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Y2S1 Pharmacology Flashcards

(108 cards)

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1
Q

What is the mechanism of action of dipyridamole?

A

Inhibits platelet phosphodiesterase → increased cAMP → inhibition of platelet activation

AND

Inhibits thromboxane A2 synthesis

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2
Q

Name 3 P2Y12 receptor antagonists

A
  1. Clopidogrel
  2. Prasugrel
  3. Ticagrelor
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3
Q

How does antagonism of the P2Y12 receptor inhibit platelet aggregation?

A

Antagonism of the P2Y12 (ADP) receptor → increased adenylate cyclase → increased cAMP → decreased platelet aggregation

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4
Q

What is the difference in mechanism of clopidogrel and prasugrel, and ticagrelor?

A

The active metabolite of the thienopyridines (clopidogrel, prasugrel) irreversibly binds to the platelet P2Y12 receptor and inhibits platelet aggregation for the life of the platelet

Ticagrelor binds reversibly to the P2Y12 receptor.

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5
Q

Name 3 glycoprotein IIb/IIIa inhibitors

A

Abciximab

Eptifibatide

Tirofiban

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6
Q

How do glycoprotein IIb/IIIa inhibitors reduce platelet aggregation?

A

They prevent the binding of fibrinogen to platelets by occupying glycoprotein IIb/IIIa receptor, thereby blocking platelet aggregation

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7
Q

Name 4 classes of medications that affect platelet adhesion and activation

A
  1. COX inhibitors
  2. Phosphodiesterase inhibitors
  3. P2Y12 receptor antagonists
  4. GP-IIb/IIIa receptor antagonists
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8
Q

Name 3 low molecular weight heparins

A
  1. Dalteparin
  2. Enoxaparin
  3. Nadroparin
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9
Q

What is the mechanism of heparins?

A

Bind to and activate antithrombin III → inactivation of clotting factors IIa (thrombin) and Xa

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10
Q

What is the major difference between the mechanism of heparin and low-molecular-weight heparins (LMWH)?

A

LMWHs have stronger effects on factor Xa

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11
Q

Which medication is used to reverse the action of heparins?

A

Protamine

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12
Q

What is the mechanism of protamine?

A

Rapidly forms a stable complex with heparin - “chemical antagonist”

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13
Q

Name 2 direct thrombin inhibitors

A
  1. Bivalirudin
  2. Dabigatran
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14
Q

Which medication is used to reverse the effects of dabigatran?

A

Ibarucizumab

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15
Q

What is the mechanism of idarucizumab?

A

Humanised monoclonal antibody fragment binds with dabigatran → stable inactive complex → reverses anticoagulant effect

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16
Q

Name 3 factor Xa inhibitors?

A
  1. Apixaban
  2. Fondaparinux
  3. Rivaroxaban
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17
Q

What is the mechanism of warfarin?

A

Vitamin K reductase inhibitor

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18
Q

The concentration of which clotting factors are affected by warfarin?

A

II, VII, IX, X

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19
Q

Which laboratory test is used to monitor coagulation in patients on warfarin?

A

International normalised ratio (INR)

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20
Q

Which laboratory measurement is used to determine the international normalised ratio?

A

Prothrombin time

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21
Q

What is used to reverse the actions of warfarin?

A

Vitamin K

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22
Q

What is the mechanism of tranexamic acid?

A

Inhibits breakdown of clots by blocking binding of plasminogen and plasmin to fibrin

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23
Q

What is the mechanism of cyclophosphamide?

A

Alkylating agent - interferes with transcription and DNA replication

AND is an immunosuppressant, having cytotoxic effects on lymphocytes

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24
Q

What is the mechanism of methotrexate?

A

Folic acid antagonist. Inhibits DNA synthesis and cell replication

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25
What is the mechanism of fludarabine?
Purine antimetabolite → inhibits DNA synthesis → apoptosis
26
What is the mechanism of 5-fluorouracil?
Pyrimidine antimetabolite → inhibits DNA synthesis → apoptosis
27
Name 6 adverse effects of cytotoxic chemotherapy drugs
1. Myelosuppression 2. Poor wound healing 3. Alopecia 4. Damage to the gastrointestinal epithelium 5. Growth depression 6. Sterility Other: teratogenicity, carcinogenicity These effects occur because chemotherapy targets all rapidly dividing cells
28
What is the mechanism of cetuximab?
Monoclonal antibody targeted against epidermal growth factor receptor (EGFR) → inhibits proliferation and inducing apoptosis of tumour cells that over-express EGFR ## Footnote *E.g. colorectal, non-small cell lung and head and neck cancer*
29
What is the mechanism of erlotinib?
Reversible inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase ## Footnote *Intracellular kinase activity drives downstream signalling of tumours*
30
What is the mechanism of pembrolizumab?
**Inhibits the binding of programmed cell death protein 1 (PD-1)** to its ligands on tumour cells This **reactivates cytotoxic T cells and anti-tumour immunity**
31
What is the mechanism of medroxyprogesterone acetate?
Activates progesterone receptors in the endometrium → antiproliferative effects against endometrial cancer
32
What is the mechanism of letrozole?
Reversible inhibition of aromatase in the adrenal cortex → decreased oestrogen synthesis Used for oestrogen-receptor-positive breast cancer in post-menopausal women
33
Why is letrozole only used in post-menopausal women?
A reduction of oestrogen synthesis by the adrenal cortex causes a compensatory increase in ovarian oestrogen production in pre-menopausal women
34
Which drug is used to stimulate neutrophil production?
Granulocyte-colony stimulating factor - filgrastim/pegfilgrastim
35
Which disease-modifying anti-rheumatoid drug (DMARD) is first-line?
Methotrexate
36
What is the mechanism of cyclosporine?
Calcineurin inhibitor Calcineurin usually stimulates the production of interleukin‑2 and other cytokines, which normally stimulate T cell proliferation and differentiation.
37
What is the mechanism of tacrolimus?
Calcineurin inhibitor Calcineurin usually stimulates the production of interleukin‑2 and other cytokines, which normally stimulate T cell proliferation and differentiation.
38
What is the mechanism of azathioprine?
Purine antimetabolite Interferes with purine synthesis, inducing DNA damage that impairs proliferation and function of B and T cells
39
What is the mechanism of mycophenylate?
Inhibits inosine monophosphate dehydrogenase → decreased guanosine synthesis → suppresses lymphocyte proliferation and antibody formation
40
List 6 immunosuppressants or immunomodulators that are used for rheumatoid arthritis
Cyclosporine Tacrolimus Azathioprine Mycophenolate Hydroxychloroquine Infliximab Corticosteroids Tofacitinib Methotrexate
41
What is the mechanism of infliximab?
Tumour necrosis factor alpha antagonist TNF-alpha is a cytokine released by various immune cells, including T helper cells
42
Which enzyme converts histadine into histamine?
Histadine decarboxylase
43
What is the main mechanism of antihistamines?
Histamine inverse agonist - binds to histamine receptors and stabilises them in their inactive form
44
Name 4 effects of antihistamines
1. Reduced mast cell release of histamine 2. Reduced recruitment of immune cells 3. Reduced itch, pain and sneezing 4. Reduced vasodilation Other: reduce bronchoconstriction
45
What is the major difference between first and second generation antihistamines?
First generation antihistamines more readily cross the BBB, causing sedaion
46
Name 3 first-generation antihistamines
1. Diphenhydramine 2. Promethazine 3. Doxylamine
47
Name 2 second-generation antihistamines
1. Loratadine 2. Fexofenadine
48
Name 3 antiresorptive drugs used for osteoporosis
Alendronate, pamidronate, etidronate (bisphosphonate) Raloxifen, tamoxifen (SERM) Denosumab (RANKL inhibitor)
49
Name an anabolic agent used for osteoporosis
Teriparatide (recombinant PTH)
50
What is the mechanism of bisphosphonates?
Induces apoptosis in osteoclasts
51
Name a simple bisphosphonate
Etidronate
52
Name 2 amino bisphosphonates
1. Alendronate 2. Pamidronate
53
How do simple and amino bisphosphonates differ in their mechanism of action?
Simple - are incorporated into ATP analogues in osteoclasts → apoptosis Amino - interfere with the anchoring of cell surface protein to the osteoclast membrane → decreased osteoclast attachment → apoptosis
54
How does oestrogen decrease osteoclast proliferation?
Decreases the transcription of RANKL in osteoblasts RANKL binds to the RANK receptor on osteoclast precursor, stimulating osteoclast maturation
55
Name a selective estrogen receptor modulator (SERM)
Raloxifene Tamoxifen
56
How do SERMs modulate oestrogen?
Oestrogen receptor agonist in bone Oestrogen receptor antagonist in the endometrium and breast
57
What is the mechanism of denosumab?
Recombinant human monoclonal antibody that binds to and inhibits RANKL, decreasing the action of osteoclasts
58
What is teriparatide?
Recombinant human PTH Intermittent PTH has anabolic effects on bone
59
How does teriparatide have anabolic effects on bone?
1. Antiapoptotic effects on osteoblasts 2. Induces osteoblast maturation
60
How do cathepsin K inhibitors treat osteoporosis?
Cathepsin K degrades type 1 collagen, leading to bone degradation ## Footnote *Novel therapy e.g. odanacatib*
61
How do sclerostin inhibitors treat osteoporosis?
Sclerostin stimulates the production of RANKL by osteocytes, reducing bone formation and stimulating osteoclasts
62
What is the mechanism of cinacalcet?
Enhances the sensitivity of PTH calcium-sensing receptors → decreases PTH release
63
What is the mechanism of tissue plasminogen activator?
Activates plasmin, the enzyme responsible for the conversion of fibrin to fibrin degradation products
64
Name a tissue plasminogen activator
1. Alteplase Other: reteplase, tenecteplase
65
What is the difference in mechanism between urokinase-type plasminogen activator and recombinant tissue plasminogen activators?
Recombinant tPA is selective to fibrin-bound plasminogen Urokinase does not discriminate between fibrin-bound plasminogen and plasma plasminogen → causes thrombolysis in clots and systemically
66
What is the mechanism of tranexamic acid?
Lysin analogue → binds lysine binding site → blocks binding of plasminogen and plasmin to fibrin → inhibits breakdown of clots
67
What is the mechanism of streptokinase?
Plasminogen activator
68
Which antiepileptic drugs are sodium channel blockers?
Carbamazepine Phenytoin Lamotrigine Sodium valproate Topiramate
69
Which antiepileptic drugs enhance GABA?
Benzodiazepines Barbiturates Gabapentin Topiramate Sodium valproate
70
Which antiepileptic drugs are calcium channel blockers?
Ethosuximide Sodium valproate Clonazepam
71
How do sodium-blocking antiepileptic medications target hyperexcitable neurons?
They are selective to highly active/excitable sodium channels - "use-dependent"
72
What effect do sodium-channel blocking antiepileptics have on neuronal depolarisation?
Decrease rate of recovery of sodium channels, increasing the refractory period of neurons This prevents repetitive neuronal firing
73
What is the first-line medication for focal seizures?
Carbamazepine
74
What is the first-line medication for generalised tonic-clonic seizures?
Sodium valproate
75
What is the first line medication for pregnant women with focal seizures?
Lamotrigine
76
Which medications are first-line for absence seizures?
Ethosuximide Sodium valproate
77
What is the mechanism of barbiturates?
Prolongs the duration of GABAA channel opening
78
What is the mechanism of benzodiazepines?
Increases the frequency of GABAA channel opening
79
What is the treatment of status epilepticus?
Benzodiazepines
80
What is the mechanism of ethosuximide?
Blockage of low-threshold T-type calcium channels in thalamic neurons
81
What are the 3 mechanisms of sodium valproate?
1. Prolongs recovery of sodium channels 2. Inhibits thalamic T-type calcium channels 3. Increases GABA production and reduces its breakdown → alteration in cellular resting membrane potentials
82
What are the proposed mechanisms of migraines?
1. Dilation of intracranial vessels (particularly meningeal vessels) 2. Recurrent activation and sensitisation of the trigeminovascular pathway 3. Reduced activation of descending pain inhibitory pathways
83
What is the major drug class used to acutely stop migraines?
"Triptans" e.g. sumatriptan
84
What is the mechanism of triptans?
Agonists at 5HT1B and 5HT1D receptors → vasoconstriction and enhancement of inhibitory descending pain pathways
85
86
What are contraindications to triptan use?
History of MI Coronary artery disease Peripheral vascular disease Angina/coronary vasospasm Uncontrolled hypertension Stroke of TIA *Small risk of serious coronary events*
87
What are potential adverse effects of triptans?
Chest, jaw and throat tightness or tingling Muscle pain and paresthesia Flushing, dizziness, weakness Transient increase in BP Serious coronary events - rare
88
Name 5 first-line medications for migraine prophylaxis
1. Amitriptyline 2. Candesartan 3. Pizotifen 4. Propranolol 5. Topiramate Other: sodium valproate, nortriptyline
89
List 4 non-analgesic drugs used for neuropathic pain
1. Amitriptyline 2. Duloxetine 3. Gabapentin 4. Pregabalin
90
How do tricyclic antidepressants treat neuropathic pain?
Promotion of descending inhibitory pain pathways **1. Inhibition of 5HT reuptake** **2. Inhibition of NA reuptake** 3. Inhibition of post-synaptic histamine receptors
91
Which drug is first-line for trigeminal neuralgia?
Carbamazepine
92
What is the mechanism of capsaicin?
Transient receptor potential vanilloid type 1 (TRPV1) receptor agonist → substance P depletion → inhibits neuropathic pain
93
What is the mechanism of lignocaine?
Voltage-gated sodium channel blocker → inhibition of conduction in peripheral nerves
94
What is the mechanism of ketamine?
Polyamine antagonist (inhibits NMDA receptors) → anaesthesia
95
What is the mechanism of macrogol?
Induces osmotic activity in the bowel (laxative)
96
What is the mechanism of lactulose?
Induces osmotic activity in the bowel (laxative)
97
What is the mechanism of senna?
Stimulatory laxative - directly stimulates nerve endings in colonic mucosa to increase intestinal motility
98
What is the mechanism of ondansetron?
Central and peripheral 5HT3 receptor blockade → antiemetic
99
What is the mechanism of metoclopramide?
Dopamine antagonist
100
What is the mechanism of ranitidine?
Inhibits H2 receptors on parietal cells, reducing gastric acid secretion
101
What is the mechanism of esomeprazole?
Proton pump inhibitor → reduces gastric acid secretion
102
What is the mechanism of aluminium/magnesium hydroxide?
Antacid - neutralises stomach acid
103
Which medication is used to reverse the effects of paracetamol overdose?
Acetylcysteine
104
Which mediation is used to reverse opioid overdose?
Naloxone
105
What is colchicine used for?
Relief of pain in acute gout Reduces inflammation: inhibits neutrophil migration, chemotaxis, adhesion and phagocytosis in inflamed tissue. In gout, it reduces inflammatory reaction to urate crystals
106
What is the mechanism of allopurinol?
Inhibits xanthine oxidase → reduces production of uric acid
107
What is the mechanism of levodopa?
Dopamine precursor
108
What is the mechanism of carbidopa?
Peripheral dopa decarboxylase inhibitor → reduce peripheral conversion of levodopa to dopamine

Y2 Revision (7 decks)

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