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Flashcards in 3/15 pharm Deck (111):
1

Clearance can be impaired w/defects in which systems?

cardiac, renal, hepatic.

2

Clearance
-equation:

Cl = (rate of elim of drug)/(plasma drug conc.)
Cl = (Vd)*(Ke)
Cl = (Q)*(Er)

Q = flow to that organ (ie. liver)
Er = extraction ratio

3

Loading dose
-equation

Loading dose = (Cp)(Vd) / (F)

Cp = target plasma concentration at steady state
F = bioavailability

4

Maintenance dose (MD)
-equation

MD = (Cp)(Cl)(t) / F

t = dosage interval (time between doses), if not administered continuously.
*If continuous, leave t out. You will also know its IV so F = 1. B/c only IV is continuous.

5

In liver or renal disease, does maintenance dose inc. or dec.?

Dec.
-less being cleared, so less dose needed.

6

Which drugs follow zero-order elimination?
-mnemonic?

-Phenytoin, Ethanol, and Aspirin (at high or toxic concentrations).

-PEA. (A pea is round, shaped like the “0” in
“zero-order.”)

7

Capacity-limited elimination
-0 or 1st order?

0 order elim.

8

Flow-dependent elimination
-0 or 1st order?

1st order elim.

9

Phase I drug metabolism

P450 system
-Reduction, oxidation, hydrolysis.

10

Phase II drug metabolism

Conjugation (Glucuronidation, Acetylation, Sulfation)

11

Which is most common P450 enzyme?

CYP3A4 = most common

12

Name 3 drugs that might cause trouble in a slow acetylator.
-which would also have a bimodal pop. distribution.

-hydralazine, isoniazid, procainamade

*HIP: its not hip to be a slow acetylator.

13

What kind of antagonist is ketamine?

-ketamine (noncompetitive antagonist) on NMDA receptors.

14

Therapeutic index:
-equation:

TI = Toxic dose/Effective dose
*high therapeutic index is good b/c that means theres a big difference btwn toxic and effective doses.

15

Whats good, a high or low therapeutic index?

High.
-Safer drugs have higher TI values.

16

Is the therapeutic index the same as therapeutic window?

No, b/c the therapeutic window would never extend all the way until the toxic dose.

17

Some receptors that respond to autonomic neurotrasmitters/drugs receive NO nerve innervation (must get ligand through blood).
-can you name these uninnervated autonomic receptors?

-muscarinic receptors on endothelium of blood vessels
-adrenoreceptors on apocrine sweat glands
-alpha-2 and beta adrenoreceptors in blood vessels.

18

para/pre, sym/pre: all release what?

ACh

19

All ganglia have what type of receptor?

Nicotinic: ligand-gated ion channels.

20

Do all sym/post release NE?

NO
-adrenal medulla releases NE and epi.
-sym/post release ACh that innervate sweat glands & piloerector muscles. These = sympathetic cholinergic.

21

sympathetic cholinergic

sym/post that releases ACh
-innervate sweat glands & piloerector muscles.

22

All glands have what receptors on them?

muscarinic
-even sweat glands that have sym/post innervation: these sym/posts dump ACh, not NE (sympathetic cholinergic).

23

adrenal medulla & sweat glands = part of sym nervous system but are innervated by _______ fibers.

cholinergic

24

Nicotinic ACh receptors
-what type of receptor is it?

-ligand-gated Na/K channels.

25

which receptors are more sensitive to activation, alpha or beta?

beta

26

Epi: acting more on alpha1 or beta2?
-low dose =
-high dose =

-low dose - acts more on beta-2
-high dose - acts more on alpha-1

*remember, beta-receptors are more sensitive.

27

Ciliary muscle innervation:

-muscarinic
-its NOT dual innervated.

*if there is an effect on accomodation, its a muscarinic (agonist or antagonist) drug

28

Cycloplega = what is it, what can cause it?

paralysis of ciliary muscles = M-antagonist

29

Gs => inc. cAMP => PKA => phosphorylates MLC kinase.
-whats the result?

smooth muscle relaxation
-hence beta-2 (Gs) causing smooth muscle relaxation in lungs.

30

Hemicholinium
-mech:
-use:

-Prevents reuptake of choline so you have less in nerve terminal so you make less ACh and release less ACh.
*NO CLINICAL USE.

31

NMJ
-what kind of receptor?

nicotinic, ACh.

32

Reserpine

-inhibit vesicular monoamine transporter (VMAT); limit dopamine vesicle packaging and release.

*used in huntingtons.

33

guanethidine

-like botulinum but for NE.
*not clinically used

34

Where do you find AChE?

-AChE is only found in the synpatic cleft.
-Not everywhere you find a M or N receptor.

*that means AChE inhibitor can not vasodilate b/c endothelial cell M3 receptors are not innervated = no synaptic cleft.

35

Can AChE inhibitors vasodilate?

-AChE is only found in the synpatic cleft.
-Not everywhere you find a M or N receptor.

*that means AChE inhibitor can not vasodilate b/c endothelial cell M3 receptors are not innervated = no synaptic cleft.

36

M agonists
-give pattern of what type of lung disease?

-obstructive, like COPD.

37

What an effect you can see via cholinomimetic drugs that you dont see w/parasym. nerve stimulation?

sweating
-b/c sweat glands have sym innervation but release ACh at the sweat glands M3 receptor.

38

Is bethanechol resistant or sensitive to AChE?

-resistant to AChE.
-not the same exact structure as ACh so its not broken down by AChE!

39

Someone at movie and gets intense pain in their eyes.

-They're in a dark room, their pupils dilate, the angle gets smaller, and this precipitates their glaucoma

40

Administer _______ to Cystic Fibrosis pt to get sweat so you can do sweat test

pilocarpine

41

Pilocarpine is resistant or sensitive to AChE?

resistant, just like bethanechol.
-not exactly the same structure as ACh so AChE doesn't break it down.

42

myasthenic crisis

not enough ACh

43

cholinergic crisis

too much ACh
-can resemble myasthenic crisis

44

Which receptors do AChE inhibitors act at?

muscarinic & nicotinic

45

atropine OD
-which AChE inhibtor can you give?

-physostigmine bc atropine gets into CNS and so does physostigmine.
*physostigmine = a tertiary amine = not charged, lipid soluble.

46

Myasthenia Gravis
-how was it historically Dx?
-how is it Dx now?

-historically: edrophonium.
-Myasthenia now diagnosed by anti-AChR Ab (anti-
acetylcholine receptor antibody) test.

47

What to watch out for before giving cholinomimetic?

COPD, asthma, peptic ulcers.

48

parathion

organophosphate
-irreversible AChE inhibtor.

49

sarin

organophosphate
-irreversible AChE inhibtor.

*nerve gas

50

organophosphate poisoning
-Tx:

-atropine (competitive inhibitor) + pralidoxime (regenerates AChE if given early).

51

why isn't atropine enough for organophosphate poisoning tx?

Atropine is a muscarinic antagonist.
-it is NOT a nicotinic antagonist!
-Nicotinic toxicity is treated by regenerating active cholinesterase w/pralidoxime.

52

Which one gets desensitized, muscarinic or nicotinic?

nicotinic
-muscarinic does NOT get desensitized.
*succinylcholine acts on nicotinic.

53

Glycopyrrolate
-mech:
-use:

muscarinic antagonist
-Parenteral: preoperative use to reduce airway secretions.
-Oral: drooling, peptic ulcer.

54

Atropine
-uses:

Used to treat bradycardia & for ophthalmic applications.

55

ACh
-its excitation of skeletal muscle & CNS mediated via which receptor?

nicotinic

56

Jimson weed
-what effects?

-atropine poisoning if you consume Jimson weed.
-aka Belladonna alkaloids.

57

hexamethonium, mecamylamine
-what are they?
-use?

-nicotinic (ganglion) blockers
-They will be used in problems b/c they block baroreflex changes in heart rate.
-If you use these you WIPE OUT the ANS, b/c all ganglia use Nn receptors.
*just remember what the predominant tone on the system is at rest, and cancel out that tone.

58

What resting tone does our heart have?

PARA

59

Epi
-low dose effects:

-B/c beta receptors are more sensitive, you will get primarily a beta response with a low dose of epi.
-THIS IS KEY. At low dose acts like isoproterinol (nonselective beta agonist).

60

Epi
-medium dose

-alpha-1 gets involved.
*alpha-1 and beta-2 antagonize each other.
-so at medium dose epi looks like a beta-1 agonist. (like DOPUTAMINE, a selective beta-1 agonist)

61

Epi
-high dose

-alpha-1 will PREDOMINATE.
-You will vasoconstrict and get inc. BP.
-You will get tachy OR reflex brady. This looks just like NE.

*you can not distinguish NE and high dose EPI in cardiac parameters.

62

NE vs high dose epi.
-differences:

-If it bronchodilates, inc. lipolysis, inc. glycogenolysis, or inc. gluconeogenesis; then it MUST be EPI,
-beta-2 does these things and NE does NOT act on beta-2.

63

How do you unmask beta-2 action of epi?

-give an alpha-1 blocker.
-alpha 1 is opposing beta-2.

64

Can NE, under any circumstances, reduce BP?

NO

65

Can epi, under any circumstances, reduce BP?

Yes, but only at low dose where beta-2 is activated but alpha-1 is not.

66

Isoproterenol
-what does it do to pulse pressure?

nonselective beta-agonist.
-inc inotropy = inc systolic.
-inc vasodilation = dec diastolic
*inc. pulse pressure.

67

cardiac stress testing
-which drug is used?

dobutamine

68

terbutaline
-mech:
-use:

-beta-2 agonist
-reduce premature uterine contractions

69

beta agonist
-can they cause hypo or hyperkalemia?

hypokalemia
-inc activity of Na/K pump which brings K into cells.

70

name some mobile pool releasers

tyramine, amphetamine, ephedrine.

71

Ephedrine
-mech:
-use:

-releases stored catecholamines.
-Nasal decongestion, urinary incontinence, hypotension.

72

Cocaine intox
-should you give beta-blockers?

-No.
-you never want to risk having unopposed alpha-1 action by blocking beta-2.
-can get hypertensive crisis.

73

amphetamine & cocaine
-predominantly the inc. in which chemical leads to addiction?

dopamine

74

Clonidine
-uses

-ADHD, severe pain, and a variety of off-label indications (e.g., ethanol and opioid withdrawal).

75

Whats the only anti-HTN drug w/approved analgesic use?

clonidine

76

phentolamine vs phenoxybenzamine
-which one is irreversible?

phenoxybenzamine = irreversible
-both =nonselective alpha blockers

77

Give ________ to patients on MAO inhibitors who eat
tyramine-containing foods

phentolamine

78

Can tamulosin also be used for HTN like other alpha-1 blockers?

-No, tamulosin more specific for smooth muscle in urinary tract.

79

Mirtazapine
-mech:
-use:
-s/e:

-alpha-2 blocker
-depression
-inc appetite, inc serum cholesterol, sedation.

80

Beta-blocker OD
-tx:

glucagon
-beta-1 & beta-2 both = Gs, they inc. cAMP.
-glucagon also = Gs, so it inc. cAMP as well.

81

beta-blockers
-can you use in a diabetic?

-Despite theoretical concern of masking hypoglycemia in diabetics, benefits likely outweigh risks; not contraindicated

82

beat-blocker
-s/e:

-Impotence
-CV adverse effects
-CNS adverse effects (seizures, sedation, sleep alterations)
-dyslipidemia (metoprolol)
-asthmatics/COPDers (may cause exacerbation)

83

beta-1 selective blockers
-mnemonic?

A to M

84

non-selective beta-blockers
-mnemonic?

N to Z

85

pindolol
-why is it better to use in asthmatics?

-partial non-selective agonist.
-it will also have some sympathetic effects, like slightly bronchodilating for instance.

86

beta-blockers
-which ones are non-selective ALPHA & beta blockers?

-carvedilol, labetalol

*dont end w/"olol".

87

Nebivolol
-what is unique about it?

Nebivolol combines cardiac-selective β1-adrenergic blockade with stimulation of β3-receptors, which activate nitric oxide synthase in the vasculature.

88

Which drugs can cause cutaneous flushing?
-mnemonic?

VANC
-Vancomycin, Adenosine, Niacin, Ca2+ channel
blockers.

89

Which drugs can cause Hyperglycemia?
-mnemonic?

Taking Pills Necessitates Having Blood Checked
-Tacrolimus
-Protease inhibitors
-Niacin
-HCTZ
-β-blockers
-Corticosteroids

90

Which drugs can cause hypothyroidism?

Lithium, amiodarone, sulfonamides

91

Which drugs can cause diarrhea?
-mnemonic?

Might Excite Colon On Accident
-Metformin
-Erythromycin
-Colchicine
-Orlistat
-Acarbose

92

Lanugo
-what is it?
-what disease is it seen in?

Fine body hair
-anorexia nervosa

93

Parotitis
-bulimia or anorexia?

Both
-there is binge/purge type of anorexia.

94

Does calcium bind troponin or tropomyosin?

-troponin C

95

Prominent U wave
-hypo or hyperkalemia?

hypokalemia

96

what happens to haptoglobin-Hb complex?

its hepatically cleared

97

Winged scapula
-common causes?

-mastectomy surgery & accidentally nick the long thoracic nerve.
-stab wounds.

98

clavicular fx
-where in clavicle?

middle 1/3

99

ACL & PCL
-connect which two bones?

tibia & femur

100

ACL & PCL
-which one more commonly injured?

ACL

101

ACL or PCL
-which one attaches to medial condyle of femur?

PCL
*anterior lateral surface of medial epicondyle of femur.

102

ACL or PCL
-which one attaches to the lateral condyle of femur?

ACL
*post. medial lateral femoral condyle.

103

Where on femur does PCL attach?

medial condyle of femur.

104

Where on femur does ACL attach?

lateral condyle of femur.

105

Septic arthritis
-usually due to what?
-how do u treat it?

gonococcus
-ceftriaxone

106

How does colchicine reduce acute inflammation of gouty arthritis?

inhibits neutrophil migration into inflamed areas.

107

Which vitamin D is created upon exposure to sun?

D3 = cholecalciferol

108

Major cause of morbidity in sarcoidodis?

pulm. fibrosis.

109

medial or lateral cruciate ligament attached to its corresponding meniscus?

MCL.

110

Ligation of sup. thyroid art:
-which nerve at risk?

-external branch of superior laryngeal n.

111

Ligation of inf. thyroid art:
-which nerve at risk?

-recurrent laryngeal n.