Antifungal Agents, Amphotericin B, and Nystatin
What inhibit ergosterols by inhibiting sterol 14-a-demethylase, a cytochrome P450 enzyme system that converts lanosterol to ergosterol?
Azoles
What is a topical agent used to treat superficial infections of the stratum corneum, squamous mucosa, and cornea?
Clotrimazole
Griseofulvin is limited to skin, hair, and nails caused by?
Dermatophytes
What is the indication of agents for influenza/viral resp infections?
Prophylaxis against and possible treatment of influenza A infection (not Influenza B). Reduces length and severity of influenza A infections
Amphoterecincause the release of____ and ______from host immune cells leading to chills, fever, vigors, hypotension, and headache.
TNF-a and IL-1
has poor bioavailability and is administered by inhalation, less than 20% absorbed systemically, mostly excreted in urine
Zanamivir
Uncommon, oral/nasal discomfort, bronchospasm, delirium, hallucinations, or other related behavior are adverse effects of what?
Zanamivir and oseltamivir
Used for Influenza A&B to decrease intensity and duration of the disease, also complications?
Zanamivir and oseltamivir
Bone marrow depression leading to anemia, hepatotoxicity, lactic acidosis, and myopathy are adverse effects of what?
Zidovudine
What is the name of a nucleoside reverse transcriptase inhibitor?
Zudovudine
contains no 3'hyrdroxyl group so like acyclovir its a chain terminator?
Zudovudine
____ is used for Prophylaxis against herpesviruses in immunocompromised patients (e.g. undergoing cancer chemotherapy)
acyclovir and similar agents
What binds to sterols(ergosterols) in cell membranes forming pores or chanels to alter the fungal cell membrane permeability and cause leakage of essential cellular components leading to death?
antifungals, amphoterecin
What inhibits metabolism of Zidovudine causing increased toxicity?
asprin, acetominaphen, indomethacin
How do you take fluconazole?
available as both oral and IV formulation
_______ inhibits corticosteroid synthesis in cases of advanced adrenal cancer.
ketoconazole
What Imadazole is used for mucocutaneous candidiasis?
ketoconazole-Nizoval
Griseofulvin is metabolized by _____ and excreted by ____
liver/ urine and feces
Zidovudine is activated by _______, by host cell thymidine kinase and other kinases to the triphosphate.
phosphorylated
Griseofulvin deposits in keratin ___ and persist after differentiation making keratin resistant to ____ infections.
precursor cells/fungal
Ketoconazole can be used to inhibit androgen production in cases of advanced _______.
prostate cancer
Allylamines inhibit fungal ergosterol synthesis by inhibiting ____ and _____.
squalene-2, and 3- epoxidase
Azoles inhibit ergosterols by inhibiting ____________, a cytochrome P450 enzyme system that converts lanosterol to ergosterol?
sterol 14-a-demethylase
What are the uses of fluconazole?
systemic candidiasis, cryptococcal meningitis, and coccidioidal meningitis. and for refractory oral and systemic candidiasis
What causes taste perversion, GI disturbances, hepatitis, rash, and contact dermatitis?
terbinafine (Lamisil)
What is chemistry of Griseofulvin?
isolated from molds of genus penecillum insoluble to water
what are adverse effects of agents used for influenza/viral resp infections?
(nervousness, anxiety, agitation, insomnia, difficulty in concentrating, lightheadedness) Exacerbations of pre-existing seizure disorders, psychiatric symptoms in PD or schizophrenia
Give prescription of Clotrimazol in Troche?
10mg troche/70 troches/14 day supply-dissolve in mouth 5xs a day and swallow. No eat/drink for 30 min.
Give prescription of Clotrimazol in cream.
15g tube, rub into affected areas 2-3xs a day for 2 weeks
Zidovudine contains no ________ so like acyclovir its a chain terminator.
3 hydroxyl group
When Zidovudine indicated?
Asymptomatic and symptomatic HIV infections
What is Zudovudine?
A nucleoside reverse transcriptase inhibitor :)
Nausea, vomiting, diarrhea, headache, and hallucinations with high dose are adverse effects of what?
Acyclovir and similar agents
Useful in treatment of genital herpes simplex, herpes simplex labialis (cold sores), herpes zoster (shingles) and varicella zoster (chicken pox)
Acyclovir and similar agents
Ketoconazole inhibits corticosteroid synthesis in cases of advanced ________.
Adrenal cancer
Inhibitor of viral uncoating Blocks the M2 proton channel in the viral envelope, inhibiting acidification of the virion interior, dissociation of matrix protein and uncoating. Also cause release of dopamine and NE and blocks NMDA receptor - mechanism of what?
Agents used for influenza or viral resp infections
Naftifine, terbinafine (Lamisil), and butenafine are all types of what?
Allylamines
What is used to treat dermathophytosis and superficial forms of candidiasis?
Allylamines
is used to treat levodopa-induced dyskinesias that develop late in the course of the disease. It does this by blocking excitatory NMDA receptors
Amantadine
what are the two agents used for Influenza or viral resp. infections?
Amantadine and Rimantadine
What cause the release ofTNF-a and IL-1 from host immune cells leading to chills, fever, vigors, hypotension, and headache.
Amphoterecin
Nephrotoxic, vasoconstricion of renal artery leading to renal ischemia are adverse effects of what?
Antifungal agents, amphoterecin, and nystatin
What should you avoid taking if you are taking Clotrimazol(other than alcohol)-why?
Benzodiazapam, bc it can increase levels of benzodiazapam due to its inhibitory of CYP450 enzyme
What are the adverse effect of Zidovudine?
Bone marrow depression leading to anemia, hepatotoxicity, lactic acidosis, and myopathy
Rapid infusion of antifungals, amphoterecin and nystatin causes what?
Cardiotoxicity
What Imidazole is used for oral candidiasis in the form of a troche?
Clotrimazol
What antifungal agent should not be taken with alcohol because oral absorption is erratic and is metabolized by the liver?
Clotrimazol
What are the three Imidazoles?
Clotrimazol, miconazole, ketoconazole
Which Triazole is used for systemic candidiasis?
Fluconazole
what is the most widely used antifungal drug?
Fluconazole
What is the mechanism of action for Griseofulvin?
Fungiscidal to growing organisms by inhibition fungal mitosis by binding to tubulin and blocking its polymerization to microtubules.
What is an adverse effect of Ketoconazole in terms of absorption?
GI absorption depends on acidic conversion to a salt in stomach so does not work if pt is taking bicarbonate, antacid, H2 blockers, proton pump inhibitor or has achlorhydia.
Leukopenia and thrombocytopenia Headache and arthralgia. are seen with which herpes fighting agents
Ganciclovir
Useful for patient with CMV in immunocomprimised patients.
Ganciclovir
ITs use is limited to skin hair, and nails caused by dermatophytes?
Griseofulvin
What is isolated from molds of genus penecillum insoluble to water?
Griseofulvin
Which antifungal agent causes GI distress, skin rashes, paresthesia, superinfection with Candida?
Griseofulvin
Which antifungal agent causesHeadache, lapses of memory, impairment of judgement?
Griseofulvin
Which antifungal agent should not be used for pilot and bus drivers?
Griseofulvin
_____deposits in keratin precursor cells and persist after differentiation making keratin resistant to fungal infections.
Griseofulvin
What azole has 2 nitrogen in a azole ring?
Imidazoles
What are the adverse effects of clotrimazole?
itchin, burning, and sensitization
What is the mechanism of action for influenza or viral resp infections
Inhibitor of viral uncoating Blocks the M2 proton channel in the viral envelope, inhibiting acidification of the virion interior, dissociation of matrix protein and uncoating. Also cause release of dopamine and NE and blocks NMDA receptor
What is the mechanism of action of antifungal agents?
It binds to sterols(ergosterols) in cell membranes forming pores or channels to alter the fungal cell membrane permeability and cause leakage of essential cellular components leading to death.
What is Nystatin?
It is a polyene macrolide antifungal agent
Used for vulvovaginitis, oral and esophageal candidiasis, and mucocutaneous candidiasis?
Ketoconazole
What Azole has fatal heptaic necrosis can occur and inhibits P450 enzyme involved in steroid synthesis causing menstrual irregularities, gynecomastia and impotence?
Ketoconazole
What azole is available in cream or lotion for common skin fungi?
Ketoconazole
What increases the levels of saquinavir?
Ketoconazole
___ can be used to inhibit androgen production in cases of advanced prostate cancer.
Ketoconazole
What is an adverse effect of indinavir?
Kidney stones-crystalluria
What is the chemistry of Antifungal agents, Amphotericin B, and Nystatin?
Large molecules with hydroxylated portion that is hydrophilic and a portion containing 4-7 double bonds that are lipophilic.
What are two meds under clotrimazole?
Lothrimin and mycelex
Hair infection?
Microsporum
What are the three type of allylamines?
Naftifine, terbinafine(Lamisil), and butenafine
Zanamivir and oseltamivir mechanism of action?
Neuraminidase inhibitor, decrease release of virus from infected cells by inhibiting the breakage of the bond between the virus particles and the host cells
What are the three NNRTI's(non-nucleoid)?
Nevarapine, delavirdine, and efavirenz
What is a polyene macrolide antifungal agent called?
Nystatin
What is the choice for candida infections of oral cavity- oral moniliasis, thrush, and denture stomatitis?
Nystatin
What is the prescription of nystatin for oral candidiasis?
Oral suspension 100,000 units/mL, 473 ml (1pint bottle) 14day supply, use tsp or 5 ml qid, rinse in mouth and hold for as long as possible before swallowing. No eat or drink 30 min after using rinse.
how are protease inhibitors taken? and how are they metabolized?
Oral-liver
is well absorbed orally and excreted largely unchanged in urine?
Oseltamivir
What are the adverse effects of Efavirenz?
Rash and various CNS disturbance
What are some adverse effects of protease inhibitors?
Redistribution of body fat(buffalo hump), n,d,v, hyperglycemia and hyperlipedimia
Bronchospasms, rash, conjunctivitis, headache, GI upset are adverse effects of what?
Ribavirin (Virazole
Phosphorylated intracellularly and inhibits viral replication of both RNA and DNA viruses partly by interfering with guanosine triphosphate (GTP) formation and subsequent viral mRNA capping, hence viral protein synthesis
Ribavirin (Virazole
Some absorption into blood when used as an aerosol. Readily absorbed from GI tract. Excreted mainly as deribosylated metabolic product in urine.
Ribavirin (Virazole
Used as aerosol for respiratory syncytial virus (RSV) infection in children. Oral form may be useful for hepatitis
Ribavirin (Virazole
Which is less toxic Amantadine or Rimantadine?
Rimantadine
acyclovir intermittent therapy for cold sores lasting less than one week dose?
Rx: 200mg q4h or 5 times per day × 5days
Acyclovir for herpes zoster infection dose?
Rx: 800mg 5 times per day × 7days
What are the three protease inhibitors?
Saquinavir, ritonavir, indinavir
What is the mechanism of action of Azoles?
The inhibit ergosterols by inhibiting sterol 14-a-demethylase, a cytochrome P450 enzyme system that converts lanosterol to ergosterol
How do the Non nucleoidRTIs work?
They inhibit HIV reverse transcriptase directly by binding adjacent to enzyme active site and inducing conformational change in this site
How do allylamines work?
They inhibit fungal ergosterol synthesis by inhibiting squalene-2 and 3-epoxidase
How to protease inhibitors work?
They inhibit protease essential for final step of new virus formation. Active against strains resistant to HIV reverse trascriptase inhibitors.
What azole has 3 nitrogens in a azole ring?
Triazoles
NNRTIs are used in combo with NRTIs or protease inhibitors. True or False.
True
Nystatin topical or oral form are not absorbed on ingestion and consequently are not associated with any DDI's. T or F
True
True or False: Clotrimazol is contraindicated if you have liver disease.
True
Toe infection?
Trychophyton
Acyclovir and similar agents are used for what?
Useful in treatment of genital herpes simplex, herpes simplex labialis (cold sores), herpes zoster (shingles) and varicella zoster (chicken pox)
What are the dental uses of Nystatin
choice of drug for candida infection of oral cavity
Ketoconazole inhibits ____ sysnthesis in cases of advanced adrenal cancer.
corticosteroid
In what form is Clotrimazole available?
cream or troche
NonnucleoidRTI's inhibit HIV reverse transcriptase by binding adjacent to _______ and inducing conformational change in this site.
enzyme active site
What are the three triazoles?
fluconazole, itraconazole, and teraconazole
What do you use for CMV retinitis and acyclovir-resistant mucocutaneous HSV infections in patients with AIDS?
foscarnet
What is an adverse effect of ritonavir?
paresthesias
Fluconazole increases the levels of what?
phenytoin, cyclosporine, warfin, and amitriptyline
What is the mechanism of action for agents used to treat herpes virus infections?
they are converted into triphosphate with viral specific thymine kinase. Triphosphate selectively inhibits virus DNA polymerase and thus inhibits DNA replication
Zidovudine acts as a substrate for reverse transcriptase and competes with ______ for incorporation in to DNA,
thymidine triphosphate
Zidovudine is activated by phosphorylated, by host cell _____ kinase and other kinases to the _______
thymidine/triphosphate
Griseofulvin is Fungiscidal to growing organisms by inhibition fungal mitosis by binding to ___ and blocking its _____.
tubulin/polymerization to microtubules