Exam 1- Intro to Pharm, Pharmacokinetics, Pharmacodynamics, Drug Development, Steroids&Biologics, Rx Writing, Antineoplastics, Pain Meds, Opioid Agonists, Pain Management

Question 1

pharmacology

Answer 1

biomedical science/study of the interaction of chemical substances or drugs with living cells, tissues, and organisms

Question 2

drug

Answer 2

natural product, chemical substance, or pharmaceutical preparation intended for administration to a human or animal to diagnose or treat a disease

Question 3

pharmacotherapeutics

Answer 3

medical science concerned with the use of drugs in the treatment of disease

Question 4

toxicology

Answer 4

the study of poisons and organ toxicity; the harmful effects of drug and other chemicals on living systems

Question 5

pharmacokinetics

Answer 5

what the body does to the drug

processes that determine the concentration of drugs in body fluid and tissues (drug plasma concentration) over time (drug absorption, distribution, biotransformation=metabolism, excretion)

Question 6

pharmacodynamics

Answer 6

what the drug does to the body

study of the actions of drugs on target organs

Question 7

What concepts are involved with pharmacokinetics?

Answer 7

Dose of drug -> Drug concentration in target organ over time

Absorption, Distribution, Biotransformation (Metabolism), and Excretion are involved

Question 8

What concepts are involved with pharmacodynamics?

Answer 8

Drug concentration in target organ over time -> Mechanism and magnitude of drug effect

Receptor binding, Signal transduction, and Physiological effect are involved

Question 9

What are 3 main drug sources?

Answer 9

Natural products- plants, microbes, animal tissues, minerals (i.e. lithium)

Chemical substance- synthetic, semisynthetic (i.e. oxycodone)

Pharmaceutical preparation

Question 10

What are some drug preparations?

Answer 10

Crude, Pure, Tablets, Capsule, Solutions, Suspensions, Skin patches, Aerosols, Ointments, Creams, Lotions, Suppositories

Question 11

Crude Drug preparation

Answer 11

Obtained from natural sources (such as opium from the dried juice of the poppy seed capsule).

Question 12

What are advantages/disadvantages of crude drug preparation?

Answer 12

A crude drug preparation retains most or all of the active and inactive compounds contained in the natural source from which it was derived. However, it is difficult to identify and quantify the effects of the prep because of multiple ingredients and the amount varies from batch to batch

Question 13

Pure Drug preparation

Answer 13

Isolation of pure drug compounds from the natural sources

i.e. morphine, insulin

Question 14

Tablet preparation

Answer 14

In the manufacture of tablets, a machine with a punch and die mechanism compresses a mixture of powdered drug and inert ingredients into a hard pill

Question 15

What are inert ingredients in tablets and what is their purpose?

Answer 15

Fillers- provide bulk

Lubricants- prevent sticking to the punch and die during manufacturing

Adhesives- maintain tablet stability

Disintegrants- facilitate solubilization of tablet when it reaches gastrointestinal fluid

Question 16

Pharmaceutical preparation

Answer 16

Pharmaceutical preparations or dosage forms are drug products suitable for administration of a specific dose of a drug to a patient by a particular route of administration.

Question 17

enteric coatings

Answer 17

A polymer coating around a tablet that will not dissolve in gastric acid but will break down in the more basic pH levels of the intestines

Question 18

What is the importance of enteric coatings?

Answer 18

To protect drugs that would otherwise be destroyed by gastric acid and to slow the release and absorption of a drug when a large dose is given at one time

Question 19

What are sustained-release or extended-release products?

Answer 19

These products release the drug from the preparation over many hours

Question 20

What are some methods used to extend the release of a drug?

Answer 20

Controlled diffusion- release of the drug from the pharmaceutical product is regulated by a rate-controlling membrane

Controlled dissolution is done by inert polymers that gradually break down in body fluids. These polymers may be part of the tablet matrix, or they may be used as coatings over small pellets of drug enclosed in a capsule

Osmotic pressure- these products contain an osmotic agent that attracts gastrointestinal fluid at a constant rate. The attracted fluid then forces the drug out of the tablet through a small laser-drilled hole

Question 21

Capsule preparation

Answer 21

Hard gelatin shell- enclose powders

Soft gelatin shell- enclose liquid or solution

Question 22

What is the most common preparation for oral route of administration? Why?

Answer 22

Tablets and capsules are the most common preparations for oral administration because they are suitable for mass production, are stable and convenient to use, and can be formulated to release the drug immediately after ingestion or to release it over a period of hours.

Question 23

What is the most common liquid drug preparation?

Answer 23

Solutions and suspensions

Question 24

Why are solutions and suspensions convenient?

Why are they less convenient than solid dosage forms?

Answer 24

Convenient because they provide a method of administering drugs to individuals unable to easily or safely swallow tablets or capsules

Less convenient than solid dosage forms because the liquid must be measured each time

Question 25

What are the oral administration preparations of solutions/suspensions?

Answer 25

syrups- sweetened aqueous solutions

elixirs- sweetened aqueous-alcoholic solutions

Question 26

How are parenteral preparations of solutions/suspension administered?

Answer 26

Sterile solutions/suspensions are administered directly into system via needle and syringe/infusion pump

Question 27

Skin Patches

Answer 27

Transdermal skin patches are drug preparations in which the drug is slowly released from the patch for absorption through the skin into the circulation

Question 28

How do skin patches regulate diffusion of drug?

Answer 28

Most skin patches use a rate-controlling membrane to regulate the diffusion of the drug from the patch

Such devices are most suitable for potent drugs, which are therefore effective at relatively low doses, that have sufficient lipid solubility to enable skin penetration.

Question 29

Aerosols

Answer 29

Drug preparation administered via inhalation through the nose or mouth.

Usually local effect, but can also be absorbed through mucosa to exert systemic effects

Question 30

Ointments & Creams

Answer 30

Drug preparation administered via topical application. The active drug is incorporated into a vehicle which enables the drug to adhere to tissue for a sufficient length of time to exert effect

Question 31

Lotions

Answer 31

Drug preparation administered via topical application. Liquid preparations often formulated as oil-in-water emulsions and are used to treat dermatologic conditions

Question 32

Suppositories

Answer 32

Drug preparation used for rectal, vaginal, or urethral administration. The active drug is incorporated into a solid base that melts or dissolves at body temperature. Can produce local or systemic effects

Question 33

What are some common routes of drug administration?

Answer 33

Enteral, Parenteral, Transdermal, Inhalation, Topical

Question 34

What are examples of enteral administration?

Answer 34

Oral- has the biggest barrier to absorption

Sublingual- drug product is placed under the tongue (quick absorption because of vasculature)

Buccal- drug is placed between cheek and gum

Rectal

Question 35

What are examples of parenteral administration?

Answer 35

Intravenous (IV)- drug is delivered directly into systemic circulation

Intramuscular (IM)

Subcutaneous (Subcut)

Intrathecal- injection of a drug through the thecal covering of the spinal cord and into the subarachnoid space

Epidural- injection of drug into space above the dural membranes of the spinal cord

Question 36

What are the advantages and disadvantages of oral route?

Answer 36

Advantages- convenient, relatively safe, and economical (easily mass produced)

Disadvantages- cannot be used for drugs that are inactivated by gastric acid, for drugs with large first-pass effect, or for drugs that irritate the gut

Question 37

What are advantages/disadvantages of IM route?

Answer 37

Advantages- suitable for suspensions and oily vehicles, absorption is rapid from solutions and is slow and sustained from suspensions

Disadvantages- may be painful, can cause bleeding if patient is receiving an anticoagulant

Question 38

What are advantages/disadvantages of Subcut route?

Answer 38

Advantages- suitable for suspensions and pellets, absorption is similar to that in IM route but is usually slower

Disadvantages- cannot be used for drugs that irritate cutaneous tissues or for drugs that must be given in large volumes

Question 39

What are advantages/disadvantages of IV route?

Answer 39

Advantages- bypasses absorption to give immediate effect, allows for rapid titration of drug, achieves 100% bioavailability

Disadvantages- poses more risks for toxicity and tends to be more expensive than other routes

Question 40

What are examples of transdermal, inhalational, and topical routes of administration?

Answer 40

Transdermal- skin patches

Inhalational- aerosols

Topical- lotions, creams, ointments

Question 41

What is the chemical name of a drug?

Answer 41

Specifies the chemical structure of the drug and uses standard chemical nomenclature

Question 42

What is the proprietary/trade/brand name of a drug?

Answer 42

The registered trademark belonging to a particular drug manufacturer and used to designate a drug product marketed by that manufacturer

Question 43

What is the non-proprietary/generic name of a drug?

Answer 43

The type of drug name most suitable for use by health care professionals.

In the United States the preferred nonproprietary names are the United States Adopted Name (USAN) designations. These designations, which are often derived from the chemical names of drugs, provide some indication of the class to which a particular drug belongs

Question 44

What are the pharmacokinetic processes?

Answer 44

Absorption, distribution, and biotransformation

Question 45

What is drug absorption?

Answer 45

Movement of drug from site of administration into the blood stream, with the rate dependent on the physical characteristics of the drug and its formulation

Question 46

How can drugs be absorbed?

Answer 46

By passive diffusion (lipid, aqueous), active transport, facilitated diffusion

Question 47

What is the affect of pH on drug absorption?

Answer 47

Only non-ionized forms are sufficiently soluble to cross cell membranes. So the ratio of ionized to non-ionized forms of a drug at a particular pH influences absorption rate

Question 48

What is drug distribution?

Answer 48

Movement of drugs from circulation into tissues and organs

Question 49

What factors affect drug distribution?

Answer 49

Ionization- non-ionized forms sufficiently soluble

Lipid solubility- higher lipid solubility (nonpolar) = more distribution

Organ blood flow- drugs are rapidly distributed into highly perfused tissues

Plasma proteins- (weak acids bind to albumin, weak bases bind to lipoproteins, glycoproteins, globulins) The extent of binding is dependent on the affinity of a drug for protein-binding sites

Molecular size- large molecules cannot easily distribute across membranes

Question 50

What is drug biotransformation?

Answer 50

Enzyme catalyzed conversion of drugs into metabolites; inactivate and detoxify to help facilitate the ability to leave body

Question 51

What processes are responsible for the decline of plasma drug concentration over time?

Answer 51

Biotransformation (metabolism) and excretion

Question 52

clearance

Answer 52

measure of rate of elimination

Question 53

What is first pass biotransformation?

Answer 53

Drugs that are absorbed from the gut reach the liver via the hepatic portal vein before entering the systemic circulation. Many drugs are extensively converted to inactive metabolites during their first pass through the gut wall and liver, and have low bioavailability after oral administration

Question 54

Phase I Biotransformation

Answer 54

Includes oxidative, hydrolytic, and reduction reactions. The drug becomes water soluble or inactive. In many cases, phase I enzymatic reactions create or unmask a chemical group required for a phase II reaction. In some cases, however, drugs bypass phase I biotransformation and go directly to phase II.

Question 55

Phase II Biotransformation

Answer 55

Drug molecules undergo conjugation reactions with an endogenous substance. Conjugation enzymes join various drug molecules with one of these endogenous substances to form water-soluble metabolites that are more easily excreted. Most conjugated drug metabolites are inactive

Question 56

microsomal cytochrome P450 (CYP) monooxygenase system

Answer 56

Family of enzymes that catalyze the biotransformation of drugs with a wide range of chemical structures

Question 57

The CYP reductase mechanism for drug oxidation

Answer 57

Four steps are involved in the CYP reaction. First, the drug substrate binds to the oxidized form of P450 (i.e., Fe 3+ ). Second, the drug P450 complex is reduced by CYP reductase, using electrons donated by the reduced form of nicotinamide adenine dinucleotide phosphate (NADPH). Third, the drug-reduced form of P450 (i.e., Fe 2+ ) interacts with oxygen. Fourth, the oxidized drug (metabolite) and water are produced.

Question 58

How can drug metabolism be altered by inhibiting/inducing CYP isoenzymes?

Answer 58

Enzyme inducers stimulate the production of CYP enzymes which increases capacity for metabolism-> drug is metabolized quicker. Thus drug concentration and effect are decreased

Enzyme inhibitors decrease the ability of binding. Drug concentration and effect are increased. Toxicity may ensue