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Sem 2 > Drugs > Flashcards

Drugs Flashcards

1
Q

HEPARIN: heparin is not absorbed through

A

gastrointestinal mucosa

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2
Q

HEPARIN: heparin is a naturally occurring anticoagulant released from

A

mast cells

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3
Q

HEPARIN: heparin binds reversibly to

A

antithrombin III

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4
Q

HEPARIN: antithrombin III inactivates coagulation enzymes

A

thrombin (factor IIa) and factor Xa

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5
Q

HEPARIN: heparin accelerates rate of inactivation of coagulation factors

A

thrombin (factor IIa) and factor Xa

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6
Q

HEPARIN: Heparin also prevents the conversion of … to …

A

fibrinogen to fibrin

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7
Q

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

A

fibrin stabilising factor

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8
Q

TICAGRELOR: Ticagrelor is a platelet ….. inhibitor

A

adhesion

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9
Q

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

A

adenosine diphosphate (ADP)

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10
Q

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

A

allosteric

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11
Q

TICAGRELOR: blockage of ADP receptors is ….

A

reversible

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12
Q

TICAGRELOR: ticagrelor does not require ….. activation

A

hepatic

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13
Q

TICAGRELOR: 5 side effects include

A

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

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14
Q

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

A

antagonist

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15
Q

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

A

beta-1 adrenergic

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16
Q

BISPROLOL: prevents release of ….

A

renin

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17
Q

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

A

beta-2 adrenergic; bronchospasm

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18
Q

BISOPROLOL: 5 side effects

A

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

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19
Q

ATORVASTATIN: competitive inhibitor of

A

HMG-CoA reductase

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20
Q

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

A

cholesterol

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21
Q

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

A

mevalonate

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22
Q

ATORVASTATIN: Atorvastatin acts primarily on

A

liver

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23
Q

ATORVASTATIN: 5 side effects

A

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

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24
Q

ASPIRIN: 4 properties

A

analgesic, antipyretic, antirheumatic, anti-inflammatory

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25
Q

ASPIRIN: analgesic, antipyretic, antirheumatic and anti-inflammatory by inhibiting synthesis and release of

A

prostaglandins

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26
Q

ASPIRIN: antipyretic because of inhibiting synthesis and release of prostaglandins and due to action on hypothalamus to produce ….

A

vasodilation

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27
Q

ASPIRIN: inhibits which two enzymes directly and irreversibly to decrease formation precursors of prostaglandins and …….

A

COX1 and COX2, thromboxanes

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28
Q

ASPIRIN: different to other NSAIDS as is

A

irreversible

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29
Q

ASPIRIN: has greater effect on which enzyme

A

COX1

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30
Q

ASPIRIN: inhibits production of thromboxane leads to ………. …………. inhibiting effect

A

platelet aggregation

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31
Q

ASPIRIN: irreversibly inhibits ….., modifies activity of …..

A

COX1, COX2

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32
Q

ASPIRIN: low dose, long term irreversibly blocks formation of thromboxane ….. (platelets) which has inhibitory effect on ………. ………. and therefore reduces chance of MI

A

A2, platelet aggregation

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33
Q

ASPIRIN: 5 side effects

A

indigestion, nausea, tinnitus, gastrointestinal bleeding, bruising

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34
Q

AMPLODIPINE: long-acting …. …. …….. blocker

A

calcium ion channel

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35
Q

AMPLODIPINE: decreased ….. ….. ….. contractility

A

arterial smooth muscle

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36
Q

AMPLODIPINE: inhibits calcium ion influx through …. ….. calcium channels by stabilising channels in …. …..

A

L-type; inactive form

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37
Q

AMPLODIPINE: normally calcium ions bind to ….. which activates myosin …. ….. ….. which catalyses to myosin

A

calmodulin; light chain kinase

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38
Q

AMPLODIPINE: inhibits vascular smooth muscle …. …… … ….. which causes a cellular pH increase

A

carbonic anhydrase I activity

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39
Q

AMPLODIPINE: 5 side effects:

A

peripheral oedema, fatigue, dizziness, nausea, dyspepsia

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40
Q

CHLORTHALIDONE: ……-like diuretic

A

thiazide-like

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41
Q

CHLORTHALIDONE: different from other thiazide-likes as …… ….. ….. incorporated into structure

A

double ring system

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42
Q

CHLORTHALIDONE: inhibits ….. …… transport across …. ….. ….. in …… limb of loop of Henle

A

sodium ion; renal tubular epithelium; ascending

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43
Q

CHLORTHALIDONE: increases sodium ion delivery to …. renal tubule

A

distal

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44
Q

CHLORTHALIDONE: indirectly increases …… ion excretion via sodium/ potassium ion exchange mechanism

A

potassium ion

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45
Q

CHLORTHALIDONE: vasodilatory effect due to inhibiting of vascular ….. …… activity and vascular ion channels

A

carbonic anhydrase

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46
Q

Which is the only diuretic currently recommended by NICE?

A

chlorthalidone

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47
Q

CHLORTHALIDONE: 5 side effects:

A

weakness, diarrhoea, chest/abdominal pain, blood in urine/stools, fever

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48
Q

CANDESARTAN: ….. receptor blocker

A

angiotensin

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49
Q

CANDESARTAN: antagonises which system?

A

renin-angiotensin-aldosterone

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50
Q

CANDESARTAN: competes with …………. for binding to ……. angiotensin II receptor (AT1 subtype) and prevents BP increase

A

angiotensin II; type 1

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51
Q

CANDESARTAN: AT1 is a _-_____ coupled receptor which mediates the ………………… and ………….. …………. effects of angiotensin II

A

G-protein; vasoconstrictive and aldosterone secreting

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52
Q

CANDESARTAN: has no … ….. side effect

A

dry cough

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53
Q

CANDESARTAN: inhibition of aldosterone secretion may increase … and …. excretion and decrease …. excretion

A

sodium ion and water; potassium ion

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54
Q

CANDESARTAN: 5 side effects:

A

dizziness, headache, chest infection, hyperkalaemia, decreased kidney function

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55
Q

ACE breaks down …… (vasodilator)

A

bradykinin

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56
Q

bradykinin accumulation in upper respiratory tract/lung leads to release of

A

prostaglandins

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57
Q

the accumulation of bradykinin and consequent release of prostaglandins striggers stimulation of …. …. ….. > nociception > cough

A

vagal C fibres

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58
Q

FUROSEMIDE: potent loop …… > inhibits water reabsorption in nephron

A

diuretic

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59
Q

FUROSEMIDE: blocks …………………. (NKCC2) in …… limb of loop of Henle

A

sodium-potassium-chloride cotransporter; ascending

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60
Q

FUROSEMIDE: blocks sodium-potassium-chloride cotransporter by …………. inhibition of ………. binding site

A

competitive; chloride

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61
Q

FUROSEMIDE: prevents transport of …. from loop of Henle lumen to basolateral …… making lumen …… which lowers the osmotic gradient

A

sodium ion; interstitium; hypertonic

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62
Q

FUROSEMIDE: 4 side effects

A

diarrhoea, urticaria, vomiting, pancreatitis

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63
Q

GLYCERYL TRINITRATE: Vasodilator used in treatment of ….. …., congestive heart failure associated with …. and perioperative hypertension

A

angina pectoris; MI

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64
Q

GLYCERYL TRINITRATE: (1) glyceryl trinitrate converted to ….

A

NO

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65
Q

GLYCERYL TRINITRATE: (2) NO activates guanylate cyclase which promotes synthesis of…

A

cGMP

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66
Q

GLYCERYL TRINITRATE: (3) cGMP activates series of protein kinase dependent phosphorylations in ……. …… cells

A

smooth muscle

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67
Q

GLYCERYL TRINITRATE: (4) phosphorylations in smooth muscle cells > dephosphorylation of myosin-light chains > release of …

A

calcium ions

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68
Q

GLYCERYL TRINITRATE: (5) release of calcium ions triggers smooth muscle …. and …..

A

relaxation and vasodilation

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69
Q

GLYCERYL TRINITRATE: side effects (4)

A

headache, dizziness, drowsiness, faster HR

70
Q

DIGOXIN: positive ….. effects and negative …. effects

A

inotropic; chronotropic

71
Q

DIGOXIN: controls …. contraction in atrial fibrillation and is involved in the management of congestive heart failure

A

ventricular

72
Q

DIGOXIN: cardiac …..

A

glycoside

73
Q

DIGOXIN: (1) inhibits ………… > increase in intracellular sodium ion concentration

A

sodium-potassium-ATPase membrane pump

74
Q

DIGOXIN: (2) increase in intracellular sodium ion concentration > …. …. …. (NCX) tried to counter > influx of ….. > increased contraction

A

sodium-calcium exchanger; calcium ions

75
Q

DIGOXIN: increases slop of …. … ….. > shortens action potential duration > decreases maximal diastolic potential

A

stage 4 depolarisation

76
Q

DIGOXIN: 5 side effects

A

diarrhoea, dizziness, vomiting, blurred vision, urticaria

77
Q

CARVEDILOL: non-selective

A

beta-blocker

78
Q

CARVEDILOL: used in the treatment of (2)

A

heart failure, hypertension

79
Q

CARVEDILOL: blocks … … and …. …… receptors

A

beta1, beta2 and alpha1 adrenergic

80
Q

CARVEDILOL: beta1 and beta2 blockage prevents binding of ….. and ….. > negative …. and ….. effects > decrease of BP

A

adrenaline and noradrenaline; inotropic and chronotropic

81
Q

CARVEDILOL: blocks binding of …… to alpha1 adrenoceptors of blood vessels > prevents …. > decrease BP

A

adrenaline; vasoconstriction

82
Q

CARVEDILOL: 5 side effects

A

dizziness, fatigue, hypotension, diarrhoea, bradycardia

83
Q

RAMIPRIL: ACE inhibitor (competitive). ramipril metabolised to ….. by liver (and kidneys)

A

ramiprilat

84
Q

RAMIPRIL: involved in the treatment of (4)

A

hypertension, congestive heart failure, MI, stroke

85
Q

RAMIPRIL: inactive ….

A

prodrug

86
Q

RAMIPRIL: inhibits rapid conversion AT1>AT2 which reduces renin> angiotensin > aldosterone which ….. BP

A

increases

87
Q

RAMIPRIL: inhibits deactivation of …… (vasodilator) which maintains …. and decreased BP

A

bradykinin; vasodilation

88
Q

RAMIPRIL: 5 side effects

A

bronchitis, chest pain, headache, diarrhoea, indigestion

89
Q

WARFARIN: Type of coumarin. Prevents blood clots forming and …..

A

migrating

90
Q

WARFARIN: Able to cross …. barrier

A

placental

91
Q

WARFARIN: Inhibits …….-dependent synthesis of clotting factors

A

Vitamin-K

92
Q

WARFARIN: Mixture of …. isomers

A

2

93
Q

WARFARIN: Inhibits ……….. > depletion of reduced form vitamin K (vitamin KH2)

A

vitamin K reductase

94
Q

WARFARIN: Inhibits synthesis of vitamin K dependent coagulation factors (4) and anticoagulant proteins (2)

A

II, VII, IX, X; C and S

95
Q

WARFARIN: depression of coagulation factors II, VII and X > decreased ….. levels > decreased ….. generated and bound to fibrin

A

prothrombin; thrombin

96
Q

WARFARIN: 5 side effects

A

haemorrhage, haemoptysis (coughing up of blood), bruising, bleeding from nose/gums, blood in urine or stools

97
Q

WARFARIN: drug which may decrease warfarin metabolism = ……. because NSAIDs interact with ……..

A

ibuprofen, coumarins

98
Q

WARFARIN (INR): measures how well ….. is working

A

warfarin

99
Q

WARFARIN (INR): if INR too high > blood clotting is …… > bruising and increased bleeding risk

A

slow

100
Q

WARFARIN (INR): if INR too low > blood clots could ……

A

still form

101
Q

WARFARIN (INR): measures how ….. blood clots

A

quickly

102
Q

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

A

sodium citrate and calcium; prothrombin

103
Q

WARFARIN (INR): normal INR (not taking warfarin) =

A

0.8-1.2

104
Q

WARFARIN (INR): normal INR (warfarin users) =

A

2.5-3.5

105
Q

LIDOCAINE: works mainly on …. receptors

A

pain

106
Q

stays in local area due to …. causing …..

A

adrenaline; vasoconstriction

107
Q

LIDOCAINE: 5 side effects:

A

red/warm skin, itching, swelling at site of application, small red/purple dots on skin, bruising

108
Q

LIDOCAINE: blocks fast voltage gated … channels preventing …. of postsynaptic neuron

A

sodium ion; depolarisation

109
Q

CEFUROXIME: broad spectrum …. antibiotic

A

cephalosporin

110
Q

CEFUROXIME: resistant to

A

beta-lactamase

111
Q

CEFUROXIME: used in treatment of

A

bacterial infections

112
Q

CEFUROXIME: interferes with ….. synthesis of wall by inhibiting final ….. needed for cross links

A

peptidoglycan; transpeptidation

113
Q

CEFUROXIME: bactericidal or bacteriostatic?

A

bactercidal

114
Q

CEFUROXIME: 5 side effects

A

diarrhoea, fever, headache, sweating, itching

115
Q

CLARITHROMYCIN: semi-synthetic ….. antibiotic

A

macrolide

116
Q

CEFUROXIME: broad spectrum …. antibiotic

A

cephalosporin

117
Q

CEFUROXIME: resistant to

A

beta-lactamase

118
Q

CEFUROXIME: used in treatment of

A

bacterial infections

119
Q

CEFUROXIME: interferes with ….. synthesis of wall by inhibiting final ….. needed for cross links

A

peptidoglycan; transpeptidation

120
Q

CEFUROXIME: bactericidal or bacteriostatic?

A

bactercidal

121
Q

CEFUROXIME: 5 side effects

A

diarrhoea, fever, headache, sweating, itching

122
Q

CLARITHROMYCIN: semi-synthetic ….. antibiotic

A

macrolide

123
Q

CLARITHROMYCIN: inhibits bacterial protein synthesis by binding to bacterial …… ribosomal subunit > inhibits ……… activity and interferes with amino acid translocation

A

50S; peptidyl transferase

124
Q

CLARITHROMYCIN: bactericidal or bacteriostatic?

A

either, depends on organism and drug concentration, but usually BACTERIOSTATIC

125
Q

CLARITHROMYCIN: 5 side effects

A

headaches, nausea, sweating, fever, diarrhoea

126
Q

Inhaled corticosteroids deposition into lung %

A

10-25%

127
Q

BECLOMETHASONE: unbound corticosteroids cross cell membrane and bind with high affinity to specific cytoplasmic receptors > 4 effects

A

inhibit leukocyte infiltration at inflammation site; interference in function of inflammatory response mediators; suppress humoral immune response; reduce oedema/scar tissue

128
Q

BECLOMETHASONE: anti-inflammatory actions involve (2)

A

lipocortins > prostaglandins and leukotrienes; phospholipase A2 inhibitory proteins

129
Q

BECLOMETHASONE: 4 side effects

A

headaches, pharyngitis, difficulty speaking, Cushing’s (long term)

130
Q

Propanolol = antagonist of

A

salbutamol

131
Q

Propanolol competes with catecholamines for ….. adrenergic receptors in heart > inhibits …… stimulation

A

beta1; sympathetic

132
Q

SALBUTAMOL: …….. adrenergic …..

A

beta2; agonist

133
Q

SALBUTAMOL: increases ….. production by activating adenylate cyclase > increased activity of …….. `

A

cAMP; protein kinase A

134
Q

SALBUTAMOL: inhibits phosphorylation of ….. and lowers intracellular calcium concentration > broncho…..

A

myosin; dilation

135
Q

SALBUTAMOL: 3 other effects of salbutamol

A

enhances mucociliary clearance, inhibits microvascular leakage, inhibits release of bronchoconstricting agents from mast cells

136
Q

SALBUTAMOL: 3 side effects

A

tachycardia, headaches, TREMORS

137
Q

BETA2 ADRENOCEPTOR AGONISTS (1) Activation of beta2 adrenoceptors is via ……. coupled receptor

A

G-protein

138
Q

synthetic beta2 agonists and …… bind to beta2 adrenceptors

A

noradrenaline

139
Q

BETA2 ADRENOCEPTOR AGONISTS (2) alpha subunit of G-protein activates …….. > catalyses production of cAMP

A

adenylyl cyclase

140
Q

BETA2 ADRENOCEPTOR AGONISTS (3) in lung, cAMP causes decrease in intracellular ….. concentration

A

calcium

141
Q

BETA2 ADRENOCEPTOR AGONISTS (4) decrease in intracellular calcium activates ….. which inactivates myosin light chain ….. and activates myosin light chain ….

A

protein kinase A; kinase; phosphatase

142
Q

BETA2 ADRENOCEPTOR AGONISTS 3 methods of smooth muscle relaxation and bronchodilation

A

decreased intracellular calcium, increased membrane potassium conductance, decreased myosin light chain kinase activity

143
Q

THEOPHYLLINE: ……. inhibitor

A

phosphodiesterase

144
Q

THEOPHYLLINE: cAMP activates protein ….. > protein phosphorylation > muscle relaxation

A

kinase A

145
Q

Theophylline is used with steroid when

A

response to beta2 agonist is inadequate

146
Q

THEOPHYLLINE: 5 side effects

A

tremor, stimulate heart, nausea, anorexia, sleep disturbances

147
Q

MUSCARINIC RECEPTOR ANTAGONISTS: main drug used =

A

ipratropium

148
Q

MUSCARINIC RECEPTOR ANTAGONISTS: used when beta2 agonist and …. insufficient

A

steroid

149
Q

MUSCARINIC RECEPTOR ANTAGONISTS: blocks action of endogenous ….. at muscarinic receptors

A

acetylcholine

150
Q

MUSCARINIC RECEPTOR ANTAGONISTS: low levels of acetylcholine released from cholinergic nerves in airways > few muscarinic receptors activated > smooth muscle …

A

relaxed

151
Q

LEUKOTRIENE RECEPTOR ANTAGONISTS: prevents which 2 types of asthma

A

exercise induced and aspirin allergic

152
Q

LEUKOTRIENE RECEPTOR ANTAGONISTS: acts at ….. leukotriene receptors and prevents actions of LTC4 and LTD4 whch are bronchial …. and stimulants of mucus secretion

A

cysteinyl; spasmogens

153
Q

LEUKOTRIENE RECEPTOR ANTAGONISTS: 2 unwanted side effects

A

headache, GI disturbance

154
Q

glucocorticoids reduce production of (3)

A

cytokines, spasmogens, leukocyte chemotaxins

155
Q

glucocorticoids bind to ….. receptors (GRalpha and GRbeta) > alter gene transcription

A

intracellular

156
Q

cromoglicate =

A

mast cell stabiliser

157
Q

OMALIZUMAB: binds to …. and inhibits binding of IgE to receptor (FcRI) on mast cells and …. > inhibits IgE asthma cascade

A

IgE; basophils

158
Q

OMALIZUMAB: 2 side effects

A

anaphylaxis; malignancies

159
Q

AGONIST stabilises receptor in

A

active form

160
Q

more receptors end up in … form when agonist present

A

active

161
Q

ANTAGONIST binds with …… to receptors in active and inactive states

A

equal affinity

162
Q

ANTAGONIST stabilises receptors in …. state

A

inactive

163
Q

ANTAGONIST preserves ….. between states

A

original drug free equilibrium

164
Q

PARTIAL AGONIST has a …. maximum response than agonist

A

lower

165
Q

PARTIAL AGONIST binds more tightly to …. form but still has appreciable affinity for … form

A

active; inactive

166
Q

INVERSE AGONIST binds more tightly to …. form of receptor

A

inactive

167
Q

INVERSE AGONIST measurable spontaneous activity of receptors will … in presence of inverse agonist

A

decrease

168
Q

when inverse agonist present, receptors end up almost entirely in …. state

A

inactive

169
Q

VARENICLINE: nicotine receptor ……. of alpha4 and beta2 subtype

A

partial agonist

170
Q

VARENICLINE: …. inhibits binding of nicotine

A

competitively

Sem 2 (11 decks)

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