Pipradrol, also known by its brand name Meratran, is a mild central nervous system

stimulant Stimulants (also known as central nervous system stimulants, or psychostimulants, or colloquially as uppers) are a class of drugs that increase alertness. They are used for various purposes, such as enhancing attention, motivation, cognition, ...

that acts as a norepinephrine-dopamine reuptake inhibitor. Developed in the United States in the 1940s and patented in 1953, pipradrol was initially marketed as an

antidepressant Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathi ...

in the mid-1950s. It was subsequently used as an adjunct treatment for various conditions, including

obesity Obesity is a medical condition, considered by multiple organizations to be a disease, in which excess Adipose tissue, body fat has accumulated to such an extent that it can potentially have negative effects on health. People are classifi ...

, senile dementia,

narcolepsy Narcolepsy is a chronic neurological disorder that impairs the ability to regulate sleep–wake cycles, and specifically impacts REM (rapid eye movement) sleep. The symptoms of narcolepsy include excessive daytime sleepiness (EDS), sleep-r ...

, and

schizophrenia Schizophrenia () is a mental disorder characterized variously by hallucinations (typically, Auditory hallucination#Schizophrenia, hearing voices), delusions, thought disorder, disorganized thinking and behavior, and Reduced affect display, f ...

. Despite its initial promise and relatively mild stimulant effects compared to stronger alternatives, concerns about its abuse potential led to its regulation and withdrawal from widespread use in many countries during the late 1970s. Pipradrol is now classified as a controlled substance in several nations, including the United Kingdom, where it is typically placed in less restrictive drug schedules due to its lower abuse potential compared to other stimulants.

Dosage

Elixir "Alertonic" with Pipradrol hydrochloride content of 0.044 mg/mL was recommended to adults only, 1 tablespoonful (15 ml.), three times daily 30 minutes before meals for limited periods only.

Side effects

Common side effects include

insomnia Insomnia, also known as sleeplessness, is a sleep disorder where people have difficulty sleeping. They may have difficulty falling asleep, or staying asleep for as long as desired. Insomnia is typically followed by daytime sleepiness, low ene ...

anorexia Anorexia nervosa (AN), often referred to simply as anorexia, is an eating disorder characterized by Calorie restriction, food restriction, body image disturbance, fear of gaining weight, and an overpowering desire to be thin. Individuals wit ...

tachycardia Tachycardia, also called tachyarrhythmia, is a heart rate that exceeds the normal resting rate. In general, a resting heart rate over 100 beats per minute is accepted as tachycardia in adults. Heart rates above the resting rate may be normal ...

, and

anxiety Anxiety is an emotion characterised by an unpleasant state of inner wikt:turmoil, turmoil and includes feelings of dread over Anticipation, anticipated events. Anxiety is different from fear in that fear is defined as the emotional response ...

. Rarer side effects include

dry mouth Xerostomia, also known as dry mouth, is a subjective complaint of dryness in the mouth, which may be associated with a change in the composition of saliva, reduced salivary flow, or have no identifiable cause. This symptom is very common and is o ...

tremor A tremor is an involuntary, somewhat rhythmic muscle contraction and relaxation involving neural oscillations, oscillations or twitching movements of one or more body parts. It is the most common of all involuntary movements and can affect the h ...

hypertension Hypertension, also known as high blood pressure, is a Chronic condition, long-term Disease, medical condition in which the blood pressure in the artery, arteries is persistently elevated. High blood pressure usually does not cause symptoms i ...

euphoria Euphoria ( ) is the experience (or affect) of pleasure or excitement and intense feelings of well-being and happiness. Certain natural rewards and social activities, such as aerobic exercise, laughter, listening to or making music and da ...

, depression, and very rarely

psychosis In psychopathology, psychosis is a condition in which a person is unable to distinguish, in their experience of life, between what is and is not real. Examples of psychotic symptoms are delusions, hallucinations, and disorganized or inco ...

convulsion A convulsion is a medical condition where the body muscles contract and relax rapidly and repeatedly, resulting in uncontrolled shaking. Because epileptic seizures typically include convulsions, the term ''convulsion'' is often used as a synony ...

Pharmacology

Pharmacodynamics

Pipradrol is a central nervous system stimulant that acts primarily as a

norepinephrine Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic compound, organic chemical in the catecholamine family that functions in the brain and human body, body as a hormone, neurotransmitter and neuromodulator. The ...

and

dopamine Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic chemical of the catecholamine and phenethylamine families. It is an amine synthesized ...

reuptake inhibitor Reuptake inhibitors (RIs) are a type of reuptake modulators. It is a drug that inhibits the plasmalemmal transporter-mediated reuptake of a neurotransmitter from the synapse into the pre-synaptic neuron. This leads to an increase in extracel ...

. Its mechanism of action involves blocking the reuptake of these

neurotransmitter A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a Chemical synapse, synapse. The cell receiving the signal, or target cell, may be another neuron, but could also be a gland or muscle cell. Neurotra ...

s, leading to increased levels in the synaptic cleft and prolonged stimulation of postsynaptic neurons. Studies have shown that pipradrol's rewarding effects may be mediated through activation of the

dopamine receptor D1 Dopamine receptor D1, also known as DRD1. It is one of the two types of D1-like receptor family receptors D1 and D5. It is a protein that in humans is encoded by the DRD1 gene. Tissue distribution D1 receptors are the most abundant kind of d ...

. Unlike amphetamines, pipradrol exhibits a more intense action on higher brain centers without significantly affecting blood pressure or respiration. It also does not decrease appetite or cause post-excitement depression typically associated with amphetamines.

Pharmacokinetics

Pipradrol is rapidly absorbed and distributed to the liver, kidney, and brain tissue. The drug is quickly metabolized and eliminated from the body, with approximately 3.5% excreted in urine and 5% in stool.

History

Pipradrol was initially developed in the United States in the 1940s, patented in 1953, and marketed in the mid 1950s as the antidepressant drug Meratran. It was subsequently used as an adjunct for the treatment of

and management of senile dementia symptoms. There have also been numerous reports demonstrating favorable effects on a variety of conditions such as

ADHD Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by symptoms of inattention, hyperactivity, impulsivity, and emotional dysregulation that are excessive and pervasive, impairing in multiple ...

, and

spasmodic torticollis Spasmodic torticollis is an extremely painful chronic neurological movement disorder causing the neck to involuntarily turn to the left, right, upwards, and/or downwards. The condition is also referred to as "cervical dystonia". Both Anatomical_te ...

. Pipradrol proved useful for these applications as its relatively mild stimulant effects gave it a good safety profile compared to stronger stimulants. It was also studied as an adjutant treatment for depression and

although it was never widely used for these purposes. Pipradrol was made illegal in many countries in the late 1970s, at the same time as many other drugs which had a history of abuse. Pipradrol is a 'phenidate' type molecule, being structurally related to the prescribed stimulant methylphenidate (Ritalin, Concerta and many other branded medicines). The relatively mild stimulant effects of pipradrol, at quantities used in commercial medicine at the time (Alertonic liquid and Meratran tablets were Australian examples), meant that pipradrol was scheduled under the less restrictive classes in most countries (i.e. Class C in United Kingdom and New Zealand) but was still considered of sufficient abuse potential to be made an illegal drug. It is now an obscure compound that is virtually unknown as an illicit drug of abuse, but is still used for some scientific research, often as a comparison drug for testing other stimulants against.

References

{{Monoamine reuptake inhibitors 2-Piperidinyl compounds Benzhydryl compounds Beta-Hydroxyamphetamines Norepinephrine–dopamine reuptake inhibitors Stimulants Tertiary alcohols Wakefulness-promoting agents