A drug administered at a high dose is generally absorbed more quickly.
Metabolism and excretion.
Higher solubility generally increases absorption.
Oral intake and intravenous.
The time it takes for the drug to dissolve in a medium.
It leads to a more rapid onset of action.
Route of administration.
Route of administration.
Disintegration of solid drug into smaller particles.
Fluids, solids, or gases.
The rate of excretion.
They stimulate or inhibit normal cellular activity.
Highly selective and competitively inhibited by other co-transported substances.
Drug effectiveness, adverse drug effects, over-dosage, and drug interactions.
Desired effect (Therapeutic effect) and undesirable effect (Adverse effect).
Principles of drug actions and interactions.
Liquid formulation is absorbed faster than tablet or capsule.
Distribution, where they enter the interstitium (extracellular fluid).
Organs with extensive blood supplies, such as the heart, liver, kidneys, and brain.
Changes in gastrointestinal (GI) motility.
Post-receptor effects and chemical reactions leading to a biological or physiological response.
Intramuscular (IM) administration.
The mechanisms of drug action and the relationships between drug concentration at the site of action and the resulting effects in the body.
The therapeutic response of most drugs is directly related to their level in the plasma.
A higher dosage to achieve the same therapeutic response or a change to a different drug in the same group.
The process where large molecules are engulfed by the cell membrane in vesicles.
It carries blood from the liver to the tissues, which is nutrient-poor and low in oxygen.
The plasma drug concentration between Minimum Effective Concentration (MEC) and Minimum Toxic Concentration (MTC).
They enter the bile and are carried into the intestinal lumen, then excreted as feces.
Undesirable effects that can be toxic or non-toxic, and may include predictable secondary effects.
The liver.
It refers to a substance that is attracted to lipids (fats).
TI = median lethal dose (LD50) / median effective dose (ED50).
Absorption, distribution, metabolism, and excretion.
The process by which drug molecules gain access to the bloodstream from the site of administration.
It can affect the ionization and solubility of the drug.
The process by which the concentration of a drug is significantly reduced before it reaches systemic circulation.
Occurs when drug levels exceed the therapeutic range, potentially due to overdose or accumulation.
Oral drugs can be extensively metabolized and often inactivated by the liver, reducing the dosage that reaches systemic circulation.
Through bile and urine.
A decreased responsiveness to a drug over the course of therapy due to adaptation.
It determines the duration of action.
Drug Z, with a TI of 10, is safer than Drug X with a TI of 4.
Because they are too large to pass through.
By pinching off the vesicles and breakdown of its membrane.
Excretion through bile.
ATP.
The formation of a drug-receptor complex.
Drug formulation and dose.
Water-soluble, charged, ionized substances.
The mechanism where drugs exert their effects on the body.
The process where all molecules absorbed from the gastrointestinal tract travel to the liver before reaching systemic circulation.
It refers to the metabolism of a drug before it reaches systemic circulation, mostly affecting orally administered drugs.
Pregnancy, age, and organ function.
Enteral (腸內).
Greater blood flow to the site of administration leads to faster absorption.
Small water-soluble metabolites.
It is crucial for understanding how drugs exert their effects on the body.
It can slow stomach motility and delay absorption of drugs taken with the meal.
They attach, elicit a response, and block other responses, binding with diminished response compared to full agonists.
To address special considerations and minimize risks.
Uncharged molecules.
A drug’s safety margin.
They are reabsorbed in the intestine and re-enter the hepatic circulation for metabolism.
Negative side effects such as allergic reactions.
Drug form, route of administration, gastric mucosa and motility, food-drug or drug-drug interactions, and changes in liver metabolism and rate of elimination.
Increased water solubility of drugs.
It diffuses across the membrane to interact with its intracellular receptor.
Certain foods can affect hepatic cytochrome P450 activity, decreasing liver metabolism and increasing half-life.
Introduction to Pathophysiology and Pharmacology.
The process of drug movement to achieve drug action, or how the body handles the drug.
Absorption, Distribution, Metabolism, Excretion.
Cross tissue membranes.
Excretion.
By interacting with receptors in the body.
They directly enter the bloodstream, allowing for rapid absorption by tissues.
Parenteral (腸外).
It may be fully used, meaning all carriers are occupied.
About 90-95%.
Minimum Toxic Concentration, the level of drug that will result in serious adverse effects.
Because of its large surface area and more permeable membranes.
They have low lipid solubility but high water solubility, making them unable to penetrate the lipid membrane.
It must be largely lipophilic and have some solubility in aqueous solutions.
Cardiac output, regional blood flow, and extent of plasma protein binding.
Amount of drug given, frequency of administration, route, and drug-food & drug-drug interactions.
They inactivate them and convert them into inactive metabolites for excretion.
Rash, nausea, and itching.
Warfarin (anticoagulant).
Peak drug levels are not necessarily above optimal therapeutic effect but depend on the accessibility of medications to their targets.
Inactive protein.
It occupies a receptor and prevents the endogenous chemical from acting.
80 minutes (4 half-lives).
It is non-ionized and readily absorbed in the stomach, but becomes ionized in the alkaline environment of the small intestine.
Passive transport, active transport, and pinocytosis.
The movement of drug through the body.
Distribution.
It influences the effectiveness of the drug.
Orally administered drugs take longer to absorb.
Increased blood flow and surface area enhance absorption.
The more rapid the dissolution, the faster the drug absorption and onset of action.
Energy from the hydrolysis of ATP.
The period of time required for 50% of the drug to be eliminated from the body.
Urinary excretion.
Drugs are poorly absorbed.
It carries nutrient-rich blood and absorbed drugs from the gastrointestinal tract to the liver.
The larger the total surface area, the quicker the absorption.
The force of attraction between the drug and the receptor.
The ability of a drug to cause the expected response.
By forming a chemical bond with specific sites, similar to a lock-and-key mechanism.
A cellular macromolecule, mostly proteins, to which a drug binds to initiate its effect.
Because it is affected by the rate of absorption and first-pass metabolism.
It refers to a substance that is attracted to water.
It initiates transmembrane signaling mechanisms.
MEC stands for Minimum Effective Concentration and MTC stands for Minimum Toxic Concentration.
They enter the biliary system.
Differences in plasma concentration after a standard dose.
Body pH.
Extent of binding of drugs to tissue proteins and special anatomic barriers.
A sweet liquid taken orally, such as an antihistaminic elixir against allergy.
A combination of different drugs or ingredients, uniformly dispersed in a liquid on shaking.
A solid unit dosage form of medicament(s) with suitable excipients, usually pressed from a powder into a solid dose.
The onset, duration, and intensity of a drug’s effect.
By being transported through circulating body fluids (plasma) to the interstitium or receptors.
A series of second messenger events is triggered within the cell.
Intravenous administration.
Enteral (腸內) and Parenteral (腸外).
Overdose (intentional or unintentional) or accumulation of the drug.
It greatly reduces the bioavailability of oral drugs.
It would take an error in magnitude of approximately 4 times the average dose to be toxic.
Drugs become less active and are converted into drug metabolites.
Minimum Effective Concentration, which is the minimum plasma concentration required to produce a therapeutic effect.
A higher TI indicates a larger margin of safety before reaching toxic levels.
They are filtered and enter the renal tubules.
6.25%.
Drug X: 10 mg; Drug Z: 20 mg.
The amount of time it takes to produce a therapeutic effect after drug administration.
Greater drug safety.
Metabolism.
Half-life (t 1/2).
Plasma half-life.
The process by which the concentration of a drug is significantly reduced before it reaches systemic circulation, affecting bioavailability.
An immediate hypersensitivity reaction leading to life-threatening respiratory distress and vascular collapse.
Dysfunction in these organs alters drug metabolism and/or excretion, leading to an increased half-life.
Accumulation of the drug and prolonged action.
It refers to the dose at which 50% of the population shows a response or dies, respectively.
Allylamine and azoles.
Aspirin (ASA).
Drug formulation and dose.
Lipid-soluble, uncharged, non-ionized substances.
The proportion of a drug that enters the circulation when introduced into the body and is available for action.
Conversion of ATP to cyclic AMP for intracellular signal induction.
A carrier (enzyme or protein) to move substances against the concentration gradient.
It increases the rate of gastric emptying.
Digestive motility; drug-food or drug-drug interactions.
They are activated as part of the second messenger events.
Enteral (腸內) and Parenteral (腸外).
It may lower the concentration gradient across intestinal mucosa and reduce absorption by passive diffusion.
They increase the risk of adverse effects.
Drug selection and dose adjustment.
Non-ionized (uncharged) and ionized (charged) forms.
If they are still lipid-soluble.
The percentage of administered drug available for activity, or the fraction of the drug that reaches systemic circulation in an unchanged form.
By comparing plasma levels of a drug after a particular route of administration with plasma drug levels achieved by intravenous (IV) injection.
Endogenous molecules such as hormones, neurotransmitters, and growth factors.
More frequently, such as every 4-6 hours.
Digoxin.
Bound drugs form a drug-protein complex that is inactive and serves as a reservoir, slowly releasing free drug when concentration drops.
A drug that produces the desired response similar to the endogenous substance.
It affects the degree of ionization of a drug.
Through binding to lipids, proteins, or nucleic acids.
Hemorrhagic cystitis from metabolites of cyclophosphamide in bladder mucosa.
The movement of drugs across the cell membrane down the concentration gradient.
Due to solubility in the membrane lipid bilayers.
Its release is part of the second messenger events that initiate the drug's action.
The study of the biochemical and physiological effects of drugs.
They delay gastric emptying.
It takes a longer time for the medication to be excreted.
Drugs that attach to receptors but do not cause a response, preventing the binding of agonists.
They attach to receptor sites and cause a response, with better fit leading to a better response.
It implies a moderate risk, as it takes 4 times the average dose to reach toxicity.
To keep its plasma concentration within the therapeutic range.
The longer the contact time, the higher the percentage of drug absorbed.
It limits absorption due to less contact time.
It occurs when the medication has reached its highest concentration in the bloodstream after absorption.
A narrow margin of safety between an effective dose and a toxic dose.
Noxious, unintentional, unexpected reactions to drug therapy occurring at normal dosages.
Unbound drugs are freely diffusible, while bound drugs serve as a reservoir, leading to slower elimination and increased half-life.
The dose required to produce a specific therapeutic response in 50% of a group of patients.
Pharmacokinetic parameters MEC and MTC.
4-8 hours.
Median toxicity dose, which is the dose that will produce a given toxicity in humans.
A drug that produces a weaker or less efficacious response than a full agonist.
Bone marrow, teeth, and adipose tissue.
They prevent many chemicals and medications from entering the CNS.
Sedatives, antianxiety agents, and anticonvulsants.
Most antitumor medications do not easily cross the blood-brain barrier.
They create a stable and strong tablet, offering branding colors and identifiable coatings.
Administering it with food or drugs containing calcium, iron, or magnesium.
48 hours (4 half-lives).
They provide a larger surface area for absorption compared to the stomach.
Their water-solubility.
Specific molecules and chemicals in the body.
Half-life (t 1/2).
Ampula of Vater, Sphincter of Oddi, and the Common bile duct.
Heart, liver, kidneys, and brain receive much greater blood flow than skin, skeletal muscles, and adipose tissue.
Median effective (therapeutic) dose.
Every 3-4 hours.
It is proportional to the number of drug-receptor complexes formed.
Enzymes, nucleic acids, or membrane-bound proteins.
>10 hours (or 24 hours).
Detoxification.
Because it is mostly ionized in the low pH environment.
Patients will have diminished ability to excrete medications and may retain drugs for an extended period.
Desirable effects such as improvement in signs and symptoms and/or physical functioning.
The process where most bile is circulated back to the liver, allowing a percentage of the drug to be recirculated numerous times before being metabolized.
Drowsiness after taking antihistamines at bedtime.
At greater intervals, such as once daily.
Most drugs are transported in combination with plasma proteins; unbound (free) drug is the active form.
They couple with transmembrane receptors when a ligand binds to them.
10 hours.
To find the dose of a drug that will be lethal in 50% of a group of animals during preclinical trials.
Grapefruit.
It increases water solubility and diminishes pharmacologic effects.
Absorption.
Excretion through urine and urinary excretion.
Because it can diffuse across membranes to reach target cells or be excreted by the kidneys.
Median lethal dose.
Drugs and other chemicals may compete for binding sites based on their affinity for plasma proteins.
The process where drugs are metabolized in the liver before reaching systemic circulation.
Most of the drug is non-ionized, favoring diffusion through the gastric mucosa.
It can affect the ionization and thus the absorption of drugs, such as with the use of antacids.
Through absorption across the mucosal lining of the small intestine.
To provide a sweet coat and aroma on foul-smelling pills, especially for children.
The movement of drugs of low lipid solubility relying on a drug transporter protein, still down the concentration gradient.
They cross renal tubular membranes easily and return to circulation.
40 hours (4 half-lives).
It affects the enzyme that metabolizes statins, potentially leading to increased plasma concentration and overdose.
Viscous concentrated solutions of sucrose, for example, cough syrup.
Hard capsules are made of a rigid shell in two pieces, while soft capsules are a single piece suitable for oils.
Because they readily cross cell membranes.
A coarse dispersion where the internal phase (insoluble solid particles) is uniformly dispersed throughout the external phase (suspending medium).
Through aqueous channels or pores.
To provide a gastric acid-resistant coating, allowing the drug to reach the targeted area without being affected by acidity.
Doses must be reduced to prevent toxicity.
Because they have a shell or container made of gelatin that contains the drug.
Ionized (charged) and water-soluble drugs.
It increases the lipid solubility of the drug and hence increases the rate of diffusion.
They must first be metabolized into more polar (hydrophilic) substances in the liver.
