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

Anti Tuberculosis Flashcards

(73 cards)

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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
Pseudoephedrine
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
26
Xylometazoline
α1 and α2 adrenergic agonist • Faster acting Nasal decongestant
27
Oxymetazoline
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
28
Cough Suppressants (Antitussives)
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
29
Cough Suppressants (Antitussives)
Benzonatate • Non-narcotic • Anesthetizes the stretch receptors and thereby reducing the cough reflex at its source • Symptomatic relief of cough
30
N-acetylcysteine?
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
Guaifenesin
Guaifenesin • increases the volume and reduces the viscosity of secretions in the trachea and bronchi.
32
Drugs for Cystic Fibrosis
❑Dornase alfa • Mucolytic agent • Recombinant human deoxyribonuclease I • Cleaves the extracellular DNA from invading neutrophils to decrease mucus viscosity.
33
❑Ivacaftor & Lumacaftor
❑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
❑Acetyl cysteine
SH groups
35
❑Bosentan
Pulmonary Hypertension Levels of ET-1 peptide are increased 10-fold in pulmonary arterial hypertension (PAH)
36
❑Epoprostenol
Pulmonary Hypertension -PGI analogue
37
❑Sildenafil
Pulmonary Hypertension PDE5 antagonist
38
What drugs will you use for non tb Mycobacterium for a prophylaxis for 1 year?
Macrolide – Azithromycin, Clarithromycin, Erythromycin • Rifabutin • Ethambutol
39
What drug will you use for your patient with leprosy
Clofazimine
40
You have a patient that has Group a Streptococcus and has pharyngitis. What will you prescribe?
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
What organism affects sinusitis
S aureus S pneumoniae H influenza Moraxella catarrhalis Streptococcus pyogenes
42
What is the initial empirici tx for sinusit
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
What is the most common organism for acute otitis media
Strep Pneumonia H Influenza Moraxella cattarrhalis
44
What is the first line of therapy for acute otitis media
Amoxicillin-clavulanate Alt • Cefdinir • Cefpodoxime • Cefuroxime • Ceftriaxone • Doxycycline • Azithromycin • Clarithromycin
45
Otitis Externa • most common causative bacteria
Otitis Externa • most common causative bacteria are Pseudomonas species Staphylococcus species, and anaerobes and gram-negative organisms.
46
Otitis Externa Tx?
• 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
Community-Acquired Pneumonia (CAP) organism?
❑S pneumoniae ❑H influenza ❑M catarrhalis
48
CAP treatment
• 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
Atypical Pneumonias organism?
Atypical Pneumonias • Mycoplasma pneumoniae • Chlamydia pneumoniae • Chlamydia psittaci • Legionella pneumophila
50
Chlamydia pneumoniae tx?
Chlamydia pneumoniae Macrolides (Azithromycin) Alt: Tetracyclines (Doxycycline) Fluoroquinolones
51
Mycoplasma pneumoniae tx?
Macrolides (Azithromycin): Children and adults ALT: Tetracyclines (Doxycycline): Older children and adults Fluoroquinolones: Adults
52
Chlamydia psittaci tx?
Chlamydia psittaci Tetracyclines (Doxycylcine) Alt: Macrolides (Azithromycin)
53
Legionella pneumophila tx?
Fluoroquinolones (levofloxacin, moxifloxacin, gemifloxacin) Macrolides (azithromycin) Alt:Tetracyclines (Doxycylcine
54
Tetracyclines MOA Drugs Interaction/toxicities
• 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
Prevents bacterial protein synthesis by binding to the 50S ribosomal subunit? Interaction/toxicity
Erythromycin • Azithromycin • Clarithromycin • cytochrome P450 inhibitor Toxicity: • Gastrointestinal upset, • QTc prolongation
56
FLUOROQUINOLONES MOA Toxicity
• Moxifloxacin • Gemifloxacin • Levofloxacin Inhibits DNA replication by binding to DNA gyrase and topoisomerase IV • Toxicity: neurotoxicity, tendonitis
57
• Amphotericin B MOA S/E
• 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
• Flucytosine
• Flucytosine • Converted by fungal enzyme cytosine deaminase to 5-fluorouracil, which then inhibits nucleic acid synthesis•Bone marrow suppression
59
Tx for histoplasmosis
Amphotericin B Azoles/triazoles
60
Tx Coccidioidomycosis
Amphotericin B Fluconazole/itraconazole
61
Tx Blastomycosis
Amphotericin B Itraconazole
62
Tx Cryptococcosis
Amphotericin B Fluconazole Flucytosine + amphotericin B
63
Tx Aspergillosis
Voriconazole Posaconazole Echinocandins (Caspofungin)
64
Mucormycosis tx
Lipid amphotericin B Echinocandins (Caspofungin)
65
Sporotrichosis TX
Itraconazole Amphotericin B
66
Pneumocystis pneumonia Tx
Trimethoprim/sulfamethoxazole
67
Fungal infections of the respiratory system
• Coccidioides immitis • Pneumocystis jeroveci • Cryptococcus neoformans • Aspergillus fumigatus • Histoplasma capsulatum • Mucor species • Sporothrix schenckii • Blastomyces dermatitidis
68
Azoles MOA S/E
•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
Echinocandins MOA S/E
Echinocandins •Disrupts cell wall synthesis by inhibiting beta-glucan synthesis •Flushing • mediated by histamine
70
❑OSELTAMIVIR & ZANAMIVIR
❑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
❑PERAMIVIR
❑PERAMIVIR • Neuraminidase inhibitor • Activity against both influenza A and B viruses • Treatment of acute uncomplicated influenza in adults – IV
72
❑AMANTADINE & RIMANTADINE
❑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
BALOXAVIR MARBOXIL
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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