" Tramadol "
Generic name : Tramadol : الاسم العلمي
Brand name : الاسم التجاري :-
amadol – contramal – tamol
tramax – tramundin – ultradol
- all of these drugs are composed of tramadol hydrochloride
- tramadol also combine with acetaminophen forming the following drugs :-
Zaldiar and Tramacet
** The chemical name is :- (±) cis-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl) cyclohexanol hydrochloride .
- It's structural formula :-
Brand name : الاسم التجاري :-
amadol – contramal – tamol
tramax – tramundin – ultradol
- all of these drugs are composed of tramadol hydrochloride
- tramadol also combine with acetaminophen forming the following drugs :-
Zaldiar and Tramacet
** The chemical name is :- (±) cis-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl) cyclohexanol hydrochloride .
- It's structural formula :-
Tramadol's powder features and the non active ingredients combined with it :-
انظر بيدج 2
انظر بيدج 2
Drug class and mechanism :
** Analgesics, Opioid , Narcotics **
-Tramadol is a man-made (synthetic) analgesic (pain reliever).
- Its exact mechanism of action is unknown but similar morphine.
- Like morphine, tramadol binds to receptors in the brain (opioid receptors) that are
important for transmitting the sensation of pain from throughout the body to.
- Tramadol, like other narcotics used for the treatment of pain, may be abused.
- Tramadol is not a nonsteroidal antiinflammatory drug (NSAID)
and does not have the increased risk of stomach ulceration and internal bleeding that can occur with NSAIDs.
- it produces euphoria and relaxation
ف البيدج التانيهNSAID توضيح ال *
Opioid receptors :-
How Does The Opioid System Control Pain, Reward And Addictive Behavior?
** Analgesics, Opioid , Narcotics **
-Tramadol is a man-made (synthetic) analgesic (pain reliever).
- Its exact mechanism of action is unknown but similar morphine.
- Like morphine, tramadol binds to receptors in the brain (opioid receptors) that are
important for transmitting the sensation of pain from throughout the body to.
- Tramadol, like other narcotics used for the treatment of pain, may be abused.
- Tramadol is not a nonsteroidal antiinflammatory drug (NSAID)
and does not have the increased risk of stomach ulceration and internal bleeding that can occur with NSAIDs.
- it produces euphoria and relaxation
ف البيدج التانيهNSAID توضيح ال *
Opioid receptors :-
How Does The Opioid System Control Pain, Reward And Addictive Behavior?
- The opioid system controls pain, reward and addictive behaviors.
- Opioids exert their pharmacological actions through three opioid
- receptors, mu, delta and kappa .
- Opioid receptors in the brain are activated by a family of endogenous –
- peptides like enkephalins, dynorphins and endorphin, which are released by neurons.
- Opioid receptors can also be activated exogenously by alkaloid opiates , the prototype of which is morphine .
Activation of opioid receptors characteristically depresses neuronal firing and inhibits neurotransmitter and hormone release .
Opioids inhibit central nervous system pathways from spinal cord to cerebral cortex, block hypothalamic and neurohypophyseal hormone release, and depress autonomic effector systems in the periphery.
The pharmacological spectrum of opioid action comprises prominent analgesic, antiperistaltic, antitussive, and mood-altering effects, but opioids also cause hypotension and respiratory depression.
Preparations :-
- Tablets (immediate release) : 50 mg.
- (extended release) : 100, 200, and 300 mg.
the differences between them :-
Immediate-release tablets and capsules release the active ingredient within a small period of time, typically less than 30 minutes.
Extended-release tablets and capsules release the active ingredient at a sustained and controlled release rate over a period of time.
Typically extended-release tablets and capsules release their ingredient with time periods of 8 hours , 12 hours , 16 hours , and 24 hours.
Delayed-release tablets and capsules release the pharmaceutical dosage after a set time.
The delayed-release tablets and capsules are frequently enteric-coated in order to prevent release in the stomach and, thus, release the dosage in the intestinal track
Storage :-
- Store at room temperature, 15-30 C (59-86 F).
- Store in a sealed container.
Prescribed for :-
- للمرضى ال عندهم الم مستمر
- Tramadol is used in the management of moderate to moderately severe pain.
- Extended release tablets are used for moderate to moderately severe chronic pain in
- adults who require continuous treatment for an extended period.
The Two Faces of Pain: Acute and Chronic:-
What is pain?
The International Association for the Study of Pain defines it as :
An unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage.
It is useful to distinguish between two basic types of pain, acute and chronic, and they differ greatly.
Acute pain, for the most part, results from disease, inflammation, or injury to tissues. This type of pain generally comes on suddenly, for example, after trauma or surgery, and may be accompanied by anxiety or emotional distress.
· The cause of acute pain can usually be diagnosed and treated, and the pain is self-limiting, that is, it is confined to a given period of time and severity. In some rare instances, it can become chronic.
· Chronic pain is widely believed to represent disease itself.
It can be made much worse by environmental and psychological factors.
Chronic pain persists over a longer period of time than acute pain and is resistant to most medical treatments.
It can—and often does—cause severe problems for patients.
A person may have two or more co-existing chronic pain conditions.
Such conditions can include chronic fatigue syndrome, endometriosis, fibromyalgia, inflammatory bowel disease, interstitial cystitis, temporomandibular joint dysfunction, and vulvodynia.
It is not known whether these disorders share a common cause.
DOSING :-
- (immediate release tablets) :-
The recommended dose of tramadol is 50-100 mg every 4-6 hours as needed for pain.
The maximum dose is 400 mg/day.
To improve tolerance patients should be started at 25 mg/day, and doses may be increased by 25 mg every 3 days to reach 100 mg/day (25 mg 4 times daily).
Thereafter, doses can be increased by 50 mg every 3 days to reach 200 mg day (50
mg 4 times daily).
Tramadol may be taken with or without food. باقي الجرعات يفضل تكون ذي الاولى من حيث الاكل او عدمه
- ( Recommended dose for extended release tablets ) :-
100 mg daily which may be increased by 100 mg every 5 days
but not to exceed 300 mg /day.
Extended release tablets should be swallowed whole and not crushed or
chewed .
Drug interactions :-
Carbamazepine :- reduces the effect of tramadol by increasing its inactivation in the body.
Quinidine :- reduces the inactivation of tramadol, thereby increasing the concentration of tramadol by 50%-60%.
Combining tramadol with monoamine oxidase inhibitors or selective serotonin inhibitors
((SSRIs ))
may result in severe side effects such as seizures or a condition called serotonin syndrome.
Tramadol may increase central nervous system and respiratory depression when combined with alcohol, anesthetics, narcotics, tranquilizers or sedative hypnotics.
Pregnancy and lactation :-
-The safety of tramadol during pregnancy has not been established.
-The safety of tramadol in nursing mothers has not been established .
1- Tramadol Pregnancy Warnings :-
Tramadol has been assigned to pregnancy category C by the FDA.
Animal studies have revealed evidence of embryotoxicity and fetotoxicity.
There are no controlled data in human pregnancy.
Tramadol should only be given during pregnancy when benefit outweighs risk.
Tramadol has been shown to cross the placental barrier, with an umbilical vein to maternal vein serum concentration ratio of 0.83.
A case of tramadol withdrawal in a neonate has been reported following long-term analgesic treatment of the mother.
At 35 hours of age, the infant showed signs of a severe withdrawal syndrome with high-pitched crying, trembling, and shortened sleeping hours.
Breast feeding women = nursing mothers
2- Tramadol Breastfeeding Warnings :-
Tramadol is excreted into human milk in small amounts.
The manufacturer suggests that tramadol should not be administered to nursing women.
Summary of Use during Lactation :-
The excretion of tramadol into milk is low and even lower amounts of the active metabolite, O-desmethyltramadol, are excreted.
With usual maternal dosage, the amount excreted into breastmilk is much less than the dose given to newborn infants for analgesia.
A study in breastfed newborn infants found no adverse effects attributable to tramadol.
Tramadol is unlikely to adversely affect nursing infant and is acceptable to use during breastfeeding. However, monitor infants for increased sleepiness (more than usual), difficulty breastfeeding, breathing difficulties or limpness, and contact a physician immediately if any of these occur.
Side effects :-
Tramadol is generally well tolerated, and side effects are usually transient.
Commonly reported side effects include :-
Nausea , constipation , dizziness , headache ,
Drowsiness , and vomiting .
Less commonly reported side effects include :-
Itching , sweating , dry mouth , diarrhea ,
rash , visual disturbances , and vertigo .
Some patients who received tramadol have reported seizures.
Abrupt withdrawal of tramadol may result in :- anxiety, sweating, insomnia, rigors,
pain, nausea, diarrhea, tremors, and hallucinations.
- Opioids exert their pharmacological actions through three opioid
- receptors, mu, delta and kappa .
- Opioid receptors in the brain are activated by a family of endogenous –
- peptides like enkephalins, dynorphins and endorphin, which are released by neurons.
- Opioid receptors can also be activated exogenously by alkaloid opiates , the prototype of which is morphine .
Activation of opioid receptors characteristically depresses neuronal firing and inhibits neurotransmitter and hormone release .
Opioids inhibit central nervous system pathways from spinal cord to cerebral cortex, block hypothalamic and neurohypophyseal hormone release, and depress autonomic effector systems in the periphery.
The pharmacological spectrum of opioid action comprises prominent analgesic, antiperistaltic, antitussive, and mood-altering effects, but opioids also cause hypotension and respiratory depression.
Preparations :-
- Tablets (immediate release) : 50 mg.
- (extended release) : 100, 200, and 300 mg.
the differences between them :-
Immediate-release tablets and capsules release the active ingredient within a small period of time, typically less than 30 minutes.
Extended-release tablets and capsules release the active ingredient at a sustained and controlled release rate over a period of time.
Typically extended-release tablets and capsules release their ingredient with time periods of 8 hours , 12 hours , 16 hours , and 24 hours.
Delayed-release tablets and capsules release the pharmaceutical dosage after a set time.
The delayed-release tablets and capsules are frequently enteric-coated in order to prevent release in the stomach and, thus, release the dosage in the intestinal track
Storage :-
- Store at room temperature, 15-30 C (59-86 F).
- Store in a sealed container.
Prescribed for :-
- للمرضى ال عندهم الم مستمر
- Tramadol is used in the management of moderate to moderately severe pain.
- Extended release tablets are used for moderate to moderately severe chronic pain in
- adults who require continuous treatment for an extended period.
The Two Faces of Pain: Acute and Chronic:-
What is pain?
The International Association for the Study of Pain defines it as :
An unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage.
It is useful to distinguish between two basic types of pain, acute and chronic, and they differ greatly.
Acute pain, for the most part, results from disease, inflammation, or injury to tissues. This type of pain generally comes on suddenly, for example, after trauma or surgery, and may be accompanied by anxiety or emotional distress.
· The cause of acute pain can usually be diagnosed and treated, and the pain is self-limiting, that is, it is confined to a given period of time and severity. In some rare instances, it can become chronic.
· Chronic pain is widely believed to represent disease itself.
It can be made much worse by environmental and psychological factors.
Chronic pain persists over a longer period of time than acute pain and is resistant to most medical treatments.
It can—and often does—cause severe problems for patients.
A person may have two or more co-existing chronic pain conditions.
Such conditions can include chronic fatigue syndrome, endometriosis, fibromyalgia, inflammatory bowel disease, interstitial cystitis, temporomandibular joint dysfunction, and vulvodynia.
It is not known whether these disorders share a common cause.
DOSING :-
- (immediate release tablets) :-
The recommended dose of tramadol is 50-100 mg every 4-6 hours as needed for pain.
The maximum dose is 400 mg/day.
To improve tolerance patients should be started at 25 mg/day, and doses may be increased by 25 mg every 3 days to reach 100 mg/day (25 mg 4 times daily).
Thereafter, doses can be increased by 50 mg every 3 days to reach 200 mg day (50
mg 4 times daily).
Tramadol may be taken with or without food. باقي الجرعات يفضل تكون ذي الاولى من حيث الاكل او عدمه
- ( Recommended dose for extended release tablets ) :-
100 mg daily which may be increased by 100 mg every 5 days
but not to exceed 300 mg /day.
Extended release tablets should be swallowed whole and not crushed or
chewed .
Drug interactions :-
Carbamazepine :- reduces the effect of tramadol by increasing its inactivation in the body.
Quinidine :- reduces the inactivation of tramadol, thereby increasing the concentration of tramadol by 50%-60%.
Combining tramadol with monoamine oxidase inhibitors or selective serotonin inhibitors
((SSRIs ))
may result in severe side effects such as seizures or a condition called serotonin syndrome.
Tramadol may increase central nervous system and respiratory depression when combined with alcohol, anesthetics, narcotics, tranquilizers or sedative hypnotics.
Pregnancy and lactation :-
-The safety of tramadol during pregnancy has not been established.
-The safety of tramadol in nursing mothers has not been established .
1- Tramadol Pregnancy Warnings :-
Tramadol has been assigned to pregnancy category C by the FDA.
Animal studies have revealed evidence of embryotoxicity and fetotoxicity.
There are no controlled data in human pregnancy.
Tramadol should only be given during pregnancy when benefit outweighs risk.
Tramadol has been shown to cross the placental barrier, with an umbilical vein to maternal vein serum concentration ratio of 0.83.
A case of tramadol withdrawal in a neonate has been reported following long-term analgesic treatment of the mother.
At 35 hours of age, the infant showed signs of a severe withdrawal syndrome with high-pitched crying, trembling, and shortened sleeping hours.
Breast feeding women = nursing mothers
2- Tramadol Breastfeeding Warnings :-
Tramadol is excreted into human milk in small amounts.
The manufacturer suggests that tramadol should not be administered to nursing women.
Summary of Use during Lactation :-
The excretion of tramadol into milk is low and even lower amounts of the active metabolite, O-desmethyltramadol, are excreted.
With usual maternal dosage, the amount excreted into breastmilk is much less than the dose given to newborn infants for analgesia.
A study in breastfed newborn infants found no adverse effects attributable to tramadol.
Tramadol is unlikely to adversely affect nursing infant and is acceptable to use during breastfeeding. However, monitor infants for increased sleepiness (more than usual), difficulty breastfeeding, breathing difficulties or limpness, and contact a physician immediately if any of these occur.
Side effects :-
Tramadol is generally well tolerated, and side effects are usually transient.
Commonly reported side effects include :-
Nausea , constipation , dizziness , headache ,
Drowsiness , and vomiting .
Less commonly reported side effects include :-
Itching , sweating , dry mouth , diarrhea ,
rash , visual disturbances , and vertigo .
Some patients who received tramadol have reported seizures.
Abrupt withdrawal of tramadol may result in :- anxiety, sweating, insomnia, rigors,
pain, nausea, diarrhea, tremors, and hallucinations.