Intro

Question 1

Prescription highlight?

Answer 1

Highlight of prescribing information

Contain FPI

Question 2

FPI?

Answer 2

Full prescribing information

Contain detailed info

Question 3

Pharmacology?

Answer 3

Pharmacognosy, kinetic, dynamic, therapeutic and toxicology

Question 4

Application of clinical pharmacology?

Answer 4

Clinical trials

Question 5

NDA

Answer 5

New drug application 💌

Question 6

Pharmacogenetic?

Answer 6

Pharmacogenomics is the study of how genes affect a person’s response to drugs. This field combines pharmacology (the science of drugs) and genomics (the study of genes and their functions)

Question 7

Drug exposure & response?

Answer 7

Exposure: measure of amount of drug concentration in plasma or other biological fluid (Cmax,Cmin, Css, AUC)

Response: drug pharmacological effect

Question 8

Toxicokinetics vs clinical toxicology?

Answer 8

Toxicokinetics: use of pharmacokinetics in drug safety evaluation study in drug design
C.t: study of adverse effects of drug and toxic substances in body 👁️

Question 9

Method of sampling of biologic specimen?

Answer 9

1. Inversive: sampling blood , spinal fluid, tissue biopsy, synovial fluid etc
2. non inversive: without surgery: sampling urine , feces , expired air etc

Question 10

Serum vs plasma

Answer 10

Serum is the liquid that remains after the clotting of blood. Whereas, plasma is the liquid that remains when anticoagulant is added to prevent clotting

Serum= Plasma - clotting factors

Question 11

plasma drug concentration time curve

Answer 11

Obtain by Drug concentration in plasma sample taken at different times interval
Plasma level 🎚️ vs time curve ⏱️

Question 12

TDM

Answer 12

Therapeutic drug monitoring
Branch of clinical pharmacology
Measurements of specific drug at designated interval to maintain a constant concentration in patient blood stream

Question 13

Therapeutic index ☝️

Answer 13

Ratio between dosage of drug causing toxic and therapeutic effect

            Lethal  or toxic dose (TD 50) TI ==-------------------------------------------------
         Medium effective dose (ED 50)

Td50 50% toxicity
Ed 50 % therapeutic effective

Question 14

Therapeutic window

Answer 14

Range of dosage that cause therapeutic effect without causing significant side effects

TW = MEC:MTC

Question 15

AUC

Answer 15

AUC (areas under curve)is the total integrated area under the plasma drug concentration–time curve. It expresses the total amount of drug that comes into systemic circulation .

Question 16

NTI ?

Answer 16

Narrow therapeutic index (NTI) drugs are defined as those drugs where small differences in dose or blood concentration may lead to dose and blood concentration dependent, serious therapeutic failures or adverse drug reactions.

Smaller difference in dosage cause serious therapeutic adverse drug reaction

Question 17

NTI drug example?

Answer 17

narrow therapeutic index drugs: 
aminoglycosides, 
ciclosporin, 
carbamazepine, 
digoxin, 
digitoxin, 
flecainide, 
lithium, 
phenytoin, 
phenobarbital, 
rifampicin, 
theophylline and 
warfarin.

Question 18

TDM?

Answer 18

Therapeutic drug monitoring (TDM) is testing that measures the amount of certain medicines in your blood.
It is done to make sure the amount of medicine you are taking is both safe and effective

Question 19

When is TDM done?

Answer 19

Therapeutic drug monitoring (TDM) should be performed when the patient has achieved steady-state concentration, has changed drug therapy, or has had a change in response to treatment (eg, toxicity).

Question 20

When is TDM done?

Answer 20

Therapeutic drug monitoring (TDM) should be performed when the patient has achieved steady-state concentration, has changed drug therapy, or has had a change in response to treatment (eg, toxicity).

Question 21

PDC?

Answer 21

Drug concentration” is derived by collecting a blood sample at any time after drug administration and measuring the amount of a drug in a given volume of blood plasma of the sample. The measured drug concentration is generally known as “plasma concentration.”

Question 22

Wide therapeutic index drugs example?

Answer 22

Ibuprofen
Calcium channel blockers
NASID

Question 23

MEC

Answer 23

Minimum effective concentration (MEC) is the minimum plasma concentration of a drug needed to achieve sufficient drug concentration at the receptors to produce the desired pharmacologic response, if drug molecules in plasma are in equilibrium with drug molecules in the various tissues

Question 24

maximum effective concentration?

Answer 24

maximum concentration The peak concentration that a drug achieves in a specified compartment after the drug has been administrated and before administration of a second dose. Cmax is the opposite of Cmin—which is the minimum (or trough) concentration that a drug achieves after dosing

Question 25

(MTC)

Answer 25

Maximum Safe Concentration (MSC): Also called as minimum toxic concentration (MTC) It is the concentration of drug in plasma above which adverse or unwanted effects are precipitated. Concentration of drug above MSC is said to be in the toxic level.

Question 26

What is onset of action?

Answer 26

The length of time it takes for a medicine to start to work. Time required to achieve MEC Onset (how quickly they act) Peak (how long it takes to achieve maximum impact) Duration (how long they last before they wear off)

Question 27

Cmax

Answer 27

Cmax is the maximum (or peak) serum concentration that a drug achieves in a specified compartment or test area of the body after the drug has been administered and before the administration of a second dose. It is a standard measurement in pharmacokinetics

Question 28

What is T max and Cmax of a drug?

Answer 28

Definition: The time it takes for a drug to reach the maximum concentration (Cmax) after administration of a drug that needs to be absorbed (e.g. an oral drug). Cmax is the highest concentration of a drug in the blood, cerebrospinal fluid, or target organ after a dose is given

Question 29

Bioavailability

Answer 29

Bioavailability refers to the extent and rate at which the active moiety (drug or metabolite) enters systemic circulation, thereby accessing the site of action.

Question 30

Type of bioavailability

Answer 30

1. Absolute Bioavailability: When the drug is administered through the intravenous route, the bioavailability of the drug achieved will be 100%. If the reference standard is an IV dose, it is referred to as Absolute Bioavailability. Route of administration oral -IM (intramuscular) -IV (intravenous) 2. Relative Bioavailability: It is the bioavailability of the drug when obtained and it is compared with a reference standard. If the reference standard is any other dosage form than the IV dose, it is referred to as Relative bioavailability. 3. Bioequivalence: When two or more than two drugs that are having the same Composition, when administered inside the body they will show statistically the same desired outcomes for patients over a given period of time. 2. Dosage form: The rate of bioavailability (from higher to lower) of drugs in the different dosage forms is as follows Solution Suspension Powder Tablets Capsules Solutions are better absorbed than suspension than powder than tablet than capsules. 3. Manufacturing variables: Various additives such as Diluent, Fillers, Absorbers, Binding agents are added to make the particular dosage form. A change in concentration of the binders will change the disintegration time of the granules. As there is an increase in disintegration time, there will be a decrease in the bioavailability of drugs. The addition of diluent, i.e, Calcium Phosphate in Tetracycline capsules will change the dissolution rate and hence bioavailability of the drug will be changed. 4. Disintegration rate: By maintaining the concentration of filler inside the particular dosage form, the rate of disintegration can be maintained which in turn will affect the bioavailability. 5. Dissolution rate: Higher the dissolution rate of the drug, the more is the bioavailability of the drug. 6. Biological Factors: A) GIT motility: When GIT motility increases, there will be a decrease in the bioavailability of the drug as well as a decrease in the rate of dissolution. B) First-pass metabolism: Drugs that are administered through the sublingual route (Nitroglycerine tablets). When drugs are taken orally, they will directly go to the hepatic portal system 4 4. Disintegration rate: By maintaining the concentration of filler inside the particular dosage form, the rate of disintegration can be maintained which in turn will affect the bioavailability. 5. Dissolution rate: Higher the dissolution rate of the drug, the more is the bioavailability of the drug. 6. Biological Factors: A) GIT motility: When GIT motility increases, there will be a decrease in the bioavailability of the drug as well as a decrease in the rate of dissolution. B) First-passs metabolism: Drugs that are administered through the sublingual route (Nitroglycerine tablets). When drugs are taken orally, they will directly go to the hepatic portal system (liver) which is the site for metabolism, drugs get metabolized in the liver rapidly and hence there will be no or negligible bioavailability. C) GIT flora: Microorganisms that are present in our GIT, higher antibiotics absorb microorganisms that are present in GIT, as a result, the functioning of the microorganism will get disturbed and as a result bioavailability of the drug will be decreased. D) Disease status: If the patient is suffering from renal failure, and was previously given higher class drugs, there will be a decrease in the rate of absorption of drugs due to the resistance developed and hence decreasing the bioavailability of drugs.

Question 31

various factors affecting Bioavailability

Answer 31

1. Physiochemical Properties A) State of drug: Drugs in solution form or suspension are better absorbed compared to solid dosage form as they require time for dissolution as well as absorption. B) Particle size: Decrease in particle size, increases surface area and hence solubility of drug increases which increase in absorption, dissolution increases and in turn bioavailability increases. C) pKa value and state of ionization: Non-ionised drugs are better absorbed than ionized drugs depending upon the surrounding ph and pKa value of the drug. D) Partition Coefficient: It is the ratio of solubility of the drug in a non-aqueous solvent to the ratio of solubility of the drug in an aqueous solvent. As there is an increase in the partition coefficient of drugs, there will be an increase in the bioavailability of drugs. E) Route of administration: When the drug is administered through the parenteral route, bioavailability achieved is 100 percent. When the drug is administered through the oral route, bioavailability decreases while the drug administered through inhalation or sublingual route the bioavailability increases. F) Plasma protein binding: When the drug is bound to the plasma protein, it will increase the therapeutic effect of the drug, i.e, duration of action of the drug