Tapain

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Tapain uses

Tapain consists of Diclofenac Sodium, Lidocaine Hydrochloride.

Diclofenac Sodium:


Pharmacological action

NSAIDs, a derivative of phenylacetic acid, Tapain has a pronounced anti-inflammatory, analgesic and mild antipyretic effect. The mechanism of action is associated with inhibition of COX activity - the main enzyme metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. Analgesic effect is due to two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system).

Inhibits synthesis of proteoglycan in cartilage.

In rheumatic diseases, Tapain (Diclofenac Sodium) reduces joint pain at rest and in motion, as well as morning stiffness and swelling of the joints, helps to increase range of motion; reduces post-traumatic and postoperative pain, and inflammatory edema.

Inhibits platelet aggregation. With prolonged use has a desensitizing effect.

When used topically in ophthalmology reduces swelling and pain in inflammatory processes non-infectious etiology.

Pharmacokinetics

After intake is absorbed from the gastrointestinal tract. Eating slows down the rate of absorption, extent of absorption is not changed. About 50% of the active substance is metabolized in the "first passage" through the liver. When used rectally absorption is slower. Time to reach Cmax in plasma after oral administration is 2-4 hours depending on the used dosage form, after rectal - 1 h, I.M. administration - 20 min. The concentration of active substance in plasma is a linear function of the applied dose.

Not cumulative. Plasma protein binding is 99.7% (predominantly albumin). Penetrates into synovial fluid, Cmax is achieved in 2-4 hours later than in plasma.

To a large extent metabolized to form several metabolites, among which two pharmacologically active, but to a lesser extent than Tapain (Diclofenac Sodium).

Systemic clearance of the active substance is about 263 ml / min. T1/2 from plasma is 1-2 h, from synovial fluid - 3-6 h. Approximately 60% of the dose was excreted as metabolites by the kidneys, less than 1% excreted in the urine as unchanged, while the rest is displayed in the form of metabolites with bile.

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Why is Tapain prescribed?

Articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), degenerative and chronic inflammatory diseases of musculoskeletal system (osteochondrosis, osteoarthritis, periartropatii), post-traumatic inflammation of soft tissue and musculoskeletal system (sprains, bruises). Pain in the spine, neuralgia, myalgia, arthralgia, pain and inflammation after surgery or injury, pain in gout, migraine, algomenorrhea, pain with Bursitis, proctitis, colic (biliary and renal), pain in infectious and inflammatory diseases of ENT organs.

For local use: the inhibition of miosis during surgery for cataract prevention of cystoid macular edema associated with removal and lens implantation, inflammatory eye non-infectious nature, post-traumatic inflammation in penetrating and nonpenetrating wound of the eyeball.

Dosage and administration

For oral use for adult single dose is 25-50 mg 2-3 times / 24 h. Frequency of admission depends on the dosage form employed, the severity of the disease and is 1-3 times / 24 h, rectally - 1 times / 24 h, for the treatment of acute conditions or the exacerbation of chronic edema use intramuscular in dose of 75 mg.

For children older than 6 years and adolescents daily dose is 2 mg / kg.

Topical applied at a dose of 2-4 g on the affected area 3-4 times / 24 h.

When used in ophthalmology frequency and duration of administration are determined individually.

The maximum oral daily dose for adults is 150 mg.

Tapain (Diclofenac Sodium) side effects

Digestive system: nausea, vomiting, anorexia, abdominal pain and discomfort in the epigastrium, flatulence, constipation, diarrhea, and in some cases - erosive-ulcerative lesions, gastrointestinal bleeding and perforation; rarely - abnormal liver function. When rectal administration - in isolated cases were observed inflammation of the colon bleeding, exacerbation of ulcerative colitis.

From the side of the central nervous system and peripheral nervous system: dizziness, headache, agitation, insomnia, irritability, fatigue, rarely - paresthesia, visual disturbances (blurred, double vision), tinnitus, insomnia, cramps, irritability, tremors, mental disorders, depression.

Hemopoietic system: rarely - anemia, leukopenia, thrombocytopenia, agranulocytosis.

Urinary system: rarely - renal failure; in predisposed patients may be swelling.

Dermatological reactions: rarely - hair loss.

Allergic reactions: skin rash, itching, when used in the form of eye drops - itching, redness, photosensitivity.

Local reactions: in the place of I.M. introducing possible burning, in some cases - the formation of infiltration, abscess, necrosis of adipose tissue in the rectal administration may be local irritation, the appearance of mucous discharge mixed with blood, painful defecation, when used externally, in rare cases - itching, redness, rash, burning sensation, when applied topically in ophthalmology may be a transient burning sensation and / or temporary blurred vision immediately after instillation.

With long-term topical use and / or drawing on a vast surface of body are possible systemic side effects due to resorptive action of Tapain (Diclofenac Sodium).

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Contraindications

known hypersensitivity to Tapain sodium or to any accessory ingredient that is part of the drug Tapain (Diclofenac Sodium);

anamnestic information about the attacks of bronchial asthma, urticaria, acute rhinitis associated with the use of aspirin or other NSAIDs;

hemodyscrasia unknown origin;

children under 6 years

pregnancy (III trimester);

lactation

increased sensitivity to sulfite (for injection solution).

children under age 15 - tablets of 50 mg to 18 years - injection.

Using during pregnancy and breastfeeding

Use during pregnancy and lactation is possible in cases where the potential benefits for the mother exceeds than the potential risk to the fetus or newborn.

Special instructions

With extreme caution is used in diseases of liver, kidney, gastrointestinal history, dyspepsia, asthma, hypertension, heart failure, after major surgery, as well as elderly patients.

When referring to a history of allergic reactions to NSAIDs Tapain and sulfites are used only in urgent cases. In the course of treatment requires systematic monitoring of liver function and kidney picture of peripheral blood.

Do not recommended the use for rectal patients with diseases of anorectal region or anorectal bleeding in history. Topical should be applied only to intact skin areas.

Avoid contact with Tapain (Diclofenac Sodium) in the eye (except for eye drops), or on mucous membranes. Patients who use contact lenses, eye drops should be applied no earlier than 5 minutes after removing the lenses.

Not recommended for children under 6 years.

During the period of treatment drugs for systemic use is not recommended alcohol consumption.

During the period of treatment may decrease the speed of psychomotor reactions. With worsening blurred vision after application of eye drops should not be driving and doing other potentially danger activities.

Tapain (Diclofenac Sodium) drug interactions

At simultaneous application with Tapain (Diclofenac Sodium) antihypertensive drugs may be weakening their actions.

There are few reports on the occurrence of seizures in patients taking both NSAIDs and antibacterial drugs quinolic series.

At simultaneous application with GCS and increased risk of side effects from the digestive system.

With simultaneous use of diuretics may decrease diuretic effect. With the simultaneous use of potassium-sparing diuretics may increase the concentration of potassium in the blood.

With simultaneous use with other NSAIDs may increase the risk of side effects.

There are reports of hypoglycemia or hyperglycemia in patients with diabetes who engaged in Tapain (Diclofenac Sodium) together with hypoglycemic drugs.

When applied simultaneously with acetylsalicylic acid may decrease the concentration of Tapain (Diclofenac Sodium) in plasma.

Although clinical studies have not found the influence of Tapain (Diclofenac Sodium) on the action of anticoagulants, describes the individual cases of bleeding when used with Tapain (Diclofenac Sodium) and warfarin.

With simultaneous use may increase digoxin, lithium, and phenytoin in blood plasma.

The absorption of Tapain (Diclofenac Sodium) from the gastrointestinal tract is reduced by simultaneous application with kolestiraminom, to a lesser extent - with colestipol.

With simultaneous use may increase the concentration of methotrexate in plasma and increased its toxicity.

With simultaneous application of Tapain (Diclofenac Sodium) could not affect the bioavailability of morphine, but the concentration of the active metabolite of morphine may be enhanced in the presence of Tapain (Diclofenac Sodium), which increases the risk of side effects metabolites of morphine, including respiratory depression.

When applied simultaneously with pentazocine described a case of great convulsions, and rifampicin - may decrease the concentration of Tapain (Diclofenac Sodium) in plasma, with ceftriaxone - increases excretion of ceftriaxone in bile; with cyclosporine - may increase cyclosporine nephrotoxicity.

Tapain in case of emergency / overdose

Symptoms: may cause hypotension, renal failure, convulsions, gastrointestinal irritation or respiratory depression. Treatment: There is no specific antidote. In acute poisoning as soon as possible to stop drug absorption from the gastrointestinal tract. There is indicated gastric lavage, activated charcoal appointment and conduct of other symptomatic and supportive therapy. The use of forced diuresis, dialysis or blood transfusion is not justified because NSAIDs largely associated with serum proteins and possess extensive metabolism.

Storage conditions

In a dry, protected from light place, at temperature not above 25°C.Common expiration date for Tapain (Diclofenac Sodium) tablets: 3 years.

Lidocaine Hydrochloride:


Pharmacological action

Tapain is an antiarrhythmic agent of class IB, local anesthetic, a derivative of acetanilide. This medication has membrane stabilizing activity. Tapain (Lidocaine Hydrochloride) 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, Tapain (Lidocaine Hydrochloride) 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.

Tapain (Lidocaine Hydrochloride) causes all kinds of local anesthesia: a terminal, infiltration and wires.

Pharmacokinetics

After IM administration absorption of Tapain (Lidocaine Hydrochloride) is almost complete. The distribution is rapid, Vd is about 1 L/kg (in patients with heart failure it is below). The protein binding depends on the concentration of the active substance in the plasma and is 60-80%. Tapain (Lidocaine Hydrochloride) 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). Tapain (Lidocaine Hydrochloride) excreted by the kidneys as metabolites, 10% unchanged.

Why is Tapain prescribed?

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.

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Dosage and administration

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 Tapain 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 (usually following the introduction of a loading dose) - 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.

Tapain (Lidocaine Hydrochloride) side effects, adverse reactions

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.

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Tapain contraindications

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 (except in cases when the probe was introduced to stimulate the ventricles), severe liver function abnormalities.

For subarachnoid anesthesia - complete heart block, bleeding, hypotension, shock, infection of the venue lumbar puncture, septicemia.

Increased sensitivity to Tapain (Lidocaine Hydrochloride) and other amide type local anesthetics.

Using during pregnancy and breastfeeding

During pregnancy and lactation be used only for health reasons. Tapain 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.

Special instructions

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.

Tapain drug interactions

Beta-blockers increase the risk of bradycardia and hypotension. Norepinephrine and beta-blockers by reducing hepatic blood flow decrease (increased toxicity), isadrine and glucagon - increase the clearance of Tapain (Lidocaine Hydrochloride). Cimetidine increases the plasma concentration of Tapain (Lidocaine Hydrochloride) (displaces from its association with proteins and slows inactivation in the liver). Barbiturates causing induction of microsomal enzymes stimulate the degradation of Tapain (Lidocaine Hydrochloride) 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 Tapain (Lidocaine Hydrochloride). Antiarrhythmics (amiodarone, verapamil, quinidine, aymalin) potentiate cardiac depression. Combination with novocainamide may cause CNS excitement and hallucinations. Tapain (Lidocaine Hydrochloride) 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.

Tapain in case of emergency / overdose

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.

Tapain pharmaceutical active ingredients containing related brand and generic drugs:

Active ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.


Tapain available forms, composition, doses:

Form of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.


Tapain destination | category:

Destination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.


Tapain Anatomical Therapeutic Chemical codes:

A medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.


Tapain pharmaceutical companies:

Pharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.


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References

  1. Dailymed."DICLOFENAC SODIUM TABLET, DELAYED RELEASE [LAKE ERIE MEDICAL DBA QUALITY CARE PRODUCTS LLC]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
  2. Dailymed."PHARMAPURERX LIDOCAINE HCL 4.12% (LIDOCAINE HYDROCHLORIDE) CREAM [PURETEK CORPORATION]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
  3. Dailymed."LIDOCAINE; TETRACAINE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).

Frequently asked Questions

Can i drive or operate heavy machine after consuming Tapain?

Depending on the reaction of the Tapain after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Tapain 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 Tapain 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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Review

sdrugs.com conducted a study on Tapain, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Tapain consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.

Visitor reports

Visitor reported useful

No survey data has been collected yet

Visitor reported side effects

No survey data has been collected yet

One visitor reported price estimates

What is your opinion about drug cost? Did you feel the cost is apt, or did you feel it is expensive?
The report given by the sdrugs.com website users shows the following figures about several people who felt the medicine Tapain is expensive, and the medicine is not expensive. The results are mixed. The perception of the cost of the medicine to be expensive or not depends on the brand name of the medicine, country, and place where it is sold, and the affordability of the patient. You can choose a generic drug in the place of the branded drug to save the cost. The efficiency of the medicine will not vary if it is generic or a branded one.
Visitors%
Not expensive1
100.0%

One visitor reported frequency of use

How often in a day do you take the medicine?
Are you taking the Tapain drug as prescribed by the doctor?

Few medications can be taken 3 times in a day more than prescribed when the doctor's advice mentions the medicine can be taken according to frequency or severity of symptoms. Most times, be very careful and clear about the number of times you are taking the medication. The report of sdrugs.com website users about the frequency of taking the drug Tapain is mentioned below.
Visitors%
3 times in a day1
100.0%

Visitor reported doses

No survey data has been collected yet

Visitor reported time for results

No survey data has been collected yet

One visitor reported administration

The drugs are administered in various routes, like oral or injection form. They are administered before food or after food. How are you taking Tapain drug, before food or after food?
Click here to find out how other users of our website are taking it. For any doubts or queries on how and when the medicine is administered, contact your health care provider immediately.
Visitors%
After food1
100.0%

Two visitors reported age

Visitors%
> 601
50.0%
30-451
50.0%

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The information was verified by Dr. Rachana Salvi, MD Pharmacology

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