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Flashcards in Pharmacology Deck (87):
1

Km

inversely related to the affinity of the enzyme for its substrate

2

Vmax

directly proportional to the enzyme concentration

3

Line-weaver burk plot

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

4

Volume of distribution

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

5

half life

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

6

zero vs. first order elimination

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

7

weak acid drugs and urine pH

- phenobarb, methotrexate, aspirin
- trapped in basic environment, treat overdose with bicarb

8

weak base drugs and urine pH

- amphetamines
- trapped in acidic environment, treat overdose with ammonium chloride

9

therapeutic index

TD50/ED50
median toxic dose/median effective dose

10

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

- Ach at nicotinic receptor at ganglion
- Ach at muscarnic receptor at tissue

11

sympathetic innervation of sweat glands

- Ach at nicotinic receptor at ganglion
- Ach at muscarinic receptor at tissue

12

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

- Ach at nicotinic receptor at ganglion
- NE at alpha/beta receptor at tissue

13

sympathetic innervation of renal vasculature and smooth muscle

- Ach at N receptor at ganglion
- Dopamine at D1 receptor at tissue

14

sympathetic innervation of adrenal medulla

- Ach at N receptors stimulates it to release Epi and NE

15

somatic innervation of skeletal muscle

- Ach directly at N receptors at tissue

16

alpha1 receptor

- Gq receptor
- inc vascular smooth muscle contraction, inc pupillary dilator contraction, inc intestinal and bladder sphincter muscle contraction

17

a2 receptor

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

18

b1 receptor

- Gs receptor
- inc HR, contractilty, renin release, lipolysis

19

b2 receptor

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

20

M1 receptor

- Gq receptor
- CNS, enteric nervous system

21

M2 receptor

- Gi receptor
- decreased HR and contractility of atria

22

M3 receptor

- Gq receptor
- inc exocrine gland secretions, inc gut peristalsis, inc bladder contraction, bronchoconstriction, inc pupillary sphincter muscle contraction, ciliary muscle contraction

23

D1 receptor

- Gs receptor
- relaxes renal vascular smooth muscle

24

D2 receptor

- Gi receptor
- modulates transmitter release, esp in brain

25

H1 receptor

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

26

H2 receptor

-Gs receptor
- inc gastric acid secretion

27

V1 receptor

- Gq receptor
- inc vascular smooth muscle contraction

28

V2 receptor

- Gs receptor
- inc H20 permability and resorption in the collecting tubules of the kidney
-V2 is found in the 2 kidneys

29

which receptors are paired with which G proteins

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

30

bethanecol

- 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"

31

carbachol

- cholinomimetic agent used for glaucoma, pupillary constriction, and relief of intraocular pressure
- "CARBon copy of AcetylCHOLine"

32

pilocarpine

potent stimulator of sweat, tears and saliva
- used for open and closed angle glaucoma
- "you cry, drool and sweat on your PILOw"

33

neostigmine

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

34

pyridostigmine

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

35

physostigmine

- anticholinergic tox (crosses BBB)

36

donepezil, rivastigmine, galantamine

Alzheimers
- inc endogenous Ach

37

edrophonium

- diagnosis of MG
- increases endogenous Ach

38

cholinesterase inhibitor poisoning (organophosphates)

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

39

atropine, homatripine, tropicamide

muscarinic antagonists that act on the eye
- produce mydriasis and cycloplegia

40

benztropine

- muscarinic antagonist that acts on the CNS
- parkinson's disease/pyramidal SE of psych meds

41

scopolamine

- muscarinic antagonist that acts on the CNS
- motion sickness

42

oxybutynin

- muscarinic antagonist that acts on GU
- reduces urgency

43

glycopyrrolate

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

44

atropine

- 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

epinephrine

- 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

norepi

- alpha1 > alpha2 > beta1
- hypotension (but dec renal perfusion)

47

isoproterenol

- B1 = B2
- electrophysiologic eval of tachyarrhythmias, can worsen ischemia

48

dopamine

- D1 = D2 > beta > alpha
- unstable bradycardia, HF, shock, inotropic and chronotropic alpha effects predominate at high doses

49

dobutamine

- B1 > B2, alpha
- heart failure (inotropic > chronotropic), cardiac stress testing

50

phenylephrine

alpha1 > alpha2
- hypotension, ocular procedures, rhinitis
- if alpha blockers given before, no pressor effect

51

albuterol, salmeterol, terbutaline

- B2 > B1
- asthma, COPD control, and reduce uterine contractions, respectively

52

amphetamine

-indirect general sympathomimetic, reuptake inhibitor, also releases stored catecholamines
- applications in narcolepsy, obesity, ADD

53

ephedrine

- indirect general sympathomimetic, releases stored catecholamines
- used for nasal decongestion, urinary incontinence, and hypotension

54

cocaine

- indirect general sympathomimetic, reuptake inhibitor
- vasoconstriction and local anesthesia

55

clonidine

- a2 agonist for hypertensive urgency, ADHD, severe pain
- tox: CNS depression, bradycardia, hypotension, respiratory depression and small pupils

56

methyldopa

- HTN in preggos
- tox: direct coombs +, SLE-like syndrome

57

phenoxybenzamine

irreverible nonselective alpha blocker
- used to treat pheo
- tox: orthostatic hypotension, reflex tachy

58

phentolamine

reversible nonselective alpha blocker
- give to pts on MAOis who eat foods with tyramine

59

prazosin, terazosin, doxazosin, tamsulosin

selective alpha 1 blockers used for BPH
- prazosin for PTSD
- tox: 1st dose orthostatic hypotension, dizziness, headache

60

mirtazepine

selective alpha 2 blocker for depression
- increases sedation, serum cholesterol and appetite

61

b1 selective beta blockers

- acebutolol, atenolol, betaxolol, esmolol, metoprolol
- A--> M (1st half of alphabet)

62

non-selective beta blockers

nadolol, pindolol, propranolol, timolol
- N to Z, second half of alphabet

63

non-selective alpha and beta antagonists

cavedilol and labetalol
(dont end in the typical olol)

64

antimuscarinic OD treatment

physostigmine salicylate, control hyperthermia

65

AchE inhibitors, organophosphate OD treatment

atropine followed by pralidoxime

66

copper, arsenic, gold OD treatment

penicillamine

67

digitalis OD treamtnet

anti-dig Fav fragments

68

cyanide OD treatment

nitrite + thiosulfate, hydroxocobalamin

69

iron OD treatment

deferoxamine, deferasirox

70

lead OD treatment

EDTA, dimercaprol, succimer, penicillamine

71

methanol, ethylene glycol poisoning

fomepizole > ethanol, dialysis

72

tPA, streptokinase, urokinase OD treatment

aminocaproic acid

73

drugs that cause flushing

VANC
- vancomycin, adenosine, niacin, Ca channel blockers

74

drugs that cause hyperglycemia

Taking Pills Necessitates Having Blood Checked
- tacrolimus, protease inhibitors, niacin, HCTZ, B blockers, corticosteroids

75

drugs that cause hypothyroidism

lithium, amiodarone, sulfonamides

76

drugs that cause hepatic necrosis

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

77

drugs that cause agranulocytosis

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

78

drugs that cause hemolysis in G6PD

hemolysis IS D PAIN
- INH, sulfonamides, dapsone, primaquine, aspirin, ibuprofen, nitrofurantoin

79

drugs that cause photosensitivity

SAT For Photo
- sulfonamides, amiodarone, tetracyclines, 5FU

80

SLE-like syndrome

-having lupus is "SHIPP-E"
- sulfa drugs, hydralazine, INH, procainamide, phenytoin, entanercept"
- also methyldopa

81

drugs that cause seizures

with seizures, I BITE My arm
- INH, buproprion, imipenem/cilastatin, tramadol, enflurane, metoclopramide

82

P450 inducers

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

P450 inhibitors

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

P450 substrates

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

85

sulfa drugs

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

86

Clearance calc

CL = rate of elimination/plasma drug conc
= Vd x Ke

87

dosage calculations

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

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