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Phase I Medicine > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is the group of drugs used to treat myasthenia gravis?

A

Muscle excitors

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2
Q

Name the two drugs used to treat myasthenia gravis

A

Edrophonium/ Tensilon

Pyridostigmine

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3
Q

What is the pharmacological name for tensilon?

A

Edrophonium

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4
Q

What is the trivial/ brand name for edrophonium?

A

Tensilon

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5
Q

What is tensilon?

A

Muscle excitor used to treat myasthenia gravis

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6
Q

How does tensilon work?

A

Competitively inhibits acetyl-cholinesterase, preventing breakdown of Ach. In MG will greatly increase muscle function.

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7
Q

Why can tensilon act as a test for MG?

A

It’s a temporary drug which will improve muscle function in MG but make other syndromes worse.

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8
Q

How does pyridostigmine work against MG?

A

Inhibits the hydrolysis of Ach by competitively inhibiting acetyl-cholinesterase. Results in the increase of Ach.

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9
Q

What class of drug is pyridostigmine?

A

Reversible cholinesterase inhibitor

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10
Q

What class of drug is tensilon/ endrophonium?

A

Cholinesterase inhibitor

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11
Q

Name the main drugs that act as muscle relaxants

A

Tubocurarine
Suxamethonium
Atracurium

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12
Q

How does Tubocurarine work?

A

Blocks the receptor site for Ach

Also causes histamine release.

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13
Q

How does Suxamethonium work?

A

Depolarises post synaptic membrane so muscle can’t contract.

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14
Q

How does Atracurium work?

A

Antagonises neurotransmitter action of Ach by competitively binding with cholinergic receptor sites on the motor end-plate.

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15
Q

What is Suxamethonium clinically used for?

A

Induced muscle relaxation/short term paralysis for tracheal intubation

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16
Q

What is Atracurium clinically used for?

A

Used adjunctively in tracheal intubation to provide skeletal muscle relaxation.

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17
Q

What is Tubocurarine clinically used for?

A

Used as a poison and spider bite antidote.

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18
Q

What receptors do Tubocurarine, Suxamethonium and Atracurium all mutually act on?

A

Cholinergic receptors

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19
Q

Which of these drugs is a cholinergic agonist?
Tubocurarine
Suxamethonium
Atracurium

A

Suxamethonium

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20
Q

What is the are the differences between Suxamethonium and Atracurium as nicotinic cholinergic drugs?

A

Suxamethonium - Depolarising Agonist

Atracurium - Non-depolarising Anatagonist

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21
Q

Why is Tropicamide commonly used for lens and retina examinations?

A

Clinically reduces eye movement

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22
Q

Name two muscarinic cholinergic receptor agonists

A

Muscarine

Pilocarpine

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23
Q

How do muscarinic cholinergic receptor agonists work?

A

Mimics action of the neurotransmitter acetylcholine by binding muscarinic Ach receptors

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24
Q

What are the clinical differences between muscarine and pilocarpine?

A

Muscarine - Hallucinogen found in magic mushrooms

Pilocarpine - Used to treat dry mouth

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25
Q

Which drug is more likely to be used to treat dry mouth?

Muscarine or Pilocarpine?

A

Pilocarpine

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26
Q

What is the pharmacological name for Botulinium A toxin?

A

Botox

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27
Q

What is Botox’ mechanism of action?

A

Attaches to neurones and sends a chemical into the neurone’s cytoplasm, preventing Ach from being released

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28
Q

What class of drug is Botulinium A toxin?

A

Acetylcholine release inhibitor

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29
Q

Does Botox act on the pre synaptic or post synaptic membrane?

A

Presynaptic

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30
Q

How is Botox clinically used?

A

Cosmetic surgery
Treatment of spasms
Treatment of dystonia

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31
Q

What class of drug is Pralidoxime?

A

Cholinsterase reactivator

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32
Q

How does Pralidoxime work clinically?

A

As an antidote to organophosphates in pesticides.

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33
Q

What is Pralidoxime’s mechanism of action against pesticides?

A

Pesticides initially inactivate Ach enzyme, meaning Ach increases. Pralidoxime cleaves the bond formed between organophosphate and Ach receptors thus inactivating their effects.

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34
Q

What class of drug is Sarin?

A

Irreversible cholinesterase Inhibitor

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35
Q

How does Sarin act on cholinergic receptors?

A

inhibits cholinesterase causing acetylecholine to build up so that nerve impulses are continually transmitted.

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36
Q

What effect does the drug Sarin have on muscle movement?

A

Causes inability for muscles to relax.

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37
Q

What group of chemical products would Sarin be found in?

A

Organophosphates

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38
Q

What would Sarin be used for?

A

A chemical weapon.

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39
Q

What class of drug is Hemicholinium?

A

Choline reuptake inhibitor

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40
Q

What class of drug is Donepezil?

A

Reversible cholinesterase enzyme inhibitor

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41
Q

What is hemicholinium’s mechanism of action?

A

Blocks reuptake of choline via high affinity choline transporter at presynaptic membrane, decreasing amount of Ach that can be made

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42
Q

What are the clinical applications of hemicholium?

A

Not used as a medication but used in research

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43
Q

What is donepezil’s mechanism of action?

A

Increases Ach concentration by temporarily stopping it from being hydrolysed.

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44
Q

True or false? Donepezil is clinically used for Alzheimers?

A

True

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45
Q

What class of drug does morphine belong to?

A

Analgesic

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46
Q

What class of drug is Bethamethasone?

A

Glucocorticoid nuclear receptor agonist/ Anti-inflammatory

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47
Q

What is bethmethasone’s mechanism of action?

A

Mimics action of cortisol by altering gene expression which decreases the supply of arachidonic acid-> reducing inflammation

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48
Q

What is the phamacological name for Paracetamol?

A

Acetaminophen

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49
Q

What is the trivial/ brand name for Acetaminophen?

A

Paracetamol

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50
Q

What is paracetamol’s mechanism of action?

A

Blocks production of prostaglandins by inhibiting COX

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51
Q

What drug classes does Paracetamol belong to?

A

COX inhibitor/Analgesic/Anti-inflammatory

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52
Q

What class of drug is Prednisolone?

A

Glucocorticoid

Anti-inflammatory

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53
Q

What is Prednisolone clinically known for?

A

It is the most commonly prescribed corticosteroid

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54
Q

What is Prednisolone’s mechanism of action?

A

Binds to cytosolic receptors to inhibit leukocyte infiltration, stops inflammatory mediators.
Thought to also act via lipocortins, phospholipase A2 inhibitory proteins which control prostaglandin and leukotrienes production.

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55
Q

What class of drug is Chlorphenamine?

A

H1 antagonist

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56
Q

What is the clinical purpose of Chlorphenamine?

A

Used in the treatment of rhinitis, urticaria, allergy, common cold, asthma and hay fever.

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57
Q

What is Chlorphenamine’s mechanism of action?

A

Competes with histamine for normal H1 receptor sites on effector cells, which subsequently leads to temporary relief of negative symptoms brought on by histamine.

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58
Q

What class of drug is Diclofenac?

A

NSAID/ Anti-inflammatory /Analgesic/ Antipyretic

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59
Q

What is morphine’s mechanism of action?

A

Mimics endogenous opoids on mu opoid receptors

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60
Q

What are opoids?

A

The body’s natural pain killer

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61
Q

What is Diclofenac’s mechanism of action?

A

Inhibits COX thus inhibiting prostaglandin synthesis. May also inhibit bacterial DNA synthesis.

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62
Q

What is a common side effect of Diclofenac?

A

GI Complaints.

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63
Q

What class of drug is hydrocortisone?

A

Glucocorticoid/ Anti-inflammatory

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64
Q

What are the clinical applications of hydrocortisone?

A

Used to treat people who lack naturally generated cortisol.

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65
Q

What are hydrocortisone’s mechanisms of action?

A

Binds to the cytosolic glucocorticoid receptor-> the newly formed receptor-ligand complex translocates itself into the cell nucleus-> binds to many glucocorticoid response elements (GRE) in the promoter region of target genes, inhibiting prostaglandins and leukotrienes.

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66
Q

What class of drug is codeine?

A

Opiate Receptor Agonist/ Analgesic/ Anti-diarrhoea

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67
Q

How is codeine clinically used?

A

Pain killer, cough medicine, anti-diarrhoea

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68
Q

How is codeine metabolised in the stomach?

A

It is converted into morphine in the stomach

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69
Q

What classes of drug does Pethidine belong to?

A

Opiate Receptor Agonist/ Analgesic

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70
Q

What are the major side effects of Pethidine?

A

Respiratory depression and Bradycardia

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71
Q

What are Pethidine’s mechanisms of action?

A

Mimics the actions of endogenous neuropeptides primarily via kappa opioid receptors (but also via mu- receptors), producing the characteristic morphine -like effects.

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72
Q

What classes of drug does Tramadol belong to?

A

Opioid receptor agonist/ Multi-target analgesic

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73
Q

What is Tramadol’s mechanism of action?

A

Acts on mu-opioid GPCRs and decreases intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters is inhibited.

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74
Q

How is tramadol used in clinical practise?

A

A very strong painkiller

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75
Q

What class of drug does Arnica Motana belong to?

A

Analgesic/ anti-inflammatory

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76
Q

Where is Arnica Motana commonly used?

A

Homeopathic remedies

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77
Q

What is Arnica Motana’s mechanism of action?

A

Affects transcription factor human telomerase.

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78
Q

What class of drug is aspirin?

A

COX-1 inhibitor/ NSAID/Anti-pyretic/Analgesic.

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79
Q

How is aspirin used clinically?

A

Blood Thinner, Painkiller

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80
Q

What is aspirin’s mechanism of action?

A

Irreversibly inhibits COX-1 and modifies the enzymatic activity of COX-2 which is required for prostaglandin and thromboxane synthesis.

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81
Q

What is the normal role of prostaglandins?

A

To promote inflammation

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82
Q

What is the normal role of thromboxane?

A

Aggregates platelets for clotting.

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83
Q

What class of drug is Ibuprofen?

A

COX-2 inhibitor/ NSAID/Anti-pyretic/Analgesic

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84
Q

What is ibuprofen’s mechanism of action?

A

Inhibits COX-2 enzyme, so inhibits production of prostaglandins

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85
Q

What is the strength of ibuprofen in relation to other NSAIDs?

A

It is weaker

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86
Q

What class of drug is naproxen?

A

COX-1 and COX-2 inhibitor/ NSAID/Anti-pyretic/Analgesic

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87
Q

What is naproxen’s mechanism of action?

A

Inhibits enzymes so less prostaglandins for inflammation. Mechanism is poorly understood.

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88
Q

What class of drug is Rifampicin?

A

Antibiotic

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89
Q

What is the alternative name for Rifampicin?

A

Rifadin

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90
Q

How is Rifampicin clinically used?

A

Used to Treat Bacterial Infections

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91
Q

What is Rifampicin’s mechanism of action?

A

Inhibits RNA polymerase and blocks the formation of bonds in the RNA backbone

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92
Q

What class of drug is Ketaconazole?

A

Fungal lanosine demethylase inhibitor

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93
Q

What class of drug is Nizoral?

A

Fungal lanosine demethylase inhibitor

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94
Q

What is the alternative name for Nizoral?

A

Ketaconazole

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95
Q

What is the alternative name for Ketaconazole?

A

Nizoral

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96
Q

How is ketaconazole clinically used?

A

Treats Fungal Infections

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97
Q

What is ketaconazole’s mechanism of action?

A

Inhibits the synthesis of ergosterol, creating pores in the fungal cell membrane

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98
Q

What class of drug is Amoxicillin?

A

Antibiotic

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99
Q

How is Amoxicillin clinically used?

A

Often used in middle ear infections, pneumonia, skin infections, UTIs etc.

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100
Q

What is Amoxicillin’s mechanism of action?

A

Binds to the penicillin binding proteins 1A located inside of the bacterial wall, inhibiting cell wall synthesis leading to cell lysis

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101
Q

What class of drug is Clarithromycin?

A

Antibiotic

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102
Q

How is Clarithromycin used clinically?

A

Used in pneumonia, H pylori infections, Lyme Disease

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103
Q

What is Clarithromycin’s mechanism of action?

A

Binds to rRNA, inhibiting the translation of peptides in bacteria.

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104
Q

What classes of drug does Metronidazole belong to?

A

Antibiotic/Antiprotozoal

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105
Q

How is Metronidazole used clinically?

A

Used for PID, C diff, Bacterial vaginosis

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106
Q

What is Metronidazole’s mechanism of action

A

Inhibits nucleic acid synthesis by disrupting the DNA of microbial cells

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107
Q

What type of antibiotic is Amoxicillin?

A

Bacteriocidal

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108
Q

What type of antibiotic is Metronidazole?

A

Bacteriostatic

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109
Q

What class of drug is Tamoxifen?

A

Oestrogen nuclear hormone receptor antagonist

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110
Q

What is Tamoxifen’s mechanism of action?

A

Pro Drug which competitively antagonises oestrogen receptors

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111
Q

What is Tamoxifen clinically used for?

A

To reduce the size of oestrogen dependant breast tumours

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112
Q

What is are the pharmaceutical names for Yasmin?

A

Ethinylestradiol/Levenorgestrel

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113
Q

How is Levenorgestrel clinically used?

A

Oral contraceptive

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114
Q

What is Ethinylestradiol’s mechanism of action?

A

Increases formation of sex hormone binding globulins, thyroid binding globulins and suppresses follicle stimulating hormone?

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115
Q

What is Levenorgestrel’s mechanism of action?

A

Increases formation of sex hormone binding globulins, thyroid binding globulins and suppresses follicle stimulating hormone?

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116
Q

How is Ethinylestradiol clinically used?

A

Oral contraceptive

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117
Q

What pharmacological effect does ethanol have on health?

A

Cellular depressant used as behaviour altering substance

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118
Q

What is ethanol’s believed mechanism of action?

A

Believed to act on to alter both GABA and glutamate receptors

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119
Q

What is the alternative name for diamorphine?

A

Heroin

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120
Q

What class of drug is heroin?

A

Mu Opiate Receptor Agonist/ Analgesic

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121
Q

True or false? Diamorphine is a recreational drug.

A

True (a.k.a. Heroin)

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122
Q

What is diamorphine’s mechanism of action?

A

Agonist to beta-endorpine, dynorphin, leu-enkephalin and met-enkephalin, so reduces pain

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123
Q

What class of drug is cocaine?

A

Noradrenaline reuptake inhibitor/sodium channel blocker

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124
Q

Is codeine a recreational drug?

A

Yes

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125
Q

What is codeine’s mechanism of action?

A

Inhibits the re-uptake of seratonin, dopamine and noradrenaline, so greater concentrations are available causing euphoric effects.

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126
Q

What is interesting about codeine?

A

Can cross the blood brain barrier

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127
Q

What type of drug is nicotine?

A

Nicotinic cholinergic receptor agonist

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128
Q

What is nicotine’s mechanism of action?

A

Binds to nicotinic acetylcholine receptors on dpoaminergic neurons in the cortico-limbic pathways of the brain. This leads to release of dopamine into synpase - produces euphoric and addictive properties of nicotine.

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129
Q

How does nicotine have an effect on adrenaline levels?

A

It binds to nicotinic receptors in adrenal medulla, depolarising them, which causes release of adrenaline.

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130
Q

What type of drug is atenolol?

A

Beta adrenoreceptor antagonist

Beta Blocker

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131
Q

What effect does atenolol have on the heart?

A

Reduces heart rate, blood pressure and cardiac output

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132
Q

What is atenolol’s mechanism of action?

A

Competes with adrenalin and noradrenalin for binding at beta-1 adrenergic receptor thus reduced heart rate

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133
Q

What function do propanolol and atenolol have in common?

A

They’re both beta blockers (beta adrenoreceptor antagonists)

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134
Q

How is propanolol used clinically?

A

Treatment of ischemic heart disease, heart failure.

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135
Q

What is propanolol’s mechanism of action?

A

Non-selective beta blocker, blocks action of both adrenalin and noradrenalin thus reducing heart rate.

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136
Q

What type of drug is bendro-flumethiazide?

A

Sodium chloride co-transporter inhibitor/ Thiazide diuretic

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137
Q

How is bendro-fumethiazide used clinically?

A

Used to treat high blood pressure

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138
Q

What is bendro-flumethiazide’s mechanism of action?

A

Inhibits sodium re-absorption

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139
Q

What class of drug is amiodarone?

A

Potassium Channel Blocker

Vaughan-Williams Class III antiarrythmic agent

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140
Q

How is amiodarone clinically used?

A

To treat ventricular and atrial fibrillation

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141
Q

What is amiodarone’s mechanism of action?

A

Blocking K+ channels delays cell repolarisation, so increase in length of action potential and increase in effective refractory period so decreased heart rate.

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142
Q

Does amiodarone only have an effect on K+ receptors?

A

No.

Capable of blocking sodium, potassium, calcium and beta receptors.

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143
Q

What type of drug is Captopril?

A

ACE inhibitor

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144
Q

What does the ‘ACE’ in ‘ACE inhibitor’ stand for?

A

Angiotensin converting enzyme

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145
Q

How is captopril used clinically?

A

Treatment of high blood pressure

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146
Q

What is captopril’s mechanism of action?

A

Prevents Angiotensin I being converted to Angiotensin II by inhibiting angiotensin converting enzyme.

This decreases the water retentive and vasodilative effects of angiotensin II so decreases blood pressure.

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147
Q

What type of drug is verapamil?

A

Calcium Channel Blocker

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148
Q

How is Verapamil used clinically?

A

Treatment of high blood pressure and angina

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149
Q

What is Verapamil’s mechanism of action?

A

Antagonises calcium channels, so blocks the influx of calcium across the cell membrane of arterial smooth muscle and myocardial cells.
Reduced afterload so reduced blood pressure

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150
Q

What type of drug is digoxin?

A

Sodium potassium ATPase inhibitor

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151
Q

How is digoxin used clinically?

A

Treats low blood pressure

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152
Q

What is digoxin’s mechanism of action?

A

Causes a reversal of the ATPase pump so increased amounts of calcium during each action potential in cardiac muscle. Increased contractility without increasing heart energy expenditure

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153
Q

What type of drug is Phenoxybenzamine?

A

Alpha adrenoceptor antagonist/ Antihypertensive

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154
Q

What is Phenoxybenzamine clinically used for?

A

Increasing blood pressure

Controlling manifestations of autonomic hyperreflexia in patients with spinal cord transection

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155
Q

What is Phenoxybenzamine’s mechanism of action

A

Blocks alpha receptors, leading to a muscle relaxation and a widening of the blood vessels. This widening results in a lowering of blood pressure.

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156
Q

What type of drug is Prazosin?

A

Alpha adrenoceptor antagonist

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157
Q

How is Prazosin used clinically?

A

Treats hypertension and congestive heart failure

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158
Q

What is Prazosin’s mechanism of action?

A

Inhibits postsynaptic a-1 adrenoceptors on vascular smooth muscle, inhibiting the vasoconstriction that circulating adrenaline and noradrenaline would cause, resulting in peripheral vasodilation.

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159
Q

What type of drug is atropine?

A

Muscarinic cholinergic receptor anatagonist

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160
Q

What is atropine clinically used for?

A

Panic disorders (reduces sweating and spasms)

Increases heart rate

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161
Q

What is atropine’s mechanism of action?

A

Binds to Ach receptors, preventing the binding and action of Ach.
Reduces action of the parasympathetic nervous system which results in dilated pupils and increased heart rate.

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162
Q

What type of drug is norepinephrine?

A

Alpha adrenoreceptor Agonist

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163
Q

What is norepinephrine more commonly known as?

A

Adrenaline

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164
Q

When is norepinephrine used clinically?

A

In emergency situations

For life-threateningly low blood pressure

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165
Q

What is norepinephrine’s mechanism of action?

A

Acts on alpha-1 adreno receptors in blood vessels to cause vasoconstriction and increase blood pressure

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166
Q

What class of drug is epinephrine?

A

Non-selective adrenergic agonist

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167
Q

When is Epinephrine clinically administered?

A

In cases of Anaphylaxis, Cardiac Arrest and Superficial bleeding

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168
Q

What is Epinephrine’s mechanism of action?

A

Acts on all major subtypes of adrenergic receptors causing a multitude of effects including increased heart rate.

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169
Q

What type of drug is dobutamine?

A

Beta-adrenoreceptor agonist

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170
Q

What is Dobutamine’s mechanism of action?

A

Directly stimulates beta-1 receptors of the heart to increase myocardial l contractility and stroke volume - leading to increased cardiac output

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171
Q

What are the side effects of Dobutamine?

A

Produces mild chronotropic, hypertensive, arrhythmogenic and vasodilative effects.

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172
Q

What type of drug is Isoprenaline?

A

Non-selective beta 1 and 2 adrenergic agonist

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173
Q

How is isprenaline used clinically?

A

Treatment of bradycardia (slow heart rate), heart block, and rarely for asthma

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174
Q

What is the trivial/brand name for salbutamol?

A

Ventolin Inhaler

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175
Q

What is the chemical name for ventolin?

A

Salbutamol

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176
Q

What type of drug is salbutamol?

A

Short Acting Beta-2 adrenoreceptor agonist (SABA)

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177
Q

What is salbutamol clinically used for?

A

Treats asthma

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178
Q

What is salbutamol’s mechanism of action?

A

Stimulation of SABA receptors leads to high levels of cyclic AMP which relaxes bronchial smooth muscle and decreases airway resistance. Also decreases release of histamine.

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179
Q

What type of drug is salmeterol?

A

Long Acting Beta adrenoceptor agonist (LABA)

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180
Q

What is salmeterol used for clinically?

A

Treats asthma and COPD symptoms

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181
Q

What is the difference between salbutamol and salmeterol?

A

Salbutamol is a short acting B2 adrenoreceptor agonist

Salmeterol is a long acting B2 adrenoreceptor agonist

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182
Q

What type of drug is orlistat?

A

Lipase inhibitor

183
Q

What is orlistat used for clinically?

A

Treating obesity

184
Q

What is orlistat’s mechanism of action?

A

Prevents breakdown of triglycerides in the intestine, so they are simply excreted.

185
Q

What type of drug is atorvostatin?

A

Statin/ Competitive inhibitor of HMG-CoA reductase

186
Q

What is atorvostatin’s mechanism of action?

A

Inhibits HMG-CoA which normally aids in cholesterol synthesis. Decreased LDL uptake by hepatocytes. Also reduced blood levels of triglycerides and increases levels of HDL. (Cholesterol excreted)

187
Q

How is atorvostatin used clinically?

A

Lowers blood cholesterol and treats CVD

188
Q

What type of drug is Bezafibrate?

A

Fibrate

189
Q

What is Bezafibrate used for clinically?

A

To lower blood cholesterol and triglycerides

190
Q

What is Bezafibrate’s mechanism of action?

A

Stimulates the action of 2 enzymes ( lipoprotein lipase and hepatic lipase) that break down triglycerides. Reduces production of triglycerides in the liver.

191
Q

What type of drug is Hydroxycobalamin?

A

Co-enzyme/ Vitamin precursor

192
Q

What is Hydroxycobalamin used for clinically?

A

Used to treat Vitamin B12 deficiency (megaloblastic anaemia)

193
Q

What is vitamin B9 more commonly known as?

A

Folic acid/ Folate

194
Q

What is vitamin B9 used for clinically?

A

Used to treat Folic Acid deficiency (megaloblastic anaemia), given in pregnancy

195
Q

What is vitamin B9’s mechanism of action?

A

Biochemically inactive so it’s converted to tetrahydrofolic acid and methyltetrahydrofolate by dihydrofolate reductase which are used to maintain normal erythropoiesis.

196
Q

What type of drug is Ferrous sulphate?

A

Oxidation Modulator

197
Q

What is Ferrous sulphate used for clinically?

A

Used to treat iron-deficiency anaemia

198
Q

What is Ferrous sulphate’s mechanism of action?

A

Passes through the GI mucosal cells directly into the blood and binds to transferrin. This transports iron into the bone marrow where it is incorporated into haemoglobin.

199
Q

How is Ferrous sulphate best absorbed?

A

With vitamin C

200
Q

What type of drug is warfarin?

A

Vitamin K Antagonist/ Anti-coagulant

201
Q

How is warfarin used clinically?

A

Used to treat blood clots

202
Q

What is warfarin’s mechanism of action?

A

Depletes the recycling of Vitamin K epioxide back into active Vitamin K by inhibiting an enzyme which aids in the reaction. Therefore inhibits the vitamin K dependent synthesis of clotting factors.

203
Q

What type of drug is clopidogrel?

A

Anti-platelet drug/ Pro-drug

204
Q

What is clopidogrel used for clinically?

A

Used to protect against strokes and heart attacks

205
Q

What is clopidogrel’s mechanism of action

A

Irreversibly inhibits a receptor called P2Y, an ADP chemoreceptor on platelet cell membranes.

Platelet activation and cross-linking by fibrin can no longer happen so platelets can’t stick together and clots can’t form.

206
Q

What type of drug is Heparin?

A

Anti-coagulant

207
Q

What is heparin used for clinically?

A

Treating DVT, pulmonary embolisms and venous thromboembolisms

208
Q

What are the two types of heparin?

A

Unfractionated (UFH)

Low molecular weight (LMWH)

209
Q

How does unfractionated heparin work?

A

UFH binds to anti-thrombin causing conformational change which increases affinity for clotting factor FXa and thrombin and inactivates them. Forms a tertiary complex between AT, thrombin and heparin to inactivate thrombin.

210
Q

How does low molecular weight heparin work?

A

It forms the same complex as UFH, but can only inactivate FXa (not thrombin)

211
Q

What type of drug is Lepirudin?

A

Anti-coagulant

212
Q

How is Lepirudin used clinically?

A

DISCONTINUED - Was used in patients previously treated with heparin, but have developed heparin-induced thrombocytopenia.

213
Q

What is Lepirudin’s mechanism of action?

A

Binds to thrombin, directly inhibiting blood clotting.

214
Q

What type of drug is Chlorpromazine?

A

Dopamine Antagonist/ Anti-emetic/ Anti-Psychotic

215
Q

What is chlorpromazine’s mechanism of action?

A

Blocks the action of dopamine in the chemical trigger zone, the cortical and limbic areas of the brain as well as the gut.

216
Q

Does chlorpromazine only target dopamine receptors?

A

Nope.

Also blocks action of 5-HT, histamine etc…

217
Q

What is chlorpromazine’s mechanism of action?

A

Increasing gut motility
Relieving nausea
To treat psychosis

218
Q

What type of drug is Domperidone?

A

D2 and D3 Antagonist/ Anti-emetic

219
Q

What is Domperidone clinically used for?

A

Increases GI peristalsis and lactation

220
Q

What is Domperidone’s mechanism of action?

A

Blocks dopamine receptors at the chemoreceptor trigger zone and in the duodenum.

221
Q

What type of drug is Metoclopramide?

A

Dopamine D2 Receptor Antagonist/ Antiemetic

222
Q

What is Metoclopramide’s mechanisms of action?

A

Blocks the action of dopamine in the chemical trigger zone

223
Q

What is metoclopramide used for clinically?

A

Relieving nausea and increasing gut motility

224
Q

What type of drug is Perphenazine?

A

D2 receptor Antagonist/ Anti-emetic/ Anti-Psychotic/ Phenothiazine.

225
Q

What is Perphenazine used for clinically?

A

Treats violent morning sickness in pregnant women and the positive symptoms of Schizophrenia

226
Q

What is Perphenazine’s mechanism of action?

A

Acts at all levels of the CNS, though the specific sites and actions are unknown.

227
Q

What type of drug is Cinnarizine?

A

Selective histamine antagonist/ Calcium channel blocker/ Anti-emetic

228
Q

What is Cinnarizine’s mechansim of action?

A

Binds to receptors (dopamine, histamine) to inhibit smooth muscle contraction

229
Q

What type of drug is Cyclizine?

A

H1 receptor antagonist/ Anti-emetic

230
Q

What is Cyclizine’s mechanism of action?

A

Mechanism of action to reduce nausea is poorly understood, may act at the CTZ.

231
Q

What type of drug is promethazine?

A

Competitive H2 receptor antagonist/ Anticholinergic/ Sedative/ Anti-emetic

232
Q

Why type of drug is Hyoscine?

A

Muscarinic antagonist

233
Q

What is Hyoscine used for clinically?

A

Used for treating spasms in the G.I. and G.U. tracts and treating motion sickness

234
Q

What is Hyoscine’s mechanism of action?

A

Inhibits communication between the vestibule and vomiting centre

235
Q

What type of drug is Ondansetron

A

Serotonin 5-HT3 receptor antagonist/ anti- emetic

236
Q

What is Ondansetron used for clinically?

A

Used particularly in chemotherapy, postoperation and radiation

237
Q

What is Ondansetron’s mechanism of action?

A

Prevents the action of sertonin on the vagus nerve and in the CTZ.

238
Q

What type of drug is Esomeprazole?

A

Proton-pump inhibitor (PPI)

239
Q

What is Esomeprazole used for clinically?

A

Peptic ulcers and reflux

240
Q

What is Esomeprazole’s mechanism of action?

A

Inhibits an enzyme involved at the H+/K+ ATPase pump at the secretory surface of the gastric parietal cell resulting in reduced secretion of gastric acid.

241
Q

What is special about Esomeprazole and Omeprazole?

A

They’re mirror images/ chiral isomers

242
Q

What type of drug is Omeprazole?

A

PPI

243
Q

What is omeprazole clinically used for?

A

Peptic ulcers and reflux

244
Q

What is omeprazole’s mechanism of action?

A

Reduced secretion of gastric acid through H+/K+ ATPase by inhibiting an enzyme involved at the pump at the secretory surface of the gastric parietal cell.

245
Q

What type of drug is Ranitidine?

A

H2 receptor antagonists

246
Q

What is Ranitidine used for clinically?

A

Peptic ulcers and reflux

247
Q

What is Ranitidine’s mechanism of action?

A

Stops histamine stimulation of parietal cells.

248
Q

What type of drug is Magnesium Trisilicate?

A

Antacid/ Laxative

249
Q

What is Magnesium Trisilicate’s mechanism of action?

A

Neutralises pH of gastric juice as it is an alkali. Also coats the GI mucosa protecting it in the future.

250
Q

What type of drug is Misoprostol?

A

Prostaglandin

251
Q

How is Misoprostol used clinically?

A

Prescribed with NSAIDs to protect stomach from injury.

Used in inducing labour and can also cause abortions.

252
Q

What is Misoprostol’s mechanism of action?

A

Replaces the PGs lost in NSAID use. Stimulates increased secretion of the protective mucus that lines the GI tract and increases mucosal blood flow, increasing mucosal resistance to injury. Also inhibits gastric acid and pepsin secretion.

253
Q

What type of drug is Gaviscon?

A

Antacid

254
Q

What is Gaviscon clinically used for?

A

Indigestion

255
Q

What is Gaviscon’s mechanism of action

A

Contains alkaline ions which neutralise stomach gastric acid. Contains an alkaline ion (bicarbonate but may also be hydroxide) and a counterion (calcium/ sodium)

256
Q

What type of drug is Azathioprine?

A

Immunosuppressive/ / Pro-drug

257
Q

What is Azathioprine used for clinically?

A

Used in organ transplantation and autoimmune diseases

258
Q

What is Azathioprine’s mechanism of action?

A

Converted into mercaptopurine which inhibits an enzyme required for the synthesis of DNA.. Most strongly affects proliferating cells, such as the T and B cells.

259
Q

What type of drug is Cyclosporine?

A

Immunosuppressant

260
Q

What is Cyclosporine used for clinically?

A

Used to prevent organ transplantation rejection (often administered IV)

261
Q

What is Cyclosporine’s mechanism of action?

A

Exerts specific and reversible inhibition of immunocompetent lymphocytes in the G0-G1 phase of the cell cycle. T-lymphocytes are preferentially inhibited. T1-helper cell is the main target. Inhibits interleukin release.

262
Q

What type of drug is Levodopa?

A

Dopamine precursor

263
Q

What is Levodopa used for clinically?

A

Used in treatments of Parkinson’s, causes lots of side effects.
Side effects include schizophrenic symptoms

264
Q

What is levodopa a precursor for?

A

The neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine.

265
Q

What type of drug is Imipramine?

A

Catecholamine uptake inhibitor/ Anti-depressant

266
Q

What is Imipramine’s mechanism of action?

A

Binds the sodium-dependent serotonin and norepinephrine transporters, reducing the re-uptake of norepinephrine and serotonin by neurones.

267
Q

What is Imipramine used for clinically?

A

Depression

268
Q

What type of drug is Dopamine?

A

Dopamine receptor agonist/ Catecholamine

269
Q

What is Dopamine’s mechanism of action?

A

Acts in the brain for reward motivated behaviour. Also acts in various other places around the body.

270
Q

What type of drug is Fluoxetine?

A

Selective Serotonin reuptake inhibitor (SSRI)/ Antidepressant

271
Q

What is the trivial/ brand name for fluoxetine?

A

Prozac

272
Q

What is Prozac’s mechanism of action?

A

Metabolized to norfluoxetine, it blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors.

273
Q

What is better about fluoextine in comparison to other SSRIs?

A

It has fewer extra-pyramidal side effects

274
Q

What type of drug is Phenelzine?

A

Monoamine oxidase inhibitor/ Antidepressant/ Anxiolytic

275
Q

What is Phenelzine’s mechanism of action?

A

Inhibits the enzyme which breaks down various neurotransmitters. Leads to an increase in the amount of neurochemicals causing anti-depressive and anxiolytic effects

276
Q

What type of drug is Diazepam?

A

GABA Receptor Agonist/ Benzodiazepine/ Muscle relaxant

277
Q

What is an alternative name for Diazepam?

A

Valium

278
Q

What is Diazepam used for clinically?

A

Used to treat anxiety.

279
Q

What is Valium’s mechanism of action?

A

Attaches to GABA on the receptors, increasing the total conduction of chloride ions across the membrane, making firing less likely.

280
Q

What type of drug is Buspirone?

A

5HT partial receptor agonist

281
Q

What is an alternative name for Buspirone?

A

Azapirone Psychotropic Drug

282
Q

What is Buspirone used for clinically?

A

Treats generalised anxiety disorder

283
Q

What is Buspirone’s mechanism of action?

A

Increases the action of serotonin which causes anxiolytic effects. Also antagonises dopamine and nordrenalin receptors. Less risk of dependence than benzodiazepines’s or barbituates.

284
Q

What type of drug is Chlopromazine?

A

Dopamine Receptor Antagonist/ Antipsychotic

285
Q

What is Chlopromazine used for clinically?

A

Treats Schizophrenia and Bipolar disorder

286
Q

What is Chlopromazine’s mechanism of action?

A

Blocks D1-D4 and 5-HT1 and 5-HT2 receptors (and others), causing anxiolytic and anti-aggressive properties.

287
Q

Why is Chlopromazine a ‘typical antipsychotic’?

A

Less extrapyramidal side effects than other antipsychotics

288
Q

What type of drug is Haloperidol?

A

Dopamine Receptor Antagonist/ Antipsychotic

289
Q

What is C used for clinically?

A

Treats schizophrenia and Tourette’s

290
Q

What is Haloperidol’s mechanism of action?

A

Binds to D2 and alpha1 receptors to antagonise them thus reducing the availability of dopamine.

291
Q

Why is Haloperidol a ‘typical psychotic’?

A

Little affinity for histamine and Ach receptors causes less extrapyramidal side effects.

292
Q

What type of drug is Risperidone?

A

Dopamine and 5HT Antagonist/ Multi-target, atypical antipsychotic

293
Q

What is Risperidone used for clinically?

A

Treats Schizphrenia, Bipolar and also used in people with Autism.

294
Q

What is Risperidone’s mechanism of action?

A

Long half life on Dopamine Receptors. Blocks 5HT for negative symptom control. Also acts on adrenalin receptors and Histamine receptors to cause drowsiness and also aid with symptom control

295
Q

What type of drug is Amitryptyline?

A

Noradrenaline/5HT reuptake inhibitor/ Tricyclic Antidepressant

296
Q

What is Amitryptyline used for clinically?

A

Treats generalised anxiety major depressive disorder.

297
Q

What is Amitryptyline’s mechanism of action?

A

Blocks the reuptake of noradrenaline and 5HT to increase the availability of the neurotransmitters. Little effect on dopamine receptors.

298
Q

What type of drug is Lithium?

A

Sodium Analogue/ Mood Stabiliser

299
Q

What is Lithium used for clinically?

A

Counteracting both mania and depression

300
Q

What is Lithium’s mechanism of action?

A

Precise mechanism currently unknown. Possibly interacts with transport of monovalent or diavalent cations in neurons. Also changes glutamate currents.

301
Q

What type of drug is Methylphenidate?

A

Noradrenaline/Dopamine Releaser.

Noradrenalin-Dopamine Reuptake Inhibitor (NDRI)/ CNS Stimulant

302
Q

What is the alternative name for Methylphenidate?

A

Ritalin

303
Q

What is Ritalin used for clinically?

A

Treats ADHD and narcolepsy

304
Q

What is Ritalin’s mechanism of action?

A

Increases availability at receptors by blocking re-uptake. Shares part of structure with catecholamines.

305
Q

What type of drug is Dexamefetamine ?

A

Noradrenaline releaser/ CNS stimulant and amphetamine enantiomer.

306
Q

What is Dexamefetamine clinically used for?

A

Prescribed for ADHD and narcolepsy

307
Q

What type of drug is Naloxone ?

A

Opiate Receptor Antagonist

308
Q

What is Naloxone clinically used for?

A

Reversing the effects of opoid medication.

309
Q

What is Dexamefetamine ‘s mechanism of action?

A

Agonising GPCR causes the release of dopamine, norepinephrine and serotonin.

310
Q

What is Naloxone’s mechanism of action?

A

Competitively antagonising opiod receptors

311
Q

What is oxygen used for clinically?

A

Used as an emergency treatment for severely low oxygen levels

312
Q

What is important about oxygen administration?

A

Various concentrations available; have to be careful with people who have chronic low oxygen because this can make their levels too high

313
Q

What type of drug is Thalidomide?

A

Anti-angiogenic/Immunosuppressive/VEGF inhibitor

314
Q

What is Thalidomide used for clinically?

A

Used for treatments of tumours

2 enantiomers - one that is effective against morning sickness and the other that is teratogenic

315
Q

Are the mechanisms of Thalidomide understood?

A

No

316
Q

What type of drug is the tetanus booster?

A

Antibody stimulator

317
Q

What are the tetanus booster’s mechanisms of action?

A

Inactivated toxic compounds from micro-organisms are injected to artifically activate immunization against tetanus

318
Q

What type of drug is Lidocaine?

A

Sodium channel blocker/ Anaesthetic

319
Q

What is lidocaine used for clinically?

A

Local anaesthetic agent used in dental procedures, can be combined with adrenaline

320
Q

What is lidocaine’s mechanism of action?

A

Mimics the actions of endogenous neuropeptides primarily via kappa opioid receptors (but also via mu- receptors), producing the characteristic morphine -like effects.

321
Q

What class of drug is methicillin?

A

Transpeptidase inhibitor

322
Q

What is methiciliin’s mechanism of action?

A

Inhibits bacterial cell wall synthesis by binding to the enzyme used to cross link the peptide used in peptidoglycan synthesis.

323
Q

What is methicillin used for clinically?

A

It isn’t. Its role has been replaced by flucloxacillin and dicloxacillin.

324
Q

What class of drug is cefuroxime?

A

transpeptidase inhibitor

325
Q

What is cerfuroxime’s mechanism of action?

A

Binds to and inhibits the enzyme that cross links the peptide chain for peptidoglycan.

326
Q

What pathogens is cerfuroxime targeted at?

A

Beta-lactamase-producing H.influenza and N.gonorrhoea.

327
Q

What conditions is cerfuroxime used for clinically?

A

Sinusitis
Ear infections
Lower respiratory tract infections
Urinary infections

328
Q

What are common side effects of cerfuroxime?

A

Hypersensitivity reactions

GIT disturbances

329
Q

What class of drug is benzylpenicillin?

A

Transpeptidase inhibitor

330
Q

Give examples of transpeptidase inhibitors

A

Methicillin
Cerfuroxime
Benzylpenicillin

331
Q

Are transpeptidase inhibitors bacteriostatic or bactericidal?

A

Bactericidal

332
Q

What is the common mechanism of action for transpeptidase inhibitors?

A

Binding to and inhibiting the enzyme that cross links the peptide chain for peptidoglycan, a component of the cell wall.

333
Q

What is benzylpenicillin used for clinically?

A

Streptococcal, gonococcal and meningococcal infections
Anthrax
Diphtheria
Gangrene

334
Q

What infectious agent is resistant to benzylpenicillin?

A

Staphylococcus

335
Q

Is oxytetracycline a broad or narrow spectrum antibiotic?

A

Broad spectrum

336
Q

What class of drug is oxytetracycline?

A

30s inhibitor

337
Q

What class of drug is erythromycin?

A

50s inhibitor

338
Q

What class of drug is gentamicin?

A

30s/50s inhibitor

339
Q

Are 30s/50s inhibitors bacteriostatic or bactericidal?

A

Bacteriostatic

340
Q

What is gentamicin’s mechanism of action?

A

Causes misreading of the mRNA message via abnormal codon: anticodon recognition. This then leads to the production of abnormal proteins.

341
Q

What is erythromycin’s mechanism of action?

A

Inhibits the translocation of the transfer RNA from the A site to the P site.

342
Q

If gentamicin is used for staph infections, what must it be used with?

A

A beta-lactam antibiotic

343
Q

What class of drug is rifampicin?

A

DNA dependent RNA polymerase inhibitor

344
Q

What is rifamicin’s mechanism of action?

A

Inhibits bacterial but not human DNA dependent RNA polymerase, causing reduced RNA synthesis in the bacterial cell.

345
Q

Is rifampicin bacteriostatic or bactericial?

A

Bactericidal

346
Q

What is rifampicin used for clinically?

A 
Tuberculosis
Leprosy
Meningococcal meningitis prophylaxis
Endocarditis
Legionnaires
Serious staph infections
347
Q

What are the side effects of rifampicin?

A

Reduces the effect of anticoagulants and oral contraceptives

348
Q

What class of drug is trimethoprim?

A

Folate antagonist

349
Q

What is trimethoprim’s mechanism of action?

A

Inhibits dihydrofolate reductase and therefore the conversion of folate to tetrahydrofolate. This stops DNA synthesis.

350
Q

What is trimethoprim used for clinically?

A

Prostatitis
UTIs
Respiratory infections

351
Q

What class of drug is sulfamethoxazole?

A

PABA analogue

352
Q

What class of drug is vancomycin?

A

Peptidoglycan inhibitor

353
Q

What is sulfamethoxazole’s mechanism of action?

A

Completely inhibits dihydropteroate synthetase, stopping DNA synthesis

354
Q

What is vancomycin’s mechanism of action?

A

Inhibits removal of an amino acid from a building block in peptidoglycan formation, so the building blocks don’t have enough energy to link up.

355
Q

What is vancomycin used for clinically?

A

MRSA infections

Pseudo-membranous colitis

356
Q

What class of drug is colistin?

A

Phospholipid detergent

357
Q

What is colistin’s mechanism of action?

A

Penetrates into and disrupts the bacterial cell membrane. It also messes up the membrane’s permeability.

358
Q

What is colistin used for clinically?

A

Infections caused by sensitive strains of gram negative bacilli.

359
Q

What class of drug is ciprofloxacin?

A

Topoisomerase II inhibitor

360
Q

Is colistin bacteriostatic or bactericidal?

A

Bactericidal

361
Q

Is ciprofloxacin bacteriostatic or bactericidal?

A

Bactericidal

362
Q

What is ciprofloxacin’s mechanism of action?

A

Inhibits topoisomerase II and IV which are needed for DNA replication, transcription, repair, supercoiling repair and recombination in bacteria.

363
Q

What is ciprofloxacin used for clinically?

A 
UTIs
Cystitis
Prostatitis
Lower respiratory tract infections
Sinusitis
Skin bone and joint infections
364
Q

What class of drug is fusidic acid?

A

Translocation inhibitor

365
Q

What is fusidic acid’s mechanism of action?

A

Interferes with bacterial protein synthesis by preventing translocation of the elongation factor G (EF-G) from the ribosome

366
Q

Is fusidic acid bacteriostatic or bactericidal?

A

Bacteriostatic

367
Q

What class of drug is ibruprofen?

A

NSAID

368
Q

What is ibruprofen’s mechanism of action?

A

Reversible inhibition of COX 1, weak inhibition of COX 2

369
Q

What class of drug is acyclovir?

A

Antiviral

370
Q

What is acyclovir’s mechanism of action?

A

Converted by viral and host cell kinases to acyclovir triphosphate which selectively inhibits viral DNA polymerase.

371
Q

What is acyclovir used for clinically?

A

Herpes simples and herpes zoster infections

372
Q

What class of drug is amantidine?

A

Antiviral

Antiparkinsonian

373
Q

What is amantidine’s mechanism of action?

A

Believed to increase dopamine release from nerve endings in the striatum. May also have antimuscarinic effects.

374
Q

What is amantidine used for clinically?

A

Parkinson’s disease

Dyskinesia associated with levodopa therapy

375
Q

What class of drug is diamorphine?

A

Analgesic

376
Q

What is diamorphine’s mechanism of action?

A

Activates opioid receptors in the brain and spinal cord to inhibit pain transmission and modify central perception of pain.

377
Q

What is diamorphine used for clinically?

A 
Moderate to severe chronic and post-operative pain
Epidural anaesthesia
Neuropathic pain
Painful cough treatment
Diarrhoea
378
Q

What class of drug is amprenavir?

A

Anti-retroviral, protease inhibitor

379
Q

What is amprenavir’s mechanism of action?

A

Inhibits HIV viral proteinase resulting in non-infectious immature viral particles.

380
Q

What class of drug is phenoxymethylpenicillin?

A

Antibiotic

381
Q

Is phenoxymethylpenicillin bacteriostatic or bactericidal?

A

Bactericidal

382
Q

What is phenoxymethylpenicillin’s mechanism of action?

A

Binds to and inhibits the enzyme that cross links the peptide chain of the newly formed ‘building block’ to the peptidoglycan backbone.

383
Q

What is phenoxymethylpenicillin used for clinically?

A

Streptococcal, gonococcal, meningococcal infections
Anthrax
Diphtheria
Gas gangrene

384
Q

What can’t phenoxymethylpenicillin be used for?

A

Staph infections

385
Q

What class of drug is Zidovudine?

A

Anti-retroviral

386
Q

What is zidovudine’s mechanism of action?

A

Phosphorylated into triphosphate form which interferes with viral DNA synthesis

387
Q

What is zidovudine used for clinically?

A

HIV

388
Q

What is the main problem with zidovudine use?

A

Resistance is likely to occur

Has to be used with other anti-retrovirals

389
Q

Give examples of antibody production stimulators

A

MMR vaccine

Influenza vaccine

390
Q

What class of drug is clotrimazole?

A

Antifungal

391
Q

What is clotrimazole’s mechanism of action?

A

Alters the permeability of the fungal cell wall by binding to phospholipids in the cell membrane. Inhibits sterols needed for cell membrane production.

392
Q

What class of drug is fluconazole?

A

Antifungal

393
Q

What is fluconazole’s mechanism of action?

A

Inhibits a P450 dependent enzyme which is important in sterol conversion and therefore cell membrane production

394
Q

Is fluconazole fungastatic or fungicidal?

A

Fungastatic

395
Q

What is fluconazole used for clinically?

A 
Candidiasis
Tinea infections
Crytococcal meningitis
Histoplasmosis
Blastomycosis
Coccidiomycosis
396
Q

What class of drug is Nystatin?

A

Antifungal

397
Q

What is Nystatin’s mechanism of action?

A

Binds to ergosterol in fungal cell membrane, increasing membrane permeability

398
Q

What is nyastatin used for clinically?

A

GIT candidiasis

399
Q

What class of drug is amphotericin?

A

Antifungal

400
Q

What is amphotericin’s mechanism of action?

A

Kills fungi by binding to the ergosterol in the fungal cell membrane, increasing cell membrane permeability

401
Q

What is amphotericin used for clinically?

A

Candidiasis
meningitis
Histoplasmosis

402
Q

What class of drug is pyrimethamine?

A

Antimalarial

403
Q

What is pyrimethamine’s mechanism of action?

A

Inhibits the malaria parasite’s dihydrofolate reductase (DHFR), interfering with thymidylate synthesis.

404
Q

What is pyrimethamine used for clinically?

A

Combined with sulfadoxine for treatment of Falciparum malaria.

405
Q

What class of drug is quinine?

A

Antimalarial

406
Q

What is quinine’s mechanism of action?

A

Thought to inhibit haem polymerase which would normally degrade haem which in itself is toxic to the parasite.

407
Q

What is quinine used for clinically?

A

Acute attacks of malignant malaria (P. falciparum)

408
Q

What class of drug is artemether?

A

Antimalarial

409
Q

What is artemether’s mechanism of action?

A

Inhibits falciparum sarcoplasmic endoplasmic reticulum calcium ATPase

410
Q

What is artemether used for clinically?

A

Uncomplicated falciparum malaria

411
Q

What class of drug is griseofulvin?

A

Antifungal

412
Q

What is griseofulvin’s mechanism of action?

A

Interacts with polymerised microtubules inhibiting spindle formation

413
Q

What is griseofulvin used for clinically?

A

Fungal infections of the skin, hair and scalp

Trichophyton infections in children

414
Q

What class of drug is clobetasone?

A

Anti-inflammatory

Corticosteroid

415
Q

What is clobetasone used for clinically?

A

Eczema

Dermatitis

416
Q

What class of drug is dacarbazine?

A

Alkylating anticancer agent

417
Q

What is dacarbazine’s mechanism of action?

A

Appears to exert cytotoxic effects, though other theories include DNA synthesis inhibition.

418
Q

Is dacarbazine cell cycle-phase specific?

A

No

419
Q

What id dacarbazine used for clinically?

A

Metastatic malignant melanoma

Secondary line therapy for Hodgkin’s disease

420
Q

What class of drug is cyclophosphamide?

A

Alkylating anticancer agent

421
Q

What is cyclophosphamide’s mechanism of action?

A

Cross-links DNA by forming covalent bonds with guanine residues on each strand which interferes with cell division, thus triggering apoptosis.

422
Q

What is cyclophosphamide used for clinically?

A

Chronic lymphocytic leukaemia
Soft tissue sarcoma
Osteogenic sarcoma
Ovarian and breast cancers

423
Q

What class of drug is rituximab?

A

Cytotoxic anticancer agent

424
Q

What is rituximab ‘s mechanism of action?

A

Binds to the CD20 antigen which leads to selective killing of B cells

425
Q

What is rituximab used for clinically?

A

Treatment of CD20 positive non-Hodgkins lymphoma
Chronic lymphocytic leukaemia
Rheumatoid arthritis

426
Q

What class of drug is doxorubicin?

A

Cytotoxic anticancer agent

427
Q

What is doxorubicin’s mechanism of action?

A

Inhibits DNA and RNA synthesis through topoisomerase II

428
Q

What is doxorubicin used for clinically?

A

Bladder cancers
Acute leukaemias
Hodgkin and non-Hodgkin lymphoma
Breast, ovarian, bladder and bronchi tumours

429
Q

What class of drug is paclitaxal?

A

Mitotic inhibitor

Anticancer agent

430
Q

What is paclitaxal’s mechanism of action?

A

Interferes with the normal function of microtubule growth.

Destroys the cell’s ability to use its cytoskeleton in a flexible manner.

431
Q

What is paclitaxal used for clinically?

A

Kaposi’s sarcoma

Lung, ovarian and breast cancers

432
Q

What is tamoxifen used for clinically?

A

Breast cancer chemotherapy

433
Q

What class of drug is tamoxifen?

A

Oestrogen receptor agonist

434
Q

What is tamoxifen’s mechanism of action?

A

Competes with endogenous oestrogen for the receptor, preventing cell activation and proliferation.

435
Q

What class of drug is 5-fluorouracil?

A

Antimetabolite

Anticancer drug

436
Q

What is 5-fluorouracil’s mechanism of action?

A

Interferes with the synthesis of dTMP and therefore DNA synthesis.
Gives rise to a fraudulent nucleotide.
Inhibits thymidylate synthetase.

437
Q

What is 5-fluorouracil used for clinically?

A

Chemotherapy for GI tract, pancreatic and breast cancers

Malignant skin conditions

438
Q

What is important to note about 5-florouracil administration?

A

High dose regimens should be followed by ‘rescue’ with folinic acid to minimise effects on bone marrow and Gi mucosa.

439
Q

What is folinic acid?

A

A form of tetrahydrofolate

440
Q

What class of drug is etoposide?

A

Anticancer agent

441
Q

What is etoposide’s mechanism of action?

A

Inhibits DNA topoisomerase II, ultimately inhibiting DNA synthesis

442
Q

Is etoposide cell cycle specific?

A

Yes. It mainly affects S and G2.

443
Q

What is etoposide used for clinically?

A 
Chemotherapy for:
Refractory testicular tumours
Small cell lung cancer
Lymphoma
Non-lymphocytic leukaemia
Glioblastoma multiforme
444
Q

Which drug is the first line treatment of small cell lung cancer?

A

Etoposide

445
Q

What class of drug is vinblastine?

A

Vinca alkaloid

446
Q

What is vinblastine’s mechanism of action?

A

Inhibits mitosis at metaphase by binding to tubular in the mitotic spindle, ultimately leading to cell death.

447
Q

What is vinblastine used for clinically?

A 
Chemotherapy for:
Breast cancer
Testicular cancer
Lymphomas
Neuroblastoma
Hodgkin's lymphoma
Non Hodgkin's lymphoma
Mycosis fungicides
Histiocytosis
Kaposi's sarcoma
448
Q

What class of drug is imatinib?

A

Anticancer

Protein kinase inhibitor

449
Q

What class of drug is tretinoin?

A

Retinoid

450
Q

What is tretinoin’s mechanism of action?

A

Binds to retinoids acid receptors, promoting detachment of cornified cells and shedding of corneocytes from the follicle

451
Q

What is tretinoin used for clinically?

A

Acne
Discolouration
Minimising appearance of wrinkles

452
Q

What is imatinib’s mechanism of action?

A

Inhibits protein kinases.

453
Q

What is imatinib used for clinically?

A

Chemotherapy for:
Chronic myeloid leukaemia
Acute lymphoblastic leukaemia
Myeloproliferative diseases

Phase I Medicine (46 decks)

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