Transtec (TRANSTEC ®)

TRADE NAME Transtec

INN Buprenorphine

CHEMICAL NAME
(2S) -2 – [17 - (cyclopropylmethyl) -4,5 a-epoxy-4-hydroxy-6-methoxy-6a ,14-ethanol-14a-morfinan-7a-yl] -3,3-dimethylbutane-2 – ol

PHARMACEUTICAL FORM
Transdermal therapeutic system

DESCRIPTION
Rectangular patch with rounded corners on the aluminized hard off the protective layer with a basis of skin color. In the center there is a reservoir – the matrix of the drug. The appearance of the matrix containing the active substance – light brown goo stamped on fabric patch.

COMPOSITION
Active ingredients:
A transdermal therapeutic system contains 20 mg buprenorphine, the rate of release of 35 mcg / hour, the area containing the active ingredient – 25 cm?. A transdermal therapeutic system contains 30 mg buprenorphine, the rate of release of 52.5 mcg / hour, the area containing the active substance-37.5 cm?. A transdermal therapeutic system contains 40 mg buprenorphine, the rate of release of 70 mcg / hour, the area containing the active ingredient – 50 cm?.
Auxiliary ingredients: adhesive matrix containing buprenorphine: [(Z)-oktadek-9-ene-1il] oleate, povidone K90, 4-oksopentanovaya acid, poly [acrylic acid-co-butyl acrylate-co-(2-ethylhexyl) acrylate] (5:15:75:5), cross-linked adhesive matrix, does not contain buprenorphine: poly [acrylic acid-co-butyl acrylate-co-(2-ethylhexyl) acrylate] (5:15:75:5), cross – associated

Pharmacotherapeutic group
Analgesic drugs: opioid receptor agonist-antagonist.
ATC code: [N02AE01] HII

Pharmacological action
It acts as an agonist-antagonist opioid receptors. A partial agonist of mu receptors and antagonist-receptor cap. Stronger on the pharmacological action of morphine in 25-50 times. To a lesser degree than morphine depresses the respiratory center. In terms of development of drug dependence with prolonged use is less dangerous than morphine.

PHARMACOKINETICS
Plasma protein binding of 96%. Metabolized in the liver. Provided through the intestines and kidneys. Penetrates the blood-brain and placental barriers. After applying the transdermal therapeutic system Buprenorphine is absorbed through the skin. The constant and stable flow of the active substance in an organism is provided by the adhesive polymer matrix system.
After applying Transtec skin buprenorphine concentration in plasma gradually increased after 12-24 hours and reaches the minimum effective level of 100 pg / ml. Cmax = 305 pg / ml (Transtec 35 ug / hour) and 624 pg / ml (Transtec 70 mcg / hour) at Tmax = 57 hours (Transtec 35 ug / hour) and 59 hours (Transtec 70 mcg / hour).
After removing the plasma concentration decreases with the half life of 30 hours.

INDICATIONS
Transtec is indicated for the treatment of medium severe and severe chronic pain when:
# Cancer
# Pain syndromes that are not cropped non-narcotic analgesics

CONTRAINDICATIONS
# Hypersensitivity,
# Drug dependency, physical,
# Inhibition of the respiratory center,
# Pregnancy and lactation,
# Age of 18 years,
# Receiving MAO inhibitors.
Be used with caution in:
# Respiratory failure
# Hepatic and / or renal failure
# Myxedema,
# Hypothyroidism
# Adrenal insufficiency,
# CNS depression,
# Craniocerebral trauma
# Toxic psychosis,
# Prostatic hyperplasia,
# Stricture of the urethra,
# Alcoholism.
Transtec should be applied with particular caution in acute alcohol intoxication, in convulsions, with a head injury, with loss of consciousness of unknown origin, with increased intracranial pressure.

APPLICATION pregnancy and lactation
Transtech Contraindicated use during pregnancy and during breastfeeding.

Dosage regimen / route of administration
Selection of the initial dose: patients not previously treated with analgesics, get 1 Transtec transdermal therapeutic system 35 mcg / hour. Patients who received non-opioid analgesics, get 1 Transtec transdermal therapeutic system 35 mcg / hour.
In the transition from opioid analgesics in the Transtec can use the following recommendations:

Evaluation of analgesic effect is carried out within 24 hours after the imposition of transdermal therapeutic system.
Transdermal therapeutic system is applied for 96 hours. In the case of poor pain relief after 96 hours is necessary to increase the dose or the imposition of a larger number of transdermal systems of this dosage, or the imposition of transdermal therapeutic system following dosing.
The method of applying transdermal therapeutic system: Transtec nevospalennuyu should stick to the skin without the hair covering (better on the upper back or chest). Maybe getting on transdermal system for water, but no soap. Transdermal system be bonded to a clean, dry skin immediately after removing the protective film and pressed for 30 seconds. It is recommended to record the date and time overlay transdermal system for carton packaging. After 96 hours remove the transdermal system and paste the following in another place. At the same place transdermal system can stick in 6 days.
Length of transdermal therapeutic system: Transtec should not be used longer than necessary. If necessary, the prolonged use of Transtech because of severity of disease, require constant medical supervision.

SIDE EFFECTS
Nausea, vomiting, sweating, dry mouth, headache, depression, agitation, anxiety, drowsiness, decreased blood pressure, shortness of breath, lethargy, depression of the respiratory center, reduced erection, slowing the rate of mental and motor reactions, skin rash.

OVERDOSAGE
Symptoms: nausea, vomiting, drowsiness, marked miosis, collapse. Treatment: To maintain the function of the respiratory and cardiovascular systems, the introduction of naloxone, adequate ventilation.

Cautions
During treatment with Transtec is not recommended to engage in activities requiring concentration of attention and quickness of psychomotor reactions.

Drug Interactions
Incompatible with MAO inhibitors. Potentiate the action of narcotic analgesics, phenothiazines, anxiolytics, sedatives, hypnotics, general anesthetics, alcohol.

PACKAGING
Standard package includes 3, 5 or 10 individually packaged therapeutic transdermal system 35 mcg / hour, 52.5 micrograms / hour or 70 mcg / hour.

SHELF LIFE 3 years.

STORAGE CONDITIONS
In the reach of children at or above 25? C. In accordance with Federal law “On Narcotic Drugs and Psychotropic Substances. The patient should be informed that the used transdermal therapeutic systems should be folded in half sticky side inwards and back doctor for destroying the established order. Unused transdermal therapeutic systems also need to return a doctor.

Holiday from drugstores
Released strictly on prescription by a special prescription form.