Antifungal Agents, Amphotericin B, and Nystatin

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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


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