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PHAR > PHAR4 - Applying PD/PK Theory (Stimulants) > Flashcards

PHAR4 - Applying PD/PK Theory (Stimulants) Flashcards

1
Q

What plant species is used for the production of cocaine?

A

Erythroxylum coca.

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2
Q

What plant is used for the production of nicotine?

A

Nicotiana tobacum.

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3
Q

What is the common effect associated with nicotine and cocaine?

A

Euphoric high.

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4
Q

Define the speed of onset.

A

Time required for the euphoric high to be felt by the individual following drug administration.

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5
Q

Discuss the link between speed of onset and reinforcing effect.

A

The greater the speed of onset, the greater the reinforcing effect.

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6
Q

Define the reinforcing effect of the drug.

A

Linked to additivity. The strength of the drug to induce additivity in the individual.

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7
Q 
Put the following routes of administration in order of speed of onset (fastest first): 
Intra-venous. 
Intranasal.
Inhalation. 
Oral.
A

Inhalation.
Intravenous.
Intranasal.
Oral.

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8
Q

What route is associated with drug injection?

A

Intravenous.

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9
Q

What route is associated with drug snorting?

A

Intranasal.

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10
Q

What route is associated with smoking a drug?

A

Inhalation.

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11
Q

What route is associated with drinking or eating the drug?

A

Oral.

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12
Q

Discuss the intravenous route of administration.

A

Injection of drug directly into bloodstream.

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13
Q

Discuss link between intravenous route of administration and speed of onset. What pathway is taken by the drug?

A

Drug injected into venous system. Pumped to the right side of heart via vena cava. Pumped to lung via pulmonary artery. Pumped back to heart via pulmonary vein. Pumped for left side of heart via the aorta to the tissues e.g. brain.

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14
Q

Discuss the oral route of administration.

A

Eating or drinking the drug - usually drug is mixed with food or beverage.

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15
Q

Discuss link between oral route of administration and speed of onset. What pathway is taken by the drug?

A

Drug goes down oesophageal tube into stomach, small intestine and then gastrointestinal tract. Stomach contents varies the time required for drug to be absorbed into venous bloodstream. Blood enters right side of heart via vena cava. Pumped to lung via pulmonary artery. Pumped back to heart via pulmonary vein. Pumped to body tissue e.g. brain, via aorta.

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16
Q

What is the main factor affecting the speed of onset for drugs administered orally?

A

Stomach contents. Full stomach takes longer for drug to be absorbed. Empty stomach means drug is absorbed faster, primarily if drug is liquid.

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17
Q

Discuss the intranasal route of administration.

A

Drug is snorted into the system.

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18
Q

Discuss link between intranasal route of administration and speed of onset. What pathway is taken by the drug?

A

Drug crosses mucous membranes of nasal sinus into capillaries surrounding it. Drug enters venous circulation. Pumped to right side of heart via vena cava. Pumped to lung via pulmonary artery. Pumped back to left side of heart via pulmonary vein. Pumped to body tissue e.g. brain via aorta.

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19
Q

What factor makes intranasal route of administration slower than intravenous route of administration?

A

Initial diffusion of drug across mucous membrane of nasal sinus to access capillary network, prior to entering venous system.

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20
Q

Discuss the inhalation route of administration.

A

Drug is smoked or inhaled into the body.

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21
Q

Discuss link between inhalation route of administration and speed of onset. What pathway is taken by the drug?

A

Drug enters lungs so diffuses through alveolar sacs. Blood pumped to left side of heart and distributed to tissues via aorta in arterial circulation.

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22
Q

Which route of administration provides the fastest speed of onset for cocaine/nicotine and why?

A

Inhalational. Venous system is bypassed. Drug enters lungs directly meaning it can go straight to the heart to be distributed.

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23
Q

Which form of cocaine is used for snorting?

A

Cocaine hydrochloride.

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24
Q

Discuss the use and chemical reactivity of cocaine hydrochloride.

A

Medicinal form of cocaine. Heating causes degradation.

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25
Q

What type of cocaine is used for inhalation?

A

Crack cocaine.

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26
Q

Discuss the formation of crack cocaine.

A

Cocaine hydrochloride (medicinal form of cocaine) is reacted with an alkaline solution. Precipitate formed is crack cocaine.

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27
Q

Which method of drug administration for nicotine and cocaine is considered to be most addictive?

A

Inhalation.

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28
Q

Which enzymes are involved in the metabolism of cocaine?

A

Cholinesterase enzymes. Hepatic and plasmic.

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29
Q

Where does cocaine metabolism occur?

A

Liver and plasma.

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30
Q

Discuss the active metabolites produced in cocaine metabolism.

A

No active metabolites formed.

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31
Q

What is the approx. half life of cocaine?

A

20-90 minutes.

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32
Q

Why is the metabolism of cocaine more rapid that the metabolism of nicotine?

A

Additional metabolism of cocaine occurs in the blood plasma by plasma cholinesterase enzymes.

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33
Q

What is the approx. half life of nicotine?

A

1-3hrs.

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34
Q

Where does nicotine undergo metabolism?

A

Liver.

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35
Q

Which enzymes are involved in the metabolism of nicotine?

A

Cytochrome P450 enzymes in the liver.

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36
Q

What active metabolites are produced during nicotine metabolism ?

A

No active metabolites.

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37
Q

What two factors affect the addictive potential of the drug?

A

Route of administration and metabolism

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38
Q

What is the link between route of administration and addictive potential?

A

Routes that give faster onset of effect result in greater addictive potential.

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39
Q

Which drug administration gives the greatest addictive potential and why?

A

Inhalation. Fastest onset of effects (within minutes). Reinforces drug use in the individual.

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40
Q

What is the link between metabolism and addictive potential of drug?

A

Faster drug metabolism results in shorter drug effect. Individual encouraged to use more. Greater addictive potential.

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41
Q

Discuss the physical action caused by the addictive potential of nicotine.

A

Cigarettes smoked at regular intervals throughout the day.

42
Q

Discuss the physical action caused by the addictive potential of cocaine.

A

Drug binging occurs - multiple takes during short time.

43
Q

What are the main drug target for cocaine?

A

Catecholamine reuptake proteins.

Sodium ion channels.

44
Q

Discuss the selectivity of cocaine. What factor affects the selectivity ?

A

Relatively low selectivity as it can bind to multiple drug targets. Effect is dose dependent.

45
Q

What effect does cocaine have on catecholamine reuptake proteins?

A

Inhibitory effect. Binds to catecholamine reuptake protein preventing neurotransmitter from binding to it so keeps neurotransmitter in the synapse.

46
Q

Discuss the link between catecholamine and catecholamine reuptake proteins.

A

Catecholamine are the endogenous agonist for catecholamine reuptake proteins, which is considered the target receptor.

47
Q

Discuss similarities between the chemical structures of cocaine, dopamine and noradrenaline.

A

Lipophilic ring. Intermediate linking bond. Amine group.

48
Q

What does cocaine behave as to a catecholamine reuptake protein?

A

Exogenous competitive antagonist.

49
Q

How does cocaine have an inhibitory effect on reuptake proteins?

A

Binds to the protein and is reuptaken at a much slower rate, preventing catecholamines from being reuptaken quickly.

50
Q

What effect does cocaine have on the affinity of a catecholamine to the catecholamine receptor?

A

No effect on affinity.

51
Q

What effect does cocaine have on dopamine receptor interactions?

A

Increases dopamine receptor interactions as less dopamine is removed.

52
Q

Discuss the formation of dopamine molecules.

A

Tyrosine amino acid residues converted into DOPA by tyrosine hydroxylase. DOPA converted into dopamine by DOPA decarboxylase.

53
Q

Discuss the process that occurs following dopamine production at the dopaminergic nerve terminal, to cause a cellular response.

A

Dopamine packaged into secretory vesicles. Action potential occurs which stimulates Ca2+ influx. Ca2+ mediated exocytosis occurs releasing dopamine into synapse. Dopamine interacts with dopamine receptors forming dopamine-receptor complexes. Cellular response transduced.

54
Q

Discuss how dopamine induced cellular response is stopped/reduced.

A

Dopamine removed from synapse by catecholamine reuptake proteins. Once back into the nerve terminal, it undergoes metabolism forming various matebolites.

55
Q

Why are there greater dopamine-receptor interactions in the presence of cocaine?

A

Cocaine prevent dopamine being removed from the synapse. Dopamine stays in synapse longer so more likely to interact with the receptors. More interactions.

56
Q

Where is the binding side for cocaine interacting with sodium ion channels?

A

Intracellular side.

57
Q

What characteristic of cocaine will allow it to bind to sodium ion channels? Explain.

A

Lipid solubility. Must cross the lipid membrane to access intracellular binding site.

58
Q

Is cocaine a weak base or a weak acid?

A

Weak base.

59
Q

Discuss ionisation of cocaine intracellularLy and extracellularly.

A

More ionised cocaine exists intracellularLy than extracellularly.

60
Q

Discuss why cocaine is required to be in the unionised state.

A

Unionised molecules have a greater lipid solubility. Allows the molecule to pass across the lipid membrane.

61
Q

Discuss why cocaine is required to be in the ionised state.

A

Ionised cocaine molecules have a greater affinity for the protein target due to the polar side chains that are present.

62
Q

What effect is caused by the binding of cocaine to sodium ion channels?

A

Inhibitory effect resulting in local anaesthetic effect.

63
Q

What is the drug target for nicotine?

A

Nicotine acetylcholine receptors.

64
Q

What is the endogenous agonist for the drug target of nicotine?

A

Acetylcholine is the endogenous agonist for nicotinic acetylcholine receptors.

65
Q

Where are nicotinic acetylcholine receptors present?

A

Autonomic/involuntary nervous system.

Somatic nervous system - skeletal muscle control.

66
Q

Give examples of processes controlled by the autonomic nervous system.

A

Heart rate. GI function. Sweating. Pupil dilation. Blood glucose levels.

67
Q

Discuss the structure of a nicotinic acetylcholine receptor.

A

Linked to a sodium ion channel. Five protein subunits surrounding central sodium ion channel pore.

68
Q

Where are the acetylcholine binding sites located on the nicotinic acetylcholine receptor?

A

On two of the five subunits, surrounding the central ion channel pore.

69
Q

Discuss the location and pathway involved in the nicotinic receptors of the autonomic nervous system.

A

Nicotinic receptors are located at the ganglion between the pre ganglionic and post ganglionic neuron.

70
Q

Discuss the location and pathway involved in the nicotinic receptors of the somatic nervous system.

A

Nicotinic receptors are located at the skeletal muscle (neuromuscular junction) just after the motor neuron.

71
Q

Where do pre ganglionic neurons originate?

A

Brain or spinal cord.

72
Q

Discuss the propagation of nerve impulses in the autonomic nervous system.

A

Signal sent from the brain/spinal cord. Propagated along pre-ganglionic neuron. Release of acetylcholine at the ganglion to the nicotinic acetylcholine receptor. Signal is then propagated along post-ganglionic neuron to the effector organ.

73
Q

Discuss the propagation of nerve impulses in the somatic nervous system.

A

Signal sent from brain or spinal cord and propagated along motor neuron to the nicotinic acetylcholine receptors at the skeletal muscle. Results in contraction of skeletal muscle.

74
Q

Why are cocaine and nicotine considered stimulants?

A

Increase cellular activity. Produce euphoric high via stimulation of dopaminergic neurons of reward pathway.

75
Q

Where do dopaminergic neurons originate from and project to?

A

Originate from ventral tegmental area.

Project to nucleus accumbens.

76
Q

Where specifically for nicotinic receptors located on the dopaminergic neuron?

A

Soma (cell body) of the neuron at the ventral tegmental area.

77
Q

Which receptor is activated by dopamine in the reward pathway for the euphoric high feeling?

A

D1 receptors.

78
Q

How does nicotine cause euphoric high feelings?

A

Binds to nicotinic acetylcholine receptors on dopaminergic neurons. Neuron stimulated allowing for dopamine release. Interaction of dopamine with d1 receptors. Euphoric high feeling produced.

79
Q

How does cocaine cause euphoric high feelings?

A

Cocaine prevents reuptake of dopamine from synapse. Dopamine continues to interact with D1 receptors in reward pathway. Greater euphoric feelings occur.

80
Q

Which nervous system’s effects are mimicked by cocaine and nicotine?

A

Sympathetic nervous system.

81
Q

Discuss the role of nicotine in affecting the sympathetic nervous system.

A

Binds to nicotinic receptors at the ganglion between the pre and post ganglionic neuron. Resultant effect is enhanced, sending signals through the post ganglionic neuron, affecting the effector organ.

82
Q

Discuss the role of cocaine in affecting the sympathetic nervous system.

A

Cocaine inhibits the reuptake of noradrenaline resulting in greater sympathetic activity at the effector organ.

83
Q

What are the symptoms of increased sympathetic nervous system activity?

A

Increased heart rate. Vasoconstriction of blood vessels.

84
Q

Discuss a toxic effect of cocaine and nicotine on the sympathetic nervous system.

A

Increase in heart rate and greater vasoconstriction of blood vessels can cause a large increase in blood pressure. Cardiovascular system affected.

85
Q

Give three common toxic effects on the cardiovascular system as a result of cocaine and nicotine.

A

Increased blood pressure.
Coronary vasoconstriction.
Increased platelet activation.

86
Q

What cardiovascular toxic effect is specific to nicotine only?

A

Blood profile changes.

87
Q

What cardiovascular toxic effect is specific to cocaine only?

A

Decreased sodium transport and inflammation.

88
Q

Discuss effects of increased blood pressure due to cocaine and nicotine.

A

Increase in blood pressure is caused by increase heart rate and contractility.
Can lead to endothelial injury in blood vessels due to the high blood pressure.
May result in increased myocardial oxygen demand, which if not met, can result in myocardial infarction.

89
Q

Which drug causes the greater increase in heart rate?

A

Cocaine increases heart rate by 50%.

Nicotine increases heart rate by 20%.

90
Q

What type of flow causes injury to blood vessels?

A

Increased turbulent flow can cause endothelial injury in blood vessels.

91
Q

Why does vasoconstriction occur as an effect of cocaine and nicotine?

A

Increased activity of the sympathetic nervous system.

92
Q

What is the main effect of coronary vasoconstriction?

A

Reduced myocardial oxygen supply.

93
Q

Give three severe health complications that can occur as a result of increased myocardial oxygen demand and decreased myocardial oxygen supply.

A

Myocardial infarction - heart attack due to decreased/d flow to heart.
Myocardial ischaemia - reduced oxygen and blood flow to heart.
Arrhythmia - irregular heartbeats.

94
Q

What is the main effect of increased platelet activation?

A

Blood clots more likely to form. Blood clots in blood vessels referred to as thrombosis.

95
Q

What is atherosclerosis?

A

Build up of substances in blood vessels which restricts blood flow.

96
Q

Discuss link between endothelial injury, atherosclerosis and increased platelet activation.

A

More endothelial injury further increases platelet activation, increasing risk of thrombosis and atherosclerosis.

97
Q

Discuss blood profile alteration due to nicotine.

A

Increased fatty acid and low density lipoprotein content in blood. Atherogenic risk increased, due of fatty acid deposit formation being more likely. Increased CVD risk.

98
Q

Cocaine blocks what ion channels?

A

Sodium.

99
Q

Discuss link between cocaine, inflammation and endothelial injury.

A

Cocaine induced inflammation which alongside the endothelial injury that may occur, these may worsen.

100
Q

Which drug has more toxic cardiovascular effects?

A

Nicotine and cocaine.

101
Q

Discuss the potency of nicotine and cocaine.

A

Potency cannot be compared between nicotine and cocaine as they act on separate drug targets.

PHAR (9 decks)

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