Usage
- Benzyl nicotinate is primarily prescribed for the topical treatment of peripheral vascular disorders, rheumatic conditions, and localized inflammation like superficial thrombophlebitis (inflammation of a vein due to a blood clot). It is also used to enhance skin absorption of other active ingredients in topical formulations and is sometimes found in cosmetic products, like lip plumpers, to temporarily increase lip fullness.
- Pharmacological classification: Vasodilator, rubefacient.
- Mechanism of Action: Benzyl nicotinate acts as a vasodilator, widening blood vessels and increasing blood flow to the application site. This leads to redness and a sensation of warmth, promoting oxygenation and nutrient delivery to the treated area. It also acts as a rubefacient, causing mild skin irritation and stimulating blood circulation.
Alternate Names
- International/Regional Variations: Nicotinic acid benzyl ester
- Brand Names: It is often included as an active ingredient in combination products. Some brand names containing benzyl nicotinate include Thrombophob, Thrombotas, and Thrombin. It is also commonly found in various cosmetic lip plumping products.
How It Works
- Pharmacodynamics: Benzyl nicotinate primarily affects the cutaneous blood vessels, causing vasodilation and increased blood flow. This leads to a localized increase in temperature, redness (erythema), and sometimes mild irritation or itching. It also improves oxygenation and nutrient delivery to the treated tissue.
- Pharmacokinetics: Primarily applied topically, benzyl nicotinate is absorbed through the skin, where it exerts its vasodilatory effects. The extent of systemic absorption depends on factors like the concentration used, the area of application, and the integrity of the skin barrier. Metabolism and elimination pathways are not well-characterized for topical application but likely involves hydrolysis to nicotinic acid, which is then metabolized in the liver and excreted in urine.
- Mode of Action: Benzyl nicotinate is believed to exert its vasodilatory effects through the release of prostaglandins, specifically prostaglandin D2 and E2. This leads to relaxation of vascular smooth muscle and widening of blood vessels.
- Receptor binding, enzyme inhibition or neurotransmitter modulation: The primary mechanism of action involves prostaglandin-mediated vasodilation, not direct receptor binding, enzyme inhibition, or neurotransmitter modulation.
- Elimination pathways: Following topical application, the absorbed portion is likely metabolized, primarily in the liver, and excreted in the urine as nicotinic acid metabolites.
Dosage
Standard Dosage
Adults:
- Topical: Apply a thin layer to the affected area 2–3 times daily, or as directed by a physician. Dosage is usually expressed as a percentage concentration of benzyl nicotinate in the topical formulation (e.g., 1-5%).
- Oral: Though uncommon, oral administration is possible under strict medical supervision. Dosage will be determined by a healthcare professional based on individual patient needs and the specific condition being treated.
Children:
- Use in children requires cautious evaluation by a pediatrician due to potential skin sensitivity and irritation.
Special Cases:
- Elderly Patients: Start with a small amount to assess tolerance, as elderly individuals may have more sensitive skin.
- Patients with Renal Impairment: Monitor closely, as renal function may influence the excretion of metabolites, even with topical use.
- Patients with Hepatic Dysfunction: Dosage adjustments may be required, as hepatic metabolism is likely involved even with topical use. Monitor carefully for any signs of systemic effects.
- Patients with Comorbid Conditions: Caution should be exercised in patients with cardiovascular diseases, as widespread vasodilation may exacerbate existing conditions.
Clinical Use Cases
Benzyl nicotinate’s use in these settings is not standard practice. It is primarily used topically for localized conditions.
Dosage Adjustments
- Dose adjustments are typically based on patient tolerance and response to therapy.
Side Effects
Common Side Effects
- Localized skin irritation (burning, itching, redness)
- Sensation of warmth at the application site
Rare but Serious Side Effects
- Allergic reactions (rash, hives, difficulty breathing, swelling of the face, lips, tongue, or throat)
Long-Term Effects
- No specific long-term effects are typically associated with topical benzyl nicotinate use.
Adverse Drug Reactions (ADR)
- Severe skin irritation or allergic reactions require immediate medical attention.
Contraindications
- Hypersensitivity to benzyl nicotinate
- Application to broken skin, open wounds, or infected areas.
- Severe cardiovascular diseases where vasodilation might be risky.
Drug Interactions
- May enhance the effects of other vasodilators.
- Use with caution with antihypertensive medications.
- Potential interaction with lipid-lowering drugs (e.g., statins).
Pregnancy and Breastfeeding
- Pregnancy: Consult a healthcare provider before use. Data on safety during pregnancy is limited.
- Breastfeeding: Consult a healthcare provider before use. Data on safety during breastfeeding is limited.
Drug Profile Summary
- Mechanism of Action: Prostaglandin-mediated vasodilation.
- Side Effects: Localized skin irritation, redness, warmth. Rarely, allergic reactions.
- Contraindications: Hypersensitivity, broken skin, severe cardiovascular disease.
- Drug Interactions: Other vasodilators, antihypertensives, lipid-lowering drugs.
- Pregnancy & Breastfeeding: Consult a healthcare provider.
- Dosage: Topical: Apply a thin layer 2–3 times/day. Oral: As prescribed.
- Monitoring Parameters: Observe for skin reactions, especially in elderly patients.
Popular Combinations
- Benzyl nicotinate is often combined with heparin in topical formulations to treat thrombophlebitis. The heparin acts as an anticoagulant while the benzyl nicotinate increases blood flow.
Precautions
- General Precautions: Assess for allergies and skin conditions. Monitor cardiovascular status.
- Specific Populations: Pregnant/breastfeeding women should consult a doctor. Use cautiously in children and elderly patients.
- Lifestyle Considerations: No specific lifestyle considerations typically apply.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Benzyl Nicotinate?
A: Topical: Apply a thin layer 2–3 times/day. Oral: Determined by a physician based on individual patient needs.
Q2: How does Benzyl Nicotinate work?
A: It acts as a vasodilator, widening blood vessels and increasing blood flow to the application site, leading to warmth and redness. It also acts as a rubefacient.
Q3: What are the common side effects?
A: Localized skin irritation, redness, and a warming sensation are common.
Q4: Can I use Benzyl Nicotinate if I am pregnant?
A: Consult your doctor before use during pregnancy, as safety data is limited.
Q5: Are there any drug interactions I should be aware of?
A: Use with caution with other vasodilators, antihypertensives, and lipid-lowering drugs.
Q6: What should I do if I experience severe skin irritation?
A: Discontinue use immediately and consult a physician.
Q7: How long does it take for Benzyl Nicotinate to work?
A: The onset of action varies, but typically, a feeling of warmth and redness occurs within minutes of topical application. Peak vasodilatory effect occurs around 10 minutes after application and may last for approximately 45 minutes.
Q8: Can Benzyl Nicotinate be used in children?
A: Use in children requires careful evaluation by a pediatrician due to potential sensitivity.
Q9: Is Benzyl Nicotinate a steroid?
A: No, benzyl nicotinate is not a steroid. It is a vasodilator.
Q10: Can I use Benzyl Nicotinate on open wounds?
A: No, avoid application on open wounds, cuts, or irritated skin.
