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1

Cyclophosphamide: MOA, use

  • alkylating agent that cross-links DNA ==> apoptosis
  • uses
    • non-Hodgkin's lymphoma
    • breast/ovarian cancer

2

Naloxone

MOA: mu-opiod receceptor antagonist

use: opiod/heroin overdose

3

Flumazenil

  • MOA: 
  • use: benzodiazepine antagonist/overdose

4

Haloperidol

  • MOA:
  • Use
    • anti-psychotic
    • delirium
    • tranquilization in agitated patient

5

Lorazepam

  • Benzodiazepine
  • MOA: allosteric modification of a specific kind of neurotransmitter receptor, the GABAA receptor, which increases the overall conductance of these inhibitory channels
  • Use: 
    • acute anxiety
    • status epilepticus

6

Morphine: MOA

  • agonist @ Mu opioid receptors
  • Mu opoid receptors = GPCR ==>
    • activation of K channels ==> increased K efflux
    • ==> hyperpolarization ==> termination of pain signaling from nerves

7

Isoproteronol MOA

  • agonist at B1 and B2 receptors w/no alpha receptor activity ==>
    • increase in cardiac contractility (B1)
    • vascular smooth muscle relaxation (B2)

8

Tx of acute mania

  • mood stabilizers = lithium, valproate, carbamazepime 
  • + atypical antipsychotic = olanzapine

9

colchicine: MOA/use/SE

  • inhibition of microtubular polymerization ==> prevention of aggregration  ==> disrupts chemotaxis and phagocytosis 
  • also inhibits formation of leukotriene B4
  • use = acute gouty arthritis
  • SE = nausea, abdominal pain, diarrhea

10

Enoxaparin: MOA

  • low molecular weight heparin
  • MOA: binding and activating antithrombin III
    • active ATIII prevents factor Xa from: prothrombin ==> thrombin
  • ==> anticoagulant effect

11

Digoxin clearance

via kidneys

12

Glucorticoids stimulate...?

liver (gluconeogenesis/glycogenolysis)

13

Valproate during pregnancy ==> ?

  • neural tube defects due to inhibition of folic acid absorption @ intestine
    • meningocele, spina bifida, etc.

14

Ebstein's anomaly association/presentation

  • "Ebstein's anomaly" = "atrialization" of R ventricle due to downward displacement of tricuspid valve
  • associated w/mother use of lithium during early pregnancy

15

Tx/recommendations after total gastrectomy

  • parental B12
  • to avoid dumping syndrome (colicky ab pain, nausea, diarrhea)
    • small meals
    • low dietary intake of simple sugars

16

Isoniazid side effects

  • peripheral neuropathy (if given w/pyroxidine)
  • hepatotoxicity
    • usually mild ==> transient elevated AST, ALT
    • elevated bilirubin
    • fever, anorexia, nauseau
    • severe ==> liver dysfxn, jaundice, bilirubinuria

17

Hib vaccine + importance

  • composed of polyribosyl-ribotol-phosphate (PRP) = component of Hib capsule
  • [conjugated w/diptheria or tetanus toxoid]
  • ==> lasting immunity against Hib in children
  • H. flu ==> epiglottitis 

18

Raloxifene: MOA

  • SERM
  • estrogen agonist @ bone ==> prevention of osteoporosis
  • estrogen antagonist @ breast ==> prevention of breast cancer

19

Atenolol: MOA + effects

  • B1 receptor antagonist
  • @ cardiac tissue and JGA, but not @ vascular smooth muscle
  • ==> decreased cAMP @ cardiac/renal

20

Tx of organophosphate poisoning

  • Atropine: reversal of muscarinic sx; no effect on nicotinic receptors
    • pts still at risk for muscle paralysis
  • Pralidoxime: reverses muscarinic and nicotinic effects of organophosphates
    • effective only if given early after the exposure

21

Drug effects:

tachyphylaxis = 

additive =

synergistic = 

permissive = 

  • tachy = decreased drug response w/repeated administration
  • additive/synergistic = two drugs with similar actions
    • additive = admin of both is equal to the sum of the effects
    • synergistic = admin of both leads to effects exceeding the sum of the drugs individually
  • permissive = admin of a different type of drug (without its own action @ desired site) leads to increased action of an effective drug if given together

22

AChE in amniotic fluid ==> dx?

  • Neural tube defects = failure of fusion of neural tube during 4th week of fetal development
  • ==> leakage of fetal CSF ==>
    • elevated alpha-fetoprotein
      • crosses placenta ==> elevated alpha-fetoprotein @ mother serum
    • acetylcholinesterase 

23

Iodine transport @ thyroid

  • sodium-iodide symporter brings iodine into thyroid against concentration gradient
  • NIS is also responsible for transporting perchlorate and pertechnetate into thyroid 
    • if potassium perchlorate is present ==> competitive inhibition

24

Drugs that interfere with iodine uptake

  • antithyroid thionamides
    • methimazole ==I thyroid peroxidase ==> blocked conversion of iodide to iodine
    • propylthiouracil
  • usually stopped 7-10 days before tx w/radioactive iodine for hyperthyroidism

25

Dobutamine impact on pressure-volume loop

  • ==> increased contractility
  • ==> higher pressures during ventricular ejection phase + greater volume expelled
  • ==> widening of P-V loop

26

Tx for severe asthmatics 

  • anti-IgE drugs to help reudce allergy triggers of asthma
  • e.g. Omalizumab ==> patients w/mod-severe allergic asthma
    • IgG1 monoclonal antibody
    • binds to IgE to prevent action of IgE w/its receeptor on mast cells ,basophils and other cells

27

Anti-metabolite drugs

  • Folate antagonist
    • Methotrexate
  • Purine Analogs
    • 6-thiopurines
      • 6-mercaptopurine
      • 6-guanopurine (?)
    • Fludarabine ==> CLL tx
    • Cladribine ==> HCL tx
  • Pyrimidine Ananologs
    • 5-FU
    • Capecitabine
    • Cytarabine
    • Gemcitabine

28

Vinblastine: MOA, SE

  • MOA:
    • inhibits MT formation of mitotic spindle
  • SE:
    • alopecia
    • constipation
    • myelosuppression
    • neurotoxicity (rare)

29

Cancer drugs that act in the M phase of the cell cycle

  • vinca alkaloids=inhibit MT fxn/spindle formation
    • vincristine
    • vinblastine
  • paclitaxel 
    • binds to tubulin and hyperstabilizes MTs that have already polymerized ==> prevents spindle breakdown

30

5-fluorouracil: MOA, use

  • anti-metabolite
  • prevents formation of thymidine vua inhibition of thymidylate synthase
  • uses
    • slow-growing solid tumors:
    • breast
    • ovarian
    • pancreatic
    • colorectal
    • gastric carcinomas

31

6-mercaptopurine: MOA, use

  • anti-metabolite
  • inhibits formation of purines
  • use = cancer drug

32

Methotrexate: MOA, use

  • anti-metabolite
  • inhibts dihydrofolate reductase ==> inhibition of DNA synthesis (via same pathway as 5-fluorouracil)
  • use = cancer drug

33

Busulfan: MOA, use

  • DNA alkylating agent (cell cyle nonspecific)
  • use = CML

34

Bleomycin: MOA, use, SE

  • inhibit replication by inducing DNA strand breaks via free radical formation
  • strand breakage interrupts G2 phase of cell cycle (after DNA synthesis)
  • uses: testicular tumors, lymphomas, squamous cell carcinoma
  • SE
    • rales, cough
    • infiltration ==> fibrosis

35

Cyclophosphamide: MOA, uses, SE

  • DNA alkylating agent (cell cycle nonspecific)
    • activated by CYP450
    • ==> apoptosis via DNA crosslinking
  • uses
    • leukemias, lymphomas
    • testicular and gyn cancers
  • SE
    • hemorrhagic cystitis

36

How to prevent major side effect of cycloposphamide

  • prevent hemorrhagic cystitis via:
    • adequate hdration
    • IV injection of mesna

37

Methotrexate rescue

  • folinic acid aka n-formyl-xxxx aka leucovorin
  • acts synergystically with 5FU

38

Common method of chemotherapy resistance

  • human multi-drug resistance gene (MDR1)
  • p-glycoprotein = transmembrane ATP-dependent efflux pump
    • broad specificity for hydrophobic compounds
    • decreases drug entry and increases efflux

39

Diuretic overuse impact on blood pH/gases

  • diuretic overuse ==> compensatory increase in aldosterone
  • aldosterone ==> sodium + H2O retention + K+ and H+ loss @ kidneys ==> metabolic alkalosis
    • "contraction alkalosis"
  • labs = high pH, high HCO3, high pCO2

40

Characteristics of drugs w/various volume of distribution

  • low Vd = 3-5 L
    • highly bound
    • charged
    • hydrophillic
    • high molecular weight
  • Vd = 14-16L = plasma + interstitial fluid
    • small molecular weight
    • hydrophillic
  • Vd = 41L = highest distribution
    • lipophillic (or hdyro)
    • uncharged

41

Isoniazid: MOA

  • antimycobacterial
  • inhibits mycolic acid synthesis

42

Buspirone: MOA/properties, use

  • MOA: partial 5HTA1 agonist
    • no muscle relaxant
    • no anti-seizure
    • little hypnosis/hallucinatory
  • Use:
    • anxiety
    • esp. @ previous abusers of anxiolytics
      • less addiction potential vs. benzos

43

a1 receptors location + effect + drugs (agonists)

  • pupil sphincter ==> mydriasis (dilation)
  • bladder ==> sphincter contraction
  • peripheral blood vessels ==> increased SBP
  • agonists
    • norepi
    • epi
    • phenylephrine
    • methoxamine

44

beta-1 receptor locations + effects + agonist drugs

  • heart ==> increased HR, contractility
  • agonsits
    • epinephrine
    • dobutamine
    • dopamine
    • isoproteronol

45

beta-2 receptor locations + effects + agonist drugs

  • bronchi ==> bronchodilation
  • uterus ==> relaxation
  • skeletal muscle bood vessels ==> vasodilation
  • agonist drugs
    • isproteronal
    • terbutaline
    • ritodrine

46

How long till continuous infusion or drug reaches  steady state?

  • IF: continuous infusion + elimination via first-order kinetics ==>
  • steady state plasma concentration @ 4-5 half lives

47

Presentation of ethylene glycol toxicity

  • ethylene glycol metabolized ==> glycolic acid & oxalic acid
  • anion-gap metabolic acidosis
  • calcium oxalate crystals in urine
  • increased osmolar gap
  • acute kidney injury/renal failure
    • damage to tubular epithelium
      • vacuolization
      • ballooning

48

Presentation of theophylline toxicity + tx

  • theophylline ==>
    • N/V + abdominal pain
    • arrhythmias
    • seizures **
  • Tx
    • gastric lavage
    • activated charcoal
    • cathartics (increase elimination via GI tract)
    • beta-blockers ==x arrhythmias
    • benzodiazepines & baribituates ==x seizures

49

Lithium: indications, side effects

  • bi-polar; manic and depressive episodes, maintenance
  • SE
    • DI
    • tremor
    • hypothyroidism
    • Epstein's anomaly

50

Valproate: indications, SE

  • manic episodes; maintence in bipolar & generalized/absence/myclonic seizures
  • SE
    • hepatotox
    • NTDs

51

Carbamazepine: indications, SE

  • manic episodes, maintence
  • partial generalized seizures
  • trigeminal neuralgia
  • SE
    • agranulocytosis
    • NTDs
    • hyponatremia (SIADH)

52

Lamotrigine: indications, SE

  • depressive episodes, maintenance in bipolar
  • focal seizures
  • SE
    • stevens-johnson
    • benign rash

53

Mood stabilizers in bipolar

  • lithium
  • valproate
  • carbamazepime
  • lamotrigine

54

Use/Effects:

Physostigmine vs. Neostigmin vs. Edrophonium

  • all AChE inhibitors
  • use = reverse atropine toxicity
  • neostigmine/edrophonium = only fxn @ peripherphy; cannot penetrate CNS
  • physostigmine = fxns @ periphery & CNS

55

5HT3-inhibitors

  • ondansetron
  • granesetron
  • dolasetron

56

Rapid and complete relief in RA [short-term]

glucocorticoids, e.g. prednisone

57

Nevirapine: MOA, similar drugs

  • NNRTI
  • inhibits reverse transcription, doesn't need phosphorylation to be active
  • other drugs
    • efavirenz
    • delaviridine

58

Canagiflozin: MOA, use, SE

  • MOA
    • oral anti-diabetic
    • = SGLT2 inhibitor ==> decreased reabsorption of glucose @ proximal renal tubule
    • ==> urinary glucose loss
  • SE
    • renal effects

59

Lithium toxicity antidote

hydrocholorthiazide ==> trapping in urine

60

thiopental: moa, use

  • lipid-soluble barbituate used as short-term anesthesia
  • ==> brain ==> rapid redistribution to skeletal muscle and adipose tssue (w/in 5-10min)
    • rapid redistribution allows for short term anesthia

61

Characteristics of serotonin syndrome

  • occurs when SSRIs are given in conjunction w/other serotonergic agens
  • sx
    • neuromuscular excitation: hyperreflexia, clonus, myoclonus, rigidity
    • autonomic stimulation: hyperthermia, tachycardia, diaphoresis, tremor
    • AMS

62

Examples of serotonergic agents

  • Anti-depressants 
    • monoamine oxidase inhibitors
    • TCA
    • SNRI
  • analgesics
    • tramadol
  • anti-emetics
    • 5-HT3 receptor antagonists (ondansetron)
  • antibiotics
    • linezolid = weak monoamine oxidase inhibitor
  • neuropsych
    • triptans

63

Tx tp prevent recurrences of genital herpes

  • daily treatment with oral valacyclovir, acyclovir, or famciclovir ==> suppression of reactivation

64

Amphotericin B: MOA, SE

  • MOA = binds ergosterol ==> pores ==> cell death
  • SE
    • renal toxicity
    • ==> vasoconstrict ==> decreased GFR 
    • direct toxin to renal epithelial cells ==> ATN, renal tubular acidosis, and electrolyte distrubances
      • **hypoK and hypoMg
    • ==> decreased EPO ==> normochromic, normocytic anemia

65

Antifungal that inhibits fungal cell wall synthesis

  • Capsofungin
  • inhibits synthesis of cell wall polysaccharide glucan

66

Phenytoin SE/toxicity

  1. CNS effects ==> cerebeller defects/ataxia
  2. gingival hyperplasia
    1. pheny ==> increased PDGF ==> stimulated macs to proliferate gingiva and alveolar bone
  3. coarsening of facial features, hirstruism
  4. interferes w/folic acid metabolism ==> megaloblastic anemia
  5. induces P450
  6. teratogen ==> fetal hydantoin syndrome

67

Phenelzine: drug class, use, other similar drugs

  • MAOIs
  • Atypical depression = mood reactivity (to positive events), leaden fatigue, rejection sensitivity, increased sleep and apetite
  • others
    • tranylcypromine

68

Rare, serious side effect of ACE-i

  • angioedema = face, lips, tonuge, eyelids, larygneal edema ==> difficulty breathing
  • most likely due to elevated bradykinin levels

69

SE: Orange/red body fluids ==> drug + MOA?

  • Rifampin
  • ihibits DNA-dependent RNA synthesis (bacterial RNA pol)

70

Contraindications for use of OCPs

  1. Prior thromboembolic event/stroke
  2. hx of estrogen-dependent tumro
  3. women > 35 who smoke heavily ==> higher risk of CV events
  4. hypertriglyceridemia
  5. decompensated or active liver disease
  6. pregnancy

71

Causes of exacerbation of mysathenia gravis

  • myasthenic crisis = undertx
  • cholinergic crisis = overtx

72

Antidote for serotonin syndrome

  • cyproheptadine = antihistamine + anti-serotonergic properties

73

Verapamil: MOA, use, SE

  • MOA = non-dihydropyriddine ca-channel blocker
    • slows conduction through AV nodes
  • use = rate control in afib w/rapid ventricular response
  • SE
    • constipation
    • gingival hyperplasia
    • bradycardia
    • first, second, or third degree AV node block

74

Leoprolide impact @ male

  • GnRH
  • transient increase, then decrease in both T and DHT

75

Vancomycin: MOA vs. Ceftriaxone: MOA

  • Vanc binds D-ala (glycoproteins @ cell wall of bacteria)
  • Ceftriaxone binds PBPs
    • PBPs = transpeptidases that cross-link peptidoglycan @ cell wall

76

Beta blocker effects in thyrotoxicosis

  • decrease noradgrenergic responses
  • decreased T4 ==> T3 conversion @ periphery

77

Anti-pseudomonals

  • Pip-Taz
  • [some] Cephs
    • Cefatadazine
    • Cefepime
  • Gentamicin
  • [some] fluoro
    • ciprofloxacin
    • levofloxacin
  • carbapenems

78

Heparain: MOA

  • binds antithrombin III and increases action

79

Drug-induced lupus: association

  • drugs metabolized by liver acteylation
  • hydralizine
  • procainamide
  • slow-acetylators are @ higher risk

80

Mast stablizing agents

  • cromolyn 
  • nedocromil
  • inhibit mast cell degranulation regardless of stimuli present
  • 2nd line for tx of allergic rhinitis and bronchial asthma

81

Niacin SE

  • vasodilation ==> flushing 
    • can potentiate anti-htn meds ==> dosage decrease
  • ==> increased insulin resistance
    • ==> dosage increase in DM meds

82

Acetozolamide: MOA, use

-MOA: inhibits CA @ proximal tubule ==> excretion of HCO3- + sodium ==> diuresis + alkaline urine + metabolic acidosis -use: open & close-angle glaucoma, others

83

DRESS syndrome

-Drug Rxn with Eosinophilia & Systemic Sx -2-8 weeks after starting new medication -esp. anticonvulsants, antibiotics, allopurinol, sulfonamides -fever, general lymph, facial swell, eosino, skin rash, organ dysfxn

84

Drug-induced lupus

-hydralazine (HTN drug, arteriolar vasodilator via K channel binding) -procainamide -isoniazid

85

opioid drug that can produce w/drawal in someone on morphine

pentacozine

86

Selegiline: MOA

MAO-B inhibitor

87

Methotrexate toxicity antidote

Folinic acid

88

Characteristics of digoxin toxicity

-nonspecific GI = N/V, abdominal pain, anorexia -neurologic = fatigue, confusion, weakness, sometimes: color vision changes -most serious complication = arrhythmias

89

Drugs not to use with partially occluded coronary arteries

-coronary artery vasodilators -vasodilation of unoccluded arteries ==> reduced blood flow through collaterals to ischemic areas ==> worsening ischemia

90

Which of these drugs would cause bradycardia: -Nifedipine -Captopril -Verapamil -Isosorbide nitrate -Prazosin

-verapamil only -all others act peripherally

91

Drugs with negative chronotropic effects @ heart

-B-blockers -non-dihydropyridine Ca-channel blockser (verapamil, diltiazem) -cardiac glycosides (digoxin) -Amiodarone and sotalol -Cholinergic agonists (pilocarpine, rivastigmine)

92

Drug effect of sildanefil is similar to what naturally occuring hormones/mechanisms

1. NO 2. ANP all ==> increased cGMP

93

DDAVP: moa, use

-vasopressin analog -little affect @ V1 receptors ==> no vasoconstriction -use: 1. central DI 2. bleeding control: induces release of procoag proteins (e.g. vWF) and stabilized factor VIII (Hemo A)

94

High vs. low potency antipsychotics

high = fluphenazine, haloperidol low = chlorpromazine, thioridazine

95

Class of anti-arrhythmics that show "use-dependence" + example

-class I anti-arrhymics (Na-cahnnel blockers) -IC = strongest association w/Na; slow to leave ==> prolonged QRS, but no effect on overall AP ==> normal QT

96

Carbamazepime: MOA, use, SE

-MOA = blocks VSSC @ neurons -use = partial, partial complex, gen TC seizures + mood stabilizer -SE = bone marrow suppression

97

Gq receptor pathway

1. binding ==> phospholipase C converts mem. phospho ==> IP3 & DAG 2. IP3 ==> increased Ca release from SR 3. Ca + DAG activate PKC 4. PKC phosphorylates 2nd mess ==> downstream effects

98

Ethambutol SE

optic neuritis, color blindness ,etc.

99

Nitrate with highest bioavailability

isosorbide mononitrate

100

Antidote for NE drip-mediated tissue necrosis

-alpha-1 receptor blocker -e.g. phentolamine

101

Tx of calcium oxalate kidney stones

hydrochlorothiazide: blocks Na/Cl transporter @ lumen ==> activation of Na/Ca exchanger ==> increased Na w/in cell in exchange for increased Ca reabsorbed

102

Adenosine: MOA, use, SE

-MOA: slowing conduction through AV node by hyperpolarizing nodal & conducting cells -use: drug of choice in paroxysmal SVT -SE: flushing, chest buring (bronchospasm), hypotension, high-grade AV block

103

Reason for methodone use

  • used to help patients recover from heroin addiction
  • very long half-life opioid agonist w/good oral bioavailablity
  • prevents withdrawal sx while weaning off heroin

104

Common causes of myopathy with elevated CK

  • inflammatory myopathy
    • skin rash and inflammatory arthritis may also be present
  • statin-induced
  • hypothyroidism
    • hypothyroid sx present
    • myoedema = mounding of m. after percussion

105

Ipratropium: MOA, use

  • Muscarinic antagonist @ bronchial smooth m.
    • less effective than B2 agonists
    • enhance B2 agonists
  • use in asthma

106

Theophylline: MOA, use

  • MOA: inhibit phosphodiesterase ==> increased cAMP ==> bronchial sm. m. dilation
  • use: asthma

107

Nicotinic receptors

  • ligand-gated ion channels
  • ACh binding ==> immediate influx of Ca2+ and Na+ and efflux of K+

108

Clozapine: MOA, use, SE

  • MOA: blocks D4 receptors
  • use: refractory psychosis/schizophrenia
  • SE
    • agranulocytosis
    • seizures

109

Insulin types

  • Basal/long-acting
    • Glargine; Determir = once daily
    • NPH = twice daily
  • Short-acting/post-prandial
    • Regular = best for IV
    • Lispro, Aspart, Glulisine = peak @ 45 min - hour
      • best for post-prand hyperglycemia 

110

Common disinfectant mechanisms:

alcohols

chlorhexadine

hydrogen peroxide

iodine

  • alcohols
    • disruption of cell membranes
    • denaturation of proteins
  • chlorhexadine
    • disruption of cell membranes
    • coagulation of cytoplasm
  • hydrogen peroxide
    • free radicals
    • sporocidal
  • iodine
    • halogenation of proteins & nucleic acids
    • sporocidal

111

Tx of idiopathic pulmonary HTN

Bosentan = endothelin antagonist ==> vasodilation @ pulm. artery

112

Sotalol: MOA, SE

  • MOA
    • K+ channel blocker
    • + mild B-blocker effects
    • Class 3 anti-arrhythmic
      • amiodarone
      • ibutilide
      • dofetilide
  • SE
    • mild bradychardia
    • prolonged QT interval

113

First-line drug for benign essential tremor + SE

  • Primidone ==> active metabolites = phenobarbitol (+ phenylethylmalonimide) ==> anticonvulsant effects
  • must monitor levels ==> AMS, sedations

114

Hyperthyroid sx that does not improve w/beta blockers

exopthalmos = due to fibroblast proliferation and ground substance production

115

Drug that ==> vasodilation + blocks platelet agg. used in PAD

Cilosotazol

116

Isoniazid: MOA, resistance

  • inhibits mycolic acid formation
  • must be processed by mycobacterial catalse-peroxidase to become active
  • resistance:
    • change mycolic acid structure/isoniazid binding site
    • decreased activity of catalase-peroxidase

117

Glucagon receptor type + other hormones w/same receptor

  • G-protein coupled receptor
  • binding ==> activated Adenylate Cyclase ==> increased cAMP ==> activated PKA
  • other hormones
    • PTH
    • B-andrenergic
    • TSH

118

Metoprolol effects 

  • B1 selective blocker
    • present @ heart & JGA
  • ==> decreased HR
  • ==> blocks renin release by JGA cells

119

V2 effects @ medullary collecting duct

  • ==> increased permeability to H20 and urea

120

Initial treatment of severe hypoglycemia

  • in the field/@home: 
    • less severe (mild-moderate) ==> fast-acting carbs; e.g. fruit juice, glucose tablet
    • unconscious: IM glucagon
  • @ hospital: IV glucose

121

Tx for combined T-C and absence seizures

  • valproic acid

122

Amphotericin B: SE

  • Nephrotoxicity and electrolyte abnormalities
  • ==> hypoK and hypoMG
  • hypoK ==> T wave flat, ST-depression, U waves

123

Bethanacol: MOA

musc. antagonist

124

Calcinuerin fxn

  • calc = protein phosphatase ==> dephosph NFAT ==> trxn factor for IL-2 ==> T cell growth and maturation
  • Cyclosporine & Tacrolimus ==I calcineurin ==> anti-rejection/immunosuppress drugs

125

Unfractionated vs. LMWH 

  • unfractionated = binds ATIII and allows activity against factor Xa and thrombin (inactivation)
  • LMWH ==> ATIII activity against Xa only

126

Insulin receptor mechanism

  • insulin ==> tyrosine kinase ==> insulin receptor substrate phosphorylization ==> activation of protein phosphatase
  • protein phosphatase ==> dephosph glycogen synthase = activated glycogen formation
    • also ==> dephosph of fructose-1,6-bisphosphatase = inactive ==> inhibition of gluconeogenesis

127

Succinylcholine: MOA, use

  • MOA: depolarizing NMJ blocker
  • use: rapid induction/intubation or for surgical intubation
  • phase I = augmented by AChEi (e.g. neostigmine)
  • phase II = reversed by AChEi

128

Methotrexate SE

  • stomatitis = painful mouth ulcers
  • hepatotoxicity = hepatitis, fibrosis, cirrhosis
  • myelosuppression ==> increased infection risk
  • B-cell lymphomas
  • pulmonary fibrosis
  • contraindicated in pregnancy

129

Terbanifine: MOA

  • inhibits squalene oxidase ==> inhibition of fungal wall formation
  • use = dermatophytoses; e.g. tinea corporis

130

Fluoroquinolones: MOA

  • bactericidal
  • inhibit DNA topoisomerase activity

131

Fluoroquinolones: adverse effects

  • GI upset
  • damage to cartilage @ children
  • tendinitis/tendon rupture in adults
  • mild
    • H/A
    • dizziness
    • rash

132

Aminoglycosides: MOA

  • bactericidal
  • block bacterial protein synthesis through inhibition of 30S ribosomal unit

133

Aminoglycosides: adverse effects

  • nephrotoxicity
  • ototoxicity

134

Macrolides: MOA

  • bacteriostatic
  • blocks protein syntehesis at 50S ribosomal unti

135

Macrolides: adverse effects

  • GI discomfort
  • acute cholestatic hepatitis
  • eosinophilia
  • skin rashes
  • more severe
    • pseudomembranous colitis
    • ventricular arrhythmias

136

Tetracyclines: MOA

  • bacteriostatic agents
  • block protein synthesis by actin at 30S ribosomal subunit

137

Tetracyclines: adverse effects

  • GI distress
  • tooth discoloration
  • inhibition of bone growth @ children
  • photosensitivity rxns
  • more severe
    • bacterial superinfection
    • hepatotoxicity

138

Trimethoprim-sulfamethoxazole: MOA

  • trimethoprim-sulfamethoxazole
    • MOA = inhibitis bacterial folate synthesis via inhibition:
    • dihydropteroate synthetase (trimetho) and dihydrofolate reductase (sulfa)

139

Penicillins: MOA

  • bactericidal
  • inhibition of cell wall synthesis via inhibition of cross-linking of peptidoglycan

140

Cisplatin: MOA, SE

  • MOA: reactive oxygen species ==> DNA crosslinks
  • SE
    • nephrotoxicity: acute tubular injury
      • antidote/prevention = amifostine + IV normal saline (chloride diuresis)
        • thiol-based cytoprotective free-radical scavenging agent
        • ==> decreased nephrotox

141

Argatroban: MOA, use, similar drugs

  • binds thrombin active site ==> direct thrombin inhibition
  • ues = HIT
  • other drugs
    • hirudin
    • lepirudin

142

Anastrozole: MOA, use

  • MOA: aromatase inhibitor ==> inhibition of estrogen synthesis
  • use: metastatic breast cancer

Decks in USMLE Step 1 Class (97):