This document provides an overview of antidiabetic drugs, classifying them based on their mechanisms of action and summarizing their uses, side effects, and contraindications. The main classes described include biguanides (e.g. metformin), sulfonylureas, meglitinides, incretin mimetics, DPP-4 inhibitors, SGLT-2 inhibitors, alpha-glucosidase inhibitors, and thiazolidinediones. Metformin is noted as the first-line oral medication for type 2 diabetes due to its efficacy, safety profile, and cost-effectiveness. All antidiabetic drugs require careful consideration of risks like hypoglycemia and drug interactions when prescribing based on a
Sitagliptin an oral anti-diabetic agentAmruta Vaidya
A concise presentation on the DPP-IV inhibitor Sitagliptin an oral anti-diabetic agent. Its general mechanism of action, pharmacokinetics, safety is included.
Manish yadav .M Pharm First year
Pharmacology . Under -guidence of
Professor Dr. Govind Singh .
M.D.University Rohtak
Department Pharmaceutical science
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
Ozempic: Preoperative Management of Patients on GLP-1 Receptor Agonists Saeid Safari
Preoperative Management of Patients on GLP-1 Receptor Agonists like Ozempic and Semiglutide
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MANAGEMENT OF ATRIOVENTRICULAR CONDUCTION BLOCK.pdfJim Jacob Roy
Cardiac conduction defects can occur due to various causes.
Atrioventricular conduction blocks ( AV blocks ) are classified into 3 types.
This document describes the acute management of AV block.
Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
Anti ulcer drugs and their Advance pharmacology ||
Anti-ulcer drugs are medications used to prevent and treat ulcers in the stomach and upper part of the small intestine (duodenal ulcers). These ulcers are often caused by an imbalance between stomach acid and the mucosal lining, which protects the stomach lining.
||Scope: Overview of various classes of anti-ulcer drugs, their mechanisms of action, indications, side effects, and clinical considerations.
Title: Sense of Smell
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
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The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
1. Antidiabetic Drug 2019
ANTIDIABETIC DRUG
1 Introduction:
Anti-diabetic drug, any drug that works to lower abnormally high glucose (sugar) levels in
the blood, which are characteristic of the endocrine system disorder known as diabetes mellitus.
Diabetes is caused by the body’s inability to produce or respond to the pancreatic
hormone insulin. One of the important physiological actions of insulin is to control blood
glucose levels. Glucose is an important nutrient for cellular metabolism, and cells must receive
neither too little nor too much. A deficiency in the pancreatic secretion of insulin, or lack of
tissue sensitivity to the hormone, leads to diabetes, the primary feature of which is elevated
blood glucose levels (hyperglycemia).
There are a number of different types of antidiabetic drug including:
1) Insulin
2) Pramlintide (Amylin)
3) GLP-1 receptor agonists (such as Byetta and Victoza)
4) Oral hypoglycemics (tablets)
2 Classification:
Page 1
2. Antidiabetic Drug 2019
2.1 Overview of Antidiabetic drug:
Class Mechanism of action Side effects Contraindications
Biguanide (metformin) Enhances
the effect of insulin
Lactic acidosis
Weight loss
Gastrointestinal
complaints are
common (e.g. diar
rhea, abdominal
cramps)
Reduced vitamin
B12absorption
Chronic kidney disease
Liver failure
Metformin must be
paused before
administration of
iodinated contrast
medium and major
surgery.
Sulfonylureas (e.g., glyburid
e, glimepiride)
Increase insulin secr
etion
from pancreaticβ-cel
ls
Risk
of hypoglycemia
Weight gain
Hematological
changes: agranulo
cytosis, hemolysis
Severe cardiovascular
comorbidity
Obesity
Sulfonamide allergy (par
ticularly long-acting sub
stances)
Meglitinides (nateglinide, rep
aglinide)
Increase insulin secr
etion
from pancreaticβ-cel
ls
Risk
of hypoglycemia
Weight gain
Severe renal
or liver failure
DPP-4
inhibitors (saxagliptin, sitagli
ptin)
Inhibit GLP-1 degra
dation →
promotes glucose-de
pendent insulin secre
tion
Gastrointestinal
complaints
Pancreatitis
Headache,
dizziness
Arthralgia
Liver failure
Moderate to severe renal
failure
GLP-1 agonists (incretin
mimetic
drugs: exenatide, liraglutide,
albiglutide)
Direct stimulation of
the GLP-1 receptor
Nausea
Increased risk
of pancreatitisand
possibly pancreati
c cancer
Preexisting,
symptomatic gastrointest
inal motility disorders
Page 2
3. Antidiabetic Drug 2019
SGLT-2
inhibitors(canagliflozin, dapa
gliflozin, empagliflozin)
Increased glucosuria
through the
inhibition
of SGLT-2 in the
kidney
Genital yeast infe
ctions and urinary
tract infections
Polyuria and dehy
dration
Diabetic
ketoacidosis
Chronic kidney disease
Recurrent urinary tract
infections
Alpha-glucosidase
inhibitors(acarbose)
Reduce intestinal
glucose absorption
Gastrointestinal
complaints
(flatulence, diarrh
ea, feeling of
satiety)
Any preexisting
intestinal conditions
(e.g., inflammatory
bowel disease)
Severe renal failure
Thiazolidinediones(pioglitaz
one)
Reduce insulin
resistance through
the stimulation of
PPARs (peroxisome
proliferator-activated
receptors)
Increase transcriptio
n of adipokines
Weight gain
Edema
Cardiac failure
Increased risk of
bone fractures (os
teoporosis)
Congestive heart failure
Liver failure
Amylin
analogs (pramlintide)
Reduce glucagon rel
ease
Reduce gastric
emptying
Increase satiety
Risk
of hypoglycemia
Nausea
Gastroparesis
3 Common contraindications of antidiabetic agents
● Type 1 diabetes mellitus: Patients require insulin therapy (see principles of insulin
therapy).
● Pregnancy and breastfeeding (also see gestational diabetes): All antidiabetic agents are
contraindicated. Antidiabetic drugs should be substituted with human insulin as early as
possible (ideally prior to the pregnancy).
Page 3
4. Antidiabetic Drug 2019
● Renal failure : Antidiabetic drugs that may be administered if GFR < 30
mL/min include DPP-4 inhibitors, incretin mimetic drugs, meglitinides,
and thiazolidinediones.
● Morbidity and surgery.
● Pause antidiabetic treatment in the following cases:
● Major surgery performed under general anesthesia.
● Acute conditions requiring hospitalization (infections, organ failure).
● Elective procedures associated with an increased risk of hypoglycemia (periods of
fasting, irregular food intake).
4 Insulinotropic agents
● Mechanism: stimulate the secretion of insulin from pancreatic β-cells.
● Glucose-independent: Insulin is secreted regardless of the blood glucose level, even if
blood glucose levels are low → risk of hypoglycemia.
● Sulfonylurea, meglitinides.
● Glucose-dependent: Insulin secretion is stimulated by elevated blood glucose levels
(postprandially). These antidiabetic agents depend on residual β-cellfunction.
● GLP-1 agonists, DPP-4 inhibitors.
5 Non-insulinotropic agents
● Mechanism:These agents do not depend on residual insulin production.
● Effective in patients with nonfunctional endocrine pancreatic β-cells..
● Biguanides (metformin), SGLT-2 inhibitor, thiazolidinediones, alpha-glucosidase
inhibitors.
5.1 Biguanides (Metformin)
5.1.1 Mechanism of action:
● enhances the effect of insulin.
● Reduction in insulin resistance via modification of glucose metabolic pathways.
● Inhibits mitochondrial glycerophosphate dehydrogenase (mGPD)..
● Decreases hepatic gluconeogenesis and intestinal glucose absorption.
● Increases peripheral insulin sensitivity.
Page 4
5. Antidiabetic Drug 2019
● Lowers postprandial and fasting blood glucose levels.
● Reduces LDL, increases HDL.
5.1.2 Indications: drug of choice in all patients with type 2 diabetes.
5.1.3 Clinical characteristics:
● Glycemic efficacy: lowers HbA1c by 1.2–2% over 3 months.
● Weight loss or weight stabilization.
● No risk of hypoglycemia.
● Beneficial effect on dyslipidemia.
● Studies show metformin reduces the risk of macroangiopathic complications in diabetic
patients.
● Cost-effective.
5.1.4 Important side effects:
● Metformin-associated lactic acidosis.
● Incidence: ∼ 8 cases/100,000 patient years.
● Clinical features: frequently nonspecific.
● Gastrointestinal prodromal symptoms: nausea, vomiting, diarrhea, abdominal pain.
● Severe symptoms: muscle cramps, hyperventilation, apathy, disorientation, coma.
Page 5
6. Antidiabetic Drug 2019
● High-risk groups.
● Elderly individuals.
● Patients with cardiac or renal insufficiency.
● Diagnostics.
● Arterial blood gas (ABG): metabolic acidosis and anion gap.
● ↑ Serum lactate.
● Treatment: discontinue metformin and treat acidosis.
● Gastrointestinal complaints are common: nausea, diarrhea, flatulence.
● Vitamin B12 deficiency.
● Metallic taste in the mouth (dysgeusia).
5.1.5 Contraindications:
● Renal failure (if creatinine clearance < 30 mL/min).
● Severe liver failure.
● Intravenous iodinated contrast medium.
● Pause metformin prior to surgery.
● Chronic pancreatitis, starvation ketosis, ketoacidosis, sepsis.
● Heart failure (NYHA III and IV), respiratory failure, shock, sepsis.
● Alcoholism.
5.1.6 Important interactions: sulfonylureas
5.2 Thiazolidinediones (glitazones, insulin sensitizers)
5.2.1 Active agents:
● Pioglitazone
● Rosiglitazone
5.2.2 Mechanism of action:
● Activation of the transcription
factor PPARγ (peroxisome proliferator-activated receptor of gamma type).
● ↑ Transcription of genesinvolved in glucose and lipid metabolism.
● ↑ levels of adipokines such as adiponectin.
Page 6
7. Antidiabetic Drug 2019
● ↑ Storage of triglycerides and subsequent reduction of products of lipid metabolism (e.g.,
free fatty acids) that enhance insulin resistance .
● Glucose utilization is increased and hepatic glucose production reduced.
5.2.3 Indications:
May be considered as a monotherapy in patients with severe renal failure and/or
contraindications for insulin therapy.
5.2.4 Clinical characteristics:
● Glycemic efficacy: lowers HbA1c by 1% in 3 months.
● Favorable effect on lipid metabolism: ↓ triglyceride, ↓ LDL, ↑ HDL.
● No risk of hypoglycemia.
5.2.5 Important side effects:
● Fluid retention and edema.
● Weight gain.
● Increased risk of heart failure.
● Increased risk of bone fractures (osteoporosis!).
5.2.6 Contraindications:
● Congestive heart failure (NYHA III or IV).
● Liver failure.
Page 7
8. Antidiabetic Drug 2019
● Pioglitazone: history of bladder cancer or active bladder
cancer; macrohematuria of unknown origin.
5.3 Sulfonylureas
5.3.1 Active agents:
● Glyburide: the standard substance of this class with a relatively long half-life.
● Glipizide: a short-acting agent.
5.3.2 Mechanism of action:
● Sulfonylureas block ATP-sensitive potassium channels of the pancreatic β-cells.
● Depolarization of the cell membrane.
● Calcium influx.
● Insulinsecretion.
● Extrapancreatic effect: decreases hepatic gluconeogenesis and increases
peripheral insulin sensitivity.
Page 8
9. Antidiabetic Drug 2019
5.3.3 Indications:
Particularly suitable for patients who are not overweight, do not consume alcohol, and adhere to
a consistent dietary routine.
5.3.4 Clinical characteristics:
● Glycemic efficacy: lowers HbA1c by 1.2% over 3 months.
● Long-term experience.
● Low-cost.
5.3.5 Important side effects:
● Life-threatening hypoglycemia.
● Increased risk in patients with renal failure.
● Weight gain.
● Hematological changes: granulocytopenia, hemolytic anemia.
● Allergic skin reactions.
● Alcohol intolerance.
● Compared to metformin, sulfonylureas are associated with more cardiovascular
(macrovascular) complications.
5.3.6 Contraindications:
● Severe cardiovascular comorbidity.
● Obesity.
● Sulfonamide allergy (particularly long-acting substances).
● Severe liver failure.
● Severe kidney failure.
5.4 Meglitinides (sulfonylurea analogue)
5.4.1 Active agents:
● Repaglinide: the leading agent in the class of meglitinides, which is well tolerated by
patients with chronic kidney disease
● Nateglinide
Page 9
10. Antidiabetic Drug 2019
5.4.2 Mechanism of action:
● Enhances insulin secretion (similar mechanism of action to that of
the sulfonylureas).
● Meglitinides should be taken shortly before meals.
5.4.3 Indications: particularly suitable for patients with postprandial peaks in blood glucose
levels.
5.4.4 Clinical characteristics:
● Glycemic efficacy: lowers HbA1c by 0.75% over 3 months.
● More expensive than sulfonylureas.
5.4.5 Important side effects:
● Life-threatening hypoglycemia (less risky than sulfonylureas).
● Increased risk in patients with renal failure.
● Weight gain.
● Hepatotoxicity (rare).
Page 10
11. Antidiabetic Drug 2019
5.4.6 Contraindications:
● Severe liver failure.
● Severe renal failure.
5.4.7 Interactions: Sulfonylureas.
5.5 Incretinmimetics (GLP-1 receptor agonists)
5.5.1 Active agents:
● Exenatide.
● Liraglutide: rapid-release formula that is administered daily.
● Albiglutide: extended-release formula that is administered once weekly.
● Dulaglutide.
5.5.2 Mechanism of action:
● Incretin effect:
1. Food intake.
2. Activation of enteroendocrine cells in the gastrointestinal tract.
3. Release of GLP-1.
4. GLP-1 degradation via the enzyme DPP-4.
5. End of the GLP-1 effect.
● Incretin mimetic drugs bind to the GLP-1 receptors and are resistant to
degradation by DPP-4 enzyme
● Increase insulin secretion, decrease glucagonsecretion, slow gastric emptying (↑
feeling of satiety, ↓ weight)
Page 11
12. Antidiabetic Drug 2019
5.5.3 Clinical characteristics:
● Glycemic efficacy: lowers HbA1c by 0.5–1.5% over 3 months
● Subcutaneous injection
● Weight loss
● No risk of hypoglycemia
5.5.4 Side effects:
● Gastrointestinal complaints (particularly impaired gastric emptying!)
● Increased risk of pancreatitis and potentially pancreatic cancer :
5.5.5 Contraindications:
● Preexisting symptomatic gastrointestinal motility disorders
● Chronic pancreatitis or a family history of pancreatic tumors
5.6 Dipeptidyl peptidase-4 inhibitors (gliptins)
5.6.1 Active agents:
● Sitagliptin
● Saxagliptin
5.6.2 Mechanism of action:
Page 12
13. Antidiabetic Drug 2019
● Gliptins indirectly increase the endogenous incretin effect by inhibiting the dipeptidyl
peptidase.
● 4 enzyme that breaks down glucagon-like peptide 1.
● Increased insulin secretion, decreased glucagon secretion, delayed gastric emptying.
5.6.3 Indications: Antihyperglycemic therapy algorithm for type 2 diabetes.
5.6.4 Clinical characteristics:
● Glycemic efficacy: lowers HbA1c by 0.5–0.75% over 3 months.No risk of
hypoglycemia unless insulin and/or insulinotropic drugs are used simultaneously.
5.6.5 Important side effects:
● Gastrointestinal complaints: diarrhea, constipation (milder than
in GLP-1 agonist exposure).
● Nasopharyngitis and upper respiratory tract infection.
● Arthralgia.
● Headaches, dizziness.
● Urinary infections (mild).
● Increased risk of pancreatitis.
● Acute renal failure.
Page 13
14. Antidiabetic Drug 2019
5.6.6 Contraindications:
● Hypersensitivity.
● Liver failure.
5.7 SGLT-2 inhibitors (gliflozins)
5.7.1 Active agents:
● Dapagliflozin
● Empagliflozin
● Canagliflozin
5.7.2 Mechanism of action:
● Reversible inhibition of the sodium-dependent glucose co-transporter (SGLT-2) in
the proximal tubule of the kidney.
● reduced glucose reabsorption in the kidney.
● glycosuria and polyuria.
5.7.3Indications: A treatment option used especially in young patients
with treatment-compliant type 2 DM without significant renal failure.
Page 14
15. Antidiabetic Drug 2019
5.7.4 Clinical characteristics:
● Glycemic efficacy: lowers HbA1c by 0.6% over 3 months.
● Promotes weight loss.
● Reduces blood pressure.
5.7.5 Important side effects:
● Urinary tract infections, genital infections (vulvovaginitis, balanitis).
● Dehydration as a result of polyuria.
● Severe diabetic ketoacidosis.
5.7.6 Contraindications:
● Chronic kidney disease.
● Recurrent urinary tract infections (e.g., in patients with anatomical or functional
anomalies of the urinary tract).
5.8 Alpha-glucosidase inhibitors
5.8.1 Active agents:
● Acarbose
● Miglitol
5.8.2 Mechanism of action:
● Inhibits alpha-glucosidase.
● Decreased intestinal glucose absorption.
● The drug is particularly effective in controlling postprandial blood glucose levels.
● The undigested carbohydrates reach the colon, where they are degraded by
intestinal bacteria, resulting in the production of intestinal gas.
Page 15
16. Antidiabetic Drug 2019
5.8.3 Clinical characteristics:
● Glycemic efficacy: lowers HbA1c by 0.8% over 3 months.
● No risk of hypoglycemia.
5.8.4 Important side effects: gastrointestinal complaints (flatulence, abdominal
discomfort, diarrhea).
5.8.5 Contraindications
● Inflammatory bowel disease.
● Conditions associated with malabsorption.
● Severe renal failure.
Page 16
17. Antidiabetic Drug 2019
References:
1. https://www.amboss.com/us/knowledge/Antidiabetic_drugs
2. American Diabetes Association. Diabetes Basics. Accessed 11/5/2018
3. MIMS. 2013. [12 December 2013]. Available from: http://www.mims.co.uk/
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