Flashcards in Last minute Deck (43):
What is the intracellular concentration of Chloride?
What number should be used in Goldmann equation?
What does a non-competitive antagonist do?
Reduce the slope and max response of an agonist
How can you find total number of antagonist binding sites in a preperation?
What does equal potency give?
Where is hepatic cytochrome p450 found?
In the ER
What is the systolic pressure in the arteriole?
What is the normal H+ conc in body fluids?
4x10-8 moles per litre
What are the n, u, m?
n=10-9, u=10-6, m=10-3
What is type II typically associated with?
Truncation in CACNA1A
What is Poisselles law for flow?
Flow- proportional to change in pressure and 4th power of radius, inversely proportional to the viscosity and length
What is Poisselles law for Resistance?
resistance- proportional to viscosity and length, inversely proportional to 4th power of radius
What does MLCK do?
Phosphorylate the serine residue 19- allow myosin cross bridges to bind to actin
What does MLCP do?
Dephosphorylation of myosin light chain
What can 3rd degree heart block do to blood pressure?
Can lower it
What are long and short QT to do with?
Ventricular action potential
Give examples of COXIBs?
Selective for cox2- Vioxx, dicholenic - musculoskeletal pain
What is omalizumab?
Humanised antibody and soluble receptors to IgE- to treat asthma
What is treatment for Long QT syndrome?
B blockers- e.g. atenolol
What is the treatment for short QT syndrome?
Quinidines, implant defibrillation
What is atrial fibrillation treatment?
Flecanide, B blockers, amodarone, Dronadorone
What are the treatments for epilepsy?
Benzos, barbiturates, uptake inhibitors of GABA, metabolic inhibitors of GABA, Calcium channel blocker, Sodium channel blocker
What is treatment for Myotonia congenital?
Sodium channel blocker -Maxiltene
What does KO human and mice AQP1 show?
Problems with urine concentration but largely healthy as not contributing full amount
What does KO of A1/A3 show in mice with and without water?
with- half the osmolality, without- quarter the osmolality
How are the alpha subunits of GABA that are sensitive to Benzos known?
Through animal models- replace a2 gene with mutated/ KO, gives no anxiolytic effects of diazapam
What are problems with vigabatrin?
what are problems with valproate?
High protein binding, rarely hepatic, teratogenic, nausea, hair loss, weight gain
What are the problems with Phenytoin?
Complex pharmacokinetics, vertigo, ataxia, headaches, rashes
What are the problems with Carbamazepine?
Microsomal enzyme induction
What are problems with Lamotigine?
Nausea, dizziness, ataxia, rashes
What Calcium channels are targeted in epilepsy?
T type in Raphe nuclei - for absence siezures
What is the structure of CACNA1A?
24 trans domains, 4 voltage sensory, 4 pore, P/Q type calcium channel
What is an experiment with CACNA1A?
barium current- shows reduce current with mutant and voltage dependance change- higher voltage needed to open
What are the risks of opioids?
Sedation, depression of respiration, inhibition of GI tract, addiction with continuous use
What is an example of an anticholinergic used to treat asthma?
What is the evidence that Myasthenia Graves is cause by antibodies?
87% patients show positive for antibodies, injection of ABs into mice- show fewer ABs then normal and size is smaller
Name a acetylcholinesterase?
Name a corticosteroid?
What study was done with malignant hypothermia?
Rabbit 614 mutation with caffeine and halothane
What in vitro screening assay undergo in lead optimisation?
Mutagenicity, clastogenicity, specific cardiac arrhythmia biomarker
What other methods other than assays are used in lead optimisation?
Overexpresed KO, Exploratory studies