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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
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

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