Talk:Loperamide: Difference between revisions

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{{headerpanel|{{Talk:Warning/Loperamide}}{{DepressantOD|opiates}}}}

{{headerpanel|{{Talk:Warning/Loperamide}}

{{DepressantOD|opiates}}}}

'''Loperamide''', commonly branded as '''Imodium''', is a synthetic [[Psychoactive class::opioid]] of the [[Chemical class::phenylpiperidine]] chemical class that is sold as an anti-diarrheal agent.

'''Loperamide''', commonly branded as '''Imodium''', is a synthetic [[Psychoactive class::opioid]] of the [[Chemical class::phenylpiperidine]] chemical class that is sold as an anti-diarrheal agent. But has off label uses as a pain relief medication, usually effective at 8mg-16mg (this method of using loperamide is not FDA approved, and can be very dangerous depending on your body, medications your taking, and how you administer this substance)

Loperamide crosses the blood-brain barrier in very small amounts, but traditionally these amounts have been considered insignificant. However, loperamide in high doses, has the potential for a significant analgesic or even [[euphoric]] effect.<ref>Poor Man's Methadone: A Case Report of Loperamide Toxicity. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26355852</ref> Use of higher-than-recommended levels of loperamide has been associated with cardiotoxicity. Large doses taken at once can cause arrhythmia and cardiac arrest in some cases, raising serious questions about the safety of recreational loperamide.<ref name="Loperamide Toxicity">Clinical Review: Loperamide Toxicity. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/28506439</ref><ref>Ventricular Tachycardia Storm Induced by Loperamide Abuse. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/30967981</ref>

Loperamide crosses the blood-brain barrier in very small amounts, but traditionally these amounts have been considered insignificant. However, loperamide in high doses, has the potential for a significant [[analgesic]] or even [[euphoric]] effect.<ref>Poor Man's Methadone: A Case Report of Loperamide Toxicity. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26355852</ref> Use of higher-than-recommended levels of loperamide has been associated with cardiotoxicity. Large doses taken at once can cause arrhythmia and cardiac arrest in some cases, raising serious questions about the safety of recreational loperamide.<ref name="Loperamide Toxicity">Clinical Review: Loperamide Toxicity. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/28506439</ref><ref>Ventricular Tachycardia Storm Induced by Loperamide Abuse. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/30967981</ref>

==History and culture==

Loperamide is a phenylpiperidine derivative, [[opioid]] [[agonist]] thought to have a low potential for central nervous effects. It was launched by Janssen Pharmaceutica in 1973. On release loperamide was classified in the US as a schedule II narcotic, before transfer to to schedule V in 1977. In November 1982 loperamide was removed from schedule V or 'decontrolled'.

Loperamide is a phenylpiperidine derivative, [[opioid]] [[agonist]] thought to have a low potential for central nervous effects. It was launched by Janssen Pharmaceutica in 1973. On release loperamide was classified in the US as a schedule II narcotic, before transfer to to schedule V in 1977. In November 1982 loperamide was removed from schedule V or 'decontrolled' and made available over-the-counter.

This appears to have been based on initial, preclinical studies indicative of dependence and [[withdrawal]] in animal studies. The consensus of later studies was that loperamide has a low potential for abuse, based on an apparent lack of central nervous effects.

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==Chemistry==

Loperamide is a phenylpiperidine derivative with a chemical structure similar to [[opioid]] [[receptor]] [[agonists]] such as [[wikipedia:diphenoxylate|diphenoxylate]] and [[wikipedia:bezitramide|bezitramide]]. Like diphenoxylate, it has a [[methadone]]-like structure and a [[piperidine]] moiety.<ref>An Introduction to Medicinal Chemistry. | https://books.google.com/books?id=Pj7xJRuhZxUC&pg=PA644#v=onepage&q&f=false</ref>

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*'''[[Effect::Pupil constriction]]'''

*'''[[Effect::Respiratory depression]]'''

*'''[[~~Constipation]]'''~~

*'''[[Effect::Abnormal heartbeat]]'''

*'''[[Abnormal heartbeat]]'''

*'''[[Effect::Increased heart rate]]'''

*'''[[Increased heart rate]]'''

*'''[[Effect::Stomach cramps]]'''

*'''[[Stomach cramps]]'''

*'''[[Effect::Difficulty urinating]]'''

*'''[[Difficulty urinating]]'''

*'''[[Effect::Decreased libido]]'''

*'''[[Decreased libido]]'''

*'''[[Effect::Orgasm suppression]]'''

*'''[[Orgasm suppression]]'''

*'''[[Effect::Appetite suppression]]'''

*'''[[Appetite suppression]]'''

*'''[[Effect::Cough suppression]]'''

*'''[[Cough suppression]]'''

*'''[[Effect::Vasodilation]]'''

*'''[[Effect::Motor control loss]]'''

*'''[[Effect::Muscle relaxation]]'''

}}

|{{effects/cognitive|

*'''[[Effect::Cognitive euphoria]]''' - This particular substance can be considered as less intense in its cognitive euphoria when compared ~~with~~ to other [[opioids]].

*'''[[Effect::Cognitive euphoria]]''' - This particular substance can be considered as less intense in its cognitive euphoria when compared to other [[opioids]].

*'''[[Effect::Anxiety suppression]]'''

*'''[[Effect::Dream potentiation]]'''

*'''[[Effect::Sleepiness]]'''

*'''[[Effect::Creativity enhancement]]'''

*'''[[Effect::Thought deceleration]]'''

}}

{{effects/visual|

The visual effects of loperamide are relatively mild across all dosages and mostly present when high doses have been consumed. When compared to other [[opioids]] that are capable of inducing visual effects, the overall visual effects of loperamide are mild. They are most similar to that of [[dissociatives]] with a mild dream-like immersive effect similar to that of [[deliriants]]. The visuals can be greatly enhanced with the addition of hallucinogens and cannabis, but one should be wary as the interactions are not well documented and the chance of cardiovascular shock, serotonin syndrome, or other fatal complications is high.

====Enhancements====

*'''[[Effect::Brightness alterations]]''' - The surroundings can become brighter with a mild high-contrast effect, be slightly darkened/gloomy, or not change at all.

*'''[[Effect::Frame rate enhancement]]''' - At common to high doses, particularly when looking around with only the eyes but keeping the head stationary, or when the view angle changes suddenly, a mild but noticeable sluggishness/latency can be perceived. This effect is similar in feel to certain sedating dissociatives. This is an inconsistently manifested effect with some people never reporting such effects.

*'''[[Effect::Immersion enhancement]]''' - This effect is most similar to that of deliriants.

====Distortions====

*'''[[Effect::Depth perception distortions]]'''

}}

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*'''[[Stimulants]]''' - Because loperamide increases BPM and BP and stimulants also do this, cardiac arrest, hypertensive crisis, stroke, and heart attack all become much more likely to occur. Besides it can be dangerous to combine depressants with stimulants due to the risk of accidental excessive intoxication. Stimulants mask the sedative effect of depressants, which is the main factor most people use to gauge their level of intoxication. Once the stimulant effects wear off, the effects of the depressant will significantly increase, leading to intensified disinhibition, motor control loss, and dangerous black-out states.

*'''[[Dissociatives]]''' - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the [[recovery position]] or have a friend move them into it.

*'''CYP450 3A4 or 2C8 inhibitors''' - Coadministration with drugs that enhance the gastrointestinal absorption or inhibit the metabolism of loperamide (e.g., potent CYP450 3A4 or 2C8 inhibitors) may increase the plasma concentrations and adverse effects of loperamide. <ref> https://www.drugs.com/drug-interactions/erythromycin-with-loperamide-simethicone-1009-0-1483-0.html?professional=1 </ref> That includes; erythromycin, ritonavir, grapefruit.

==Legal status==

Loperamide is legal and available in over-the-counter preparations in most parts of the world.

==Extraction and smoking==

Loperamide can be extracted from the parenting product, usually pills, specifically non gel pills. Loperamide is extracted with ethyl alcohol, when extracted, the resulting product tends to be a green or teal group of crystals, which is loperamide and coloring from the medications manufacture. These crystals are often then removed from the container that they were formed in, and put into a smoking device of some sort, usually a pipe designed for crystalline substances. However according to experience reports from Erowid, extracted loperamide smells very strongly of chemicals, and was compared to the smell that of methamphetamine and crack cocaine.

==See also==

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*[https://en.wikipedia.org/wiki/Loperamide Loperamide (Wikipedia)]

*[https://www.erowid.org/pharms/loperamide/ Loperamide (Erowid Vault)]

*[https://isomerdesign.com/PiHKAL/explore.php?id=8677 Loperamide (~~TiHKAL /~~ Isomer Design)]

*[https://isomerdesign.com/PiHKAL/explore.php?id=8677 Loperamide (Isomer Design)]

==References==

[[Category:Psychoactive substance]]

~~[[Category:Depressant]]~~

[[Category:Opioid]]

[[Category:~~Piperidine~~]]

[[Category:Diphenylpropylamine]]

[[Category:Phenylpiperidine]]

[[Category:Approval]]

~~[[Category:Proofread]]~~

@@ Line 1: / Line 1: @@
 {{Approval}}
-{{headerpanel|{{Talk:Warning/Loperamide}}{{DepressantOD|opiates}}}}
+{{headerpanel|{{Talk:Warning/Loperamide}}
+{{DepressantOD|opiates}}}}
 {{SummarySheet}}
 {{Talk:SubstanceBox/Loperamide}}
-'''Loperamide''', commonly branded as '''Imodium''', is a synthetic [[Psychoactive class::opioid]] of the [[Chemical class::phenylpiperidine]] chemical class that is sold as an anti-diarrheal agent.
+'''Loperamide''', commonly branded as '''Imodium''', is a synthetic [[Psychoactive class::opioid]] of the [[Chemical class::phenylpiperidine]] chemical class that is sold as an anti-diarrheal agent.  But has off label uses as a pain relief medication, usually effective at 8mg-16mg (this method of using loperamide is not FDA approved, and can be very dangerous depending on your body, medications your taking, and how you administer this substance)
-Loperamide crosses the blood-brain barrier in very small amounts, but traditionally these amounts have been considered insignificant. However, loperamide in high doses, has the potential for a significant analgesic or even [[euphoric]] effect.<ref>Poor Man's Methadone: A Case Report of Loperamide Toxicity. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26355852</ref> Use of higher-than-recommended levels of loperamide has been associated with cardiotoxicity. Large doses taken at once can cause arrhythmia and cardiac arrest in some cases, raising serious questions about the safety of recreational loperamide.<ref name="Loperamide Toxicity">Clinical Review: Loperamide Toxicity. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/28506439</ref><ref>Ventricular Tachycardia Storm Induced by Loperamide Abuse. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/30967981</ref>
+Loperamide crosses the blood-brain barrier in very small amounts, but traditionally these amounts have been considered insignificant. However, loperamide in high doses, has the potential for a significant [[analgesic]] or even [[euphoric]] effect.<ref>Poor Man's Methadone: A Case Report of Loperamide Toxicity. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26355852</ref> Use of higher-than-recommended levels of loperamide has been associated with cardiotoxicity. Large doses taken at once can cause arrhythmia and cardiac arrest in some cases, raising serious questions about the safety of recreational loperamide.<ref name="Loperamide Toxicity">Clinical Review: Loperamide Toxicity. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/28506439</ref><ref>Ventricular Tachycardia Storm Induced by Loperamide Abuse. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/30967981</ref>
 ==History and culture==
-Loperamide is a phenylpiperidine derivative, [[opioid]] [[agonist]] thought to have a low potential for central nervous effects. It was launched by Janssen Pharmaceutica in 1973. On release loperamide was classified in the US as a schedule II narcotic, before transfer to to schedule V in 1977. In November 1982 loperamide was removed from schedule V or 'decontrolled'.
+Loperamide is a phenylpiperidine derivative, [[opioid]] [[agonist]] thought to have a low potential for central nervous effects. It was launched by Janssen Pharmaceutica in 1973. On release loperamide was classified in the US as a schedule II narcotic, before transfer to to schedule V in 1977. In November 1982 loperamide was removed from schedule V or 'decontrolled' and made available over-the-counter.
 This appears to have been based on initial, preclinical studies indicative of dependence and [[withdrawal]] in animal studies. The consensus of later studies was that loperamide has a low potential for abuse, based on an apparent lack of central nervous effects.
@@ Line 18: / Line 19: @@
 ==Chemistry==
+{{chemistry}}
 Loperamide is a phenylpiperidine derivative with a chemical structure similar to [[opioid]] [[receptor]] [[agonists]] such as [[wikipedia:diphenoxylate|diphenoxylate]] and [[wikipedia:bezitramide|bezitramide]]. Like diphenoxylate, it has a [[methadone]]-like structure and a [[piperidine]] moiety.<ref>An Introduction to Medicinal Chemistry. | https://books.google.com/books?id=Pj7xJRuhZxUC&pg=PA644#v=onepage&q&f=false</ref>
@@ Line 43: / Line 45: @@
 *'''[[Effect::Pupil constriction]]'''
 *'''[[Effect::Respiratory depression]]'''
-*'''[[Constipation]]'''
+*'''[[Effect::Abnormal heartbeat]]'''
-*'''[[Abnormal heartbeat]]'''
+*'''[[Effect::Increased heart rate]]'''
-*'''[[Increased heart rate]]'''
+*'''[[Effect::Stomach cramps]]'''
-*'''[[Stomach cramps]]'''
+*'''[[Effect::Difficulty urinating]]'''
-*'''[[Difficulty urinating]]'''
+*'''[[Effect::Decreased libido]]'''
-*'''[[Decreased libido]]'''
+*'''[[Effect::Orgasm suppression]]'''
-*'''[[Orgasm suppression]]'''
+*'''[[Effect::Appetite suppression]]'''
-*'''[[Appetite suppression]]'''
+*'''[[Effect::Cough suppression]]'''
-*'''[[Cough suppression]]'''
+*'''[[Effect::Vasodilation]]'''
+*'''[[Effect::Motor control loss]]'''
+*'''[[Effect::Muscle relaxation]]'''
 }}
 |{{effects/cognitive|
-*'''[[Effect::Cognitive euphoria]]''' - This particular substance can be considered as less intense in its cognitive euphoria when compared with to other [[opioids]].
+*'''[[Effect::Cognitive euphoria]]''' - This particular substance can be considered as less intense in its cognitive euphoria when compared to other [[opioids]].
 *'''[[Effect::Anxiety suppression]]'''
 *'''[[Effect::Dream potentiation]]'''
 *'''[[Effect::Sleepiness]]'''
+*'''[[Effect::Creativity enhancement]]'''
+*'''[[Effect::Thought deceleration]]'''
+}}
+{{effects/visual|
+The visual effects of loperamide are relatively mild across all dosages and mostly present when high doses have been consumed. When compared to other [[opioids]] that are capable of inducing visual effects, the overall visual effects of loperamide are mild. They are most similar to that of [[dissociatives]] with a mild dream-like immersive effect similar to that of [[deliriants]]. The visuals can be greatly enhanced with the addition of hallucinogens and cannabis, but one should be wary as the interactions are not well documented and the chance of cardiovascular shock, serotonin syndrome, or other fatal complications is high.
+====Enhancements====
+*'''[[Effect::Brightness alterations]]''' - The surroundings can become brighter with a mild high-contrast effect, be slightly darkened/gloomy, or not change at all.
+*'''[[Effect::Frame rate enhancement]]''' - At common to high doses, particularly when looking around with only the eyes but keeping the head stationary, or when the view angle changes suddenly, a mild but noticeable sluggishness/latency can be perceived. This effect is similar in feel to certain sedating dissociatives. This is an inconsistently manifested effect with some people never reporting such effects.
+*'''[[Effect::Immersion enhancement]]''' - This effect is most similar to that of deliriants.
+====Distortions====
+*'''[[Effect::Depth perception distortions]]'''
 }}
 }}
@@ Line 86: / Line 104: @@
 *'''[[Stimulants]]''' - Because loperamide increases BPM and BP and stimulants also do this, cardiac arrest, hypertensive crisis, stroke, and heart attack all become much more likely to occur. Besides it can be dangerous to combine depressants with stimulants due to the risk of accidental excessive intoxication. Stimulants mask the sedative effect of depressants, which is the main factor most people use to gauge their level of intoxication. Once the stimulant effects wear off, the effects of the depressant will significantly increase, leading to intensified disinhibition, motor control loss, and dangerous black-out states.
 *'''[[Dissociatives]]''' - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the [[recovery position]] or have a friend move them into it.
+*'''CYP450 3A4 or 2C8 inhibitors''' -  Coadministration with drugs that enhance the gastrointestinal absorption or inhibit the metabolism of loperamide (e.g., potent CYP450 3A4 or 2C8 inhibitors) may increase the plasma concentrations and adverse effects of loperamide. <ref> https://www.drugs.com/drug-interactions/erythromycin-with-loperamide-simethicone-1009-0-1483-0.html?professional=1 </ref> That includes; erythromycin, ritonavir, grapefruit.
 ==Legal status==
 {{LegalStub}}
 Loperamide is legal and available in over-the-counter preparations in most parts of the world.
+==Extraction and smoking==
+Loperamide can be extracted from the parenting product, usually pills, specifically non gel pills.  Loperamide is extracted with ethyl alcohol, when extracted, the resulting product tends to be a green or teal group of crystals, which is loperamide and coloring from the medications manufacture.  These crystals are often then removed from the container that they were formed in, and put into a smoking device of some sort, usually a pipe designed for crystalline substances.  However according to experience reports from Erowid, extracted loperamide smells very strongly of chemicals, and was compared to the smell that of methamphetamine and crack cocaine.
 ==See also==
@@ Line 100: / Line 122: @@
 *[https://en.wikipedia.org/wiki/Loperamide Loperamide (Wikipedia)]
 *[https://www.erowid.org/pharms/loperamide/ Loperamide (Erowid Vault)]
-*[https://isomerdesign.com/PiHKAL/explore.php?id=8677 Loperamide (TiHKAL / Isomer Design)]
+*[https://isomerdesign.com/PiHKAL/explore.php?id=8677 Loperamide (Isomer Design)]
 ==References==
 {{reflist}}
 [[Category:Psychoactive substance]]
-[[Category:Depressant]]
 [[Category:Opioid]]
-[[Category:Piperidine]]
+[[Category:Diphenylpropylamine]]
+[[Category:Phenylpiperidine]]
 [[Category:Approval]]
-[[Category:Proofread]]
 {{#set:Featured=true}}