Introduction pharmacology Flashcards
Drug producing 50% of maximum clinical effect?
Effective concentration (EC50)
Drug producing 50% of maximum clinical effect in 50% of subject?
Effective dose (ED50)
Drug dose required to produce a toxic effect in 50% of subject?
Toxic dose(TD50)
Drug dose causing death in 50% of subject?
Letha; dose(LD50)
dose of drug will be between ED50 and TD50?
Therapeutic window
What does ionized (H2O soluble) does to the absorption?
Decrease absorption
What does unionized (lipid soluble) does in the body?
Increase absorption
Is Ka inversely proportional to pKa?
yes
Increase in ka causes complete or partial dissociation?
complete dissociate
Are ionized in acidic conditions
Basic drugs
Are ioniozed in basic conditions
Acidic drugs
HA mean?
acid unionized
A- mean?
acid ionized
B means
base unionized
HB+ means
base ionized
What are the families of receptors?
Ligand-gated ion channels
G-protein coupled receptors
Enzyme linked receptors
intracellular receptors
Decrease in pH cause acidity to?
increase
Increase in Ka causes acidity to?
increase
decrease in pka causes acid to?
increase
Example of ligand-gated ion channels are?
cholinergic nicotinic receptor
ligand-gated ion channel causes:
cell membrane
neurotransmission
muscle contraction
In G-protein coupled receptor, GDP switches to?
GTP
When the drug/ligand binds to GPCR what does it triggers?
phosphorylation
WHat subunit binds to gtp to cause cellular response?
alpha
WHat is the example of GPCR
alpha adrenergic receptors
Example of enzyme-linked receptor?
insulin receptor
Which enzyme is involved in enzyme-linked receptor?
tyrosine kinase
once tyrosine kinase is ______ it triggers response
phosphorylated
Example of intracellular receptors:
steroid
thyroid
nuclear receptor
What does intracellular receptors do?
targets DNA to cause gene modification
Ocuurs when one signalling molecule produces changes in thousands of proteins
Signal amplification
drug binds to receptor?
Affinity
drug produces clinical response
potency
Increase in potency cause __ in drug concentration
decrease
drug to produce response during interaction with receptor
efficacy
drug-receptor complex to prduce maximal clinical effect
intrinsic activity
ability of 1 drug molecule to interact with 1 receptor to produce response
intrinsic efficacy
What are the 4 types of drug interaction?
Synergism
Addition
potentiation
antagonism
This drug interaction means combination drug has greater effect than individual drugs (Effect Ab» Effect A + effect of B)
Synergism
This drug interaction means one drug increases the effect (or protects the) of another drug.
potentiation
Example. of potentiation
Levodopa+carbidopa and amoxicillin+clavulinic acid
This drug-receptor interactions activates the receptor?
Agonist
This drug-receptor interactions inhibits/attenuates agonist effect?
antagonist
produces Full effect
Full agonist
does not produce 100% activation
partial agonist
produces opposite effects of the agonist and effect is below the baseline
inverse agonist
Example of inverse agonist
anti-histamines
drugs binds to agonistis receptor site, can be overcome by increase in agonist
competitive inhibition
drug binds to allosteric site
non-competitive inhibition
Reversible antagonist can be reversed with increase in?
substrate
Produces lower effect after prolong use of drug same dose
Downregualtion
Example of downregulations are”
opoids
alcohol
nicotine
Produces higher effect after prolong use with same dose?
supersensitization
example of supersensitization
antipsycotic drugs
dyskinesia
send signals from BRAIN to ORGANS
Efferent
send signals from ORGANs to BRAIN
Afferent
This ANS nerve has long preganglionic nerve and short postganglionic nerve?
Parasympathetic
In parasympathetic system postganglionic nerve Ach binds to which receptor
Muscarinic receptor
This system also known as rest and digest
Parasympathetic
This ANS system responses to emergency situation
sympathetci
In this ANS system has NE at posganglionic nerve and binds to :
sympathetic and binds to alpha and beta
Is the origin of sympatheic nerve?
thoracolumbar
origin of parasympathetic nerve?
craniumsacral
This is also known as fear, fight and flight?
sympathetic
What are the sympathetic effects on Heart?
Increase cardiac outputs (increase in BP and HR). increase conductivity
What are the sympathetic effects on BV?
Vasoconstriction and vasodilation
Vasoconstrictions happens in which blood vessel?
skin and mucus membrane
vasodilation happens in which BV?
coronary and skeletal muscle
What are the sympathetic effects on Respiratory system?
bronchodilation
What are the sympathetic effects on GIT?
constipation and urinary retention (relaxes the sphincter)
What are the sympathetic effects on male sex organ?
ejaculation
What are the sympathetic effects on female sex organ?
relaxation of uterus
What are the sympathetic effects on Eyes?
mydriasis
far accomodation (ciliary muscles relaxes)
closes canal of schlemm (increase in IOP-glaucome)
What are the sympathetic effects on Exocrine glands?
viscous secretions causes dry mouth
What are the sympathetic effects on metabolism?
glycogenolysis
lipolysis
gluconeogenesis
This system control the radial muscle?
sympathetic
Parasympathetic control which muscle in the eyes?
circular muscle