TRAMADOL

Supervisors :
Dr Asninda Binti Bin Yamin,
Dr Erwina Binti Hashim

Presenter : Siti Nur Hidayah Binti Saudi

 TRAMADOL
• Tramadol is a opioid (narcotic) analgesics.
• Tramadol is used to treat moderate to severe pain.
• Centrally acting analgesic
• Considered safe , as it does not cause respiratory depression
and addiction compared to other opioid analgesics.
• Tramadol when administered by parenteral route has less
abuse potential.
• Antidote : Naloxone
 PHARMACOLOGY
Mechanism of Action
• Centrally acting analgesic
• Produces analgesic action by exhibiting agonist activity to MOR, central GABA
catecholamine and Serotonergic receptors.

Dosage
• Available dosage forms include capsules, tablets, including extended release
formulations and injections.
• 2-3 mg/kg (adult 50-100 mg) oral or IV (usual max 400 mg/day, up to 600
mg/day)

Absorption
• Bioavailability : Immediate release, 75% ; extended release, 85-90%
• Onset : 2-3 hr
• Duration : 9 hr
• Peak plasma time : Immediate release, 1.5 hr ; extended release, 12 hr
Metabolism
• Metabolized in liver by O and N-demethylation and by
conjugation reactions to form glucuronide and sulfates.
• O-desmethyltramadol (M1) is catalysed by CYP2D6 enzymes
and N-desmethytramadol (M2) catalysed by CYP3A4.
• Metabolites : M1 metabolite has 200-fold greater affinity for
opioid receptors.

Elimination
• Half-life: 6-8 hr
• Excretion : Urine (90%)
 CONTRAINDICATION

• Allergic to tramadol
• Known or suspected gastrointestinal obstruction, including paralytic ileus
• Seizure disorders
• Acute intoxication with alcohol
• Concomitant use with centrally acting analgesics, psychotropic drugs,
opioids, anaesthetics and sedative drugs.
• Severe renal or hepatic impairment
• Severe/acute bronchial asthma, significant respiratory depression
 SIDE EFFECT
• The most common adverse effects of tramadol include
nausea, dizziness, dry mouth, indigestion, vomiting,
constipation, drowsiness and headache.
• Compared to other opioids, respiratory depression and
constipation are considered less of a problem with tramadol.
• Can decrease mental or physical capacity to perform
potentially hazardous tasks ( e.g : driving or use machines)
 USAGE IN PREGNANCY

• Prolonged use of opioid analgesics during pregnancy may cause neonatal

opioid withdrawal syndrome.
• Available data in pregnant women are insufficient to inform a drug-
associated risk for major birth defects and miscarriage.

Labor and delivery

• Use of tramadol during labor may lead to respiratory depression in the neonate
• Opioids cross the placenta and may produce respiratory depression and psycho-
physiologic effects in neonates.
• An opioid antagonist, such as naloxone, must be available for reversal of opioid-
induced respiratory depression in the neonates.
• Opioid analgesics, can prolong labor through actions which temporarily reduce
the strength, duration, and frequency of uterine contractions.
 USAGE IN LACTATION
• Its use during lactation is also generally advised against, but a
small trial found that infants breastfed by mothers taking
tramadol were exposed to about 2.88% of the dose the
mothers were taking.
• There was no evidence of this dose having a harmful effect on
the newborn.
 REFERENCES
• Basic & Clinical Pharmacology, 12th Edition (LANGE Basic Science)
• Obstetrics and Gynaecology Protocol State of Kedah 2017
• Muna Subedi, Shalini Bajaj, An overview of tramadol and its usage in pain
management and future perspective,2019 (443-451)
• https://reference.medscape.com/drug/ultram-er-tramadol