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KG - Pharmacology > Antituberculosis & Antihelmintics > Flashcards

Antituberculosis & Antihelmintics Flashcards

1
Q

characteristics of LATENT TB INFECTION?

A
  • TB bacilli live dormant inside lung, do not cause destruction of organs
  • no signs/symptoms of disease
  • not infectious
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2
Q

characteristics of TB DISEASE

A
  • TB bacilli progressively invade and damage a part (or parts) of the body
  • signs/symptoms of disease appear
  • can be infectious
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3
Q

signs/symptoms of TB?

A
  • cough > 3 wks
  • extreme tiredness
  • weight loss
  • sweating at night
  • fever
  • no appetite
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4
Q

how is TB spread?

A
  • by droplet nuclei

- expelled when an INFECTIOUS person w/ TB sneezes, speaks, sings, or coughs

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5
Q

bacteria of TB?

A
  • Mycobacterium tuberculosis
  • acid-fast bacteria
  • slow generation time (15-20 hrs)
  • facultative intracellular parasite, usu of macrophages
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6
Q

list of first line drugs for TB?

A
  • Isoniazid
  • Rifampin
  • Pyrazinamide
  • Ethambutol
  • Streptomycin
  • Rifabutin
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7
Q

list of second line drugs for TB?

A
  • Cycloserine
  • p-aminosalicylic acid
  • Ethionamide
  • Amikacin or kanamycin
  • Capreomycin
  • Fluoroquinolones
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8
Q

which drugs should be administered for first line treatment of ACTIVE, drug-sensitive TB?

A
  • Isoniazid
  • Rifampin
  • Pyrazinamide
  • Ethambutol
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9
Q

why treat active TB with all four first line TB agents?

A
  • treats disease & helps reduce Mtb drug resistance

- reduces transmission rates in first 2 months

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10
Q

which drugs can be used as monotherapy in latent TB disease?

A
  • Isoniazid

- Rifampin

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11
Q

mechanism of ISONIAZID (INH, Nydrazid)?

A
  • inhibits biosynthesis of MYCOLIC ACID

- prodrug that required KatG

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12
Q

therapeutic use of Isoniazid (INH)?

A
  • can be prophylaxis (alone) - but can cause liver damage (must weigh benefits of prophylaxis vs. risks of INH associated hepatitis, esp in pts > 35 y.o.
  • w/ active TB always use w/ Rif, EMB, PZA
  • can reach intracellular bacilli
  • bacteriostatic, when given w/ Rif = bactericidal
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13
Q

pharmacokinetics of Isoniazid (INH)?

A
  • ORAL
  • GI absorption good
  • METABOLISM BY ACETYLATION (liver) inactivates drug
  • metabolic rate depends on individuals - some “rapid” and some ““slow” metabolizers
  • half of whites/blacks = “slow”, many eskimos/native americans/asians = “rapid”
  • excretion via urine
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14
Q

toxicities of Isoniazid (INH)?

A
  • HEPATITIS, abnormal liver tests, jaundice 2.5%
  • CNS stimulation/convulsions, insomnia, restlessness, psychic episodes
  • peripheral neuritis in slow acetylators
  • headache, vertigo
  • HEMOLYSIS in ppl w/ G6PD
  • constipation, diff micturition, orthostation hypotension, eosinophilia, albuminuria, skin rashes, allergy, bone marrow depression, liver damage
  • lupus like syndrome (HIP drugs - hydrazine, INH, procainamide)
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15
Q

mechanisms Rifampin (Rimactane)?

A
  • group of structurally similar complex macrocyclic antibiotics
  • inhibits DNA DEPENDENT RNA POLYMERASE
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15
Q

mechanisms Rifampin (Rimactane)?

A
  • group of structurally similar complex macrocyclic antibiotics
  • inhibits DNA DEPENDENT RNA POLYMERASE
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16
Q

toxicities of Rifampin?

A
  • not serious
  • GI upset - nausea, vomiting, cramps, epigastric pain, diarrhea, headache, dizziness
  • hypersensitivity or allergy
  • HEPATIC ENZYME INDUCTION - cytochrome P450 interactions can enhance metabolism of endogenous substrates, incl adrenal hormones, thyroid hormones, vit D, HAART
  • imparts harmless ORANGE color to urine, sweat, tears, contact lenses
  • decreases effectiveness of birth control - induces liver metabolism of progestins
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16
Q

Rifampin use?

A
  • to treat pulmonary TB in combo with other TB drugs
  • oral
  • can be used to treat latent TB (bactericidal)
  • effective against MTB - most like INH
  • effective against leprosy
  • inhibits growth of G+ cocci, some G- microbes (E coli, pseudomonas, proteus, klebsiella), chlamydia, pox virus
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17
Q

toxicities of Rifampin?

A
  • not serious
  • GI upset - nausea, vomiting, cramps, epigastric pain, diarrhea, headache, dizziness
  • hypersensitivity or allergy
  • HEPATIC ENZYME INDUCTION - cytochrome P450 interactions can enhance metabolism of endogenous substrates, incl adrenal hormones, thyroid hormones, vit D, HAART
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17
Q

toxicities of Rifampin?

A
  • not serious
  • GI upset - nausea, vomiting, cramps, epigastric pain, diarrhea, headache, dizziness
  • hypersensitivity or allergy
  • HEPATIC ENZYME INDUCTION - cytochrome P450 interactions can enhance metabolism of endogenous substrates, incl adrenal hormones, thyroid hormones, vit D, HAART
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18
Q

mechanisms Rifampin (Rimactane)?

A
  • group of structurally similar complex macrocyclic antibiotics
  • inhibits DNA DEPENDENT RNA POLYMERASE
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19
Q

Ethambutol is not recommended for which group of ppl?

A

in children below age 13 - bc of adverse effects on vision, phys exam should include ophthalmoscopy, finger perimetry, and testing of color discrimination

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20
Q

toxicities of Rifampin?

A
  • not serious
  • GI upset - nausea, vomiting, cramps, epigastric pain, diarrhea, headache, dizziness
  • hypersensitivity or allergy
  • HEPATIC ENZYME INDUCTION - cytochrome P450 interactions can enhance metabolism of endogenous substrates, incl adrenal hormones, thyroid hormones, vit D, HAART
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21
Q

for which group of individuals is Rifampin NOT recommended?

A

HIV treated individuals

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22
Q

mechanism of ETHAMBUTOL (Myambutol)?

A
  • inhibits ARABINOSYL TRANSFERASES involved in synthesis of arabinogalactan
  • bacteriostatic
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23
Q

pharmacokinetics of ethambutol?

A
  • given in combo w/ INH, Rif, PZA for active disease
  • bacteriostatic
  • oral, well absorbed, gets into CNS
  • renal elimination
  • excreted in feces & urine
  • dose adjustment needed in renal failure
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24
Q

toxicities of Ethambutol?

A
  • DECREASE VISUAL ACUITY AND LOSS OF GREEN-RED PERCEPTION - usu reversible when discontinuing drug
  • allergy, GI distress, numbness, joint pain, peripheral neuritis
  • w/ renal insufficiency give smaller dose
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25
Q

Ethambutol is not recommended for which group of ppl?

A

in children below age 13 - bc of adverse effects on vision, phys exam should include ophthalmoscopy, finger perimetry, and testing of color discrimination

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26
Q

w/ HIV individuals, which drug replaces Rifampin for active TB drug combo?

A

RIfabutin bc less potent inducer of P450 enzymes

- has become first line drug

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27
Q

second line antiTb agents & method of admin?

A
  • Cycloserine = oral, bacteriostatic
  • p-aminosalicylic acid = oral, bacteriostatic
  • Ethionamide = oral, bacteriostatic
  • Amikacin or kanamycin = IM, bactericidal
  • Capreomycin = IM, bactericidal
  • Fluoroquinolones = oral or IV, bactericidal
  • Rifapentine = analog of Rifampin

*lower potency or greater toxicity

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28
Q

side effects of Pyrazinamide?

A
  • hyperuricemia
  • not gouty polyarthralgia
  • HEPATIC DYSFUNCTION
  • myalgia
  • GI irritation
  • porphyria
  • photosensitivity
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29
Q

why is Pyrazinamide a critical first line drug?

A

responsible for reducing therapy to the current standard of 6 months (instead of 9-12 months)

30
Q

info about Streptomycin?

A
  • protein synthesis inhibitor (30S ribosome)
  • bactericidal
  • parenteral, limited tissue penetration, cell penetration poor, therefore good for extracellular Mtb
  • renal excretion (filtration), dose adjustment needed w/ renal failure
  • dose related toxicity: OTOTOXICITY, NEPHROTOXICITY
  • renewed interest in drug w/ increase in MDR, XDR
31
Q

info about Rifabutin (Mycobutin)?

A
  • inhibits DNA dependent RNA polymerase
  • bactericidal
  • oral, well absorbed, enterohepatic cycling
  • metabolites ORANGE COLORED
32
Q

w/ HIV individuals, which drug replaces Rifampin for active TB drug combo?

A

RIfabutin bc less potent inducer of P450 enzymes

- has become first line drug

33
Q

second line antiTb agents & method of admin?

A
  • Cycloserine = oral, bacteriostatic
  • p-aminosalicylic acid = oral, bacteriostatic
  • Ethionamide = oral, bacteriostatic
  • Amikacin or kanamycin = IM, bactericidal
  • Capreomycin = IM, bactericidal
  • Fluoroquinolones = oral or IV, bactericidal
  • Rifapentine = analog of Rifampin
34
Q

mechanism of fluoriquinolones?

A
  • sec line tb drug

- MDR Mtb (all first line)

35
Q

mechanism of action p-aminosalicylic acid?

A
  • sec line tb drug

- folic acid synthesis inhibitor

36
Q

mechanism of action ethionamide?

A
  • sec line tb drug

- inhibits peptide synthesis

37
Q

mechanism of action cycloserine?

A
  • sec line tb drug
  • ICWS
  • analog of D-ala
38
Q

XDR TB resistant to which meds?

A

INH, Rif, fluoroquinolones, usu kanamycin/capreomycin/amikamycin

39
Q

mechanism of action kanamycin/amikacin?

A
  • sec line tb drug
  • aminoglycoside
  • MDR Mtb
40
Q

mechanism of fluoriquinolones?

A
  • sec line tb drug

- MDR Mtb (all first line)

41
Q

treatment of MAC?

A
  1. clarithromycin or azithromycin
  2. ethambutol
  3. third oral drug (rifabutin, clofazimine, rifampin (if no HIV), cipro)

*can add IV amikacin in some cases if resistance to clarithromycin

42
Q

define: XDR TB

A

extensively multidrug resistant TB

43
Q

MDR TB resistant to which meds?

A

INH, Rif

44
Q

XDR TB resistant to which meds?

A

INH, Rif, fluoroquinolones, usu kanamycin/capreomycin/amikamycin

45
Q

how is mycobacterium avium complex (MAC) transmitted?

A
  • soil, water, birds

- common environmental pathogen, infection following inhalation or swallowing bacterial

46
Q

characteristics of MAC?

A
  • intrinsically resistant to anti-TB and antimicrobials
  • treatment w/ 2 or 3 antimicrobials for 12 months
  • co-infection w/ HIV common (20-30%)
47
Q

treatment of MAC?

A
  1. clarithromycin or azithromycin
  2. ethambutol
  3. third oral drug (rifabutin, clofazimine, rifampin (if no HIV), cipro)

*can add IV amikacin in some cases if resistance to clarithromycin

48
Q

toxicity of dapsone?

A
  • nausea, vomiting, headache, dizziness
  • dose related hemolysis
  • methemoglobinemia, leukopenia, agranulocytosis, allergic derm, sometimes exfoliative derm,
  • w/ liver damage.. fever
  • peripheral neuritis
  • nasal obstruction improves 3-6 months
49
Q

why treat leprosy w/ multi drug therapy?

A
  • treatment w/ only one drug will lead to resistance

- treatment w/ dapsone or another mono therapy = unethical practice

50
Q

treatment of leprosy?

A
  • PB leprosy patients = 1-5 patches get rifampin & dapsone

- MB leprosy patients = > 5 patches get rifampin, dapsone & clofazimine

51
Q

which is most widely used drug to treat leprosy?

A

dapsone - also cheapest

52
Q

mechanism of action of DAPSONE?

A
  • similar to sulfonamides
  • PABA antagonistic
  • interferes w/ nutrition of m. leprae
  • interferes w/ folic acid synthesis
53
Q

admin/absorption/fate of dapsone?

A
  • ORAL
  • GI absorption almost complete & rapid
  • excretion slow
54
Q

toxicity of dapsone?

A
  • nausea, vomiting, headache, dizziness
  • dose related hemolysis
  • methemoglobinemia, leukopenia, agranulocytosis, allergic derm, sometimes exfoliative derm,
  • w/ liver damage.. fever
  • peripheral neuritis
  • nasal obstruction improves 3-6 months
55
Q

thalidomide has orphan drug status for treatment of ____.

A
  • primary brain malignancies
  • kaposi’s sarcoma
  • HIV wasting syndrome
  • LEPROMATOUS LEPROSY
  • recurrent aphthous ulcers and stomatitis
  • TREATMENT OF MYCOBACTERIUM INFECTIONS
  • treatment and prevention of graft vs host dz
  • multiple myeloma
56
Q

mechanism of action clofazimine?

A

binds preferentially to MYCOBACTERIAL DNA (GUANINE) and inhibits reproduction and growth

57
Q

pharmacokinetics of clofazimine?

A
  • oral admin
  • incompletely absorbed from GI tract
  • GI disturbances, hepatitis, jaundice
58
Q

toxicities of clofazimine?

A
  • GI DISTURBANCES - anorexia, diarrhea, nausea/vomiting, colicky/burning pain (50% pts)
  • skin discoloration (75-100% pts)
  • HEPATITIS
  • crystalline deposits of clofazimine seen in many tissues and organs, lower dose w/ GI upset
59
Q

what is the DOC for moderate to severe Erythema Nodosum Leprosum (ENL)?

A

Thalidomide

60
Q

contraindications of Thalidomide?

A

100% contraindicated in pregnant women - very teratogenic

61
Q

thalidomide has orphan drug status for treatment of ____.

A
  • primary brain malignancies
  • kaposi’s sarcoma
  • HIV wasting syndrome
  • LEPROMATOUS LEPROSY
  • recurrent aphthous ulcers and stomatitis
  • TREATMENT OF MYCOBACTERIUM INFECTIONS
  • treatment and prevention of graft vs host dz
  • multiple myeloma
62
Q

three blood flukes (shistosomes)?

A
  • Schistosoma mansoni
  • Schistosoma haematobium
  • Schistosoma japonicum
63
Q

three types of worms?

A
  • roundworms (nematodes)
  • tapeworms (cestodes)
  • flukes (trematodes, shistosomes)
64
Q

characteristics of ROUNDWORMS (nematodes)?

A
  • non-segmented, cylindrical
  • infection: after ingestion of food contaminated w/ embryonic eggs
  • some live in blood, tissues
  • hookworms go in lungs
65
Q

characteristics of TAPEWORMS (cestodes)?

A
  • segmented, flatworm, suckers for attachment
  • eggs, passed in feces
  • larvae - may invade intestinal wall, get into bloodstream and lodge in eye/live/brain
  • adults - intestinal parasites
  • may grow to 20 ft
  • mild illness = abdominal discomfort, hunger, indigestion, anorexia, Vit B deficiency
66
Q

characteristics of FLUKES (trematodes)?

A
  • non-segmented flat worms, two suckers
  • eggs mature before entering humans
  • acquired through food or penetration of skin
  • mature in intestine, lung, liver
  • diarrhea, abdominal pain, anorexia
  • LIVER FLUKE - bile duct blockage, liver enlargement, URQ pain
  • LUNG FLUKE - cough, hemoptysis, chest pain
67
Q

characteristics of BLOOD FLUKES (shistosomes)?

A
  • penetrate skin in contact w/ contaminated H2O (snail intermediate host)
  • go through lymphatics to blood and liver
  • following maturation migrate into mesenteric or vesicular vein, adults mate/lay eggs
  • eggs pass through wall of intestine or bladder, may go to lung or liver
  • malaise, fever, intestinal discomfort
  • after eggs released - fever, abdominal pain, liver tenderness
68
Q

three blood flukes (shistosomes)?

A
  • Schistosoma mansoni
  • Schistosoma haematobium
  • Schistosoma japonicum
69
Q

mechanism of anti-hemintic therapy?

A

interferes w/:

  • energy metabolism
  • neuromuscular coordination
  • microtubular function
  • cell permeability
70
Q

drugs for Roundworms/nematodes?

A
  • pyrantel pamoate (Antiminth)

- Ivermectin (Mectizan)

71
Q

characteristics Pyrantel pamoate (antiminth)?

A
  • oral, broad spectrum
  • effective against roundworm, pinworm, hookworm
  • neuromuscular blocking agent that causes release of Ach & inhibition of cholinesterases
  • results in paralysis followed by expulsion of worms
  • little absorbed, few effects on humans - dizziness, drowsiness, headache
  • available OTC
72
Q

characteristics Ivermectin (Mectizan)?

A
  • oral
  • effective against nematodes, insects, acarine parasites
  • DOC for filaria infestation
  • used for THREADWORM, roundworm, cutaneous larva migraines
  • PARALYZES parasite, intensifies GABA-mediated transmission of signals in peripheral nerves
  • minimal side effects, pruritis, tender lymph nodes, fever
73
Q

drugs for Tapeworms (cestodes)?

A

Praziquantel (Biltricide)

74
Q

drugs for Flukes (Trematodes)?

A
  • Praziquantel (Biltricide)

- Biothionol (Bitin)

75
Q

characteristics of Praziquantel (Biltricide)?

A
  • oral
  • DOC for all shistosomes, effective against most cestodes & trematodes
  • thought to act by increases worm’s permeability to Ca2+, results in contraction and paralysis of worm’s muscles, dislodgment, death
  • well absorbed from GI tract - used for systemic infections
  • few systemic effects - nausea, vomiting, abdominal discomfort from release of dead worms’ proteins
  • not recommended for pregnant women (possible abortion)
76
Q

characteristics of Biothionol (Bitin)?

A
  • given orally
  • absorbed from GI tract
  • uncouples oxidative phosphorylation
  • active against flukes, incl liver & lung fluke
  • DOC for sheep liver flukes
  • side effects mild - nausea, vomiting, headache, diarrhea, dizziness, urticaria, rash
  • rxn to antigens released from dying worms

KG - Pharmacology (8 decks)

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