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PHAR 300 > Class #8-Nicotine > Flashcards

Class #8-Nicotine Flashcards

1
Q

Nicotine found in, its used is?

A

Tobacco plant and also other, insecticide by plants.

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2
Q

Absorption?

A

Blood in lung -> heart -> brain, very lipid soluble. 7 seconds between smoke and in brain. Same time as IV.

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3
Q

Any burned biomass produces?

A

1000s of drugs.

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4
Q

Compound in cigarette?

A

CO, ciliotoxin and irritant, tar, carcinogen

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5
Q

Cigarettes will kill?

A

600 millions people currently alive on planet earth

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6
Q

Numbers of cancer caused by smoking? %?

A

14 different kinds of cancer, 30% of cancer deaths due to smoking in canada.

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7
Q

Side effects of smoking?

A

Death of ciliated cells in lungs = cannot get rid of stuff in lungs

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8
Q

Synergy between asbestos and smoking in lung cancer risks

A

90 X times greater

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9
Q

1/3 of CHD death are due to smoking b/c?

A

HTA, CO, endothelial injury, atherosclerosis, plt aggregation, peripheral vascular disease

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10
Q

Nicotine … to blood flow to….?

A

decrease, in skin, hair, eyes, gums

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11
Q

Other big killer? % will die of lung disease?

A

COPD, 20% of smokers.

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12
Q

Cigarette will direcly kill? %

A

50%

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13
Q

1.main stream vs 2.side stream

A
  1. in lungs

2. out of cig. Contains differents chemicals

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14
Q

nicotine is …. soluble? … base?

A

lipid, weak.

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15
Q

NIcotine absortion?

A

nose, mouth, intestines

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16
Q

First pass in nicotine?

A

no b/c in lungs

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17
Q

Smoker controle bioavailability?

A

Yes, by altering the way they smoke, not conscious.

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18
Q

GI absorption

A

Since its weak base, will not be absorbed in stomach b/c weak base in acid envir. = ionized = not lipid soluble. But weak base in basic envir. = intestine = unionized = lipid soluble

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19
Q

Distribution?

A

Everywhere b/c highly lipid soluble, also foetus and beast milk.

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20
Q

Child eat 2 cigarette or cigar =?

A

Death, but gets to Chemoreceptor Trigger Zone = zomiting center. Most case start vomiting.

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21
Q

Metabolism?

A

Cytocrome P450 - CYP2A6

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22
Q

2a6 met. other drugs so..

A

Interactions to certain drugs

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23
Q

Half-life

A

2hours, sleep 8 hours, which is 4half-life so zero nicotine in blood.

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24
Q

Metabolite?

A

Nicotine to Cotinine

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25
Q

PS 2A6 varies so.

A

Weaker, so smoke less cig. b/c less effective

26
Q

CYP2A6 also..

A

active procarcinogen, so defective 2A6 decrease carcinogens

27
Q

Excretion?

A

urine,

28
Q

alkaline urine?

A

decrease excretion

29
Q

Nicotinic receptor is the..

A

First understood ion channels (Na+)

30
Q

Nicotinic receptor react to endogenous?

A

acetylcholine

31
Q

Nicotinic receptor where?

A

Sympathetic ganglia and parasympathetic ganglia, in somatic skeletal muscles, CNS sympathetic adrenal glands

32
Q

Nicotinic receptor exogenous antagonist?

A

Curare

33
Q

Muscarinic receptor endogenous agonist?

A

Acetylcholine

34
Q

Muscarinic receptor exogenous agonist?

A

Muscarine

35
Q

Muscarinic receptor exogenous antagonist?

A

Atropine

36
Q

Nicotinic receptor ion? stimulaiton =?

A

Na+ and some Ca++ in cells, depolarization

37
Q

Muscarinic receptor type of receptor? ion?

A

GPCR, K+ out of cells, hyperpolarization

38
Q

Nicotine is both?

A

Agonist and antagonist.

39
Q

Nicotinic receptor number of subunits? each subunit # of domains?

A

5, crossing membrane 4 times

40
Q

Nicotinic receptor most common subunits?

A

Combination of 2alpha and 3beta. or just 5alpha

41
Q

Number of different Nicotinic receptor alpha variants?

A

9

42
Q

NUmber of different Nicotinic receptor beta variants?

A

3

43
Q

MOst common and studied Nicotinic receptor subunits type?

A

2 (alpha4) and 3 (beta2)

44
Q

To open Nicotinic receptor ion channel need?

A

2 molecules bound at the two binding sites

45
Q

State of Nicotinic receptor?

A

Standby ->open -> desensitized -> standby

46
Q

nicotine does? with both a/antagonist?

A

Keep it desensitized for longer period of time b/c binds longer to receptor. This is why its both a/antagonist.

47
Q

Since block receptor =

A

More nicotinic receptors in prefrontal cortex. Also stimulation and block of autonomic ganglia.

48
Q

Nicotine poisoning?

A

CNS excitation followed by inhibition: tremor - convulsions - paralysis - death from resp. failure

49
Q

Nicotinic receptor on … neurones?

A

Noradrenaline, acetylcholine, glumatate, GABA, Dopamine

50
Q

Heteromeric =

A

Consisted of different part (Eg. 2 alpha4 and 3 beta2 subunits in Nicotinic receptor)

51
Q

Most frequent Homomeric Nicotinic receptor. Passage for which ion?

A

5 alpha7 subunits. Ca++ ONLY

52
Q

2 alpha4 and 3 beta2 subunits in Nicotinic receptor mainly passage for ion?

A

Mainly Na+, also little Ca++

53
Q

Mouse created in lab with no B2 subunit =

A

Cannot get addicted to nicotine, b/c no dopamine increase.

54
Q

Alpha4 subunits essential for?

A

Dopamine release in reward pathway

55
Q

What is MAO?

A

Mono amine oydase, takes back amine neuroreceptors in presynaptic terminal and MAO brokes it down. MOAI = increase amines activity

56
Q

Link with MAO and cigs?

A

There are MAO inhibitors in cigarettes.

57
Q

MAO inhibitors are?

A

Also a class of antidepressants.

58
Q

Epidemiology of smoking prevalence in psy. illnesses?

A

88% in schizo, 74% in depression, 80 in alcoholism, 29% gen. pop.

59
Q

Average smoker smokes for

A

20years

60
Q

Effect of nicotine on dopamine receptors.

A
  1. Increase inhibition of the GABA neurone which inhibits the dopamine release so in the end increase dopamine prod. (less inhibition)
  2. Excitation of Glutamate neurone which stimulate the dopamine neurone to release dopamine. (more excitation)
61
Q

Nicotine withdrawl Sx?

Time?

A

Depressed, sleep disturbed, difficulty concentration, irritability, decreased heart rate.
Time: After 1 months feel better then before.

62
Q

To stop Rx? How?

A
  1. Buproprion blocks nicotinic receptors in VTA on dopaminergic neurones. First used has antidepressant.
  2. Verenicline, partial agonist of nicotinic receptors. Decrease response to nicotine
  3. Rx blocks 2A6
  4. Topiramate = decrease dopamine release

PHAR 300 (14 decks)

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