Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm Exam 8 > Drug MOA/SE/Use > Flashcards

Drug MOA/SE/Use Flashcards

1
Q

Zidovudine MOA

A

thymidine analogue (w/ 3’-azido) prevents phosphodiester linkage, inhibiting RT & viral replication

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Zidovudine Resistance

A

common in newly infected pts & those previously Tx w/ this drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Zidovudine S/E

A

Extreme ANEMIA & NEUTROPENIA in compromised bone marrow function pts;
GI (n/v, diarrhea, hepatitis)
HEMA (anemia, granulocytopenia, thrombocytopenia, bone marrow toxicity)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Zidovudine can be used w/ all other NRTIs except?

A

Stavudine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Which pt condition warrants extreme caution when using Zidovudine?

A

Bone marrow compromised pts

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

HIV+ pregnant females using which drug during wks 14-34 along + infants until 6 wks, can reduce transmission rates to 8%

A

Zidovudine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Didanosine MOA

A

ideoxyinosine, w/ a 3’-H instead of a 3’-OH; Activation to ddATP, competitive inhibition of RT enzyme

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Didanosine S/E

A

Peripheral neuropathy, potentially fatal pancreatitis, GI disturbances

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What limits Didanosine?

A

Lowered absorption d/t gastric pH or food

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Lamivudine MOA

A

3’-Carbon replaced by 3’-Sulfur; Competitive inhibition of RT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Lamivudine S/E

A

Less cellular toxicity - but less potent than Zidovudine; Related to Didanosine, but NO risk for peripheral neuropathy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What limits Lamivudine?

A

Rapid RESISTANCE if on monotherapy!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Which NRTIs have action against HBV?

A

Lamivudine & Emtricitabine & Tenofovir

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Emtricitabine MOA

A

5’-Fluorinated derivative of Lamivudine (3’-Sulfur); Competitive inhibition of RT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Emtricitabine S/E

A

BEST TOLERATED! Hyperpigmentation of palms & soles

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Abacavir MOA

A

Nucleoside Analog - Competitive inhibition of RT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Abacavir S/E

A

3-9% Severe HSN rxn - rash, fever, malaise

Respiratory or GI Sx

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Preferred Tx for Tx-naive patients

A

Epzicom & Truvada combination drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Epzicom

A

Abacavir/Lamivudine combination pill

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Truvada

A

Emtricitabine/Tenofovir combination pill

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Tenofovir MOA

A

NucleoTide analog - Competitive inhibition of RT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Tenofovir S/E

A

n/v, diarrhea, renal toxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Tenofovir Use

A

Active against HBV & NRTI-RESISTANT strains

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Limitations of Efavirenz

A

contraindicated during pregnancy - neural tube defects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Efavirenz MOA

A

binds directly to RT to alter enzyme’s catalytic site

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Efavirenz S/E

A

CNS Sx: Dizziness, HA, insomnia, inability to concentrate & rash

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Atripla

A

Efavirenz/Emtricitabine combination pill

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Ritonavir S/E

A

Common: n/v, weakness, diarrhea
Circumoral & peripheral parethesia (tingling/numbness)
Elevated liver enzymes
inhibits p450 -> drug toxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Ritonavir MOA

A

Peptidomimetic inhibitor of HIV protease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Ritonavir Uses

A

w/ other NRTIs or at low doses to “BOOST” serum concentrations of other PIs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Most commonly used PI

A

Nelfinavir

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Nelfinavir S/E

A

well tolerated - nausea, diarrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Indinavir S/E

A

Nephrolithiasis, Dermatologic changes (alopecia, dry skin & mucous membranes)
Asymptomatic hyperbilirubinemia, HA, blurred vision, dizziness

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

Atazanavir S/E

A

GI disturbance, ABNORMAL FAT DISTRIBUTION, Elevated liver enzymes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

Chloroquine/Hydrochloroquine MOA

A

Interferes w/ Hgb digestion -> heme accumulation & toxicity to Plasmodium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

Chloroquine/Hydrochloroquine S/E

A

(Less than Quinine)
Retinal & Corneal toxicity (visual dysfunction);
CNS - HA, dizzy, tinnitus; GI: take w/ food
Immunologic: rash, blood dyscrasia, lupus-like

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

Chloroquine/Hydrochloroquine should be used w/ caution in pts w/

A

liver disease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

Chloroquine/Hydrochloroquine should not be used in pts w/

A

psoriasis & porphyria

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

Chloroquine/Hydrochloroquine is used to Tx

A

Clinical cure for ALL forms
Radical care for P. falciparum & P. malariae
Prophylaxis for sensitive forms

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

At high doses Chloroquine/Hydrochloroquine may be used for

A

Anti-inflammatory action @ HIGH doses - for RA & Lupus Erythematosus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

Resistance to Chloroquine/Hydrochloroquine via

A

P. falciparum - involves a transport pump that removes the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

Quinine/Quinidine S/E

A 
Cinchonism: HA, nausea, dizziness, blurred vision, tinnitus, deafness
GI irritation  (n/v), Depressant effect on heart & mild neuromuscular blockade
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

Quinine/Quinidine Contraindications

A

Pregnancy - birth defects & abortion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

Quinine/Quinidine at low doses is used for

A

Muscle relaxant @ LOW doses - for nocturnal leg cramps

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

Quinine/Quinidine is used to Tx

A

Clinical cure for ALL forms
Gametocytocidal for P. vivax & P. malariae
Tx of Chloroquine-resistant P. falciparum
Analgesic & Antipyretic effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
46
Q

Mefloquine S/E

A

Less toxic than Chloroquine

GI upset, Myocardium depression, Seizures, Aggrevation of latent psychoses

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
47
Q

Mefloquine should be used w/ caution in pts w/

A

Caution w/ pt Hx of mental illness, epilepsy, CV disorders

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
48
Q

Mefloquine is used to Tx

A

Tx & Prophylaxis of Chloroquine-resistant strains of P. falciparum

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
49
Q

Pyrimethamine/Proguanil MOA

A

dihydrofolate reductase inhibitor in erythrocytic forms & some effect on sporozoites & pre-erythrocytic forms

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
50
Q

Pyrimethamine/Proguanil Use

A

Px of Chloroquine-resistant strains of P. falciparum & Presumptive Tx when used w/ Sulfonamides

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
51
Q

Atovaquone + Proguanil MOA

A

depolarizes mitochondria to inhibit ETC

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
52
Q

Atovaquone + Proguanil Use

A

Alternative to Mefloquine & Doxycycline fp Px of Chloroquine-resistant P. falciparum

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
53
Q

Which drug is rapidly becoming the PRIMARY Tx for most forms of Malaria?

A

Coartem: combination of Artemisinin/Artemether + Lumefantrine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
54
Q

Atovaquone + Proguanil S/E

A

RARE: HA, abd pain, unknown safety during pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
55
Q

Which antibiotic class can be used as a Tx & Px alternative for malaria?

A

Tetracycline (Doxycycline)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
56
Q

Primaquine action

A

Active against tissue forms of all species, gametocytocidal, little effect on the erythrocytic forms & will not suppress active disease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
57
Q

Primaquine S/E

A

Acute - Mild; Chronic - Increasing severity

GI upset, CNS (HA, dizzy), Hemolytic anemia (in G6PD deficient ind)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
58
Q

Contraindications for Primaquine

A

pregnancy - teratogenic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
59
Q

Primaquine Uses

A

Radical cure for P. vivax & P. ovale by eradicating the tissue forms
Causal Prophylaxis - but it is not used d/t toxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
60
Q

Tetracycline (Doxycycline) MOA

A

Inhibition of plasmodial protein synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
61
Q

Tetracycline (Doxycycline) S/E

A

Phototoxicity, Permanent discoloration of teeth in children

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
62
Q

Tetracycline (Doxycycline) Contraindication

A

pregnancy & children < 8

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
63
Q

Most common helminthic infection in the US

A

Enterobius vermicularis (pinworm)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
64
Q

Enterobius vermicularis (pinworm) Sx

A

Perianal irritation & pruritus, anorexia, restlessness, insomnia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
65
Q

Ascaris lumbricoides (roundworm) Sx

A

“Light” infections are aSx, while “Heavy” infections cause abd pain, allergic responses to metabolites (rash, asthma), insomnia, restlessness, appendicitis, bile duct occlusion, intestinal perforation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
66
Q

Necator americanus (hookworm) Sx

A

Iron-deficient anemia (mental dullness)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
67
Q

T. solium & T. saginata Sx

A

GI upset, loss of appetite, T. solium larvae can penetrate the GIT & migrate to produce cysticercosis (encyst in visceral organs, muscle, CNS); Neurocysticercosis may cause Neurogenic & Psychiatric Sx, increased ICP, severe HA, intellectual deterioration, decreased visual acuity & seizures

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
68
Q

Entamoeba histolytica Sx

A

Inflammation, severe bloody diarrhea, possible spread to liver (hepatic abscess)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
69
Q

Giardia lamblia Sx

A

profuse, watery, foul-smelling diarrhea, abd distention, cramping, anorexia, nausea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
70
Q

Trichomonas vaginalis Sx

A

greenish, malodorous discharge, vulvar pruritus, dyspareunia, dysuria, friable cervix

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
71
Q

Cryptosporidium parvum Sx

A

large amt of watery diarrhea w/ vomiting, cramping, flatulence

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
72
Q

Enterobius vermicularis Tx

A

Albendazole or Pyrantel

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
73
Q

Mild Ascaris lumbricoides Tx

A

Albendazole

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
74
Q

Heavy Ascaris lumbricoides Tx

A

Pyrantel

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
75
Q

Necator americanus Tx

A

Albendazole

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
76
Q

T. solium & T. saginata Tx

A

Praziquantel

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
77
Q

aSx Entamoeba histolytica Tx

A

Iodoquinol or Paromomycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
78
Q

Sx Entamoeba histolytica Tx

A

Metronidazole followed by Iodoquinol or Paromomycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
79
Q

Giardia lamblia Tx

A

Metronidazole or Nitazoxanide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
80
Q

Trichomonas vaginalis Tx

A

Metronidazole

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
81
Q

Cryptosporidium parvum in AIDS pt Tx

A

Paromomycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
82
Q

Cryptosporidium parvum in immunocompromised pt Tx

A

Nitazoxanide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
83
Q

Albendazole MOA

A

Binds to free b-tubulin of the parasite to inhibit MT polymerization & MT-dependent glucose uptake

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
84
Q

Albendazole S/E

A

GI: n/v, diarrhea, abd pain
Teratogenic potential - use only if benefits > risks; Increase liver enzymes & hepatotoxicity
Leukopenia (<1%)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
85
Q

Albendazole Uses

A
  1. Enterobius Vermicularis (Pinworm),
  2. Mild/aSx Ascaris lumbricoides (roundworm),
  3. Necator americanus (hookworm)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
86
Q

Pyrantel MOA

A

Activation of cholinergic nicotinic receptors, resulting in a depolarizing neuromuscular blockade & paralysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
87
Q

Pyrantel S/E

A

GI: n/v, cramps; HA, dizziness, drowsiness

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
88
Q

Pyrantel Uses

A
  1. Enterobius Vermicularis (Pinworm)

2. Heavy Ascaris lumbricoides (roundworm) infection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
89
Q

Pyrantel should be used w/ caution in

A

pts w/ liver disease, pregnancy, & children <2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
90
Q

Praziquantel MOA

A

Induces muscle contraction then spastic paralysis by causing an increase in Ca2+ influx

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
91
Q

Praziquantel S/E

A

Dizziness, drowsiness, HA, decreased mental alertness; GI: abd pain, n/v
Increase liver enzymes
Urticaria, rash, low-grade fever, arthralgia, myalgia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
92
Q

Praziquantel Uses

A

Taenia solium, Taenia saginata, Neuroschistosomiasis, used as Tx & Px

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
93
Q

Praziquantel should be used w/ caution in

A

avoid w/ pregnancy if possible

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
94
Q

Metronidazole MOA

A

reduced & binds to intracellular macromolecules (DNA), inhibition of DNA synthesis, etc

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
95
Q

Metronidazole S/E

A

Drug Interactions - disulfiram-like rxn w/ EtOH, increases oral anticoagulant activity
Nausea, HA, dry-mouth/metallic taste
Infrequent - Vomiting, diarrhea, insomnia, dark urine, weakness, dizziness, seizures, peripheral neuropathies
Carcinogenic potential

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
96
Q

Metronidazole Uses

A
  1. Sx Entamoeba histolytica
  2. Giardia lamblia
  3. Trichomonas vaginalis
  4. Anaerobic bacteria - GNR, Bacteroides fragilis, & GPC, C. difficile
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
97
Q

Metronidazole should not be used in

A

1st trimester - carcinogenic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
98
Q

Iodoquinol S/E

A

Neurotoxicity - optic neuritis & loss of vision

Mild GI upset

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
99
Q

Iodoquinol Uses

A

Alone in aSx Entamboeba histolytica or following Metronidazole for Sx E. histolytica

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
100
Q

Paromomycin MOA

A

Aminoglycoside & inhibits protein synthesis by binding to the 30S ribosomal subunit

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
101
Q

Paromomycin S/E

A

GI: anorexia, n/v, epigastric burning, increased GI motility, abd cramps, diarrhea
Potential nephrotoxicity, ototoxicity, & neuromuscular blocking effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
102
Q

Paromomycin Uses

A
  1. Alone in aSx Entamboeba histolytica or following Metronidazole for Sx E. histolytica
  2. Drug of choice for C. parvum infection in AIDS pts
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
103
Q

Nitazoxanide MOA

A

Interferes w/ anaerobic energy metabolism by inhibiting pyruvate:ferredoxin 2-oxidoreductase enzyme depependent electron transfer rxn

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
104
Q

Nitazoxanide S/E

A

displaces highly-bound drugs (Warfarin)
Common - abd pain, diarrhea, nausea, HA
Unlike Metronidazole - free of carcinogenic potential

105
Q

Nitazoxanide Uses

A
  1. C. parvum in immunocompetent children (1-11), adolescents, & adults
  2. G. lamblia in children >1, adolescents, & adults
106
Q

Mechlorethamine MOA

A

7-N of guanine alkylation, producing an alkylated purine (multiple sites of alkylation cause cross-linking of DNA strands); Results in miscoding of DNA strands, incomplete repair of alkylated segment -> DNA strand breaks, depurination, abnormal base pairing

107
Q

Mechlorethamine S/E

A

Toxicity - bone marrow, spermatogenesis, GIT, hair follicles
Acute toxicity - n/v, phlebitis
Delayed toxicity - bone marrow depression (leukopenia, thrombocytopenia, anemia; immunosuppression, alopecia, *Secondary neoplasia

108
Q

Mechlorethamine Uses

A

Hodgkin’s Disease

109
Q

Mechlorethamine, CCS or CCNS?

A

CCNS - although primarily M & G1

110
Q

Cyclophosphamide MOA

A

activated by p450; alkylation cause cross-linking of DNA strands; Results in miscoding of DNA strands, incomplete repair of alkylated segment -> DNA strand breaks, depurination, abnormal base pairing

111
Q

Cyclophosphamide S/E

A

Toxicity - bone marrow, spermatogenesis, GIT, hair follicles
Acute toxicity - n/v, phlebitis
Delayed toxicity - bone marrow depression (leukopenia, thrombocytopenia, anemia; immunosuppression, alopecia, *Secondary neoplasia

112
Q

Cyclophosphamide Uses

A

Immunosuppressive agent: Wegener’s granulomatosis, RA, Organ transplantation
Acute & Chronic Leukemia: Hodgkin’s & Non-Hodgkin’s, Burkitt’s lymphoma, Multiple myelomas, testicular cancer, breast cancer, lung cancer, ovarian/endometrial/cervical carcinoma

113
Q

Cyclophosphamide, CCS or CCNS?

A

CCNS

114
Q

Carmustine MOA

A

activation -> alkylation cause cross-linking of DNA strands; Results in miscoding of DNA strands, incomplete repair of alkylated segment -> DNA strand breaks, depurination, abnormal base pairing

115
Q

Carmustine S/E

A

Toxicity - bone marrow, spermatogenesis, GIT, hair follicles
Acute toxicity - n/v, phlebitis
Delayed toxicity - bone marrow depression (leukopenia, thrombocytopenia, anemia; immunosuppression, alopecia, *Secondary neoplasia

116
Q

Carmustine Uses

A

Brain tumors, Hodgkin’s & Non-Hodgkin’s lymphomas, Multiple Myeloma

117
Q

Carmustine, CCS or CCNS?

A

CCNS

118
Q

Cisplatin MOA

A

Bifunctional alkylator that causes inter-intrastand DNA cross-linking & disruption of DNA double helix which interferes w/ DNA synthesis

119
Q

Cisplatin S/E

A

nephrotoxicity + ototoxicity;
Toxicity - bone marrow, spermatogenesis, GIT, hair follicles
Acute toxicity - n/v, phlebitis
Delayed toxicity - bone marrow depression (leukopenia, thrombocytopenia, anemia; immunosuppression, alopecia, *Secondary neoplasia

120
Q

Cisplatin Uses

A

Testicular, ovarian, bladder, gastric, esophageal, pancreatic, lung, head/neck tumors

121
Q

Cisplatin, CCS or CCNS?

A

CCNS, but G1 most sensitive

122
Q

Methotrexate MOA

A

Dihydrofolate reductase inhibitor prevents the conversion of Folic acid to Tetrahydrofolate -> inability to convert deoxyuridylate to thymidylate blocks DNA, RNA, & protein synthesis

123
Q

Methotrexate S/E

A

Acute - n/v, diarrhea

Delyaed - GI/oral ulcers, bone marrow suppression, alopecia, hepatotoxicity, pulmonary infiltrates, fever

124
Q

Methotrexate Uses

A

Psoriasis & RA;

Acute lymphocytic leukemia, Non-Hodgkin’s lymphomas, leukemia, breast, pancreatic & bladder carcinoma

125
Q

Methotrexate, CCS or CCNS?

A

CCS in S phase

126
Q

Which protein allows normal cells to bypass the block caused by Methotrexate?

A

Leucovorin

127
Q

Resistance to Methotrexate is via

A

decreased uptake by tumor cells & increased concentration of target enzyme

128
Q

Mercaptopurine MOA

A

Converted by HGPRT to a nucleotide, which inhibits enzymes of purine interconversion. Results in inhibition of purine nucleotide synthesis & metabolism, and alters the synthesis & function of RNA & DNA

129
Q

Mercaptopurine S/E

A

Acute: infrequent n/v, diarrhea
Delayed: gradual bone marrow depression

130
Q

Mercaptopurine Uses

A

Immunosuppressant

Maintenance of remission of acute lymphocytic, acute myelogenous & CNS leukemia

131
Q

Mercaptopurine, CCS or CCNS?

A

CCS - S phase

132
Q

Mercaptopurine is metabolized by

A

xanthine oxidase to 6-thiouric acid

133
Q

The metabolism of Mercaptopurine can be blocked by what drug?

A

Allopurinol

134
Q

Fluorouracil MOA

A

Activated to 5-deoxyuridine
binds thymidylate synthetase covalently to block the conversion of deoxyuridylate to thymidylate (rate-limiting step in DNA synthesis)

135
Q

Fluorouracil S/E

A

Delayed: n/v, oral/GIT ulcerations, bone marrow depression

136
Q

Fluorouracil Uses

A

Carcinoma of breast, colon, pancreatic, ovarian, head, gastric, esophageal, head/neck

137
Q

Fluorouracil, CCS or CCNS?

A

CCS - S phase

138
Q

Fluorouracil resistance occurs via

A

decreased activation & increased inactivation

139
Q

Cytarabine MOA

A

Active Cytarabine triphosphate competes w/ Deoxycitidine triphosphate to cause DNA pol inhibition

140
Q

Cytarabine S/E

A

Delayed: n/v, bone marrow depression, megaloblastosis, leukopenia, thrombocytopenia

141
Q

Cytarabine Uses

A

Remission induction in acute non-lymphocytic leukemia; Acute lymphocytic leukemia; Chronic myelocytic leukemia; Meningeal leukemia

142
Q

Cytarabine, CCS or CCNS?

A

CCS - S phase

143
Q

Daunorubicin Hydrochloride MOA

A

Intercalate & bind to DNA b/w base pairs on adjacent strands, resulting in uncoiling of DNA & destroy the DNA template to inhibit DNA-directed RNA & DNA pols

144
Q

Daunorubicin Hydrochloride S/E

A

Acute - n/v, red urine, tissue necrosis, arrhythmias

Delayed - bone-marrow depression, alopecia, GI upset, & CARDIOMYOPATHY

145
Q

Daunorubicin Hydrochloride Uses

A

Acute Non-Lymphocytic Leukemia of adults

146
Q

Daunorubicin Hydrochloride, CCS or CCNS?

A

CCNS but most effective in S phase

147
Q

Doxorubicin Hydrochloride MOA

A

Intercalate & bind to DNA b/w base pairs on adjacent strands, resulting in uncoiling of DNA & destroy the DNA template to inhibit DNA-directed RNA & DNA pols

148
Q

Doxorubicin Hydrochloride S/E

A

Acute - n/v, red urine, tissue necrosis, arrhythmias

Delayed - bone-marrow depression, alopecia, GI upset, & CARDIOMYOPATHY

149
Q

Doxorubicin Hydrochloride Use

A

Synergistic in combination; Lymphoma, Leukemia, Hodgkin’s disease, ovarian, lung, bladder, neuroblastoma

150
Q

Doxorubicin Hydrochloride, CCS or CCNS?

A

CCNS but most effective in S phase

151
Q

Daunorubicin Hydrochloride & Doxorubicin Hydrochloride resistance occurs via

A

diminished drug uptake

152
Q

Vinblastine Sulfate MOA

A

Bind tubulin & disrupt the mitotic spindle apparatus, preventing segregation of chromosomes -> Metaphase arrest

153
Q

Vinblastine Sulfate S/E

A

Acute - local reactivity

Delayed - neurological, constipation, alopecia, mild bone depression

154
Q

Vinblastine Sulfate Use

A

Breast carcinoma, acute leukemia, Hodgkin’s & Non-Hodgkin’s lymphoma

155
Q

Vinblastine Sulfate, CCS or CCNS?

A

CCS for M phase

156
Q

Vincristine Sulfate MOA

A

Bind tubulin & disrupt the mitotic spindle apparatus, preventing segregation of chromosomes -> Metaphase arrest

157
Q

Vincristine Sulfate S/E

A

Acute - mild n/v, phlebitis

Delayed - neurological, bone-marrow depression

158
Q

Vincristine Sulfate Use

A

Hodgkin’s disease, Kaposi’s sarcoma, Testicular, bladder, lung carcinoma

159
Q

Vincristine Sulfate, CCS or CCNS?

A

CCS for M phase

160
Q

Etoposide MOA

A

Complexes w/ topoisomerase II & DNA, resulting in DNA breaks, no resealing of the breaks -> cell death

161
Q

Etoposide S/E

A

Acute - n/v, diarrhea (IV - 15%, oral - 55%)

Delayed - leukopenia 10-14d & recovery by 3wks; Alopecia in 66%

162
Q

Etoposide Uses

A 
Testicular cancer (w/ bleomycin + cisplatin)
Small Cell Carcinoma of lung (w/ cisplatin)
163
Q

Etoposide, CCS or CCNS?

A

CCS for G2

164
Q

Paclitaxel MOA

A

Anti-MT agent; promotes MT assembly by enhancing tubulin polymerization

165
Q

Paclitaxel S/E

A

Acute - n/v (52%)
Delayed - bone marrow suppression: neutropenia, leukopenia, thrombocytopenia, anemia; HSN; peripheral neuropathy (60%)
Alopecia (~100%)

166
Q

Paclitaxel Uses

A

Metastatic Ovarian or Breast Cancer

Non-Small Cell Carcinoma of lung

167
Q

Paclitaxel, CCS or CCNS?

A

CCS for G2 & M phases

168
Q

Prednisone or Dexamethasone MOA

A

Inhibits phospholipase A2 & COX-2;

Suppresses mitosis in lymphocytes

169
Q

Prednisone or Dexamethasone S/E

A

Iatrogenic Cushing’s Syndrome, osteoporosis, infections; Psychiatric disturbances, peptic ulcer, HTN, edema, adrenal suppresion, obesity, dyslipidemia

170
Q

Prednisone or Dexamethasone Uses

A

Palliative management of Leukemia & Lymphoma in adults,
Acute Leukemia of childhood,
Breast Cancer

171
Q

Tamoxifen MOA

A

competitively binds to estrogen receptors -> inhibits the expression of estrogen-related genes

172
Q

Tamoxifen S/E

A

Extremely well tolerated,
Most common - Menopausal Sx
Short-term: hot flashes, HA, fatigue, n/v, vaginal dryness, skin rashes
Long-term: visual disturbances, vaginal bleeding, ocular toxicity, thromboembolic events, thrombocytopenia & leukopenia
Most serious - potential tumor-promoting activity -> inceased incidence of endometrial cancer

173
Q

Tamoxifen Use

A

Estrogen-receptor (+) Invasive breast cancer,
Adjuvant therapy of breast cancer to reduce risk of recurrence & development of new cancers
Used frequently in men w/ breast cancer

174
Q

Tamoxifen, CCS or CCNS?

A

CCS blocks G1 phase

175
Q

Imatinib Mesylate MOA

A

inhibits Bcr-Abl tyrosine kinase, preventing phosphorylation of the kinase substrate by ATP, which inhibits cell proliferation & induces apoptosis in Bcr-Abl (+)

176
Q

Imatinib Mesylate S/E

A

Acute - abdominal pain, n/v, diarrhea

Delayed - fatigue, joint pain, muscle cramps, fluid retention, superficial edema & rash

177
Q

Imatinib Mesylate Uses

A

Ph(+) Chronic Myeloid Leukemia in blast crisis,
Acute Lymphocytic Leukemia,
Dermatofibrosarcoma, Hypereosinophilic syndrome & Chronic eosinophilic leukemia

178
Q

Imatinib Mesylate, CCS or CCNS?

A

CCS - G1

179
Q

Bcr-Abl Fusion Protein

A

a constitutively abnormal tyrosine kinase created by t(9:22) Philadelphia chromosomal translocation seen w/ CML

180
Q

Trastuzumab MOA

A

IgG1 mAb that binds HER-2 receptors (EGF), blocks EGF binding & down-regulates tyrosine kinase signaling activity

181
Q

Trastuzumab S/E

A

Acute - n/v, diarrhea

Delayed - anemia, neutropenia, infections, fatigue, fever, HA, infusion rxn, rash, & cardiomyopathy

182
Q

Trastuzumab Use

A

Adjuvant for Breast Cancer: 30% are EGF-2 overexpressing, give w/ Doxorubicin, Cyclophosphamide + Paclitaxel
HER-2 Overexpressing Metastatic Breast Cancer: give w/ Paclitaxel (1st line Tx)

183
Q

Trastuzumab, CCS or CCNS?

A

CCS for G1 arrest

184
Q

Breast Cancer Tx:

A

CMF: Cyclophosphamide + Methotrexate + Fluorouracil & Tamoxifen

185
Q

Bladder Cancer:

A

M-VAC: Methotrexate + Vinblastine + Adriamycin + Cisplatin

186
Q

Cervical Cancer Tx:

A

BIP: Bleomycin + Ifosfamide + Cisplatin

187
Q

Lung Cancer Tx:

A

CAE: Cyclophosphamide + Doxorubicin (Adryamicin) + Etoposide

188
Q

Which Chemotherapeutic drug is lipid soluble & can be used for brain cancer Tx?

A

Carmustine

189
Q

Which Chemotherapeutic drug causes ototoxicity & nephrotoxicity S/Es?

A

Cisplatin

190
Q

Which Chemotherapeutic drug causes Cardiotoxicity S/Es?

A

Daunorubicin Hydrochloride & Doxorubicin Hydrochloride

191
Q

Which Chemotherapeutic drug causes Neurological toxicity S/Es?

A

Vinblastine Sulfate & Vincristine Sulfate

192
Q

Ph(+) Chronic Myeloid Leukemia in blast crisis may be treated using

A

Imatinib Mesylate

193
Q

c-kit receptor (+)- GI Stromal tumor may be treated using

A

Imatinib Mesylate

194
Q

Antipsychotic drug used as an antiemetic?

A

Prochlorperazine

195
Q

Which drugs are more potent than Chlorpromazine

A

Trifluoperazine & Fluphenazine

196
Q

Trifluoperazine & Fluphenazine S/E

A

less sedation & less anticholinergic (CV effects), but MORE EPS

197
Q

Chlorpromazine S/E

A

More sedation & more anticholinergic (CV effects, but LESS EPS

198
Q

Potent Phenothiazine that comes in long-acting forms

A

Fluphenazine

199
Q

Phenothiazine MOA

A

D2-antagonist

200
Q

Potent antipsychotic w/ the greatest risk of EPS

A

Haloperidol

201
Q

Clozapine MOA

A

Blocks D4 & 5-HT2 receptors

202
Q

Clozapine Uses

A

May work in pts unresponsive to other meds, effective against + & - Sx

203
Q

Clozapine S/E

A

agranulocytosis, seizures, weight gain, hyperglycemia, type II DM

204
Q

Olanzapine

A

Clozapine w/o agranulocytosis risk

205
Q

Risperidone MOA

A

Blocks both DA2 & 5-HT2 receptors

206
Q

Risperidone S/E

A

Weight gain, hyperglycemia

207
Q

Olanzapine Uses

A

Scizophrenia & Mania

208
Q

Aripiprazole MOA

A

Partial agonist/antagonist at D2 & 5-HT1a receptors

209
Q

Aripiprazole S/E

A

Less likely to cause weight gain & hyperglycemia; Little tendency to cause EP S/E

210
Q

Imipramine MOA

A

Inhibit the synaptic reuptake of NE & 5-HT

211
Q

Amitriptyline MOA

A

Inhibit the synaptic reuptake of NE & 5-HT

212
Q

Fluoxetine

A

Selectively inhibit the reuptake of 5-HT

213
Q

Amitriptyline S/E

A

GREATEST Anticholinergic S/E (dry mouth, constipation, urine retention, loss of accomodation), More sedation, Weight gain

214
Q

Drug used for the Tx of Enuresis & Urinary Incontinence

A

Imipramine

215
Q

Fluvoxamine MOA

A

Selectively inhibit the reuptake of 5-HT

216
Q

Sertraline MOA

A

Selectively inhibit the reuptake of 5-HT

217
Q

Paroxetine MOA

A

Selectively inhibit the reuptake of 5-HT

218
Q

Citalopram MOA

A

Selectively inhibit the reuptake of 5-HT

219
Q

Escitalopram MOA

A

Selectively inhibit the reuptake of 5-HT

220
Q

Venlafaxine & Desvenlafaxine MOA

A

Inhibits both NE, 5-HT, & DA reuptake; Mild Stimulant Activity

221
Q

Duloxetine MOA

A

Inhibits both NE, 5-HT, & DA reuptake; Mild Stimulant Activity

222
Q

Trazodone MOA

A

Inhibit the reuptake of 5-HT & block 5-HT-2 receptors

223
Q

Nefazodone MOA

A

Inhibit the reuptake of 5-HT & block 5-HT-2 receptors

224
Q

Bupropion MOA

A

Selectively inhibits DA reuptake; Mild Stimulant Activity “Psychic Energizer”

225
Q

Mirtazepine MOA

A

Blocks presynaptic alpha-2-adrenergic receptors; Enhances the synaptic release of NE & 5-HT; Also blocks some 5-HT receptor subtypes

226
Q

Atomoxetine MOA

A

Selective NE reuptake inhibitor

227
Q

Phenelzine MOA

A

Prevent the metabolic breakdown of NE, 5-HT, & DA, by inhibiting MAO-A & MAO-B

228
Q

Tranylcypromine MOA

A

Prevent the metabolic breakdown of NE, 5-HT, & DA, by inhibiting MAO-A & MAO-B

229
Q

Selegiline MOA

A

Selective inhibitor of MAO-B, prevents the metabolic breakdown of DA only

230
Q

Lithium Carbonate Use

A

Most Effective drug for Manic-Depressive Disorder

231
Q

Valproic Acid Analogs

A

Anti-epileptic Agent; Mania

232
Q

Carbamazepine Use

A

Anti-epileptic Agent; Mania

233
Q

Clonazepam Use

A

Mania

234
Q

Cannabinoids

A

specific canabinoid receptors in CNS

Endogenous compounds: analog of archidonic acid, arachidonylethanolamide

235
Q

Salvia MOA

A

Active compound is Salvinorin A

Agonist at kappa opioid & D2 receptors

236
Q

Kratom MOA

A

Agonist activity at mu-opioid receptor

237
Q

Cannabinoids Uses

A

Adjunct to Cancer Chemotherapy (antiemetic)

Prevention of wasting in AIDS pts

238
Q

Lithium Carbonate MOA Theory - Ionic

A

alters neuronal distribution of effect of Na+, K+, or Ca2+ in CNS

239
Q

Lithium Carbonate MOA Theory - Biogenic Amine

A

alters release, reuptake, or metabolism of NT amine

240
Q

Lithium Carbonate MOA Theory - Phospholipid

A

alters phopholipid metabolism involved in the phosphoinositide signaling pathway

241
Q

Duloxetine Use

A

Neuropathic Pain

242
Q

Fluoxetine S/E

A

Least Anticholinergic effects, Causes less weight gain, less sedation, less CV effects
HA, anxiety, tremor, agitation, nausea, sexual dysfunction in Males

243
Q

Fluvoxamine Use

A

OCD

244
Q

Paroxetine S/E

A

Higher drug interaction potential; More weight gain than other SSRIs

245
Q

Which SSRI has the greatest potential for withdrawal syndrome?

A

Paroxetine (rapid acting)

246
Q

Tx for Bulemia, Anorexia, Related Eating Disorders

A

SSRIs

247
Q

Venlafaxine & Desvenlafaxine S/E

A

nausea, nervousness, anxiety, sweating

Fewer CV effects, but may cause HTN, tachycardia, palpitations, & sexual dysfunction

248
Q

Venlafaxine & Desvenlafaxine Use

A

Depression, GAD

May work in pts refractory to SSRIs

249
Q

Which drug is recommended for nighttime Tx of depression

A

Trazodone or Nefazodone

250
Q

Trazodone S/E

A

Lower incidence of Anticholinergic & CV S/E

May cause: priapism, sexual dysfunction in Males, VERY sedating

251
Q

Bupropion Use

A

Nicotine, Cocaine, Amphetamine Dependence

252
Q

Which drug is recommended for pts w/ depression & anxiety?

A

Mirtazepine

253
Q

Drug for the Tx of ADHD in children & adults

A

Atomoxetine

254
Q

Which drug causes potentially fatal Tyramine interactions & interactions w/ many drugs?

A

Phenelzine & Tranylcypromine

255
Q

Serotonin Syndrome

A

switching b/w MAO-I & other classes may cause severe fever, convulsions, death if 3-4wks isn’t provided b/w switch

256
Q

Which drug is offered as a transdermal patch for depression?

A

Selegiline

257
Q

Which drug is used to tx Parkinson’s Disease?

A

Selegiline

258
Q

Contraindications for Lithium Carbonate

A

pts w/ impaired renal function, CV or thyroid Ds, or during pregnancy

259
Q

Drug interactions for Lithium Carbonate

A

NSAIDs, Diuretics, any drug altering renal function; Carbamazepine, methyldopa, anti-depressants/psychotics enhance neurotoxicity

Pharm Exam 8 (3 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions