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CVS II Drugs Used in Angina Pectoris > Anti Tuberculosis > Flashcards

Anti Tuberculosis Flashcards

1
Q

What are the first line agents for anti-tuberculosis drugs

A

First-line agents
• Rifampin
• Isoniazid (INH)
• Pyrazinamide
• Ethambutol

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2
Q

ISONIAZD
Mechanism of action:

Resistance:

Pharmacokinetics:

A

Mechanism of action:
• prodrug and must be activated by bacterial catalase peroxidase
(KatG).
• inhibits synthesis of mycolic acids
Resistance:
• under expression of enzyme (KatG) required for activation
Pharmacokinetics:
• Metabolism - acetylation by liver N-acetyltransferase
-genetically determined
-rapid acetylators – decreased plasma conc
-slow acetylators - increased plasma conc

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3
Q

ISONIAZID Adverse Reactions

A

Hepatitis
• Drug-induced systemic lupus erythematosus
• Peripheral neuropathy
- relative pyridoxine deficiency
- more likely to occur in slow acetylators
• Sideroblastic anemia

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4
Q

Rifampin
MOA
Resistance
Pharmacokinetics
Adverse Rxn

A

MOA: *Binds to the β subunit of bacterial DNA-dependent RNA polymerase *Inhibits RNA synthesis
Resistance:point mutations in the gene
for the β subunit of RNA polymerase. *reduced binding of rifampin
to RNA polymerase.
Pharmacokinetics:
• Strong inducer most cytochrome P450 isoforms (CYP1A2,2C9, 2C19, 2D6, and 3A4)
Adverse Reactions:
• imparts a harmless orange color to urine, sweat, and tears
• cholestatic jaundice and occasionally hepatitis
• light-chain proteinuria
• a flu-like syndrome characterized by fever, chills, myalgias,
anemia, and thrombocytopenia.
• acute tubular necrosis

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5
Q

Ethambutol
MOA
Resistance
Adverse Rxn

A

MOA: Inhibits mycobacterial
arabinosyl transferases
• Inhibits polymerization
reaction of arabinoglycan,
an essential component of
the mycobacterial cell wall
Resistance:
Resistance• mutations resulting in
overexpression of gene for
arabinosyl transferases
Adverse Rxn:retrobulbar neuritis
- The most common serious adverse event
- loss of visual acuity and red-green color blindness

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6
Q

PYRAZINAMIDE (PZA)
MOA
Resistance
Adverse Rxn

A

Mechanism of Action:
• Pyrazinamide is converted to pyrazinoic acid—the active
form of the drug—by mycobacterial pyrazinamidase
• Pyrazinoic acid disrupts mycobacterial cell membrane
metabolism and transport functions.
Resistance:
• impaired uptake of pyrazinamide
• mutations in pyrazinamidase that impair conversion of PZA to its active form
Adverse Reactions:
• hepatotoxicity
• hyperuricemia

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7
Q

What’s the treatment protocols for active infection in the intensive phase?

A

Two months of Rifampin: PLUS Isoniazid , Pyrazinamide ,
and Ethambutol

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8
Q

What’s the treatment protocols for active infection in the continuation phase?

A

Four months of Rifampin: PLUS Isoniazid

❑Adjuvant treatment
• Pyridoxine

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9
Q

What’s the treatment protocols for active infection in the latent infection phase?

A

isoniazid for 9 months

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10
Q

Second-line drugs for tuberculosis

A

• Streptomycin
• Amikacin
• Capreomycin
• Aminosalicylic acid
• Clofazimine
• Cycloserine
• Ethionamide
• Levofloxacin
• Moxifloxacin
• Linezolid
• Rifabutin
• Rifapentine

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11
Q

Used if strains are resistant to first-line agents?

A

Fluoroquinolones
Levofloxacin
Moxifloxacin

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12
Q

Used in combination with other second- line drugs for
multidrug-resistant strains

A

Linezolid

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13
Q

Penetrates cells poorly and is active mainly against
extracellular tubercle bacilli
• Site of action is the ribosome subunit 30S
• Interferes with the synthesis of ribosomal proteins
• Ototoxic - Vertigo and hearing loss
• Nephrotoxic

A

Streptomycin

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14
Q

• Indicated for streptomycin-resistant or multidrug-resistant
strains
• Nephrotoxic
• Ototoxic - tinnitus, deafness, and vestibular disturbances

A

Capreomycin

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15
Q

Amikacin

A

• Indicated for streptomycin-resistant or multidrug-resistant
strains

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16
Q

Cycloserine

A

• a structural analog of D-alanine
• inhibits cell wall synthesis
Adverse effects:
• Peripheral neuropathy
• Central nervous system dysfunction
• Pyridoxine ameliorates neurologic toxicity

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17
Q

Ethionamide

A

• Blocks the synthesis of mycolic acids
• Hepatotoxic
• Neurologic symptoms may be alleviated by pyridoxine

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18
Q

Aminosalicylic Acid (PAS)

A

• structurally similar to p-amino-benzoic acid (PABA)
• folate synthesis antagonist
• very high concentrations in the urine can result in crystalluria

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19
Q

RIFAMYCINS

A

Rifabutin
• Bacterial RNA polymerase inhibitor
• Both substrate and inducer of cytochrome P450 enzymes
• Less potent inducer than Rifampin
• Often used in place of rifampin for treatment of tuberculosis in
patients with HIV infection on antiretroviral therapy
• Similar rates of hepatotoxicity compared to rifampin
Rifapentine
• Potent inducer of cytochrome P450 enzymes
• Combined with isoniazid is an effective short-course treatment for
latent tuberculosis infection

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20
Q

Bedaquiline

A

• inhibits adenosine 5′-triphosphate (ATP) synthase in
mycobacteria
• risk of QTc prolongation

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21
Q

Pretomanid

A

acts as a respiratory poison following nitric oxide release

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22
Q

Rifapentine

A

• Potent inducer of cytochrome P450 enzymes
• Combined with isoniazid is an effective short-course treatment for
latent tuberculosis infection

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23
Q

Rifabutin

A

• Bacterial RNA polymerase inhibitor
• Both substrate and inducer of cytochrome P450 enzymes
• Less potent inducer than Rifampin
• Often used in place of rifampin for treatment of tuberculosis in
patients with HIV infection on antiretroviral therapy
• Similar rates of hepatotoxicity compared to rifampin

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24
Q

Nasal Decongestants

A

Phenylephrine
• postsynaptic α-receptor stimulant
• Nasal spray to act as a decongestant in
hay fever & the common cold

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25
Q

Pseudoephedrine

A

Nasal Decongestants

Pseudoephedrine
• Similar to ephedrine - has both an
alpha and beta agonist properties
• Alpha receptor mediated
vasoconstriction in the respiratory
mucosa shrinks swollen nasal mucous
membranes
• Relief of nasal congestion or eustachian
tube congestion

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26
Q

Xylometazoline

A

α1 and α2 adrenergic agonist
• Faster acting
Nasal decongestant

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27
Q

Oxymetazoline

A

Oxymetazoline
• Long- Acting Topical Nasal
Decongestant
• Direct acting alpha agonist (1 &
2A)
• For the temporary relief of nasal
congestion or stuffiness caused
by hay fever or other allergies,
colds, or sinus trouble

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28
Q

Cough Suppressants (Antitussives)

A

Dextromethorphan
• Opioid derivative NMDA blocker
• Decreases the sensitivity of cough receptors
• Interrupts the transmission of cough impulses
by depressing the medullary cough center
• Reported to be free of addictive potential
• Produces less constipation compared to codeine

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29
Q

Cough Suppressants (Antitussives)

A

Benzonatate
• Non-narcotic
• Anesthetizes the stretch receptors and thereby
reducing the cough reflex at its source
• Symptomatic relief of cough

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30
Q

N-acetylcysteine?

A

Mucolytics (Expectorants)
opens disulfide bonds, reducing the viscosity of
mucous
• Dilution of thick mucus makes it easier to cough
up, or drain
• To reduce congestion related to sinusitis,
bronchitis, asthma
• Used to ease congestion in pneumonia and
other chronic respiratory diseases

31
Q

Guaifenesin

A

Guaifenesin
• increases the volume and reduces the viscosity
of secretions in the trachea and bronchi.

32
Q

Drugs for Cystic Fibrosis

A

❑Dornase alfa
• Mucolytic agent
• Recombinant human deoxyribonuclease I
• Cleaves the extracellular DNA from invading neutrophils to decrease
mucus viscosity.

33
Q

❑Ivacaftor & Lumacaftor

A

❑Ivacaftor & Lumacaftor
• These are effective only in people with certain mutations - G551D
• Ivacaftor increasing chloride ion transport by increasing the channel-
open probability (or gating) of the CFTR protein

34
Q

❑Acetyl cysteine

A

SH groups

35
Q

❑Bosentan

A

Pulmonary Hypertension
Levels of ET-1 peptide are increased 10-fold in pulmonary arterial
hypertension (PAH)

36
Q

❑Epoprostenol

A

Pulmonary Hypertension
-PGI analogue

37
Q

❑Sildenafil

A

Pulmonary Hypertension
PDE5 antagonist

38
Q

What drugs will you use for non tb Mycobacterium for a prophylaxis for 1 year?

A

Macrolide – Azithromycin, Clarithromycin, Erythromycin
• Rifabutin
• Ethambutol

39
Q

What drug will you use for your patient with leprosy

A

Clofazimine

40
Q

You have a patient that has Group a Streptococcus and has pharyngitis. What will you prescribe?

A

PCN to reduce the rates of acute rheumatic fever
Benzathine PCN G IM -weekly/monthly
If allergic to PCN please give Cephalosporing, clindamycin and macrolides

41
Q

What organism affects sinusitis

A

S aureus
S pneumoniae
H influenza
Moraxella catarrhalis
Streptococcus pyogenes

42
Q

What is the initial empirici tx for sinusit

A

Amoxicillin or amoxicillin-clavulanate blocks beta lactam
Third generation oral cephalosporin(cefixime or cefpodoxime) prescribed with or without/o clindamycin<——(Gram +)
PCN allergic pt levofloxacin or moxifloxacin
Metronidazole—-anaerobic
Tazobactam—-pseudomonas
Imipenem—-G-ve
Gentamicin G-ve
Tobramycin G-ve

43
Q

What is the most common organism for acute otitis media

A

Strep Pneumonia
H Influenza
Moraxella cattarrhalis

44
Q

What is the first line of therapy for acute otitis media

A

Amoxicillin-clavulanate
Alt
• Cefdinir
• Cefpodoxime
• Cefuroxime
• Ceftriaxone
• Doxycycline
• Azithromycin
• Clarithromycin

45
Q

Otitis Externa
• most common causative bacteria

A

Otitis Externa
• most common causative bacteria are Pseudomonas species
Staphylococcus species, and anaerobes and gram-negative
organisms.

46
Q

Otitis Externa Tx?

A

• The topical fluoroquinolones ofloxacin and ciprofloxacin provide coverage against both pathogens.
• Topical Polymyxin B and neomycin.
• Polymyxin B is effective against P. aeruginosa, while
neomycin is effective against S. aureus.
• Topical aminoglycosides (eg, tobramycin and gentamicin) are
also effective against both S. aureus and P. aeruginosa.

47
Q

Community-Acquired Pneumonia (CAP) organism?

A

❑S pneumoniae
❑H influenza
❑M catarrhalis

48
Q

CAP treatment

A

• Amoxicillin/clavulanate
• Cefpodoxime
• Macrolide
• Doxycycline
• Moxifloxacin, Levofloxacin
• In patients with penicillin allergy: a respiratory fluoroquinolone AND
aztreonam
• If MRSA is suspected, vancomycin or Linezolid

49
Q

Atypical Pneumonias organism?

A

Atypical Pneumonias
• Mycoplasma pneumoniae
• Chlamydia pneumoniae
• Chlamydia psittaci
• Legionella pneumophila

50
Q

Chlamydia pneumoniae tx?

A

Chlamydia pneumoniae
Macrolides (Azithromycin)
Alt: Tetracyclines (Doxycycline)
Fluoroquinolones

51
Q

Mycoplasma pneumoniae tx?

A

Macrolides (Azithromycin):
Children and adults
ALT: Tetracyclines (Doxycycline):
Older children and adults
Fluoroquinolones: Adults

52
Q

Chlamydia psittaci tx?

A

Chlamydia psittaci
Tetracyclines (Doxycylcine)
Alt: Macrolides (Azithromycin)

53
Q

Legionella pneumophila tx?

A

Fluoroquinolones
(levofloxacin, moxifloxacin,
gemifloxacin)
Macrolides (azithromycin)
Alt:Tetracyclines (Doxycylcine

54
Q

Tetracyclines
MOA
Drugs
Interaction/toxicities

A

• Doxycycline
• Minocycline
• Methacycline
• Tigecycline
MOA:Prevents bacterial protein synthesis
by binding to the 30S ribosomal subunit
Interaction
• divalent cations impair oral absorption
Toxicity:
• Gastrointestinal upset, hepatotoxicity,
photosensitivity, deposition in bone and
teeth

55
Q

Prevents bacterial protein
synthesis by binding to the
50S ribosomal subunit? Interaction/toxicity

A

Erythromycin
• Azithromycin
• Clarithromycin
• cytochrome P450
inhibitor
Toxicity:
• Gastrointestinal
upset,
• QTc prolongation

56
Q

FLUOROQUINOLONES
MOA
Toxicity

A

• Moxifloxacin
• Gemifloxacin
• Levofloxacin

Inhibits DNA replication by binding to DNA
gyrase and topoisomerase IV

• Toxicity: neurotoxicity, tendonitis

57
Q

• Amphotericin B MOA
S/E

A

• Binds to ergosterol in the membrane
forming pores through which electrolytes
and other cell content leak
•Fevers, chills, and flu-like reaction
•Renal toxicity
• hydrate
• supplement potassium and
magnesium
•Anemia

58
Q

• Flucytosine

A

• Flucytosine

• Converted by fungal enzyme cytosine
deaminase to 5-fluorouracil, which then
inhibits nucleic acid synthesis•Bone marrow suppression

59
Q

Tx for histoplasmosis

A

Amphotericin B
Azoles/triazoles

60
Q

Tx Coccidioidomycosis

A

Amphotericin B
Fluconazole/itraconazole

61
Q

Tx Blastomycosis

A

Amphotericin B
Itraconazole

62
Q

Tx Cryptococcosis

A

Amphotericin B
Fluconazole
Flucytosine + amphotericin B

63
Q

Tx Aspergillosis

A

Voriconazole
Posaconazole
Echinocandins (Caspofungin)

64
Q

Mucormycosis tx

A

Lipid amphotericin B
Echinocandins (Caspofungin)

65
Q

Sporotrichosis TX

A

Itraconazole
Amphotericin B

66
Q

Pneumocystis pneumonia Tx

A

Trimethoprim/sulfamethoxazole

67
Q

Fungal infections of the respiratory system

A

• Coccidioides immitis
• Pneumocystis jeroveci
• Cryptococcus neoformans
• Aspergillus fumigatus
• Histoplasma capsulatum
• Mucor species
• Sporothrix schenckii
• Blastomyces dermatitidis

68
Q

Azoles
MOA
S/E

A

•Inhibits 14-alpha-demethylase,
which is key in ergosterol
synthesis in fungi
•Fungistatic
•Anti-androgen effects
via inhibiting
testosterone synthesis
• gynecomastia (in
particular,
ketoconazole)
•Inhibits cytochrome
P450

69
Q

Echinocandins
MOA
S/E

A

Echinocandins
•Disrupts cell wall
synthesis by inhibiting
beta-glucan synthesis
•Flushing
• mediated by histamine

70
Q

❑OSELTAMIVIR & ZANAMIVIR

A

❑OSELTAMIVIR & ZANAMIVIR
competitively and reversibly
inhibit viral neuraminidase
• clumping of newly released
influenza virions to each other
and to the membrane of the
infected cell
• Oseltamivir – oral
• Zanamivir - inhalation
• Zanamivir can cause cough,
bronchospasm

71
Q

❑PERAMIVIR

A

❑PERAMIVIR
• Neuraminidase inhibitor
• Activity against both influenza A and B viruses
• Treatment of acute uncomplicated influenza in adults – IV

72
Q

❑AMANTADINE & RIMANTADINE

A

❑AMANTADINE & RIMANTADINE
• Block the M2 proton ion channel
• Inhibit uncoating of the viral RNA within infected host cells
• Active against influenza A only
• Central nervous system adverse effects (marked behavioral changes,
delirium, hallucinations, agitation, and seizures) less frequent with
rimantadine than with amantadine
• amantadine - Skin rash – livedo reticularis

73
Q

BALOXAVIR MARBOXIL

A

BALOXAVIR MARBOXIL
• prodrug that is converted by
hydrolysis to the active baloxavir
• a cap-dependent endonuclease
inhibitor that interferes with viral
RNA transcription and blocks
virus replication
• activity against both influenza A
and influenza B.

CVS II Drugs Used in Angina Pectoris (18 decks)

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