Block 3 Pharmacology Flashcards

1
Q

Chlorpromazine - class

A

Dopamine receptor antagonist - phenothiazine based antipsychotic.

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2
Q

Chlorpromazine - MoA

A

Competitively binds D2 receptors in CTZ (5-HT, H and M), reduces activity of vomiting centre.

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3
Q

Chlorpromazine - uses

A

Nausea and vomiting.

Prochlorperazine used now.

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4
Q

Perphenazine - class

A

Dopamine receptor antagonist - antipsychotic phenothiazine

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5
Q

Perphenazine - MoA

A

Binds D1 and D2 receptors to inhibits their activity in CTZ and vomiting centre.

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6
Q

Perphenazine - uses

A

Severe nausea and vomiting.

15x more potent than chlorpromazine.

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7
Q

Metoclopramide - class

A

Dopamine receptor antagonist - benzoic acid derivative

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8
Q

Metoclopramide - MoA

A

Inhibits gastric smooth muscle relaxation produced by dopamine. Raises threshold in CTZ. Increases resting pressure of lower oesophageal sphincter so decreases reflux. Increases motility of stomach, oesophagus and intestines.

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9
Q

Metoclopramide - uses

A

GERD, nausea and vomiting.

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10
Q

Domperidone - class

A

Dopamine receptor antagonist - benzimidazole

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11
Q

Domperidone - MoA

A

Blocks dopamine receptos in CTZ, speeds up gastric peristalsis.

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12
Q

Domperidone - uses

A

Nausea and vomiting.

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13
Q

Aspirin - class

A

NSAID

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14
Q

Aspirin - MoA

A

Irreversibly binds COX and inhibits activity -> reduces prostaglandin production.
Analgesic, antipyretic and anti-inflammatory.

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15
Q

Aspirin - uses

A

Aches and pains.

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16
Q

Ibuprofen - class

A

NSAID

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17
Q

Ibuprofen - MoA

A

Irreversibly binds COX2 receptors -> reduces prostaglandin production.

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18
Q

Ibuprofen - uses

A

Aches and pains.

Side effects - GI bleed as reduced prostaglandins.

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19
Q

Naproxen - class

A

NSAID

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20
Q

Naproxen - MoA

A

Irreversibly binds COX receptors -> reduces prostaglandin production.

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21
Q

Naproxen - uses

A

RA, osteoarthritis, tendinitis.

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22
Q

Omeprazole - class

A

Proton-pump inhibitor

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23
Q

Omeprazole - MoA

A

Irreversibly binds H+/K+-ATPase enzyme in gastric parietal cell and blocks the release of H+ into gastric lumen.
72 hours with max effects at 2 hours.

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24
Q

Omeprazole - uses

A

Duodenal ulcers, GERD, heartburn

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25
Q

Esomeprazole - class

A

PPI

S isomer of omeprazole

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26
Q

Esomeprazole - MoA

A

Inhibits H+/K+-ATPase enzyme -> reduces gastric acid secretion.

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27
Q

Esomeprazole - uses

A

Peptic ulcers, GERD, heals erosive oesophagitis and eradication of H. pylori.

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28
Q

Cyclizine - class

A

Histamine receptor antagonist - piperazine derivative antihistamine.

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29
Q

Cyclizine - MoA

A

Blocks histamine receptors in CTZ, prevents overstimulation of histamine synapses in vomiting centre and reduces motion sickness.

30
Q

Cyclizine - uses

A

Nausea, vomiting, dizziness and vertigo.

31
Q

Cinnarizine - class

A

Histamine receptor antagonist and calcium channel blocker.

32
Q

Cinnarizine - MoA

A

Competitive inhibitor of H1 receptors.

Blocks L-type and T-type voltage gated Ca2+ channels -> inhibits vascular smooth muscle contraction.

33
Q

Cinnarizine - uses

A

Vertigo, motion sickness, nausea and vomiting.

34
Q

Promethazine - class

A

Histamine receptor antagonist

35
Q

Promethazine - MoA

A

Competitive antagonist of H1 receptors.

Central anticholinergic, sedative and local anaesthetic effects.

36
Q

Promethazine - uses

A

Nausea, vomiting and allergic disorders

37
Q

Ranitidine - class

A

Histamine receptor antagonist

38
Q

Ranitidine - MoA

A

Competitive inhibitor of histamine at parietal cell H2 receptors. Suppresses normal secretion of gastric acid.
Inverse agonist as reduces effects of gastrin.

39
Q

Ranitidine - uses

A

Peptic ulcers, dyspepsia and reflux oesophagitis.

40
Q

Amoxicillin - class

A

Beta-lactam antibiotic

41
Q

Amoxicillin - MoA

A

Binds and inactivates penicillin-binding protein 1A in bacterial cell wall -> inhibits cell wall synthesis -> cell lysis.

42
Q

Amoxicillin - uses

A

Gram + and - bacteria in ear, nose, throat and skin.
H. pylori.
Used with clavulanic acid -> beta-lactamase inhibitor (prevents resistance).

43
Q

Clarithromycin - class

A

Macrolide antibiotic

44
Q

Clarithromycin - MoA

A

Binds 50S subunits of bacterial ribosome - blocks translocation of aminoacyl tTNA and polypeptide synthesis -> prevents growth of bacteria.

45
Q

Clarithromycin - uses

A

Tonsilitis, acute maxillary sinusitis.

H. pylori

46
Q

Hyoscine - class

A

Cholinergic receptor antagonist

47
Q

Hyoscine - MoA

A

Competitive inhibitor of muscarinic cholinergic receptor. Stops nerve impulses between CTZ and vestibular system and PNS.

48
Q

Hyoscine - uses

A

Colicky abdo pain, excessive salivation, IBS and motion sickness.

49
Q

Magnesium trisilicate - class

A

Antacids

50
Q

Magnesium trisilicate - MoA

A

Directly neutralises stomach acid, inhibits peptic enzymes.

Aluminium hydroxide delivers growth factors to injured mucosa, antacids promotes angiogenesis of injured mucosa.

51
Q

Magnesium trisilicate - uses

A

Dyspepsia and oesophageal reflux.

52
Q

Metronidazole - class

A

Nitroimidazole antibacterial and antiprotozoal.

DNA synthesis inhibitor.

53
Q

Metronidazole - MoA

A

Binds to bacterial DNA and disrupts the helical structure and inhibits nucleic acid synthesis -> cell death.

54
Q

Metronidazole - uses

A

Anaerobic and mixed infections. H. pylori, Crohn’s, diarrhoea.

55
Q

Misoprostol - class

A

Prostaglandin agonist

56
Q

Misoprostol - MoA

A

Binds prostaglandin receptor on parietal cells and reduces gastric acid secretion via reducing cAMP through Gi.
Increases bicarbonate production and increases thickness of mucus layer.

57
Q

Misoprostol - uses

A

Ulcerations induced by NSAIDs

58
Q

Ondansetron - class

A

5-HT3 receptor antagonist

59
Q

Ondansetron - MoA

A

Inhibits 5-HT3 receptors to prevent stimulation of vomiting centre via CTZ and vagus nerve.

60
Q

Ondansetron - uses

A

Nausea, vomiting associated with chemotherapy and radiation.

61
Q

Atorvastatin - class

A

HMG-CoA reductase inhibitor

62
Q

Atorvastatin - MoA

A

Competitive inhibitor of HMG-CoA reductase -> decreases plasma LDL levels due to increased hepatic uptake of LDL and inhibiting cholesterol synthesis.

63
Q

Atorvastatin - uses

A

Prevention of arterial diseases.

64
Q

Bezafibrate - class

A

Antilipemic agent - benzene derivative

65
Q

Bezafibrate - MoA

A

Increased transcription of apoA1 and 5 -> increased hepatic LDL uptake. Activates triglyceride lipase and reduces cholesterol synthesis.

66
Q

Bezafibrate - uses

A

Primary hyperlipidaemia.

67
Q

Orlistat - class

A

Lipase inhibitor

68
Q

Orlistat - MoA

A

Reversibly binds and blocks pancreatic and gastric lipase -> reduces breakdown of TAG -> undigested TAG excreted.

69
Q

Orlistat - uses

A

Obesity.

Used with fat-soluble vitamins.

70
Q

Thalidomide - class

A

Hypnotic, antiemetic.

71
Q

Thalidomide - MoA

A

Immunosuppressive and anti-angiogenic activity. Inhibits release of TNFalpha from monocytes and modulates cytokine action.
Teratogenic activity.

72
Q

Thalidomide - uses

A

Morning sickness (caused embryological deformities), multiple myeloma and leprosy.