Term
|
Definition
| Elimination rate (not constant) is directly proportional to the drug concentration in the plasma. This is considered a non-linear process. Mathematically platting concentration vs. time will give you a straight line. |
|
|
Term
|
Definition
| Elimination rate is independent of drug concentration in the plasma. A set amount of drug is eliminated at each interval. This is a linear process. |
|
|
Term
|
Definition
| Bind to and activate receptor to produce effect |
|
|
Term
|
Definition
| Bind to receptor and prevent termination of action (example: SSRIs prevent reuptake of serotonine thereby increasing concentration at synapse) |
|
|
Term
|
Definition
| Bind to and activate receptor to produce effect, but not a great response regardless of concentration |
|
|
Term
|
Definition
| A relationship between the quantity of a certain drug in the body to the concentration (C) of that same drug in the blood or plasma. May be in relation to blood, plasma, or water. Equation: Vd= Amount of drug in the body/C. A high volume of distribution means the drug did not stay in the vasculature but rather dispersed into the extravascular tissue. A low vd is defined when drugs are retained within the vascular space |
|
|
Term
|
Definition
Harm, injury, or unpleasant affect associated with taking medication of normal dose during normal use. Adverse drug reaction (ADR) can happen following a single dose or after prolonged use. It can also occur when using a combination of drugs. ADR is different from “side effect”. ADRs can be classified by 6 types: dose-related (Augmented), non-dose-related (Bizarre), dose-related and time-related (Chronic), time-related (Delayed), withdrawal (End of use), and failure of therapy (Failure) . Adverse effects can be local, or systemic.
Reference: www.ncbi.nlm.nih.gov/pubmed/11062960 |
|
|
Term
|
Definition
| Actions of the drug on the body, including pharmacologic effect and clinical response (effectiveness vs. toxicity). |
|
|
Term
|
Definition
| Governs the absorption, distribution, and elimination of drugs and are of great importance in the choice and administration of a particular drug for a particular patient. |
|
|
Term
|
Definition
| Bind to receptor and compete with and prevent other molecules from binding there.May be overcome by increased amounts of agonists. |
|
|
Term
|
Definition
| The fraction of unchanged drug reaching the systemic circulation after administration of the drug by any route. Example: Intravenous route 100% bioavailability |
|
|
Term
|
Definition
| ACE inhibitors:(second and third tremester) cause renal damage. |
|
|
Term
|
Definition
Any substance, agent, or process that interferes with normal prenatal
development, causing the formation of one or more developmental abnormalities of
the fetus. |
|
|
Term
|
Definition
| inhibitor that competes for receptor site and prevents binding to receptor site by other molecules |
|
|
Term
|
Definition
| Indicates time required to obtain 50'% steady state or to decay 50% from steady state conditions. Is dependent on volume of distribution and clearance. |
|
|
Term
|
Definition
| What the body does to a drug (absorption, distribution, metabolism and excretion of drug) |
|
|
Term
|
Definition
| is the unchanged drug reaching the systemic circulation following administrattin by any route |
|
|
Term
|
Definition
| absorbed across gut wall , portal blood delivers drug to liver, before systemic circulation |
|
|
Term
|
Definition
| The study of the actions of a drug on the body |
|
|
Term
| Adverse drug reaction (ADR) |
|
Definition
| A harmful or unintended responce from the patient after taking a drug. THe FDA estimates that 300,000 ADRs happen in hospitals each year as a result of confusing or insufficent informaion. ADRs are the fourth leading carese of death. This is higher than pulmonary disease, AIDS, accidents, and automobile deaths. |
|
|
Term
|
Definition
| Is a medication that: 1. results in a set of malformations to a fetus; 2. exerts its effects at a particular stage in fetal developement; and 3. is dose-dependent |
|
|
Term
| Some Examples of Teratogens |
|
Definition
| ACE Inhibitors: Renal Damage, Methotrextate: Multiple Congential Malformations and Warafrin: different toxic effects depending on the trimester |
|
|
Term
| Volume of Distribution (Vd) |
|
Definition
| V=(Amount of Drug in Body)/C Amount of space available to the drug. Concentration can relate to blood, plasma, or water (unbound drug). Think of plasma, red blood cells, and extravascular tissue as three separate "compartments" with each compartment being larger than the preceding compartment. Now think of a dose (500mg) and ask the question, how much of the dose is in each compartment? If most of the dose remains in the plasma the drug has a low Vd, if the dose has dispersed from the plasma into the RBCs it has a moderate Vd, and if most of the drug gets to the extravascular tissue it has a high Vd. |
|
|
Term
|
Definition
| Binds with a receptor to prevent a response or block an action of agonist molecules. May be structurally similar to the agonist and will bind to the receptor but will not elicit a reaction. |
|
|
Term
| Competitive-reversible antagonists |
|
Definition
| Compete with the endogenous agonist for binding sites. Increasing the concentration of the antagonist will progressively inhibit the agonist response. |
|
|
Term
| Non-competitive or irreversible antagonists |
|
Definition
| Binds to the receptor by either forming a covalent bond or so tightly that the receptor is unavailable for binding of the agonist. |
|
|
Term
|
Definition
| The rate of elimination is dependent on the drug concentration in the body and is not constant |
|
|
Term
|
Definition
| The rate of elimination is constant despite the amont of the drug in the body |
|
|
Term
|
Definition
| The time required to change the amount of drug in the body by half during elimination |
|
|
Term
|
Definition
|
|
Term
| Why is knowing half life useful? |
|
Definition
| It indicates the time required for a drug to attain or decay by 50% from steady state in a body, which is important in assessing how effective a drug regime is when needing to use multiple or ongoing drug dosages |
|
|
Term
|
Definition
| The rate and extent to which a drug is absorbed and becomes available in the general circulation. |
|
|
Term
|
Definition
| The study of biochemicals and physiologic effects of drugs and their mechanisms of action. The actions of the drug on the body. |
|
|
Term
|
Definition
| drug that binds to and activate a receptor to bring about effect |
|
|
Term
|
Definition
| blocks the molecule that terminates the agonist(essentially it slows the 'death' of the agonist thus prolonging its effect) |
|
|
Term
|
Definition
| Agonists that cause almost or all of the receptor pool to become activated |
|
|
Term
|
Definition
| Agonists that bind with sites in receptor pool but do not evoke as much of a response as a full agonist, no matter how high the concentration |
|
|
Term
|
Definition
| Agonists that binds to the receptor site to render it 'inactive' (similar to antagonist only instead of blocking the receptor site from agonists- like an antagonist does, it binds to the agonist receptor sites and renders the receptor inactive) |
|
|
Term
|
Definition
| bind to receptors but do not activate generation of a signal. |
|
|
Term
|
Definition
| drug that binds to a receptor, competing with and preventing binding by other molecules. |
|
|
Term
|
Definition
| the presence of the antagonist at the receptor site blocking the access of the agonist to the receptor and preventing the usual agonist effect. |
|
|
Term
|
Definition
| in the presence of fixed concentration of agonist, increasing concentrations of a reversible competitive antagonist progressively will inhibit the agonist response; high antagonist concentrations prevent response completely. |
|
|
Term
|
Definition
| causes a downward shift of the maximum, with no shift of the curve on the dose axis unless spare receptors are present, therefore the receptor is unavailable for binding of agonist. |
|
|
Term
|
Definition
| a harmful or unintended response to a drug. Fourth leading cause of death in the United States. |
|
|
Term
|
Definition
| Non-linear process. The rate of elimination is not constant, but dependent on drug concentration. A constant fraction of the drug is eliminated by its first half-life, no matter what the dose. The rate of metabolism of most drugs follows the rule of first order kinetics and is independent of the dose. |
|
|
Term
|
Definition
| Linear process. The rate of drug elimination is constant, or proceeds at a rate that is independent of concentration. |
|
|
Term
|
Definition
| The substance or process 1) results in a typical and unique set of malformations (showing selection for a certain group of target organs and 2) creates an effect at a specific stage of fetal development |
|
|
Term
|
Definition
| Most Common: "Statins" or HMGCoA reductase inhibitors (ex: simvastatin); ACE inhibitors (ex: enalapril); Quinolones (ex: ciprofloxacin); amphetamines; tricyclic antidepressants (amitriptyline). Table 59-1, pp. 1042-1043 for more examples. |
|
|
Term
|
Definition
| The time required to change the amount of drug in the body to one half during elimination. Half lives indicate time reqauired to reach 50% steady state or 50% decay. A 50% steady state(or decay state) concentration is reached at one half-live, 75% after 2, and 90% after 4. T1/2 = (0.7 x volume) / clearance |
|
|
Term
| Volume of Distribution (Vd) |
|
Definition
| The measurement of the apparent space in the body available to contain the drug. It relates to the amount of drug in the body (space) to the concentration of the drug in blood or plasma. Can be expressed at the equation V= amount of drug in the body/concentration of the drug. The Vd may related to blood, plasma or water. A high Vd = the drug did not stay in the bloodstream but floated out to the extravascular spaces. When there is a low Vd the drug remains in the blood stream and not in the extravascular tissue. |
|
|
Term
|
Definition
| A reduction in the bioavailability of a drug that occurs as it passes through the liver and is partially metabolized before being able to exert its' effect on the systemic circulation |
|
|
Term
|
Definition
| The study of how the body acts on a drug. Primarily concerns the absorption, distribution, and elimination of a drug. Physiologic and pathologic processes create variance among individuals. |
|
|
Term
| Pharmacodynamics definition |
|
Definition
| The study of the actions of a drug on the body |
|
|
Term
| 4 components of pharmacodynamics |
|
Definition
| 1) pharmacologic effect, 2) clinical response, 3) toxicity, 4) efficacy |
|
|
Term
|
Definition
| mechanism of action (MOA) of the drug |
|
|
Term
|
Definition
| Measurement of treatment, how well the MOA caused the desired response, what the patient feels |
|
|
Term
|
Definition
| Unwanted effects of a drug (sometimes extensions of pharmacologic response) |
|
|
Term
|
Definition
| How well a drug does its job |
|
|
Term
| 4 influences on pharmacodynamics (variations in drug responsiveness): |
|
Definition
| 1) alterations in drug reaching receptors, 2) variations in concentration of endogenous ligands, 3) alterations in number & function of receptors, 4) changes in components of responses distal to the receptor |
|
|
Term
|
Definition
| Amount of drug needed to produce a given effect |
|
|
Term
|
Definition
| Effective dose for 50% - the median dose for which the population has responded |
|
|
Term
|
Definition
| Lethal dose for 50% - the median dose for which the population has died |
|
|
Term
|
Definition
| Ratio of the ED50 (median effective dose- desired effect) to the TD50 (median toxic dose- undesired effect) |
|
|
Term
|
Definition
| The rate of elimination of a drug is dependent on the drug's plasma concentration (non-linear elimination rate) |
|
|
Term
|
Definition
| The rate of drug elimination is constant over time (linear elimination) and is not related to the drug's concentration |
|
|
Term
|
Definition
| Drugs that bind or activate a receptor to directly or indirectly bring about an effect |
|
|
Term
|
Definition
| Full, partial, indirect, and inverse |
|
|
Term
|
Definition
| Bind to a receptor and elicit the maximum response |
|
|
Term
|
Definition
| Bind to a receptor but elicit a lower response at full receptor capacity |
|
|
Term
|
Definition
| Inhibit molecules responsible for the termination of an endogenous agonist |
|
|
Term
|
Definition
| Bind to a receptor but induces an opposite pharmacological effect of an agonist by reversing constitutive activity of receptors; decreases activated receptor (Ra) activity below its basal level |
|
|
Term
|
Definition
| The actions of the body on the drug that govern the absorption, distribution, and elimination of drugs. Are of great importance when deciding to administer a specific medication to a specific patient population. |
|
|
Term
|
Definition
| The movement of a substance, or drug, into various compartments. This can be achieved through aqueous diffusion, liquid diffusion, special carriers, endocytosis, and exocytosis. |
|
|
Term
|
Definition
| Means half life-The time the body takes to eliminate half the drug |
|
|
Term
|
Definition
|
|
Term
|
Definition
| The passive flux of molecules down a concentration gradient. |
|
|
Term
| Henderson-Hasselbach Equation |
|
Definition
| Used to calulate the ionization of weak acids and weak bases. |
|
|
Term
| Delirium, GI bleeding, falls, fractures |
|
Definition
| Examples of adverse drug reactions (ADEs) |
|
|
Term
| Adverse Drug Reactions (ADEs) |
|
Definition
| A harmful or unintended response to a drug |
|
|
Term
|
Definition
| A guideline used to identify medications whose risk outweigh their benefits in geriatric populations |
|
|
Term
|
Definition
| The fraction, the amount of a drug that goes to the systemic circulation unchanged after administration, by any route, whether, oral, IM, IV, suppository, etc. |
|
|
Term
|
Definition
| First Pass Hepatic Elimination equation: ER=CLliver/Q The passage of the drug through the gut wall and its subsequent metabolism in the liver or portal blood, CYP3A4 enzyme system in the gut wall, or its excretion into the bile, before it is delivered into the systemic circulation. |
|
|
Term
| FDA teratogenic risk category A |
|
Definition
| Controlled studies in women fail to demonstrate a risk to the fetus in the first trimester(and there is no evidence of a risk in late trimesters), and the possibility of fetal harm appears remote |
|
|
Term
| FDA teratogenic risk category B |
|
Definition
| Either animal-reproduction studies have not demonstrated a fetal risk, but there are no controlled studies in pregnant women, or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the first trimester (and there is no evidence of a risk in later trimesters) |
|
|
Term
| FDA teratogenic risk category C |
|
Definition
| Either studies in animals have revealed adverse effects on the fetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus |
|
|
Term
| FDA teratogenic risk category D |
|
Definition
| There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk |
|
|
Term
| FDA teratogenic risk category X |
|
Definition
| Studies in animals or human beings have demonstrated fetal abnormalities or there is evidence of fetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant |
|
|
Term
| Pharmacokinetic Changes in relation to Absorption in geriatrics- |
|
Definition
| Little evidence of any major alteration in drug absorption with age. Conditions associated with age may alter-such as altered nutritional habits, greater consumption of nonprescription drugs, and slower gastric emptying |
|
|
Term
| Pharmacokinetic Changes in relation to Distribution in geriatrics |
|
Definition
| Reduced lean body mass, reduced body water and increased fat. Decrease in serum albumin, which binds many drugs, especially weak acids. |
|
|
Term
| Pharmacokinetic Changes in relation to Metabolism in geriatrics |
|
Definition
| Certain drugs are metabolized more slowly. Heart failure may dramatically alter the ability of the liver to metabolize drugs by reducing hepatic blood flow. |
|
|
Term
| Pharmacokinetic Changes in relation to Elimination in geriatrics |
|
Definition
| Age related decline of renal capacity. Marked prolongation of the half-life of many drugs, and the possibility of accumulation to toxic levels if dosage is not reduced in size or frequency |
|
|
Term
|
Definition
| A substance that is harmful to an embryo and fetus resulting in fetal malformation or negatively affecting fetal development |
|
|
Term
|
Definition
| ACE Inhibitors, Warfarin, Thalidomide, Valproic Acid, Methotrexate, Lithium, Cytarabine, Carbamazepine, Busulfan, Selective Serotonin Reuptake Inhibitors (SSRIs), Trimethadione, Phencyclidine, Phenytoin, Alcohol, Tetracycline, Aminoglycosides |
|
|
Term
|
Definition
| Group of closely related compounds characterized by a macrocyclic lactone ring to which deoxy sugars are attached. |
|
|
Term
|
Definition
| Erythromycin, clarithromycin, azithromycin, ketolides |
|
|
Term
|
Definition
| Inhibit DNA gyrase to block bacterial DNA synthesis. This enzyme is used to coil/uncoil DNA during replication. Gram negative (older generation) and gram positive (newer generation) coverage. Excellent absorption and tissue penetration. Adjust for impaired renal function. Resistance is of concern. |
|
|
Term
|
Definition
| Levofloxacin, Moxifloxacin,ciprofloxacin |
|
|
Term
| QUINOLONES ADVERSE REACTIONS |
|
Definition
Well tolerated, some ADRs include NVD, h/a, dizziness, tendonitis. Not recommended
in children under 18 y/o (may damage cartilage). QT prolongation. |
|
|
Term
|
Definition
| Enzymes bacteria develop to lyse the beta lactam ring which deactivates the molecules antibiotic properties. This leaves penicillins and cephalosporins ineffective. |
|
|
Term
|
Definition
| Sulfonamides are are synthetic bacteriostatic antibiotics that inhibit folate synthesis. Humans have to acquire folate, but bacteria synthesize their own. Sulfamethoxazole (SMZ) may be combined with another sulfonamide called trimethoprim (TMP). Together these work to block different steps in the process of folate synthesis. For example, using sulfamethoxazole together with trimethoprim creates a synergistic effect because of where each drug inhibits folate synthesis. The synergist effect makes sure the bacteria isn't able to replicate and therefore the drugs do their job effectively. Pharmacokinetics: SMZ/TMP can be given orally or IV. Both drugs have a similar half-life and are well absorbed in the gut and the distribution into the body fluid and tissue is wide. It also penetrates the CSF. SMZ/TMP are indicated for a broad spectrum of gram-positive and many gram-negative bacteria. They are given orally to treat a variety of infections such as UTIs, P jiroveci pneumonia, salmonella, prostatitis. They are even able to fight Staph-aureus (MRSA). These drugs are excreted by the kidneys. ADRs include: NV, fever, rash, photosensitivity, diarrhea, and for those patients with inflammatory bowel dz they may have folate deficiencys, |
|
|
Term
|
Definition
| Inhibits bacterial cell wall sysnthesis. Only bactericidal against Gram + bacteria. Not absorbed well PO, must be given IV for systemic infecitons. Can be given PO for colitis infections from C. diff...but Flagyl (Metronidazole) is much better for that. 10% of patients develop an ADR from Vanco: Red neck syndrome, ototoxicity, and phlebitis common. Excreted by the kidneys |
|
|
Term
|
Definition
| GRAM NEGATIVE (bactericidal).Mostly used in combination with B-lactam atb in gran negative bacteria, in combination with Vancomicyn or B-lactam for gram-positive endocarditis and TB.They are water soluble and more active in alkaline PH. must be given IM/IV for systemic infections. Normal 1/2 life in serum; 2-3 hrs. Excreted by kidneys.Adverse effects: ototoxic and nephrotoxic (with incorrect dosing) |
|
|
Term
|
Definition
| Beta Lactam antibiotic with mostly gram + spectrum. Bacteriocidal drugs that act by inhibiting cell wall synthesis. Prototype drug is penicillin VK. ADRs include allergic reactions, GI upset, and risk for seizures in pt.s with renal failure. |
|
|
Term
| Antistaphylococcal penicillin |
|
Definition
| Prototype is Nafcillin. Targets staph- and strep- but not gram - bacteria. |
|
|
Term
|
Definition
| Targets gram + and some gram - bacteria. Drugs include Ampicillin and Amoxicillin |
|
|
Term
| Extended spectrum Penicillin |
|
Definition
| Increased activity against gram - bacteria. Drugs include Ticarcillin and Piperacillin. Can be combined with beta lactamase inhibitors such as clavulanic acid and sulbactam to broaden their spectrum |
|
|
Term
|
Definition
| Broad spectrum, bacteriostatic, inhibit protein synthesis, enter the organism through passive diffusion and active transport, attach reversibly to ribosome. |
|
|
Term
|
Definition
| impaired influx or increased efflux, inability to bind to ribosome r/t creation of proteins that interfere and enzymatic inactivation |
|
|
Term
| Tetracyclines Adverse reactions |
|
Definition
| Otic- tinitus. Can cause photosensitivity.No use in preganacy or peds- attches to ca+ and deposits in teeth of child. Watch closely with impaired renal and heaptic function, GI-N,V,D, take with food, destroys usual flora of GI, candidiasis. |
|
|
Term
|
Definition
| H. pylori, Gram + and Gram -, chlamydia, Lyme, Bronchitis, Community aquired pneumonia, MRSA,Acne |
|
|
Term
| Kinetics of tetracyclines |
|
Definition
| 60-70% absorbed, food helps with GI upset but impairs absorption, excreted in urine ans feces. Short, medium and long serum half lives. |
|
|
Term
|
Definition
| More stable than penicillin to many bacterial B lactamases resulting in a broader spectrum. Many compounds divided into four groups/generations that depend of spectrum of antimicrobial activity. |
|
|
Term
| First generation cephalosporin |
|
Definition
| Narrow spectrum, active against gram-positive cocci, minimal activity against gram-negative cocci, enterococci, and MRSA. Cephalexin is the prototype. Example: Cefazolin |
|
|
Term
| Second generation cephalosporin |
|
Definition
| Wider spectrum, less gram-positive coverage and added gram-negative coverage. No CNS entry. Active against H. influenzae. Example: Cefoxitin |
|
|
Term
| Third generation cephalosporin |
|
Definition
| Even wider spectrum, more coverage of gram-negative bacteria. Yes CNS entry. Used for serious infections where other drugs were resistant. Not enterobacter infections. Example: Cefixime, Ceftriaxone |
|
|
Term
| Fourth generation cephalosporin |
|
Definition
| Used in treatment of enterobacter infections and still under investigation on role in treating resistant strains. Example: Cefepime |
|
|
Term
|
Definition
| Inhibition of protein synthesis. |
|
|
Term
|
Definition
| Mutation of receptor site, modification of receptor by a constitutively expressed methylase, enzymatic inactivation |
|
|
Term
| Clindamycin Clinical uses. |
|
Definition
treatment of skin and soft tissue infections caused by streptococci and staphylococci..
Anaerobic infections caused by Bacteroids.
Endocarditis prophylaxis in dental work |
|
|
Term
| Clindamycin adverse effects |
|
Definition
| Diarrhea, nausea, rash, impaired liver function, neutropenia, c-difficile. |
|
|
Term
|
Definition
| Competitive inhibitor of the beta lactam enzyme. EX:clavulanic acid,sulbactam, tozabactam |
|
|
Term
|
Definition
| MOA: irreversible inhibitor of protein synthesis; binds at the 30s ribosomal subunit. Works mostly against gram negative bacteria and works better when paired with beta-lactams. Only given IV. Side effects include: hearing loss and renal failure when the trough concentration is greater than 2. Examples include: Gentamicin and Tobramycin |
|
|
Term
|
Definition
| An enzyme produced by bacteria that serves as a mechanism of resistance against antibiotics |
|
|
Term
|
Definition
| A class of beta lactam antibiotics similar to penicillin but more stable and broad spectrum, a product from the fungus Cephalosporium Acremoniun. Generally distributes to lungs, kidneys, urine, synovial, pleural, and pericardial fluids and primary elimination occurs through kidneys except nafcillin. Avoid in patients with anaphylaxis to penicillin, can cross fetal barriers, breast milk, and should not be used with calium meds, heparin, and lactated ringers. Monitor patients with renal failure for toxicity. |
|
|
Term
| First Generation Cephalosporin |
|
Definition
| Active against - gram positive cocci; e.g. staph, pneumonia, UTI's, strep, cellulitis, & surgical prophylaxis; e.g. Ancef, Kefzol, Keflex. Activiity minimal for gram-negative cocci, enterococci, and MRSA. |
|
|
Term
| Second Generation Cephalosporin |
|
Definition
| Stronger than first generation, Activity against- gram negative enterobactor, pseudomonas, & salmonella. Without CNS there is poor gram-positive coverage. Treats sinusitis, otitis media, lower respiratory, diverticulitis, peritonits, & PID. Cefuroxime can cross blood brain barrier and treats meningitis; e.g. Cefzil, Cechlor, Lorabid |
|
|
Term
| Third Generation Cephalosporin |
|
Definition
| Stronger, broader spectrum gram-negative bacteria such as E-coli, gonorrhea; less side effects, higher absorption & distribution, can penetrate CNS & blood brain barrier. Treats serious infections, hospital acquired infections, sepsis, pneumonia, bacterial meningitis; e.g. Omnicef, Rochephin, Suprax. |
|
|
Term
| Fourth Generation Cephalosporin |
|
Definition
| Broader spectrum than third generation with activity against gram-positive organisms the similar to first generation and strong activity against gram-negative agents such as strepococci, hospital acquired infections; e.g. Cefepime |
|
|
Term
|
Definition
| MOA: Action may be inhibitory or bactericidal, particularly at higher concentrations. Inhibition of protein synthesis occuring via binding to the 50S ribosomal RNA. Works against some Gram + and Gram - organisms. |
|
|
Term
|
Definition
| Commonly used to treat community aquired pneumonia, Chlamydiae infections, and useful as a penecillin substitute in a patient with Penecillin allergies. |
|
|
Term
| Macrolides Adverse Reactions |
|
Definition
| Adverse Reactions: Anorexia, nausea, vomiting, diarrhea. Because metabolites inhibit P450 enzymes which in turn can increase the serum concentrations of many drugs including warfarin, methylprednisolone, and digoxin. Examples include: Erythromycin, clarithromycin, azithromycin. |
|
|
Term
| Sulfamethoxazole/ Trimethoprim (SMZ/TMP) MOA |
|
Definition
| A combination of sulfonamide and trimethoprim blocks the sequential steps in folate synthesis. Blocking folate synthesis prevents DNA synthesis so bacteria is not able to reproduce. |
|
|
Term
| Sulfamethoxazole/ Trimethoprim SMZ/TMP Adverse Effects |
|
Definition
| Nausea and vomiting, drug fever, vasculitis, renal damage, and CNS disturbances can occur. precipitation of drug in urine(pt need to remain well hydrated) |
|
|
Term
|
Definition
| Vancomycin inhibits cell wall synthesis but it is NOT a beta lactam. Only active against gram+ bacteria and Flavobacterium. |
|
|
Term
| Vancomycin Pharmacokinetics |
|
Definition
| Poor intestinal absorption so usually given by IV. Only given orally for antibiotic-associated colitis r/t C. dificile. |
|
|
Term
|
Definition
| Broad spectrum bacteriostatic antibiotics that inhibit protein synthesis acting at the 30 S ribosomal unit. Active against many gram-positive and gram-negative bacteria, including anaerobes, rickettsiae, chlamydiae, mycoplasmas and some protoza. |
|
|
Term
| Tetracyclines Clinical Use |
|
Definition
| Drug of choice for infections caused by rickettsiae. Also excellent drugs for the treatment of Mycoplasma pneumonia, chlamdiae, and some spirochetes. Used in some regimens for the treatment of H pylori. Used in acne and lymes disease. |
|
|
Term
| Tetracyclines Pharmokinetics |
|
Definition
1.Widely distributed to tissues and body fluids execept cerebrospinal fluid
2.Tigecycline is poorly absorbed orally and must be intravenously
3.Absorption after oral administration is approx. 60-70% for tetracycline with 95-100% absorption for doxycycline and minocycline |
|
|
Term
| Tetracycline Mechanisms of resistance |
|
Definition
1. impaired influx or increased efflux by an active transportan protein pump
2. ribosome protection due to production of proteins that interfere with tetracycline binding to the ribosome
3. enzymatic inactivation |
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Term
| Tetracycline Adverse Reactions |
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Definition
| Tetracyclines are readily bound to calcium deposited in newly formed bone or teeth in young children therefore it is contraindicated in pregancy and in small children. Nausea/vomiting/diarrhea. Vestibular reactions. Photosensitivity. Can impair hepatic function. |
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Term
| Quinolones: Mechanism of Action |
|
Definition
Inhibits DNA replication by binding to topoisomerace II (DNA gyrase)
and topoisomerase IV |
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Term
| (Fluoro)quinolones: Pharmacokinetics |
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Definition
*High bioavailability (80-95%)
*Distributed widely in body fluids and tissues
*Serum half-lives of 3-10 hours
*Oral absorption impaired by antacids (take 2hrs before or 4hrs after)
*Eliminated by renal mechanisms; need dosage adjustment for CrCl <50mL/min
*IV serum concentrations similar to PO |
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Term
|
Definition
Generally well-tolerated
Common: nausea, vomiting, diarrhea
Occasionally headache, dizziness, rash, insomnia, elevated LFTs occur |
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Term
| (Fluoro)quinolones: Clinical Use and Examples |
|
Definition
Active against gram(+) and gram(-) bacteria. Treat UTIs, bacterial diarrhea, infections of soft tissues/bones/joints, intra-abdominal and respiratory tract infections.
Fluoroquinolone examples: Ciprofloxacin, Levofloxacin, Moxifloxacin
Quinolone example: Nadalixic acid |
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Term
|
Definition
| beta lactam compound with a four membered lactam ring |
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Term
|
Definition
| 1) Penicillins 2) Antistaphylococcal PCN 3) extended spectrum PCN |
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Term
|
Definition
| example) PCN G- has the greatest activity against gram + orgs and gram - cocci and non beta lactamase producing anaerobes, little activity against gram - rods |
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Term
|
Definition
| example)nafcillin-resistant to staphy. B-lactamases, active against staph and strep., not enterococci, anaerobic bacteria, or gram - cocci and rods |
|
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Term
|
Definition
| example)ampicillin and antipseudomonal PCN- have the same antibacterial spectrum of PCN and have better activity against gram - orgs |
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Term
|
Definition
| inhibits bacterial growth by interfering with the transpeptidation reaction of bacterial cell wall synthesis so cells become damaged and die |
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Term
|
Definition
| most are due to hypersensitivity |
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Term
|
Definition
| Most Penicillins are rapidly excreted by the kidneys and need adjusted does according to kidney function, absorption of most oral penicliins except amoxicillin cannot be taken with food, 1-2 hours before or after meals is advised |
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Term
| Quinolone (fluoroquinolones- main class) *definition/MOA* |
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Definition
| Antibacterial antibiotics that block bacterial synthesis (block bacterial DNA gyrase & topisomerase enzymes from unwinding & replicating) |
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Term
|
Definition
| kills gram(-) aerobic bacteria (excellent at this), not as effective against gram(+) bacteria. HIGH Bioavailability (80-95%). |
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Term
|
Definition
-Generally well tolerated.
-Nausea, Vomiting, Diarrhea.
-May damage cartilage & cause arthropathy.
-Not recommended for <18yrs old |
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|
Term
| Quinolone *examples of drug* |
|
Definition
-Ciprofloxacin (most well known/effective)
-levofloxacin |
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|
Term
|
Definition
GOOD against Staph Aureus (though not good/resistant to MRSA).
BAD: bacteria can quickly become resistant to quinolones. |
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Term
|
Definition
| Enzymes produced by some bacteria that inactivate beta-lactam antibiotics by lyses of the beta-lactam ring. Reside in the periplasmic space or on the outer surface of the cytoplasmic membrane, where they destroy beta-lactam antibiotics that penetrate the outer membrane. |
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Term
|
Definition
| Is the most common mechanism of resistance to penicillins and other beta-lactams. |
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Term
| Beta-lactamase inhibitors |
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Definition
| Potent inhibitors of many but not all bacterial ß-lactamases and can protect hydrolyzable penicillins from inactivation by these enzymes. |
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|
Term
| SMZ/TMP Sulfonamides/Trimethoprim MOA |
|
Definition
| Synthergystic action blocks folic acid synthesis inhibiting cell from making purines required for DNA |
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Term
|
Definition
| Hypersensitivity, skin rashes, urine precipitation. Need to stay well hydrated. Most allergenic antibiotic. |
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|
Term
|
Definition
|
|
Term
|
Definition
| Provides coverage for gram negative, gram positive, chlamydiae, some protozoa |
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|
Term
| Drugs that fight gram NEGATIVE bacteria |
|
Definition
-Monobactram (ie: aztreonam)
-Fluoroquinilones (1st gen best- ie: ciprofloxacin)
-Aminogylcosides (ie: gentamycin) |
|
|
Term
| Drugs that fight gram POSITIVE bacteria |
|
Definition
-Penicillins (ie: amoxicillin)
-Cephalosporins (1st gen best ie: cephalexin)
-Glycopeptide- (ie: vancomycin) |
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Term
|
Definition
| Same as penicillin (prevent bacterial growth by preventing cell wall production) but more stable with a broader spectrum of activity |
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|
Term
| 1st generation Cephalosporin |
|
Definition
| narrow: Active against gram + cocci, minimal against gram -, penetrates soft tissue = surgical prophylaxis drug of choice (Cefazolin) tx: UTI, cellulitis, soft tissue abcess |
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|
Term
| 2nd generation cephalosporin |
|
Definition
| Wider: Active grainst same gram + cocci, but better gram - coverage. Tx: sinusitis, otitis, lower resp. tract infection, PID, CAP, diverticulitis |
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Term
| 3rd generation cephalosporin |
|
Definition
| Better against gram - cocci than 2nd. Able enter CSF = cross BBB. Reserved for serious infections, ex: menigitis. |
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Term
| 4th generation cephalosporin |
|
Definition
| Cefepime. Good activity against most penicillin-non-susceptible strains of streptococci. Use to treat enterbacter infections. Can penetrate the CSF. |
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|
Term
| Cephalosporin adverse effects and considerations |
|
Definition
| Most adverse rxn are hypersensitivity. Adjusted doses for renal failure patients. CNS toxicity including seizure were found in high doses and pt with CRF. Less than 10% of pt with an true penicillin allergy react to cephalosproins. |
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Term
|
Definition
| IRREVERSIBLE inhibition of protein synthesis at the ribosomal level (30s ribosomal subunits) |
|
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Term
|
Definition
| Mostly Gram NEGative bacteria with some outliers (pseudomonas, proteus, enterobacter, klebsiella |
|
|
Term
| Aminoglycoside Adverse Drug Reactions |
|
Definition
| Mostly dose related with a trough concentration of >2 and include: nephrotoxicity and ototoxicity (vestibular or sensory depending on drug) |
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|
Term
| Aminoglycoside Resistance Mechanisms from Bacteria |
|
Definition
1) Bacterial enzyme inactivation
2) Imparied entry INTO the cell
3) Bacterial receptor alteration |
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|
Term
| Aminoglycoside Pharmacokinetics |
|
Definition
Absorption: NO ORAL absorption so all IV administration
Distribution: One compartment model
Excretion: Kidney and is renal dependent so renal function is very important and serum concentrations must be checked
Other: Concentration dependent killing; post antibiotic effect; often single daily doses are effective |
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|
Term
| Aminoglycoside clinical Uses |
|
Definition
| Mostly against Gram- NEG but most always used with Beta-lactam antibiotic to extent coverage to gram positives. Some common clinical uses include: sepsis by aerobic gram negative bacteria; endocarditis caused by streptococci, staphylococci or enterococci |
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|
Term
|
Definition
| block bacteria DNA synthesis by blocking the enzyme DNA gyrase (topoisomerase II) |
|
|
Term
|
Definition
| excellent absorption and tissue penetration,eliminated by the kidneys |
|
|
Term
| quinolones: adverse reactions |
|
Definition
| N/V/D (most common), dizziness, HA, insomnia, prolonged QT.tendon rupture Not recommended under age 18 |
|
|
Term
| Clindamycin spectrum of coverage |
|
Definition
| Has good gram + coverage but is used mostly for anaerobic infections |
|
|
Term
| Clindamycin Adverse Effects |
|
Definition
| Common adverse effects include diarrhea, nausea, and skin rashes. Clindamycin has been associated with pseudomembranous colitis d/t C. difficile. |
|
|
Term
| Clindamycin Resistance 3 Mechanisms |
|
Definition
| 1. Mutation of the ribosomal receptor site 2. Modification of the receptor by a constitutively expressed methylase 3. Enzymatic inactivation of clindamycin |
|
|
Term
| Penicillins share this unique chemical component w/ cephalosporins, monobactams, carbapenems & beta lactamase inhibitors |
|
Definition
|
|
Term
| Penicillins - inhibition or death of cell? |
|
Definition
| Bacteriocidal to actively growing cells |
|
|
Term
|
Definition
| Interferes w/ cell wall synthesis by binding to PBPs in the peptidoglycan cell wall & prevents cross-linking, which leads to cell wall holes and rupture. |
|
|
Term
| Penicillins- class of Antibiotics |
|
Definition
|
|
Term
| Antibiotic classes that inhibit the synthesis of DNA |
|
Definition
| fluoroquinolones, trimethoprim, sulfonamides |
|
|
Term
| Antibiotic classes that inhibit the synthesis of cell wall |
|
Definition
| Beta-lactams (penicillins, cephalosporins, carbapenems, monobactams), Non-beta-lactams (vancomycin, cycloserin, bacitracin, fosfomycin) |
|
|
Term
| Antibiotic classes that bind to the 50S ribosomal subunit |
|
Definition
| Chloramphenicol, clindamycin, macrolides |
|
|
Term
| Antibiotic classes that bind to the 30S ribosomal subunit |
|
Definition
| tetracyclines, aminoglycosides |
|
|
Term
|
Definition
|
|
Term
| Beta-lactamase ( β- lactamase) |
|
Definition
| An enzyme produced by bacteria that lyses the β-lactam ring in the structure of penicillins, cephalosporins, and other β-lactam antibiotics thereby inactivating the antibiotic. |
|
|
Term
| The most common mechanism of bacterial resistance. |
|
Definition
| Beta-lactamase production. (Hundreds of different β- lactamases have been identified). |
|
|
Term
| Beta-lactamase Inhibitors: |
|
Definition
Clavulanic acid
Sulbactam
Tazobactam |
|
|
Term
|
Definition
| A group of closely related compounds characterized by a macrocyclic lactone ring to which deoxy sugars are attached. |
|
|
Term
|
Definition
| Erythromyocin, Clarithromycin, Azithromycin, Ketolides |
|
|
Term
| Beta-lactamase Inhibitors: MOA |
|
Definition
| Inhibits beta-lactamase activity by competitively binding to the enzyme. These drugs always work in conjuction with β-lactam penicillin antibiotics to make them more effective. |
|
|
Term
|
Definition
| Binds to ribosomal subunits of susceptible bacteria and suppresses protein synthesis. |
|
|
Term
| Erythromyocin Common Uses |
|
Definition
| Mild to moderate respiratory tract infections, skin & soft-tissue infections caused by Bordetella pertussis, community-acquired pneumonia, Chlamydia trachomatis, and Streptococcus pneumoniae |
|
|
Term
| Erythromyocin Contradindications |
|
Definition
| preexisting hepatic disease, hypersensitivity |
|
|
Term
|
Definition
| Binds to ribosomal subunits of susceptible bacteria and suppresses protein synthesis. |
|
|
Term
|
Definition
| Mild to moderate infections of the upper and lower respiratory tract, uncomplicated skin and skin-strucutre infections caused by streptococcus pneumonia, complex infections in AIDS patients |
|
|
Term
| Clarithromycin Side Effects |
|
Definition
| nausea, vomitting, diarrhea, hepatotoxicity, abdominal pain, vaginitis, leukopenia, rash, uticaria, pruritis, Stevens-Johnson syndrome, headache |
|
|
Term
|
Definition
| Binds to ribosomal subunits of susceptible bacteria and suppresses protein synthesis; much greater spectrum of activity than erythromycin; more effective against gram (-) organisms |
|
|
Term
|
Definition
| 1.) Reduced permeability of the cell membrane or active efflux. 2.) Production of esterase that hydrolyze macrolides. 3.) Modification of the ribosomal binding site by chromosomal mutation or by macrolide-inducible or constitutive methylase. |
|
|
Term
|
Definition
| Inhibits cell wall synthesis by binding to the D-Ala-D-Ala terminus of nascent peptidoglycan. This inhibits the transglycosylase, preventing fruther elongation of peptidoglycan and cross-linking. The peptidoglycan is thus weakened and the cell becomes susceptible to lysis. |
|
|
Term
|
Definition
| Used for infections caused by gram positive bacteria including sepsis, endocarditis, and meningitis. Also C difficile colitis - oral formulation. 1st choice drug for gram-positive cocci Methicillin-resistant. |
|
|
Term
| Vancomycin contraindications/precautions |
|
Definition
| Is poorly absorbed from the intestinal tract and is administered orally only for the treatment of antibiotic-associated colitis caused by C difficile. |
|
|
Term
| Vancomycin pharmocokinetics |
|
Definition
| Oral-NO SYSTEMIC ABSORPTION, IV administration. Renal clearance half-life 6 hours. |
|
|
Term
|
Definition
| In combination with gentamicin is an alternative treatment of enterococcal endocarditis in a patient with serious penicillin allergy |
|
|
Term
| Vancomycin considerations |
|
Definition
| 90% of the drug is excreted by glomerular filtration. The dosage is reduced accordingly in patients with renal insufficiency. |
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