Obesity and Diabetes Flashcards
Risks of obesity
- Type 2 diabetes
- Cardiovascular diseases
- Osteoarthritis
- Hormone dependent cancers
- Respiratory problems
Types of Pharmacotherapy for obesity
- Appetite suppressors
- Lipase inhibitors
- Antidiabetic
- Combination preparations
Appetite suppressor drugs
- Phentermine
- Bupropion
- Sibutramine
- Amphetamine
- Lorcaserin
MOA of appetite suppressor drugs
Mostly inhibit reuptake of noradrenaline. could also target serotonin or dopamine which are important in modulation of satiety signals by stimulation of hypothalamic satiety center in the brain
Adverse effects of appetite suppressors
- Dry mouth
- Insomnia
- Increased HR and BP
- Constipation
Contraindication of appetite suppressors
- History of hypertension
- Cardiovascular disease
- Arrhythmia, heart failure, stroke
MOA of Lorcaserin and contraindication
- selective 5-HT receptor agonist decreasing appetite
- Serotonin syndrome, renal dysfunction
Lipase inhibitor
Orlistat
MOA of Orlistat and adverse effects
- irreversibly binds to serine residues on gastric and pancreatic lipases, Prevents breakdown of dietary fats to fatty acid and glycerol
- Oily spotting, flatulence with discharge, increased defecation
comment on the effects of Orlistant
- interferes with absorption of fat soluble vitamins ADEK
and with fetal development
Antidiabetic drugs
Metformin
Liraglutide
MOA of metformin
inhibits neuropeptide Y expression, reducing food intake and decreasing body weight
Adverse effects and contraindications of metformin
- GI disturbances, anorexia, metallic taste
- renal/hepatic insufficiency,
MOA of Liraglutide
Long-acting glucagon-like agonist, reduces gastric emptying, slowing the rate of nutrient absorption and reducing food intake
Adverse effects and contraindications of Liraglutide
- Hypoglycaemia, nausea, diarrhoea, constipation, headaches, kidney failure and fatigue
- pregnancy, gall bladder disease, thyroid abnormalities
Combination drugs
- Phentermine+ Topiramate
- Naltrexone
MOA of Phentermine and topiramate
-Phentermine: stimulant to counteract sedative effects of topiramate, and weight loss effects
- Topiramate anticonvulsant wit weight loss effects
Adverse effects of Phentermine and Topiramate and their contraindications
Topiramate: suicidal ideation, cognitive dysfunction
Phentermine: Increases HR
- Pregnancy, Hypertension, diabetes
MOA of naltrexone
is a u receptor antagonist, results appetite suppression
Adverse effects and contraindication of naltrexone
- nausea constipation, headache, dizziness, insomnia, dry mouth
- Epilepsy, hypertension
Metabolic disorders leading to diabetes
- Deceased carbohydrate metabolism
- Increased protein and lipid metabolism
DM symptoms
- Exceed renal glucose threshold
- polyuria
- dehydration (polydipsia)
- amyotrophy
DM associated complications
- nephropathy
- hypertension
- peripheral neuropathy
- Myocardial infarction
- sorbitol-induced cataracts
Insulin types
porcine
bovine
Insulin plasma half-life
10 mins
What is inulin combined with to aid glucose absorption and how does it help
- pramlintide
- slows down gastric emptying
Short acting insulin types
-Insulin lispro
-Insulin aspart
- Insulin glulisine
Intermediate acting insulin types
- crystalline insulin zinc
- Insulin isophane
Long acting insulin
- Insulin glargine
- Insulin detemir
Oral hypoglycaemics
- Biguanides
- Thiazolidinediones
- sulfonylureas
- alpha- glucosidase inhibitors
- GLP-1 agonist
Drug in biguanide class and its MOA
- Metformin
- Reduces hepatic glucose production, increases glucose uptake and utilization in skeletal muscle. Reducing LDL and VLDL. Prevents hyperglycaemia
what do biguanides do and what are the adverse effects
- Sensitizers: increase peripheral glucose uptake
- anorexia, metallic taste
Drug in class thiazolidinedione and its MOA
- Pioglitazone
- bind PPARG, leading to improved insulin sensitivity and beta cell function. Enhance fatty acid and glucose uptake
Function of thiazolidinediones and their adverse effects
- sensitizers: Increase peripheral glucose uptake
- peripheral oedema, increased subcutaneous fat, water retention
which thiazolidinediones were withdrawn and why
- Troglitazone and Rosiglitazone
- due to toxicity
Drugs in class sulfonylureas and their MOA
- Tolbutamide, tolazamide, chlorpropamide, acetohexamide
- Bind to sulfonylurea receptor(Katp) on beta cell mem. Blocking Katp depolarizes cell mem, causing Ca2+ influx and insulin release. Maintaining high insulin, enhancing glucose uptake and reducing hepatic glucose production
Function of sulfonylureas and their Adverse effects
- Secretagogues: increase insulin secretion
- Hypoglycaemia, weight gain, GI disturbances, jaundice, nausea
Drugs in class meglitinides and their MOA
- Repaglinide, nateglinide
- short acting secretagogues acting on Katp channels. Taken before meals, increase Ca2+ influx increase insulin release. Maintaining high insulin levels and enhancing glucose uptake. But are less effective than sulfonylureas
Adverse effects of meglitinides
Hypoglycaemia and weight gain
Drugs in class alpha-glucosidase inhibitors and their MOA
- Acarbose
- Reversibly inhibits intestinal alpha-glucosidase, which is responsible for hydrolysis of oligosaccharides to glucose. This results in the delayed digestion of carbohydrates and starch in the small intestines
Function and adverse effects of alpha-glucosidase inhibitors
- delay carbohydrate digestion
- fermentation of starch, leading to flatulence, diarrhoea
Drugs in class SGLT2 and their MOA
- Empagliflozin, Dapagliflozin
- block re-uptake of glucose and sodium that has been filtered through the kidneys, Results in excess glucose and sodium excretion. good for hypertension
Adverse effects of SGLT2
- Urinary and genital infections
Drug names in class Dipeptidyl peptidase inhibitors(DPP-IV) and their MOA
- Sitagliptin, saxagliptin
- inhibit DPP-IV. DPP-IV inactivated incretin hormones. Increased incretin inhibit glucagon and increase insulin decreasing gastric emptying and blood glucose
Function and adverse effects of DPP-IV inhibitors
- incretin mimetics
- headache
- contraindicated in pancreatic cancer, severe liver disease and heart disease
Drugs in class glucagon-like peptide-1 and their MOA
- Exenatide, Liraglutide
- If glucose levels are elevated it increases insulin secretion and inhibits glucose release
Function and adverse effects of GLP-1
- Incretin mimetics
- GI disturbances, diarrhoae, constipation, headache, dizziness
