PHARMACOLOGY M1.1 - 1.2 Flashcards by Sky Blue

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

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study of drugs

Pharmacology

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is the body of knowledge concerned with the action of chemicals on biologic systems.

Pharmacology

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2 Nature of drug

Pharmacodynamics and pharmacokinetics

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receptor, receptor sites and inert binding sites

Pharmacodynamics

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movement of drugs in body, absorption, distribution, metabolism, elimination

Pharmacokinetics

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4 Drug development and regulation

safety and efficacy
animal testing
clinical trials
Patients and generic drugs

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is defined as the science of substances used to prevent, diagnose, and treat disease.

MEDICAL PHARMACOLOGY

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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

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the science of medical use of drugs, was developed as the precursor to pharmacology

Materia Medica

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developed the methods of experimental physiology and pharmacology

Francois Magendie and his student Claude Bernard

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It may be defined as any substance that brings about a change in biologic function through its chemical actions.

Drug

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activator of a specific molecule

Agonist

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inhibitor of a specific molecule

Antagonist

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“the target molecule” for drug

Receptor

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A drug may be synthesized within the body

HORMONES

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it may be chemicals not synthesized in the body

Xenobiotics - “stranger”

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refers to a drug that have almost exclusively harmful effects

poison

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The dose of the drug makes the poison

Paracelsus

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Full name of Paracelsus

theophrastus phillipus auroleus bosbastus von hohenheim

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may be solid, liquid or gas. It may be organic or inorganic.

Drugs

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very strong; not reversible. Aspirin (acetyl group) and cyclooxygenase is an example of this type of interaction

Covalent

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weaker than covalent; vary from relatively strong linkages between permanently charged ionic molecules to weaker hydrogen bonds and very weak induced dipole forces

Electrostatic

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usually quite weak; it is the interaction of highly lipid-soluble drugs with the lipids of the cell membrane

Hydrophobic

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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

(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