Pharmacology: Drugs, Action, and origin
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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 drug can be defined as any natural, synthetic, or endogenous molecule that can exert a physiological and/or ______ effect on a cell, tissue, organ, or whole organism.

biochemical

The field of __________ encompasses drug properties, synthesis, molecular mechanisms of action, and cellular communication.

pharmacology

In pharmacology, drugs are also called medication or medicine, and are used for treating, curing, preventing, or diagnosing a disease or to promote health and ______.

<p>well-being</p> Signup and view all the answers

Traditionally, drugs were obtained through extraction from ______ plants, but more recently also by organic synthesis.

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

The interactions of a drug with a biological system (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

Decoding the genomes of humans and other organisms has opened new doors for research and __________ __________.

<p>disease treatment</p> Signup and view all the answers

The guiding principle of medicine, Primum non nocere, translates to 'First do no ______'.

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

______ is what a drug does to the body.

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

__________ disorders are a result of heritable abnormalities in an individual's DNA.

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

__________ __________ involves inserting a healthy gene into somatic cells to correct a genetic abnormality.

<p>Gene therapy</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

A drug's pharmacodynamics can be affected by physiologic changes due to a disease, ______, or other drugs.

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

Genetic ______, thyrotoxicosis, and malnutrition can affect pharmacodynamic responses.

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

Increased sensitivity to certain drugs can often be attributed to small genetic modifications that decrease the activity of a particular __________ responsible for eliminating that drug.

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

The two main areas of pharmacology deal with the actions of drugs on the body (______) and the fate of drugs in the body (pharmacokinetics).

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

Disorders like myasthenia gravis and Parkinson disease, can alter ______ responses.

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

__________ is the study of genetic variations that cause individual differences in drug response.

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

Pharmacokinetics involves the ______, distribution, metabolism, and excretion (ADME) of chemicals from biological systems.

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

Pharmacodynamic drug–drug interactions can result in competition for receptor binding sites, or alter ______ response.

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

The discovery and development of drugs and __________ has significantly increased lifespan and improved quality of life.

<p>immunotherapy/vaccinations</p> Signup and view all the answers

Pharmacology usually overlaps with ______, which is the science of drug preparation; much of it deals with clinical pharmacology/therapeutics.

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

[Blank] is the branch of pharmacology dealing with the undesirable effects of drugs on biological processes, or generally the study of poisons.

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

Receptors, the targets of drug action, are macromolecules involved in chemical ______ between and within cells.

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

New scientific insights, sometimes inferred from the development of new mechanisms of action, have been essential, along with __________ __________ __________.

<p>controlled clinical trials</p> Signup and view all the answers

The search for __________ __________, agents that treat disease or produce desirable effects without harm, has driven scientific discovery for over a century.

<p>magic bullets</p> Signup and view all the answers

Receptors can be located on the cell surface membrane, ______ or within the cytoplasm.

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

The primary challenge in drug development is identifying, testing, approving, and utilizing drugs that maximize __________ while minimizing __________.

<p>efficacy, toxicity</p> Signup and view all the answers

Osmotic diuretics like mannitol create an osmotic load within the renal tubule, resulting in the obligate excretion of ______.

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

When administered orally, ammonium chloride is metabolized by the liver into urea, while ______ is excreted in the urine, acidifying it.

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

The loss of Cl- results in an obligatory loss of ______ in the urine, thus lowering pH.

<p>H+</p> Signup and view all the answers

[Blank] such as EDTA can bind to divalent cations like lead.

<p>Chelating agents</p> Signup and view all the answers

Digitalis glycosides increase myocardial contractility by inhibiting the membrane enzyme, ______.

<p>Na+-K+-ATPase</p> Signup and view all the answers

Sulfonamides act as antibacterial agents by inhibiting the synthesis of ______ in bacteria.

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

General anesthetics are thought to alter the function of membrane proteins by disorganizing the structure of the surrounding ______.

<p>lipid membranes</p> Signup and view all the answers

Aspirin forms a covalent bond with ______, preventing the production of prostaglandins and thromboxane A2.

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

The anti-clotting effect of aspirin is achieved by preventing the production of ______, a cyclooxygenase produced substance.

<p>thromboxane A2</p> Signup and view all the answers

The effects of aspirin, which is covalently bound to cyclooxygenase, can only be reversed by synthesizing new ______ in new ______, a process that takes several days.

<p>enzymes, platelets</p> Signup and view all the answers

[Blank] act as targets for antimetabolites and some antibiotics.

<p>Nucleic acids</p> Signup and view all the answers

[Blank] bonds are strong bonds that are not readily broken.

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

Flashcards

Pharmacology

The study of the uses, effects, and modes of action of drugs.

Drug

Any natural, synthetic, or endogenous molecule that exerts a physiological or biochemical effect on a cell, tissue, organ, or organism.

Pharmacodynamics

The actions of a drug on the body, involving interactions between chemicals and biological receptors.

Pharmacokinetics

The fate of drugs in the body, including absorption, distribution, metabolism, and excretion (ADME).

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Pharmacy

The science of drug preparation.

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Clinical Pharmacology/Therapeutics

The use of drugs in the treatment of disease.

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Toxicology

The branch of pharmacology dealing with the undesirable effects of drugs or the study of poisons.

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Drug Source

Molecules synthesized in the body OR molecules not synthesized in the body.

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Poisons

Drugs that almost exclusively have harmful effects.

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Xenobiotics

Molecules not synthesized in the body.

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Pharmacology's Scope

The study of drug properties, synthesis, mechanisms, and cellular communication.

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Genomics in Pharmacology

Using our understanding of the human genome to identify and potentially correct DNA abnormalities in hereditary disorders, and understanding variance in drug response.

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Pharmacogenomics

The study of genetic variations that cause individual differences in drug response.

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Importance of Drugs

Increased lifespan and improved quality of life. Also, provide insights into disease mechanisms.

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Alternative Treatments

Treatments that haven't necessarily undergone rigorous scientific validation.

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Magic Bullets

Agents that treat disease or produce desirable effects but lack harm

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Drug Development Goal

Maximizing efficacy while minimizing toxicity.

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Double-Blind Trial

A clinical trial where neither the participants nor the researchers know who is receiving a particular treatment. This procedure is utilized to prevent bias in research results.

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Gene Therapy

Adding a working gene to cells to correct a genetic disorder.

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Genetic Disease

A heritable abnormality in DNA.

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Primum non nocere

First, do no harm. Guiding principle in medicine to prioritize patient safety.

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Receptor Site

The pharmacologic response is influenced by the drug's concentration at this site.

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Factors Affecting Pharmacodynamics

Genetic mutations, aging, or other drugs can alter the effects of a medication.

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Drug Receptors

Macromolecules on the cell surface, in the cytoplasm, or in the nucleus involved in chemical signaling.

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Osmotic Diuretics (Mannitol)

These compounds are not reabsorbed by the kidney and create an osmotic load, leading to water excretion.

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Magnesium Sulfate (as a laxative)

Causes obligate excretion of water in the intestines through osmotic mechanisms.

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Ammonium Chloride

Used to acidify urine by the liver metabolizing ammonium ion to urea and excreting chloride.

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Drug Approval Processes

The body's approval process for drugs.

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Pharmacodynamic Drug-Drug Interactions

Competition for binding sites or altered postreceptor response may occur.

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Cl- Loss Effect on Urine pH

Lowering urine pH due to Cl- loss, resulting in obligatory H+ loss.

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Chelating Agents

Agents like EDTA that bind divalent cations like lead (Pb2+).

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Enzyme Inhibition by Drugs

Drugs inhibit enzymes via competitive, non-competitive, or irreversible blockade at a substrate or cofactor binding site.

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Digitalis Mechanism

Digitalis glycosides increase heart muscle contraction by blocking Na+-K+-ATPase.

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Selective Toxicity

Drugs must have selective toxicity towards bacterial or tumour cells.

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Sulfonamide Action

Sulfonamides inhibit folate synthesis, effective antibacterial agents.

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Antimetabolites

Counterfeit substitutes that incorporate into faulty mRNA.

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Non-Specific Drug Binding

Drugs bind non-specifically to macromolecular targets, altering membrane protein function.

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Covalent Bonds (Drugs)

Strong, permanent bonds. Drug effects last until new enzymes are synthesized.

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Aspirin's Covalent Action

Aspirin binds covalently to cyclooxygenase preventing prostaglandin production.

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Study Notes

  • Pharmacology studies the uses, effects, and modes of action of drugs, spanning from natural to synthetic origins exert physiological or biochemical effects on organisms.
  • Drugs, also called medications, are used for treating, curing, preventing, or diagnosing diseases, and for health promotion.
  • Historically derived from medicinal plants, drugs are now also created through organic synthesis.
  • Drug interactions with biological systems are bidirectional.
  • Over 350,000 drugs have been approved worldwide.
  • There are over 147 Diclofenac-sodium and 60 Paracetamol (Acetaminophen) preparations available in some countries.
  • Most drugs have a single international name but may have various trade names.
  • Historically, pharmacologically active substances, such as those from plants and animals, were used to combat diseases.
  • Drugs can consist of molecules synthesized in the body, like hormones or neurotransmitters (e.g., dopamine), or xenobiotics not synthesized in the body.
  • Poisons almost exclusively have harmful effects.
  • Pharmacology comes from the Greek words 'pharmakon' (drug or poison) and 'logos' (word or discourse).
  • The key areas of pharmacology are pharmacodynamics (drug actions on the body) and pharmacokinetics (drug fate in the body).
  • In broad terms, pharmacodynamics studies drug and biological receptor interactions.
  • Pharmacokinetics studies the ADME (absorption, distribution, metabolism, and excretion) of chemicals in biosystems.
  • Pharmacology commonly overlaps with pharmacy (drug preparation) and includes clinical pharmacology/therapeutics (drug use for disease treatment).
  • Toxicology studies harmful drug effects on biosystems, and studies poisons.
  • Pharmacology integrates drug properties, synthesis, mechanisms of action, and cellular communication.
  • Understanding the genetic basis of diseases and drug responses is enhanced by decoded genomes, with potential for gene therapy and personalized medicine.
  • Pharmacogenomics studies the genetic factors behind individual differences in drug responses.
  • Drug discovery has increased lifespan and improved quality of life.
  • New scientific insights, along with controlled clinical trials, have been essential to this progress.
  • Finding "magic bullets" to treat diseases or give desirable effects without harm has driven scientific discovery for over 100 years.
  • Approving and using drugs which maximize efficacy while minimizing toxicity is a challenge.
  • Focus on "primum non nocere": "First do no harm" due to risks, ensuring safety>efficacy in drug approval and prescription.

Pharmacodynamics

  • Studies the biochemical, physiologic, and molecular impacts of drugs, including receptor interactions and chemical effects.
  • Drug binding to its target defines the pharmacologic response.
  • A drug's effect is impacted by its concentration at the receptor site.
  • A drug's pharmacodynamics can be altered by disease, aging, or other drugs.
  • Disorders affecting pharmacodynamic responses include genetic mutations, and forms of insulin-resistant diabetes.
  • Receptor sensitivity can be affected by these disorders.
  • Aging can alter receptor binding or postreceptor sensitivity.
  • Drug-drug interactions can compete for receptor binding sites, or change postreceptor response.

Drug Receptors

  • Upon entering the body are distributed to their site of action.
  • Receptors, located in the target tissue or organ, are macromolecules involved in cellular communication.
  • Receptors may be located on the cell surface, membrane, nucleus, or cytoplasm.
  • For exerting an effect, drugs bind to specific cell receptors.
  • Other targets of drug include:
  • Water: Osmotic diuretics such as mannitol cause excretion by creating an osmotic load in the kidney.
  • Hydrogen ions: Ammonium chloride acidifies urine via liver metabolism, resulting in chloride loss.
  • Metal ions: Chelating agents such as EDTA bind divalent actions to treat poisoning.
  • Enzymes: They serve as target for therapeutically useful drugs, inhibiting via competitive or irreversible blockade.
  • Nucleic Acids: Targeted by antimetabolites such as 5-Fluorouracil
  • Some drugs, e.g. general anaesthetics, non-specifically alter membrane protein function

Drug-Receptor Bonds

  • 3 types: covalent, electrostatic, and hydrophobic.
  • Covalent bonds are very strong and not easily broken.
  • Aspirin, which forms a covalent bond with cyclooxygenase, its target, and its effect is irreversible.
  • Electrostatic bonds are more common and weaker.
  • They encompass ionic linkages, hydrogen bonds, and Van Der Waals forces.
  • Hydrophobic interactions occur when molecules avoid water.
  • Usually found in the interactions between highly lipid-soluble drugs and lipids in the cell membranes.

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Pharmacology studies drugs' uses, effects, and actions, natural to synthetic, on organisms. Drugs treat, cure, prevent, or diagnose diseases and promote health. They can be synthesized or derived from natural sources and interact bidirectionally with biological systems.

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