Appetite stimulants and suppresents: its complete descrtiption, uses and side effects with note on assessment

1. Dr. KRVS Chaitanya
R
APPETITE
STIMULANTS
& SUPPRESENTS
Dr. Koppala RVS Chaitanya
Department of Pharmacology

2. Dr. KRVS Chaitanya
APPETITE STIMULANTS
Orexigenices agents
 Drug, hormone or compound that stimulate appetite and induce hyperphagiz, this can
be medication or naturally occurring neuropeptide hormone such as Ghrelin, Ovexin
and Neuropeptide Y, that increase hunger and increase food consumption.
Indications:
 Appetite loss of muscle wasting due to cystic fibrosis, anorexia, old age and cancer or
AIDS.
 Used in depression, grief of sadness, first trimester pregnancy, nausea, vomiting,
dementia, colon/ovarian/stomach/pancreatic cancers, liver or kidney cancers, HIV,
hepatitis, COPD, drug use, hypothyroidism.
Appetite stimulants are medications prescribed to increase appetite and improve the
nutritional status of patients experiencing severe weight loss associated with certain chronic
illnesses. The FDA-approved appetite stimulant is megestrol acetate, a progestin, which is a
synthetic derivative of progesterone, the natural female sex hormone.
Megestrol acetate was originally developed as a contraceptive, but the side effect of weight
gain led to its use as an appetite stimulant. Megestrol acetate prevents ovulation and the
release of estrogen from the ovaries and is also used in palliative care for advanced stages of
endometrial and breast cancers.
It is not clear how exactly megestrol increases appetite. Studies suggest that progesterone
plays a major role in reducing inflammation and improving nutritional status in the late stages
of pregnancy. It is believed that megestrol’s anti-inflammatory activity may be a reason for
an increase in appetite, resultant weight gain, and improvement in quality of life.
Megestrol is thought to reduce inflammation by inhibiting the production of pro-
inflammatory proteins (cytokines) such as tumour necrosis factor-a, interleukin-1, and
interleukin-6. Megestrol may also stimulate the synthesis, release, and transport of
neuropeptide Y, a peptide in the brain that stimulates appetite.
Examples:
1. 5HT2C Receptor antagonists
Mirtazapine,
Olanzapine,
Quetiaprine,
Amitriptyline,
Cyproheptadine,
Luvaridone,
Pizotifen.

3. Dr. KRVS Chaitanya
2. H1 Receptor antagonists Pizotifen
3. Dopamine antagonists
Haloperidol,
Chlorpromazine,
Risperidone
4. Adrenergic antagonists
Propranolol,
Salbutamol,
Flerobuterol,
Zilpaterol,
Clonidine.
5. CB1 Receptor agonist
Dronabinol,
Nabilone
6. Corticosteroids
Dexamethasone,
Prednisolone,
Hydrocorticsone
7. Anabolic steroids
Oxandrolone,
Boldenone,
Testosterone
8. Sulfonylurea
Glibenclamide,
Chlorpropamide,
Tolbutamide
9. Mood stabilizers
Lithium,
Valproate,
Carbamazepine,
Gabapentin
10. Ghrelin Receptor agonist
Anamorelin,
GHRP-6,
Ibutamoren,
Ipamorelin,
Pralmorelin.
11. MC4 receptor antagonist Melanocortin 4
12. Miscellaneous
Insulin,
zinc,
Megestrol acetate,
Vitamin B1,
Omega-3-FA,
Bitter herbs.
HOW ARE APPETITE STIMULANTS USED?
Appetite stimulants are oral tablets and suspensions used to stimulate appetite in the
following conditions:
FDA-Approved
 The FDA has approved megestrol acetate, oxandrolone, and dronabinol as appetite
stimulants

4. Dr. KRVS Chaitanya
 Acquired immune deficiency syndrome (AIDS)-related anorexia (loss of appetite) and
cachexia (a wasting syndrome that causes significant weight loss, resulting in extreme
weakness)
Palliative treatment of advanced disease in:
 Breast cancer
 Endometrial cancer
WHAT ARE SIDE EFFECTS OF APPETITE STIMULANTS?
Side effects of appetite stimulants may include the following:
 Hypertension (high blood pressure)
 Insomnia
 Mood swings
 Rash
 Sweating, hot sweats
Menstrual disorders such as:
 Amenorrhea (absence of menstruation)
 Breakthrough bleeding
 Change in menstrual flow
 Spotting
 Impotence
Gastrointestinal issues such as:
 Diarrhea
 Flatulence
 Indigestion
 Nausea
 Vomiting
 Weight gain
Blood coagulation disorders such as:
 Deep vein thrombosis (blood clot formation in deep veins)
 Pulmonary embolism (blood clot in lungs)
 Thrombophlebitis (inflammation of veins with blood clots)
 Anemia (low red blood cell count)
 Adrenal insufficiency (a condition in which the adrenal gland doesn’t produce enough
hormones)
 Asthenia (abnormal weakness)
 Overdose may cause:

5. Dr. KRVS Chaitanya
 Shortness of breath
 Cough
 Unsteady gait
 Listlessness
 Chest pain
APPETITE SUPPRESSANTS:
INTRODUCTION:
Obesity and overweight have become global health concerns, driving the search for effective
weight management strategies.
Appetite suppressants are one such strategy, aiming to regulate food intake and promote
weight loss.
This lecture will explore the mechanisms of appetite regulation, the efficacy of appetite
suppressants, and safety considerations associated with their use.
I. Appetite Regulation Mechanisms:
A. Neural Regulation:
1. Hypothalamus: Key center for appetite regulation, integrating signals of hunger and
satiety.
2. Neurotransmitters: Dopamine, serotonin, and norepinephrine influence appetite by
modulating neural pathways.
B. Hormonal Regulation:
1. Leptin: Produced by adipose tissue, signals satiety and regulates long-term energy
balance.
2. Ghrelin: Secreted by the stomach, stimulates appetite and promotes food intake.
C. Gut-Brain Axis:
1. Gut hormones such as peptide YY (PYY) and glucagon-like peptide-1 (GLP-1)
communicate with the brain to regulate appetite.
II. Types of Appetite Suppressants:
A. Pharmaceutical Agents:
1. Stimulants: Examples include amphetamines and phentermine, which act on
neurotransmitter pathways to suppress appetite.
2. Serotonin Modulators: Drugs like sibutramine inhibit serotonin reuptake,
promoting satiety.
3. GLP-1 Agonists: Mimic the action of GLP-1 to enhance satiety and reduce food
intake.

6. Dr. KRVS Chaitanya
B. Natural Compounds:
1. Fiber: Increases feelings of fullness and promotes weight loss by reducing calorie
intake.
2. Plant Extracts: Compounds like Hoodia gordonii and Garcinia cambogia have been
studied for their potential appetite-suppressing effects.
III. Efficacy of Appetite Suppressants:
A. Short-Term Efficacy:
1. Many appetite suppressants show effectiveness in reducing food intake and
promoting initial weight loss.
B. Long-Term Efficacy:
1. Mixed results exist regarding the sustainability of weight loss with appetite
suppressants.
2. Adherence to lifestyle modifications is crucial for long-term success.
IV. Safety Considerations:
A. Side Effects:
1. Common side effects include insomnia, dry mouth, and gastrointestinal
disturbances.
2. Stimulant-based appetite suppressants may carry a risk of addiction and
cardiovascular complications.
B. Drug Interactions:
1. Potential interactions with other medications should be carefully evaluated.
C. Regulatory Oversight:
1. FDA regulations govern the approval and monitoring of pharmaceutical appetite
suppressants.
D. Patient Selection and Monitoring:
1. Healthcare providers should assess individual risk factors and monitor patients
closely during treatment.
Appetite suppressants offer a potential tool for weight management but require careful
consideration of their mechanisms, efficacy, and safety profiles. A comprehensive
understanding of appetite regulation mechanisms and individual patient factors is essential
for informed decision-making and successful outcomes. Further research is needed to
optimize the efficacy and safety of appetite suppressants, ensuring their role as part of a
multifaceted approach to combating obesity and promoting overall health.

7. Dr. KRVS Chaitanya
Examples:
 Chitosan
 Chromium picolinaet
 Linoleic acid
 Glucomannan
 Guar gum
 Green tea extract
 Green coffee extract
 Hoodia
 7-Keto DHEA
 Ephedra
 Bitter orange
 Diethyl propion
 Liraglutide
 Naltrexone – bupropion
 Phendimetrazine
 Phenteramine
 Phenteramine topiramate
 Nopal
 L cantitine fumarate
 Vitamin B16, B12
 Orlistat
 Semaglutide
 Setmelanotide
Contraindications:
 Glaucoma
 Heart disease
 Hyperthyroidism
 Liver disease
 BMR/BMI < 30
Indication
 BMI > 30 (obesity)
 BMI > 27 + Diabetes, High blood pressure

8. Dr. KRVS Chaitanya