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Drug form:
drops for the reception inside, capsules, capsule-acting,
injection, the solution for the reception inside, rektalnye
suppositories, tablets, coated tablets, pills-acting, tablet
prolonged action
Pharmacological Effects:
Anodyne synthetic analgesic, with the central and Action Action
on the spinal cord (contributes to the opening of K + and Ca2 +
- channels, cerebrovascular causes membrane and inhibits pain
impulses holding), reinforces the effect of sedative drugs.
Activates Opiate receptors (mu-, delta-,-kappa) for the pre -
and postsynaptical membrane system notsitseptivnoy afferent
fibers in the brain and the alimentary canal. Slowing the
destruction of catecholamines, stabilize their concentrations in
the central nervous system. It is a mixture of 2 ratsemicheskuyu
enantiomers - pravovraschayuschih (+) and levovraschayuschih
(-), each of which was different from others ENART affinity. (+)
Tramadol is a selective agonist mu-opioid receptors, as well as
selectively inhibits reverse neyronalny seizure of serotonin.
(-) Tramadol inhibits reverse neyronalny hostage noradrenaline.
Mono-O-dezmetiltramadol (M1 metabolite) also selectively
stimulates Mu-Opiate receptors. Tramadol affinity for opioid
receptors is 10 times weaker than that of codeine, and in 6000
times weaker than that of morphine. Evidence analgeziruyuschego
actions 5-10 times weaker than morphine. Analgesic effect due to
declining activity and the increase notsitseptivnoy
antinotsitseptivnoy systems. In therapeutic doses does not
affect meaningfully on hemodynamics and respiration, does not
alter the pressure in the pulmonary artery, slightly slowing
peristalsis of the bowel, while not causing constipation. Has
some protivokashlevoe and sedative effect. Inhibits the
respiratory center, excites a trigger zone vomitoxin center, the
nucleus oculomotor nerve. In long application may develop
tolerance. Analgesic action develops over 15-30 min after
administration of inwards and lasts until 6 pm
Indications:
Pain Syndrome (severe and moderate intensity, including
inflammation, trauma, vascular origin). Anaesthesia during
painful diagnostic or therapeutic interventions.
Contraindications:
Hypersensitivity state, accompanied by oppression or respiratory
expressed oppression CNS (alcohol poisoning, hypnotics drugs,
narcotic analgesics and other psychoactive drugs), pregnancy,
lactation period (in the case of a lengthy application), a
children's age (up to 1 year - for parenteral introduction;
before 14 years - to receive oral), receiving MAO inhibitors,
severe hepatic and / or renal failure (SEF less than 10 ml /
min). C caution. Drug abuse, confusion, intracranial
hypertension, head trauma, epileptic syndrome (cerebral
genesis), in patients against a backdrop of a more uncertain in
the abdomen genesis.
Adverse actions:
So part of the nervous system: increased sweating, dizziness,
headache, weakness, increased fatigue, slow, paradoxical CNS
stimulation (nervousness, agitation, anxiety, tremor, muscle
cramps, euphoria, emotional lability, hallucinations),
drowsiness, disruption of sleep, confusion , in coordination of
movements, convulsions central genesis (with the / in the
introduction or in high doses, while the appointment of
antipsychotic drugs (neuroleptics), depression, amnesia, the
violation of cognitive function, paresthesia, volatility gait.
on the part of the digestive system: dry mouth, nausea ,
vomiting, flatulence, stomach ache, diarrhea or constipation,
difficulty in swallowing. on the part of the SSA: vasodilation
manifestations - tachycardia, tilt hypotension, syncope,
collapse. Allergicheskie reaction: rash, itching, Exanthema,
bulleznaya rash. hand So urinary system: difficulty urinating,
dysuria, the delay of urine. hand So senses: violation of view,
the taste. on the part of the respiratory system: pectoris.
Miscellaneous: violation of the menstrual cycle. With long-term
use - to medication. sharply When lifting - syndrome "lifting".
Overdose. Symptoms : miosis, vomiting, collapse, coma,
convulsions, respiratory depression centre apnea. Treatment:
ensuring patency respiratory tract, respiratory maintenance and
operation of the SOFA. Opiatopodobnye effects can be kupirovany
naloxone, convulsions - benzodiazepine.
Dosing and dose:
W / in, in / m, p / k, inside, rectally. Inside: a single
application for adults and children over 14 years - to 0.05 g
(tablets, capsules) with a small amount of liquid or 20 cps
solution (or drops) for the reception inside a small amount of
liquid or sugar. After a 30-60 min can be repeated reception at
the same dose, but no more than 8 doses per day. Tablets retard
- 100-200 mg every 12 hours Daily dose - 0.4 g (in exceptional
cases, such as cancer patients may decline to 6 h interval and
increased daily intake). Rectal - 0.1 g. Multiplicity reception
- up to 4 times a day. W / in slowly, and / or to / m: 0.05-0.1
g. If the effect is insufficient, then after 20-30 min after the
/ in the introduction could go infusion at a speed 12 mg / h or
appoint an additional inside. Total daily intake - 0.4 g.
Children over the age of 1 year - into just a drop or
parenterally (w / w in / m, p / k), in a dose of 1-2 mg / kg.
Daily dose - 4-8 mg / kg (1 cps - 2.5 mg). Persons older people
and patients with renal insufficiency requires individual dosage
(possibly lengthening T1 / 2). At least 30 spacecraft ml / min
and in patients with hepatic insufficiency requires 12 hour
interval between admission regular doses of medication.
Cautions:
Do not apply to therapy syndrome "lifting" of drugs. You should
not use ethanol at the same time. As if a reception there was no
need to interrupt breast-feeding. During the period of treatment
must be careful when driving vehicles and taking other
potentially dangerous activities that require high concentration
and psychomotor speed reactions.
Interaction:
Pharmaceutical solutions incompatible with diclofenac,
indometacin, fenilbutazona, diazepam, flunitrazepama,
nitroglycerin. Effects Enhances LS, depressing the central
nervous system, and ethanol. Inductors mikrosomalnogo oxidation
(including carbamazepine, barbiturates) reduces
analgeziruyuschego pronounced effect and duration of action.
Long-term use of opioid analgesics or barbiturates encourages
the development of cross-tolerance. Generalized increase
expressivity analgeziruyuschego effect, the duration of
anesthesia increases in combination with barbiturates. Naloxone
activates breathing, eliminating analgesia after applying opioid
analgesics. MAO inhibitors, furazolidon, procarbazine,
antipsychotic drugs (Diuretics) increases the risk of
convulsions (reduction Seizure threshold). Quinidine tramadol
increases the plasma concentration and reduces M1 metabolite
through competitive inhibition of CYP2D6 isoenzyme.
Proprietary preparations
Grünenthal, which still owns the patent to tramadol, has
cross-licensed the agent to pharmaceutical companies
internationally. Thus, tramadol is marketed under many trade
names around the world, including:
Adolan
Adolonta
Anadol
Boldol
Calmador
Contramal
Crispin
Dolol
Dromadol
Ixprim
Lumidol
Mandolgin
Mandolgine
Mosepan
Nobligan
Poltram
Ralivia
Sintradon
Siverol
Tiparol
Toplagic
Tradol
Tradolan
Tradonal
Tralgit
Tralodie
Tramacet
Tramacip
Tramake Insts
Tramadin
Tramadolor
Tramal
Tramalgic
Tramahexal
Tramacet
Tramazac
Trama-Klosidol
Tramedo
Trodon
Ultracet
Ultram and Ultram ER
Veldrol
Zaldiar - combined with paracetamol
Zaledor
Zamadol
Zamudol
Zydol
Zytram
Zytrim
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