Pharmacology Chapter Quiz

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Questions and Answers

Which term describes the ability of a substance to produce maximal effects following receptor binding?

  • Antagonist
  • Partial Agonist
  • Inverse Agonist
  • Full Agonist (correct)

What term refers to the ability of a drug to bind to a receptor or target protein?

  • Affiinity (correct)
  • Efficacy
  • Constitutional activity
  • Intrinsic activity

Which of the following accurately describes a Partial Agonist?

  • Produces some effects and inhibits others (correct)
  • Inhibits all effects attributed to receptor interaction
  • Produces maximal clinical effects
  • Acts as an antagonist in all scenarios

What is the role of constitutional activity in drug-receptor interactions?

<p>It generates receptor effects without a ligand (B)</p> Signup and view all the answers

Osmotic diuretics operate primarily through what mechanism?

<p>Colligative mechanism (D)</p> Signup and view all the answers

What is the primary action of Aspirin in terms of platelet function?

<p>Irreversibly inhibits COX and TXA2 synthesis (B)</p> Signup and view all the answers

Which condition is indicated for the use of Argatroban?

<p>Heparin-induced thrombocytopenia (HIT) (D)</p> Signup and view all the answers

What type of drugs are Clopidogrel and Prasugrel?

<p>P2Y12 ADP receptor inhibitors (C)</p> Signup and view all the answers

Which of the following is NOT an antidote for warfarin toxicity?

<p>Bivalirudin (C)</p> Signup and view all the answers

What adverse effect is specifically associated with Lepirudin?

<p>Anaphylaxis (A)</p> Signup and view all the answers

What is the rationale for postponing surgery after the use of Aspirin?

<p>Prolonged bleeding time requiring hemostasis (D)</p> Signup and view all the answers

Which factor may necessitate a review of warfarin dosage?

<p>Elevated baseline PT-INR (B)</p> Signup and view all the answers

What is the main mechanism of action for Direct Thrombin Inhibitors?

<p>Directly inhibit IIa by active site binding (D)</p> Signup and view all the answers

What is the primary focus of pharmacodynamics in pharmacology?

<p>Study of the interactions of drugs with the body (D)</p> Signup and view all the answers

Which classification of drugs is primarily used to supplement lacking endogenous substances?

<p>Replenishers (D)</p> Signup and view all the answers

What type of receptors are involved in signal transduction and are the most common in the study of pharmacology?

<p>G Protein-coupled Receptors (GPCR) (D)</p> Signup and view all the answers

What is the primary function of chemotherapeutic agents?

<p>Killing or inhibiting growth of foreign cells (B)</p> Signup and view all the answers

What mechanism do ligand-gated receptors utilize to allow ion movement?

<p>Change in conformity of the receptor gate (B)</p> Signup and view all the answers

Which of the following best describes pharmacokinetics?

<p>The processes a drug undergoes as it is absorbed and eliminated (C)</p> Signup and view all the answers

What type of drug is Edrophonium primarily classified as?

<p>Diagnostic Agent (C)</p> Signup and view all the answers

Which type of receptors are known to exist as monomers and include kinases?

<p>Nuclear receptors (B)</p> Signup and view all the answers

Which classification of drugs includes analgesics and antipyretics?

<p>Functional Modifiers (B)</p> Signup and view all the answers

What is a characteristic function of transporters in pharmacology?

<p>Facilitating drug absorption and distribution (C)</p> Signup and view all the answers

What is the primary goal of the coagulation cascade during clot formation?

<p>To form cross-linked fibrin (A)</p> Signup and view all the answers

Which factor is primarily targeted by indirect thrombin inhibitors such as heparin?

<p>Factor X (C)</p> Signup and view all the answers

What does Virchow's Triad include as one of the three factors contributing to clot formation?

<p>Endothelial injury (B)</p> Signup and view all the answers

Which of the following is a characteristic of low molecular weight heparins?

<p>Better safety profiles than unfractionated heparin (C)</p> Signup and view all the answers

What is a common side effect associated with the use of heparin?

<p>Thrombocytopenia (B)</p> Signup and view all the answers

What is the primary mechanism of action of coumarins like warfarin?

<p>Inhibit vitamin K epoxide reductase (B)</p> Signup and view all the answers

Which anticoagulant is safe to use in pregnant patients?

<p>Heparin (C)</p> Signup and view all the answers

The formation of which type of thrombus is primarily associated with arterial clots?

<p>Platelet-rich white thrombi (B)</p> Signup and view all the answers

What is the preferred route of administration for low molecular weight heparins?

<p>Subcutaneously (D)</p> Signup and view all the answers

Which of the following factors is NOT part of Virchow's Triad?

<p>Infection (A)</p> Signup and view all the answers

What is the primary mechanism of action for HMG-CoA reductase inhibitors?

<p>Inhibit HMG-CoA reductase enzyme (B)</p> Signup and view all the answers

Which agent is primarily used for the treatment of sizable pulmonary embolisms and acute ischemic strokes?

<p>Alteplase (B)</p> Signup and view all the answers

Which of the following treatments is specifically indicated for managing hereditary bleeding disorders?

<p>Cryoprecipitate and fresh frozen plasma (D)</p> Signup and view all the answers

What common side effect is associated with the use of fibrates?

<p>Rhabdomyolysis (B), Formation of gallstones (C)</p> Signup and view all the answers

What is the role of vitamin K in medical treatment?

<p>Prophylaxis for hemorrhagic disease of the newborn (B)</p> Signup and view all the answers

Which of the following agents directly inhibits plasminogen conversion to plasmin?

<p>Tranexamic acid (B)</p> Signup and view all the answers

What pharmacological action does cilostazol have?

<p>Inhibits platelet aggregation (A)</p> Signup and view all the answers

Which of the following is NOT a criterion for therapeutic equivalence set by the FDA?

<p>Same packaging and branding (A)</p> Signup and view all the answers

Which of the following conditions would most likely require a combination of lipid-lowering agents?

<p>Elevated LDL and VLDL levels simultaneously (C), Refractory low HDL levels (D)</p> Signup and view all the answers

In the context of anticoagulants, which agent is known to cause thrombocytopenia as an adverse effect?

<p>Abciximab (C)</p> Signup and view all the answers

What is the primary objective of drug distribution in the body?

<p>To allow drugs to reach biological sites of action (A)</p> Signup and view all the answers

Which drug is known to have high protein binding?

<p>Warfarin (A)</p> Signup and view all the answers

What is the main application of vitamin B12 in treating anemias?

<p>Support normal red blood cell formation (A)</p> Signup and view all the answers

What is the mechanism of action of niacin in lipid metabolism?

<p>Inhibits VLDL secretion (B)</p> Signup and view all the answers

What role does Phase I metabolism play in drug biotransformation?

<p>Unmasks or adds a functional group (C)</p> Signup and view all the answers

In terms of enzyme activity, what is the consequence of genetic polymorphism?

<p>Variability in drug metabolism among different individuals (C)</p> Signup and view all the answers

Which of the following is an alternative to oral iron therapy for severe iron deficiency?

<p>Iron dextran (D)</p> Signup and view all the answers

Where does the majority of drug excretion occur in the body?

<p>Kidneys (C)</p> Signup and view all the answers

How do phosphodiesterase (PDE) inhibitors aid in medical treatments?

<p>Enhance vasodilation (C)</p> Signup and view all the answers

Which lipid-lowering medication is known for having a high incidence of hepatotoxicity?

<p>HMG-CoA reductase inhibitors (D)</p> Signup and view all the answers

What neurotransmitter is primarily released by postganglionic sympathetic neurons?

<p>Norepinephrine (A)</p> Signup and view all the answers

Which of the following neurotransmitters is involved in the preganglionic sympathetic response?

<p>Acetylcholine (C)</p> Signup and view all the answers

Which of the following drugs is a natural catecholamine?

<p>Norepinephrine (C)</p> Signup and view all the answers

What characterizes the sympathetic nervous system in terms of neuron arrangement?

<p>Two-neuron chain with ganglia located near the spinal cord (B)</p> Signup and view all the answers

What is the rate-limiting enzyme in the biosynthesis of catecholamines?

<p>Tyrosine hydroxylase (C)</p> Signup and view all the answers

Which of the following statements about drug metabolism is TRUE?

<p>First pass metabolism can inactivate some active drugs (B)</p> Signup and view all the answers

Which part of the autonomic nervous system is responsible for controlling involuntary functions?

<p>Autonomic Nervous System (A)</p> Signup and view all the answers

What is a major feature distinguishing the parasympathetic nervous system's structure?

<p>Short preganglionic fibers and ganglia located near the effector organs (B)</p> Signup and view all the answers

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Flashcards

Affinity

The ability of a drug to bind to its specific target protein, like a receptor.

Intrinsic Activity

The ability of a drug to initiate a chain of events leading to a biological effect after it's bound to a receptor.

Full Agonist

A drug that produces the maximum possible effect when binding to its receptor.

Partial Agonist

A drug that only partially activates a receptor, producing less than the maximum effect.

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Antagonist

A drug that binds to a receptor but does not produce any effect on its own. It can block the actions of other drugs.

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Pharmacology

The study of drugs and their effects on living organisms.

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Drugs

Substances used for the diagnosis, prevention, treatment, or mitigation of diseases.

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Diagnostic agents

Drugs that are used to determine the presence or severity of a disease or condition.

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Replenishers

Drugs that are used to replace substances that are lacking in the body.

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Functional modifiers

Drugs that alter the normal function of the body or affect disease processes.

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Chemotherapeutic agents

Drugs used to kill or inhibit the growth of cells considered harmful or foreign to the body.

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Pharmacodynamics (PD)

The study of how drugs interact with the body, focusing on their biochemical and physiological effects.

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Pharmacokinetics (PK)

The study of how the body processes drugs, including absorption, distribution, metabolism, and elimination.

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Receptors

Cellular macromolecules or assemblies that are directly involved in chemical signaling within the cells.

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GPCR (G Protein-coupled Receptor)

A type of receptor that spans the cell membrane seven times and is activated by binding to a ligand, leading to a cascade of intracellular events.

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Vasospasm

A spasm or narrowing of blood vessels, often occurring in the context of injury or damage, hindering blood flow.

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Platelet-Fibrin Plug

A temporary plug formed at the site of injury to stop bleeding, involving platelets, fibrin, and specific proteins like von Willebrand factor.

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Coagulation Cascade

A complex series of reactions involving clotting factors, leading to the formation of stable fibrin, which strengthens the platelet plug.

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Virchow's Triad

The three main factors that contribute to the formation of unwanted blood clots: endothelial injury, blood stasis, and hypercoagulability.

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White Thrombi

Abnormal clotting in arteries, often rich in platelets, creating a white appearance due to the platelet composition.

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Red Thrombi

Abnormal clotting in veins, often rich in fibrin, creating a red appearance due to the fibrin composition.

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Foreign Body

Presence of foreign material (e.g., implants, stents) within the circulatory system that triggers blood clots.

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Indirect Thrombin Inhibitors

A class of medications that inhibit the formation of thrombin, thus preventing blood clotting.

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Heparin

A natural anticoagulant, extracted from pig intestines, that binds to antithrombin III, preventing the formation of clots.

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Low Molecular Weight Heparins (LMWH)

A group of anticoagulants related to heparin but with lower molecular weight, offering improved safety profiles.

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Warfarin

Warfarin is a drug used to prevent blood clots, primarily in patients with atrial fibrillation or those who have had a blood clot previously. It acts by inhibiting the synthesis of vitamin K-dependent clotting factors.

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INR

The international normalized ratio (INR) is a standardized test that measures the clotting time of blood in comparison to a normal control. It's used to monitor the effectiveness of warfarin therapy.

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Vitamin K and Warfarin

Vitamin K is a necessary cofactor for the production of clotting factors. If you consume too much vitamin K, it can counteract warfarin's effect. If you have a low level of vitamin K, warfarin's effect may be too strong.

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Heparin-induced Thrombocytopenia (HIT)

Heparin-induced thrombocytopenia (HIT) is a rare but serious complication of heparin therapy. It causes a decrease in platelet count, increasing the risk of bleeding.

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Aspirin

Aspirin is a commonly used medicine that irreversibly inhibits the production of thromboxane A2, a powerful platelet aggregator. This blocks platelets from sticking together and forming unwanted clots.

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P2Y12 ADP Receptor Inhibitors

P2Y12 ADP Receptor Inhibitors, such as clopidogrel, ticlopidine, and prasugrel, prevent platelets from activating by blocking the action of adenosine diphosphate (ADP).

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P2Y12 ADP Receptor Inhibitors - PCI

Percutaneous coronary intervention (PCI) is a minimally invasive procedure to open blocked or narrowed coronary arteries. These drugs help to prevent blood clots from forming on stents placed during PCI to prevent heart attacks.

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Therapeutic Equivalence

Drugs that are pharmaceutical equivalents and can be expected to have the same clinical effect and safety profile. They are interchangeable and considered safe to substitute.

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Drug Distribution

The process of drug movement from the systemic circulation to different body compartments (organs and tissues). This allows drugs to reach their target sites.

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Protein Binding

The amount of drug bound to plasma proteins, primarily albumin, alpha-1 acid glycoprotein, and globulin. It influences drug distribution and duration of action.

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Volume of Distribution (Vd)

A hypothetical volume of body fluid that would be needed to contain a given drug dose at the same concentration as in the plasma. It helps estimate loading doses and predict where drug distributes.

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Drug Metabolism (Biotransformation)

The chemical alteration of a drug by the body, usually in the liver. It typically makes drugs more water-soluble and easier to excrete.

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First Pass Effect/Metabolism

The initial metabolism a drug undergoes before reaching the systemic circulation, often in the liver. This can significantly reduce the amount of drug reaching the target site.

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Phase I Metabolism

The process of adding or unmasking a functional group on a drug molecule. This often increases its polarity.

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Phase II Metabolism (Conjugation)

The process of attaching a polar conjugate (like glucuronic acid) to a drug molecule. This makes it more water soluble and easier to excrete.

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Prodrug, Active, and Toxic Metabolites

Some drugs are given as inactive forms (pro-drugs) but are activated by the body's metabolism. Others stay active or become toxic.

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Enzyme Inhibition/Induction

The inhibition or induction of drug metabolism by other drugs or factors. This can either decrease or increase drug levels in the body.

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Genetic Polymorphism

Differences in enzyme activity due to genetic variations. This can affect how people metabolize drugs and leads to variable drug responses.

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Drug Excretion

The removal of drugs from the body, primarily through the kidneys. This involves filtration and sometimes active secretion.

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Autonomic Nervous System (ANS)

The major subdivisions of the autonomic nervous system: sympathetic (fight or flight), parasympathetic (rest and digest), and enteric (controls the gut).

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Efferent Neurons

The neurons that transmit signals from the CNS to the body's organs and muscles. These are part of the efferent pathway of the nervous system.

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Synapse

The junction between two neurons where chemical signals are transmitted. This is where neurotransmitters are released and received.

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Antiplatelet

A type of drug that reduces the stickiness of platelets, preventing them from clumping together and forming clots.

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Antithrombotic

A drug that prevents or slows down the formation of blood clots.

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Thrombolytic

A type of drug that breaks down existing blood clots.

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Prothrombotic

A type of drug that promotes blood clotting.

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Vitamin K Deficiency

A condition caused by a deficiency of vitamin K, resulting in abnormal bleeding.

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Antifibrinolytic

A drug that blocks the conversion of plasminogen to plasmin, preventing clot breakdown.

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Dyslipidemia

A condition characterized by high levels of lipids (fats) in the blood.

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Lipid-Lowering Drug

A drug that lowers cholesterol levels in the blood.

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HMG-CoA Reductase Inhibitor

A type of drug that inhibits the enzyme HMG-CoA reductase, reducing cholesterol production.

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Fibrate

A type of drug that activates PPAR-alpha, increasing the breakdown of triglycerides.

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Bile Acid Sequestrant

A type of drug that binds to bile acids in the gut, preventing their reabsorption and lowering cholesterol.

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Sterol Absorption Inhibitor

A type of drug that blocks the absorption of cholesterol in the gut.

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HDL-Raising Drug

A type of drug that increases HDL (good cholesterol) levels in the blood.

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Anemia

A condition characterized by a decrease in the number of red blood cells.

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Hematopoietic Growth Factor

A drug that stimulates the production of red blood cells.

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Study Notes

Pharmacology Study Notes

  • Definitions

    • Pharmacology is the study of drugs.
    • Drugs are used in diagnosis, prevention, treatment, and mitigation of diseases.
    • Classification of Drugs includes:
      • Diagnostic agents (e.g., Edrophonium for Myasthenia Gravis diagnosis)
      • Radiopharmaceuticals (e.g., Technetium 99m sestamibi for MI)
      • Replenishers (e.g., Cyanocobalamin for B12 deficiency)
      • Functional Modifiers (e.g., analgesics, antipyretics)
      • Chemotherapeutic Agents (e.g., anti-infectives, antineoplastics)
  • Branches of Pharmacology

    • Pharmacodynamics (PD) focuses on what the drug does to the body.
    • Pharmacodynamics studies drug effects in the body and mechanisms behind them.
    • Pharmacokinetics (PK) focuses on what the body does to the drug.
    • Pharmacokinetics studies drug movement in the body that reaches/leaves the site of action.
    • Pharmacotherapeutics studies the rational use of drugs in disease management.

Pharmacodynamics

  • Drug Action Mechanisms

    • Receptor-mediated action involves specific receptors.
    • Receptors are cellular macromolecules or assemblies of macromolecules that facilitate chemical signaling between and within cells.
  • Types of Receptors

    • G Protein-coupled Receptors (GPCRs) are 7-transmembrane spanning receptors; they involve signal transduction.
    • Ion channels are regulated by membrane potential changes; they permit ion movement.
      • Examples include voltage-gated Na+, K+, and Ca2+ channels.
    • Ligand-gated receptors (ionotropic) alter gate configuration to allow ion passage, e.g., nicotinic and GABAa receptors.
    • Kinase/Catalytic receptors exist as monomers and induce downstream signaling. Important for receptor binding site, kinase domain, and downstream molecules.
    • Enzymes are targets; examples of drugs targeting enzymes such as ACE, COX and MAO.
    • Transporters, or carriers, are responsible for movement of molecules across membranes (e.g., Na+/K+ ATPase).

Principles of Pharmacodynamics

  • Protein Targets
    • Drugs act on proteins
  • Drug Targets
    • Ligands, receptors; binding sites, kinase domain, downstream molecules
    • Enzymes (ACE, COX, MAO).
    • Transporters (Na+/K+ ATPase)
    • Structural Proteins (e.g., tubulin)
  • Other Mechanisms (Non-receptor-mediated)
    • Direct chemical interaction (e.g., antacids)
    • Colligative properties (osmotic diuretics)
    • Counterfeit incorporation (analogs, e.g. 5-FU)

Drug-Receptor Interactions

  • Affinity - ability to bind to a receptor or target protein

  • Intrinsic Activity - ability to trigger a biochemical response

  • Constitutive Activity - ability to initiate a response even without a ligand

  • Orthosteric Site - primary binding site for endogenous ligands

  • Allosteric Site - secondary binding site, altering ligand binding and activity.

    • Allosteric agonists enhance ligand binding; Allosteric antagonists inhibit ligand binding
  • Agonists, Inverse Agonists, and Antagonists

    • Agonists stabilize the active receptor state
    • Inverse agonists stabilize the inactive receptor state
    • Antagonists maintain the equilibrium between inactive and active states
    • Full agonists produce maximal clinical effects
    • Partial agonists produce submaximal effects
    • Antagonists prevent agonist binding without inducing a response
  • Clinical Antagonists

    • drugs producing opposite effects of another drug or endogenous agonist.

Dose Response Relationship

  • Hill Equation
    • Relates drug concentration/dose to the resulting effect (E)
    • Emax: maximal effect
    • [A]50: concentration producing half-maximal effect
    • nH: Hill coefficient (slope of the log-transformed curve)
  • Dose Response Graph provides details on potency (dose generating 50% of effect) and efficacy (maximum achievable response).

Pharmacodynamics

  • Pharmacokinetic processes

    • Absorption, distribution, metabolism, and excretion (ADME) -Transport Processes : Passive transport (diffusion, filtration) & Carrier-mediated transport (active and facilitated)
  • Fick's law describes rate of diffusion across membrane surfaces.

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