CENTRADOL ER

TAPENTADOL HYDROCHLORIDE

Tapentadol is indicated for the relief of moderate to severe acute pain in patients 18 years of age or older.

Opioid analgesics

Dutasteride & Tamsulosin combination capsules contain Dutasteride (a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5 alpha-reductase, an intracellular enzyme that converts testosterone to DHT) and Tamsulosin (an antagonist of alpha1A-adrenoceptors in the prostate). Dutasteride is a synthetic 4-azasteroid compound which inhibits the androgen primarily responsible for the initial development and subsequent enlargement of the prostate gland. Dutasteride is a competitive and specific inhibitor of both type 1 and type 2 5 alpha-reductase isoenzymes, with which it forms a stable enzyme complex. Smooth muscle tone is mediated by the sympathetic nervous stimulation of alpha1-adrenoceptors, which are abundant in the prostate, prostatic capsule, prostatic urethra, and bladder neck. Blockade of these adrenoceptors can cause smooth muscles in the bladder neck and prostate to relax, resulting in an improvement in urine flow rate and a reduction in symptoms of BPH. Tamsulosin, an alpha1-adrenoceptor blocking agent, exhibits selectivity for alpha1-receptors in the human prostate.

As with many centrally-acting analgesic medications, the dosing regimen should be individualized according to the severity of pain being treated, the previous experience with similar drugs and the ability to monitor the patient. The dose is 50 mg, 75 mg, or 100 mg every 4 to 6 hours depending upon pain intensity. On the first day of dosing, the second dose may be administered as soon as one hour after the first dose, if adequate pain relief is not attained with the first dose. Subsequent dosing is 50 mg, 75 mg, or 100 mg every 4 to 6 hours and should be adjusted to maintain adequate analgesia with acceptable tolerability. Daily doses greater than 700 mg on the first day of therapy and 600 mg on subsequent days have not been studied and are not recommended.

Increased risk of serotonin syndrome with other drugs that enhance monoaminergic neurotransmission (e.g. TCAs, triptans, SSRIs, serotonin and norepinephrine reuptake inhibitors). Enhanced sedative effect with benzodiazepines, barbiturates, antipsychotics, H1-antihistamines and other opioids. Increased potential for addiction with mixed 8-opioid agonists/antagonists (e.g. nalbuphine, pentazocine) or partial 8-opioid agonists (e.g. buprenorphine). Increased systemic exposure with strong inhibitors of UGT1A6, UGT1A9 and UGT2B7 isoenzymes. Decreased efficacy with strong enzyme inducers (e.g. rifampicin, phenobarbital).

This drug is contraindicated in patients with impaired Pulmonary Function, It is also contraindicated in patients with acute or severe bronchial asthma or hypercapnia in unmonitored settings or the absence of resuscitative equipment. This drug is contraindicated in any patient who has or is suspected of having paralytic ileus.

The following treatment-emergent adverse events may happen: heart rate increased, heart rate decreased, visual disturbance, abdominal discomfort, impaired gastric emptying, irritability, edema, drug withdrawal syndrome, hypersensitivity, involuntary muscle contractions, sensation of heaviness, hypoesthesia, paresthesia, disturbance in attention, sedation, dysarthria, memory impairment, ataxia, presyncope, syncope, coordination abnormal, seizure, urticaria, blood pressure decreased etc.

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. This preparation should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Neonates whose mothers have been taking Tapentadol should be monitored for respiratory depression.

Symptoms: Vomiting, miosis, CV collapse, consciousness disorders up to coma, convulsions and resp depression up to resp arrest. Management: Re-establish a patent airway and institute assisted or controlled ventilation. GI decontamination with activated charcoal or by gastric lavage may be considered within 2 hr after intake. Pure opioid receptor antagonists (e.g. naloxone) may be given as antidote.

Tapentadol should be administered with caution to patients with conditions accompanied by hypoxia, hypercapnia respiratory problems such as: asthma, chronic obstructive pulmonary disease etc. Besides this in case of patient with sleep apnea syndrome, myxedema, kyphoscoliosis, central nervous system (CNS) depression should have to be cautious prior administration of Tapentadol. Patients receiving other mu-opioid agonist analgesics, general anesthetics, phenothiazines, other tranquilizers, sedatives, hypnotics, or other CNS depressants (including alcohol) concomitantly with Tapentadol may exhibit additive CNS depression.

Store in a cool and dry place, protected from light and moisture. Keep the medicine out of the reach of children.