Exam 1 Study Guide Flashcards
What are the 2 most common sources for measuring drug amount?
Plasma Concentration
Urine Concentration
What is the difference between quantitative measurements and qualitative measurements?
Quantitative measurements can actually be measured by a medical professional (blood sugar, blood pressure, temperature)
Qualitative measurements are subjective and come from the patient and cannot be measured (pain)
What is bioavailability?
The proportion of an administered dose of unchanged drug that reaches systemic circulation
What is clearance?
The volume of plasma cleared of drug per unit of time
What is half life of a drug?
The time required for plasma concentration of a drug to decrease by 50% (remember it is exp onential so we would have to take the natural log of the rate to get a linear rate)
What is the volume of distribution?
An indicator of how well distributed a drug is in the body
(think of how liver failure causes a decrease in albumin released from the liver which would increase the volume of distribution because less drug is being captured by albumin and more is getting circulated)
What does pharmaceutics examine?
The physiochemical properties (solubility, molecular weight and size) of drugs and dosage forms as it relates to dosage form design
Dosage form outside, of the body
What does biopharmaceutics examine?
The interrelationships between the physiochemical properties of drugs, the dosage forms, and the route of administration on the rate and extent of drug absorption into the body
It looks at how the dosage form works in the body
What does pharmacokinetics look at?
The movement of the drug inside the body after it has been released from its dosage form
What does LADME stand for?
Liberation Absorption Distribution Metabolism Excretion
What does liberation mean from LADME?
The drug is released from the dosage form
What does absorption mean in LADME?
The drug is absorbed in the bloodstream
What does distribution mean in LADME?
Drug is sent to different parts of the body
What does metabolism mean in LADME?
The drug is attached and used by enzymes or receptors in the body
What does excretion in LADME mean?
The drug is sent out of the body or filtered in the kidneys, bile, feces, or sweat
What can be find in the United States Pharmacopeia?
Monographs Dietary Supplements Dosage forms Compounded preparations (Mom Diets, Dad Compounds)
What can be found in the National Formulary?
Anything that is not contained in the USP (inactive ingredients)
What can be found in a drugs Monograph?
The strength, purity, quality, and packaging/labeling
As a drug increases in scheduling or class (1->5) what is the relation of likelihood for potential abuse?
As the class increases, the likelihood for potential abuse goes down
What is the main difference between class 1 and 2?
Class 1/ Schedule 1 drugs have no medical use federally and have a higher potential for abuse than schedule 2. Schedule 2 drugs have medical use.
What schedule does Methamphetamines fall in?
Class II - used to treat ADHD (Ritalin)
What class or schedule does the drug Cocaine fall in?
Schedule II - used for an anesthetic in surgery
What are the 3 parts of the NDC (what do they tell us)?
The first 5 (manufacturer)
The second 4 (drug)
The last 2 (package size)
Are dietary supplements FDA approved?
No they are not legally considered drugs so they are not FDA approved but the FDA still oversees their manufacturing to make sure they are safe for the public
What labeling must be on dietary supplements?
“This product is not intended to diagnose, treat, cure, or prevent any disease.”
If a drug has been recalled due to some patients developing seizures and blood clots, what class of recall would this be?
Class I : the use or exposure of the drug may cause serious adverse health consequences or death
If there is a problem with the labeling of a drug package due to misspelling, what drug class recall would this be?
Class III: not serious
If a drug was recalled due to an exposure of Norovirus in a batch of drugs, what class of recall would this be?
Class II: Medically reversible adverse health consequences
What are the ways a drug is considered a new drug?
Combined into one dosage form (Lisinopril/HCTZ)
New dosage form (from a tablet to a suppository)
New route or dosage schedule (Going from every 6 hours to once daily)
A change in the formulation
What is an IND Application?
Investigational New Drug application - must be submitted before clinical trials
What is an NDA?
New Drug Application where the FDA must approve the drug to be sold in the market
When is an sNDA given to the FDA?
A supplemental new drug application is provided to the FDA when their is a change in the already FDA approved drug.
When is an ANDA submitted to the FDA?
When a patent runs out for the FDA approved brand named drug in order to get approval for a generic equivalent
What does a treatment IND allow for?
A Treatment IND allows an experimental drug to be used to treat a patient while clinical testing and FDA review are still taking place.
What is meant when a drug is considered an Orphan Drug?
Drugs intended for the treatment of “rare diseases and conditions” (less than 200,00 people have the disease)
Incentives are given to the company who does research on this drug in order to promote a cure
What must be included on a drugs label?
Description of drug Clinical Pharmacology Contraindications Indications and Usage Precautions Adverse reactions Drug abuse and dependence Overdosage symptoms Drug dosage and administration How the drug is supplied
When would you see a drug with a black box around the label?
When a drug has a serious adverse reaction
What amount of drug would be given to few patients in phase 0 of clinical trials?
A micro-dose to see if there are any reactions to humans that did not show up in animals
What is mainly looked at in Phase I of clinical trials
The safety of the drug (only 20-100 patients)
What is looked at in phase II of clinical trials?
The effectiveness of the drug (also may still look at safety as the number of patients increase)
What is looked at in phase III of clinical trials?
Effectiveness, safety, and the correct dosage
What is phase IV looking at in clinical trials?
To see if there are any reactions or problems post marketing to the public that were not seen in Phases 0-3 of clinical trials
What are the 2 types of intermolecular forces?
Attractive forces and repulsive forces
What happens when there are repulsive forces between two molecules?
The electron clouds get too close to each other and potential energy becomes more positive (non favorable - must put energy in to pull them apart)
What is happening to the potential energy when there are two molecules that are attracted to one another?
Potential energy is negative which is favorable (inversely proportional with distance)
What is the re in a potential energy diagram?
The equilibrium of attractive and repulsive forces (where PE is most negative- most favorable)
What are the 2 types of attractive intermolecular forces?
Cohesive (between two like or same molecules)
Adhesive (between 2 different molecules)
What causes van der waal forces?
When there are interactions between 2 different dipoles
What are the strongest van der waal forces and why?
Keesom Forces
They are permanent dipoles of polar molecules
(since they are permanent dipoles they are the strongest of the dipole interactions)
When do Debye Forces occur?
When one molecule with a permanent dipole (keesom) repels electrons of another molecule and creates a TEMPORARY dipole in the other molecule
(pushes electrons away from its own charge)
INDUCED DIPOLE - DIPOLE
When do London-Forces occur?
When internal vibrations in NONpolar molecules produce ATTRACTION and two induced dipoles are created
What is happening in hydrogen bonding?
An interaction between a molecule with a hydrogen atom (donor) and a strongly electronegative atom (acceptor)
(hydrogen is tiny and can get close to the electronegative atom)
What is happening in an Ion-Dipole force?
An interaction between and ion (charged atom) and a dipole (NaCl in water)
When can ion-induced dipole forces happen?
When a NONpolar molecule may be polarized by an electron cloud of an ion (charged atom) and it may make a bond with the charged atom
What causes hydrophobic interactions?
Forces of an attraction between non-polar molecules suspended in water or an aqueous solution
(the hydrophobic nature of non polar molecules causes them to be pushed together in water and surrounded by water)
What kind of shape and particle size does matter have in a solid state?
A fixed shape and particle size
What kind of intermolecular forces does matter have in a solid state?
Very strong intermolecular forces
How are the molecules and atoms arranged in a crystalline solid form?
They are arranged in REPETITIVE three-dimensional lattice units.
What lattice system has the highest symmetry? Lowest?
Cubic has the highest (would not be found in drugs)
Triclinic has the lowest symmetry
What are the 7 lattice systems in order of most symmetrical to least symmetrical?
Cubic Tetragonal Orthorhombic Rhombohedral Hexagonal Monoclinic Triclinic
What are polymorphs?
Chemical entities that exist in more than one crystalline structure
How would polymorphs arise?
Changes in intermolecular bonding patterns (bonding between molecules)
Conformational changes in the molecule (changes in shape in molecule
Molecular orientations between neighboring molecules (where the molecule is when around neighboring molecules)
What physical properties are different in polymorphs?
Melting points, solubilities, stability, and density
What effect does the crystal form have on bioavailability?
Different crystal forms can have different bioavailability
some have higher concentrations in plasm and some lower
What is the difference between a hydrate and a solvate?
A hydrate is when you include water into the crystal lattice
A solvate is when a solvent is included into the crystal lattice
How do hydrates compare in solubility of water when compared to the anhydrous form of the crystal?
Hydrates are less soluble in water than the anhydrous form (the hydrates already have water so why would they trade for other water molecules?)
What are salt crystals?
Salt forms of drug substances (acids and the bases)
How do co-crystals differ from salt crystals?
Co-crystals are crystalline materials composed of two or more different molecules and interact NON-IONICALLY
What are counterions?
The corresponding compound in a salt (sodium is the counter ion for hydrochloride)
What are amorphous solids?
Non-crystalline solids - the particles are not organized in a defined lattice pattern (scattered with no pattern)
(RANDOM molecular arrangement)
Do amorphous solids have a distinct melting point?
No they do not - the melting point is rather defined by the GLASS TRANSITION TEMPERATURE (Tg)
(Tg think of melting plastic or glass- kind of goey)
Considering amorphous solids are in a random pattern, would they be more or less stable than crystals?
Less stable - more randomized and less organized
WEAK INTERMOLECULAR FORCES
Would amorphous solids be more easily dissolved in water than crystals?
Yes. They are random and require less energy to dissolve
What do amorphous dispersions do for a substance?
Increase the solubility and the stability.
get the solubility of the amorphous solid and the stability of the crystalline lattice
Define polymeric solids
They are large molecules that are formed together from small monomers into a chain and are covalently linked
Why would one use a polymer in a mixture of a drug?
To increase the thickness (thickening agent) To suspend a drug into To stablize lotions Create coatings for tablets (THEY ARE NATURALLY LIKE RUBBER)
Is a liquid more or less dense than a gas?
More dense than a gas
What is vapor pressure?
The equilibrium pressure (where vapor and liquid states are equal)
(when boiling water and it is bubbling into gaseous form)
For a liquid with a higher vapor pressure, would it be harder or easier for molecules to escape the liquid surface?
Easier, it has weaker intermolecular forces and a lower boiling temperature
What is surface tension?
The energy needed to expand a liquid surface area (the stronger the intermolecular forces the greater the surface tension)
Does gas have a higher or lower compressibility than liquid?
Higher compressibility (large space between gas molecules with no intermolecular attractions)
What variable affects both the pressure and volume of the gas?
Temperature (partial pressure is directly proportional to the concentration of gas)
Define boiling point
The temperature at which vapor pressure = atmospheric pressure (liquid to gas)
Define melting point
The temperature at which solid changes to a liquid
What happens during sublimation?
A solid is converted to a gas
What is the eutectic point?
The lowest temperature at which eutectic mixtures melt
