Helex Actions

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How do you administer this medicine?

Actions of Helex in details

infoThe action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Pharmacology: Pharmacodynamics: Helex tablets contain a triazolobenzodiazepine. The benzodiazepines have qualitatively similar properties: Anxiolysis, hypnosedation, myorelaxation and anticonvulsion. There are, however, quantitative differences in their pharmacodynamic properties that have led to varying patterns of therapeutic application.

Currently, there is a general agreement that the action of benzodiazepines is a result of the potentiation of the neural inhibition that is mediated by γ-aminobutyric acid (GABA).

Pharmacokinetics: Following oral administration, peak concentrations of Helex tablets in plasma occur in 1-2 hrs following administration. The mean half-life (t½) of Helex is 12-15 hrs.

Following oral administration, peak concentrations of Helex in plasma occur between 5 and 11 hrs following administration. The mean t½ of Helex is 11.2 hrs.

Helex is mainly oxidized. The predominant metabolites are α-hydroxy-Helex and a benzophenone derived from Helex. Plasma levels of these metabolites are extremely low. The biological activity of α-hydroxy-Helex is approximately ½ that of Helex. Their t½ appear to be of the same order of magnitude as that of Helex. The benzophenone metabolite is essentially inactive. Helex and its metabolites are excreted primarily in the urine.

In vitro, Helex is bound (80%) to human serum protein.

Toxicology: Preclinical Safety Data: Mutagenicity, Carcinogenicity, Fertility and Ocular Effects: Helex was not mutagenic in the in vitro Ames test. Helex did not produce chromosomal aberrations in the in vivo micronucleus assay in rats up to the highest dose tested of 100 mg/kg, which is 500 times greater than the maximum recommended daily human dose of 10 mg/day.

No evidence of carcinogenic potential was observed during 2-year bioassay studies of Helex in rats at doses up to 30 mg/kg/day (150 times the maximum recommended daily human dose of 10 mg/day) and in mice at doses up to 10 mg/kg/day (50 times the maximum recommended daily human dose of 10 mg/day).

Helex did not impair fertility in rats up to the highest dose tested of 5 mg/kg/day, which is 25 times the maximum recommended daily human dose of 10 mg/day.

When rats were treated orally with Helex at 3 mg/kg/day, 10 mg/kg/day and 30 mg/kg/day (15-150 times the maximum recommended daily human dose of 10 mg/day) for 2 years, a tendency for a dose-related increase in the number of cataracts (females) and corneal vascularization (males) was observed. These lesions did not appear until after 11 months of treatment.

How should I take Helex?

Take Helex exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.

Your doctor may occasionally change your dose to make sure you get the best results from this medication.

Helex may be habit-forming and should be used only by the person it was prescribed for. Helex should never be shared with another person, especially someone who has a history of drug abuse or addiction. Keep the medication in a secure place where others cannot get to it. Do not crush, chew, or break a Helex extended-release tablet. Swallow the tablet whole. It is specially made to release Helex slowly in the body. Breaking the tablet would cause too much Helex to be released at one time.

Contact your doctor if this medicine seems to stop working as well in treating your panic or anxiety symptoms.

Your symptoms may return when you stop using Helex after using it over a long period of time. You may also have seizures or withdrawal symptoms when you stop using Helex.

Withdrawal symptoms may include blurred vision, trouble concentrating, loss of appetite, diarrhea, muscle twitching, numbness or tingling, or increased sensations.

Do not stop using Helex suddenly without first talking to your doctor. You may need to use less and less before you stop the medication completely.

To be sure this medication is helping your condition, your doctor will need to check your progress on a regular basis. Do not miss any scheduled visits to your doctor.

Store Helex at room temperature away from moisture, heat, and light. Remove any cotton from the bottle of disintegrating tablets, and keep the bottle tightly closed.

Keep track of how many pills have been used from each new bottle of this medicine. Benzodiazepines are drugs of abuse and you should be aware if any person in the household is using this medicine improperly or without a prescription.

Helex administration

infoAdministration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results.

Do not crush, chew, or break an extended-release tablet. Swallow the pill whole. It is specially made to release medicine slowly in the body. Breaking the pill would cause too much of the drug to be released at one time.

Measure the liquid form of Helex with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

Do not swallow the orally disintegrating tablets whole. Allow it to dissolve in your mouth without chewing.

Contact your doctor if this medicine seems to stop working as well in treating your panic or anxiety symptoms.

You may have seizures or withdrawal symptoms when you stop using Helex. Ask your doctor how to avoid withdrawal symptoms when you stop using Helex.

Keep track of the amount of medicine used from each new bottle. Helex is a drug of abuse and you should be aware if anyone is using your medicine improperly or without a prescription.

Store at room temperature away from moisture and heat.

Helex pharmacology

infoPharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Pharmacodynamics

CNS agents of the 1,4 benzodiazepine class presumably exert their effects by binding at stereospecific receptors at several sites within the central nervous system. Their exact mechanism of action is unknown. Clinically, all benzodiazepines cause a dose-related central nervous system depressant activity varying from mild impairment of task performance to hypnosis.

Pharmacokinetics

Absorption

Following oral administration of Helex (immediate-release) tablets, Helex is readily absorbed. Peak concentrations in the plasma occur in one to two hours following administration. Plasma levels are proportional to the dose given; over the dose range of 0.5 to 3.0 mg, peak levels of 8.0 to 37 ng/mL were observed. Using a specific assay methodology, the mean plasma elimination half-life of Helex has been found to be about 11.2 hours (range: 6.3–26.9 hours) in healthy adults.

The mean absolute bioavailability of Helex from Helex XR tablets is approximately 90%, and the relative bioavailability compared to Helex tablets is 100%. The bioavailability and pharmacokinetics of Helex following administration of Helex XR tablets are similar to that for Helex tablets, with the exception of a slower rate of absorption. The slower absorption rate results in a relatively constant concentration that is maintained between 5 and 11 hours after the dosing. The pharmacokinetics of Helex and two of its major active metabolites (4-hydroxyalprazolam and α-hydroxyalprazolam) are linear, and concentrations are proportional up to the recommended maximum daily dose of 10 mg given once daily. Multiple dose studies indicate that the metabolism and elimination of Helex are similar for the immediate-release and the extended-release products.

Food has a significant influence on the bioavailability of Helex XR tablets. A high-fat meal given up to 2 hours before dosing with Helex XR tablets increased the mean Cmax by about 25%. The effect of this meal on Tmax depended on the timing of the meal, with a reduction in Tmax by about 1/3 for subjects eating immediately before dosing and an increase in Tmax by about 1/3 for subjects eating 1 hour or more after dosing. The extent of exposure (AUC) and elimination half-life (t1/2) were not affected by eating.

There were significant differences in absorption rate for the Helex XR tablet, depending on the time of day administered, with the Cmax increased by 30% and the Tmax decreased by an hour following dosing at night, compared to morning dosing.

Distribution

The apparent volume of distribution of Helex is similar for Helex XR and Helex tablets. In vitro, Helex is bound (80%) to human serum protein. Serum albumin accounts for the majority of the binding.

Metabolism

Helex is extensively metabolized in humans, primarily by cytochrome P450 3A4 (CYP3A4), to two major metabolites in the plasma: 4-hydroxyalprazolam and α-hydroxyalprazolam. A benzophenone derived from Helex is also found in humans. Their half-lives appear to be similar to that of Helex. The pharmacokinetic parameters at steady-state for the two hydroxylated metabolites of Helex (4-hydroxyalprazolam and α-hydroxyalprazolam) were similar for Helex and Helex XR tablets, indicating that the metabolism of Helex is not affected by absorption rate. The plasma concentrations of 4-hydroxyalprazolam and α-hydroxyalprazolam relative to unchanged Helex concentration after both Helex XR and Helex tablets were always less than 10% and 4%, respectively. The reported relative potencies in benzodiazepine receptor binding experiments and in animal models of induced seizure inhibition are 0.20 and 0.66, respectively, for 4-hydroxyalprazolam and α-hydroxyalprazolam. Such low concentrations and the lesser potencies of 4-hydroxyalprazolam and α-hydroxyalprazolam suggest that they are unlikely to contribute much to the pharmacological effects of Helex. The benzophenone metabolite is essentially inactive.

Elimination

Helex and its metabolites are excreted primarily in the urine. The mean plasma elimination half-life of Helex following administration of Helex XR tablet ranges from 10.7–15.8 hours in healthy adults.

Special Populations

While pharmacokinetic studies have not been performed in special populations with Helex XR tablets, the factors (such as age, gender, hepatic or renal impairment) that would affect the pharmacokinetics of Helex after the administration of Helex tablets would not be expected to be different with the administration of Helex XR tablets.

Changes in the absorption, distribution, metabolism, and excretion of benzodiazepines have been reported in a variety of disease states including alcoholism, impaired hepatic function, and impaired renal function. Changes have also been demonstrated in geriatric patients. A mean half-life of Helex of 16.3 hours has been observed in healthy elderly subjects (range: 9.0–26.9 hours, n=16) compared to 11.0 hours (range: 6.3–15.8 hours, n=16) in healthy adult subjects. In patients with alcoholic liver disease the half-life of Helex ranged between 5.8 and 65.3 hours (mean: 19.7 hours, n=17) as compared to between 6.3 and 26.9 hours (mean=11.4 hours, n=17) in healthy subjects. In an obese group of subjects the half-life of Helex ranged between 9.9 and 40.4 hours (mean=21.8 hours, n=12) as compared to between 6.3 and 15.8 hours (mean=10.6 hours, n=12) in healthy subjects.

Because of its similarity to other benzodiazepines, it is assumed that Helex undergoes transplacental passage and that it is excreted in human milk.

Race

Maximal concentrations and half-life of Helex are approximately 15% and 25% higher in Asians compared to Caucasians.

Pediatrics

The pharmacokinetics of Helex after administration of the Helex XR tablet in pediatric patients have not been studied.

Gender

Gender has no effect on the pharmacokinetics of Helex.

Cigarette Smoking

Helex concentrations may be reduced by up to 50% in smokers compared to non-smokers.

Drug-Drug Interactions

Helex is primarily eliminated by metabolism via cytochrome P450 3A (CYP3A). Most of the interactions that have been documented with Helex are with drugs that inhibit or induce CYP3A4.

Compounds that are potent inhibitors of CYP3A would be expected to increase plasma Helex concentrations. Drug products that have been studied in vivo, along with their effect on increasing Helex AUC, are as follows: ketoconazole, 3.98 fold; itraconazole, 2.70 fold; nefazodone, 1.98 fold; fluvoxamine, 1.96 fold; and erythromycin, 1.61 fold.

CYP3A inducers would be expected to decrease Helex concentrations and this has been observed in vivo. The oral clearance of Helex (given in a 0.8 mg single dose) was increased from 0.90±0.21 mL/min/kg to 2.13±0.54 mL/min/kg and the elimination t1/2 was shortened (from 17.1±4.9 to 7.7±1.7 h) following administration of 300 mg/day carbamazepine for 10 days. However, the carbamazepine dose used in this study was fairly low compared to the recommended doses (1000–1200 mg/day); the effect at usual carbamazepine doses is unknown.

Interactions involving HIV protease inhibitors (eg, ritonavir) and Helex are complex and time dependent. Short-term low doses of ritonavir (4 doses of 200 mg) reduced Helex clearance to 41% of control values, prolonged its elimination half-life (mean values, 30 versus 13 h) and enhanced clinical effects. However, upon extended exposure to ritonavir (500 mg, twice daily), CYP3A induction offset this inhibition. Helex AUC and Cmax was reduced by 12% and 16%, respectively, in the presence of ritonavir.

The ability of Helex to induce or inhibit human hepatic enzyme systems has not been determined. However, this is not a property of benzodiazepines in general. Further, Helex did not affect the prothrombin or plasma warfarin levels in male volunteers administered sodium warfarin orally.



References

  1. DailyMed. "ALPRAZOLAM: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. NCIt. "Alprazolam: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
  3. EPA DSStox. "Alprazolam: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Helex 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 Helex. 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.

User reports

3 consumers reported administration

When best can I take Helex, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Helex should be taken Empty stomach. In any case, this may not be the right description on how you ought to take this Helex. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Helex can be taken.
Users%
Empty stomach2
66.7%
After food1
33.3%


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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