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name Antituberculous Drugs
- 1. Isoniazid (INH)
- 2. Rifampin
- 3. Ethambutol
- 4. Pyrazinamide
- 5. Aminoglycosides
- 6. Capreomycin
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1. Isoniazid (INH)
MOA
Inhibition of mycolic acid synthesis (Cell wall synthesis)
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1. Isoniazid (INH)
Resistance: high and low
- High Resitance: Deletion in katG gene
- encode catalase enzyme needed for INH bioactivation
- Low resistance
: Deletion in INHA gene - gene encoding acyl carrier protein (Target)
-
Isoniazid (INH)
Adverse Effects:
- Hepatitis
- Neuritis
- Hemolysis in G6PD deficiency
- SLE in slow acetylators
-
Why Pyridoxine (Vit B6) is used with INH?
- Help prevent numbness and tingling that occur
- secondary to Isoniazid neuritis
-
Rifampin
MOA
inhibits DNA-dependant RNA polymerase
-
Rifampin
Resistance
Mutationin polymerase enzyme
-
Rifampin
Adverse Effects:
- Red-orange discoloration of urine
- sweat, and tears
- Proteinuria
- Flu-like symptoms
- Thrombocytopenia
- Induces p450
-
Ethambutol
MOA
Inhibitssynthesis of Arabinogalactan (Component of cell wall)
-
Ethambutol
Adverse effects:
- Loss of red green acuity
- Retrobulbar neuritis
-
Pyrazinamide
Adverse effects:
- Arthralgia due to hyperuricemia
- Hepatotoxicity
- Increase porphyrin synthesis
-
Aminoglycosides
MOA
Inhibit protein synthesis
-
Aminoglycosides
Adverse effects buzz word:
- Streptomycin: Hearing loss, ataxia, nephrotoxicity
- Amikacin: Nystagmus
- Kanamycin: Electrolyte abnormalities
-
Capreomycin
Adverse effects
Hearing loss, ataxia
-
Capreomycin
Buzz word
No cross resistance with aminoglycosides Used as 2nd line for Rx of resistant TB with Aminosalicylic acid and cycloserine
-
name
Disseminated Mycobacterium Avium Complex
DMAC
Azithromycin + Rifabutin + Ethambutol
-
Rifabutin: Similar to
Rifampin
-
Disseminated Mycobacterium Avium Complex
DMAC
Adverse effects:
- Rashes, GI effects
- Neutropenia
- Induces p450
- No Hepatotoxicity
-
Clinical TB
TB screening
- PPD=Purified Protein Derived
- Screen Asymptomatic Population
-
TB screening
What's +ve?
- > 10mm of induration
- (not erythema)
-
TB screening
What's -ve risk?
- > 5mm with HIV +ve
- or Close contact
-
For anyone PPD +ve
What you do next?
Chest X-Ray
-
if Chest X-Ray -ve
Rx INH alone for 6 Months
-
if Chest X-Ray +ve
- Sputum Cultures
- if +ve --> Rx 4 drugs
- if -ve --> Rx INH alone for 6 Months
-
BCG immunization gives only
3-4 mm induration for 5 years
-
If after 10 years PPD >10mm induration
- Don't blame it on BCG
- You gotta follow protocol
- Chest X-Ray
-
How long you treat TB?
4 Drugs X 2 months (INH-Rif-PZA-Ethamb) + 2 Drugs X 4 months (INH-Rif) = 6 months
-
How long you treat TB?
What if HIV +ve?
- Initial therapy stay the same then increase duration
- 4 Drugs X 2 months (INH-Rif-PZA-Ethamb) + 2 Drugs X 7 months (INH-Rif)= 9 Months
-
A 37y/old Prisonner, cough, fever, sputum
SOB, lung infiltrate, sputum AFB +ve
- Never answer PPD in a case of TB
- Answer Rx
- 4 Drugs X 2 months + 2 Drugs X 4 months
-
Pregnant with +ve PPD Be careful here
- Answer Chest X-Ray with lead Apron(2nd Trimester)
- if -ve ->Wait until delivery Then INH alone bc INH is bad to the baby "Teratogenic"
- if +ve -> Sputum Cultures if -ve Rx INH alone, if +ve Rx 4 drugs
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Side Effects of Isoniazid
Neuritis
-
name
Antiprotozoal
- 1. Giardiasis: Giardia Lamblia
- 2. Amebiasis: Entamoeba Histolytica
- 3. Trichomoniasis: Trichomonas vaginalis
- 4. Leishmaniasis: Leishmania Brasiliensis
- 5. Trypanosomiasis: Trypanosoma cruzi
- 6. Toxoplasmosis: Toxoplasma Gondii
- 7. Pneumocystosis: Pneumocystis carinii
- 8. Malaria
-
1. Giardiasis: Giardia Lamblia
- Most common water born disease
- Back-packer's diarrhea
-
Metronidazole Rx for
- 1. Giardiasis: Giardia Lamblia
- 2. Amebiasis: Entamoeba Histolytica
- 3. Trichomoniasis: Trichomonas vaginalis
-
2. Amebiasis: Entamoeba Histolytica
Asymptomatic/non-invasive intestinal amebiasis
Diloxanide
-
3. Trichomoniasis: Trichomonas vaginalis
Rx?
- Metronidazole
- Gotta Rx the partner
-
4. Leishmaniasis: Leishmania Brasiliensis
American mucocutaneous leishmaniasis
Rx?
Stibogluconate
-
5. Trypanosomiasis: Trypanosoma cruzi
American Trypanosomiasis (Chagas disease)
Rx?
Nifurtimox
-
5. Trypanosomiasis: Trypanosoma cruzi
African trypanosomiasis (Sleeping sickness)
Rx?
Suramin + Melarsoprol
-
6. Toxoplasmosis: Toxoplasma Gondii
Rx?
Pyrimethamine + Sulfadiazine
-
7. Pneumocystosis: Pneumocystis carinii
Rx?
- Trimethoprin-Sulphamethoxazole
- IV Pentamidine
- Atovaquone
-
8. Malaria
PlasmodiumFalciparum: Rx?
Chloroquine
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8. Malaria
Plasmodium Malariae Rx?
Chloroquine
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8. Malaria
Plasmodium Vivax
Rx?
Chloroquine + Primaquine
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8. Malaria
Plasmodium Ovale
Chloroquine + Primaquine
-
Prophylaxis for chloroquine-sensitive Malaria:
- Chloroquine +/- Primaquine
- Second line: Pyrimethamine-sulfadoxine, Hydroxychloroquine
-
Prophylaxis for Chloroquine-Resistant Malaria:
- Mefloquine
- Second line: Atovaquone-proquanil, Doxycycline
-
Rx for Chloroquine-Resistant Malaria
Quinine +/- Doxycycline
-
Adverse effects of Antimalarial
Chloroquine:
Pruritis, ocular dysfunction, hemolysis (Avoid in psoriasis)
-
Adverse effects of Antimalarial
Mefloquine
- Syncope,extrasystoles
- Avoid in seizure and cardiac arrhythmias
-
Adverse effects of Antimalarial
Primaquine:
- Neutropenia, hemolysis
- Avoid in pregnancy, G6PD deficiency.
-
Adverse effects of Antimalarial
Quinine:
- Cinchonism, CNS defects, hemolysis
- Avoid in pregnancy
-
Intestinal Nematodes: (Worms)
Rx?
- Mebendazole
- Pyrantel pamoate
-
Mebendazole MOA
Decrease glucose uptake and microtubular structure
-
Tissue Nematodes Rx?
Ivermectin
-
Cestodes (Tapeworms) & Trematodes (Flukes)
Rx:
Praziquantel
-
Praziquantel
MOA
Increase Ca++ influx
-
Thiabendazole: MOA
inhibits fumarate reductase
-
Dibucaine: MOA
inhibits Na+ permeability
-
Piperazine: MOA
Inhibits acetylcholine leading to muscle paralysis
-
-
Dapsone Rx of
leprosyand dermatitis herpitiformis
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Thalidomide:
FDA approved for Rx of
Erythema nodosum leprosum
-
Thalidomide:
FDA pregnancy category
- X
- Physicians should alert male and female patients in effective methods of birth control
- bc Risk of phocomelia (absent arms and legs)
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