Usage
Xantinol nicotinate is prescribed for managing peripheral vascular diseases (PVD), such as intermittent claudication, and cerebrovascular disorders. It is classified as a peripheral vasodilator and acts by widening blood vessels to improve blood flow in the affected areas.
Alternate Names
While “xantinol nicotinate” is the commonly used generic name, it may also be referred to as “xanthinol nicotinate.” Brand names include Complamina and Complamina Retard.
How It Works
Pharmacodynamics: Xantinol nicotinate is a combination of xanthinol and nicotinic acid. It primarily works by relaxing the smooth muscles in the walls of small arteries and capillaries. This vasodilatory effect increases blood flow and oxygen delivery to peripheral tissues, like the limbs, and cerebral tissues. It also decreases peripheral vascular resistance. It appears to have effects on blood viscosity, cholesterol levels, and fibrinogen levels in some patients.
Pharmacokinetics: Xantinol nicotinate is administered orally. Absorption, metabolism, and elimination pathways are not fully elucidated in current literature, but hepatic metabolism is likely involved.
Mode of Action: The drug’s primary effect is the direct relaxation of vascular smooth muscle. This results in vasodilation and improved blood flow. It appears to increase erythrocyte flexibility and nutritive microcirculation. It may improve cerebral metabolism by increasing glucose uptake across the blood-brain barrier. Some studies suggest it inhibits platelet aggregation.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: The precise mechanisms through which xantinol nicotinate interacts at the cellular and molecular level are not comprehensively documented. It is known to affect vascular smooth muscle, but the specific receptors, enzymes, or neurotransmitters involved require further investigation.
Dosage
Standard Dosage
Adults:
The standard dosage is 150-300 mg three times daily, with meals. Some sources suggest up to 600 mg three times a day or a total daily dose of 3g, particularly for PVD. Sustained-release formulations (e.g., Complamina Retard) are available and usually prescribed as 500mg or 1g twice daily. It is important to adhere to the specific dosage prescribed by a physician.
Children:
Use in children under 18 is generally not recommended, though some sources indicate caution. Consultation with a pediatrician is crucial.
Special Cases:
- Elderly Patients: Use with caution due to potential increased sensitivity to side effects. Dosage adjustments may be necessary.
- Patients with Renal Impairment: Exercise caution. Dose adjustments based on the degree of renal impairment may be required.
- Patients with Hepatic Dysfunction: Exercise caution. Dose modifications may be necessary.
- Patients with Comorbid Conditions: Use cautiously in patients with heart disease (especially recent myocardial infarction or cerebrovascular accident), hypotension, active peptic ulcer disease, gout, or glaucoma. Close monitoring is advised in such cases.
Clinical Use Cases
Dosage recommendations for specific clinical situations (intubation, surgical procedures, mechanical ventilation, ICU use, emergency situations) are not well established. The drug’s primary use remains in managing PVD and cerebrovascular disorders.
Dosage Adjustments
Dose adjustments based on individual patient factors are determined by the treating physician. These adjustments may be necessary for renal/hepatic impairment, heart disease, hypotension, etc.
Side Effects
Common Side Effects
- Flushing (reddening of the skin and sensation of warmth)
- Headache
- Dizziness
- Nausea
- Increased heart rate
- Generalized itching and rash
- Gastrointestinal discomfort (especially on an empty stomach)
Rare but Serious Side Effects
- Hypoglycemia
- Hypotension
- Severe allergic reactions
Long-Term Effects
The long-term effects of xantinol nicotinate are not well documented.
Adverse Drug Reactions (ADR)
ADRs requiring immediate intervention are primarily related to severe allergic reactions, significant hypotension, or hypoglycemia.
Contraindications
- Hypersensitivity to xantinol nicotinate
- Severe hemorrhage
- Recent myocardial infarction
- Recent cerebrovascular accident
- Severely compromised cardiac function
- Pregnancy (unless absolutely necessary and under strict medical supervision)
- Breastfeeding (unless absolutely necessary and under strict medical supervision)
- Arterial bleeding
- Severe hypotension
Drug Interactions
- Antihypertensive medications (increased risk of hypotension)
- Anticoagulants/antiplatelet drugs (increased risk of bleeding)
- Other vasodilators (additive effects)
- Ganglion blockers and sympatholytic agents
- Alcohol (potential for increased hypotension)
Pregnancy and Breastfeeding
The drug is generally contraindicated in both pregnancy and breastfeeding unless the potential benefit outweighs the risks. Its safety profile in these situations is not well-established.
Drug Profile Summary
- Mechanism of Action: Peripheral vasodilator, improves blood flow to peripheral and cerebral tissues.
- Side Effects: Flushing, headache, dizziness, nausea, itching, rash, gastrointestinal discomfort. Rare: hypotension, hypoglycemia, allergic reactions.
- Contraindications: Hypersensitivity, severe hemorrhage, recent MI, recent stroke, severe cardiac dysfunction, pregnancy, breastfeeding.
- Drug Interactions: Antihypertensives, anticoagulants, other vasodilators, ganglion blockers, sympatholytics.
- Pregnancy & Breastfeeding: Generally contraindicated.
- Dosage: Adults: 150-600 mg TID; or 500mg-1g sustained release BID. Max: 1.8g/day- 3g/day. Children: Not recommended.
- Monitoring Parameters: Blood pressure, heart rate, blood glucose, signs of bleeding.
Popular Combinations
Specific popular drug combinations are not prominently featured in available literature. However, it’s important to be aware of potential interactions with commonly prescribed medications.
Precautions
- Pre-existing conditions: Evaluate for heart, liver, or kidney disease, hypotension, peptic ulcer disease, gout, glaucoma.
- Pregnant women: Contraindicated unless benefit outweighs risk.
- Breastfeeding mothers: Contraindicated unless benefit outweighs risk.
- Children and Elderly: Use with caution and under strict medical supervision.
- Lifestyle Considerations: Alcohol may potentiate hypotension; Maintain a healthy diet and exercise regimen. Driving may be affected by side effects such as dizziness.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Xantinol Nicotinate?
A: The standard adult dosage ranges from 150-300 mg three times daily with meals. For sustained-release formulations, 500mg-1g twice a day is typical. The maximum dosage is usually 1.8g-3g per day. Pediatric use is generally not recommended.
Q2: What are the primary uses of Xantinol Nicotinate?
A: Primarily used for peripheral vascular disease (PVD) like intermittent claudication, and cerebrovascular disorders.
Q3: What is the mechanism of action of this drug?
A: Acts as a peripheral vasodilator, relaxing blood vessel walls, thereby increasing blood flow and oxygen delivery to tissues.
Q4: What are the common side effects?
A: Flushing, headache, dizziness, nausea, itching, rash, gastrointestinal discomfort are common. Less common side effects include hypotension and hypoglycemia.
Q5: Are there any serious side effects I should be aware of?
A: Rarely, serious side effects such as severe hypotension, hypoglycemia, and allergic reactions can occur.
Q6: What are the contraindications for this drug?
A: Contraindicated in hypersensitivity, severe hemorrhage, recent MI or stroke, severely compromised cardiac function, pregnancy, and breastfeeding. Should be used with caution in those with liver or kidney impairment, low blood pressure, heart disease, or active peptic ulcer disease.
Q7: Does Xantinol Nicotinate interact with other medications?
A: Yes, potential interactions exist with antihypertensives, anticoagulants, other vasodilators, ganglion blockers, and sympatholytics.
Q8: Can this medicine be used during pregnancy or while breastfeeding?
A: Generally contraindicated during pregnancy and breastfeeding unless the benefits clearly outweigh the potential risks.
Q9: What precautions should I take when prescribing this medication?
A: Carefully evaluate patients for pre-existing conditions like heart, liver, or kidney disease. Exercise caution in elderly patients and those with comorbid conditions. Monitor for side effects, especially hypotension and hypoglycemia.
Q10: Are there any specific monitoring parameters for patients on Xantinol Nicotinate?
A: Monitor blood pressure, heart rate, blood glucose, and look for any signs of bleeding. Close monitoring is especially important in patients with comorbid conditions.
