Mesocarb

Pharmacological Profile and Status

Mesocarb (Mesocarbum) belongs to a distinct group of psychostimulants — sydnoneimine derivatives. In the clinical practice of the Russian Federation, it is the primary used representative of this group.

The drug possesses pronounced pharmacological activity, but its key feature lies in comparison with classic stimulants. When compared with amphetamine (which belongs to phenylalkylamine derivatives), mesocarb demonstrates a lesser psychostimulatory effect. At the same time, its safety profile is advantageous: the drug exerts a less pronounced negative effect on the autonomic functions of the body.

Mechanism of action

The drug's site of action is localized predominantly in the central nervous system (CNS). Peripheral sympathomimetic action is extremely negligible, which largely determines its safety for the cardiovascular system.

At the microscopic level, the mechanism of action is as follows:

1. The drug acts on the presynaptic terminals of neurons.
2. There is an active displacement of the neurotransmitter norepinephrine from its storage sites — presynaptic vesicles.
3. The released norepinephrine enters directly into the synaptic cleft.
4. The result of this process is a powerful activation of noradrenergic nerve impulse transmission.

Features of the Psychostimulatory Effect

Mesocarb's action is generally characterized as "mild". Unlike the effects of amphetamines, the clinical picture upon taking sydnoneimine derivatives has a number of fundamental differences:

• Smooth onset: the stimulating effect builds up gradually; it is not abrupt.
• Absence of euphoria: the drug lacks the initial stage of euphoria typical of amphetamines.
• Preservation of energy balance: the most important advantage of the drug is that it does not cause the "crash" phenomenon — meaning the subsequent depletion of the body's energy resources after the action wears off.
• Low risk of dependence: drug dependence on mesocarb develops significantly slower than on phenylalkylamine derivatives.

Clinical application

Given the drug's ability to mildly activate the CNS without subsequent depletion, it is prescribed for conditions requiring increased vitality. The main indications include:

• General weakness and various asthenic states.
• Narcolepsy (a condition accompanied by pathological sleepiness).
• Subdepressive states.

Side Effects and Precautions

Despite the fact that mesocarb provokes an increase in blood pressure (BP) to a lesser degree compared to analogues, it is capable of causing a number of adverse reactions.

• Psychoneurological sphere: patients may report internal anxiety and increased irritability. Important rule: the drug is strictly not recommended to be prescribed in the evening, as this will inevitably lead to insomnia.
• Autonomic and somatic manifestations: increased blood pressure, development of hyperthermia, constipation, and an anorexigenic effect (marked loss of appetite) are possible.
• Immune system: various allergic reactions are possible.

Briefly: answers to topical questions

Class and exam questions

What else to study on this topic

• Comparative characteristics of sydnoneimine and phenylalkylamine derivatives
• Mechanisms of drug dependence development during psychostimulant intake
• The role of norepinephrine in the regulation of the sleep-wake cycle in narcolepsy
• Anorexigenic effect of psychostimulants: mechanisms of appetite loss
• The effect of psychostimulants on the autonomic nervous system and hemodynamics

Other topics in the section "Agents Used in Psychiatry and Neurology"

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