tramadol capsules general information

Clinical and pharmacological classification / ATC code
- ATC code: N02AX02 opioids / other opioids / tramadol

Mechanism of Action
Opioid analgesics mimic the effect of endogenous opioid peptides (endorphins, enkephalins, dynorphins) after. On the one hand, the transmission of pain impulses is inhibited and the other changed the perception of pain in the thalamus and the limbic system.
Tramadol has opioiderge effect and also inhibits the norepinephrine uptake and release of serotonin.
The analgesic potency of tramadol is about one tenth that of morphine. The effect can also be improved by increasing the dose does not.

Trade name
Austria Adamon long retard, retard Contramal, Cromatodol, Noax uno, Tradolan, Tramabene, tramadol, tramadol hydrochloride "1 A Pharma," tramadol hydrochloride "Actavis" Tramadolor, Tramal, Tramal retard Tramastad, Tramundal


Types of applications
non-invasive:
- Oral (capsules, tablets, drops)
- Suppositories

invasive:
- Vials and solutions

Indications
- Moderate to severe pain
- Medium and, unlike acute and chronic pain pethidine
- For painful diagnostic and therapeutic procedures
- Post-operative and post-traumatic pain
- In oncology phase II of the WHO recommendations

Contraindications
absolute:
known hypersensitivity to active or excipient
central respiratory depression, significant obstruction of the airways
Coadministration with MAO inhibitors, lactation

relative:
severe impairment of liver function, circulatory shock, traumatic brain injury and increased intracranial pressure, acute abdomen, prostatic hypertrophy, myasthenia gravis, impaired renal function the dose should be reduced in pregnancy



Dosage
Standard dosage

Dosage must be individualized, as with all centrally acting analgesics.

Adults:
Single dose:
Oral: 50-100 mg
20-40 drops
Supp: 100 mg
sustained-release tablets: initially 50 mg 12-hourly
up to 100 mg 8-hourly
Dose interval: 4-6h
maximum daily dose: 400 mg (= 8 x 20 drops)

Children:
Mg/kg/4h 0.5 to 1.5; retard: 0.5-2mg / kg/8h

S.C. and i.m.:
Single dose: 50-100 mg maximum daily dose of 400 mg

i.v.:
Single dose: 50-100 mg (10 mg diluted in slow careful titration)

for continuous infusion: initially 1.5 mg / kg / slow up-titration period, followed in order to maintain approximately 15 mg / h


Side effects
General: allergic reactions of any kind (rare), sweating, dizziness
CNS: sedation up to the anesthesia, euphoria (especially during rapid influx), miosis
Cardiovascular: hypotension, orthostasis
Respiratory: respiratory depression (especially during rapid influx), cough attenuation
Stomach: central bed. Nausea and vomiting, due to contraction of smooth muscle leads to constipation
Liver and pancreas and gall bladder contraction of inputs
Kidney and bladder: Ureterkontraktion, inhibition of Miktionsreflexes
Skin: itching, skin redness

Interactions
all drugs with action on the CNS: CNS dysfunction is reinforced
high serum progesterone concentration: analgesic. Effect increases
Naloxonempfindlichkeit: at long-term opiate medication increases
MAO inhibitors: central dysfunction
Warfarin: possible potentiation of warfarin
Tricycl. Antidepressants: a central serotonin activity increases
SSRIs: central serotonin activity increases

Precautions
No indications:
- Acute and chronic mild to moderate pain with entzündl. Component
- Pain, which respond to weaker painkillers
- Perioperative Analgesieführung

Colic (gall bladder, kidney ,....) can be effectively treated with opiates, the underlying cause (spasm) give, however. Therefore, opiates for the treatment of colic in connection with an antispasmodic apply.
The road to drive is restricted as with all centrally acting analgesics.

Pharmacokinetics

Absorption: p.o. to about 65% to about rectal. 78% bioavailable
First-pass effect is relatively small.
Protein binding: 4%
maximum plasma concentration after 2h
β-terminal half-life: parent compound 6h,
analgesic and antitussive active metabolite M1 approximately 9h
Elimination: Renal


General assessment
In inflammatory pain, a combination with NSAIDs or metamizol is useful.
Increasing the dose above 400 mg / day to avoid. A switch to a potent opioid is to be preferred.