Pharm II MOAs Flashcards

1
Q

Sulfonamide MOA?

A

PABA agonist inhibiting folic acid synthesis

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2
Q

Diaminopyrimidines MOA?

A

Folic acid inhibitor. Reversibly binds and inhibits dihydrofolate reducatase enzyme.

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3
Q

Sulfonamides and Diaminopyrimidines are static or cidal?

A

Static

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4
Q

Beta-Lactam MOA?

A

Inhibits bacterial cell wall synthesis via transpeptidase enzyme inhibition

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5
Q

Beta-lactam resistance achieved by?

A
  1. Production of b-lactamase enzyme. 2. Permeability of cell wall decreased (gram -). 3. Reduced sensitivity of penicillin binding protein.
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6
Q

30S ribosomal subunit protein synthesis inhibitors?

A

Aminoglycosides, Tetracyclines

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7
Q

50s Ribosomal subunit protein synthesis inhibitors?

A
  1. Macrolides, 2. Lincosamides, 3. Chloramphenicol derivatives
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8
Q

All protein synthesis inhibitors are bacteriostatic except?

A

Aminoglycosides

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9
Q

MOA of Flouroquinolones and Metronidazole MOA?

A

DNA inhibitors

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10
Q

MOA of Rifampin

A

RNA inhibitor

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11
Q

MOA of Bacitracin

A

Inhibits peptidoglican synthesis in bacteria by non-specifically blocking phosphorylase reactions

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12
Q

MOA of Nitrofurans

A

Inhibits energy production

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13
Q

MOA of Virginamycin

A

Protein synthesis inhibitor via 23S ribosomal subunit

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14
Q

Antimicrobials interfering with cell membrane?

A

Polymyxin B, Colistin (poly E)

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15
Q

MOA Benzimidazoles?

A

Irreversibly binds to nematodal tubulin, specifically beta-tubulin

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16
Q

Levamisole MOA?

A

Ganlionic stimulant and direct cholinergic drug. Causes paralysis. Can also act as an immune stimulant at low intermittent dosage.

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17
Q

Depolarizing neuromuscular blocking agents?

A

Pyrantel, Morantel, Epsiprantel

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18
Q

Organophosphate compounds MOA?

A

Irreversible inhibition of acetylcholinesterase

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19
Q

Macrocyclic Lactones MOA?

A
  1. Bind selectively with high affinity to glutamate-gated chloride channels. 2. Increases release of GABA from nervous system. 3. Affects egg formation and causes sterility.
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20
Q

Praziquantel MOA?

A

Ca2+ ion flux across surface membranes of exposed parasite-> paralysis, surface swellings, lesions -> lyse

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21
Q

Rafoxanide / Closantel MOA?

A

ATP production inhibition.

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22
Q

Clorsulon MOA

A

Affects glycolytic enzymes and deprives the fluke of its main source of metabolic energy

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23
Q

Nitromidazole / Nitrofurans MOA?

A

Nitro group is cleaved off -> produces unstable intermediates -> DNA destruction

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24
Q

Polyether ionophor MOA?

A

Lipophilic complexes with alkali metals -> change membrane integrity/ internal osmolality

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25
Q

Arsenieals MOA?

A

Binds to disulphide bridges inhibiting enzyme systems

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26
Q

Thiamine analog MOA?

A

Analogue of thiamine -> inhibition of active thiamine transport to protozoa

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27
Q

Thiazine derivatives MOA?

A

Act on apicoplasts

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28
Q

Organophosphates MOA

A

Irreversible inhibition of Ache

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29
Q

Carbomates MOA?

A

Reversible inhibition of Ache

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30
Q

Pyrethrins/Pyrethroids MOA?

A

Interacts with Na channels in membrane

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31
Q

Fipronil MOA

A

GABA and Glutamate Cl ion channel blockers

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32
Q

Imidacloprid MOA?

A

Competitive inhibition of post=synaptic nicotiic receptor (nAChe)

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33
Q

Amitraz MOA?

A

Inhibition of monoamino exidase

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34
Q

IGRs and IDIs MOA?

A

Mimic juvenile hormone resp. inhibition of chitin synthesis

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35
Q

Where do anti-fungals act?

A

Wall, Membrane, intracellular

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36
Q

Intracellular anti-fungals and their MOAs?

A

Flucytosine - pyrimidine analogue: DNA synthesis interference via thymidylate synthesis. Griseofulvin - Mitotic inhibitor: Interferes with mitosis by binding to microtubules

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37
Q

Wall anti-fungal and MOAs?

A

Echinocandins - Inhibits fungal beta glucan synthesis -> exposure of antigens -> host immune response

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38
Q

Anti-fungal acting on cell membrane and MOA? (hint: ergosterol)

A

Polyenes - Form pores in funcal membrane by binding to ergosterol -> electrolyte imbalance. Azoles - Selectively blocks ergosterol synthesis by inhibiting demethylation of lanosterol -> ergosterol. Allylamines - inhibits squalene epoxidase to block ergos

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39
Q

Nucleoside Reverse Transcriptase Inhibitors MOA?

A

(Retrovirus) Causes viral DNA chain termination via phosphorylation of host enzyme -> competition for proviral DNA synthesis

40
Q

Viral DNA Polymerase Inhibitors MOA?

A

(DNA virus) Inhibits viral DNA polymerase via viral thymidine kinase. Only affects infected cells

41
Q

M2-Ion Channel Inhibitors MOA?

A

(RNA virus) Inhibits RNA/ viral release via H+ influx -> acidification of endosome

42
Q

Neuramidase/ Sialidase inhibitors MOA?

A

(RNA virus) Inhibits Neuramidase/ sialidase -> affects viral shedding

43
Q

Ribavirin MOA?

A

(DNA and RNA virus) Inhibits viral replication at multiple sites

44
Q

Interferons MOA?

A

(DNA, Retrovirus) Antiviral via synthesis of enxymes interfering w/ viral replication. Immune modulating via cell-cell interaction: converst effects w/o additional interferon. Alpha/Delta determines WBC targets.

45
Q

Alkylating Agents MOA?

A

Form covalent bonds with DNA -> prevention of replication and transcription

46
Q

Antimetabolites MOA?

A

Block metabolic bathways of DNA synthesis.

47
Q

Cytotoxic Antibiotics MOA?

A

Blocks mammalian cell division via interaction with DNA

48
Q

MOA of Doxorubicin and anthracyclines?

A

Inhibits DNA by interfereing with RNA polymerase and topoisomerase II

49
Q

MOA of Dactinomycin?

A

Intercalates in DNA interfering with RNA polymerase and popoisomerase II

50
Q

MOA of Bleomycin?

A

Fragmentation of DNA chains (acts on non-deviding cells)

51
Q

MOA Mitomycin ?

A

Activated to give an alkylating metabolite

52
Q

Plant Derivatives MOA?

A

Inhibits microtubules/ mitosis

53
Q

Vinca Alkaloid MOA?

A

Inhibit microtubule polymerisation -> arrests in metaphase = no spindle formation or division.

54
Q

Taxanes

A

Stabilize microtubules in polymerized state

55
Q

Tyrosine Kinase Inhibitors MOA?

A

Inhibits tyrosine kinase -> prevent downstream growth signaling.

56
Q

Cancer vaccine MOA? (BCG)

A

Stim immune response to recognize tumor cells

57
Q

Anticancer Vaccine MOA? (L-Asparanginase)

A

catalyzes hydrolysis (à l-aspartic acid + ammonia) à ↓protein synthesis

58
Q

Monoclonal Antibodies MOA

A

Specific for certain cancer receptors

59
Q

Dirlotapide MOA?

A

Selectively inhibits microsomal triglyceride protein transfer-> blocking fat absorption

60
Q

Omeprazole MOA?

A

Inhibition of proton pump

61
Q

Ranatadine MOA?

A

Competitive inhibition of secretion of PCT -> increased serum levels

62
Q

PGE analog (misoprostal) MOA?

A

Inhibits acids, increases mucous production, stabilizes mast cells

63
Q

Sucrafate MOA?

A

in acidic environment, sucrose released and polymerizes over uclders forming a protective barrier

64
Q

Bismuth Subsaliciate MOA?

A

Bismuth- Absorbs E. coli enterotoxin. Subsaliciate - decreases excess secretions

65
Q

Chalogogues MOA? (Mg Sulfate)

A

contract Gall bladder

66
Q

Cholerectics (Glycocholate, Taurocholate, UDCA) MOA?

A

increase bile secretion

67
Q

Eulsifying agents (dimethicone, poloxalene) MOA?

A

Reduces frothy bloat

68
Q

Clenbuterol MOA?

A

B2 agonist = relaxes the bladder

69
Q

Phenoxybenzamine MOA?

A

A agonist = contraction of urethra

70
Q

Prazosine MOA?

A

A1 antagonist = relax hypertonic urethra

71
Q

Diazepam MOA?

A

GABA agonist (central)

72
Q

Dantrolene MOA?

A

Sk. Mm. Relaxant

73
Q

Probenidice/ Sulphinpyrazone MOA?

A

competitive inhibition of ACID active secretion (TCT) -> increase in circulation

74
Q

Carboanhydrase Inhibitors MOA?

A

Increase secretion of bicarb, Na, K, and water by inhibiting carbonic anhydrase.

75
Q

Loop Diuretics MOA?

A

Inhibit Na/K/Cl- carrier -> formation of osmotic gradient.

76
Q

Thiazine Diuretics (Chlorothiazide, Hydrochlorothiazide) MOA?

A

Binds to the Cl- site of the Na/Cl- symport system. (slide 20 diagram is wrong) -> decreased active reabsorption of Na, Cl-.

77
Q

K Sparing Distal Diuretics MOA?

A

Inhibition of Na/K exchange at aldosterone dependent sites

78
Q

Spironolactone (K sparing diuretic) MOA?

A

competes with aldosterone

79
Q

Amiloride/ Triameterene (K sparing diuretic) MOA?

A

Decreases activity of the pump directly

80
Q

Osmotic Duretics MOA?

A

Molecules filtered in the glomerulus are not reabsorbed in the tubuels and thus act on those parts of the nephron that are freely permiable to water. Water moves into the tubules following the osmotic gradient created.

81
Q

Furosemide MOA?

A

Osmotic loop diuretic

82
Q

Cardiac Glycosides (digitalis, digoxin) MOA?

A

Na/K/ATP pump inhibitors

83
Q

Phosphodiesterase inhibitors MOA?

A

Selective inhibitor of phosphodiesterase isoenzymeIII -> accumulation of cAMP -> increases cardiac contraction and peripheral vasolilation. (positive inotropic action)

84
Q

B- adrenoceptor agonist ( dubutamine) MOA?

A

agonist of beta 1 receptors in the heart .

85
Q

Aminophylilline MOA?

A

Inhibition of phophodiesterase enxyme in cardiac tissue. (bronchodilator)

86
Q

Sodium nitroprusside MOA?

A

release NO, increase NO mediated vasodilation

87
Q

Hydralazine and Minoxidil MOA?

A

Influences K ion influx -> arterial vasodilation

88
Q

Prazosin MOA?

A

A1 antagonist (inhibits vasoconstriction)

89
Q

Nitroglycerin MOA?

A

release NO, increase NO mediated vasodilation

90
Q

Isoxsuprine MOA?

A

B2 antagonist

91
Q

Ca channel blockers (amlodipine) MOA?

A

Inhibits Ca channels -> decrease in sm. Mm. tone

92
Q

Class 1 anti-arrhythmic agents MOA?

A

Membrane stabilizers via blockade of voltage gated Na channels ( decreases Na+ influx during 0 phase)

93
Q

Class II anti-arrhythmic agents MOA?

A

Beta blockers: block beta 1 receptors on the heart

94
Q

Class III anti-arrhythmic agents MOA?

A

Prolong action potential: 1. K+ channel blockade in cardiac mm. 2. weak blocker of calcium channels. 3. inhibitor of beta-adrenoceptors.

95
Q

Class IV anti-arrhythmic agents MOA?

A

Calcium channel blockers

96
Q

Acetylcysteine MOA?

A

Breaks disulphydryl bonds -> mucolytic effect

97
Q

Bromhexine/ Dembrexine MOA?

A

increase mucous production, mucus gland secretion and mucociliary clearance