Pharmacology: Drug Action and Effects
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[Blank] is the branch of medical sciences concerned with the study of the uses, effects, and modes of action of drugs.

Pharmacology

A ______ is any natural, synthetic, or endogenous molecule that can exert a physiological and/or biochemical effect on a cell, tissue, organ, or whole organism.

drug

Drugs, also called medication or medicine, are used for treating, curing, preventing, or ______ a disease, or to promote health and well-being.

diagnosing

The interactions of a drug with a biological system, or the body, are ______; the drug interacts with the body, and the body also interacts with the drug.

<p>bidirectional</p> Signup and view all the answers

Substances derived from plants and animals have been sources of pharmacologically active compounds used to treat disease since early human ______.

<p>history</p> Signup and view all the answers

Molecules not synthesized in the body are called ______, derived from the Greek word xenos, meaning 'stranger'.

<p>xenobiotics</p> Signup and view all the answers

[Blank] are drugs that almost exclusively have harmful effects.

<p>Poisons</p> Signup and view all the answers

The term pharmacology is derived from the Greek words pharmakon, meaning a drug or ______, and logos, meaning a word or discourse.

<p>poison</p> Signup and view all the answers

[Blank] is the degree to which a drug acts on a given site relative to other sites; it relates largely to physicochemical binding of the drug to cellular receptors.

<p>Selectivity</p> Signup and view all the answers

A drug's ability to affect a given receptor is related to the drug's ______ (probability of the drug occupying a receptor at any given instant) and intrinsic efficacy or activity.

<p>affinity</p> Signup and view all the answers

The pharmacologic effect is determined by the duration of time that the ______ persists (residence time).

<p>drug-receptor complex</p> Signup and view all the answers

The lifetime of the drug-receptor complex is affected by ______ (conformational changes) that control the rate of drug association and dissociation from the target.

<p>dynamic processes</p> Signup and view all the answers

The ability of a drug to bind to a receptor is influenced by ______ as well as by intracellular regulatory mechanisms.

<p>external factors</p> Signup and view all the answers

Receptor ______ affects adaptation to drugs (eg, desensitization, tachyphylaxis, tolerance, acquired resistance, postwithdrawal supersensitivity).

<p>up-regulation and down-regulation</p> Signup and view all the answers

Ligands bind to precise molecular regions, called ______, on receptor macromolecules.

<p>recognition sites</p> Signup and view all the answers

A drug's affinity and activity are determined by its ______.

<p>chemical structure</p> Signup and view all the answers

Drugs that bind to molecular sites not designated as receptors, such as plasma proteins, undergo ______ drug binding.

<p>nonspecific</p> Signup and view all the answers

[Blank] agonists bind to a different or adjacent site on the receptor.

<p>allosteric</p> Signup and view all the answers

[Blank] agonists stabilize the receptor in its inactive conformation.

<p>inverse</p> Signup and view all the answers

If a substance normally decreases cellular function, an antagonist will ______ cellular function.

<p>increase</p> Signup and view all the answers

[Blank] antagonists form a stable, permanent bond with the receptor.

<p>irreversible</p> Signup and view all the answers

[Blank] antagonists slowly dissociate from their receptor.

<p>pseudo-irreversible</p> Signup and view all the answers

In ______ antagonism, the agonist and antagonist can bind simultaneously, but the antagonist reduces or prevents the agonist's action.

<p>noncompetitive</p> Signup and view all the answers

In reversible competitive antagonism, increasing the concentration of the ______ can overcome the antagonism.

<p>agonist</p> Signup and view all the answers

Using the topical route, a cream like ______ can be applied to the lips for treating herpes labialis.

<p>acyclovir</p> Signup and view all the answers

For sterilization of the gut before surgery, a tablet that is not absorbed, such as ______, can administered via the GI tract.

<p>neomycin</p> Signup and view all the answers

A retention ______ involves injecting a solution into the rectum and holding for a specific period of time, such the the use of methylprednisolone in the treatment of ulcerative colitis.

<p>enema</p> Signup and view all the answers

For evacuation of bowels, a suppository containing ______ can be administered in solid form into the rectum.

<p>bisacodyl</p> Signup and view all the answers

For bronchial asthma and chronic obstructive pulmonary disease, medications like salbutamol and ______ bromide can be administered via inhalation.

<p>ipratropium</p> Signup and view all the answers

For cutaneous candidiasis antifungal, such as ______, can be used as an ointment, cream, lotion or powder.

<p>clotrimazole</p> Signup and view all the answers

To treat malignancy involving limbs, some anticancer drugs can be administered via the ______ route.

<p>intra-arterial</p> Signup and view all the answers

In rheumatoid arthritis, ______ can be directly injected into the joint space.

<p>triamcinolone</p> Signup and view all the answers

In facilitated passive diffusion, a ______ in the membrane combines reversibly with the substrate molecule.

<p>carrier molecule</p> Signup and view all the answers

Unlike passive diffusion, active transport can move substances against their ______.

<p>concentration gradient</p> Signup and view all the answers

The family of ATP-dependent proteins are included in ______ transports.

<p>active</p> Signup and view all the answers

If drug concentration is high enough to saturate carrier mechanism, kinetics are ______.

<p>zero-order</p> Signup and view all the answers

In pinocytosis, the cell membrane invaginates, encloses fluid or particles, then fuses again forming a ______.

<p>vesicle</p> Signup and view all the answers

The ______ of a drug predicts its movement and availability at sites of action.

<p>molecular size and shape</p> Signup and view all the answers

Facilitated passive diffusion is a ______ transport system.

<p>carrier-mediated</p> Signup and view all the answers

The process of engulfing fluid or particles by a cell is called ______.

<p>pinocytosis</p> Signup and view all the answers

A potential drug's effect results in a ______ benefit to the patient.

<p>therapeutic</p> Signup and view all the answers

Drug design involves creating molecules that are complementary in shape and ______ to the target biomolecule.

<p>charge</p> Signup and view all the answers

The molecule that either activates or inhibits a biological target is a ______.

<p>drug</p> Signup and view all the answers

When computer-based modeling is used in drug design, it is referred to as ______-aided drug design.

<p>computer</p> Signup and view all the answers

Knowledge of the three-dimensional structure of the biological target is known as ______-based drug design.

<p>structure</p> Signup and view all the answers

Adhering to standards of maintenance and care is needed when using ______ for research and teaching.

<p>animals</p> Signup and view all the answers

[Blank] ethics are important when using ______s for pre-clinical testing.

<p>animal</p> Signup and view all the answers

Following the principles of good ______ practice is important in the conduct of experiments.

<p>laboratory</p> Signup and view all the answers

Flashcards

Pharmacology

The branch of medical science concerned with the study of the uses, effects, and modes of action of drugs.

Drug

Any natural, synthetic, or endogenous molecule that can exert a physiological and/or biochemical effect on a cell, tissue, organ, or whole organism.

Xenobiotic

A drug or chemical substance that is foreign to the body and not produced by the body itself.

Poisons

Drugs that almost exclusively have harmful effects on the body.

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Pharmakon

Greek word for drug or poison.

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Logos

Greek word for word or discourse.

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Drug-Body Interactions

The interaction of a drug with a biological system also interacts bidirectionally with the body.

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Xenobiotics

Molecules not synthesized in the body.

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Selectivity

The degree to which a drug acts on a specific site relative to other sites. Influenced by binding.

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Drug Affinity

Probability of a drug occupying a receptor at any given moment.

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Intrinsic Efficacy (Activity)

Degree to which a ligand activates receptors and leads to a cellular response.

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Drug-Receptor Complex Residence Time

The time a drug-receptor complex remains together; longer = prolonged effect. Affected by conformational changes.

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Receptor Upregulation

Increase in receptor density and binding affinity, can result from chronic therapy or drug withdrawal.

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Receptor Downregulation

Decrease in receptor density and binding affinity; can results from chronic drug exposure.

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Adaptation via Receptor Regulation

Adaptation to drugs which affect sensitivity to the drug.

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Recognition Sites

Specific molecular regions on receptor macromolecules where ligands bind.

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Non-specific Drug Binding

Binding to sites other than receptors (e.g., plasma proteins).It prevents the drug from binding to the receptor, thus inactivating the drug.

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Agonists

Drugs that activate receptors to produce a desired response.

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Allosteric Agonists

Agonists that bind to a different site on the receptor.

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Inverse Agonists

Stabilize the receptor in its inactive conformation, opposing normal agonists.

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Antagonists

Drugs that prevent receptor activation.

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Reversible Antagonists

Readily dissociate from their receptor.

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Irreversible Antagonists

Form a stable, permanent bond with their receptor.

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Competitive Antagonism

Binding of the antagonist prevents agonist binding.

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Drug Design

Designing molecules to complement the shape and charge of a biomolecular target for binding.

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Computer-Aided Drug Design

Drug design using computer modeling techniques.

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Structure-Based Drug Design

Drug design based on knowing the 3D structure of the biomolecular target.

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Animal Ethics

The moral principles and guidelines governing the use of animals in research and teaching.

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Good Laboratory Practice (GLP)

Standards for quality control in research, ensuring reliability and reproducibility of experiments.

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Maintenance of Stock (Animals)

Maintaining a population of animals for research purposes.

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Separate Housing of Species

Housing different species separately in animal facilities to prevent disease transmission and stress.

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Topical Drug Administration

Application of drug to skin/mucous membrane for local effect, minimizing systemic side effects.

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Troches

Small lozenges that dissolve in the mouth (cheek and gum), gradually releasing the drug; absorbed into bloodstream.

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Enemas

Administration of drugs into the rectum in liquid form for bowel evacuation or retention of medication.

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Suppository

Administration of a solid drug form into the rectum for local or systemic effect, e.g., bowel evacuation.

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Local Administration (Eye, Ear, Nose)

Drug delivery via drops, ointments, or sprays to treat eye, ear, or nose conditions.

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Bronchial Inhalation

Drug delivery via inhalation for conditions like asthma or COPD.

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Intra-arterial Route

Rare route of drug administration directly into an artery, mainly for diagnostic studies or anticancer drugs.

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Oral Route

Drug administration by mouth, the most common and acceptable route.

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Facilitated Passive Diffusion

Uses a carrier molecule to help drugs cross the membrane, following the concentration gradient. No energy is required.

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Active Transport

Drug passage that requires energy and a carrier to move drugs against a concentration gradient.

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Pinocytosis / Exocytosis

The process where a cell engulfs fluid or particles by invaginating its membrane to form a vesicle. Requires energy.

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Transporter Selectivity & Saturation

Membrane transporters show specificity for drug structures and can become saturated.

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Zero-Order Kinetics (in Transport)

Drug transport where the rate is constant because the carrier proteins fully saturated.

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Factors Affecting Drug Transfer

Size and shape, ionization, lipid solubility, and protein binding all affect drug movement.

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Drug's Journey to Action Site

Drugs usually need to cross multiple cell membranes to reach their action site.

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Plasma Membrane as a Barrier

Common barrier to drug distribution, made of lipids and proteins.

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