Chemotherapeutic Agents Flashcards
are used to destroy both organisms that invade the body (e.g., bacteria, viruses, parasites, protozoa, fungi) and abnormal cells within the body (e.g., neoplasms, cancers)
Chemotherapeutic drugs
organisms that invade the body
bacteria, viruses, parasites, protozoa, fungi
abnormal cells within the body
neoplasms, cancers
These drugs affect cells by altering cellular function or disrupting cellular integrity, causing cell death, or by preventing cellular reproduction, eventually leading to cell death.
Chemotherapeutic drugs
Chemotherapeutic drugs affect cells by
altering cellular function or disrupting cellular integrity, causing cell death, or by preventing cellular reproduction, eventually leading to cell death.
the basic structural unit of the body
Cell
Each cell has a ____________________________________________, which contains a variety of ______________
nucleus, a cell membrane, and cytoplasm; organelles
contains all genetic material necessary for cell reproduction and for the regulation of cellular production of proteins.
Nucleus
Nucleus contains a spherical mass called
nucleolus
sites of protein synthesis
ribosomes
Within this nucleolus are dense fibers and proteins that will eventually become _____________________
ribosomes
essential for cellular integrity and is equipped with many mechanisms for maintaining cell homeostasis.
Celll Membrane
mainly composed of proteins and lipids— phospholipids, glycolipids, and cholesterol
lipoprotein structure
a lipoprotein structure, mainly composed of
proteins and lipids— phospholipids, glycolipids, and cholesterol
power plants” within each cell that produce energy in the form of ATP,which allows the cell to function.
Mitochondria
membrane-covered organelles that contain specific digestive enzymes that can break down proteins, nucleic acids, carbohydrates, and lipids
Lysosomes
are responsible for digesting worn or damaged sections of a cell when the membrane ruptures and the cell dies.
Lysosomes
designed to target foreign organisms that have invaded and infected the body
ANTI-INFECTIVE AGENTS
ANTI-INFECTIVE AGENTS:
THERAPEUTIC ACTION
- interfere with biosynthesis of the pathogen cell wall.
- interfere with the steps involved in protein and DNA synthesis, functions necessary to maintain the cell and allow for cell division.
- alter the permeability of the cell membrane to allow essential cellular components to leak out
ANTI-INFECTIVE ACTIVITY:
- Bactericidal
- Bacteriostatic
active against the infective microorganisms that they actually cause the death of the cells they affect.
Bactericidal
not as aggressive; they interfere with the ability of the cells to reproduce or divide
Bacteriostatic
a complex interaction among chemical mediators, leukocytes, lymphocytes, antibodies, and locally released enzymes and chemicals.
HUMAN IMMUNE RESPONSE
It is difficult to treat any infections for two reasons:
- Anti-infective drugs cannot totally eliminate the pathogen without causing severe toxicity in the host
- Patients do not have the immune response in place to deal with even a few invading organisms.
refers to the ability over time to adapt to an anti-infective drug and produce cells that are no longer affected by a particular drug.
RESISTANCE
Resistance can be
natural or acquired
ACQUIRING RESISTANCE:
- Producing an enzyme that deactivates the antimicrobial drug
2 Changing cellular permeability to prevent the drug from entering the cell or altering transport systems. - Altering binding sites on the membranes which then no longer accept.
- Producing a chemical that acts as an antagonist to the drug.
ANTI-INFECTIVE AGENTS
PURPOSE:
- For Treatment of Systemic Infections.
- identification of the correct pathogen and selection of a drug (sensitivity)
- Combination Therapy
- Prophylaxis
synergistic, which means that they are more powerful when given in combination
Combination Therapy
to prevent infections before they occur.
Prophylaxis
Inhibit protein synthesis
AMINOGLYCOSIDES
used to treat serious infections caused by susceptible strains of gram negative bacteria, including Pseudomonas aeruginosa, E. coli, Proteus species, the Klebsiella–Enterobacter– Serratia group, Citrobacter species, and Staphylococcus.
AMINOGLYCOSIDES
AMINOGLYCOSIDES is
Bactericidal
A. AMINOGLYCOSIDES
PHARMAKOKINETICS
- poorly absorbed from the GI tract but rapidly absorbed after intramuscular (IM) injection. widely distributed throughout the body, cross the placenta and enter breast milk, and are excreted unchanged in the urine
AMINOGLYCOSIDES
CONTRAINDICATIONS/ CAUTIONS:
Allergy
Hepatic disease
Renal disease
Preexisting Hear loss
Herpes/ Mycobacterial Infection
Myasthenia gravis or parkinsonism
Lactation
AMINOGLYCOSIDES
ADVERSE EFFECTS:
- Black box warning alerting health care professionals to the serious risk of: ototoxicity and nephrotoxicity.
- GI effects include nausea, vomiting, diarrhea, weight loss, stomatitis, and hepatic toxicity.
- Cardiac effects can include palpitations, hypotension, and hypertension
- Hypersensitivity reactions include purpura, rash, urticaria, and exfoliative dermatitis.
AMINOGLYCOSIDES
Observe for :
OTOTOXICITY
NEPHROTOXICITY
are a relatively new class of broad-spectrum antibiotics
CARBAPENEMS
used to treat serious infections caused by susceptible strains of S. pneumoniae, Haemophilus infl uenzae, Moraxella catarrhalis, S. aureus, Streptococcus pyogenes, E. coli and others.
CARBAPENEMS
indicated for treating serious intra-abdominal, urinary tract, skin and skin structure, bone and joint, and gynecological infect
CARBAPENEMS
First drug of Class
Meropenem
CARBAPENEMS
PHARMAKOKINETICS
- Rapidly absorbed if given IM
- They are widely distributed throughout the body, although it is not known whether they cross the placenta or enter breast milk.
- excreted unchanged in the urine
CARBAPENEMS
CONTRAINDICATIONS/ CAUTIONS:
- allergy to any of the carbanems or beta-lactams
- seizure disorders
- meningitis
- lactation
- Use caution during pregnancy
- Ertapenem is not recommended for use in patients younger than 18 years of age.
CARBAPENEMS
ADVERSE EFFECTS:
- GI tract can limit the use of carbapenems in some patients.
- Pseudomembranous colitis, Clostridium difficile diarrhea
nausea and vomiting can lead to serious dehydration and
electrolyte imbalances. - Superinfections can occur with any of the carbapenems.
- CNS effects can include headache, dizziness, and altered mental state.
- Seizures
CARBAPENEMS
Monitor the patient regularly for signs of:
- pseudomembranous colitis
- severe diarrhea,
- superinfections
- confusion and seizures
- phlebitis
basically interfere with the cell wall–building ability of bacteria when they divide
CEPHALOSPORINS
are largely effective against the same gram-positive bacteria that are affected by penicillin G, as well as the gram-negative bacteria P. mirabilis, E. coli, and K. pneumoniae (use the letters PEcK as a mnemonic
First-generation cephalosporins
are effective against the previously mentioned strains, as well as H. influenzae, Enterobacter aerogenes, and Neisseria species (remember HENPeCK)
Second-generation cephalosporins
which are effeCtive against all of the previously mentioned strains relatively weak against gram-positive bacteria but are more potent against the gram-negative bacilli, as well as against Serratia marcescens (remember HENPeCKS).
Third-generation cephalosporins
cephalosporins are in development. The first drug of this group, cefepime (Maxipime), is active against gram-negative and gram-positive organ isms, including cephalosporin-resistant staphylococci and P. aeruginosa.
Fourth-generation cephalosporins
CEPHALOSPORINS
PHARMAKOKINETICS
- are well absorbed from the GI tract
- others are absorbed well after IM injection or IV administration
- are primarily metabolized in the liver and excreted in the urine.
- These drugs cross the placenta and enter breast milk.
CEPHALOSPORINS
CONTRAINDICATIONS/ CAUTIONS:
- allergies to cephalosporins or penicillins
- Use with caution in patients with hepatic or renal impairment
- use with caution in pregnant or lactating patients
CEPHALOSPORINS
ADVERSE EFFECTS:
- GI tract and include nausea, vomiting, diarrhea, anorexia, abdominal pain, and flatulence. Pseudomembranous colitis
- CNS symptoms include headache, dizziness, lethargy, and paresthesias.
- Nephrotoxicity
- Hepatotoxicity
- Superinfection
CEPHALOSPORINS
Monitor the patient regularly for signs:
Nephrotoxicity
Hepatotoxicity
Superinfection
Diarrhea
They interfere with the action of DNA enzymes necessary for the growth and reproduction of the bacteria.
FLUOROQUINOLONES
are indicated for treating infections caused by susceptible strains of gram-negative bacteria, including E. coli, P. mirabilis, K. pneumoniae, etc.
FLUOROQUINOLONES
FLUOROQUINOLONES
PHARMAKOKINETICS
- are absorbed from the GI tract, metabolized in the liver, and excreted in the urine and feces.
- drugs are widely distributed in the body and cross the placenta and enter breast milk
FLUOROQUINOLONES
CONTRAINDICATIONS/ CAUTIONS:
- allergy to fluoroquinolones
- pregnancy
- Use with caution in the presence of renal dysfunction
FLUOROQUINOLONES
ADVERSE EFFECTS:
- most common are headache, dizziness, insomnia, and depression
- GI effects include nausea, vomiting, diarrhea, and dry mouth
- Box Warning was added to all drugs in this class in 2009 reporting the risk of tendinitis and tendon rupture.
- immunological effects include bone marrow depression
fever, rash, and photosensitivity
FLUOROQUINOLONES
Monitor the patient for :
CNS: headache, dizziness, tinnitus,confusion, mental depression
GI upsets
bone marrow depression
PHOTOTOXICITY/ PHOTOSENSITIVITY
HEPATOTOXICITY
NEPHROTOXICITY
bactericidal effects by interfering with the ability of susceptible bacteria to build their cell walls when they are dividing.
PENICILLINS
drugs prevent from biosynthesizing the framework of the cell wall, and the bacteria with weakened cell walls swell and then burst from osmotic pressure within the cell.
PENICILLINS
are indicated for the treatment of streptococcal infections, including pharyngitis, tonsillitis, and others.
PENICILLINS
At high doses, these drugs are also used to treat meningococcal meningitis.
PENICILLINS
PENICILLINS
PHARMAKOKINETICS
- rapidly absorbed from the GI tract, reaching peak levels
- sensitive to the gastric acid levels in the stomach and should be taken on an empty stomach to ensure adequate absorption.
- excreted unchanged in the urine
- enter breast milk
PENICILLINS
CONTRAINDICATIONS/ CAUTIONS:
- allergy to penicillin and cephalosporins
- pregnancy
- Use with caution in the presence of renal disease
PENICILLINS
ADVERSE EFFECTS:
- Common adverse effects include nausea, vomiting, diarrhea, abdominal pain, glossitis, stomatitis, gastritis, sore mouth, and furry tongue.
- Superinfections, including yeast infections
- Pain and inflammation at the injection site
- Hypersensitivity reactions may include rash, fever, wheezing, and, with repeated exposure, anaphylaxis
work by inhibiting protein synthesis in a wide range of bacteria, leading to the inability of the bacteria to multiply
TETRACYCLINES
indicated for treatment of infections caused by Rickettsiae, Mycoplasma pneumoniae, Borrelia recurrentis, H. infl uenzae, Haemophilus ducreyi, Pasteurella pestis, ETC.
TETRACYCLINES
TETRACYCLINES
PHARMAKOKINETICS
-absorbed adequately, but not completely, from the GI tract.
Absorption is affected by food, iron, calcium, and other drugs in the stomach.
- cross the placenta and pass into breast milk
TETRACYCLINES
CONTRAINDICATIONS/ CAUTIONS:
- allergy to tetracyclines or to tartrazine
- pregnancy and lactation
- ophthalmic preparation: patients who have fungal, mycobacterial, or viral ocular infections
- used with caution in children younger than 8 years of age
TETRACYCLINES
ADVERSE EFFECTS:
- direct irritation of the GI tract and include nausea, vomiting, diarrhea, abdominal pain, glossitis, and dysphagia.
- Fatal hepatotoxicity related to the drug’s irritating effect on the liver
- Skeletal effects involve damage to the teeth and bones.
- Dermatological effects include photosensitivity and rash.
- Superinfections
- Local effects, such as pain and stinging with topical or ocular application
- Hypersensitivity reactions
the group of bacteria that contain the pathogens that cause tuberculosis and leprosy.
Mycobacteria
Mycobacteria
the group of bacteria that contain the pathogens that cause tuberculosis and leprosy.
cause serious infectious diseases:
Mycobacterium tuberculosis - PTB
Mycobacterium leprae- LEPROSY OR HANSEN’S DISEASE
Mycobacterium avium-intracellulare -mycobacterium avium complex in AIDS
ANTITUBERCULOSIS DRUGS
Treatment duration:
6 months to 2 years
ANTITUBERCULOSIS DRUGS
First-line drugs :
- isoniazid (Nydrazid)
- rifampin (Rifadin)
- pyrazinamide (generic)
- ethambutol (Myambutol)
- streptomycin (generic),
- rifapentine (Priftin).
ANTITUBERCULOSIS DRUGS
Second-line drugs :
- ethionamide (Trecator-SC),
- capreomycin (Capastat),
- cycloserine (Seromycin)
- rifabutin (Mycobutin).
the mainstay of leprosy treatment
Dapsone (generic)
inhibits folate synthesis
Dapsone (generic)
used for treatment of P. carinii pneumonia in AIDS patients
Dapsone (generic)
Dapsone (generic)
Adverse Effects
- CNS effects, such as neuritis, dizziness, headache, malaise,
drowsiness, and hallucinations. - irritating to the GI tract, causing nausea, vomiting, anorexia,
stomach upset, and abdominal pain.
ANTIMYCOBACTERIALS
PHARMAKOKINETICS
- Well absorbed from the GI tract.
- metabolized in the liver and excreted in the urine
- cross the placenta and pass into breast milk
Inhibits the synthesis of mycolic acids and acts to kill actively growing organisms in the extracellular environment
Isoniazid
Inhibits the growth of dormant organisms in the macrophages and caseating granulomas
Isoniazid
Is active only during cell division and is used in combination with other antitubercular medications
Isoniazid
Isoniazid
Side and adverse effects
a. Hypersensitivity reactions
b. Peripheral neuritis
c. Neurotoxicity
d. Hepatotoxicity and hepatitis; increased liver function test levels
e. Pyridoxine deficiency
f. Irritation at injection site with intramuscular administration
g. Nausea and vomiting
h . Dry mouth
i. Dizziness
k. Vision changes
Isoniazid
Contraindications and cautions
a. Contraindicated in clients with hypersensitivity or with acute liver disease
b. Use with caution in clients with chronic liver disease, alcoholism, or renal
impairment.
c. Use with caution in clients taking hepatotoxic medications because the risk for
hepatotoxic ity increases.
d. Alcohol increases the risk of hepatotoxicity.
e. May increase the risk of toxicity of carbamazepine and phenytoin
g. May decrease ketoconazole concentrations
Inhibits bacterial RNA synthesis
Rifampicin
Binds to DNA-dependent RNA polymerase and blocks
RNA transcription
Rifampicin
Used with at least 1 other antitubercular medication
Rifampicin
Rifampicin
Contraindications and cautions
a. Contraindicated in clients with hypersensitivity
b. Used with caution in clients with hepatic dysfunction or alcoholism
c. Use of alcohol or hepatotoxic medications may increase the risk of hepatotoxicity.
d. Decreases the effects of several medications, including oral anticoagulants, oral
hypoglycemics, chloramphenicol, digoxin, disopyramide phosphate, mexiletine, quinidine polygalacturonate, fluconazole, methadone hydrochloride, phenytoin, and
verapamil hydrochloride
Rifampicin
Side and adverse effects
a. Hypersensitivity reaction, including fever, chills, shivering, headache, muscle and bone pain, and dyspnea.
b. Heartburn, nausea, vomiting, diarrhea
c. Red-orange–colored body secretions
d. Vision changes
e. Hepatotoxicity and hepatitis
f. Increased uric acid levels
g. Blood dyscrasias
h. Colitis
Interferes with cell metabolism and multiplication by inhibiting 1 or more metabolites in susceptible organisms
Ethambutol
Inhibits bacterial RNA synthesis and is active only during
cell division
Ethambutol
Slow-acting and must be used with other bac tericidal
agents
Ethambutol
Ethambutol
Contraindications and cautions
a. Contraindicated in clients with hypersensitivity or optic neuritis and in children younger than 13 years
b. Used with caution in clients with renal dysfunction, gout, ocular defects, diabetic retinopathy, cataracts, or ocular inflammatory conditions
c. Used with caution in clients taking neurotoxic medications because the risk for neurotoxicity increases
Ethambutol
Side and adverse effects
a. Hypersensitivity reactions
b. Anorexia, nausea, vomiting
c. Dizziness
d. Malaise
e. Mental confusion
f. Joint pain
g. Dermatitis
h. Optic neuritis
i. Peripheral neuritis
j. Thrombocytopenia
k. Increased uric acid levels
Aminoglycosides Drugs
amikacin
gentamicin
kanamycin
neomycin
streptomysic
tobramysin
Treatment of serious gram-negative infections
amikacin (Amikin)
Treatment of Pseudomonas infections and a wide variety of gram-negative infections
gentamicin (Garamycin)
Treatment of hepatic coma and to decrease gastrointestinal (Gl) normal flora
kanamycin (Kantrex)
Suppression of Gl normal flora preoperatively; treatment of hepatic coma; topical treatment of skin wounds
neomycin (Mycifradin)
Fourth drug in combination therapy regimen for treatment of tuberculosis;
streptomycin (generic)
Short-term IV or IM treatment of serious infec-tions; ocular infections caused by susceptible bacteria; nebulizer management of cystic fibrosis and P. aeruginosa infections
tobramycin (TOBI, Tobrex)
Carbapenems Drugs
doripenem
ertapenem
imipenem-cilastatin
meropenem
Treatment of complicated intra-abdominal infections or complicated UTis, including pyelonephritis, caused by susceptible bacteria
doripenem
Treatment of community-acquired pneumonia, complicated genitourinary infections, acute pelvic infections, complicated intra-abdominal infections, skin and skin-structure
ertapenem
Treatment of serious respiratory, intra-abdominal, urinary tract, gynecological, bone and joint, skin and skin-structure infections; septicemia, endocarditis, bone and joint infections, and polymicrobic infections
imipenem-cilastatin
Treatment of bacterial meningitis, complicated skin and skin-structure infections, intra-abdominal infections
meropenem
Treatment of bacterial meningitis, complicated skin and skin-structure infections, intra-abdominal infections
meropenem
FIRST-GENERATION CEPHALOSPORINS
cefadroxil
cefazolin
cephalexin
SECOND-GENERATION CEPHALOSPORINS
cefaclor
cefoxitin
cefprozil
cefuroxime
THIRD-GENERATION CEPHALOSPORINS
cefdinir
cefotaxime
cefpodoxime
ceftazidime
ceftibuten
ceftizoxime
ceftriaxone
FOURTH-GENERATION CEPHALOSPORINS
cefditoren
cefepime
ceftaroline
Floroquinolones Drugs
ciprofloxacin
gemifloxacin
levoflaxacin
mixofloxcin
norflocaxin
ofloxacin