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Flashcards in Pharm DIT Deck (88):
1

Parasympathetic Nerves

CN 3, 7, 9 ad 10

2nd and 3rd sacral spinal nerves

2

AChE block due to ?

Antidote?

organophosphate poisoning - see excess cholinergic effects

Atropine and pralidoxime

3

Location of ACh receptors - Nicotinic and muscarinic

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

4

Sympathetic length of preganglionic nerves vs parasympathetic

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

5

Parasympathetic activation -> (9)
GI
Bladder
Eye
Lung
Heart
Lacrimal
Salivary glands
Uterus
Penis/cliterus

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

6

Why choniergic excess not the same as parasympathetic activation?

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

DUMBBE*LLS*

7

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

Test w/?

Rx?

myasthenia Gravis

Edrophonium - tensilon test

Pyridostigmine

8

Thyectomy might be implicated in this disorder of general weakness

Myasthenia gravis

9

Direct Agonists - Cholimetric (4)

-chols

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

10

Old test for asthma

methacholine challenge - ACh agonist

11

Potent stimulator of sweat, tears and saliva

pilocarbine

12

Cholinergic agonist used to treat glaucoma

carbachol

13

Cholinergic used for urinary retention or postoperative ileus

Bethanechol

14

Indirect agonists (anticholinesterases) (6)

-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

15

Alzheimer drugs work by?

3?

indirectly increasing the ACh

Doneprezil
rivastigmine
galantamine

16

Side effects of atropine overdose?

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

17

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

Change in medications and addition of an anticholinergic

be wary of anti-muscarinics as well

18

Anticholinergic Drugs (4)

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

19

Anticholinergics used in Rx of urge incontinence (4)

On The Darn Toliet

oxybutynin
tolteridine
Darifenacin/solifenacin
Trospium

20

Eye dilation short term (3)

Homatopine
tropicamide
Cyclopentolate
-act as antimuscarinic

21

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

Benztropium

anti - muscarinic

22

Rx for motion sickness and decreases salivation

Scopolamine

23

Anti muscarinic Rx for COPD

Ipratropium
Tiotropium

24

Alpha 1 stim (5)

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

25

Alpha 2 stim (2)

inhibits NE release on presynaptic auto receptor
lowers insulin release acting on pancreatic Beta cells

26

Beta 1 stim (4)

increase HR
Increase contractility
increase in Renin
increase in lipolysis

27

Beta 2 stim (5)

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

28

Rx for pheochromocytoma

alpha antagonist - nonselective
Phenoxybenzamine

29

HTN medication in pregnancy

STOP what drug?

alpha methydopa

Ace inhibitor

30

Selective Alpha1 a d blocker used in BPH

Tamsulosin

31

nonselective alpha blockers (2)

phenoxybenzamine - irreversible

phentolamine - reversible

32

Alpha 1 selective blocker ? (3)

USed for

HTN and urinary retention w/ BPH

- zosins
parazosin
terazosin
doxazosin

- tamsulosin

33

alpha 1 and Beta 1 blockers (2)

used for

carvediol
labetelol

used for slowing the heart and lowering peripheral resistance

34

Partial beta agonists -> antagonist (2)

Useful for ?

acetebutolol
pindolol

useful for HTN w/ bradycardia, NOT for CAD

35

Nonselective Beta blockers(3)

Worry about using in who?

propranolol
nadolol
timolol

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

36

Selective Beta 1 blockers(3)

esmolol
atenolol
metoprolol

37

betal blockers used in glaucoma

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

38

Beta blockers are primarily used for (6)

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

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

39

Worrisome Side effects of Beta blockers (3)

bradycardia and AV block -> CHF

masking of hypoglycemia in beta blockers

bronchospasm w/ nonselective beta blockers

40

3 enzymes used in the production epinephrine/NE

2 cofactors?

-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

drug inhibiting the packaging of ACh

Vesamicol

42

Drug inhibiting the packaging of NE

reserpine

43

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

Ca 2+

44

Black widow spider toxin has what effect on nerve transmission

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

45

What toxin causes flaccid paralysis at the cholinergic junction

Botulinism

46

Choline is brought into the cholinergic nerve by what mech?

What inhibits this?

Na cotransport brings in

Hemicholinium inhibits

47

Enzyme making ACh

choline acetyltransferase combining acetyl Co A and Choline

then packaged in vesicles

48

4 things that can happen to ACh in the synaptic cleft

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

49

4 things that can happen to NE in the synaptic cleft

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

Drugs blocking reuptake of NE in synaptic cleft (2)

TCAs and Cocaine

51

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

Ca - natural
Amphetamine
Tyramine
Ephedrine

52

2 drugs that block NE release

Guanethidine
betrylium - Ca channel blocker

53

angiontensin II effect on the presynaptic Noradrenergic neuron

leads to increase in NE release

54

Alpha2 and M2 on presynaptic noradrenergic neuron

decreases NE release

55

Gq uses what receptors

Qc HAVe 1 M&M

Gq uses
H1
alpha1
Vasopressin 1
M1
M3

56

Gi uses what receptors

MAD 2s

M2
Alpha 2
D2

57

Gs uses what receptors

Leftovers from
Qc HAVe 1 M&M
MAD2s

Beta1
beta2
D1
V2
H2

58

Receptor Gq pathway
4 steps

other way to get this path?

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

Receptor Gs pathway
2 steps

implicated in what disease?

adenylyl cyclase converts ATP ->cAMP

cAMP levels activate protein kinase A

implicated in Cholera

60

Receptor Gi pathway
2 Steps

implicated in what disease

BLOCKS adenylyl cyclase from converting ATP ->cAMP

low cAMP levels DO NOT activate protein kinase A

implicated in pertussIs

61

H1 vs H2 stimulation ->

3 vs 1 function

nasal and bronchial mucus secretions and contraction of bronchioles and puritus

vs

gastric acid secretion

62

V1 vs V2 stimulation

increased smooth muscle contrition (pressor in codes)

vs

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

63

M1 vs M2 vs M3

enteric nervous system

decreased HR and contractility (SA node)

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

64

D1 vs D2

relaxes the renal vasculature

modulates brain NT

65

Km =

related to?

affected by?

amount of substrate needed for 1/2 Vmax

inversely related to affinity. higher affinity -> smaller Km

affected by competitive inhibition

66

Vmax

related to?

Affected by?

the maximum rate at which a reaction proceeds

directly relates to enzyme concentration

- affected by noncompetitive inhibiors

67

Linewaver burk plot

x- axis

Y axis

Slope

x axis = 1/-km

y axis = 1/vmax

slope =Km/Vmax

68

Role of Noncompetative inhibitor on

Vmax

Km

As seen on lineweaver

Vmax decreases - seen as a higher y intercept


Km does not change - seen at the same point

69

Role of competitive inhibitor on

V max
Km

As seen on lineweaver

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

Adding an enzyme affects the line weaver plot how?

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

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

71

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

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

drug is infused how long to reach steady state?

4-5 half lives to 94% Concentration

73

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

Stop the infusion for one half life

74

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

No change on loading dose

Decreases maintenance dose

75

efficacy of a drug is?

what can drop efficacy? (2)

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

potency of a drug is?

what can drop the potency

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

Therapeutic Index =

LD50/ED50

Lethal dose for 50%/Effective dose for 50%

78

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

ex of poor therapeutic index drugs? (4)

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

Warfarin, lithium, anti-seizure, digoxin

79

Phase 1 metabolism completes the following reactions (3)

to get what metabolites?

reduction
oxidation
hydrolysis

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

80

Phase 2 metabolism completes the following reactions? (4)

to get what metabolites

Glucuronidation
acetylation
Sulfation
methylation

Inactive, VERY polar metabolites -> renal excreteted

81

Geriatric patients lose this metabolism 1st?

Cyp 450 is characterized by this metabolism?

Phase 1 - reduction/oxidation/sulfation

Phase 1 again

82

Slow acetylators means what?

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

83

2 enzymes in alcohol metabolism and drugs that inhibit them

limiting reagent in both?

alcohol dehydrogenase - fomepizole

acetaldehyde dehydrogenase -disulfiram

NAD which picks up the H -> NADH

84

Disulfram like reaction drugs?(4)

metronidazole
certain cephalosporins
procarbazine
1st gen sulfaureas (tobutamide)

85

11 drugs that induce Cyp 450

CRACK AMIGOS

Cimetidine
Ritonavir = protease inhibitors
Amiodarone
Ciprofloxacin
Ketoconazole

Acute Alcohol
Macrolides
Isoniazid
Grapefruit Juice
Omeprazole
Sulfonamide

86

7 drugs that inhibit Cyp 450

Guiness, Coronas, and PBRS induces CHRONIC ALCOHOLISM

Griseofulvin
Carbamazapine
Phenytoin
barbituates
Rifampin
St johns Wart
Chronic Alcoholism

87

ASA overdose how do you clear it?

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

Amphetamine overdose how do you clear it?

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