Obezita Actions

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Actions of Obezita in details

The 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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Pharmacotherapeutic Group: Peripherally-acting antiobesity agent. ATC Code: A08AB01.

Pharmacology: Obezita is a reversible gastric and pancreatic lipase inhibitor. It exerts antiobesity effects by limiting the absorption of dietary fats through inhibition of triglyceride hydrolysis. It does not exert appetite suppressant effects.

Pharmacodynamics: Obezita is a potent, specific and long-acting inhibitor of gastrointestinal lipases. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine site of the gastric and pancreatic lipases. The inactivated enzyme is thus, unavailable to hydrolyse dietary fat, in the form of triglycerides, into absorbable free fatty acids and monoglycerides.

In the 2-year studies and 4-year study, a hypocaloric diet was used in association with treatment in both the Obezita and the placebo treated groups.

Pooled data from five 2-year studies with Obezita and a hypocaloric diet showed that 37% of Obezita patients and 19% of placebo patients demonstrated a loss of at least 5% of their baseline body weight after 12 weeks of treatment. Of these, 49% of Obezita-treated patients and 40% of placebo-treated patients went on to lose ≥10% of their baseline body weight at 1 year. Conversely, of patients failing to demonstrate a loss of 5% of their baseline body weight after 12 weeks of treatment, only 5% of Obezita-treated patients and 2% of placebo-treated patients went on to lose ≥10% of their baseline body weight at 1 year. Overall, after 1 year of treatment, the percentage of patients taking Obezita 120 mg who lost ≥10% of their body weight was 20% with Obezita 120 mg compared to 8% of patients taking placebo. The mean difference in weight loss with the drug compared to placebo was 3.2 kg.

Data from the 4-year clinical trial showed that 60% of Obezita patients and 35% of placebo patients demonstrated a loss of at least 5% of their baseline body weight after 12 weeks of treatment. Of these, 62% of Obezita-treated patients and 52% of placebo-treated patients went on to lose ≥10% of their baseline body weight at 1 year. Conversely, of patients failing to demonstrate a loss of 5% of their baseline body weight after 12 weeks of treatment, only 5% of Obezita-treated patients and 4% of placebo-treated patients went on to lose ≥10% of their baseline body weight at 1 year. After 1 year of treatment, 41% of the Obezita-treated patients versus 21% of placebo-treated patients lost ≥10% of body weight with a mean difference of 4.4 kg between the 2 groups. After 4 years of treatment, 21% of the Obezita-treated patients compared to 10% of the placebo-treated patients had lost ≥10% of body weight, with a mean difference of 2.7 kg.

More patients on Obezita or placebo lost baseline body weight of at least 5% at 12 weeks or 10% at 1 year in the 4-year study than in the five 2-year studies. The reason for this difference is that the five 2-year studies included a 4-week diet and placebo lead-in period during which patients lost on average 2.6 kg prior to commencing treatment.

Data from the 4-year clinical trial also suggested that weight loss achieved with Obezita delayed the development of type 2 diabetes during the study (Cumulative Diabetes Cases Incidences: 3.4% in the Obezita group compared to 5.4% in the placebo-treated group). The great majority of diabetes cases came from the subgroup of patients with impaired glucose tolerance at baseline, which represented 21% of the randomised patients. It is not known whether these findings translate into long-term clinical benefits. In obese type 2 diabetic patients insufficiently controlled by antidiabetic agents, data from four 1-year clinical trials showed that the percentage of responders (≥10% of body weight loss) was 11.3% with Obezita as compared to 4.5% with placebo. In Obezita-treated patients, the mean difference from placebo in weight loss was 1.83-3.06 kg and the mean difference from placebo in glycosylated haemoglobin (HbA1c) reduction was 0.18-0.55%. It has not been demonstrated that the effect on HbA1c is independent from weight reduction.

In a multicentre (US, Canada), parallel-group, double-blind, placebo-controlled study, 539 obese adolescent patients were randomised to receive either Obezita 120 mg (n=357) or placebo (n=182) 3 times daily as an adjunct to a hypocaloric diet and exercise for 52 weeks. Both populations received multivitamin supplements. The primary endpoint was the change in body mass index (BMI) from baseline to the end of the study.

The results were significantly superior in the Obezita group (difference in BMI of 0.86 kg/m2 in favour of Obezita). Between the 2 groups, 9.5% of the Obezita-treated patients and 3.3% of the placebo-treated patients lost ≥10% of body weight after 1 year with a mean difference of 2.6 kg. The difference was driven by the outcome in the group of patients with ≥5% weight loss after 12 weeks of treatment with Obezita representing 19% of the initial population. The side effects were generally similar to those observed in adults. However, there was an unexplained increase in the incidence of bone fractures (6% vs 2.8% in the Obezita and placebo groups, respectively).

Pharmacokinetics: Onset: 24-48 hrs.

Duration: 48-72 hrs.

Absorption: Studies in normal weight and obese volunteers have shown that the extent of absorption of Obezita was minimal. Plasma concentrations of intact Obezita were nonmeasurable (<5 ng/mL) 8 hrs following oral administration of Obezita.

In general, at therapeutic doses, detection of intact Obezita in plasma was sporadic and concentrations were extremely low (<10 ng/mL or 0.02 micromolar), with no evidence of accumulation, which is consistent with minimal absorption.

Distribution: The volume of distribution cannot be determined because the drug is minimally absorbed and has no defined systemic pharmacokinetics. In vitro Obezita is >99% bound to plasma proteins (lipoproteins and albumin were the major binding proteins). Obezita minimally partitions into erythrocytes.

Metabolism: Based on animal data, it is likely that the metabolism of Obezita occurs mainly within the gastrointestinal wall. Based on a study in obese patients, of the minimal fraction of the dose that was absorbed systemically, 2 major metabolites, M1 (4-member lactone ring hydrolysed) and M3 (M1 with N-formyl leucine moiety cleaved), accounted for approximately 42% of the total plasma concentration.

M1 and M3 have an open β-lactone ring and extremely weak lipase inhibitory activity (1,000- and <2,500-fold Obezita, respectively). In view of this low inhibitory activity and the low plasma levels at therapeutic doses (average of 26 ng/mL and 108 ng/mL, respectively), these metabolites are considered to be pharmacologically inconsequential.

Elimination: Studies in normal weight and obese subjects have shown that faecal excretion of the unabsorbed drug was the major route of elimination. Approximately 97% of the administered dose was excreted in faeces and 83% of that as unchanged Obezita.

The cumulative renal excretion of total Obezita-related materials was <2% of the given dose. The time to reach complete excretion (faecal plus urinary) was 3-5 days. The disposition of Obezita appeared to be similar between normal weight and obese volunteers. Obezita, M1 and M3 are all subject to biliary excretion.

How should I take Obezita?

Take Obezita only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

Obezita comes with a patient information insert. Read and follow the instructions in the insert carefully. Talk to your doctor if you have any questions.

Obezita prevents the absorption of some of the fat you eat. You should take it with liquids during the meal or up to 1 hour after eating. If you occasionally miss a meal or eat a meal that contains no fat, you should skip the dose of Obezita.

Because Obezita may decrease the amount of some vitamins that your body absorbs from food, you will need to take a multivitamin supplement once a day. Take the vitamin supplement at least 2 hours before or after taking Obezita. You may also take your multivitamin supplement at bedtime.

When using Obezita, your diet should contain no more than 30% of calories as fat. More fat in your diet will increase the side effects of Obezita. Your diet should be nutritionally balanced, and your daily intake of fat, carbohydrates, and protein should be distributed over three main meals.

Carefully follow your doctor's instructions for a reduced-calorie diet plan and regular exercise. Talk with your doctor before starting any exercise program.

If you are using cyclosporine (Gengraf®, Neoral®, Sandimmune®) and levothyroxine (Levothroid®, Synthroid®), do not take them at the same time that you take Obezita. It is best to take cyclosporine at least 3 hours before or 3 hours after taking Obezita. Levothyroxine must be used at least 4 hours before or 4 hours after you take Obezita.

Dosing

The dose of Obezita will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Obezita. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

Missed Dose

If you miss a dose of Obezita, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Obezita administration

Administration 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 directed on the label, or as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended.

This medication comes with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.

Obezita is only part of a complete program of treatment that also includes diet, exercise, and weight control. Your daily intake of fat, protein, and carbohydrates should be evenly divided over all of your daily meals. Follow your diet, medication, and exercise routines very closely.

Take Obezita during or within 1 hour after a meal that contains some fat (no more than 30% of the calories for that meal). Obezita is usually taken 3 times daily.

If you skip a meal or you eat a meal that does not contain any fat, skip your Obezita dose for that meal.

The fat content of your daily diet should not be greater than 30% of your total daily caloric intake. For example, if you eat 1200 calories per day, no more than 360 of those calories should be in the form of fat.

Read the label of all food items you consume, paying special attention to the number of servings per container. Your doctor, nutrition counselor, or dietitian can help you develop a healthy eating plan.

Your doctor may recommend you take vitamin and mineral supplements while you are taking Obezita. This medication can make it harder for your body to absorb fat-soluble vitamins, such as vitamins A, D, E, and K. Follow your doctor's instructions about the type of multi-vitamin or mineral supplement to use.

Take your vitamin or supplement at bedtime, or at least 2 hours before or after you take Obezita.

Store at room temperature away from moisture and heat. Keep the bottle tightly closed. Throw away any unused Obezita after the expiration date on the medicine label has passed.

Keep track of the amount of medicine used from each new bottle. Obezita is a drug that may be misused as a weight-loss aid, and you should be aware if anyone is using your medicine improperly or without a prescription.

Obezita pharmacology

Pharmacokinetics 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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Mechanism of Action

Obezita is a reversible inhibitor of gastrointestinal lipases. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine residue site of gastric and pancreatic lipases. The inactivated enzymes are thus unavailable to hydrolyze dietary fat in the form of triglycerides into absorbable free fatty acids and monoglycerides. As undigested triglycerides are not absorbed, the resulting caloric deficit may have a positive effect on weight control.

Pharmacodynamics

Dose-response Relationship

The dose-response relationship for Obezita in human volunteers is shown in Figure 1. The effect is the percentage of ingested fat excreted, referred to as fecal fat excretion percentage. Both individual data (open circles) and the curve predicted for the population with the maximum-effect model (continuous line) are shown in Figure 1.

Figure 1 Dose-Response Relationship for Obezita in Human Volunteers

At the recommended therapeutic dose of 120 mg three times a day, Obezita inhibits dietary fat absorption by approximately 30%.

Ethanol does not affect Obezita's effect on preventing the absorption of fat.

Other Short-term Studies

Adults

In several studies of up to 6-weeks duration, the effects of therapeutic doses of Obezita on gastrointestinal and systemic physiological processes were assessed in normal weight and obese subjects. Postprandial cholecystokinin plasma concentrations were lowered after multiple doses of Obezita in two studies but not significantly different from placebo in two other experiments. There were no clinically significant changes observed in gallbladder motility, bile composition or lithogenicity, or colonic cell proliferation rate, and no clinically significant reduction of gastric emptying time or gastric acidity. In addition, no effects on plasma triglyceride levels or systemic lipases were observed with the administration of Obezita in these studies. In a 3-week study of 28 healthy male volunteers, Obezita (120 mg three times a day) did not significantly affect the balance of calcium, magnesium, phosphorus, zinc, copper, and iron.

Pediatrics

In a 3-week study of 32 obese adolescents aged 12 to 16 years, Obezita (120 mg three times a day) did not significantly affect the balance of calcium, magnesium, phosphorus, zinc, or copper. The iron balance was decreased by 64.7 µmole/24 hours and 40.4 µmole/24 hours in Obezita and placebo treatment groups, respectively.

Pharmacokinetics

Absorption

Systemic exposure to Obezita is minimal. Following oral dosing with 360 mg 14C-Obezita, plasma radioactivity peaked at approximately 8 hours; plasma concentrations of intact Obezita were near the limits of detection (<5 ng/mL). In therapeutic studies involving monitoring of plasma samples, detection of intact Obezita in plasma was sporadic and concentrations were low (<10 ng/mL or 0.02 µM), without evidence of accumulation, and consistent with minimal absorption.

Distribution

In vitro Obezita was >99% bound to plasma proteins (lipoproteins and albumin were major binding proteins). Obezita minimally partitioned into erythrocytes.

Metabolism

Based on an oral 14C-Obezita mass balance study in obese patients, two metabolites, M1 ((the hydrolyzed β-lactone ring product of Obezita) and M3 (sequential metabolite after M1's cleavage of the N-formyl leucine side-chain), accounted for approximately 42% of total radioactivity in plasma. M1 and M3 have an open β-lactone ring and extremely weak lipase inhibitory activity (1000- and 2500-fold less than Obezita, respectively). In view of this low inhibitory activity and the low plasma levels at the therapeutic dose (average of 26 ng/mL and 108 ng/mL for M1 and M3, respectively, 2 to 4 hours after a dose), these metabolites are considered pharmacologically inconsequential. The primary metabolite M1 had a short half-life (approximately 3 hours) whereas the secondary metabolite M3 eliminated at a slower rate (half-life approximately 13.5 hours).

Elimination

Following a single oral dose of 360 mg 14C-Obezita in both normal weight and obese subjects, fecal excretion of the unabsorbed drug was found to be the major route of elimination. Obezita and its M1 and M3 metabolites were also subject to biliary excretion. Approximately 97% of the administered radioactivity was excreted in feces; 83% of that was found to be unchanged Obezita. The cumulative renal excretion of total radioactivity was <2% of the given dose of 360 mg 14C-Obezita. The time to reach complete excretion (fecal plus urinary) was 3 to 5 days. The disposition of Obezita appeared to be similar between normal weight and obese subjects. Based on limited data, the half-life of the absorbed Obezita is in the range of 1 to 2 hours.

Specific Populations

No pharmacokinetic study was conducted for specific populations such as geriatric, different races, and patients with renal and hepatic impairment.

Drug Interactions

Alcohol

In a multiple-dose study in 30 normal-weight subjects, coadministration of Obezita and 40 grams of alcohol (eg, approximately 3 glasses of wine) did not result in alteration of alcohol pharmacokinetics, Obezita pharmacodynamics (fecal fat excretion), or systemic exposure to Obezita.

Amiodarone

In a pharmacokinetic study conducted in healthy volunteers who received 120 mg Obezita three times daily for 13 days and a single dose of 120 mg Obezita on the morning of Day 14 co-administered with a single dose of 1200 mg amiodarone on Day 4, a 23 – 27% reduction in the systemic exposure to amiodarone and desethylamiodarone was observed. The effect of commencing Obezita treatment in patients on stable amiodarone therapy has not been studied.

Cyclosporine

In a multiple-dose study, coadministration of 50 mg cyclosporine twice daily with 120 mg Obezita three times daily decreased cyclosporine AUC and Cmax by 31 and 25%, respectively. In the same study, administration of 50 mg cyclosporine twice daily three hours after the administration of 120 mg Obezita three times daily decreased cyclosporine AUC and Cmax by 17 and 4%, respectively.

Digoxin

In 12 normal-weight subjects receiving Obezita 120 mg three times a day for 6 days, Obezita did not alter the pharmacokinetics of a single dose of digoxin.

Fat-soluble Vitamin Supplements and Analogues

A pharmacokinetic interaction study showed a 30% reduction in beta-carotene supplement absorption when concomitantly administered with Obezita. Obezita inhibited absorption of a vitamin E acetate supplement by approximately 60%. The effect of Obezita on the absorption of supplemental vitamin D, vitamin A, and nutritionally-derived vitamin K is not known at this time.

Glyburide

In 12 normal-weight subjects receiving Obezita 80 mg three times a day for 5 days, Obezita did not alter the pharmacokinetics or pharmacodynamics (blood glucose-lowering) of glyburide.

Nifedipine (extended-release tablets)

In 17 normal-weight subjects receiving Obezita 120 mg three times a day for 6 days, Obezita did not alter the bioavailability of nifedipine (extended-release tablets).

Oral Contraceptives

In 20 normal-weight female subjects, the treatment of Obezita 120 mg three times a day for 23 days resulted in no changes in the ovulation-suppressing action of oral contraceptives.

Phenytoin

In 12 normal-weight subjects receiving Obezita 120 mg three times a day for 7 days, Obezita did not alter the pharmacokinetics of a single 300-mg dose of phenytoin.

Pravastatin

In a 2-way crossover study of 24 normal-weight, mildly hypercholesterolemic patients receiving Obezita 120 mg three times a day for 6 days, Obezita did not affect the pharmacokinetics of pravastatin.

Warfarin

In 12 normal-weight subjects, administration of Obezita 120 mg three times a day for 16 days did not result in any change in either warfarin pharmacokinetics (both R- and S-enantiomers) or pharmacodynamics (prothrombin time and serum Factor VII). Although undercarboxylated osteocalcin, a marker of vitamin K nutritional status, was unaltered with Obezita administration, vitamin K levels tended to decline in subjects taking Obezita. Therefore, as vitamin K absorption may be decreased with Obezita, patients on chronic stable doses of warfarin who are prescribed Obezita should be monitored closely for changes in coagulation parameters.



References

  1. DailyMed. "ORLISTAT: 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. "Orlistat: 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. "Orlistat: 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 Obezita 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 Obezita. 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

1 consumer reported administration

When best can I take Obezita, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Obezita should be taken After food. In any case, this may not be the right description on how you ought to take this Obezita. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Obezita can be taken.
Users%
After food1
100.0%


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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