Usage
- Pyritinol is prescribed as an adjunct therapy for various cerebrovascular disorders affecting blood flow and blood vessels in the brain, and mental function disorders characterized by disturbances in cognition, emotional regulation, or behavior. It is also used in the treatment of vegetative dysfunction in children and adolescents.
- Pharmacological Classification: Nootropic.
- Mechanism of Action: Pyritinol influences neurotransmitter signaling pathways, including N-methyl-d-aspartate, γ-aminobutyric acid, and acetylcholine. It demonstrates anti-inflammatory and antioxidant properties, and reduces plasma viscosity.
Alternate Names
- Pyridoxine disulfide
- Pyrithioxine
- Brand Names: Encephabol, Encefabol, Cerbon 6
How It Works
- Pharmacodynamics: Pyritinol improves cerebral function by enhancing glucose uptake and utilization, promoting nucleic acid metabolism, increasing cortical acetylcholine release and cholinergic transmission, stabilizing cell membrane structure and function via lysosomal enzyme inhibition, and preventing free radical formation. It also exhibits hemorheological effects by improving blood fluidity. In EEG studies, it increases cortical activity, possibly by activating different brain regions.
- Pharmacokinetics: Pyritinol crosses the blood-brain barrier and accumulates in the gray matter, particularly the hippocampus, cerebral nuclei, cerebellum, and cortex. It does not accumulate even with repeated oral administration and does not reach toxic concentrations, even in patients with renal impairment. Minimal amounts are excreted in human milk.
- Mode of Action: Pyritinol improves cerebral metabolism and central cholinergic transmission, normalizes cerebral microcirculation, and protects nerve cells against hypoxia, poor perfusion, and metabolic disturbances.
- Elimination Pathways: Primarily renal excretion.
Dosage
Standard Dosage
Adults:
- 600 mg daily, divided into three doses.
Children:
- 6-15 years: 100 mg three times daily (tablet) or 5 ml three times daily (liquid).
- <6 years: 2.5-10 ml daily (liquid).
- Infants (up to 1 year): 1.25 ml twice daily.
- 1-6 years: 2.5 ml twice daily.
- Pediatric Safety Considerations: The last dose should be administered no later than the late afternoon to avoid sleep disturbances.
Special Cases:
- Elderly Patients: Dosage adjustments may be necessary based on individual patient response and tolerance.
- Patients with Renal Impairment: No specific dosage adjustments are typically required.
- Patients with Hepatic Dysfunction: Caution should be exercised.
- Patients with Comorbid Conditions: Use with caution in rheumatoid arthritis and autoimmune diseases. Regular clinical checkups and lab tests are recommended.
Clinical Use Cases
The standard dosage is generally applied across clinical settings. No specific dosage adjustments are mentioned in the sources for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Adjustments may be necessary for patients with chronic conditions, with therapy lasting at least 6-8 weeks.
Side Effects
Common Side Effects
- Epigastric distress
- Anorexia
- Nausea
- Vomiting
- Headache
- Insomnia
- Rash
- Pruritus
- Restlessness
- Dizziness
Rare but Serious Side Effects
- Acute pancreatitis
- Severe cholestatic hepatitis
- Allergic reactions (skin rashes, itching, swelling)
- Proteinuria (rarely to the point of nephritic syndrome)
- Hematuria
- Muscular weakness
- Polymyositis
- Stomatitis
- Onycholysis
Long-Term Effects
Not specifically described in the sources.
Adverse Drug Reactions (ADR)
- See rare but serious side effects.
Contraindications
- Hypersensitivity to pyritinol or any components of the formulation
- Pre-existing kidney damage
- Severe liver dysfunction
- Severe changes in blood count
- Autoimmune diseases (e.g., lupus erythematosus, myasthenia gravis, pemphigus)
- Active peptic ulcers
Drug Interactions
- Penicillamine
- Gold preparations (e.g., gold sodium thiomalate)
- Sulfasalazine
- Levamisole
- Anticholinergic drugs
Pregnancy and Breastfeeding
- Pyritinol crosses the placenta, but animal studies show no teratogenic or embryotoxic effects. Minimal amounts are excreted in breast milk. Use during pregnancy and lactation only after careful assessment of the benefit-risk ratio.
Drug Profile Summary
- Mechanism of Action: Enhances cerebral metabolism, cholinergic transmission, and microcirculation. Exhibits antioxidant and anti-inflammatory effects.
- Side Effects: Epigastric distress, anorexia, nausea, vomiting, headache, insomnia, rash, restlessness. Rarely, pancreatitis and hepatitis.
- Contraindications: Hypersensitivity, severe liver/kidney disease, autoimmune diseases.
- Drug Interactions: Penicillamine, gold preparations, sulfasalazine, levamisole, anticholinergics.
- Pregnancy & Breastfeeding: Use with caution after assessing benefit-risk ratio.
- Dosage: Adults: 600 mg/day divided three times. Children: Variable depending on age; see detailed dosage guidelines.
- Monitoring Parameters: Liver function tests, renal function tests. For rheumatoid arthritis patients, regular clinical and laboratory assessments are required.
Popular Combinations
Not specified in the sources.
Precautions
- Pre-screening for allergies, metabolic disorders, organ dysfunction.
- Pregnant Women: Use with caution after assessing benefit-risk ratio.
- Breastfeeding Mothers: Use with caution after assessing benefit-risk ratio.
- Children & Elderly: Dosage adjustments based on age and tolerance.
- Lifestyle Considerations: Monitor for impaired reactivity at treatment initiation and dose increases, which can impact activities like driving.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Pyritinol?
A: Adults: 600 mg/day in three divided doses. Children: See detailed dosage guidelines above.
Q2: How should Pyritinol be administered?
A: Orally, with food. Tablets should be swallowed whole.
Q3: What are the common side effects of Pyritinol?
A: Epigastric distress, anorexia, nausea, vomiting, headache, insomnia, rash, pruritus, restlessness, and dizziness.
Q4: What are the serious side effects of Pyritinol?
A: Acute pancreatitis, severe cholestatic hepatitis, allergic reactions.
Q5: Is Pyritinol safe to use during pregnancy and breastfeeding?
A: Use with caution after a careful assessment of the benefit-risk ratio with your physician.
Q6: What are the contraindications for Pyritinol use?
A: Hypersensitivity to pyritinol, pre-existing kidney damage, severe liver dysfunction, severe changes in blood count, and autoimmune diseases.
Q7: Does Pyritinol interact with other medications?
A: Yes, it can interact with penicillamine, gold preparations, sulfasalazine, levamisole, and anticholinergics.
Q8: How long should Pyritinol treatment typically last?
A: At least 6-8 weeks, especially for chronic conditions.
Q9: Are there any special precautions for patients with rheumatoid arthritis taking Pyritinol?
A: Yes, regular clinical check-ups and laboratory tests are recommended.
Q10: Can Pyritinol be used in children?
A: Yes, but with adjusted dosages. The last daily dose should not be given in the late afternoon or evening to prevent sleep disturbances.
