Neurology/ MSK Pharmacology Flashcards
1
Q
What should levodopa be prescribed with
A
Dopamine decarboxylase inhibitor (e.g. carbidopa or benserazide) to prevent peripheral metabolism of L-dopa to dopamine
2
Q
Co-beneldopa=
A
(Levodopa + benserazide)
3
Q
Co-careldopa =
A
(Levodopa + carbidopa)
4
Q
MAO of co-beneldopa
A
Increases central dopamine levels; carbidopa/benserazide prevents peripheral breakdown of levodopa.
5
Q
Ix of levodopa + carb inhib
A
PD
6
Q
SE of levodopa
A
Dyskinesia, nausea, hallucinations, postural hypotension.
7
Q
Interactions of leodopa
A
- redued effect with AP
- avoid MAO inhibitors (hypertensive crisis risk).
8
Q
Dopamine receptor agonists
A
Pramipexole, Ropinirole, Rotigotine
9
Q
Mechanism of Pramipexole, ,
A
Stimulate dopamine receptors (D2/D3). Used in PD
10
Q
Mechanism of ropinirole
A
Stimulate dopamine receptors (D2/D3). Used in PD
11
Q
mechanism of rotigotine
A
Stimulate dopamine receptors (D2/D3). Used in PD
12
Q
SE of dopamine receptor agonists
A
Impulse control disorders, nausea, dizziness, hallucinations.
13
Q
MAOB inhobitors
A
- Rasagiline, Selegiline)
- Used in PD
14
Q
Ix of MAO-B inhibitors
A
pd
15
Q
SE of MAOB ihib
A
Insomnia, headache, nausea
16
Q
MAOB interactions
A
- SEROTONIN SYNDROME WITH SSRIS
- avoid tyramine rich foods - cheese. salami, pepperoni, alcohol, fermented products
17
Q
Entacapone MAO
A
- Inhibits catechol-O-methyltransferase → prolongs effect of levodopa.
- used in PD as an adjunct to levodopa
18
Q
SE of entacapone
A
Diarrhoea, orange urine, dyskinesia.
19
Q
Orphenadrine MAO
A
- antimuscarinic used for tremor in PD
20
Q
Procyclidine MAO
A
antimuscarinic used in PD for tremor
21
Q
How do Orphenadrine and Procyclidine work
A
Inhibits muscarinic receptors in CNS → balances cholinergic excess in Parkinson’s.
22
Q
SE of orphenadrine and procyclidine
A
Dry mouth, constipation, urinary retention, confusion.
23
Q
Carbamazepine MAO
A
Inhibits voltage-gated Na+ channels → stabilises neuronal membranes.
24
Q
Phenytoin MAO
A
Inhibits voltage-gated Na+ channels → stabilises neuronal membranes.
25
Lamotrigine MAO
Inhibits voltage-gated Na+ channels → stabilises neuronal membranes.
26
carbamazepine Ix
Trigeminal neuralgia, epilepsy
27
SE of carbamazepine, phenytoun and lamotrigine
sedation, ataxia
28
specific side effect with carbamazepine
hyponatreamia
29
side effect of lamotrigine
rash
30
interactions of carbamazepine, phenytounm lamotrigene
Enzyme inducers → reduce levels of other drugs (e.g., OCPs).
31
MAO of clonazepam, diazepam, lorazapam
Enhance GABA activity at GABA-A receptors → CNS depression.
32
phenobarbital MAO
- barbiturate, CNS depressants.
- enhancement of GABAergic - GABA-A transmission -> prolongs duration that chloride channel is open
- increases chloride influx, hyperpolarises the neuron
33
Indications of benzos and phenobarbital
Epilepsy (esp. status epilepticus for benzodiazepines).
34
SE of clonazepam, diazepam, lorazepam
Sedation, tolerance, dependence, respiratory depression.
35
Vigabatrin MAO
Inhibits GABA transaminase → ↑ GABA.
36
Valproate MAO
Increases GABA + inhibits Na+ channels.
37
Gabapentin/ pregabalin MAO
GABA analogues; inhibit voltage-gated Ca²⁺ channels.
38
other GABA related antieplieptics
- vigabatri
- valproate
- gabapentin/ pregabalin
39
side effect of antieplieptics
Sedation
40
pregabalin SE
Weight gain
41
vigabatrin SE
visual field defects
42
valproate SE
teratogenic, hepatoxic
43
interactions
- Valproate ↑ levels of lamotrigine,
-aspirin may displace valproate
44
topiramate MAO
- Blocks glutamate receptors, Na+ channels.
- antiepileptic
45
ethosuximide MAO
Blocks T-type calcium channels (esp. in absence seizures).
46
Levetiracetam
modulates the presynaptic vesicle protein 2A
47
topiramate Ix
prophylaxis of migraine, epilepsy
48
SE of topiramate
Cog impairment, teratogenicity
49
ethosuximide SE
GI upset
50
levetiracetam SE
Behavioural changes
51
Sumatriptan, Zolmitriptan MAO
Agonist at 5-HT1B/1D → cranial vasoconstriction, inhibits neuropeptide release.
52
Sumatriptan and Zolmitriptan ix
Migraine - acute Tx
53
SE of triptans
Chest pain, dizziness, tingling., nausea
54
interactions of triptans
Avoid with SSRIs/SNRIs (risk of serotonin syndrome), MAOIs.
55
propanolol mechanism
Non-selective β-blocker; modulates vascular tone and central neurotransmission.
56
Ix of propanolol
Migraine prophylaxis
57
SE of propanolo
Fatigue, bradycardia, depression.
58
Propanolol int
Additive bradycardia with verapamil, masks hypoglycaemia.
59
Amitryptiline MAO
Inhibits reuptake of serotonin/noradrenaline.
60
Drugs used in migraine prophylaxis
Amitryptiline, Topiramate, sodium valproate, gabapentin
61
SE of amitriptyline
anticholinergic SE
62
Interactions of amitruptyline
Amitriptyline ↑ sedation with alcohol; caution with serotonergic agents.
63
Z drugs
- non benzo hypntocis: zolpidem, zopiclone
- used for insomnia
64
Mechanism of Zopiclone and Zolpidem
- enhance GABA-A activoty at benzo site
65
SE of zolpidem and zopiclone
Sedation, dizziness, dependence.
66
Benzo used for insomnia
Temazepam
67
Temazepam MAO
Binds to GABA-A receptor → increased GABA effect.
68
Temezapam SE
Tolerance, dependence, drowsiness.
69
Temesepam interactions
Increased sedation with alcohol, opioids.
70
Benzylpenicillin (Penicillin G) MAO
Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), preventing peptidoglycan cross-linking → cell lysis (bactericidal).
71
benzylpenicillin Ix
meningitis
72
SE of benzylpen
- Hypersensitivity reactions (rash, anaphylaxis)
Seizures (at high doses or in renal impairment)
Diarrhoea
73
Ceftriaxone
inhibits cell wall synthesis (bactericidal), cephlasporin
74
SE of ceftrioxone
- diarrhoea
- rash
- HSN reactions
75
Interactions of ceftrioxones
Calcium-containing IV solutions → precipitates (AVOID in neonates!)
76
Cefotaxime
Beta lactam (Cephlasporin) - inhib bacterial cell wall synthesis
77
Cefotaxime iX
Neonatal meningitis (better than ceftriaxone due to safer profile in neonates)
78
Ampicillin MAO
Inhibits cell wall synthesis (bactericidal); broad-spectrum penicillin.
79
ampicillin Ix
- listeria meningitis
- emplirial meningitis Tx
80
Interactions of ampicillin
Allopurinol → ↑ risk of rash
81
Dexamethasone iX
Cerebral oedema (e.g., due to space-occupying lesions), meningitis.
82
dexmeth SE
Hyperglycaemia, mood changes, immunosuppression.
83
Ix of aciclovir
Viral encephalitis (e.g., HSV).
84
SE of aciclovir
Nephrotoxicity (ensure hydration), GI upset.
85
Anticoagulants in stroke
apixaban, wafarin
86
Apixaban MAO
Factor Xa inhibitor (DOAC).
87
apixaban int
CYP3A4 interactions (e.g. amiodarone).
88
alteplase MAO
Recombinant tPA → converts plasminogen to plasmin → clot breakdown.
89
Ix of ateplase
Acute ischaemic stroke (within 4.5 hrs).
90
Aspirin mechanism
Inhibits COX1 and COX2 (COX 1-> inhibits thromboxane A2)
91
Clopidogrel MAO
Inhibits ADP receptor on platelets.
92
dipyridamole MAO
Inhibits phosphodiesterase → ↑ cAMP in platelets.
93
Secondary stroke prevention drugs
Aspirin, Clopidogrel, Dipyridamole
94
statin Ix
secondary prevention post stroke
95
SE of statin
Myopathy, raised LFTs, GI upset.
96
Int of statins
clarithromycin
97
anticholinesterase drugs
- Donepezil, Galantamine, Rivastigmine
- used in alz
98
Mao donezepil
Inhibit acetylcholinesterase → ↑ acetylcholine in CNS.
99
MAO galantimine
Inhibit acetylcholinesterase → ↑ acetylcholine in CNS.
100
MAO rivastigmine
Inhibit acetylcholinesterase → ↑ acetylcholine in CNS.
101
SE of anticholinesterase drugs
bradyria - additive with BB
102
Mematine mechanism
Uncompetitive NMDA receptor antagonist; blocks excessive glutamate activity, reducing excitotoxicity.
103
Ix of mematine
Moderate to severe Alzheimer's disease.
104
SE of mematine
Dizziness, confusion, headache, constipation, hallucinations, agitation.
105
Cautions of mematine
Caution with other NMDA antagonists (e.g., amantadine, ketamine); potential additive effects.
106
Non selective NSAIDs
- ibuprofen and naproxen - Inhibit COX-1 and COX-2 enzymes, reducing prostaglandin synthesis.
`
107
SE of NSAIDs
Gastrointestinal irritation, ulcers, renal impairment, increased cardiovascular risk.
108
Interactions of NSAIs
Increased bleeding risk with anticoagulants;
109
celecoxib MAO
Selective COX-2 inhibition, reducing inflammation with fewer GI effects.
110
Ix of celecoxib
Osteoarthritis, rheumatoid arthritis, acute pain.
111
SE of celecoxib
RI, CVD, sulfonamide allery reactions
112
Interactions of celecoxib
Similar to non-selective NSAIDs; caution with other nephrotoxic agents.
113
DMARDs
- RA
- sulfasalazine
- hydroxychloroquinine
- leflunomide
- methotrexate
- azathioprine
- ciclosporin
- penicillamine
114
sulfasalazine MAO
5-ASA, inhibits prostagladin and leukotriene production
115
ix of sulfasalazine
RA and UC
116
Sulfasazline SE
Rash, GI upset, hepatotoxicity, hematologic abnormalities.
117
hydroxychloroquinine
Ihibits antigen presentation, IL-1 and IL-6
118
hydroxychloroquinine indications
Rheumatoid arthritis, systemic lupus erythematosus.
119
SE of hydroxychloroquinine
- retinal toxicity - bulls eye retinopathy
- QT prolongation
120
Leflunomide MAO
Inhibits dihydroorotate dehydrogenase, reducing pyrimidine synthesis.
121
leflunomide Ix
RA
122
SE of leflunomide
Hepatotoxicity, hypertension, GI symptoms, teratogenicity.
123
interactions of leflunomide
- Increased liver toxicity with methotrexate;
- contraindicated in pregnancy.
124
methotrexate mehanism
Inhibits dihydrofolate reductase, affecting DNA synthesis.
125
se of methotrexate
Bone marrow suppression, hepatotoxicity, pulmonary fibrosis.
126
avoid ? with live vaccines
methotrexate
127
azathioprine MAO
Purine analog; inhibits DNA synthesis, suppressing immune response.
128
se of azathioprine
Leukopenia, hepatotoxicity, increased infection risk.
129
Azathioprine int
alloprinol
130
Ciclosporin MAO
Calcineurin inhibitor; reduces T-cell activation
131
ciclosporin indications
Rheumatoid arthritis, organ transplantation.
132
SE of ciclpsoroin
- Nephrotoxicity,
- hypertension,
- hirsutism,
- gingival hyperplasia.
133
penicillinamine MAO
Chelates heavy metals; modulates immune response.
134
ix of penicillamine
Rheumatoid arthritis, Wilson's disease.
135
adalimumab MAO
: Bind TNF-α, inhibiting its pro-inflammatory effects.
136
Infliximab MAO
TNF-A inhib
137
Etanercept MAO
TNF-A inhib
138
TNF-A Ix
Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis.
139
Key side effect of TNF-A
TB risk (infection in general) screen for TB b4 starting
140
other biologics for RA
- anakinra
- tocilizumab
- abatacept
- rituximab
141
Anakinra MAO
IL-1 antagonist
142
Indications of Anakinra
Rheumatoid arthritis
* Still’s disease
143
SE of anakinra
* Injection site reactions
* Increased risk of infections
* Neutropenia
144
Anakinra Int
* Avoid with TNF inhibitors → ↑ infection risk
145
Tocilizumab MAO
IL-6 Receptor Antagonist)
146
SE of Tocilizumab
* Elevated LFTs
* Neutropenia
* Hyperlipidaemia
* GI perforation (esp. if diverticulitis)
147
Abatacept MAO
* Inhibits CD80/86 on APCs (T cell co-stim modulator) → ↓ T-cell activation
148
SE OF abatacept
* Increased infection risk
* Headache, nausea
149
Int of abatacept
* Increased infection risk
* Headache, nausea
150
Rituximab MAO
Anti-CD20 mab -> Binds CD20 → B-cell depletion
151
rituximab Ix
* RA (with methotrexate), especially if anti-TNF agents ineffective
* Non-Hodgkin lymphoma, CLL
152
Rituximab SE
* Hypogammaglobulinaemia
* Reactivation of HBV
153
colchine MAO
* Inhibits microtubule polymerization → ↓ neutrophil activity & inflammation
154
ix of colchicine
* Acute gout attacks
155
SE of colchicine
* GI upset (nausea, diarrhoea)
* Myopathy, bone marrow suppression (at high doses)
156
Int of colchicine
* Increased toxicity with CYP3A4 inhibitors (e.g. clarithromycin)
* Dose adjust in renal/hepatic impairment
157
allopurinol MAO
* Inhibits xanthine oxidase → ↓ uric acid synthesis
158
allopurinol ix
- Gout prophylaxis
* Tumour lysis syndrome
159
Allopurinol SE
* Rash (including SJS), GI upset
* Hypersensitivity syndrome (especially in renal impairment)
160
Febuxostat MAO
* Non-purine selective xanthine oxidase inhibitor
161
Ix of febuxostat
* Gout prophylaxis (esp. if allopurinol intolerant)
162
SE of febuostat
CVD risk, liver function
163
what also interacts w azathioprine
feboxostat
164
Rasburicase MAO
Recombinant urate oxidase → converts uric acid to allantoin (more soluble)
165
iX OF RUBRICASE
Intravenous prophylaxis against gout during cancer chemotherapy
166
se of rubricase
* Haemolysis (contraindicated in G6PD deficiency)
* Methemoglobinaemia
167
Avoid rasburicase with
other urate-lowering therapies concurrently
168
