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PHARMACOLOGY 2 > BLOCK 12 > Flashcards

BLOCK 12 Flashcards

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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
what is the 'gold' injection called?
aurothiomalate
26
what can chloroquine be used to treat?
malaria and rheumatoid arthritis
27
how does chloroquine treat rheumatoid arthritis?
its thught to be able to reduce levels of inflmmatory agents such as IL6 and TNF alpha
28
whats the moa for methotrextae for treating RA?
inhibits folic acid reductase so DNA synthesis cannot proceed due to a lack of purine and pyrimidines so it affects rapidly dividing cells
29
what type of drug is sulfasalazine?
an immunomodulatory agents | DMARD
30
what type of drug is prednisolone?
a glucocorticoid receptor agonist
31
what is prednisolones moa?
can cross cell membranes and bind to corticosteroid receptors which lead to changes in DNA transcription, reducing the production of inflammatory proteins
32
what are some indications for prednisolone?
endocrine, rheumatic, and hematologic disorders; collagen, dermatologic, ophthalmic, respiratory, and gastrointestinal diseases; allergic and edematous states; and other conditions like tuberculous meningitis.
33
what type of drug is raloxifene?
a SERM
34
outline the moa of raloxifene on bones?
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
35
what is alendronic acid?
a nitrogen containing bisphosphonate
36
what are some indications of alendronic acid?
corticosteroid induced osteoporosis and pagets disease and to prevent osteoporosis in postmenopausal women
37
whats the moa of alendronic acid?
inhibition of farnesyl pyrophosphate synthase in osteocasts which reduces their activity, reducing bone resoption and turnover
38
what type of drug is digoxin?
a cardiac glycoside (Na+,K+ ATPase inhibitor)
39
what is digoxin used to treat?
congestive heart failure and supraventricular arrhythmias
40
what type of drug is betaxolol?
beta 1 adrenergic antagonist
41
where are most beta 1 receptors located? what does it bind?
within the heart | epinephrine and norepinephrine
42
whats the effect of betaxolol?
reduction in HR, CO, systolic and diastolic bp
43
what are the indications of betaxolol?
Chronic open-angle glaucoma, | Ocular hypertension
44
what is often used for ischaemic heart disease instead of betaxolol?
bisoprolol
45
what type of drug is diazepam?
a benzodiazepine
46
how do benzodiazepines work?
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
what is diazepam used to treat?
muscle spasms tetanus anxiety
48
what type of drug is propofol?
an IV anaesthetic agent
49
how does propofol work?
its a GABA A receptor agonist which enhances opening of Cl- channels and causing hyperpolarization
50
what are the indications of propofol?
induction and maintenance of anaesthesia
51
what type of drug is lamotrigine?
an anti convulsant
52
how does lamotrigine work?
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
what are the indications of lamotrigine?
epilepsy and bipolar disorder
54
what type of drug is carbamazepine?
an anticonvulsant
55
how does carbamazepine work?
its believed to inhibit sustained repetitive firing by blocking Na+ channels
56
what are the indications of carbamazepine?
tonic-clonic seizures trigeminal neuralgia diabetic neuropathy
57
what type of drug is phenytoin?
an anticonvulsant
58
how does phenytoin work?
its a non-specific Na+ channel blocker
59
what type of drug is sodium valproate?
an anti-convulsant
60
how may sodium valproate work?
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
what are the indications of sodium valproate?
epilepsy or bipolar disorder
62
what type of drug is donepezil?
a reversible acetylcholinesterase inhibitor
63
whats the moa of donepezil?
reversible inhibition of acetylcholinesterase leading to an increase in acetylcholine at cholinergic synapses, enhancing cholinergic function
64
what are the idnications of donepezil?
mild to moderate dementia
65
what type of drug is suxamethonium?
a depolarising nicotinic cholinergic receptor antagonist
66
how does suxamethonium work?
it mimicks acetylcholine at the neuromuscular junction - its hydrolysed much slower causing depolarisation and therefore desensitisation and muscle relaxation
67
what are the indications of suxamethonium?
Neuromuscular blockade (short duration) during surgery and intubation
68
what type of drug is levodopa
a dopamine replacement therapy
69
how does levodopa work?
its taken orally, crosses the blood brain barrier and in the brain is taken up by dopaminergic neurons and converted to dopamine
70
what are the indications of levodopa?
parkinsons
71
what type of drug is bromocriptine?
a dopamine agonist
72
what are the indications of bromocriptine?
parkinsons dysfunctions associated with hyperprolactinemia acromegaly pulmonary fibrosis
73
what is used instead of bromocriptine for parkinsons and why?
pramipexole or ropinirole as there were concerns about fibrotic reactions
74
what type of drug is gabapentin?
an anticonvulsant
75
how does gabapentin work?
it increases the synaptic cocnentration of GABA and therefore reduces the release of neurotransmitters which reduces axon excitability
76
what are the indications of gabapentin?
used less for epilepsy these days | used more for neuropathic pain or as an adjunct in chronic pain syndromes
77
what type of drug is selegiline?
dopamine therapy
78
how does selegiline work?
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
what are the indications of selegiline?
parkinsons disease and potentially depression
80
what type of drug is isoflurane?
a general anaesthetic agent
81
what are the indications of isoflurane?
induction and maintenance of anaesthesia
82
what type of drug is atracurium?
a competitive cholinergic receptor antagonist
83
how does atracurium work?
competitively binds to cholinergic receptors on motor end plates, preventing ACh from binding and causing muscle relaxation
84
what reverses the effects of atracurium?
acetylcholinesterase inhibitors such as neostigmine or pyridostigmine
85
what are the indications of atracurium?
Neuromuscular blockade
86
what type of drug is memantine?
an NMDA receptor antagonist
87
how does memantine work?
it binds to NMDA rceptor operated cation channels, preventing MG2+ from binding so it protects against chronically elevated concentrations of glutamate
88
what are the idnications of memantine?
alzheimers, vascular dementia, chronic pain, psychiatric disorders, mild cognitive impairment
89
what type of drug is fentanyl?
an opiod analgesic
90
how does fentanyl work?
selectively binds to and activates the mu-receptor in the central nervous system (CNS) thereby mimicking the effects of endogenous opiates.
91
what are the idnications of fentanyl?
chronic intractable pain | breakthrough pain
92
NSAIDs offer great pain relief but which 2 drugs are they often used in adjunct with?
fentanyl and tramadol

PHARMACOLOGY 2 (7 decks)

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