Chemotherapeutic Drugs Flashcards

(90 cards)

1
Q

Competitively inhibit the incorporation of PABA (para-aminobenzoic acid) into folic acid

A

Sulfonamide

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2
Q

first clinical use of sulfonamide

A

1936

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3
Q

mass production of penicillin

A

1941

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4
Q

Harmful effects of chemotherapeutic drugs have resulted from _____________ or _____________.

A

allergic reactions or inadvertent IV overdose

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5
Q

competitive enzyme inhibitor, blocks the synthesis of folic acid in bacterial cell

A

Sulfonamide

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6
Q

Sulfonamide inhibits the enzyme

A

Dihydropteroate synthase

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7
Q

Trimethoprim inhibits the enzyme

A

Dihydrofolate reductase

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8
Q

After acute overdose of antimicrobials, most agents cause only

A

nausea, vomiting, and diarrhea

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9
Q

Biological origin of Streptomycin

A

Streptomyces griseus

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10
Q

Biological origin of Gentamicin

A

Micromonospora purpurea

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11
Q

Biological origin of Tobramycin

A

Streptomyces tenebrarius

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12
Q

Biological origin of Kanamycin

A

Streptomyces kanamyceticus

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13
Q

Biological origin of Neomycin

A

Streptomyces fradiae

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14
Q

Active against Pseudomonas aeruginosa

A

Amikacin, Gentamicin, Tobramycin

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15
Q

Most ototoxic aminoglycosides

A

Neomycin, Kanamycin, Amikacin

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16
Q

Most vestibulotoxic aminoglycosides

A

Streptomycin, Gentamicin

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17
Q

Most nephrotoxic aminoglycosides

A

Neomycin, Tobramycin, Gentamicin

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18
Q

Trimethoprim poisoning can cause:

A

Megaloblastic anemia
Leukopenia
Granulocytopenia

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19
Q

Trimethoprim poisoning antidote

A

Leucovorin

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20
Q

Leucovorin other names

A

● Wellcovorin ● Citrovorum factor ● Folinic acid

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21
Q

Chemical name of Leucovorin

A

5-formyltetrahydrofolate

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22
Q

Used to treat unintentional folic acid antagonist overdose

A

Leucovorin

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23
Q

Aka Diamino-diphenyl-sulfone (DDS)

A

Dapsone

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24
Q

Dapsone is combined with

A

Clofazimine & Rifampin

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25
Average elimination half-life of dapsone
30 hours
26
Average elimination half-life of dapsone overdose
77 hours
27
Disorder characterized by the presence of a higher-than-normal level of methemoglobin
Methemoglobinemia
28
clamps of damaged hemoglobin
Heinz-Erlich bodies
29
Dapsone is metabolized by 2 primary routes
● Acetylation ● CYP450 Oxidation
30
Dapsone toxic effects are caused by the p-450 metabolites, including
–Methemoglobinemia –Sulfhemoglobinemia –Heinz body hemolytic anemia
31
may occur owing to depletion of intracellular glutathione by oxidative metabolites
Hemolysis
32
Dapsone therapeutic ranges from
50-300 mg/d
33
Death has occurred with dapsone overdose of
1.4 g and greater
34
Px with ____________________ may experience greater dapsone toxicity at lower doses.
G6PD deficiency, congenital hemoglobin abnormalities, and underlying hypoxemia
35
form of hemoglobin that does not bind oxygen.
Methemoglobin
36
Decreases oxyhemoglobin saturation Unresponsive to methylene blue
Sulfhemoglobinemia
37
A reducing agent and is employed as a medication for the treatment of methemoglobinemia
METHYLENE BLUE
38
Effective in the treatment of Parkinson’s disease
Amantadine
39
Prophylaxis against parkinsonian side effects of neuroleptic agents
Amantadine
40
Used in therapy of cocaine addiction
Amantadine
41
4 cardinal features of Parkinsonism
a. Bradykinesia b. Muscular Rigidity c. Resting Tremor d. Postural Instabilit
42
BN of Amantadine
Symmetrel
43
•Enhance the release of dopamine •Prevent dopamine reuptake in the peripheral and CNS •Has anticholinergic properties, especially in overdose
Amantadine
44
Amantadine intoxication causes:
✓Agitation ✓Visual hallucinations ✓Nightmares ✓Tremor ✓Disorientation ✓Delirium ✓Slurred speech ✓Ataxia ✓Myoclonus ✓Seizures ✓Heart failure ✓Rarely, ventricular arrhythmias
45
Amantadine withdrawal may result in:
✓Hyperthermia ✓Rigidity
46
Amantadine serum level associated with toxicity
> 1.5 mg/L
47
Neuroleptic malignant syndrome (NMS) antidote
Dantrolene
48
NMS is characterized by
a. Fever b. Muscular Rigidity due to muscle contraction c. Altered mental status d. Autonomic dysfunction
49
not effectively removed by dialysis because the volume of distribution is very large
Amantadine
50
Amantadine volume of distribution
5 L/kg
51
Optical isomer of quinidine
Quinine
52
Once used for treatment of malaria and for chloroquine-resistant cases
Quinine
53
Treatment of nocturnal muscle cramps (idiopathic and common to older patients)
Quinine
54
Banned due to its toxic effect and also used as an abortifacient
Quinine
55
Toxic dose of quinine in adults
3-4 g
56
Fatal dose of quinine in children
1 g
57
Mild intoxication of quinine produces
✓Nausea ✓Vomiting ✓ Cinchonism
58
Clinical presentation of cinchonism includes
Tinnitus Deafness Vertigo Headache Visual disturbances
59
Severe intoxication of quinine may cause
• ataxia • obtundation • convulsions • coma • respiratory arrest •with massive intoxication quinidine-like cardiotoxicity
60
Retinal toxicity of quinine occurs _______ hours after ingestion
9-10
61
Retinal toxicity of quinine
 blurred vision  impaired color perception constriction of visual fields blindness macular edema disk pallor pupils are fixed and dilated retinal artery spasm
62
previously been recommended for quinine-induced blindness
Stellate ganglion block
63
Plasma quinine levels above ________ have been associated with visual impairment
10 mg/L
64
87% of patients with levels above _________ reported blindness.
20mg/L
65
Levels with have been associated with cardiac toxicity.
16mg/L
66
an injection of local anesthetic in the sympathetic nerve tissue of the neck
stellate ganglion block
67
used in the treatment of rheumatoid arthritis
Chloroquine and hydroxychloroquine
68
blocks the synthesis of DNA and RNA and also has some quinidine-like cardiotoxicity
Chloroquine
69
oxidizing agents and can cause methemoglobinemia or hemolytic anemia (especially in patients with G6PD deficiency)
Primaquine and quinacrine
70
Lethal dose of chloroquine for an adult is
30-50 mg/kg
71
Therapeutic dose of chloroquine phosphate for malaria prophylaxis
500 mg once a week
72
Therapeutic dose of chloroquine phosphate for malaria treatment
2.5 g over 2 days
73
Primaquine and quinacrine intoxication cause:
•GIT upset •Severe methemoglobinemia •Hemolysis •Ototoxicity •Retinopathy
74
Amodiaquine can cause:
Fatal neutropenia
75
Mefloquine in therapeutic dose or overdose can cause:
• Dizziness • Vertigo • Hallucinations • Psychosis • Seizures
76
Treat cardiotoxicity as for quinidine poisoning with ______________
sodium bicarbonate 1-2 meq/kg IV
77
may be useful in treating hypotension via combined vasoconstrictor and inotropic actions
Epinephrine infusion
78
has been reported to reduce mortality in animals and to ameliorate cardiotoxicity in human cases
High-dose diazepam (2 mg/kg IV, given over 30 mins)
79
Hydrazide derivative of isonicotinic acid
ISONIAZID (INH)
80
Known to cause hepatitis on chronic use
ISONIAZID (INH)
81
Acute overdose of INH causes
seizures and metabolic acidosis
82
Active form of Vit. B6
pyridoxal 5-phosphate
83
INH Acute ingestion of as little as _____ can produce toxicity
1.5 g
84
Chronic therapeutic INH use may cause:
✓Peripheral neuritis ✓Hepatitis ✓Hypersensitivity reactions
85
Do not induce emesis because of the risk of rapid onset of coma and seizures.
Isoniazid
86
Gastric lavage for massive ingestions
Isoniazid
87
Enhanced Elimination of isoniazid
Forced diuresis and dialysis
88
A __________ dose produces a peak INH concentration of 3 mg/L at 1 hour.
5 mg/kg
89
Other toxic effects of quinine
✓Hypokalemia ✓Hypoglycemia ✓Hemolysis ✓Congenital malformations
90
May aggravate cardiotoxicity of quinine
Acidification of the urine