OSCE/ OSPE Flashcards
Exp:4 BIOAVAILABILITY OF DRUGS
Absolute bio= _______ x _______
___________________
________________
AUC.oral x100
___________________
AUC injected
Exp:4 BIOAVAILABILITY OF DRUGS
Absorption from the gut depends on many factors including:
gastro-intestral ______
gastro-intestral intestinal _____
Particle _____
________________________ with gut cortents
gastro-intestral motility
gastro-intestral intestinal pH
particle size
physicochemical interaction with gut cortents
Exp:4 BIOAVAILABILITY OF DRUGS
For IV administration, bioavailability is ??
100%
Relative bioavailability
Exp:4 BIOAVAILABILITY OF DRUGS
___________ Drug
—————————
____________ Drug
AUC Test Drug
—————————
AUC Standard Drug
Exp:4 BIOAVAILABILITY OF DRUGS
To be bioequivalent, the relative bioavailability of two related must be _______ , that is they must show comparable bioavailability and similar times to achieve ______________________
+/- 20%
peak blood concentrations
Exp:4 BIOAVAILABILITY OF DRUGS
Objectives of the Experiment
1. To measure the ___________________ of _____ different brands of _____
Finally we will be able to conclude whether the _____ brands of ______ are ____________.
relative bioavailability
four
ASA
four
Aspirin
bioequivalent.
Exp:4 BIOAVAILABILITY OF DRUGS
MATERIALS AND METHODS
The Subjects
The subjects will be composed of a random sample of __________________ .
The subjects must not have taken any other drug at least ______ prior to the experiment.
These will also have ________ the night before the experiment and a ______ on the morning of the experiment.
8 - 10 students in the class
One week
an overnight fast
light breakfast
Exp:4 BIOAVAILABILITY OF DRUGS
The Drug
______ is being used as its metabolites can be easily obtained from the urine.
______ different brands of ASA will be obtained from a pharmacy.
An established brand, such as ________ will be used as the standard drug.
Aspirin
Four
Bayer’s Aspirin
Exp:4 BIOAVAILABILITY OF DRUGS
METHOD
At ______ time, each subject will be asked to completely _______________ and the urine saved for analysis.
Then each will be given ____ mg of ASA to ingest.
To ensure adequate diuresis, the drug will be given along with ______-______ ml of _____.
Thereafter, urine samples will be collected from the subjects _____, _____, _____, _____, _____, _____, _____, _____, _____, _____, _____ hour intervals and the volume noted.
zero time
empty his/her bladder
600
500 - 1000 ml of water.
0.25h, 0.5h, 1.0h, 2.0h, 3.0h, 4.0h, 5.0h, 6.0h, 8.0h, 12.0h, 24.0 hour
Exp:4 BIOAVAILABILITY OF DRUGS
METHOD
This stepwise method will then be used to determine the concentration of ASA in each sample of urine.
Treat a ___ml aliquot with _____________ to precipitate the proteins in it.
_________ it, then treat with _______ reagent (_______ reagent) to give it ______.
Get the ________ reading on the _____________.
Make ______ dilutions (various concentrations) of ______, get the _______ of these dilutions and do a ____________
Read the __________ of your samples from the _______ to get the corresponding ___________.
From this, a graph of ________________ vs. ________ can be plotted which will be used to determine bioavailability.
5ml ; Trichloroacetic acid
Centrifuge ; colour ; Trinders ; colour.
absorbance ; spectrophotometer.
serial ; pure ASA; absorbance ;standard curve.
absorbance ; standard curve ; concentrations.
log concentration vs. time
Exp:4 BIOAVAILABILITY OF DRUGS
From this graph, the area under the curve can be calculated by using the __________
trapezoidal rule.
Exp 34: Evaluation of Anti-Ulcer Agents
GENERAL PROTOCOL
____ animals for _____-______
_______ animals with _______ at ____th or ___th hr
Administer ________ at ___th or ___th hr
_______ animals at ___th or __th hr and ________________
Open stomach via the __________
Quantify and analyse the ________
Examine (______) for _______
Estimate degree of ulceration(s) (Ulcer index)
Fast ; 12 - 16hrs.
Pretreat ; anti-ulcer agents ; 13 ; 17
ulcerogen ; 14 ; 18
Sacrifice ; 15 ; 19 ; harvest their stomachs
greater curvature
gastric secretions
grossly ; ulcers
Exp 34: Evaluation of Anti-Ulcer Agents
Specific Protocols
Group 1 : ____________
Pretreat 2 animals each with:
________ (___ mg/kg)
________ (___ ug/kg)
_______ _______ (__ml/rat)
_________ (_____ ug/kg)
And
control animals with ________ (____ ml/kg)
Induce ulcer(s) with __ ml of ________
Absolute Ethanol
Cimetidine (100 mg/kg)
misoprostol (50 ug/kg)
magnesium trisillicate (1ml/rat)
omeprazole (200 ug/kg)
distilled water (10 ml/kg)
1 ml of Absolute ethanol.
Exp 34: Evaluation of Anti-Ulcer Agents
Group II: ____ N ____
Pretreat 2 animals each as above and induce ulcer with __ ml of _________
0.6 N HCI
1ml of 0.6 N HCI.
Exp 34: Evaluation of Anti-Ulcer Agents
Questions:
What are the mechanisms of anti-ulcer effects of cimetidine, omeprazole and misoprostol.
Cimetidine: Histamine H2 Receptor Antagonist
Omeprazole:Proton Pump Inhibitor (PPI)
Misoprostol: Prostaglandin Analog
Exp 34: Evaluation of Anti-Ulcer Agents
What do you understand by cytoprotection?
Cytoprotection refers to the process of ___________ from various __________________, such as toxins, oxidative stress, or physical damage.
protecting cells
harmful factors or injuries
Exp 34: Evaluation of Anti-Ulcer Agents
Percentage protection =
Ulcer index in ________
__________________________
Ulcer index in ________
Ulcer index in test drug
__________________________
Ulcer index in control
Exp 34: Evaluation of Anti-Ulcer Agents
Ulcer index =
______ of _______ ______ of ______
——————— : ————————
______ of ______ ______ of ______
Ulcer index =
area of ulcer Length of ulcer
——————— : ————————
area of stomach Length of stomach
Exp 34: Evaluation of Anti-Ulcer Agents
Dose of cimetidine
Conc of cimetidine
Dose of absolute ethanol
100mg/kg
20mg/ml
1ml
Exp 34: Evaluation of Anti-Ulcer Agents
Ulcerations occur at _____ of stomach
Haemorrhages occur __________ of stomach
Walls
In between walls
Exp 26: Anticonvulsant action of Drugs
Materials : subject:
(Young or Adult?)
(Male or Female?)
_______ ________
Adult male albino mice
Exp 26: Anticonvulsant action of Drugs
Materials: DRUGS
_____________ (___mg/ml) (__ml/kg)
________ (___mg/ml) (__ml/kg)
unknown A (____mg/ml)
unknown B (_____mg/ml) (plant extracts).
Pentylene tetrazol ; 10 ; 100
diazepam ; 1 ; 10
unknown A (100mg/ml)
unknown B (100mg/ml)
Exp 26: Anticonvulsant action of Drugs
Materials!
Animals: ________
Drugs:
______
______ (___mg/ml)
unknown A (____mg/ml), unknown B (_____mg/ml) (plant extracts).
Others: Needles, syringes, oral ______, stop watches, weighing balance.
Adult male albino mice
PTZ
diazepam ; 1
100;100
cannula
Exp 26: Anticonvulsant action of Drugs
Procedure: The animals are divided into four groups - I, II, Ill and IV and treated as follows:
GROUP1:
Equal number of mice will receive ________ (___ml/kg, i.p), _______ (___ mg/kg. i.p), _______ (____,______,_____,______ mg/kg, p.o) _______. before ______ (___ mg/kg, i.p)
GROUP II:
________, ________, ________ (____,____,___,_____ mg/kg, p.o )
_____ before _________.
GROUP III:
________, ________ (___ mg/kg, i.p), ________, ________. before ________ (____mg/kg, i.m).
GROUP IV: ________, ________, ________, ____ before ________.
distilled water 2.5ml ; phenobarbitone 20 mg ; unknown A ; 50, 100, 200, 400mg ; 30 mins ; picrotoxin
Distilled water; phenobarbitone ; unknown B ; 50, 100, 200; 30mins; picrotoxin
Distilled water ; diazepam; 2 mg; unknown A ; 30 mins ; strychnine ; 1 mg
Distilled water; diazepam ; unknown B; 30 mins ; strychnine.
Exp 26: Anticonvulsant action of Drugs
Any mouse that does not convulse in _______ after ________________ administration is considered protected.
30 mins
PTZ
Exp 26: Anticonvulsant action of Drugs
QUESTIONS:
1. What are the mechanisms of action of the convulsant and anticonvulsant drugs used in this experiment?
Phenobarbital: is a barbiturate. enhances the inhibitory action of the neurotransmitter gamma-aminobutyric acid (GABA) in the brain.
Diazepam: is a benzodiazepine. enhances the effect of GABA by binding to GABAa receptors
Strychnine: antagonist to the inhibitory neurotransmitter glycine in the spinal cord and brainstem.
Pictotoxin: convulsant alkaloid that acts as a non-competitive antagonist of the GABAA receptor chloride ion channel.
Exp 26: Anticonvulsant action of Drugs
QUESTIONS:
Explain the terms - fits, seizure, convulsion and epilepsy.
fits” is a less precise term often used informally to describe episodes of abnormal brain activity while “seizure” is the medical term for such episodes.
“Convulsion” refers to the muscle spasms and movements that can occur during some seizures
“epilepsy” is a medical condition characterized by recurrent seizures.
Exp 26: Anticonvulsant action of Drugs
Dose of distilled water : ____ml/kg
Dose of diazepam: ___ml/kg
The route of administration of each drug was ______
In group 1, _____ was used instead of picrotoxin
In group 4, _____ was used instead of strychnine
10; 10
Oral
Pentylenetetrazol
Pentylenetetrazol
Exp 40: TEST FOR ANTI-INFLAMMATORY AGENTS
Animals:
Young or Adult
albino ( rats or mice?)
Animals: adult albino rats
Exp 40: TEST FOR ANTI-INFLAMMATORY AGENTS
Drugs: _______,__________,__________ drugs
Acetylsalicylic, ibruprofen , test
Exp 40: TEST FOR ANTI-INFLAMMATORY AGENTS
Animals:______________
Drugs: ________ ,_________, __________ drugs
adult albino rats
Acetylsalicylic, ibruprofen, test
Exp 40: TEST FOR ANTI-INFLAMMATORY AGENTS
Inflammatory agents: any of these below ( 0.1 ml in normal saline) can be used
___% _____________
___% _________
___mg/ml ______________
___ug/mI ___________
_______% v/v solution of ______
1% carrageenan
4% formalin
1mg/ml histamine
5ug/mI serotonin
0.5% v/v solution of fresh egg white.
Exp 40: TEST FOR ANTI-INFLAMMATORY AGENTS
Procedure:
Divide animals into groups and measure the average ____________ of the (left or right?) ________ of each animal is determined (D•), after 3 or 4 measurements.
The test agents are afterwards injected ______ (____) or _____ (____) before injecting the _______ agents.
__________ is measured immediately after _________ injection and subsequently at _________ interval for ______.
The left paw receives the same amount of _______ and serves as the ____________ for each animal.
paw diameter ; right hind paw
intraperitoneally ; 30min
orally ;1hr
phlogistic ; Paw diameter
carrageenan ; 30 min
2hr.; saline
vehicle control
Exp 40: TEST FOR ANTI-INFLAMMATORY AGENTS
Percentage inhibition after time t is calculated as:
___________________________ x 100
________________________
(D, D.) control
(D1 D•) control (D1 D•) x 100
________________________
(D, D.) control
Exp 40: TEST FOR ANTI-INFLAMMATORY AGENTS
Plot a graph of ________________ against ______
% inhibition against time
Exp 1A : Dose-Response curve
EXPERIMENT 1A
DOSE-RESPONSE CURVE
The isolated ________ ——— preparation will be used.
_________ of _____ sex weighing between _____ and ______g are provided.
guinea-pig ileum
Guinea-pigs of either sex
200 and 300g
Exp 1A : Dose-Response curve
EXPERIMENT 1A
DOSE-RESPONSE CURVE
Process:
Stun the animal by a _______________ and bleed it out. Open the ________ , remove the _________ portion of the _______ just above the patch of ______ and clean the lumen with _________ using a ____ml ______.
Cut off a segment _______ long and suspend in the ——ml _____ containing __________ , aerated with oxygen and maintained at ___ C.
By means of a ___________ , attach the _______ end of the muscle to a hook on the ___________ , arranged at the bottom of the organ-bath and attach its upper end by a thread fo a _______ or a ______________.
Adjust the tension on the muscle to _____ weigh and record its movements on a ________ or a (slowly or rapidly?) moving _________
sharp blow on the head ; bleed it out
abdomen ; terminal ; ileum
lymph tissue ; lumen ; Tyrode solution
5.0ml pipette; 3-4cm
50ml organ-bath ; Tyrode solution
35 C.; looped thread
lower ; acrator glass tubing
transducer ; light frontal-writing lever.
0.2g; recorder
slowly moving smoked drum.
Exp 1A : Dose-Response curve
EXPERIMENT 1A
DOSE-RESPONSE CURVE
Put on the ________ for ______
Add ____ml of ____ g/ml ___________ and leave to act for _____.
__________ kymograph or recorder and ________________. _____ the bath.
After ______. switch on the kymograph/recorder, allow to run for _____.
Add 0.2ml of 10 g/ml.
Repeat procedures 2 and 3
Add 0.4ml of 10 g/ml.
Repeat procedures 2 and 3
Continue to increase the dose by doubling the concentration until there are constant heights of contraction.
(Higher conc. of ACh-100 g/ml, 1 mg/ml will be provided).
Repeat steps 1-8 for ____ and ________.
kymograph ; 1 minute
0.1 ml of 10 g/ml ; Acetylcholine ;30secs.
Switch off ; wash out the drug. Refill
2mins. ; 30secs.
5-HT and Histamine.
Exp 1A : Dose-Response curve
EXPERIMENT 1A
DOSE-RESPONSE CURVE
When you have obtained the maximal contraction, remove the kymograph paper carefully and varnish it. Measure the contractions; plot a graph of _____ (x-axis) against _______ i.e.________ (y-axis).
log-dose
response
height of contraction