Newer Trends In Anti Obesity Drugs 03

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 

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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

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BMI

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UNDER WEIGHT NORMAL WEIGHT OVERWEIGHT OBESE MORBIDLY OBESE

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12 – 18.9 18.9 – 24.9 24.9 – 29.9 29.9 > 30 < 35

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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 Hypertension Diabetics Arthrosclerosis Heart failure Stroke Renal failure Gallbladder disease Cancer

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Others Menstrual abnormalities Pregnancy complications Osteo arthritis Flat feet

TREATEMENT OF OBESITY  2) 3) 4) 

The treatment is depend on following factors:Actual BMI Presence of central distribution of fat 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 

2) 3)

Surgery : - It is done for person who are significantly obese i.e. having BMI more than 35. There are two type of surgery available: Rouxeny gastric bypass surgery Adjustable gastric binding

ROUXENY BYPASS SURGERY

BY USING FDA APPROVED DRUGS 1)

Orlistat

Chemical IUPAC Name

Chemical Formula

Chemical Structure

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

C29H53NO5

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 

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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 Drug

of Class

Pharmacokinetics

Bioavailability %

Cmax (Ng/ ml)

Tmax Hour s

T½ Hour s

Sibutramine

Serotunin Inhibitor

> 97%

4

3.4

14

Orlistat

Lipaseinhibito r

< 1%

< 10

2-4

1-2

Phenetermin CNS e stimulants

< 25%

< 6%

1-2

1-2

ALTERNATE TREATEMENT

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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: Over eating Heavy,sweets,cold unctous food. Fried food. Preserved,canned food

Life style Day sleep. Physical rest. Mental rest. Sluggish routine.

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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. 279280. 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

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stimulant in Analeptic stimulant. By David A Taylor, Charles R Craig & Robot published by lippincot. William & Willinkins. 

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Pharmacological basis of therapeutics : 9th edition, Drug acting at

synaptscs. By Goodman & Gillman. Page no. 219-220. 

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Clinical Pharmacology : 9th edition diabetes mellitus, obesity- obesity &

appetite control. By Bannett, M.J. Brown. Pub. Churchil Livingstone Page no. 696698. 

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Modern Pharmacology with clinical pathology : 6th edition- CNS

Clinical Pharmacy & therapeutic : 3rd edition, Endocrene disorder. By

Roger Walker, Clive Edward. Pub.