Module 02: Basic Principles of Pharmacology Flashcards
This is cited as a science dedicated to the study of rate processes such as absorption, distribution, metabolism, and excretion of a drug and the multiple interrelationships affecting same, such as incomplete absorption, saturability in transport, biotransformation, or binding.
Pharmacokinetics
What are the different routes for medications?
(A) Oral (PO)
(B) Sublingual route (SL)
(C) Buccal route (Bu)
(D) Intravenous route (IV)
(E) Intramuscular route (IM)
(F) Subcutaneous route (SC or SQ)
(E) Inhalation route (INH)
What are the different kinds of medications administered?
(A) Nasal Spray
(B) Rectal (tablets or suppositories)
(C) Vaginal (Tablets or suppositories)
(D) Cutaneous Route
(E) Otic (Ointments or drops)
(F) Ocular or Ophthalmic
(G) Transdermal patches
What are the different biochemical paths of drug administration?
(A) Passive diffusion
(B) Facilitated passive diffusion
(C) Active Transport
(D) Pinocytosis
This is known as the movement against a concentrated gradient using energy (ATP).
Active Transport
This is characterized as the movement along the concentration gradient without energy.
Passive Transport
(1) Simple Diffusion
(2) Facilitated Diffusion
This movement involves the transport of extracellular fluids along with its contents of small dissolved molecules (solutes).
Pinocytosis (pino which means to drink and kytos which pertains to the word cell)
What are the requirements of pinocytosis in order for it to transpire or occur?
Requires a considerable amount of cellular energy in the form of ATP to run.
These are known to activate the process of pinocytosis when they make contact to the plasma membrane.
Ions sugars or amino acids
What are the steps of pinocytosis?
(A) Solutes bind to the cell membrane.
(B) The cell membrane starts to fold inwards and the cell membrane continues to fold.
(C) Both ends of the fold meet, producing a pinosome.
This pertains to the fraction of administered drug that reaches the systemic circulation intact.
Bioavailability
Bioavailability is characterized to be a determiner of what?
It determines the dosage required for each drug via each route of administration.
Based on the hypothetical dose-response curve (relationship) in pharmacodynamics, this is known as the location of the curve along the dose axis.
Potency
Based on the hypothetical dose-response curve (relationship) in pharmacodynamics, this is characterized as the greatest attainable response.
Maximal efficacy or ceiling effect
Based on the hypothetical dose-response curve (relationship) in pharmacodynamics, this is characterized as the change in response per unit dose.
Slope
What are the factors causing low bioavailability?
(A) Insufficient time for absorption in the GIT (poorly dissolved drugs)
(B) Chemical reactions that reduce absorption can decrease bioavailability (drug interactions, gastric acids or enzymes, etc.)
(C) Age, sex, physical activity, genetic phenotype, stress disorders (malabsorption syndromes) or previous GI surgery (bariatric surgery) can also affect drug bioavailability
Enumerate drug administrations depending on their bioavailability.
(A) Intravenous
(B) Intramuscular
(C) Oral tablet
(D) Sublingual or buccal (powder)
(E) Oral capsule
What are the different factors affecting distribution?
(A) Volume distribution
(B) Protein binding
(C) Blood brain barrier
This is defined as the theoretical volume of fluid into which the total drug administered would have to be diluted to produce the concentration in plasma.
Volume Distribution
What are some drugs that can bind with plasma proteins?
(1) Albumin lipoproteins, a-1acid glycoprotein (AGP)
This factor affecting drug distribution is characterized to either enhance or detract from a drug’s performance.
Protein binding
Explain the difference between drugs that are minimally-protein bound to those that are highly protein bound drugs?
Drugs that are minimally protein bound penetrate tissue better than those that are highly protein bound drugs, but they are excreted much faster.
Why do highly protein-bound drugs increase the risk for toxicity?
Because when administered together they will compete for protein binding sites, thus increasing the risk for toxicity (eg 95% vs 90% protein binding)
What are the characteristics of highly protein bound drugs?
(1) Poorer tissue penetration
(2) Decreased access to privileged sites
(3) Slower excretion
(4) Longer plasma half life
What are the characteristics of minimally protein bound drugs?
(1) Better tissue penetration
(2) Enhanced access to privileged sites
(3) Faster excretion
(4) Shorter plasma half life
What happens to protein binding occurring outside the bloodstream?
Compounds can bind with macromolecules in skin, breast milk, tissues and organs including the placenta. They become stuck and are thus prevented from reaching the site of their intended action.
This is known as an endothelial lining in the blood vessels in the brain where cells are tightly pressed together creative a selective semi-permeable membrane between blood and the interstitium of the bran (tight junction proteins).
Blood brain barrier
What is the role of the blood brain barrier?
To protect the brain from foreign substances including 98% of available drugs in the market
What drugs are known to have the capacity to cross the Blood Brain Barrier by diffusion and others via transport proteins?
Highly lipid soluble drugs and those with low molecular weight (benzodiazepine and enoxaparin)
What drugs that cannot cross the Blood Brain Barrier by diffusion and others via transport proteins?
Water soluble drugs (penicillin and atenolol) and drugs not bound with transport proteins (free drugs)
This refers to the fraction of a drug that is not bound to serum proteins and is immediately available to distribute in the body, interact with biological membranes, and bind to receptors.
Free drugs
What are other biological barriers?
(A) Placental barrier
(B) Skin barrier
(C) Breastmilk
The goal of this process in pharmacokinetics is to make the drug easier to excrete.
Drug metabolism
What are some processes that fall under drug metabolism?
Oxidation, reduction, hydrolysis, hydration, conjugation, condensation or isomerization
How does drug metabolism work?
It typically inactivates drugs, some drug metabolites are pharmacologically active- sometimes even more so than the parent compound.
This is characterized as the principal site of drug metabolism within the human body.
Liver
This is known as a drug that requires activation in order to have its therapeutic effect. This is also characterized as an inactive or weakly active substance metabolized into an active pharmacologic substance.
Prodrug
Prodrugs are often designed to what?
Improve a drug’s bioavailability
How do prodrugs work?
Prodrug’s parent compounds that contain regions or additional chemical groups that mask the drugs’ active zone and or alters drug solubility (promoiety), but can be enzymatically or chemically cleaved or altered by site specific enzymes, exposing the drug’s active zone and allowing the drug to activate it’s receptor resulting in a therapeutic effect.
What is the active drug of codeine?
Morphine
What is the active drug of clopidogrel?
Thiol-derivative