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Step 1 Flash Cards > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Km

A

inversely related to the affinity of the enzyme for its substrate

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2
Q

Vmax

A

directly proportional to the enzyme concentration

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3
Q

Line-weaver burk plot

A

X intercept = 1/-Km
Y intercept = 1/Vmax
slope = Km/Vmax

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4
Q

Volume of distribution

A

Vd = amount of drug in body/ plasma concentration

- Vd low if drug is in the blood only, med if in the interstitial space, and high if in all tissues including fat

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5
Q

half life

A
  • drugs infused at a constant rate take 4-5 HL to reach steady state
  • takes 3.3 HL to reach 90% steady state levels
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6
Q

zero vs. first order elimination

A
  • zero = constant amount cleared per unit time
  • PEA - phenytoin, ethanol, aspirin
  • first = constant fraction cleared per unit time
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7
Q

weak acid drugs and urine pH

A
  • phenobarb, methotrexate, aspirin

- trapped in basic environment, treat overdose with bicarb

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8
Q

weak base drugs and urine pH

A
  • amphetamines

- trapped in acidic environment, treat overdose with ammonium chloride

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9
Q

therapeutic index

A

TD50/ED50

median toxic dose/median effective dose

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10
Q

parasympathetic innervation of cardiac smooth muscle, gland cells and nerve terminals

A
  • Ach at nicotinic receptor at ganglion

- Ach at muscarnic receptor at tissue

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11
Q

sympathetic innervation of sweat glands

A
  • Ach at nicotinic receptor at ganglion

- Ach at muscarinic receptor at tissue

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12
Q

sympathetic innervation of cardiac smooth muscle, gland cells and nerve terminals

A
  • Ach at nicotinic receptor at ganglion

- NE at alpha/beta receptor at tissue

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13
Q

sympathetic innervation of renal vasculature and smooth muscle

A
  • Ach at N receptor at ganglion

- Dopamine at D1 receptor at tissue

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14
Q

sympathetic innervation of adrenal medulla

A
  • Ach at N receptors stimulates it to release Epi and NE
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15
Q

somatic innervation of skeletal muscle

A
  • Ach directly at N receptors at tissue
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16
Q

alpha1 receptor

A
  • Gq receptor
  • inc vascular smooth muscle contraction, inc pupillary dilator contraction, inc intestinal and bladder sphincter muscle contraction
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17
Q

a2 receptor

A
  • Gi receptor

- decreases sympathetic outflow, dec insulin release, dec lipolysis, inc platelet aggregation

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18
Q

b1 receptor

A
  • Gs receptor

- inc HR, contractilty, renin release, lipolysis

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19
Q

b2 receptor

A
  • Gs receptor
  • vasodilation, bronchodilation, inc HR, contractility, lipolysis, insulin release
  • decreased uterine tone, ciliary muscle releaxation, inc aqueous humor production
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20
Q

M1 receptor

A
  • Gq receptor

- CNS, enteric nervous system

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21
Q

M2 receptor

A
  • Gi receptor

- decreased HR and contractility of atria

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22
Q

M3 receptor

A
  • Gq receptor
  • inc exocrine gland secretions, inc gut peristalsis, inc bladder contraction, bronchoconstriction, inc pupillary sphincter muscle contraction, ciliary muscle contraction
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23
Q

D1 receptor

A
  • Gs receptor

- relaxes renal vascular smooth muscle

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24
Q

D2 receptor

A
  • Gi receptor

- modulates transmitter release, esp in brain

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25
Q

H1 receptor

A
  • Gq receptor

- inc nasal and bronchial mucus production, inc vascular permeability, contraction of bronchioles, pruritis and pain

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26
Q

H2 receptor

A
  • Gs receptor

- inc gastric acid secretion

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27
Q

V1 receptor

A
  • Gq receptor

- inc vascular smooth muscle contraction

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28
Q

V2 receptor

A
  • Gs receptor
  • inc H20 permability and resorption in the collecting tubules of the kidney
  • V2 is found in the 2 kidneys
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29
Q

which receptors are paired with which G proteins

A 
HAVE 1 M and M --- Gq
- H2, a1, V1, M1 and M3
MAD 2s ----- Gi
- M2, a2, D2
all the rest work on Gs
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30
Q

bethanecol

A
  • cholinomimetic drug used for post op ileus, neurogenic ileus and urinary retention
  • activates Bowel and Bladder smooth muscle, resistant to AchE
  • “bethany call me maybe if you want to move your bowel or bladder”
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31
Q

carbachol

A
  • cholinomimetic agent used for glaucoma, pupillary constriction, and relief of intraocular pressure
  • “CARBon copy of AcetylCHOLine”
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32
Q

pilocarpine

A

potent stimulator of sweat, tears and saliva

  • used for open and closed angle glaucoma
  • “you cry, drool and sweat on your PILOw”
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33
Q

neostigmine

A
  • postop and neurogenic ileus and urinary retention, myasthenia gravis, reversal of NMJ blockade
  • inc endogenous Ach
  • Neo = No CNS penetration
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34
Q

pyridostigmine

A

-myasthenia gravis (long acting), does not penetrate the CNS

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35
Q

physostigmine

A
  • anticholinergic tox (crosses BBB)
36
Q

donepezil, rivastigmine, galantamine

A

Alzheimers

- inc endogenous Ach

37
Q

edrophonium

A
  • diagnosis of MG

- increases endogenous Ach

38
Q

cholinesterase inhibitor poisoning (organophosphates)

A

DUMBBELSS
- diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle and CNS, Lacrimation, Sweating, Salivation

39
Q

atropine, homatripine, tropicamide

A

muscarinic antagonists that act on the eye

- produce mydriasis and cycloplegia

40
Q

benztropine

A
  • muscarinic antagonist that acts on the CNS

- parkinson’s disease/pyramidal SE of psych meds

41
Q

scopolamine

A
  • muscarinic antagonist that acts on the CNS

- motion sickness

42
Q

oxybutynin

A
  • muscarinic antagonist that acts on GU

- reduces urgency

43
Q

glycopyrrolate

A
  • muscarinic antagonist that acts on GI and resp
  • parenteral: preop use to reduce airway secretions
  • oral: drooling, peptic ulcer
44
Q

atropine

A
  • muscarinic antagonist. used to treat bradycardia and for ophthalmic applications
  • inc pupil dilation, dec airway secretions, dec acid secretion, dec GI motility, dec urgency in cystitis (blocks DUMBBELSS)
  • tox: hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter
45
Q

epinephrine

A
  • beta > alpha
  • anaphylaxis, open angle glaucoma, asthma, hypotension, alpha effects predominate at high doses
  • inc HR, SBP, dec DBP at low doses, inc DBP at high doses
  • if alpha blockers given before, net depressor effect
46
Q

norepi

A
  • alpha1 > alpha2 > beta1

- hypotension (but dec renal perfusion)

47
Q

isoproterenol

A
  • B1 = B2

- electrophysiologic eval of tachyarrhythmias, can worsen ischemia

48
Q

dopamine

A
  • D1 = D2 > beta > alpha

- unstable bradycardia, HF, shock, inotropic and chronotropic alpha effects predominate at high doses

49
Q

dobutamine

A
  • B1 > B2, alpha

- heart failure (inotropic > chronotropic), cardiac stress testing

50
Q

phenylephrine

A

alpha1 > alpha2

  • hypotension, ocular procedures, rhinitis
  • if alpha blockers given before, no pressor effect
51
Q

albuterol, salmeterol, terbutaline

A
  • B2 > B1

- asthma, COPD control, and reduce uterine contractions, respectively

52
Q

amphetamine

A
  • indirect general sympathomimetic, reuptake inhibitor, also releases stored catecholamines
  • applications in narcolepsy, obesity, ADD
53
Q

ephedrine

A
  • indirect general sympathomimetic, releases stored catecholamines
  • used for nasal decongestion, urinary incontinence, and hypotension
54
Q

cocaine

A
  • indirect general sympathomimetic, reuptake inhibitor

- vasoconstriction and local anesthesia

55
Q

clonidine

A
  • a2 agonist for hypertensive urgency, ADHD, severe pain

- tox: CNS depression, bradycardia, hypotension, respiratory depression and small pupils

56
Q

methyldopa

A
  • HTN in preggos

- tox: direct coombs +, SLE-like syndrome

57
Q

phenoxybenzamine

A

irreverible nonselective alpha blocker

  • used to treat pheo
  • tox: orthostatic hypotension, reflex tachy
58
Q

phentolamine

A

reversible nonselective alpha blocker

- give to pts on MAOis who eat foods with tyramine

59
Q

prazosin, terazosin, doxazosin, tamsulosin

A

selective alpha 1 blockers used for BPH

  • prazosin for PTSD
  • tox: 1st dose orthostatic hypotension, dizziness, headache
60
Q

mirtazepine

A

selective alpha 2 blocker for depression

- increases sedation, serum cholesterol and appetite

61
Q

b1 selective beta blockers

A
  • acebutolol, atenolol, betaxolol, esmolol, metoprolol

- A–> M (1st half of alphabet)

62
Q

non-selective beta blockers

A

nadolol, pindolol, propranolol, timolol

- N to Z, second half of alphabet

63
Q

non-selective alpha and beta antagonists

A

cavedilol and labetalol

dont end in the typical olol

64
Q

antimuscarinic OD treatment

A

physostigmine salicylate, control hyperthermia

65
Q

AchE inhibitors, organophosphate OD treatment

A

atropine followed by pralidoxime

66
Q

copper, arsenic, gold OD treatment

A

penicillamine

67
Q

digitalis OD treamtnet

A

anti-dig Fav fragments

68
Q

cyanide OD treatment

A

nitrite + thiosulfate, hydroxocobalamin

69
Q

iron OD treatment

A

deferoxamine, deferasirox

70
Q

lead OD treatment

A

EDTA, dimercaprol, succimer, penicillamine

71
Q

methanol, ethylene glycol poisoning

A

fomepizole > ethanol, dialysis

72
Q

tPA, streptokinase, urokinase OD treatment

A

aminocaproic acid

73
Q

drugs that cause flushing

A

VANC

- vancomycin, adenosine, niacin, Ca channel blockers

74
Q

drugs that cause hyperglycemia

A

Taking Pills Necessitates Having Blood Checked

- tacrolimus, protease inhibitors, niacin, HCTZ, B blockers, corticosteroids

75
Q

drugs that cause hypothyroidism

A

lithium, amiodarone, sulfonamides

76
Q

drugs that cause hepatic necrosis

A

Liver “HAVAc”

- halothane, Amanita phalloides (death cap mushroom), Valproic acid, Acetaminophen

77
Q

drugs that cause agranulocytosis

A

Dapsone, Clozapine, Carbamezapine, Colchicine, Methimazole, Propylthiouracil
- Drugs CCCrush Myeloblasts and Promyelocytes

78
Q

drugs that cause hemolysis in G6PD

A

hemolysis IS D PAIN

- INH, sulfonamides, dapsone, primaquine, aspirin, ibuprofen, nitrofurantoin

79
Q

drugs that cause photosensitivity

A

SAT For Photo

- sulfonamides, amiodarone, tetracyclines, 5FU

80
Q

SLE-like syndrome

A
  • having lupus is “SHIPP-E”
  • sulfa drugs, hydralazine, INH, procainamide, phenytoin, entanercept”
  • also methyldopa
81
Q

drugs that cause seizures

A

with seizures, I BITE My arm

- INH, buproprion, imipenem/cilastatin, tramadol, enflurane, metoclopramide

82
Q

P450 inducers

A

Chronic Alcoholic Mona Steals Phen-Phen and Never Refuses Greasy Carbs

  • chronic alcohol use
  • modafinil
  • St. John’s wart
  • phenytoin
  • phenobarb
  • Nevirapine
  • Rifampin
  • Griseofulvin
  • Carbamezapine
83
Q

P450 inhibitors

A 
A cute Gentleman "Cipps" Iced Grapefruit juice Quickly and Kept Munching on Soft Cinammon Rolls
acute alcohol abuse
gembifrozil
cipro
isoniazid
grapefruit juiice
quinidine
amiodarone
ketoconazole
macrolides
sulfonamides
cimetidine
ritonavir
84
Q

P450 substrates

A

anti-epileptics, antidepressants, antipsychotics, anesthetics, theophylline, warfarin, statins, OCPs
– Always, Always, Always, Always Think When Starting Others

85
Q

sulfa drugs

A

Popular FACTSSS

- probenecid, furosemide, acetazolamide, celecoxib, thiazides, sulfonamide abx, sulfasalazine, sulfonureas

86
Q

Clearance calc

A

CL = rate of elimination/plasma drug conc

= Vd x Ke

87
Q

dosage calculations

A

loading dose = Cp x Vd / F
maintenance dose = Cp x CL x t / F

Cp = target plasma concentration
t = dosage interval
F = bioavailability

Step 1 Flash Cards (36 decks)

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