Drug Interaction:
MAOI , alcohol, benzidoazepines, barbiturates, opiods,
antipsychotics, antihistamines,
other CNS depressants, SSRIs, SNRIs,
rifampicin, St Johns wart, triptans,
other strong enzymes induceres
Indication:
NUCYNTA® (tapentadol) immediate-release oral tablets C-II
Initial U.S. Approval: 2008
Tapentadol Extended release tablet 100mg/150mg/200mg (Additional Strength)
Indication-
For use in patients under hospital setting for severe acute pain for a period not
exceeding 5 days
Approved by FDA on 09-12-2013 (Ref- FDA approved List- 2014)
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
1.Tapentadol Hcl Tablets 18-04-2011
50mg/75mg/100mg
For the relief of Moderate to Severe Acute Pain in adults 18 years
of age and older
2.Tapentadol E.R tablet 09-12-2013
100/150/200mg
Addl.stgth
For Use in in-patients under Hospital Setting for Severe to Acute pain
for a period not exceeding 5 days
3.Tapentadol ER Tablet 12-11-2013
50mg
Addl.stgth
For use in in-patients for dose Titration under Hospital sttings for
Severe Acute Pain for a period not exceeding 5 days
Moderate to severe acute pain
Adverse Reaction:
Risk of dependence, Anorexia, anxiety, depression, agitation,
attention disturbances, confusion, hallucination, sleep disorders,
dizziness, somnloence, headache, tremor, flushing,
g-i upset, pruritus, hyperthidrosis, rash, muscle spasm,
dyspnea, asthenia, fatigue, respiratory and CNS depression,
feeling of body temperature change , mucosal dryness, odema
Contra-Indications:
Severe renal renal/hepatic impairment
Significant respratory depression,
acute or severe asthma
Hypercapnia, confirmed or suspected paralytic ileus.
During or within 14 days of MAOIs
Lactation
Special Precaution-
Moderate hepatic impairment
Increased intracranial pressure
Impaired consciuouness, head injury, brain tumor,
History of or risk facors for seizures,
Biliary tract discease
Acute pancreatitis
Severe obesity, sleep apnea syndrome
Myxodema, kyphoscoliosis
drug absuers,
With draw gradually
Elderly
Labour and delivery
Pregnancy
Dosages/ Overdosage Etc:
Indication-
For use in patients under hospital setting for severe acute pain for a period not
exceeding 5 days
Indication-
Moderate to severe acute pain
Dosage-
Initially -usally 50mg every 4-6 hours with additional 50mg 1 hour after first dose if necessary
Max - 700mg daily on day 1
Maintenance .Max 600mg daily
Consider switching to prolonged release preparation if long term treatment is anticipated
and stable dosing acheived
Patients below 16 years not recommended
Patient Information:
PATIENT COUNSELING INFORMATION
Physicians are advised to discuss the following issues with patients for whom they
prescribe NUCYNTA®:
1. Instructions for Use Patients should be advised NUCYNTA® should be taken only
as directed and to report episodes of breakthrough pain and adverse experiences
occurring during therapy to their physician. Individualization of dosage is essential
to make optimal use of this medication.
2. Patients should be advised not to adjust the dose of NUCYNTA® without consulting
their physician
3.Patients should be advised that it may be appropriate to taper dosing when
discontinuing treatment with NUCYNTA® as withdrawal symptoms may
occur
4.The physician can provide a dose schedule to accomplish a gradual
discontinuation of the medication.
5. Misuse and Abuse Patients should be advised that NUCYNTA® is a potential
drug of abuse. Patients should protect NUCYNTA® from theft, and
NUCYNTA® should never be given to anyone other than the individual
for whom NUCYNTA® was prescribed
6. Interference with Cognitive and Motor Performance As NUCYNTA® has
the potential to impair judgment, thinking, or motor skills, patients should
be cautioned about operating hazardous machinery, including automobiles
7.Pregnancy Patients should be advised to notify their physician if they
become pregnant or intend to become pregnant during treatment with
NUCYNTA®
8. Nursing Patients should be advised not to breast-feed an infant during
treatment with NUCYNTA®
9. Monoamine Oxidase Inhibitors Patients should be informed not to take
NUCYNTA® while using any drugs that inhibit monoamine oxidase.
10.atients should not start any new medications while taking NUCYNTA®
until they are assured by their healthcare provider that the new medication
is not a monoamine oxidase inhibitor.
11. Seizures- Patients should be informed that NUCYNTA® could cause
seizures if they are at risk for seizures or have epilepsy.
Such patients should be advised to use NUCYNTA® with care
Patients should be advised to stop taking NUCYNTA® if they have a
seizure while taking NUCYNTA® and call their healthcare provider right away.
12. Serotonin Syndrome Patients should be informed that NUCYNTA® could
cause rare but potentially life-threatening conditions resulting from
concomitant administration of serotonergic drugs (including Serotonin
Reuptake Inhibitors, Serotonin and Norepinephrine Reuptake Inhibitors
and tricyclic antidepressants)
13.Patients should be advised to inform their physicians if they are taking,
or plan to take, any prescription or over-the-counter drugs as there is a
potential for interactions
14. Alcohol- Patients should be advised to avoid alcohol while taking
NUCYNTA® .
Pharmacology/ Pharmacokinetics:
CLINICAL PHARMACOLOGY
1. Mechanism of Action
Tapentadol is a centrally-acting synthetic analgesic.
Although its exact mechanism is unknown, analgesic efficacy is thought to be due
to mu-opioid agonist activity and the inhibition of norepinephrine reuptake.
Absorption
Mean absolute bioavailability after single-dose administration (fasting) is approximately
32% due to extensive first-pass metabolism. Maximum serum concentrations of
tapentadol are typically observed at around 1.25 hours after dosing.
Food Effect
The AUC and Cmax increased by 25% and 16%, respectively, when NUCYNTA® wa
administered after a high-fat, high-calorie breakfast. NUCYNTA® may be given
with or without food.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1. Pregnancy
Pregnancy Category C.
There are no adequate and well controlled studies of NUCYNTA® in pregnant
women. NUCYNTA® should be used during pregnancy only if the potential
benefit justifies the potential risk to the fetus.
2. Nursing Mothers-
There is insufficient/limited information on the excretion of tapentadol in human
or animal breast milk. Physicochemical and available
pharmacodynamic/toxicological data on tapentadol point to excretion in
breast milk and risk to the suckling child cannot be excluded.
NUCYNTA® should not be used during breast-feeding.
3. Pediatric Use-
18 years of age have not been established. NUCYNTA® is not recommended
in this population.
4. Geriatric -
Use Of the total number of patients in Phase 2/3 double-blind, multiple-dose
clinical studies of NUCYNTA®, 19% were 65 and over, while 5% were 75
and over. No overall differences in effectiveness were observed between
these patients and younger patients. The rate of constipation was higher
in subjects greater than or equal to 65 years than those less than
65 years (12% vs. 7%).
In general, recommended dosing for elderly patients with normal renal and hepatic function is the same as for younger adult patients with normal renal and hepatic function. Because elderly patients are more likely to have decreased renal and hepatic function, consideration should be given to starting elderly patients with the lower range of recommended doses [se
