Gelotralib is an pain medicine similar to an opioid. Gelotralib is used to treat moderate to severe pain.
The extended-release form of Gelotralib is for around-the-clock treatment of pain. This form of Gelotralib is not for use on an as-needed basis for pain.
Gelotralib may also be used for purposes not listed in this medication guide.
Gelotralib indications
An indication is a term used for the list of condition or symptom or illness for which the medicine is prescribed or used by the patient. For example, acetaminophen or paracetamol is used for fever by the patient, or the doctor prescribes it for a headache or body pains. Now fever, headache and body pains are the indications of paracetamol. A patient should be aware of the indications of medications used for common conditions because they can be taken over the counter in the pharmacy meaning without prescription by the Physician.
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Adults
Gelotralib® (Gelotralib hydrochloride) is indicated for the management of moderate to moderately severe pain in adults.
Geriatrics ( > 65 Years of Age)
Healthy elderly subjects aged 65 to 75 years administered Gelotralib have plasma concentrations and elimination half-lives comparable to those observed in healthy subjects less than 65 years of age. Gelotralib® should be administered with greater caution in patients older than 75 years, due to the greater potential for adverse events in this population.
Pediatrics ( < 18 Years of Age)
The safety and effectiveness of Gelotralib® have not been studied in the pediatric population. Therefore, use of Gelotralib® tablets is not recommended in patients under 18 years of age.
How should I use Gelotralib?
Use Gelotralib orally disintegrating tablets as directed by your doctor. Check the label on the medicine for exact dosing instructions.
Take Gelotralib orally disintegrating tablets by mouth with or without food.
To open the blister pack, peel back the foil on the blister. Do NOT push the tablet through the foil.
Do NOT chew, break, or split the tablet.
To take Gelotralib orally disintegrating tablets, place the tablet in your mouth. Let it dissolve, and then swallow it with saliva. Gelotralib orally disintegrating tablets may be taken with or without water.
If you miss a dose of Gelotralib orally disintegrating tablets and you are taking it regularly, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.
Ask your health care provider any questions you may have about how to use Gelotralib orally disintegrating tablets.
Uses of Gelotralib in details
There are specific as well as general uses of a drug or medicine. A medicine can be used to prevent a disease, treat a disease over a period or cure a disease. It can also be used to treat the particular symptom of the disease. The drug use depends on the form the patient takes it. It may be more useful in injection form or sometimes in tablet form. The drug can be used for a single troubling symptom or a life-threatening condition. While some medications can be stopped after few days, some drugs need to be continued for prolonged period to get the benefit from it.
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Use: Labeled Indications
Pain management:
Extended release: Management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate.
Immediate release: Management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate.
Limitations of use: Reserve Gelotralib for use in patients for whom alternative treatment options (eg, nonopioid analgesics) are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain. Gelotralib ER is not indicated as an as-needed analgesic.
Off Label Uses
Premature ejaculation
Data from mostly placebo-controlled clinical trials suggest that Gelotralib may be beneficial for the treatment of premature ejaculation.
Gelotralib description
A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of morphine. It also has a depressant action on the cough center and may be given to control intractable cough associated with terminal lung cancer. Gelotralib is also used as part of the treatment of dependence on opioid drugs, although prolonged use of methadone itself may result in dependence. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3)
Gelotralib dosage
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Gelotralib Dosage
Generic name: Gelotralib HYDROCHLORIDE 100mg
Dosage form: capsule, extended release
The information at Drugs.com is not a substitute for medical advice. Always consult your doctor or pharmacist.
General Dosing Considerations
Gelotralib® is an extended-release formulation intended for once a day dosing in adults aged 18 years and older. The capsules must be swallowed whole with liquid and must not be split, chewed, dissolved or crushed. Chewing, crushing or splitting the capsule could result in the uncontrolled delivery of Gelotralib, in overdose and death.
Do not administer Gelotralib® at a dose exceeding 300 mg per day. Do not use Gelotralib® more than once daily or concomitantly with other Gelotralib products.
Patients Not Currently on Gelotralib Immediate-Release Products
Initiate treatment with Gelotralib® at a dose of 100 mg once daily and titrated up as necessary by 100 mg increments every five days to achieve a balance between relief of pain and tolerability.
Patients Currently on Gelotralib Immediate-Release Products
Calculate the 24-hour Gelotralib IR dose and initiate a total daily dose of Gelotralib® rounded down to the next lowest 100 mg increment. The dose may subsequently be individualized according to patient need. Due to limitations in flexibility of dose selection with Gelotralib®, some patients maintained on Gelotralib IR products may not be able to convert to Gelotralib®.
Patients 65 Years of Age and Older
Initiate dosing of an elderly patient (over 65 years of age) should be initiated cautiously, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function and of concomitant disease or other drug therapy. Gelotralib® should be administered with even greater caution in patients over 75 years, due to the greater frequency of adverse events seen in this population.
Patients with Renal Impairment
The limited availability of dose strengths and once daily dosing of Gelotralib® do not permit the dosing flexibility required for safe use in patients with severe renal impairment. Do not use Gelotralib® in patients with creatinine clearance less than 30 mL/min.
Patients with Hepatic Impairment
The limited availability of dose strengths and once daily dosing of Gelotralib hydrochloride extended-release capsules do not permit the dosing flexibility required for safe use in patients with severe hepatic impairment. Do not use Gelotralib® in patients with severe hepatic impairment (Child-Pugh Class C).
Discontinuation of Treatment
Withdrawal symptoms may occur if Gelotralib® is discontinued abruptly. Clinical experience with Gelotralib suggests that withdrawal symptoms may be reduced by tapering Gelotralib®.
Food Effects
Gelotralib® may be taken without regard to food.
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Other brands: Gelotralib, Gelotralib, Gelotralib, Rybix ODT
CYP2D6 and CYP3A4 Inhibitors: Concomitant administration of CYP2D6 and/or CYP3A4 inhibitors, such as quinidine, fluoxetine, paroxetine and amitriptyline (CYP2D6 inhibitors), and ketoconazole and erythromycin (CYP3A4 inhibitors), may reduce metabolic clearance of Gelotralib increasing the risk for serious adverse events including seizures and serotonin syndrome.
Serotonergic Drugs
There have been postmarketing reports of serotonin syndrome with use of Gelotralib and SSRIs/SNRIs or MAOIs and α2-adrenergic blockers. Caution is advised when Gelotralib is coadministered with other drugs that may affect the serotonergic neurotransmitter systems, such as SSRIs, MAOIs, triptans, linezolid (an antibiotic which is a reversible non-selective MAOI), lithium, or St. John's Wort. If concomitant treatment of Gelotralib with a drug affecting the serotonergic neurotransmitter system is clinically warranted, careful observation of the patient is advised, particularly during treatment initiation and dose increases.
Triptans
Based on the mechanism of action of Gelotralib and the potential for serotonin syndrome, caution is advised when Gelotralib is coadministered with a triptan. If concomitant treatment of Gelotralib with a triptan is clinically warranted, careful observation of the patient is advised, particularly during treatment initiation and dose increases.
Use With Carbamazepine
Patients taking carbamazepine, a CYP3A4 inducer, may have a significantly reduced analgesic effect of Gelotralib. Because carbamazepine increases Gelotralib metabolism and because of the seizure risk associated with Gelotralib, concomitant administration of Gelotralib and carbamazepine is not recommended.
Use With Quinidine
Coadministration of quinidine with Gelotralib resulted in a 50-60% increase in Gelotralib exposure and a 50-60% decrease in M1 exposure. The clinical consequences of these findings are unknown.
Use With Digoxin and Warfarin
Post-marketing surveillance of Gelotralib has revealed rare reports of digoxin toxicity and alteration of warfarin effect, including elevation of prothrombin times.
Potential for Other Drugs to Affect Gelotralib
In vitro drug interaction studies in human liver microsomes indicate that concomitant administration with inhibitors of CYP2D6 such as fluoxetine, paroxetine, and amitriptyline could result in some inhibition of the metabolism of Gelotralib.
Administration of CYP3A4 inhibitors, such as ketoconazole and erythromycin, or inducers, such as rifampin and St. John's Wort, with Gelotralib may affect the metabolism of Gelotralib leading to altered Gelotralib exposure.
Potential for Gelotralib to Affect Other Drugs
In vitro drug interaction studies in human liver microsomes indicate that Gelotralib has no effect on quinidine metabolism. In vitro studies indicate that Gelotralib is unlikely to inhibit the CYP3A4-mediated metabolism of other drugs when administered concomitantly at therapeutic doses. Gelotralib is a mild inducer of selected drug metabolism pathways measured in animals.
The most commonly reported adverse reactions are dizziness, nausea, constipation, headache, somnolence and vomiting as presented in Table 1.1.
Clinical Trial Adverse Drug Reactions
Because clinical trials are conducted under very specific conditions the adverse reaction rates observed in the clinical trials may not reflect the rates observed in practice and should not be compared to the rates in the clinical trials of another drug. Adverse drug reaction information from clinical trials is useful for identifying drug-related adverse events and for approximating rates.
Incidence of Adverse Reactions for Gelotralib® in Chronic Trials of Non-Malignant Pain (Non-titration Trials)
Gelotralib® was administered to 550 patients during the double-blind or open-label extension periods in studies of chronic non-malignant pain. Of these patients, 375 were 65 years old or older. Table 1.1 reports the cumulative incidence rate of adverse reactions by 7, 30 and 90 days for the most frequent reactions (5% or more by 7 days). The most frequently reported events were in the central nervous system and gastrointestinal system. The overall incidence rates of adverse experiences in these trials were similar for Gelotralib® and the active control groups, acetaminophen with codeine, and aspirin with codeine; however, the rates of withdrawals due to adverse events appeared to be higher in the Gelotralib® group. In the Gelotralib treatment groups, 16.8-24.5% of patients withdrew due to an AE, compared to 9.6-11.6% for acetaminophen with codeine and 18.5% for aspirin with codeine.
Table 1.1: Cumulative Incidence of Adverse Reactions for Gelotralib® in Chronic Trials of Non-Malignant Pain
Percentage of Patients with Adverse Reaction
N = 427
Up to 7 Days
Up to 30 Days
Up to 90 Days
Dizziness/Vertigo
26%
31%
33%
Nausea
24%
34%
40%
Constipation
24%
38%
46%
Headache
18%
26%
32%
Somnolence
16%
23%
25%
Vomiting
9%
13%
17%
Pruritus
8%
10%
11%
“CNS Stimulation” Number of patients with adverse event; numbers shown are all events regardless of relationship to study drug.
Incidence 1% to less than 5% possibly causally related: the following lists adverse reactions that occurred with an incidence of 1% to less than 5% in clinical trials, and for which the possibility of a causal relationship with Gelotralib® exists.
Incidence less than 1%, possibly causally related: the following lists adverse reactions that occurred with an incidence of less than 1% in clinical trials and/or reported in post-marketing experience.
Body as a Whole: Accidental injury, Allergic reaction, Anaphylaxis, Death, Suicidal tendency, Weight loss, Serotonin syndrome (mental status change, hyperreflexia, fever, shivering, tremor, agitation, diaphoresis, seizures and coma).
Other adverse experiences, causal relationship unknown
A variety of other adverse events were reported infrequently in patients taking Gelotralib® during clinical trials and/or reported in post-marketing experience. A causal relationship between Gelotralib® and these events has not been determined. However, the most significant events are listed below as alerting information to the physician.
Other Adverse Experiences Previously Reported in Clinical Trials or Post-Marketing Reports with Gelotralib Hydrochloride
Adverse events which have been reported with the use of Gelotralib products include: allergic reactions (including anaphylaxis, angioneurotic edema and urticaria), bradycardia, convulsions, drug dependence, drug withdrawal (including agitation, anxiety, gastrointestinal symptoms, hyperkinesia, insomnia, nervousness, tremors), hyperactivity, hypoactivity, hypotension, worsening of asthma and respiratory depression. Other adverse events which have been reported with the use of Gelotralib products and for which a causal association has not been determined include: difficulty concentrating, hepatitis, liver failure, pulmonary edema, Stevens-Johnson syndrome and suicidal tendency.
Serotonin syndrome (whose symptoms may include mental status change, hyperreflexia, fever, shivering, tremor, agitation, diaphoresis, seizures and coma) has been reported with Gelotralib when used concomitantly with other serotonergic agents such as SSRIs and MAOIs. Post-marketing experience with the use of Gelotralib-containing products included rare reports of delirium, miosis, mydriasis, and speech disorder, and very rare reports of movement disorder including dyskinesia and dystonia.
Cases of hypoglycemia have been reported in patients taking Gelotralib, mostly in patients with pre-disposing risk factors, including diabetes, elderly and renal insufficiency. Caution should be exercised when prescribing Gelotralib to diabetic patients. More frequent monitoring of blood glucose levels may be appropriate, including at initiation or dose increase.
Drug Abuse, Addiction And Dependence
Gelotralib may induce psychic and physical dependence of the morphine-type (μ-opioid). Dependence and abuse, including drug-seeking behaviour and taking illicit actions to obtain the drug are not limited to those patients with a prior history of opioid dependence. The risk in patients with substance abuse has been observed to be higher. Gelotralib is associated with craving and tolerance development.
A Risk Management program to support the safe and effective use of Gelotralib® has been established. The following are considered to be the essential components of the Risk Management program:
Commitment to not emphasize or highlight the scheduling status of Gelotralib® (i.e., not listed under a schedule to the CDSA) in its advertising or promotional activities.
Inclusion of a PAAB-approved fair balance statement in all Gelotralib® advertising and promotional materials.
Assurance that health-care education activities on pain management with Gelotralib® include balanced, evidence-based and current information. Commitment to take reasonable actions to inform health-care professionals that there is Health Canada-approved patient information on benefits and risks, and to ensure that this information can be readily accessed through electronic and/or hard copy sources.
Withdrawal Symptoms
Withdrawal symptoms may occur if Gelotralib® is discontinued abruptly. These symptoms may include: anxiety, sweating, insomnia, rigors, pain, nausea, tremors, diarrhea, upper respiratory symptoms, piloerection, and rarely, hallucinations. Other symptoms that have been seen less frequently with Gelotralib® discontinuation include: panic attacks, severe anxiety, and paresthesias. Clinical experience suggests that withdrawal symptoms may be relieved by reinstitution of opioid therapy followed by a gradual, tapered dose reduction of the medication combined with symptomatic support.
You should not take Gelotralib if you are allergic to it, if you have ever been addicted to drugs or alcohol, or if you have ever attempted suicide. Do not take Gelotralib while you are intoxicated (drunk) or taking any of the following: alcohol or street drugs, narcotic pain medicine, sedatives or tranquilizers, or medicine for depression, anxiety, or mental illness.
Seizures (convulsions) have occurred in some people taking Gelotralib. Gelotralib may be more likely to cause a seizure if you have a history of seizures or head injury, a metabolic disorder, or if you are taking certain medicines such as antidepressants, muscle relaxers, narcotic, or medicine for nausea and vomiting.
Seek emergency medical attention if you think you have used too much of this medicine. A Gelotralib overdose can be fatal.
Gelotralib may be habit-forming and should be used only by the person it was prescribed for. Keep the medication in a secure place where others cannot get to it.
Do not crush the Gelotralib tablet. This medicine is for oral (by mouth) use only. Powder from a crushed tablet should not be inhaled or diluted with liquid and injected into the body. Using this medicine by inhalation or injection can cause life-threatening side effects, overdose, or death.
The results of a survey conducted on ndrugs.com for Gelotralib are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Gelotralib. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.
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