Lab report
Acknowledgement: In order to obtain the data for this experiment #collected the data as labpartner.
Introduction:
Morphine is an agonist of all three opioid receptors but especially the mu-receptors, the clinical use of the
drug is as a painkiller typically used as analgesia for patients that have had trauma, have cancer or other types
of severe pain. Morphine causes adverse effects such as: respiratory depression, vomiting, sedation, urinary
retention, increased intracranial pressure, hypotension. Other effects of morphine are: euphoria, depression of
cough reflex, decrease motility of the gastrointestinal tract, increased tone of circular smooth muscle, increased
tone anal sphincter, which might result in constipation. Morphine is contraindicated in patients with head
trauma or severe brain injury because the drug depresses respiratory and diabetes cerebral vessels and increases
cerebrospinal fluid pressure. Asthmatic patients should not receive morphine due to bronchoconstriction,
patients with liver disease should have another analgesia because of the active metabolite of morphine.
Morphine is contraindicated in patients with renal dysfunction. The drug may prolong the 2nd stage of labor.
Naloxone is an competitive antagonist of opioid mu-receptors, clinically the drug is used in patients which have
overdosed on morphine.
Drug affinity refers to the strength of the attraction between a drug molecule and its target protein in the
body. The greater the affinity of a drug for its target protein, the more effectively it will bind to the protein and
exert its therapeutic effects. On the other hand, a drug with low affinity for its target protein may not bind
effectively and may have reduced therapeutic efficacy. Drug affinity is an important factor in determining the
potency and efficacy of a drug. It is also important to consider the affinity of a drug for other proteins in the
body, as this can influence its side effects and potential for interactions with other drugs.
A graded dose-response curve is a graphical representation of the relationship between the dose of a drug
and the response it elicits. It shows how the magnitude of the response increases as the dose of the drug
increases. The curve is typically sigmoidal, meaning it has an S-shaped curve, with the steepest part of the
curve representing the maximal response of the drug. At the low end of the curve, the response to the drug is
minimal and increases as the dose increases. As the dose continues to increase, the response eventually reaches
a plateau, where further increases in dose do not lead to a significant increase in response. The shape of the
curve can be influenced by several factors, including the affinity of the drug for its target, the efficiency of the
drug in activating the target, and the presence of competing drugs or substances that can affect the response.
1
, IC50 (half maximal inhibitory concentration) and EC50 (half maximal effective concentration) are both
measures of drug potency, used to describe the concentration of a drug required to produce a certain response in
a target system. IC50 is used to describe the concentration of a drug that is required to inhibit the activity of a
particular target (e.g. enzyme, receptor) by 50%. It is often used to evaluate the effectiveness of a drug in
inhibiting a particular target, and to compare the potency of different drugs against the same target. EC50 is
used to describe the concentration of a drug that is required to produce a particular response in a target system
(e.g. tissue, organism) by 50%. It is often used to evaluate the effectiveness of a drug in producing a particular
response, and to compare the potency of different drugs in producing the same response. In general, the lower
the IC50 or EC50 value, the more potent the drug is considered to be.
Drug efficacy refers to the ability of a drug to produce a desired therapeutic effect. A drug with high efficacy
is one that produces a strong and consistent response, while a drug with low efficacy may produce a weaker or
less consistent response. The efficacy of a drug can be influenced by a variety of factors, including its chemical
structure, the type and severity of the condition being treated, and individual patient characteristics such as age,
weight, and overall health.
Method:
Aim for simulation experiments: evaluate the efficacy by EC50 of the drugs Morphine and Naloxone by
dose response curve. Data were collected in the following manner:. stimulation took place in the superior
ganglion (S.C ganglion) which is in the general circulation (vein). Observations are made of the measurements
from blood pressure (BP), heart rate (HR), Nicotinic membrane (Nic. Mem.) and skeletal muscle (Sk. Mus.) by
the software “The virtual Cat V2.6.2 (26/3/14)”. In order to generate a dose response curve (for simulation 2
and 3) the gms values from the Nic. Mem. was recorded and converted to Log10
First simulation was with only Naloxone doses in the following order: 20 mcg/kg (wait for 3 peaks), 50
mcg/kg (wait for 3 peaks) and 100 mcg/kg results in Figure 1.
Simulation 2: Inject only Morphine without Naloxone, at all provided doses by the “The virtual Cat
V2.6.2 (26/3/14)” software; which are 0.1 mg/kg, 0.2 mg/kg, 0.5 mg/kg, 1 mg/kg, 2 mg/kg, 5 mg/kg, 10 mg/kg,
20 mg/kg, 100 mg/kg and 200 mg/kg Figure 5, 6, 7 and 8. The aim of the simulation was to administer
injections of morphine until the peaks are at zero.
Simulation 3: was performed by Morphine injections in the presence of one initial dose of Naloxone, until
the peaks reached zero Figure 1, 2, 3 and 4.
EC50 was calculated by dividing the maximal response by two and then reading off the graph, for both curves
with the log10 values converted see table 3 and 5. The maximal response is in this incident the baseline
measurement 50gms, converted to log10. The calculations are then as follows: 1. =
0.849485002.
Results:
Following this section are two tables where the average of the responses are recorded:
2
Acknowledgement: In order to obtain the data for this experiment #collected the data as labpartner.
Introduction:
Morphine is an agonist of all three opioid receptors but especially the mu-receptors, the clinical use of the
drug is as a painkiller typically used as analgesia for patients that have had trauma, have cancer or other types
of severe pain. Morphine causes adverse effects such as: respiratory depression, vomiting, sedation, urinary
retention, increased intracranial pressure, hypotension. Other effects of morphine are: euphoria, depression of
cough reflex, decrease motility of the gastrointestinal tract, increased tone of circular smooth muscle, increased
tone anal sphincter, which might result in constipation. Morphine is contraindicated in patients with head
trauma or severe brain injury because the drug depresses respiratory and diabetes cerebral vessels and increases
cerebrospinal fluid pressure. Asthmatic patients should not receive morphine due to bronchoconstriction,
patients with liver disease should have another analgesia because of the active metabolite of morphine.
Morphine is contraindicated in patients with renal dysfunction. The drug may prolong the 2nd stage of labor.
Naloxone is an competitive antagonist of opioid mu-receptors, clinically the drug is used in patients which have
overdosed on morphine.
Drug affinity refers to the strength of the attraction between a drug molecule and its target protein in the
body. The greater the affinity of a drug for its target protein, the more effectively it will bind to the protein and
exert its therapeutic effects. On the other hand, a drug with low affinity for its target protein may not bind
effectively and may have reduced therapeutic efficacy. Drug affinity is an important factor in determining the
potency and efficacy of a drug. It is also important to consider the affinity of a drug for other proteins in the
body, as this can influence its side effects and potential for interactions with other drugs.
A graded dose-response curve is a graphical representation of the relationship between the dose of a drug
and the response it elicits. It shows how the magnitude of the response increases as the dose of the drug
increases. The curve is typically sigmoidal, meaning it has an S-shaped curve, with the steepest part of the
curve representing the maximal response of the drug. At the low end of the curve, the response to the drug is
minimal and increases as the dose increases. As the dose continues to increase, the response eventually reaches
a plateau, where further increases in dose do not lead to a significant increase in response. The shape of the
curve can be influenced by several factors, including the affinity of the drug for its target, the efficiency of the
drug in activating the target, and the presence of competing drugs or substances that can affect the response.
1
, IC50 (half maximal inhibitory concentration) and EC50 (half maximal effective concentration) are both
measures of drug potency, used to describe the concentration of a drug required to produce a certain response in
a target system. IC50 is used to describe the concentration of a drug that is required to inhibit the activity of a
particular target (e.g. enzyme, receptor) by 50%. It is often used to evaluate the effectiveness of a drug in
inhibiting a particular target, and to compare the potency of different drugs against the same target. EC50 is
used to describe the concentration of a drug that is required to produce a particular response in a target system
(e.g. tissue, organism) by 50%. It is often used to evaluate the effectiveness of a drug in producing a particular
response, and to compare the potency of different drugs in producing the same response. In general, the lower
the IC50 or EC50 value, the more potent the drug is considered to be.
Drug efficacy refers to the ability of a drug to produce a desired therapeutic effect. A drug with high efficacy
is one that produces a strong and consistent response, while a drug with low efficacy may produce a weaker or
less consistent response. The efficacy of a drug can be influenced by a variety of factors, including its chemical
structure, the type and severity of the condition being treated, and individual patient characteristics such as age,
weight, and overall health.
Method:
Aim for simulation experiments: evaluate the efficacy by EC50 of the drugs Morphine and Naloxone by
dose response curve. Data were collected in the following manner:. stimulation took place in the superior
ganglion (S.C ganglion) which is in the general circulation (vein). Observations are made of the measurements
from blood pressure (BP), heart rate (HR), Nicotinic membrane (Nic. Mem.) and skeletal muscle (Sk. Mus.) by
the software “The virtual Cat V2.6.2 (26/3/14)”. In order to generate a dose response curve (for simulation 2
and 3) the gms values from the Nic. Mem. was recorded and converted to Log10
First simulation was with only Naloxone doses in the following order: 20 mcg/kg (wait for 3 peaks), 50
mcg/kg (wait for 3 peaks) and 100 mcg/kg results in Figure 1.
Simulation 2: Inject only Morphine without Naloxone, at all provided doses by the “The virtual Cat
V2.6.2 (26/3/14)” software; which are 0.1 mg/kg, 0.2 mg/kg, 0.5 mg/kg, 1 mg/kg, 2 mg/kg, 5 mg/kg, 10 mg/kg,
20 mg/kg, 100 mg/kg and 200 mg/kg Figure 5, 6, 7 and 8. The aim of the simulation was to administer
injections of morphine until the peaks are at zero.
Simulation 3: was performed by Morphine injections in the presence of one initial dose of Naloxone, until
the peaks reached zero Figure 1, 2, 3 and 4.
EC50 was calculated by dividing the maximal response by two and then reading off the graph, for both curves
with the log10 values converted see table 3 and 5. The maximal response is in this incident the baseline
measurement 50gms, converted to log10. The calculations are then as follows: 1. =
0.849485002.
Results:
Following this section are two tables where the average of the responses are recorded:
2
