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x SCO summer 2015 Pharmacology > Final exam > Flashcards

Flashcards in Final exam Deck (408):
1

HIV drug selection strategy:

Varying mechanisms, toxicities, patient symptoms, drug interactions, and adherence/administration convenience

2

How do supplements differ from drugs and OTC medications?

they are legally considered food supplements used for health maintenance even if they're really "drugs"

3

What drugs can cause jaundice?

Macrolides/Ketolides,

4

Efavirenz

HIV drug, NNRTI that causes conformational change to HIV-1 reverse transcriptase. P450 inducer, *great half-life, can cause vivid dreams

5

What drugs can cause crystalluria?

Sulfonamides

6

Moa: inhibits protein and RNA synthesis in trypanosomiasis

Benznidazole. Tx Chagas disease

7

Rifampin AE:

Uncommon Nausea, vomiting, rash. Orange feces, urine, and tears. Increase p450 metabolism

8

What are the 3 approaches of developing a new drug?

New drug targets, new drugs based on receptor structure, modification of known molecule

9

Metronidazole

Mixed Amebicides AND tx Giardiasis. Moa form cytotoxic compounds that bind to proteins and DNA. *AE metallic taste, rare neurological disorder. resistance not a problem. Tx of choice for Giardiasis.

10

Ginseng

Botanical/Herbal. used as an upper: increased NT in CNS. anti-inflammatory, anti-cancer

11

What supplement has antibiotic effects?

Echinacea, Garlic

12

Rimantadine

Respiratory flu drug. inhibits viral uncoating. Blocks viral membrane matrix protein M2 so viral and host membrane can't fuse.

13

What do Trophozoites do?

Entamoeba histolytica trophozoites multiply and invade intestinal mucosa or feed on intestinal bacteria

14

What treats pneumonia in immunocompromised patients?

Cotrimoxazole (Trimethoprim + Sulfamethoxazole)

15

Ofloxacin

*2nd line antimycobacterial and 2nd Gen Fluoroquinolone. Enters bacteria via diffusion; uses dual mechanism to inhibit DNA gyrase and topoisomerase IV. *inexpensive

16

What is the resistance of aminoglycosides?

Resistance not severe when topical

17

Which malaria drug has a very long half-life?

Mefloquine

18

Itraconazole

*Antifungal, Azole. Inhibits P450 enzyme that converts lanosterol to ERGOSTEROL, disrupting fungal membrane. *Tx histoplasmosis, take with food (needs acid)

19

What are the two forms of
Entamoeba histolytica?

Cyst and Trophozoite (survives in body)

20

How long do drug patents last? What is the average effective patent life of a drug?

20 years but includes approval time. Average effective patent life for major pharmaceuticals is around 11 years

21

What causes dysentery?

Entamoeba histolytica

22

AE Linezolid:

Thrombocytopenia, Anemia, Optic and peripheral neuropathy. Caution with MAOIs and SSRIs

23

Which drugs are the luminal Amebicides

Iodoquinol and Paromomycin (think IodoParo luminal)

24

What supplement is used for decreasing blood pressure?

Garlic

25

What are the limitations to pre-clinical testing?

Time-consuming and expensive (can take up to 6 years), Large numbers of animals needed to obtain valid data, Animal to human toxicity data not always predictive, and Rare adverse effects are not likely to be identified.

26

Which rifamycin has the longest half-life?

Rifapentine

27

What is the resistance of Amphotericin B?

Infrequent

28

What is the commonly diagnosed intestinal parasite in the U.S?

Giardia lamblia

29

Posaconazole

*Antifungal, Azole. Inhibits P450 enzyme that converts lanosterol to ERGOSTEROL, disrupting fungal membrane. *the most broad spectrum azole

30

Chloroquine

Systemic Amebicides AND tx Malaria. Prevents malaria from digesting Hb; pH increases, heme accumulates, parasite AND rbc lyse! rapidly oral, cure in 4 days. Tx erythrocytic form. AE: minimal, can cause bull's-eye maculopathy. Malaria resistance become a problem--combo therapy resolves. ALSO tx inflam disease like rheumatoid arthritis and lupus

31

Which amebicide is actually an aminoglycoside antibiotic?

Paromomycin (luminal amebicide)

32

Darunavir

HIV protease inhibitor. inhibits HIV aspartyl protease to prevent viral maturation. MANY drug-drug interactions.

33

Which drug class causes vestibular problems?

Tetracyclines

34

MOA: Inhibits many enzymes involved in energy metabolism of Trypanosomiasis

Suramin (Trypanosomiasis)

35

Amikacin

PSI Aminoglycoside. Binds to 30s ribo subunit preventing protein synthesis initiation AND cause misreading of mRNA causing wrong AA insertion.

36

5 classes of HIV drugs:

1 Nucleoside/tide reverse transcriptase inhibitors (NRTIs), 2 Nonnucleoside reverse transcriptase inhibitors (NNRTIs), 3 Protease inhibitors, 4 Entry inhibitors, 5 Integrase inhibitors

37

Linezolid

PSI, "other". binds to 50s subunit to inhibit ribosome complex formation.

38

Abacavir

HIV drug, NRTI, nucleoside/tide integrates into DNA, terminating DNA elongation. *good for renal failure patients. can cause a fatal allergic reaction upon second exposure

39

AE for Amphotericin B:

It has a low therapeutic index. , Fever/Chills, Muscle spasm, Vomiting, Headache, Hypotension. Cumulative: renal impairment

40

AE of tetracyclines:

Gastric discomfort w/ Ca++ Food. Severe sunburns. Vestibular problems. Pseudotumor cerebri

41

What supplement is used as antidepressant?

St. John’s Wort

42

What portion of the world is exposed/infected with Tb?

1/3

43

What drugs are neuraminidase inhibitors?

Oseltamivir and Zanamivir (OselZana)

44

Ganciclovir

Cytomegalovirus drug. Guanosine analog gets incorporated into viral DNA via DNA poly. avoid in pregnancy, and renal failure. Available in ocular preparation (Zirgan). Easy dosing but expensive

45

Which antimycobacterial involves prodrugs?

Isoniazid and Ethionamide

46

What are the phases of new drug?

Drug discovery, screening, preclinical testing, human testing, clinical trials, (phase 1-4)

47

Which Fluoroquinolone is bad systemically but good for UTIs and GI disease?

Norfloxacin

48

What drug class competes with dihydropteroate synthetase and inhibit folate production?

Sulfa drugs

49

Coenzyme Q10

Purified Supplements. used for hypertension, improving output in heart failure, prevents statin-induced myopathy

50

Resistance for tetracyclines:

Widespread

51

Sulfacetamide

Antifolate. Prohibits bacterial production of folate because drug is PABA analogue and competes with dihydropteroate synthetase.

52

Which drugs are dangerous for pregnant women?

Tetracyclines, Trimethoprim (antifolate), Fluoroquinolones, Isoniazid (first line), Inhibitors of viral uncoating (caution), Ribavirin (Hepatitis), Ganciclovir (cytomeg and corneal herpes), Antiprotozoal agents,

53

Emetine

Systemic Amebicides. inhibits protein synthesis. Via IM; oral might cause vomiting. Can concentrate in liver for a month

54

Nifurtimox

tx Trypanosomiasis, acute Chagas.MOA: oxygen radicals toxic to both host/parasite but human enzymes fix damage. Adverse Effects:, Hypersensitivity (acute and delayed), GI problems (sometimes severe), Peripheral neuropathy

55

What is the goal of phase 1 clinical trials?

Determine the probable limits of the safe clinical dosing range. Absorption, half-life, and metabolism are also often studied in this phase

56

What ophthalmic drug causes lots of irritation? Which is easy on the eye?

The inexpensive Trifluridine irritates and requires frequent dosing. The more expensive Ganciclovir is easier on the eye and has easier dosing.

57

How are macrolides/ketolides administered?

Oral is good. Erythromycin should NOT be given IV

58

Which trypanosomiasis drug is recommended
as prophylaxis in hematopoietic stem cell transplant recipients?

Benznidazole

59

What can cause ototoxicity?

Aminoglycosides, macrolides (esp erythromycin), Capreomycin (2L antimycobacterial)

60

What is the spectrum of Aminoglycosides?

Gram - (including pseudomonas) , some +

61

AE of NRTI:

Mainly due to inhibition of mitochondrial DNA polymerase; Can include peripheral neuropathy, pancreatitis, and lipoatrophy; All have been associated with potentially fatal liver toxicity

62

Which malaria drug is reserved for severe/resistant cases?

Quinine

63

What is the treatment of choice for Giardiasis?

Metronidazole for 5 days

64

What supplement is used for cartilage nutrient?

Glucosamine (purified supplement)

65

What drugs interact with bacterial RNA polymerase to block transcription?

Rifamycins (1L antimycobacterial)

66

Which are the drugs that prohibit viral uncoating?

Rimantadine and Amantadine

67

Which NRTI has a conveniently long half-life?

Tenofovir

68

What can cause bull's eye maculopathy?

Chloroquine (systemic amebicide and malaria drug) and Primaquine (Malaria drug)

69

What drugs are used to treat MRSA?

Vancomycin, Bacitracin, Ceftaroline (5th gen) (kinda Telavancin, kinda Daptomycin). Linezolid [PSI](except in MRSA bacteremia), Cotrimoxazole (antifolate)

70

What is included with an Investigational New Drug (IND)?

Composition, chemical/manufacturing info, animal studies data, clinical trial plans, names and credentials, relevant data for humans

71

What's the difference between acute, subacute, and chronic toxicity?

Acute is determined of maximum dose, subacute is long-term dose toxicity (weeks to months), and Chronic toxicity is even longer

72

Demeclocycline

PSI, Tetracycline. reversibly binds to 30s ribo. subunit preventing tRNA binding--translation stops.

73

Rifampin

*First-line antimycobacterial. inhibits RNA polymerase to prevent transcription. induces P450, ORANGE POOP

74

Tetracycline

PSI, Tetracycline. reversibly binds to 30s ribo. subunit preventing tRNA binding--translation stops.

75

What 1st line antimycobacterial is preferred for HIV patients?

Rifabutin

76

Which Fluoroquinolone have the longest half-lives?

Levofloxacin and moxifloxacin

77

AE: cinchonism: Nausea, Vomiting, Tinnitus, Vertigo

Quinine (malaria drug)

78

What drugs are bad with antacids?

Quinine (malaria drug),
Fluoroquinolones and Tetracyclines (PSI)

79

Between acyclovir,
Valacyclovir, and Famciclovir, which is safest in pregnancy?

Famciclovir (anti-herpes)

80

What is the oral mouthwash for thrush?

Nystatin

81

What is the goal in phase 4 post marketing?

Monitor the safety of the new drug under actual conditions of use in large numbers of patients. Requires reporting by all physicians using the medications (because some adverse effects may become apparent only after chronic dosing)

82

Melatonin

Purified Supplements. used for jet lag, insomnia, and improving sleep

83

HIV treatment now consists of suppressing HIV replication, allowing for restoration of ___ cells and immunocompetence

CD4 or T Helper Cells

84

Benznidazole

tx Trypanosomiasis. alternative for Chagas disease. Moa: inhibits protein and RNA synthesis. Recommended as prophylaxis in hematopoietic stem cell transplant recipients.

85

What is the second-line antifungal if amphotericin B or azole fails?

Caspofungin (Echinocandin)

86

Milk Thistle

Botanical/Herbal. used for treating liver disease, anti-cancer, promotes lactation

87

What drug causes squalene to build up to toxic levels?

Terbinafine (antifungal)

88

Ethambutol

First-line antimycobacterial. interferes with cell wall synthesis *EOM pain primary complaint with red/green color deficiency and optic neuritis

89

Which of the Amebicides can cause optic neuritis?

Iodoquinol.

90

Etravirine

HIV drug, NNRTI that causes conformational change to HIV-1 reverse transcriptase. P450 inducer,

91

How are Sulfonamides metabolized and excreted?

Liver metabolized kidney excreted

92

Mefloquine

Malaria drug. *tx erythrocytic form. Has very long half life. good for pregnant. AE: Nausea and vomiting, Dizziness, Disorientation and depression, Cardiac arrest possible if taken concurrently with quinine or (quinidine)

93

Macrolides/Ketolides contraindications:

Hepatic dysfunction, arrhythmia

94

What drug can cause vivid dreams?

Efavirenz (NNRTI)

95

What is clinically equivalent to acyclovir but have longer half lives?

Valacyclovir, Famciclovir (anti-herpes)

96

Spectrum of Rifamycins:

+/-, mycobacteria, Leprosy

97

St. John’s Wort

Botanical/Herbal. used as antidepressant, antiviral and anticarcinogenic

98

Pharmacokinetics for tetracyclines:

Avoid calcium, iron, antacids (reduces plasma concentration). Do not give to children, can cross placenta. Bile secreted.

99

AE for Trimethoprim:

Folic acid deficiency (leads to anemia, Leukopenia, Granulocytopenia)

100

Which amebicide is effective against both trophozoite and cyst forms?

Iodoquinol (luminal)

101

Adverse Effects:, Hypersensitivity (acute and delayed), GI problems (sometimes severe), Peripheral neuropathy

Nifurtimox (trypanosomiasis)

102

What is the most potent Tb medication?

Isoniazid

103

Primaquine

Malaria drug. perhaps toxic metabolites. *treats EXOerythrocytic forms, including in liver, gametocytic forms. can cause bull's-eye maculopathy. AE: can aggravate lupus/arthritis

104

How is one typically infected by Giardia lamblia?

Contaminated water (or food). Fecal-oral route

105

Which anti-viral is given intranasally?

Zanamivir

106

Voriconazole

*Antifungal, Azole. Inhibits P450 enzyme that converts lanosterol to ERGOSTEROL, disrupting fungal membrane. *inhibits P450, increasing warfarin conc

107

What leprosy drug also has anti-inflammatory activity?

Clofazimine

108

Which macrolide has a good half-life and high Vol of distribution?

Azithromycin

109

What supplement is used for increasing wbc?

Echinacea

110

AE Isoniazid (1L antimycobacterial):

Hepatitis and idiosyncratic hepatotoxicity, Peripheral neuritis, Mental abnormalities, convulsions, Optic neuritis, Hypersensitivity

111

Nystatin

*Antifungal, Polyene Antibiotic. binds to ergosterol in membrane making ion pore > death. *Tx topical Candida and Thrush mouthwash

112

Which NRTI has many antiretroviral drug interactions?

Tenofovir

113

Antibacterial spectrum for tetracyclines:

Considered broad spectrum, Gram(-) and Gram(+), Also against other organisms

114

What supplement is used for lowering cholesterol?

Garlic

115

What are the malaria drugs?

Chloroquine, Mefloquine, Primaquine, Quinine (think qui-quine). Chloroquine is also a systemic amebicide

116

Enfuvirtide

HIV drug, entry inhibitor that binds to viral transmembrane glycoprotein, preventing the conformational change that allows entry in cell.

117

What supplement used as an upper: increased NT in CNS?

Ginseng

118

AE Methenamine:

GI distress, formaldehyde reacts with Sulfonamides

119

What drug colors feces, urine, and tears ORANGE?

Rifampin (1L antimycobacterial)

120

Dolutegravir

HIV integrase inhibitor that inhibits final step of integration of viral DNA into host DNA. NO P450 interactions. *extensive liver metabolism once or twice dosing (twice if previous treatment with other integrase inhibitors.

121

Streptomycin

Second-line antimycobacterial aminoglycoside. MoA not given.

122

Tx fungal infections of nails?

Terbinafine (antifungal)

123

What drug interferes with the synthesis of B-glucan, causing lysis and cell death?

Echinocandins

124

Which antiviral has few side effects?

Lamivudine (anti hep/NRTI) .(rarely headaches/dizziness)

125

What is the mechanism of HIV protease inhibitors?

They inhibit HIV aspartyl protease to prevent the maturation of viral particles, making noninfectious virions

126

Elvitegravir

HIV integrase inhibitor that inhibits final step of integration of viral DNA into host DNA. NO P450 interactions. *only in combination with Tenofovir/Emtricitabine/Elvitegravir/Cobicistat

127

What drugs can cause GI disturbances?

Chloramphenicol (PSI), methenamine and nitrofurantoin (UTI tx), Flucytosine (antifungal), Ethionamide (2L antimycobacterial), HIV protease inhibitors, Nifurtimox (trypanosomiasis)

128

What drugs are bad to have with Zinc?

Fluoroquinolones

129

Which drug can cause tinnitus and vertigo?

Quinine (malaria drug)

130

What inhibits fungus until skin sloughs off?

Griseofulvin

131

What supplement is used for treating BPH (inflamed prostate)

Saw Palmetto

132

Goals for HIV treatment

Maximally and durable suppress viral load, replication, Restore and preserve immunologic function, Reduce HIV-related morbidity and mortality, Improve quality of life

133

How is the resistance in Cotrimoxazole?

Not frequent because bacteria needs to resist both drugs (Trimethoprim + Sulfamethoxazole)

134

Rifapentine

*First-line antimycobacterial. inhibits RNA polymerase to prevent transcription. *has long half-life

135

Flucytosine

Antifungal, "Other". drug enters fungal cell and is converted into the antimetabolite 5-FU

136

What is the mechanism of NRTIs?

Nucleoside/tide reverse transcriptase inhibitors are analogs that are incorporated into viral DNA by viral reverse transcriptase (once drug is phosphorylated). This terminates DNA chain elongation.

137

Emtricitabine

HIV drug, NRTI, nucleoside/tide integrates into DNA, terminating DNA elongation * has NO significant drug interactions.

138

What drugs can cause optic neuritis?

Isoniazid (Antimycobacterial), Ethambutol (1L antimycobacterial), Ethionamide (2L antimycobacterial), Iodoquinol (luminal amebicide)

139

Moa:
Prevents malaria from digesting Hb; pH increases, heme accumulates, parasite AND rbc lyse!

Chloroquine (also systemic amebicide )

140

What drug can cause hepatitis?

Isoniazid (1L Antimycobacterial)

141

Macrolides

Second-line antimycobacterial and PSI. Binds to 50s ribo. subunit (can inhibit its formation) to block peptidyl transferase center to prevent AA elongation.

142

Food impairs absorption of what drug?

Isoniazid (1L antimycobacterial)

143

Why are supplements not more widely accepted by the medical community?

Clinical studies are poorly designed and Do not account for placebo effect. Most studies not peer reviewed.

144

Clarithromycin

*PSI, Macrolide/Ketolide. Binds to 50s ribo. subunit (can inhibit its formation) to block peptidyl transferase center to prevent AA elongation. *also Tx H influenzae

145

Nitazoxanide

Tx Giardiasis

146

Sulfadiazine

Antifolate. Prohibits bacterial production of folate because drug is PABA analogue and competes with dihydropteroate synthetase. *COMBINED with pyrimethamine in toxoplasmosis tx.

147

What drugs can cause changes in glucose and lipid metabolism?

HIV protease inhibitors

148

What drugs can cause connective tissue problems?

Fluoroquinolones

149

Cotrimoxazole (Bactrim)

Antifolate. Trimethoprim + Sulfamethoxazole. Tx UTIs, Respiratory tract infections, Pneumocystis jiroveci pneumonia in immunocompromised patients

150

Tipranavir

HIV protease inhibitor. inhibits HIV aspartyl protease to prevent viral maturation. MANY drug-drug interactions. *cause severe and fatal hepatitis, rare intracranial hemorrhages

151

Which Fluoroquinolone is poor against pseudomonas and not good for UTIs?

Moxifloxacin

152

What disease causes some to be asymptomatic, others to have serious diarrhea (esp. in immunocompromised patients)?

Giardiasis (Giardia lamblia)

153

Which HIV protease inhibitor can cause diarrhea and is NOT boosted by Ritonavir?

Nelfinavir

154

Azithromycin (Zithromax, Zpak)

PSI, Macrolide/Ketolide. Binds to 50s ribo. subunit (can inhibit its formation) to block peptidyl transferase center to prevent AA elongation.

155

What drugs are best acidic?

Methenamine, nitrofurantoin.

156

Who should not take tetracyclines?

Kidney deficient (Doxycycline is ok), motherly women, children under 8, warfarin takers

157

What is the goal of neuraminidase inhibitors?

Decrease the intensity and duration of symptoms within 1-2 days of infection.

158

Antibacterial spectrum of Macrolides/Ketolides:

Similar to penicillin G (gram +)

159

What supplement is used for increasing blood flow and vasodilation?

Ginkgo

160

Methenamine

Urinary Tract Antiseptic. Makes formaldehyde at low 5.5 pH

161

Maraviroc

HIV drug, entry inhibitor that blocks binding of viral membrane to host cell on CCR5 receptor

162

Which drugs have a dual mechanism against bacteria?

Fluoroquinolones

163

Interferon

Viral Hepatitis drug. MoA poorly known: inhibit viral RNA translation

164

Norfloxacin

*2nd line antimycobacterial and 2nd Gen Fluoroquinolone. Enters bacteria via diffusion; uses dual mechanism to inhibit DNA gyrase and topoisomerase IV. *Tx GI disease and UTIs

165

What is the goal of phase 2 clinical trials?

determine efficacy

166

Drug resistance of NRTIs:

Only between same analog class

167

What drugs are used prophylactically in patients exposed to meningitis

Rifampin (1L antimycobacterial)

168

What is used prophylactically for sleeping sickness?

Suramin (trypanosomiasis)

169

Which drug class causes phototoxicity?

Tetracyclines, Fluoroquinolones

170

What is the drug of choice for histoplasmosis?

Itraconazole

171

What causes Chagas disease

American: trypanosomiasis via insect feces

172

Famciclovir

Herpesvirus drug. ?Guanosine analog gets incorporated into viral DNA via DNA poly. safest in pregnancy

173

Who is involved in phase 3 clinical trials?

larger numbers of patients with the target disease (usually thousands of patients)

174

Pyrazinamide

First-line antimycobacterial. Inhibits growth by lowering intracellular pH *can cause precipitate gout

175

Who is involved in phase 2 clinical trials?

100-200 subjects with target disease.

176

Which trypanosomiasis drugs treat American Chagas disease?

Nifurtimox and Benznidazole (alternative)

177

What's the difference between first and second line antimycobacterials?

Second line drugs are no more effective than first line agents but toxicities may be more serious.

178

What NRTI is best taken when fasting?

Didanosine

179

What is the goal of phase 3 clinical trials?

Establish and confirm safety and efficacy; designed to minimize errors caused by placebo effects and disease variations; Usually performed in settings similar to what is anticipated for the ultimate use of the drug (hospitals, clinics, etc)

180

How is Linezolid administered?

Oral is completely absorbed (IV also available)

181

Tx UTI:

Methenamine and nitrofurantoin (UTI antiseptics), Norfloxacin (fluoroquinolone),

182

MoA: interferes with heme polymerization.

Quinine (malaria drug)

183

What are the different types of amebicidal drugs?

Luminal, systemic, or mixed (both)

184

Tobramycin

PSI Aminoglycoside. Binds to 30s ribo subunit preventing protein synthesis initiation AND cause misreading of mRNA causing wrong AA insertion.

185

Which HIV protease inhibitor is a CYP450 inhibitor?

Ritonavir

186

What has been shown to block (dry) ARMD in mice? Through what mechanism?

NRTI (HIV drug), NRTIs block inflammation

187

Trimethoprim + Sulfamethoxazole makes

Cotrimoxazole

188

What phase of clinical trials has the highest failure rate?

Phase 2 with only 25% of drugs passing.

189

Ethionamide

Second-line antimycobacterial. Prodrug gets converted and blocks mycolic acid production

190

Clindamycin

PSI, "other". Binds to 50s ribo. subunit (can inhibit its formation) to block peptidyl transferase center to prevent AA elongation.

191

Sulfamethoxazole

Antifolate. Prohibits bacterial production of folate because drug is PABA analogue and competes with dihydropteroate synthetase.

192

Clofazimine

Antimycobacterial, Leprosy drug. binds to DNA to prevent using it as a template for replication. Has anti-inflammatory properties good for skin lesions

193

Isoniazid

*First-line antimycobacterial. Prodrug gets converted and blocks mycolic acid production. *most potent Tb medication. Absorption impaired w/ food

194

Summarize the forms of malaria

Sporozoite > cyst > merozoites released > trophozoite in RBC > gametocytes > repeat. Spock Cycles Mel's Trophy Game

195

What is the most broad spectrum azole?

Posaconazole

196

What drug can bacteria NOT form resistance to?

Methenamine (UTI antiseptic) because it makes formaldehyde

197

What causes sleeping sickness? Disease and vector

Africa: trypanosomiasis via tsetse fly

198

Mitochondrial DNA is susceptible to what drug class?

NRTI (HIV drug)

199

What can cause EOM pain as a primary complaint?

Ethambutol causing optic neuritis

200

Which drugs are the mixed Amebicides?

Metronidazole, Tinidazole (think MetronTin mixed). They are also part of Giardiasis tx.

201

What is an antiviral and HIV treatment?

Tenofovir and Lamivudine (anti hep and NRTI)

202

Azoles should not be used with ___

Amphotericin B

203

What is a treatment for erythrocytic forms of malaria?

Chloroquine (also systemic amebicide) is drug of choice, Mefloquine, Quinine

204

Suramin

tx Trypanosomiasis. moa:Inhibits many enzymes involved in energy metabolism. used prophylactically for sleeping sickness.

205

What is the life cycle of malaria?

Injected sporozoites from mosquito migrate through the blood to the liver to form cysts. Merozoites released and invade RBC and becomes trophozoite. Some trophozoites become gametocytes and get picked up by mosquitos.

206

Atazanavir

HIV protease inhibitor. inhibits HIV aspartyl protease to prevent viral maturation. MANY drug-drug interactions. *can cause slow heart rate

207

What disease is attracted to the macula?

toxoplasma gondii

208

What Parasite grows in blood and eventually invades CNS?

trypanosomiasis via tsetse fly causes Sleeping sickness (in Africa)

209

Quinine

Malaria drug. *interferes with heme polymerization. reserved for severe/resistant cases. AE: cinchonism: Nausea, Vomiting, Tinnitus, Vertigo

210

Which NNRTI has a long half-life and is the most preferred?

Efavirenz

211

What supplement is anti-pathogen?

Echinacea

212

What is the mechanism of NNRTIs?

They cause conformational change to HIV-1 reverse transcriptase and does not need to be activated by cellular enzymes. They don't affect the host cells.

213

What drugs can cause liver toxicity?

Isoniazid (1a Antimycobacterial) Ethionamide (2L Antimycobacterial), NRTI (HIV drug),

214

What is often given with
Amphotericin B?

Flucytosine

215

AE Sulfonamides:

Crystalluria, allergies, anemia, increase warfarin levels by inhibiting p450.

216

Which anti-CMV needs to be activated by viral enzyme?

Ganciclovir

217

Cidofovir

Cytomegalovirus drug. cytosine analog inhibits DNA synthesis wo/ need of viral enzymes. *Tx cmv-induced retinitis in AIDS patients

218

Which trypanosomiasis drugs treat African sleeping sickness?

Pentamidine and Suramin (prophylaxis)

219

Chloramphenicol

PSI, "other". binds to 50s ribo subunit to inhibit peptide bond formation.

220

Tx acute Chagas

Nifurtimox (trypanosomiasis)

221

What supplement is used for increasing cognition and concentration?

Ginkgo

222

Which integrase inhibitor is only available in combination?

Elvitegravir. With Tenofovir/ Emtricitabine/ Elvitegravir/ Cobicistat

223

How is Leishmaniasis transmitted?

Through sandfly bites

224

Cycloserine

Second-line antimycobacterial. Inhibits cell wall synthesis. *Exacerbates epileptic seizures

225

What drug can cause folic acid deficiency?

Trimethoprim (antifolate drug)

226

Which malaria drug is good for pregnant people?

Mefloquine (malaria drug)

227

Spectrum of chloramphenicol?

Very strong Broad spectrum

228

What is the treatment of choice for HSV encephalitis?

Acyclovir (anti-herpes)

229

What drug class binds to tissues undergoing calcification (children under 12)

Tetracycline

230

Which anti-viral would you not want to give to COPD or asthma people?

Zanamivir

231

What can be used to treat pneumonia in HIV patients?

Dapsone (leprosy drug)

232

Tigecycline

**PSI, "Tetracycline"; actually a glycylcycline. reversibly binds to 30s ribo. subunit preventing tRNA binding--translation stops. *Extended spectrum. Tx MRSA, resistant s. Pneumoniae. NOT Tx pseudomonas

233

What supplement used as an anti-cancer?

Ginseng , Milk Thistle, and St. John’s Wort

234

Zidovudine (AZT)

HIV drug, NRTI, nucleoside/tide integrates into DNA, terminating DNA elongation. *can be used for prophylaxis and is toxic to bone marrow

235

Which amebicide is also used for malaria and arthritis/lupus?

Chloroquine

236

Which antiviral is particularly bad for people with renal failure?

Amantadine (uncoating inhibitor), high dose Acyclovir (anti-herpes), Cidofovir (anti-CMV)

237

What drugs bind to the 50s ribosomal subunit?

Chloramphenicol, Clindamycin, Linezolid, Macrolides/Ketolides.

238

Which anti-CMV doesn't need to be activated by viral enzyme?

Cidofovir

239

Viruses that cause the flu contain the enzyme _____

Neuraminidase

240

How is resistance for macrolides/ketolides?

It's becoming a problem. Drug has decreased 50s affinity in resistance

241

Acyclovir

Herpesvirus drug. Guanosine analog gets incorporated into viral DNA via DNA poly. *tx HSV encephalitis

242

Nelfinavir

HIV protease inhibitor. inhibits HIV aspartyl protease to prevent viral maturation. MANY drug-drug interactions. *can cause diarrhea and is NOT boosted by Ritonavir

243

Rilpivirine

HIV drug, NNRTI that causes conformational change to HIV-1 reverse transcriptase

244

Lopinavir

HIV protease inhibitor. inhibits HIV aspartyl protease to prevent viral maturation. MANY drug-drug interactions.

245

Pyrimethamine

tx Toxoplasmosis, combined with sulfadiazine.

246

Doxycycline

**PSI, Tetracycline. reversibly binds to 30s ribo. subunit preventing tRNA binding--translation stops. *liver excreted

247

Amantadine

Respiratory flu drug. inhibits viral uncoating. Blocks viral membrane matrix protein M2 so viral and host membrane can't fuse. *can cross BBB, bad for kidney failure people

248

What antifungal induces p450 activity?

Griseofulvin ("other")

249

What drugs can cause skin rash?

Cotrimoxazole (antifolate) and rifampin, rifabutin (1L antimycobacterial) (NOT rifapentine)

250

Which NRTI can be used for prophylaxis and is toxic to bone marrow?

Zidovudine (AZT)

251

Which HIV protease inhibitor can cause severe and fatal hepatitis, rare intracranial hemorrhages?

Tipranavir

252

Echinacea

Botanical/Herbal. used for increasing wbc, anti-inflammatory, and anti-pathogen

253

Preclinical testing is finding out what toxicities?

Acute, subacute, and chronic

254

Iodoquinol

Luminal Amebicides. *effective against both trophozoite and cyst forms. can cause optic neuritis

255

How can a supplement be pulled from the market?

FDA has to prove that it is harmful before use can be restricted or removed from the market

256

What is the combo treatment for toxoplasma gondii?

pyrimethamine and sulfadiazine

257

Glucosamine

Purified Supplements. used for cartilage nutrient

258

Saquinavir

HIV protease inhibitor. inhibits HIV aspartyl protease to prevent viral maturation. MANY drug-drug interactions.

259

Ribavirin

Viral Hepatitis drug. guanosine analog causes dec guanosine triphosphate, blocking DNA/RNA synthesis.

260

Which malaria drug can cause depression?

Mefloquine

261

How much does it take to develop a drug?

$150 million to several billion

262

Ganciclovir has much less toxic with easier dosing than…_____

Trifluridine

263

Zanamivir

Respiratory flu drug. Inhibits neuraminidase, kills virus. via intranasal. not for COPD/asthma people

264

AE HIV protease inhibitors:

FAT REDISTRIBUTION, Paresthesias, GI disturbances, Changes in glucose and lipid metabolism

265

Micafungin

Antifungal, Echinocandin. lyses cell wall.

266

Melarsoprol

tx Trypanosomiasis. tx sleeping sickness or Chagas disease, perhaps?

267

Nevirapine

HIV drug, NNRTI that causes conformational change to HIV-1 reverse transcriptase. P450 inducer,

268

Which drugs hardly interact with P450?

Linezolid (PSI), Azithromycin (Macrolides)

269

What drug class inhibits the cytochrome P450 system?

Azoles (and Macrolides/Ketolides except Azith), this can increase Warfarin drug concentration

270

Which drugs are the systemic Amebicides?

Chloroquine, Dehydroemetine, Emetine, (Think Chlo-emetine system). Chloroquine is also part of malaria tx.

271

What drugs can cause Optic and peripheral neuropathy?

Linezolid (other PSI)

272

What is the distribution of Aminoglycosides?

Bad for systemic versions, they cross the placenta. High concentrations in inner ear and renal cortex

273

What supplement promotes lactation?

Milk Thistle

274

Which "tetracycline" has expanded spectrum?

Tigecycline.

275

What supplement is used for treating liver disease?

Milk Thistle

276

What can cause nephrotoxicity?

Aminoglycosides, Capreomycin (2L antimycobacterial)

277

Sodium stibogluconate

tx Leishmaniasis. orally poor. AE: Can cause pain at the injection site, GI upsets, and cardiac arrhythmias.

278

Fluconazole

Antifungal, Azole. Inhibits P450 enzyme that converts lanosterol to ERGOSTEROL, disrupting fungal membrane.

279

How is Amphotericin B administered? Eliminated?

SLOWLY through IV.
Excreted through BOTH kidney and liver

280

What kind of resistance can Trimethoprim encounter?

Gram (-) from altered enzyme

281

What is used to treat abdominal bacterial infections associated with trauma?

Clindamycin

282

AE for Cotrimoxazole:

Skin rash (esp in elderly), Nausea, vomiting, Anemia or thrombocytopenia

283

Saw Palmetto

Botanical/Herbal. used for treating BPH (inflamed prostate)

284

Where does Trimethoprim tend to accumulate?

In acidic environments because the drug is a weak base

285

Which drugs are P450 inducers?

NNRTIs (HIV drugs), Griseofulvin (antifungal), and Isoniazid, Rifampin, Rifabutin (1L antimycobacterial)

286

What is the drug of choice for erythrocytic forms of malaria?

Chloroquine (also systemic amebicide)

287

Which drugs are never given as a single agent?

Isoniazid (1L antimycobacterial), Rifamycins (1L antimycobacterial)

288

What can cause gray baby syndrome?

Chloramphenicol because baby can't excrete the drug well

289

Can you use a different tetracycline for bacteria that is resistant to a tetracycline?

Nope!

290

What drugs bind to the 30s ribosomal subunit?

Tetracyclines, Aminoglycosides

291

MOA:
oxygen radicals toxic to both host/parasite but human enzymes fix damage.

Nifurtimox (trypanosomiasis)

292

AE nitrofurantoin:

Hemolytic anemia, GI disturbances, Neurological problems, Chronic use can result in interstitial pulmonary fibrosis

293

Which antiviral can cross the BBB?

Amantadine (uncoating inhibitor)

294

What is the treatment for EXOerythrocytic forms of malaria?

Primaquine

295

Paromomycin

Luminal Amebicides. *aminoglycoside antibiotic. it doesn't get absorbed through GI and kills food source

296

Ritonavir

HIV protease inhibitor. inhibits HIV aspartyl protease to prevent viral maturation. MANY drug-drug interactions. *P450 inhibitor, boosts performance of other protease inhibitors

297

Elimination of Macrolides/Ketolides:

Kidney. They inhibit p450 enzyme system (Azithromycin does NOT inactivate P450 enzymes)

298

Dapsone

Antimycobacterial, Leprosy drug. Inhibits folate synthesis. concentrates in skin, Tx pneumonia in HIV patients

299

What is approved for treatment of cytomegalovirus induced retinitis in AIDS patients?

Cidofovir

300

How is Cotrimoxazole administered?

Orally

301

How do you administer interferons for hep tx?

IV or IM because it's made of recombinant DNA

302

What class of drugs have tons of interactions?

HIV protease inhibitors

303

Capreomycin

Second-line antimycobacterial. Inhibits protein synthesis

304

Amphotericin B

Antifungal, Polyene Antibiotic. binds to ergosterol in membrane making ion pore > death.

305

Trimethoprim

Antifolate. Inhibits dihydrofolate reductase, preventing dihydrofolic acid to tetra

306

Which stage of Giardia lamblia is resistant to drugs?

The four-nucleate cyst (as opposed to the binucleate trophozoite)

307

What is the antifungal precursor to 5-FU?

Flucytosine

308

Which amebicide kills off the protozoal food source?

Paromomycin (luminal amebicide)

309

What is the pharmacokinetics of HIV protease inhibitors? (bioavailability, metabolism)

Poor oral bioavailability, P450 metabolized, good for renal impairment.

310

What drug can decrease glomerular filtration rate?

Amphotericin B

311

Ciprofloxacin (Cipro)

*2nd line ANTIMYCOBACTERIAL and 2nd Gen Fluoroquinolone. Enters bacteria via diffusion; uses dual mechanism to inhibit DNA gyrase and topoisomerase IV. *most potent against Pseudomonas

312

Gemifloxacin

2nd line antimycobacterial and 4nd Gen Fluoroquinolone. Enters bacteria via diffusion; uses dual mechanism to inhibit DNA gyrase and topoisomerase IV.

313

Spectrum of
Fluoroquinolones:

Both +/- , including (-) like Pseudomonas, H. influenzae, Moraxella, Chlamydia

314

Terbinafine

*Antifungal, "Other". Squalene builds up because drug prevents conversion into ERGOSTEROL by inhibiting squalene epoxidase. *Tx nail infection

315

What inhibits the p450 enzyme lanosterol to ergosterol, disrupting membrane structure and function?

Azoles

316

What drug binds ergosterol in the plasma membrane and forms a pore for electrolytes?

Amphotericin B

317

Which HIV protease inhibitor can cause slow heart rate?

Atazanavir

318

AE for Flucytosine:

Neutropenia, Thrombocytopenia, Bone marrow depression--bad for immunocompromised, Caution in patients undergoing chemotherapy, GI disturbances common

319

Which antifolate drug is good against MRSA?

Cotrimoxazole

320

What is used for pre-CNS involvement of sleeping sickness?

Pentamidine (trypanosomiasis)

321

Griseofulvin

Antifungal, "Other". Inhibits fungal mitosis until skin sloughs it off.

322

Minocycline

PSI, Tetracycline. reversibly binds to 30s ribo. subunit preventing tRNA binding--translation stops.

323

Which tetracycline is good for people with renal disease?

Doxycycline

324

Dehydroemetine

Systemic Amebicides. inhibits protein synthesis. Via IM; oral might cause vomiting. Can concentrate in liver for a month

325

What drug is restricted to topical Candida infections

Nystatin because it's systemically toxic

326

Tenofovir

Viral Hepatitis drug. nucleotide analog inhibits viral reverse transcriptase.
HIV drug, NRTI, nucleoside/tide integrates into DNA, terminating DNA elongation. *long half-life, many antiretroviral drug interactions

327

What is often given with
Flucytosine?

Amphotericin B

328

___ should not be taken with Sulfonamides because they cancel out

Methenamine

329

Lamivudine

Viral Hepatitis drug. inhibits HBV DNA poly and HIV rev transcriptase. *Has few side effects.
ALSO HIV drug, NRTI, nucleoside/tide integrates into DNA, terminating DNA elongation. *does NOT affect mitochondrial DNA synthesis

330

What supplement is anti-inflammatory?

Echinacea and Ginseng

331

Didanosine

HIV drug, NRTI, nucleoside/tide integrates into DNA, terminating DNA elongation *take when fasting, AE Pancreatitis and peripheral neuropathy

332

What drug combo can make HIV UNDETECTABLE in 60-95% of patients?

A protease inhibitor and two NRTIs

333

Spectrum of viral uncoating inhibitors:

Influenza A

334

What supplement is used for jet lag, insomnia, and improving sleep?

Melatonin (purified supplement)

335

Boceprevir

Viral Hepatitis drug. Bind to active site of HCV protease

336

Contraindications for Fluoroquinolones:

Pregnancy, nursing mothers, children under 18, arrhythmia

337

How are NRTIs excreted?

Kidney, except abacavir!

338

What supplement is used for hypertension, improving output in heart failure, prevents statin-induced myopathy.

Coenzyme Q10 (purified supplement)

339

AE of aminoglycosides:

Ototoxicity, nephrotoxicity, neuromuscular paralysis, bad allergic reactions

340

Which antivirals are antimetabolites?

Ribavirin (anti hep),
Acyclovir (anti-herpes)

341

What is the drug of choice for chlamydia infections?

Azithromycin (z-pak)…. (Fluoroquinolones are also good)

342

What are confounding variables found in clinical trials?

Variable nature of most diseases, Presence of other diseases or risk factors, Subject and observer bias (Placebo effect)

343

Tinidazole

Mixed Amebicides AND alternative tx Giardiasis. Moa form cytotoxic compounds that bind to proteins and DNA. *shorter treatment, more expensive, used in other countries before US.

344

What drugs cause epigastric distress?

Macrolides/Ketolides

345

Lepers who are allergic to ___ might also be allergic to Dapsone

Sulfa drugs

346

Why are mycobacterial resistant to most antibiotics?

Grow more slowly, Can be dormant, Cell wall impermeable to many drugs, can be intracellular

347

Fosamprenavir

HIV protease inhibitor. inhibits HIV aspartyl protease to prevent viral maturation. MANY drug-drug interactions.

348

What drugs should not get acidic?

Sulfonamides

349

Which NRTI does NOT affect mitochondrial DNA synthesis?

Lamivudine (has less side effects). Remember Emtricitabine has NO significant drug interactions

350

Only __% of marketed drugs return their R&D investments

20%

351

Rifabutin AE:

UVEITIS, Uncommon Nausea, vomiting, rash. (Orange feces, urine, and tears..?). p450 inducer

352

Raltegravir

HIV integrase inhibitor that inhibits final step of integration of viral DNA into host DNA. NO P450 interactions

353

Rifabutin

*First-line antimycobacterial. inhibits RNA polymerase to prevent transcription. *Good for HIV patients that need it. increase P450 metabolism. Can cause uveitis

354

Valacyclovir (Valtrex)

Herpesvirus drug.?Guanosine analog gets incorporated into viral DNA via DNA poly

355

Moxifloxacin

*2nd line ANTIMYCOBACTERIAL and 4nd Gen Fluoroquinolone. Enters bacteria via diffusion; uses dual mechanism to inhibit DNA gyrase and topoisomerase IV. *Poor activity against pseudomonas, NO tx for UTIS because not concentrated in urine. Has long half-life

356

What decreases testosterone and cortisol production?

Azoles

357

___% of health care expense in the U.S. is on prescription drugs

10-12% of health care expense in the U.S. is on prescription drugs

358

AE chloramphenicol:

GI disturbances, Candida overgrowth, Anemia (can be fatal), Gray baby syndrome

359

Fidaxomicin

PSI, Macrolide/Ketolide. Binds to 50s ribo. subunit (can inhibit its formation) to block peptidyl transferase center to prevent AA elongation.

360

What disease causes a dendritic pattern on the cornea?

Herpetic Keratitis

361

AE Ethionamide:

GI irritation, Hepatotoxicity, Optic Neuritis, Peripheral neuropathies

362

Ginkgo

Botanical/Herbal. used for increasing blood flow and vasodilation; increasing cognition and concentration.

363

Which drugs bind to the 30s ribosomal subunit?

Tetracyclines, Aminoglycosides

364

What drug can cause some visual disturbances?

Terbinafine (antifungal)

365

What strategies can prevent mycobacterial resistance?

Use multiple drugs, LONG duration, increase compliance through directly observed therapy. (DOT)

366

What drugs can lead to fat redistribution?

HIV protease inhibitors

367

Methenamine should not be taken with __ because they cancel out

Sulfonamides

368

What drugs are bad to have with Ca++, Iron, Antacids?

Fluoroquinolones and Tetracyclines

369

Hepatitis __ and __ are the most common causes of chronic hepatitis, cirrhosis, and hepatocellular carcinoma

B and C

370

Erythromycin

*PSI, Macrolide/Ketolide. Binds to 50s ribo. subunit (can inhibit its formation) to block peptidyl transferase center to prevent AA elongation. *not via IV! oral is good

371

Tx Leishmaniasis

Sodium stibogluconate

372

What drug have flu-like AE?

Interferons (anti Hep)

373

Which amebicide inhibits protein synthesis?

Dehydroemetine and Emetine

374

Caspofungin

*Antifungal, Echinocandin. lyses cell wall. *second-line antifungal if amphotericin B or azole fails

375

Which Fluoroquinolone is most potent against pseudomonas?

Ciprofloxacin

376

What can cause precipitate gout?

Pyrazinamide (1L antimycobacterial)

377

What's in a new drug application? How long does it take to get approval?

Full reports of all preclinical and clinical data. Can take months to years to gain approval, but If urgent need for the drug is perceived, the process of FDA review can be accelerated.

378

Oseltamivir (Tamiflu)

Respiratory flu drug. Inhibits neuraminidase, kills virus.

379

Nitrofurantoin

Urinary Tract Antiseptic. bacteria makes drug a toxic intermediate that damages their DNA

380

What foods/supplements should you avoid when taking tetracyclines?

Calcium (dairy) reduces bioavailability; avoid antacids or iron supplements

381

Which NRTI can cause a fatal allergic reaction upon second exposure?

Abacavir

382

Gentamicin

PSI Aminoglycoside. Binds to 30s ribo subunit preventing protein synthesis initiation AND cause misreading of mRNA causing wrong AA insertion.

383

What supplement is used as an antiviral?

St. John’s Wort

384

What was revealed in the Herpetic Eye Disease Study I and II?

"there really no point in treating herpetic keratitis with both topical and/or oral medication". Oral (acyclovir) will work by itself for the corneal disease. Oral acyclovir given 400mg bid (twice a day) is effective in reducing the recurrence of herpetic eye disease by almost half

385

Who is involved in phase 1 clinical trials?

Small number (20-100) of healthy volunteers

386

What is the recommended HIV drug class combination?

Two NRTIs (w/ different mechanisms) and one other class (NNRTI, protease inhibitor, integrase inhibitor). For some reason entry inhibitors isn't listed.

387

Levofloxacin (Levaquin)

*2nd line ANTIMYCOBACTERIAL and 3nd Gen Fluoroquinolone. Enters bacteria via diffusion; uses dual mechanism to inhibit DNA gyrase and topoisomerase IV. *Long half-life

388

Anidulafungin

Antifungal, Echinocandin. lyses cell wall.

389

Trifluridine (Viroptic)

Herpesvirus drug. Fluorinated pyrimidine nucleotide inhibits incorporation of thymide triphosphate into viral DNA ; drug also incoporates into viral DNA. Cheap but short half life

390

Which drugs inhibit P450?

Azoles, Macrolides/Ketolides (except Azithromycin)

391

Neomycin

PSI Aminoglycoside. Binds to 30s ribo subunit preventing protein synthesis initiation AND cause misreading of mRNA causing wrong AA insertion.

392

Telithromycin

PSI, "Ketolide". Binds to 50s ribo. subunit (can inhibit its formation) to block peptidyl transferase center to prevent AA elongation.

393

What does the cell membrane of fungi contain?

Ergosterol

394

What drugs can cause peripheral neuropathy?

Didanosine and other NRTIs, Nifurtimox (trypanosomiasis), Linezolid (PSI), Ethionamide (2L Antimycobacterial)

395

Garlic

Botanical/Herbal. used for lowering cholesterol, decreasing blood pressure, antibiotic effects.

396

Which form of Entamoeba histolytica is infective?

The cyst form

397

Pentamidine

tx. Trypanosomiasis. used for pre-CNS involvement of sleeping sickness

398

Telaprevir

Viral Hepatitis drug. Bind to active site of HCV protease

399

AE Macrolides/Ketolides:

Epigastric distress, cholestatic jaundice, ototoxicity

400

Which malaria drugs in combination can cause cardiac arrest?

Mefloquine with quinine (malaria drug) or (quinidine).

401

What drugs can cause Anemia?

chloramphenicol and Linezolid (other PSI), nitrofurantoin (UTI antiseptic), Sulfonamides, and Cotrimoxazole and Trimethoprim (antifolates)

402

How are generic drugs approved? What's required?

Through an abbreviated new drug application (ANDA). Must demonstrate equivalence.

403

WHO recommends what for treatment of leprosy? For how long?

The triple-drug regimen: dapsone, clofazimine, and rifampin for 6 to 24 months

404

Spectrum of Isoniazid (1L antimycobacterial):

M Tuberculosis, intracellular bacteria

405

Ketoconazole

*Antifungal, Azole. Inhibits P450 enzyme that converts lanosterol to ERGOSTEROL, disrupting fungal membrane. * more side effects, limited to topical

406

What drug class can cause pseudotumor cerebri?

Tetracyclines

407

Which antiviral should be avoided in pregnancy?

Ganciclovir (anti-CMV)

408

Which NRTI has NO significant drug interactions?

Emtricitabine. Remember Lamivudine does NOT affect mitochondrial DNA synthesis.