Pharm II MOAs Flashcards
1
Q
Sulfonamide MOA?
A
PABA agonist inhibiting folic acid synthesis
2
Q
Diaminopyrimidines MOA?
A
Folic acid inhibitor. Reversibly binds and inhibits dihydrofolate reducatase enzyme.
3
Q
Sulfonamides and Diaminopyrimidines are static or cidal?
A
Static
4
Q
Beta-Lactam MOA?
A
Inhibits bacterial cell wall synthesis via transpeptidase enzyme inhibition
5
Q
Beta-lactam resistance achieved by?
A
- Production of b-lactamase enzyme. 2. Permeability of cell wall decreased (gram -). 3. Reduced sensitivity of penicillin binding protein.
6
Q
30S ribosomal subunit protein synthesis inhibitors?
A
Aminoglycosides, Tetracyclines
7
Q
50s Ribosomal subunit protein synthesis inhibitors?
A
- Macrolides, 2. Lincosamides, 3. Chloramphenicol derivatives
8
Q
All protein synthesis inhibitors are bacteriostatic except?
A
Aminoglycosides
9
Q
MOA of Flouroquinolones and Metronidazole MOA?
A
DNA inhibitors
10
Q
MOA of Rifampin
A
RNA inhibitor
11
Q
MOA of Bacitracin
A
Inhibits peptidoglican synthesis in bacteria by non-specifically blocking phosphorylase reactions
12
Q
MOA of Nitrofurans
A
Inhibits energy production
13
Q
MOA of Virginamycin
A
Protein synthesis inhibitor via 23S ribosomal subunit
14
Q
Antimicrobials interfering with cell membrane?
A
Polymyxin B, Colistin (poly E)
15
Q
MOA Benzimidazoles?
A
Irreversibly binds to nematodal tubulin, specifically beta-tubulin
16
Q
Levamisole MOA?
A
Ganlionic stimulant and direct cholinergic drug. Causes paralysis. Can also act as an immune stimulant at low intermittent dosage.
17
Q
Depolarizing neuromuscular blocking agents?
A
Pyrantel, Morantel, Epsiprantel
18
Q
Organophosphate compounds MOA?
A
Irreversible inhibition of acetylcholinesterase
19
Q
Macrocyclic Lactones MOA?
A
- 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.
20
Q
Praziquantel MOA?
A
Ca2+ ion flux across surface membranes of exposed parasite-> paralysis, surface swellings, lesions -> lyse
21
Q
Rafoxanide / Closantel MOA?
A
ATP production inhibition.
22
Q
Clorsulon MOA
A
Affects glycolytic enzymes and deprives the fluke of its main source of metabolic energy
23
Q
Nitromidazole / Nitrofurans MOA?
A
Nitro group is cleaved off -> produces unstable intermediates -> DNA destruction
24
Q
Polyether ionophor MOA?
A
Lipophilic complexes with alkali metals -> change membrane integrity/ internal osmolality
25
Arsenieals MOA?
Binds to disulphide bridges inhibiting enzyme systems
26
Thiamine analog MOA?
Analogue of thiamine -> inhibition of active thiamine transport to protozoa
27
Thiazine derivatives MOA?
Act on apicoplasts
28
Organophosphates MOA
Irreversible inhibition of Ache
29
Carbomates MOA?
Reversible inhibition of Ache
30
Pyrethrins/Pyrethroids MOA?
Interacts with Na channels in membrane
31
Fipronil MOA
GABA and Glutamate Cl ion channel blockers
32
Imidacloprid MOA?
Competitive inhibition of post=synaptic nicotiic receptor (nAChe)
33
Amitraz MOA?
Inhibition of monoamino exidase
34
IGRs and IDIs MOA?
Mimic juvenile hormone resp. inhibition of chitin synthesis
35
Where do anti-fungals act?
Wall, Membrane, intracellular
36
Intracellular anti-fungals and their MOAs?
Flucytosine - pyrimidine analogue: DNA synthesis interference via thymidylate synthesis. Griseofulvin - Mitotic inhibitor: Interferes with mitosis by binding to microtubules
37
Wall anti-fungal and MOAs?
Echinocandins - Inhibits fungal beta glucan synthesis -> exposure of antigens -> host immune response
38
Anti-fungal acting on cell membrane and MOA? (hint: ergosterol)
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
39
Nucleoside Reverse Transcriptase Inhibitors MOA?
(Retrovirus) Causes viral DNA chain termination via phosphorylation of host enzyme -> competition for proviral DNA synthesis
40
Viral DNA Polymerase Inhibitors MOA?
(DNA virus) Inhibits viral DNA polymerase via viral thymidine kinase. Only affects infected cells
41
M2-Ion Channel Inhibitors MOA?
(RNA virus) Inhibits RNA/ viral release via H+ influx -> acidification of endosome
42
Neuramidase/ Sialidase inhibitors MOA?
(RNA virus) Inhibits Neuramidase/ sialidase -> affects viral shedding
43
Ribavirin MOA?
(DNA and RNA virus) Inhibits viral replication at multiple sites
44
Interferons MOA?
(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
Alkylating Agents MOA?
Form covalent bonds with DNA -> prevention of replication and transcription
46
Antimetabolites MOA?
Block metabolic bathways of DNA synthesis.
47
Cytotoxic Antibiotics MOA?
Blocks mammalian cell division via interaction with DNA
48
MOA of Doxorubicin and anthracyclines?
Inhibits DNA by interfereing with RNA polymerase and topoisomerase II
49
MOA of Dactinomycin?
Intercalates in DNA interfering with RNA polymerase and popoisomerase II
50
MOA of Bleomycin?
Fragmentation of DNA chains (acts on non-deviding cells)
51
MOA Mitomycin ?
Activated to give an alkylating metabolite
52
Plant Derivatives MOA?
Inhibits microtubules/ mitosis
53
Vinca Alkaloid MOA?
Inhibit microtubule polymerisation -> arrests in metaphase = no spindle formation or division.
54
Taxanes
Stabilize microtubules in polymerized state
55
Tyrosine Kinase Inhibitors MOA?
Inhibits tyrosine kinase -> prevent downstream growth signaling.
56
Cancer vaccine MOA? (BCG)
Stim immune response to recognize tumor cells
57
Anticancer Vaccine MOA? (L-Asparanginase)
catalyzes hydrolysis (à l-aspartic acid + ammonia) à ↓protein synthesis
58
Monoclonal Antibodies MOA
Specific for certain cancer receptors
59
Dirlotapide MOA?
Selectively inhibits microsomal triglyceride protein transfer-> blocking fat absorption
60
Omeprazole MOA?
Inhibition of proton pump
61
Ranatadine MOA?
Competitive inhibition of secretion of PCT -> increased serum levels
62
PGE analog (misoprostal) MOA?
Inhibits acids, increases mucous production, stabilizes mast cells
63
Sucrafate MOA?
in acidic environment, sucrose released and polymerizes over uclders forming a protective barrier
64
Bismuth Subsaliciate MOA?
Bismuth- Absorbs E. coli enterotoxin. Subsaliciate - decreases excess secretions
65
Chalogogues MOA? (Mg Sulfate)
contract Gall bladder
66
Cholerectics (Glycocholate, Taurocholate, UDCA) MOA?
increase bile secretion
67
Eulsifying agents (dimethicone, poloxalene) MOA?
Reduces frothy bloat
68
Clenbuterol MOA?
B2 agonist = relaxes the bladder
69
Phenoxybenzamine MOA?
A agonist = contraction of urethra
70
Prazosine MOA?
A1 antagonist = relax hypertonic urethra
71
Diazepam MOA?
GABA agonist (central)
72
Dantrolene MOA?
Sk. Mm. Relaxant
73
Probenidice/ Sulphinpyrazone MOA?
competitive inhibition of ACID active secretion (TCT) -> increase in circulation
74
Carboanhydrase Inhibitors MOA?
Increase secretion of bicarb, Na, K, and water by inhibiting carbonic anhydrase.
75
Loop Diuretics MOA?
Inhibit Na/K/Cl- carrier -> formation of osmotic gradient.
76
Thiazine Diuretics (Chlorothiazide, Hydrochlorothiazide) MOA?
Binds to the Cl- site of the Na/Cl- symport system. (slide 20 diagram is wrong) -> decreased active reabsorption of Na, Cl-.
77
K Sparing Distal Diuretics MOA?
Inhibition of Na/K exchange at aldosterone dependent sites
78
Spironolactone (K sparing diuretic) MOA?
competes with aldosterone
79
Amiloride/ Triameterene (K sparing diuretic) MOA?
Decreases activity of the pump directly
80
Osmotic Duretics MOA?
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
Furosemide MOA?
Osmotic loop diuretic
82
Cardiac Glycosides (digitalis, digoxin) MOA?
Na/K/ATP pump inhibitors
83
Phosphodiesterase inhibitors MOA?
Selective inhibitor of phosphodiesterase isoenzymeIII -> accumulation of cAMP -> increases cardiac contraction and peripheral vasolilation. (positive inotropic action)
84
B- adrenoceptor agonist ( dubutamine) MOA?
agonist of beta 1 receptors in the heart .
85
Aminophylilline MOA?
Inhibition of phophodiesterase enxyme in cardiac tissue. (bronchodilator)
86
Sodium nitroprusside MOA?
release NO, increase NO mediated vasodilation
87
Hydralazine and Minoxidil MOA?
Influences K ion influx -> arterial vasodilation
88
Prazosin MOA?
A1 antagonist (inhibits vasoconstriction)
89
Nitroglycerin MOA?
release NO, increase NO mediated vasodilation
90
Isoxsuprine MOA?
B2 antagonist
91
Ca channel blockers (amlodipine) MOA?
Inhibits Ca channels -> decrease in sm. Mm. tone
92
Class 1 anti-arrhythmic agents MOA?
Membrane stabilizers via blockade of voltage gated Na channels ( decreases Na+ influx during 0 phase)
93
Class II anti-arrhythmic agents MOA?
Beta blockers: block beta 1 receptors on the heart
94
Class III anti-arrhythmic agents MOA?
Prolong action potential: 1. K+ channel blockade in cardiac mm. 2. weak blocker of calcium channels. 3. inhibitor of beta-adrenoceptors.
95
Class IV anti-arrhythmic agents MOA?
Calcium channel blockers
96
Acetylcysteine MOA?
Breaks disulphydryl bonds -> mucolytic effect
97
Bromhexine/ Dembrexine MOA?
increase mucous production, mucus gland secretion and mucociliary clearance
