Drug Receptors and Interactions

These flashcards cover key vocabulary terms and concepts related to drug receptors and interactions, focusing on definitions and examples necessary for exam preparation.

Druable target

A drug target that is approachable and has a defined binding pocket.

Validation of target

Validation of a target involves checking for compensatory mechanisms and differences between animal models and humans.

Economic viability of drug targets

An assessment of whether a drug target is profitable to pursue, particularly in relation to rare diseases in developing countries.

GPCR

G-Protein Coupled Receptors, which make approximately 35% of drug targets.

Duggable genome

The subset of the human genome that expresses proteins able to bind drug-like molecules.

Pharmaceautical intervention

Pharmaceutical interventions are aimed at recognizing endogenous chemicals.

Ligand

A molecule that binds to a receptor to induce a response.

Agonist

A substance that activates a receptor to produce a response.

Antagonist

A substance that binds to a receptor but does not produce a response.

Partial agonist

A substance that binds to a receptor and produces a response less than that of a full agonist.

Inverse agonist

A substance that binds to a receptor and decreases its activity compared to baseline.

Orphan receptors

Receptor-like proteins predicted without an identified endogenous ligand; potential drug targets.

Efficacy

The greatest effect produced by a drug.

Potency

The amount of drug required to produce a given intensity of effect.

Constitutive activity

Activity of receptors in the absence of a ligand.

Active state

The conformation of a receptor that induces a biological response upon activation.

Inactive state

The conformation of a receptor that does not produce a biological response.

Allosteric site

An additional site on a receptor where a ligand can bind and alter the receptor's activity.

Orthosteric site

The primary active site where ligands bind and induce a response.

EC50

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

kD

The dissociation constant representing the drug concentration required to saturate 50% of receptors.

Binding affinity

The strength of interaction between a drug and its receptor.

Spare receptors

Receptors that exist in excess of those required to produce a full effect.

Chemical bonding

Forces that govern receptor affinity including ionic, hydrogen, and hydrophobic bonds.

Positive allosteric modulators

Compounds that bind to an allosteric site enhancing the effect of an orthosteric agonist.

Negative allosteric modulators

Compounds that bind to an allosteric site reducing the effect of an orthosteric agonist.

Neutral allosteric ligands

Compounds that bind to an allosteric site without affecting the activity of the orthosteric ligand.

Allosteric modulation

Dynamic changes in receptor activity due to ligand binding at sites other than the active site.

Competitive antagonist

A drug that binds to the same site as the agonist in a reversible manner.

Non-competitive antagonist

A drug that binds to an agonist binding site either irreversibly or pseudo-irreversibly.

Irreversible antagonists

Antagonists that form a permanent bond with receptors preventing activation.

Pharmacodynamics

The study of how drugs affect an organism.

Pharmacokinetics

The study of how drugs are absorbed, distributed, metabolized, and eliminated in the body.

Drug receptor binding

The interaction where a drug binds to a receptor to elicit a response.

Transcription factors

Proteins that bind to specific DNA sequences to control the transcription of genetic information.

Agonist vs Antagonist

Agonists activate receptors; antagonists prevent activation.

Enzyme inhibitors

Compounds that decrease the activity of enzymes.

Tyrosine kinase receptors

Receptors that exercise their action through phosphorylation of tyrosines.

Ion channels

Membrane proteins that allow ions to flow into or out of a cell.

Second messengers

Intracellular signaling molecules that mediate cellular responses to extracellular signals.

Transcription and translation

Processes by which genetic information is copied and protein synthesis occurs.

Drug efficacy vs potency

Efficacy refers to the maximal response a drug can produce; potency refers to the amount of drug needed to produce an effect.

Furosemide

A diuretic with greater efficacy than hydrochlorothiazide.

Hydrophobic bonds

Non-polar interactions that can influence drug-receptor affinity.

Electrostatic bonds

Attractive forces between charged groups that can affect drug binding.

Van der Waals bonds

Weak attractions due to transient dipoles that impact drug interactions.

Drug affinity measurement

Graphically represented through the drug concentration versus response curve.

Dopaminergic neurotransmission

Transmission relying on the neurotransmitter dopamine in the brain.

Aripiprazole

A partial agonist used to treat depression and autism.

L-Dopa

A dopamine agonist indicated for Parkinson's disease treatment.

Seroquel (Quetiapine)

An antagonist for dopamine receptors used in schizophrenia and bipolar disorders.

Haloperidol

An inverse agonist used to manage severe schizophrenia symptoms.

Economic factors in drug development

Considerations surrounding the profitability and marketability of drug targets.

Drug metabolism classification

Involves phase I and phase II reactions that modify drugs in the body.

G-proteins

Molecules that transmit signals from receptors to target proteins in a cell.

Drug discovery phase

The stage of research intended to identify potential new drugs.

Clinical trials

Research studies that test how well new medical approaches work in people.

Bayesian statistics

Statistical methods that can be applied in evaluating clinical trials.

Molecular docking

A method used to predict how small molecules (ligands) will bind to a receptor.

Clinical efficacy

The performance of a drug in clinical settings to achieve a therapeutic outcome.

Drug interaction types

The classification of how different drugs affect each other's pharmacological effects.

Receptor agonism

The process by which an agonist interacts with and activates a receptor.

Acute pharmacological effects

Immediate effects resulting from drug interaction with receptors.

Chronic pharmacological effects

Effects that develop over time with continued drug administration.

Patient compliance

The degree to which a patient correctly follows medical advice regarding medication dosages.

Genetic polymorphisms

Variations in genes that can influence patient responses to drugs.

Pharmaceutical marketing

Strategies used in promoting and selling drugs to healthcare providers and patients.

Adverse effects

Unwanted or harmful reactions to a drug.

Drug approval process

Regulatory pathway that drugs must follow to be approved for public use.

Clinical endpoints

Outcomes used to measure the effectiveness of a treatment in clinical trials.

Therapeutic index

The ratio between the toxic and therapeutic dose of a drug.

Bioavailability

The fraction of an administered dose of drug that reaches the systemic circulation.

Formulary

A list of medications that are approved for use within a particular healthcare system.

Drug reformulation

The process of altering the composition of a drug to enhance its effectiveness or safety.

Medication error

Mistakes in prescribing, dispensing, or administering drugs.

Antidiuretic hormone

Hormone that helps control water balance in the body.

Bioequivalence

The property wherein two drugs with identical active ingredients yield the same bioavailability.

Nanomedicine

The application of nanotechnology for drug delivery and treatment.

Pharmacy compounding

The process of creating personalized medication preparations for patients.

Pharmacogenetics

The study of how genes affect an individual’s response to drugs.

Therapeutic drug monitoring

The clinical practice of measuring specific drug levels in a patient's bloodstream.

Drug formulations

Combinations of active and inactive ingredients to create a medicine.

Regulatory affairs

Profession related to ensuring compliance with regulations governing drug development and approval.

Placebo effect

The beneficial effect in a patient following a treatment that is not due to the properties of the treatment itself.

Over-the-counter drugs

Medications that can be purchased without a prescription.

Prescription drugs

Medicines that require a medical prescription to be dispensed.

Controlled substances

Drugs that are subject to regulations because of their potential for abuse.

U.S. Food and Drug Administration (FDA)

The agency responsible for protecting public health by regulating food, pharmaceuticals, and other health-related products.

International Conference on Harmonisation (ICH) guidelines

Guidelines to promote uniform standards in the development of medicines globally.

Clinical research organization (CRO)

Service organization that provides support to the pharmaceutical industry in the form of research services.

Compounding pharmacies

Pharmacies specialized in preparing personalized medications.

Drug withdrawal effects

Physical or mental symptoms that occur when a drug is eliminated from a patient's body.

Monoclonal antibodies

Antibodies made by identical immune cells that are all clones of a unique parent cell.

Vaccines

Biological preparations that provide acquired immunity to particular diseases.

Gene therapy

An experimental technique that uses genes to treat or prevent disease.

Homeopathic medicine

A system of alternative medicine that treats illness with highly diluted substances.

Biologic drugs

Medicinal products made from living organisms or contain components of living organisms.