3/15 pharm Flashcards
(111 cards)
1
Q
Clearance can be impaired w/defects in which systems?
A
cardiac, renal, hepatic.
2
Q
Clearance
-equation:
A
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
Q
Loading dose
-equation
A
Loading dose = (Cp)(Vd) / (F)
Cp = target plasma concentration at steady state F = bioavailability
4
Q
Maintenance dose (MD) -equation
A
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
Q
In liver or renal disease, does maintenance dose inc. or dec.?
A
Dec.
-less being cleared, so less dose needed.
6
Q
Which drugs follow zero-order elimination?
-mnemonic?
A
-Phenytoin, Ethanol, and Aspirin (at high or toxic concentrations).
-PEA. (A pea is round, shaped like the “0” in
“zero-order.”)
7
Q
Capacity-limited elimination
-0 or 1st order?
A
0 order elim.
8
Q
Flow-dependent elimination
-0 or 1st order?
A
1st order elim.
9
Q
Phase I drug metabolism
A
P450 system
-Reduction, oxidation, hydrolysis.
10
Q
Phase II drug metabolism
A
Conjugation (Glucuronidation, Acetylation, Sulfation)
11
Q
Which is most common P450 enzyme?
A
CYP3A4 = most common
12
Q
Name 3 drugs that might cause trouble in a slow acetylator.
-which would also have a bimodal pop. distribution.
A
- hydralazine, isoniazid, procainamade
* HIP: its not hip to be a slow acetylator.
13
Q
What kind of antagonist is ketamine?
A
-ketamine (noncompetitive antagonist) on NMDA receptors.
14
Q
Therapeutic index:
-equation:
A
TI = Toxic dose/Effective dose
*high therapeutic index is good b/c that means theres a big difference btwn toxic and effective doses.
15
Q
Whats good, a high or low therapeutic index?
A
High.
-Safer drugs have higher TI values.
16
Q
Is the therapeutic index the same as therapeutic window?
A
No, b/c the therapeutic window would never extend all the way until the toxic dose.
17
Q
Some receptors that respond to autonomic neurotrasmitters/drugs receive NO nerve innervation (must get ligand through blood).
-can you name these uninnervated autonomic receptors?
A
- muscarinic receptors on endothelium of blood vessels
- adrenoreceptors on apocrine sweat glands
- alpha-2 and beta adrenoreceptors in blood vessels.
18
Q
para/pre, sym/pre: all release what?
A
ACh
19
Q
All ganglia have what type of receptor?
A
Nicotinic: ligand-gated ion channels.
20
Q
Do all sym/post release NE?
A
NO
- adrenal medulla releases NE and epi.
- sym/post release ACh that innervate sweat glands & piloerector muscles. These = sympathetic cholinergic.
21
Q
sympathetic cholinergic
A
sym/post that releases ACh
-innervate sweat glands & piloerector muscles.
22
Q
All glands have what receptors on them?
A
muscarinic
-even sweat glands that have sym/post innervation: these sym/posts dump ACh, not NE (sympathetic cholinergic).
23
Q
adrenal medulla & sweat glands = part of sym nervous system but are innervated by _______ fibers.
A
cholinergic
24
Q
Nicotinic ACh receptors
-what type of receptor is it?
A
-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.
