative, antipruritic;

Front 19

treatment of allergic rhinitis and chronic urticaria

Back 19

second generation drugs

Front 20

clinical uses of H1 blockers

Back 20

immediate allergies (hay fever, rhinitis, urticaria);
anti-tussive agents
prophylaxis of motion sickness and vestibular disturbance
nausea and vomiting during pregnancy

Front 21

motion-sickness treatment

Back 21

scopolamine, diphenhydramine, promethazine;
piperazines - cyclizine and meclizine, but these have marked sedation

Front 22

trt of nausea and vomiting during pregnancy

Back 22

Piperazine derivs used to be used, but withdrawn b/c of teratogenic effects

Front 23

adverse effects of H1 blockers

Back 23

sedation and antimuscarinic effects (dry mouth, blurred vision); orthostatic hypotension;
some adverse interactions with first gen drugs and other sedatives (benzodiazepines, alcohol)

Front 24

adverse effects of H1 blockers cont'd.

Back 24

concomittant admin with macrolide, ketoconazole, itraconazole prolongs QT interval; lethal arrhythmias; not seen in Loratadine and acrivastine

Front 25

reditabs

Back 25

antoher formulation of loratadine

Front 26

Ethanolamines

Back 26

significant antimuscarinic activity; marked sedation;

Front 27

Diphenhydramine

Back 27

treats cough, anti-emetic, treats vomiting, vertigo; can treat drug-induced extrapyramidal symptoms; mild cases of Parkinson's;

Front 28

diphenhydramine vs. other antihistamines

Back 28

greater anticholinergic effects; antidyskinetic action;

Front 29

other uses of diphenhydramine

Back 29

relief from insect bites, minor burns, sunburn, minor abrasions; anesthetic effect; tolerance with prolonged use

Front 30

administration of diphenhydramine

Back 30

oral, topical, IV, IM

Front 31

Promethazine

Back 31

a phenothiazine; anticholinergic, sedative, antemetic, local anesthetic; used in cough and cold products

Front 32

Azelastine

Back 32

nasal spray; treats allergic rhinitis, sneezing, nasal pruritus; for patients who don't respond to fexofenadine

Front 33

mechanism of azelastine

Back 33

inhibits H1 receptor and inhibits release of histamine from mast cells;
inhibits leukotrienes

Front 34

loratadine

Back 34

most widely-used second gen.; not associated with prolonged QT or torsades de pointes

Front 35

mechanism of loratadine

Back 35

binds preferentially at H1 receptors in periphery than in brain; taken once daily

Front 36

effects of loratadine

Back 36

anticholinergic, adrenergic blocker, antispasmodic, local anesthetic

Front 37

Desloratadine

Back 37

active metabolite of loratadine; relieves symptons of allergic rhinitis, perennial rhinitis;, and chronic idiopathic urticaria

Front 38

fexofenadine

Back 38

active metabolite of terfenadine; similar to loratadine

Front 39

Cetirizine

Back 39

active metabolite of hydroxyzine, but has higher affinity for H1 receptor; only antihistamine approved for infants as young as 6 months;
higher incidence of somnolence than fexofenadine and loratadine

Front 40

mechanism

Back 40

blocks receptor as well as prevents release of mast cell mediators; oral admin

Front 41

Cyproheptadine

Back 41

also serotonin antag; increases appetite; useful for Cushing's syndrome, vascular headache, anorexia, anorgasmy caused by SSRI's

Front 42

Anti-asthmatic agents

Back 42

beta agonists, corticosteroids, mediator release inhibitors, muscarinic antagonists, methyl xanthine, anti-leukotriene agents, omalizumab, cetirizine, roflumilast, soluble IL-4 receptor

Front 43

asthma

Back 43

syndrome characterized by increased responsiveness of tracheobronchial tree to variety of stimuli

Front 44

mechanisms

Back 44

relaxation of broncial tone with beta agonists, theophylline, muscarinic antagonists, andn leukotriene antagonists;
constriction of bronchial tone via acetyl choline, leukotrienes, and adenosine

Front 45

beta-2 agonists

Back 45

sympathomimetics that cause relaxation and dilation of bronchial smooth muscle by activiting adenylyl cyclase

Front 46

beta-2 agonist vs. epinephrine

Back 46

both are sympathomimetics, but beta-2 agonist is preferred b/c it has local effects only, rather than all effects of EPI

Front 47

short-acting sympathomimetics

Back 47

albuterol, metaproterenol, terbutaline;
used for acute episodes of bronchospasm

Front 48

long-acting sympathomimetics

Back 48

salmeterol, formoterol;
used in prophylaxis

Front 49

terbutaline administration

Back 49

inhalant, oral, parenteral

Front 50

albuterol administration

Back 50

inhalant, oral, oral sustained release

Front 51

salmeterol and formeterol administration

Back 51

inhalants

Front 52

toxicity of beta agonists

Back 52

skeletal muscle tremor; some cardiac effects (positive ionotropic effect); tachycardia arrhythmia with excessive use

Front 53

toxicity of short-acting mimetics

Back 53

tolerance; responsiveness to drug can be restored by corticosteroids

Front 54

isoetharine

Back 54

similar to isoproterenol;
short-acting beta 2 agonist
metabolized by COMT (catechol-O-methyl transferase)

Front 55

metaproterenol and terbutaline

Back 55

not metabolized by COMT, so they are long-acting; can be administered orally

Front 56

albuterol

Back 56

similar to metaproterenol; not metabolized by COMT; most appopriate choice for acute asthma attacks

Front 57

salmeterol

Back 57

highly selective beta-2-agonist; long-term use; prevention of bronchospasm in adults with reversible COPD; should not be used for acute attacks

Front 58

salmeterol:fluticasone (Advair) combination

Back 58

combo of corticosteroid and beta agonist; inhalant; not suitable for acute attacks

Front 59

pirbuterol

Back 59

inhalant only

Front 60

bitolterol

Back 60

pro-drug; used for acute, chronic, and exercise-induced asthma; duration of action about 5-8 hrs

Front 61

Catecholamines (also sympathomimetics)

Back 61

epinephrine, isoproterenol

Front 62

mechanism of catecholamines

Back 62

EPI activates alpha and beta receptors;
alpha - relieves mucosal edema and congestion of upper airway;

Front 63

EPI

Back 63

used for acute bronchospasm, resiratory manifestations of anaphylaxis, severe asthma exacerbation, and status asthmaticus

Front 64

isoproterenol

Back 64

non-selective beta agonist; adverse cardiac effects

Front 65

aerosol corticosteroids

Back 65

hydrocortisone, mometasone, flunisolide, triamcinolone, beclomethasone, fluticasone, budesonide, betamethasone, prednisolone

Front 66

mechanism of corticosteroids

Back 66

inhibit leukotrienes, prostaglandins, and thromboxanes, reduc bronchiole contraction, vascular permeability, and mucus secretion in airways

Front 67

prednisone vs. prednisolone

Back 67

prednisone is converted to predinsolone in the liver

Front 68

effects of corticosteroids on immune system

Back 68

reduce inflammatory and immune components of asthma, inhibit activity of mast cells, eosinophils, neutrophils, macrophages, lymphocytes

Front 69

adverse effects of corticosteroids

Back 69

inhalation of corticosteroids can cause changes in the oropharyngeal microflora, leading to infections such as oral candidiasis

Front 70

anticholinergic drugs

Back 70

similar effects as beta-adrenergic agonists; cholinergic and adrenergic are opposites

Front 71

ipratropium (Atrovent)

Back 71

oral-inhalational and nasal spray; only approved anticholinergic for bronchodilation; similar to atropine

Front 72

mechanism of ipratropium

Back 72

synthetic quaternary antimuscarinic agent; competitve antagonist of muscarinic cholinergic receptors;
decreases formation of cGMP, decreasing contractility of smooth muscle

Front 73

adverse effects of ipratropium

Back 73

xerostomia; but not known to cause tremor or arrhythmias like the beta agonists do

Front 74

bronchoconstriction reflex

Back 74

mediated by vagus nerve;
stimuli: allergens, cold, emotions;
impulse travels via vagus to initiate efferent action of vagal fibers to release ACh, causing constriction, mucus production, and degranulation of mast cells; also coughing

Front 75

benefits of ipratropium over beta agonists

Back 75

beta agonists are more portent for reversing acute bronchospasm, but ipratropium is more potent and less toxic for patients with COPD, especially those with psychogenic exacerbations

Front 76

tiotropium (Handihaler)

Back 76

used for COPD, not asthma;
similar to ipratropium but administered only once daily (ipratropium must be taken up to 4 times per day)

Front 77

mechanism of tiotropium

Back 77

acetylcholine antagonist (blocks M1, M2, and M3 receptors);
bronchodilation, bronchoprotection

Front 78

administration of tiotropium

Back 78

dry powder via oral inhalation;

Front 79

methyl xanthines

Back 79

aminophylline, theophylline, dyphylline, oxtriphylline, pentoxifylline;
NOT THEOBROMINE OR CAFFEINE

Front 80

effects of methyl xanthines

Back 80

relaxation of bronchial smooth muscle and pulmonary blood vessels; anti-inflammatory and immunomodulatory

Front 81

mechanism of methyl xanthines

Back 81

inhibition of type III and type IV phosphodiesterase, increasing cAMP, and causing relaxation; at clinical doses, however, inhibition is not great

Front 82

adensoine receptor mechanism of methyl xanthines

Back 82

binding to adenosine receptors, inactivating them;
A1 receptor stimulation causes inhibition of cAMP, while A2 stimulation causes increased cAMP; theophylline inhibitis both -- non-bronchodilatory effect of methylxanthines;
questionable mechanism

Front 83

physiological effects of methyl xanthines

Back 83

increased respiratory strength, endurance, and cetnral ventilatory drive; bronchodilation

Front 84

adverse CNS effects of methyl xanthines

Back 84

headache, anxiety, restlessness, insomnia, tremor, convulsions

Front 85

adverse GI effects of methyl xanthines

Back 85

nausea, diarrhea, vomiting, gastroesoph. reflux, anorexia, abdominal pain

Front 86

adverse cardiovascular effects of methyl xanthines

Back 86

large overdoses cause arrhtymias, palpitations, supraventricular tachycardia, ventricular arrhythmia, and hypotention

Front 87

adverse renal effects of methyl xanthines

Back 87

diuresis

Front 88

drug interactions that increase theophylline levels

Back 88

beta blockers, mexiletine, Ca channel blockers, quinolones, cimetidine, ranitidine, erythromycin, corticosteroids, ephedrine, flu virus vaccine and in liver failure, renal failure, CHF, and pneumonia

Front 89

drug interactions that decrease theophylline levels

Back 89

barbiturates, beta agonists, rifampin, phenytoin, cigarette smoking

Front 90

theophylline:aminophylline combo

Back 90

used for the trt of acute exacerbations of reversible airway obstruction including status asthmaticus for patietns who do not respond to first-line therapies and have not receive theophylline in the previous 24 hrs

Front 91

inhibitors of mast cell degranulation (mast cell stabilizers)

Back 91

cromolyn sodium, nedocromil; OTC

Front 92

cromolyn sodium

Back 92

synthetic compound; no bronchodilator activity, but inhibits antigen-induced bronchospasm; also used orally for inflammatory bowel disease, systemic mastocytosis, ulcerative colitis

Front 93

solutions of cromolyn sodium

Back 93

ophthalmic for allergic conjunctivitis; nasal for allergic rhinitis

Front 94

mechanism of cromolyn sodium

Back 94

inhibition of mast cell degranulation by inhibting the calcium influx caused by the IgE Ab-Ag complex; prevent release of histamine and slow-reacting substance of anaphylaxis; ineffective for trt of acute attack - extremely prophylactic

Front 95

nedocromil

Back 95

more potent than cromolyn sodium

Front 96

clinical use of cromolyn

Back 96

asthma in children; prophylactic against mild to moderate asthma as well as antigen and exercise-induced bronchoconstriction; reduce need for bronchodilators and severity of symptoms

Front 97

leukotriene antagonists, lipoxygenase inhibitors

Back 97

zileuton, zafirlukast, montelukast

Front 98

Zileuton

Back 98

oral; inhibits first enzyme in LOX pathway, preventing formation of leukotrienes and subsequent inflammatory response; reduces nasal congestion in allergic rhinitis; good for patients exposed to cold, dry air

Front 99

adverse symptoms of zileuton

Back 99

flu-like symptoms, headache; increases liver enzymes, therefore contraindicated in patients with liver disease and elevated transaminase

Front 100

zafirlukast

Back 100

leukotriene receptor antagonist; effective in controlling persistent asthma symptoms in adults and children over 5; can be used in combo iwth corticosteroids or beta agonists

Front 101

limitations of zafirlukast

Back 101

not used for management of acute exacerbations of bronchospasm

Front 102

mechanism of zafirlukast

Back 102

inhibits binding of leukotrienes D4 and E4; oral administration, can also be inhaled

Front 103

metabolism of zafirlukast

Back 103

done by cytochrome P450 CYP2C9; may inhibit activity of cytochrome isoenzymes CYP3A4 and CYP2C9

Front 104

montelukast (Singulair)

Back 104

available in chewable form for children; oral; does not inhibit the CYP3A4 and CYP2C9; approved for children as young as 12 months

Front 105

mechanism of montelukast

Back 105

selective antagonist of LTD4 at the receptor CysLT1; metabolized by liver, but does not inhibit cytochrome P450 isoenzymes

Front 106

Omalizumab (Xolair)

Back 106

very expensive!
monoclonal antibody (ends in "ab") against IgE, first biologic therapy for the use of trt of asthma

Front 107

mechanism of omalizumab

Back 107

prevents binding of IgE to the Fc receptor

Front 108

administration of omalizumab

Back 108

approved for patients 12 and over; subcutaneous injection;

Front 109

action of omalizumab in early phase of allergic response

Back 109

prevents binding of IgE to mast cells, inhibiting degranulation of mast cells

Front 110

action of omalizumab in late phase of allergic response

Back 110

binds to IgE and prevents it from bidning its Fc receptor on monocytes, eosinophils, dendritic cells, and platelets

Front 111

soluble IL-4 receptor

Back 111

investigational; this receptor is a cytokine antagonist that inhibits IL-4, which normally stimulates production of IgE

Front 112

Roflumilast

Back 112

investigational; trt of COPD and asthma by inhibiting PDE4 to maintain higher levels of cAMP, allowing bronchodilation

Front 113

Antimicrobials

Back 113

penicillins, cephalosporins, other cell wall synthesis inhibitors, cell wall disrupting agents

Front 114

beta lactams

Back 114

penicillins, cephalosporins, carbapenems, monobactams

Front 115

other cell wall synthesis inhibitors

Back 115

vancomycin, bacitracin, cycloserine, polymyxins, fosfomycin

Front 116

beta-lactamase inhibitors

Back 116

clavulanic acid, sulbactam, tazobactam

Front 117

cephalosporins

Back 117

beta lactams that have a 6-membered ring rather than the 4-membered ring of other beta lactams

Front 118

Penicillins

Back 118

three classes: natural (penicillin G), antistaphylococcal, and extended spectrum

Front 119

mechanism of penicillins

Back 119

inhibit cross-linking step in synthesis of bacterial cell wall; bactericidal; do not act on mycobacteria, fungi protozoa, or viruses b/c these orgnaisms lack a peptidoglycan cell wall

Front 120

mechanism of penicillins cont'd.

Back 120

bind to penicillin-binding proteins, which are enzymes involved in cell wall synth; this blocks cross-linking;

Front 121

action of penicillin on gram-positive vs. gram-negative bacteria

Back 121

penicillins get thru the cell wall easily in gram-pos bacteria, but porins are necessary for entry into the gram-negative bacteria

Front 122

penicillin G (benzylpenicillin)

Back 122

natural penicillin; used for trt of gram pos cocci, bacilli, gram neg cocci, and spirochetes as well as oral anaerobes;
susceptible to beta lactamase, unstable at acidic pH (of gastric env)

Front 123

uses of penicillin G

Back 123

trt of gas gangrene due to clostridium; dphtheria, anthrax, actinomycosis, listeria; also highly active against Treponema pallidum

Front 124

use of penicillin G to treat enterococci

Back 124

requires aminoglycoside;

Front 125

procain penicillin G, and benzathine penicillin G

Back 125

repository form of penicillin that has duration of action 12-24 hrs; used for beta hemolytic streptococcal infection

Front 126

Penicillin V

Back 126

more stable in acidic environment than penicillin G; oral; poor bioavailability so only useful for minor infections; narrow spectrum; high minimal lethal concentration, not good choice for bacteremia

Front 127

characteristics of both penicillin G and V

Back 127

should be administered at least 1 hr before meals or 2-3 hrs after; probenecid prolongs duration of penicillin in body; 99% of drug eliminited by the kidney

Front 128

prophylactic uses of penicillins

Back 128

streptococcal infections, recurrence of rheumatic fever, gonorrheal ophthalmia in neonates, surgical procedures in patients with valvular disease, dental extractions, tonsillectomy, intestinal and genitourinary operations

Front 129

antistaphylococcal penicillins (gram-positive cocci)

Back 129

also anti-strep; these drugs are resistant to strep and staph beta lactamases; inactive against enterococci, anaerobic bacteria, gram-neg cocci and rods;

Front 130

examples of antistaph and strep penicillins

Back 130

methicillin, nafcillin, oxacillin, cloxacillin, dicloxacillin

Front 131

methicillin

Back 131

nephrotoxic; rarely used; poor oral absorption

Front 132

oxacillin

Back 132

oral; 8 times as potent as methicillin; given IV for serious systemic staphylococcal infections

Front 133

nafcillin

Back 133

any route of administration; can casue neutropenia; given IV for serious systemic staphylococcal infection

Front 134

dicloxacillin

Back 134

highly resistant to penicillinase (beta lactamase); very effective via oral admin

Front 135

extended spectrum penicillins

Back 135

effective against gram-negative bacteria; ampicillin and amoxicillin; carbenicillin, ticarcillin, piperacillin, azlocillin, mezlocillin (these are antipseudomonal penicillins)

Front 136

ampicillin

Back 136

drug of choice for aerobic and facultative anaerobic gram positive bacilli Listeria;

Front 137

amoxicillin

Back 137

given orally only; used prophylactically for patients with abnormal heart valves undergoing oral surgery; acid stable; not resistant to penicillinase; used along with beta lactamase inhibitors to prevent hydrolysis of amox.;

Front 138

ampicillin and amoxicillin combos with beta lactamase inhibitors

Back 138

Augmentin - amox-clavulanic acid;
Unasyn - ampicillin-sublactam, used for trt of intra-abdominal and gynecological infections;
Zosyn - piperacillin-tazobactam

Front 139

carbenicillin and ticarcillin

Back 139

similar to ampicillin; effective against indole-positive Proteus and Pseudomonas

Front 140

ureido-penicillins

Back 140

azlocillin, mezlocillin, piperacillin; effective against Klebsiella pneumoniae, a facultative gram-neg rod

Front 141

piperacillin

Back 141

most potent ureido-penicillin; can cause platelet dysfunction

Front 142

kinetics of all penicillins

Back 142

cross placental barrier, but no teratogenic effects; penetration of CSF occurs only with inflammation

Front 143

adverse effects of penicillins

Back 143

hypersensitivity, skin rashes, Steven-Johnson syndrome; highest incidence with ampicillin; diarrhea, interstitial nephritis, neurotoxicity, seizures, platelet dysfunction; fever; anaphylaxis

Front 144

cephalosporins

Back 144

have 6-membered sulfur containing ring adjoining the beta lactam ring, making them highly resistant to pellicinase

Front 145

cephalosporinase

Back 145

a beta lactamase expressed by some bacteria; most cephalosporins are resistant to it

Front 146

organisms not susceptible to cephalosporins

Back 146

methicillin-resistant Staph aureus, Listeria monocytogenes, Clostridium difficile, Enterococci

Front 147

kinetics of cephalosporins

Back 147

administered parenterally and orally; most do not penetrate CNS; most excreted in urine; excretion blocked by probenecid; all are active against gram-pos cocci and many gram-pos bacilli

Front 148

applications of cephalosporins

Back 148

S. aureus infections of the skin, osteomyelitis, endocarditis; drug of choice in Klebsiella pneumoniae and Pneumonococcal pneumoniae caused by S. pyogenes

Front 149

parenteral cephalosporins

Back 149

used for Gonococcal disease, respiratory and urinary gram-neg bacterial infections

Front 150

prophylactic use of cephalosporins

Back 150

used in perioperative infections

Front 151

first generation cephalosporins

Back 151

cefazolin, cefadroxil, cephalexin, cephradine, cephalothin, cephapirin;
substitutes for penicillin G

Front 152

PEcK drugs

Back 152

first gen cephalosporins - active against Proteus, E.coli, and Klebsiella

Front 153

specifics about PEcK drugs

Back 153

not active against enterococci or pseudomonas aeruginosa; excretion via kidneys;

Front 154

cefazolin

Back 154

drug of choice in surgical prophylaxis; only first gen cephalosporin used parenterally; alternative to anti-Staph. penicillins and in patients allergic to penicillin

Front 155

Second generation cephalosporins

Back 155

Cefaclor, cefamandole, cefmetazole, cefprozil, cefoxitin, cefonicid, cefotetan, cefuroxime, loracarbef;
active against more gram-neg organisms than first gen

Front 156

HENPEck drugs

Back 156

second gen cephalosporins; active against: Haemophilus influenzae, Enterobacter aerogenes, Neisseria, and PEcK

Front 157

specifics about second gen cephalosporins

Back 157

not recommended against enterobacter; not active against enterococci or pseudomonas aeruginosa

Front 158

Cefaclor

Back 158

second gen cephalosporin that is highly susceptible to beta-lactamase; use has diminished

Front 159

third generation cephalosporins

Back 159

broad-spectrum drugs; expanded gram-neg coverage; some can cross BBB (therefore can treat meningitis);
includes: cefdinir, cefixime, cefoperazone, cefotaxime, ceftazidime, ceftizoxime, ceftriaxone, ceftibuten, cefditoren, cefpodoxime

Front 160

first-line drugs for N. gonorrhoeae

Back 160

ceftriaxone and cefixime (3rd gen)

Front 161

cephalosporins active against P. aeruginosa

Back 161

ceftazidime and cefoperazone (3rd gen)

Front 162

cephalosporins against Bacteroides fragilis (gram neg anaerobic rod)

Back 162

ceftizoxime, moxalactam (3rd gen)

Front 163

cephalosporins excreted through biliary tract (not kidney)

Back 163

cefoperazone and ceftriaxone (3rd gen)

Front 164

trt of meningitis

Back 164

3rd gen cephalosporins; meningitis caused by highly penicillin-resistant strains of pneumococci may not respond; rifampin or vancomycin may be necessary

Front 165

third gen vs. first gen cephalosporins

Back 165

for gram-pos cocci, first gen is better; for gram-neg bacilli, 3rd gen is better

Front 166

fourth generation cephalosporins

Back 166

cefepime and cefpirome (cefpirome not in US)

Front 167

cefepime

Back 167

more resistance to hydrolysis by the chromosomal beta-lactamase of Enterobacter than are 3rd gen drugs; active against P. aeruginosa, Enterobacteriaceae, S. aureus, S. pneumoniae, Hemophilus, Neisseria

Front 168

oral cephalosporins

Back 168

first gen - cefadroxil, cephalexin, cephradine;
second gen - cefaclor, cefprozil, cefuroxime;
third gen - cefdinir, cefixime, cefpodoxime, ceftibuten

Front 169

adverse effects of cephalosporins

Back 169

disulfiram-like symptoms with those that contain MTTZ (not 3rd gen), superinfection, renal damage, local tissue reactions, bleeding due to vit K effects

Front 170

carbapenems

Back 170

synthetic beta lactams; imipenem, meropenem

Front 171

imipenem

Back 171

metabolized to potentially nephrotoxic compounds in renal tubules by dehydropeptidase; cilastatin inhibits this enzyme and is therefore compounded with imipenem

Front 172

imipenem/cilastatin

Back 172

broaest spectrum of all beta lactams; cannot be used against methicillin-resistant bacteria

Front 173

meropenem

Back 173

slightly greater activity than imipenem agaisnt gram-neg aerobes, less activity against gram-pos.

Front 174

adverse effects of carbapenems

Back 174

leads to seizures when there are excessive levels in patients with renal impairment

Front 175

monobactams

Back 175

aztreonam - free beta lactam ring; specific for enterobacteria; active against gram-neg rods (Pseudomonas, Serratia marcescens); not active against gram-pos coci and anaerobic bacteria

Front 176

administration of monobactams

Back 176

IV or IM (100% bioavailability with IM)

Front 177

aztreonam

Back 177

monobactam; low allergic reactions - penicillin alternative for gram-neg infections; can be substituted for aminoglycosides (beta lactamase inhibitors) to trt UTI and RTI;
also treats osteomyelitis, gonorrhea, gynecologic and intra-abdominal infections

Front 178

vancomycin

Back 178

oral and parenteral; used as reserve, or rescue, drug;
useful against methicillin-resistant staph infections; used to trt sepsis, endocarditis

Front 179

oral admin of vancomycin

Back 179

to treat pseudomembranous colitis caused by Clostridium difficile

Front 180

restrictions for vancomycin

Back 180

used to treat only serious infections by beta-lactam resistant gram-pos. bacteria

Front 181

action of vancomycin

Back 181

inhibits cell wall phospholipid synth and peptidoglycan polymerization

Front 182

vancomycin + aminoglycosides

Back 182

for enterococcal infections

Front 183

adverse effects of vancomycin

Back 183

ototoxicity, nephrotoxicity -- risk of these increased when used with aminoglycosides;
"red man" or "red neck" syndrome -- due to release of histamine

Front 184

fosfomycin

Back 184

inhibits early stage of cell wall synthesis; analogue of PEP; single-dose, oral; trts UTI in women who are pregnant

Front 185

bacitracin

Back 185

nephrotoxic if administered systemically; proteinuria, hematuria, nitrogen retention; used only topically! - local effects only; usually combined with polymyxin and neomycin

Front 186

polymyxin B and polymyxin E

Back 186

active against gram-neg bacteria - restricted to trting these infections; only polymyxin B in US

Front 187

action of polymyxins

Back 187

detergent action; they are amphipathic and interact with phospholipids to disrupt cell membrane

Front 188

resistance to polymyxins

Back 188

proteus and neisseria

Front 189

toxicity of polymyxins

Back 189

nephrotoxicity and neurotoxicity, therefore not used for systemic admin

Front 190

use of polymyxins

Back 190

treatment of corneal ulcers, external otitis

Front 191

cycloserine

Back 191

only cell wall synthesis inhibitor that can treat tuberculosis; adverse effects: CNS toxicity, headache, tremors, psychosis, convulsions

Front 192

Protein synthesis inhibitors

Back 192

tetracyclines, macrolides and ketolides, aminoglycosides, spectinomycin, chloramphenicol, clindamycin

Front 193

tetracyclines

Back 193

end in "cycline"; 4 fused 6-membered rings; isolated from Streptomyces; synthetic derivs: methacycline, doxycycline, minocycline

Front 194

activity of tetracyclines

Back 194

wide range; little activity against fungi; bacteriostatic; useful against chancroid (H. ducreyi), Legionella pneumophilia, H. pylori, Y. pestis and Francisell tularensis; effective against Rickettsiae and anearobic organisms

Front 195

tetracycline againest spirochetes

Back 195

Borrelia (Lyme disease), T. pallidum (syphilis), Chlamydia, mycoplasma

Front 196

effect of tetracycline on intestinal flora

Back 196

occasionally produces colitis by toxin from C. difficile

Front 197

mechanism of tetracycline

Back 197

bind 30S ribosome so that protein synth does not occur in bacteria

Front 198

kinetics of tetracycline

Back 198

minocycline - absorbed well, enters brain in absence of inflammation therefore useful for eradication of meningococcal carrier-state; absorption of tetracyclines is inhibited by divalent and trivalent ions (Mg2+, Ca2+, Al3+) -- cannot be taken with milk

Front 199

short-acting tetracyclines

Back 199

chlortetracycline, oxytetracycline, tetracycline

Front 200

intermediate-acting

Back 200

demeclocycline, metachycline

Front 201

long-acting

Back 201

doxycycline, minocycline

Front 202

resistance to tetracyclines

Back 202

Vibrio cholera, gonococci

Front 203

clinical uses of tetracyclines

Back 203

drugs of choice for Mycoplasma pneumoniae, Chlamydiae, Rickettsiae, Spirochetes, H. pylori, protozoal infection, brucella infections

Front 204

demeclocycline

Back 204

inhibits action of ADH in renal tubule; useful for trt of inappropriate secretion of ADH

Front 205

adverse effects of tetracycline

Back 205

brown coloration of fetal teeth if mother takes it; photosensitization with demeclocycline and doxycycline

Front 206

Macrolides and Ketolides

Back 206

Erythromycin, Clarithromycin, Azithromycin, Dirithromycin

Front 207

mechanism of macrolides and ketolides

Back 207

bind 50S ribosome; aminoacyl translocation is blocked; cells are more permeable to the non-ionized form of the drug, so the drugs have increased activity at alkaline pH

Front 208

erythromycin

Back 208

bacteriostatic normally, but bacteriocidal at high conc; not useful for atypical infections; useful to patients who are resistant to penicillin and have Staph. aureus infection; not active against aerobic enteric gram-neg bacilli

Front 209

Clarithromycin

Back 209

more potent against strains of Staph and Strep that are resistant to erythromycin; active against M. catarrhalis (flora of upper resp tract), Chlamydia, Borrelia, M. pneumoniae

Front 210

Azithromycin

Back 210

less active than erythro against gram-pos (Strep and Enterococci); more active against H. influenzae and Campylobacter

Front 211

activity against Mycobacterium avium

Back 211

clarithromycin and azithromycin --- good for atypical infections

Front 212

resistance to macrolides

Back 212

gram-negative rods: esterases
gram-positive bacteria: methylase

Front 213

kinetics of macrolides

Back 213

sensitive to acid env; erythromycin is esterified to improve stability; azithromycin - extensive tissue distribution and high conc in cells; other

Front 214

clinical uses of azithromycin

Back 214

trt of Chlamydia during pregnancy; single does; atypical mycobacterial infections in AIDS patients (also clarithromycin)

Front 215

aminoglycosides

Back 215

amikacin, gentamycin, neomycin, netilmicin, streptomycin, tobramycin, kanamycin, paromomycin

Front 216

use of aminoglycosides

Back 216

trt infections caused by aerobic gram-neg bacteria; bactericidal; ototoxicity and nephrotoxicity are major limitations

Front 217

mechanism of aminoglycocides

Back 217

transported across bacterial membrane in energy-dependent phase I that can be blocked by anaerobic conditions; in an anaerobic atmosphere, these drugs are less effective;
bind to polysomes and act on 30S subunit to block the formation of translation initiation complex, cause misreading of the mRNA, and disrupt polysomes;

Front 218

Kanamycin

Back 218

should not be used against p. aeruginosa and Serratia

Front 219

Gentamycin, Kanamycin, Tobramycin, Netilmycin, Amikacin

Back 219

limited action against gram-positive; Strep. pneumoniae and Strep. pyogenes are highly resistant; genta and tobra active against most strains of staph aureus and staph epidermidis

Front 220

ototoxicity with aminoglycosides

Back 220

ototoxicity - can occur in children if used during pregnancy; increased by loop diuretics; most vestibular toxic are gentamycin and streptomycin;

Front 221

nephrotoxicity with aminoglycosides

Back 221

mostly by neomycin, tobramycin, and gentamycin; potentiated by amphotericin B, vancomycin, cephalothin, cisplatin and cyclosporine, loop diuretics

Front 222

neuromuscular effects of aminoglycosides

Back 222

respiratory paralysis - rare; mostly with neomycin

Front 223

Spectinomycin

Back 223

trt for gonorrhea in patients who are allergic to penicillin or gonococci are resistant to other medications; IM (painful)

Front 224

Chloramphenicol

Back 224

useful for meningococcal infection b/c it crosses BBB; binds 50S ribosome, inhibits transpeptidation (transfer of peptide to its amino acid acceptor)

Front 225

action of chloramphenicol

Back 225

broad spectrum; bacteriostatic; active against aerobic and anaerobic gram-pos and gram-neg.; alternative to beta lactams for meningitis

Front 226

clinical uses of chloramphenicol

Back 226

toxic, therefore not used systemically; back-up for severe salmonella infections, meningitis, rickettsia; commonly used topically

Front 227

toxicity of chloramphenicol

Back 227

inhibition of red cell maturation; Gray baby syndrome (lack of glucuronosyl transferase to eliminate drug); cyanosis, cardiovascular collapse with accumulation of drug

Front 228

drug interactions with chloramphenicol

Back 228

inhibits metabolism of phenytoin, coumarin, and tolbutamide

Front 229

Clindamycin

Back 229

a lincosamide; mechanism similar to macrolides, even though they are not chemically related

Front 230

clinical uses of clindamycin

Back 230

effective against gram-pos aerobe, as well as gram-pos and gram-neg anaerobes; used to trt infections caused by strains taht are resistant to less toxic antimicrobials; trt of sever infections of Bacteroides; prophylaxis of endocarditis in patients with valvular disease

Front 231

clinical uses of clindamycin, cont'd

Back 231

useful against P. carinii and T. gondii; prophylactic for endocarditis as a result of bacteremia due to dental procedures

Front 232

adverse effects of clindamycin

Back 232

GI irritation, rashes, hepatic dysfunction, superinfection b/c the drug eliminates intestinal microflora

Front 233

drugs that cause inhibition of DNA synthesis

Back 233

folate synthesis inhibitors, folate reduction inhibitors, quinolones

Front 234

folate synthesis inhibitors

Back 234

sulfonamides - "sulfa"

Front 235

folate reduction inhibitors

Back 235

pyrimethamine, trimethoprim, proguanil

Front 236

folate synthesis and redcution inhibitors

Back 236

Trimethoprim-Sulfamethoxazole (Co-trimoxazole); Pyrimethamine-Sulfadoxine

Front 237

Sulfonamides

Back 237

insoluble in water; wide range, treat gram-pos and gram-neg; many bacteria develop resistance;

Front 238

mechanism of sulfonamides

Back 238

antimetabolite; analogues of PABA and therefore prevent normal utilization of PABA by bacteria to synthesize folic acid

Front 239

synergists of sulfonamide

Back 239

trimethoprim (inhibitor of dihydrofolate reductase); combo of these 2 causes sequential block of folate synthesis and bactericidal action

Front 240

resistance to sulfonamides

Back 240

plasmid-mediated mutation, random mutation, increased capacity to inactivate drug, alternate pathways of folic acid synthesis, increased production of PABA, decreased uptake of drug due to reduction in permeabiity

Front 241

short-acting sulfonamides

Back 241

sulfisoxazole and sulfamethizole

Front 242

intermediate acting sulfonamides

Back 242

sulfamethoxazole, sulfadiazine

Front 243

sulfisoxazole

Back 243

rapidly absorbed and excreted; low renal toxicity, low incidence of crystalluria

Front 244

sulfonamides for UTI antiseptic and analgesic

Back 244

sulfisoxazole-phenazopyridine (orange-red urine);
sulfamethoxazole-phenazopyridine

Front 245

sulfonamides for trt of otitis media

Back 245

sulfisoxazole acetyl + erythromycin

Front 246

sulfamethoxazole

Back 246

longer half-life than sulfisoxazole; crystalluria more common b/c drug is insoluble; used with trimethoprim as co-trimoxazole

Front 247

sulfadiazine

Back 247

crosses CSF

Front 248

sulfasalazine

Back 248

poorly absorbed; used for ulcerative colitis (preferred over corticosteroids), regional enteritis, but relapse is common; also used for granulomatous colitis

Front 249

topical sulfonamides

Back 249

sulfacetamide, silver sulfadiazine, combo of sulfabenzamide, sulfacetamide, and sulfathiazole;
mafenide; sulfadoxine

Front 250

sulfacetamide

Back 250

used for opthlamic infections

Front 251

silver sulfadiazine

Back 251

prevention of infection in burns

Front 252

triple combo (sulfabenzamide, sulfacetamide, sulfathiazole)

Back 252

bacterial vaginosis caused by Hemophilus (Gardnerella) vaginalis

Front 253

Mafenide

Back 253

prevention of iinfection in burns; adverse: candida superinfection, intense pain, allergic rxn

Front 254

sulfadoxine

Back 254

long-acting; trt of plasmodium falciparum; used in combo with pyrimethamine

Front 255

Oral trimethoprim

Back 255

folate reduction inhibitor; used in acute uncomplicated UTI

Front 256

oral trimethoprim-sulfamethoxazole

Back 256

prevents folate synthesis and reduction; effective in P. carinii pneumonia, Shigellosis, Salmonella, UTI, ear infection, prostatitis, respiratory pathogens, Klebsiella; alternative to beta lactams for URI and community-acquired pneumonia; also used for methicillin-resistant Staph

Front 257

IV trimethoprim-sulfamethoxazole

Back 257

P. carinii in AIDS patients; gram-neg sepsis, shigellosis, typhoid fever, UTI

Front 258

oral pyrimethamine-sulfadoxine

Back 258

trt of Leishmaniasis (parasitic protozoa), toxoplasmosis (also protozoa); falciparum malaria (esp for Mefloquine-resistant strains); adverse: Steven-Johnson syndrome, so only used prophylactically in high-risk cases

Front 259

Proguanil

Back 259

folate reductase inhibitor; active metabolite: cycloguanil; used in combo with atovaquone to prevent and trt malaria

Front 260

adverse rxns of sulfonamides and folate inhibitors

Back 260

hemolytic anemia; Steven-Johnson

Front 261

Quinolones

Back 261

fluoroquinolones ("oxacin"); quinolones: Nalidixic acid and Cinoxacin

Front 262

UTI antiseptics

Back 262

methenamine, nitrofurantoin

Front 263

mechanism of quinolones

Back 263

acts on A subunit of DNA gyrase (topoisomerase II in euk), which prevents its strand-cutting function, inhibiting supercoiling; also inhibit topoisomerase IV; bactericidal

Front 264

kinetics of quinolones

Back 264

do not penetrate CNS, but good oral bioavailability to other tissues; renal elimination for ofloxacin, lomefloxacin, cinoxacin

Front 265

non-renally eliminated quinolones

Back 265

pefloxacin and nalidixic acid

Front 266

pefloxacin

Back 266

should not be used in patients with hepatic failure

Front 267

antimicrobial spectrum for quinolones

Back 267

E. coli, Salmonella, Shigella, Enterobacter, campylobacter, Neisseria --- see page C50

Front 268

fluoroquinoloens for UTI

Back 268

norfloxacin (approved in US for UTI ONLY); ciprofloxacin, ofloxacin, TMP-SMX (folate inhib)

Front 269

fluoroquin for prostatitis

Back 269

norfloxacin, cipro, ofloxacin; effective when TMP-SMX is not

Front 270

fluoroquin for STD's

Back 270

not active against T. pallidum; CI = pregnancy;
Chlamydia urethritis - ofloxacin;
Gonorrhea - ofloxacin, cipro (single dose);
Chancroid (due to H. ducreyi) - 3 days of cipro

Front 271

fluoroquinolones for GI and abdominal infections

Back 271

traveler's diarrhea, Shigellosis - norfloxacin, cipro, ofloxacin;
cholera - norfloxacin;
S. typhi enteric fever - cipro and ofloxacin

Front 272

fluoroquinolones for Respiratory tract infections

Back 272

poor activity against strep pneumoniase and anaerobic bacteria -- beta lactams better;
Sparfloxacin (new) can act against these;
good activity against H. influenzae, C. pneumoniae, legionella pneumophilia; useful for trt of P. aeruginosa and patients with CF

Front 273

fluoroquinolones for bone joint and soft tissue infections

Back 273

cipro - shouldnt be given to children or pregnant women; also trts diabetic foot ulcers

Front 274

treatment of TB (also M. avium complex in AIDS patients)

Back 274

multi-drug regimen; Cipro + clarithromycin and amikacin, or with rifampin, ethambutol and clofazimine for MAC in HIV patients)

Front 275

neutropenic cancer trt

Back 275

quinolones prophylactically decrease gram-neg bacteremia

Front 276

toxicity of fluoroquinolones

Back 276

not recommended for young or pregnant patients due to cartilage erosion; tendonitis, joint swelling;
Sparfloxacin - arrhythmia, photosensitivity

Front 277

drugs used for trt of tuberculosis (antimycobacterial)

Back 277

first-line: isoniazid, rifampin, ethambutol. pyrazinamide, streptomycin;
second-line: amikacin, cipro, ethionamide, p-aminosalicylic acid, capreomycin, cycloserine, viomycin, PAS, thiacetazone, kanamycine, clofazimine, clarithromycin, rifabutin, rifapentine, quinolones

Front 278

mycobacteria

Back 278

aerobic bacilli, acid-fast (not gram-pos or gram-neg); mycolic acid

Front 279

isoniazid

Back 279

BEST; inhibits synth of enzymes needed for synth of mycolic acid; bacteriostatic; used in most drug regimes and in prophylaxis of skin test converters;

Front 280

admin of isoniazid and its adverse effects

Back 280

oral, IM;
hepatotoxicity, neurotoxicity; alleviated by pyridoxine; anemia, lupus-like syndrome, liver enzymes monitored in high-risk patients

Front 281

rifampin

Back 281

second-most imp; bactericidal; blocks RNA synth by binding DNA-dep. RNA polymerase; used for TB and leprosy; prophylactic for INH-intolerant patients

Front 282

kinetics

Back 282

oral; goes to CNS; turns urin, sputum and saliva red-orange; eliminated in orange feces; adverse: GI upset; hepatits in alcoholics and elderly; proteinuria, impaired antibody response; CANNOT BE USED WITH PROTEASE INHIBITORS IN HIV PATIENTS

Front 283

rifabutin

Back 283

semisynthetic; active agianst some of the rifampin-resistant strains; active against MAI and non-tubuerculous mycobacteria

Front 284

Ethambutol

Back 284

bacteriostatic; unknown mechanism; oral, CNS; used for TB in combo regimen; adverse: Green blindness, retinal damage, peripheral neuritis, confusion

Front 285

pyrazinamide

Back 285

deriv of nicotinic acid; bactericidal; converted to active drug by the M. tuberculosis; similar to isoniazid, but specific for TB

Front 286

streptomycin

Back 286

used in combo trt for tuberculosis meningitis and organ tuberculosis; an aminoglycoside

Front 287

Leprsy (Hansen's disease)

Back 287

sulfones - dapsone, acedapsone;
clofazimine - binds DNA, skin discoloration

Front 288

Dapsone

Back 288

inhibition of folic acid synth; eliminated in urine; alternative drug for P. carnii in AIDS patients;
adverse: GI, fever, rash, methemoglobinia; hemolysis in G6PDH deficiency

Front 289

acedapsone

Back 289

repository form of dapsone

Front 290

atypical mycobacterial infections

Back 290

MAC, MAI, M. ulcerans, M. marinum, M. abscessus, M. haemophilum, M. xenopi

Front 291

drugs for atypical myobacterial infections

Back 291

antimycobacterials: ethambutol, rifampin, rifabutin;
other antibiotics: erythromycin, amikacin, azithromycin, clarithromycin, cipro

Front 292

opportunistic mycoses

Back 292

fungal infections in patients who are immune-comproised

Front 293

endemic mycoses

Back 293

distributed evenly throughout world

Front 294

amphotericin B

Back 294

antifungal; amphipathic; interacts with ergosterol in fungal membrane to make it leaky to Na, K, H;
used for severe fungal infections; IV for fungal meningitis and systemic infections; bladder irrigation for Candida cystitis; cream for superficial Candida;

Front 295

adverse effects of amphotericin B

Back 295

flushing, chills, fever, headache, anemia, whistling respiration, decreased renal function, azotemia (urea in blood); lipid formulations bind to mammalian membranes less readily -- reduce renal impairment caused by this drug, but costly

Front 296

flucytosine

Back 296

antifungal; converted to 5-fluorouracil and inhibits thymidylate synthase; fungistatic; used for systemic candidiasis, cryptococcal infection, combo with amphotericin B for cryptococcal meningitis; adverse: bone marrow suppression, GI effects

Front 297

imidazoles and triazoles

Back 297

antifungals; triazoles have less effect on human sterol synth and are more slowly metabolized than imid; inhibits 14-alpha demethylase necessary for synth of ergosterol; drugs end in "azole

Front 298

clotrimazole

Back 298

topical, oral trouche (lozenge) for oropharyngeal candidiasis (used often in AIDS pt)

Front 299

miconazole (Monistat)

Back 299

topical and parenteral; cutaneous candidiases and vulvovaginitis due to C. albicans; also oral candidiasis

Front 300

itraconazole

Back 300

oral and parenteral; suppressive therapy of histoplasmosis in HIV pts; similar to ketoconazole

Front 301

fluconazole (Diflucan)

Back 301

effective for immunocompromised pt; more specificity than ketoconazole; primary trt of cryptococcal meningitis in AIDS pt; trt of mucosal candidiases (orophar, esoph)

Front 302

Ketoconozaole

Back 302

only antifungal that is routinely used systemically; first antifungal agent avail for deep sytemic mycoses; drugs that increase gastric pH reduce absorpiton of ketoconazole; effective for deep-seated candidiasis; oral and pharyngeal cand. in AIDS pt.

Front 303

tioconazole, terconazole, butoconazole

Back 303

vaginal ointment, vaginal suppository, and vaginal cream, resp.

Front 304

adverse effects of ketoconazole

Back 304

prolongs QT interval, causing ventricular tachycardia, torsade de pointes, not recommended for pregnant or nursing women b/c of endocrinological abnormalities due to inhibition of steroid biosynth.

Front 305

nystatin

Back 305

similar to amphotericin B; topical, but foul taste; toxic parenterally; used for Candida infections of mucosa, skin, intestine, vagina

Front 306

Griseofulvin

Back 306

antifungal; fungistatic; disrupts mitotic spindle formation; binds keratin; systemic for diseases of skin, hair, nails;

Front 307

ciclopirox

Back 307

antifungal; cream and lotion, acts on cell membrane

Front 308

tolnaftate and butenafine

Back 308

for dermatophyte infections; topical

Front 309

naftifine and terbinafine

Back 309

inhibit squalene epoxidase

Front 310

DNA viruses

Back 310

enter host nucleus, transcribe viral DNA to mRNA using host RNA pol; makes viral proteins;
exception: poxvirus has its on RNA pol

Front 311

RNA viruses

Back 311

host cell is usually not involved in RNA replication; rubella, rhabdoviruses, picornavirus, arenavirus, arbovirus, orthomyxovirus, paramyxoviruses, retrovirus

Front 312

antiviral agents

Back 312

inhibit replication of virus; do not usually eliminate non-replicating or latent viruses; must undergo phosphorylation to be effective

Front 313

classes of antivirals

Back 313

Anti-herpetic, anti-CMV agents; influenza A agents; RSV agents; Anti-retroviral - NRTI's, NNRTI's, protease inhibitors, fusion inhibitors

Front 314

HSV 1 and HSV 2

Back 314

HSV 1: disease of mouth, face, skin, esophagus, brain;

HSV 2: genitals, rectum, skin, hands, meninges

Front 315

Acyclovir

Back 315

anti-herpetic;
guanine analogue;
inhibits vDNA pol; trts HSV I and 2, varicella zoster, CMV (prophylaxis in transplant pt); topical, oral, IV

Front 316

idoxuridine and trifluridine

Back 316

ant-herpetic;
inhibits DNA synth; topical trt of HSV I keratitis (trifluridine is more potent); ocular epithelial HSV and trifluridine for primary keratoconjunctivitis

Front 317

adverse effects of idoxuridine ad trifluridine

Back 317

parenteral admin causes marrow death; pain, pruritis, edema of eyelids, inflammation

Front 318

vidarabine

Back 318

anti-herpetic;
adenosine analog; inhibits DNA pol; HSV encephalitis, neonatal herpes, herpes zoster, varicella zoster, HSV keratitis; less allergenic than idoxuridine; teratogenic

Front 319

ganciclovir

Back 319

anti-herpetic;
inhibits DNA pol; must be phosphorylated;
chronic suppression CMV retinitis in immunocomp pt. and acyclovir-resistant HSV; CMV prophylaxis in transplant pt; adverse: leukopenia, thrombocytopenia, CNS side effects

Front 320

Foscarnet

Back 320

anti-herpetic; PHOSPHATE analogue (not base analogue); inhibits vRNA pol, DNA pol, HIV RT; admin IV for CMV retinitis in immunocomp pt; herpes in AIDS pt and HSV resistant to acyclovir and ganciclovir; adverse: nephrotoxicity, electrolyte disturbance

Front 321

ribavirin

Back 321

purine nucleoside analogue; must be phosphorylated; trt of influenza A and B, RSV (bronchitis, pneumonia); aerosol form approved for RSV bronchiolitis and pneumonia in hospitalized children;
IV for immune suppresed pt. and Lassa fever;
adverse: myelosuppression, conjunctival irritation with aerosol

Front 322

cidofovir

Back 322

anti-herpetic; HSV 1 and 2, CMV; phosphorylation not necessary

Front 323

fomivirsen

Back 323

inhibits CMV through antisense mechanism that inhibits protein synth; IV for CMV retinitis in AIDS pt

Front 324

NRTI's

Back 324

nucleoside reverse transcriptase inhibitors; anti-retroviral;
azidothymidine, zidovudine - thymine analogues;
also Didanosine, Zalcitabine, Lamivudine, Stavudine; pg C77

Front 325

abacavir

Back 325

guanine analogue, NRTI; HIV

Front 326

NNRTI's

Back 326

nevirapine, delavirdine, efavirenz; bind RT at different site than do NRTI's; do not requre phosphorylation

Front 327

retroviral protease ihibitors

Back 327

ritonavir, saquinavir, indinavir, nelfinavir, amprenavir, atazanvir; inhibit cleavage of precursors to viral proteins and enzymes; used for HIV; CI for use with rifampin

Front 328

amantadine and rimantadine

Back 328

inhibit M2 protein of influenza A virus, inhibiting replication; also effective against influenza C; rimantadine: prophylaxis and trt in adults, but only prophylaxis in children;
amantidine also useful in trt of parkinsonism; adverse: neurotoxic effects

Front 329

zanamivir and oseltamivir

Back 329

ihibit viral neuraminidase, essential for replication;
trt of influenza A and B; zanamivir: intranasal; oseltamivir: oral prodrug, activated by liver;
decrease duration and intensity of flu

Front 330

Palivizumab

Back 330

monoclonal antibody against F glycoprotein on RSV; IM; adverse: aminotransferase elevation

Front 331

interferons (IFN)

Back 331

cytokines; affect viral RNA and DNA synth;
IFN-alpha for hep B, C; Kaposi's sarcoma in HIV pt.; genital warts; herpes zoster in cancer pt.