Annoying Slide Flashcards
Dose response curve is _____ shape
Log of dose response curve is _____ shape
Hyperbolic
Sigmoid
Thresholds based on acute responses, such as ____, are more (easy to or difficult to ?) determine, while thresholds for chemicals that cause ___ or other chronic responses are more (easy to or difficult to ?)determine.
death
Easy to
cancer
Difficult to
When a threshold is difficult to determine, toxicologists look at the _________________ to give them information about the toxicity of a chemical.
A sharp increase in the slope of the curve can suggest _____________ as the dose increases, as illustrated by line A on the next graph.
A relatively flat slope suggests that the effect of an increase in dose is ______
slope of the dose-response curve
increasingly higher risks of toxic responses
minimal
Quantal dose response curve relates dose to _______
Graded dose response curve relates dose to _______
Frequency of effect
Intensity of effect
the penicillin molecule binds to a bacterial enzyme ______ and prevents “____” in the bacterial ______ leading to death of the bacteria.
transpeptidase
cross links
cell wall.
The interaction between penicillin and the enzyme depends on the ________
Large amounts of penicillin _______ the enzyme and in the presence of small amounts, the enzyme _______
amounts of penicillin present.
completely blocks
resumes its normal function.
thyrotoxicosis can affect a drug’s pharmacodynamics
T/F
T
Drugs can impart new functions on any system, organ or cell.
T/F
F
Drugs (except those gene based)
Do NOT impart new functions on any system, organ or cell.
Only alter the PACE of ongoing activity.
STIMULATION: selective enhancement of the level of activity of specialized cells, e.g _____ on the heart, _____ on salivary glands.
DEPRESSION: selective diminution of activity of specialized cells, e.g. ______ on the CNS, _____ on the heart, _____ on gastric secretion.
adrenaline
pilocarpine
barbiturates
quinidine
omeprazole
Silent receptors
These are sites which bind specific drugs but no pharmacological response is elicited. They are better called ______ or ________ e.g. ________
Drug acceptors or Sites of loss
plasma proteins.
Autoantibodies can also mimic the effects of agonists
T/F
T
Myasthenia Gravis:
Antibodies against the ________ receptors at ________
cholinergic nicotinic
motor end plate.
Testicular feminisation:
_________ syndrome (AIS) is when a person who is genetically ____ is resistant to ___ hormones .
As a result, the person has some of the physical traits of a ______, but the genetic makeup of a ______.
Androgen insensitivity
male; male
woman; man
Familial Hypercholesterolaemia
People who have this condition are born with it. This change prevents the body from __________________________________
ridding itself of the type of cholesterol that can build up in the arteries and cause heart disease.
Effectors of Go
Substrates of Go
Inhibits Calcium channel
Potassium channel in heart
Most things that go for Gi also go for Go
T/F
T
Activation of adenyl Cyclase could result in:
(Contraction or relaxation?) (smooth muscle)
(Increased or reduced ?) contractility of heart
______
______
(activation or inhibition?) of secretion/mediator release
hormone secretion (activation or inhibition?) , among others.
Relaxation
Increased
glycogenolysis
Lipolysis
Inhibition
Activation
cAMP activity is terminated by _______, which _____ it to _____
phophodiestarases
hydrolyse
5-AMP
Activation of phospholipase C catalyzes the cleavage of membrane-bound ____________ into the second messenger _____________ and ________
phophatidylinositol 4,5 biphosphate (PIP2)
inositol (1, 4, 5) triphosphate (IP3)
diacylglycerol (DAG).
IP3/DAG pathway
Main Results:
Mediates /modulates (contraction or relaxation?)
Secretion/transmitter release
Neuronal (excitability or hyper polarization?)
________ movements
_______ synthesis
Cell _______
Contraction
excitability
Intracellular
Eicosanoid
Proliferation
Occupancy theory: response is proportional to the ______________; maximal response occurs when _____________
fraction of occupied receptors
all the receptors are occupied.
Rate theory: response is proportional to the ________________.
Here, _____ of receptor ______ determines whether a molecule is agonist, partial agonist or antagonist.
rate of Drug-Receptor complex dissociation
duration; dissociation
Stephenson’s theory: response is proportional to the ____________
Ariens’ theory: response is a function of _______
fraction of occupied receptor and the intrinsic activity.
affinity
Based on Arien’s theory, maximum response can’t be produced without 100 % receptor occupation.
T/F
F
It can
The induced-fit theory:
______ is not necessarily complementary with the ____ conformation.
Rather binding produces a ______ of both the ______ and ______ as a dynamic process
binding site; ligand
plastic molding
ligand and the receptor
______ theory nullifying the obsolete “key and lock” concept
The induced fit theory
In the induced fit theory , agonist induces _______ change; antagonist induced ________ change and partial agonist induces __________ change.
a conformational
no conformational
partial conformational
Theophylline is a beta2 agonist
T/F
F
PDE inhibitor
Ephedrine is a beta 2 agonist
T/F
T
the response ( _______ ) is plotted against the logarithm of the drug concentration (________)
ordinate
abscissa
fentanyl evokes a given response at a low concentration. ———- evokes the same response only at (lower or higher?) concentrations.
meperidine
Higher
Zidovudine is used to treat _________
HIV
ispaghula is a ______
Bulk laxative
Pralidoxime as a _______ reactivator.
Cholestyramine for __________
choline esterase
sequestration of bile acids and cholesterol in the gut.
Dimercaprol, penicillamine, desferrioxamine as ______.
chelating agents
Angiotensin converting enzyme inhibitors e.g. ______
captopril
Reversible anticholinesterases e.g. ________ ,———-
neostigmine, physostigmine
Irreversible anticholinesterases e.g. ______________
organophosphorus compounds
Aspirin inhibits cyclooxygenase enzyme and therefore _______ synthesis.
prostaglandin
Monoamine oxidase inhibitors used to treat depression e.g. _______.
imipramine
Proton pump inhibitors: e.g. ______ inhibit the H+/K+ ATPase in parietal cells of stomach.
omeprazole
Inhibition of choline carrier by ______.
hemicholinium
Inhibition of noradrenaline vesicular uptake by _______.
Inhibition of neuronal reuptake of noradrenaline by _______.
Inhibition of neuronal reuptake of serotonin by ________.
Inhibition of weak acid (e.g. uric acid) carrier by drugs (e.g. _____
reserpine
desipramine
fluoxetine
probenecid
Eg of silent proteins
Plasma proteins
_______ antagonizes mercuric ion
And it’s _____ type of antagonism.
dimercaprol
Chemical
NaHCO3 as an ______.
Dimercaprol as _________
antacid
Chelating agents
penicillamine as __________
Chelating agent
desferrioxamine as _______
chelating agents.
quinidine (opens or blocks?) sodium channels
Blocks
procainamide is a sodium channel ______
Blocker
local anaesthetics block the sodium channels
T/F
T
nifedipine
______ channel blocker
Calcium
verapamil
______ channel (opener or blocker ?)
Calcium
Blocker
diltiazem opens the voltage gated calcium channels
T/F
F
Blocks it
amiodarone
______ channel blocker
Potassium
sulfonylureas.
_______ channel blocker
Potassium
Characteristics of Receptor:
- specificity - a drug only binds to _______ and causes _______ effect.
- selectivity – a drug binds to _______ receptors with _______ than to other receptors.
*saturability – a receptor has a ______________, and is therefore saturated at _______ concentrations.
one single type of receptor; one single
one or a few types of; higher affinity
limited number of binding sites; high ligand
scopolamine
Agonist, antagonist, partial , or inverse
Antagonist
phenoxybenzamine
Agonist, antagonist, partial , or inverse
Antagonist
Beta carbolines
Agonist, antagonist, partial , or inverse
Inverse
receptors without known ligands (_________).
Orphan receptors
orphan receptors can occur as a result of ________
Molecular cloning
Alpha-1-adrenergic. ___
Alpha 2-adrenergic ___
vii. GABA B ___
viii. 5-HT1 ____
ix. 5-HT2 ____
x. H2 ——
Gq
Gi, Go
Gi, Go
Gi, Go
Gq
Gs
Most common classification of receptors is by _______
Transduction pathway
Go decreases _____ channel
Calcium
Additive drug combinations
Aspirin+ ________ as _______ or _____
Paracetamol
Analgesic or antipyretic
Additive drug combinations
Nitrous oxide +________ as _____
Halothane
General anaeethetics
Additive drug combinations
Amlodipine + _______ as _____
Atenolol
Anti hypertensive
Additive drug combinations
Ephedrine +_______ as ______
Theophylline
Bronchodilator
Additive drug combinations
Glibenclamide + _______ as _______
Metformin
As hypoglycaemic
Imipramine
Competitive or non competitive
Non competitive
Desipramine
Competitive or non competitive
non competitive
Neostigmine works by ______
Physical or chemical mechanism?
None
Biochemical mechanism ( receptors)
Flumazenil
GABA agonist or antagonist??
Antagonist
Penicillin
High or low TI
High TI
Digoxin
Low or high TI
Low TI
What is margin of safety?
Ratio of LD1 to ED99
Adrenaline is a replacement drug
T/F
F
Familial hypercholesteremia is a receptor related disease
T/F
T
Drug distribution
it is not in phases
T/F
F
It is
Drug distribution
delivery to the muscle occurs first
T/F
F
Drug distribution
the ____ is one of the organs which the drug first reaches
Liver
Drug distribution
the _____ phase involves a far larger mass of the body than the _____ phase
second
First
Essential medicines are Cost effective treatment
T/F
T
Concerning log dose response curve
between 30-70% of the curve are straight lines
T/F
T
Concerning log dose response curve
Penicillin has a (high or low ?) therapeutic index
digoxin has a (high or low?) therapeutic index
High
Low
tyramine containing foods cause cheese crisis
T/F
T
High plasma protein binding means a (high or low ?) volume of distribution
Low
Ionization of bases make them less ionic
T/F
F
Drug concentrations in the brain are often similar to plasma concentrations
T/F
F
Which of the following drug interactions should be avoided
Aminoglycoside + penicillins
Probenecid + penicillin
Amoxicillin+ clavulanic acid
Ibuprofen + paracetamol
Antacids + tetracycline
Antacids + tetracycline
What happens when tetracyclines are taken together with antacids?
Tetracyclines form insoluble complex molecules by metal ion chelation with various antacids; tetracycline absorption may be decreased by more than 90% by this interaction.
Tyramine containing foods should be taken with monoamine oxidase
inhibitors(MAOIs)
T/F
F
Should not
Garlic causes increased bleeding when used with anti coagulants
T/F
T
Tetracycline is better taken with food
T/F
F
The following are factors that affect bioavailability of a drug , except?
a) Nature of drug
b) Intestinal motility
c) Age of the patient
d) All of the above
e) None of the above
Age of the patient
Cholestyramine does not act on receptors
T/F
T
Antacids function by acting on receptors
T/F
F
Phenobarbitone is an enzyme inhibitor
Valproate is an enzyme inhibitor
T/F
F
T
Metformin lowers blood sugar by_____________
Glibenclamide lowers blood sugar by __________
Helping your body make better use of the insulin
Increasing the amount of insulin produced by the pancreas
Mention one inducer of CYP2D6
Dexamethesone
