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targets
uGaseous
unitrous oxide
uThese factors often determine route of
administration
uSome liquid drugs are easily vaporised and
can be inhaled
uhalothane and amyl nitrate
Copyright UTS, 2017 Slide 14 of 45
Drug Size
uVary from v. small eg lithium (MW
7 daltons) Rx bipolar depression, to
uV. Large eg tissue plasminogen
activator (TPA) (a protein of MW
59,050 daltons) Rx fibrinolytic
therapy
uBut most have masses of 100-1000
daltons, which alter the body's
function by interactions at the
molecular level
uquinine
quinidine
umeclobemide metoclopramide
utrimipramine trimethoprim
Copyright UTS, 2017 Slide 27 of 45
Nicotinic acetylcholine receptor
ACh
Side view Top view
6 nm
Pore
~0.7 nm diameter
Out
Membrane 3 nm
In
2 nm
ACh
CH3
Cavity H3 C O CH3
N C
H2 C Possible
Cavity O electron donor
O H group
Glutamate C N
O Possible
N H-bond
site
Histidine
Anionic
group
Nicotinic acetylcholine receptor
uReceptors
uSensingelements for chemical communication
(hormone, neurotransmitter, neurohormones
etc)
uExample: D2 dopamine
uAgonist:dopamine
uAntagonist: chlorpromazine
uIon channels
uMay be blocked by a drug or the gating operation
may be modulated
uLocal anaesthetics (eg. procaine) physically block
the voltage-gated sodium channel
uBenzodiazepines (eg diazepam) bind to a region of
the GABA-receptor/chloride channel complex
uMost facilitate the opening of the channel by GABA
uEnzymes
uDrugs may be competitive (eg neostigmine -
AChE enzyme) or non-competitive (eg aspirin -
COX enzyme) inhibitors of enzymes
uPumps
uDrugs may inhibit the action of carrier molecules
eg proton pump inhibitors (eg. omeprazole)
u Chemical effects
u Protamine - antagonist of the anticoagulant heparin is due
to interaction of highly +ve charged protamine molecule with
highly -ve charged heparin molecule
u Physiological effects
u Antacids - eg. AlOH3 (acts as a physiological buffer)
u Cathartics (purgatives)
u Ingestion of non-absorbable material (eg lactulose or
MgSO4) increases water content of faeces and promotes
defaecation
Slope
Variability
Potency
Log Dose
Copyright UTS, 2017 Slide 38 of 45
Dose-response relationships 2
uPotency
uInherent ability of drug to combine with receptors -
depends on drug affinity
uImportant for dosage but unimportant for clinical
purposes as long as it can be administered
conveniently
uNo justification that the more potent of two drugs is
clinically superior (toxicity is also important)
Slope is important
ED50 ED50
Emax