Pharmacology Flashcards
pre-synaptic processes
- choline is transported into the terminal by choline transporter (symport with Na+)
- ACh is synthesised in the cytosol with acetyl coenzyme A by choline acetyltransferase
- ACh is concentrated in vesicles by the vesicular ACh transporter
- when an AP causes depolarisation the Ca2+ enters and causes vesicles in active zones to undergo exocytosis
- ACh diffuses into the synaptic cleft and activates nAChR in endplate region
post-synaptic processes
- two ACh molecules activate each nAChR
- channel equally permeable to Na+ and K+
- when the gate opens, Na+ influxes at a faster rate than K+ effluxes
- causes simultaneous opening of many nAChR
describe the structure of nAChR
pentamers of glycoprotein subunits surrounding central cation pore with a gate that only opens when ACh binds
what terminates ACh?
hydrolysis by acetylcholinesterase
examples of clinical conditions associated with the NMJ
- neuromyotonia
- LEMS
- myasthenia gravis
- botox
- curare
describe neuromyotonia
autoantibodies to K+ channels leading to excitability
management of neuromyotonia
anti-convulsant e.g. carbamazepine
phenytoin (Na+ channels)
three classes of drugs used to treat inflammatory arthritis
- NSAIDs
- DMARDs
- biologics
examples of NSAIDs
ibuprofen
diclofenac
role of NSAIDs
anti-inflammatory
adverse of NSAIDs
GI ulceration
CVS
when should DMARDs be started?
within 3 months
examples of DMARDs
methotrexate
leflunomide
sulfasalazine
hydroxychloroquine
adverse of methotrexate
leukopenia
thrombocytopenia
teratogenic
when is hydroxychloroquine used?
connective tissue diseases
examples of biologics
etanercept
infliximab
rituximab
adverse of biologics
risk of infection (TB)
malignancy risk (skin)
contraindicated in pulmonary fibrosis and heart failure
acute gout management
colchicine
NSAIDs
steroids
adverse of colchicine
diarrheoa
prophylaxis of gout
allopurinol
febuxostat
uricosurics
