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73 Cards in this Set
- Front
- Back
What is considered the best anti-TB drug?
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Isoniazid
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How is Isoniazid metabolized?
Acetyl Transferase Polymorphism? |
Acetylation in the liver and excreted in the urine.
People can be fast or slow acetylators |
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What is the most common side effect of isoniazid?
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Neuropathy
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What does Isoniazid do to the liver?
What are the symptoms? What potentiates hepatotoxicity? |
Hepatotoxicity
Fatigue, nausea, anorexia, yellow skin Alcohol, Rifampin, Pyrazinamide |
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What does Isoniziad do to the p450 system?
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Inhibits p450 so it will increase levels of other drugs
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What are included in the Rifamycin family?
What kind of drugs are they? |
Rifampin
Rifapentine Rifabutine Family of broad spectrum antibiotics |
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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. |
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What is the mechanism of action of Rifamycins?
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They inhibit bacterial RNA-polymerase blocking protein syntehsis. They are selective since it doesn't act on mammalian RNA polymerase
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Bacterial resistance of rifamycins.
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Occurs quickly by protein mutations that reduce the affinity of RNA-polymerase to these drugs.
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How are rifamycins eliminated?
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Hepatic Metabolism
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What types of infections can Rifamycins treat?
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TBC, MAC, Leprosy, and short term treatment of nasopharynx infection caused by Neissara menigitdis and MRSA
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What do rifamycins do to the P450 system?
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Strongly induces them
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What is pyrazimide?
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Bactericidal for M. Tuberculosis
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How is pyrazimide metabolized?
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Well absorbed in GI. Metabolized to 5-OH pyrzinoic acid and excreted by kidneys.
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What is ethambutol?
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It is a bacteriostatic drug effective only against M. Tuberculosis.
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What is the mechanism of action of Ethambutol?
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Blocks the incorporation of mycolic acid to the cell wall.
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How is ethambutol metabolized?
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Absorbed well in the GI. Excreted by Kidneys. It inhibits renal excretion of uric acid.
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What are side effects of Ethambutol?
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Dose related optic neuritis: Blurred vision
Disturbance of color discrimination Allergic Reactions: Pruritis Dermatitis GI Disturbances |
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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. |
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Describe Aminosalicylic acid.
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Analog of PABA.
Mechanism is similar to sulfonamides. Only effective towards M. Tb A bacteriostatic drug. |
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Metabolism of Aminosalicylic acid?
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Absorbed from GI, and excreted in urine.
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SE of Aminosalicylic acid?
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Main: GI disturbances
Other: Allergic reactions, goiter, and hepatoxicity. |
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Describe Ethionoamide
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Prodrug only active against M Tb.
Structurally similar to Isoniazid |
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What is the mechanism of action of Ethionamide?
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Disruption of mycolic acid synthesis
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SE of Ethionamide?
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Hepatotoxic
GI disturbances |
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What type of drug is cycloserine and how does it work?
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It is a bacteriostatic drug. It inhibits enzymes involved in cell wall synthesis
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What is cycloserine used for?
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Treat drug resistant TB.
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SE of Cycloserine?
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CNS Effects
Peripheral neuropathy Hepatoxicity Folate Deficiency |
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Capreomycin (Describe)
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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. |
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Kanamycin and Amikacin (Describe)
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Aminoglycoside antibiotics
Combo with first line drugs to treat drug resistant TB |
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Ofloxacin and Ciproflaxcin (Describe)
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Fluroquinolone antibiotics.
Combo with first line drugs to treat drug resistant TB Prophylaxis |
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What are the two classes of leprosy?
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Paucibacillary (PB)
Multibacillary (MB) - skin lesions |
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What must you do with drugs therapy if there is a chance of resistance?
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Use a combination therapy
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Describe Dapsone
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Related to sulfonamides and has similar mechanism of action. Bactericidal or bacteriostatic.
To avoid resistance it is used with Rifamin and Clofazimine |
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SE of Dapsone
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Se: N/V, anorexia, HA, Rashes
Like sulfonamides it can cause hemolytic anemia |
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Describe Clofazimine
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bactericidal
Used in combo with Dapsone and Rifampin |
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Metabolism of Clofazimine
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Absorbed partially in GI. Retained in tissue for a long time. Very long t1/2
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SE of clofazimine
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Red pigmentation of Skin and conjunctiva, may discolor, urine sweat, tears, and saliva
Can cause intestinal pain and obstructions |
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What is a common infection in HIV patients?
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MAC usually caused by M. avium or M. Intracellulare.
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Where does the MAC infection usually reside and where does it spread in HIV patients?
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Usually limited to Lungs and GI.
In HIV spreads to: Blood, bone marrow, liver, spleen, brain, kidney, and skin |
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SE of Rifabutin
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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. |
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What does Rifabutin do to p450 system?
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Induces it
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What is ribabutin prescribed for?
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Prophylaxis of MAC
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What does clarithromycin do to p450?
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Inhibits
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What does azithromycin do to p450?
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Does not inhibit
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What is the drug therapy for treating disseminated MAC?
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Ethambutol + one of those macrolides
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How does amphotericin B work?
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Binds to ergosterol and causes membrane leakages. (K+)
Fungicidal or fungistatic |
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SE ofAmphotericin B
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Nephrotoxic
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Route of administration of Amphotericin B
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Is not absorbed in GI so must be given IV.
If fungal meningitis then it must be intrathecal |
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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 |
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What drug causes a synergistic effect with AmphotericinB?
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Flucytosine
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What does nystatin treat? and why is this so?
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GI fungal infections (Candidiasis) since it is not absorbed in GI tract.
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What is the mechanism of action of Imidazles and triazoles?
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Inhibit enzyme needed during egrosterol synthesis.
Fungicidal or static |
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What do aozles do to p450?
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Inhibits
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What must patients avoid taking when on Keoconazole?
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PPI, antacids etc.
This drug needs acidic environemnts |
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How is ketoconazole metabolized?
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Metabolized in liver excreted in bile.
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SE of Ketoconazole
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Hepatoxocitiy
This drug inhibits steroid synth so there will be endocrine SE. |
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Parenteral Administeration of Miconzaole can cause?
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Phlebitis
Nausea Rash Vomiting Thrombocytosis Pruritis Fever |
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What does Itraconazole treat?
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Blastomycosis
Histoplasmosis Aspergillosis Oral/Esophageal Candidiasis Onychomycosis |
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Mechanism of action of Itraconazole
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Inhibits synthesis of Ergosterol
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SE of itraconaozle
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N/V Diarrhea, HA, rash, abdominal pain
Negative inotropic effect on heart |
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What does fluconazole treat?
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Oropharyngeal and Esophageal cadidiasis
Meningitis caused by Crytoccocus Neoformans and Coccidiodes Immitis |
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SE of Fluconazole?
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All the obvious ones
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What is the mechanism of action of Caspofungin
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inhibits 1,3-b-glucan synthase, which helps synthesize cell walls
Fungicidal against Candida ssp. |
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SE of caspofungin
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May cause histamine release
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SE of topical Azoles
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Skin: Erythema, Edema, Urticaria, Pruritus
Intravaginal: Burning sensation and lower abdominal cramps |
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What is Griseofulvin prescribed for?
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If topical azoles don't work.
Treats: Onychomycosis Dermatophytoses (mainly tinea capitis) |
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Metabolism of Griseofulvin
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GI absorption. Fatty foods increase absorption.
Excreted in Feces. |
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SE of Griseofulvin
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All the obvious ones
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What does Griseofulvin do to the p450 system?
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May induce it.
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How do the Topical Allylamines work?
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Inhibits Squalene 2-3 epoxidase that is used for ergosterol synth.
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Oral terbinafine is used for?
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Onychomycosis
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What does Tolfnaftate work against?
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Dermatophytic infections and not candida
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