Micro Drugs Period 6 - Cory

Front 1

Beta Lactams--MOA

Back 1

Inhibits transpeptidase (needed for cell wall synthesis)-- Bactericidal

Front 2

Beta Lactams--PK

Back 2

oral absorption varies, don't use topical,dont cross BBB

Front 3

Beta Lactams--Resistance Mech

Back 3

Penicillinase, decreased uptake by G(-)

Front 4

Beta Lactams--AR

Back 4

Allergy, toxicity, GI upset

Front 5

Penicillin G

Back 5

Not effective orally; Good against G(+) and G(-) cocci, not good against G(-) rods and anaerobes; Beta-lactamse sensitive

Front 6

Penicillin G -- Clinical Uses

Back 6

S. pneum, Staph, N. meningitidis, Clstridium sp., Treponema pallidum

Front 7

Penicillin V

Back 7

Better oral absorption than penicillin G, otherwise about the same.

Front 8

Oxacillin

Back 8

Beta Lactam, resistant to beta-lactamase; produces more side effects

Front 9

Oxacillin -- Clinical Uses

Back 9

Mixed Staph and Strep infections, Enterococci and MRSA are resistant

Front 10

Amoxicillin

Back 10

Beta Lactam; effective against non-lactamase G(-), e.g. E. coli, H. flu, Salmonella, Shigella

Front 11

Piperacillin

Back 11

Beta-Lactam; not penicillinase resistant; reserved for bad infections, e.g. Pseudomonas

Front 12

Clavulanic Acid

Back 12

Beta-lactamase inhibitor; synergistic use with amoxicillin

Front 13

Cephalosporins

Back 13

Inhibit cell wall synthesis

Front 14

1st generation Cephalosporins

Back 14

Cephalexin; Good against G(+) and some CA G(-); Do not cross BBB

Front 15

2nd generation Cephalosporins

Back 15

Extended G(-) spectrum, some efficacy against oral and bowel anaerobes

Front 16

3rd generation Cephalosporins

Back 16

Cross BBB; Good for meningitis caused by pneumococci, meningococci, H flu, and susceptable E coli, Kleb, and pen resistant N. gonorrhea

Front 17

4th generation Cephalosporins

Back 17

Enhanced resistance to beta-lactamase; crosses BBB;

Front 18

Imipenem -- MOA + PK

Back 18

Beta-lactam containing, inhibits cell wall synthesis; coadmnister with cilastatin; crosses BBB; beta-lactamase resistant

Front 19

Imipenem -- Clinical + Toxicity

Back 19

Used to treat nosocomial infections, not for CA, MRSA, or VRE

Front 20

Aztreonam -- MOA and PK

Back 20

Monocylic lactam, inhibits cell wall synthesis; poor oral absorption; penetrated inflamed CNS

Front 21

Aztreonam -- Clinical

Back 21

Active against G(-) rods, not against G(+) or anaerobes. Mild adverse reactions

Front 22

Vancomycin -- MOA and PK

Back 22

Bacterial cell wall synthesis inhibitor; poor oral absorption, distributes throughout the body including inflamed meninges.

Front 23

Vancomycin-- Resistance and Toxicity

Back 23

Plasmid Encoded-leads to to production of altered cell wall subunits; Ototoxic and nephrotoxic

Front 24

Vancomycin- Clinical

Back 24

Active against most G(+) cocci and bacilli, not effective against most G(-); Combination with aminoglycoside is synergystic

Front 25

Daptomycin

Back 25

Depolarizes G(+) bacterial membrane; IV administration; used to treat MRSA

Front 26

Gentamicin -MOA and PK

Back 26

Aminoglycoside; interferes with bacterial protein synthesis, causes insertion of incorrect amino acid; bacteriocidal; poor oral absorption

Front 27

Gentamicin - resistance and toxicity

Back 27

Resistance not a big issue; Low therapeutic index; ototoxic and nephrotoxic; limits use

Front 28

Gentamicin - Clinical

Back 28

Most effective against G(-) aerobes, E. coli, Klebsiella, Pseudomonas.

Front 29

Tetracycline - MOA and PK

Back 29

Inhibits protein synthesis; bacteriostatic; widely distributed, crosses BBB even in absence of inflammation; crosses placenta; Contraindicated in renal insufficiency

Front 30

Tetracycline - Drug interactions

Back 30

Due to CYP450 metabolism; oral contraceptive efficacy may be reduced, warfarin levels increased

Front 31

Tetracycline - Adverse Reactions

Back 31

Psudomembranous colitis; photosensitivity; incorporation into growing teeth; avoid during pregnancy and before 8 yo

Front 32

Tetracycline - Clinical

Back 32

DOC for Lyme dz, RMSP, Q fever, M. pneumonia, Chlamydia; Broad spectrum

Front 33

Choramphenicol - MOA and PK

Back 33

Protein synthesis inhibitor, bacteriostatic; Widely distributed, crosses BBB even in absence of inflammation; crosses placenta;

Front 34

Chloraphenicol - Resistance and toxicity

Back 34

Plasma encoded, reduced drug permeability; hematologic toxicity; grey baby syndrome

Front 35

Chloramphenicol - Clinical

Back 35

Toxicity limits use; used for sever anaerobic infections; Cheap and bread spectrum

Front 36

Erythromycin - MOA and PK

Back 36

Protein synthesis inhibitor, bacteriostatic; oral administration, does not cross BBB

Front 37

Erythromycin -Resistance

Back 37

Major problem; decreased permeation of drug through cell envelope; methylase activity; inactivation by esterase

Front 38

Erythromycin - Toxicity

Back 38

Very safe; CYP450 inhibitor;

Front 39

Erythromycin - Clinical

Back 39

G(-) and G(+) aerobes ans some anaerobes. Often used in penicillin-allergic patients

Front 40

Telithromycin - MOA and PK

Back 40

Semi-synthetic macrolide-Protein synthesis inhibitor; Oral administration

Front 41

Telithromycin - Toxicity and Clinical

Back 41

GI effects; Contraindicated in Myasthenia gravis; Approved for CA pneumonia, sinusitis, bronchitis

Front 42

Clindamycin - MOA and PK

Back 42

Protein synthesis inhibitor; oral administration; resistance simaler to erythromycin

Front 43

Clindamycin - Toxicity and Clinical

Back 43

Diarrhea; pseudomembranous colitis; Mostly used as alternative therapy;

Front 44

Streptogramins

Back 44

Protein synthesis inhibitor; no oral absorption; inhibits metabolism of cyclosporine, CCB, NNRTI, PI; used for Vanco resistant E. faecium

Front 45

Linezolid

Back 45

Protein synthesis inhibitor; oral administration; used for vanco resistant E. faecium and MRSA

Front 46

Sulfonamides - MOA

Back 46

Competitive inhibitors of PABA, blocking synthesis of folate, blocking synthesis of nucleotides. Bacteriostatic.

Front 47

Sulfonamides - PK

Back 47

Rapidly absorbed, distributed throughout the body, including CNS; Reduce dosage in renal failure

Front 48

Sulfonamides - Resistance

Back 48

Significant; Drug inactivation; overproduction of PABA, ect.

Front 49

Sulfonamides - Toxicity

Back 49

Acute hemolytic anemia seen in pts with G6PD def; aplastic anemia; hypersensitivity rxns

Front 50

Trimethoprim - MOA and PK

Back 50

Targets folate biosynthetic pathway; inhibits bacterial dihydrofolate reductase; oral avail; crosses BBB

Front 51

Trimethoprim - Resistance and Toxicity

Back 51

Plasma encoded dihydrofolate reductace resistance; problems in pts with pre-existing folate deficiency

Front 52

Trimethoprim - Clinical

Back 52

Combined with sulfamethoxazole; H. flu, P. carinii, Salmonella, Shigella, AOM (not first line)

Front 53

Ciprofloxacin - MOA and PK

Back 53

Inhibit gyrase and topoisomerase IV; bactericidal; oral administration; concentrates in urine

Front 54

Ciprofloxacin - Resistance and Toxicity

Back 54

Results form mutations in gyrase or reduced drug uptake; Generally well tolerated

Front 55

Ciprofloxacin - Clinical

Back 55

Effective vs. most the of the bugs causing UTI's, though not first line therapy.

Front 56

Nitrofurantoin - MOA and PK

Back 56

Damage DNA; More effective at low pH-acidify urine; concentrate in the urine; contraindicated in renal insufficiency

Front 57

Nitrofurnatoin - Clinical

Back 57

Uncomplicated lower UTI; Most E. coli; most G(+)

Front 58

Methenamine - MOA and PK

Back 58

Releases formaldehyde in acidic urine; must be enteric coated

Front 59

Methenamine - Toxicity and Clinical

Back 59

Contraindicated in hepatic insufficiency d/t ammonia production; Very broad spectrum, used for chronic supressive therapy; not used for acute UTI's or upper UTI's

Front 60

Fosfomycin - MOA and PK

Back 60

Cell wall synthesis inhibitor (blocks peptidoglycan synth.);excreted unchanged in urine

Front 61

Fosfomycin - Clinical

Back 61

Used for one-dose treatment of uncomplicated UTI by E. faecalis or E. coli

Front 62

Isoniazid - MOA

Back 62

Inhibits mycolic acid biosynthesis; bacteriostatic for non-deviding cells, bactericidal for dividing cells

Front 63

Isoniazid - PK

Back 63

Oral or IV dosing; goes to all body fluids including CSf ans pleural fluid

Front 64

Isoniazid - Resistance and Toxicity

Back 64

Mutants are easily selected, even at high doses; rash, fever; Jaundice; peripheral neuritis

Front 65

Isoniazid - Clinical

Back 65

Used to treat TB; Not effective in monotherapy; used as preventative therapy

Front 66

Rifampin - MOA and PK

Back 66

Inhibits bacterial DNA dependant RNA polymerase; oral dose; well distributed, including CNS

Front 67

Rifampin - Resistance and Toxicity

Back 67

One-step resistance developes spontaneously; Rash, fever N&V

Front 68

Rifampin - Clinical

Back 68

Used to treat TB; not effective as mono therapy; also used for nasopharyngeal carriers of N. meningitidis

Front 69

Ethambutol - MOA and PK

Back 69

MOA unknown; only effective against mycobacterium that are dividing; oral avail.

Front 70

Ethambutol - Toxicity and Clinical

Back 70

Diminished visual acuity, skin rash, drug fever; Used to treat TB

Front 71

Pyrazinamide

Back 71

MOA is unknown; resistance if used alone; Used to treat TB

Front 72

Chloroquine - MOA and PK

Back 72

Likely interferes with heme metabolism; tocix to parasite; well absorbed oral, IM, sub-q; tissue sequestration

Front 73

Chloroquine - Toxicity and Resistance

Back 73

Oral dosing very safe; contraindicated in renal insufficiency or blood disorders; Useless in most parts of the world

Front 74

Chloroquine - Clinical

Back 74

Treatment of acute attacks by sensitive strains of falciparum and no-falciparum; prophylaxis in some areas

Front 75

Mefloquine - MOA and PK

Back 75

Blood schizonticide-not effective against hepatic stages; Oral dosing only; single dose prophylaxis okay due to slow elimination

Front 76

Mefloquine - Toxicity and Resistance

Back 76

CNS effects- anxiety and psychosis; Nausea; Some resistance in drug treated patients

Front 77

Mefloquine - Clinical

Back 77

Used for acute attacks of chloroquine resistant strains; prophylaxis in areas where chloroquine resistant strains are endemic

Front 78

Primaquine - MOA and PK

Back 78

Kills late hepatic stages and latent tissue forms of vivax and ovale; not effective against erythrocytic forms; oral dosing

Front 79

Primaquine - Toxicity and Resistance

Back 79

Few toxicity at lower doses; hemolytic anemia in pts with G6PD def.; Resistance overcome with higher/miltiple doses

Front 80

Primaquine - Clinical

Back 80

Used to effect a radical cure of P. vivax and P. ovale following clinical cure

Front 81

Quinine - MOA and PK

Back 81

MOa unkown, acts as schizonticide; Oral or IM;

Front 82

Quinine - Toxicity

Back 82

Hearing and vision effects; Gi distress; hypoglycemia; Hypersensitivity; Hemolytic anemia in G6PD def.; enhanced effects of neuromuscular blocking agents

Front 83

Quinine - Clinical

Back 83

Used to treat attacks of drug resistant P. falciparum; not useful in prophylaxis; Combination therapy with doxycycline

Front 84

Malarone

Back 84

Combination of atovaquone and proguanil; treatment and prophylaxis of MDR P. falciparum

Front 85

Metronidazole - MOA and PK

Back 85

Systemic anti-amebal; blocks DNA synthesis; oral administration; penetrates body fluids and tissue;

Front 86

Metronidazole - Toxicity

Back 86

HA, nausea, dry mouth; GI upset; CNS effects; disulfram like effect in alcoholics; carcinogenic in rats and mice

Front 87

Metronidazole - Clinical

Back 87

Used to treat Trichomonas vaginalis, Giardiasis, amebiasis

Front 88

Paromomycin

Back 88

Luminal anti-amebal; broad spectrum anti-biotoc; not significantly absorbed

Front 89

Diiodohydroxyquin

Back 89

Luminal amebicide; poorly absorbed; well tolerated

Front 90

Pentamidine

Back 90

Treatment of PCP; higher pulmonary concentration acheived by inhalation; Toxicity major problem; rash, neutropenia, nephrotoxicity

Front 91

Mebendazole - MAO and PK

Back 91

Broad spectrum anti-intestinal roundworm; binds to tubulin, interferes with organell transport; low absorption

Front 92

Mebendazole - Toxicity

Back 92

Teratogen in rodents, dont use in pregnancy or young children

Front 93

Mebendazole - Clinical

Back 93

Used to treat roundworm infections by; Ascaris lumbricoides, Trichuris trichiura, Ancylostoma duodonale, Trichinella spirales

Front 94

Praziquantel - MOA and PK

Back 94

Increases cellular calcium permebility; oral administration

Front 95

Praziquantel - Toxicity

Back 95

GI distress; HA, dizziness, drowsiness; rash and fever

Front 96

Praziquantel - Clinical

Back 96

used to treat trematodes (flukes) and cestodes (tapeworms)

Front 97

Amphotericin B - MOA and PK

Back 97

Forms pores in fungal plasma membrane; Fungistatic; Poor oral absorption

Front 98

Amphotericin B - Clinical

Back 98

i.v. for systemic infections; intrathecal for meningitis; very toxic, but is DOC for many fungal infections

Front 99

Flucytosine - MOA and PK

Back 99

Fungistatic; inhibits DNA synthesis by blocking thymidylate synthetase; orally absorbed; enters CNS

Front 100

Flucytosine - Toxicity

Back 100

Nausea, vomiting, rash; Use with caution in pt with renal insufficiency; may cause reversible neutropenia or thrombocytopenia

Front 101

Flucytosine - Clinical

Back 101

Resistance is a major problem, so give with Amphotericin B; Used for systemic infections.

Front 102

Ketoconazole - MOA and PK

Back 102

Inhibits fungal ergosterol sythesis; oral dosing, dont take with antacids; does not cross BBB

Front 103

Ketoconazole - Toxicity

Back 103

Nausea, vomiting, rash; gynocomastia; p450 inhibitor; some resistance

Front 104

Ketoconazole - Clinical

Back 104

Used for chronic mucocutaneous candidiasis and paracoccidiomycosis; otherwise not a first choice drug

Front 105

Fluconazole - MOA and PK

Back 105

Inhibits ergosterol synthesis; well absorbed orally; crosses BBB;

Front 106

Fluconazole - Toxicity

Back 106

Generally well tolerated; rare reversible thrombocytopenia; P450 inhibitor

Front 107

Fluconazole - Clinical

Back 107

Used to treat oropharyngeal and esophageal candidiasis; also prophylaxis in organ transplant pts

Front 108

Terbinafine - MOA and PK

Back 108

Blocks ergosterol synthesis; oral and topical administration; accumulates in hair and nails, secreted in sebum

Front 109

Terbinafine - Toxicity

Back 109

GI complaints and skin reactions; not recommended in pts with liver dz

Front 110

Terbinafine - Clinical

Back 110

Oral used for onychomycosis of nails d/t dermatophytes; topical for for skin infections by Trichophyton and candida

Front 111

Capsofungin - MOA and PK

Back 111

Inhibits fungal cell wall synthesis; i.v. only;

Front 112

Capsofungin - Clinical

Back 112

Effective against susceptible Aspergillus and Candida

Front 113

Griseofulvin - MOA and PK

Back 113

Inhibits mitotic functions; oral drug for superficial infections;

Front 114

Griseofulvin - Toxicity

Back 114

P450 inducer; nausea, vomiting, headache;

Front 115

Griseofulvin - Clinical

Back 115

Effective against Epidermophyton, Microsporum, Trichophyton; not effective against Candida

Front 116

Nystatin - MOA and PK

Back 116

Forms pore in plasma membrane; used topically only; though can be used orally to treat bowel infection

Front 117

Nystatin - Clinical

Back 117

Treatment of Candida infections of skin, mucus membranes and bowel

Front 118

Clotrimazole and Miconazole -

Back 118

Inhibit ergosterol synthesis; topical only; oral, vaginal; skin Candida