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Pharm_Part2 Flashcards

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USMLE® Step 1 flashcards
1
Q

1st generation H1 blockers

A

Diphenhydramine, dimenhydrinate, chlopheniramine Clinical uses: Allergy, motion sickness, sleep aid Toxicity: Sedation, antimuscarinic, anti-α-adrenergic

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2
Q

2nd generation H1 blockers

A

Loratadine, fexofenadine, desloratadine, cetirizine (-adine) Clinical uses: Allergy Toxicity: Far less sedating than 1st generation because of ↓ entry into CNS

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3
Q

ACE inhibitors: Names

A

Captopril, enalapril, lisinopril (-pril)

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4
Q

Acetazolamide

A

Mechanism: Carbonic anhydrase inhibitor. Causes self-limited NaHCO3 diuresis and reduction in total-body HCO3- stores Clinical use: Glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness Toxicity: Hyperchloremic metabolic acidosis, neuropathy, NH3 toxicity, sulfa allergy

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5
Q

Adalimumab

A

TNF-α inhibitors Mechanism: Anti-TNF antibody Clinical use: Rheumatoid arthritis, psoriasis, ankylosing spondylitis

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6
Q

Advantages (5) & Disadvantages (4) of Oral contraception

A

Advantages: Reliable (<1% failure); ↓ risk of endometrial and ovarian cancer; ↓ incidence of ectopic pregnancy; ↓ pelvic infections; regulation of menses Disadvantages: Taken daily; No protection against STDs; ↑ triglycerides; Depression, weight gain, nausea, hypertension; Hypercoagulable state

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7
Q

Albuterol

A

Asthma drug, relaxes bronchial smooth muscle (β2). Use during acute exacerbation.

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8
Q

Allopurinol

A

Gout drug, chronic gout. Inhibits xanthine oxidase. ↓ conversion of xanthine to uric acid. Also used in lymphoma and leukemia to prevent tumor lysis associated urate nephropathy. ↑ concentrations of azathioprine and 6-MP (both normally metabolized by xanthine oxidase)

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9
Q

Alzheimer’s drugs: Two types

A

Memantine: NMDA receptor antagonist Donepezil: Acetylcholinesterase inhibitors

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10
Q

Anastrozole / exemestane

A

Aromatase inhibitors used in postmenopausal women with breast cancer

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11
Q

Anesthetics - General principles: Drug with ↓ solubility in blood

A

rapid induction and recovery time

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12
Q

Anesthetics - General principles: Drugs with ↑ solubility in lipids

A

↑potency = 1/MAC

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13
Q

Antidote: Benzodiazepines

A

Flumazenil (competitive antagonist at GABA benzodiazepine receptor)

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14
Q

Antidote: Neuromuscular blocking drugs

A

Neostigmine, edrophonium, and other cholinesterase inhibitors

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15
Q

Antidote: Tricyclic antidepressants

A

NaHCO3 for CV toxicity

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16
Q

Antipsychotic with low potency

A

Thioridazine, chlorpromazine - non neurologic side effects (anticholinergic, antihistamine, and α blockade effects)

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17
Q

Antipsychotics (neuroleptics): Names

A

Haloperidol + “-azine”s

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18
Q

Antipsychotics with high potency

A

Haloperidol, trifluoperazine, fluphenazine - neurologic side effects (extrapyramidal symptoms).

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19
Q

Arachidonic acid products

A

Lipoxygenase pathway yields Leukotrienes LTB4 is a neutrophil chemotactic agent LTC4, D4, E4 function in bronchoconstriction, vasoconstriction, contraction of smooth muscle, and ↑ vascular permeability PGI2 inhibits platelet aggregation and promotes vasodilation

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20
Q

Asthma drugs (7)

A

①non-specific β-agonists: Isoproterenol ②β2-agonists: Albuterol, Salmeterol ③Methylxanthines: Theophylline ④Muscarinic antagonists: Ipratropium ⑤Cromolyn ⑥Corticosteroids: Beclomethasone, prednisone ⑦Antileukotrienes: Zileuton; Zafirlukast / Montelukast

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21
Q

Atypical antipsychotics: Names

A

Olanzapine, clozapine, quetiapine, risperidone, aripiprazole, ziprasidone (-apine, -idone, aripiprazole)

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22
Q

Beclomethasone / prednisone

A

Asthma drug, inhibit the synthesis of virtually all cytokines. Inactivate NF-kB, the transcription factor that induces the production of TNF-α, among other inflammatory agents. 1st-line therapy for chronic asthma.

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23
Q

Biphosphonates (-dronate)

A

Mechanism: Inhibit osteoclast activity; reduce both formation and resorption of hydroxyapatite Clinical use: Malignancy-associated hypercalcemia, Paget’s disease of the bone, post menopausal osteoporosis Toxicity: Corrosive esophagitis (except zoledronate), nausea, diarrhea, osteonecrosis of the jaw

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24
Q

Bosentan

A

Used to treat pulmonary hypertension. Competitively antagonizes endothelin-1 receptors, decreasing pulmonary vascular resistance.

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25
Q

Bupropion

A

Also used for smoking cessation. ↑ NE and dopamine via unknown mechanism. Toxicity: stimulant effects (tachycardia, insomnia), headache, seizure in bulimic patients. No sexual side effects.

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26
Q

Butorphanol

A

Mechanism: Partial agonist at opioid mu receptors, agonist at kappa receptors. Clinical use: Pain; causes less respiratory depression than full agonists Toxicity: Causes withdraw if on full opioid agonist

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27
Q

Clinical use: ACE inhibitors

A

Hypertension, CHF, diabetic renal disease

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28
Q

Clinical use: Acetaminophen

A

Antipyretic, analgesic, but lacking anti-inflammatory properties. Used instead of aspirin to prevent Reye’s syndrome in children with viral infection.

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29
Q

Clinical use: Antipsychotics

A

Schizophrenia (primarily positive symptoms), psychosis, acute mania, Tourette’s syndrome

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30
Q

Clinical use: Aspirin

A

Low dose (<300 mg/day): ↓ platelet aggregation. Intermediate dose (300-2400 mg/day): antipyretic and analgesic High dose: (2400-4000 mg/day): anti-inflammatory

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31
Q

Clinical use: Atypical antipsychotics

A

Schizophrenia - both positive and negative symptoms

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32
Q

Clinical use: Barbiturates

A

Sedative for anxiety, seizures, insomnia

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33
Q

Clinical use: Benzodiazepines

A

Anxiety, spasticity, status epilepticus, detoxification (especially alcohol withdrawal-DTs), night terrors, sleepwalking, general anesthetic (amnesia, muscle relaxation), hypnotic (insomnia)

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34
Q

Clinical use: Buspirone

A

Generalized anxiety disorder. Does not cause sedation, addiction, or tolerance. Does not interact with alcohol (vs. barbiturates, benzodiazepines)

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35
Q

Clinical use: Clomipramine

A

OCD

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36
Q

Clinical use: COX-2 inhibitors (celecoxib)

A

Rheumatoid and osteoarthritis; patients with gastritis or ulcers

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37
Q

Clinical use: Duloxetine

A

Depression, diabetic peripheral neuropathy, duloxetine has greater effect on NE

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38
Q

Clinical use: Imipramine

A

Bed wetting

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39
Q

Clinical use: K+-sparing diuretics

A

Hyperaldosteronism, K+ depletion, CHF

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40
Q

Clinical use: Lithium

A

Mood stabilizer for bipolar disorder; blocks relapse and acute manic events. Also SIADH.

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41
Q

Clinical use: Monoamine oxidase (MAO) inhibitors

A

Atypical depression, anxiety, hypochondiasis

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42
Q

Clinical use: Nonbenzodiazepine hypnotics

A

Insomnia (失眠)

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43
Q

Clinical use: Olanzapine

A

OCD, anxiety disorder, depression, mania, Tourette’s syndrome

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44
Q

Clinical use: Phenytoin

A

Tonic-clonic seizures. Also a class IB antiarrhythmic.

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45
Q

Clinical use: Sildenafil / vardenafil

A

Erectile dysfunction

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46
Q

Clinical use: SSRIs

A

Depression, OCD, bulimia, social phobias

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47
Q

Clinical use: Tricyclic antidepressants

A

Major depression, fibromyalgia

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48
Q

Clinical use: Venlafaxine

A

Depression, generalized anxiety disorder

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49
Q

Clomiphene

A

Estrogen partial agonist, partial agonist at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and ↑ release of LH and FSH from pituitary, which stimulates ovulation. Used to treat infertility and PCOS. May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, and visual disturbances

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50
Q

CNS stimulants

A

Methylphenidate, dextroamphetamine, mixed amphetamine salts Mechanism: ↑ catecholamines at the synaptic cleft, especially NE and dopamine Clinical use: ADHD, narcolepsy, appetite control

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51
Q

Colchicine

A

Gout drug, acute gout (with NSAIDs). Binds and stabilizes tubulin to inhibit polymerization, impairing leukocyte chemotaxis and degranulation. GI side effects, especially if given orally. (Note: indomethacin is less toxic, also used in acute gout)

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52
Q

Complications: Succinylcholine

A

Hypercalcemia, hyperkalemia, hyperthermia

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53
Q

Contraindication: Barbiturates

A

in porphyria

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54
Q

Contraindication: Mannitol

A

Anuria, CHF

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55
Q

Contraindication: Monoamine oxidase (MAO) inhibitors

A

with SSRI or meperidine (to prevent serotonin syndrome)

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56
Q

Contraindication: Oral contraception

A

smokers > 35 years of age (↑ risk of cardiovascular events), patients with history of thromboembolism and stroke or history of estrogen-dependent tumor

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57
Q

Contraindications: Estrogens

A

ER-positive breast cancer, history of DVTs

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58
Q

Cromolyn

A

Asthma drug, prevents release of mediators from mast cells. Effective only for the prophylaxis of asthma. Not effective during an acute asthmatic attack. Toxicity is rare.

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59
Q

Dantrolene

A

Used in the treatment of malignant hyperthermia, which is caused by inhalation anesthetics (except N2O) and succinylcholine. Also used to treat neuroleptic malignant syndrome (a toxicity of antipsychotic drugs) MOA: prevents the release of Ca2+ from the sarcoplasmic reticulum of skeletal muscle

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60
Q

Dinoprostone

A

PGE2 analog causing cervical dilation and uterine contraction, inducing labor

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61
Q

Diuretics: electrolyte changes: Blood pH

A

↓(acidemia): Carbonic anhydrase inhibitors ↑(alkalemia): Loop diuretics and thiazides

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62
Q

Diuretics: electrolyte changes: Details

A

Check FA2011 page475, very important mechanisms!!!

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63
Q

Diuretics: electrolyte changes: Urine Ca2+

A

↑Loop diuretics ↓Thiazides

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64
Q

Diuretics: electrolyte changes: Urine K+

A

↑ in all except K+-sparing diuretics. Serum K+ may ↓ as a result.

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65
Q

Diuretics: electrolyte changes: Urine NaCl

A

↑ in all diuretics. Serum NaCl may ↓ as a result.

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66
Q

DOC: 1st line for acute Status epilepsy

A

Benzodiazepines

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67
Q

DOC: 1st line for seizures of eclampsia

A

MgSO4, benzodiazepines

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68
Q

DOC: 1st line for Status epilepsy prophylaxis

A

Phenytoin

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69
Q

DOC: 1st line for trigeminal neuralgia

A

Carbamazepine

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70
Q

DOC: 1st line of epilepsy drugs in pregnant women, children

A

Phenobarbital

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71
Q

DOC: Acute pulmonary edema, maintenance programs for addicts

A

Methadone

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72
Q

DOC: ADHD

A

Methylphenidate (Ritalin), Amphetamines (Dexedrine)

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73
Q

DOC: Alcohol withdrawal

A

Benzodiazepines

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74
Q

DOC: Anorexia/bulimia

A

SSRI

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75
Q

DOC: Anxiety

A

Benzodiazepines, Buspirone, SSRI

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76
Q

DOC: Atypical depression

A

MAO inhibitors, SSRIs

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77
Q

DOC: Bipolar disorder

A

“Mood stabilizers”: Lithium, Valproic acid, Carbamazepine Atypical antipsychotics

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78
Q

DOC: Closure of a PDA

A

Indomethacin

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79
Q

DOC: Depression

A

SSRIs, SNRIs, TCAs

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80
Q

DOC: Depression with insomnia

A

Mirtazapine

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81
Q

DOC: Diarrhea

A

Loperamide / Diphenoxylate

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82
Q

DOC: Essential or familial tremors

A

β-blockers, e.g., propranolol

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83
Q

DOC: Obsessive-compulsive disorder

A

SSRIs, Clomipramine

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84
Q

DOC: Pain, cough suppression

A

Dextromethorphan

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85
Q

DOC: Panic disorder

A

SSRIs, TCAs, Benzodiazepines

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86
Q

DOC: Polycystic ovarian syndrome (to prevent hirsutism)

A

Ketoconazole and spironolactone

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87
Q

DOC: PTSD

A

SSRIs

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88
Q

DOC: Schizophrenia

A

Antipsychotics

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89
Q

DOC: Serotonin syndrome

A

Cyproheptadine, 5-HT2 receptor antagonist

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90
Q

DOC: Social phobias

A

SSRIs

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91
Q

DOC: Tourette’s syndrome

A

Antipsychotics (haloperidol)

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92
Q

Donepezil

A

Alzheimer’s drugs, also galantamine, rivastigmine. Mechanism: Acetylcholinesterase inhibitors. Toxicity: Nausea, dizziness, insomnia

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93
Q

Drug class: Amiodarone

A

Class III antiarrhythmics

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94
Q

Drug class: Amitriptyline

A

Tricyclic antidepressants

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95
Q

Drug class: Amoxapine

A

Tricyclic antidepressants

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96
Q

Drug class: Bretylium

A

Class III antiarrhythmics

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97
Q

Drug class: Chlordiazepoxide

A

Benzodiazepines

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98
Q

Drug class: Citalopram

A

SSRIs

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99
Q

Drug class: Clomipramine

A

Tricyclic antidepressants

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100
Q

Drug class: Desipramine

A

Tricyclic antidepressants

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101
Q

Drug class: Dextromethorphan

A

Opioid analgesics for cough

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102
Q

Drug class: Diatiazem

A

Calcium channel blockers

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103
Q

Drug class: diaze-, -pam, -lam

A

Benzodiazepines

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104
Q

Drug class: Diltiazem

A

Class IV antiarrhythmics

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105
Q

Drug class: Disopyramide

A

Class IA antiarrhythmics

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106
Q

Drug class: Dofetilide

A

Class III antiarrhythmics

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107
Q

Drug class: Doxepin

A

Tricyclic antidepressants

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108
Q

Drug class: Duloxetine

A

SNRIs

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109
Q

Drug class: Encainide

A

Class IC antiarrhythmics

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110
Q

Drug class: eszopiclone

A

Nonbenzodiazepine hypnotics

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111
Q

Drug class: Flecainide

A

Class IC antiarrhythmics

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112
Q

Drug class: Fluoxetine

A

SSRIs

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113
Q

Drug class: Ibutilide

A

Class III antiarrhythmics

114
Q

Drug class: Imipramine

A

Tricyclic antidepressants

115
Q

Drug class: Isocarboxazid

A

MAOI

116
Q

Drug class: Ketorolac

A

NSAIDs

117
Q

Drug class: Lidocaine

A

Class IB antiarrhythmics

118
Q

Drug class: methimazole

A

Hyperthyroidism drug

119
Q

Drug class: Mexiletine

A

Class IB antiarrhythmics

120
Q

Drug class: Naproxen

A

NSAIDs

121
Q

Drug class: Nifedipine

A

Calcium channel blockers

122
Q

Drug class: Nortriptyline

A

Tricyclic antidepressants

123
Q

Drug class: Paroxetine

A

SSRIs

124
Q

Drug class: Phenelzine

A

MAOI

125
Q

Drug class: Procainamide

A

Class IA antiarrhythmics

126
Q

Drug class: Propafenone

A

Class IC antiarrhythmics

127
Q

Drug class: Quinidine

A

Class IA antiarrhythmics

128
Q

Drug class: Selegiline

A

MAOI, selective MAO-B inhibitor

129
Q

Drug class: Sertraline

A

SSRIs

130
Q

Drug class: Sotalol

A

Class III antiarrhythmics

131
Q

Drug class: Thiopental

A

Barbiturates, used for induction of anesthesia

132
Q

Drug class: Thiopentals

A

Barbiturates

133
Q

Drug class: Tocainide

A

Class IB antiarrhythmics

134
Q

Drug class: Tranylcypromine

A

MAOI

135
Q

Drug class: Venlafaxine

A

SNRIs

136
Q

Drug class: Verapamil

A

Calcium channel blockers

137
Q

Drug class: Zaleplon

A

Nonbenzodiazepine hypnotics

138
Q

Drug class: Zolpidem (Ambien)

A

Nonbenzodiazepine hypnotics

139
Q

Drug use: Pirenzepine

A

Muscarinic antagonist

140
Q

Drug use: Propantheline

A

Muscarinic antagonists

141
Q

Epilepsy drug toxicities: Diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis, induction of cytochrome P-450, SIADH, Stevens-Johnson syndrome

A

Carbamazepine

142
Q

Epilepsy drug toxicities: Ethosuximide

A

EFGH - Ethosuximide, Fatigue, GI, Headache

143
Q

Epilepsy drug toxicities: GI distress, fatigue, headache, urticaria, Stevens-Johnson syndrome

A

Ethosuximide

144
Q

Epilepsy drug toxicities: GI distress, rare but fetal hepatotoxicity (measure LFTs), neural tube defects in fetus (spina bifida), tremor, weight gain. Contraindicated in pregnancy.

A

Valproic acid

145
Q

Epilepsy drug toxicities: Nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, megaloblastic anemia, teratogenesis (fetal hydantoin syndrome), SLE-like syndrome, induction of cytochrome P-450

A

Phenytoin

146
Q

Epilepsy drug toxicities: Sedation, tolerance, dependence

A

Benzodiazepines

147
Q

Epilepsy drug toxicities: Sedation, tolerance, dependence, induction of cytochrome P-450

A

Phenobarbital

148
Q

Estrogens (ethinyl estradiol, DES, mestranol)

A

Mechanism: Bind estrogen receptors Clinical use: Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women; use in men with androgen-dependent prostate cancer. Toxicity: ↑ risk of endometrial cancer, bleeding in postmenopausal women, ↑ risk of thrombi

149
Q

Etanercept

A

TNF-α inhibitors Mechanism: Recombinant form of human TNF that binds TNF (Decoy receptor) Clinical use: Rheumatoid arthritis, psoriasis, ankylosing spondylitis

150
Q

Ethacrynic acid

A

Mechanism: Phenoxyacetic acid dericative (NOT a sulfonamide). Essentially same action as furosemide. Clinical use: Diuresis in patients allergic to sulfa drugs Toxicity: Similar to furosemide; can be used in hyperuricemia, acute gout (never used to treat gout)

151
Q

Evolution of EPS side effects

A

4h acute dystonia (muscle spasm, stiffness, oculogyric crisis) 4d akinesia (parkinsonian symptoms) 4wk akathisia (restlessness) 4mo tardive dyskinesia

152
Q

Expectorants (2)

A

Guaifenesin: Expectorant - removes excess sputum; does not suppress cough reflex. N-acetylcysteine: Mucolytic - can loosen mucous plugs in CF patients. Also used as an antidote for acetaminophen overdose.

153
Q

Fetal hydantoin syndrome

A

Intrauterine growth restriction with microcephaly and develop minor dysmorphic craniofacial features and limb defects including hypoplastic nails and distal phalanges (birth defects).

154
Q

Finasteride (Propecia)

A

a 5α-reductase inhibitor (↓ conversion of testosterone to dihydrotestosterone). Useful in BPH. Also promotes hair growth - used to treat male-pattern baldness

155
Q

Flutamide

A

a nonsteroidal competitive inhibitor of androgens at the testosterone receptor. Used in prostate carcinoma.

156
Q

Furosemide

A

Mechanism: Sulfonamide loop diuretic. Inhibits cotransport system (Na+, K+, 2Cl-) of thick ascending limb of loop of Henle. Abolishes hypertonicity of medulla, preventing concentration of urine. ↑Ca2+ excretion Clinical use: Edematous states (CHF, cirrhosis, nephrotic syndrome, pulmonary edema), hypertension, hypercalcemia

157
Q

Glaucoma drugs: Cholinomimetics

A

Direct: Pilocarpine, carbachol Indirect: Physostigmine, echothiophate

158
Q

Glaucoma drugs: Diuretics

A

Acetazolamide, dorzolamide (-zolamide)

159
Q

Glaucoma drugs: Emergencies

A

Pilocarpine

160
Q

Glaucoma drugs: Prostaglandin

A

Latanoprost (PGF2α)

161
Q

Glaucoma drugs: α-agonists

A

Epinephrine, Brimonidine

162
Q

Glaucoma drugs: β-blockers

A

Timolol, betaxolol, carteolol

163
Q

Hormone replacement therapy (HRT)

A

Used for relief or prevention of menopausal symptoms (e.g., hot flashes, vaginal atrophy) and osteoporosis (↑estrogen, ↓osteoclast activity) Unopposed estrogen replacement therapy (ERT) ↑ the risk of endometrial cancer, so progesterone is added. Possible ↑ CV risk

164
Q

Huntington’s drugs

A

Disease: ↑dopamine, ↓GABA+ACh Reserpine + tetrabenazine - amine depleting Haloperidol - dopamine receptor antagonist

165
Q

Hydrochlorothiazide

A

Mechanism: Thiazide diuretic. Inhibits NaCl reabsorption in early distal tubule, reducing diluting capacity of the nephron. ↓ Ca2+ excretion Clinical use: Hypertension, CHF, idiopathic hypercalciuria, nephrogenic diabetes insipidus Toxicity: Hypokalemic metabolic alkalosis, hyponatremia, hyperglycemia, hyperlibidemia, hyperuricemia, and hypercalcemia. Sulfa allergy

166
Q

Infliximab

A

TNF-α inhibitors Mechanism: Anti-TNF antibody Clinical use: Crohn’s disease, rheumatoid arthritis, ankylosing spondylitis Toxicity: Predisposes to infections (reactivation of latent TB)

167
Q

Intravenous anesthetics: Arylcyclohexylamines (Ketamine)

A

PCP analogs that act as dissociative anesthetics. Block NMDA receptors. Cardiocascular stimulants. Cause disorientation, hallucication, and bad dreams. ↑cerebral blood flow.

168
Q

Intravenous anesthetics: Barbiturates

A

Thiopental - high potency, high lipid solubility, rapid entry into brain. Used for induction of anesthesia and short surgical procedures. Effect terminated by rapid redistribution into tissue and fat. ↓cerebral blood flow.

169
Q

Intravenous anesthetics: Benzodiazepines

A

Midazolam most common drug used for endoscopy; used adjunctively with gaseous anesthetics and narcotics. May cause severe postoperative respiratory depression, ↓BP (treat overdose with flumazenil), and amnesia

170
Q

Intravenous anesthetics: Opiates

A

Morphine, fentanyl used with other CNS depressants during general anesthesia

171
Q

Intravenous anesthetics: Propofol

A

Used for rapid anesthesia induction and short procedures. Less postoperative nausea than thiopental. Potentiates GABA(A).

172
Q

Ipratropium

A

Asthma drug, competitive block of muscarinic receptors, preventing bronchoconstriction. Also used for COPD, with ↓ production of mucus.

173
Q

Isoproterenol

A

Asthma drug, relaxes bronchial smooth muscle (β2). Adverse effect is tachycardia (β1).

174
Q

K+-sparing diuretics: Names

A

Spironolactone, Triamterene, Amiloride, Eplerenone

175
Q

Latanoprost

A

PGF2α, ↑outflow of aqueous humor Side effects: Darkens color of iris (browning)

176
Q

Leuprolide

A

Mechanism: GnRH analog with agonist properties when used in pulsatile fasion; antagonist properties when used in continuous fasion Clinical use: Infertility (pulsatile), prostate cancer (continuous - use with flutamide), uterine fibroids Toxicity: Antiandrogen, nausea, vomiting

177
Q

Local enesthetics: Two groups

A

Esters - procaine, cocaine, tetracaine Amides - Lidocaine, mepivacaine, bupivacaine (amides have 2 i’s in name)

178
Q

Losartan

A

an angiotensin II receptor antagonist. It is not an ACE inhibitor and does not cause cough.

179
Q

Mannitol

A

Mechanism: Osmotic diuretic, ↑tubular fluid osmolarity, producing ↑ urine flow Clinical use: Shock, drug overdose, ↑intracranial / intraocular pressure Toxicity: Pulmonary edema, dehydration

180
Q

Maprotiline

A

Blocks NE reuptake. Toxicity: sedation, orthostatic hypotension.

181
Q

Mechanism: ACE inhibitors

A

Inhibit angiotensin-converting enzyme, reducing levels of angiotensin II and preventing inactivation of bradykinin, a potent vasodilator. Renin release is ↑ due to loss of feedback inhibition

182
Q

Mechanism: Acetaminophen

A

Reversibly inhibits cyclooxygenase, mostly in the CNS. Inactivated peripherally.

183
Q

Mechanism: Antipsychotics

A

All typical antipsychotics block dopamine D2 receptors (↑[cAMP]1)

184
Q

Mechanism: Aspirin

A

Irreversibly inhibit cyclooxygenase (both COX-1 and COX-2). Block prostaglandin synthesis.

185
Q

Mechanism: Benzodiazepines

A

Facilitate GABA(A) action by ↑frequency of Cl- channel opening. ↓REM sleep. Most have long half-lives and active metabolites

186
Q

Mechanism: Buspirone

A

Stimulates 5-HT1A receptors

187
Q

Mechanism: COX-2 inhibitors (celecoxib)

A

Reversibly inhibit specifically the cyclooxygenase (COX) isoform 2, which is found in inflammatory cells and vascular endothelium and mediates inflammation and pain; spares COX-1, which helps maintain the gastric mucosa. Thus, should not have the corrosive effects of other NSAIDs on the GI lining.

188
Q

Mechanism: L-dopa/carbidopa

A

↑level of dopamine in brain. Unlike dopamine, L-dopa can cross blood-brain barrier and is converted by dopa decarboxylase in the CNS to dopamine

189
Q

Mechanism: Lithium

A

Possibly related to inhibition of phosphoinositol cascade

190
Q

Mechanism: Local anesthetics

A

Block Na+ channels by binding to specific receptors on inner portion of channel. Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons. 3° amine local anesthetics penetrate membrane in uncharged form, then bind to ion channels as charged form

191
Q

Mechanism: Monoamine oxidase (MAO) inhibitors

A

Nonselective MAO inhibition ↑ levels of amine neurotransmitters (NE, serotonin, dopamine)

192
Q

Mechanism: Nonbenzodiazepine hypnotics

A

Act via the BZ1 receptor subtype and is reversed by flumazenil

193
Q

Mechanism: Selegiline

A

Selectively inhibites MAO-B, which preferentially metabolizes dopamine over NE and 5-HT, thereby increasing the availability of dopamine

194
Q

Mechanism: Sildenafil / vardenafil

A

Inhibit cGMP phosphodiesterase, causing ↑ cGMP, smooth muscle relaxation in the corpus cavernosum, ↑ blood flow, and penile erection. Sildenafil and vardenafil fill the penis.

195
Q

Mechanism: SNRIs

A

Inhibit serotonin and NE reuptake

196
Q

Mechanism: Spironolactone

A

a competitive aldosterone receptor antagonist in the cortical collecting tubule

197
Q

Mechanism: SSRIs

A

Serotonin-specific reuptake inhibitors

198
Q

Mechanism: Triamterene / Amiloride

A

act at the cortical collecting tubule by blocking Na+ channels in the DCT

199
Q

Mechanism: Tricyclic antidepressants

A

Block reuptake of NE and serotonin

200
Q

Memantine

A

Alzheimer’s drug Mechanism: NMDA receptor antagonist; helps prevent excitotoxicity (mediated by Ca2+) Toxicity: Dizziness, confusion, hallucinations

201
Q

Mifepristone (RU-486)

A

Mechanism: Competitive inhibitor of progestins at progesterone receptors Clinical use: Termination of pregnancy. Administered with misoprostol (PGE1) Toxicity: Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain

202
Q

Mirtazapine

A

α2 antagonist (↑ release of NE and serotonin) and potent 5-HT2 and 5-HT3 receptor antagonist. Toxicity: sedation, ↑ appetite, weight gain, dry mouth.

203
Q

MOA: Atypical antipsychotics

A

Block 5-HT2, dopamine, α, and H1 receptors

204
Q

MOA: Barbiturates

A

Facilitate GABA(A) action by ↑duration of Cl- channel opening, thus ↓neuron firing

205
Q

MOA: Carbamazepine

A

↑Na+ channel inactivation

206
Q

MOA: Ethosuximide

A

Blocks thalamic T-type Ca2+ channels

207
Q

MOA: H1 blockers

A

Reversible inhibitors of H1 histamine receptors

208
Q

MOA: Ketoconazole

A

Inhibits steroid synthesis (inhibits desmolase)

209
Q

MOA: Opioids analgesics

A

Act as agonists at opioid receptors (mu=morphine, delta=enkephalin, kappa=dynorphin) to modulate synaptic transmission - open K+ channels, close Ca2+ channels → ↓synaptic transmission. Inhibit release of ACh, NE, 5-HT, glutamate, substance P

210
Q

MOA: Phenytoin

A

Use-dependent blockade of Na+ channels; ↑refractory period; inhibition of glutamate release from excitatory presynaptic neuron

211
Q

MOA: Spironolactone

A

Inhibits steroid binding

212
Q

MOA: Valproic acid

A

↑Na+ channel inactivation, ↑GABA concentration

213
Q

Molecular: GABA(A)-R

A

A ligand-gated chloride channel binded by benzos, barbs, and EtOH

214
Q

Monitoring: Lithium

A

Narrow therapeutic window requires close monitoring of serum levels. Almost exclusively excreted by the kidneys; most is reabsorbed at the proximal convoluted tubules following Na+ reabsorption

215
Q

Monoamine oxidase (MAO) inhibitors: Names

A

Phenelzine, tranylcypromine, isocarboxazid, selegiline (selective MAO-B inhibitor)

216
Q

Name Inhaled anesthetics (3)

A

Halothane, -flurane, nitrous oxide

217
Q

Neuroleptic malignant syndrome (NMS)

A

rigidity, myoglobinuria, autonomic instability, hyperpyrexia. Treatment: dantrolene, D2 agonists (e.g., bromocriptine) FEVER: Fever, Encephalopathy, Vitals unstable, Elevated enzymes, Rigidity of muscles

218
Q

Neuromuscular blocking drugs: Two groups

A

Depolarizing: Succinylcholine Nondepolarizing: Tubocurarine, -curium, -curonium

219
Q

NSAIDs

A

Ibuprofen, naproxen, indomethacin, ketorolac Mechanism: Reversibly inhibit cyclooxygenase (both COX-1 and COX-2). Block prostaglandin synthesis. Clinical use: Antipyretic, analgesic, anti-inflammatory. Toxicity: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers.

220
Q

Order of nerve blockade: Local anesthetics

A

Small myelinated fibers > Small unmyelinated fibers > Large myelinated fibers > Large unmyelinated fibers

221
Q

Parkinson’s disease drugs: Four groups

A

Agonize dopamine receptors: a.ergot: Bromocriptine b.non-ergot: pramipexole ropinirole ↑dopamine: Amantiadine, L-dopa/carbidopa Prevent dopamine breakdown: Selegiline, -capone Curb excess cholinergic activity: Benztropine

222
Q

Principle: Local anesthetics in acidic tissue

A

In infected (acidic) tissue, alkaline anesthetics are charged and cannot penetrate membrane effectively. More anesthetic is needed in these cases.

223
Q

Probenecid

A

Gout drug, chronic gout. Inhibits reabsorption of uric acid in PCT (also inhibits secretion of penicillin)

224
Q

Progestins

A

Mechanism: Bind progesterone receptors, reduce growth, and ↑ vascularization of endometrium Clinical use: Used in oral contraceptives and in the treatment of endometrial cancer and abnormal uterine bleeding

225
Q

Raloxifene

A

Estrogen partial agonist, agonist on the bone; reduces resorption of bone; used to treat osterporosis

226
Q

Reason: Why not use salicylates to treat gout?

A

All but the highest doses depress uric acid clearance. Even high doses (5-6 g/day) have only minor uricosuric activity

227
Q

Ritodrine / Terbutaline

A

β2-agonists that relax the uterus; reduce premature uterine contractions

228
Q

Salmeterol

A

Asthma drug, long-acting agent for prophylaxis. Adverse effects are tremor and arrhythmia.

229
Q

Seizures: Almost always from temporal lobe (mood changes, illusions, hallucinations); impaired consciousness and postictal state are present

A

Complex partial, DOC: Carbamazepine

230
Q

Seizures: Brief arrhythmic jerking movements, last < 1 sec, usually occur in clusters for a few minutes; no loss of consciousness

A

Myoclonic, DOC: Valproic acid

231
Q

Seizures: Brief episode of staring, but no postictal confusion

A

Absence, DOC: Ethosuximide, valproate

232
Q

Seizures: Generalized tonic extension of the extremities, followed by clonic rhythmic movements; loss of consciousness and prolonged postictal confusion are present

A

Tonic-clonic, DOC: Phenytoin, carbamazepine, and valproate

233
Q

Seizures: One body part is involved; no loss of consciousness and no postictal confusion

A

Simple partial, DOC: Carbamazepine

234
Q

Serotonin syndrome

A

Hyperthermia, myoclonus, cardiovascular collapse, flushing, diarrhea, seizures

235
Q

Short acting benzodiazepines (3)

A

Triazolam, Oxazepam, Midazolam → Highest addictive potential

236
Q

Side effects: Tricyclic antidepressants

A

Sedation, α-blocking effects, atropine-like side effects. 3° TCAs (amitriptyline) have more anticholinergic effects than do 2° TCAs (nortriptyline). Desipramine is the least sedating and has lower seizure threshold.

237
Q

SNRIs: Names

A

Venlafaxine, duloxetine

238
Q

SSRIs: Names

A

Fluoxetine, paroxetine, sertraline, citalopram

239
Q

Steven-Johnson syndrome

A

Prodome of malaise and fever followed by rapid onset of erythmatous / purpuric macules (oral, ocular, genital). Skin lesions progress to epidermal necrosis and sloughing

240
Q

Sumatriptan

A

Mechanism: 5-HT(1B/1D) agonist. Causes vasoconstriction, inhibition of trigeminal activation and vasoactive peptide release. Half-life < 2 hours Clinical use: Acute migraine, cluster headache attacks. Toxicity: Coronary vasospasm (contraindicated in patients with CAD or Prinzmetal’s angina), mild tingling

241
Q

Tamoxifen

A

Estrogen partial agonist, antagonist on the breast tissue; used to treat and prevent recurrence of ER-positive breast cancer

242
Q

Tamsulosin

A

α1-antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective for α1(A,D) receptors (found in prostate) vs. vascular α1(B) receptors

243
Q

Tardive dyskinesia

A

stereotypic oral-facial movements due to long-term antipsychotic use. Often irreversible.

244
Q

Testosterone (methyltestosterone)

A

Mechanism: Agonist at androgen receptors Clinical use: Treat hypogonadism and promote development of 2° sex characteristics; stimulation of anabolism to promote recovery after burn or injury; treat with ER-positive breast cancer (exemastane) Toxicity: Causes masculinization in females; reduces intratesticular testosterone in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy. Premature closure of epiphyseal plates. ↑LDL, ↓HDL

245
Q

Theophylline

A

Asthma drug, likely causes bronchodilation by inhibiting phosphodiesterase, thereby ↓ cAMP hydrolysis. Usage is limited because of narrow therapeutic index (cardiotoxicity, neurotoxicity); metabolized by P-450. Blocks actions of adenosine.

246
Q

Toxicity: ACE inhibitors

A

Cough, Angioedema, Proteinuria, Taste changes, hypOtesion, Pregancy problems, Rash, Increased renin, Lower angiotensin II. CAPTOPRIL. Also, hyperkalemia. Avoid with bilateral renal artery stenosis because ACE inhibitors significantly ↓ GFR by preventing constriction of efferent arterioles

247
Q

Toxicity: Acetaminophen

A

Overdose produces hepatic necrosis; acetaminophen metabolite depletes glutathione and forms toxic tissue adducts in liver. N-acetylcysteine is antidote - regenertates glutathione.

248
Q

Toxicity: Antipsychotics

A
  1. Highly lipid soluble and stored in body fat; thus, very slow to be removed from body. 2. Extrapyramidal system (EPS) side effects. 3. Endocrine side effects (e.g., dopamine receptor antaganism → hyperprolactinemia → galactorrhea) 4. Side effects arising from blocking muscarinic (dry mouth, constipation), α (hypotension), and histamine (sedation) receptors. 5. Neuroleptic malignant syndrome (NMS) / Tardive dyskinesia
249
Q

Toxicity: Aspirin

A

Gastric upset. Chronic use can lead to acute renal failure, interstitial nephritis, and upper GI bleeding. Reye’s syndrome in children with viral infection.

250
Q

Toxicity: Atypical antipsychotics

A

Fewer extrapyramidal and anticholinergic side effects than traditional antipsychotics

251
Q

Toxicity: Barbiturates

A

Dependence, additive CNS depression effects with alcohol, respiratory or cardiovascular depression (can lead to death), drug interactions owing to induction of liver microsomal enzymes (cytochrome P-450)

252
Q

Toxicity: Benzodiazepines

A

Dependence, additive CNS depression effects with alcohol. Less risk of respiratory depression and coma than with barbiturates

253
Q

Toxicity: Bupivacaine

A

CNS excitation, severe cardiovascular toxicity

254
Q

Toxicity: Chlorpromazine

A

Corneal deposits

255
Q

Toxicity: Clozapine

A

may cause agranulocytosis

256
Q

Toxicity: Cocaine

A

Hypertension, hypotension, and arrhythmias

257
Q

Toxicity: COX-2 inhibitors (celecoxib)

A

↑ risk of thrombosis. Sulfa allergy. Less toxicity to GI mucosa (lower incidence of ulcers, bleeding than NSAIDs)

258
Q

Toxicity: Enflurane

A

Proconvulsant

259
Q

Toxicity: Halothane

A

Hepatotoxicity

260
Q

Toxicity: K+-sparing diuretics

A

Hyperkalemia (can lead to arrhythmias), endocrine effects with aldosterone antaganists (e.g., spironolactone causes gynecomastia, antiandrogen effects)

261
Q

Toxicity: L-dopa/carbidopa

A

Arrhythmias from peripheral conversion to dopamine. Long-term use can → dyskinesia following administration, akinesia between doses. Carbadopa, a peripheral decarboxylase inhibitor, is given with L-dopa in order to ↑ the bioavailability of L-dopa in the brain and to limit peripheral side effects

262
Q

Toxicity: Lithium

A

Tremor, sedation, edema, heart block, hypothyroidism, polyurea (ADH antagonist causing nephrogenic diabetes insipidus). Fetal cardiac defects include Ebstein anomaly and malformation of the great vessels.

263
Q

Toxicity: Methoxyflurane

A

Nephrotoxicity

264
Q

Toxicity: Monoamine oxidase (MAO) inhibitors

A

Hypertensive crisis with tyramine ingestion (in many foods, such as wine and cheese) and β-agonists; CNS stimulation.

265
Q

Toxicity: Nitrous oxide

A

Expansion of trapped gas

266
Q

Toxicity: Nonbenzodiazepine hypnotics

A

Ataxia, headaches, confusion. Shorter duration because of rapid metabolism by liver enzymes. Unlike older sedative-hypnotics, cause only modest day-after psychomotor depression and few amnestic effects. Lower dependence risk than benzodiazepines

267
Q

Toxicity: Olanzapine / Clozapine

A

may cause significant weight gain

268
Q

Toxicity: Opioid analgesics

A

Addiction, respiratory depression, constipation, miosis (pinpoint pupils), additive CNS depression with other drugs. Tolerance does not develop to miosis and constipation.

269
Q

Toxicity: Phenytoin

A

Nystagmus, ataxia, diplopia, sedation, SLE-like syndrome, induction of cytochrome P-450. Chronic use produces gingival hyperplasia in children, peripheral neuropathy, hirsutism, megaloblastic anemia (↓folate absorption). Teratogenic (fetal hydantoin syndrome).

270
Q

Toxicity: Selegiline

A

May enhance the adverse effects of L-dopa

271
Q

Toxicity: Sildenafil / vardenafil

A

Headache, flushing, dyspepsia, impaired blue-green color vision. Risk of life-threatening hypotension in patients taking nitrates.

272
Q

Toxicity: SNRIs

A

↑ BP most common; also stimulant effects, sedation, nausea

273
Q

Toxicity: SSRIs

A

Fewer than TCAs. GI distress, sexual dysfunction (anorgasmia). “Serotonin syndrome” with any drug that ↑ serotonin (e.g., MAO inhibitors)

274
Q

Toxicity: Thioridazine

A

Retinal deposits

275
Q

Toxicity: Tricyclic antidepressants

A

Tri-C’s: Convulsions, Coma, Cardiotoxicity (arrhythmias); also respiratory depression, hyperpyrexia. Confusion and hallucinations in elderly due to anticholinergic side effects.

276
Q

Tramadol

A

Mechanism: Very weak opioid agonist; also inhibits serotonin and NE reuptake (works on multiple neurotransmitters - “tram it all” in) Clinical use: Chronic pain Toxicity: Similar to opioids. Decreases seizure threshold

277
Q

Trazodone

A

Primarily inhibits serotonin reuptake. Used for insomnia, as high doses are needed for antidepressant effects. Toxicity: sedation, nausea, priapism, postural hypotension.

278
Q

Tricyclic antidepressants: Names

A

Imipramine, amitriptyline, desipramine, nortriptyline, clomipramine, doxepin, amoxapine (-ipramine, -triptyline, doxepin, amoxapine)

279
Q

Zafirlukast, montelukast

A

block leukotriene receptors. Especially good for aspirin-induced asthma.

280
Q

Zileuton

A

A 5-lipoxygenase pathway inhibitor. Blocks conversion of arachidonic acid to leukotrienes

USMLE (12 decks)

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