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PHARMACOLOGY 2 > BLOCK 12 > Flashcards

BLOCK 12 Flashcards

1
Q

what does azathioprine do?

A

it inhibits pruine synthesis which inhibits DNA and RNA synthesis leading to inhibition of cellular proliferation

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2
Q

how does azathioprine work?

A

it incorporates thiopurine analogues into the DNA causing chain termination

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3
Q

what are the indications for azathioprine?

A

autoimmune diseases e.g. myasthenia gravis and crohns

prevention of transplant rejection

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4
Q

what is a common side effect of azathioprine?

A

bone marrow suppression

so in long term treatment you should monitor bloods for signs of myelosuppression

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5
Q

what are contraindications of azathioprine?

A

if taking purine analogues
very low of absent TPMT activity
(as you get older you should reduce the dose)

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6
Q

what enzyme metabolises azathioprine?

A

Thiopurine methyltransferase (TPMT)

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7
Q

what type of drug is diclofenac?

A

an NSAID

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8
Q

what is diclofenacs Moa?

A

inhibits COX1 and COX 2 causing analgesic effects

affects the hypothalamus causing anti-pyretic effects

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9
Q

what are the indications for diclofenac?

A

inflammatory conditions of the oral cavity

can be used for pain, dysmenorrhoea and occular inflammation but naproxen tends to be used instead

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10
Q

what type of drug is celecoxib?

A

NSAID

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11
Q

what is celecoxibs moa?

A

inhibits COX2 causing a reducation in prostaglandins

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12
Q

what does COX 1 do?

A

causes platelet aggregation
reduces HCL secretion in stomach and increases mucus production
causes vasodilation in kidney

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13
Q

what does COX 2 do?

A

production of prostagladins that mediate pain and support the inflammatory response

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14
Q

what are the indications of celecoxib?

A

rheumatoid arthritis, osteoarthritis, familial adenomatous polyposis

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15
Q

what are the effects of cyclophosphamide?

A

antineoplastic and antimmunosuppression

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16
Q

what type of drug is cyclophosphamide?

A

a chemotherapy agent - bifunctional alkylating agent

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17
Q

what are cyclophosphamide’s 3 mechanisms of action?

A

aklyaltion
crosslinking DNA strands
induction of DNA mispairing = mutation

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18
Q

what are the indications for cyclophosphamide?

A

myelomas
leukaemias
rheumatoid arthritis

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19
Q

what are contraindications for celecoxib?

A

acute porphyria
diabetic mellitus
haemorrhagic cystitis
mediastinal irradiation - current or past

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20
Q

what is calcitriol?

A

the active form of vitamin D

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21
Q

how is calcitriol formed?

A

cholecalciferon is converted to 25-hydroxycholecalciferol in the liver by 25-hydroxylase
25-hydroxycholecalciferon is then converted to 1,25-dihydroxycholecalciferol in the kidneys by 1-hydroxylase

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22
Q

how are 25-hydroxycholecalciferol and 1,25-dihydroxycholecalciferol carried around in the blood and why?

A

bound to vitamin D binding protein because theyre both hydrophobic

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23
Q

what is calcitriols effects?

A

increased blood calcium levels by absorbing more from the gut

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24
Q

what are indications for giving vitamin D?

A

vitamin D deficiency or insufficiency
refractory rickets (vitamin D resistant rickets)
familial hypophosphatemia
hypoparathyroidism
management of hypocalcemia
renal osteodystrophy in patients with chronic renal failure undergoing dialysis

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25
Q

what is the ‘gold’ injection called?

A

aurothiomalate

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26
Q

what can chloroquine be used to treat?

A

malaria and rheumatoid arthritis

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27
Q

how does chloroquine treat rheumatoid arthritis?

A

its thught to be able to reduce levels of inflmmatory agents such as IL6 and TNF alpha

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28
Q

whats the moa for methotrextae for treating RA?

A

inhibits folic acid reductase so DNA synthesis cannot proceed due to a lack of purine and pyrimidines so it affects rapidly dividing cells

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29
Q

what type of drug is sulfasalazine?

A

an immunomodulatory agents

DMARD

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30
Q

what type of drug is prednisolone?

A

a glucocorticoid receptor agonist

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31
Q

what is prednisolones moa?

A

can cross cell membranes and bind to corticosteroid receptors which lead to changes in DNA transcription, reducing the production of inflammatory proteins

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32
Q

what are some indications for prednisolone?

A

endocrine, rheumatic, and hematologic disorders; collagen, dermatologic, ophthalmic, respiratory, and gastrointestinal diseases; allergic and edematous states; and other conditions like tuberculous meningitis.

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33
Q

what type of drug is raloxifene?

A

a SERM

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34
Q

outline the moa of raloxifene on bones?

A

it can activate transforming growth factor beta 3 which is a bone matrix protein with antiosteoclastic properties
resulting in reduced bone resorption and icnreased mineral density, slowing the rate of bone los

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35
Q

what is alendronic acid?

A

a nitrogen containing bisphosphonate

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36
Q

what are some indications of alendronic acid?

A

corticosteroid induced osteoporosis and pagets disease and to prevent osteoporosis in postmenopausal women

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37
Q

whats the moa of alendronic acid?

A

inhibition of farnesyl pyrophosphate synthase in osteocasts which reduces their activity, reducing bone resoption and turnover

38
Q

what type of drug is digoxin?

A

a cardiac glycoside (Na+,K+ ATPase inhibitor)

39
Q

what is digoxin used to treat?

A

congestive heart failure and supraventricular arrhythmias

40
Q

what type of drug is betaxolol?

A

beta 1 adrenergic antagonist

41
Q

where are most beta 1 receptors located? what does it bind?

A

within the heart

epinephrine and norepinephrine

42
Q

whats the effect of betaxolol?

A

reduction in HR, CO, systolic and diastolic bp

43
Q

what are the indications of betaxolol?

A

Chronic open-angle glaucoma,

Ocular hypertension

44
Q

what is often used for ischaemic heart disease instead of betaxolol?

A

bisoprolol

45
Q

what type of drug is diazepam?

A

a benzodiazepine

46
Q

how do benzodiazepines work?

A

they bind to benzodiazepine receptors which increases the affinity of GABA, enhancing its effects and opening the CL- channel causing hyperpolarisation and preventing further cell excitation

47
Q

what is diazepam used to treat?

A

muscle spasms
tetanus
anxiety

48
Q

what type of drug is propofol?

A

an IV anaesthetic agent

49
Q

how does propofol work?

A

its a GABA A receptor agonist which enhances opening of Cl- channels and causing hyperpolarization

50
Q

what are the indications of propofol?

A

induction and maintenance of anaesthesia

51
Q

what type of drug is lamotrigine?

A

an anti convulsant

52
Q

how does lamotrigine work?

A

potentially is the inhibition of voltage sensitive Na+ and Ca2+ channels which stabilises neuronal membranes and modulates presynaptic transmitter release of glutamate and aspartate

53
Q

what are the indications of lamotrigine?

A

epilepsy and bipolar disorder

54
Q

what type of drug is carbamazepine?

A

an anticonvulsant

55
Q

how does carbamazepine work?

A

its believed to inhibit sustained repetitive firing by blocking Na+ channels

56
Q

what are the indications of carbamazepine?

A

tonic-clonic seizures
trigeminal neuralgia
diabetic neuropathy

57
Q

what type of drug is phenytoin?

A

an anticonvulsant

58
Q

how does phenytoin work?

A

its a non-specific Na+ channel blocker

59
Q

what type of drug is sodium valproate?

A

an anti-convulsant

60
Q

how may sodium valproate work?

A

1- increases GABA levels in the brain by inhibiting enzymes that catabolise GABA
2- Altering the properties of voltage dependant Na+ channels
3- acts as a histone deacetylase inhibitor

61
Q

what are the indications of sodium valproate?

A

epilepsy or bipolar disorder

62
Q

what type of drug is donepezil?

A

a reversible acetylcholinesterase inhibitor

63
Q

whats the moa of donepezil?

A

reversible inhibition of acetylcholinesterase leading to an increase in acetylcholine at cholinergic synapses, enhancing cholinergic function

64
Q

what are the idnications of donepezil?

A

mild to moderate dementia

65
Q

what type of drug is suxamethonium?

A

a depolarising nicotinic cholinergic receptor antagonist

66
Q

how does suxamethonium work?

A

it mimicks acetylcholine at the neuromuscular junction - its hydrolysed much slower causing depolarisation and therefore desensitisation and muscle relaxation

67
Q

what are the indications of suxamethonium?

A

Neuromuscular blockade (short duration) during surgery and intubation

68
Q

what type of drug is levodopa

A

a dopamine replacement therapy

69
Q

how does levodopa work?

A

its taken orally, crosses the blood brain barrier and in the brain is taken up by dopaminergic neurons and converted to dopamine

70
Q

what are the indications of levodopa?

A

parkinsons

71
Q

what type of drug is bromocriptine?

A

a dopamine agonist

72
Q

what are the indications of bromocriptine?

A

parkinsons
dysfunctions associated with hyperprolactinemia
acromegaly
pulmonary fibrosis

73
Q

what is used instead of bromocriptine for parkinsons and why?

A

pramipexole or ropinirole as there were concerns about fibrotic reactions

74
Q

what type of drug is gabapentin?

A

an anticonvulsant

75
Q

how does gabapentin work?

A

it increases the synaptic cocnentration of GABA and therefore reduces the release of neurotransmitters which reduces axon excitability

76
Q

what are the indications of gabapentin?

A

used less for epilepsy these days

used more for neuropathic pain or as an adjunct in chronic pain syndromes

77
Q

what type of drug is selegiline?

A

dopamine therapy

78
Q

how does selegiline work?

A

irreversibly inhibits monoamine oxidase type B which blocks the metabolism of dopamine within the nigrostriatal pathways of the CNS, enhancing dopaminergic activity in the substantia nigra

79
Q

what are the indications of selegiline?

A

parkinsons disease and potentially depression

80
Q

what type of drug is isoflurane?

A

a general anaesthetic agent

81
Q

what are the indications of isoflurane?

A

induction and maintenance of anaesthesia

82
Q

what type of drug is atracurium?

A

a competitive cholinergic receptor antagonist

83
Q

how does atracurium work?

A

competitively binds to cholinergic receptors on motor end plates, preventing ACh from binding and causing muscle relaxation

84
Q

what reverses the effects of atracurium?

A

acetylcholinesterase inhibitors such as neostigmine or pyridostigmine

85
Q

what are the indications of atracurium?

A

Neuromuscular blockade

86
Q

what type of drug is memantine?

A

an NMDA receptor antagonist

87
Q

how does memantine work?

A

it binds to NMDA rceptor operated cation channels, preventing MG2+ from binding so it protects against chronically elevated concentrations of glutamate

88
Q

what are the idnications of memantine?

A

alzheimers, vascular dementia, chronic pain, psychiatric disorders, mild cognitive impairment

89
Q

what type of drug is fentanyl?

A

an opiod analgesic

90
Q

how does fentanyl work?

A

selectively binds to and activates the mu-receptor in the central nervous system (CNS) thereby mimicking the effects of endogenous opiates.

91
Q

what are the idnications of fentanyl?

A

chronic intractable pain

breakthrough pain

92
Q

NSAIDs offer great pain relief but which 2 drugs are they often used in adjunct with?

A

fentanyl and tramadol

PHARMACOLOGY 2 (7 decks)

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