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Flashcards in Drugs Deck (170):
1

HEPARIN: heparin is not absorbed through

gastrointestinal mucosa

2

HEPARIN: heparin is a naturally occurring anticoagulant released from

mast cells

3

HEPARIN: heparin binds reversibly to

antithrombin III

4

HEPARIN: antithrombin III inactivates coagulation enzymes

thrombin (factor IIa) and factor Xa

5

HEPARIN: heparin accelerates rate of inactivation of coagulation factors

thrombin (factor IIa) and factor Xa

6

HEPARIN: Heparin also prevents the conversion of ... to ...

fibrinogen to fibrin

7

HEPARIN: heparin inhibits formation of stable fibrin clot by inhibiting activation of

fibrin stabilising factor

8

TICAGRELOR: Ticagrelor is a platelet ..... inhibitor

adhesion

9

TICAGRELOR: Ticagrelor blocks .......... ........... receptors

adenosine diphosphate (ADP)

10

TICAGRELOR: Ticagrelor is an ........ antagonist as it has a different binding site to ADP

allosteric

11

TICAGRELOR: blockage of ADP receptors is ....

reversible

12

TICAGRELOR: ticagrelor does not require ..... activation

hepatic

13

TICAGRELOR: 5 side effects include

nosebleeds, bruising, shortness of breath, bleeding, headache/dizziness

14

BISOPROLOL: competitive, cardioselective beta-1 adrenergic .....

antagonist

15

BISOPROLOL: prevents activation of ...... ............ receptors by adrenaline which would increase heart rate and blood pressure

beta-1 adrenergic

16

BISPROLOL: prevents release of ....

renin

17

BISOPROLOL: at higher does, bisoprolol competitively blocks ..... ......... receptors in bronchial and vascular smooth muscle vasodilation and .......

beta-2 adrenergic; bronchospasm

18

BISOPROLOL: 5 side effects

slow HR, headaches, nausea, tiredness, changes in bowel movements

19

ATORVASTATIN: competitive inhibitor of

HMG-CoA reductase

20

ATORVASTATIN: HMG-CoA reductase is involved in the rate determining step of ............ biosynthesis

cholesterol

21

ATORVASTATIN: HMG-CoA reductase catalyses HMG-CoA to .....

mevalonate

22

ATORVASTATIN: Atorvastatin acts primarily on

liver

23

ATORVASTATIN: 5 side effects

back/ joint pain, constipation, indigestion, headaches, nausea

24

ASPIRIN: 4 properties

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