PDA BIGGIEQUIZ (goodluck)

Pharmacology

The study of the action and effects of chemical substances (drugs) on living systems, from individual cells to complex body organs.

Pharmacodynamics

The term used to describe how the drug affects the body (includes biochemical, cellular, and physiological effects of drugs, as their mechanisms of action).

Receptors

A macromolecule or component of a cell or organism that interacts with a drug/ligand and initiates the chain of events leading to the drug's observed effects.

Binding affinity

A measure of the attraction force between the receptor and the drug.

Intrinsic activity

A measure of the ability of a drug to generate an effect.

Selectivity

A measure of the ability of the drug to solely interact with its intended target.

Up-regulation

Increase the number of receptors.

Down-regulation

Decrease the number of receptors.

Desensitization

An intrinsic pharmacological property of the receptor where, in the prolonged presence of an agonist, the receptor becomes desensitized/inactivated (i.e., decrease or loss in response).

Signal transduction

The process by which receptors transmit the message after sensing the ligand.

Transmembrane receptors

Integral component of the cell membrane with extracellular ligand binding domain and intracellular signal transmitting domain.

Intracellular receptors

Receptors found in the nucleus or translocated to the nucleus after ligand binding, with ligands that are lipid soluble to cross the plasma membrane.

Receptor Reserve or Spare Receptor

Maximal effect does not require occupation of all receptors by agonist; EC50 is less than Kd for this system.

Agonist

A substance that activates a receptor to produce a biological response.

Antagonist

A substance that blocks or dampens the biological response by binding to and blocking a receptor.

EC50

The concentration of a drug that produces 50% of its maximum effect.

Kd

The equilibrium dissociation constant, a measure of the affinity of the drug for its receptor.

Potency

The amount of drug needed to produce a given effect.

Efficacy

The maximum effect that can be achieved with a drug.

What is the goal of drug therapy?

To achieve a desired beneficial effect with minimal adverse effects.

What is the relationship between drug concentration and its effects?

A relationship exists between the beneficial or toxic effect of a drug and its plasma concentration.

What are the two main principles combined to clarify the dose-effect relationship?

Pharmacodynamics and pharmacokinetics.

What is the therapeutic range?

The concentration range between minimal effective concentration for therapeutic response and minimal toxic concentration.

What does pharmacokinetics study?

What the body does to the drug; the relationship of drug dose and drug concentration.

What does pharmacodynamics study?

What the drug does to the body; the relationship of drug concentration and drug effect.

What is drug disposition?

The fate of a drug after its absorption, including distribution, metabolism, and excretion.

What is absorption in pharmacology?

The movement of a drug from its site of administration to the systemic circulation.

What is Cmax?

The maximum concentration of a drug in the bloodstream after administration.

What is the definition of drug metabolism?

The processes by which biochemical reactions alter drugs within the body.

What is enterohepatic recycling?

The process where drugs and metabolites are reabsorbed back into the body from the intestine.

What are the routes of administration?

The paths by which a drug is brought into contact with the body, including enteral, parenteral, topical, and transdermal.

What is the primary organ for drug metabolism?

The liver.

What is excretion in pharmacology?

The process whereby drugs or metabolites are irreversibly transferred from internal to external environment.

What are the three types of elimination?

Cellular, renal, and hepatic.

What is the role of CYP P450s?

A family of proteins specialized to metabolize various compounds.

What is the significance of the half-life (t1/2) in pharmacokinetics?

It is the time required for the concentration of the drug in the bloodstream to reduce to half its initial value.

What is the purpose of drug clearance (CL)?

To measure the rate at which a drug is removed from the body.

What is the difference between an active drug and a prodrug?

An active drug is pharmacologically active, while a prodrug is inactive until metabolized into an active form.

What is the function of ABC transporters?

To mediate drug secretion to the filtrate during renal excretion.

What is the importance of drug distribution?

It refers to the transport processes that deliver a drug to various body areas after absorption.

What are the implications of drug toxicity?

Toxicity occurs when drug concentrations exceed the minimal toxic concentration, leading to adverse effects.

What is the definition of a therapeutic window?

The range of drug concentrations that provide therapeutic effects without causing toxicity.

What is the significance of renal excretion?

It is a primary route through which many drugs are eliminated from the body.

What are the potential outcomes of drug metabolism?

Conversion to an inactive drug, conversion to a more active or toxic metabolite, or conversion of a prodrug to an active drug.

What is the role of transport processes in drug distribution?

They deliver drugs to various body areas, evidenced by changing concentrations in tissues and fluids.

What is the first step in drug discovery?

Identify disease

What is the typical duration for drug development?

12-15 years

What is the average cost for developing a drug?

Up to $1.2 billion

What is the success rate of drugs from initial development to FDA approval?

Less than 2% for biological activity and less than 10% for clinical trials.

What does SAR stand for in medicinal chemistry?

Structure-activity relationship

What is a lead compound?

A compound with desirable biological activity but likely needs improvement.

What are the sources of 'hits' in drug discovery?

Synthetic origin (50%), plants (25%), microorganisms (12%), animals (6%), minerals (6%), biotechnology (1%).

What is the significance of natural products in drug discovery?

They can be isolated from whole plants/animals, selected parts, extracts, or synthesized.

Give an example of a natural product used in medicine.

Cocaine, used as a prototype for amino alcohol esters.

What is the mechanism of action (M.O.A.) of sulfonamides?

They interfere with folic acid synthesis by competing with PABA for the enzyme dihydropteroate synthetase.

What is the role of high-throughput screening (HTS) in drug discovery?

It allows for rapid testing of many compounds for desired pharmacological effects.

What is Lipinski's Rule of Five?

Criteria for orally active drugs: MW < 500, H-bond donors ≤ 5, H-bond acceptors ≤ 10, Log P ≤ 5.

What are the two types of computer-aided drug design?

Structure-based drug design (SBDD) and ligand-based drug design (LBDD).

What is the difference between hard drugs and soft drugs?

Hard drugs are chemically stable, while soft drugs have shorter lifetimes and faster onset.

What are functional groups in organic chemistry?

Structural units responsible for the characteristic behavior of molecules.

What is the significance of heteroatoms in organic compounds?

They confer different physical and chemical properties to the substance.

What are alkanes?

Hydrocarbons consisting only of carbon and hydrogen with single bonds.

What are the numerical roots for carbon chains in alkanes?

Meth- (1), Eth- (2), Prop- (3), But- (4), Pent- (5), Hex- (6), Hept- (7), Oct- (8), Non- (9), Dec- (10).

What is the main characteristic of alkenes?

They contain at least one carbon-carbon double bond (C=C).

What is the role of branching in alkanes?

Branching lowers boiling point due to decreased surface contact.

What is the significance of the discovery of penicillin?

It was the first antibiotic and marked a major achievement in chemotherapy.

What are the two main types of synthesis in drug development?

Conventional synthesis and combinatorial chemistry.

What is the purpose of QSAR studies in drug design?

To relate chemical structure to biological activity.

What is the importance of the Brookhaven protein database?

It provides access to X-ray and NMR structures of proteins for drug design.

What is the definition of a 'hit' in drug discovery?

A new active compound identified for desired pharmacological effects.

What is the role of combinatorial libraries in drug discovery?

They allow for the rapid synthesis and screening of multiple compounds.

What is the mechanism of action of antibiotics like penicillins?

They inhibit bacterial cell wall synthesis.

What are alkenes chemically less stable than?

Alkanes

What modification occurs to double bonds of lipids?

They are modified to vicinal diols.

What is olefinic oxidation?

Non-aromatic double bond oxidation.

What is the role of Cyto-P450 in metabolism?

It catalyzes the hydroxylation of aromatic hydrocarbons.

What is a major product of aromatic hydroxylation?

p-hydroxy derivatives.

What is the effect of aromatic hydroxylation on drug solubility?

It significantly increases water solubility, leading to rapid drug elimination.

What are halogenated hydrocarbons commonly used for?

As inhalation anesthetics.

What is a side effect of halothane?

Severe liver dysfunction (hepatic necrosis).

What is the main characteristic of alcohols?

They are organic compounds with a hydroxyl group (-OH) bound to a saturated carbon.

What distinguishes primary, secondary, and tertiary alcohols?

The number of carbon atoms bonded to the carbon with the hydroxyl group.

What happens to alcohols in the presence of oxidizing agents?

They can be oxidized to acids, aldehydes, or ketones.

What is the antidote for methanol poisoning?

Ethanol, as it competes with alcohol dehydrogenase.

What defines phenols?

They are compounds with a hydroxyl group directly bonded to an aromatic ring.

How do phenols differ from alcohols in terms of acidity?

Phenols are weakly acidic, while alcohols are neutral.

What is the effect of resonance on phenolate ions?

Resonance stabilizes the ionized form.

What is the general formula for ethers?

R-O-R', where R and R' are alkyl or aryl groups.

What is a significant risk associated with ethers?

They can form peroxides in the presence of air, which are explosive.

What is the primary characteristic of aldehydes?

They contain a carbonyl group with at least one hydrogen substituent.

What distinguishes ketones from aldehydes?

Ketones have two substituents that are not hydrogen.

What is the role of CYP450 in ether metabolism?

It catalyzes the O-dealkylation of ethers.

What are the physical properties of halogenated hydrocarbons?

They have poor water solubility and are lipophilic.

What is the significance of p-hydroxylation in drug metabolism?

It enhances the elimination of drugs by increasing their water solubility.

What is a common use of hydrofluoroalkanes (HFAs)?

They are used as propellants in asthma inhalers.

What is the impact of halogenation on flammability?

An increase in halogens decreases flammability.

What is a unique property of tertiary alcohols?

They are stable to oxidase enzymes.

What happens to phenols when exposed to air?

They are prone to oxidation, leading to highly colored products.

How should salts of phenols be stored?

In closed, amber containers with antioxidants to protect from light and oxygen.

What is the general structure of a ketone?

R1 and R2 are alkyl or aryl groups, with a carbonyl group (C=O) in the center.