PCEUT 531 LECT 1

How does a drug work in the body?

binding to receptor

dosage form includes

API & excipients

_ is a physical form of a drug product that incorporates an active pharmaceutical ingredient along with excipients to ensure accurate dosing, protect drug integrity, prevent contamination, improve clinical effectiveness, and afford a means of identification and strength of dose (the form of the whole drug product).

drug dosage form

__ is the substance that provides the drug effect

API

__ is everything that isnt the API

excipient

what are the sources of drug substance?

chemical synthesis, plants, animals, microorganisms, and biotech

what source are most drugs sourced from?

chemical synthesis

Large, complex APIs made by living systems (small organic, protein & peptides, nucleic acid and cells are part of __)

Biologics (chemical forms)

biologics usually have __ oral absorption and since made by living organisms there could only be biosimilar & not identical.

lower (hydorphillic)

physical forms of APIs are

solid, liquid gas

T/F the physical forms of the APIs are similar to the final dosage form.

False

lipid membrane permeability is characterized by __

Log (P) value

__ is the process of combining active ingredients with inactive to create useable drug

pharmaceutical formulation

“by mouth”

PO

oral routes

tablets, capsules, solutions, syrups, elixirs, suspensions, powders

sublingual routes

Tablets, troches, lozenges

inhalation routes

Aerosols, nebulizers

topical/ transdermal routes

ointments, creams, gels, patches

eye/ear routes

Solutions, suspensions; ocular inserts and ointments

nasal routes

Solutions, sprays, inhalants, ointments

rectal routes

Enemas, suppositories, ointments

vaginal routes

Douches, sponges, ointments, creams, suppositories, tablets

IV, SC, IM routes

Solutions, suspensions

__ targets Histamine H2 receptor and is used to treat GERD

famotidine (pepcid)

__ targets COX-1 &2 and is used for pain relief, fever and inflammation

Ibuprofen (advil)

__ targets HMG-CoA reductase and lowers cholesterol

Atorvastatin (Lipitor)

__ matters since it changes the PK and PK decides the PD

formulation

higher therapuetic index (TI)=

safer med

TI=

TC50/EC50

__ is drug concentration required to produce 50% of the maximum possible response.

EC50

__ Is drug concentration that causes 50% adverse effect or toxicity.

TC50

Lower TI =

very toxic med

what comes first:

• distribution

• excretion

• absorption

• metabolism

• 
  

• 
  

absorption

__ Is what the body does to the drug (duration; ADME; Time course of drug concentration in the body, set by ADME)

PK (pharmacokinetics)

__ is what the drug does to the body (reversible; efficacy; the effect produced when the drug interacts with its target)

PD (pharmacodynamics)

More soluble crystal form, or smaller particles→ PK change would be __ absorption

higher (PD=stronger & faster effect)

Extended release tablets→ __ Cmax

lower (fewer side effects, and less dosing)

enteric coating→ PK is med is protected from acid → PD is __ drug absorbed

more

liquid filled capsules & tabs→ __ dissolution step→ __absorption→__ onset

no, faster, faster

__ is the highest plasma concentration after a dose

Cmax

__ is time when Cmax occurs

Tmax

__ is the fraction of the dose reaching the blood stream

bioavailability

__ is the time for the concentration to fall by 50% (decides how fast the drug leaves the body)

half-life

__ is the amount in body ÷ plasma concentration at time 0 (also relates the total amount of drug in the body to its plasma concentration)

volume distribution

__ is the Metabolism in gut wall and liver before reaching circulation

first pass effect

is when the generic matches brand in Cmax, Tmax and AUC

bioequivalence

__ depends on blood flow, protein/fat binding and membrane transporter

distribution

where does most metabolism occur?

liver, intestine, kidney and lungs

(M) __ is oxidation, reduction, hydrolysis, metabolites are often still active

Phase I (CYP)

__ is conjugation with polar molecules→ water-soluble & inactive

Phase II (UGT, SULTS)

A more soluble crystal form dissolves __ and is absorbed __.

faster, better