Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

First Aid Pharmacology > step_1_pharm_20140606001619 > Flashcards

step_1_pharm_20140606001619 Flashcards

1
Q

Epinephrine

A

alpha-agonistdecrease aqueous humor synthesis via vasoconstrictionSE: mydriasis, not for closed-angle glaucoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Brimonidine

A

alpha-agonist (alpha 2)decrease aqueous humor synthesisSE: blurry vision, ocular, hyperemia, foreign body sensation, ocular allergic reaction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Timolol, bextaolol, carteolol

A

decrease aqueous humor synthesisSE: none

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Acetazolamide

A

diureticsdecrease aqueous humor synthesis via inhibition of carbonic anhydraseSE: none

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Pilocarpine

A

direct cholinomimeticsincrease outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular meshworkSE: Miosis and cyclospasm (contraction of ciliary muscle)Use in emergencies - very effective at opening meshwork into canal of Schlemm

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Carbachol

A

direct cholinomimeticsincrease outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular meshworkSE: Miosis and cyclospasm (contraction of ciliary muscle)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Physostigmine, echothiophate

A

indirect cholinomimeticsincrease outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular meshworkSE: Miosis and cyclospasm (contraction of ciliary muscle)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Latanoprost (PGF2alpha)

A

prostaglandinincrease outflow of aqueous humorSE: darkens color of iris

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Morphine, fentanyl, codeine, heroin, methadone, dextromethorphan, diphenoxylate

A

opioid analgesicsagonist at opioid receptors (mu = morphine, delta = enkephalin, kappa = dynorphin) to modulate synaptic transmission. Inhibit release of Ach, NE, 5-HT, glutamate, substance PSE: addiction, respiratory depression, constipation, miosis (pinpoint pupil)Toxicity treated by naloxone or naltrexone (opioid receptor antagonist)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Butorphanol

A

mu-opioid receptor parital agonist and kappa receptor agonistUses: severe pain (migtaine, labor)Causes less respiratory depression than full agonistCan cause opioid withdrawal symptoms if patient is also taking full opioid agonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Tramadol

A

very weak opioid agonist; also inhibits serotonin and NE reuptakeUses: chronic painSE: similar to opioids. decreases seizure threshold

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Phenytoin

A

simple, comlpex, tonic-clonic (1st line), status epilepticus (1st line for prophylaxis)use-dependent blockade of Na channels; inhibition of glutamate release from excitatory presynaptic neuronfosphenytoin for parenteral useSE: nystagmus, diplopia, ataxia, sedation, gingival, hyperplasia, hirsutism, megaloblastic anemia (decreased folate), fetal hydantoin syndrome, SLE-like syndrome, induction of P-450, lymphadenopathy, Steven-Johnson syndrome, osteopenia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Carbamazepine

A

simple, complex, tonic-clonic, trigeminal neuralgia (1st line for all)increase Na channel inactivationSE: diplopia, ataxia, blood dyscrasias, liver toxicity, teratogenesis, induction of P-450, Steven-Johnson syndrome

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Lamotrigine

A

simple, complex, tonic-clonicblocks VG-Na channelsSE: Steven-Johnson syndrome

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Gabapentin

A

simple, complex, tonic-clonic, peripheral neuropathy, postherpetic neuralgia, migraines prophylaxis, bipolar disorderdesigned as GABA analog, but primarily inhibits high-voltage-activated Ca channelsSE: sedation, ataxia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Topiramate

A

simple, complex, tonic-clonic, migraine preventionblocks Na channels, increase GABA actionSE: sedation, mental dulling, kidney stones, weight loss

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Phenobarbital

A

simple, complex, tonic-clonic (1st line in children)increase GABAa actionSE: sedation, tolerance, dependence, induction of P-450

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Ethosuximide

A

1st line for absenceblocks thalamic T-type Ca channelsSE: GI distress, fatigue, headache, urticaria, Steven-Johnson syndromeEFGH - Etho, Fatigue, GI, Headache

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Benzodiazepines

A

diazepam, lorazepam, triazolam, oxazepam, midazolamUses: 1st line for acute status epilepticus (diaz-, loraz-), seizures of eclampsia, anxiety, spasticity, detox (alcohol withdrawal), night terrors, sleepwalking, anesthetic (muscle relaxation), hypnoticMOA: facilitate GABAa action by increased frequency of Cl channel opening, decrease REM sleepSE: dependence, addictive CNS depression effects with alcohol. less risk of respiratory depression and coma than with barbituratesTreat overdose with flumazenil (competative antagonist)Most have long half-lives and active metabolites except triazolam, oxazepam, and midazolam - higher addictive potential

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Barbiturates

A

phenobarbital, pentobarbital, thiopental, secobarbitalfacilitate GABAa action by increased duration of Cl channel opening, thus decrease neuron firingcontraindicated in porphyriaUses: sedative for anxiety, seizures, insomnia, induction, of anesthesia (thiopental)SE: respiratory and cardiovascular depression, CNS depression (with alcohol), dependence, induces P-450overdose treatment is supportive (assist respiration and maintian BP)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Valproic acid

A

simple, complex, tonic-clonic (1st line), absence, myoclonicincrease Na channel inactivation, increase GABAconcentraitonSE: GI distress, rare but fatal hepatotoxicity, nueral tube defects in fetal (spina bifida), tremor, weight gainContraindicated in pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Non-benzo hypnotics

A

zolpidem, zaleplon, eszopicloneact via BZ1 subunit of the GABA receptorreversed by flumazenilUse: insomniaSE: ataxia, headaches, confusionrapid metabolism by liver enzymes, only modest day-after psychomotor depression, lower dependence risk

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Inhaled anesthetics

A

halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, NOEffects: myocardial depression, repiratory depression, nausea/emesis, increased cerebral blood flow (decreased cerebral metabolic demand)SE: hepatotoxicity (halothane), nephrotoxicity (mehoxyflurane), proconvulsant (enflurane), malignant hyperthermia (all but NO), expansion of trapped gas in a body cavity (NO)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Thiopental

A

IV anesthetics - barbiturateshigh potency, high lipid solubility, rapid entry into brainUse: induction of anesthesia and short surgical proceduresterminated by rapid redistribution into tissue and fatdecrease cerebral blood flow

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Midazolam

A

IV anesthetic - benzodiazepineUse: endoscopy; used adjunctively with gaseous anesthetic and narcoticsSE: postop respiratory depression, decreased BP (treat with flumazenil), amnesia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Arylcyclohexylamines (ketamine)

A

IV anesthetic - PCP analogblock NMDA receptors, cardiovascular stimulantSE: disorientation, hallucination, and bad dreamsincrease cerebral blood flow

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Propofol

A

IV anesthesticpotentiates GABAaUse: sedation in ICU, rapid anesthesia induction, and short proceduresless postop nausea than thiopental

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Local anesthetics

A

Esters - procaine, cocaine, tetracaineAmides - lidocaine, mepivacaine, bupivacaine (2 i’s)block Na channels by binding specific receptors on inner portion of channel; preferentially bind to activated Na channels (rapid firing neurons)tertiary amine - penetrate membrane in uncharged form then bind ion channels as charged formcan be given with vasoconstrictors to enhance local actionin infected tissue (acidic), alkaline anesthetics are charged and cannot penetrate membrane –> increase doseOrder of blockage: small myl > small unmyl > large myl > larger unmylOrder of loss: pain, temp, touch, pressureUse: minor surgical procedures, spinal anesthesiaSE: CNS excitation, severe CV toxicity (bupivacaine), HTN, hypotension, arrhythmias (cocaine)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Succinylcholine

A

depolarizing NMBAch receptor agonist –> sustained muscle depolarization and prevents muscle contractionPhase I (prolonged depolarization) - no antidotes (potentiated by AchE inhibitors)Phase II (repolarized but blocked) - antidote is neostigmineSE: hypercalcemia, hyper kalemia, and malignant hyperthermia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Nondepolarizing NMB

A

tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuroniumcompetitive antagonists - compete with Ach for receptorReversal of block - neostigmine, edrophonium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Dantrolene

A

prevents release of Ca from SR of skeletal muscleUse: malignant hyperthermia, neuroleptic malignant syndrome

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Dopamine agonists

A

bromocriptine (ergot), pramipexole, ropinirole (non-ergot)non-ergot preferred

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Increase dopamine

A

amantadine - increase dopamine release (also for influenza A and rubella) SE: ataxiaL-dopa/carbidopa (converted to dopamine in CNS)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

Prevent dopamine breakdown

A

selegiline - MAO type B inhibitorentacapone, tolcapone - COMT inhibitors – prevent L-dopa peripheral degradation, thereby increasing availability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

L-dopa/carbidopa

A

increase levels of dopamine in brainSE: arrhythmias from increased peripheral formation of catecholamines; long term use dyskinesia following administration, akinesia between doses

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

Selegiline

A

MAO-B inhibitor, which preferentially metabolizes dopamine over NE and 5-HTUse: adjunctive agent to L-dopa in treatment of Parkinson’s diseaseSE: enhance SE of L-dopa

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

Memantine

A

NMDA receptor antagonist; helps prevent excitotoxicity (mediated by Ca)Use: Alzheimer’sSE: dizziness, confusion, hallucinations

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

Donepezil, galantamine, rivastigmine

A

acethylcolinesterase inhibitorsUse: Alzheimer’sSE: nausea, dizziness, insomnia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

Sumatriptan

A

5-HT 1B/1D agonistinhibits trigeminal nerve activation; prevents vasoactive peptide release –> vasoconstrictionUse: acute migraine, cluster headache attacksSE: coronary vasospasm (contraindicated in CAD and Prinzmetal’s angina), mild tingling

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

H2 blockers

A

cimetidine, ranitidine, famotidine, nizatidine (-tidine)Reversible block of H2-receptor –> decreased H+ secretion by parietal cellsUses: peptic ulcer, gastritis, mild esophageal refluxSE: cimetidine is a potent inhibitor of P-450; antiandrogenic effects (prolactin release, gynecomastia, impotence); can cross blood-brain barrier (confusion, dizziness, headaches) and placenta; cimetidine and ranitidine decrease renal excretion of creatinine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

PPI

A

omeprazole, lansoprazole, esomeprazole, pantoprazole, dexlansoprazoleirreversibly inhibit H+/K+ ATPase in stomach parietal cellsUses: peptic ulcer, gastritis, esophageal reflux, ZE syndromeSE: increased risk of C. difficle infection, pneumonia. hip fractures, decreased serum Mg with long term use

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

Bismuth, sucralfate

A

bind to ulcer base, providing physical protection and allowing HCO- secretion to reestablish pH gradient in the mucous layerUses: increased ulcer healing, traveler’s diarrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

Misoprostol

A

PGE1 analog. increase production and secretion of gastric mucous barrier; decreased acid productionUses: prevention of NSAID-induced peptic ulcers; maintenance of PDA, induce laborSE: diarrhea, contraindicated in women of childbearing potential

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

Octreotide

A

Long-acting somatostain analogUses: acute variceal bleeds, acromegaly, VIPoma, and carcinoid tumorsSE: nausea, cramps, steatorrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

Aluminum hydroxide

A

SE: hypokalemia, constipation and hypophosphatemia, proximal muscle weakness, osteodystrophy, seizuresAluminimum amount of feces

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
46
Q

Magnesium hydrozide

A

SE: hypokalemia, diarrhea, hyporeflexia, hypotension, cardiac arrestMg = must go to the bathroom

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
47
Q

Calcium carbonate

A

SE: hyperkalemia, hypercalcemia, rebound acid increase; can chelate and decrease effectiveness of other drugs (tetracycline)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
48
Q

Osmotic laxatives

A

magnesium hyroxide, magnesium citrate, polyethylene gycol, lactuloseprovide osmotic load to draw water outlactulose also treats hepatic encephalopathy since gut flora degrade it into metabolites (lactic acid and acetic acid) that promote nitrogen excretion as NH4Uses: constipationSE: diarrhea, dehydration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
49
Q

Inflizimab

A

monoclonal antibody to TNF-alphaCrohn’s disease, UC, RASE: infection (including reactivation of latent TB), fever, hypotension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
50
Q

Sulfasalazine

A

combination of sulfapyridine (antibacterial) and 5-aminosalicyclic acid (anti-inflammatory); activated by colonic bacteriaUse: UC, Crohn’s diseaseSE: malaise, nausea, sulfonamide toxicity, reversible oligospermia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
51
Q

Ondansetron

A

5-HT3 antagonist. powerful central-acting antiemeticUses: control vomiting postoperatively and in patients undergoing cancer chemotherapySE: headache, constipation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
52
Q

Metoclopramide

A

D2 receptor antagonist. increased resting tone, contractility, LES tone, motility. does not influence colon transport timeUses: diabetic and post-surgery gastroparesis, antiemeticSE: increased parkinsoniam effects. Restlessness, drowsiness, depression, nausea, diarrhea. drug interaction with digoxin and diabetic agentscontraindicated in patient with small bowel obstruction or Parkinson’s disease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
53
Q

CNS stimulants

A

methylphenidate, dextroamphetamine, methamphetamineincreases catecholamines at the synaptic cleft, especially NE and dopamineUses: ADHD, narcolepsy, appetite control

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
54
Q

Antipsychotics (neuroleptics)

A

haloperidol, trifluoperazone, fluphenazine, thioridazine, chlorpromazine (-azines)block D2 receptors (increase cAMP)Uses: schizophrenia (positive symptoms), psychosis, acute mania, Tourette’sSE: lipid soluble and stored in body fat, hyperprolactin, High potency: Try to Fly High (TFH) - extrapyramidal symptoms SE: NMS (rigidity, myoglobinuria, autonomic instability, hyperpyrexia), tardive dyskinesia (stereotypic oral-facial movements as a result of long-term antipsychotic use)NMS - Fever, Enchephalopathy, Vital insability, Elevated enzymes, Rigidity of muscles (FEVER)Low potency: Cheating Thieves are low (CT) - non-neurologic SE: blocking muscarinic, alpha 1 and histamine receptorsC - corneal deposits; T - retinal deposits

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
55
Q

Atypical antipsychotics

A

olanzopine, clozapine, quetiapine, risperidone, aripiprazole, ziprasidonevaried effects on 5-HT, dopamine, and alpha and H1 receptorsUses: schizophrenia (both positive and negative), bipolar, OCD, anxiety disorder, depression, mania, Tourette’sSE: fewer extrapyramidal and anticholinergic SEolan/cloza - weight gaincloza - agranulocytosis (monitor WBC weekly) and seizureZipra - may prolong QT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
56
Q

Lithium

A

Possibly related to inhibition of phosphoinositol cascadeUses: mood stabilizer for bipolar disorder; blocks relapse and acute manic events, SIADHSE: tremor, sedation, edema, heart block, hypothyroidism, polyuria, teratogenesis, Ebstein anomaly and malformation of great vesselsnarrow therapeutic window, exclusively secreted by kindeys; most is reabsorbed at proximal convoluted tubule following Na

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
57
Q

Buspirone

A

stimulates 5-HT1A receptorsUses: GAD, requires 1-2 weeks to see effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
58
Q

SSRIs

A

fluoxetine, paroxetine, setraline, citalopramUses: depression, GAD, panic disorder, OCD, bulimia, social phobias, PTSDSE: GI distress, sexual dysfunciton, serotonin syndrome (treat with cyproheptadine)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
59
Q

SNRIs

A

venlafaxine, duloxetine (greater effect on NE)inhibit serotonin and NE reuptakeUses: depression; V - also for GAD; D - diabetic peripheral neuropathySE: increased BP, nausea, sedation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
60
Q

Tricyclic antidepressants

A

amitriptyline, nortriptyline, imipramine, desipramine, clomipramine, doxepin, amoxopine (-iptyline or -ipramine)block reuptake of NE and serotoninUses: major depression, betwetting (im-), OCD (clom-), fibromyalgiaSE: sedation, alpha1 blocking effects (postural hypotension), atropine-like, convulsions, coma, cardiotoxicity (treat with NaHCO3), respiratory depression, hypersyrexianortriptyline in elderly with anticholenergic SE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
61
Q

MAO inhibitors

A

tranylcypromin, phenelzine, isocarboxazid, selegiline (MAO-B selective)nonselective MAO inhibition increases levels of amine NT (NE, serotonin, dopamine)Uses: atypical depression, anxiety, hypochondriasisSE: HTN crisis, CNS stimulationcontraindicated with SSRIs, TCAs, St. John’s Wort, meperidine, and dextromethorphan

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
62
Q

Bupropion

A

atypical anti-depressantincrease NE and dopamine via unknown mechanismSE: stimulant effects, headache, seizure in bulimic patientsalso used for smoking cessation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
63
Q

Mirtazapine

A

atypical anti-depressantalpha2-antagonist (increase release of NE and serotonin) and potent 5-HT2 and 5-HT3 receptorSE: sedation (desirable for insomnia), increased appetite, weight gain (desirable for elderly), dry mouth

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
64
Q

Maprotiline

A

atypical anti-depressantblocks NE reuptakeSE: sedation, orthostatic hypotension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
65
Q

Trazodone

A

atypical anti-depressantinhibits serotonin reuptakeUses: insomnia, high dose for antidepressant effectSE: sedation, nausea, priapism, postural hypotension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
66
Q

Alcohol withdrawal

A

benzodiazepines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
67
Q

Anxiety

A

SSRIs, SNRIs, buspirone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
68
Q

ADHD

A

methylphenidate, amphetamines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
69
Q

Bipolar disorder

A

lithium, valproate, carbamazepine, atypical antiphyschotics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
70
Q

Bulimia

A

SSRIs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
71
Q

Depression

A

SSRIs, SNRIs, TCAs, buspirone, mirtazapine (especially with insomnia)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
72
Q

OCD

A

SSRIs, clomipramine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
73
Q

Panic disorder

A

SSRIs, venlafaxine, benzodiazepines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
74
Q

PTSD

A

SSRIs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
75
Q

Schizophrenia

A

Antipsychotics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
76
Q

Social phobias

A

SSRIs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
77
Q

Tourette’s syndrome

A

antipsychotics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
78
Q

Insulin

A

Rapid acting: Lispro, Aspart, GlulisineShort-acting: regularIntermediate: NPHLong-acting: Glargine, Detemirbind insulin receptor (tyrosine kinase activity)Liver: increase glucose stored as glycogenMuscle: increased glycogen and protein synthesis, K uptakeFat: aids TG storageUses: DM 1 & 2, gestational diabetes, life-threatening hyperkalemia, stress-induced hyperglycemiaSE: hypoglycemia, very rarely hypersensitivity reactions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
79
Q

Biguanides

A

Metformindecreases gluconeogenesis, increases glycolysis, increases peripheral glucose uptakeUses: oral - 1st line for DM2SE: GI upset, lactic acidosis (contraindicated in patients with renal failure)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
80
Q

Sulfonylureas

A

1st gen: tolbutamide, chlorpropamide2nd gen: glybutide, glimepriride, glipizideclose K+ channel in beta-cell membrane, so depolarizes –> triggering insulin release via Ca influxUses: DM2, requires some islet functionSE: 1st - disulfiram-like effects; 2nd - hypoglycemia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
81
Q

Glitazones/thiazolidinediones

A

pioglitazone, rosiglitazoneincrease insulin sensitivity in peripheral tissues. bind PPAR-gamma nuclear transcription regulator (activate fatty acid storage and glucose metabolism)Use: monotherapy in DM2 or combinedSE: weight gain, edema, hepatotoxicity, HF

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
82
Q

Alpha-glucosidase inhibitors

A

acarbose, miglitolinhibit intestinal brush-border alpha-glucosidases, delayed sugar hydrolysis and glucose absorption –> decreased postprandial hyperglycemiaUse: montherapy for DM2 or conbinedSE: GI disturbances

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
83
Q

Amylin analongs

A

pramlintidedecreased glucagonUses: DM 1 & 2SE: hypoglycemia, nausea, diarrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
84
Q

GLP-1 analogs

A

exenatide, liraglutideincreases insulin, decreases glucagon releaseUse: DM2SE: nausea, vomiting, pancreatitis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
85
Q

DPP-4 inhibitors

A

linagliptin, saxagliptin, sitagliptinincrease insulin, decrease glucagon releaseUse: DM2SE: mild urinary or respiratory infections

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
86
Q

PTU

A

block peroxidase (organification of iodide and coupling), blocks 5’-deiodinase (decreases peripheral conversion of T4 to T3)Use: hyperthyroidSE: skin rash, agranulocytosis, aplastic anemia, hepatotoxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
87
Q

Methimazole

A

block peroxidase (organification of iodide and coupling)Use: hyperthyroidSE: skin rash, agranulocytosis, aplastic anemia, teratogen

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
88
Q

Levothyroxine, triiodothyronine

A

thyroxine replacementUse: hypothyroidism, myxedemaSE: tachycardia, heat intolerance, tremors, arrhythmias

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
89
Q

GH

A

GH deficiency, Turner syndrome

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
90
Q

Somatostatin

A

octreotideacromegaly, carcinoid, gastrinoma, glucagonoma, esophageal varices

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
91
Q

Oxytocin

A

stimulates labor, uterine contractions, milk let-down; control uterine hemorrhage

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
92
Q

Demeclocycline

A

ADH antagonistUse: SIADHSE: nephrogenic DI, photosensitivity, abnormalities of bone and teeth

93
Q

Glucocorticoids

A

hydrocortisone, prednisone, triamcinolone, dexamethasone, beclomethasonedecrease the production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX-2Uses: Addision’s disease, inflammation, immune suppressio, asthmaSE: iatrogenic Cushing’s, adrenal insufficiency when drug stopped abruptly after chronic use

94
Q

Mannitol

A

osmotic diureticincrease tubular fluid osmolarity; producing increased urine flow, decrease intracranial/intraocular pressureUses: drug overdose, elevated intraocular/intracranial pressureSE: pulmonary edema, dehydrationContraindicated in anuria, CHF

95
Q

Acetacolamide

A

CA inhibitorcauses self-limited NaHCO3 diuresis and reduction in total-body HCO3-Uses: glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness, pseudotumor cerebriSE: hyperchloremic metabolic acidosis, paresthesias, NH3 toxicity, sulfa allergy

96
Q

Furosemide

A

sulfonamide loop diureticinhibits cotransport system (Na, K, Cl) of TAL of Henle; abolishes hypertonicityof medulla, preventing concentration of urinestimulate PGE release (vasodilatory effect on afferent arteriole); increase Ca excretion (Loops Lose Ca)SE: Ototoxicity, Hypokalemia, Dehydration, Allergy, Nephritis (interstitial), Gout (OH DANG)

97
Q

Ethacrynic acid

A

loop diureticphenoxyacetic acid derivative; same action as furosemideSE: similar to furosemide; can cause hyperuricemia

98
Q

Hydrochlorothiazide

A

thiazide diureticinhibits NaCl reabsorption in early distal tubule, reducing capacity of the nephron, decrease Ca excretionUse: HTN, CHF, idiopathic hypercalciuria, nephrogenic DISE: hypokalemic metabolic alkalosis, hyponatremia, hyperglycemia, hyperlipidemia, hyperuricemia, and hypercalcemia, sulfa allergy (HyperGLUC)

99
Q

K sparing diuretics

A

spironolactone, eplerenonecompetitive aldosterone receptor antagonists in the cortical collecting tubuletriamterene, amilorideact on cortical collecting tubule by blocking Na channelsUse: hyperaldosteronism, K+ depletion, CHFSE: hyperkalemia (arrhythmia), endocrine effect with spironolactone (gynecomastia, antiandrogen effects)

100
Q

ACE inhibitors

A

captopril, enalapril, lisinoprilinhibit ACE –> decreases angiotensin II –> decreases GFR by preventing constriction of the efferent arterioles; also prevents inactivation of of bradykinin, a potent vasodilatorUse: HTN, CHF, proteinuria, diabetic renal disease; prevent unfavorable heart remodeling as a result of chronic hypertensionSE: cough, angioedema, teratogen (fetal renal malformation), creatinine increase, hyperkalemia, hypotensionAvoid in bilateral renal artery stenosis because ACE inhibitors will further decrease GFR –> renal failure

101
Q

Penicillin

A

penicillin G (IV and IM form), penicillin V (oral)beta-lactambind penicillin-binding proteins; block transpeptidase cross-linking of peptidoglycan; activate autolytic enzymesUses: gram-positive organisms (S. pnuemoniae, S. pyogenes, Actinomyces); N. meningitidis Treponema pallidum, syphilisbactericidal for gram-positive cocci, gram-positive rods, gram-negative cocci, and spirochetesnot penicillinase resistantSE: hypersensitivity reaction, hemolytic anemiaResistance: beta-lactamases cleave beta-lactam ring

102
Q

Oxacillin, nafcillin, dicloxacillin

A

penicillinase-resistant penicillinssame as penicillin; resistant because bulky R group blocks accessUses: S. aureus (except MRSA; resistant because altered penicillin-binding protein target site)SE: hypersensitivity reactions; interstital nephritis

103
Q

Ampicillin, amoxicillin

A

aminopenicillinssame as penicillin; wider spectrum, penicillinase sensitive; combine with clavulanic acid to protect against beta-lactamaseamoxicillin has greater oral bioavailablityUses: H. influenzae, E. coli, Listeria, Proteus, Salmonella, Shigella, enterococci (HELPSS)SE: hypersensitivity reactions; ampicillin rash; pseudomembranous colitisResistance: beat-lactamase cleaves beta-lactam ring

104
Q

Ticarcillin, piperacillin

A

antipseudomonalssame as penicilinUses: Psudomonas spp., gram-negative rods; susceptible to penicillinase; use with clavulanic acidSE: hypersensitivity reaction

105
Q

Beta-lactamase inhibitors

A

clavulanic acidsulbactamtazobactum

106
Q

Cephalosporins

A

beta-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicilinases; bactericidal1st gen (cefazolin, cephalexin) - gram-positive cocci, Proteus, E. coli, Klebsiella (PEcK)cefazolin used prior to surgery to prevent S. aureus wound infections2nd gen (cefoxitin, cefaclor, cefuroxime) - gram-positive cocci, H. influenzae, Enterobacter aerogenes, Neiseria spp., Proteus, E. coli, Klebsiella, Serratia (HEN PEcKS)3rd gen (ceftriaxone, cefotaxime, ceftazidime) - serious gram-negative infections resistant to other beta-Ceftriaxone - meningitis and gonorrheaCeftazidime - Pseudomonas4th gen (cefepime) - increase activity against Pseudomonas and gram-positive organismsSE: HSR, vitamin K deficiency, increase nephrotoxicity of aminoglycosides

107
Q

Aztreonam

A

monobactam resistant to beta-lactamases; prevent cross-linking by binding to PBP3synergistic with aminoglycosidesUses: gram-negative rods onlyfor penicillin-allergic patients and those with renal insufficiency who can’t tolerate aminoglycosidesSE: nontoxic; GI upset

108
Q

Imipenem/cilastatin, meropenem

A

imipenem - broad spectrum beta-lactamase-resistant carbapenemalways administered with cilastatin (inhibitor of renal dehydropeptidase I) to decrease inactivation of drug in renal tubulesUse: gram-positive cocci, gram-negative rods and anarodes; SE limit effects use to life-threatening infectionsSE: GI distress, skin rash, and CNS toxicity (seizures) at high plasma levels

109
Q

Vancomycin

A

inhibits cell wall peptidoglycan formation by binding D-ala D-ala portion of cell wall precursorsUse: gram-positive only - serious, multidrug-resistant organisms, including MRSA, enterococci, and C. difficileSE: Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing - red man syndrome (prevented by pretreatment with anti-histamines and slow infusion rates)Resistance: amino acid change of D-ala D-ala to D-ala D-lac

110
Q

Aminoglycosides

A

gentamicin, neomycin, amikacin, tobramycin, strptomycinbactericidal; inhibit formation of initiation complex and cause misreading mRNA; block translation; require O2 uptake - ineffective against anaerobesUse: severe gram-negative rod infections; bowel surgery (neomycin)synergistic with beta-lactam antibioticsSE: Nephrotoxicity (especially when used with cephalosporins), Neuromuscular blockage, Ototoxicity (with loop diuretics); tertogen

111
Q

Tetracyclines

A

tetracycline, doxycycline, demeclocycline, minocyclinebacteriostatic; bind to 30S and prevent attachment of aminoacyl-tRNA; limited CNS penetrationdoxycycline - fecally eliminated; can be used in patients with renal failuredo not take with milk, antacid, or iron-containg preparations because divalent cations inhibit its absorption in the gutUse: Borrelia burgdorferi, M. peneumoniae; Rickettsia and Chlamydia (accumulates intracellularly)SE: GI distress, discoloration of teeth and inhibition of bone growth in children, photosensitivitycontraindicated in pregnancyResistance: decreased uptake into cells or increased efflux out of cell by plasmid-encoded transport pumps

112
Q

Macrolides

A

azithromycin, clarithromycin, erythromycininhibit protein synthesis by blocking translocation; bind to the 23S rRNA of the 50S ribosomal subunit; bacteriostaticUse: atypical pneumonias (mycoplasma, chlamydia, legionella), STDs (chlamydia), gram-positive cocci (strep in patient allergic to penicillin)SE: Motility issues, Arrhythmia caused by prolonged QT, acute Cholestatic hepatic hepatitis, Rash eOsinophilia (MACRO); increased concentration of throphyllines, oral anticoagulantsResistance: methylation of 23S rRNA binding site

113
Q

Chloramphenicol

A

blocks peptidyltransferase at 50S ribosomal subunit; bacteriostaticUse: Meningitis (Hib, N. meningitidis, S. pntumoniae)SE: anemia (dose dependent), aplastic anemia (dose independent), gray baby syndrome (premature infants b/c of lack of UDP-glucuronyl tranferase)Resistance: plasmid-encoded acetyltransferase that inactiavtes drug

114
Q

Clindamycin

A

blocks peptide transfer at 50S ribosomal subunit; bacteriostaticUse: anaerobic infections in aspiration pneumonia; oral infections with mouth anaerobes; anaerobes above the diaphragmSE: pseudomembranous colitis (C. diff), fever, diarrhea

115
Q

Sulfonamides

A

sulfamethoxazole, sulfisoxazole, sulfadiazinePABA antimetabolites inhibit dihydropteroate synthase; bacteriostaticUse: gram-positive, gram-negative, Nocardia, Chlamydia, UTISE: hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity (tubulointerstitial nephritis), photosensitivity, kernicterus in infants, displace other drigs from albuminResistance: altered enzyme (bacterial dihydropteroate synthase), decreased uptake, or increased PABA synthesis

116
Q

Trimethoprim

A

inhibits bacterial dihydrofolate reductase; bacteriostaticUse: combo with SMX - UTIs, Shigella, Salmonella, Pneumocystis pneumonia (treatment and prophylaxis)SE: megaloblastic anemia, leukopenia, granulocytopeniaTMP: Treats Marrow Poorly

117
Q

Fluoroquinolones

A

ciprofloxacin, norfloxacin, enoxacin, nalidicic acidinhibit DNA gyrase (topo II) and topo IV; bacteriocidal; don’t take with antacidsUse: gram-negative rods of urinary and GI tracts (Pseusomonas), Neisseria, some gram-positive organismsSE: GI upset, superinfections, skin rashes, headache, dizziness, less common - tendonitis, tendon rupture (> 60 or taking prednisone), leg cramps, myalgias; prolonged QTcontraindicated in pregnant women and in children because cartilage damageResistance: chromosome-encoded mutation in DNA gyrase, plasmid-mediated resistance, efflux pumps

118
Q

Metronidazole

A

forms free radical toxic metabolites in the bacterial cell that damage DNA; bacteriocidal, antiprotozoalUse: Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes, H. pylori (with PPI and clarithromycin) (GET GAP)SE: disulfiram-like reaction with alcohol; headache, metallic taste

119
Q

Isoniazid

A

decrease synthesis of mycolic acids; bacterial catalase-peroxidase needed to convert INH to active metaboliteUse: Mycobacterium tuberculosis prophylaxisdifferent half-lives in fast vs. slow acetylatorsSE: neurotoxicity, hepatotoxicity. Vit B6 can prevent neurotoxicity, lupus

120
Q

Rifampin

A

inhibits DNA-dept RNA-polymeraseUse: Mycobacterium tuberculosis; delays resistance to dapsone when used in leprosy; meningococcal prophylaxis and chemoprophylaxis in contacts of children with HibSE: minor hepatotoxicity and drug interaction (increase P450), orange body fluids, rapid resistance if used alone

121
Q

Pyrazinamide

A

thought to acidify intracellular environment via conversion to pyrazinoic acidUse: TBSE: hyperuricemia, hepatotoxicity

122
Q

Ethambutol

A

decreases carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltarnsferaseUse: TBSE: optic neuropathy (red-green cold blindness)

123
Q

Amphotericin B

A

binds ergosterol (unique to fungi); form membrane pores that allow leakage of electrolytesUse: serious, systemic mycoses. Cryptococcus, Blastomyces, Coccidioides, Histoplasma, Candida, Mucorsupplement K and Mg because of altered renal tubule permeabilitySE: fever/chills, hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis

124
Q

Nystatin

A

binds ergosterol (unique to fungi); form membrane pores that allow leakage of electrolytes; topical b/c too toxic for systemic useUse: “swish and shallow” for oral candidiasis, topical for diaper rash or vaginal candidiasis

125
Q

Azoles

A

fluconazole, ketoconazole, clotrimazole, miconazole (-nazole)inhibit fungal sterol synthesis, by inhibiting P-450 enzyme that converts lanosterol to ergosterolUse: local and less serious systemic mycosesfluconazole - cryptococcal meningitis in AIDSitraconazole - Blastomyces, Coccidioides, HistoplasmaSE: testosterone synthesis inhibition (gynecomastia), liver dysfunction (inhibit P450)

126
Q

Flucytosine

A

inhibits DNA and RNA biosynthesis by conversion to 5-fluorouracil by cytosine deaminaseUse: systemic fungal infections (Crypto) in combo with amphotericin BSE: bone marrow suppression

127
Q

Caspofungin, micafungin

A

inhibits cell wall synthesis by inhibiting synthesis of beta-glucanUse: invasive aspergillosis, CandidaSE: GI upset, flushing (by histamine release)

128
Q

Terbinafine

A

inhibits the fungal enzyme squalene epozidaseUse: dermatophytoses (onchomycosis - fungal infection of finger or toe nails)SE: abnormal LFTs, visual disturbances

129
Q

Griseofluvin

A

interferes with microtubule function; disrupts mitosis; deposits in keratin-containing tissuesUse: oral treatment of superficial infections, inhibits growth of dermatophytes (tinea, ringworm)SE: teratogenic, carcinogenic, confusion, headache, increase P450 and warfarin metabolism

130
Q

Chloroquine

A

blocks detoxification of heme into hemozoin; heme accumulates and is toxic to plasmodiaUse: plasmodial species other than P. falciparum (resistance due to membrane pump that decreases intracellular concentration)SE: retinopathy

131
Q

Zanamivir, oseltamivir

A

inhibit influenza neuraminidase, decreasing the release of progeny virusUse: treatment and prevention of influenza A and B

132
Q

Ribavirin

A

inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenaseUse: RSV, chronic hepatitis CSE: hemolytic anemia, severe teratogen

133
Q

Acyclovir

A

monophosphotylated by HSV/VZV thymidine kinase; guanosine analog; triphosphate formed by cellular enzymes; preferentially inhibits viral DNA polymerase by chain terminationUse: HSV and VZV; weak against EBV; no activity against CMV; prophylaxis in immunocompromisedfor herpes zoster - famciclovirSE: noneResistance: mutated viral thymidine kinase

134
Q

Ganciclovir

A

5’-monophosphate formed by a CMV viral kinase; guanosine analog; triphosphate formed by cellular kinases; preferentially inhibits viral DNA polymeraseUse: CMV, especially in immunocompromisedvalganciclovir (prodrug) - better oral bioavailabilitySE: leukopenia, neutropenia, thrombocytopenia, reanl toxicityResistance: mutated CMV DNA polymerase or lack of viral kinase

135
Q

Foscarnet

A

viral DNA polymerase inhibitor that binds to the pyrophosphate-binding site of the enzymedoesn’t require activation by viral kinaseUse: CMV retinitis in immunocompromised when ganciclover fails; acyclovir-resistant HSVSE: nephrotoxicityResistance: mutated DNA polymerase

136
Q

Cidofvir

A

preferentially inhibit viral DNA polymerasedoesn’t require phosphorylation by viral kinaseUse: CMV retinitis in immunocompromised; acyclovir-resistant HSVlong half-lifeSE: nephrotoxicity (coadminister with probenecid and IV saline to reduce toxicity)

137
Q

1st gen H1 blockers

A

diphenhydramine, dimenhydrinate, chlorpheniraminereversible inhibitors of H1 histamine receptorsUse: allergy, motion sickness, sleep aidSE: sedation, antimuscarinic, anti-alpha-adrenergic

138
Q

2nd gen H1 blockers

A

loratadine, fexofenadine, desloratadine, cetirizine (-adine)Use: allergySE: less sedating then 1st gen because of decreased entry into CNS

139
Q

Albuterol

A

beta 2 agonistrelaxes bronchial smooth muscle (increase cAMP)Use: acute asthma exacerbation

140
Q

Salmerterol, formoterol

A

beta 2 agonist (increase cAMP)Use: long-acting agents for prophylaxisSE: tremor, arrhythmia

141
Q

Theophylline

A

methylxanthinecauses bronchodilation by inhibiting phosphodiesterase, thereby resulting in increased cAMP due to decreased cAMP hydrolysis; blocks action of adenosine (which promotes bronchoconstriction)Use: asthma, but limited because of narrow TISE: cardiotoxicity, neurotoxicity, blocks action of adenosine; metabolized by P450

142
Q

Ipratropium

A

muscarinic antagonistcompetitive block of muscarinic receptors, preventing bronchoconstrictionUse: asthma, COPDtiotropium = long acting

143
Q

Beclomethasone, fluticasone

A

corticosteroidsinhibit the synthesis of virtually all cytokines; inactivate NF-kB (transcription factor that induces production of TNF-alpha)Use: 1st line for chronic asthma

144
Q

Monrelukast, zafirlukast

A

anti-leukotrieneblock leukotriene receptorsUse: especially good for aspirin-induced asthma

145
Q

Zileuton

A

anti-leukotriene5-lipoxygenase pathway inhibitor; block conversion of arachidonic acid to leukotrienes Use: asthma

146
Q

Omalizumab

A

monoclonal anti-IgE antibodybind mostly unbound antibodiesUse: allergic asthma resistant to inhaled steroids and long-acting beta 2 agonists

147
Q

Bosentan

A

competitively antagonizes endothelin-1 receptors, deceasing pulmonary vascular resistanceUse: pulmonary HTN

148
Q

Dextromethorphan

A

antitussiveantagonizes NMDA glutamate receptors; synthetic codeine analog - mild opioid effect when used in excessnaloxone used for overdoes

149
Q

Pseudoephedrine, phenylephrine

A

sympathomimetic alpha agonist - non-prescription nasal decongestantUse: reduce hyperemia, edema, nasal congestion; open obstructed eustachian tubesSE: HTN; CNS stimulation/anxiety (pseudoephedrine)

150
Q

Ca channel blockers

A

nifedipine, verapamil, diltiazem, amlodipineblock VG L-type Ca channels of cardiac and smooth muscle and thereby reduce muscle contractilityvascular smooth muscle - amlodipine = nifedipine > diltiazem > verapamilheart - verapamil > diltiazem > amlodipine = nifedipineUse: HTN, angina, arrhythmias (not nifedipine), Prinzmetal’s angina, Raynaud’sSE: cardiac depression, AV block, peripheral edema, flushing, dizziness, and constipation

151
Q

Hydralazine

A

increase cGMP –> smooth muscle relaxationvasodilates arterioles > veins; afterload reductionUse: severe HTN (1st line in pregnancy w/ methyldopa), CHFfrequently administered with a beta-blocker to prevent reflex tachycardiaSE: compensatory tachycardia (contraindicated in angina/CAD), fluid retention, nausea, headache, angina, lupus-like syndrome

152
Q

Nitroprusside

A

short acting; increased cGMP via direct release of NOUse: malignant HTNSE: cyanide toxicity (releases cyanide)

153
Q

Fenoldopam

A

D1 receptor agonist - coronary, peripheral, renal, splanchnic vasodilationreduce BP, increase natriuresisUse: malignant HTN

154
Q

Nitroglycerin, isosorbide dinitrate

A

vasodilate by releasing nitric oxide in smooth muscle, causing increase in cGMP and smooth muscle relaxationdilate veins&raquo_space; arteries; decrease preloadUse: angina, pulmonary edemaSE: reflex tachycardia, hypotension, flushing, headache, “Monday disease” in industrial exposure

155
Q

HMG-CoA reductase inhibitors

A

statins(3) decreases LDL, (1) increase HDL, (1) decrease TGsinhibit conversion of HMG-CoA to mevalonate, a cholesterol precursor; increased LDLRSE: hepatotoxicity (increased LFTs), rhabdomyolysis

156
Q

Niacin

A

vitamin B3(2) decrease LDL, (2) increase HDL, (1) decrease TGinhibits lipolysis in adipose tissue; reduces hepatic VLDL secretion into circulation; vasodilatory effectSE: red, flushed face (decreased by aspirin or long-term use), hyperglycemia (acanthosis nigricans), hyperuricemia (gout)

157
Q

Bile acid resins

A

cholestryamine, colestipol, colesevelam (coles-)(2) decrease LDLprevents intestinal reabsorptoin of bile acids; liver must use cholesterol to make moreSE: tastes bad and causes GI discomfort, decreased absorption of fat-soluble vitamins; cholesterol gallstones

158
Q

Cholesterol absorption blockers

A

ezetimibe(2) decrease LDLprevent cholestrol reabsorption at small intestine brush borderSE: rare, increased LFTs, diarrhea

159
Q

Fibrates

A

gemfibrozil, clofibrate, bezafibrate, fenofibrate(1) decrease LDL, (1) increase HDL, (3) decrease TGupregulate LPL –> increase TG clearanceSE: myositis, hepatotoxicity (increased LFTs), cholesterol gallstones

160
Q

Digoxin

A

cardiac glycosidedirect inhibition of Na/K ATPase leads to indirect inhibition of Na/Ca exchanger/antiport; increased intracellular Ca concentration –> positive inotropystimulates vagus nerve –> decreased HRUse: CHF (increased contractility); atrial fibrillarion (decreased conduction at AV node and depression of SA node)SE:cholinergic - nausea, vomiting, diarrhea, blurry yellow visionECG - increased PR, decreased QT, ST scooping, T-wave inversion, arrhythmia, AV blockcan lead to hyperkalemia, poor prognostic indicatorfactors predisposing to toxicity - renal failure (decreased excretion), hypokalemia, quinidine (decreased clearance)Antidote: slowly normalize K, lidocaine, cardiac pacer, anti-digoxin Fab fragments, Mg75% bioavailability, 20-40% protein bound, half-life: 40 hours, urinary excretion

161
Q

Class I General

A

Na channel blockerslocal anestheticsslow or block conduction; decreases slope of phase 0 depolarization and increase threshold for firing in abnormal pacemaker cellsstate dependent - selectively depress tissue that is frequently depolarizedhyperkalemia causes increased toxicity for all class I

162
Q

Class IA

A

quinidine, procainamide, disopyramideincrease AP duration, increase effective refractory period, increase QT interval affect both atrial and ventricular arrhythmias; reentrant and ectopic supraventricular and venricular tachycardiaSE: thrombocytopenia, torsades de pointes due to increased QT intervalquinidine - cinchonism = headache, tinnitusprocainamide - reversible SLE-like syndromedisopyramide - HF

163
Q

Class IB

A

lidocaine, mexiletine, tocainide (maybe phenytoin)decrease AP duration; preferentially affect ischemic or depolarized Purkinje and ventricular tissueUse: acute ventricular arrhythmias (especially post-MI), digitalis-induced arrhythmiasSE: local anesthetic, CNS stimulation/depression, CV depression

164
Q

Class IC

A

flecainide, propafenoneno effect on AP durationUse: ventricular tachycardias that progress to VF and in intractable SVT; usually only last resort in refractory tachyarrhythmiascontraindicated in structural heart disease and post-MISE: proarrhythmic, especially post-MI (contraindicated); significantly prolongs refractory period in AV node

165
Q

Class II

A

beta-blocker: metroprolol, propranolol, esmolol, atenolol, timololdecreases SA and AV nodal activity by decreasing cAMP, decreased Ca currents; suppress abnormal pacemakers by decreasing slope of phase 4Use: ventricular tachycardia, SVT, slowing ventricular rate during atrial fibrillation and atrial flutterSE: impotence, exacerbation of asthma, CV effects (bradycardia, AV block, CHF), CNS effects (sedation sleep alteration)may mask signs of hypoglycemiametoprolol can cause dyslipidemia; treat overdose with glucagonpropranolol - exacerbate vasospasm in Prinzmetal’s angina

166
Q

Class III

A

K channel blocker: amiodarone, ibutilide, dofetilide sotalolincrease AP duration, increase ERP, increase QT intervalUse: when other antirrhythmics failSE:sotalol - torsades de pointes, excessive beta blockibutilide - torsadesamiodarone - pulmonary fibrosis, hepatotoxicity, hypo/hyperthyroid (check PFTs, LFTs, TFTs), corneal and skin (blue/gray) deposits, neurological effects, constipation, CV effects (bradycardia, heart block, CHF)

167
Q

Class IV

A

Ca channel blockers - verapamil, diltiazemdecrease conduction velocity, increase ERP, increase PR intervalUse: prevention of nodal arrhythmias (SVT)SE: constipation, flushing, edema, CV effects (CHF, AV block, sinus node depression)

168
Q

Adenosine

A

increase K out of cell –> hyperpolarizing the cell and decreasing CaUse: 1st line for diagnosing and abolishing supraventricular tachycardiavery short acting (~15 sec)SE: flushing, hypotension, chest paineffects blocked by caffeine and theophylline

169
Q

Mg

A

effective in torsades de pointes and digoxin toxicity

170
Q

Aspirin

A

NSAIDirreversibly inhibit COX-1 and COX-2 by acetylation, which decreases synthesis of both TXA2 and prostagladinsincreases bleeding time; no effect on PT, PTTUse: low dose (< 300 mg/day) - decrease platelet aggregationintermediate dose (300-2400) - antipyretic and analgesichigh dose (2400-4000): anti-inflammatorySE: gastric ulceration, tinnitus (CN VIII), acute renal failure (chronic use), interstitial nephritis, upper GI bleeding, Reye’s syndrome; respiratory alkalosis

171
Q

NSAIDs

A

ibuprofen, naproxen, idomethacin, ketorolac, diclofenacreversibly inhibit COX-1 and COX-2 –> block PG synthesisUse: antipyretic, analgesic, anti-inflammatory; indomethacin to close PDASE: interstitial nephritis, gastric ulcer, renal ischemia

172
Q

Celecoxib

A

COX-2 inhibitorsreversibly inhibit COX-2 (spares COX-1 = maintains gastric mucosa and spares platelet function)Use: RA, osteoarthritis; patients with gastritis or ulcersSE: increases risk of thrombosis, sulfa allergy

173
Q

Acetaminophen

A

reversibly inhibits COX, mostly in CNS; inactivated peripherallyUse: antipyretic, analgesic, but not anti-inflammatory, use instead of aspirin in childrenSE: overdose produces hepatic necrosis; depletes glutathioneN-acetylcysteine is antidote - regenerates glutathione

174
Q

Bisphosphaonates

A

alendronate (-dronates)pyrophosphate analongs; bind hydroxyapatite in bone, inhibiting osteoclast activityUse: osteoporosis, hypercalcemia, Paget’s disease of boneSE: corrosive esophagitis, osteonecrosis of the jaw

175
Q

Allopurinol

A

inhibits xanthine oxidase, decrease conversion of xanthine to uric acidUse: chronic gout, tumor lysis syndromeincreases concentrations of azathioprine and 6-MPdo not give salicylates

176
Q

Febuxostat

A

inhibits xanthine oxidaseUse: chronic gout

177
Q

Probenecid

A

inhibits reabsorption of uric acid in PCTUse: chronic goutalso inhibits secretion of penicillin

178
Q

Colchicine

A

binds and stabilizes tubulin to inhibit polymerization, impairing leukocyte chemotaxis and degranulationUse: chronic goutSE: GI; avoid in elderly or renal problems

179
Q

Etanercept

A

fusion protein (receptor for TNF-alpha + IgG Fc), produced by recombinant DNATNF decoy receptorUse: RA, psoriasis, ankylosing spondylitisSE: reactivation of latent TB

180
Q

Infliximab, adalimumab

A

anti-TNF-alpha monoclonal antibodyUse: Crohn’s disease, RA, ankylosing spondylitis, psoriasisSE: reactivation of latent TB

181
Q

Rasburicase

A

recombinant version of urate oxidaseUse: tumor lysis syndrome

182
Q

Haparin

A

cofactor for the activation of antithrombin, decrease thrombin, decrease factor Xa. short half-lifeUse: immediate anticogulation for pulmonary embolism, acute coronary syndrome, MI, DVTused during pregnancy (doesn’t cross placenta); follow PTTSE: bleeding, thrombocytopenia (HIT), osteoporosis, drug-drug interactionsrapid reversal with proamine sulfate (positive charged molecule that binds negatively charged heparin)LMW haparins act more on Factor Xa, longer actingHIT - development of IgG antibodies against haparin bound platelet factor 4 –> complex activates platelets

183
Q

Lepirudin, bivalirudin

A

derivatives of hirudin, anticoagulant used by leechesinhibit thrombinused as alternative to haparin for patients with HIT

184
Q

Warfarin (coumadin)

A

interferes with normal synthesis and gamma-carboxylation of vitamin K-dependent clotting factors II, VII, IX, and X, protein C and Smetabolized by P450; monitor PT; long half-lifeUse: chronic anticoagulant (after STEMI, venous thromboembolism prophylaxis, prevention of stroke in atrial fibrillation)don’t use in pregnant womenSE: bleeding, teratogenic, skin/tissues necrosis, drug-drug interactionsreversal - vitamin K; rapid - fresh frozen plasma

185
Q

Thromobolytics

A

alteplase (tPA), reteplase (rPA), tenecteplase (TNK-tPA) = fibrin specificstreptokinase = non-specificdirectly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots; increases PT, PTT, no change in platelet countUse: early MI, early ischemic stroke, direct thrombolysis of PESE: bleedingcontraindicated in patients with active bleeding, history of intracranial bleeding, recent surgery, known bleeding diathesis, severe HTNtreat toxicity with aminocaproic acid (inhibitor of fibrinolysis)

186
Q

ADP receptor inhibitor

A

clopidogrel, ticlopidine, prasugrel, ticagrelorinhibit platelet aggregation by irreversible blocking ADP receptor; inhibit fibrinogen binding by preeventing glycoprotein IIb/IIIa from binding fibrinogenUse: acute coronary syndrome, coronary stenting, decreased, decreased incidence of recurrence of thrombotic strokeSE: neutropenia (ticlopidine)

187
Q

Cliostazol, dipyridamole

A

prosphodiesterase II inhibitor; increase cAMP in platelets, thus inhibiting platelet aggregation; vasodilationUse: intermittent claudication, coronary vasodilation, prevention of stroke or TIA (combined with aspirin), angina prophylaxisSE: nausea, headache, facial flushing, hypotension, abdominal pain

188
Q

GP IIb/IIIa inhibitors

A

abciximab, eptifibatide, tirofibanbind to glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregationUse: acute coronary syndromes, percutaneous transluminal coronary angioplastySE: bleeding, thrombocytopenia

189
Q

Methotrexate (MTX)

A

antimetabolite (S phase specific)folic acid analog that inhibits dihydrofolate reductase –> decreased dTMP –> decreased DNA and protein synthesisUse: luekemias, lymphomas, choriocarcinoma, sarcomas, abortion, ectopic pregnancy, RA, psoriasisSE: myelosuppression (reversible with leucovorin (folinic acid)); macrovesicular fatty change in liver; mucositis, teratogenic

190
Q

5-fluorouracil (5-FU)

A

pyrimidine analog bioactivated to 5F-dUMP which covalently complexes folic acid; complex inhibits thymidylate synthase –> decreases dTMP –> decreased DNA and protein synthesisUse: colon cancer, basal cell carcinoma (topical)SE: myelosuppression (rescue with thymidine), photosensitivity

191
Q

Cytarabine (arabinofuranosyl cytidine)

A

pyrimidine analog –> inhibition of DNA polymeraseUse: leukemia, lymphomasSE: leukopenia, thrombocytopenia, megaloblastic anemia

192
Q

Azathioprine, 6-mercaptopurine (6-MP), 6 thioguanine (6-TG)

A

purine (thiol) analogs –> decreased de novo purine synthesis; activated by HGPRTUse: leukemiasSE: bone marrow, GI, liver, increased toxicity with allopurinol (metabolized by xanthine oxidase)

193
Q

Dactinomycin

A

intercalates in DNAUse: Wilm’s tumor, Ewing’s sarcoma, rhabdomyosarcoma; childhood tumorsSE: myelosuppression

194
Q

Doxorubicin, daunorubicin

A

generate free radicals; noncovalently intercalate in DNA –> breaks in DNA –> decreased replicationUse: solid tumors, leukemias, lymphomasSE: cardiotoxicity (dilated cardiomyopathy), myelosuppression, alopecia; toxic after extravasationuse dexrazoxane (iron chelating agent), used to prevent cardiotoxicity

195
Q

Bleomycin

A

induces free radical formation, which causes breaks in DNA strands (act in G2)Use: testicular cancer, Hodgkin’s lymphomaSE: pulmonary fibrosis, skin changes, minimal myelosuppression

196
Q

Cyclophosphamide, ifosfamide

A

alkylating agentscovalently X-linked (interstrand) DNA at guanine N-7; reactivated by liverUse: solid tumors, leukemia, lymphomas, and some brain cancersSE: myelosuppression; hemorrhagic cystitis (prevented by mensa - thiol group binds toxic metabolite)

197
Q

Nitrosoureas

A

carmustine, lomustine, semustine, streptozocin (-stine)alkylating agentsrequires bioactivation; cross BBB –> CNSUse: brian tumors (GBM)SE: CNS toxicity (dizziness, ataxia)

198
Q

Busulfan

A

alkylates DNAUse: CML, also used to ablate patient’s bone marrow before bone marrow transplantationSE: pulmonary fibrosis, hyperpigmentation

199
Q

Vincristine, vinblastine

A

alkaloids that bind to tubulin in M phase and block polymerization of microtubules so that mitotic spindle cannot form (work in M phase)Use: solid tumors, leukemias, lymphomasSE: vincristine - neurotoxicity, paralytic ileusvinblastine - blast bone marrow (suppression)

200
Q

Paclitaxel, other taxols

A

hyperstabilizes polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cant occur)Use: ovarian, breast carcinomasSE: myelosuppression, hypersensitivity

201
Q

Cisplatin, carboplatin

A

cross-link DNAUse: testicular, bladder, ovary and lung carcinomasSE: nephrotocity, acoustic nerve damage (prevent with amifostine - free radical scavenger - and chloride diuresis

202
Q

Etoposide, teniposide

A

inhibit topoisomerase II –> increased DNA degradationact in S, G2Use: solid tumors, leukemias, lymphomasSE: myelosuppression, GI irritation, alopecia

203
Q

Hydroxyrea

A

inhibits ribonucleotide reductase –> decreases DNA synthesis (S-phase specific)Use: melanoma, CML, sickle cell disease (increase HbF)SE: bone marrow suppression, GI upset

204
Q

Prednisone, prednisolone

A

may trigger apoptosis; may even work on nondividing cellsUse: CLL, non-Hodgkin’s lymphoma (part of combination therapy), immmunosuppresionSE: Cushing-like symptoms; immunosuppression, cataracts, acne, osteoporosis, HTN, peptic ulcers, hyperglycemia, psychosis

205
Q

Tamoxifen, raloxifene

A

SERMs - receptor antagonists in breast and agonist in bone; block the binding of estrogen to estrogen receptor-positive cellsUse: breast cancer treatment and prevention; prevent osteoporosisSE:tamoxifen - partial agonist in endometrium, which increases the risk of endometrial cancer; “hot flashes”ralozifene - no increase in endometrial carcinoma b/c is an endometrial antagonist

206
Q

Trastuzumab (herceptin)

A

monoclonal antibody against HER-2 (tyrosine kinase); antibody-dependent cytotoxicityUse: HER-2-positive breast cancerSE: cardiotoxicity

207
Q

Imatinib (gleevec)

A

Philadelphia chromosome bcr-abl tyrosine kinase inhibitorUse: CML, GI stromal tumorsSE: fluid retention

208
Q

Rituximab

A

monoclonal antibody against CD20, which is found on most B-cell neoplasmsUse: non-Hodgkin’s lymphoma, RA (with MTX)

209
Q

Vemurafenib

A

small molecule inhibitor of forms of B-Raf kinase with the V600E mutationUse: metastaic melanoma

210
Q

Bevacizumab

A

monoclonal antibody against VEGF; inhibits angiogenesisUse: solid tumors

211
Q

Leuprolide

A

GnRH analog with agonist properties when used in pulsatile fashionantagonist properties when used in continuous fashionUse: infertility (pulsatile), prostate cancer (continuous with flutamide), uterine fibroids (continuous), precocious puberty (continuous)SE: antiandrogen, nausea, vomiting

212
Q

Testosterone, methyltestosterone

A

agonist at androgen receptorsUse: treats hypogonadism and promotes development of secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injurySE: cause masculinization in females; reduces intratesticular testosterone in males by inhibiting release of LH (gonadal atrophy); premature closure of epiphyseal plate; increase LDL, decrease HDL

213
Q

Finasteride

A

antiandrogen5alpha-reductase inhibitorUse: BPH; male pattern baldness

214
Q

Flutamide

A

antiandrogennonsteroidal competitive inhibitor of androgens at the testosterone receptorUse: prostate carcinoma

215
Q

Ketoconazole

A

antiandrogeninhibits steroid synthesis (inhibits 17,20-desmolase)Use: PCOS - to prevent hirsutismSE: gynecomastia, amenorrhea

216
Q

Spironolactone

A

antiandrogeninhibits steroid bindingUse: PCOS - to prevent hirsutismSE: gynecomastia, amenorrhea

217
Q

Estrogens

A

ethyl estradiol, DES, mestranolbind estrogen receptorsUse: hypogonadism or ovarian failure, mentral abnormalities, HRT in postmenopausal women; use in men with andeogen-dependent prostate cancerSE: increase risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina (DES), increase risk of thrombicontraindication - ER-postive breast cancer, history of DVTs

218
Q

Clomiphene

A

SERMpartial agonist at estrogen receptors in hypothalamus; prevent normal feedback inhibition and increase release of LH and FSH –> ovulationUse: infertility, PCOSSE: hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances

219
Q

Tamoxifen

A

SERMantagonist on breast tissueUse: treat and prevent recurrence of ER-positive breast cancer

220
Q

Raloxifene

A

SERMagonist on bone; reduces resorption of boneUse: osteoporosis

221
Q

HRT

A

Use: relief or prevention of menopausal symptoms and osteoporosisunopposed ERT increases the risk of endometrial cancer, so progesterone is addedpossible increased CV risk

222
Q

Anastrozole/exemestane

A

aromatase inhibitors used in postmenopausal women with breast cancer

223
Q

Progestins

A

bind progesterone receptors, reduce growth and increase vascularization of endometriumUse: oral contraceptives; endometrial cancer, abnormal uterine bleeding

224
Q

Mifepristone

A

competitive inhibitor of progestins at progesterone receptorsUse: termination of pregnancy; administered with misoprostolSE: heavy bleeding, GI effects, abdominal pain

225
Q

Oral contraception

A

FILL IN

226
Q

Terbutaline

A

beta 2 agonist that relaxes the uterus; reduces premature uterine contractions

227
Q

Tamsulosin

A

alpha 1 antagonist (selective for 1A,D in prostate vs 1B vascular)inhibit smooth muscle contractionUse: BPH

228
Q

Silenafil, vardenafil

A

inhibit phosphodiesterase 5, causing increase cGMP, smooth muscle relaxation in corpus cavernosum, increased blood flow and penile erectionUse: EDSE: headache, flushing, dyspepsia, impaired blue-green color visionrisk of life-threatening hypotension in patients taking nitrates

229
Q

Danazol

A

synthetic androgen that acts as partial agonist at androgen receptorsUse: endometriosis and hereditary angioendemaSE: weight gain, edema acne, hirsutism, masculinization, decreased HDL levels, hepatotoxicity

First Aid Pharmacology (1 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions