BUFYL

Uses

Bupivacaine is indicated for the production of local or regional anaesthesia or analgesia for surgery, for oral surgery procedures, for diagnostic and therapeutic procedures, and for obstetrical procedures. The routes of administration and indicated Bupivacaine concentrations are: Local infiltration: 0.25% Peripheral nerve block: 0.25%, 0.5% Sympathetic block: 0.25% Lumbar epidural: 0.25%, 0.5% and 0.75% (non-obstetrical) Caudal: 0.25%, 0.5%Fentanyl is indicated for the management of breakthrough pain in patients with cancer who are already receiving and who are tolerant to opioid therapy for their underlying persistent cancer pain. Patients considered opioid tolerant are those who are taking at least 60 mg of oral morphine/day, at least 25 mcg of transdermal Fentanyl/hour, at least 30 mg of oxycodone daily, at least 8 mg of oral hydromorphone daily or an equianalgesic dose of another opioid for a week or longer.

Dosage

BUFYL dosage

Each 30 ml contains 150 mg Bupivacaine Hydrochloride (anhydrous) USP.The dose of any local anaesthetic administered varies with the anaesthetic procedure, the area to be anaesthetized, the vascularity of the tissues, the number of neuronal segments to be blocked. In recommended doses, Bupivacaine produces complete sensory block, but the effect on motor function differs among the three concentrations.0.25% when used for caudal, epidural, or peripheral nerve block, produces incomplete motor block. Should be used for operations in which muscle relaxation is not important, or when another means of providing muscle relaxation is used concurrently. Onset of action may be slower than with the 0.5% or 0.75% solutions.0.5% provides motor blockade for caudal, epidural, or nerve block, but muscle relaxation may be inadequate for operations in which complete muscle relaxation is essential.Maximum dosage limit must be individualized in each case after evaluating the size and physical status of the patient, as well as the usual rate of systemic absorption from a particular injection site. Most experience to date is with single doses of Bupivacaine up to 175 mg. These doses may be repeated up to once every three hours. In clinical studies to date, total daily doses up to 400 mg have been reported. Until further experience is gained, this dose should not be exceeded in 24 hours.The following dosages have generally proved satisfactory and are recommended as a guide for use in the average adult. These dosages should be reduced for young, elderly or debilitated patients. Local Infiltration: 0.25%: up to max (mg) Epidural: 0.5%: 50-100 mg Epidural: 0.25%: 25-50 mg Caudal: 0.5%: 75-150 mg Caudal: 0.25%: 37.5-75 mg Peripheral Nerves: 0.5%: 25 mg to max. Peripheral Nerves: 0.25%: 12.5 mg to max. Sympathetic 0.25%: 50-125 mgOral- Starting Dose:The initial dose of Fentanyl should be 100 mcg. Re-dosing patients within a single episode: Dosing may be repeated once during a single episode of breakthrough pain if pain is not adequately relieved by one Fentanyl dose. Re-dosing may occur 30 minutes after the start of administration of Fentanyl and the same dosage strength should be used. Increasing the dose: Titration should be initiated using multiples of the 100 mcg Fentanyl tablet. Patients require to titrate above 100 mcg can be instructed to use two 100 mcg tablets (one on each side of the mouth in the buccal cavity). If this dose is not successful in controlling the breakthrough pain episode, the patient may be instructed to place two 100 mcg tablets on each side of the mouth in the buccal cavity (total of four 100 mcg tablets). Titrate above 400 mcg by 200 mcg increments bearing in mind using more than 4 tablets simultaneously has not been studied and it is important to minimize the number of strengths available to patients at any time to prevent confusion and possible overdose. To reduce the risk of overdose during titration, patients should have only one strength of Fentanyl tablet available at any one time. Dosage Adjustment:Generally, the dose of Fentanyl should be increased when patients require more than one dose per breakthrough pain episode for several consecutive episodes. Injection- Fentanyl injection can be administered intravenously either as a bolus or by infusion & by intramuscular route also. The dose of fentanyl should be individualized according to age, body weight, physical status, underlying pathological condition, use of other drugs and type of surgery and anesthesia. Doses in excess of 200mcg are for use in anesthesia only. As a premedicant, 1-2 ml fentanyl may be given intramuscularly 45 minutes before induction of anesthesia. After IV administration in unpremedicated adult patients, 2ml fentanyl may be expected to provide sufficient analgesia for 10-20 minutes in surgical procedures involving low pain intensity. 10 ml fentanyl injected as a bolus gives analgesia lasting about one hour. The analgesia produced is sufficient for surgery involving moderately painful procedures. Giving a dose of 50mcglkg fentanyl will provide intense analgesia for some four to six hours, for intensely stimulating surgery. Fentanyl may also be given as an infusion. In ventilated patients, a loading dose of fentanyl may be given as a fast infusion of approximately 1 mcg/kg/min for the first 10 minutes followed by an infusion of approximately 0.1 mcg/kg/min. Alternatively the loading dose of fentanyl may be given as a bolus. Infusion rates should be titrated to individual patient response; lower infusion rates may be adequate. Unless it is planned to ventilate post operatively, the infusion should be terminated at about 40 minutes before the end of surgery. Lower infusion rates, e.g. 0.05-0.08 mcg/kg/min. are necessary if spontaneous ventilation .is to be maintained. Higher infusion rates (up to 3 mcg/kg/min) have been used in cardiac surgery. Fentanyl is chemically incompatible with the induction agents thiopentone & methohexitone because of wide differences in pH Use in elderly and debilitated patients: It is wise to reduce the dosage in the elderly and debilitated patients. The effect of the initial dose should be taken into account in determining supplemental doses. Transdermal-Intractable chronic pain: Adult:Patches deliver fentanyl in doses that range from: 12-100 mcg/hr. Doses should be individually titrated based on previous use of opioids. Opioid-naive patients: Initially, ≤25 mcg/hr; it is recommended to initially titrate w/ low doses of short-acting opioids before starting fentanyl patches. Patients receiving a strong opioid analgesic: Initial dose should be based on the previous 24-hr opioid requirements. During transfer to fentanyl patches, previous opioid treatment should be phased out gradually. If patient requires doses >100 mcg/hr, >1 patch may be used; consider alternative or additional therapy if doses >300 mcg/hr are required. Replace patch every 72 hr and apply the new patch to a different site; avoid using the same area of skin for a few days. Elderly:Dose reduction may be needed. Tablet Administration: Patients should remove the tablet from the blister strip and immediately place the entire tablet in the buccal cavity (above a rear molar, between the upper cheek and gum). Patients should not attempt to split the tablet. The tablet should not be chewed or swallowed, as this will result in lower plasma concentrations than when taken as directed. The tablet should be left between the cheek and gum until it has disintegrated, which usually takes approximately 14-25 minutes. After 30 minutes, if remnants from the tablet remain, they may be swallowed with a glass of water.

Side Effects

Central Nervous System and Neurological: Restlessness, excitement, nervousness, dizziness, tinnitus, blurred vision, miosis, nausea, vomiting, numbness of the tongue and perioral region, chills, tremors, muscle twitching, convulsions. Cardiovascular System Reactions: Myocardial depression and peripheral vasodilatation resulting hypotension and bradycardia, ventricular arrhythmia, cardiac arrest. Hypersensitivity: urticaria, pruritus, erythema, angioneurotic edema ,tachycardia, sneezing, nausea, vomiting, dizziness, syncope, excessive sweating, elevated temperature, and possibly, anaphylactoid reactions.As with other narcotic analgesics, the most common serious adverse reactions reported to occur with Fentanyl are respiratory depression, apnoea, muscular rigidity, myoclonic movements, and bradycardia. Respiratory depression is more likely to occur with intravenous administration if a dose is given too rapidly and it rarely occurs with intramuscular administration.

Precaution

Local anaesthetics should only be employed by clinicians who are well versed in diagnosis and management of dose-related toxicity and other acute emergencies which might arise from the block to be employed, and then only after ensuring the immediate availability of oxygen, other resuscitative drugs, cardiopulmonary resuscitative equipment, and the personal resources needed for proper management of toxic reactions and related emergencies.Should be given cautiously to the elderly, the debilitated and to children, to patients with epilepsy, impaired cardiac conductions, shock, liver damage and myasthenia gravis.The lowest dosage of local anaesthetic that results in effective anaesthesia should be used to avoid high plasma levels and serious adverse effects. The rapid injection of a large volume of local anaesthetic solution should be avoided and fractional (incremental) doses should be used when feasible. Careful and constant monitoring of cardiovascular and respiratory (adequacy of ventilation) vital signs and the patient's state of consciousness should be performed after each local anaesthetic injection. Because of the risk of systemic adverse effects when local anaesthetics are absorbed too rapidly, they should not be injected into inflamed or infected tissues and should not be applied to damaged mucosa.Opioid analgesics impair the mental and/or physical ability required for the performance of potentially dangerous tasks (e.g. driving a car or operating machinery). Patients taking Fentanyl should be warned of these dangers and should be counseled accordingly. The use of concomitant CNS active drugs requires special patient care and observation.Chronic pulmonary disease: Fentanyl should be titrated with caution in patients with chronic obstructive pulmonary disease or pre-existing medical conditions predisposing them to respiratory depression. Head injuries and increased intracranial pressure: Opioids may obscure the clinical course of a patient with a head injury and should be used only if clinically warranted.Cardiac disease: Intravenous Fentanyl may produce bradycardia. Therefore, Fentanyl should be used with caution in patients with bradyarrhythmias.Hepatic or renal disease: Fentanyl should be used with caution because of the hepatic metabolism and renal excretion of Fentanyl.

Interaction

Bupivacaine should be used with caution in patients receiving other local anaesthetics or agents structurally related to amide‐type local anaesthetics, e.g. certain anti‐arrhythmics, such as lidocaine and mexiletine, since the systemic toxic effects are additive.Specific interaction studies with Bupivacaine and anti arrhythmic drugs class III (e.g. amiodarone) have not been performed, but caution should be advised.Co-administration of different antifungals, macrolide antibiotics, CNS depressant drugs like ketoconazole, itraconazole, troleandomycin, clarithromycin, nelfinavir, and nefazadone may enhance or prolong the effects of Fentanyl. The concomitant use of amprenavir, aprepitant, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, and verapamil with Fentanyl may also result in an increase in Fentanyl plasma concentrations, which could increase or prolong adverse drug effects and may cause potentially fatal respiratory depression.

Pregnancy & Breastfeeding use

Bupivacaine injection should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Caution should be exercised when administered during lactation.Pregnancy category C. There are no adequate and well-controlled studies in pregnant women. Fentanyl should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Fentanyl is excreted in human milk; therefore Fentanyl should not be used in nursing women because of the possibility of sedation and/or respiratory depression in their infants.

Contraindication

Hypersensitivity to Bupivacaine, other amide type local anaesthetics or other components of these preparations; Intravenous regional anaesthesia; obstetrical paracervical block anaesthesia.Fentanyl is contraindicated in the management of acute or postoperative pain. This product must not be used in opioid non-tolerant patients. Fentanyl is contraindicated in patients with known intolerance or hypersensitivity to any of its components or the drug Fentanyl.

Special Warning

Use in Children: Administration to children under 12 years of age is not recommended until further experience is gained in this group.

Acute Overdose

In insufficient overdosage, Fentanyl would produce narcosis, marked skeletal muscle rigidity. Cardio-respiratory depression and cyanosis may also occur. In the presence of hypoventilation or apnoea, oxygen should be administered and respiration should be assisted. A specific narcotic antagonist, such as naloxane, should be available for use as indicated to manage respiratory depression.

Storage Condition

Keep in a cool & dry place, protected from light. Keep out of the reach of children.Store between 20-25°C. Protect from light.

Innovators Monograph

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