Drugs Flashcards
1
Q
HEPARIN: heparin is not absorbed through
A
gastrointestinal mucosa
2
Q
HEPARIN: heparin is a naturally occurring anticoagulant released from
A
mast cells
3
Q
HEPARIN: heparin binds reversibly to
A
antithrombin III
4
Q
HEPARIN: antithrombin III inactivates coagulation enzymes
A
thrombin (factor IIa) and factor Xa
5
Q
HEPARIN: heparin accelerates rate of inactivation of coagulation factors
A
thrombin (factor IIa) and factor Xa
6
Q
HEPARIN: Heparin also prevents the conversion of … to …
A
fibrinogen to fibrin
7
Q
HEPARIN: heparin inhibits formation of stable fibrin clot by inhibiting activation of
A
fibrin stabilising factor
8
Q
TICAGRELOR: Ticagrelor is a platelet ….. inhibitor
A
adhesion
9
Q
TICAGRELOR: Ticagrelor blocks ………. ……….. receptors
A
adenosine diphosphate (ADP)
10
Q
TICAGRELOR: Ticagrelor is an …….. antagonist as it has a different binding site to ADP
A
allosteric
11
Q
TICAGRELOR: blockage of ADP receptors is ….
A
reversible
12
Q
TICAGRELOR: ticagrelor does not require ….. activation
A
hepatic
13
Q
TICAGRELOR: 5 side effects include
A
nosebleeds, bruising, shortness of breath, bleeding, headache/dizziness
14
Q
BISOPROLOL: competitive, cardioselective beta-1 adrenergic …..
A
antagonist
15
Q
BISOPROLOL: prevents activation of …… ………… receptors by adrenaline which would increase heart rate and blood pressure
A
beta-1 adrenergic
16
Q
BISPROLOL: prevents release of ….
A
renin
17
Q
BISOPROLOL: at higher does, bisoprolol competitively blocks ….. ……… receptors in bronchial and vascular smooth muscle vasodilation and …….
A
beta-2 adrenergic; bronchospasm
18
Q
BISOPROLOL: 5 side effects
A
slow HR, headaches, nausea, tiredness, changes in bowel movements
19
Q
ATORVASTATIN: competitive inhibitor of
A
HMG-CoA reductase
20
Q
ATORVASTATIN: HMG-CoA reductase is involved in the rate determining step of ………… biosynthesis
A
cholesterol
21
Q
ATORVASTATIN: HMG-CoA reductase catalyses HMG-CoA to …..
A
mevalonate
22
Q
ATORVASTATIN: Atorvastatin acts primarily on
A
liver
23
Q
ATORVASTATIN: 5 side effects
A
back/ joint pain, constipation, indigestion, headaches, nausea
24
Q
ASPIRIN: 4 properties
A
analgesic, antipyretic, antirheumatic, anti-inflammatory
25
ASPIRIN: analgesic, antipyretic, antirheumatic and anti-inflammatory by inhibiting synthesis and release of
prostaglandins
26
ASPIRIN: antipyretic because of inhibiting synthesis and release of prostaglandins and due to action on hypothalamus to produce ....
vasodilation
27
ASPIRIN: inhibits which two enzymes directly and irreversibly to decrease formation precursors of prostaglandins and .......
COX1 and COX2, thromboxanes
28
ASPIRIN: different to other NSAIDS as is
irreversible
29
ASPIRIN: has greater effect on which enzyme
COX1
30
ASPIRIN: inhibits production of thromboxane leads to .......... ............. inhibiting effect
platelet aggregation
31
ASPIRIN: irreversibly inhibits ....., modifies activity of .....
COX1, COX2
32
ASPIRIN: low dose, long term irreversibly blocks formation of thromboxane ..... (platelets) which has inhibitory effect on .......... .......... and therefore reduces chance of MI
A2, platelet aggregation
33
ASPIRIN: 5 side effects
indigestion, nausea, tinnitus, gastrointestinal bleeding, bruising
34
AMPLODIPINE: long-acting .... .... ........ blocker
calcium ion channel
35
AMPLODIPINE: decreased ..... ..... ..... contractility
arterial smooth muscle
36
AMPLODIPINE: inhibits calcium ion influx through .... ..... calcium channels by stabilising channels in .... .....
L-type; inactive form
37
AMPLODIPINE: normally calcium ions bind to ..... which activates myosin .... ..... ..... which catalyses to myosin
calmodulin; light chain kinase
38
AMPLODIPINE: inhibits vascular smooth muscle .... ...... ... ..... which causes a cellular pH increase
carbonic anhydrase I activity
39
AMPLODIPINE: 5 side effects:
peripheral oedema, fatigue, dizziness, nausea, dyspepsia
40
CHLORTHALIDONE: ......-like diuretic
thiazide-like
41
CHLORTHALIDONE: different from other thiazide-likes as ...... ..... ..... incorporated into structure
double ring system
42
CHLORTHALIDONE: inhibits ..... ...... transport across .... ..... ..... in ...... limb of loop of Henle
sodium ion; renal tubular epithelium; ascending
43
CHLORTHALIDONE: increases sodium ion delivery to .... renal tubule
distal
44
CHLORTHALIDONE: indirectly increases ...... ion excretion via sodium/ potassium ion exchange mechanism
potassium ion
45
CHLORTHALIDONE: vasodilatory effect due to inhibiting of vascular ..... ...... activity and vascular ion channels
carbonic anhydrase
46
Which is the only diuretic currently recommended by NICE?
chlorthalidone
47
CHLORTHALIDONE: 5 side effects:
weakness, diarrhoea, chest/abdominal pain, blood in urine/stools, fever
48
CANDESARTAN: ..... receptor blocker
angiotensin
49
CANDESARTAN: antagonises which system?
renin-angiotensin-aldosterone
50
CANDESARTAN: competes with ............. for binding to ....... angiotensin II receptor (AT1 subtype) and prevents BP increase
angiotensin II; type 1
51
CANDESARTAN: AT1 is a _-_____ coupled receptor which mediates the ..................... and .............. ............. effects of angiotensin II
G-protein; vasoconstrictive and aldosterone secreting
52
CANDESARTAN: has no ... ..... side effect
dry cough
53
CANDESARTAN: inhibition of aldosterone secretion may increase ... and .... excretion and decrease .... excretion
sodium ion and water; potassium ion
54
CANDESARTAN: 5 side effects:
dizziness, headache, chest infection, hyperkalaemia, decreased kidney function
55
ACE breaks down ...... (vasodilator)
bradykinin
56
bradykinin accumulation in upper respiratory tract/lung leads to release of
prostaglandins
57
the accumulation of bradykinin and consequent release of prostaglandins striggers stimulation of .... .... ..... > nociception > cough
vagal C fibres
58
FUROSEMIDE: potent loop ...... > inhibits water reabsorption in nephron
diuretic
59
FUROSEMIDE: blocks ...................... (NKCC2) in ...... limb of loop of Henle
sodium-potassium-chloride cotransporter; ascending
60
FUROSEMIDE: blocks sodium-potassium-chloride cotransporter by ............. inhibition of .......... binding site
competitive; chloride
61
FUROSEMIDE: prevents transport of .... from loop of Henle lumen to basolateral ...... making lumen ...... which lowers the osmotic gradient
sodium ion; interstitium; hypertonic
62
FUROSEMIDE: 4 side effects
diarrhoea, urticaria, vomiting, pancreatitis
63
GLYCERYL TRINITRATE: Vasodilator used in treatment of ..... ...., congestive heart failure associated with .... and perioperative hypertension
angina pectoris; MI
64
GLYCERYL TRINITRATE: (1) glyceryl trinitrate converted to ....
NO
65
GLYCERYL TRINITRATE: (2) NO activates guanylate cyclase which promotes synthesis of...
cGMP
66
GLYCERYL TRINITRATE: (3) cGMP activates series of protein kinase dependent phosphorylations in ....... ...... cells
smooth muscle
67
GLYCERYL TRINITRATE: (4) phosphorylations in smooth muscle cells > dephosphorylation of myosin-light chains > release of ...
calcium ions
68
GLYCERYL TRINITRATE: (5) release of calcium ions triggers smooth muscle .... and .....
relaxation and vasodilation
69
GLYCERYL TRINITRATE: side effects (4)
headache, dizziness, drowsiness, faster HR
70
DIGOXIN: positive ..... effects and negative .... effects
inotropic; chronotropic
71
DIGOXIN: controls .... contraction in atrial fibrillation and is involved in the management of congestive heart failure
ventricular
72
DIGOXIN: cardiac .....
glycoside
73
DIGOXIN: (1) inhibits ............ > increase in intracellular sodium ion concentration
sodium-potassium-ATPase membrane pump
74
DIGOXIN: (2) increase in intracellular sodium ion concentration > .... .... .... (NCX) tried to counter > influx of ..... > increased contraction
sodium-calcium exchanger; calcium ions
75
DIGOXIN: increases slop of .... ... ..... > shortens action potential duration > decreases maximal diastolic potential
stage 4 depolarisation
76
DIGOXIN: 5 side effects
diarrhoea, dizziness, vomiting, blurred vision, urticaria
77
CARVEDILOL: non-selective
beta-blocker
78
CARVEDILOL: used in the treatment of (2)
heart failure, hypertension
79
CARVEDILOL: blocks ... ... and .... ...... receptors
beta1, beta2 and alpha1 adrenergic
80
CARVEDILOL: beta1 and beta2 blockage prevents binding of ..... and ..... > negative .... and ..... effects > decrease of BP
adrenaline and noradrenaline; inotropic and chronotropic
81
CARVEDILOL: blocks binding of ...... to alpha1 adrenoceptors of blood vessels > prevents .... > decrease BP
adrenaline; vasoconstriction
82
CARVEDILOL: 5 side effects
dizziness, fatigue, hypotension, diarrhoea, bradycardia
83
RAMIPRIL: ACE inhibitor (competitive). ramipril metabolised to ..... by liver (and kidneys)
ramiprilat
84
RAMIPRIL: involved in the treatment of (4)
hypertension, congestive heart failure, MI, stroke
85
RAMIPRIL: inactive ....
prodrug
86
RAMIPRIL: inhibits rapid conversion AT1>AT2 which reduces renin> angiotensin > aldosterone which ..... BP
increases
87
RAMIPRIL: inhibits deactivation of ...... (vasodilator) which maintains .... and decreased BP
bradykinin; vasodilation
88
RAMIPRIL: 5 side effects
bronchitis, chest pain, headache, diarrhoea, indigestion
89
WARFARIN: Type of coumarin. Prevents blood clots forming and .....
migrating
90
WARFARIN: Able to cross .... barrier
placental
91
WARFARIN: Inhibits .......-dependent synthesis of clotting factors
Vitamin-K
92
WARFARIN: Mixture of .... isomers
2
93
WARFARIN: Inhibits ........... > depletion of reduced form vitamin K (vitamin KH2)
vitamin K reductase
94
WARFARIN: Inhibits synthesis of vitamin K dependent coagulation factors (4) and anticoagulant proteins (2)
II, VII, IX, X; C and S
95
WARFARIN: depression of coagulation factors II, VII and X > decreased ..... levels > decreased ..... generated and bound to fibrin
prothrombin; thrombin
96
WARFARIN: 5 side effects
haemorrhage, haemoptysis (coughing up of blood), bruising, bleeding from nose/gums, blood in urine or stools
97
WARFARIN: drug which may decrease warfarin metabolism = ....... because NSAIDs interact with ........
ibuprofen, coumarins
98
WARFARIN (INR): measures how well ..... is working
warfarin
99
WARFARIN (INR): if INR too high > blood clotting is ...... > bruising and increased bleeding risk
slow
100
WARFARIN (INR): if INR too low > blood clots could ......
still form
101
WARFARIN (INR): measures how ..... blood clots
quickly
102
WARFARIN (INR): testing INR requires blood sample and a chemical (2) which allows blood to clot (Prothrombin > thrombin = ...... time) > compared with normal person to give INR
sodium citrate and calcium; prothrombin
103
WARFARIN (INR): normal INR (not taking warfarin) =
0.8-1.2
104
WARFARIN (INR): normal INR (warfarin users) =
2.5-3.5
105
LIDOCAINE: works mainly on .... receptors
pain
106
stays in local area due to .... causing .....
adrenaline; vasoconstriction
107
LIDOCAINE: 5 side effects:
red/warm skin, itching, swelling at site of application, small red/purple dots on skin, bruising
108
LIDOCAINE: blocks fast voltage gated ... channels preventing .... of postsynaptic neuron
sodium ion; depolarisation
109
CEFUROXIME: broad spectrum .... antibiotic
cephalosporin
110
CEFUROXIME: resistant to
beta-lactamase
111
CEFUROXIME: used in treatment of
bacterial infections
112
CEFUROXIME: interferes with ..... synthesis of wall by inhibiting final ..... needed for cross links
peptidoglycan; transpeptidation
113
CEFUROXIME: bactericidal or bacteriostatic?
bactercidal
114
CEFUROXIME: 5 side effects
diarrhoea, fever, headache, sweating, itching
115
CLARITHROMYCIN: semi-synthetic ..... antibiotic
macrolide
116
CEFUROXIME: broad spectrum .... antibiotic
cephalosporin
117
CEFUROXIME: resistant to
beta-lactamase
118
CEFUROXIME: used in treatment of
bacterial infections
119
CEFUROXIME: interferes with ..... synthesis of wall by inhibiting final ..... needed for cross links
peptidoglycan; transpeptidation
120
CEFUROXIME: bactericidal or bacteriostatic?
bactercidal
121
CEFUROXIME: 5 side effects
diarrhoea, fever, headache, sweating, itching
122
CLARITHROMYCIN: semi-synthetic ..... antibiotic
macrolide
123
CLARITHROMYCIN: inhibits bacterial protein synthesis by binding to bacterial ...... ribosomal subunit > inhibits ......... activity and interferes with amino acid translocation
50S; peptidyl transferase
124
CLARITHROMYCIN: bactericidal or bacteriostatic?
either, depends on organism and drug concentration, but usually BACTERIOSTATIC
125
CLARITHROMYCIN: 5 side effects
headaches, nausea, sweating, fever, diarrhoea
126
Inhaled corticosteroids deposition into lung %
10-25%
127
BECLOMETHASONE: unbound corticosteroids cross cell membrane and bind with high affinity to specific cytoplasmic receptors > 4 effects
inhibit leukocyte infiltration at inflammation site; interference in function of inflammatory response mediators; suppress humoral immune response; reduce oedema/scar tissue
128
BECLOMETHASONE: anti-inflammatory actions involve (2)
lipocortins > prostaglandins and leukotrienes; phospholipase A2 inhibitory proteins
129
BECLOMETHASONE: 4 side effects
headaches, pharyngitis, difficulty speaking, Cushing's (long term)
130
Propanolol = antagonist of
salbutamol
131
Propanolol competes with catecholamines for ..... adrenergic receptors in heart > inhibits ...... stimulation
beta1; sympathetic
132
SALBUTAMOL: ........ adrenergic .....
beta2; agonist
133
SALBUTAMOL: increases ..... production by activating adenylate cyclase > increased activity of ........ `
cAMP; protein kinase A
134
SALBUTAMOL: inhibits phosphorylation of ..... and lowers intracellular calcium concentration > broncho.....
myosin; dilation
135
SALBUTAMOL: 3 other effects of salbutamol
enhances mucociliary clearance, inhibits microvascular leakage, inhibits release of bronchoconstricting agents from mast cells
136
SALBUTAMOL: 3 side effects
tachycardia, headaches, TREMORS
137
BETA2 ADRENOCEPTOR AGONISTS (1) Activation of beta2 adrenoceptors is via ....... coupled receptor
G-protein
138
synthetic beta2 agonists and ...... bind to beta2 adrenceptors
noradrenaline
139
BETA2 ADRENOCEPTOR AGONISTS (2) alpha subunit of G-protein activates ........ > catalyses production of cAMP
adenylyl cyclase
140
BETA2 ADRENOCEPTOR AGONISTS (3) in lung, cAMP causes decrease in intracellular ..... concentration
calcium
141
BETA2 ADRENOCEPTOR AGONISTS (4) decrease in intracellular calcium activates ..... which inactivates myosin light chain ..... and activates myosin light chain ....
protein kinase A; kinase; phosphatase
142
BETA2 ADRENOCEPTOR AGONISTS 3 methods of smooth muscle relaxation and bronchodilation
decreased intracellular calcium, increased membrane potassium conductance, decreased myosin light chain kinase activity
143
THEOPHYLLINE: ....... inhibitor
phosphodiesterase
144
THEOPHYLLINE: cAMP activates protein ..... > protein phosphorylation > muscle relaxation
kinase A
145
Theophylline is used with steroid when
response to beta2 agonist is inadequate
146
THEOPHYLLINE: 5 side effects
tremor, stimulate heart, nausea, anorexia, sleep disturbances
147
MUSCARINIC RECEPTOR ANTAGONISTS: main drug used =
ipratropium
148
MUSCARINIC RECEPTOR ANTAGONISTS: used when beta2 agonist and .... insufficient
steroid
149
MUSCARINIC RECEPTOR ANTAGONISTS: blocks action of endogenous ..... at muscarinic receptors
acetylcholine
150
MUSCARINIC RECEPTOR ANTAGONISTS: low levels of acetylcholine released from cholinergic nerves in airways > few muscarinic receptors activated > smooth muscle ...
relaxed
151
LEUKOTRIENE RECEPTOR ANTAGONISTS: prevents which 2 types of asthma
exercise induced and aspirin allergic
152
LEUKOTRIENE RECEPTOR ANTAGONISTS: acts at ..... leukotriene receptors and prevents actions of LTC4 and LTD4 whch are bronchial .... and stimulants of mucus secretion
cysteinyl; spasmogens
153
LEUKOTRIENE RECEPTOR ANTAGONISTS: 2 unwanted side effects
headache, GI disturbance
154
glucocorticoids reduce production of (3)
cytokines, spasmogens, leukocyte chemotaxins
155
glucocorticoids bind to ..... receptors (GRalpha and GRbeta) > alter gene transcription
intracellular
156
cromoglicate =
mast cell stabiliser
157
OMALIZUMAB: binds to .... and inhibits binding of IgE to receptor (FcRI) on mast cells and .... > inhibits IgE asthma cascade
IgE; basophils
158
OMALIZUMAB: 2 side effects
anaphylaxis; malignancies
159
AGONIST stabilises receptor in
active form
160
more receptors end up in ... form when agonist present
active
161
ANTAGONIST binds with ...... to receptors in active and inactive states
equal affinity
162
ANTAGONIST stabilises receptors in .... state
inactive
163
ANTAGONIST preserves ..... between states
original drug free equilibrium
164
PARTIAL AGONIST has a .... maximum response than agonist
lower
165
PARTIAL AGONIST binds more tightly to .... form but still has appreciable affinity for ... form
active; inactive
166
INVERSE AGONIST binds more tightly to .... form of receptor
inactive
167
INVERSE AGONIST measurable spontaneous activity of receptors will ... in presence of inverse agonist
decrease
168
when inverse agonist present, receptors end up almost entirely in .... state
inactive
169
VARENICLINE: nicotine receptor ....... of alpha4 and beta2 subtype
partial agonist
170
VARENICLINE: .... inhibits binding of nicotine
competitively
