TDM Flashcards

(348 cards)

1
Q

Entails analysis, interpretation, and evaluation of drug concentration in serum, plasma, or whole blood samples

A

THERAPEUTIC DRUG MONITORING

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2
Q

Used to establish maximum benefits with minimal toxic effects for drugs whose correlation with dosage, effect or toxicity is not clear

A

THERAPEUTIC DRUG MONITORING

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3
Q

T/F

TDM is a routine laboratory test

A

F
NOT a routine laboratory test: Majority of drugs available in the market have its standard dosage (established)

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4
Q

Assesses drugs with NARROW THERAPEUTIC INDEX

A

THERAPEUTIC DRUG MONITORING

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5
Q

MAIN PURPOSE of TDM

A
  • Ensure the drug dosage will produce maximal therapeutic benefit
  • Identify when the drug is outside the therapeutic range
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6
Q

concentration of drug in the human sample that will produce pharmacologic/therapeutic benefit

A

Therapeutic range

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7
Q

effect if < TR

A

inefficacy

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8
Q

effect if > TR

A

toxicity

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9
Q

therapeutic range of a drug is almost the start of the toxic level (causes adverse effects)

A

Narrow therapeutic index

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10
Q

dose that provides therapeutic benefits (safe & effective) in most healthy population

A

STANDARD DOSAGE

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11
Q

T/F

Standard dose is used in diseased state

A

F

Not utilized in diseased state (diseased patients have alteration in physiologic condition) – can affect the predicted concentration of the standard dose

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12
Q

What must be done during diseased state to fit the individual needs

A

dosage regimen by performing TDM

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13
Q

FACTORS AFFECTING CIRCULATING CONCENTRATION OF DRUG

A

Route of Administration
Absorption
Drug Distribution
Free vs Bound Drug
Drug Metabolism
Drug Elimination

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14
Q

considered to achieve maximum therapeutic benefit of the drug

A

Route of Administration

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15
Q

Most direct and effective route of administration with 100% bioavailability

A

Intravenous (IV)

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16
Q

most common and least invasive route of administration

A

Oral (GI absorption)

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17
Q

Route of Administration done by Inhalation or skin absorption (transdermal patch)

A

Transcutaneous

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18
Q

Route of Administration done by rectal delivery and performed if oral delivery is not possible among infants (not all the time)

A

Suppository

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19
Q

Routes of Drug Administration based on the effectivity in drug delivery or in bioavailability

A

IV
IM
SC
Transcutaneous
Suppository
Oral

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20
Q

fraction of administered dose of drug that reaches the site of action or the circulation

A

Bioavailability

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21
Q

When drugs are absorbed, it can circulate in the blood either as?

A

free drug or protein-bound drug

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22
Q

active drug which exhibits therapeutic benefit

A

free / unbound drug

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23
Q

T/F

Only free drugs exhibit therapeutic benefit

A

F
Some protein-bound drugs may also exhibit therapeutic benefit.

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24
Q

2 fates of circulating drug

A
  1. distributed to the site of action (target of the drug) → shows biologic response
  2. metabolized and eliminated in their metabolite form
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25
Things to consider in Drug Absorption
Formulation of Drug Active transport Passive Diffusion Stomach (acidic) Small intestine (slightly alkaline)
26
form of drug that is dissolved before absorption? what form has fast absorption?
Tablet/capsule Liquid – fast absorption
27
Absorption intended for dietary constituents
Active transport
28
Absorption of majority of the drug from the GI tract → bloodstream (no energy required)
Passive Diffusion
29
Requirement for Passive Diffusion of drugs
drug must be hydrophobic/non-ionized state
30
Organ that efficiently absorbs weak acid drug
Stomach
31
Organ that efficiently absorbs weak base drug
Small intestine
32
T/F Amount of absorbed drug in GI tract (stomach, intestines) is predictable
T
33
T/F Vomiting patients may have orally administered drugs
F drug must be administered through IM/IV
34
Ability of drug to leave the circulation depends on their
lipid solubility
35
Relative proportion of the drug in the circulation and tissue/site of action
Drug Distribution
36
type of drugs that can cross cell membrane and lipid compartment
Hydrophobic drugs
37
type of drugs that can cross cell membrane but cannot reach lipid compartment
Polar (non-ionized)
38
type of drugs that can cross cell membrane at a slow rate
Polar (ionized)
39
formula of Volume of Distribution (Vd) index
Vd = D/C
40
what is D in Volume of Distribution (Vd) index formula
IV injected dose of drug (mg/g)
41
what is C in Volume of Distribution (Vd) index formula
Conc. of drug in the blood (mg/L or g/L)
42
Vd of Hydrophobic Drugs
43
Vd of Ionized/Bound Drugs
44
Acidic drug binds to
albumin
45
Basic drug binds to
a1-acid glycoprotein
46
only the free/unbound can interact with its site of action and result in a biologic response
Drug dynamics
47
T/F Increased free/unbound drugs in the circulation means that there will be increased therapeutic response.
F Increased free/unbound drugs in the circulation does not mean that there will be increased therapeutic response -- can lead to TOXICITY
48
T/F There is a standard percentage/conc. of the absorbed drug that can be free or protein-bound
T
49
How many protein bound and free absorbed digoxin in circulation
25% protein-bound 75% free
50
T/F When there is changes in blood protein content, Digoxin for example with 25% protein-bound may increase >25% due to higher chance to bind to protein
T
51
Factors that changes Free vs Bound drugs
* Inflammation * Hepatic disease * Malignancies * Nephrotic syndrome * Pregnancy * Malignancy * Malnutrition
52
Drug Metabolism
First-Pass Metabolism Pharmacogenomics
53
All drugs/substances absorbed by GI passes the hepatic portal system (liver) for metabolism before it enters the circulation
First-Pass Metabolism
54
T/F Efficacy of some drugs depends on the generation of metabolites
T
55
Process of parent drug (administered) generated into its metabolites
Biotransformation
56
Capacity of individual to metabolize drug when there is impaired liver function
reduced
57
Examines variation (influenced by genes) in hepatic metabolism rates between individuals
Pharmacogenomics
58
Drug Elimination
Hepatic metabolic processes Renal filtration
59
drug elimination wherein liver alters drugs into its metabolites and these metabolites are conjugated to make them water-soluble
Hepatic metabolic processes
60
drug elimination wherein kidneys filters conjugated metabolites into the urine
Renal filtration
61
Specimens for TDM
Serum, Plasma, Whole Blood
62
blood collection tube for serum in TDM
plain tube only
63
blood collection tube for plasma in TDM
heparinized tube
64
use of SST [yellow/gold] in TDM may cause? reason?
false ↓ gel separator may absorb some drugs
65
drugs absorbed by gel separator
phenytoin phenobarbital lidocaine quinidine carbamazepine
66
These Ca-binding anticoagulants interfere with drug analysis
EDTA, citrates, oxalates
67
Method for TDM
HPLC Immunoassays GC-MS (gold standard)
68
single most important factor in TDM
Timing of Blood Collection
69
lowest conc. of drug measured in the blood
Trough Concentration
70
what is the timing of collection to determine trough conc.?
collect blood right before administration of next dose
71
what is the timing of collection to determine peak conc. of orally administered drugs?
1hr after administration (except Digoxin)
72
what is the timing of collection to determine peak conc. of intravenously administered drugs?
30 mins. after administration
73
highest conc. of drug measured in the blood
Peak Concentration
74
determines if the drug already reached the toxicity level
Peak Concentration
75
exception for determination of peak concentration from oral drugs
Digoxin collect blood 8-10 hr after initial dose
76
time required for serum conc. of drug to be decreased/reduced by half
Half-life
77
Categories of TDM DRUGS
1. Cardioactive 2. Antibacterial 3. Antiepileptic (Anticonvulsant) 4. Psychoactive 5. Bronchodilator 6. Immunosuppressive 7. Antineoplastic
78
Types of Cardioactive drugs
cardiac glycosides anti-arrhythmic
79
T/F All drugs under each categories must undergo TDM
F *not all drugs under each categories undergo TDM; only selected drugs
80
EXAMPLES OF CARDIOACTIVE DRUGS
DIGOXIN QUINIDINE PROCAINAMIDE DISOPYRAMIDE LIDOCAINE
81
brand name of DIGOXIN
Lanoxin
82
Protein-bound DIGOXIN
25%
83
TR of DIGOXIN
0.8-2 ng/ml
84
Peak conc. of DIGOXIN
2-3 hr
85
Half-life of DIGOXIN
38 hr
86
Toxic range of DIGOXIN
>2-3 ng/ml
87
manifestation of DIGOXIN toxicity
* Nausea * Vomiting * Visual disturbances * Premature ventricular contraction (PVC) * Atrioventricular node blockage
88
DIGOXIN is used as tx for? what is the mechanism?
CHF inhibit Na-K ATPase pump = ↓ IC K+ = ↑ K+ in circulation = ↑ IC Ca2+ → promote cardiac contractility
89
digoxin metabolite
Digoxigenin
90
Timing of Blood Collection for Digoxin
8-10 hr (after administration); correlated with digoxin conc. in tissue
91
Method for DIGOXIN
IA
92
brand name/s of QUINIDINE
Quinidex Extentabs Cardioquin Quinora
93
Protein-bound QUINIDINE
70-80%
94
TR of QUINIDINE
2-5 ug/ml
95
2 common formulation of QUINIDINE
Quinidine Sulfate Quinidine Gluconate
96
formulation of quinidine with complete and rapid GI absorption
Quinidine Sulfate
97
peak conc. of Quinidine Sulfate
2 hr
97
quinidine that is slow-release formulation and has a slower absorption
Quinidine Gluconate
98
peak conc. of Quinidine Gluconate
4-5 hr
99
half-life of QUINIDINE
6-8 hr
100
manifestation of QUINIDINE toxicity
* Nausea * Vomiting * Abdominal discomfort * Thrombocytopenia * Tinnitus * CV toxicity (PVC)
101
occur if blood conc. of Quinidine is 2x the upper limit of TR (10 ug/mL)
CV toxicity (PVC)
102
Naturally occurring drug – extracted from barks of fever tree (Cinchona spp.)
QUINIDINE
103
QUNIDINE is tx for
cardiac arrhythmia
104
methods for QUINIDINE
Chromatography, IA
105
brand name of PROCAINAMIDE
Procanbin Procan SR Pronestyl
106
Protein-bound PROCAINAMIDE
20%
107
TR of PROCAINAMIDE
4-8 ug/ml
108
peak conc. of PROCAINAMIDE
1 hr
109
half-life of PROCAINAMIDE
4 hr
110
manifestations of PROCAINAMIDE toxicity
* myocardial depression * arrhythmia
111
PROCAINAMIDE is a tx for
cardiac arrhythmia
112
cardioactive drug metabolized in the liver
PROCAINAMIDE
113
A parent drug; effective form is its metabolite – NAPA
PROCAINAMIDE
114
method for PROCAINAMIDE
IA
115
procainamide metabolite
N-acetylprocainamide (NAPA)
116
inclusions in TOTAL PROCAINAMIDE
conc. of parent drug (procainamide) & conc. of metabolite (NAPA) as these 2 has same effect
117
brand name of DISOPYRAMIDE
Norpace
118
TR of DISOPYRAMIDE
3-7.5 ug/ml
119
peak conc. of DISOPYRAMIDE
1-2 hr
120
half-life of DISOPYRAMIDE
7 hr
121
toxic ranges of DISOPYRAMIDE?
> 4.5 ug/ml > 10 ug/ml
122
Toxic range of DISOPYRAMIDE with anticholinergic effect
>4.5 ug/ml
123
Toxic range of DISOPYRAMIDE with cardiac effects
>10 ug/ml
124
anticholinergic effects of DISOPYRAMIDE
Dry mouth Constipation
125
cardiac effects of DISOPYRAMIDE
Bradycardia – slower than normal heart rate AV node blockage
126
A Quinidine substitute – esp. if adverse effects of quinidine is unacceptable
DISOPYRAMIDE
127
methods for DISOPYRAMIDE
Chromatography, IA
128
cardioactive drug with TR that is also its toxic range? what is the TR and toxic range that is similar?
DISOPYRAMIDE >4.5 ug/ml (within 3-7.5 ug/ml)
129
TR of LIDOCAINE
1.5-4 ug/ml
130
Toxic range of LIDOCAINE
4-8 ug/ml >8 ug/ml
131
manifestation of LIDOCAINE toxicity if 4-8 ug/ml
CNS depression
132
manifestation of LIDOCAINE toxicity if >8 ug/ml
seizure, ↓ BP and cardiac output
133
Corrects ventricular arrhythmia
LIDOCAINE
134
Prevent ventricular fibrillation
LIDOCAINE
135
LIDOCAINE is a tx for
AMI
136
EXAMPLES OF ANTIBACTERIALS
AMINOGLYCOSIDES TEICOPLANIN VANCOMYCIN CHLORAMPHENICOL
137
Protein-bound AMINOGLYCOSIDES
10%
138
TR of AMINOGLYCOSIDES
Dependent on aminoglycosides used
139
peak conc. of AMINOGLYCOSIDES
1-2 hr
140
half-life of AMINOGLYCOSIDES
2-3 hr
141
toxic range of AMINOGLYCOSIDES
any conc. above TR of aminoglycosides
142
toxicity of aminoglycosides
Nephrotoxicity Ototoxicity
143
toxicity of aminoglycosides with hearing and balance impairment
Ototoxicity
144
toxicity of aminoglycosides with impairment of PCT function
Nephrotoxicity
145
REVERSIBLE Nephrotoxicity of Aminoglycosides
* Electrolyte imbalance * Proteinuria (Albuminuria)
146
IRREVERSIBLE Nephrotoxicity of Aminoglycosides
(chronic toxicity) * Tissue Necrosis * Kidney Failure
147
antibacterial drugs that are protein synthesis inhibitors
AMINOGLYCOSIDES CHLORAMPHENICOL
148
aminoglycosides is effective against
Gram negative bacteria
149
Examples of aminoglycosides
Gentamicin Tobramycin Amikacin Kanamycin
150
Methods for aminoglycosides
Chromatography, IA
151
Administration of aminoglycosides
IV or IM
152
bioavailability of aminoglycosides
100% (administered IV/IM) --> toxicity is much faster/common
153
Protein-bound TEICOPLANIN
90-95%
154
highly protein bound antibacterial drug
TEICOPLANIN (90-95%)
155
TR of TEICOPLANIN
10-60 mg/L 20-60 mg/L
156
TR of TEICOPLANIN used as tx for endocarditis
10-60 mg/L
157
TR of TEICOPLANIN used as tx for staph. infection
20-60 mg/L
158
half-life of TEICOPLANIN
70-100 hr
159
manifestation of TEICOPLANIN toxicity
* Nausea * Vomiting * Fever * Diarrhea * Mild hearing loss
160
TEICOPLANIN is a tx for
Methicillin-resistant Staphylococcus aureus (MRSA)
161
TEICOPLANIN is effective against
Aerobic & anaerobic gram positive cocci and bacilli
162
antibacterial drug not metabolized by the liver
TEICOPLANIN
163
Administration of TEICOPLANIN
IV or IM
164
brand name of VANCOMYCIN
Vancocin HCl
165
protein-bound VANCOMYCIN
55%
166
TR of VANCOMYCIN
5-10 ug/mL
167
peak conc. of VANCOMYCIN
1 hr
168
half-life of VANCOMYCIN
4-6 hr
169
antibacterial drug wherein TR is the toxic range? what is the toxic range?
VANCOMYCIN 10 ug/mL
170
common toxic effect of vancomycin characterized by erythemic flushing of extremities
Red-man syndrome
171
toxic range of vancomycin that exhibits nephrotoxicity
>10 ug/ml
172
toxic range of vancomycin that exhibits ototoxicity
>40 ug/ml
173
vancomycin is tx for
Gram positive cocci and bacilli
174
Cell wall inhibitor; kills microbes by destruction or inhibition of cell wall synthesis
vancomycin
175
administration of vancomycin
IV
176
manifestation of CHLORAMPHENICOL toxicity
Blood dyscrasia (aplastic anemia)
177
CHLORAMPHENICOL is a tx for
Gram negative bacteria
178
antibacterial drug effective against gram negative bacteria
AMINOGLYCOSIDES CHLORAMPHENICOL
179
antibacterial drug effective against gram positive cocci and bacilli
TEICOPLANIN VANCOMYCIN
180
Examples of PSYCHOACTIVE DRUGS (Anti-psychotic drugs)
LITHIUM TRICYCLIC ANTIDEPRESSANT (TCA) CLOZAPINE OLANZAPINE
181
brand name/s of LITHIUM
Eskalith Lithobid
182
Protein-bound lithium
Lithium salts, so it doesn’t bind to protein
183
TR of LITHIUM
0.5-1.2 mmol/l
184
peak conc. of LITHIUM
2-4 hr
185
half-life of LITHIUM
10-35 hr
186
toxic ranges of LITHIUM
1.5-2 mmol/L >2 mmol/L
187
manifestation of LITHIUM toxicity if 1.5-2 mmol/L
apathy lethargy speech difficulties muscle weakness
188
manifestation of LITHIUM toxicity if >2 mmol/L
muscle rigidity seizures coma
189
LITHIUM uses this that does not bind to proteins
lithium salts
190
Mood-altering drugs
LITHIUM
191
LITHIUM is a tx for
recurrent depression bipolar disorder
192
Administration of LITHIUM
Oral (completely and rapidly absorbed by GI)
193
protein-bound TCA
85-95%
194
2 forms of TCA
Amitriptyline Imipramine
195
TR of Amitriptyline (a TCA)
120-150 ng/ml
196
TR of Imipramine (a TCA)
150-300 ng/ml
197
peak conc. of TCA
2-12 hr
198
manifestation of TCA toxicity when there is slight increase
drowsiness constipation blurred vision memory loss
199
manifestation of TCA toxicity at higher levels
seizures cardiac arrhythmia unconsciousness
200
TCA includes?
amitriptyline imipramine doxepin
201
TCA is a tx for
depression insomnia extreme apathy loss of libido
202
Administration of TCA
oral
203
antipsychotic drug that is metabolized into its metabolize forms? what are these?
TCA Imipramine → desipramine Amitriptyline → nortriptyline
204
Therapeutic effects of this drug is not seen for the first 2-4 weeks after initiation of therapy; hence, effects of TCAs only occur after 4 weeks
TCA
205
brand name of CLOZAPINE
Clozaril FazaClo
206
protein-bound CLOZAPINE
97%
207
TR of CLOZAPINE
350-420 ng/ml
208
peak conc. of CLOZAPINE
2 hr
209
half-life of CLOZAPINE
8-16 hr
210
manifestation of CLOZAPINE toxicity
seizures
211
CLOZAPINE is a tx for
Treatment-refractory schizophrenia
212
brand name of OLANZAPINE
Zyprexa
213
protein-bound OLANZAPINE
93%
214
TR of OLANZAPINE
20-50 ng/ml
215
peak conc. of OLANZAPINE
5-8 hr
216
half-life of OLANZAPINE
21-54 hr
217
Thienobenzodiazepine derivative
OLANZAPINE
218
OLANZAPINE is a tx for
schizophrenia acute manic episodes bipolar disorders (recurrent)
219
Administration of OLANZAPINE
Oral IM (fast-acting formulation)
220
EXAMPLES OF IMMUNOSUPPRESIVE DRUGS
CYCLOSPORINE TACROLIMUS (FK-506) SIROLIMUS (RAPAMYCIN) MYCOPHENOLIC ACID (MPA)
221
Cyclic polypeptide with potent immunosuppressive activity
CYCLOSPORINE
222
function is to suppress graft-vs-host rejection (heterotopic transplanted organ) → piggyback transplant
CYCLOSPORINE
223
specimen of choice for CYCLOSPORINE? reason?
whole blood cyclosporine is sequestered inside the cell, including RBCs
224
BRAND NAME/S of CYCLOSPORINE
Gengraf Neoral Sandimmune
225
Protein-bound CYCLOSPORINE
>98%
226
TR of CYCLOSPORINE
Depends on transplanted organ
227
TR of CYCLOSPORINE if the transplanted organs are – liver, heart, pancreas
200-350 ng/m
228
TR of CYCLOSPORINE if the transplanted organ is kidneys
100-300 ng/ml
229
peak conc. of CYCLOSPORINE
1-6 hr
230
toxic range of CYCLOSPORINE
350-400 ng/ml
231
toxicity of CYCLOSPORINE
*nephrotoxic * Renal tubular dysfunction * Glomerular dysfunction
232
heart, liver, pancreas; attaching donor’s organ to the original patient’s organ
Piggyback transplant
233
brand name/s of TACROLIMUS
Hecoria Envarsus Prograf Astagraf
234
protein-bound TACROLIMUS
>98%
235
TR of TACROLIMUS
10-15 ng/ml
236
aka FK-506
TACROLIMUS
237
toxicity of TACROLIMUS
Nephrotoxicity Thrombus formation
238
100x more potent than cyclosporine
TACROLIMUS
239
function is to suppress transplant rejection, and graft-vs-host disease
TACROLIUMUS
240
specimen of choice for TACROLIMUS
whole blood
241
SIROLIMUS is aka
RAPAMYCIN
242
brand name of SIROLIMUS
Rapamune
243
protein-bound SIROLIMUS
92% bound to LPP
244
TR of SIROLIMUS if administered w/ cyclosporine
4-12 ug/L
245
TR of SIROLIMUS if – if cyclosporine is not used/discontinued
12-20 ug/L
246
toxicity of SIROLIMUS
Blood dyscrasia (anemia, leukopenia, and thrombocytopenia → aplastic anemia) Hyperlipidemia
247
Antifungal agent with immunosuppressive activity
SIROLIMUS
248
a prophylactic drug to prevent graft rejection before kidney transplant
SIROLIMUS
249
Specimen of choice for SIROLIMUS
Whole Blood
250
drugs used in conjunction with cyclosporine or tacrolimus
SIROLIMUS MYCOPHENOLIC ACID
251
brand name of MPA
Myfortic
252
Protein-bound MPA
95%
253
toxicity of MPA
Nausea Vomiting Diarrhea Abdominal pain
254
Prodrug of mycophenolate mofetil
MPA
255
a Lymphocyte proliferation inhibitor and immunosuppressive drug
MPA
256
supplemental therapy with cyclosporine & tacrolimus esp. if the patient is a renal transplant patient
MPA
257
brand name/s of METHOTREXATE
Otrexup Rasuvo
258
toxicity of METHOTREXATE
Cytotoxicity
259
administered to lessen and ensure nonlethal cytotoxicity produced by methotrexate
Leucovorin (Leucovorin rescue)
260
Destroys neoplastic cells by inhibiting DNA synthesis
METHOTREXATE
261
DNA synthesis inhibitor
METHOTREXATE
262
Can both affect normal and neoplastic cells since they both have DNA (but neoplastic cells are more susceptible)
METHOTREXATE
263
METHOTREXATE is a tx for
Psoriasis
264
brand name/s of THEOPHYLLINE
Theo-Dur Thea-24 Uniphyl
265
Protein-bound THEOPHYLLINE
50-60% (usually bound to ALBUMIN)
266
TR of THEOPHYLLINE
10-20 mg/L
267
formulation of THEOPHYLLINE with 1-2 hr peak conc.
rapid-release formulation
268
formulation of THEOPHYLLINE with 4-8 hr peak conc.
modified-release formulation
269
toxicity of THEOPHYLLINE if >20 ug/ml
nausea, vomiting, diarrhea
270
toxicity of THEOPHYLLINE if >30 ug/ml
cardiac arrhythmia, seizures
271
THEOPHYLLINE is a tx for
asthma stable COPD
272
a bronchodilator
THEOPHYLLINE
273
an anti-neoplastic drug
METHOTREXATE
274
Types of seizures
Grand mal seizure/Tonic–Clonic Complex Partial Seizure Petit mal/ Absent/ Starting Seizure
275
Types of seizure that lasts for >5mins
Tonic–Clonic (Grand mal seizure)
276
Types of seizure that arises from one side of brain
Complex Partial Seizure
277
Types of seizure that black out for a minute
Petit mal/ Absent/ Starting Seizure
278
brand name/s of PHENOBARBITAL
Luminal Solfoton
279
brand name/s of PHENYTOIN
Dilantin
280
brand name/s of VALPROIC ACID
Depakote Depakene
281
brand name/s of CARBAMAZEPINE
Tegretol
282
brand name/s of ETHOSUXIMIDE
Zarontin
283
brand name/s of FELBAMATE
Felbatol
284
brand name/s of GABAPENTIN
Neurontin
285
brand name/s of LAMOTRIGINE
Lamictal
286
brand name/s of OXCARBAZEPINE
Trileptal
287
brand name/s of TIAGABINE
Gabitril
288
brand name/s of TOPIRAMATE
Topamax
289
brand name/s of ZONISAMIDE
Zonegran
290
protein-bound PHENOBARBITAL
50%
291
protein-bound PHENYTOIN (Diphenylhydantoin)
87-97%
292
protein-bound VALPROIC ACID
93%
293
protein-bound CARBAMAZEPINE
70-80%
294
protein-bound ETHOSUXIMIDE
<5%
295
protein-bound FELBAMATE
30%
296
protein-bound GABAPENTIN
Do not bind to protein
297
protein-bound LAMOTRIGINE
55%
298
protein-bound OXCARBAZEPINE
40%
299
protein-bound TIAGABINE
96%
300
protein-bound TOPIRAMATE
15%
301
protein-bound ZONISAMIDE
60%
302
toxicity of PHENOBARBITAL
Drowsiness Fatigue Depression Reduced mental capacity
303
Slow-acting barbiturate
PHENOBARBITAL
304
tx for all types of seizures except petit mal
PHENOBARBITAL
305
administration of PHENOBARBITAL
oral; slow GI absorption but complete
306
inactive proform of phenobarbital
Primidone
307
Primidone is a tx for
Grand mal seizure
308
Readily absorbed by GI; undergo first-pass metabolism to form PHENOBARBITAL
Primidone
309
toxicity of PHENYTOIN
Seizures Ataxia – difficulty in balanced walking Coma Vit D deficiency Seizures
310
PHENYTOIN is a tx for
tonic-clonic seizure
311
proform of phenytoin; IM drug
Fosphenytoin
312
rapidly absorbed within 75 mins after administration → already metabolized
Fosphenytoin
313
Conditions when protein-binding is ↓
Anemia Hypoalbuminemia Coadministration of same binding properties as phenytoin
314
toxic value of VALPROIC ACID
>120 ug/mL
315
most common toxicity of VALPROIC ACID
* Nausea * Lethargy * Weight gain
316
more serious toxicity of VALPROIC ACID (>200 ug/mL)
Pancreatitis Hyperammonemia Hallucinations
317
VALPROIC ACID is a tx for
petit mal seizure
318
Inhibit metabolism of other anti-epileptic drugs
VALPROIC ACID
319
CARBAMAZEPINE toxicity
Ataxia Leukopenia Seizures Aplastic anemia
320
CARBAMAZEPINE toxicity if >15 ng/mL
Aplastic anemia
321
usually has RARE TOXICITY, often tolerable, self-limiting
ETHOSUXIMIDE
322
CARBAMAZEPINE is a tx for
seizure and facial pain
323
ETHOSUXIMIDE is a tx for
petit mal seizure
324
PRIMIDONE toxicity
Anemia Ataxia Nausea
325
PRIMIDONE is a tx for
tonic-clonic and complex partial seizure
326
FELBAMATE toxicity
Fatal aplastic anemia Hepatic failure
327
FELBAMATE is a tx for
Mixed-seizure disorders (children) Lennox-Gastaut syndrome Refractory epilepsy (adults)
328
administration of FELBAMATE
Oral (most common; almost complete absorption of felbamate in GI tract)
329
GABAPENTIN toxicity
*mild * Fatigue * Ataxia * Dizziness * Weight gain
330
GABAPENTIN is a tx for
AED for patients with o Liver disease o Acute Intermittent Porphyria (w/ partial onset seizures)
331
GABAPENTIN administration
Oral (60% bioavailability)
332
T/F Gabapentin is metabolized by the liver
F
333
LAMOTRIGINE toxicity
Usually evident if given with valproic acid as it can inhibit metabolism of other AED * dizziness * GI disturbances * rashes
334
LAMOTRIGINE is a tx for
partial or generalized tissues
335
OXCARBAZEPINE toxicity
Similar with carbamazepine
336
OXCARBAZEPINE is a tx for
partial seizures tonic-clonic seizures
337
OXCARBAZEPINE Administration
oral (immediately into licarbazepine)
338
metabolite of OXCARBAZEPINE
Licarbazepine
339
TIAGABINE toxicity
confusion stuttering mild sedation PARESTHESIA
340
TIAGABINE is a tx for
partial seizures
341
has toxicity of change of taste with particular foods (diet coke and beet)
TOPIRAMATE
342
TOPIRAMATE toxicity
change of taste with particular foods (diet coke and beer) “pins and needles” sensation in extremities
343
TOPIRAMATE administration
Oral (almost completely absorbed; almost 100% bioavailability)
344
ZONISAMIDE toxicity
breathing difficulty low BP slow heart rate loss of consciousness
345
an anticonvulsant
ZONISAMIDE
346
ZONISAMIDE is a tx for
partial and generalized seizure
347
administration of ZONISAMIDE
Oral