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Pharmacology · Drugs and Prescriptions

Tramadol

*Tramadol*

Tramadol is an analgesic with a mixed mechanism of action, belonging to the group of agents affecting the central nervous system. The drug combines opioid and non-opioid effects, providing effective pain relief for moderate to severe pain syndromes.

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Mechanism of actionOpioid receptor agonist and norepinephrine/serotonin reuptake inhibitor.
Dosage formsCapsules, tablets, oral drops, injection ampoules, suppositories.
Routes of administrationOral, parenteral (IV, IM, SC), and rectal.
Safety profileLow abuse potential, minimal respiratory depression, and minimal impact on gastrointestinal motility.
How to write a prescription
Rp.: Caps. Tramadoli 0,05
D.t.d. N 20
S. Внутрь по 1-2 капсулы при болях, не более 8 капсул в сутки

Alternative prescriptions: Capsulas Tramadoli 0,05; Tab. Tramadoli 0,05; Sol. Tramadoli 5% - 2 ml

Dosage form
Caps. 0.05 g; tab. 0.05 and 0.1 g; oral solution drops 0.1 g; amp. soln. 5% 1 and 2 ml; suppositories 0.1 g
Administration
Oral 0.05–0.1 g (Max daily dose 0.4 g); IV, IM, SC 0.05–0.1 g (Max daily dose 0.4 g); rectal 0.1 g (Max daily dose 0.4 g)
Group
Agents affecting the central nervous system
3 min readFor medical studentsUpdated 09/24/2026
Material prepared by WhiteCoat Pro editorial team based on platform study guidesReviewed by medical editor: Aulov A. A., general practitioner · 09/24/2026

Mechanism of action

The pharmacodynamics of Tramadol are unique and comprise two components:

  1. Opioid component: acts as a central non-selective agonist of $\mu$-, $\delta$-, and $\kappa$-opioid receptors.
  2. Non-opioid (monoaminergic) component: inhibits the neuronal reuptake of norepinephrine and serotonin, which enhances descending inhibitory pathways on pain impulse transmission in the spinal cord.

Pharmacological effects

The drug exhibits pronounced analgesic activity, although it is weaker than morphine. Its key advantage over classical opioids lies in its improved safety profile: Tramadol causes virtually no respiratory depression, does not decrease gastrointestinal motility (lower risk of constipation), and does not increase urinary tract tone.

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Indications

Used for the management of pain of various etiologies:

  • Postoperative pain.
  • Pain in malignancies.
  • Pain associated with myocardial infarction.
  • Traumatic injuries.

Prescription details

The drug is available in a wide range of dosage forms: capsules (0.05 g), tablets (0.05 and 0.1 g), drops (0.1 g), 5% ampoules (1 and 2 ml), and suppositories (0.1 g).

Dosing regimen:

  • Oral: 0.05–0.1 g (Max daily dose 0.4 g).
  • Parenteral (IV, IM, SC): 0.05–0.1 g (Max daily dose 0.4 g).
  • Rectal: 0.1 g (Max daily dose 0.4 g).

Briefly: answers to topical questions

What effects does tramadol have on the central nervous system?

Tramadol exerts an analgesic effect on the central nervous system via a dual mechanism.

  • Opioid component — acts as a central non-selective agonist of $\mu$-, $\delta$-, and $\kappa$-receptors.
  • Non-opioid component — acts as a selective serotonin reuptake inhibitor and inhibits neuronal norepinephrine reuptake, enhancing descending inhibitory influences on pain transmission in the spinal cord.

In overdose, the drug causes altered mental status, seizures, agitation, and respiratory depression, and may also precipitate serotonin syndrome due to excessive serotonergic activity in the CNS.

What side effects does tramadol cause?

Tramadol causes several adverse reactions involving the gastrointestinal tract and central nervous system. The main side effects of the drug include:

  • Common reactions — nausea, constipation, sleep disturbances, and dizziness.
  • Severe risks — venous thromboembolism, hip fractures, and increased mortality (compared to NSAIDs).
  • Specific complications — development of serotonin syndrome and the risk of developing tolerance and drug dependence with long-term use.

What are the contraindications to tramadol?

Sources indicate that tramadol is contraindicated in children under 14 years of age. For gonarthrosis, the drug is prescribed to patients aged 18 years and older.

How to memorize

Tramadol is a "double strike": opioid receptor + monoamines (serotonin/norepinephrine).

Class and exam questions

Why is tramadol considered safer than morphine?

It has a significantly lower abuse potential, causes virtually no respiratory depression, and does not induce severe constipation because it does not affect GI motility as strongly as classical opioids.

What is the non-opioid component of tramadol's action?

It blocks the reuptake of serotonin and norepinephrine, enhancing descending inhibitory pathways that suppress pain transmission in the spinal cord.

What is the maximum daily dose (MDD) of tramadol for various routes of administration?

Regardless of the route of administration (oral, parenteral, or rectal), the maximum daily dose is 0.4 g.

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What else to study on this topic

  • Comparative table of opioid analgesic potency.
  • Tramadol metabolism and the role of active metabolites.
  • Principles of combination pain therapy using non-opioid analgesics.
  • Differences between full agonists and mixed-mechanism agonists.
  • Pharmacokinetic features of transdermal drug delivery systems.

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