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MBBS II ERS > L37 - Drugs Used in Sexually Transmitted Diseases > Flashcards

L37 - Drugs Used in Sexually Transmitted Diseases Flashcards

1
Q

List antibiotics against: cell wall synthesis?

A

 Beta lactams: penicillins, cephalosporins, cephamycins, carbapenems, monobactams

 Non-beta lactams: vancomycin, bacitracin

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2
Q

List antibiotics against: cell membrane?

A

Cell membrane permeability: polymyxins

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3
Q

List antibiotics against: Protein synthesis?

A

 50S subunit: macrolides, linezolid

 30S subunit: tetracyclines, aminoglycosides

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4
Q

List antibiotics against: Folate metabolism?

A

 Sulfonamides (inhibits PABA > DHF A)

 Trimethoprim (inhibits DHF A > THF A)

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5
Q

List antibiotics against: Nucleic acid synthesis?

A

 DNA: metronidazole, quinolones

 RNA polymerase: rifampin

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6
Q

Compare the effects of bacteriostatic and bactericidal antibiotics?

A

Bacteriostatic (e.g. tetracycline) – inhibits growth of bacteria + rely on immunity, may relapse

Bactericidal (e.g. penicillins) – kills bacteria directly

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7
Q

List narrow and broad spectrum antibiotics?

A

Narrow = penicillin G, vancomycin

Broad = tetracyclines, amoxillin, augmentin

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8
Q

Give 4 reasons for combination antibiotics?

A
  • Synergistic action for eradication
  • Treat mixed bacterial infection
  • Overcome resistance
  • Reduce toxicity by reducing dose
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9
Q

List 2 diseases caused by Gonococci + one complication?

A

urethritis (purulent discharge), cervicitis

complication: pelvic inflammatory disease

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10
Q

Treatment regiment for gonococcal infection?

A

single intramuscular injection of ceftriaxone + single oral dose of azithromycin

** highly effective against penicillin- and tetracycline-resistant strains**

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11
Q

Which antibiotics are no longer effective against gonococcal infections?

A

Oral cephalosporins (e.g. cefixime) / fluoroquinolones

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12
Q

List 2 diseases caused by Chlamydial infection and outline treatment options? ADR?

A

urethritis, cervicitis

2 main options***:
 Azithromycin (oral)
 Doxycycline (oral)

Alternatives:
tetracycline / erythromycin / ofloxacin

ADR: Mild GI disturbance

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13
Q

Treatment option of all stages of syphilis? Treatment for early latent syphilis?

A 
All stages:
Penicillin G (IV preferred, oral compliance is low)

Early latent stage:
long-acting preparations (e.g. weekly single IM injection of benzathine penicillin G)

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14
Q

Treatment of STD with multiple pathogens e.g. gonococcal + chlamydial co-infection?

A

2 options:

1) Single dose of IM ceftriaxone + single dose of oral azithromycin
2) Single dose of IM ceftriaxone + oral doxycycline for 7 days

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15
Q

Causative pathogens of Pelvic inflammatory disease?

A

Neisseria gonorrhoeae + Chlamydia trachomatis +/- anaerobic bacteria

at Upper female reproductive tract

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16
Q

Describe the route of spread of bacteria causing PID after intercourse with infected male?

A

Bacteria enter vagina through semen

> > pass through cervix, uterus, fallopian tube, ovaries

> > exit to peritoneal cavity

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17
Q

Inpatient* treatment option for pelvic inflammatory disease?

A

broad spectrum antimicrobial coverage:

1) IV cefoxitin / cefotetan (= cephamycins) + oral doxycycline (tetracycline)
2) IV clindamycin (inhibits 50S) + aminoglycoside (e.g. streptomycin)

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18
Q

Outpatient treatment option for pelvic inflammatory disease?

A

single IM dose of ceftriaxone + oral doxycycline ± metronidazole

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19
Q

List 3 vaginal infections?

A

Bacterial vaginosis

Trichomoniasis

Vulvovaginal candidiasis

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20
Q

Treatment for Bacterial vaginosis?

A

3 options:

1) oral metronidazole
2) Metronidazole gel applied intravaginally
3) Clindamycin (oral / intravaginal)

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21
Q

Treatment for Trichomoniasis? *caused by Trichomonas vaginalis *

A

Single dose metronizadole or Tinidazole

anti-bacterial, anti-parasitic

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22
Q

Treatment for vulvovaginal candidiasis?

A

Topical azole antifungal agents against Candida:

1) Intravaginal use: clotrimazole, miconazole
2) Oral fluconazole
3) AmB deoxycholate and flucytosine for resistant strains

23
Q

List antifungal agents that alter cell membrane permeability?

A

Target cell membrane: Azoles, Polyenes, Terbinafine

Target cell wall: Echinocandins

24
Q

List antifungal agents that alter DNA synthesis?

A

Flucytosine

25
Q

List antifungal agents that alter Microtubule structures?

A

griseofulvin

26
Q

Treatment options for uncomplicated genital herpes?

A

1) Acyclovir (oral)
2) Valacyclovir
3) Famciclovir

2,3 are acyclovir derivatives with higher bioavailability

27
Q

Causative pathogen of Genital warts and treatment options?

A

human papillomavirus (HPV)

1) imiquimod cream (= immune response modifier)
2) Podofilox solution / gel (aka podophyllotoxin = antimitotic drug)
3) Sinecatechins ointment

Recurred warts:
local intra-lesional alfa interferon

28
Q

Treatment for complicated/ severe genital herpes?

A

foscarnet and cidofovir

IV acyclovir

29
Q

MoA of acyclovir?

A

= acyclic guanosine derivative, inhibits viral DNA synthesis

  • Selectively activated in infected cells by viral-specific thymidine kinase + cellular kinases
  • Competitive inhibition of viral DNA polymerase with deoxyguanosine triphosphate (dGTP)
  • Incorporate dGTP into viral DNA (primer strand)&raquo_space; chain terminal
30
Q

Compare the indication of acyclovir based on diff. preparations?

A 
IV = serious HSV infection (can use foscarnet, cidofovir)
Oral = treat primary infections

(Topical = ineffective)

31
Q

Compare the activation of Valacyclovir and Famiciclovir?

A

Valacyclovir = Ester of ACV&raquo_space; converted to ACV

Famiciclovir = metabolized to the active penciclovir, same MoA as ACV

32
Q

Describe how retroviruses incorporate its genetic material into host?

A

uses own reverse transcriptase*

|&raquo_space; DNA incorporated into host DNA by integrase*

33
Q

Explain why antiretroviral therapy (ART) is multi-drug combo?

A
  • Maximize inhibition of viral replciaiton
  • Minimize drug toxicities
  • Different targets in viral mechanism = lower resistance
34
Q

List 5 categories of antiretroviral drugs?

A
  • Entry inhibitors
  • NRTI and NNRTIs
  • Integrase inhibitor
  • Protease inhibitor
  • integrase strand transfer inhibitors (INSTI)
35
Q

Outline the typical regimen for HIV infection?

A

1) 2 NRTI + INSTI/NNRTI/PI

2) dolutegravir (PI, DTG) + lamivudine (NRTI: 3TC)

36
Q

4 primary goals of ART for HIV infection?

A

Reduce HIV-associated morbidity and mortality

preserve immunologic function: increase CD4 T cells, decrease opportunistic infections

suppress plasma HIV viral load

prevent HIV transmission

37
Q

Name 2 NRTIs and give MoA?

A

zidovudine (AZT) and lamivudine (3TC)

1) bioactivation by cellular kinases into triphosphate form
2) Compete with native nucleotides to inhibit HIV reverse transcriptase
3) Incorporate into viral DNA for chain termination

38
Q

Admin, PK and ADR of NRTIs?

A

Oral
well absorbed and well distributed (t1/2 = 1h)

anemia and neutropenia

Lipodystrophy, Lactic acidosis, hepatic steatosis

39
Q

Name one NtRTI and give one advantgae over NRTI?

A

Tenofovir (TDF) = nucleotide analogue (NtRTI) = nucleoside + 1 phosphate group

Faster action: no need to be activated by enzyme

40
Q

Name 3 Non-NRTIs /NNRTI?

A

Non-nucleoside reverse transcriptase inhibitors:

nevirapine (NVP), efavirenz (EFV), delavirdine (DLV)

41
Q

MoA of NNRTIs?

A

Bind non-competitively and reversibly to directly inhibit the HIV-1 reverse transcriptase

42
Q

ADR of NNRTIs?

A

General:

  • Rash
  • D/D interaction

Efavirenz = Neuropsychiatric

Nevirapine* = hepatotoxicity, Rash

43
Q

Name 3 protease inhibitors?

A

saquinavir (prototype)

ritonavir**, lopinavir

** Used as a booster of bioavailability of other PI**

All oral intake

44
Q

MoA of protease inhibitors?

A

Specifically inhibit HIV-1 protease

> > cannot produce mature infectious virions

45
Q

ADR of Protease inhibitors?

A

Rapid emergence of resistance

D/D interactions (CYP450)

GI disturbances

Lipodystrophy, Hyperlipidemia, Insulin resistance, diabetes

46
Q

Name 3 INSTI, MoA, ADR?

A

Integrase Strand Transfer Inhibitors (INSTI): Raltegravir**, dolutegravir & elvitegravir

Inhibits catalytic activity of HIV-1 integrase
» prevents propagation of the viral infection into host CD4 cells
» prevent HIV replication

Low ADR = preferred

47
Q

Name 2 viral entry inhibitors?

A

Maraviroc

Enfuviritide

48
Q

MoA of Enfuvirtide?

A

Fusion inhibitor

inhibits the fusion of the viral transmembrane glycoprotein gp41 with the host cell (CD4) surface

49
Q

MoA of Maraviroc?

A

antagonist of the CCR5 chemokine co-receptor on CD-4 T-cells

> > prevents interaction between HIV gp120 and the CCR5 protein

> > prevent HIV fusion

50
Q

Which class of ART cause lactic acidosis and hepatic steatosis?

A

all NRTI

51
Q

Which class of ART cause Hyperlipidemia, insulin resistance and diabetes?

A

All PI

52
Q

Which class of ART cause rash?

A

All NNRTI, especially Nevirapine

53
Q

Which class of ART cause increased bleeding in hemophiliacs?

A

All PI

MBBS II ERS (37 decks)

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