Pharm Exam 1 Flashcards
What is CYP/Cytochrome P450?
Enzymes in the liver and gut wall that work together to process drugs
affinity
degree of attraction between drug and receptor
Antagonists
Prevent receptor activation by endogenous regulatory molecules and drugs
When patients are allergic to PCN what drug is used instead?
macrolides
Common receptors (9)
Cholinergic receptors
-nicotinic and muscarinic
Adrenergic
-Alpha 1&2 and Beta 1&2
Opiod
-Mu, kappa, delta
Cephalosporin interactions with other drugs
interferes with vitamin K so adjust blood thinners
use with aspirin and NSAIDs increased effect of platelet inhibition and leads to risk of bleeding
IM injections not recommended
Code of ethics
promote health
prevent illness
restore health
alleviate suffering
Mechanisms of actions of penicillins, cephalosporins, vancomycin, and imipenem?
inhibators of cell wall synthesis
General treatment for protozoa and helminths (and c diff)
metronidazole-flagyl
protein drug targets
membrane receptors
intracellular receptors
enzymes
ion channels
carriers or transporters
drugs that are synthetic/semisynthetic
most drugs
Impact of food on drug absorption
decreased absorption or rate of absorption (milk and tetracycline or fiber and digoxin)
increased absorption (high calorie meal and saquinavir)
extended-spectrum penicillins
carbenicillin and ticarcillin (interferes with platelet fx)
pseudomonas a. and klebsiella
examples of drugs that come from animals
hormones and heparin
How is cephalosporin eliminated?
kidneys
consequences of drug-drug interactions (3)
intensification of effects
reduction of effects
creation of a unique response
Properties of an ideal drug (3) plus 7
effective
safe
selective
reversible
predictable
easy to give
no interactions
low cost
stable chemically
simple generic name
drug interactions with fluoroquinolones
inhibit theophylline and warfarin
bind with antacids, calcium, iron, foods, and decrease bioavalability
What stage does penicillin work best in?
inflammatory phase of infection
non opportunistic fungi
coccidiodes, histoplasma, blastomyces
How does hepatic transformation affect drugs?
inactivation
change to active metabolite
activation of a pro drug to an active substance
activation to a toxic metabolite
what does miconazole treat
common OTC
tinea pedis, cutaneous candida, and other ringworms
given IV if allergic to amphotericin B
Agonists
molecules that activate receptors
affinity and high intrinsic activity
Dobutamine mimics NE at cardiac receptors
can make processes go faster or slower
What is the mechanism of action for fluoroquinolones
inhibition of DNA synthesis
Beta lactamase inhibitors and their combos
clavulanic acid + amoxicillin or ticarcillin
sulbactam + ampicillin
tazobactam + piperacillin
Nystatin
treatment for oral thrush via lozenges
mechanism of action of macrolides and aminoglcosides
inhibitors of protein synthesis
antagonist
a drug which has affinity but no intrinsic activist. Binds to receptor and does not activate it and blocks other molecules. Beta-blockers and metoprolol
What happens in the pharmacodynamic phase?
drug receptor interaction
What are the two absorption routes?
Parenteral (outside intestines) or enteral (intestines)
CDiff/Pseudomembranous colitis process and treatment
destruction of normal flora allows c. diff to flourish
C. Diff causes toxin that erodes cell lining of GI tract
treated with metronidazole
mechanism of action for sulfonamides and trimethoprim
inhibits folic acid synthesis
Are macrolides bacteriocidal or bacteriorstatic
bacteriostatic
narrow spectrum w/ penicillinase resistance and what it works on
nafcillin and dicloxicillin
staph aureus
drug
any chemical substance other than those required for normal sustenance which produces a biological effect
What is the main site of drug metabolism?
liver
3 basic mechanisms of drug-drug interactions (pharmacodynamic interactions)
at the same receptor: inhibitory
at separate sites: potentative (stronger) (diazepam and morphine) or inhibitory (hydrochlorothiazide and spironlactone)
combined toxicity should not be used together
What are 5 variables relating to drug distribution in the body?
- blood flow to tissues
- ability of drug to exit vascular system
- body fat
- protein binding
- blood-brain barrier
what is the most common fluoroquinolones
ciprofloxin
Drugs that cause steven johnson syndrome
penicillins, sulfas, quinolones, phenytoin, carbamazepine, barbiturates, and lamictal
Mechanism of action of amphotericin
binds to ergosterol membrane of the fungus and pokes holes in it
VRSA
vancomycin resistant staph aureus
examples of drugs that come from microorganisms
some antibiotics
What happens in the pharmacokinetic phase?
absorption
distribution
metabolism
excretion
pharmacology
study of drug or medicine
What is the spectrum and types of bacteria fluoroquinolones are good for?
broad spectrum bactericidal
gram neg and some gram pos
drugs from genetic engineering
epogen and interferon
tolerance
a change in the responsiveness to drugs
What are the three steps of kidney excretion of drugs?
glomerular filtration
passive re-absorption
active secretion/transport
Induction at P450
Enhances metabolism of the drugs taken concurrently which prevents effectiveness of drug therapy
Metabolized too fast to be effect
opportunistic fungi
cryptococcus, aspergillus, and candida
VISA
vancomycin insensitive staph aureus
erythromycin is the first line treatments for (3)
legionella pneumophila, whooping cough, and diphtheria
implication of sulfonamides and trimethoprim
crystalluria- H2o and cranberry juice
toxic nephrosis from sulfur crystals
anemia
SJS
allergy
toxicology
the study of adverse effects of drugs and other chemicals
therapeutic index
ratio between lethal dose (LD50) and effective dose (ED50), wider TI is better
relative potency
the amount of a drug that must be given to illicit a response
What happens in the pharmaceutical phase?
disintegration and dissolution of drug form
drug becomes available for absorption
What are the three isoforms of CYP450 dedicated to metabolizing drugs?
CYP 1,2,3
CYP3A4- 50% of drug transformation
CYP2D6- 30%
CYP 1A2, 2C19, 2C9, and 2E1- 20%
What are 4 variables related to drug absorption?
route of administration
blood flow to the site
solubility of the drug (acid/base)
concentration of the drug
MRSA
methicillin resistance staph aureus
side effects vs. adverse reactions
side effects are predictable; adverse reactions are unpredictable (anaphylaxis)
VRE
vancomycin resistant enterococcus faecaelis
Besides the kidneys, where can drugs be excreted?
lungs, sweat, saliva, mammary glands, and dialysis.
What are the three aminoglycosides and how are they administered
IV only
amikacin
gentamycin
tobramycin
biologic half-life
rate of metabolism and excretion determines half life (time it takes to excrete 50% of the drug and for it to decrease by 50% in the body). Does not change with dose of drug.
mechanism of actions of the -azole antifungals
block the synthesis of sterol by inhibiting P450
Are macrolides broad or narrow spectrum?
broad
types of allergic reactions to PCN
immediate 2-30 mins, anaphylaxis
accelerated 1-72 hours, weals and hives, rashes
days to weeks, rashes
agonist
a drug which has affinity and intrinsic affinity
A drug or substance that binds to a receptor inside a cell or on its surface and causes the same action as the substance that normally binds to the receptor. B-agonists and albuterol
Which bacteria are fluoroquinolones good for?
e.coli, klebsiella, salmonella, campylobacter jejuni, p. aeruginosa, h. flu, and anthrax spores
What are the major implications of aminoglycosides
ototoxic and nephrotoxic
pharmacotherapeutics
use of drugs to treat disease
pharmacokinetics
how the body interacts with the drug
5 “rights” plus an additional 5
- right drug
- right patient
- right dose
- right route
- right time
- right assessment
- right documentation
- right evaluation
- right of patient to education
- right of patient to reduce care
pharmacodynamics
how drug interacts with cells, tissues, and organs
maximal efficacy
the largest effect that a drug can produce
Adverse reactions for fluoroquinolones
insomnia, c diff, achilles tendon rupture in the elderly, steven johnson syndrome, QT prolongation.
three phases of drug interaction
- pharmaceutical
- pharmacokinetic
-drug become available for action- - pharmacodynamic
-effect of drug is seen-
What are the three ways the liver affects drugs in order to remove them from the body?
Increase H2O solubility for urine elimination
Inactivates the chemical
Coverts the chemical for elimination through the gut
broad spectrum penicillin and what it works on
ampicillin and amoxicillin
H Flu, E coli, P mirabilis, neisseria, salmonella, shigella
signs and symptoms of a suprainfection related to penicillin use
darkened tongue, creamy vaginal discharge, watery diarrhea with cramping
How is amphotericin B administered
IV or intrathecally (spinal fluid)
What type of bacteria is vancomycin active against?
gram pos
efficacy
ability of a drug to initiate biologic activity as a result of binding to a given receptor
Shared adverse reactions of antimicrobial agents
antibiotic associated colitis
allergic or hypersensitive reaction
suprainfection
4 primary mechanisms of antibiotic resistance
descrease concentration of the drug at it’s site of action
alter the drug target molecule
antagonist production
drug inactivation
What are the two ways drugs exert their action?
Activate a series of cellular events creating a biological effect
bind to receptors without stimulating them and block other chemicals from binding with the receptor
Uses for sulfonamides and trimethoprim
UTI pathogens such as e.coli, klebsiella, p. mirabilis.
pneumocystis carinii pneumonia
acute exacerbations of chronic bronchitis
prostatitis and sinusitis
How are vancomycin and imipenem administered
IV only
Symptoms of SJS and type of hypersensitivity
type IV hypersensitivity
flu like symptoms within two weeks of starting drug
rash follows, followed by skin sloughing
MDR-TB
multi drug resistant TB
implications of amphotericin B
-fever and chills, give tylenol and antihistamine before giving
-nephrotoxicity in 80% of patients
-alveolar hemorrhage
drugs that come from minerals
calcium and iron
narrow spectrum penicillins and what they work on
penicillin G, V, or VK
streptococcus and neisseria
what do penicillins interact with?
oral contraceptives, anti-coagulants, and aminoglycides
What is the main site for drug excretion?
kidneys
examples of drugs that come from plants
digitalis and atropine
Inhibition at P450
One drug blocks the enzymes that metabolize the other drugs leading to increased blood concentrations of unmetabolized drug (toxic)
which drug is the choice for all candida species
fluconazole
What parts of the body are fluoroquinolones good for and which aren’t they?
good for lungs, prostate, and GU, bad for CSF
Spectrum and type of bacteria for aminoglycosides
narrow spectrum and gram negative
What generation of cephalosporins have CSF penetration?
3rd and 4th
