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NEWER TRENDS IN

ANTIOBESITY DRUGS
By : - Sandesh.
Harakchand. Jain.
Guided by : - Mrs. Vidula
Damle
INDEX

INTRODUCTION TO OBESITY
MEASUREMENT OF OBESITY
FEATURES OF OBESITY
FACTORS CAUSING OBESITY
RISK FACTOR OF OBESITY
EFFECT OF OBESITY ON BODY
TREATEMENT AVAILABLE
REFERENCE
INTRODUCTION TO OBESITY
• DEFINITION : - Obesity is term to describe body weight
i.e. much higher than what considered healthy.
• An obese person has 50 – 100 % of increase chance of
premature death than normal person.
• In India 30000/year death occurs due to obesity. Obesity
increase the rate of other chronic disease.
• In India 6% total health cost spend on treatment of
obesity.
• Alternate names : - Obese, Sthaulya, Overweight.
MEASUREMENT OF OBESITY
 The obesity can be measured by various
methods, but experts says body mass
index measurement is most accurate
measure to check body fat.
 BMI Can be defined as measurement of
body fat on basis of weight & height
measurement.
 A person is said to be obese when his BMI
is more than 30.
 BMI is measure in two ways this are : -
 1) By BMI calculator
 2) By visualizing directly from BMI Table
BMI CATEGORY
 CATEGORY  BMI

 UNDER  12 – 18.9
WEIGHT  18.9 – 24.9
 NORMAL  24.9 – 29.9
WEIGHT  29.9 > 30
 OVERWEIGHT  < 35
 OBESE
 MORBIDLY
OBESE
FEATURES OF OBESITY

• Sluggish movement
• Debility
• Excessive hunger
• Excessive thirst
• Short life span
• Increase in blood pressure
• Psychological consequences
CAUSES OF OBESITY
 Genes & metabolism
 Culture
 Environment
 Large food intake
 Secondary lifetime
EFFECT OF OBESITY ON BODY
RISK FACTOR OF OBESITY
 LIFE THREATING  Others
 Hypertension  Menstrual
 Diabetics abnormalities
 Arthrosclerosis  Pregnancy
 Heart failure complications
 Stroke
 Osteo arthritis
 Flat feet
 Renal failure
 Gallbladder disease
 Cancer
TREATEMENT OF OBESITY
 The treatment is depend on following factors:-
2) Actual BMI
3) Presence of central distribution of fat
4) Presence of other coronary disease
 For treatement combined approach are
required : -
f) Physiological measures
g) Pathological measures
PHYSIOLOGICAL APPROACH
► Behavior modification
► Diet
► Exercise
► Control of body weight
PATHOLOGICAL APPROACH
 Surgery : - It is done for person who
are significantly obese i.e. having
BMI more than 35. There are two
type of surgery available: -
2) Rouxeny gastric bypass surgery
3) Adjustable gastric binding
ROUXENY BYPASS SURGERY
BY USING FDA APPROVED
DRUGS
1) Orlistat

1-(3-hexyl-4-oxo-oxetan-2-yl)tridecan-2-yl 2-
Chemical IUPAC Name
formylamino-4-methyl-pentanoate

Chemical Formula C29H53NO5

Chemical Structure
CLINICAL PHARMACOLOGY
• M.O.A : - It is a reversible lipase inhibitor. It
exerts its pharmacological activity in the
lumen of stomach & small intestine by
forming covalent bond between active
serine residue & gastric & pancreatic
lipase.
• Absorption: - Well absorbed orally the
average absolute bio availability of intact
orlistat assessed on male rate at oral dose
of 150 – 1000mg/ kg/day & in male dog
100 – 1000mg/kg/day was found to be
0.12% - 0.59% & 0.7 – 1.9% respectively.
HOW ORLISTAT WORKS
DRUG DRUGINTERACTION
 SIDE EFFECTS : -
Bowel movement habits.

 Elimination

 Metabolism
PHENTERMINE
 DESCRIPTION : - Phentermine hcl capsules content
phentermine hcl 30mg
 Clinical Pharmacology
 M.O.A : - It is sympathominetic amine which have
pharmacological activity similar to pro drug amphetamines.
Action include C.N.S & elevation of blood pressure.
 Drug interaction : - Alcohol interaction
 Overdose : overdose include
tremor,restlessness,hyperreflexia,hallucination,fatique,isomia,
hypertension etc.
 Dosages:one cap to be taken two hours before milk and
evenning administration at night should be inhibited.
 Sideeffect:include cardiovascular:palpitation,tachycardia.
CNS:Isomia,dizziness,headache etc
G.I.T:Dryness of mouth.
Iv of phenotamine has been sujjested for severe s.i.
SIBUTRAMINE
DESCRIPTION
Chemically it is a racemic mixtures of the
(+) & (-) & enatiomers of
cyclobutanemethanamine.
Empirical formula: - C17H29 C12NO
Molecular weight : - 334.33
CLINICAL PHARMACOLOGY
 M.O.A :- Produces therapeutic effect by serotonin
dopamine & nor epinephrine reuptake inhibition
 Pharmacodynamics : - Act by secondary (M1) & primary
(M2) amine.It is potent inhibitor of serotonin &
norpinephrine in vivo not invitro. But its metabolities are
capable of inhibiting both in vivo& invitro.In in
humenbrain M1&M2 are inhibitng dopamine.
 Absorption :Tmax(1.2 hours) on oral administration
peak plasma con. Of M1&M2 are reached with in 3-4
hours.
 Excretion:approx 85% was found to be excreated in
urine.
 Comparison : -
Name of Class Pharmacokinetics
Drug

Bioavailability % Cmax Tmax T½


(Ng/ Hour Hour
ml) s s

Sibutramine Serotunin > 97% 4 3.4 14


Inhibitor

Orlistat Lipaseinhibito < 1% < 10 2-4 1-2


r

Phenetermin CNS < 25% < 6% 1-2 1-2


e stimulants
ALTERNATE TREATEMENT

 In ayurvedic obesity is defines as excessive


physical growth of body.It is also known as
sthaulya
 It involves detoxification & cleansing of body
 Detoxification in the sense that it will remove all
toxins from the body& cleansing in sense to
cleaning of sinus.
How sthaulya is managed by ayurvedic
metods

 Heavy &non nourising food should be avoided


 Ruksha-ushna basti
 Body massage with unctous herbal powder.
 Drugs like: Guduchi, Mukta,Haritaki,Bibitaki,Amalaki.
 Others:Takrarista,Hooney,Shilajatu,vidanji
lauha,phycical&mental exercise.
Yoga is a form of exercise
which help in physical & mental
strength.
There are various type of asana
involve in yoga.
HERBS AVAILABLE
 Trifla: - Form of most important herbs for balancing 5
element.
 Instructions : - 1 tea spoon at bedtime

 Somalatarasayana : - It is form of food jam consisting of


herbs & spices in a base of honey, rice syrup & ghee.
Dos (pathya)
Ayurvedic advocates specific dietary and lifestyle
changes for sthaulya.
Dietary :Fresh healty food at regular interval.
low fat diet
high fiber diet
plenty of fresh vegetable fruits.
Lifestyle :gradual increase in night awakening
physical exercise, mental exercise, strong
motivation.
Don'ts (apatya)
Dietary: Life style
Over eating Day sleep.
Heavy,sweets,cold Physical rest.
unctous food. Mental rest.
Fried food. Sluggish routine.
Preserved,canned
food

REFERENCE
Introduction to Pharamacology : 10th edition, Drug
that effect the
digestive system – Absorption inhibitor, Issue year
2005, By Mary Kaye Asperheim : Pub. Elseveir
Saunders. Page no. 148.
– Pharamacology : 2nd edition, Drug abuse – CNS
Stimulant page no. 279-
280. By George M. Brenner, & Creig. W. Stevens. Pub.
Elseveir Saunders. Page no. 279-280.
– Essentials at Medical Pharamacology : 5th edition
Drug Acting on CNS
In-central use . By K.D. Tripati. Pub. Jaypee Page no.
118.
– Integrated Pharmacology: 2nd edition, Drug use in
Disorder of Nutrition
Obesity. By Page, Curtis, Sutter, Walker, Hoffman. Pub.
Elseveir Mosby. Page no. 566-568.
– Pathologic Basic of Disease : 7th edition – Enviorment
& nutritional
 Modern Pharmacology with clinical pathology
: 6th edition- CNS
 stimulant in Analeptic stimulant. By
David A Taylor, Charles R Craig & Robot
published by lippincot. William &
Willinkins.
 Clinical Pharmacology : 9th edition diabetes
mellitus, obesity- obesity &
 appetite control. By Bannett, M.J.
Brown.
 Pub. Churchil Livingstone Page no. 696-
698.
 Pharmacological basis of therapeutics : 9th
edition, Drug acting at
 synaptscs. By Goodman & Gillman.
Page no. 219-220.
 Clinical Pharmacy & therapeutic : 3rd edition,
Endocrene disorder. By
 Roger Walker, Clive Edward. Pub.

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