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PDA Block 3 > PDA Block 3 Week 3 > Flashcards

PDA Block 3 Week 3 Flashcards

1
Q

Mebendazole

A
  • Immobilizes and kills parasite
  • selective damage to microtubules - intestinal roundworms
  • kills some ova
  • poorly absorbed
  • low systemic toxicity
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2
Q

Albendazole

A
  • immobilizes and kills parasite
  • hepatic metabolite (albendazole sulfoxide) responsible for activity
  • Echinococcus (Hydatid cyst)
  • Cutaneous larval migrans
  • metabolite well distributed
  • elevated hepatic enzymes, abdominal pain, N/V, headache
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3
Q

Thiabendazole

A
  • Hook worm: inhibits energy metabolism, mitochonidrial fumarate reductase
  • Strongyloides: blocks microtubule assembly - Strongyloides
  • cutaneous larva migrans
  • oral form absorbed rapidly
  • N/V, dizziness
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4
Q

Pyrantel pamoate

A
  • Hook worm: inhibits energy metabolism, mitochonidrial fumarate reductase
  • Strongyloides: blocks microtubule assembly - Strongyloides
  • cutaneous larva migrans - oral form absorbed rapidly
  • N/V, dizziness
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5
Q

Praziquantel

A
  • increases calcium permeability → muscle contraction (followed by spastic paralysis)
  • schistosoma
  • some activity against other trematodes
  • also for Cestodes

-abdominal discomfort, nausea

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6
Q

Paromomycin sulfate

A
  • 3rd choice drug for Tapeworm
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7
Q

Chloroquine

A
  • blood schizonticide
  • parasitized erythrocytes concentrate the drug ( >25 fold) by pH dependent mechanism into acidic vacuoles
  • only intraerythrocytic trophozoites that are actively degrading hemoglobin are suceptible
  • inhibit heme -polymerization, allowing heme to accumulate to toxic levels
  • Prophylaxis: prevent attacks of all 4 species of Malaria (if they are chloroquine sensitive)
  • Treatment: eradicate P, malaria and chloroquine-sensitive P, falciparum
  • Target blood schizonts of P. vivax and ovale ( does not target liver hypnozoites)
  • usually well tolerated
  • visual impairment with extended use
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8
Q

Mefloquine

A
  • similar to chloroquine
  • blood schizonticide -Treatment: chloroquine-resistant P. falciparum

-prophylaxis in chloroquine-resistant areas

  • contraindicated in those with epilepsy or psychiatric disorders
  • psychiatric effects: anxiety, paranoia, depression
  • Vestibular effects: dizziness, vertigo
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9
Q

Atovaquone + proguanil

A
  • Block pyrimidine synthesis
  • Atovaquone: selectively inhibits malarial mitochondrial electron transport (cytochrome bc1)
  • Produanil: prodrug that inhibits malarial dihydrofolate reductase→ blocks folate synthesis & pyrimidine synthesis
  • synergistic effects on mitochondria w/ atovaquone
  • Prevention and treatment of chloroquine-resistant P.Falciparum
  • N/V, diarrhea, rash
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10
Q

Quinine

A
  • similar to chloroquine
  • blood schizonticide against all 4
  • agent for severe, acute attacks
  • alternate for chloroquine resistant P. Falciparum

-Cinchonism: headache, visual disturbance, dizziness, tinnitus, GI irritation, n/v. CV effects

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11
Q

Doxycycline

A
  • Decrease malarial protein synthesis
  • depress dihydroorotate dehydrogenase activity (interferes with pyrimidine synthesis)
  • effective for multidrug resistant P. falciparum
  • GI disturbance: enterocolitis
  • Candida superinfection in colon
  • Photosensitization with rash—sunlight makes rash worse
  • Teeth discoloration—avoid use in children (<8)
  • Contraindicated in pregnancy
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12
Q

Primaquine

A
  • metabolites can act as oxidants
  • kills liver hypnozoites
  • radical cure or terminal prophylaxis of P. Vivax and P. Ovale
  • used in conjunction with blood schizonticide (chloroquine)
  • used in combo with clindamycin to treat pneumocystis jiroveci in AIDS pt
  • hemolytic reactions in G6PD deficiency
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13
Q

Metronidazole

A
  • disrupts DNA
  • Tissue amebicide for mild to severe symptomatic infections of E. hystolytica
  • n.v. anorexia, diarrhea, transient leukopenia, neutropenia, thrombophlebitis after IV infusion, bacterial and fungal superinfections (candida)
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14
Q

Iodoquinol

A
  • unknown, effective for trophozoites in bowel lumen
  • luminal amebicide
  • use in combo with metronidazole for mild to severe infections of E. histolytica
  • Diarrhea and other GI symotoms
  • contraindicated for those hypersensitive to iondine –containing preparation
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15
Q

Atovaquone

A
  • Ubiquinone analog: inhibits mitochondrial electron transport →disrupts protozoal pyrimidine synthesis

-Pneumocystis jiroveci prophylaxis or treatment
- Toxoplasma gondii
(+rifabutin)

-nausea, diarrhea, vomiting, rash

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16
Q

Nitazoxanide

A
  • inhibits pyruvate: ferredoxin oxidoreductase (required for anaerobic energy metabolism - Giardia lamblia
  • Crytposporidium parvum

-Diarrhea, nausea, abdominal pain

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17
Q

Nematode (Roundworm) Rx

A

Mebendazole
Albendazole
Thiabendazole
Pyrantel pamoate

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18
Q

Trematode Rx

A

Praziquantel

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19
Q

Cestode Rx

A

Praziquantel
Albendazole
Paromomycin sulfate

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20
Q

Malarial Rx

A

Chloroquine
Mefloquine
Atovaquone + proguanil
Quinine

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21
Q

Rx: pneumocystis jiroveci

A
  1. Trimethoprim +Sulfamethoxazole (TMP-SMX)
  2. Clindamycin + Primaquine
  3. Atovaquone
  4. Dapsone
22
Q

Active Immunization

A

Vaccination (e.g. polio, smallpox, measles, influenza, herpes zoster [chickenpox,
shingles], hepatitis A, hepatitis B, rabies, etc.)

23
Q

Passive immunization

A
  • Injection of immune globulin often blocks viral penetration
24
Q

Amantadine

A
  • blocks viral uncoating by interfering with influenza A M2 protein (ion channel responsible for acid mediated dissociation of ribonucleoprotein complex) - Prophylaxis against influenza A but not B
  • Reduces fever in 50% of pt and illness duration by 1-2 days if given within first 2 days of illness
  • for last few years, influenza strains have been amantadine resistant - CNS: slurred speech, anxiety, confusion, depression, headache
  • Excreted unchanged in urine→ reduce dose in renal disease
25
Q

Oseltamivir

A
  • Tamiflu
  • inactive prodrug that is converted to oseltamivir carboxylate ( competitive inhibitor of influenza NA)
  • interferes with viral release from infected cells and viral penetration into respiratory epithelium - treatment of uncomplicated influenza A and B in pt >1 yo
  • must be given within 48 hours of symptom onset
  • flu prophylaxis in pt > 1yo - n/v/diarrhea
  • bronchitis
26
Q

Trifluridine

A
  • interferes with DNA synthesis; Thymidine analog
  • ophthalmic Tx of kerato-conjunctivitis and recurrent epithelial keratitis due to Herpes Simplex types 1 and 2
  • burning, stinging, hypersensitivity
27
Q

Acyclovir

A
  • inhibits DNA polymerase
  • phosphorylated form is produced 40-100x faster in infected cells by herpes thymidine kinase
  • inhibits herpes DNA pol 10-30x more than host cell DNA pol
  • acts as a competitive inhibitor of dGTP and as a DNA chain terminator - IV: serious systemic herpes virus simplex (HSV)
  • oral: primary genital herpes
  • oral: primary herpetic gingiovostomatosis
  • Topical: primary genital herpes (not recurrent)
  • Misc: chickenpox in children - generally well tolerated
  • rash, itching, n/v, headache, fatigue
28
Q

Famciclovir

A
  • prodrug that is converted to penciclovir which is then phosphorylated (inhibits viral DNA pol) - Acute herpers zoster (shingles) <3 dyas duration
  • Tx and suppression of recurrent genital herpes
  • similar to acyclovir
  • rash, itching, n/v, headache, fatigue
29
Q

Penciclovir

A
  • inhibits DNA polymerase
  • Topical: tx for recurrent herpes of the lips and face
  • rash
30
Q

Ganciclovir

A
  • inhibits DNA pol
  • phosphorylation is catalyzed by CMV protein kinase
  • virustatic - Tx of CMV retinitis in AIDS pt
  • CMV prophylaxis for transplant recipients
  • slow progression not cure - bone marrow suppression, leukopenia, thrombocytopenia, anemia
  • may enhance bone marrow suppression when given with zidovudine (AZT)
31
Q

Foscarnet

A
  • selectively inhibits CMV DNA pol by binding to its pyrophosphate-binding site
  • Does not require conversion to triphosphate form to be active
  • AIDS pt with CMV (cytomegalovirus) retinitis
  • slow progression, not cure
  • approved for acyclovir-resistant herpes simplex
  • Renal damage (reversible)
  • electrolyte imbalances
  • seizure
32
Q

Lamivudine

A
  • nucleoside analog inhibitor of RT domain of HepB DNA pol (must be phosphorylated to be active)
  • HBV
  • n/v/ diarrhea
33
Q

Tenofovir

A
  • esterified adenosine monophosphate analog (phosphorylated to active nucleotide)→ inhibits RT domain of Hep B DNA pol
  • HBV
  • GI upset
34
Q

Ribavirin

A
  • interferes with viral mRNA synthesis
  • mono-P inhibits inosine 5P dehydrogenase ( thus GTP synthesis)
  • Tri-P inhibits GTP dependent capping of viral mRNA - aerosol use in infants & young children with severe lower RSV
  • HCV in combo with interferon-alpha

-Aerosol: use with caution in assisted ventilation (can precipitate in respiratory equp.)
-pulmonary function deterioration, rash
IV/oral: anemia, bone marrow suppression

35
Q

Interferon

A
  • induce host cells to produce enzymes that block translation of viral mRNA
  • approved antiviral uses for recombinant alpha interferons: Condyloma acuminata, HepB and C, PEG alfa 2a and PEG-alfa-2b in combo with ribavirin are specifically useful for HepC
  • flu like syndrome
  • Leukopenia, bone marrow suppression
  • neurotoxicity, myalgia
36
Q

Boceprevir

A
  • reversible inhibitor of HepC NS3 (HCV poly protein) protease (blocks formation of infectious virus particles) - Hep C genotype 1 in combo with PEG interferon + ribavirin
  • boceprevir + PEG-interferon Alpha +ribavirin
  • same SE as interferon + ribavirin
  • increase incidence/severity of anemia and neutropenia
  • contraindicated with drugs that are CYP3A substrates or induces
37
Q

Zidovudine

A
  • Thymidine nucleoside analog: phosphorylated by cellular kinase
  • Blocks nucleic acid synthesis by inhibiting RT
  • AZT tri-P acts as a DNA chain terminator
  • nucleoside RT inhibitor for HIV in adults and children
  • Bone marrow suppression, neutropenia, anemia
  • drugs that inhibit glucuronyl transferase (acetaminophen) increase hematologic toxicity of AZT and should be avoided
  • myopathy w/prolonged use
38
Q

Emtricitabine

A
  • Fluorinated analog of 3TC that inhibits RT by competing for dCTP
  • incorporations into DNA (chain termination)
  • combo therapy for HIV infect pt
  • headache, diarrhea, nausea
39
Q

Abacavir

A
  • nucleoside analog inhibitor of RT
  • combo therapy for HIV
  • hypersensitivity rxn (ass. With HLA-B*5701 antigen)
40
Q

Efavirenz

A
  • Non-nucleoside inhibitor of RT
  • doesn’t require phosphorylation for activity
  • part of multi-drug therapy for HIV
  • Rash, CNS/psychiatric symptoms, nightmares
41
Q

Lopinavir

A
  • prevents viral protease from cleaving Gag-pol polypeptide into functional proteins
  • results in non-infectious virus particles
  • used in combo with RT inhibitors (HIV-1 and HIV-2)
  • significantly decreases viral blood load
  • Diabetes (insulin resistance)
  • alterations in lipid metabolism
  • fat redistribution
  • alters metabolism of many other drugs (CYP3A)
  • diarrhea
42
Q

Ritonavir

A
  • PI & Blocks metabolism of lepinavir
  • Used to boost levels of PIs
  • avoid other CYP3A drugs
43
Q

Enfuvirtide

A
  • inhibits fusion of viral and cellular membranes
  • binds to gp41 subunits of HIV, blocking conformation change for membrane fusion
  • used against HIV-1 ONLY
  • Tx HIV infected with detectable viral replication despite ongoing therapy
  • local injection site rxn
  • diarrhea, nausea, fatigue
44
Q

Maraviroc

A
  • chemokine co-receptor (CCR5) antagonist
    – prevent interaction with HIV gp 120
  • Blocks entry of HIV into cells - Tx of CCR5 tropic HIV-1
  • hepatotoxicity
  • possible CV events (ischemia, infarction)
45
Q

Raltegravir

A
  • inhibits HIV-1 integrase acitivity, preventing integration of HIV-1 DNA into genome
  • Tx HIV-1 new and Tx-experience
  • works virus that is resitant to other drugs
  • generally well-tolerated
46
Q

RX HIV

A
  • Zidovudine (AZT)
  • Lamivudine (3TC)
  • Tenofovir
  • Emtricitabine (FTC)
  • Abacavir
    Efavirenz
  • Lopinavir+ ritonavir
  • Enfuvirtide
    Maraviroc
    Raltegravir
47
Q

RX influenza

A
  • Amantadine

- Oseltamivir

48
Q

HSV Rx

A
  • EYE: Trifluridine
  • LIPS/FACE: penciclovir & Acyclovir
  • GENITAL: acyclovir & Famciclovir
  • Acyclovir resistant: Foscarnet

Herpes zoster (Shingles): Famciclovir

49
Q

CMV

A
  • Ganciclovir

- Foscarnet

50
Q

RSV

A
  • Ribavirin
51
Q

HEP B

A

Lamivudine (3TC)

  • Tenofovir
  • interferon-alpha
52
Q

HEP C

A

Ribavirin + interferon –alpha +boceprevir

PDA Block 3 (4 decks)

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