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Summary Mid-term study guide
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This is a mid-term study guide for NPs taking advanced pharmacology
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Mid Term Study Guide NR 566Chapter 79: Antifungal agents
Itraconazole (Sporanox) drug interactions: Food increases absorption of
capsules but decreases absorption of suspension. Administration with
cola enhances absorption. Itraconazole inhibits CYP3A4 (the 3A4
isoenzyme of cytochrome P450) thus it can increase levels of other
drugs: cisapride, pimozide, dofetilide, and quinidine- when present at
high levels pts can have fatal ventricular dysrhythmias.
Cyclosporine, digoxin, warfarin, and sulfonylurea-type oral
hypoglycemics are other drugs of concern. (p 716-717)
Therapeutic uses of Caspofungin: Antifungal that inhibits biosynthesis
of B1,3-d glucan, an essential component of the cell wall of some fungi
including Aspergillus and Candida. It’s approved for treating invasive
aspergillosis and systemic Candida candida related esophagitis,
peritonitis, pleural space infections, and intraabdominal abscesses. (p
718)
Griseofulvin Indications: Administered orally to treat dermatophytic
infections of the hair, skin, and nails. Dermatophytic infections respond
relatively quickly (3-8 weeks), infections of the palms may require 2-3
months of treatment and a year or more may be needed to eliminate
toenail infections. (p 721)
Oral terbinafine Indications: Highly active against dermatophytes
and less active against Candida species. Oral therapy is used for
ringworm and onychomoses (fungal infection of the nails). (p 721-22)
Azole use in older adults: Azoles inhibit hepatic cytochrome P450
drug metabolizing enzymes and can increase levels of other drugs.
Avoid use with drugs metabolized by CYP3A4 (warfarin, cyclosporine,
digoxin). Older adults have a higher risk of achlorhydria than do
younger individuals and may not predictably absorb some antifungal
agents. In addition, common drugs prescribed to prescribed to older
adults including warfarin, phenytoin, and oral hypoglycemic agents,
and increased by azoles. (p 718)
Pharmacokinetics of Amphotericin B: Poorly absorbed through GI
tract so oral therapy cannot be used for systemic infection. Must be
given IV; when drug leaves vascular system it undergoes extensive
binding to sterol-containing membranes of tissues. Ampho B does not
readily penetrate to CSF. (p 715)
Treatment Choice for systemic mycoses: AmphoB (polyene
antibiotics), Azoles (fluconazole, Itraconazole, Ketoconazole),
Echinocandins (Anidulafungin, Capsofungin, Pyrimidine analogs
(Flucytosine) (p 716)
Drug Interaction with Itraconazole: Itraconazole inhibits
CYP3A4 (the 3A4 isoenzyme of cytochrome P450) thus it can increase
1
, levels of other drugs: cisapride, pimozide, dofetilide, and quinidine-
when present at high levels pts can have fatal ventricular
dysrhythmias. Cyclosporine, digoxin, warfarin, and sulfonylurea-type
oral hypoglycemics are other drugs of concern. (p 716-717)
Adverse effects of Caspofungin: Fever and phlebitis at injection
site. Less common are headache, rash, nausea, vomiting. Caspofungin
can cause affects related to histamine release ie: facial flushing, rash,
pruritus and a sense of warmth.
Tinea Pedis Treatment: Tolnaftate (Tinactin) or other topical
treatments (p 720)
Ampho B: Minimizing nephrotoxicity Total dose greater than 4gm
leads to residual kidney impairment. Kidney damage can be minimized
by infusing 1L NS on days AmphoB is given. Other nephrotoxic drugs
should be avoided. Monitor renal function Q 3-4 days. If plasma
creatinine rises above 3.5mL/dL amphoB dose should be reduced.
Chapter 80
Oseltamivir (Tamiflu) MOA: Antiviral effects derive from inhibiting
neuraminidase, a viral enzyme required for replication. As a result of
neuraminidase inhibition, newly formed viral particles are unable to bud off
from the cytoplasmic membrane of infected host cells. Hence, viral spread is
stopped. (p 742)
Oseltamivir (Tamiflu) Administration: oral med that can provide some
protection for those who haven’t had flu shot. Dosing should begin no more
than 2 days after onset of symptoms. Benefits decline when treatment is
delayed. When treatment is started w/in 12 hours of symptoms, duration is
reduced by more than 3 days; duration is reduced by less than 2 days if
treatment started within 24 hours of symptoms. (p 742)
Oseltamivir (Tamiflu) Indications: Candidates for prophylactic therapy
include family members of those with the flu and residents of nursing homes.
To protect family members dosing should begin within 48 hrs of exposure
and should continue for 10 days. To protect residents of nursing homes or
high-risk members of the community at large, dosing can be done
continuously for up to 42 days. (p 742)
Acyclovir- Route of administration considerations: Can be
administered topically, orally, or intravenously. Oral bioavailability is low,
ranging from 15-30%. No significant absorption occurs with topical use. With
normal kidney function, the half-life of acyclovir of 2.5 hours., the half-life is
prolonged by renal impairment reaching 20 hours in anuric patients so
dosages should be reduced in pts with renal impairment (p 723)
2
, Purpose of annual flu vaccine: annual vaccine is the best protection
against flu since the influenza viruses continuously change (p 740)
Flu vaccine contraindications: Pregnant women should not receive the
live vaccine, they should get the inactivated vaccine. One contraindication is
noted- severe allergic reaction to the flu vaccine or vaccine component. A
precaution is use in a pt that has had a moderate to severe acute illness at
the time of vaccination. (p 741)
Palivizumab (Synagis) indications: Palivizumab is a monoclonal antibody
indicated for prevention of RSV infection in premature infants and in young
children with chronic lung disease. (p 743)
Acyclovir indication: It is the agent of first choice for most infections
caused by HSV and VZV.
Acyclovir MOA: Inhibits viral replication by suppressing the synthesis of
viral DNA. To exert antiviral effects, acyclovir must first undergo activation.
The critical step in activation is conversion of acyclovir to acyclo-guanosine
monophosphate (GMP) by thymidine kinase. When formed acyclo-GMP is
converted to acyclo-guanosine triphosphate (GTP), the compound directly
responsible for inhibiting DNA synthesis. Acyclo-GTP suppresses DNA
synthesis by 1) inhibiting viral DNA polymerase and 2) becoming
incorporated into the growing strand of viral DNA, which blocks further
strand growth. HSV is especially sensitive to acyclovir. CMV is inherently
resistant to the drug because acyclovir is a poor substrate for the form of
thymidine kinase produced by this virus. (p 723)
Ch 81- Antiviral Agents II: Drugs for HIV
Infection
Protease inhibitors (PIs)- Adverse effects: Hyperglycemia, development
of diabetes, lipodystrophy (fat redistribution) elevation of serum
transaminases and decreased cardiac conduction velocity. They can also
increase bleeding in pts with hemophilia Hyperglycemia/diabetes typically
occurs after 2 months of treatment but can happen earlier. Hyperglycemia
can be controlled with insulin and oral antidiabetic agents (ex: metformin) (p
753).
Integrase Strand Transfer Inhibitors (INSTIs) MOA: target HIV by
terminating the integration of HIV into DNA. Integrase is one of three viral
enzymes needed for HIV replication. Integrase inserts HIV genetic material
into the DNA of CD4 cells. By inhibiting integrase, these drugs prevent
insertion of HIV DNA and thereby stop HIV replication. Integrase inhibitors
are combined with other antiretroviral agents to treat adults infected with
HIV-1(p 756)
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