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USLME Kiss my ass and pray > Pharm DIT > Flashcards

Pharm DIT Flashcards

1
Q

Parasympathetic Nerves

A

CN 3, 7, 9 ad 10

2nd and 3rd sacral spinal nerves

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2
Q

AChE block due to ?

Antidote?

A

organophosphate poisoning - see excess cholinergic effects

Atropine and pralidoxime

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3
Q

Location of ACh receptors - Nicotinic and muscarinic

A

Nn - parasympathetic pre-ganglia synapse

Nm - neuromuscular junction for somatic transmission

Muscarinic - parasympathetic post ganglia synapse

  • Odd one of muscarinic receptor for sympathetic stimulation of sweat glands
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4
Q

Sympathetic length of preganglionic nerves vs parasympathetic

A

Sympathetic nerves are short pre ganglionic and long post ganglion - pretty much all turn on at once

parasympathetic ganglionic have longer preganglionic neurons -> more selectivity

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5
Q 
Parasympathetic activation -> (9)
GI
Bladder
Eye
Lung
Heart
Lacrimal
Salivary glands
Uterus
Penis/cliterus
A 
GI - increased digestion -> more transit and increased recall sphincter tone
Bladder - wall contraction and relaxed sphincter
Eye - mitosis and ciliary contraction
Heart - decreased HR and contractility
Lung - bronchospasm
Lacrimal gland - stimulates tears
salivary gland - water secretion
Uterus - contracts
Penis - erects
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6
Q

Why choniergic excess not the same as parasympathetic activation?

A

organophosphate poisoning-

Have some nicotinic receptors at the neuromuscular junction that are activated and not parasympathetic

Also have sweat glands w/ muscarinic receptors that are sympathetic innervated

DUMBBELLS

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7
Q

Presentation of ptosis and diplopia that worsens throughout the day is?

Test w/?

Rx?

A

myasthenia Gravis

Edrophonium - tensilon test

Pyridostigmine

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8
Q

Thyectomy might be implicated in this disorder of general weakness

A

Myasthenia gravis

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9
Q

Direct Agonists - Cholimetric (4)

A

-chols

bethanechol - urinary retention or illeus
carbachol - glaucoma
Pilocarbine - salivattion stimulant
Methacholine - asthma test inducer

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10
Q

Old test for asthma

A

methacholine challenge - ACh agonist

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11
Q

Potent stimulator of sweat, tears and saliva

A

pilocarbine

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12
Q

Cholinergic agonist used to treat glaucoma

A

carbachol

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13
Q

Cholinergic used for urinary retention or postoperative ileus

A

Bethanechol

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14
Q

Indirect agonists (anticholinesterases) (6)

A

-stigmines

Neostigmine - reverses neuromuscular blockafe, myasthenia gravis (NO CNS)

pyridiotigmine - myasthenia gravis

edrophonium - short acting

physostigmine - Atropine overdose (CNS action)

Alzeheimer drugs - doneprezil, galantine, rivastigmine

Ecothiophate - open angle glycoma

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15
Q

Alzheimer drugs work by?

3?

A

indirectly increasing the ACh

Doneprezil
rivastigmine
galantamine

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16
Q

Side effects of atropine overdose?

A

muscarinic blockade

hot as a hare - hyperthermia
dry as a bone - decreased secretions
red as a beet - flushing
blind as a bat - cyclopegia (loss of accommodation w/ ciliary muscle)
mad as a hatter - delirium
bloated as a toad - illeus and constipation

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17
Q

Have a elderly patient that has acute onset of delirium look for?

A

Change in medications and addition of an anticholinergic

be wary of anti-muscarinics as well

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18
Q

Anticholinergic Drugs (4)

A 
1st Gen H1
- diphenhydramine
-doxylamine
- chlorpherniramine
Neuroleptics
- thioridazine
-chlopromazine
- clozapine
-olanzapine
Tricyclic antidepressants
Amantidine
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19
Q

Anticholinergics used in Rx of urge incontinence (4)

A

On The Darn Toliet

oxybutynin
tolteridine
Darifenacin/solifenacin
Trospium

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20
Q

Eye dilation short term (3)

A

Homatopine
tropicamide
Cyclopentolate
-act as antimuscarinic

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21
Q

Rx for tremors and rigidity seen w/ Parkinson’s meds

A

Benztropium

anti - muscarinic

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22
Q

Rx for motion sickness and decreases salivation

A

Scopolamine

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23
Q

Anti muscarinic Rx for COPD

A

Ipratropium

Tiotropium

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24
Q

Alpha 1 stim (5)

A

vascular smooth muscle contraction
pupillary dilator contraction -> mydriasis
intestinal and bladder sphincter contraction
increased peripheral resistance (reflex bradycardia)
increase BP

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25
Q

Alpha 2 stim (2)

A

inhibits NE release on presynaptic auto receptor

lowers insulin release acting on pancreatic Beta cells

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26
Q

Beta 1 stim (4)

A

increase HR
Increase contractility
increase in Renin
increase in lipolysis

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27
Q

Beta 2 stim (5)

A 
bronchodialation
vasodilatation (minimal)
increase in HR (secondary)
increase lipolysis
decrease uterine tone - tocolysis
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28
Q

Rx for pheochromocytoma

A

alpha antagonist - nonselective

Phenoxybenzamine

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29
Q

HTN medication in pregnancy

STOP what drug?

A

alpha methydopa

Ace inhibitor

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30
Q

Selective Alpha1 a d blocker used in BPH

A

Tamsulosin

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31
Q

nonselective alpha blockers (2)

A

phenoxybenzamine - irreversible

phentolamine - reversible

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32
Q

Alpha 1 selective blocker ? (3)

USed for

A

HTN and urinary retention w/ BPH

  • zosins
    parazosin
    terazosin
    doxazosin
  • tamsulosin
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33
Q

alpha 1 and Beta 1 blockers (2)

used for

A

carvediol
labetelol

used for slowing the heart and lowering peripheral resistance

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34
Q

Partial beta agonists -> antagonist (2)

Useful for ?

A

acetebutolol
pindolol

useful for HTN w/ bradycardia, NOT for CAD

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35
Q

Nonselective Beta blockers(3)

Worry about using in who?

A

propranolol
nadolol
timolol

do not use in asthma/COPD or emphysema due to loss of beta 2 -> bronchospasm

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36
Q

Selective Beta 1 blockers(3)

A

esmolol
atenolol
metoprolol

37
Q

betal blockers used in glaucoma

A

Opthalmic use
(beta 2 blocking of aqueous humor)
Nadolol
timolol

38
Q

Beta blockers are primarily used for (6)

A 
Angina pectoris (CAD)
HTN
aortic disection
Anxiety
SVT 
Gaucoma (timolol)

Maybe CHF(pulm edema worries), hyperthyroid symptoms, migrane prophylaxis

39
Q

Worrisome Side effects of Beta blockers (3)

A

bradycardia and AV block -> CHF

masking of hypoglycemia in beta blockers

bronchospasm w/ nonselective beta blockers

40
Q

3 enzymes used in the production epinephrine/NE

2 cofactors?

A

-Phenylalanine start
phenylalanine hydroxylase

-tyrosine(brought in w/ Na)
tyrosine hydroxylase (blocked by metyrosine)
-LDOPA
dopamine decarboxylase (w/B6

-NE-> Epi w/ Vitamin C

41
Q

drug inhibiting the packaging of ACh

A

Vesamicol

42
Q

Drug inhibiting the packaging of NE

A

reserpine

43
Q

Natural stimulator for the release of ACh and NE from the presynaptic terminal

A

Ca 2+

44
Q

Black widow spider toxin has what effect on nerve transmission

A

increases the release of ACh leading to spastic paralysis and cholinergic excess

45
Q

What toxin causes flaccid paralysis at the cholinergic junction

A

Botulinism

46
Q

Choline is brought into the cholinergic nerve by what mech?

What inhibits this?

A

Na cotransport brings in

Hemicholinium inhibits

47
Q

Enzyme making ACh

A

choline acetyltransferase combining acetyl Co A and Choline

then packaged in vesicles

48
Q

4 things that can happen to ACh in the synaptic cleft

A

bind to receptor
bind to autoreceptor - presynaptic regulating release
diffuse away
acted on by AChE which lyse into choline(recycled) and Acetyl coA

49
Q

4 things that can happen to NE in the synaptic cleft

A 
Act on Alpha 1, Beta 1 and 2 post synaptic neuron
Act on Alpha 2 prenaptically
Reuptake into presynaptic
Metabolized
- COMT -> methylation
-MAOI - > oxidizes
50
Q

Drugs blocking reuptake of NE in synaptic cleft (2)

A

TCAs and Cocaine

51
Q

4 substances that induce the release of NE in the synaptic cleft

A

Ca - natural
Amphetamine
Tyramine
Ephedrine

52
Q

2 drugs that block NE release

A

Guanethidine

betrylium - Ca channel blocker

53
Q

angiontensin II effect on the presynaptic Noradrenergic neuron

A

leads to increase in NE release

54
Q

Alpha2 and M2 on presynaptic noradrenergic neuron

A

decreases NE release

55
Q

Gq uses what receptors

A

Qc HAVe 1 M&M

Gq uses
H1
alpha1
Vasopressin 1
M1
M3
56
Q

Gi uses what receptors

A

MAD 2s

M2
Alpha 2
D2

57
Q

Gs uses what receptors

A

Leftovers from
Qc HAVe 1 M&M
MAD2s

Beta1
beta2
D1
V2
H2
58
Q

Receptor Gq pathway
4 steps

other way to get this path?

A

phospholipase C

PIP2 from lipids spit to DAG and IP3

DAG -> Protein Kinase C

IP3 -> release Ca (smooth muscle contraction)

Tyrosine Kinase (does the Ras path too)

59
Q

Receptor Gs pathway
2 steps

implicated in what disease?

A

adenylyl cyclase converts ATP ->cAMP

cAMP levels activate protein kinase A

implicated in Cholera

60
Q

Receptor Gi pathway
2 Steps

implicated in what disease

A

BLOCKS adenylyl cyclase from converting ATP ->cAMP

low cAMP levels DO NOT activate protein kinase A

implicated in pertussIs

61
Q

H1 vs H2 stimulation ->

3 vs 1 function

A

nasal and bronchial mucus secretions and contraction of bronchioles and puritus

vs

gastric acid secretion

62
Q

V1 vs V2 stimulation

A

increased smooth muscle contrition (pressor in codes)

vs

increased reabsorption of H2O in the collecting tubules (2 for 2 kidneys)

63
Q

M1 vs M2 vs M3

A

enteric nervous system

decreased HR and contractility (SA node)

increased gland secretion, gut peristalsis, bronchconstriction, bladder contraction, mitosis, ciliary muscle contraction (accommodation)

64
Q

D1 vs D2

A

relaxes the renal vasculature

modulates brain NT

65
Q

Km =

related to?

affected by?

A

amount of substrate needed for 1/2 Vmax

inversely related to affinity. higher affinity -> smaller Km

affected by competitive inhibition

66
Q

Vmax

related to?

Affected by?

A

the maximum rate at which a reaction proceeds

directly relates to enzyme concentration

  • affected by noncompetitive inhibiors
67
Q

Linewaver burk plot

x- axis

Y axis

Slope

A

x axis = 1/-km

y axis = 1/vmax

slope =Km/Vmax

68
Q

Role of Noncompetative inhibitor on

Vmax

Km

As seen on lineweaver

A

Vmax decreases - seen as a higher y intercept

Km does not change - seen at the same point

69
Q

Role of competitive inhibitor on

V max
Km

As seen on lineweaver

A

V max does not change - hits the same y axis

Km increases ( need more substrate to get 1/2 Vmax)

-seen as a x intercept closer to zero

70
Q

Adding an enzyme affects the line weaver plot how?

A

The 1/-Km (x axis does not change)

The y axis (1/Vmax) drops down closer to zero

71
Q

Increasing the affinity of a drug affects the line weaver plot how?

A

The (1/Vmax, y axis, does not change) no added enzyme

The x axis( 1/-Km) shifts to the left,
Higher affinity means a smaller Km

-vs an x axis shift to the right (closer to 0) means more substrate is needed due to lesser affinity (same as giving a competitive inhibitor)

72
Q

drug is infused how long to reach steady state?

A

4-5 half lives to 94% Concentration

73
Q

How would you drop a dose by half if toxic levels seen in a patient?

A

Stop the infusion for one half life

74
Q

Kidney trouble will affect which loading dose and maintenance dose how if renal cleared?

A

No change on loading dose

Decreases maintenance dose

75
Q

efficacy of a drug is?

what can drop efficacy? (2)

A

the MAX EFFECT a drug can produce, related to Vmax. NEED to know max response of a drug to determine efficacy

noncompetitive antagonists and partial agonist

76
Q

potency of a drug is?

what can drop the potency

A

the DOSE of a drug needed to achieve a given effect, inversely related to Km

competetative inhibitors can decrease potency - shift the curve to the right

Partial agonists can have variable effects on potency while always dropping the efficacy

77
Q

Therapeutic Index =

A

LD50/ED50

Lethal dose for 50%/Effective dose for 50%

78
Q

What is better when looking at therapeutic index - high or low value?

ex of poor therapeutic index drugs? (4)

A

High therapeutic index - more dose needed to kill than compared to needed to have therapeutic effect.

Warfarin, lithium, anti-seizure, digoxin

79
Q

Phase 1 metabolism completes the following reactions (3)

to get what metabolites?

A

reduction
oxidation
hydrolysis

slightly polar, water soluble, slightly active(toxic or prodrug active)

80
Q

Phase 2 metabolism completes the following reactions? (4)

to get what metabolites

A

Glucuronidation
acetylation
Sulfation
methylation

Inactive, VERY polar metabolites -> renal excreteted

81
Q

Geriatric patients lose this metabolism 1st?

Cyp 450 is characterized by this metabolism?

A

Phase 1 - reduction/oxidation/sulfation

Phase 1 again

82
Q

Slow acetylators means what?

A

Phase II metabolism is impaired and going to see higher drug levels in patients w/ increased toxicity and side effects

83
Q

2 enzymes in alcohol metabolism and drugs that inhibit them

limiting reagent in both?

A

alcohol dehydrogenase - fomepizole

acetaldehyde dehydrogenase -disulfiram

NAD which picks up the H -> NADH

84
Q

Disulfram like reaction drugs?(4)

A

metronidazole
certain cephalosporins
procarbazine
1st gen sulfaureas (tobutamide)

85
Q

11 drugs that induce Cyp 450

A

CRACK AMIGOS

Cimetidine
Ritonavir = protease inhibitors
Amiodarone
Ciprofloxacin
Ketoconazole
Acute Alcohol
Macrolides
Isoniazid
Grapefruit Juice
Omeprazole
Sulfonamide
86
Q

7 drugs that inhibit Cyp 450

A

Guiness, Coronas, and PBRS induces CHRONIC ALCOHOLISM

Griseofulvin
Carbamazapine
Phenytoin
barbituates
Rifampin
St johns Wart
Chronic Alcoholism
87
Q

ASA overdose how do you clear it?

A

Acidic drugs you want to alkalinize the urine by given NaHCO3

HA -> H + A-
(shifts the formula to the L by taking away Hs) A- is an anion that gets trapped in the urine

88
Q

Amphetamine overdose how do you clear it?

A

Basic drugs you want to acidify the urine by giving NH4Cl

BH+ <- H + B
(shifts the formula to the R by adding more H and trapping the polarized basic drug in the urine

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