February 8, 2023

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Today’s drug is tramadol brand names ultram conzip and adolo therapeutic category is that it’s an analgesic opioid dosage form and strength tramadol comes in a tablet a 50 milligram and 100 milligram tablet it comes in an extended release tablet in 100 200 and 300 milligrams and it comes in a solution with a concentration of 5 milligrams per 1 milliliter and

It also comes in an extended release capsule in a 100 150 200 and 300 milligram strength the indication is for pain management the immediate release and extended release tablets are used to manage chronic severe pain when alternative options are inadequate tramadol is reserved for when non-opioid alternatives are not tolerated or ineffective it’s important

To note that extended release tramadol is not indicated for as needed use and the lowest effective dose is generally used when treating pain some off-label indications are for premature ejaculation and restless leg syndrome or rls dosing by indications for pain management that is considered moderate to severe in adults for acute pain initiate 50 milligrams by

Mouth every four to six hours as needed alternate dosing is 25 to 50 milligrams by mouth three times a day max dosing is between 50 and 100 milligrams by mouth every four to six hours with a max of 400 milligrams per day for treating chronic pain for the immediate release tablet it’s initiated between 25 to 50 milligrams every day as needed when treating chronic

Pain immediate release tablets are initiated between 25 and 50 milligrams every six hours as needed at typically less than 300 milligrams per day if required dose increase up to 50 to 100 milligrams by mouth every four to six hours with a max of 400 milligrams per day one using extended release tablets to treat chronic pain initiate at 100 milligrams by mouth

Every day and may increase up to 100 milligrams a day every five days up to 300 milligrams per day for off-label uses premature ejaculation dosing is typically between 25 to 50 milligrams one to three hours prior to sexual activity when treating restless leg syndrome the dosing is between 50 and 100 milligrams at bedtime in pediatrics for pain management that is

Considered moderate to severe there is limited data so make sure to refer to the most current literature when treating acute pain for pediatrics between the age of four and less than or equal to 16 years of age the weight-based dosing is between one to two milligrams per kilogram per dose every four to six hours in adolescence greater than or equal to 17 years

Of age the dose range is between 25 to 100 milligrams every four to six hours titrating every three days up to the lowest effective dose the max dose is 400 milligrams per day when treating chronic pain in pediatrics for adolescents greater than or equal to 18 years of age 100 milligrams every day titrating every 5 days up to the lowest effective dose max of

300 milligrams per day mechanism of action and pharmacology tramadol as both the drug and as the active metabolite binds to the mu opioid receptor by binding to the mu opioid receptor this blocks the ascending pain pathways as well as altering the response and perception to pain tramadol also blocks reuptake of both serotonin and norepinephrine which plays an

Important role in the descending inhibitory pain pathway tramadol is metabolized extensively hepatically via the sip 3a4 and zip2d6 pathway the sip 2d6 pathway results in an active metabolite or m1 tramadol is excreted in the urine with 30 percent unchanged drug and 60 as the metabolite the onset of action for the immediate release formulation is within one hour

With a peak effect between two to three hours the half-life elimination for the immediate release form is around six hours with the active metabolite m1 being around 7 hours the extended release formulation is between 8 to 10 hours while the metabolite is between 9 and 11 hours tramadol is poorly protein-bound at around 20 in the plasma special populations and

Considerations in patients with renal impairment the excretion is decreased in patients with hepatic impairment the auc is increased while the elimination half-life is also increased in the elderly the serum concentration is increased as well as the elimination half-life is increased and for a gender consideration women have 12 percent higher peak concentrations

And 35 percent higher auc when compared to men in patients that are poor metabolizers of tramadol there is an increased concentration of drug at around 20 percent and a decrease in the formation of the metabolite by about 40 percent regarding the discontinuation of therapy a gradual taper down is recommended to minimize withdrawal side effects some general side

Effects are nausea vomiting constipation lightheadedness dizziness drowsiness and headache a major concern of tramadol is serotonin syndrome this can be identified by witnessing agitation abnormal heartbeat and severe nausea vomiting and diarrhea another concern is for qt prolongation and another concern is in pregnancy this medication does cross the placenta

Tramadol is not commonly used to treat pain during pregnancy tramadol has numerous black box warnings the first is for addiction abuse and misuse addiction can lead to overdose which may lead to death the next black box warning is for the risk of medication errors the next black box warning is for the risk of medication errors milligram and milliliter can get

Confused with prescribing dispensing and administering the solution the next black box warning is for life-threatening respiratory depression serious fatal and life-threatening respiratory depression may cause death another black box warning is for accidental ingestion this can be fatal in children the next black box warning is in ultra rapid metabolizers which

Is seen in children so this is seen specifically in the sip 2d6 polymorphism use should be avoided in children less than 12 as well as less than 18 years of age because there may be an increased sensitivity some of the other black box warnings are for opioid analgesic rems interactions with drugs affecting the sip p450 isoenzymes and neonatal opioid withdrawal

Syndrome when there is use during pregnancy as well as the use with benzodiazepines or other cns depressants drug interactions some of the general interactions are in maoist drug interactions some of the general interactions are with maois mixed opioid agonists and antagonists amphetamines anticholinergic agents and other cns depressants serotonin affecting

Substances such as antiometics and antidepressants sip 2d6 inhibitors sip 2d6 inducers sip 3a4 inducers and sip 3a4 inhibitors as well as hypoglycemia associated agents monitoring parameters level of pain relief respiratory status ekg and heart rate bowel function suicidal behavior and ideation addiction abuse and misuse as well as pregnancy patient counseling

Information tramadol is used to ease pain generally minor side effects are experienced such as dizziness nausea vomiting and diarrhea as well as headache

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#32: tramadol (Ultram) | Pain Management when Alternatives are Not Tolerated | Drug Cards Daily By Drug Cards Daily