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Flashcards in PHARM 1 LINERS ALL Deck (500):
1

Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs)

Half-life (T1/2)

2

Relates the amount of drug in the body to the plasma concentration

Volume of distribution (VD)

3

Plasma concentration of a drug at a given time

Cp

4

The ratio of the rate of elimination of a drug to its plasma concentration

Clearance (CL)

5

The elimination of drug that occurs before it reaches the systemic circulation

First pass effect

6

The fraction of unchanged drug that reaches systemic circulation after administration

Bioavailability (F)

7

When the rate of drug input equals the rate of drug elimination

Steady state

8

Different steps of Phase I

Oxidation, reduction, hydrolysis

9

Barbiturates, phenytoin, carbamazepine, and rifampin all do this

Induce CYP450

10

Cimetidine, ketoconazole, isoniazid, and grapefruit all do this

Inhibit CYP450

11

Name 3 Phase II conjugation reactions

Glucuronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation, water conjugation

12

Constant percentage of drug metabolized per unit time

First order kinetics

13

Constant amount of drug metabolized per unit time

Zero order kinetics

14

Target plasma concentration times (volume of distribution divided by bioavailability)

Loading dose (Cp*(Vd/F))

15

Concentration in the plasma times (clearance divided by bioavailability)

Maintenance dose (Cp*(CL/F))

16

Strength of interaction between drug and its receptor

Affinity

17

Selectivity of a drug for its receptor

Specificity

18

Amount of drug necessary to elicit a biologic effect compared with another drug

Potency

19

Ability of drug to produce the maximal biologic effect

Efficacy

20

Ability of a drug to produce maximal response after binding to the receptor

Full agonist

21

Ability to produce less than maximal response after binding to the receptor

Partial agonist

22

Ability to bind reversibly to the same site as the drug and without activating the effector system

Competitive antagonist

23

Ability to bind irreversibly to the active site or bind to a site distinctly separate from the agonist binding site

Noncompetitive antagonist

24

Mechanism of action (MOA) utilizes intracellular receptors

Steroid and hormones

25

Mechanism of action (MOA) utilizes transmembrane receptors that have intrinsic enzymatic activity

Insulin, EGF, TGFbeta, PDGF, ANP

26

Mechanism of action (MOA) utilizes ligand gated ion channels

Acetylcholine, nicotine

27

Dose which produces therapeutic response in 50% of the population

ED50

28

Dose which is toxic in 50% of the population

TD50

29

Dose which is lethal to 50% of the population

LD50

30

Window between therapeutic effect and toxic effect

Therapeutic index

31

Drugs that have a high margin of safety is indicated by

High therapeutic index

32

Drugs that have a narrow margin of safety is indicated by

Low therapeutic index

33

Antidote used for lead poisoning (without encephalopathy)

Dimercaprol, Edetate calcium disodium, or succimer

34

Antidote used for cyanide poisoning

Nitrites, sodium thiosulfate, hydroxocobalamin (cyanokit)

35

Antidote used for anticholinergic poisoning

Physostigmine

36

Antidote used for organophosphate/anticholinesterase poisoning

Atropine, pralidoxime (2-PAM)

37

Antidote used for iron salt toxicity

Deferoxamine

38

Antidote used for acetaminophen (APAP) toxicity

N-acetylcysteine

39

Antidote for severe lead poisoning (with encephalopathy)

Dimercaprol AND CaEDTA (edetate calcium disodium)

40

Antidote for arsenic, mercury, and gold poisoning

Dimercaprol

41

Antidote used in Wilson's disease (copper poisoning)

Penicillamine

42

Antidote used for heparin toxicity

Protamine Sulfate

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 toxicity

Ethanol

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-blocker overdose and hypoglycemia

Glucagon

54

Antidote useful for some drug induced Torsade de pointes

Magnesium sulfate

55

Antidote for hyperkalemia

sodium polystyrene sulfonate (Kayexalate)

56

Method to reduce 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 "Thiamine-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 cardio-toxicity by chelating iron

Dexrazoxane

69

Blows DNA (breaks DNA strands), limiting SE in pulmonary fibrosis

Bleomycin

70

MOPP regimen used in Hodgkin's disease (HD)

Mechlorethamine + oncovorin (vincristine) + procarbazine, and prednisone

71

Regimen used for non-Hodgkin's lymphoma

CHOP (cyclophosphamide, oncovin(vincristine), doxorubicin and prednisone), rituximab (rituxan)

72

Regimen used for breast cancer

CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+

73

Alkylating agent, vesicant that causes tissue damage with extravasation

Mechlorethamine

74

Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis

Cyclophosphamide

75

Prevention of cyclophosphamide induced hemorrhagic cystitis

Hydration and mercaptoethanesulfonate (MESNA)

76

Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation

Vincristine

77

Binds tubulin and prevents the disassembly of microtubules during the M phase of the cell cycle inducing mitotic arrest

Paclitaxel (taxol)

78

Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides

Cisplatin

79

Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression

Carboplatin

80

Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)

L-asparaginase

81

Used for hairy cell leukemia; it stimulates NK cells

Interferon alpha

82

Anti-androgen used for prostate cancer

Flutamide (Eulexin)

83

Anti-estrogen used for estrogen receptor + breast cancer

Tamoxifen

84

Some cell cycle specific anti-cancer drugs

Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)

85

Some cell cycle non-specific drugs

Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea

86

Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonist

Odansetron, granisetron, dolasetron, palonosetron

87

Nitrosoureas with high lipophilicity, used for brain tumors

Carmustine (BCNU) and lomustine (CCNU)

88

Alkylating agent that produces disulfiram-like reaction with ethanol

Procarbazine

89

Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors

Octreotide

90

Somatotropin (GH) analog used in GH deficiency (dwarfism)

Somatrem

91

GHRH analog used as diagnostic agent

Sermorelin

92

GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively

Leuprolide

93

GnRH antagonist with more immediate effects, used for infertility

Ganirelix

94

Hormone inhibiting prolactin release

Dopamine

95

ACTH analog used for diagnosis of patients with corticosteroid abnormality

Cosyntropin

96

Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis

Desmopressin (DDAVP)

97

Agent of choice for the treatment of hypothyroidism

Levothyroxine (T4)

98

An isomer of T3 which may be used in myxedema coma

Liothyronine (T3)

99

Anti-thyroid drugs

Thioamides (methimazole, propylthiouracil), potassium iodide, radioactive iodine (131I)

100

Thioamide agents used in hyperthyroidism

Methimazole and propylthiouracil (PTU)

101

Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and indicated for pregnant women in 1st trimester

Propylthiouracil (PTU)

102

Propylthiouracil (PTU) mechanism of action

Inhibits thyroid peroxidase

103

Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism

Iodide salts (potassium iodide)

104

Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy

Radioactive iodine

105

Used for the symptomatic treatment of thyrotoxicosis by blocking cardiac adverse effects

Beta-blockers such as propranolol and esmolol

106

3 zones of adrenal cortex and their products

Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)

107

Pneumonic for 3 zones of adrenal cortex

GFR

108

Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)

Glucocorticoids

109

Short acting GC's

Cortisone and hydrocortisone (equivalent to cortisol)

110

Intermediate acting GC's

Prednisone, methylprednisolone, prednisolone, oaramethasone, fluprednisone and triamcinolone

111

Long acting GC's

Betamethasone, dexamethasone, and paramethasone

112

Mineralocorticoids

Fludrocortisone and deoxycorticosterone

113

Some side effects of corticosteroids

Hyperglycemia, Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis

114

Period of time of therapy after which GC therapy will need to be tapered

5-7 days

115

Used for Cushing's syndrome (increased corticosteroid) and sometimes for adrenal function test

Metyrapone

116

Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis

Aminoglutethimide

117

Antifungal agent used for inhibition of all gonadal and adrenal steroids

Ketoconazole

118

Antiprogestin used as potent antagonist of GC receptor

Mifepristone

119

Diuretic used to antagonize aldosterone receptors

Spironolactone

120

Common SE of spironolactone

Gynecomastia and hyperkalemia

121

Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss

Estrogen

122

Antiestrogen drugs used for fertility and breast cancer respectively

Clomiphene and tamoxifen

123

Common SE of tamoxifen and raloxifene

Hot flashes

124

Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and currently being tested for treatment of breast cancer (Stars study)

Raloxifene

125

Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy

Diethylstilbestrol (DES)

126

Estrogen mostly used in oral contraceptives (OC)

Ethinyl estradiol and mestranol

127

Anti-progesterone used as abortifacient

Mifepristone (RU-486)

128

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)

129

Oral contraceptive available in a transdermal patch

Ortho-Evra

130

Converted to more active form DHT by 5 alpha-reductase

Testosterone

131

5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness

Finasteride (Proscar and Propecia respectively)

132

Anabolic steroid that has potential for abuse

Nandrolone and stanozolol

133

Anti-androgen used for hirsutism in females

Cyproterone acetate

134

Alpha cells in the pancreas produce

Produce glucagon

135

Beta cells in the pancreas produce

Produce insulin

136

Beta cells are found

Islets of Langerhans

137

Delta cells in the pancreas produce

Produce Somatostatin

138

Product of proinsulin cleavage used to assess insulin production

C-peptide

139

Endogenous insulin

Normal C-peptide

140

Very rapid acting insulin, having fastest onset and shortest duration of action

Lispro (Humalog)/Apidra (glulisine)

141

Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia

Regular (Humulin R)

142

Long acting insulin

NPH insulin

143

Ultra long acting insulin, has over a day duration of action

Glargine (Lantus)

144

Major side effect of insulin

Hypoglycemia

145

Important in synthesis of glucose to glycogen in the liver

GLUT 2

146

Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation

GLUT 4

147

Examples of alpha-glucosidase inhibitors (AGI)

Acarbose, miglitol

148

MOA of AGI's

Act on intestine, delay absorption of glucose

149

SE of AGI's

Flatulence (do not use beano to tx), diarrhea, abdominal cramps

150

Alpha-glucosidase inhibitor associated with elevation of LFT's

Acarbose

151

Amino acid derivative for treatment of Type II diabetes

Nateglinide

152

MOA of nateglinide

Stimulates rapid and transient release of insulin through closure of the ATP-sensitive K+ channel

153

Biguanide

Metformin

154

Drugs available in combination with metformin

Acroplus Met progutazone and metformin, Janumet and Janumet XR Sitagliptin and Metformin, Glyburide, glipizide, and rosiglitazone

155

MOA of metformin

Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity

156

Most important potential SE of metformin

Lactic acidosis

157

Meglitinide

Repaglinide

158

MOA of repaglinide

Insulin release from pancreas; faster and shorter acting than sulfonylurea

159

First generation sulfonylurea

Chlorpropamide, tolbutamide, tolazamide, etc.

160

Second generation sulfonylurea

Glyburide, glipizide, glimepiride, etc.

161

MOA of both generations

Insulin release from pancreas by modifying K+ channels

162

Common SE of sulfonylureas, repaglinide, and nateglinide

Hypoglycemia

163

Sulfonylurea NOT recommended for elderly because of very long half life

Chlorpropamide

164

Thiazolidinediones

Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)

165

Reason troglitazone was withdrawn from market

Hepatic toxicity

166

MOA of thiazolindinediones

Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism

167

SE of Thiazolindinediones

Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism; if used over one year, bladder Cancer; with CHF, may cause new or worsening CHF

168

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

169

Available bisphosphonates

Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid

170

MOA of Bisphosphonates

Inhibits osteoclast bone resorption

171

Uses of bisphosphonates

Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy

172

Major SE of bisphosphonates

Chemical esophagitis

173

Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia

Etidronate

174

Used for prevention of postmenopausal osteoporosis in women

Calcium reguators Bisphosphonates: alendronate, risedronate, ibandronate, Estrogen (HRT-Hormone replacement therapy)

175

Increase bone density, also being tested for breast CA tx.

Raloxifene (SERM-selective estrogen receptor modulator)

176

Used intranasally and decreases bone resorption

Calcitonin (salmon prep)

177

Used especially in postmenopausal women, dosage should be 1500 mg

Calcium

178

Vitamin given with calcium to ensure proper absorption

Vitamin D

179

Disease caused by excess ergot alkaloids

St. Anthony's Fire

180

A class of endogenous substances that include histamine, serotonin, prostaglandins, and vasoactive peptides that work in autocrine or paracrine manner

Autacoids

181

Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea

Zollinger-Ellison Syndrome

182

Drug that causes contraction of the uterus

Oxytocin

183

Distribution of histamine receptors H1, H2, and H3

Smooth muscle and mast cells; stomach, heart, and mast cells; nerve endings, CNS respectively

184

1st generation antihistamine that is highly sedating

Diphendydramine

185

1st generation antihistamine that is least sedating

Chlorpheniramine

186

2nd generation antihistamines

Fexofenadine, loratadine, and cetirizine

187

Generation of antihistamine that has the most CNS effects

First generation due to being more lipid-soluble

188

Major indication for H1 receptor antagonist

Use in IgE mediated allergic reaction (allergic rhinitis, urticaria)

189

Antihistamine that is indicated for allergies, motion sickness, and insomnia

Diphenhydramine

190

H1 antagonist used in motion sickness

Dimenhydrinate and other 1st generation

191

Most common side effect of 1st generation antihistamines

Sedation, anticholinergic

192

H2 blocker that causes the most interactions with other drugs

Cimetidine

193

Clinical use for H2 blockers

Acid reflux disease, duodenal ulcer and peptic ulcer disease

194

Receptors for serotonin (5HT-1) are located

Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance

195

5HT-1D/1B agonist used for migraine headaches

Sumatriptan, naratriptan, and rizatriptan

196

Triptan available in parenteral and nasal formulation

Sumatriptan

197

H1 blocker that is also a serotonin antagonist

Cyproheptadine

198

5HT2 antagonist mediate synaptic excitation in the CNS and smooth muscle contraction

Ketanserin, cyproheptadine, and ergot alkaloids (partial agonist of alpha and serotonin receptors)

199

Agents for reduction of postpartum bleeding

Oxytocin and ergonovine

200

Agents used in treatment of carcinoid tumor

Cyproheptadine

201

emesis

Ondansetron, granisetron, dolasetron and palonosetron

202

5ht-3 antagonist that has been MOST associated with QRS and QTc prolongation and should not be used in patients with heart disease

Dolasetron

203

Drug used in ergot alkaloids overdose, ischemia and gangrene

Nitroprusside

204

Reason ergot alkaloids are contraindicated in pregnancy

Uterine contractions

205

SE of ergot alkaloids

Hallucinations resembling psychosis

206

Ergot alkaloid used as an illicit drug

LSD

207

Dopamine agonist used in hyperprolactinemia

Bromocriptine

208

Peptide causing increased capillary permeability and edema

Bradykinin and histamine

209

Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema

Bradykinin

210

Drug causing depletion of substance P (vasodilator)

Capsaicin

211

Prostaglandins that cause abortions

Prostaglandin E1 (misoprostol), PGE2, and PGF2alpha

212

Difference between COX 1 and COX 2

COX 1 is constitutive while COX 2 may be induced during inflammation, although COX 2 is constitutive in some tissues

213

Drug that selectively inhibits COX 2

Celecoxib

214

Inhibitor of lipoxygenase

Zileuton

215

Major SE of zileuton

Liver toxicity

216

Inhibitor of leukotrienes (LTD4) receptors and used in asthma

Zafirlukast and montelukast

217

Used in pediatrics to maintain patency of ductus arteriosis

PGE1 (Alprostadil)

218

Approved for use in severe pulmonary HTN

PGI2 (epoprostenol)

219

Prostaglandin used as 2nd line treatment of erectile dysfunction

PGE1 (Alprostadil)

220

Irreversible, nonselective COX inhibitor

Aspirin (or other salicylates)

221

Class of drugs that reversibly inhibit COX

NSAIDS

222

Primary endogenous substrate for Nitric Oxidase Synthase

Arginine

223

MOA and effect of nitric oxide

Stimulates cGMP which leads to vascular smooth muscle relaxation

224

Long acting beta 2 agonist used in asthma

Salmeterol

225

Muscarinic antagonist used in COPD

Ipratropium, tiotropium

226

MOA action of cromolyn

Blocks opening of Cl channels to prevent mast cell degranulation

227

Enzyme which theophylline inhibits

Phosphodiesterase

228

Methylxanthine derivative used as a remedy for intermittent claudication

Pentoxifylline

229

Antidote for severe CV toxicity of theophylline

Beta blockers

230

MOA of corticosteroids

Induce lipocortins to

231

SE of long term (>5 days) corticosteroid therapy and remedy

Adrenal suppression and weaning slowly, respectively

232

MOA of fluoroquinolones

Inhibit DNA gyrase (topoisomerase II) and topoisomerase IV

233

MOA of penicillin

Block cell wall synthesis by inhibiting transpeptidase and block peptidoglycan cross-linkage

234

Drug used for MRSA

Vancomycin

235

Vancomycin MOA

Binds D-Ala-D-Ala on murein monomers and prevent polymerization of the murein monomers

236

Type of resistance found with vancomycin

Point mutation

237

Meningitis prophylaxis in exposed patients

Rifampin

238

Technique used to diagnose perianal itching, and the drug used to treat it

Scotch tape technique

239

Two toxicities of aminoglycosides

nephro and ototoxicity

240

Drug of choice for Legionnaires' disease

Azithromycin (or macrolides)

241

MOA of sulfonamides

Inhibit dihydropteroate synthase

242

Penicillins active against penicillinase secreting bacteria

Methicillin, nafcillin, and dicloxacillin

243

Cheap wide spectrum antibiotic DOC of otitis media

Amoxicillin

244

Class of antibiotics that have 10% cross sensitivity with penicillins

Cephalosporins

245

PCN active against pseudomonas

Carbenicillin, piperacillin and ticarcillin

246

Antibiotic causing red-man syndrome, and prevention

Vancomycin, can be prevented by infusion

247

Drug causes teeth discoloration

Tetracycline

248

Mechanism of action of tetracycline

Decreases protein synthesis by binding to 30S ribosome and prevent binding of tRNA to A site

249

Drug that causes gray baby syndrome and aplastic anemia

Chloramphenicol

250

Drug notorious for causing pseudomembranous colitis

Clindamycin

251

Drug of choice for tx of pseudomembranous colitis

Metronidazole

252

Treatment of resistant pseudomembranous colitis

ORAL vancomycin

253

Anemia caused by trimethoprim

Megaloblastic anemia

254

Reason fluoroquinolones are contraindicated in children and pregnancy

Cartilage damage

255

DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas

Metronidazole

256

Treatment for TB patients (think RIPE)

Rifampin, Isoniazid, Pyrazinamide, and Ethambutol

257

Metronidazole SE if given with alcohol

Disulfiram-like reaction

258

Common side effect of Rifampin

Orange urine discoloration

259

MOA of nystatin

Bind ergosterol in fungal cell membrane

260

Neurotoxicity with isoniazid (INH) prevented by

Administration of Vit. B6 (pyridoxine)

261

Toxicity of amphotericin

Nephrotoxicity

262

SE seen only in men with administration of ketoconazole

Gynecomastia

263

Topical DOC in impetigo

Topical mupirocin (Bactroban)

264

DOC for influenza A and B

Oseltamivir or Zanamivir

265

DOC for RSV

Ribavirin

266

DOC for CMV retinitis

Ganciclovir

267

SE for ganciclovir

Myelosuppression

268

Anti-viral agents associated with Stephen Johnson syndrome

Nevirapine, amprenavir

269

HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism

Protease inhibitors

270

Antivirals that are teratogens

Delavirdine, efavirenz, and ribavirin

271

Antivirals associated with neutropenia

Ganciclovir, zidovudine, saquinavir, interferon

272

HIV med used to reduce transmission during birth

AZT (zidovudine)

273

Drug used for African sleeping sickness

Suramin

274

Drug used in Chagas disease

Nifurtimox

275

Cephalosporins able to cross the BBB

Cefixime (2nd) and 3rd generation

276

DOC for N. gonorrhea

Ceftriaxone

277

Cephalosporins that cause kernicterus in neonates

Ceftriaxone or cefuroxime

278

SE of INH

Peripheral neuritis and hepatitis

279

Aminoglycoside that is least ototoxic

Streptomycin

280

Drug used in exoerythrocytic cycle of malaria

Primaquine

281

Oral antibiotic of choice for moderate inflammatory acne

Minocycline

282

Drug of choice for leprosy

Dapsone

283

DOC for herpes and its MOA

Acyclovir; activated by viral thymidine kinase, results in inhibition of viral DNA replication

284

Anti-bacterials that cause hemolysis in G6PD-deficient patients

Sulfonamides

285

Mechanism of action of macrolides (erythromycin, clarithromycin)

Inhibit protein synthesis by binding to domain V of 23S rRNA of 50S ribosome subunit

286

Antibacterials for optimal treatment of acute uncomplicated cystitis

Nitrofurantoin, trimethoprim-sulfamethoxazole, fosfomycin

287

Antibacterials for optimal treatment of acute pyelonephritis

Fluoroquinolones (ciprofloxacin, levofloxacin), trimethoprim-sulfamethoxazole

288

Lactam that can be used in PCN allergic patients

Aztreonam

289

SE of imipenem

Seizures

290

Anti-viral with a dose limiting toxicity of pancreatitis

Didanosine (ddI)

291

Common side effect of hypnotic agents

Sedation

292

Occurs when sedative hypnotics are used chronically or at high doses

Tolerance

293

The most common type of drug interaction of sedative hypnotics with other depressant medications

Additive CNS depression

294

Major effect of benzodiazepines on sleep at high doses

REM is decreased

295

Neurologic SE of benzodiazepines

Anterograde amnesia

296

Reason benzos are used cautiously in pregnancy

Ability to cross the placenta

297

Main route of metabolism for benzodiazepines

Hepatic

298

Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)

Lorazepam, oxazepam, and temazepam

299

MOA for benzodiazepines

increase the FREQUENCY of GABA-mediated chloride ion channel opening

300

Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)

Flumazenil

301

Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin

Diazepam

302

Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia

Clonazepam

303

Benzodiazepines that are the most effective in the treatment of panic disorder

Alprazolam and Clonazepam

304

Benzodiazepine that is used for anesthesia

Midazolam

305

DOC for status epilepticus

Diazepam

306

Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs

Chlordiazepoxide and Diazepam

307

Agents having active metabolites, long half lives, and a high incidence of adverse effects

Diazepam, Flurazepam, chlordiazepoxide, and clorazepate

308

Barbiturates may precipitate this hematologic condition

Acute intermittent porphyria

309

Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property

Liver enzyme INDUCTION

310

Barbiturates MOA

Increase the DURATION of GABA-mediated chloride ion channels

311

Barbiturate used for the induction of anesthesia

Thiopental

312

Important drug interaction with chloral hydrate

May displace coumadin from plasma proteins

313

Site of action for zaleplon and zolpidem

Benzodiazepine receptor BZ1 (although are not considered benzodiazepines)

314

Good hypnotic activity with less CNS SE than most benzodiazepines

Zolpidem, zaleplon

315

Agent that is a partial agonist for the 5-HT1A receptor

Buspirone

316

Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety

Buspirone

317

Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)

Ethanol

318

Agent with zero-order kinetics

Ethanol, theophylline, tolbutamide, warfarin, aspirin, phenytoin

319

Rate limiting step of alcohol metabolism

Aldehyde dehydrogenase

320

System that increases in activity with chronic exposure and may contribute to tolerance

Microsomal ethanol oxidizing system (MEOS)

321

Enzyme that metabolizes acetaldehyde to acetate

Aldehyde dehydrogenase

322

Agents that inhibit aldehyde dehydrogenase

Disulfiram, metronidazole, certain sulfonylureas and cephalosporins

323

Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension

Disulfiram

324

The most common neurologic abnormality in chronic alcoholics

Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)

325

Agent that is teratogen and causes a fetal syndrome

Alcohol

326

Agent that competes for alcohol dehydrogenase in the case of methanol overdose

Ethanol

327

Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure

Fomepizole

328

Most frequent route of metabolism

Hepatic enzymes

329

Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine

Sodium blockade

330

MOA for benzodiazepines and barbiturates

GABA-related targets

331

MOA for Ethosuximide

Calcium channels

332

MOA for Valproic acid at high doses

Affect calcium, potassium, and sodium channels

333

Drugs of choice for generalized tonic-clonic and partial seizures

Valproic acid, Phenytoin and Carbamazepine

334

DOC for febrile seizures

Phenobarbital

335

Drugs of choice for absence seizures

Ethosuximide and valproic acid

336

Drug of choice for myoclonic seizures

Valproic acid

337

Drugs of choice for status epilepticus

IV diazepam (or lorazapam) followed by phenytoin

338

Drugs that can be used for infantile spasms

Corticosteroids

339

Anti-seizure drugs used also for bipolar affective disorder (BAD)

Valproic acid, carbamazepine, phenytoin and gabapentin

340

Anti-seizure drugs used also for Trigeminal neuralgia

Carbamazepine

341

Anti-seizure drugs used also for pain of neuropathic orgin

Gabapentin

342

Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism

Phenytoin

343

SE of phenytoin

Gingival hyperplasia, nystagmus, diplopia and ataxia

344

Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida

Carbamazepine

345

Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress

Valproic acid

346

Laboratory value required to be monitored for patients on valproic acid

Serum ammonia and LFT's

347

SE for Lamotrigine

Stevens-Johnson syndrome

348

SE for Felbamate

Aplastic anemia and acute hepatic failure

349

Anti-seizure medication also used in the prevention of migraines

Valproic acid

350

Carbamazepine may cause

Agranulocytosis

351

Anti-seizure drugs used as alternative drugs for mood stabilization

Carbamazepine, gabapentin, lamotrigine, and valproic acid

352

MOA of general anesthetics

Unclear, thought to increase the threshold for firing of CNS neurons

353

Inhaled anesthetic with a low blood/gas partition coefficient

Nitrous oxide

354

Inversely related to potency of anesthetics

Minimum alveolar anesthetic concentration (MAC)

355

Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents

Halothane and methoxyflurane

356

Most inhaled anesthetics SE

Decrease arterial blood pressure

357

Inhaled anesthetics are myocardial depressants

Enflurane and halothane

358

Inhaled anesthetic causes peripheral vasodilation

Isoflurane

359

Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis

Halothane

360

Inhaled anesthetics, less likely to lower blood pressure than other agents, and has the smallest effect on respiration

Nitrous oxide

361

Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency

Methoxyflurane

362

Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia

Nitrous oxide

363

Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm

Desflurane

364

DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics

Dantrolene

365

IV barbiturate used as a pre-op anesthetic

Thiopental

366

Benzodiazepine used adjunctively in anesthesia

Midazolam

367

Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose

Flumazenil

368

This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery

Ketamine

369

Opioid associated with awareness during surgery and post-operative recall, but still used for high-risk cardiovascular surgeries

Fentanyl

370

State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide

Neuroleptanesthesia

371

Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension

Propofol

372

MOA of local anesthetics (LA's)

Block voltage-dependent sodium channels

373

This may enhance activity of local anesthetics

Hyperkalemia

374

This may antagonize activity of local anesthetics

Hypercalcemia

375

Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity

Vasodilation

376

Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery

Cocaine

377

Longer acting local anesthetics which are less dependent on vasoconstrictors

Tetracaine and bupivacaine

378

These LA's have surface activity

Cocaine and benzocaine

379

Most important toxic effects of most local anesthetics

CNS toxicity

380

Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction

Cocaine

381

LA causing methemoglobinemia

Prilocaine

382

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

383

These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)

Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic

384

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

385

Agent with long duration of action and is most likely to cause histamine release

Tubocurarine

386

Non-depolarizing antagonist has short duration

Mivacurium

387

Agent can block muscarinic receptors

Pancuronium

388

Agent undergoing Hofmann elimination (breaking down spontaneously)

Atracurium

389

One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur

Succinylcholine

390

During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine

Cholinesterase inhibitors

391

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

392

Facilitates GABA presynaptic inhibition

Diazepam

393

GABA agonist in the spinal cord

Baclofen

394

Similar to clonidine and may cause hypotension

Tizanidine

395

DOC for malignant hyperthermia by acting on the sarcoplasmic reticulum or skeletal muscle

Dantrolene

396

Agent used for acute muscle spasm

Cyclobenzaprine

397

Antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible

Drug induced Parkinsonism

398

Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB

L-dopa

399

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

400

Clinical response that may fluctuate in tx of Parkinson's dx

On-off-phenomenon

401

Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma

Levodopa

402

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

403

Non ergot agents used as first-line therapy in the initial management of Parkinson's

Pramipexole and ropinirole

404

Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis

Amantadine

405

Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt's

Selegiline

406

Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)

Entacapone and Tolcapone

407

Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects

Benztropine

408

Agent effective in physiologic and essential tremor

Propranolol

409

Agents used in Huntington's Disease

Tetrabenazine (amine depleting drug), Haloperidol (antipsychotic)

410

Agents used in Tourette's dx

Haloperidol or pimozide

411

Chelating agent used in Wilson's disease

Penicillamine

412

Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor

Older antipsychotic agents, D2 receptors

413

Side effects occuring in antipsychotics that block dopamine

EPS, hyperprolactinemia, amennorrhea, galactorrhea, neuroleptic malignant syndrome

414

Antipsychotics that reduce positive symptoms only

Older antipsychotics

415

Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation

Olanzapine and aripiprazole

416

Atypical antipsychotic causing high prolactin levels

Risperidone

417

Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes

Olanzapine

418

Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker

Haloperidol

419

Drug used in neuroleptic malignant syndrome

Dantrolene

420

Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)

Muscarinic blockers

421

Antipsychotics having the strongest autonomic effects

Chlorpromazine or Thioridazine

422

Antipsychotic having the weakest autonomic effects

Haloperidol

423

Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias

Thioridazine

424

Agent with greater affinity to 5HT2A receptor; reserved for refractory schizophrenia, and can cause weight gain and agranulocytosis

Clozapine

425

Anti-psychotics shown not to cause tardive dyskinesia

Clozapine and quetiapine

426

Anti-psychotics available in depot preparation

Fluphenazine and haloperidol

427

Reduced seizure threshold

Low-potency typical antipsychotics and clozapine

428

Orthostatic hypotension and QT prolongation

Low potency and risperidone

429

Increased risk of developing cataracts

Quetiapine

430

Major route of elimination for Lithium

Kidneys

431

Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop

Lithium toxicity, lithium-induced nephrogenic diabetes insipidus

432

Drug increases the renal clearance hence decreases levels of lithium

Theophylline

433

Lithium is associated with this congenital defect

Cardiac anomalies; contraindic: pregnancy&lactation

434

DOC for bipolar affective disorder

Lithium

435

SE of lithium

Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus

436

Example of three antidepressants that are indicated for obsessive compulsive disorder

Clomipramine, fluoxetine and fluvoxamine

437

Neurotransmitters affected by the action of antidepressants

Norepinephrine and serotonin

438

Usual time needed for full effect of antidepressant therapy

2 to 3 weeks

439

Population group especially sensitive to side effects of antidepressants

Elderly patients

440

All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion

Side-effect profile and prior pt response

441

Well-tolerated and are first-line antidepressants

SSRI's, bupropion, and venlafaxine

442

Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression

Monamine oxidase inhibitors

443

Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)

Hypertensive crisis

444

MAOI should not be administered with SSRI's or potent TCA's due to development of this condition

Serotonin syndrome

445

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)

446

Three C's associated with TCA toxicity

Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)

447

Agents having higher sedation and antimuscarinic effects than other TCA's

Tertiary amines

448

TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects

Amitriptyline

449

TCA used in chronic pain, enuresis, and OCD

Imipramine

450

TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep

Doxepin

451

TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms

Clomipramine

452

Secondary amines that have less sedation and more excitation effect

Nortriptyline, Desipramine

453

Antidepressant associated with neuroleptic malignant syndrome

Amoxapine

454

Antidepressant associated with seizures and cardiotoxicity

Maprotiline

455

Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure

Venlafaxine

456

Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake

Venlafaxine

457

Antidepressant also used for sleep that causes priapism

Trazodone

458

Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure

Nefazodone

459

Unicyclic antidepressant least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures

Bupropion

460

Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating

Mirtazapine

461

SE of mirtazapine

Liver toxicity, increased serum cholesterol

462

Except for these agents all SSRI have significant inhibition of CytP450 enzymes

Citalopram and its metabolite escitalopram

463

SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx

Fluoxetine

464

SSRI indicated for premenstrual dysphoric disorder

Fluoxetine (Sarafem)

465

Some of SSRIs' therapeutic effects beside depression

Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrual dysphoric disorder), OCD

466

SSRI's less likely to cause a withdrawal syndrome

Fluoxetine

467

Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons

Ascending pathways

468

Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release and pain transmission

Presynaptic mu, delta, and kappa receptors

469

Activation of these receptors open K+ ion channels to cause membrane hyperpolarization

Postsynaptic Mu receptors

470

Tolerance to all effects of opioid agonists can develop except

Miosis, convulsions and constipation

471

All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction

Meperidine

472

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

473

Strong opioid agonists

Morphine, methadone, meperidine, and fentanyl

474

Opioids used in anesthesia

Morphine and fentanyl

475

Opioid used in the management of withdrawal states

Methadone

476

Opioid available trans-dermally

Fentanyl

477

Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema

Morphine

478

Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome

Meperidine

479

Moderate opioid agonists

Codeine, hydrocodone, and oxycodone

480

Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures

Propoxyphene

481

Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal

Buprenorphine

482

Opioid antagonist that is given IV and had short DOA

Naloxone

483

Opioid antagonist that is given orally in alcohol dependency programs

Naltrexone

484

These agents are used as antitussive

Dextromethorphan, Codeine

485

These agents are used as antidiarrheal

Diphenoxylate, Loperamide

486

Inhalant anesthetics

NO, chloroform, and diethyl ether

487

Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation

Fluorocarbons and Industrial solvents

488

Cause dizziness, tachycardia, hypotension, and flushing

Organic nitrites

489

Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression

Steroids

490

Readily detected markers that may assist in diagnosis of the cause of a drug overdose include

Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses

491

Most commonly abused in health care professionals

Heroin, morphine, oxycodone, meperidine and fentanyl

492

This route is associated with rapid tolerance and psychologic dependence

IV administration

493

Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome

Abstinence syndrome

494

Treatment for opioid addiction

Methadone, followed by slow dose reduction

495

This agent may cause more severe, rapid and intense symptoms (abstinence syndrome) to a recovering addict

Naloxone

496

Sedative-Hypnotics action

Reduce inhibition, suppress anxiety, and produce relaxation

497

Additive effects when Sedative-Hypnotics used in combination with these agents

CNS depressants

498

Common mechanism by which overdose result in death

Depression of medullary and cardiovascular centers

499

Date rape drug

Flunitrazepam (rohypnol)

500

The most important sign of withdrawal syndrome

Excessive CNS stimulation (seizures)