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73 Cards in this Set

  • Front
  • Back
What is considered the best anti-TB drug?
Isoniazid
How is Isoniazid metabolized?

Acetyl Transferase Polymorphism?
Acetylation in the liver and excreted in the urine.

People can be fast or slow acetylators
What is the most common side effect of isoniazid?
Neuropathy
What does Isoniazid do to the liver?

What are the symptoms?

What potentiates hepatotoxicity?
Hepatotoxicity

Fatigue, nausea, anorexia, yellow skin

Alcohol, Rifampin, Pyrazinamide
What does Isoniziad do to the p450 system?
Inhibits p450 so it will increase levels of other drugs
What are included in the Rifamycin family?

What kind of drugs are they?
Rifampin
Rifapentine
Rifabutine

Family of broad spectrum antibiotics
How is the absorption of rifamycin?

How is the distribution of rifamycin?
They are well absorbed in the GI (Rifampin in the absence of food)

They are well distributed to body tissues and fluids including CSF.
What is the mechanism of action of Rifamycins?
They inhibit bacterial RNA-polymerase blocking protein syntehsis. They are selective since it doesn't act on mammalian RNA polymerase
Bacterial resistance of rifamycins.
Occurs quickly by protein mutations that reduce the affinity of RNA-polymerase to these drugs.
How are rifamycins eliminated?
Hepatic Metabolism
What types of infections can Rifamycins treat?
TBC, MAC, Leprosy, and short term treatment of nasopharynx infection caused by Neissara menigitdis and MRSA
What do rifamycins do to the P450 system?
Strongly induces them
What is pyrazimide?
Bactericidal for M. Tuberculosis
How is pyrazimide metabolized?
Well absorbed in GI. Metabolized to 5-OH pyrzinoic acid and excreted by kidneys.
What is ethambutol?
It is a bacteriostatic drug effective only against M. Tuberculosis.
What is the mechanism of action of Ethambutol?
Blocks the incorporation of mycolic acid to the cell wall.
How is ethambutol metabolized?
Absorbed well in the GI. Excreted by Kidneys. It inhibits renal excretion of uric acid.
What are side effects of Ethambutol?
Dose related optic neuritis: Blurred vision
Disturbance of color discrimination

Allergic Reactions:
Pruritis
Dermatitis

GI Disturbances
What is the difference between first line and second line drugs of TB?

How are they used?
2nd line drugs are more toxic and less effective.

In combo with first line drugs to treat pulmonary and disseminated tb.
Describe Aminosalicylic acid.
Analog of PABA.
Mechanism is similar to sulfonamides.
Only effective towards M. Tb
A bacteriostatic drug.
Metabolism of Aminosalicylic acid?
Absorbed from GI, and excreted in urine.
SE of Aminosalicylic acid?
Main: GI disturbances

Other: Allergic reactions, goiter, and hepatoxicity.
Describe Ethionoamide
Prodrug only active against M Tb.

Structurally similar to Isoniazid
What is the mechanism of action of Ethionamide?
Disruption of mycolic acid synthesis
SE of Ethionamide?
Hepatotoxic

GI disturbances
What type of drug is cycloserine and how does it work?
It is a bacteriostatic drug. It inhibits enzymes involved in cell wall synthesis
What is cycloserine used for?
Treat drug resistant TB.
SE of Cycloserine?
CNS Effects
Peripheral neuropathy
Hepatoxicity
Folate Deficiency
Capreomycin (Describe)
Cyclic Peptide related to aminoglycosides antibiotics

Inhibits protein synth of mycobacterium

Combo with first line TB drugs to treat drug resistant TB.

Cranial Nerve toxicity. Nephrotoxic.
Kanamycin and Amikacin (Describe)
Aminoglycoside antibiotics

Combo with first line drugs to treat drug resistant TB
Ofloxacin and Ciproflaxcin (Describe)
Fluroquinolone antibiotics.

Combo with first line drugs to treat drug resistant TB

Prophylaxis
What are the two classes of leprosy?
Paucibacillary (PB)
Multibacillary (MB) - skin lesions
What must you do with drugs therapy if there is a chance of resistance?
Use a combination therapy
Describe Dapsone
Related to sulfonamides and has similar mechanism of action. Bactericidal or bacteriostatic.

To avoid resistance it is used with Rifamin and Clofazimine
SE of Dapsone
Se: N/V, anorexia, HA, Rashes

Like sulfonamides it can cause hemolytic anemia
Describe Clofazimine
bactericidal

Used in combo with Dapsone and Rifampin
Metabolism of Clofazimine
Absorbed partially in GI. Retained in tissue for a long time. Very long t1/2
SE of clofazimine
Red pigmentation of Skin and conjunctiva, may discolor, urine sweat, tears, and saliva

Can cause intestinal pain and obstructions
What is a common infection in HIV patients?
MAC usually caused by M. avium or M. Intracellulare.
Where does the MAC infection usually reside and where does it spread in HIV patients?
Usually limited to Lungs and GI.

In HIV spreads to: Blood, bone marrow, liver, spleen, brain, kidney, and skin
SE of Rifabutin
Rash, GI upset and Neutropenia

Can produce brown-orange color in urine, sweat, tears and saliva

Uveitis have occured in patients taking Rifabutin in combo with clarithromycin.
What does Rifabutin do to p450 system?
Induces it
What is ribabutin prescribed for?
Prophylaxis of MAC
What does clarithromycin do to p450?
Inhibits
What does azithromycin do to p450?
Does not inhibit
What is the drug therapy for treating disseminated MAC?
Ethambutol + one of those macrolides
How does amphotericin B work?
Binds to ergosterol and causes membrane leakages. (K+)

Fungicidal or fungistatic
SE ofAmphotericin B
Nephrotoxic
Route of administration of Amphotericin B
Is not absorbed in GI so must be given IV.

If fungal meningitis then it must be intrathecal
SE of Amphotericin B when it is being administrated?

What can do you before you administer?
Fever, chills, rigors, nausea, HA.

Pretreat with aspirin or acetaminophen
What drug causes a synergistic effect with AmphotericinB?
Flucytosine
What does nystatin treat? and why is this so?
GI fungal infections (Candidiasis) since it is not absorbed in GI tract.
What is the mechanism of action of Imidazles and triazoles?
Inhibit enzyme needed during egrosterol synthesis.

Fungicidal or static
What do aozles do to p450?
Inhibits
What must patients avoid taking when on Keoconazole?
PPI, antacids etc.
This drug needs acidic environemnts
How is ketoconazole metabolized?
Metabolized in liver excreted in bile.
SE of Ketoconazole
Hepatoxocitiy
This drug inhibits steroid synth so there will be endocrine SE.
Parenteral Administeration of Miconzaole can cause?
Phlebitis
Nausea
Rash
Vomiting
Thrombocytosis
Pruritis
Fever
What does Itraconazole treat?
Blastomycosis
Histoplasmosis
Aspergillosis
Oral/Esophageal Candidiasis
Onychomycosis
Mechanism of action of Itraconazole
Inhibits synthesis of Ergosterol
SE of itraconaozle
N/V Diarrhea, HA, rash, abdominal pain

Negative inotropic effect on heart
What does fluconazole treat?
Oropharyngeal and Esophageal cadidiasis

Meningitis caused by Crytoccocus Neoformans and Coccidiodes Immitis
SE of Fluconazole?
All the obvious ones
What is the mechanism of action of Caspofungin
inhibits 1,3-b-glucan synthase, which helps synthesize cell walls

Fungicidal against Candida ssp.
SE of caspofungin
May cause histamine release
SE of topical Azoles
Skin: Erythema, Edema, Urticaria, Pruritus

Intravaginal: Burning sensation and lower abdominal cramps
What is Griseofulvin prescribed for?
If topical azoles don't work.
Treats:
Onychomycosis
Dermatophytoses (mainly tinea capitis)
Metabolism of Griseofulvin
GI absorption. Fatty foods increase absorption.

Excreted in Feces.
SE of Griseofulvin
All the obvious ones
What does Griseofulvin do to the p450 system?
May induce it.
How do the Topical Allylamines work?
Inhibits Squalene 2-3 epoxidase that is used for ergosterol synth.
Oral terbinafine is used for?
Onychomycosis
What does Tolfnaftate work against?
Dermatophytic infections and not candida