What is Tramadol?
Tramadol is a drug used to treat mild to moderate pain. The product ingredient is Tramadol hydrochloride (hcl).
The brand names of Tramadol in United States are: Ultram, Tramadol Hydrochloride ER, Tramal and Ultram ER.
Mechanism of action (MOA) of Tramadol
Central-acting analgesic, non-selective pure agonist of the opioid receptors µ, delta and kappa, with greater affinity for µ.
Therapeutic indications, uses and benefits of Tramadol
moderate to severe pain
Adjust dose according to pain intensity and response. Administer the time strictly required.
Adults and children >12 years
Oral, immediate release forms: initial, 50-100 mg; maintenance, 50-100 mg/6-8 h.
Oral, delayed forms administered every 12 h: 50-200 mg/12 h.
Oral, delayed forms administered every 24 h: initial, 100-200 mg/24 h; if pain is not relieved, increase dose in increments of 100 mg up to 300 mg or up to a maximum of 400 mg/day.
Oral, BID delay forms: 75 mg/12 h.
Intramuscular, Subcutaneous, Intravesono or in infusion: initial, 100 mg; in 1 to h, 50-100 mg (moderate pain) or 50 mg every 10-20 min (severe pain) without exceeding 250 mg in total; maintenance, 50-100 mg/6-8 h.
For all routes, max. 400 mg/day.
Children < 12 years
Not recommended; can only be used parenterally at a unit dose of 1-2 mg/kg.
Mode of administration of Tramadol
Solid oral forms: take whole, without dividing or chewing, with enough liquid and with or without food.
Liquid oral forms: take with a little liquid or sugar, with or without meals.
Injectable: parenteral administration: Intramuscular, subcutaneous, intravenous (slow injection, 2-3 minutes) or can be administered diluted by perfusion or by a patient-controlled analgesia device, under medical supervision, in a conveniently equipped resuscitation room.
Contraindications of Tramadol
Hypersensitivity to tramadol; acute intoxication or overdose with CNS depressants (alcohol, hypnotics, other opiate analgesics).
Concomitant with MAOI or that have been treated during the previous 2 weeks; concomitant with linezolid; severe hepatic or renal impairment; epilepsy not adequately controlled with treatment.
Severe respiratory failure; during lactation if long-term treatment (more than 2 or 3 days) is necessary; for treatment of opioid withdrawal syndrome.
Warnings and precautions with Tramadol
Over 75 years of age, moderate renal and hepatic insufficiency: prolong dosing intervals.
Caution in opioid dependents, with tendency to abuse, cranial trauma, shock, disturbance of knowledge of unknown origin, respiratory depression, intracranial hypertension, acute porphyria, biliary tract alterations, epileptics, tendency to convulsions or treated with substances that lower the convulsive threshold or metabolized by CYP3A4 or CYP2D6 or CNS depressants.
Risk of tolerance and dependence, especially in the long term can induce tolerance and physical or psychic dependence (reduce doses gradually). As tramadol is metabolized through CYP2D6, the ultra-fast metabolizers of CYP2D6 are at risk of developing opioid toxicity, even at routinely prescribed doses. In severe cases, this may include symptoms of circulatory and respiratory depression, which can be life-threatening and very rarely life-threatening.
Extreme caution should be exercised when administering to children for the relief of postoperative pain and close monitoring of symptoms of opioid toxicity, including respiratory depression.
No recommended for use in children who may have impaired respiratory function, including neuromuscular disorders, severe heart or respiratory disease, pulmonary or upper respiratory tract infections, multiple trauma or extensive surgical procedures. These factors may worsen symptoms of opioid toxicity.
Contraindicated in severe liver failure. In moderate insufficiencies, prolong dosing intervals.
Contraindicated in severe renal failure. In moderate insufficiencies, prolong dosing intervals.
- Toxicity enhanced by: central depressants, alcohol, ritonavir.
- Risk of respiratory depression from: other morphine derivatives, benzodiazepines, barbiturates.
- Decreased effect of: carbamazepine, buprenorphine, nalbufine, pentazocine.
- Risk of seizures with: SSRIs, serotonin/norepinephrine reuptake inhibitors, tricyclic antidepressants, antipsychotics, and other seizure lowering medications such as bupropion, mirtazapine, tetrahydrocannabinol.
- Increases INR and ecchymosis with: coumarinics.
- Increased requirements for: ondasetron (postoperative pain).
Pregnancy and Tramadol
Its use during pregnancy is not recommended unless it is clearly necessary. It crosses the placental barrier and regardless of dosage, chronic use may induce withdrawal symptoms in neonates.
High doses administered in the last weeks of gestation, even for short periods, may induce respiratory depression in neonates.
Animal studies have not demonstrated any teratogenic effect, but at high doses fetotoxicity appeared due to maternal toxicity.
During the lactation period, approximately 0.1% of the maternal dose is secreted into the milk.
SIt is recommended not to administer tramadol during lactation. After administration of a single dose of tramadol, it is usually not necessary to interrupt lactation. However, if repeated administration over several days, more than 2 or 3 days is necessary, lactation should be discontinued.
Breastfeeding is contraindicated if long-term treatment after birth is necessary.
Effects on driving ability
Opioid analgesics may decrease the mental and/or physical ability needed to perform potentially dangerous tasks (e.g. driving a car or using machines), especially at the onset of treatment, after an increase in dose or a change in formulation, and/or when administered in conjunction with other medications.
Patients should be advised not to drive or use machines if they feel drowsy, dizzy or visually impaired while taking tramadol, or until the ability to perform these activities is found not to be affected.
Adverse reactions and side effects of Tramadol
Dizziness, headaches, confusion, drowsiness, nausea, vomiting, constipation, dry mouth, sweating, fatigue.
In case of respiratory depression use naloxone as an antidote.
⭐⭐⭐⭐⭐ VIDEO OF TRAMADOL/ULTRAM (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
PubChem CID: 33741
NCI Thesaurus: C29507