Chemotherapeutic Agents Pt. 2 and 3 Flashcards
(228 cards)
1
Q
The exact mechanism of action is unknown.
A
Pyrazinamide
2
Q
May be bacteriostatic or bactericidal, depending on its concentration at the infection site and on the susceptibility
of the infecting organism
A
Pyrazinamide
3
Q
Pyrazinamide
Contraindications and cautions
A
a. Contraindicated in clients with hypersensitivity
b. Used with caution in clients with diabetes mellitus, renal impairment, or gout, and in children
c. May decrease the effects of allopurinol, colchicine, and probenecid
d. Cross-sensitivity is possible with isoniazid, ethionamide, or nicotinic acid.
4
Q
Pyrazinamide
Side and adverse effects
A
a. Increases liver function tests and uric acid levels
b. Arthralgia, myalgia
c. Photosensitivity
d. Hepatotoxicity
e. Thrombocytopenia
5
Q
Inhibits mycobacterial DNA-dependent RNA polymerase and suppresses protein synthesis
A
Rifabutin
6
Q
Used to prevent disseminated Mycobacterium avium complex (MAC) disease in clients with advanced HIV infection
A
Rifabutin
7
Q
Used to treat active MAC disease and tuberculosis in clients with HIV infection
A
Rifabutin
8
Q
Rifabutin
Cautions
A
a. Can affect blood levels of some medications, including oral contraceptives and some medications used to treat HIV infection
b. A nonhormonal method of birth control should be used instead of an oral contraceptive.
9
Q
Used only for pulmonary tuberculosis
A
Rifapentine
10
Q
Can affect blood levels of some medications, including oral contraceptives and warfarin, and some medications used to treat HIV infection
A
Rifapentine
11
Q
Rifapentine
Side and adverse effects
A
a. Red-orange–colored body secretions
b. Hepatotoxicity
12
Q
a. Mechanism of action is unknown.
b. Used to treat MDR-TB when significant resistance to other medications is expected
c. Administered intramuscularly
A
Capreomycin sulfate
13
Q
Capreomycin sulfate
Contraindications and cautions
A
a. The risk of nephrotoxicity, ototoxicity, and neuromuscular blockade is increased with the use of aminoglycosides or loop diuretics.
b. Used with caution in clients with renal insuf ficiency, acoustic nerve impairment, hepatic disorder, myasthenia gravis, or parkinsonism
c. Not administered to clients receiving streptomycin
14
Q
Capreomycin sulfate
Side and adverse effects
A
a. Nephrotoxicity
b. Ototoxicity
c. Neuromuscular blockade
15
Q
OTHER ANTIBIOTICS
A
Ketolide
- telithromycin
Lincosamides
- clindamycin
- lincomycin
Lipoglycopeptides
- televacin
Macrolides
- azithromycin
- clarithmycin
- arythromycin
Monobactam
- aztreonam
16
Q
binds to specific ribosome subunits, leading to cell death in susceptible bacteria, which includes several strains resistant to other antibiotics
A
Telithromycin
17
Q
KETOLIDES
PHARMACOKINETICS
A
- It is rapidly absorbed through the GI tract, reaching peak levels in 1 hour.
- distributed, may cross the placenta, and does pass into breast milk.
- metabolized in the liver with a half-life of 10 hours.
- excreted in the urine and feces
18
Q
KETOLIDES
CONTRAINDICATION AND CAUTIONS:
A
- known allergy to any component of the drug or to macrolide antibiotics
- known congenital prolonged QT interval, bradycardia, or any proarrhythmic condition with myasthenia gravis, which is a black box warning with this drug
- Use with caution in cases of renal or hepatic impairment
- Use with caution with pregnant and lactating patients
19
Q
KETOLIDES
ADVERSE EFFECTS:
A
- GI tract: nausea, vomiting, taste alterations, and the potential for pseudomembranous colitis.
- Superinfections
- Serious hypersensitivity reactions, including anaphylaxis
20
Q
react at almost the same site in bacterial protein synthesis
A
LINCOSAMIDES
21
Q
These drugs are used in the treatment of severe infections when a less-toxic antibiotic cannot be used.
A
LINCOSAMIDES
22
Q
LINCOSAMIDES
PHARMACOKINETICS
A
- are rapidly absorbed from the GI tract or from IM injections
- metabolized in the liver and excreted in the urine and feces.
- cross the placenta and enter breast milk
23
Q
LINCOSAMIDES
CONTRAINDICATIONS AND CAUTIONS
A
- with caution in patients with hepatic or renal impairment,
- Use during pregnancy and lactation only if the benefit clearly outweighs the risk to the fetus or neonate
24
Q
LINCOSAMIDES
ADVERSE EFFECTS:
A
- with caution in patients with hepatic or renal impairment,
- Use during pregnancy and lactation only if the benefit clearly outweighs the risk to the fetus or neonate
25
are semisynthetic derivatives of vancomycin
LIPOGLYCOPEPTIDES (TELEVANCIN)
26
They inhibit bacterial cell wall synthesis by interfering with the polymerization and cross-linking of peptidoglycans
LIPOGLYCOPEPTIDES (TELEVANCIN)
27
They bind to the bacterial membrane and disrupt the membrane barrier function causing bacterial cell death
LIPOGLYCOPEPTIDES (TELEVANCIN)
28
It is only approved for use in treating complicated skin and skin-structure infections in adults
LIPOGLYCOPEPTIDES (TELEVANCIN)
29
LIPOGLYCOPEPTIDES (TELEVANCIN)
PHARMACOKINETICS
- available as an IV drug only.
- It is rapidly absorbed with peak levels occurring at the end of the infusion.
- The drug is widely distributed, may cross the placenta, and may pass into breast milk.
- Its site of metabolism is not known; It has a half-life of 8 to 9 hours.
- It is excreted in the urine.
30
LIPOGLYCOPEPTIDES (TELEVANCIN)
CONTRAINDICATIONS AND CAUTIONS
- contraindicated with known allergy to any component of the drug
- Black Box Warning with pregnant and lactating patients
31
LIPOGLYCOPEPTIDES (TELEVANCIN)
ADVERSE EFFECTS:
- nausea, vomiting, taste alterations, diarrhea, loss of appetite, and risk of C. difficile diarrhea.
- Nephrotoxicity
- There is a risk of prolonged QTc interval.
- A transfusion reaction called red man syndrome with flushing, sweating, and hypotension can occur with rapid infusion.
- Infusion site reactions with pain and redness.
32
are antibiotics that interfere with protein synthesis.
MACROLIDES
33
Macrolides include
erythromycin (Ery-Tab, Eryc, and others), azithromycin (Zithromax), clarithromycin (Biaxin), and dirithromycin (Dynabac).
34
may be bactericidal or bacteriostatic, exert their effect by binding to the bacterial cell membrane and changing protein
MACROLIDES
35
MACROLIDES
PHARMACOKINETICS
- are widely distributed throughout the body; they cross the placenta and enter the breast milk
- absorbed in the GI tract
36
Erythromycin
PHARMACOKINETICS
metabolized in the liver, with excre tion mainly in the bile to feces
37
Azithromycin and clarithromycin
PHARMACOKINETICS
mainly excreted unchanged in the urine, making it necessary to monitor renal function
38
Dirithromycin
PHARMACOKINETICS
converted from the prodrug dirithromycin to erythromycylamine in the intestinal wall and excreted through the feces
39
MACROLIDES
CONTRAINDICATIONS AND CAUTIONS:
- contraindicated in patients with a known allergy to any macrolide
- Ocular preparations are contraindicated for viral, fungal, or mycobacterial infections of the eye
- Use with caution in patients with hepatic dysfunction,renal disease, pregnant and lactating women
40
MACROLIDES
ADVERSE EFFECTS:
- abdominal cramping, anorexia, diarrhea, vomiting, and pseudomembranous colitis.
- Other effects include neurological symptoms such as confusion, abnormal thinking, and uncontrollable emotions
- hypersensitivity reactions ranging from rash to anaphylaxis
- superinfections
41
structure is unique, and little cross-resistance occurs
aztreonam
42
It is effective against gram-negative enterobacteria and has no effect on grampositive or anaerobic bacteria.
MONOBACTAM (AZTREONAM)
43
disrupts bacterial cell wall synthesis, which promotes leakage of cellular contents and cell death in susceptible bacteria
MONOBACTAM (AZTREONAM)
44
The drug is indicated for th treatment of urinary tract, skin, intra-abdominal, and gynecological infections, as well as septicemia.
MONOBACTAM (AZTREONAM)
45
MONOBACTAM (AZTREONAM)
PHARMACOKINETICS
- Aztreonam is available for IV and IM use only
- half-life is 1.5 to 2 hours.
- The drug is excreted unchanged in the urine.
- It crosses the placenta and enters breast milk
46
MONOBACTAM (AZTREONAM)
CONTRAINDICATIONS AND CAUTIONS
- contraindicated with any known allergy to aztreonam.
- Use with caution in patients with a history of acute allergic reaction to penicillins or cephalosporins
- caution with renal or hepatic dysfunction and in pregnant and lactating women
47
MONOBACTAM (AZTREONAM)
ADVERSE EFFECTS
- The adverse effects associated are relatively mild.
- Local GI effects include nausea, GI upset, vomiting, and diarrhea.
- Hepatic enzyme elevations
- Other effects include inflammation, phlebitis, and discomfort at injection sites, as well as the potential for allergic response, including anaphylaxis.
48
An infection caused by a fungus is called a
mycosis
49
Fungi differ from bacteria in that the fungus has a _______________________ that is made up of _______________________________________ and a _________________that contains ___________________.
rigid cell wall; chitin and various polysaccharides; cell membrane; ergosterol
50
resistant to antibiotics
ANTI-FUNGAL AGENTS
51
a large group of antifungals used to treat systemic and topical fungal infections
AZOLE ANTIFUNGALS
52
AZOLE ANTIFUNGALS include
fluconazole (Diflucan), itraconazole (Sporanox), ketoconazole (Nizoral), posaconazole (Noxafi l), terbinafi ne (Lamisil), and voriconazole (Vfend)
53
bind to sterols and can cause cell death (a fungicidal effect) or interfere with cell replication (a fungistatic effect)
AZOLE ANTIFUNGALS
54
Ketoconazole
PHARMACOKINETICS
absorbed rapidly from the GI tract, and metabolized in the liver and excreted through the feces.
55
Fluconazole
PHARMACOKINETICS
reaches peak levels within 1 to 2 hours after administration, excreted unchanged in the urine.
56
Itraconazole
PHARMACOKINETICS
slowly absorbed from the GI tract and is metabolized in the liver, excreted in the urine and feces.
57
Posaconazole
PHARMACOKINETICS
given orally, has a rapid onset of action, metabolized in the liver and excreted in the feces
58
Terbinafine
PHARMACOKINETICS
rapidly absorbed from the GI tract, extensively metabolized in the liver, and excreted in the urine with a half-life of 36 hours.
59
Voriconazole
PHARMACOKINETICS
reaches peak levels in 1 to 2 hours if given orally, and metabolized in the liver with a half-life of 24 hours and is excreted in the urine.
60
AZOLE ANTIFUNGALS
CONTRAINDICATIONS AND CAUTIONS
- Contraindicated with patients with hepatic failure
- Use in caution for liver and renal impairment
- Should not be used in pregnancy and lactating mothers
61
AZOLE ANTIFUNGALS
ADVERSE EFFECTS:
- Many of the azoles are associated with liver toxicity
- can cause severe effects on a fetus or a nursing baby.
62
ECHINOCANDIN ANTIFUNGALS include
anidulafungin, caspofungin, and micafungin
63
work by inhibiting glucan synthesis.
ECHINOCANDIN ANTIFUNGALS
64
is an enzyme that is present in the fungal cell wall but not in human cell walls
Glucan
65
PHARMACOKINETICS
Anidulafungin
- is given as a daily IV infusion for at least 14 days.
- metabolized by degradation and excreted in the feces
66
Caspofungin
PHARMACOKINETICS
- is available for IV use.
- slowly metabolized in the liver and bound to protein and widely distributed throughout the body excreted through the urine.
67
PHARMACOKINETICS
Micafungin
- is an IV drug
- It has a rapid onset
- excreted in the urine
68
CONTRAINDICATIONS AND CAUTIONS:
Anidulafungin
- may cross the placenta and enter breast milk
- should not be used by pregnant or lactating women.
- Caution must be used in the presence of hepatic impairment
69
Caspofungin
CONTRAINDICATIONS AND CAUTIONS:
- can be toxic to the liver;
- embryotoxic in animal studies, great caution during pregnancy and lactation
70
Micafungin
CONTRAINDICATIONS AND CAUTIONS:
should be used during pregnancy and lactation only if the benefits clearly outweigh the risks.
71
ECHINOCANDIN ANTIFUNGALS
ADVERSE EFFECTS:
- hepatic toxicity
- Potentially serious hypersensitivity reactions
- bone marrow suppression
72
OTHER ANTIFUNGALS
amphotericin B (Abelcet, AmBisome, Amphotec), fl ucytosine (Ancobon), griseofulvin (generic), and nystatin (Mycostatin, Nilstat).
73
TOPICAL ANTIFUNGALS Examples:
ketoconazole ( Nizoral,), sertaconazole nitrate (Ertaczo),
sulconazole (Exelderm), terbinafine (Lamisil),
74
Fungi that cause mycoses
DERMATOPHYTES
75
mycoses include tinea infections such as
- athlete’s foot (tinea pedis),
- jock itch (tinea cruris),
- yeast infections of the mouth and vagina often caused by
Candida
76
work to alter the cell permeability of the fungus, causing prevention of replica and fungal death
TOPICAL ANTIFUNGALS
77
TOPICAL ANTIFUNGALS
PHARMACOKINETIC
These drugs are not absorbed systemically and do not undergo metabolism or excretion in the body.
78
TOPICAL ANTIFUNGALS
CONTRAINDICATIONS AND CAUTIONS
contraindications are limited to a known allergy to any of these drugs and open lesions
79
TOPICAL ANTIFUNGALS
ADVERSE EFFECTS
local effects include irritation, burning, rash, and swelling
80
single-celled organisms that pass through several stages in their life cycles
Protozoa
81
thrive in tropical climates, but may also survive and reproduce in any area where people live in very crowded and unsanitary conditions.
Protozoa
82
protozoal infections that can be caused by insect bites:
malaria
trypanosomiasis
leishmaniasis)
83
protozoal infections that result from ingestion
amebiasis
giardiasis
trichomoniasis
84
is a parasitic disease through the bite of a female Anopheles mosquito, an insect that harbors the protozoal parasite
MALARIA
85
FOUR PROTOZOAL PARASITES:
- Plasmodium falciparum
- Plasmodium vivax
- Plasmodium malariae
- Plasmodium ovale
86
is considered to be the most dangerous type of protozoan.
Plasmodium falciparum
87
causes a milder form of the disease, which seldom results in
death.
Plasmodium vivax
88
is endemic in many tropical countries and causes very mild signs and symptoms in the local population
Plasmodium malariae
89
which is rarely seen, seems to be in the process of being eradicated
Plasmodium ovale
90
are usually given in com bination form to attack the Plasmodium.
ANTI-MALARIALS
91
ANTI-MALARIALS drugs can be:
- schizonticidal
- gametocytocidal
- sporontocidal
- schizonts as prophylactic or antirelapse agents
92
-acting against the red-blood-cell phase of the life cycle
schizonticidal
93
acting against the gametocytes
gametocytocidal
94
acting against the parasites that are developing in the mosquito
sporontocidal
95
work against tissue
schizonts as prophylactic or antirelapse agents
96
is currently the mainstay of antimalarial therapy
Chloroquine
97
directly toxic to parasites that absorb it; it is acidic, and it decreases the ability of the parasite to synthesize DNA, leading to a blockage of reproduction.
Chloroquine
98
increases the acidity of plasmodial food vacuoles, causing cell rupture and death.
Primaquine
99
is used in combination to suppress malaria; it acts by blocking the use of folic acid in protein synthesis by the Plasmodium
Pyrimethamine
100
inhibits nucleic acid synthesis, protein synthesis, and glycolysis in P. falciparum.
Quinine
101
ANTI-MALARIALS
PHARMACOKINETIC
Generally metabolized in the liver
Excreted in the urine
102
ANTI-MALARIALS
CONTRAINDICATIONS AND CAUTIONS:
- allergy to any of these drugs;
- liver disease
- alcoholism
- lactation
- avoided during pregnancy
- Use caution in patients with retinal disease
103
ANTI-MALARIALS
ADVERSE EFFECTS
- Central nervous system (CNS) effects include headache and dizziness.
- Immune reaction effects related to the release of merozoites fever, shaking, chills, and malaise
- Nausea, vomiting,
- dyspepsia
- anorexia
- Hepatic dysfunction
- Dermatological effects include rash, pruritus, and loss of hair
- Cinchonism (nausea, vomiting, tinnitus, and vertigo) may occur with high levels of quinine or
primaquine.
104
an intestinal infection caused by Entamoeba histolytica, is often known as amebic dysentery
Amebiasis
105
Early signs of amebiasis include
mild to fulminate diarrhea
106
Two stages of Amebiasis:
- Cystic, dormant stage
- Trophozoite stage
107
the protozoan can live for long periods outside the body or in the human intestine
Cystic, dormant stage
108
in the ideal environment—the human large intestine
Trophozoite stage
109
is a disease caused by a protozoan that is passed from sand fl ies to humans
Leishmaniasis
110
fly injects an asexual form of this flagellated protozoan and digested by human macrophages.
promastigote
111
formed inside the macrophages as the promastigote divides
promastigote
112
can cause serious lesions in the skin, the viscera, or the mucous membranes of the host.
amastigotes
113
is caused by infection with Trypanosoma
Trypanosomiasis
114
caused by Trypanosoma brucei gambiense, (transmitted by the tsetse fly)
African sleeping sickness
115
invades the CNS, leading to an acute inflammation that results in lethargy, prolonged sleep, and even death.
African sleeping sickness
116
which is caused by Trypanosoma cruzi
Chagas’ disease
117
This protozoan results in a severe cardiomyopathy that accounts for numerous deaths and disabilities in South American regions.
Trypanosoma cruzi
118
is a common cause of vaginitis
Trichomonas vaginalis
119
caused by Trichomonas vaginalis
Trichomoniasis
120
This infection is usually spread during sexual intercourse
Trichomoniasis
121
In women, causes reddened, inflamed vaginal mucosa, itching, burning, and a yellowish-green discharge
Trichomoniasis
122
caused by Giardia lamblia, which survive outside the body and allow transmission through contaminated water or food, and trophozoites
Giardiasis
123
Diarrhea, rotten egg–smelling stool, and pale and mucus-filled stool are commonly seen.
Giardiasis
124
is an endemic protozoan that does not usually cause illness in humans.
Pneumocystis jiroveci i
125
immune system becomes suppressed because of acquired immune deficiency syndrome (AIDS) or AIDS-related complex
Pneumocystis jiroveci Pneumonia
126
Other antiprotozoals include
- atovaquone (Mepron)
- metronidazole (Flagyl, MetroGel, Noritate)
- nitazoxanide (Alinia)
- pentamidine (Pentam 300, NebuPent)
- tinidazole (Tindamax)
127
act to inhibit DNA synthesis in susceptible protozoa, interfering with the cell’s ability to reproduce, subsequently leading to cell death.
OTHER PROTOZOAL AGENTS
128
infections in the gastrointestinal (GI) tract or other tissues due to worm infestation
HELMINTHIC INFECTIONS
129
two types of HELMINTHIC INFECTIONS due to worm
infestation:
the nematodes (or roundworms)
the platyhelminths (or flatworms)
130
remain in intestine (Helminth Infections)
Pinworms
131
attach to wall of colon (Helminth Infections)
Whipworms
132
burrow into intestine; can enter lungs, liver, and other tissue
Threadworms
133
burrow into intestine; enter the blood and infect lungs
Ascaris
134
attach to the wall of the intestine
hookworms
135
live in the intestine, ingesting nutrients from the host
cestodes
136
TISSUE-INVADING WORM INFECTIONS
- Trichinosis
- Filariasis
- Schistosomiasis
137
is the disease caused by ingestion of the encysted larvae of the roundworm, Trichinella spiralis, in undercooked pork.
Trichinosis
138
They can penetrate skeletal muscle and can cause an inflammatory reaction in cardiac muscle and in the brain
Trichinosis
139
refers to infection of the blood and tissues of healthy individuals by worm embryos, which enter the body via insect bites.
Filariasis
140
This may lead to severe swelling of the hands, feet, legs, arms, scrotum, or breast—a condition called elephantiasis
Filariasis
141
is a platyhelminthic infection by a fluke that is carried by a snail
Schistosomiasis
142
severe infestation may lead to abdominal pain and diarrhea, as well as blockage of blood fl ow to areas of the liver, lungs, and CNS.
Schistosomiasis
143
act on metabolic pathways that are present in the invading worm but are absent or significantly different in the human host.
ANTI-HELMINTHIC DRUGS
144
ANTI-HELMINTHIC DRUGS
- albendazole (Albenza)
- ivermectin (Stromectol)
- mebendazole (Vermox)
- praziquantel (Biltricide)
- pyrantel (Antiminth, Pin-Rid, Pin-X, Reese’s Pinworm)
145
PHARMACOKINETIC
Mebendazole
is not metabolized in the body, and most of it is excreted unchanged in the
feces. A small amount may be excreted in the urine
146
Albendazole
PHARMACOKINETIC
is poorly absorbed from the GI tract and metabolized in the liver and primarily excreted in urine
147
Ivermectin
PHARMACOKINETIC
readily absorbed from the GI tract. metabolized in the liver and excretion is through the feces
148
Praziquantel
PHARMACOKINETIC
rapidly absorbed from the GI tract,metabolized in the liver and excretion through the urine
149
Pyrantel
PHARMACOKINETIC
poorly absorbed, and most of the drug is excreted unchanged in the feces and some found in the urine
150
ANTI-HELMINTHIC DRUGS
CONTRAINDICATIONS AND CAUTIONS
- known allergy to any of these drugs
- Pregnancy and lactation-Women of childbearing age should be advised to use barrier contraceptives while taking these drugs.
- Pyrantel has not been established as safe for use in children younger than 2 years
- Use caution in the presence of renal or hepatic disease
151
ANTI-HELMINTIC DRUGS
ADVERSE EFFECTS
- abdominal discomfort, diarrhea, or pain
- headache and dizziness; fever, shaking, chills, and malaise
- Renal failure and severe bone marrow depression are associated with albendazole
152
- particle is composed of a piece of DNA or RNA inside a protein.
- replicates in the host cell.
Virus
153
act to prevent the replication of that particular virus.
Interferons
154
invade the respiratory tract and cause the signs and symptoms of respiratory “flu.
Influenza A, B and RSV
155
Agents for Influenza A and Respiratory Viruses
- amantadine
- oseltamivir
- ribavirin
- rimantadine
- zanamivir
156
is the only antiviral agent that is effective in treating H1N1 and avian flu.
Oseltamivir
157
AGENTS FOR INFLUENZA A AND RESPIRATORY VIRUSES
Pharmacokinetics
Generally absorbed in the GI and excreted through urine.
158
AGENTS FOR INFLUENZA A AND RESPIRATORY VIRUSES
Contraindications and Cautions:
- with caution in patients who have any renal impairment
- Embryotoxic - should be used during pregnancy and lactation only if the benefi ts clearly outweigh the risks to the fetus or neonate.
159
AGENTS FOR INFLUENZA A AND RESPIRATORY VIRUSES
Adverse Effects:
- light-headedness
- dizziness, and insomnia
- nausea
- orthostatic hypotension
- urinary retention
160
account for a broad range of conditions: cold sores, encephalitis,shingles,genital infections
Herpes viruses
161
Herpes viruses account for a broad range of conditions:
cold sores, encephalitis,shingles,genital infections
162
different since it can affect the eye, respiratory tract, and liver and reacts to many of the same drug.
Cytomegalovirus (CMV)
163
AGENTS FOR HERPES AND CYTOMEGALOVIRUS examples
acyclovir (Zovirax), cidofovir (Vistide), famciclovir (Famvir), foscarnet (Foscavir), ganciclovir (Cytovene), valacyclovir (Valtrex), and valganciclovir (Valcyte)
164
AGENTS FOR HERPES AND CYTOMEGALOVIRUS
Pharmacokinetics
- Most of the agents are readily absorbed and excreted through the kidney and remained unchained in the urine
- It crosses into breast milk
165
AGENTS FOR HERPES AND CYTOMEGALOVIRUS
Adverse Effects
- nausea and vomiting
- headache,
- depression
- paresthesias,
- neuropathy,
- rash
- hair loss
- Renal dysfunction and renal failure
166
attacks the helper T cells (CD4 cells) within the immune system.
human immunodeficiency virus (HIV)
167
The human immunodeficiency virus (HIV) attacks the __________________________________________ within the immune system.
helper T cells (CD4 cells)
168
causes acquired immune deficiency syndrome (AIDS) and AIDSrelated complex (ARC), diseases that are characterized by the emergence of a variety of opportunistic infections and cancers.
human immunodeficiency virus (HIV)
169
AGENTS FOR HIV AND AIDS
NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS Includes:
delavirdine (Rescriptor), efavirenz (Sustiva), etravirine (Intelence), and nevirapine (Viramune) and rilpivirine (Edurant)
170
They prevent the transfer of information that would allow the virus to carry on the formation of viral DNA. As a result, the virus is unable to take over the cell and reproduce
NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
171
NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
Pharmacokinetics
- generally absorbed directly in the GI tract
- metabolized in the liver
- Excreted through feces and urine
172
NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
Contraindications and Cautions
- There are no adequate studies of nonnucleoside reverse transcriptase inhibitors in pregnancy,
-use should be limited to situations in which the benefi ts clearly outweigh any risks.
173
NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
Contraindications and Cautions
- There are no adequate studies of nonnucleoside reverse transcriptase inhibitors in pregnancy,
-use should be limited to situations in which the benefi ts clearly outweigh any risks.
174
NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
Adverse Effects
- GI related—dry mouth, constipation or diarrhea, nausea, abdominal pain, and dyspepsia.
- Dizziness, blurred vision, and headache
- A flu-like syndrome of fever, muscle aches and pains, fatigue, and loss of appetite
175
NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS include the following agents:
abacavir (Ziagen), didanosine (Videx), emtricitabine (Emtriva), lamivudine (Epivir), stavudine (Zerit XR), tenofovir (Viread), and zidovudine (Retrovir).
176
compete with the naturally occurring nucleosides within the cell that the virus would use to build the DNA chain. chain cannot lengthen and cannot insert and cannot reproduce.
NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
177
NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
Pharmacokinetics
- Generally absorbed in the GI tract
- Metabolized in the liver
- Excreted in the urine and feces
178
is the only agent that has been proven to be safe when used during pregnancy and caution if with bone marrow supression
zidovudine
179
used with caution in the presence of hepatic dysfunction or severe renal impairment
Tenofovir, zidovudine, and emtricitabine
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NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
Adverse Effects
- Serious-to-fatal hypersensitivity reactions (fever, chills, rash, fatigue, GI upset, flu-like symptoms)
- Serious pancreatitis, hepatomegaly, and neurological problem
- Severe hepatomegaly with steatosis
- Severe bone marrow suppression
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PROTEASE INHIBITORS include:
atazanavir (Reyataz), darunavir (Prezista). fosamprenavir (Lexiva), indinavir (Crixivan), lopinavir (Kaletra), nelfi navir (Viracept), ritonavir (Norvir), saquinavir (Fortovase), and tipranavir (Aptivus).
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block protease activity within the HIV virus
PROTEASE INHIBITORS
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is essential for the maturation of an infectious virus; without it, an HIV is immature and noninfective.
Protease
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PROTEASE INHIBITORS
Pharmacokinetics
- Generally absorbed in the GI tract
- Metabolized in the liver
- Excreted in the urine and feces
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PROTEASE INHIBITORS
ontraindications and Cautions
- use during pregnancy should be limited
- limited to situations in which the benefi ts clearly outweigh any risks
- Use in caution with Hepatic Dysfunction
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PROTEASE INHIBITORS
Adverse Effects
- GI effects, including nausea, vomiting, diarrhea, anorexia, and changes in liver function
- Elevated cholesterol and triglyceride levels
- Rashes, pruritus, and the potentially fatal Steven–Johnson syndrome
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- intended to target the abnormal cells that compose the neoplasm or cancer
- unfortunately, normal cells also are affected
ANTINEOPLASTIC AGENTS
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start with a single cell that is genetically different from the other cells in the surrounding tissue. eventually producing a tumor or neoplasm .
Cancer
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2 TYPES OF CANCER:
SARCOMA
CARCINOMA
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originated from mesenchyme and are made up of embryonic connective tissue cells
SARCOMA
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originated from epithelial cells
CARCINOMA
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ALKYLATING AGENTS include:
altretamine (Hexalen), bendamustine (Treanda), busulfan (Busulfex, Myleran), carboplatin (Paraplatin), carmustine (BiCNU, Gliadel), chlorambucil (Leukeran), cisplatin (Platinol-AQ), cyclophosphamide (Cytoxan, Neosar)
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produce their cytotoxic effects by reacting chemically with portions of the RNA, DNA, or other cellular proteins, most potent when they bind with cellular DNA
ALKYLATING AGENTS
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These drugs are most useful in the treatment of slow-growing cancers such as various lymphomas, leukemias, myelomas, some ovarian, testicular, and breast Cancer
ALKYLATING AGENTS
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ALKYLATING AGENTS
Pharmacokinetics
- They are metabolized and sometimes activated in the liver.
- Excreted in the urine.
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ALKYLATING AGENTS
Contraindications and Cautions
- contraindicated during pregnancy and lactation
Caution to any individual with:
- known allergy to any of them;
- with bone marrow suppression
- with suppressed renal or hepatic function
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ALKYLATING AGENTS
Adverse Effects
- Hematological effects include bone marrow suppression, with leukopenia, thrombocytopenia, anemia, and pancytopenia.
- GI effects include nausea, vomiting, anorexia, diarrhea, and mucous membrane deterioration
- Hepatic toxicity and renal toxicity
- Alopecia, or hair loss
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ANTIMETABOLITES include
capecitabine (Xeloda), cladribine (Leustatin), clofarabine (Clolar), cytarabine (DepoCyt, Tarabine PFS), fl oxuridine (FUDR), fl udara bine (Fludara), fluorouracil (Adrucil, Carac, Efudex, Fluoroplex), gemcitabine (Gemzar), mercaptopurine (Purinethol), methotrexate (Rheumatrex, Trexall)
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inhibit DNA production in cells that depend on certain natural metabolites toproduce their DNA
ANTIMETABOLITES
200
most effective in rapidly dividing cells, preventing cell replication, and leadingto cell death
ANTIMETABOLITES
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ANTIMETABOLITES
Pharmacokinetics
- Generally absorbed in the GI tract
- Metabolized in the liver
- Excreted in the urine and feces
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ANTIMETABOLITES
Contraindications and Cautions
- contraindicated during pregnancy and lactation
Caution is necessary to any individual with:
- known allergy
- bone marrow suppression
- with renal or hepatic dysfunction
- with known GI ulcerations or ulcerative diseases
203
ANTIMETABOLITES
Adverse Effects
- Hematological effects include bone marrow suppres sion, with leukopenia, thrombocytopenia, anemia, and pancytopenia,
- Toxic GI effects include nausea, vomiting, anorexia, diarrhea, and mucous membrane deterioration
- CNS effects include headache, drowsiness, aphasia, fatigue, malaise, and dizziness.
- possible hepatic or renal toxicity,
- Alopecia
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ANTINEOPLASTIC ANTIBIOTICS include:
bleomycin (Blenoxane), dactinomycin (Cosmegen), dau norubicin (DaunoXome), doxorubicin (Adriamycin, Doxil), epirubicin (Ellence), idarubicin (Idamycin), mitomycin (Mutamycin), mitoxantrone (Novantrone), and valrubicin (Valstar)
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break up DNA links, and others prevent DNA synthesis
ANTINEOPLASTIC ANTIBIOTICS
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are cytotoxic and interfere with cellular DNA synthesis by insert ing themselves between base pairs in the DNA chain
ANTINEOPLASTIC ANTIBIOTICS
207
ANTINEOPLASTIC ANTIBIOTICS
Pharmacokinetics
- Generally absorbed in the GI tract
- Metabolized in the liver
- Excreted in the urine and feces
208
ANTINEOPLASTIC ANTIBIOTICS
Adverse Effects
- bone marrow suppression
- leukopenia, thrombocytopenia, anemia, and pancytopenia
- Toxic GI effects include nausea, vomiting, anorexia, diarrhea, and mucous membrane deterioration
- renal or hepatic toxicity
- Alopecia
209
MITOTIC INHIBITORS include
cabazitaxel (Jevtana), docetaxel (Taxotere), etoposide (Toposar, VePesid), ixabepilone (Ixempra), paclitaxel (Abraxane, Onxol, Taxol), teniposide (Vumon), vinblastine (Velban), vincristine (Oncovin, Vincasar), and vinorelbine (Navelbine)
210
interfere with the ability of a cell to divide; they block or alter DNA synthesis, thus causing cell death
MITOTIC INHIBITORS
211
are used for the treatment of a variety of tumors and leukemias
MITOTIC INHIBITORS
212
MITOTIC INHIBITORS
Pharmacokinetics
- Generally, these drugs are given intravenously because they are not well absorbed from the GI tract
- metabolized in the liver
- excreted primarily in the feces
- safer for use in patients with renal impairment
213
MITOTIC INHIBITORS
Pharmacokinetics
- Generally, given intravenously because they are not well absorbed from the GI tract
- metabolized in the liver
- excreted primarily in the feces
- safer for use in patients with renal impairment
214
MITOTIC INHIBITORS
Contraindications and Cautions
- should not be used during pregnancy or lactation
Use caution when giving to anyone with:
- known allergy to the drug or related drugs
- bone marrow suppression
- renal or hepatic dysfunction
- known GI ulcerations or ulcerative diseases
215
MITOTIC INHIBITORS
Adverse Effect
- bone marrow suppression
- leukopenia, thrombocytopenia, anemia, and pancytopenia
- GI effects include nausea, vomiting, anorexia, diarrhea, and mucous membrane deterioration
- Alopecia
- necrosis and cellulitis if extravasation occurs
216
HORMONES AND HORMONE MODULATORS include
anastrazole (Arimidex), bicalutamide (Casodex), degarelix (Degarelix for Injection), estramustine (Emcyt), exemestane (Aromasin), fl utamide (generic), fulvestrant (Faslodex), goserelin (Zoladex), histrelin (Vantas), letrozole (Femara), megestrol (Megace)
217
are receptor-site specific or hormone specific to block the stimulation of growing cancer cells that are sensitive to the presence of that hormone
HORMONES AND HORMONE MODULATORS
218
indicated for the treatment of breast cancer in postmenopausal women or in other women without ovarian function and some for prostatic cancers.
HORMONES AND HORMONE MODULATORS
219
HORMONES AND HORMONE MODULATORS
Pharmacokinetics
- readily absorbed from the GI tract
- metabolized in the liver
- excreted in the urine.
220
HORMONES AND HORMONE MODULATORS
Contraindications and Cautions
- contraindicated during pregnancy and lactation
- Hypercalcemia is a contraindication to the use of toremifene
Use caution when giving to an individual with:
- known allergy to any of these drugs
- bone marrow suppression
- with renal or hepatic dysfunction
221
HORMONES AND HORMONE MODULATORS
Adverse Effects
- Menopause-associated effects include hot fl ashes, vaginal spotting, vaginal dry ness, moodiness, and depression.
- bone marrow suppression
- GI toxicity, including hepatic dysfunction.
- Hypercalcemia d/t blockage of estrogen needed for calcium deposition
- increase the risk for cardiovascular disease
221
3 GROUPS OF DRUGS AVAILABLE )ANCER CELL–SPECIFIC AGENTS)
1. protein tyrosine kinase inhibitors
2. an epidermal growth factor inhibitor
3. a proteasome inhibitor
222
no devastating effects on healthy cells in the body and would be more effective against particular cancer cells.
CANCER CELL–SPECIFIC AGENTS
223
act on specific enzymes that are needed for protein building by specific tumor cells and blocking of these enzymes inhibits tumor cell growth and division
PROTEIN TYROSINE KINASE INHIBITORS
224
PROTEIN TYROSINE KINASE INHIBITORS include
include everolimus (Afinitor), gefitinib (Iressa), imatinib (Gleevec), lapatinib (Tykerb), nilotinib (Tasigna), pazopanib (Vorient), sorafenib (Nexavar), sunitinib (Sutent), and temsirolimus (Torisel).
225
for chronic myelocytic leukemia (CML).
PROTEIN TYROSINE KINASE INHIBITORS
226
PROTEIN TYROSINE KINASE INHIBITORS
Pharmacokinetics
- Slowly absorbed by the GI
- Metabolized by the liver
- excreted through the feces
227
PROTEIN TYROSINE KINASE INHIBITORS
Contraindications and Cautions
- All of these drugs are in pregnancy category D.
- Women of childbearing age should be advised to use barrier contraceptives while taking this drug.
- only if the benefits to the mother clearly outweigh the risks to the baby
- contraindicated with patients who have or who are at risk for prolonged QT intervals (hypokalemia, hypomagnesia,)
