Usage
Buphenine hydrochloride is a vasodilator, primarily prescribed for peripheral vascular diseases like Raynaud’s disease, thromboangiitis obliterans (Buerger’s disease), arteriosclerosis obliterans, and other conditions affecting blood circulation in the extremities. It aims to improve blood flow and alleviate symptoms such as pain, numbness, and coldness in the hands and feet. It belongs to the pharmacological class of sympathomimetic amines and acts as a peripheral vasodilator. Although primarily used for peripheral vascular diseases, it has off-label uses in conditions like night leg cramps, diabetic vascular disease, frostbite.
Alternate Names
Buphenine is also known as Nylidrin or Nylidrin hydrochloride.
How It Works
Pharmacodynamics: Buphenine acts as a beta-2 adrenergic receptor agonist, leading to vasodilation, primarily in skeletal muscle vasculature. It also possesses some beta-1 adrenergic activity resulting in a positive inotropic effect on the heart. Buphenine relaxes smooth muscle in the blood vessel walls, reducing peripheral resistance and increasing blood flow.
Pharmacokinetics: Buphenine is administered orally. Absorption, distribution, metabolism, and excretion details are not clearly defined in the provided literature. It is known to be metabolized in the liver and excreted through the kidneys. More research is required to provide detailed pharmacokinetic parameters.
Mode of Action: Buphenine’s primary mode of action is stimulating beta-adrenergic receptors, leading to smooth muscle relaxation and vasodilation. This effect is believed to be mediated by increased intracellular cAMP, which ultimately decreases intracellular calcium concentration and vascular tone. Elimination pathways are presumed renal, but further research is needed.
Dosage
Standard Dosage
Adults:
The standard adult dosage of Buphenine is 3-12 mg, three to four times a day, with a maximum daily dose of 90 mg.
Children:
Safety and efficacy not established for children under 2 years of age. For children aged 2-12 years, 2-6 mcg/kg administered slowly intravenously or intramuscularly every 4-6 hours has been used in some clinical settings for pain management. For children over 12 years, the adult dose of 0.3 mg IV/IM every 6 hours is often applied. Slow intravenous administration over at least 2 minutes is recommended, with possible repeat of up to 0.3 mg once, 30-60 minutes after the initial dose, if needed.
Special Cases:
Dosage adjustments may be necessary for patients with renal or hepatic impairment, but specific recommendations are lacking in the provided literature. For elderly patients, it’s generally advised to start with a lower dose and titrate gradually based on response and tolerability due to potential age-related changes in drug clearance and sensitivity. Specific guidelines for patients with comorbid conditions like diabetes or cardiovascular disease are not available, hence careful monitoring is necessary.
Clinical Use Cases
The provided sources do not specify dosages for Buphenine use in specific clinical situations like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. If its use in these settings is considered, it is recommended to consult specialized literature and guidelines.
Side Effects
Common Side Effects
Common side effects include trembling, nervousness, weakness, dizziness, palpitations, nausea, and, less commonly, anemia. Tachycardia (rapid heart rate) is also a potential side effect due to the drug’s beta-adrenergic stimulation.
Rare but Serious Side Effects
Hypotension (low blood pressure) can occur, potentially leading to fainting or cardiovascular complications. Monitoring blood pressure is crucial, especially during initial treatment or dose adjustments.
Long-Term Effects
Data regarding the long-term effects of Buphenine is limited. Continuous monitoring of patients on long-term Buphenine therapy is recommended to assess efficacy and monitor potential adverse effects.
Contraindications
Buphenine is contraindicated in patients with recent myocardial infarction (MI), hyperthyroidism, paroxysmal tachycardia, and severe angina pectoris. Its use in patients with severe coronary artery disease, uncontrolled hypertension, or a history of stroke should be avoided.
Drug Interactions
Buphenine can interact with beta-blockers, reducing its vasodilatory effects. Concurrent use with other sympathomimetic drugs might exacerbate cardiovascular side effects. Caution is necessary when combining Buphenine with other vasodilators or antihypertensives, as it can cause dangerously low blood pressure. Interactions with MAOIs may lead to excessive vasodilation and severe hypotension, so concomitant use should be avoided. Patients taking anticoagulants or antiplatelet medications should inform their doctor before using Buphenine. Information regarding interactions with other medications is limited.
Pregnancy and Breastfeeding
The safety of Buphenine during pregnancy has not been clearly established. Some sources suggest it might be unsafe and could pose a risk to the fetus, while others suggest its use only when absolutely necessary under strict medical supervision. Data regarding Buphenine’s excretion into breast milk and potential neonatal side effects is insufficient, making its use during breastfeeding generally not recommended.
Drug Profile Summary
- Mechanism of Action: Beta-2 adrenergic receptor agonist, causing peripheral vasodilation. Also has some beta-1 activity.
- Side Effects: Trembling, nervousness, weakness, dizziness, palpitations, nausea, anemia, tachycardia, hypotension.
- Contraindications: MI, hyperthyroidism, paroxysmal tachycardia, severe angina, severe coronary artery disease, uncontrolled hypertension, stroke history.
- Drug Interactions: Beta-blockers, other sympathomimetic drugs, vasodilators, antihypertensives, MAOIs, anticoagulants, antiplatelet medications.
- Pregnancy & Breastfeeding: Use with caution in pregnancy, if at all; breastfeeding is not generally recommended due to limited safety data.
- Dosage: Adults: 3-12 mg 3-4 times/day, up to 90 mg/day. Children (2-12 years): 2-6 mcg/kg IV/IM every 4-6 hours. Children (>12 years): 0.3 mg IV/IM every 6 hours.
- Monitoring Parameters: Blood pressure, heart rate, signs of peripheral circulation improvement, adverse effects.
Popular Combinations
Specific data on popular Buphenine drug combinations are limited within the provided sources.
Precautions
- General Precautions: Pre-screening for allergies, cardiovascular conditions, metabolic disorders, and renal/hepatic function is recommended.
- Specific Populations: Caution is advised in pregnant and breastfeeding women and in patients with renal or hepatic impairment. Dosage adjustments may be necessary in elderly patients.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Buphenine?
A: For adults, the typical dosage is 3-12 mg three to four times daily, with a maximum daily dose of 90 mg. Children’s dosage differs based on age and administration route, requiring consultation with pediatric guidelines.
Q2: What are the common side effects of Buphenine?
A: Common side effects include trembling, nervousness, weakness, dizziness, palpitations, nausea, and occasionally anemia. Tachycardia is also commonly reported.
Q3: What are the serious side effects of Buphenine?
A: Hypotension can be a serious side effect, potentially leading to fainting or cardiovascular complications.
Q4: Is Buphenine safe to use during pregnancy?
A: Its safety during pregnancy is not definitively established. It should be used with caution and only when the benefits outweigh the potential risks, under strict medical supervision.
Q5: Can I breastfeed while taking Buphenine?
A: Data on Buphenine’s presence in breast milk and its effects on infants are limited. It’s generally advised to avoid breastfeeding while on Buphenine.
Q6: What conditions is Buphenine used to treat?
A: Primarily, it’s used for peripheral vascular diseases like Raynaud’s disease, thromboangiitis obliterans, and arteriosclerosis obliterans. It can also be prescribed for night leg cramps and other circulatory disorders.
Q7: How does Buphenine work?
A: It acts as a beta-2 adrenergic receptor agonist, causing vasodilation in peripheral blood vessels and improving blood flow.
Q8: What are the contraindications for Buphenine use?
A: Contraindications include recent myocardial infarction, hyperthyroidism, paroxysmal tachycardia, and severe angina pectoris. Caution is advised in patients with severe coronary artery disease, uncontrolled hypertension, or a history of stroke.
Q9: Does Buphenine interact with other medications?
A: Yes, it can interact with beta-blockers, other sympathomimetic agents, vasodilators, antihypertensives, MAOIs, anticoagulants, and antiplatelet medications. Provide a complete medication history to your doctor before starting Buphenine.
