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297 Cards in this Set
- Front
- Back
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The pure food and drug act provides...
This act prohibits.... |
standards for drug purity and labeling (strength and purity);
misbranding or adulteration of drugs by prohibiting interstate commerce of misbranded and adulterated foods and drugs |
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The Pure Food and Drug Act was amended to prohibit:
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false or fraudulent advertising claims
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Examples of things outlawed by the Pure Food and Drug Act:
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Misbranded (labeling is false and misleading, doesn't contain adequate directions for use), adulterated (manufacturing is noncompliant with current good manufacturing processes, is packaged under unsanitary conditions)
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Federal Food, Drug, and Cosmetic act originally did not require...
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prior clearance by FDA of drug testing in humans
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Premarketing clearance for safety makes sure that:
Does this through: |
new drugs are safe as well as pure in order to be introduced into interstate commerce.;
requiring adequate testing of a compound to prevent marketing of a possibly toxic substance |
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Durham-Humphrey Amendments is responsible for...
Also provides rules for... |
separating drugs into Legend drugs and non legend drugs;
dispensing legend drugs |
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Legend drugs are those that...
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require a Rx
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Nonlegend drugs are those that....
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do not require an Rx; OTC drugs
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Legend drugs are those drugs that....
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cannot be safely used without medical supervision by a licensed practitioner
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Kefauver-Harris amendments provide...
they require... before any new drug can be placed in interstate commerce |
premarketing clearance for efficacy.;
proof of efficacy as well as safety |
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Kefauver-Harris Amendments also regulate the guidelines for conducting......
Also strengthened... |
clinical trials;
FDAs authority over human testing of new drugs |
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Kefauver-Harris Amendments also regulate the guidelines for conducting......
Also strengthened... |
clinical trials;
FDAs authority over human testing of new drugs |
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Comprehensive Drug Abuse Prevention and Control act of 1970 established....
Also regulates.... |
control (registration, FDA) and enforcement (DEA) over drugs;
Production, distribution, exportation, and importation of controlled substance |
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Comprehensive Drug Abuse Prevention and Control act of 1970 established....
Also regulates.... |
control (registration, FDA) and enforcement (DEA) over drugs;
Production, distribution, exportation, and importation of controlled substance |
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Poison Prevention Packaging Act enforced...
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child resistant containers
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The child resistant containers applies to _____ and ______ with 2 exceptions: ____ and ____
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all controlled substances;
All legend drugs; sublingual nitroglycerin and oral contraceptives |
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Poison Prevention Packaging Act enforced...
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child resistant containers
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Orphan Drug Amendmants encourage the pharmaceutical industry to....
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develop drug products for rare diseases or medical conditions for whose marketing would not otherwise be profitable since the affected pt population is too small
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Poison Prevention Packaging Act enforced...
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child resistant containers
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FDA Amendments Act of 2007 gave the GDA authority to...
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require risk evaluation an mitigation strategies for managing known of potential serious drug risks.
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The child resistant containers applies to _____ and ______ with 2 exceptions: ____ and ____
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all controlled substances;
All legend drugs; sublingual nitroglycerin and oral contraceptives |
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Poison Prevention Packaging Act enforced...
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child resistant containers
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The child resistant containers applies to _____ and ______ with 2 exceptions: ____ and ____
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all controlled substances;
All legend drugs; sublingual nitroglycerin and oral contraceptives |
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Orphan Drug Amendmants encourage the pharmaceutical industry to....
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develop drug products for rare diseases or medical conditions for whose marketing would not otherwise be profitable since the affected pt population is too small
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Orphan Drug Amendmants encourage the pharmaceutical industry to....
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develop drug products for rare diseases or medical conditions for whose marketing would not otherwise be profitable since the affected pt population is too small
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The child resistant containers applies to _____ and ______ with 2 exceptions: ____ and ____
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all controlled substances;
All legend drugs; sublingual nitroglycerin and oral contraceptives |
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FDA Amendments Act of 2007 gave the GDA authority to...
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require risk evaluation an mitigation strategies for managing known of potential serious drug risks.
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Orphan Drug Amendmants encourage the pharmaceutical industry to....
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develop drug products for rare diseases or medical conditions for whose marketing would not otherwise be profitable since the affected pt population is too small
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FDA Amendments Act of 2007 gave the GDA authority to...
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require risk evaluation an mitigation strategies for managing known of potential serious drug risks.
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FDA Amendments Act of 2007 gave the GDA authority to...
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require risk evaluation an mitigation strategies for managing known of potential serious drug risks.
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Schedule 1 drug characteristics:
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high abuse and NO accepted medical use in US
(hallucinogens, marijuana, methaqualone) |
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Schedule 2 drug characteristics:
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currently accepted medical use in the US with high abuse potential that results in severe physical or psych dependence.
(opiates, metahdone, amphetamines) |
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Schedule 3 drug characteristics:
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abuse potential less than schedule 2.
(barbituates and anabolic steroids included) |
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Schedule 4 drug characteristics:
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abuse potential less than schedule 3
(includes benzodiazepines, chloral hydrate/nonbarbituate sedatives) |
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Schedule 5 drug characteristics:
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lowest abuse potential
(antitussive, antidiarrheal opiate-like drugs) |
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In AL, codeine-containing cough syrups require _____ and are placed in schedule ___.
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Rx;
III |
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What are the 4 things included on a written Rx?
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date, name and address of pt, 'sig'/signature
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The 'Sig' on an Rx functions to....
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give directions to the pt that is placed on the label of the medication
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Schedule II drugs allows ___ refills.
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NO
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Schedule III-V allows ____ refills...
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5 max (or 6 mo from date Rx was written)
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Signature has two different lines for AL. These are:
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"Dispense as written" or "Product selection permitted"
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"Dispense as written" indicates that
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the pharmacy is not allowed to substitute the brand name for a generic
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"Product selection permitted" allows....
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permission for the generic substitution if requested
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The prescribers actual signature is required for schedule ___ drugs.
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II
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DEA # of each physician is required on the Rx for...
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all controlled substances
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There are no verbal Rx's allowed for schedule ___ drugs in AL. Schedule ___-____ are allowed verbal orders.
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II;
III-V |
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For schedule II drugs, the Rx needs the prescribers ........
It must be signed the same ____ and ___ refills are allowed. |
actual signature;
day; NO |
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A podiatrist can only prescribe controlled substances for....
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ailments of the foot
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Optometrists can prescribe analgesics in schedule ____ (duration not longer than 96 hours), ___, and ___ with the exception of....
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III, IV, V;
Class III agents containing hydrocodone |
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Registered nurse practitioners can prescribe...
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legend drugs not including controlled substances
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Pre-clinical phase of drug development begins with _____ which begins with....
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discovery;
patent application for compounds with biological activity |
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Phase 1 of drug development includes testing of...
Subjects are: |
the safety and tolerance of intended dosing regimens;
paid healthy volunteers |
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Phase 2 of drug development includes testing of...
Subjects include: |
efficacy in treatment of disease in which it is intended as well as the short-term side effects and risks in actual pts;
several hundred subjects used at multiple sites |
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Phase 3 of drug testing expands on.....
Subjects include: Conducted by.... |
the results of phase 2;
several thousand subjects; numerous qualified physicians in multiple test centers (double-blind) |
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Phase 3 evaluates the...
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benefit-risk relationships and detection of less common and rare side effects/adverse reactions
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Phase 4 consists of the.....
Monitors the..... This phase may uncover... |
post-marketing surveillance;
safety under actual conditions of usage with annual reports toxic symptoms that occur with a very low incidence |
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Generic drugs must be __________ as the brand name. This means that....(3)
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pharmaceutically equivalent.;
they contain the same active ingredients, are of the same dosage form and route of admin, are identical in strength or conc |
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Bioavailability is the.....
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rate and extent to which the active ingredient or active moiety is absorbed from the drug product and becomes available at the site of drug action
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Drug products are considered bioequivalent if they are....
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complarably bioavailable.
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In general, a drug is considered to be bioequivalent to a reference drug if....
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the rate and extent of absorption of the drug do not show a significant difference from the rate and extent of absorption of the reference drug
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If two drug products are bioequivalent and tested under the same conditions, their plasma concentration-time curves should be...
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virtually superimposable or the differences very small and lie within defined limits
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Drugs are considered therapeutically equivalent only if...
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they are pharmaceutically equivalent and if they can be expected to have the same clinical effect and safety profile when administered to its under conditions specified in the labeling.
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FDA considers a drug to be therapeutically equivalent if it meets the following 4 criteria:
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is pharmaceutically equivalent to reference product; is bioequivalent to the reference point; is adequately labeled; is manufactured in compliance with CGMP regulations
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Currently, dietary supplements are not considered to be...
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new drugs
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Dietary Supplement Health and Education Act of 1994 states that health claims that describe the effects of a substance on a disease or health related condition require....
Nutrient content or structure/function claims... |
premarket approval;
do not require premarket approval by the FDA |
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Certain publications are excluded from misbranding provisions since they are not considered....
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labeling when used in connection of the sale of dietary supplements
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What are the 2 types of receptors?
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membrane (integral) and intracellular (proteins, nucleic acids)
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In the presence of full agonist, equilibrium is shifted towards the receptors......
This produces a... |
active state conformation;
maximal pharmacological response |
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A drug with lower affinity for the active state and some affinity for the inactive state=
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partial agonist
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A ____________ binds to both active and inactive receptor conformations with equal affinity and produces no response.
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competitive antagonist
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Upregulation is a..
The receptor then becomes...... to even very small amounts of agonist producing an ..... |
deficient production or inadequate release of an endogenous agonist results in lack of exposure of the receptor to its endogenous agonist.;
supersensitive; exaggerated response |
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Downregulation is the=
Results in a ____ receptor sensitive and a _____ response |
overexposure to excessively high amounts of the agonist for prolonged periods;
decreased; decreased |
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A full agonist drug is one which...
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causes activation of a receptor to produce a pharmacologic response that is the same that is produced by the endogenous ligand for that receptor
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Direct acting agonists:
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Interacts directly with the same site as the endogenous ligand
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Partial agonist drug is one which...
cannot produce the... |
interacts with a receptor but produces a much weaker pharmacologic response than a full agonist;
maximal (100%) response produced by full agonists but can bind to the receptor with high affinity similar to full agonists |
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Competitive antagonists are drugs which..
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interact with the same receptor site as the endogenous agonist to block the actions of the endogenous agonist
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The competitive antagonists have no...
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pharmacological properties of its own except to block access to the receptor for the endogenous ligand/agonist drugs.
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When competitive antagonists bind to the receptor the normal biological response is..
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diminished or abolished
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Noncompetitive antagonists are ________. They form a ____ bond with the same receptor site as occupied by the endogenous agonist.
Once bonded, the receptor is permanently _____ and undergoes...... |
irreversible; covalent;
inactivated ;protein turnover |
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Affinity is the measure of...
Interaction occurs through.. |
a drugs ability to interact with a receptor;
binding to the receptor via non covalent forces (agonist, comp antagonist) or covalent forces (noncompetitive antagonists) |
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Agonists have ____ affinity;
Antagonists have ___ Affinity; Partial agonists usually have ____ affinity that may even be... |
high; high;
high, even higher than the full agonist |
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IF a full agonist with high affinity and a partial agonist with equally high affinity compete for the same receptor, the _____ behaves like a competitive antagonist towards the ____.
Dose-resposne curve is shifted to the _____. |
Partial agonist ; full agonist
right |
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Efficacy is the measure of a drugs ability to...
The drug-receptor complex interacts with some type of.... |
produce a pharmacologic response after interaction with a receptor has occurred.;
transducer mecahnism to produce the final biologic resposne |
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Agonists have ____ efficacy
Antagonists have ____ efficacy Partial agonists have ___ efficacy |
high;
zero; low |
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Potency is the measure of the...
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dose of a full agonist required to produce the max pharmacologic response (when comparing 2 full agonists)
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A competitive (reversible) antagonist is a drug molecule that will....
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compete with an agonist for binding to the receptor
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The response of an agonist is abolished or diminished if the antagonist....
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can successfully compete for the receptor site
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The competition between an agonist and a competitive antagonist can be overcome by....
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flooding the receptor site with a very lg concentration of agonist and full response can be restored
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Competitive antagonists bind to the receptor site using...
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non-covalent forces
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A non-competitive irreversible antagonist is a drug molecule which....
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binds to the receptor and does not dissociated and cannot be displaced by increasing agonist concentration
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If the non-competitive antagonist concentration is high enough, so many receptors....
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become inactivated that the full response cannot occur (although some pharmacologic activity of the agonist is usually still present)
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Non-competitive antagonists bind to the receptor usually through _______ bonds which are very _____ and effectively.......
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covalent;
stable; inactivate the tumor permanently (if tx a tumor) |
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Full biological responses cannot occur when non-competitive antagonists bind to the receptors and the inactivated receptors undergo _____ and ......
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turnover;
new receptors are synthesized |
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Low doses of non-comp irreversible antagonists inactivate many receptors but...
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there are still enough 'spare' receptors left over to produce the full response
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Effective dose 50 =
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the dose which produces a desired therapeutic effect in 50% of test subjects
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Lethal dose 50=
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dose which is lethal to 50% of test subjects
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Therapeutic index equation
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TI= LD50/ED50
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A very low therapeutic index means that....
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there is a small difference between the doses of a drug which produce therapeutic effects and the doses of a drug which causes lethal effects
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Drug allergy is not ___-related, not ____ initially but recurrence upon rechallenge is, is not a receptor ____ but rather is ___-mediated
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dose;
predictable; interaction; immune |
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In a drug allergy, ______ can occur.
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anaphylaxis
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Side effects are...
By definition, they are ______. |
unwanted effects of drugs that appear at normal doses required for therapeutic response;
tolerable |
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Toxicity is..
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unwanted effects of drugs that appear as drug dosage is increased beyond the dose required for therapeutic responses
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Intolerance occurs at...
Effects are.... |
normal therapeutic doses;
Severe and disabling, usually requiring d/c of drug |
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Idiosyncrasy is the genetically determined....
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abnormal responses to drugs due to enzyme deficiencies or inability to detoxify
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Some allergic reactions to drugs may be _____ responses and not mediated by the immune system
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idiosyncratic
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Renal clearance of a substance is the...
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volume of plasma that is completely cleared of the substance by the kidneys per unit time
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In order to estimate GFR, you need a substance that is...
In this case, the amount filtered = amount _______ |
freely filtered (unbound to plasma proteins) and is neither reabsorbed or secreted;
secreted |
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A MW of ____ is small enough to allow filtration
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5200
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____ clearance is the most widely used for the clinical estimation of GFR
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Creatinine
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If Clearance<GFR then net _____ must of occurred.
If Clr >GFR then net _____ must have occured |
absorption;
Secretion |
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The clearance of creatinine is important because it as as an indicator of _____ as measured by the GFR and also can be used to.....
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renal fx;
design and modify drug dosing regiments |
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Drugs which are entirely or mainly dependent on glomerular filtration for elimination from the body will have _________ in renal disease.
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altered dosing regimens
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Additive effects:
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combination of two drugs acting through different mechanisms producing a pharmacological effect that is the sum of the two individual drug effects
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Synergistic effects:
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combination of two drugs producing an effect that is greater than the sum of the two individual effects
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Antagonism:
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combined effect is less than the effect produced by the active drug alone; the second drug eliminates or diminishes the activity of the first drug
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Drug absorption is delayed in the presence of ______.
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food
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Solid food slows _____ which results in the delaying of ____ and lowering drug-peak levels
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gastric emptying;
absorption |
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Food may promote drug absorption in some cases. For very ____-soluble or ____-insoluble drugs, absorption is enhanced when taken with fatty meals.
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lipid;
water |
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Grapefruit juice has a few different effects on drug absorption. They are:
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inhibits 3A4 isoenzyme of the cytochrome P450 system; inhibits intestinal P-glycoprotin, may cause plasma concentrations of the affected rugs to rise markedly and cause toxicity
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The interaction with drugs and grapefruit juice only occurs when...
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drugs are administered orally exhibiting high first-pass effects
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Absorption can be due to ____ and _____ containing antacids or due to _______ via ____ or ____ by divalent and trivalent cations
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charcoal; aluminum/magnesium hydroxide;
complexation; cholestyramine or chelation |
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Certain drugs and foreign chemicals stimulate the activity of _____ in the liver (ex. _____) by inducing...
This is called.... |
drug-metabolizing enzymes;
P450 system; the synthesis of these enzymes; Induction |
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The net effect of induction is to ....
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increase the metabolism of other drugs normally metabolized in the liver and to decrease their pharmacologic effects
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Several days of phenobarbital tx are required for _____ effects to appear, with maximal effects in _____. These effects may persist for some time after.........
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inducing;
2-3 weeks; The drug is withdrawn |
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Induces may also stimulate ....... via .......
_______ is included in this class |
their own metabolism;
an increased synthesis of metabolizing enzymes; Rifampin |
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Certain drugs may inhibit the activity of........
By interfering with the metabolism of other drugs, inhibitors may ____ or ____ the activity of drugs normally metabolized in the liver result in in..... ______ is in this class |
drug-metabolizing microsomal enzymes in the liver;
increase or prolong; increased plasma levels and toxicity; Cimetidine (tagumet) |
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Probenecid is a ______ agent which competitively inhibits the ____ of many anionic drugs. This results in decreased ________, ______ and increased ________.
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tubular blocking agent;
active tubular secretion; urinary excretion, drug retention, and increased half-life; |
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Organic acids exist as _____ at plasma pH
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anions
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Drugs are chemicals that cause.......... due to interaction with ______.
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changes in the biological system;
biological receptors |
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The fact that a receptor exists indicates the ......
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presence of an endogenous ligand for that receptor
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The lower Molecular Weight limit of a drug is set by the requirement of __________.
There must be _____ present on drugs to interact with the complementary receptor structures. |
receptor specificity;
functional groups |
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A sufficient number of chemical function groups must be present on a drug in order for....
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receptor binding to successfully occur
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Irreversible bonds are ____ bonds and are very ___ and usually.....
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covalent bonds;
strong; irreversible in biological systems |
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Reversible interactions are _____ bonds
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non-covalent
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Since individual non covalent bonds are weak and since only a few are formed, there must be a very _______ to the receptor if the drug-receptor interaction is to occur
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specific fit
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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Full agonists produce ____% of the biological response (same degree of response as....)
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100;
the natural ligand |
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Direct-acting agonists are drugs which .......... causing the production of the ........
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directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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Full agonists produce ____% of the biological response (same degree of response as....)
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100;
the natural ligand |
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Receptors in a biological system virtually always interact with only one _______ of an enantiomeric pair, with the other being inactive.
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stereoisomer
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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Direct-acting agonists are drugs which .......... causing the production of the ........
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directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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Full agonists produce ____% of the biological response (same degree of response as....)
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100;
the natural ligand |
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One of the enantiomers has much greater _____ than the other due to...
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activity;
a higher affinity for the receptor |
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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Full agonists produce ____% of the biological response (same degree of response as....)
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100;
the natural ligand |
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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Full agonists produce ____% of the biological response (same degree of response as....)
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100;
the natural ligand |
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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Direct-acting agonists are drugs which .......... causing the production of the ........
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directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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Direct-acting agonists are drugs which .......... causing the production of the ........
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directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
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Full agonists produce ____% of the biological response (same degree of response as....)
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100;
the natural ligand |
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Transcellular movement is dependent on _____ and _______.
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lipid solubility (Kp) and concentration
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Direct-acting agonists are drugs which .......... causing the production of the ........
|
directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
|
|
Full agonists produce ____% of the biological response (same degree of response as....)
|
100;
the natural ligand |
|
|
Full agonists produce ____% of the biological response (same degree of response as....)
|
100;
the natural ligand |
|
|
Full agonists produce ____% of the biological response (same degree of response as....)
|
100;
the natural ligand |
|
|
Full agonists produce ____% of the biological response (same degree of response as....)
|
100;
the natural ligand |
|
|
Full agonists produce ____% of the biological response (same degree of response as....)
|
100;
the natural ligand |
|
|
Direct-acting agonists are drugs which .......... causing the production of the ........
|
directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
|
|
Full agonists produce ____% of the biological response (same degree of response as....)
|
100;
the natural ligand |
|
|
Direct-acting agonists are drugs which .......... causing the production of the ........
|
directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
|
|
Direct-acting agonists are drugs which .......... causing the production of the ........
|
directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
|
|
Direct-acting agonists are drugs which .......... causing the production of the ........
|
directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
|
|
Direct-acting agonists are drugs which .......... causing the production of the ........
|
directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
|
|
Direct-acting agonists are drugs which .......... causing the production of the ........
|
directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
|
|
Direct-acting agonists are drugs which .......... causing the production of the ........
|
directly bind to the receptor;
identical biological effect normally caused by the endogenous ligand for that receptor |
|
|
Indirect acting agonists produce the same biological action as the direct-acting agonist but use.......which then binds....
|
different mechanisms to increase levels of the endogenous ligand
to the receptor and produces the pharmacological action |
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|
Partial agonists bind .......... but cannot....
_____% response is produced |
directly to the receptor;
fully activate the post receptor mechanisms to produce the biological response; <100 |
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|
Antagonists are drugs which...
|
inhibit the binding of any other substances to the receptor site
|
|
|
Competitive, reversible antagonists bind directly to the ______ usually with ____ affinity.
|
agonist receptor site;
very high |
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Non-competitive, irreversible antagonists bind directly to the _____ with _____ affinity. The ___ bonding results in.....
|
the agonist receptor site;
high; covalent; receptor inactivation |
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Desensitization is the _____ or _____ of receptor activation when agonist is present for prolonged intervals
|
attenuation; elimination
|
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Tachyphylaxis is....
|
very rapid desensitization (minutes to hours) after drug administration
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|
Tolerance is....
|
slowly adapting (days to weeks) desensitization after drug administration
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Transduction is the ____ of the receptor by an agonists which causes cellular signaling mechanisms to become _____ ultimately producing......
|
stimulation;
activated; the biological effect |
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____ Route of administration is the most likely route for the first-passe effect to take place
|
Oral
|
|
|
First-pass effect is.....
|
drug metabolism within the gut wall or liver which may inactivate a portion of the absorbed dose before it even makes it to the systemic circulation
|
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|
Sublingual route has a very _____ response.
|
rapid
|
|
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Buccal route has a ___ release of the active ingredient and is not intended for....
|
slow;
rapid relief of acute conditions |
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Enteric coats are _______ that are resistant to ____ and function to....
This coat dissolves rapidly in the more ____ fluids of the _____ |
polymers;
gastric acid; protect the tablet core from exposure to the acid environment of the stomach; basic; upper SI |
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Gastric emptying of a large object such as an intact enteric-coated depends on.....
|
phase 2 of the migrating motility complex (MMC)
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Disadvantages of Oral route includes:
|
food interactions, inactivated by gastric acid, first-pass effect
|
|
|
Do NOT crush any ______ drugs
|
extended-release or enteric coated
|
|
|
Advantages of sublingual route includes:
|
rapid absorption an donset, avoids exposure to gastric acid and first-pass effect
|
|
|
Advantages of IV route:
|
most rapide acting
|
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Advantages for IM route:
|
suitable for suspensions and depot forms
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|
The rate of absorption of an IM or Subcue injections are dependent on....
|
the blood flow at the injection site
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|
The rate of absorption via IM is usually ______ than subcue
|
faster
|
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Advantages of Subcue route:
|
suitable for suspensions and implants
|
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|
Disadvantages of Subcue route:
|
slower onset than IV or IM
|
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Ophthalmic topical route must be ___ drops or ointments.
|
sterile
|
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|
Sprays may be used for _____ effects
|
systemic
|
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Aerosols are intended for ___ effects
|
localized
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Ointments and transdermal systems may be used for either ____ or ____ effects
|
local; transdermal
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Gastruc emptying usually occurs only on an ____ stomach when the pyloric opening is.....
|
empty; large enough to allow the intact dosage of form to pass
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Extended-release tablets allow .....
|
reducing dosing frequency for better compliance
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Release of drug from oral solutions, elixirs, and syrups is...
|
immediate
|
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Release of drug from the route of admin is dependent on...
|
the dosage form
|
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For immediate release and solid oral dosage forms _____ is the rate limiting step in drug liberation
|
dissolution
|
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In a suspension, the drug particles must completely _____ for release to occur
|
dissolve
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In a capsule, _____ of the drug particles is the rate- limiting stem;
In a tablet = |
dissolution;
dissolution |
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For delayed-release tablets, _______ of the intact tablet into the duodenum is the rate limiting step
|
gastric emptying
|
|
|
___ diffusion is the most common mechanism.
|
passive
|
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Passive diffusion involves the _____ gradient (which is the ______ force for passive diffusion)
|
concentration ;
driving |
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Movement of drug across lipid membranes is favored for the ______ form of the drug (which is more _____ soluble form) which can more easily.......
|
non-ionized;
lipid-; dissolve in and pass through biological membranes |
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The ability of drug molecules to pass through biologic membranes depends on the drugs _______ which is a measure of....
|
partition coefficient (Kp);
a drugs ability to dissolve in a lipid phase compared to an aqueous phase |
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In general, the higher the Kp for a drug, the ____ will be its extent and rate of absorption.
|
better
|
|
|
For a drug to be absorbed via facilitated diffusion, it has the same principles as passive diffusion except....
Does not require _____ |
it needs a carrier molecule
energy |
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The carrier used in facilitated diffusion has both ___ and ____ specificity for certain drugs with complementary chemical structures
|
structural; stereoisomer
|
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The carrier system in facilitated diffusion may become ___ and achieve a...... even when.....
|
saturated;
maximal rate or transport; the drug concentration is increasing |
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Facilitated diffusion of a drug may be inhibited by other substances which.......
Inhibitors must bear ____ and ____ similarity to the normal drug substrate in order to bind to the carrier mechanism |
compete for binding sites on the carrier mechanism;
structural; stereoisomeric |
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|
Oral drugs are absorbed in the....
This is due to.... |
GI epithelial cell membrane barrier in the SI;
the large surface area available for drug contact |
|
|
Things that affect gastric emptying include: (2)
|
ingestion of large fluid volumes;
cholinergic agonists and prokinetic agents |
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|
Factors which decrease gastric emptying include: (4)
|
ingestion of solid food; alcohol; anticholinergics; high fat content meals
|
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|
During the process of drug absorption in the GIT, there are two potential sites of metabolism of a drug to occur: (2)
The the drug is metabolized in either of these areas, it is said to have undergone ______ metabolism In this case, the drug is actively _____ before it even reaches the systemic circulation |
gut wall and liver;
first-pass; metabolized |
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Drugs given orally must be given in very _____ doses compared to parenterally to achieve therapeutic effects because of the 1st pass effect
|
large
|
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Drugs may be given rectally if they can be liberated and absorbed in the lower parts of the rectum to avoid...
|
first-pass effect
|
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Percutaneous administartion has to pass through a _____ barrier.
Needs to penetrate through the stratum _____= rate limiting step |
thick epithelial;
corneum |
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|
Factors promoting percutanous absorption include (5):
|
large application area;
Damage to the stratum corneum; hydration/occlusive dressing; Application around hair follicles Dimethyl sulfoxide |
|
|
Drug sequestration occurs concentrating the drug in...
|
one or more tissues
|
|
|
If two or more drugs compete for plasma protein binding sites, the drug with the lower affinity will be..........
If this occurs, it may cause _____ effects due to...... |
dispelled from the binding sites;
toxic; its elevated free concentration in plasma (a displacement drug interaction) |
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|
There are no intracellular pores between the brain capillaries and endothelium membranes to the presence of ________ (occluding zonulae);
______ sheath also surrounds brain capillaries. This causes a severe...... |
tight junctions;
Astrocyte; limitation on movement of ionized or highly polar species of drugs |
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|
In order for drugs to gain access to the brain tissue from capillaries, drugs must diffuse across ________ (___ soluble, ___ form) or be....
|
endothelial cells;
lipid- non-ionized; transported by a carrier (as is glucose and amino acids) |
|
|
CSF-Brain barrier is composed of _____ cells lining the ventricles which are not connected by _____. These regions are very ___ allowing virtually.....
|
epithelial;
occluding zonulae; permeable; unrestricted passage of drugs from the CSF to the brain |
|
|
Drugs with very high values of Vd (volume of distribution) exhibit ______ tissue distribution; that is, the binding sites in tissue have a much ___ _ affinity for the drug than do the plasma protein binding sites.
|
extensive;
greater |
|
|
Drug distribution favors movement out of ____ and into the _____. Consequently, very ___ tissue concentrations and very ____ plasma concentrations are observed.
|
plasma; tissues;
high; low |
|
|
Chloroquine is sequestered in the ___ result in in extremely large vale for Vd. It is so tightly bound that its release is _____ and the half-life is greatly ______
|
liver;
slow; greatly |
|
|
Detoxification mechanisms are the...
|
chemical conversion of a toxic substance to a less toxic metabolite
|
|
|
Termination of drug action is the...
|
chemical conversion of a pharmacologically active drug to an inactive metabolite
|
|
|
The net effect of detoxification and termination of drug action is the conversion of a relatively ____-soluble drug molecule to a much more ____, ___-soluble drug metabolite which can readily be excreted.
|
lipid;
polar; water; |
|
|
Polar metabolites are (3 characteristics)
|
poorly reabsorbed from the renal tubules, secreted into renal tubules, more easily secreted in bile
|
|
|
Where in the liver does drug metabolism occur?
These cells contain ______ of the ____ system. |
smooth ER in hepatocytes;
drug-metabolizing enzymes; cytochrome P450 |
|
|
What are the 3 major sites of drug metabolism?
|
liver, gut wall/mucosal surfaces, plasma
|
|
|
Phase 1 of the biotransofmation of a drug is the....
This turns a ____, ____ substance into a ____ and ___ Substance; ___ by enzymes also occurs |
oxidation by the microsomal cytochrome P450 system;
non-polar, lipid soluble; polar, water soluble; hydrolysis |
|
|
The major function of the cytochrome P450 system is to...
|
add an oxygen atom to the drug substrate
|
|
|
Phase2 of biotransformation reactions occur in the ___ and ____. The transferase enzymes are found mostly in the ___.
____ occurs resulting in a metabolite that may actually be more ____-soluble than the parent drug. However, this metabolite undergoes further phase ___ reactions to finally yield the more ___ metabolites |
liver, gut wall;
cytosol; N-acetylation; lipid; 1; polar |
|
|
Glucuronide conjugates are virtually always ____, very ____, ______ and rapidly _____ by the kidney or into the bile.
|
inactive; very polar; ionized; excreted
|
|
|
In order for phase II reactions to occur, a site for ____ must be present in the substrate.
The original parent drug molecule may already contain this site (no phase 1 reaction needed) and a phase II reaction then occurs enabling the.... |
conjugation;
conjugated metabolite to be excreted |
|
|
What are the two conjugation reactions that occur during phase 2 of the biotransformation reactions?
|
glucuronide conjugation, N-acetylation
|
|
|
A phase I react may be used to introduce a ______ into a substrate which is then followed by...
|
conjugated site;
phase II |
|
|
Some drugs may be sufficiently polar in the parent drug form that neither phase I or phase II reactions are required for...
|
successful elimination by the kidney
|
|
|
Prodrugs are a .....
When administered, it needs to be _______ to an ____ form of the drug. |
chemical precursor form of a drug which is pharmacologically inactive;
metabolized; active |
|
|
Conversion of a prodrug to an active form takes place in.....
The reaction that usually accomplishes this activation is either a ______ or ______. |
SI, liver, plasma, or any other metabolizing tissue;
phase I activation; hydrolysis |
|
|
What is the most important excretory route for drugs?
|
kidney
|
|
|
Which form of a drug is filtered at the glomerulus?
|
free drug
|
|
|
Active tubular secretion of a drug occurs at the...
|
proximal tubule
|
|
|
Drugs which undergo extensive tubular secretion have greatly decreased ______.
There are separate carriers for ___ and ____. |
half-lives;
anions and cations |
|
|
Weak acids (____ and ____) exist in plasma mainly as the ____ form which are the substrates for the___ secretory transporters
|
penicillin, glucuronic conjugates;
ionized (anionic); anionic |
|
|
Weak bases (_____) are ____ in the plasma
|
cimetidine;
pronated |
|
|
Passive tubular reabsorption is the......
|
reabsorption of drugs form the PT occurring by passive diffusion
|
|
|
Driving force for passive reabsorption is the ____ between the drug in the glomerular filtrate (____) and drug in the blood (____)
|
concentration gradient;
higher; lower |
|
|
The lipid-soluble, non-ionized form of the drug is _____ during passive reabsorption. Therefore, the degree of reabsorption depends on both the _____ of the drug and ____ of tubular fluid
|
reabsorbed;
pKa; pH |
|
|
Bacteria in the intestinal tract may chemically alter _____ into.......
|
drug metabolites;
more lipid-soluble forms that can be reabsorbed across the gut wall into portal blood circulation |
|
|
If a substance is a polar metabolite (glucuronide conjugate of a drug), gut bacteria can _______ the polar metabolite which results in...
This is reabsorbed from the SI back into the mesenteric blood and is carried to.... This enterohepatic cycling may greatly.... |
deconjugate;
the regeneration of the more lipid-soluble parent subtance; the liver; prolong the drugs persistence in the body and increase the half life |
|
|
Total body clearance is constant over....
|
the range of plasma drug concentrations
|
|
|
Some drugs (phenytoin) exhibit ______ elimination. In this case, the total clearance is dependent on...
These drugs exhibit plasma conc profiles in which plasma concentration rises _______ in relation to the dosing increase resulting in a very ______ increase in plasma concentration compared to the very ____ increase in dose |
capacity-limited elimination;
plasma concentration; disproportionately; large; small |
|
|
Half-life is defined as...
|
the time required for the plasma concentration of a drug to decline by 50%
|
|
|
The half life is dependent on both___ and ___
|
Vd and total clearance
|
|
|
The vast majority of drugs exhibit first-order kinetics for which the half-life is ________ of dosage
|
independent
|
|
|
Time to achieve steady-state conditions during chronic dosing, for first order kinetic drugs, depends only on _____
|
the half life of the drug
|
|
|
For a single IV infusion, at the plateau of the rising drug concentration the rate of drug input from the constant-rate infusion exactly equals the rate of ________. This is referred to as the ______.
|
elimination of the drug;
steady=state |
|
|
The time to reach steady-state is independent of the _______ and depends only on the....
|
rate of infusion; drug half-life
|
|
|
The rate of infusion does determine the _____ of the steady-state concentration.
For drugs with 1st-rorder kinetics (so that total clearance remains constant) doubling the infusion rate with ____ the steady-state concentration |
values;
doubles |
|
|
Changing the infusion rate will change the steady-state concentration but it will always take ___ Drug half-lives to reach ___% of the new steady-state concentration
|
7; 99
|
|
|
Some time is required for therapeutic plasma levels to be reached after starting an infusion. If the levels are required immediately, an IV ______ may be given to achieve the desired concentration.
|
loading dose
|
|
|
For a single oral dose, the drug concentration rises to a peak value and during this absorption phase, the drug is being...
During this phase, some elimination through clearance mechanisms is taking place however.... |
absorbed from its site of application;
absorption greatly predominates causing the plasma levels to increase |
|
|
At the peak concentration of an oral dose, the rate of absorption ________ the rate of elimination;
After the peak concentration, the levels begin to _____. Some residual absorption may still be taking place; however..... |
exactly equals;
decline; elimination greatly predominates |
|
|
Multiple IV bolus dosing: The time to attain the steady-state depends only on the....... and the average steady-state plasma concentration depends only on the rate of...........for drugs with first-order kinetics for which total clearance remains constant
|
drug half-life;
drug input |
