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Define Cidal Activity:
Irreversible loss of ability to reproduce
What is the term for irreversible loss of ability to reproduce?
Activity is described as quantitively or qualitatively?
What three names are assigned to each antimicrobial?
Ampicillin is a Chemical, trade or generic name?
Ominipen, Principen and Amcillin are trade, generic or chemical names?
What is the generic name for Ominipen, Principen and Amcillin?
What are the two general modes of application for Antimicrobial agents?
Topic and Systemic are two divisions of what antimicrobial characteristic?
Mode of Application
What types of Systemic modes of application were discussed in class?
Oral, Parenteral and Rectal are what general type of application mode?
What seven general areas of action in the cell are common in antimicrobials?
- 50s subunit
- 30s subunit
- Cell membrane
- Cell wall
- What action of microbial drugs is commonly taken against the Ribosome?
- Inhibition of protein synthesis
An antimicrobial drug that inhibits protein synthesis has effects in what area of the cell?
What common drugs are active against the ribosomal 50s subunit?
Chloramphenicol, Erythromycin and Clindamycin all have antimicrobial activity against what cellular component?
50s ribosomal subunit
What common antimicrobial drugs are active against the 30s ribosomal subunit?
Aminoglycosides, Tetracycline, Streptomycin and Amikacin all have activity antimicrobial against what cellular component?
The 30s ribosomal subunit
What antimicrobial is active against the cell membrane?
Polymixins haveantimicrobial activity against what cellular component?
The Cell Membrane
What type of activity do antimicrobials that are active against the cell wall have?
Block Cell wall synthesis and repair
Antimicrobials that block synthesis and repair of the cell wall are:
Penicillins, Cephalosporins, Vancomycin, Bactitracin and Monobactones have what antimicrobial activity?
Block synthesis and repair of the Cell Wall
What actions do Antimicrobials that are active against DNA have?
- Inhibit gyrase
- Inhibit RNA polymerase
Antimicrobials that inhibit gyrase and RNA polymerase have activity against what cellular component?
What antimicrobial inhibits gyrase, and thus the unwinding of DNA?
What antimicrobials inhibit RNA polymerase?
Quionolones, Ciprofloxacin and Rifampin all have activity against what cellular component?
Quinolones and Ciprofloxacin have what specific antimicrobial activity?
Rifampin has what specific antimicrobial activity?
Inhibits RNA polymerase
What action do antimicrobials have against the cytoplasm?
Inhibit folic acid metabolism
Antimicrobials that act against the cytoplasm have what specific action?
Inhibit folic acid metabolism
What drugs inhibit folic acid metabolism
- Sulfonamides (Sulfa drugs)
Trimethoprim and Sulfonamides have activity against what cellular component?
Trimethoprim and Sulfonamides have what specific antimicrobial action?
Inhibit folic acid metabolism
What are the five characteristics of an ideal antibiotic?
- High therapeutic Index
- Few Adverse Reactions
- Variety of administration routes
- Good absorption and Distribution
- Resistance develops infrequently
Selective, Cidal, Narrow-Spectrum, high Therapeutic Index, Few adverse Reactions, Variety of administration routes, Good absorption and Distribution, Resistance develops infrequently are characteristics that describe what?
The Ideal Antimicrobial
Describe the characteristics that describe an antimicrobial with “Few Adverse Reactions”?
- Toxicity-dose related (predictable)
- Allergy (non-allergenic)
- Idiosyncratic reactions –not dose related
What characteristic of toxicity would be ideal?
Dose related toxicity –i.e. predictable
What characteristic of idiosyncratic reactions is most ideal?
Not dose related
What type of administration route is characteristic of an ideal antimicrobial?
A variety of routes available
What characteristic of absorption and distribution would an ideal antimicrobial exhibit?
- High level
- Distributing to difficult to reach areas like:
- CNS, prostate and aqueous humor of the eye
What are the three mechanisms of resistance used my microbes?
- Antibiotic inactivating enzymes
- Altered target
- Reduced accumulation (reduced permeability and active efflux)
Antibiotic inactivating enzymes, altered targets and Reduced accumulation (via reduced permeability and active efflux) are mechanisms for what?
What five questions should be considered before selecting an antibiotic?
- Will the antibiotic be absorbed
- Where will it be absorbed?
- Will it penetrate the CNS or Prostate?
- Will is transfer to breast milk?
- How will it be excreted?
What is the easiest direct route of absorption?
In what ways may rapid absorption of intravenous infusions be offset?
- By rapid excretion
- By slow infusion
Slow infusion or rapid excretion can offset what characteristic of Intravenous absorption?
Rapid and direct infiltration of the blood
What variable exists for intramuscular routes?
Rate of fluid exchange
What groups of patients should receive special consideration prior to receiving IM administration?
- Diabetics –due to poor circulation
- Hypotensive patients –due to low blood pressure
Why should Hypotensive patients receive special consideration prior to intramuscular administration?
- IM admin. is dependent on fluid exchange rates
- Hypotensive patients have low blood pressure that affects this rate
Why should Diabetics receive special consideration prior to receiving Intramuscular administration?
- Intramuscular admin. Absorption is dependent on the rate of fluid exchange
- Diabetics have poor circulation that affects this rate
What is the explanation for a massive delayed rapid drug release in a patient who received an IM injection?
- Previous Hypotension that caused accumulation of the drug at the IM site
- Current increase in BP caused a rapid release of the drug
What is a potential absorption advantage of IM injections?
Extends the duration of therapeutics levels by delaying drug entry into the blood stream
What route of administration can delay drug entry into the blood stream and extend the duration of therapeutic levels?
What is an example of an IM injection that is designed to release into the blood stream slowly and maintain therapeutic levels?
Penicillin and Procaine
Procaine Penicillin or a Penicillin salt is more soluble?
What is the advantage of Procaine Penicillin IM injection?
- It is less soluble than salt forms of penicillin
- Thus, it releases into the blood stream at a slower rate
Procaine Penicillin or Procaine salts allow for a loner interval between doses?
What should be injected intramuscularly with penicillin to slow the release prolong the interval between doses?
What factor plays the most significant role in determining the absorption of oral doses?
What state are oral doses most likely to be absorbed?
Lest polar state
The least polar state is important for what type of dosage?
The stomach is acidic or alkaline?
The small intestine if acidic or alkaline?
What two factors discussed in class influence the absorption rates for oral doses?
- Intestinal transit time
Intestinal transit time and chemistry are important influencing factors for what route of administration?
Antacids decrease uptake of what oral drugs?
Acidic drugs and flouroquinolones
What reduces uptake of Acidic drugs and flouroquinolones?
Gastric Acid production varies with age (T/F)?
Kids and geriatric patients have what characteristic that alters their absorption of oral drugs?
Higher stomach pH