Centradol Injection

Description

Dosage Information

Here’s a breakdown of the typical dosages for Centradol:

Adults

• Oral (Immediate Release) for Moderate to Severe Pain:
  • Chronic Pain: Start with 25 mg every morning, increasing by 25-50 mg/day every three days up to 50-100 mg every 4-6 hours as needed. Do not exceed 400 mg/day.
  • Acute Pain: 50-100 mg every 4-6 hours as needed. Do not exceed 400 mg/day.
• Oral (Extended Release):
  • Start with 100 mg once daily, increasing by 100 mg/day every five days. Do not exceed 300 mg/day.
• Parenteral (IM/IV) for Moderate to Severe Pain:
  • 50-100 mg every 4-6 hours, administered over 2-3 minutes.
• Postoperative Pain:
  • Initially, 100 mg, followed by 50 mg every 10-20 minutes if needed, up to a total of 250 mg in the first hour (including the initial dose). Afterward, 50-100 mg every 4-6 hours, with a maximum daily dose of 600 mg.

Elderly Patients (>75 years)

• The dosing interval should be increased.

Children

• Immediate Release (Moderate-to-Severe Pain):
  • Under 17 years: Safety and efficacy are not established.
  • Over 17 years (Acute): 50-100 mg every 4-6 hours as needed. Do not exceed 400 mg/day.
  • Over 17 years (Chronic): 25 mg every morning initially, increasing by 25-50 mg/day every three days in separate doses up to 50-100 mg every 4-6 hours as needed. Do not exceed 400 mg/day.
• Extended Release:
  • Under 18 years: Safety and efficacy are not established.

Special Populations

• Hepatic Impairment:
  • Severe: For immediate release, use 50 mg every 12 hours. Extended release is not recommended.
• Renal Impairment:
  • Creatinine Clearance (CrCl) 10-30 ml/min: Increase dosing interval to every 12 hours.
  • CrCl <10 ml/min: Contraindicated.

Administration

Centradol can be taken with or without food.

Important Considerations

Contraindications

Do not use Centradol in patients who are:

• Suicidal
• Suffering from acute alcoholism
• Experiencing head injuries or raised intracranial pressure
• Have severe renal impairment
• Lactating

Precautions

Use with caution in patients with:

• Emotional disturbance or depression
• A history of epilepsy or risk of seizures
• Head injury
• Increased intracranial pressure
• Renal and hepatic impairment
• Elderly individuals
• Pregnant or lactating women

Patient Counseling

This medication may impair your ability to drive or operate machinery.

Monitoring

During treatment, healthcare providers should monitor:

• Pain relief
• Respiratory rate
• Blood pressure
• Pulse rate
• Signs of tolerance, abuse, or suicidal ideation

Pregnancy and Lactation

• Lactation: The drug is excreted in breast milk at high concentrations and is not recommended for nursing mothers.
• Pregnancy: Use with caution.

Drug Interactions

• Increased Risk of Convulsions or Serotonin Syndrome: Occurs with SSRIs, SNRIs, TCAs, and other seizure threshold-lowering drugs (e.g., bupropion, mirtazapine, tetrahydrocannabinol).
• Decreased Serum Concentrations: May occur with carbamazepine.
• Potentiation of Antidepressant Effect: May enhance the effect of norepinephrine, 5-HT agonists, or lithium.
• Increased INR and Ecchymoses: Seen with coumarin derivatives (e.g., warfarin).
• Potentially Fatal Interactions: Increased risk of seizure and serotonin syndrome with MAOIs.

Side Effects

Many side effects are dose-dependent and vary among individuals.

Very Common (>10%)

Constipation, nausea, dizziness, vertigo, headache, somnolence, vomiting, agitation, anxiety, emotional lability, euphoria, hallucinations, nervousness, spasticity, dyspepsia, asthenia, pruritus.

Common (1-10%)

Diarrhea, dry mouth, sweating, hypertonia, malaise, menopausal symptoms, rash, urinary frequency, urinary retention, vasodilation, visual disturbance.

Less Common (<1%)

Abnormal gait, amnesia, cognitive dysfunction, depression, difficulty in concentration, dysphoria, dysuria, fatigue, menstrual disorder, motor system weakness, orthostatic hypotension, paresthesia, seizures, suicidal tendencies, syncope, tachycardia, tremor.

Frequency Not Defined

Abnormal electrocardiogram (ECG), angioedema, bronchospasm, flushing, hypertension, hypotension, myocardial ischemia, palpitation, urticaria, withdrawal syndrome.

Potentially Fatal

Respiratory depression.

Mechanism of Action

Tramadol works by inhibiting the reuptake of norepinephrine and serotonin and enhancing serotonin release. It alters the perception and response to pain by binding to mu-opiate receptors in the central nervous system (CNS).