Sheet1 Flashcards
(500 cards)
1
Q
Time it takes for amount of drug to fall to half of its value; this is a constant in first order kinetics (majority of drugs)
A
Half-life (T1/2)
2
Q
Relates the amount of drug in the body to the plasma concentration
A
Volume of distribution (VD)
3
Q
Plasma concentration of a drug at a given time
A
Cp
4
Q
The ratio of the rate of elimination of a drug to its plasma concentration
A
Clearance (CL)
5
Q
The elimination of drug that occurs before it reaches the systemic circulation
A
First pass effect
6
Q
The fraction of administered dose of a drug that reaches systemic circulation
A
Bioavailability (F)
7
Q
When the rate of drug input equals the rate of drug elimination
A
Steady state
8
Q
This step of metabolism makes a drug more hydrophilic and hence augments elimination
A
Phase I
9
Q
Different steps of Phase I
A
Oxidation, reduction, hydrolysis
10
Q
Inducers of Cytochrome P450 (CYP450)
A
Barbiturates, phenytoin, carbamazepine, and rifampin
11
Q
Inhibitors of CYP450
A
Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
12
Q
Products of Phase II conjugation
A
Glucuronate, acetic acid, and glutathione sulfate
13
Q
Type of kinetics when a constant percentage of substrate is metabolized per unit time
A
First order kinetics
14
Q
Drug elimination with a constant amount metabolized regardless of drug concentration
A
Zero order kinetics
15
Q
Target plasma concentration times (volume of distribution divided by bioavailability)
A
Loading dose (Cp*(Vd/F))
16
Q
Concentration in the plasma times (clearance divided by bioavailability)
A
Maintenance dose (Cp*(CL/F))
17
Q
Strength of interaction between drug and its receptor
A
Affinity
18
Q
Selectivity of a drug for its receptor
A
Specificity
19
Q
Amount of drug necessary to elicit a biologic effect; refers to the drug’s strength
A
Potency
20
Q
Maximum response achieveable from a drug
A
Efficacy
21
Q
Ability of a drug to produce 100% of the maximum response regardless of the potency
A
Full agonist
22
Q
Ability to produce less than 100% of the response
A
Partial agonist
23
Q
Ability to bind reversibly to the same site as the drug and without activating the effector system
A
Competitive antagonist
24
Q
Class of drugs with ability to decrease the maximal response to an agonist
A
Noncompetitive antagonist
25
A hormone whose mechanism of action (MOA) utilizes intracellular receptors
Thyroid and steroid hormones
26
A hormone whose MOA utilizes transmembrane receptors
Insulin
27
Class of drugs whose MOA utilizes ligand gated ion channels
Benzodiazepines and calcium channel blockers
28
Median effective dose required for an effect in 50% of the population
ED50
29
Median toxic dose required for a toxic effect in 50% of the population
TD50
30
Dose which is lethal to 50% of the population
LD50
31
Window between therapeutic effect and toxic effect
Therapeutic index
32
Term for a high margin of safety
High therapeutic index
33
Term for a narrow margin of safety
Low therapeutic index
34
Antidote used for lead poisoning
Dimercaprol, EDTA
35
Antidote used for cyanide poisoning
Nitrites
36
Antidote used for anticholinergic poisoning
Physostigmine
37
Antidote used for organophosphate/anticholinesterase poisoning
Atropine, pralidoxime (2-PAM)
38
Antidote used for iron salt toxicity
Deferoxamine
39
Antidote used for acetaminophen (APAP) toxicity
N-acetylcysteine (Mucomyst)
40
Antidote for arsenic, mercury, lead, and gold poisoning
Dimercaprol
41
Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
Penicillamine
42
Antidote used for heparin overdose
Protamine
43
Antidote used for warfarin toxicity
Vitamin K and Fresh frozen plasma (FFP)
44
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid
45
Antidote used for methanol and ethylene glycol
Ethanol or fomepizole
46
Antidote used for opioid toxicity
Naloxone (IV), naltrexone (PO)
47
Antidote used for benzodiazepine toxicity
Flumazenil
48
Antidote used for tricyclic antidepressants (TCA)
Sodium bicarbonate
49
Antidote used for carbon monoxide poisoning
100% O2 and hyperbaric O2
50
Antidote used for digitalis toxicity
Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
51
Antidote used for beta agonist toxicity (eg. Metaproterenol)
Esmolol
52
Antidote for methotrexate toxicity
Leucovorin
53
Antidote for beta-blockers and hypoglycemia
Glucagon
54
Antidote useful for some drug induced Torsade de pointes
Magnesium sulfate
55
Antidote for hyperkalemia
sodium polystyrene sulfonate (Kayexalate)
56
Antidote for salicylate intoxication
Alkalinize urine, dialysis
57
Constant proportion of cell population killed rather than a constant number
Log-kill hypothesis
58
Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
Pulse therapy
59
Toxic effect of anticancer drug can be lessened by rescue agents
Rescue therapy
60
Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
Allopurinol
61
Pyrimidine analog that causes "Thymine-less death" given with leucovorin rescue
5-flouracil (5-FU)
62
Drug used in cancer therapy causes Cushing-like symptoms
Prednisone
63
Side effect of Mitomycin
SEVERE myelosuppression
64
MOA of cisplatin
Alkylating agent
65
Common toxicities of cisplatin
Nephro and ototoxicity
66
Analog of hypoxanthine, needs HGPRTase for activation
6-mercaptopurine (6-MP)
67
Interaction with this drug requires dose reduction of 6-MP
Allopurinol
68
May protect against doxorubicin toxicity by scavenging free radicals
Dexrazoxane
69
Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis
Bleomycin
70
Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm
Testicular cancer
71
ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP
Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine
72
Regimen used for non-Hodgkin's lymphoma
CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
73
Regimen used for breast cancer
CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
74
Alkylating agent, vesicant that causes tissue damage with extravasation
Mechlorethamine
75
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
Cyclophosphamide
76
Prevention of cyclophosphamide induced hemorrhagic cystitis
Hydration and mercaptoethanesulfonate (MESNA)
77
Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation
Vincristine
78
Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
Paclitaxel (taxol)
79
Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides
Cisplatin
80
Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression
Carboplatin
81
Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
L-asparaginase
82
Used for hairy cell leukemia; it stimulates NK cells
Interferon alpha
83
Anti-androgen used for prostate cancer
Flutamide (Eulexin)
84
Anti-estrogen used for estrogen receptor + breast cancer
Tamoxifen
85
Aromatase inhibitor used in breast cancer
Letrozole, anastrozole
86
Newer estrogen receptor antagonist used in advanced breast cancer
Toremifene (Fareston)
87
Some cell cycle specific anti-cancer drugs
Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
88
Some cell cycle non-specific drugs
Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea
89
Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonists
Odansetron, granisetron
90
Nitrosoureas with high lipophilicity, used for brain tumors
Carmustine (BCNU) and lomustine (CCNU)
91
Produces disulfiram-like reaction with ethanol
Procarbazine
92
Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors
Octreotide
93
Somatotropin (GH) analog used in GH deficiency (dwarfism)
Somatrem
94
GHRH analog used as diagnostic agent
Sermorelin
95
GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively
Leuprolide
96
GnRH antagonist with more immediate effects, used for infertility
Ganirelix
97
Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
Bromocriptine
98
Hormone inhibiting prolactin release
Dopamine
99
ACTH analog used for diagnosis of patients with corticosteroid abnormality
Cosyntropin
100
Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
Desmopressin (DDAVP)
101
SE of OCs
Increased thromboembolic events
102
Most widely used thyroid drugs such as Synthroid and Levoxyl contain
L-thyroxine (T4)
103
T3 compound less widely used
Cytomel
104
Anti-thyroid drugs
Thioamides, iodides, radioactive iodine, and ipodate
105
Thioamide agents used in hyperthyroidism
Methimazole and propylthiouracil (PTU)
106
Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy
PTU
107
PTU (propylthiouracil) MOA
Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
108
Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
Iodide salts
109
Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma
Thyroxine
110
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
Radioactive iodine
111
Radio contrast media that inhibits the conversion of T4 to T3
Ipodate
112
Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3
Beta-blockers such as propranolol
113
Vitamins containing iron should NOT be taken simultaneously with levothyroxine because
Iron deiodinates thyroxine
114
Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because
Estogens increase maternal TBG
115
3 zones of adrenal cortex and their products
Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
116
Pneumonic for 3 zones of adrenal cortex
GFR
117
Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)
Glucocorticoids
118
Short acting glucocorticoids
Cortisone and hydrocortisone (equivalent to cortisol)
119
Intermediate acting glucocorticoids
Prednisone, methylprednisolone, prednisolone, and triamcinolone
120
Long acting glucocorticoids
Betamethasone and dexamethasone
121
Mineralocorticoids
Fludrocortisone and deoxycorticosterone
122
Some side effects of corticosteroids
Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis, stria, thinning of skin
123
Period of time of therapy after which GC therapy will need to be tapered
5-7 days
124
Used for Cushing's syndrome (increased corticosteroid)
Dexamethasone suppression test
125
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
Aminoglutethimide
126
Antifungal agent used for inhibition of all gonadal and adrenal steroids
Ketoconazole
127
Antiprogestin used as potent antagonist of GC receptor
Mifepristone
128
Diuretic used to antagonize aldosterone receptors
Spironolactone
129
Common SE of spironolactone
Gynecomastia and hyperkalemia
130
Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss
Estrogen
131
Antiestrogen drugs used for fertility and breast cancer respectively
Clomiphene and tamoxifen
132
Common SE of tamoxifen and raloxifene
Hot flashes
133
Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and prophylaxis in women with risk factors for breast cancer
Raloxifene
134
Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
Diethylstilbestrol (DES)
135
Estrogen mostly used in oral contraceptives (OC)
Ethinyl estradiol and mestranol
136
Anti-progesterone used as abortifacient
Mifepristone (RU-486)
137
Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)
Combination oral contraceptives (OC)
138
Oral contraceptive available in a transdermal patch
Ortho-Evra
139
Converted to more active form DHT by 5 alpha-reductase
Testosterone
140
5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness
Finasteride (Proscar and Propecia respectively)
141
Anabolic steroid that has potential for abuse
Nandrolone, oxymetholone, and oxandrolone
142
Anti-androgen used for hirsutism in females
Cyproterone acetate
143
Drug is used with testosterone for male fertility
Leuprolide
144
What do alpha cells in the pancreas produce?
Glucagon
145
What do beta cells in the pancreas produce?
Insulin
146
Where are beta cells found in the pancreas?
Islets of Langerhans
147
What do delta cells in the pancreas produce?
Somatostatin
148
Product of proinsulin cleavage used to assess insulin abuse
C-peptide
149
Exogenous insulin contains
Little C-peptide
150
Endogenous insulin contains
Normal C-peptide
151
Very rapid acting insulin, having fastest onset and shortest duration of action
Lispro (Humalog), aspart, glulisine
152
Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia
Regular (Humulin R)
153
Long acting insulin
Ultralente (humulin U)
154
Ultra long acting insulin, has over a day duration of action
Glargine (Lantus), detemir
155
Major SE of insulin
Hypoglycemia
156
Important in synthesis of glucose to glycogen in the liver
GLUT 2
157
Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation
GLUT 4
158
Examples of alpha-glucosidase inhibitors (AGI)
Acarbose, miglitol
159
MOA of AGI's
Act on intestine, delay digestion and absorption of glucose formed from digestion of starch and disacchrides
160
SE of AGI's
Flatulence (do not use beano to tx), diarrhea, abdominal cramps
161
Alpha-glucosidase inhibitor associated with elevation of LFT's
Acarbose
162
Amino acid derivative, active as an insulin secretagogue
Nateglinide
163
MOA of nateglinide
Insulin secretagogue - closes ATP-sensitive K+ channel
164
Biguanide
Metformin
165
Drugs available in combination with metformin
Glyburide, glipizide, and rosiglitazone
166
MOA of metformin
Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity
167
Vascular effects of metformin
Decreased micro and macro vascular disease
168
Most important potential SE of metformin
Lactic acidosis
169
Incidence of hyoglycemia with metformin
None
170
Meglitinide class of drugs
Repaglinide
171
MOA of repaglinide
Insulin release from pancreas; faster and shorter acting than sulfonylurea
172
First generation sulfonylurea
Chlorpropamide, tolbutamide, tolazamide, etc.
173
Second generation sulfonylurea
Glyburide, glipizide, glimepiride, etc.
174
MOA of both generations
Insulin release from pancreas by modifying K+ channels
175
Common SE of sulfonylureas, repaglinide, and nateglinide
Hypoglycemia
176
Sulfonylurea NOT recommended for elderly because of very long half life
Chlorpropamide
177
Thiazolidinediones
Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
178
Reason troglitazone was withdrawn from market
Hepatic toxicity
179
MOA of thiazolindinediones
Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism
180
SE of Thiazolindinediones
Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism
181
Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation
Glucagon
182
Available bisphosphonates
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
183
MOA of Bisphosphonates
Inhibits osteoclast bone resorption
184
Names of three bisphosphonates available IV
Pamidronate, zoledronate, ibandronate
185
Uses of bisphosphonates
Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
186
Major SE of bisphosphonates
Chemical esophagitis
187
Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
Etidronate
188
Used for prevention of postmenopausal osteoporosis in women
Estrogen (HRT-Hormone replacement therapy)
189
Increase bone density, also being tested for breast CA prophylaxis
Raloxifene (SERM-selective estrogen receptor modulator)
190
Used intranasally and decreases bone resorption
Calcitonin (salmon prep)
191
Used especially in postmenopausal women, dosage should be 1500 mg
Calcium
192
Vitamin given with calcium to ensure proper absorption
Vitamin D
193
Disease caused by excess ergot alkaloids
St. Anthony's Fire
194
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
Autocoids
195
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
Zollinger-Ellison Syndrome
196
Drug that causes contraction of the uterus
Oxytocin
197
Distribution of histamine receptors H1, H2, and H3
Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
198
Prototype antagonist of H1 and H2 receptors
Diphenhydramine and cimetridine, respectively
199
1st generation antihistamine that is highly sedating
Diphendydramine
200
1st generation antihistamine that is least sedating
Chlorpheniramine or cyclizine
201
2nd generation antihistamines
Fexofenadine, loratadine, and cetirizine
202
Generation of antihistamine that has the most CNS effects
First generation due to being more lipid-soluble
203
Major indication for H1 receptor antagonist
Use in IgE mediated allergic reaction
204
Antihistamine that can be used for anxiety and insomnia and is not addictive
hydroxyzine (Atarax)
205
H1 antagonist used in motion sickness
Dimenhydrinate, meclizine, and other 1st generation
206
Most common side effect of 1st generation antihistamines
Sedation
207
Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.
Terfenadine and astemizole (have been removed from the market)
208
H2 blocker that causes the most interactions with other drugs
Cimetidine
209
Clinical use for H2 blockers
Acid reflux disease, duodenal ulcer and peptic ulcer disease
210
Receptors for serotonin (5HT-1) are located
Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
211
5HT-1d agonist used for migraine headaches
Sumatriptan, naratriptan, and rizatriptan
212
Triptan available in parenteral and nasal formulation
Sumatriptan
213
H1 blocker that is also a serotonin antagonist
Cyproheptadine
214
Agents for reduction of postpartum bleeding
Oxytocin, ergonovine and ergotamine
215
Agents used in treatment of carcinoid tumor
Ketanserin cyproheptadine, and phenoxybenzamine
216
5HT-3 antagonist used in chemotherapeutic induced emesis
Ondansetron, granisetron, dolasetron and alosetron
217
5HT-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
Dolasetron
218
DOC to treat chemo-induced nausea and vomiting
Odansetron
219
Drug used in ergot alkaloids overdose, ischemia and gangrene
Nitroprusside
220
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
221
SE of ergot alkaloids
Hallucinations resembling psychosis
222
Ergot alkaloid used as an illicit drug
LSD
223
Dopamine agonist used in hyperprolactinemia
Bromocriptine
224
Peptide causing increased capillary permeability and edema
Bradykinin and histamine
225
Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
Bradykinin
226
Drug causing depletion of substance P (vasodilator)
Capsaicin
227
Prostaglandins that cause abortions
Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
228
Difference between COX 1 and COX 2
COX 1 is found throughout the body and COX 2 is only in inflammatory tissue
229
Drug that selectively inhibits COX 2
Celecoxib and rofecoxib
230
Inhibitor of lipoxygenase
Zileuton
231
Major SE of zileuton
Liver toxicity
232
Inhibitor of leukotrienes (LTD4) receptors and used in asthma
Zafirlukast and montelukast
233
Used in pediatrics to maintain patency of ductus arteriosis
PGE1
234
Approved for use in severe pulmonary HTN
PGI2 (epoprostenol)
235
Prostaglandin used in the treatment of impotence
Alprostadil
236
Irreversible, nonselective COX inhibitor
Aspirin
237
Class of drugs that reversibly inhibit COX
NSAIDS
238
Primary endogenous substrate for Nitric Oxidase Synthase
Arginine
239
MOA and effect of nitric oxide
Stimulates cGMP which leads to vascular smooth muscle relaxation
240
Long acting beta 2 agonist used in asthma
Salmeterol
241
Muscarinic antagonist used in asthma
Ipratropium
242
MOA action of cromolyn
Mast cell stabilizer
243
Methylxanthine derivative used as a remedy for intermittent claudication
Pentoxifylline
244
MOA of corticosteroids
inhibit phospholipase A2
245
SE of long term (>5 days) corticosteroid therapy and remedy
Adrenal suppression and weaning slowly, respectively
246
MOA of quinolones
Inhibit DNA gyrase
247
MOA of penicillin
Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
248
Drug used for MRSA
Vancomycin
249
Vancomycin MOA
Blocks peptidoglycan synthesis
250
Type of resistance found with vancomycin
Point mutation
251
Meningitis prophylaxis in exposed patients
Rifampin
252
Technique used to diagnose perianal itching, and the drug used to treat it
Scotch tape technique and mebendazole
253
Two toxicities of aminoglycosides
nephro and ototoxicity
254
DOC for Legionnaires' disease
Erythromycin
255
MOA of sulfonamides
Inhibit dihydropteroate synthase
256
Penicillins active against penicillinase secreting bacteria
Methicillin, nafcillin, and dicloxacillin
257
Cheap wide spectrum antibiotic DOC for otitis media
Amoxicillin
258
Class of antibiotics that have 10% cross sensitivity with penicillins
Cephalosporins
259
PCN active against pseudomonas
Carbenicillin, piperacillin and ticarcillin
260
Antibiotic causing red-man syndrome, and prevention
Vancomycin, infusion at a slow rate and antihistamines
261
Drug causes teeth discoloration
Tetracycline
262
MOA of tetracycline
Decreases protein synthesis by inhibiting 30S ribosome
263
Drug that causes gray baby syndrome and aplastic anemia
Chloramphenicol
264
Drug notorious for causing pseudomembranous colitis
Clindamycin
265
DOC for tx of pseudomembranous colitis
Metronidazole
266
Treatment of resistant pseudomembranous colitis
ORAL vancomycin
267
Anemia caused by trimethoprim
Megaloblastic anemia
268
Reason fluoroquinolones are contraindicated in children and pregnancy
Cartilage damage
269
DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas
Metronidazole
270
Treatment for TB patients (think RIPE)
Rifampin, Isoniazid, Pyrazinamide, and Ethambutol
271
Metronidazole SE if given with alcohol
Disulfiram-like reaction
272
Common side effect of Rifampin
Red urine discoloration
273
MOA of nystatin
Bind ergosterol in fungal cell membrane
274
Neurotoxicity with isoniazid (INH) prevented by
Administration of Vit. B6 (pyridoxine)
275
Toxicity of amphotericin
Nephrotoxicity
276
SE seen only in men with administration of ketoconazole
Gynecomastia
277
Topical DOC in impetigo
Topical mupirocin (Bactroban)
278
DOC for influenza A
Amantadine
279
DOC for RSV
Ribavirin
280
DOC for CMV retinitis
Ganciclovir
281
SE for ganciclovir
Neutro, leuko and thrombocytopenia
282
Anti-viral agents associated with Stephen Johnson syndrome
Nevirapine, amprenavir
283
HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism
Protease inhibitors
284
Antivirals that are teratogens
Delavirdine, efavirenz, and ribavirin
285
Antivirals associated with neutropenia
Ganciclovir, zidovudine, saquinavir, and interferon
286
HIV med used to reduce transmission during birth
AZT (zidovudine)
287
Drug used for African sleeping sickness
Suramin
288
Drug used in Chagas disease
Nifurtimox
289
Cephalosporins able to cross the BBB
Cefuroxime (2nd) generation, Ceftazidime, Ceftriaxone
290
Cephalosporins NOT able to cross the BBB
Cefixime (3rd) generation
291
Drug used for N. gonorrhea in females
Ceftriaxone
292
Cephalosporin causes kernicterus in neonates
Ceftriaxone or cefuroxime
293
SE of INH
Peripheral neuritis and hepatitis
294
Aminoglycoside that is least ototoxic
Streptomycin
295
Drug used in exoerythrocytic cycle of malaria
Primaquine
296
Oral antibiotic of choice for moderate inflammatory acne
Minocycline
297
Drug of choice for leprosy
Dapsone, rifampin and clofazimine combination
298
DOC for herpes and its MOA
Acyclovir; incorporated into viral DNA and chain termination
299
Anti-microbials that cause hemolysis in G6PD-deficient patients
Sulfonamides
300
MOA of erythromycin
Inhibition of protein synthesis at the 50s subunit of ribosome
301
Anti-biotic frequently used for chronic UTI prophylaxis
sulfamethoxazole/ trimethoprim
302
Lactam that can be used in PCN allergic patients
Aztreonam
303
SE of imipenem
Seizures
304
Anti-viral with a dose limiting toxicity of pancreatitis
Didanosine
305
Common side effect of hypnotic agents
Sedation
306
Occurs when sedative hypnotics are used chronically or at high doses
Tolerance
307
The most common type of drug interaction of sedative hypnotics with other depressant medications
Additive CNS depression
308
Benzodiazepines used to promote sleep
Temazpam, trizolam, flurazepam
309
Benzodiazepine used for anxiety
Alprazolam
310
Non-benzodiazepine used as an anxiolytic
Buspirone
311
Non-benzodiazepine used for sleep
Zolpidem
312
Major effect of benzodiazepines on sleep at high doses
REM is decreased
313
Neurologic SE of benzodiazepines
Anterograde amnesia
314
Reason benzos are used cautiously in pregnancy
Ability to cross the placenta
315
Main route of metabolism for benzodiazepines
Hepatic
316
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
Lorazepam, oxazepam, and temazepam
317
MOA for benzodiazepines
increase the FREQUENCY of GABA-mediated chloride ion channel opening
318
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
Flumazenil
319
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
Diazepam
320
Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
Clonazepam
321
Benzodiazepines that are the most effective in the treatment of panic disorder
Alprazolam and Clonazepam
322
Benzodiazepine that is used for anesthesia
Midazolam
323
DOC for status epilepticus
Diazepam
324
Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
Chlordiazepoxide and Diazepam
325
Agents having active metabolites, long half lives, and a high incidence of adverse effects
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
326
Barbiturates may precipitate this hematologic condition
Acute intermittent porphyria
327
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
Liver enzyme INDUCTION
328
Barbiturates MOA
Increase the DURATION of GABA-mediated chloride ion channels
329
Barbiturate used for the induction of anesthesia
Thiopental
330
Site of action for zaleplon and zolpidem
Benzodiazepine receptor BZ1 (although do not have a benzodiazepine ring structure)
331
Good hypnotic activity with less CNS SE than most benzodiazepines
Zolpidem, zaleplon
332
Agent that is a partial agonist for the 5-HT1A receptor
Buspirone
333
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
Buspirone
334
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
Ethanol
335
Agent with zero-order kinetics
Ethanol
336
Rate limiting step of alcohol metabolism
Aldehyde dehydrogenase
337
System that increases in activity with chronic ethanol exposure and may contribute to tolerance
MEOS
338
Enzyme that metabolizes acetaldehyde to acetate
Aldehyde dehydrogenase
339
Agents that inhibit acetaldehyde dehydrogenase
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
340
Agent that inhibits alcohol dyhydrogenase and its clinical use
FOMEPIZOLE - used to prevent formation of toxic metabolites from methanol and ethylene glycol ingestion
341
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
Disulfiram
342
The most common neurologic abnormality in chronic alcoholics
Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
343
Agent that is teratogen and causes a fetal syndrome
Ethanol
344
Agent that is the antidote for methanol overdose
Ethanol, fomepizole
345
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
Fomepizole
346
Most frequent route of metabolism
Hepatic enzymes
347
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
Sodium channel blockade
348
MOA for benzodiazepines and barbiturates
GABA-related targets
349
MOA for Ethosuximide
Calcium channels
350
MOA for Valproic acid at high doses
Affect calcium, potassium, and sodium channels
351
Drugs of choice for generalized tonic-clonic and partial seizures
Valproic acid and Phenytoin
352
DOC for febrile seizures
Phenobarbital
353
Drugs of choice for absence seizures
Ethosuximide and valproic acid
354
Drug of choice for myoclonic seizures
Valproic acid
355
Drugs of choice for status epilepticus
IV diazepam for short term (acute) treatment; phenytoin for prolonged therapy
356
Drugs that can be used for infantile spasms
Corticosteroids
357
Anti-seizure drugs used also for bipolar affective disorder (BAD)
Valproic acid, carbamazepine, phenytoin and gabapentin
358
Anti-seizure drugs used also for Trigeminal neuralgia
Carbamazepine
359
Anti-seizure drugs used also for pain of neuropathic orgin
Gabapentin
360
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
Phenytoin
361
SE of phenytoin
Gingival hyperplasia, nystagmus, diplopia and ataxia
362
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida
Carbamazepine
363
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
Valproic acid
364
Laboratory value required to be monitored for patients on valproic acid
Serum ammonia and LFT's
365
SE for Lamotrigine
Stevens-Johnson syndrome
366
SE for Felbamate
Aplastic anemia and acute hepatic failure
367
Anti-seizure medication also used in the prevention of migraines
Valproic acid
368
Carbamazepine may cause
Agranulocytosis
369
Anti-seizure drugs used as alternative drugs for mood stabilization
Carbamazepine, gabapentin, lamotrigine, and valproic acid
370
MOA of general anesthetics
Most are thought to act at GABA-A receptor - chloride channel
371
Inhaled anesthetic with a low blood/gas partition coefficient
Nitrous oxide
372
Inversely related to potency of anesthetics
Minimum alveolar anesthetic concentration (MAC)
373
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
Halothane and methoxyflurane
374
Most inhaled anesthetics SE
Decrease arterial blood pressure
375
Inhaled anesthetics are myocardial depressants
Enflurane and halothane
376
Inhaled anesthetic causes peripheral vasodilation
Isoflurane
377
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
Halothane
378
Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
Nitrous oxide
379
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
Methoxyflurane
380
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
Nitrous oxide
381
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
Desflurane
382
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
Dantrolene
383
IV barbiturate used as a pre-op anesthetic
Thiopental
384
Benzodiazepine used adjunctively in anesthesia
Midazolam
385
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
Flumazenil
386
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
Ketamine
387
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
Fentanyl
388
State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
Neuroleptanesthesia
389
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
Propofol
390
MOA of local anesthetics (LA's)
Block voltage-dependent sodium channels
391
This may enhance activity of local anesthetics
Hyperkalemia
392
This may antagonize activity of local anesthetics
Hypercalcemia
393
Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity
Vasodilation
394
Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery
Cocaine
395
Longer acting local anesthetics which are less dependent on vasoconstrictors
Tetracaine and bupivacaine
396
These LA's have surface activity
Cocaine and benzocaine
397
Most important toxic effects of most local anesthetics
CNS toxicity
398
Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction
Cocaine
399
LA causing methemoglobinemia
Prilocaine
400
Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation
Neuromuscular blocking drugs
401
These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
402
These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)
Nondepolarizing type antagonists
403
Agent with long duration of action and is most likely to cause histamine release
Tubocurarine
404
Non-depolarizing skeletal muscle antagonist that has short duration
Mivacurium
405
Skeletal muscle agent that can block muscarinic receptors
Pancuronium
406
Skeletal muscle agent that undergoes Hofmann elimination (breaks down spontaneously)
Atracurium
407
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur
Succinylcholine
408
During Phase I these agents worsen muscle paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
Cholinesterase inhibitors
409
Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
Spasmolytic drugs
410
Facilitates GABA presynaptic inhibition
Diazepam
411
GABA agonist in the spinal cord
Baclofen
412
Similar to clonidine and may cause hypotension
Tizanidine
413
DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
Dantrolene
414
Agent used for acute muscle spasm
Cyclobenzaprine
415
Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog)
Drug induced Parkinsonism
416
Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
L-dopa
417
This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)
Carbidopa
418
Clinical response that may fluctuate in tx of Parkinson's dx
On-off-phenomenon
419
Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
Levodopa
420
Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia
Bromocriptine
421
Non ergot agents used as first-line therapy in the initial management of Parkinson's
Pramipexole and ropinirole
422
Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis
Amantadine
423
Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients
Selegiline
424
Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
Entacapone and Tolcapone
425
Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
Benztropine
426
Agent effective in physiologic and essential tremor
Propranolol
427
Agents used in Huntington's Disease
Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic)
428
Agents used in Tourette's dx
Haloperidol or pimozide
429
Chelating agent used in Wilson's disease
Penicillamine
430
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
Older antipsychotic agents, D2 receptors
431
MOA of neuroleptics
Dopamine blockade
432
Side effects occuring in antipsychotics that block dopamine
Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
433
Antipsychotics that reduce positive symptoms only
Older antipsychotics
434
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
Olanzapine, aripiprazole, and sertindole
435
Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
Risperidone
436
Atypical antipsychotic causing high prolactin levels
Risperidone
437
Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes
Olanzapine
438
Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker
Haloperidol
439
Drug used in neuroleptic malignant syndrome
Dantrolene
440
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
Muscarinic blockers
441
Antipsychotic having the strongest autonomic effects
Thioridazine
442
Antipsychotic having the weakest autonomic effects
Haloperidol
443
Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias
Thioridazine
444
Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause fatal agranulocytosis
Clozapine
445
Anti-psychotic not shown to cause tardive dyskinesia
Clozapine
446
Anti-psychotics available in depot preparation
Fluphenazine and haloperidol
447
Reduced seizure threshold
Low-potency typical antipsychotics and clozapine
448
Orthostatic hypotension and QT prolongation
Low potency phenothiazines and ziprasidone
449
Increased risk of developing cataracts
Quetiapine
450
Major route of elimination for Lithium
Kidneys
451
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
Lithium toxicity
452
Drug increases the renal clearance hence decreases levels of lithium
Theophylline
453
Lithium is associated with this congenital defect
Cardiac anomalies and is contraindicated in pregnancy or lactation
454
DOC for bipolar affective disorder
Lithium
455
Concern using lithium
Low therapeutic index
456
SE of lithium
Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
457
Example of three antidepressants that are indicated for obsessive compulsive disorder
Clomipramine, fluoxetine and fluvoxamine
458
Neurotransmitters affected by the action of antidepressants
Norepinephrine and serotonin
459
Usual time needed for full effect of antidepressant therapy
2 to 3 weeks
460
Population group especially sensitive to side effects of antidepressants
Elderly patients
461
All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion
Side-effect profile and prior pt response
462
Well-tolerated and are first-line antidepressants
SSRI's, bupropion, and venlafaxine
463
Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression
Monamine oxidase inhibitors
464
Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)
Hypertensive crisis
465
MAOI should not be administered with SSRI's or potent TCA's due to development of this condition
Serotonin syndrome
466
Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly
Tricyclic antidepressants (TCA)
467
Three C's associated with TCA toxicity
Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)
468
Agents having higher sedation and antimuscarinic effects than other TCA's
Tertiary amines
469
TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects
Amitriptyline
470
TCA used in chronic pain, enuresis, and ADD
Imipramine
471
TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep
Doxepin
472
TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms
Clomipramine
473
Secondary amines that have less sedation and more excitation effect
Nortriptyline, Desipramine
474
Side effects seen with tricyclic antidepressants
Muscarinic blockade (dry mouth, constipation); weak alpha-1 block (orthostatic hypotension); weak hisamine block (sedation)
475
Antidepressant associated with neuroleptic malignant syndrome
Amoxapine
476
Antidepressant associated with seizures and cardiotoxicity
Maprotiline
477
Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure
Venlafaxine
478
Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake
Venlafaxine
479
Antidepressant also used for sleep that causes priapism
Trazodone
480
Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure
Nefazodone
481
Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures
Bupropion
482
Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating
Mirtazapine
483
SE of mirtazapine
Liver toxicity, increased serum cholesterol
484
Except for these agents all SSRI have significant inhibition of CytP450 enzymes
Citalopram and its metabolite escitalopram
485
Side effects frequently seen with SSRIs
CNS stimulation; GI upset
486
Antidepressants with no effect on BP, no sedation
SSRIs
487
SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx
Fluoxetine
488
SSRI indicated for premenstrual dysphoric disorder
Fluoxetine (Sarafem)
489
Some of SSRIs' therapeutic effects beside depression
Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrual dysphoric disorder), OCD
490
SSRI less likely to cause a withdrawal syndrome
Fluoxetine
491
Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
Ascending pathways
492
Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
Presynaptic mu, delta, and kappa receptors
493
Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
Postsynaptic Mu receptors
494
Tolerance to all effects of opioid agonists can develop except
Miosis and constipation
495
All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
Meperidine
496
SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone
Opioid Analgesics
497
Strong opioid agonists
Morphine, methadone, meperidine, and fentanyl
498
Opioids used in anesthesia
Morphine and fentanyl
499
Opioid used in the management of withdrawal states
Methadone
500
Opioid available trans-dermally
Fentanyl
