Pack : 5 Ml Pack


A-CAINE EYE DROPS is a local anesthetic for ophthalmic instillation. Each mL of sterile, aqueous solution contains: Active: Proparacaine Hydrochloride 5 mg (0.5%). Preservative: Chlorbutal 5 mg (0.5%).


Label Claim: Each ML Contains :

• Proparacaine Hydrochloride U.S.P ............0.5% w/v
• Chlorbutol I.P. ...........................................0.5% w/v (as preservative
• Aqueous Base .................................q.s


Primary packing - 5ml Opaque Poly bottles White caps & Nozzles.
Secondary Packing - Labels, Cartons, Shrink Pack & Shipper box.


12 months from the date of manufacturing.


Store in Refrigerator after the container is opened. Keep in cool & dark place.


5ml of solution in Opaque poly bottles with white caps & nozzles in properly sealed.


A-CAIN EYE DROPS is a rapid acting local anesthetic suitable for ophthalmic use. With a single drop, the onset of anesthesia begins within 30 seconds and persists for 15 minutes or longer. The main site of anesthetic action is the nerve cell membrane where proparacaine interferes with the large transient increase in the membrane permeability to sodium ions that is normally produced by a slight depolarization of the membrane. As the anesthetic action progressively develops in a nerve, the threshold for electrical stimulation gradually increases and the safety factor for conduction decreases; when this action is sufficiently well developed, block of conduction is produced.
The exact mechanism whereby proparacaine and other local anesthetics influence the permeability of the cell membrane is unknown; however, several studies indicate that local anesthetics may limit sodium ion permeability by closing the pores through which the ions migrate in the lipid layer of the nerve cell membrane. This limitation prevents the fundamental change necessary for the generation of the action potential.


A-CAIN EYE DROPS is indicated for procedures in which a topical ophthalmic anesthetic is indicated: corneal anesthesia of short duration, e.g. tonometry, gonioscopy, removal of corneal foreign bodies, and for short corneal and conjunctival procedures.


A-CAIN EYE DROPS should be considered contraindicated in patients with known hypersensitivity to any of the ingredients of this preparation.


NOT FOR INJECTION - FOR TOPICAL OPHTHALMIC USE ONLY. Prolonged use of a topical ocular anesthetic is not recommended. It may produce permanent corneal opacification with accompanying visual loss.


Usual Dosage: Removal of foreign bodies and sutures, and for tonometry: 1 to 2 drops (in single instillations) in each eye before operating. Short corneal and conjunctival procedures: 1 drop in each eye every 5 to 10 minutes for 5 to 7 doses.


A-CAIN EYE DROPS is supplied in one Opeque Polethylene Bottle packed with printed labeled in a unit carton and, Such 25 Carton Packed in a Shrink Sleeves. Such 12 shrinks packed in a shipper.


Local Anesthetic

(Bupivacaine Hydrochloride Injection USP 0.5% W/V)


B-CAINE (Bupivacaine Hydrochloride Injection USP 0.5% w/v) is used as a local or regional anesthetic for various procedures. Its safety and effectiveness depend on proper dosage, correct administration and readiness for emergencies. Bupivacaine is a prescription medication used to prevent pain and induce spinal anesthesia. Bupivacaine belongs to a group of drugs called local anesthetics. These work by numbing one small area of the body (local) or blocking pain in an area of the body (regional). This medication is available in an injection form to be administered by injection via local infiltration, peripheral nerve block, or caudal and lumbar blocks by a healthcare professional.


Each ML Contains:

Bupivacaine Hydrochloride USP
Eq. to anhydrous
• Bupivacaine Hydrochloride......... 5.0 mg
• Methylparaben USP............. 1.0 mg
(As preservative)
• Water for Injection USP......... q.s.


Pharmacodynamic :

Bupivacaine has a similar mechanism of action to other local anesthetic in nerve axons in the peripheral nervous system. It also interferes with the function of all organs in which conduction or transmission of impulses occur. These include effects on the CNS, the autonomic ganglia, the neuromuscular junction and all forms of muscle fibres. At high doses it produces surgical anaesthesia, while at lower doses it produces sensory block (analgesia) with less pronounced motor block. Following absorption, Bupivacaine may cause stimulation of the CNS followed by depression and, in the cardiovascular system, it acts primarily on the myocardium where it may decrease electrical excitability, conduction rate, force of contraction and eventually cardiac arrest.

Pharmacokinetic Properties:

Like other local anesthetic, the rate of systemic absorption of Bupivacaine is dependent upon the total dose and concentration administered, the route of administration and the vascularity of the tissue locally. Bupivacaine is about 95% bound to plasma proteins, mainly to alpha-1- acid glycoprotein at low concentrations and to albumin at high concentrations. In adults, the terminal half-life of Bupivacaine is 2.7 hours. In neonates and some young infants, terminal elimination half-lives could be as long as 8 to 12 hours. The maximum blood concentration varies with the site of injection.
Amide local anesthetic including Bupivacaine have been shown to have diminished clearance in neonates and infants less than 3 months of age, with steady maturation until they reach levels of adult clearance at about 8 months of age. Foetal concentrations are lower than maternal concentrations because only the free, unbound drug is available for placental transfer. Local anesthetic are distributed to some extent to all body tissues, with higher concentrations found in highly perfused organs such as liver, heart and brain. In children the pharmacokinetics is similar to that in adults. Bupivacaine is metabolised in the liver and is excreted in the urine mainly as metabolites, with only 5 to 6% as unchanged drug.


Indications And Usage:

B-CAINE (Bupivacaine Hydrochloride Injection USP 0.5% w/v) is available in an injection form to be administered by injection via local infiltration, peripheral nerve block, or caudal and lumbar blocks by a healthcare professional. The dose, frequency and route of administration will vary, depending on the indication for use.

Dosage And Administration:

Take B-CAINE (Bupivacaine Hydrochloride Injection USP 0.5% w/v) exactly as prescribed by your doctor. Follow the directions on your prescription label carefully. The dose your doctor recommends may be based on the following:
• The condition being treated
• Other medical conditions you have
• Other medications you are taking
• How you respond to this medication
• Your weight
• Your height
• Your age
• Your gender


Bupivacaine is contraindicated in patients with known hypersensitivity reactions to Bupivacaine or amino-amide anesthetics. It is also contraindicated in obstetrical paracervical blocks and intravenous regional anaesthesia because of potential risk of tourniquet failure and systemic absorption of the drug and subsequent The 0.75% formulation is contraindicated in epidural anesthesia during labor because of the association with refractory cardiac arrest.

Over Dosage:

The dose, frequency, and route of administration will vary, depending on the indication for use.
Accidental intravascular injections of local anesthetic may cause immediate (within seconds to a few minutes) systemic toxic reactions. In the event of overdose, systemic toxicity appears later (15-60 minutes after injection) due to the slower increase in local anesthetic blood concentration.

Special Warnings And Precautions For Use:

There have been reports of cardiac arrest during the use of bupivacaine for epidural anaesthesia. or peripheral nerve blockade where resuscitative efforts have been difficult, and were required to be prolonged before the patient responded. However, in some instances resuscitation has proven impossible despite apparently adequate preparation and appropriate management.
Like all local anaesthetic drugs, bupivacaine may cause acute toxicity effects on the central nervous and cardiovascular systems if utilised for local anaesthetic procedures resulting in high blood concentrations of the drug. This is especially the case after unintentional intravascular administration or injection into highly vascular areas. Ventricular arrhythmia, ventricular fibrillation, sudden cardiovascular collapse and death have been reported in connection with high systemic concentrations of bupivacaine.
Adequate resuscitation equipment should be available whenever local or general anaesthesia is administered. The clinician responsible should take the necessary precautions to avoid intravascular injection .
Before any nerve block is attempted, intravenous access for resuscitation purposes should be established. Clinicians should have received adequate and appropriate training in the procedure to be performed and should be familiar with the diagnosis and treatment of side effects, systemic toxicity or other complications.
Major peripheral nerve blocks may require the administration of a large volume of local anaesthetic in areas of high vascularity, often close to large vessels where there is an increased risk of intravascular injection and/or systemic absorption. This may lead to high plasma concentrations.

Interaction With Other Medicinal Products And Other Forms Of Interaction :

Bupivacaine should be used with caution in patients receiving other local anesthetic or agents structurally related to amide-type local anesthetic, 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.

Pregnancy And Lactation :

There is no evidence of untoward effects in human pregnancy. In large doses there is evidence of decreased pup survival in rats and an embryological effect in rabbits if Bupivacaine is administered in pregnancy. Bupivacaine should not therefore be given in early pregnancy unless the benefits are considered to outweigh the risks.Foetal adverse effects due to local anesthetic, such as foetal bradycardia, seem to be most apparent in paracervical block anaesthesia. Such effects may be due to high concentrations of anesthetic reaching the foetus. Bupivacaine enters the mother's milk, but in such small quantities that there is no risk of affecting the child at therapeutic dose levels.

Effects On Ability To Drive And Use Machines :

In general, it is sufficient to allow 2 - 4 hours post nerve block or until full functions have returned following regional nerve block. In many situations, patients receive a sedative or other CNS depressant drug e.g., Diazepam, Midazolam to allow the block to be performed. One must allow adequate time for the effects of these drugs to clear.Depending on dosage, local anesthetic may have a very mild effect on mental function and coordination even in the absence of overt CNS toxicity and may temporarily impair locomotion and alertness.

Undesirable Effects :

Accidental sub-arachnoid injection can lead to very high spinal anaesthesia possibly with apnoea and severe hypotension.
The adverse reaction profile for Bupivacaine Hydrochloride is similar to those for other long acting local anesthetic. Adverse reactions caused by the drug per se are difficult to distinguish from the physiological effects of the nerve block (e.g., decrease in blood pressure, bradycardia), events caused directly (e.g., nerve trauma) or indirectly (e.g., epidural abscess) by needle puncture.
Neurological damage is a rare but well recognised consequence of regional and particularly epidural and spinal anaesthesia. It may be due to several causes, e.g. direct injury to the spinal cord or spinal nerves, anterior spinal artery syndrome, injection of an irritant substance, or an injection of a non-sterile solution. These may result in localised areas of paraesthesia or anaesthesia, motor weakness, loss of sphincter control and paraplegia. Occasionally these are permanent.
The adverse reactions considered at least possibly related to treatment with Bupivacaine Hydrochloride from clinical trials with related products and post-marketing experience are listed below by body system organ class and absolute frequency. Frequencies are defined as very common (1/10), common (1/100, <1/10), uncommon (1/1,000, < 1/100), rare (1/10,000, < 1/1,000), including isolated reports, or not known (identified through post-marketing safety surveillance and the frequency cannot be estimated from the available data).

Table Of Adverse Drug Reaction (ADR)

System Organ Class

Frequency Classification

Adverse Drug Reaction

Immune system disorders


Allergic reactions, anaphylactic reaction/shock

Nervous system disorders


paraesthesia, dizziness Following epidural injection of some local anaesthetic agents including bupivacaine, high sympathetic blockade may occasionally result in ocular and other symptoms similar to those seen in Horner's syndrome. These effects are encountered more com monly in pregnant women.


Signs and symptoms of CNS toxicity (convulsions, circumoral paraesthesia, numbness of the tongue, hyperacusis, visual disturbances, loss of consciousness, tremor, light headedness, tinnitus, dysarthria, muscle twitching)


Neuropathy, peripheral nerve injury, arachnoiditis, paresis and paraplegia

Eye disorders



Cardiac disorders




Cardiac arrest, cardiac arrhythmias

Vascular disorders

Very Common




Respiratory disorders


Respiratory depression



Renal and Urinary


Urinary retention

Hepatic dysfunction, with reversible increases of SGOT, SGPT, alkaline phosphatase and bilirubin, have been observed following repeated injections or long-term infusions of Bupivacaine. If signs of hepatic dysfunction are observed during treatment with Bupivacaine, the drug should be discontinued.


Store below 30°C. Protected from light. Do not allow to freeze. Keep out of reach of children.


24 Months.


B-CAINE (Bupivacaine Hydrochloride Injection USP 0.5% w/v) supplied in 10 mL glass vial.