PHARMACOLOGY M1.1 - 1.2 Flashcards
can be defined as the study of substances that interact with living systems through chemical processes. These interactions usually occur by binding of the substance to regulatory molecules and activating or inhibiting normal body processes. These substances may be chemicals administered to achieve a beneficial therapeutic effect on some process within the patient or for their toxic effects on regulatory processes in parasites infecting the patient.
Pharmacology
study of drugs
Pharmacology
is the body of knowledge concerned with the action of chemicals on biologic systems.
Pharmacology
2 Nature of drug
Pharmacodynamics and pharmacokinetics
receptor, receptor sites and inert binding sites
Pharmacodynamics
movement of drugs in body, absorption, distribution, metabolism, elimination
Pharmacokinetics
4 Drug development and regulation
- safety and efficacy
- animal testing
- clinical trials
- Patients and generic drugs
is defined as the science of substances used to prevent, diagnose, and treat disease.
MEDICAL PHARMACOLOGY
is the branch of pharmacology that deals with the undesirable effects of chemicals on living systems, from individual cells to humans to complex ecosystem.
TOXICOLOGY
the science of medical use of drugs, was developed as the precursor to pharmacology
Materia Medica
developed the methods of experimental physiology and pharmacology
Francois Magendie and his student Claude Bernard
It may be defined as any substance that brings about a change in biologic function through its chemical actions.
Drug
activator of a specific molecule
Agonist
inhibitor of a specific molecule
Antagonist
“the target molecule” for drug
Receptor
A drug may be synthesized within the body
HORMONES
it may be chemicals not synthesized in the body
Xenobiotics - “stranger”
refers to a drug that have almost exclusively harmful effects
poison
The dose of the drug makes the poison
Paracelsus
Full name of Paracelsus
theophrastus phillipus auroleus bosbastus von hohenheim
may be solid, liquid or gas. It may be organic or inorganic.
Drugs
very strong; not reversible. Aspirin (acetyl group) and cyclooxygenase is an example of this type of interaction
Covalent
weaker than covalent; vary from relatively strong linkages between permanently charged ionic molecules to weaker hydrogen bonds and very weak induced dipole forces
Electrostatic
usually quite weak; it is the interaction of highly lipid-soluble drugs with the lipids of the cell membrane
Hydrophobic
beta-blocker
chirality (stereoisomerism)
is a potent beta blocker
(S)(-) isomer
is a hundred fold weaker at the beta receptor
(R)(+) isomer
of ketamine is more potent and is less toxic
(+) enantiomer
- Is the study of how the body absorbs, distributes, metabolizes, and excretes drugs
- What the body does to the drug
PHARMACOKINETICS
- It includes the measurement of responses to drugs and how response relates to drug dose or concentration
- Describes the action of drugs
- What the drug does to the body
PHARMACODYNAMICS
– the study of the use of drugs to treat diseases.
PHARMACOTHERAPEUTICS (PHARMACOTHERAPY)
PHARMACOTHERAPEUTICS (PHARMACOTHERAPY)
use of drug treatment is to:
- Cure a disease
- Delay disease progression
- Alleviate the signs and/or symptoms of the disease
- Facilitate nonpharmacologic therapeutic intervention
is the study of the relationship of genetic factors to variations in drug response
PHARMACOGENETICS
is the study of the cost effectiveness of drug treatments
PHARMACOECONOMICS
is the study of the effect of drugs on population
PHARMACOEPIDEMIOLOGY
study of drug’s adverse effects
TOXICOLOGY
is the study of a poison, usually one produced by or occurring in a plant or microorganism
TOXINOLOGY
study of doses
POSOLOGY
study of drug’s manufacture, preparation and dispensing of drugs
PHARMACY
is the study of preparing and dispensing drugs
PHARMACEUTICS
is the study of the identification and preparation of crude drugs from natural sources
PHARMACOGNOSY
the science of drug preparation and the medical use of drugs
MATERIA MEDICA
is the application of all principles in pharmacy to humankind
CLINICAL PHARMACY
Four pharmacokinetic properties determine the onset, intensity, and the duration of drug action
ADME
from the site of administration permits entry of the drug (either directly or indirectly) into plasma.
Absorption
the drug may then reversibly leave the blood- stream and distribute into the interstitial and intracellular fluids.
Distribution
the drug may be biotransformed by metabolism by the liver or other tissues.
Metabolism
the drug and its metabolites are eliminated from the body in urine, bile, or feces.
Elimination
ADME Explained
Absorption, distribution, metabolism, excretion
For a chemical compound to become a marketable drug, that compound must have favourable properties in addition to efficacy (its therapeutic effect) and safety.
Absorption, Distribution, Metabolism and Excretion
- A compound’s ability to pass through barriers such as the intestinal lining, the nasal lining, the lungs or the skin.
ABSORPTION
- How the compound is distributed around the body and its propensity to accumulate in certain tissues or organs.
DISTRIBUTION
- How the body breaks down the compound, normally by the liver. The key issues are drug-drug interactions, and the effects of the metabolites (the new chemicals created as a result of metabolism).
METABOLISM
- The rate and process through which the compound exits the body.
EXCRETION
route, get into the system rapidly and more efficiently
INTRAVASCULAR
not undergo absorption since it is administered directly into the systemic circulation
IV
(oral, peroral, rectal, etc) need to undergo a liberation process (depending on the dosage form used) prior to absorption. Drugs that undergo absorption, especially via the GI tract need to be in solution.
extravascular
Explain difference between oral and peroral
peroral-direct swallowing the absorption is stomach
oral-inside the mouth the absorption is mouth cavity
drug molecules cross the biological membrane more rapidly and efficiently than the ionized, more polar moieties.
Small, nonionic, and lipophilic
is the process by which a drug leaves the systemic circulation and enters the various compartments (tissue compartments).
Disposition
collective term of distribution, metabolism, elimination
Disposition
e.g. CNS, heart, etc
distribution
which organ undergo metabolism and excretion
liver
for excretion
kidneys
process terminates the action of the drug by promoting its CLEARANCE
ELIMINATION
Meaning ng CLEARANCE
total volume that will undergo excretion
provides the fundamental concept of the PK characteristics of drugs based on the degree of ionization as influenced by pH.
Henderson-Hasselbalch equation
- At low pH (acid environment) weak acids are in their unionized form.
- The unionized form is more lipophilic, and thus can cross the membrane rapidly and efficiently through passive diffusion.
- Weak acids remain unionized in the acid region of the GIT (stomach), thus optimum absorption occurs in this area.
- At high pH (basic environment) weak acids become ionized, thus more polar in character.
- Excretion is favorable when the drug is in its ionized form.
WEAK ACIDS
- are best absorbed in the alkaline region of the GIT (small intestines) because they are in their unionized form. As mentioned earlier, unionized moieties are nonpolar and lipophilic, so can cross the membranes more efficiently.
- To promote the excretion of weak bases, an acid environment (low pH) is desired since it could make alkaline drugs become more ionized. More ionized forms of the drug are polar and less lipophilic (hydrophilic), and thus are excretable.
- Permeation across the membrane is an important PK principle that determines the ability of the drug to reach circulation and be distributed to various organs and reach its site of action.
WEAK BASES
This law describes the passive flux of molecules down a concentration gradient (from a region of higher concentration to a region of lower concentration)
FICK’S LAW
against the concentration gradient
active transport system
along the concentration gradient
passive
utilized a carrier or transporter to cross the membrane
active transport and facilitated diffusion (carrier-mediated)
Vesicular transport is a mechanism of drug permeation that involves the engulfment of impermeant molecules by the vesicles in the cell membrane via
endocytosis (pinocytosis or phagocytosis)
Vesicular transport release into the cell, and expulsion of the material via
membrane vesicles (exocytosis)
Meaning disintegration and dissolution
disintegration - time
dissolution - amount
vesicular transport system - liquid
pinocytosis
vesicular transport system - large molecules
phagocytosis
drug leaves systemic circulation
disposition
med for diabetic to block carbohydrates after ng first na subo inom ng gamot
acarbose
well-closed container
paghindi magvovolatilized
no API
nitrostat
The next event leads to understanding how drugs work at the organ and tissue levels, real advances in basic pharmacology during this time were accompanied by an outburst of unscientific claims by manufacturers and marketers of worthless
“patent medicines.”
The molecular mechanisms of action of many drugs have been
identified, and numerous receptors have been isolated, structurally characterized, and cloned
It is the relation of the individual’s genetic makeup to his or her response to specific drugs. This leads to several advances in therapeutics such as:
1) Investigation of small interfering RNAs (siRNAs) and microRNAs (miRNAs) as therapeutic agents
2) Short nucleotide chains called antisense oligonucleotides (ANOs), were synthesized to be complementary to natural RNA or DNA
