Chapter 8 Pharmacology
with antiviral agents, to kill the virus, often the ____ must also be harmed
the host cell must also be harmed.
Penciclovir is available
topically
How is anti viral agent Docosanol 10% available
topically and without a prescription
what is often required for toxicity of AZT Zidovudine
transfusions
what is optimal duration of therapy for nucleoside/nucleotide analogs?
unknown, but at least 5 years and some are treated indefinitely
which form of nystatin contains no sugar and may be ideal for patients with diabetes
vaginal tablets
when is hepatitis considered chronic
when it lasts more than 6 months
With Herpes Simplex, most anti viral agents are either ____ or _____ analogs to inhibit ____ synthesis.
with herpes simplex most anti viral agents are either purine or pyrimidine analogs to inhibit DNA synthesis
name of the nucleoside/nucleotide reverse transcriptase inhibitor drug
zidovudine (AZT)
how does zidovudine (AZT) affect cells already containing HIV?
zidovudine does not effect cells already containing HIV
zidovudine is well absorbed ____. Metabolized by the ____ and excreted by ____
zidovudine is well absorbed orally, metabolized by the liver and excreted by the kidneys
zidovudine (AZT) terminates synthesis of viral ____ and inhibits _____ synthesis
zidovudine terminates synthesis of viral DNA and inhibits HIV synthesis.
patients should take saquinavir __ hours after a full meal and should avoid ____
take saquinavir 2 hours after a full meal and avoid sunlight
Nevirapine inhibit the same enzymes as the _____ analogs
nevirapine inhibit the same enzymes as the nucleoside analogs.
Nevirapine is specific for?
nevirapine is specific for HIV-1
does acyclovir prevent transmission and recurrence of infection?
no
How is the absorption of Nystatin and how is it excreted?
not absorbed from mucous membranes or intact skin. Poorly absorbed from GI tract. When taken orally, it is not absorbed, it is excreted unchanged in the feces.
acyclovir is not effective in treatment of ______ but still used extensively.
not effective treating herpes labialis
what are normally the three drugs used in HAART
nucleoside, non-nucleoside reverse transcriptase inhibitor, and a protease inhibitor
what 4 antifungal agents is candida albicans managed with?
nystatin, clotrimazole, ketoconazole, fluconazole
ketonazole is only available in form of
oral tablets
how are interferons used?
parenterally
what advantages (2) does penciclovir have over acyclovir
penciclovir achieves higher concentration within the cell penciclovir remains in the cells longer
penciclovir can reduce both ____ of the lesion and ____ of the lesions on the lips and face
penciclovir can reduce both duration of the lesion and pain of the lesions on the lips and face
with extended use of Ketonazole, patients should have periodic ______ function tests.
periodic liver function tests
Protease inhibitors , Boceprevir and telaprevir are used in combination with?
previous drugs for treatment of chronic Hepatitis C
what can sudden discontinuation of nucleoside/nucleotide analogs cause?
rapid increase in HEP B virus DNA levels and a severe flare up of the disease that can be fatal
what do famciclovir and valacyclovir treat
recurrent episodes of genital herpes acute localized varicella-zoster infection
when used alone, nonnucleoside reverse transcriptase inhibitors such as nevirapine, resistance to them develops _____, and they are often combined with the _____ analogs and the ______ inhibitors.
resistance develops quickly; they are often combined with the nucleoside analogs and protease inhibitors.
What forms is Nystatin available in?
rinse and expectorated, pastilles, vaginal tablet, cream.
Saquinavir prevents maturation of _____ infected cells
saquinavir prevents maturation of HIV infected cells
in what forms is Clotrimazole available
slow dissolving sugar containing lozenge and OTC cream
mechanism of ketonazole is to alter membrane permeability and inhibit _____ transport.
alter membrane permeability and inhibit purine transport
the OTC cream of Clotrimazole is applied to skin or _____ canal to treat denture _____.
applied to skin or vaginal canal to treat denture stomatitis.
The rinse and expectorated form of Nystatin, is a ______ suspension, containing ____% sucrose
aqueous suspension containing 50% sucrose
nucleoside/nucleotide analogs are better tolerated and have better rates of ____ suppression than _____
better rates of virologic suppression than interferons
what is the mechanism of action of clotrimazole?
binds to fungal cell membrane, alters permeability of the cell membrane
name the two protease inhibitors
boceprevir telaprevir
Toxicity of zidovudine (AZT) can be _____ depression leading to anemia, granulocytopenia, and thrombocytopenia
bone marrow depression
with the slow dissolving sugar lozenge of clotrimazole, drug is bound to the _____ mucosa and slowly released. Patients with ____ may have difficulty dissolving this product.
bound to oral mucosa; patients with xerostomia my have trouble dissolving.
adverse reaction to topical administration of acyclovir?
burning, stinging, itching, rash, mild pain
what is the most common oral fungus?
candida albicans
what are the two common fungal and viral infections in the dental office?
candida albicans and Herpes simplex virus
Agents that alter the amount of _____ acid could reduce absorption of ketonazole. What are the name of the agents that alter stomach acid?
stomach acid. These agents that alter stomach acid re H2 receptor blockers, H+ pump inhibitors, anticholinergic agents, antacids.
What is another way the aqueous suspension of Nystatin can be taken
frozen and used as popsicle
how long does it take for pastilles to dissolve? Pastilles allow to bathe lesions in the antifungal agent for a longer period than with the aqueous solution of Nystatin.
15 minutes
Clotrimazole produced elevated liver enzymes in ___ % patients
15% patients had elevated liver enzymes.
atleast ___ hours should elapse between the ingestion of agents that reduce stomach acid and the administration of ketonazole.
2 hours
Vaginal tablets of Nystatin are for use in vaginal infections. Occasionally they are used orally and dissolved in the mouth ____ times daily which allows the drug to remain in contact with the infected oral mucosa.
4 times daily
how many nucleoside/nucleotide analogs are currently available for treatment of chronic hepatitis B?
5
name for chronic disease produced by retrovirus human immunodeficiency virus
AIDS- Acquired Immunodeficiency Syndrome
what two drugs inhibit the metabolism of AZT and potentiate the toxicity
Acetaminophen, and aspirin
What anti viral agent is less toxic to uninfected cells because it is preferentially taken up by infected cells
Acyclovir
How often do adverse reactions to Nystatin occur? High doses of Nystatin will cause? How often are hypersensitivity reactions to Nystatin?
Adverse reactions to Nystatin are minor and infrequent. High doses of Nystatin cause nausea, vomiting, diarrhea Hypersensitivity reactions to Nystatin are rare.
drug name for protease inhibitor
Saquinavir
most frequent adverse reaction with ketonazole
nausea and vomiting
adverse reactions to nonnucleoside reverse transcriptase inhibitors ( nevirapine) ? (4)
CNS: headache, drowsy Rash GI effects: diarrhea, nausea Elevated Liver Function Test values.
what are the other acyclovir adverse effects from oral administration
CNS: vertigo, dizzy, insomnia, irritable, mental depression GI: nausea , vomiting, diarrhea Acne, hair loss, arthralgia, fever, menstrual abnormality, sore throat
What is the name for the synthetic anti fungal agent for the local treatment of oropharyngeal candidiasis (oral thrush)
Clotrimazole
Famciclovir and Valacyclovir are anti viral agents and pro drugs; Famciclovir is converted to? Valacyclovir is converted to?
Famciclovir is converted to penciclovir Valacyclovir is converted to acyclovir
what is the mechanism of action of fluconazole? to inhibit fungal _______ enzymes and prevent synthesis of ____ in the fungal cell membranes.
Fluconazole inhibits fungal CYP-450 enzymes and prevents synthesis of ergosterol in the fungal cell membranes.
what is the most common adverse reaction with Clotrimazole?
GI tract (abdominal pain, diarrhea, nausea)
HAART is the combination of several different classes of ______ drugs and can do what to the rate of replication of HIV?
HAART is combination of several different classes of anti-retroviral drugs and slows rate of HIV replication
how is HIV 2 different from HIV 1?
HIV2 is transmitted from a woman to child while child is in the womb. HIV1 is transmitted during sex, sharing bodily fluids, and IV substance abuse, and during pregnancy/childbirth
oral administration of acyclovir adverse effects... most common?
Headache is most common
what are the most common causes of chronic hepatitis, accounting for almost two thirds of all hepatitis cases?
Hepatitis B and C
People with hepatitis ___ are most at risk for developing chronic hepatitis
Hepatitis C patients are most at risk for developing chronic hepatitis
Zidovudine (AZT) toxicity can cause CNS effects , as well as _______ that occurs in almost half the patients.
nausea occurs in almost half the patients with AZT toxicity
name for anti fungal agent used for treatment and management of mucocutaneous and oral pharyngeal candidiasis
Ketoconazole
What is the name of the nonnucleoside reverse transcriptase inhibitor
Nevirapine
is there any harm if the aqueous suspension of Nystatin is swallowed? It will not eradicate ______ candidiasis either.
No harm if nystatin swallowed- it is not absorbed. It will not eradicate pharyngeal candidiasis either.
_______ interfere with action of HIV infected cells while _____ prevent maturation of HIV infected cells.
Nuceloside/Nucleotide reverse transcriptase inhibitors and Non nucleoside reverse transcriptase inhibitors interfere with action of HIV cells while Protease inhibitors prevent maturation of HIV infected cells.
what is the first class of drugs developed to treat HIV
Nucleoside/Nucleotide Reverse Transcriptase Inhibitor
What is the name of the prescription anti-fungal agent produces by Streptomyces noursei, and that is used for both treatment and prevention of oral candidiasis
Nystatin
sugar content is a must that diabetics take into account if they swallow the suspension of _____
Nystatin
Acyclovir has anti viral action against... ( 5)
Simplex types 1 and 2 Varicella-zoster Epstein-Barr Herpes simiae (B Virus) Cytomegalovirus
what can occur at interferon injection site
necrosis
adverse reactions for saquinavir
Rash, hyperglycemia, parasthesis GI: pain, diarrhea, vomiting, buccal mucosa ulceration
when taken orally, Acyclovir is absorbed between ___ and ____% Does food affect absorption of acyclovir?
acyclovir is 15%-30% absorbed when taken orally. no food does not affect acycolvir
absorption of ketonazole requires an ____ environment for dissolution and absorption,
acidic environement to absorb ketonazole
what are the antiviral agents (5)
acyclovir docosanol penciclovir famciclovir and valacyclovir
zidovudine is distributed to most body tissue, including ______ fluid
cerebrospinal fluid
clotrimazole is not recommended in pregnant women or children younger than?
children younger than 3
cream form of nystatin is used on the tissue area surrounding _____. To treat _____ ______.
cream form of nystatin is used on the tissue area surrounding dentures. To treat denture stomatitis.
Docosanol 10% decreases healing time in patients with reccurent ______ herpes when started within ___ hours of the appearance of prodromal symptoms
docosanol 10% decrease healing time in patients with recurrent orolabial herpes when started within 12 hours of the appearance of prodromal symptoms.
what is the oral antifungal agent used to treat oropharyngeal and esophageal candidiasis, serious systemic candida infection, vaginal candidiasis, and candidial infections that do not respond to other agents. Also used prophylactically in immunocompromised patients.
fluconazole
most serious adverse reaction with Ketonazole
hepatotoxicity
oral use of acyclovir treats ______ with unimpressive results
herpes labialis with unimpressive results
what virus has the most interest to the dental worker
herpes virus
Nystatin's mechanism of action is to bind to the fungal cell membrane, _______ membrane permeability, and allows leakage of ____ and other essential cellular constituents.
increase membrane permeability; allow leakage of potassium
how does ketonazole affect anti coagulant warfarin?
increase warfarin blood levels and increase bleeding risk.
what has FDA approved for treating chronic hepatitis B and hepatitis C?
interferon-a
what are endogenous proteins with antiviral, cytotoxic, and immunomodulating action
interferons
what does chronic hepatitis usually lead to
jaundice anorexia malaise
What is the pastille form of Nystatin?
licorice-flavored, rubbery, contains sugar
chronic hepatitis is inflammation of the ___
liver
HAART- Highly active Anti-retroviral Therapy is used for?
management of HIV / AIDS for improved effect by combining drugs
topical use of acyclovir has limited and non life threatening initial and recurrent ______ herpes simplex (HSV-1) in immunocompromised patients
mucocutaneous
