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Nicotinic Acid Derivatives

Acidum nicotinicum et derivata

For medical students2 min readUpdated 2026-10-10

Nicotinic acid derivatives were developed to minimize the adverse effects of the parent compound while preserving its vasodilating activity. These agents are effective in treating cerebral and peripheral circulatory disorders.

Parent CompoundNicotinic acid provides pronounced vasodilation
Cerebral Blood FlowPreferential dilation of cerebral blood vessels
Antiplatelet EffectsReduction of platelet aggregation
Combination DrugsCombination with theophylline or GABA

Rationale and Characteristics of the Parent Compound

Nicotinic acid itself has the property of dilating blood vessels both peripherally and in the brain. However, its main drawback is poor patient tolerance due to pronounced adverse effects. For this reason, in clinical practice involving cerebral blood flow disorders, modified derivatives are preferred because they retain the necessary therapeutic efficacy while being significantly better tolerated.

Xanthinol Nicotinate

This is a combination drug whose chemical structure combines elements of nicotinic acid and theophylline.

Pharmacodynamic properties:

  1. Vasodilation: dilates peripheral and cerebral blood vessels.
  2. Hemodynamics: improves blood flow in both vascular beds.
  3. Metabolic Effect: reduces the severity of cerebral hypoxia.
  4. Rheology: exerts a moderate antiplatelet effect, decreasing platelet aggregation tendency.

The main indication for prescription is peripheral and cerebral circulatory disorders developing against the background of atherosclerosis.

Nicotinoyl-GABA (Picamilon)

This agent is classified as a GABA derivative (gamma-aminobutyric acid). Its chemical molecule combines fragments of GABA and nicotinic acid. The main pharmacological feature of picamilon is its selective (preferential) dilation of cerebral blood vessels, making it an important tool in managing cerebrovascular disorders.

Mnemonic

Xanthinol nicotinate is a Combination molecule (nicotinic acid + theophylline). Picamilon has a Peak activity in the brain (GABA derivative with selective action on cerebral vessels).

Frequently asked questions

What specific adverse effects does pure nicotinic acid cause that lead to poor tolerability?

Pure nicotinic acid causes the following adverse effects:

  • Vascular reactions — flushing of the face, neck, and upper chest, sensation of warmth.
  • Allergic reactions.
  • Pruritus.
  • Gastrointestinal and cardiovascular disturbances.
  • Liver dysfunction with prolonged use of high doses, accompanied by an excessive increase in NAD and NADP levels.
What other drugs belong to the nicotinic acid derivative group besides xanthinol nicotinate and picamilon?

Sources mention the following drugs containing nicotinic acid or its moiety:

  • Hydroxymethylnicotinamide (Hydroxymethylnicotinamidum) — a derivative of nicotinic acid amide and formaldehyde; a synthetic choleretic agent.
  • Nicergoline (Nicergoline) — an ergot alkaloid derivative containing an ergoline nucleus and a brominated nicotinic acid residue; possesses alpha-adrenolytic and myotropic antispasmodic activity.
  • Enduracin — a extended-release formulation of nicotinic acid.
What is the mechanism of the vasodilating action of nicotinic acid itself?

The vasodilating action of nicotinic acid is mediated by the stimulation of prostaglandin synthesis, specifically prostaglandins D2 and E2. Prostaglandin D2 activates DP1 receptors in cutaneous blood vessels, leading to vasodilation, facial flushing, and a sensation of warmth.

Why are nicotinic acid derivatives often used instead of pure nicotinic acid?

Pure nicotinic acid causes pronounced vasodilation but has poor patient tolerance due to adverse reactions. Derivatives preserve the vasodilating properties while offering better tolerability.

What components make up the xanthinol nicotinate molecule?

The chemical structure of this drug includes elements of nicotinic acid and theophylline.

Which pharmacological group does Picamilon belong to?

Picamilon (nicotinoyl-GABA) belongs to gamma-aminobutyric acid (GABA) derivatives.

What are the main indications for xanthinol nicotinate?

It is prescribed for cerebral and peripheral circulatory disorders that develop in the setting of atherosclerosis.

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