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The study of substances that interact with living systems through chemical processes, especially by binding to regulatory molecules and activating or inhibiting normal body processes

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PHARMACOLOGY

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PHARMACOLOGY 1 - Details

Levels:

1) Chapter 1 View
2) Chapter 2 View
3) Chapter 3 View
4) Chapter 4 - Cholinergic Agonists View
5) CHAPTER 5 - CHOLINERGIC ANTAGONISTS View
6) Chapter-6.pdf View
7) CHAPTER 7 Adrenergic Antagonists View
8) ANXIOLYTIC & HYPNOTIC DRUGS View
9) ANTIPSYCHOTICS CHAPTER 11 View
10) Drugs Neurodegenerative CHAPTER 8 View
11) Drugs for Epilepsy Chapter 12 View
12) CHAPTER 13 general anesthetics View
13) CHAPTER 14 local anesthetics View
14) CHAPTER 16 View

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The study of substances that interact with living systems through chemical processes, especially by binding to regulatory molecules and activating or inhibiting normal body processes

PHARMACOLOGY

The science of substances used to prevent, diagnose and treat disease.

Medical Pharmacology

The branch of pharmacology that deals with the UNDESIRABLE effects of chemicals on living systems, from individual cells to humans to complex ecosystems.

TOXICOLOGY

The science of drug preparation and the medical use of drugs -- the precursor of pharmacology

Materia Medica

Two General Principles (PHARMACOLOGY)

1 All substances can under circumstances be toxic, and the chemicals in botanicals are no different from chemicals in manufactured drugs except for the proportion of impurities 2 All dietary supplements and all therapies promoted as health-enhancing should meet the same standards of efficacy and safety as conventional drugs and medical therapies

The study of the GENETIC VARIATIONS that cause differences in drug response among individuals or populations.

Pharmacogenomics (also called Pharmacogenetics)

The absorption, distribution, metabolism, and excretion of a drug

Pharmacokinetics

The biochemical and physical effects of drugs and the mechanisms of drug actions

Pharmacodynamics

The use of drugs to prevent and treat disease

Pharmacotherapeutics

A scientific name that precisely describes its atomic and molecular structure

Chemical Name

Nonproprietary name Abbreviation of the chemical name

Generic Name

Brand name/ Proprietary name Selected by the drug company selling the product Protected by copyright

Trade Name

Family Drugs that share similar characteristics Ex: Beta-adrenergic blockers

Pharmacologic Class

Groups drugs by therapeutic use Ex: Antihypertensives

Therapeutic Class

1 the most active component in plants, react with acids to form a salt that can dissolve more readily in body fluids (Atropine, Nicotine, Colchicine, Hyoscine) 2 also an active component in plants (Ex: Digoxin, Senna)

1 Alkaloids 2 Glycosides

1 give products the ability to attract and hold water (Ex: Seaweed extractions) 2 of which the chief source is pine tree sap, commonly act as local irritants or as laxatives 3 thick and sometimes greasy liquids, are classified as volatile or fixed

1 Gums 2 Resins 3 Oils

POWER PLANT:

1 Alkaloids 2 Glycosides 3 Gums 4 Resins 5 Oils

Animal Magnetism Drugs obtained from animal sources

1 hormones such as insulin 2 oils and fats (usually fixed) - cod liver oil 3 enzymes - pancreatin and pepsin 4 vaccines

Mineral Springs: __

• Iron • Iodine • Epsom salt

Drugs produced in the laboratory

Down to DNA

Routes of Administration

• buccal, sublingual, translingual • gastric • intradermal • intramuscular • intravenous • oral • rectal and vaginal • respiratory • subcutaneous • topical

Any substance that brings about a change in biologic function through its chemical actions

DRUG

1 activator -has affinity to the receptor and intrinsic activity 2 Inhibitor -has affinity only

1 AGONIST 2 ANTAGONIST

Inhibitor has affinity only

ANTAGONIST

Specific molecule in the biologic system that plays a regulatory role and where the drug molecule interacts

RECEPTOR

May interact directly with other drugs

Chemical Antagonists

From Greek "xenos," meaning stranger not synthesized in the body

XENOBIOTICS

Drugs that have almost exclusively harmful effects

POISONS

Poisons of biologic origin (ie. synthesized by plants and animals, in contrast to inorganic poisons such as lead and arsenic)

TOXINS

The Physical Nature of Drugs

• Solid - Aspirin, Atropine • Liquid - Nicotine, Ethanol • Gaseous - Nitrous Oxide

Drug Size, SMALLEST and LARGEST

1 Smallest -- Lithium ion (MW 7) 2 Largest -- Alteplase (MW 59,050) 3 Most drugs -- MW 100-1000

Three major types of bonds

1 covalent, 2 electrostatic and 3 hydrophobic

Very strong bond and in many cases not reversible under biologic conditions EX. Aspirin with cyclooxygenase enzyme; DNA-alkylating agents used in cancer chemotherapy

COVALENT BONDS

Vary from relatively strong linkages between permanently charged ionic molecules to weaker hydrogen bonds and very weak induced dipole interactions such as van der Waals forces WEAKER THAN COVALENT BONDS

Electrostatic Bonding

Usually quite weak and are probably important in the interactions of highly lipid-soluble drugs with the lipids of cell membranes and perhaps in the interaction of drugs with the internal walls of receptor "pockets"

HYDROPHOBIC BONDS

Dependent on the chirality (stereoisomerism) of the drug chemical structure

DRUG SHAPE

Implies the ability to predict the appropriate molecular structure of a drug on the basis of information about its biologic receptor

Rational Drug Design

Must undergo extensive animal studies

IND - Investigational New Drug

1 actions of drug on the body 2 actions of the body on the drug

1 Pharmacodynamics 2 Pharmacokinetics

• Liberation of an active ingredient from the dosage form • Absorption into systemic circulation • Distribution • Metabolism in the body • Excretion of the drug from the body • Response

LADMERS

The drug is tested on healthy volunteers

Phase I

Involves trials with people who have the disease for which the drug is thought to be effective.

Phase II

Large number of patients in medical research centers receive the drug provides information about infrequent or rare adverse effects FDA will approve a new drug application if satisfactory

Phase III

Voluntary and involves postmarket surveillance of the drug's therapeutic effects at the completion of phase III.

Phase IV

Exceptions to the Rule

1 Public health threat of disease like AIDS, COVID-19 2 Sponsors of drugs that reach phase II or III clinical trials can apply for FDA approval of treatment IND status

1 actions of drug on the body 2 actions of the body on the drug

1 Pharmacodynamics 2 Pharmacokinetics

LADMERS

• Liberation of an active ingredient from the dosage form • Absorption into systemic circulation • Distribution • Metabolism in the body • Excretion of the drug from the body • Response

The transfer of a drug from the site of administration to the bloodstream

Absorption

The drug moves from a region of high concentration to one of lower concentration - does not involve a carrier and not saturable - movement is along the concentration gradient

Passive Diffusion

• directly proportional to the concentrations, surface area and permeability coefficient • inversely proportional to the thickness of the membrane

Fick's Law of Diffusion

Drugs enter the cell through specialized transmembrane carrier proteins that facilitate the passage of large molecules – movement is along concentration gradient – does not require energy & can be saturated – may be inhibited by compounds that compete for the carrier

Facilitated Diffusion

Involves specific carrier proteins that span the membrane – energy-dependent & saturable – movement is against the concentration gradient – selective and may be competitively inhibited by other cotransported substances

Active Transport

Engulfment of a drug by the cell membrane and transport into the cell by pinching off the drug-filled vesicle

Endocytosis

Reverse of endocytosis

Exocytosis

Factors influencing absorption

1 Effect of pH on drug absorption 2 Blood flow to the absorption site 3 Total surface area available for absorption 4 Contact time at the absorption surface

Absorbs nutrients in the small intestine

Microvilli

Responsible for transporting various molecules, including drugs, across cell membranes - "pumps" drugs out of the cells - associated with multi-drug resistance

Expression of P-glycoprotein

• the fraction (F) of the administered dose that reaches the systemic circulation • determined by comparing plasma levels of drugs after a particular route of administration with levels achieved by IV administration

Bioavailability

Bioavailability is usually measured using __

Area Under the Curve (AUC)

1) 100% Bioavailability, most rapid onset 2) 5 to <100 Bioavailability, most convenient; may have significant First Pass Effect

1 Intravenous 2 Oral

Factors Influencing Bioavailability: when a drug is absorbed from the GI tract, it enters the PORTAL CIRCULATION before entering the systemic circulation

First-pass Hepatic Metabolism

Factors Influencing Bioavailability

1 First-pass Hepatic Metabolism 2 Solubility of the drug 3 Chemical instability 4 Nature of the drug formulation

Show comparable bioavailability and similar times to achieve peak blood concentrations

BIOEQUIVALENCE

Pharmaceutically equivalent with similar chemical and safety profiles

THERAPEUTIC EQUIVALENCE

If the drugs have the same dosage form, contain the same active ingredient, and use the same route of administration

Pharmaceutical Equivalence

The process by which a drug reversibly leaves the bloodstream and enters the instertitium (extracellular fluid) and the tissues

DRUG DISTRIBUTION

The process by which a drug reversibly leaves the bloodstream and enters the instertitium (extracellular fluid) and the tissues.

DRUG DISTRIBUTION

In Drug distribution, many drugs bind to __, including albumin, with an equilibrium between bound and free molecules Competition between drugs for plasma protein binding sites may increase the "__,“ possibly enhancing the effects of the drug displaced

Plasma proteins, free fraction

What are the Special Barriers to Distribution?

1 Placental (most small molecular weight drugs cross the placental barrier; fetal blood levels are usually lower than maternal) 2 Blood-brain (permeable only to lipid-soluble drugs or those of very low molecular weight)

• Concentration of drug at the receptor site • Commonly measured in the blood (Exception for topical agents)

EFFECTIVE DRUG CONCENTRATION

Plasma concentration is a function of

– the rate of input of the drug (by absorption) into the plasma – the rate of distribution – and the rate of elimination

Pharmacokinetics TWO BASIC PARAMETERS

1 CLEARANCE 2 VOLUME OF DISTRIBUTION

The measure of the ability of the body to eliminate the drug

CLEARANCE

The measure of the apparent space in the body available to contain the drug.

VOLUME OF DISTRIBUTION

The ratio of the amount of drug in the body to the drug concentration in the plasma or blood

Volume of distribution -Can be affected by liver and kidney disease

METABOLISM OF DRUGS Three major routes:

– Hepatic metabolism – Biliary metabolism – Urinary metabolism

Metabolism (Biotransformation) PHASES

1) Phase I (Functionalization) – Redox Reactions and hydrolysis. 2) Phase II (Conjugation) – Attacks certain drugs with existing functional groups and attaches conjugate molecules

What kind of reaction is common for neonates?

Sulfation

Metabolism (Biotransformation) May be affected by

• Drug Interactions due to inducers, inhibitors, and substrates • Genetic factors • Disease states DRUG WITH INDUCER - FASTER DRUGS WITH INHIBITOR - SLOWER

An inactive precursor chemical that is readily absorbed and distributed and then converted to the active drug by biologic processes inside the body Can be Active to Active, Inactive to Active

Prodrug

EXCRETION; Renal elimination of drugs:

– Glomerular filtration – Proximal tubular secretion – Distal tubular reabsorption

Excretion process

1 Glomerular filtration of water and unbound drugs and metabolites 2 Active tubular secretion of acidic and basic drugs and metabolites 3 Active reabsorption of acidic and basic endogenous compounds and passive reabsorption of lipophilic drugs 4 Urinary excretion of drugs and metabolites that are filtered and or actively secreted and not reabsorbed

Describes the actions of a drug on the body and the influence of drug concentrations on the magnitude of the response

PHARMACODYNAMICS

The component of a cell or organism that interacts with a drug and initiates the chain of events leading to the drug's observed effects

RECEPTOR

• Their ligands are presently unknown • May prove useful targets for the development of new drugs.

ORPHAN RECEPTORS

• MEDIATE the actions of endogenous chemical signals such as neurotransmitters, autacoids and hormones.

REGULATORY PROTEINS

• also identified as drug receptors • may be inhibited or activated by binding a drug • Ex: dihydrofolate reductase for methotrexate

ENZYMES

Membrane receptor for digitalis glycosides a TRANSPORT PROTEIN

Na+/K+ ATPase Pump