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78 Cards in this Set
- Front
- Back
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Antagonist
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Prevents Binding by other molecules on a receptor.
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Competitive Antagonists
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AKA: reversable
Surmountable, Both Antagonist and agonist bind to site receptor and compete |
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Irreversible Antagonist
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AKA: Non-competitive
Drug binds to the receptor and stays bounds. High Affinity |
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Agonist
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Drugs bind to and activate the receptor
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Partial Agonists
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Blocks the agonist binding site with less response than a full agonist. *Hovers Over Sight*
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Reversible Antagonists
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Readily Dissociate for receptor
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Chemical Antagonists
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**Ionically Binds**
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Pharmacological Antagonist
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Same action as an Agonist
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Physiologic Antagonist
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Opposite effect of the agonist
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Agonist
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Bind, directly or indirectly bring about the effect
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Affinity
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How well binds to the receptor
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Efficacy
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How well it causes a response
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Full Agonists
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Produces a full response at full receptor occupancy
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Partial Agonists
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Lower responses at full receptor occupancy
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Adverse Drug Reactions
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Harmful or unintended response
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Calcium Channel Blocker
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Ca2+ Blocking
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Cytokins
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Receptor for many polypeptide growth factors
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Potency
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The amount of drug needed to produce an effect.
Evaluated with Strength and Effectivness |
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Solubility of Water
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More Charged = More water soluble = Directly Proportional
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Solubility of Lipids
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More Charged = Less Lipid soluble = Inversely proportional
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Aqueous Diffusion
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Higher to Lower concentration = Fick's Law
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Lipid Diffusion
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Fick's Law =MOST IMPORTANT LIMITING FACTOR FOR DRUG PERMEATION IS THE LIPID BARRIERS
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Osmosis
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Water through semi-permeable membrane...Fick's Law
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Lipophilicity
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Ability of a chemical compound to dissolve in fats, oils, lipids and NON-Polar solvents
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Therapeutic Index
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Lethal Dose (LD50) / Effective Dose (ED50)
High value is better than low |
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Toxicology
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Undesirable effects of chemical on living systems
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Forensics
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Application of basic sciences to solve crimes
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Pharmacology
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Study of substances that interact with living systems through chemical processes
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Pharmacodynamics
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Effect of DRUG on the BODY
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Pharmacokinetics
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Effect of BODY on the DRUG
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Bioavailability
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Fraction of unchanged drug reaching the systemic circulation following administration
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Maximum Effect
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(EMAX) Efficacy of a drug is the maximum effect achievable
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Delayed Effect
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Changes in drug effect often delayed in relation to changes in the plasma
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Cumulative Effects
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Drug effects may be related to cumulative action
IE: Chemotherapy |
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Immediate Effects
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Drug effects are DIRECTLY related to plasma concentration
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Receptor
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Specific component of a cell that interacts with a drug and initiates a chain of events
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GABA Receptor
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The Chief inhibitory neurotransmitter in the CNS
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Orphan Receptors
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Special Drug research done to create drugs that can bind to these. Have unknown ligands
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Half Life
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Time required to change the amount of drug in the body by one-half
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Absorption
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Determined by site of administration and drug formulation
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Zero Order Absorption
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Rate of absorption is INDEPENDENT of drug remaining in gut
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First Order Absorption
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Rate is PROPORTIONAL to amount of drug in gut
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Volume of Distribution
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Amount/Concentration
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Metabolism
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Common Sense??
Based on a number of factors |
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Elimination
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Clearance
= Rate of Elimination / Drug concentration |
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Two major sites of drug elimination
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Renal and Hepatic
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Steady State elimination
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Rate of Drug Administration = Rate of Elimination
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First Order Elimination
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Rate of drug eliminated is DIRECTLY proportional to concentration of the drug
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Capacity Limited Elimination
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Once saturation has occurred, the rate of elimination fails to increase with increased drug amount.
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What Quantifies Drug Safety?
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The Therapeutic Index
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Protonation
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Combining with a proton
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Effective Dose
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ED50
50% of population manifests given effect |
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Toxic Dose
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TD50
50% of population manifests given toxic effect |
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Lethal Dose
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LD50
Dose which kills 50% of subjects |
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Biotransformation
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Occurs between absorption and elimination
Phase I and Phase II |
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Phase I of Biotransformation
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Makes a drug more polar
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Phase II of Biotransformation
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Makes a drug even more polar than Phase I or "Highly Polar"
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Quantal Dose Response
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Shows Population response to different doses of a drug
ED50 is used |
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All-or-None Effect
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Used in Sleep Medications
-Either you fall asleep or you do not. |
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Clearance is the most important factor to...?
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Determining Drug Concentration
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Which route of administration has the most rapid onset?
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Intravenous
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Which route of administration is most convenient?
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Oral
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Which route is very slow, but used for its lack of first pass effect?
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Trans-dermal
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Drug Trial Phase 1
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Small Number of HEALTHY people.
IS IT SAFE? |
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Drug Trial Phase 2
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Modest number of SICK people.
DOES IT WORK ON PATIENTS? |
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Drug Trials Phase 3
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Larger group of SICK people.
DOES IT WORK IN A DOUBLE BLIND? |
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Drug Trials Phase 4
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Post Marketing Surveillance
Does not really ever end unless the drug is pulled from the market etc. |
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Acute Toxicity
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1 Dose, 2 Species
Rather Quickly |
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Subacute Toxicity
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3 Doses, 2 species,
4 Weeks to 3 months |
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Chronic Toxicity
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6 Months or longer
-Rodent and non rodent species |
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Carcinogenic Potential
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When drug is intended for prolonged use. 2 years, 2 species
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Mutagenic Potential
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Effects on genetic Stability
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Investigative Toxicology
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Determins sequence of mechanisms of toxic action
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Creatine Clearance
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Quantitative Indicator of Renal Function
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FDA
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Grants Approval for marketing of new drugs
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IND
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Key Words = Filed with FDA once a drug is Ready to be studied in humans
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NDA
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Key Words = Phase 3 is successful....Submitted to request permission to market
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ANDA
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Key Words = GENERIC APPROVAL
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