Материал: 2016_Kaplan_USMLE_Step_1_Lecture_Notes_Pharmacology

USMLE Step I λ Pharmacology

DMARDs, 235–236, 246 drug lists, 245–246

eicosanoid pharmacology and, 229, 229–234 glucocorticoids, 239–240, 246

histamine and antihistamines, 221–222, 245 in gastrointestinal dysfunction, 223–226, 245 in gout, 237–238, 246

in migraine headaches, 228

in rheumatoid arthritis, 235–236 NSAIDs, 231–233, 245

serotonergic systems and, 227–228, 245 Infliximab

characteristics/uses, 235 clinical uses, 310

Infusion rate, 15–16

effect on plasma level, 16 equation, 16

Inhalants, as drugs of abuse, 164 Inhaled anesthetics, 153, 153–154, 167

minimal alveolar anesthetic concentration, 154–155 properties, 153

rates of onset/recovery, 154 Inotropes, 98, 98–99 Insecticides, 48

activation, 47 Insulin release, 273 Insulins

characteristics/uses, 273 forms, 273

Integrase inhibitors, 203 Interferon-α, clinical uses of, 310 Interferon-β, clinical uses of, 310 Interferon-γ, clinical uses of, 310 Interleukin-11, clinical uses of, 303 Interventions. See Antidotes

Intracellular receptors, signalling systems and, 23 Intraocular pressure (IOP), increase in, 65 Intravenous anesthetics, 154, 167

Intrinsic sympathomimetic activity (ISA), beta blockers and, 62 Inulin clearance, 14

Iodide, 286

Ion channels, membrane receptors coupled to, 23 Ionization, 4–5

renal clearance of drugs and, 5 Ipratropium, characteristics/uses, 50, 242 Irido-corneal angle, 65

Iron poisoning, 316 antidote for, 317

Irreversible AChE inhibitors, 46 Irreversibly-acting cholinomimetics, 48 Isoniazid (INH), 11, 191

prophylaxis, 191

Isoproterenol, as beta adrenergic agonist, 59 Isosorbide/Isosorbide dinitrate

as antianginal, 111 for heart failure, 97

Itraconazole, characteristics/uses, 196

334

J

Janus kinases (JAKs), 26

K

K+. See Potassium (K+) entries Kanamycin, 191

Ketamine

as drug of abuse, 164 characteristics/uses, 154

Ketoconazole, 279 characteristics/uses, 196

Ketorolac, 232 K+-sparing agents, 87, 121

L

Labetalol, 63 Lactic acid, 4 Lactulose, 4

“LAME”organisms, not covered by cephalosporins, 182 Lamivudine

in HIV prophylaxis, 203 mechanism of action, 200 side effects, 202

Lamotrigine, characteristics/uses, 151

L-aromatic amino acid decarboxylase (DOPA decarboxylase), 56 Latanoprost, 230

L-DOPA. See Levodopa (L-DOPA) Lead poisoning, 317

antidote for, 317

Leflunomide, characteristics/uses, 235 Leishmaniasis, stibogluconate for, 207 Leukotrienes (LTs), characteristics/uses, 230 Leuprolide, 282, 287

Levodopa (L-DOPA)

as antiparkinsonian drug, 144

as antiparkinsonian drug, 142, 142f, 144 blood-brain barrier and, 8

inhibitors of metabolism, 145 Levofloxacin, characteristics/uses, 190 Lidocaine

as local anesthetic, 155

as Na+ channel blocker, 107 characteristics/uses, 107 first-pass effect, 7

Linezolid

characteristics/uses, 187–188 mechanism of action, 179, 185 Lipid-soluble drugs, redistribution of, 9

Lisinopril, 92

Lispro, 273 Lithium

characteristics/uses, 140

loop diuretics interaction with, 85 Loading dose (LD)

effect, 15–16, 16 equation, 16

Local anesthetics, 155, 167 mode of action, 155

nonmicrosomal metabolism, 11 Log-kill hypothesis, 299 Lomustine, cell-cycle specificity, 299

Long QT syndrome, treatment of, 108 Loop diuretics, 85, 85–86

Loop of Henle, 84

Loperamide, 161

Lopinavir, in HIV prophylaxis, 203 Loratadine, properties of, 222 Lorazepam

characteristics/uses, 134

seizure states/drugs of choice, 149 Losartan, 92

Low-molecular weight heparin (LMW), 260 Lugol’s solution, 286

Lungs, muscarinic receptor activation and, 46 Luteinizing hormone (LH), 287

M

Macrolides characteristics/uses, 187

cytochrome P450 isozymes and, 10 drug list, 209

for community-acquired pneumonia, 187 mechanism of action, 179, 185 mechanism of resistance, 179

Magnesium, as antiarrhythmic, 109 Maintenance dose (MD), 14, 16 Malaria, drugs for treating, 207–208

antiprotozoal agents, 207–208 chloroquine-resistant, 208 chloroquine-sensitive, 207

Malathion, 46, 48

Malignant hyperthermia, 157

Maraviroc, mechanism of action, 200, 204 Marijuana, as drug of abuse, 164

M blockers, 49–50 atropine, 49–50, 315

as antidote, 317 characteristics/uses, 50 common toxic syndromes, 315 drug lists, 71

in treating asthma, 242 MDEA, as drug of abuse, 164

MDMA (ecstasy), as drug of abuse, 164 Meclizine

as antiemetic, 225 properties, 222

Medroxyprogesterone, 281 Mefloquine, 208

Melatonin, characteristics/uses, 319 Membrane, drug transport modes across, 5

Membrane receptors, coupled to ion channels, 23 Menotropins, 287

Index

Meperidine

as M blocker, 52 characteristics/uses, 160

Mepivacaine, as local anesthetic, 155 6-Mercaptopurine

cell-cycle specificity, 299 characteristics/uses, 301

drug interaction with allopurinol, 237 Mercury poisoning, 316

antidote for, 317 Meropenem

characteristics/uses, 183 mechanism of action, 183

Mesolimbic-mesocortical tracts, 143 Mestranol, 279, 282

Metabolism, in pharmacokinetics, 3 alcohols, 137

Metaproterenol, in treating asthma, 242 Metformin

characteristics/uses, 275 modes of action, 275

Methacholine, cholinergic properties, 47 Methadone

as drug of abuse, 164 characteristics/uses, 160

Methicillin, 181

Methimazole, 286 placental barrier and, 8

Methotrexate

cell-cycle specificity, 299 characteristics/uses, 235, 301 toxicity, 302

Methyldopa

as α2 adrenergic agonist, 58, 94 characteristics/uses, 94

Methylnaltrexone, characteristics/uses, 160 Methylphenidate, 141

Metoclopramide, 225 Metoprolol

characteristics, 62 for heart failure, 97

Metronidazole, 138

as antiprotozoal agent, 207 characteristics/uses, 190

Metyrapone, 279

Mexiletine, as Na+ channel blocker, 107 Miconazole, 196

Microsomal metabolism, 10 Midazolam

characteristics/uses, 134, 154 grapefruit juice and, 10

Mifepristone, 230, 279, 281

Migraine headaches, drugs for treating, 63, 228 Milrinone, for heart failure, 99

Minimal alveolar anesthetic concentration (MAC), 154–155 Minocycline, 186

Minoxidil, as direct-acting vasodilator, 94 Miosis, 43

335

USMLE Step I λ Pharmacology

Mirtazapine, 140

as alpha blocker, 63 Misoprostol, 224, 230 Monoamine oxidase (MAO), 56

forms, 61

inhibitors, characteristics/uses, 140 metabolism, 11

Monoclonal antibodies, clinical uses of, 310 Montelukast, 243

Morphine

as drug of abuse, 164 characteristics/uses, 159 contraindications/cautions, 159 duality of action, 225 metabolism, 11

Motion sickness, drugs for treating, 50, 222 Muromonab, clinical uses of, 310 Muscarinic agonists, 47, 72

Muscarinic antagonists, 44, 225 Muscarinic receptors, 39

activators, 46, 47–49 mechanism of action, 46

Muscarinic stimulation, 44

Myasthenia, drugs for treating, acetylcholinesterase inhibitors, 48

Mycobacterium avium-intracellulare (MAC), 191 Mycobacterium tuberculosis, 191 Mycophenolate, 309

Mydriasis, 43

N

Na+. See Sodium (Na+) entries N-acetylcysteine, 233 Nafarelin, 287

Nafcillin, 181

Nalbuphine, characteristics/uses, 160 Naloxone

as antidote, 317 characteristics/uses, 160

in reversing respiratory depression, 164 Naltrexone, characteristics/uses, 160 Naproxen, 232

Natural medicinals, 318–319 Nausea, drugs for treating, 222, 225 Nedocromil, in treating asthma, 242 Nelfinavir, mechanism of action, 200 Neostigmine, characteristics/uses, 48

Nephrogenic diabetes insipidus, thiazides for, 86 Nephrolithiasis, thiazides for, 86 Nephrotoxicity, 138

Nesiritide, for heart failure, 99 Neuroeffector junctions

adrenergic, 55, 55–58 cholinergic, 45, 45–47

Neuromuscular blocking agents, drug list, 167 Neurotransmitters

autonomic nervous system, 39 drugs of abuse and, 165–166

336

Nevirapine, mechanism of action, 200 Niacin, as antihyperlipidemic, 118, 119 Nicotinic acid, 121

as antihyperlipidemic, 117

Nicotinic receptor antagonists, 50–51, 156 ganglion blocking agents, 50–51

neuromuscular blocking drugs. See CNS pharmacology Nicotinic receptors, 23, 39

activation, 47, 156 mechanism of action, 46 subunits, 156

Nifedipine, as calcium-channel blocker, 93 Nifurtimox, as antiprotozoal agent, 207 Nigrostriatal tract, 143

Nitrates, as antianginal drugs, 111, 111–112 Nitric oxide signaling, 25, 94

Nitroglycerin

as antianginal, 111 first-pass effect, 7

Nitroprusside, as direct-acting vasodilator, 94 Nitrosoureas, cell-cycle specificity, 299 Nitrous oxide, characteristics, 153

NNRTIs (nonnucleoside reverse transcriptase inhibitors), 202 Noncompetitive antagonists, 22

Nonmicrosomal metabolism, 11

Nonnucleoside reverse transcriptase inhibitors (NNRTIs), 202 Nonsteroidal antiinflammatory drugs (NSAIDs), 231–233, 234

adverse cardiovascular events associated with, 233 drug list, 245

for migraine headaches, 228 for rheumatoid arthritis, 236

Nordiazepam, 9 Norepinephrine (NE), 40, 56

actions, 56 clinical uses, 61

cocaine blocking uptake, 155 dopamine as precursor, 144 drugs of abuse and, 165

indirect-acting adrenergic receptor agonists and, 61 as mixed-acting adrenergic agonist, 58

nicotinic receptor activation, 47 nonmicrosomal metabolism, 11 receptors for, 24

Norethindrone, 281 Norgestrel, 282

Nucleic acid synthesis inhibitors, 188–190, 193–194 direct-acting, 190

folic acid synthesis inhibitors, 179, 188, 188–189, 193–194 mechanism of action, 179

Nucleoside reverse transcriptase inhibitors (NRTIs), 202 side effects, 202

Nutritional supplements, characteristics/uses, 321 Nystatin, characteristics/uses, 195–196

O

Octreotide, 287

Olanzapine, characteristic properties, 147

Omeprazole, for treating H. pylori ulcers, 190, 224 Ondansetron

as antiemetic, 225 serotonergic systems and, 227

Open-angle glaucoma, 65

Ophthalmology. See also Glaucoma, drugs for treating effect of ANS drugs on eye, 43

M blockers used in, 50 Opioid analgesics, 159–161

antidote for, 317

as drugs of abuse, 164 characteristics/uses, 160 common toxic syndromes, 315 drug list, 167

duality of action, 225

for migraine headaches, 228

Oral administration, doubling oral doses, 15 Oral contraceptives, characteristics/uses, 282–283 Oral hypoglycemics

modes of action, 274 sulfonylureas, 274

Organophosphates activation, 47 characteristics/uses, 48 toxicology, 48

Orlistat, as antihyperlipidemic, 119, 121 Oseltamivir

characteristics/uses, 204 mechanism of action, 200, 203

Osmotic diuretics, 84

Overactive bladder, M blocker therapy for, 50 Oxacillin, 181

Oxazepam, characteristics/uses, 134 Oxybutynin, characteristics/uses, 50 Oxygen, as antidote, 317

Oxytocin, 287

P

Paclitaxel, cell-cycle specificity, 299 Palivizumab, clinical uses of, 310 Pamidronate, 289

Paraoxon, 48

Parasympathetic nervous system (PANS), 39 ANS dominance and, 50

blood pressure control mechanisms, 40–41 characteristics of ganglion blockers, 51 nicotinic receptor activation, 47

Parathion, 46, 48

Parenteral formulations, antipsychotic drugs, 147

Parkinson’s disease, drugs for treating. See Antiparkinsonian drugs Paroxetine, 139

Partial agonists, 20 duality, 21

Passive diffusion, 5

Patent ductus arteriosus, 230 PCP, as drug of abuse, 164

Pegloticase, characteristics/uses, 238

Penicillamine

as antidote, 317

for heavy metal poisoning, 316 Penicillins, 181–182

characteristics/uses, 181–182 chemical structure, 180 drug list, 209

mechanism of action, 179, 181 mechanism of resistance, 179, 181

Pentazocine, characteristics/uses, 160

Peptic ulcer disease (PUD), drugs for treating, 190, 223–225 mechanisms of action, 224

Performance anxiety, drugs for treating, 63 Perjunctional nerve terminal, 56 Permeation, 4–5

factors in, 4 ionization, 4–5, 5

modes of drug transport across a membrane, 5 Pharmacodynamics, 19–28

definitions in, 19

drug development and testing, 27

graded (quantitative) dose-response curves, 19–22 quantal (cumulative) dose-response curves, 22–23 signaling mechanisms, 23–26

Pharmacokinetics absorption, 3, 6–7, 225 biotransformation, 9 calculations in, 16 distribution, 3, 8–9 drug biodisposition, 3 elimination, 12–14 excretion, 3 metabolism, 3 metabolism in, 9–11 permeation, 4–5 redistribution, 9 steady state, 14–16

Phenelzine, 140 Phenobarbitol, 134

Phenoxybenzamine, as alpha blocker, 61 Phentolamine, as alpha blocker, 61 Phenylephrine, as α1 adrenergic agonist, 58 Phenytoin

characteristics/uses, 150–151 cytochrome P450 isozymes, 10 seizure states/drugs of choice, 149

Philocarpine, cholinergic properties, 47 pH levels, 6–7

pH levels, 4 urinary, 5

Phosphodiesterase (PDE) inhibitors as antianginal, 113

for heart failure, 99 Photoxicity, 186 Physiological antagonism, 22 Physostigmine

as antidote, 48, 317 characteristics/uses, 48

337

USMLE Step I λ Pharmacology

Pilocarpine, mechanism of action, 66 Pindolol, characteristics, 62 Pioglitazone, characteristics/uses, 275 Piperacillin, 181

Pituitary disorders, drugs for treating, 287 drug list, 291

pKa levels, 4 pKq levels

pKq levels, 4

Placental barrier to distribution, 8 FDA pregnancy risk categories, 27

Plasma concentration

and dose relationship, 15 effect of loading dose on, 15

Plasma decay curve, first-order elimination, 13 Plasma level curves, 6

bioavailability, 7 Plasma-protein-binding sites, 8 Plasminogen, 263

Plateau principle, 14

Platelet-derived growth factor (PDGF), 26 Polyenes, 195–196

Postjunctional receptors, 46

Post-myocarial infarction, antihypertensive use in, 94 Potassium (K+)

as arrhythmogenic, 108

conditions associated with. See Hyperkalemia; Hypokalemia K+-sparing agents as diuretics, 87

Potassium (K+) channel blockers, 63, 108

Potassium (K+) channels, direct-acting vasodilators and, 94 Potassium (K+) current, fast-response fibers, 101, 101–104 Potency

antagonism and potentiation, 21, 21–22 defined, 19

of full and partial agonists, 20 Pramipexole, as antiparkinsonian drug, 145 Pramlintide, 276

Prasugrel, characteristics/uses, 266 Praziquantel, 208

Prazosin, as alpha blocker, 62, 93 Prednisone, 239

Pregnancy, HIV prophylaxis in, 203 Pregnancy risk

alcohol, 137

antibacterial agents, 185, 190 FDA categories, 27 prostaglandins, 230

Premarin (conjugated estrogens), 279 Presynaptic membrane depolarization, 46, 56 Primaquine, 207, 208

Probenecid, 190 characteristics/uses, 238

Procainamide

as Na+ channel blocker, 106 characteristics/uses, 107 metabolism, 11

Procaine, as local anesthetic, 155

338

Procarbazine

cell-cycle specificity, 299 characteristics/uses, 301 toxicity, 302

Prochlorperazine, 225 Prodrugs, 9 Progestins

characteristics/uses, 282, 283 drug list, 291

in oral contraceptives, 281–282 Prolactin-inhibiting hormone (PIH), 287 Promethazine

as antiemetic, 225 properties, 222

Propofol, characteristics/uses, 154 Propranolol

as beta-blocker, 107 characteristics/uses, 62, 63, 107 for migraine headaches, 228

Propylthiouracil (PTU), 286 placental barrier and, 8

Prostacyclin

for pulmonary hypertension, 95, 231 receptors for, 24

Prostaglandins (PGs), characteristics/uses, 229, 230–231 Protamine, as antidote, 317

Protease inhibitors (PI) characteristics/uses, 203 mechanism of action, 203, 205

Protease Inhibitors (PIs) characteristics/uses, 205

Protein-binding, 8 Protein C deficiency, 261 Protein synthesis, 184

Protein synthesis inhibitors, 184–188, 193 drug list, 209

mechanism of action, 179 mechanisms, 185

Proton pump inhibitors, 224 Proximal convoluted tubule (PCT), 84

Pulmonary hypertension, drugs for treating, 95 Pupillary size mechanisms, 43

Purified nutritional supplements, 319 Pyrantel pamoate, 208 Pyrazinamide, 191

Pyridostigmine, characteristics/uses, 48 Pyrimethamine

as antimalarial, 207

as antiprotozoal agent, 207 characteristics/uses, 188 mechanism of action, 179

Q

Quantal (cumulative) dose-response (D-R) curves, 22–23 therapeutic index, 22, 22–23

Quantitative D-R curves. See Graded (quantitative) dose-response (D-R) curves