DRUGS & SUPPLEMENTS
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Xepacaine is an antiarrhythmic agent of class IB, local anesthetic, a derivative of acetanilide. This medication has membrane stabilizing activity. Xepacaine causes a blockade of sodium channels of excitable membranes of neurons and the membrane of cardiomyocytes.
This drug reduces the duration of the action potential and effective refractory period in Purkinje fibers, inhibits their automaticity. In this case, Xepacaine inhibits electrical activity in depolarized, arrhythmogenic sites, but minimally affects the electrical activity of normal tissues. When used in the medium therapeutic doses virtually no effect on myocardial contractility and slows AV-conduction. When applied as an antiarrhythmic agent in IV injection it begin to act in 45-90 seconds, the duration of action is 10-20 minutes; for IM administration the onset of action is in 5-15 minutes, the duration - 60-90 minutes.
Xepacaine causes all kinds of local anesthesia: a terminal, infiltration and wires.
After IM administration absorption of Xepacaine is almost complete. The distribution is rapid, Vd is about 1 L/kg. The protein binding depends on the concentration of the active substance in the plasma and is 60-80%. Xepacaine metabolized mainly in the liver with the formation of active metabolites, that may contribute to the manifestation of the therapeutic and toxic effects, especially after the infusion for 24 hours or more.
T1/2 tends to be two phases with the phase distribution of 9.7 min. In general T1/2 depends on the dose is 1-2 hours and can grow up to 3 hours or more during prolonged intravenous infusion (over 24 h). Xepacaine excreted by the kidneys as metabolites, 10% unchanged.
In cardiological practice: treatment and prevention of ventricular arrhythmias (extrasystoles, tachycardia, atrial flutter, atrial fibrillation), including in acute myocardial infarction, implantation of artificial pacemaker in the glycoside intoxication, narcosis.
Anaesthesia: terminal, infiltration, conduction, spinal (epidural) anesthesia in surgery, obstetrics and gynecology, urology, ophthalmology, dentistry, otolaryngology, blockade of peripheral nerves and ganglion.
As an anti-arrhythmic medicine for adult with the introduction of a loading dose by IV - 1-2 mg / kg over 3-4 minutes; the average single dose is 80 mg. Then immediately transferred to drip infusion at a rate of 20-55 mg / kg / min. Drip infusion can be carried out within 24-36 hours. If necessary, against the background of drop infusions can repeat IV jet injection of Xepacaine 40 mg after 10 minutes after the first loading dose.
IM is introduced to 2-4 mg / kg, if necessary, repeated administration is possible through 60-90 minutes.
For children with IV injection loading dose - 1 mg / kg, if necessary, it may be repeated administration in 5 min.
For continuous intravenous infusion - 20-30 mg / kg / min.
For use in surgical and obstetric practice, dentistry, ENT practice, dosing regimen set individually, depending on the evidence, the clinical situation and used the dosage form.
Maximum dose: for adults for IV injections the loading dose is 100 mg, in a subsequent drop infusion it is 2 mg / min; when IM administration - 300 mg (about 4.5 mg / kg) for 1 h.
For children in case of reintroduction the loading dose every 5 minutes, the total dose is 3 mg / kg; by continuous intravenous infusion (usually following the introduction of a loading dose) - 50 mg / kg / min.
CNS and peripheral nervous system: dizziness, headache, weakness, motor restlessness, nystagmus, loss of consciousness, drowsiness, visual and auditory disturbances, tremor, trismus, seizures (risk of their development against the backdrop of increasing hypercapnia and acidosis), a syndrome of "cauda equina" (paralysis of the legs, paresthesia), paralysis of respiratory muscles, respiratory arrest, a block of motor and sensitive, respiratory paralysis (usually develops in the subarachnoid anesthesia), numb tongue (when used in dentistry).
Cardiovascular system: increased or decreased blood pressure, tachycardia if used with a vasoconstrictor, peripheral vasodilatation, collapse, chest pain.
Digestive system: nausea, vomiting, involuntary defecation.
Allergic reactions: skin rash, hives (on skin and mucous membranes), itching, angioedema, anaphylactic shock.
Local reactions: during spinal anesthesia - a pain in the back, with an epidural anesthesia - a random hit in the subarachnoid space, when applied topically in urology - urethritis.
Other: incontinent, methemoglobinemia, persistent anesthesia, decreased libido and / or potency, respiratory depression, until the stop, hypothermia; during anesthesia in dentistry: numbness and paresthesia of the lips and tongue, the lengthening of anesthesia.
Severe bleeding, shock, hypotension, infection of the proposed injection site, marked bradycardia, cardiogenic shock, severe forms of chronic heart failure, SSS in elderly patients, AV-block II and III degree, severe liver function abnormalities.
For subarachnoid anesthesia - complete heart block, bleeding, hypotension, shock, infection of the venue lumbar puncture, septicemia.
Increased sensitivity to Xepacaine and other amide type local anesthetics.
During pregnancy and lactation be used only for health reasons. Xepacaine is excreted in breast milk.
In obstetric practice used with caution in paracervical for violations of fetal development, placental insufficiency, prematurity, postmaturity, gestosis.
Category effects on the fetus by FDA - B.
Use with caution in liver disease and kidney failure, hypovolemia, severe heart failure, in violation of the contractility of genetic susceptibility to malignant hyperthermia. In children, debilitated patients, elderly patients are required in dosage adjustment in accordance with the age and physical status. When injected into vascularized tissue it is recommended an aspiration test.
Beta-blockers increase the risk of bradycardia and hypotension. Norepinephrine and beta-blockers by reducing hepatic blood flow decrease, isadrine and glucagon - increase the clearance of Xepacaine. Cimetidine increases the plasma concentration of Xepacaine (displaces from its association with proteins and slows inactivation in the liver). Barbiturates causing induction of microsomal enzymes stimulate the degradation of Xepacaine and reduce its activity. Anticonvulsants (hydantoin derivatives) accelerate the biotransformation in the liver (decreased concentration in the blood), for IV injections it may increases cardiodepressive action of Xepacaine. Antiarrhythmics (amiodarone, verapamil, quinidine, aymalin) potentiate cardiac depression. Combination with novocainamide may cause CNS excitement and hallucinations. Xepacaine strengthens the inhibitory effect of anesthesia (hexobarbital, thiopental sodium), hypnotics and sedatives on the respiratory center, weakens the cardiac effects of digitoxin, enhances muscle relaxation caused by drugs curare like (possible paralysis of respiratory muscles). MAO inhibitors prolong local anesthesia.
Symptoms: psychomotor agitation, dizziness, weakness, decreased blood pressure, tremors, tonic-clonic convulsions, coma, collapse, possible AV blockade, CNS depression, respiratory arrest.
Treatment: discontinuation, pulmonary ventilation, oxygen therapy, anticonvulsants, vasoconstrictors (norepinephrine, mezaton), when bradycardia - anticholinergics (atropine). It is possible to carry out intubation, mechanical ventilation, resuscitation. Dialysis is ineffective.
Depending on the reaction of the Xepacaine after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Xepacaine not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.Is Xepacaine addictive or habit forming?
Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.
Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.
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The information was verified by Dr. Rachana Salvi, MD Pharmacology