Cetilistat 1) What is Cetilistat?Cetilistat, under the brand name (CETISLIM, CHECKWT or KILFAT)is a new drug that is currently undergoing experimentation and clinical trialsin various parts of the world for its effectiveness.
It is classified under the”anti-obesity or anorectic drugs” category. Obesity happens to be one ofthe major issues of the modern times, mostly in the developing &industrialized countries. Statistics suggest that the number of deaths anddiseases reported worldwide by obesity and overweight are higher than thatreported by underweight. Cetilistat is an intra-orally active anti-obesity drug.
Itprimarily functions as a gastrointestinal and pancreatic lipase inhibitor. Itis also experimented with the treatment of Diabetes Mellitus (DM) especiallytype 2 with successful results. (Citeurl: http://www.
fda.gov/drugs/resourcesforyou/consumers/questionsanswers/ucm136187.htm )Cetilistatis used as a supplement to diet and exercise for a short term in the treatmentof obesity. It is also used for purposes that are not listed in the medicationguide. Cetilistatis an experimental anti-obesity drug and is currently being researched on inthe Japan, U.S, and Europe. Because Cetilistat is undergoing clinical trials,there is no efficacy or safety profile as yet for this drug. 2) How did Cetilistat start?Withthe rising numbers of patients suffering from obesity and prevalence ofassociated risks increasing, weight management has become an essential part ofa healthy lifestyle.
The focus is mainly on modifications in lifestyle. It canbe achieved by consuming balanced nutrition, reducing the intake of saturatedfat, shifting to a diet that has moderate levels of calories and increasingone’s physical activity.Alongwith the above-mentioned measures, pharmacological options are used. The availabilities for weight management are limitedare right now. Amongst the common ones are Orlistat (pancreatic and gastriclipase inhibitor). Phentermine (sympathomimetic drug) is used but not approvedin all countries for treatment of obese patients, diagnosed or not diagnosedwith diabetes. Sibutramine (a reuptake inhibitor that works in combination ofboth serotonin and nor epinephrine) it acts on the central nervous system toincrease satiety. Rimonabant (Cannabinoid 1 receptor blocker) which wasrecently eliminated from the market.
Cetilistat,noble drug, is a highly lipophilic benzoxazinone inhibitor of pancreatic and gastriclipases, it is currently undergoing development for the management of weight inobese patients with or without any concerning medical complications. Cetilistat (ATL-962) wasinitially developed by Alizyme, a company specializing in biopharmaceuticals incollaboration with Takeda Pharmaceutical. The global rights of the drug aretransferred to “NORGINA BV” afterAlizyme shifted to administration. (Citeurl: http://en.wikipedia.org/wiki/Cetilistat )In December 2008, A Phase IIIclinical study of Cetilistat was started by Takeda in Japan.
As a result ofprogress to pivotal Phase III trials, Phase II clinical trials were encouraged.The survey showed significant weight loss by the use of Cetilistat. It was alsowell tolerated in patients suffering from obesity clinically. The drug waspromoted.
In August 2003, Takedaevaluated Phase II of European data and in January 2004 in collaboration withAlizyme made an agreement to exclusively develop, generate, manufacture anddistribute Cetilistat in Japan. Takeda submitted a New Drug Application (NDA)in October 2012 to Japan’s Ministry of Health, Labour and Welfare forCetilistat as the treatment of obesity. The company’s development and researchis focused on treatment of GI disorders, cancer, diabetes and obesity.(Citeurl: http://www.
drugdevelopment-technology.com/projects/cetilistat/) 3) Ingredients of Cetilistat”Cetilistat” itselfis the active salt ingredient that is marketed in the form of “Citislim Tablet”Salt – 60mgMolecularformula: C25H39NO3IUPACName2-hexadecoxy-6-methyl-3, 1-benzoxazin-4-oneMESHnames1. 2-(hexadecyloxy)-6-methyl-4H-3,1-benzoxazin-4-one2. ATL-9623.
Cetilistat MOLECULARWEIGHT: 401.591g/mol https://pubchem.ncbi.nlm.nih.
gov/compound/Cetilistat#section=Pharmacology-and-Biochemistry 4) Does Cetilistat work?There have been limitedreviews regarding the user of the drug since it’s still under research andexperimentation. There is no guarantee given that the medicine will work forall. Diet and exercise have to be added along with its use. It can only beprescribed by a doctor and is formulated for short-term use.
The formula is notvery long lasting and changes need to be kept without support from the drug.Prolonged use can cause addiction. It also leads to gastrointestinalcomplications.The substance may reduce theappetite of obese individuals. There are many other facets of weight loss that havenot been addressed, such as metabolic rate and thermogenesis. Moreover,Cetilistat has its fair share of side effects that come along with its use. Notonly does it limit the people who may want to use this product, but thepotential for abuse makes the potential audience even narrower.
While trying tomanage weight to a healthy level, it sometimes becomes imperative that peopleunderstand that sacrifices need to be made to get results. However, youroverall well-being shouldn’t be one of those things.The updated research suggeststhat Cetilistat is tolerated well as compared to the widely available Orlistatwhich is also a lipase inhibitor. 5) Cetilistat Benefits and Results · Treatment of obesity· Treatment of Diabetes Mellitus· Treatment of dyslipidemia Accordingto a study published by Peter Kopleman in the year 2010, Cetilistat istolerated more than Orlistat with fewer gastrointestinal complications.Asurvey was carried out for 2 weeks where patients were randomized to placebo. Cetilistatin dosages of 40, 80, or 120 mg thrice daily or Orlistat 120 mg three times aday for 12 weeks. The initial endpoint was evident change in body weightcompared to where we started from.
Secondary endpoints demonstrated othervariations in glycemic control and obesity. Reductions in body weight weresimilar in patients who were given Cetilistat in dosages of 80 or 120 mg t.i.d.or Orlistat in dosage of 120mg. Significantreductions are observed with drugs vs. placebo (3.86 kg, P = 0.
02;4.33 kg, P = 0.0003; 3.79 kg, P = 0.009).
Inthe 40 mg t.i.d. and placebo groups, reductions of 2.95 kg, P =0.959 and 2.87 kg were observed respectively. Glycosylated hemoglobin (HbA1c)levels were noted as decreased significantly.
Cetilistat was well tolerated,and showed fewer discontinuations due to adverse events (AEs) than in theplacebo and Orlistat groups. Discontinuation due to gastrointestinal adverseeffects was significantly worse in the Orlistat group compared to the 120 mg Cetilistatand placebo groups. Significant reductions in body weight were found with theintake of drugs compared to the placebo. In obese patients who were diabetic,glycemic levels were significantly improved as opposed to placebo groups.Therefore, Cetilistat proved to be well tolerated. Cases of discontinuations weresimilar in placebo due to adverse effects.
6) Cetilistat and weight loss?Cetilistat is a lipase inhibitor, which has a similar modeof action to Roche’s anti-obesity Orlistat (Xenical) which in 1997 receivedregulatory approval. These drugs act in the gastrointestinal tract to inhibit lipasesthat are enzymes responsible for the breakdown of dietary fats. By inhibitingthe dissolution and subsequent digestion of fats from the intestine, theseinhibitors reduce fat intake and calories, therefore aiding in weight loss. Inshort, it results in weight loss andabsorbs lipids from food. This drug acts peripherally on the system to reducethe appetite, without affecting or damaging the brain. 7) How to use Cetilistat?Consultwith your medical doctor or your physician before intending to start with themedication. It is not advisable to adjust dosage for yourself.
Cetilistat needsto be taken as prescribed by the doctor. It is advised not to take in larger orsmaller quantity than recommended. Only take medicine for the time prescribed,do not take it for a short or long time period.
Before starting Cetislim Tablet, inform your physician about your in-use list of medications,over the counter products (e.g., vitamins, herbal supplements, etc.
). Anyconcerning genetic disorders or familial history, any allergies, pre-existingdiseases, and current health conditions (e.g.
, pregnancy, lactation, upcomingsurgery, etc.). Some chronic or acute health conditions may make you moresusceptible to the side-effects of the drug. Use as directed by your doctor orfollow the direction printed on the product insert.
Dosage is dependent on yourcondition. Tell your doctor if your condition persists or worsens. Essentialcounseling points are listed below.· Consultyour doctor if suffering from diabetes or taking other herbal or nutritionalproducts · Take the tablet at least 1hour after the meal or during the meal· Dosages of 60-100 mg areusually prescribed. Do not exceed unless advised.· Eat a healthy diet andkeep yourself hydrated· Control your fat intakewhile using this drug, a hypo caloric diet is recommended. · Increase your physicalactivity during the period of utilizing the medication· Cetilistatis also contraindicated with warfarin and levothyroxine as this could causeincreased risk of bleeding and hypothyroidism· If taking cyclosporineand/or levothyroxine, separate administration of those drugs and this drug byminimum 4-5 hours. (Citeurl: http://www.
tabletwise.com/cetislim-tablet) Storageof Cetislim Tablet· The tabletsshould be preserved and stored at room temperature.· Keep them away from any heat or exposure todirect light. Do not freeze tablets unless mentioned by package insert. Strictly keep medicines away from children and pets.· Do not flush medicationsdown the toilet or pour them into drainage unless instructed to do so.
Medicines discardedin this manner contaminate the environment. Kindly consult with your physicianor pharmacist for more details on how to safely remove CetislimTablet.(Citeurl: http://www.learnaboutrxsafety.
org/quick-scoop.aspx#safely ) 8) What happens if you miss a dose?Start your treatment with a set schedule and as early aspossible. You need to be compliant to your medication and your doctor’s advice.Missing a dose initially hinders the results that are expected. If you forgetto take it during mid-treatment, the effectiveness reduces. Some patients showsigns of early withdrawal from a drug if consistent doses dosages are missed.· If a dose is missed, take it at the earliest whenyou remember.
· If you recall that you’ve missed a dose and it’stime for your next dose, then do not take it an till an hour before your nextscheduled dose.· An extra dose should not be taken to make up fora missed dose.· Resume your schedule of doses after the nextdose.· If you have difficulty taking it on time, setyourself a reminder on phone or alarm.· Ask members of family to keep you reminded.· Kindly consult a doctor to issue you a newschedule or change your dosage routine and adjust it to your convenience tomake up for the doses missed. .
pdf )(Citeurl: http://www.nhs.uk/chq/Pages/860.aspx?CategoryID=73 ) 9) What happens if you overdose?· Be very careful when youstart your medication and ask your pharmacist how and when to use them. · The effectiveness of themedicine does not improve if you take it in larger quantities thanprescribed. Neither will one achieve results quicker if you use the drugin more quantity or shorter intervals.· Increase quantities causesevere adverse effects and poisoning to the system.
· Overdose results incomplications that can be fatal.· Seek medical help from thenearest health centre or emergency immediately if you feel that you or anybodyhas overdosed on Cetilistat medicine.· Bring a medicine box, container, or label withyou to help doctors with necessary information.· Do not give your medicinesto other people even if you know that they have the same condition or it seems that they may have similar problems.
This may lead to over dosage.· Kindly consult yourphysician or pharmacist for product information.(Citeurl: http://www.emedicinehealth.
com/drug_overdose/article_em.htm ) 10) Usage in childrenAfterthe appropriate consideration and evaluation of the medical condition of achild or adult, the options available should be discussed before proceedingwith any sort anti-obesity drugs. The first line of treatment should however bediet, exercise and lifestyle modifications. After trying all these diligently,if no response is appreciated or is inadequate we opt towards the rigoroustherapy.Children,especially during their spurt, are not encouraged to use these drugs as it can have potential effects on their heightand growth. Treatment if not producing results otherwise can be delayedtill height growth is complete.(citeurl:https://books.
google.com.pk/books?id=1W2M1lnHeccC=PA335=PA335=cetilistat+dosage+in+children=bl=wEHA873i2A=xu2gowGrQ41wLYO20JwLFdoflZ8=en=X=0ahUKEwjSgoq3gN3YAhULGCwKHZhCBGkQ6AEILjAB ) 11) Cetilistat Reviews?”I started out at 290 pounds! It’s been longer than 15 dayssince I’ve been using this medicine. Feel great about the results. Never feltbetter. I’m consuming a low calorie diet and my exercise is under check as well””Works like a lifesaver for me but leaves me feeling veryenergetic than before. On the other hand, I have had an increased appetitesince its use””One month down but the effect is slow. Hoping to see someinches going down the drain soon””Started having extreme discomfort in stomach, diarrhea, andanxiety attacks from not being able to breathe with such a tight chest””I am taking it every morning and so far no weight loss at all””Had a bad experience with all the side effects” 12) Cetilistat potential side effects Cetilistat reported with side effects that are gastro anddigestive tract related.
· Fecal incontinence· Defecation urgency· Rectal discharge· Fatty stools· Oily stools· Malabsorption of vitamins· Deficiency of nutrients· Gallstones may develop· Renal stones can accumulate· Skin disorders· Subcutaneous tissue abnormalities· Reduction in serum concentrations of Vitamin D and E· Reduced level of beta-carotene Cetilistat is also contraindicated withwarfarin and levothyroxine as this could cause increased risk of bleeding andhypothyroidismRare· seeing, hearing, or feeling things that are not there· severe mental changesIncidents not known· anxiety· burning while urinating· chest pain or discomfort· decreased ability to exercise· difficult or painful urination· dizziness· dry mouth· fainting· fast, irregular and racing heartbeat· pounding pulse· tachycardia· the feeling of warmth· a headache· hyperventilation· increased need to urinate· irritability· nausea· numbness or tingling in the limbs or legs· pain or discomfort in the arms, jaw, back or neck· passing urine more often· redness of the face, neck, arms, and, occasionally, upper chest· restlessness· shakiness in the legs, arms, hand or feet· shortness of breath· sweating· swelling of the feet or lower legs· trembling or shaking of the hands or feet· possible trouble in breathing· disturbance with sleeping· difficulty with thinking,speaking or walking· vomiting weaknessSymptoms of overdose· abdominal or stomach cramps· blurred vision· change in consciousness· convulsions· diarrhea· discouragement· dizziness, faintness, or lightheadedness when getting up suddenly fromlying or sitting position· fast, slow, or irregular heartbeat· feeling sad or empty· lack of appetite· lightheadedness· loss of consciousness· loss of interest or pleasure· overactive reflexes· panic· physical attempt to injure· pounding in the ears· rapid breathing· sweating· tiredness· possible trouble with concentration· unusual tiredness or weakness· violent actionsIncidents not known· decreased interest in sexual intercourse· difficulty having a bowel movement (stool)· inability to have or keep an erection· increase in sexual ability, desire, drive or performance· increased interest in sexual intercourse· a loss in endocrinal ability, desire related to sex, drive orperformance· sleeplessness· stomach pain· unable to sleepNote:Drinking alcohol can increase some side effects of phendimetrazine.Sideeffects for Healthcare professionals may include:(Frequencyis not reported)Cardiovascular; Valvular heart disease,palpitation, tachycardia, elevated blood pressure, ischemic events andflushing.Respiratory, Pulmonary Hypertension.
Psychiatric; Psychotic state,insomnia, agitation, libido changes.Nervous System; Overstimulation,restlessness, tremor, dizziness, headache.Gastrointestinal; dry mouth, stomachpain, diarrhea, constipation.Genitourinary: Urinary frequency,dysuria.Ocular; Blurred vision.
Dermatologic: Sweating. 13) Cetilistat warningsAsCetilistat is in experimental trials, there is no care or usefulness profilefor this medication. People in certain inhabitants, however, could face severehealth dangers if consuming Cetilistat. For instance, people having transplantscould suffer from organ rejections if they take these anti-rejectionmedications.It isrecommended that you consult with your physician or private doctor before youuse the drug as treatment for your diseases.
Consuming it without consultationor knowing the after effects of the medicine can result in a number of problemswhich can be disastrous. In order to keep yourself protected and out of danger,you need to be aware of certain health frauds such as:· Assurancesof an “easy” solution for cases like over-weight, hair loss, orimpotency.·Statements such as “technical innovation,” “amazingtreatment,” “secret elements,” and “ancientmedication.”·Using terminologies such as “hunger motivation area” and “thermogenesis”for a weight reduction product.·Guarantees that the drug is safe as it is a combination of natural ingredients.·Falsely advertisements done by doctors and professionals just for money.
·Using experience of previous customers in order to penetrate and develop themarket.·Making people think that their product is free of any harmful effects(Citeurl: http://www.fda.gov/drugs/resourcesforyou/consumers/questionsanswers/ucm136187.htm ) Any kind of drug or medicine that is labeled as supplement orotherwise should undergo tests by the Food and Drug Authority. Marketing of thedrugs is approved after proper research, survey and experimentation.
Distributorsmust be aware of the authenticity of the manufacturer before purchasing theirproducts and not get mislead. Any labeled supplement that contains the drugsibutramine is not categorized as a dietary supplement. 14) Cetilistat alternatives · Serotonin and nor adrenaline reuptake inhibitors (anorecticagents)· Endocannabinoid receptor antagonist· Lipase inhibitors like Orlistat· b 3-adrenoreceptor agonists· Leptin agonists· Melanocortin-3 agonists (Citeurl: http://www.
gov/pubmed/25100293 ) 15) Cetilistat pricePrice of the tablet ranges from $15.90 for apack of ten capsules of 60mgCiteurl:https://www.unitedpharmacies-uk.md/Akumentis Healthcare is anactive seller of the medication.Cetilistat is recommended after theprescription of a doctor.
It is available in strengths of 60mg, 80mg 120 mg.Packaging includes ten tablets.(citeurl: https://pubchem.ncbi.nlm.
nih.gov/compound/Cetilistat#section=Chemical-Vendors/ ) 16) LawsuitsNolawsuits have been reported against the use of the product so far.