FINAL 01 - Drugs Affecting the Cardiovascular System Flashcards
1
Q
Mannitol, sorbitol, isosorbide, glycerin, and urea are examples of __________ (Types of diuretics)
A
Osmotic diuretics
2
Q
Enzyme that catalyzes the formation of carbonic acid (H2CO3) from carbon dioxide and water
A
Carbonic anhydrase
3
Q
Works by inhibiting carbonic anhydrase (Types of diuretics)
A
Carbonic anhydrase inhibitors
4
Q
Contains a benzothiadiazine 1,1-dioxide nucleus (Types of diuretics)
A
Thiazide diuretics
5
Q
A structurally diverse group of sulfonamide derivatives that do not contain benzothiadiazine rings (Types of diuretics)
A
Thiazide-like diuretics
6
Q
Metolazone is a type of __________ (Thiazide-like diuretics)
A
Quinazolinone derivatives
7
Q
Chlorthalidone is a type of ___________ (Thiazide-like diuretics)
A
Phthalimidine derivatives
8
Q
Indapamide is a type of ___________ (Thiazide-like diuretics)
A
Indolines
9
Q
Furosemide and bumetanide are examples of __________ (Loop diuretics)
A
Sulfonamide
10
Q
Torsemide is an example of __________ (Loop diuretics)
A
Sulfonylurea
11
Q
Ethacrynic acid is an example of ___________ (Loop diuretics)
A
Phenoxyacetic acid derivative
12
Q
Useful in patients who are allergic to sulfonamides (Loop diuretics)
A
Ethacrynic acid
13
Q
Spironolactone and eplerenone are examples of ___________ (Potassium-sparing diuretics)
A
Aldosterone antagonists
14
Q
Triamterene and amiloride are examples of __________ (Potassium-sparing diuretics)
A
ENaC blockers
15
Q
Triamterene is an example of __________ (Potassium-sparing diuretics)
A
Pteridine
16
Q
Amiloride is an example of __________ (Potassium-sparing diuretics)
A
Aminopyrazine
17
Q
__________ are examples of positive inotropic drugs
A
Cardiac glycosides
18
Q
2 portions of cardiac glycosides (GA)
A
Glycone, Aglycone
19
Q
Derived from plant origin; possesses a 5-membered, beta-saturated lactone ring (Types of cardiac glycosides)
A
Cardenolides
20
Q
Derived from animal origin; possesses a 6-membered lactone ring with 2 conjugated double bonds (Types of cardiac glycosides)
A
Bufadienolides
21
Q
From Digitalis purpurea; lipid soluble, shorter t1/2 (Examples of cardiac glycosides)
A
Digitoxin
22
Q
From Digitalis lanata; water soluble, shorter t1/2 (Examples of cardiac glycosides)
A
Digoxin
23
Q
Strophanthus gratus is the source of ___________ (toxic form) (Examples of cardiac glycosides)
A
G-strophanthin (Ouabain)
24
Q
Strophanthus kombe is the source of ___________ (less toxic form) (Examples of cardiac glycosides)
A
K-strophanthin
25
Example of adrenergic, non-glycosidic positive inotropic agent
Dobutamine
26
Example of dopaminergic agonist, non-glycosidic positive inotropic agent
Dopamine
27
2 examples of PDE3 inhibiting, non-glycosidic positive inotropic agent (AM)
Amrinone, Milrinone
28
Ambrisentan, bosentan, and sitaxsentan are examples of ___________; they are only indicated for pulmonary hypertension
Endothelin receptor antagonists
29
Reserpine, guanethidine, and guanadrel are examples of ___________
Adrenergic neuron blocking agent
30
Blocks vesicular amine transporter in noradrenergic nerves and depletes transmitter stores (Examples of adrenergic neuron blocking agents)
Reserpine
31
Interferes with amine release and replaces norepinephrine in vesicles (Examples of adrenergic neuron blocking agents) (GG)
Guanethidine, Guanadrel
32
Prazosin, terazosin, and doxazosin are examples of __________
α1 Adrenergic blockers
33
On conversion to α-methylnorepinephrine, it acts on α2 adrenergic receptors to inhibit the release of norepinephrine (Centrally acting adrenergic drugs)
Methyldopa
34
Clonidine, guanabenz, and guanfacine are examples of ___________ (Centrally acting adrenergic drugs)
α2 Adrenergic agonists
35
Are aryloxypropanolamines (β-adrenergic blockers)
Non-selective β-blockers (1st generation)
36
Has a presence of para-substituents on the aromatic ring and the absence of meta-substituents (β-adrenergic blockers)
β1-selective blockers (2nd generation)
37
The arylalkyl group with nearby methyl group in these molecules is responsible for its α1-blocking activity (β-adrenergic blockers)
β-blockers with α1-antagonist activity (3rd generation)
38
Hydralazine and Na nitroprusside ___________ (Examples of vasodilatory drugs)
Releases nitric oxide
39
Diazoxide and minoxidil are ___________ (Examples of vasodilatory drugs)
Potassium channel openers
40
Sildenafil, vardenafil, and tadalafil are examples of __________; they are used in the treatment of erectile dysfunction (Examples of vasodilatory drugs)
PDE-5 inhibitors
41
2 main classes of calcium channel blockers (DN)
Dihydropyridines, Non-dihydropyridines
42
Disopyramide, quinidine, and procainamide are examples of __________ antiarrhythmic drugs
Class IA
43
Lidocaine, mexiletine, tocainide, and phenytoin are examples of ___________ antiarrhythmic drugs
Class IB
44
Moricizine, flecainide, propafenone, and encainide are examples of ___________ antiarrhythmic drugs
Class IC
45
Propranolol and esmolol are examples of ___________ antiarrhythmic drugs
Class II
46
Sotalol, amiodarone, and bretylium tosylate are examples of ___________ antiarrhythmic drugs
Class III
47
The N-ring must contain a __________ to mimic the C-terminal carboxylate of ACE substrates (SAR of ACE inhibitors)
Carboxylic acid
48
Large hydrophobic heterocyclic rings ___________ potency and alter pharmacokinetic parameters (SAR of ACE inhibitors)
Increases
49
The zinc-binding groups can be either __________, ____________, or a ___________ (SAR of ACE inhibitors) (SCP)
Sulfhydryl, Carboxylic acid, Phosphinic acid
50
The ___________ group shows superior binding to zinc (SAR of ACE inhibitors)
Sulfyhydryl
51
Sulfhydryl-containing compounds produce ___________ incidence of skin rash and taste disturbances (SAR of ACE inhibitors)
High
52
Sulfhydryl-containing compounds can form dimers and disulfides, which may __________ duration of action (SAR of ACE inhibitors)
Shorten
53
Compounds that bind to zinc through either a carboxylate or phosphinate mimic the peptide hydrolysis transition state and ___________ binding (SAR of ACE inhibitors)
Enhance
54
__________ of the carboxylate or phosphinate produces an orally bioavailable prodrug (SAR of ACE inhibitors)
Esterification
55
X is usually ____________ to mimic the side chain of alanine (SAR of ACE inhibitors)
Methyl
56
Within the dicarboxylate series, when X equals ___________, this produces a compound that does not require prodrug for oral activity (SAR of ACE inhibitors)
N-butylamine
57
All ACE inhibitors are prodrugs except __________ and __________ (CL)
Captopril, Lisinopril
58
An acidic group (___________, ____________, or ___________) is thought to mimic either the Tyr4 phenol or the Asp1 carboxylate of angiotensin II (SAR of ARBs) (CPP)
Carboxylic acid, Phenyl tetrazole, Phenyl carboxylate
59
In the biphenyl series, the tetrazole and carboxylate groups must be in the ___________ position for optimal activity (SAR of ARBs)
Ortho
60
The __________ group is superior in terms of metabolic stability, lipophilicity, and oral bioavailability (SAR of ARBs)
Tetrazole
61
The __________ group of the model compound provides hydrophobic binding and most likely, mimics the side chain of Ile5 of angiotensin II (SAR of ARBs)
N-butyl
62
The n-butyl group can be replaced with either an ___________ or an ___________ group (SAR of ARBs) (EN)
Ethyl ether, N-propyl
63
Substitution can vary at the "__________" position (carboxylic acid, hydroxymethyl group, ketone, benzimidazole ring) (SAR of ARBs)
R
64
The first nonpeptide, low molecular weight, orally active, transition-state renin inhibitor
Aliskiren
65
Are structural analogs of HMG-CoA (Types of dyslipidemia drugs)
HMG-CoA reductase inhibitors (Statins)
66
___________ and ___________ are lactones and prodrugs, activated by hydrolysis in the liver to their respective β-hydroxy acids (Examples of statins) (LS)
Lovastatin, Simvastatin
67
Pravastatin, fluvastatin, atorvastatin, pitavastatin, and rosuvastatin are not ___________ (Examples of statins)
Prodrugs
68
Can be chemically classified as analogs of phenoxyisobutyric acid (Types of dyslipidemia drugs)
Fibrates
69
Are peroxisome proliferator activated receptor-alpha (PPAR-α) agonists (Types of dyslipidemia drugs)
Fibrates
70
The ____________ group is essential for activity (SAR of fibrates)
Isobutyric acid
71
Fibrates which contains an ____________, are prodrugs and require in vivo hydrolysis (SAR of fibrates)
Ester
72
Substitution at the ___________ position of the aromatic ring with a chloro group or a chlorine-containing cyclopropyl ring produces compounds with significantly longer half-lives (SAR of fibrates)
Para
73
Although most compounds contain a phenoxyisobutyric acid, the addition of an ____________ spacer, as seen in gemfibrozil, results in an active drug (SAR of fibrates)
N-propyl
74
Are large polymeric cationic exchange resins that are insoluble in water (Types of dyslipidemia drugs)
Bile acid-binding resins
75
They bind bile acids in the intestinal lumen and prevent their reabsorption (Types of dyslipidemia drugs)
Bile acid-binding resins
76
Inhibits lipolysis; prevents the release of FFAs and glycerol from fatty tissues (Types of dyslipidemia drugs)
Niacin/Nicotinic acid/Vitamin B3
77
Inhibit the synthesis of apoprotein A1, a major protein component of HDL (Types of dyslipidemia drugs)
Probucol
78
Has two tertiary butylphenol groups linked by a dithiopropylidene bridge, giving it a high lipophilic character with strong antioxidant properties (Types of dyslipidemia drugs)
Probucol
79
A plant sterol, whose structure is identical with that of cholesterol, expected for the substituted ethyl group on C24 of its side chain (Types of dyslipidemia drugs)
β-Sitosterol
80
Decreases cholesterol absorption in the intestine by blocking the absorption of the sterol at the Brush border (Types of dyslipidemia drugs)
Sterol absorption inhibitor (Ezetimibe)
81
The β-lactam in its structure binds to NPC1L1 protein on the GI tract that is responsible for cholesterol absorption (Types of dyslipidemia drugs)
Sterol absorption inhibitor (Ezetimibe)
82
Aspirin is a __________ (Types of antiplatelets)
COX-1 inhibitor
83
Irreversibly acetylates platelet COX-1 enzyme (Examples of COX-1 inhibitors)
Aspirin (Acetylsalicylic acid)
84
Dipyridamole and cilostazol are examples of __________ (Types of antiplatelets)
PDE-3 inhibitors
85
Dipyridamole is made of __________ (Examples of PDE-3 inhibitors)
Pyrimido pyrimidine
86
Cilostazol is made of __________ (Examples of PDE-3 inhibitors)
Quinolinone
87
__________ and __________ inhibit PDE-3 and adenosine uptake (Examples of PDE-3 inhibitors) (DC)
Dipyridamole, Cilostazol
88
Inhibit P2Y12 receptor which is an ADP receptor in platelets (Types of antiplatelets)
ADP inhibitors
89
__________ are irreversible inhibitors; examples include ticlopidine, clopidogrel, and prasugrel (Types of ADP inhibitors)
Thienopyridines
90
__________ are reversible inhibitors; examples include ticagrelor and cangrelor (Types of ADP inhibitors)
Non-thienopyridines
91
Causes blockade of platelet glycoprotein IIb/IIIa receptors (Types of antiplatelets)
GIIb/IIIa inhibitors
92
__________ is a chimeric monoclonal antibody (Examples of GIIb/IIIa inhibitors)
Abciximab
93
____________ is a cyclic peptide (Examples of GIIb/IIIa inhibitors)
Eptifibatide
94
Is peptidomimetic; a nonpeptide (Examples of GIIb/IIIa inhibitors)
Tirofiban
95
__________ and __________ are vitamin K antagonists, which inhibits vitamin K epoxide reductase (Types of anticoagulants) (CI)
Coumarin derivatives, Indandiones
96
Dicoumarol, acenocoumarol, phenprocoumon, and warfarin are examples of __________ (Examples of vitamin K antagonists)
Coumarin derivatives
97
Phenindione and anisindione are examples of __________ (Examples of vitamin K antagonists)
Indanedione
98
A heterogenous mixture of sulfonated mucopolysaccharides (Types of anticoagulants)
Heparin
99
3 types of heparin (ULS)
Unfractionated heparin, Low molecular weight heparin, Synthetic heparin derivative
100
Enoxaparin, dalteparin, and tinzaparin are examples of ___________ (Types of heparin)
Low molecular weight heparin (LMWH)
101
Fondaparinux (a pentasaccharide) is an example of __________ (Types of heparin)
Synthetic heparin derivative
102
2 types of direct thrombin inhibitors (PO)
Parenteral, Oral
103
A recombinant derivative of hirudin (Examples of parenteral direct thrombin inhibitors)
Lepirudin
104
A synthetic, 20-amino-acid polypeptide (Examples of parenteral direct thrombin inhibitors)
Bivalirudin
105
A peptidomimetic (Examples of parenteral direct thrombin inhibitors)
Argatroban
106
A non-peptidomimetic prodrug (Examples of oral direct thrombin inhibitors)
Dabigatran etexilate
107
Apixaban and rivaroxaban are examples of ___________ (Types of anticoagulants)
Oral direct factor Xa inhibitors
108
Streptokinase and urokinase are __________ fibrinolytics/thrombolytic drugs
1st generation
109
Alteplase, prourokinase, and anistreplase are examples of __________ fibrinolytics/thrombolytic drugs
2nd generation
110
Reteplase and tenecteplase are examples of __________ fibrinolytics/thrombolytic drugs
3rd generation
111
Antidote for heparin (Examples of coagulants)
Protamine sulfate
112
An arginine-rich, highly basic group of simple proteins derived from salmon sperm (Examples of coagulants)
Protamine sulfate
113
Antidote for warfarin and other vitamin K antagonists (Examples of coagulants)
Vitamin K1 (Phylloquinone, phytomenadione, or phytonadione)
114
Inhibits plasminogen activation (Examples of antifibrinolytics) (AT)
Aminocaproic acid, Tranexamic acid
115
Chemically similar to lysine (Examples of antifibrinolytics)
Aminocaproic acid
116
Analog of aminocaproic acid (Examples of antifibrinolytics)
Tranexamic acid
117
A serine protease inhibitor that blocks kallikrein and plasmin (Examples of antifibrinolytics)
Aprotinin
