Cetilistat results. (Citeurl: http://www.fda.gov/drugs/resourcesforyou/consumers/questionsanswers/ucm136187.htm ) Cetilistat is used

Cetilistat

 

 

1) What is Cetilistat?

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Cetilistat, under the brand name (CETISLIM, CHECKWT or KILFAT)
is a new drug that is currently undergoing experimentation and clinical trials
in various parts of the world for its effectiveness. Cetilistat is classified
under the “anti-obesity or anorectic drugs” category. Obesity happens to
be one of the major issues of the modern times, mostly in the developing &
industrialized countries. Statistics suggest that the number of deaths and
diseases reported worldwide by obesity and overweight are higher than those
calculated by underweight.

Cetilistat is an intra-orally active anti-obesity drug. It
primarily functions as a gastrointestinal and pancreatic lipase inhibitor. It
is also experimented with the treatment of Diabetes Mellitus (DM) especially
type 2 with successful results.

(Citeurl: http://www.fda.gov/drugs/resourcesforyou/consumers/questionsanswers/ucm136187.htm )

Cetilistat
is used as a supplement to diet and exercise for a short term in the treatment
of obesity. Cetilistat is also used for purposes that are not found in the
medication guide.

Cetilistat
is an experimental anti-obesity drug and is currently being researched on in
the 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?

According
to the rising numbers of patients suffering from obesity and prevalence of
associated risks increasing, weight management has become an essential part of
a healthy lifestyle. The focus is mainly on modifications in lifestyle. It can
be achieved by consuming balanced nutrition, reducing the intake of saturated
fat, shifting to a diet that has moderate levels of calories and increasing
one’s physical activity.

Along
with the above-mentioned measures, pharmacological options are used. The availabilities for weight management are limited
right now. A few of the common ones are Orlistat (pancreatic and gastric
lipase inhibitor). Phentermine (sympathomimetic drug) is used but not approved
in all countries for treatment of obese patients, diagnosed or not diagnosed
with diabetes. Sibutramine (a reuptake inhibitor that works in combination of
both serotonin and nor epinephrine) it acts on the central nervous system to
increase satiety. Rimonabant (Cannabinoid 1 receptor blocker) which was
recently eliminated from the market. Cetilistat,
noble drug, is a highly lipophilic benzoxazinone inhibitor of pancreatic and gastric
lipases, it is currently undergoing development for the management of weight in
obese patients with or without any concerning medical complications. 

Cetilistat (ATL-962) was
initially developed by Alizyme, a company specializing in biopharmaceuticals in
collaboration with Takeda Pharmaceutical. The global rights of the drug are
transferred to “NORGINA BV” after
Alizyme shifted to administration. (Citeurl: http://en.wikipedia.org/wiki/Cetilistat )

In December 2008, A Phase III
clinical study of Cetilistat was started by Takeda in Japan. As a result of
progress to pivotal Phase III trials, Phase II clinical trials were encouraged.
The survey showed significant weight loss by the use of Cetilistat. It was also
well tolerated in patients suffering from obesity clinically. The drug
therefore got promoted.

In August 2003, Takeda
evaluated Phase II of European data and in January 2004 in collaboration with
Alizyme agreed  to exclusively develop,
generate, manufacture and distribute Cetilistat in Japan. Takeda submitted a
New Drug Application (NDA) in October 2012 to Japan’s Ministry of Health,
Labour and Welfare for Cetilistat as the treatment of obesity. The company’s development
and research are focused on the treatment of GI disorders, cancer, diabetes and
obesity.

(Citeurl: http://www.drugdevelopment-technology.com/projects/cetilistat/)

 

 

 

 

3) Ingredients of Cetilistat

“Cetilistat” itself
is the active salt ingredient that markets in the form of “Citislim Tablet.”

Salt – 60mg

Molecular
formula:  C25H39NO3

IUPAC
Name

2-hexadecoxy-6-methyl-3, 1-benzoxazine-4-one

MESH
names

1. 
2-(hexadecyloxy)-6-methyl-4H-3,1-benzoxazine-4-one

2. 
ATL-962

3. 
Cetilistat

 MOLECULAR
WEIGHT: 401.591
g/mol

 

https://pubchem.ncbi.nlm.nih.gov/compound/Cetilistat#section=Pharmacology-and-Biochemistry

 

 

 

4) Does Cetilistat work?

There have been limited
reviews regarding the user of the drug since it’s still under research and
experimentation. There is no guarantee given that the medicine will work for
all. Diet and exercise have to be added along with its use. It can only be
prescribed by a doctor and is formulated for short-term use. The formula is not
very long lasting and changes need to be kept without support from the drug.
Prolonged intake can cause addiction. It also leads to gastrointestinal
complications.

The substance may reduce the
appetite of obese patients. There are many other facets of weight loss that have
not been addressed, such as metabolic rate and thermogenesis. Moreover,
Cetilistat has its fair share of side effects that come along with its use. Not
only does it limit the people who may want to use this product, but the
potential for abuse makes the potential audience even narrower. While trying to
manage weight to a healthy level, it sometimes becomes imperative that people
understand that sacrifices need to be made to get results. However, your
overall well-being shouldn’t be one of those things.

The updated research suggests
that Cetilistat is tolerated well as compared to the widely available Orlistat
which is also a lipase inhibitor.

 

5) Cetilistat Benefits and Results

·        
Treatment of obesity

·        
Treatment of Diabetes Mellitus

·        
Treatment of dyslipidemia

·        
Reduction in body weight

·        
Improvement in glycemic levels of diabetic patients

·        
Well tolerated compared to other drugs

 

According
to a study published by Peter Kopleman in the year 2010, Cetilistat is
tolerated more than Orlistat with fewer gastrointestinal complications.

A
survey was carried out for 2 weeks where patients were randomized to placebo. Cetilistat
in dosages of 40, 80, or 120 mg thrice daily or Orlistat 120 mg three times a
day for 12 weeks. The initial endpoint was evident change in body weight
compared to where we started from. Secondary endpoints demonstrated other
variations in glycemic control and obesity. Reductions in body weight were
similar in patients who were given Cetilistat in dosages of 80 or 120 mg t.i.d.
or Orlistat in dosage of 120mg.

Significant
reductions are observed with drugs vs. placebo (3.86 kg, P = 0.02;
4.33 kg, P = 0.0003; 3.79 kg, P = 0.009). In
the 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 the
placebo and Orlistat groups. Discontinuation due to gastrointestinal adverse
effects was significantly worse in the Orlistat group compared to the 120 mg Cetilistat
and placebo groups. Significant reductions in body weight were found with the
intake 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 were
similar in placebo due to adverse effects.

 

 

6) Cetilistat and weight loss?

Cetilistat is a lipase inhibitor, which has a similar mode
of action to Roche’s anti-obesity Orlistat (Xenical) which in 1997 received
regulatory approval. These drugs act in the gastrointestinal tract to inhibit lipases
that are enzymes responsible for the breakdown of dietary fats. By inhibiting
the dissolution and subsequent digestion of fats from the intestine, these
inhibitors reduce fat intake and calories, therefore aiding in weight loss. In
short, it results in weight loss and
absorbs lipids from food. This drug acts peripherally on the system to reduce
the appetite, without affecting or damaging the brain.

 

7) How to use Cetilistat?

Consult
with your medical doctor or your physician before intending to start with the
medication. It is not advisable to adjust dosage for yourself. Cetilistat needs
to be taken as prescribed by the doctor. It is advised not to take it in larger
or smaller 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.). Any
concerning genetic disorders or familial history, any allergies, pre-existing
diseases, and current health conditions (e.g., pregnancy, lactation, upcoming
surgery, etc.). Some chronic or acute health conditions may make you more
susceptible to the side-effects of the drug. Use as directed by your doctor or
follow the direction printed on the product insert. Dosage is dependent on your
condition. Tell your doctor if your condition persists or worsens. Essential
counseling points are listed below.

·      
Consult
your doctor if suffering from diabetes or taking other herbal or nutritional
products

·      
Take the tablet at least 1
hour  after the meal or during the meal

·      
Dosages of 60-100 mg are
usually prescribed. Do not exceed unless advised.

·      
Eat a healthy diet and
keep yourself hydrated

·      
Control your fat intake
while using this drug, a hypo caloric diet is recommended.

·      
Increase your physical
activity during the period of utilizing the medication

·      
Cetilistat
is also contraindicated with warfarin and levothyroxine as this could cause
increased risk of bleeding and hypothyroidism

·      
If taking cyclosporine or levothyroxine,
separate administration of those drugs and this drug by minimum 4-5 hours.

 

 

(Citeurl: http://www.tabletwise.com/cetislim-tablet)

 

 

 

Storage
of Cetislim Tablet

·        
The tablets
should be preserved and stored at room temperature.

·        
 Keep them away from any heat or exposure to
direct light. Do not freeze tablets unless mentioned by package insert. Strictly keep medicines away from children and pets.

·        
Do not flush medications
down the toilet or pour them into drainage unless instructed to do so. Medicines discarded
in this manner contaminate the environment. Kindly consult with your physician
or pharmacist for more details on how to safely remove  Cetislim
Tablet.

(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 as
possible. 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 forget
to take it during mid-treatment, the effectiveness reduces. Some patients show
signs of early withdrawal from a drug if consistent doses dosages are missed.

·       If a dose is missed, take it at the earliest when
you remember.

·       If you recall that you’ve missed a dose and it’s
time for your next dose, then do not take it till an hour before your next
scheduled dose.

·       An extra dose should not be taken to make up for
a missed dose.

·       Resume your schedule of doses after the next
dose.

·       If you have difficulty taking it on time, set
yourself a reminder on phone or alarm.

·       Ask members of family to keep you reminded.

·       Kindly refer to a doctor to issue you a new
schedule or change your dosage routine and adjust it to your convenience to
make up for the doses missed.

 

.

 (Citeurl: http://www.pharmacy.ca.gov/publications/miss_dose.pdf )

(Citeurl: http://www.nhs.uk/chq/Pages/860.aspx?CategoryID=73 )

 

 

9) What happens if you overdose?

·        
Be very careful when you
start your medication and ask your pharmacist how and when to use them.

·        
The effectiveness of the
medicine does not improve if you take it in larger quantities than
prescribed. Neither will one achieve results quicker if you use the drug
in more quantity or shorter intervals.

·        
Increase quantities cause
severe adverse effects and poisoning to the system.

·        
Overdose results in
complications that can be fatal.

·        
Seek medical help from the
nearest health centre or emergency immediately if you feel that you or anybody
has overdosed on Cetilistat medicine.

·        
 Bring a medicine box, container, or label with
you to help doctors with necessary information.

·        
Do not give your medicines
to 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 your
physician or pharmacist for product information.

(Citeurl: http://www.emedicinehealth.com/drug_overdose/article_em.htm )

 

 

10) Usage in children

After
the appropriate consideration and evaluation of the medical condition of a
child or adult, the options available should be discussed before proceeding
with any sort anti-obesity drugs. The first line of treatment should, however,
be diet, exercise and lifestyle modifications. After trying all these
diligently, if no response is appreciated or is inadequate we opt towards the
rigorous therapy.

Children,
especially during their puberty, are not encouraged to use these drugs as it
can have potential effects on their
height and growth. Treatment if not producing results otherwise can be
delayed untill 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 days
since I’ve been using this medicine. Feel great about the results. Never felt
better. 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 very
energetic than before. On the other hand, I have had an increased appetite
since its use”

“One month down but the effect is slow. Hoping to see some
inches going down the drain soon”

“Started having extreme discomfort in stomach, diarrhea and
panic attacks”

“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 and
digestive 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 with
warfarin and levothyroxine as this could cause increased risk of bleeding and
hypothyroidism

Rare

·      
seeing, hearing, or feeling things that are not there

·      
severe mental changes

Incidents 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 weakness

Symptoms of overdose

·      
abdominal or stomach cramps

·      
blurred vision

·      
change in consciousness

·      
convulsions

·      
diarrhea

·      
discouragement

·      
dizziness, faintness, or lightheadedness when getting up suddenly from
lying 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 actions

Incidents 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 or
performance

·      
sleeplessness

·      
stomach pain

·      
unable to sleep

Note:
Drinking alcohol can increase some side effects of phendimetrazine.

Side
effects for Healthcare professionals may include:

(Frequency
is not reported)

Cardiovascular; Valvular heart disease,
palpitation, tachycardia, elevated blood pressure, ischemic events and
flushing.

Respiratory, Pulmonary Hypertension.

Psychiatric; Psychotic state,
insomnia, agitation, libido changes.

Nervous System; Overstimulation,
restlessness, tremor, dizziness, headache.

Gastrointestinal; dry mouth, stomach
pain, diarrhea, constipation.

Genitourinary: Urinary frequency,
dysuria.

Ocular; Blurred vision.

Dermatologic: Sweating.

 

 

13) Cetilistat warnings

As
Cetilistat is in experimental trials, there is no care or usefulness profile
for this medication. People in certain inhabitants, however, could face severe
health dangers if consuming Cetilistat. For instance, people having transplants
could suffer from organ rejections if they take these anti-rejection
medications.

It is
recommended that you consult with your physician or private doctor before you
use the drug as treatment for your diseases. Consuming it without consultation
or knowing the after effects of the medicine can result in a number of problems
which can be disastrous. In order to keep yourself protected and out of danger,
you need to be aware of certain health frauds such as:

· Assurances
of an “easy” solution for cases like over-weight, hair loss, or
impotency.

·
Statements such as “technical innovation,” “amazing
treatment,” “secret elements,” and “ancient
medication.”

·
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 the
market.

·
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 or
otherwise should undergo tests by the Food and Drug Authority. Marketing of the
drugs is approved after proper research, survey and experimentation. Distributors
must be aware of the authenticity of the manufacturer before purchasing their
products and not get mislead. Any labeled supplement that contains the drug
sibutramine is not categorized as a dietary supplement.

 

14) Cetilistat alternatives

 

·        
Serotonin and nor adrenaline reuptake inhibitors (anorectic
agents)

·        
Endocannabinoid receptor antagonist

·        
Lipase inhibitors like Orlistat

·        
b 3-adrenoreceptor agonists

·        
Leptin agonists

·        
Melanocortin-3 agonists

 

 

 

(Citeurl: http://www.ncbi.nlm.nih.gov/pubmed/25100293 )

 

 

 

15) Cetilistat price

Price of the tablet ranges from $15.90 for a
pack of ten capsules of 60mg

Citeurl:https://www.unitedpharmacies-uk.md/

Akumentis Healthcare is an
active seller of the medication.

Cetilistat is recommended after the
prescription 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) Lawsuits

No
lawsuits have been reported against the use of the product so far.