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Integrated Medical Sciences > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Agonist of muscarinic receptor

A

Muscarine

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2
Q

Antagonist of muscarinic receptor

A

Atropine

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3
Q

Agonist of nicotinic receptor

A

Nicotine

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4
Q

Antagonist of nicotinic receptor

A

Curare

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5
Q

Is a muscarininc receptor a G protein coupled or NT gated receptor?

A

G-protein coupled

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6
Q

Is a nicotinic receptor a G protein coupled or NT gated receptor?

A

NT gated

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7
Q

Is an adrenergic receptor a G protein coupled or NT gated receptor?

A

G-protein coupled

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8
Q

What is ACh made from? What enzyme?

A 
Choline and Acetyl CoA
Choline acetyltransferase (ChAT)
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9
Q

What is ACh broken down into? What enzyme?

A

Choline and Acetic Acid

Acetylcholinesterase (AChE)

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10
Q

Sympathetic NS is which spinal levels?

A

T1-L2

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11
Q

Parasympathetic NS is which spinal levels?

A

Brain stem, S2-S4

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12
Q

What are the subtypes of nicotinic receptors?

A

Neuronal, muscle

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13
Q

What are the subtypes of muscarinic receptors?

A 
M1 (gastric parietal cells)
M2 (heart - negative chronotropic effects)
M3 (GIT, lacrimal)
M4 (adrenal medulla, CNS)
M5 (CNS)
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14
Q

What does vesamicol?
What NT does it affect?
Does it increase or decrease activity?

A

Prevent ACh packing into vesicles?
ACh
Decrease

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15
Q

What does botulinum toxin do?
What NT does it affect?
Does it increase or decrease activity?

A

Prevents attachment/exocytosis of vesicles from presynaptic neuron?
ACh
Decrease

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16
Q

What does hemicholinium do?
What NT does it affect?
Does it increase or decrease activity?

A

Prevents re-uptake of choline to pre-synaptic neuron
ACh
Decrease

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17
Q

Tubocurarine

A

Compete with ACh for nicotinic ACh receptor
ACh
Decrease

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18
Q

Atropine

A

Compete with ACh for muscarinic ACh receptor
ACh
Decrease

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19
Q

Anticholinesterases

A

Inhibit breakdown of ACh to choline and acetic acid
ACh
INCREASE

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20
Q

What are the effects of NE binding to alpha 1 receptors?

A

EXCITATORY

Vasoconstriction (except heart, skeletal muscle, liver)
Sphincters close
Arrestor pilli contract
Radial muscle of pupil dilates

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21
Q

What are the effects of NE binding to alpha 2 receptors?

A

INHIBITORY

Feedback inhibition = inhibit NE release
Increase glucagon –> increase glucose

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22
Q

What are the effects of NE binding to beta 1 receptors?

A

HEART
Increase HR, increase contractility –> increase CO

KIDNEY
Increase renin –> increase BP

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23
Q

What are the effects of NE binding to beta 2 receptors?

A

Smooth muscle relaxation
LUNGS - bronchodilation
HEART, SKELETAL MUSCLE, LIVER - dilation

Increase glycogenolysis and gluconeogenesis –> increase glucose

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24
Q

What are the effects of NE binding to beta 3 receptors?

A

Lipolysis at adipose tissue

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25
In blood vessels: Alpha 1 receptors are found ____________ and are stimulated by _____________. Beta 2 receptors are found ____________ and are stimulated by _____________.
Alpha 1 receptors are found NEAR THE NERVE and are stimulated by NERVES Beta 2 receptors are found THROUGHOUT THE VESSEL and are stimulated by ADRENALINE FROM THE ADRENAL MEDULLA
26
At low epinephrine levels..... At high epinephrine levels....
At low epinephrine levels - B2 are occupied (have high affinity --> dilation) At high epinephrine levels - A1 are occupied (more of them --> constriction)
27
What do MAO inhibitors do? What NT does it affect? Does it increase or decrease activity?
Antidepressants Prevent action of monoamine oxidase (MAO) in pre-synaptic neuron (i.e., prevents NE breakdown) NE Increase
28
What do COMT inhibitors do? What NT does it affect? Does it increase or decrease activity?
Anti-parkinson's Prevent action of COMT in post-synaptic neuron (i.e., prevents NE breakdown) NE Increase
29
What do NE re-uptake inhibitors do? EXAMPLE? What NT does it affect? Does it increase or decrease activity?
E.g., coccaine Prevent re-uptake of NE to pre-synaptic neuron NE Increase
30
What does reserpine do? What NT does it affect? Does it increase or decrease activity?
Prevents packaging of NE into vesicles? NE Decrease
31
What does alpha-meethyltryosine do? What NT does it affect? Does it increase or decrease activity?
Mimics and competes with tyrosine (precursor for NE - i.e., disrupts NE synthesis) NE Decrease
32
What drugs end in "---pril"?
ACE inhibitors
33
What drugs end in "---sartan"?
Angiotensin receptor antagonist / blocker (ARBs)
34
What drugs end in "---iren"?
Renin inhibitors
35
What drugs end in "---ones"?
Potassium sparing diuretics
36
What drugs end in "---olol" or "---alol"?
B adrenergic receptor blockers | i.e., beta blockers
37
What is the apoprotein on LDL? | What about the receptor to which it binds?
ApoB-100 | ApoB-100 receptor
38
What is uptake by HDL?
Non-esterified cholesterol
39
What is the LDL subtype that underpins atherogenesis?
Lp(a)
40
What does Lp(a) do?
It resembles and competes with plasminogen. Plasminogen can be activated to plasmin which dissolves clots. Lp(a) instead reduces plasmin --> promoting thrombosis
41
What effect do statins have on dyslipiademia?
Decrease LDL, TG | Increase HDL
42
What is contraindicated with statins?
P450 is an enzyme involved in statin metabolism Drugs/grapefruit inhibiting P450 microsomal enzymes MUST be avoided (otherwise statin levels increase)
43
What effect do statins have on liver enzymes?
Increase
44
Use of statins and fibrates increase the risk of....
Myositis (inflammation of skeletal muscle) Rhabdomyolysis (potentially fatal skeletal muscle breakdown, and renal toxicity, due to myoglobin)
45
What effect do fibrates have on dyslipiademia?
Large decrease in TG Modest decrease in LDL Modest increase in HDL
46
How do fibrates work?
Bind and activates nuclear receptor (PPARa) which: - increases synthesis of lipoprotein lipase - increase LDL uptake by liver - decrease VLDL production by liver
47
How do statins work?
Inhibit cholesterol synthesis in liver (ENDOGENOUS) - competitive inhibition of HMG-CoA reductase Decreased cholesterol --> increased expression of LDL receptors in liver --> clearance of LDL from blood
48
Can bile acid binding resins be taken orally? How do they work?
YES - but they are not absorbed Interfere with administration of fat soluble vitamins and some drugs (anion exchange resin, resin bound bile acids are excreted - not absorbed, liver obligated to form new bile acids from cholesterol --> decreasing serum LDL) Also reduces cholesterol absorption from intestine
49
What % of bile acids are usually reabsorbed?
90-95%
50
Can ezetimibie be taken orally? How do they work?
YES - it is absorbed DOES NOT interfere with absorption of fat soluble vitamins Adjunct treatment to statins (endogenous) whereas ezetimibie is (exogenous) Inhibits sterol carrier protein required for cholesterol absorption --> decreased absorption of cholesterol --> decreased LDL in liver --> increases LDL clearance from plasma to liver
51
What do omega 3 fish oils do?
Decrease TG Decrease clotting Decrease inflammation Requires high dose
52
What does nicotinic acid do?
Decrease LDL Increase HDL BUT requires very high dose - not well tolerated
53
What % of O2 consumption does heart use? What % of cardiac output does heart receive?
11% 4% - relatively poorly perfused
54
Name three vasodilators? Name one vasoconstrictor?
NO PGI2 PGE2 (dilators) Endothelia 1 (constrict)
55
Do nitrates dilate arteries or veins more?
Veins
56
Can nitrates be taken orally?
NO - significant hepatic first pass metabolism - degraded They are taken via sublingual administration or transdermal patches
57
How long do short acting vs long acting nitrates last?
30 mins 4-6 hrs
58
What drug can be used as prophylactic treatment of angina?
B antagonists (beta blockers)
59
AMI treatment is aimed at ________, via:
repercussion ``` clot busters (fibrinolytic therapy) angioplasty (stent) ```
60
How is an AMI diagnosed?
Typical rise and fall of biochemical marker (troponin, CKMB) AND one of the following: - ischaemic symptoms - ECG changes - coronary artery intervention
61
Times for CK...
Increase in 3-6 hrs | Peaks 16-30 hrs
62
True or false? | CKMB mass index is better than CKMB activity?
True BUT - concurrent skeletal muscle injury masks rise in CKMB due to AMI Unreliable if Total CK
63
Times for aspartate aminotransferase...
Appears 6-8 hrs Peak 24-48 hrs Return to baseline 4-6 days
64
Times for myoglobin...
``` Early appearance (2-3 hrs) Peak 6-9 hrs Rapid clearance - return to baseline (36 hrs) ```
65
Times for troponin...
Early rise 3-6 hrs | Long diastolic window (7-10 days) - due to bimodal release
66
What does it mean if CK doesn't go up, but troponin does?
Likely to be unstable angina - due to the fact that troponin is very sensitive and can detect minimal injury
67
BNP assay has an excellent ____________
negative predictive value (rules out HF as a cause of dyspnea)
68
What does the LAD artery supply?
Apex, anterior LV, IV septum
69
What does the LCX artery supply?
LV lateral wall
70
What does the RCA supply?
RV, posterior LV, IV septum

Integrated Medical Sciences (1 decks)

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