TOPIC 2 Flashcards by M.A.Lance Evangelista

MOLECULAR DISCOVERY &
CHARACTERIZATION

GOAL DRUG
PRODRUG
BIOASSSAY
LEAD COMPOUND

How well did you know this?

Not at all

Perfectly

identified during drug
discovery and
development

It serves as the
starting point.

chosen based on their
ability to interact with
a specific target

Lead Compound

How well did you know this?

Not at all

Perfectly

the ultimate
objective in drug
development,
which is to create a
safe and effective
medication

Goal Drug

How well did you know this?

Not at all

Perfectly

an inactive or less
active precursor
molecule of a drug
that undergoes a
chemical or
enzymatic
transformation
within the body to
become an active
therapeutic agent

Prodrug

How well did you know this?

Not at all

Perfectly

A compound that requires
metabolic biotransformation
after administration to
produce the desired pharmacologically active compound

Prodrugs

How well did you know this?

Not at all

Perfectly

Aspirin is a prodrug of?

Salicylic acid

How well did you know this?

Not at all

Perfectly

Enalapril ->

enalaprilat

How well did you know this?

Not at all

Perfectly

Epinephrine ->

Dipivefrin

How well did you know this?

Not at all

Perfectly

Epinephrine -> Dipivefrin:

◦ Enhanced solubility
◦ Enhanced lipophilic character
◦ Enhanced duration of action

How well did you know this?

Not at all

Perfectly

Reserpine

▫ Rauwolfia serpentina
▫ (reserpine) tranquilizer and hypotensive
agent

How well did you know this?

Not at all

Perfectly

Periwinkle

▫ Vinca rosea
▫ Vinblastin and Vincristine
▫ For cancer

How well did you know this?

Not at all

Perfectly

Pacific Yew Tree

Taxus brevifolia

How well did you know this?

Not at all

Perfectly

Animal Source

Endocrine glands of cattle, sheep and swine
Pregnant mares.
Embryo

How well did you know this?

Not at all

Perfectly

Endocrine glands of cattle, sheep and swine

Thyroid extract, insulin and pituitary hormone
(replacement therapy)

How well did you know this?

Not at all

Perfectly

Pregnant mares

Source of estrogens

How well did you know this?

Not at all

Perfectly

Embryo

vaccines

How well did you know this?

Not at all

Perfectly

Microbiological Source

penicillin, cephalosphorin,
tetracyclines,
aminoglycosides, lovastatin

How well did you know this?

Not at all

Perfectly

Genetic engineering

Recombinant DNA

Monoclonal Antibody production

How well did you know this?

Not at all

Perfectly

PRE- CLINICAL TRIAL:

●Chemical and physical characterization
●Pharmacology
●Pharmacokinetics
●Pharmacodynamics
●Analytical studies
●Toxicology
●Pharmaceutics
●File IND Application

How well did you know this?

Not at all

Perfectly

Once passed
with pre clinical
submit

INVESTIGATIONAL
NEW DRUG (IND)

How well did you know this?

Not at all

Perfectly

the science of the properties of the drugs
and its effects in the body

Pharmacology

How well did you know this?

Not at all

Perfectly

the study of the interaction of drugs
with cells

Pharmacodynamics

How well did you know this?

Not at all

Perfectly

the handling of a drug within the
body, it includes the ADME processes

Pharmacokinetics

How well did you know this?

Not at all

Perfectly

are observational studies that are aimed
at objective examination and assessment − analysis − of
causal relationships between exposure to potential disease
determinants (risk factors) and subsequent disease

Analytical studies

How well did you know this?

Not at all

Perfectly

the study of the A/E of the chemical agents on living organisms

Toxicology

the general area of study concerned with the formulation, manufacturing stability and effectiveness of a pharmaceutical dosage form

Pharmaceutics

an exclusive rights to the use and profits of a novel pharmaceutical for a limited term

Patent the drug

PRE- CLINICAL TRIAL Special consideration is given on

Orphan drugs and Treatment IND, Emergency IND

Physical – Chemical Characterization:

* Solubility * Partition coefficient * Dissolution rate * Physical form * Stability

preclinical data to check whether the product is safe for initial testing in humans

Animal Pharmacology and Toxicology Studies

information about composition, manufacturer, stability, and controls used for manufacturing the drug substance and the drug product

manufacturing information

detailed plan for proposed clinical studies to assess whether the initial phase trials will expose subjects to unnecessary risks

clinical protocols and investigator information

schedule of dosage

Dosage Regimen

the amount that may be expected to produce, in adults, the medicinal effect for which it is intended

Usual dose

amounts of drug that may be prescribed within the work of usual medical practice

Usual dosage range

dose administered to children

Pediatric dose

also the priming or loading dose, is the amount required to attain the desired concentration of the drug in the blood or tissues

Initial dose

the amount administered to a patient before exposure or contraction of the illness

Prophylactic dose

the amount which is administered to a patient after the exposure or contraction of an illness

Therapeutic dose

The relationship between the desired and undesired effects of a drug

Therapeutic Index

Therapeutic Index:

TD50/ ED50

Factors Affecting the Dose

Age Pharmacogenetics– genetic polymorphism Body Weight Body Surface Area - nomogram Sex Pathologic State Tolerance Concomitant Drug therapy Time and conditions of administration Dosage Form and Route of Administration

Phase I:

Tolerance and safety 20 – 100 healthy volunteer Toxicological studies

Phase II

100 – 300 first controlled studies on patients Efficacy and therapeutic index

Phase III

1000 – 3000 extended clinical trials dose, efficacy, toxicity and side effects Performed with the final dosage form developed in phase II Side effects are monitored

Phase IV

Post marketing studies Drug product may be improved Modification on drug formulation as obtained from manufacturing scale up and validation process may be done Additional clinical studies

NDA is submitted to the FDA for _____ showing product is effective by all parameters

review and approval

The data gathered during the animal studies and human clinical trials of an ______ become part of the NDA.

Investigational New Drug (IND)

increase in the batch size from the clinical batch, submission batch, or to the full-scale production batch size, using the finished, marketed product.

Scaleup

USP–NF <795>

Pharmaceutical Compounding- Nonsterile Preparations

USP–NF <797>

Pharmaceutical Compounding- Sterile Preparations

USP–NF <1160>

Pharmaceutical Calculations in Prescription Compounding

USP-NF <1163>

Quality Assurance in Pharmaceutical Compounding

USP-NF <1176>

Prescription Balances and Volumetric Apparatus

USP-NF <85>

Bacterial Endotoxins Test

USP-NF <1151>

Pharmaceutical dosage form

USP-NF <795>

Pharmacy Compounding- Nonsterile Preparations

USP-NF <797>

Pharmacy Compounding- Sterile Preparations

USP-NF <800>

Hazardous Drugs

is “that which holds the article and is or may be in direct contact with the article.”

Container

is “that which is in direct contact with the article at all times. The closure is part of the container.

Immediate container

It protects the contents from extraneous solids and from loss of the article under ordinary conditions of handling, shipment, storage, and distribution.

Well-closed container

protects the contents from contamination by extraneous liquids, solids, or vapors; from loss of the article; and from efflorescence, deliquescence, or evaporation under the ordinary or customary conditions of handling, shipment, storage, and distribution and is capable of tight reclosure

Tight container

impervious to air or any other gas under the ordinary or customary conditions of handling, shipment, storage, and distribution.”

Hermetic container and Sterile hermetic

Other containers:

Multiple-unit containers and Multiple-dose container Single dose container Single-unit package

Plastic containers advantages

Lightness of weight Versatility Convenience For unit dose delivery

movement of the product components outward toward the container

Permeability

movement of the components of the container into the contents

Leaching

binding of molecules to polymer materials

Sorption

deformation which may be softening, hardening and other physical changes in the plastic container

Alteration of container

A test used to determine resistance to water attack Amount of alkali that release into the the content

LEACHING

is used to reduce the risk of poisoning in children via the ingestion of potentially hazardous items including certain prescription and over-the-counter (OTC) medications, pesticides, and household chemicals.

Child-resistant (C-R) packaging

one that is significantly difficult to open by children 5 years under

Child-resistant (C-R) packaging

Child-resistant (C-R) packaging 4 Basic designs:

1. align the arrows 2. press down and turn 3. squeeze and turn 4. latch top

Cold:

between 2°C and 8°C ****not more than 8°C

freezer

− 25°C and − 10°C ( **** some below 20c)

Cool:

8°C and 15°C

Room temperature:

Ambiance temperature” Temperature prevailing in a working area.

Controlled room temperature

20°C to 25°C but also allows for temperature variations between 15°C and 30°C The mean kinetic temp (MKT) should not exceed 25c

Warm:

30°C and 40°C

Excessive heat:

Above 40°C

Protection from light

Light-resistant container

Protection for freezing

Protect the product from Freezing

TOPIC 2 Flashcards

(83 cards)