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1
Q

Common mechanisms of Drug resistance?

A

Spontaneous mutations in target proteins, Natural enzymes that inactivate agent, Spontaneous changes in membrane permaability

2
Q

Molecular Targets for Antimicrobial drugs

A

Cell Wall synthesis, DNA gyrase, DNA-Direction RNA polymerase, Protein synthesis, Cell membrane, Folic acid metabolism, Periplasmic space

3
Q

Gram negative vs Gram positive

A

Gram negative has small cell wall, gram positive have big cell wall

4
Q

B-lactam anibiotic classes

A

Cephalosporins and penicillins

5
Q

Mechanism of Beta-lactam Action

A

Bind to Pencillin binding proteins, Inhibits peptidoglycan synthesis, Stimulates Autolysins, results in cell lysis

6
Q

Beta Lactams are inactivated by?Static or cidal?Most effective against Gram pos or Neg?

A

B-lactamASES, Gram positive but can have effect on negative

7
Q

What is the allergen from Pencillins?

A

Penicillinoic acid

8
Q

Natural Pencillins, Route, and Target, CNS penetration?

A

G, V, G (Benzathine), G is iv/im, V is oral, G B is IM long acting. Gram positive. No CNS

9
Q

What does MRSA really stand for?

A

Resistant to all Beta lactams

10
Q

Semisynthetic Pencillins ases resistant, route, used for? CNS penetration?

A

Nafcillin, Dicloxacillin.. Good CNS with meniges inflammation

11
Q

Semisynthetic Pencillins (Extended spectrum). Route, Spectrum? Combination of?

A

Amoxicillin, Ampicillin, Piperacillin Extended to Gram + and some Gram -. Combination of minopencillin + Beta-lactamase inhibitor(Clavulanate, Sulbactam,Tazobactam)

12
Q

Synthetic Penicillin-Like (Carbapenems), Spectrum? Co-admined with?

A

Imipenem/Cilastatin. Broadest spectrum Most + and - . Coadministered with Cilastatin. Inhibitor of the degradation renal enzymes

13
Q

Semi-synthetic monobactams. Spectrum? Not affected by?What patients?

A

Aztreonam. Inhibits PBP of Gram NEGATIVE ONLY, beta lactamases. Good for B-lactam allergic patients with gram negative

14
Q

Cephalosporins are used as what in hospital settings?Natural product of?

A

Prophylaxis, molds

15
Q

1st Generation Cephalorsporins, Specrum, Used for?

A

Cephazolin (Ancef), Cephalexin (Keflex), Gram + and Some gram -, Surgical prophylaxis, UTI

16
Q

2nd Generation Cephalorsporins, Spectrum? Used for?

A

Cerfuroxime (Zinacef), Cefuroxime axitel (Ceftin), Intermediate Spectrum. Gram + and extended Gram Negative.

17
Q

Third Generation Cephalorsporins. Spectrum? Used for? Special consideration?

A

Ceftriaxone (Rocephin), Ceftazidime (Fortaz), Broad spectrum Gram + and Gram Negative. CNS penetration

18
Q

Fourth Generation cephalosporins. Spectrum? Used for?

A

Cefepime (Maxiprime). Very broad Gram + and Negative. Aerobic. Used for limited resistants and nosocomial infections

19
Q

B-Lactam adverse reactions. 3 stages and effects

A

1st immediate= anaphylaxis <72 hours Milder, maybe rash. 3rd is Late reaction Drug fever

20
Q

Tetracycline bacteriostatic or bacteriocidal?

A

Static

21
Q

Tetracycline mechanism

A

Blocks tRNA bind=Block protein synthesis 30s

22
Q

Tetracycle spectrum? UV? Divalent metals?

A

Very broad spectrum. Forms complexes with Teeth and Bones. Absorbs UV causing inflammatory response

23
Q

Chloramphenicol block wwhat ribsome?

A

50s

24
Q

Chloramphenicol spectrum? Cidal or static? Alternative for?

A

Extremely broad. Static. Alternative to Beta lactams for CNS

25
Q

Chloramphenicol side effects bone marrow? Babys?

A

Grey baby, Bone marrow toxicity

26
Q

Macrolide/Ketolides block what ribsome?Static or cidal?Spectrum?

A

50S, static, NO CNS, Gram positive with limited negative

27
Q

Macrolide and Ketolide Protoypes

A

Erythromycin, Azithromycin, Clarithrymycin, Telithromycin, Clindamycin

28
Q

Polumyxin spectrum? Acts on? Static or cidal? ROUTE?

A

Gram Negative bacteria. Acts on lipid membrane. BacteriCIDAL, TOPICAL only

29
Q

Bacitracin Route? Spectrum? Mechanism?

A

Topical only. Limited to Gram positive. Blacks cell wall synthesis

30
Q

Vancomycin Route? Spectrum? Mechanism?

A

IV/IM, Limited to Gram positive. Blocks cell wall synthesis

31
Q

Inhibitors of Cell wall synthesis?

A

Bactracin and vancomycin

32
Q

Tigecycline is for? Spectrum? Mechamism?Class?

A

Resistant strains. Tetracyline. Blocks tRNA binding on 30s ribosome. Broad + and - spectrum

33
Q

Quinupristin/Dalfopristin (Synercid). Spectrum? Class? Used for? Mechanism?

A

Blocks protein synthesis on 30s ribosome. Used for ONLY Gram positive. For resistant Vanomycin strains. Macrolide class

34
Q

Linezolid. Spectrum?Class? Used for? Mechanism?

A

Oxazolidone class. Blocks protein synthesis at TRNA formation. Broad against Gram positive. For VRSA

35
Q

Daptomycin. Class?Spectrum?Used for?

A

Natural derived class. Used for MRSA and VRE. Gram positive

36
Q

Mercaptopurine mechanism, converted to?

A

Blocks purine synthesis by being an analog of purine bases hypoxanthine or adenine, T-IMP

37
Q

Azathioprine is?

A

prodrug of 6-MP

38
Q

Methotrexate mechanism, inhibits what enzyme and synthesis

A

Inhibits dihydrofolate redutase and inhibits synthesis of thymidine and purines

39
Q

5-Flurouracil mechanism, inhibits what? Inhibits synthesis of what?

A

Inhibits thymidylate synthase, inhibiting synthesis of thymidine

40
Q

Hydroxyurea inhibits what?

A

ribonucleotide reductase

41
Q

Anti-microtubules are considered to be what phase specific agents?

A

M phase

42
Q

Anti dna nucleotide synthesis is for what phase?

A

G1

43
Q

Vinca alkaloids mechanism? Vincristine, Vinblastine, Vinorelbine

A

Binds to tubulin and inhibit tublin polymerization

44
Q

Taxanes (Paclitaxel, Docetaxel) mechanism

A

prevent depolymerization

45
Q

Anthracyclines (doxorubicin, Daunorubicin mechanism

A

Insert into DNA, inhibits topoisomerase II and induce production of ROS. Deforming DNA

46
Q

Bleomycin (blenozane, Cipla, Bleocip), anesthesia concerns

A

Requires metal and oxygen for its activity, causes DNA damage by producing ROS. Causes pulmonary fibrosis

47
Q

Nitroden mustards:cyclophosphamide

A

Alklyating agents, crosslinking DNA.

48
Q

Tamoxifen is?

A

Selective estrogen receptor modulator for breast cancer

49
Q

Aromtase inhibitor (Anastrozole)

A

Blocks estrogen synthesis

50
Q

Imatinib (Gleevec)

A

Inhibits Tyrosine kinase inhibitor for Chronic myeloid leukemia

51
Q

Trastuzumab (Herceptin)

A

Monoclonal antibody against HER2, for breast cancer, cardiotoxic

52
Q

Bevacizumab (Avastin)

A

Monoclomal antibody againsst Angiogensis

53
Q

FDA Pregnacy rating ABCDX

A

A, adequate studies show no risk, B Animal studies fail to show risk, no study in human. C-Animals positive, no studies Human. D-Positive in human studies but may be used. X-Animals/Human positive and risks outweight benefits. N-No classification

54
Q

Thalidomide concerns, which enantomer?

A

Presciped for pregnacy associated nausea, bilateral limb reduction, kidney eyes ears heart deformities. S enantiomer

55
Q

Diethylstilbesterol (DES)

A

Oral synthetic nonsteroidal estrogen analog, Use to prevent miscarriages. Teratogen seen 20-30 years later

56
Q

Fetal Alcohol syndrome

A

Most common cause of mental retardation, completely preventable

57
Q

Phenytoin (Dilatin)

A

Antiepileptic medicationm, will show and resemble FAS (feal alcohol syndrome), epoxide hydrolase 1. Fetal Hydantoin syndrome

58
Q

Mechanism of Nicotine/Tobacco tetragenic effects

A

Growth retardation, restrictions uterine blood vessels chronic hypoxia and malnutrition

59
Q

Retinoids Isotretinoin(acutane)

A

Vitamin A analog, for acne causing fetal abnormality

60
Q

Gamma Globulin (IgG) mechanism viruses

A

Blocks the attachment of virus particles to host cells

61
Q

Amantadine rimantadine

A

Targets m2 protein of influeza A virus and prevents uncoating of vesicle by blocking acidification of vesicle

62
Q

Oseltamivir (Tamiflu

A

Targets influenza A and B and prevents replication and host cleavage from host cell nueraminidase inhibitor. Inhibits respiratory spread

63
Q

Acyclovir mechanism, what is needed for it to work? Prodrug?

A

Inhibits viral dna polymerase, requires viral hymidine kinase for activation. Used for herpes infections

64
Q

Forscarnet mechanism and uses

A

Effective against herpes simplex virus that are deficient in thymidine kinase, used for cytomegalovirus reitinitis and acyclovir ressitant herpes

65
Q

Ribavirin uses

A

Used for chronic treatment of hep C and respiratory syncytial virus

66
Q

Zidovudine (AZT)

A

Emtricitabine-reverse transcriptase inhibitors

67
Q

Fuzeon mechanism

A

Interferes with Entry of HIV-1 into cells. Inhibits fusion or viral and cellular membranes

68
Q

Amophotericin B spectrum and mech, side effect

A

broad spectrum severe antifungal agent, big ring structure and one side is hydrophobic because it binds to membrane creating a channel to lose intracellular components. Renal toxicity

69
Q

Griseofukvin mechanismm spectrum?

A

Binds to microtubules causing nterference with mitotic spingle formation and dividing cells, narrow spectrum, atheletes foot

70
Q

Azole mechanism

A

Inhibits ergosterol synthesis, leading to damaged and leaking cell membranes

71
Q

Fluconazole mechanism, spectrum class

A

Very broad spectrum for most candida. single oral fose for yeast infection. For fungal meningiutis, high concentration in CNS. Triazoles

72
Q

Voriconazole for what?

A

active against molds such as aspergillus, for invasive aspergillosis

73
Q

Itraconazole spectrum, interesting properities?

A

broad spectrum, low gastric pH for absorption

74
Q

Posaconazole uses

A

prevent candida and aspergillus infections in immunocompromised patients

75
Q

Ketoconazole what class? For?

A

Class imidazole, broad spectrum effective against fungi

76
Q

Amtimetabolite drug, uses in combination with

A

for systemic fungal infection such as cryptococcal menigitis, combination with amphotericin B

77
Q

New class of antifungal agents

A

Glucan synthase inhibitors, the echinocandins

78
Q

Enchinocandins, Glucan synthase inhibitors

A

Caspofungin, blocks cell wall synthesis, micafungin, anidulafungin

79
Q

Schedule I drugs

A

High potential for abuse and no approved medical use such as heroin

80
Q

Schedule II drugs

A

high potential for abuse but has accepted medical use such as morphine, oxycodone. No automatic refills

81
Q

Scheduled III drugs

A

Moderate potential for abuse and refills can happen 5 times in 6 months

82
Q

Schedule 4 drugs

A

lower potential for abuse and same regulations as 3

83
Q

Schedule V drugs

A

limited potential for abuse, no dispense and refils

84
Q

IND application is?

A

Investigational New drug. Preclinical data, trial design, informed consent form

85
Q

Phase 0 clinical trials

A

microdosing trials, sub therapeutic dose and kinetic and dynamic data

86
Q

Phase 1 clinical trials

A

Tests safety of drug not efficiacy.

87
Q

Phase 2 trials

A

Tests for safety and efficacy,

88
Q

Phase 3

A

Randomized efficacy is compared to the standard treatment

89
Q

NDA is?

A

establishment of DA sets standards for the safety of the ingredients of the drug, labeling and package insert

90
Q

Phase 4 clinical trial

A

additional safety data, or additional uses or in combination with other drugs, increase the “label” of the drug

91
Q

5 Diuretic classes

A

Carbonic anhydrase inhibitor, thiazides, osmotics, K sparing, loops

92
Q

2 high ceiling dieurtics

A

Loop and osmotics

93
Q

3 low ceiling dieurtics

A

K sparing, carbonic anhydrase inhibitor, thiazides

94
Q

Carbonic anhydrase inhibitor site of action and mechanism. Prototype

A

Increased bicarb rentention in the proximal tubule, Acetazolamide

95
Q

Osmotic dieuretic protoype and location and mechanism

A

Proximal tubule and descending loops of henle, Mannitol, increases water excretion

96
Q

Loop dieurtic protoype, site of action, mechianism

A

Furosemide (Lasix), loop of henle. Blocks na k and cl reabsorption

97
Q

Thiazides site of action, mechanism, protoype, side effect

A

Distal tubule, blocks Na cl co transporter.hypokalemia. Hydrochlorothiazide

98
Q

K+ sparing dieurtics, mechanism, site and prototype

A

Collecting duct, blocks Na+ channel, can cause hyperkalemia. Triamteren and amiloride

99
Q

K+ sparing dieurtic that Is an antagonist of aldosterone receptor

A

Spironolactone

100
Q

How do dieurtics cause hypokalemia?

A

Increased NA reabsorption causes excess K excretion

101
Q

Aminoglycosides cidal or static? Mechanism?

A

Cidal, block protein synthesis

102
Q

Aminoglycosides used for?

A

Aerobic gram negative bacteria

103
Q

Streptomycin history and primary use

A

Multidrug resistant TB, first amingolycoside to be developed

104
Q

Isoniazid use, mechanism

A

mycolic acid synthesis inhibition, for TB

105
Q

Rifampin mechanism and uses, side effects

A

TB gram +- and inhibits RNA synthesis and inhibits RNA polymerase in prokaryotic cells, liver toxicity

106
Q

Ethambutol used for only? Static or cidal, indications for use

A

Only for mycobacteria, bacteriostatic, has to be used in combination

107
Q

Pyrazinamide uses, mechanism and interesting factor

A

active at acidic ph, used for TB, inhibits fatty acid synthesis

108
Q

Is combination therapy mandatory for TB?

A

Yes

109
Q

Lunelle dosage and frequency

A

Estradiol and medroxyprogesterone injection every ~30 days

110
Q

Nuvaring contents

A

Ethinyl estradiol

111
Q

Orthoevra contents, rsk

A

E+ P, worn for 7 days, patch risk of blood clots

112
Q

Ctinuous E + p pill, no period

A

Lybrel

113
Q

Yasmin contents and side effects

A

drospirenone plus ethinlestradiol, hyperkalemia, heart problems DVT

114
Q

Progrestin alone therapy does what

A

Endometrial changes, thickening of mucus, prevents ovulation

115
Q

Progesterin only drugs

A

Minipill, depo provera, mirena, implanon

116
Q

Clomiphere uses and mechianism

A

fertility pill, estrogen receptor antagonist

117
Q

Tamoxifen class, what for

A

SERM, breast cancer

118
Q

Raloxifene for? Does what

A

Estrogen antagonist in breast and uterin, agonist in bone. Prevents osteroporosis post menopausal

119
Q

Femara use, mechanism

A

Aromatase inhibitor, reduces estrogen production for breast cancer treatment

120
Q

4 synthetic corticosteroids

A

prednisone, prednisolone, dexamethasone, betamethasone

121
Q

Echanism of action of corticosteroids

A

gene regulation

122
Q

Is alderstrone part of the pituary axis?

A

no, renin angiotensin

123
Q

Treatment of adrenocortical insuffieciency

A

cortisol

124
Q

Treatment of inflammation and immunosuppression

A

Intermediate and long acting

125
Q

Mineralcorticoids effects

A

salt rention and hypertension

126
Q

Most widely used mineralcorticoid

A

fludrocortisone

127
Q

Inhibition of adrenal cortical steroids

A

aminoglutethimide

128
Q

Treatment of hypothroidism

A

Levothryoxine or Liothyronine, Synthroid or L-t3

129
Q

Graves is?

A

caused by hyperthroidism

130
Q

Drug of choice for thryoid storm

A

propanolol

131
Q

Sulfonamides inhibti what? Clinical use?

A

synthesis of dihydropteroate, burn patients, inflammatory disorder of GIT, respiratory infection UTI

132
Q

Trimethoprime mechanism, incombination with

A

inhibits reductase enzyme for tetrahydrofolate, co0trimoxazole

133
Q

Fluoroquinolones mechanism, spectrum?

A

inhibit DNA gyrase, Gram negative aerobic

134
Q

Fluoroquinolones drugs

A

Ciprofoxacin (anthrax),

135
Q

How does mylanta work?

A

decrease acid in stomach

136
Q

Mucosal protectants from acid in stomach

A

Peptobismol, Misoprostol, Sucralfate

137
Q

H2 receptor antagonist

A

Cimetidine, Rantitide, Famotidine, Nizatidine

138
Q

Proton pump inhibitors, pro drugs?7

A

Omeprazole (Prilosec, Lansoprazole Rabeprazole, esomeprazole, all pro drugs

139
Q

Eradication of h.pylori always requires?

A

multidrug therapy such as PPI, antibiotic 1 and 2, amoxicillin clarithromycin and omeprazol