ANTIDM DRUGS Flashcards
Insulin causes translocation of glucose transporters (GLUT4) to the cell membrane. This leads to (3)
- increase glucose uptake
- increase in glycogen synthase activity
- increased glycogen formation
Effects of Insulin
- increase glycogen and protein synthesis
- decreased protein catabolism
- increased TG storage
Duration of Action of Intermediate Acting Insulin
18-24hrs
peak: 8-12hrs
Duration of Action of Rapid Acting Insulin
3-4hrs
Duration of Action of Short Acting Insulin
5-7hrs
Duration of Action of Long Acting Insulin
18-28hrs
Rapid Acting Insulin Peak
0.25-0.5hrs
Short Acting Insulin Peak
0.5-3hrs
Intermediate Acting Insulin Peak
8-12hrs
Long Acting Insulin Peak
8-16hrs
Initiation of insulin therapy causes activation of residual pancreatic beta cells
Honeymoon Period
At Risk for Insulin-related Hypoglycemia
Advanced Renal Disease, Elderly, Children <7y
RAPID ACTING INSULIN
Mabilis. Walang L. A. G.
Lispro
Aspart
Glulisine
SHORT ACTING INSULIN
Tao lang. Regular lang.
Regular (Humulin R)
LONG ACTING INSULIN
ULTRA bilis
ULTRALENTE
ULTRA-LONG ACTING
Mas mabilis sa ULTRAlente yung DETERMINED.
DETEMIR
Glargine
Lantus
INSULIN SECRETAGOGUES
Sulfonylureas
Meglitinides
(increases insulin secretion)
MOA: INSULIN SECRETAGOGUES
increases insulin secretion by closing ATP-sensitive K+ channels
(requires islet cell function)
1st Generation SU
T. A. C. T.
Tolazamide
Acetohexamide
Chlorpropamide
Tolbutamide
2nd Generation SU
5Gs
Glipizide Glyburide Glimepiride Glibenclamide Gliclazide
MEGLITINIDES
- glinides, -glitinide
MEGLITINIDE
REPAGLINIDE
NATEGLINIDE
MITIGLINIDE
SU with SE-cholestatic jaundice
Glibenclamide
SU with least hypoglycemic SE
Meglitinides
INSULIN SENSITIZERS
BIGUANIDES
THIAZOLIDINEDIONES
MOA: BIGUANIDES
Metformin
activates AMP-stimulated protein kinase leading to inhibition of hepatic and renal gluconeogenesis
MOA: THIAZOLIDINEDIONES
-glitazone
regulates gene expression by binding PPAR Alpha and PPAR Gamma»_space;
- increases tissue sensitivity,
- increase glucose uptake in muscle and adipose
- inhibits hepatic gluconeogenesis, - effects on lipid metabolism and distribution of body fat
- control of fasting and postprandial glucose
Other Effects of Biguanides
- stimulate glucose uptake and glycolysis in peripheral tissues
- slows glucose absorption from the GIT
- reduced plasma glucagon levels
- reduced risk of DM in high risk patients
- reduced post prandial and fasting glucose
DOC for obese diabetics
Metformin
Contraindicated in hepatic and renal disease
Metformin
A decrease in endogenous insulin production by increasing insulin sensitivity of tissues
Insulin Sparing Effect
Anti - DM drug that does not cause hypoglycemia
Metformin
Thiazolidinediones are contraindicated in
pregnant, with chronic liver disease and with CHF
Rosiglitazone binds to both PPAR alpha and PPAR gamma. TRUE OR FALSE.
FALSE
binds only to PPAR alpha
Thiazolidinedione - that increases risk for MI
Rosiglitazone
Thiazolidinedione - that increases risk for Bladder CA
Pioglitazone
Thiazolidinedione - that increases risk for CHF
Rosiglitazone, Troglitazone
ALPHA GLUCOSIDASE INHIBITORS
M. A. V.
MIGLITOL
ACARBOSE
VOGLIBOSE
AMYLIN ANALOG
PRAMLINTIDE
INCRETIN MODULATORS
GLP - 1 AGONISTS
DPP4 INHIBITORS
GLP - 1 AGONISTS
- tide
Exenatide Liraglutide Lixisenatide Semaglutide Dulaglutide
DPP4 INHIBITORS
-GLIPTINS
sitagliptin saxagliptin linagliptin vildagliptin teneligliptin
SGLT2 INHIBITORS
-gliflozin
Dapagliflozin
Empagliflozin
Canagliflozin
MOA: ACARBOSE, MIGLITOL, VOGLIBOSE
inhibits intestinal alpha glucosidase (decrease glucose absorption - decrease post prandial glucose)
MOA: PRAMLINTIDE
activates amylin receptors
- reduce postmeal glucose excursions
- suppresses glucagon release
- delay gastric emptying time
- reduces appetite (anorectic effect)
MOA: EXENATIDE, LIRAGLUTIDE
activates GLP - 1 receptors
augments glucose-stimulated insulin release from pancreatic B cells
- reduce postmeal glucose excursions
- suppresses glucagon release
- delay gastric emptying time
- reduces appetite (anorectic effect)
MOA: SITAGLIPTIN, LINAGLIPTIN
inhibits DPP4 that degrades GLP-1 and other incretins»_space; raises circulating GLP-1 levels
augments glucose-stimulated insulin release from pancreatic B cells
- reduce postmeal glucose excursions
- suppresses glucagon release
- delay gastric emptying time
- reduces appetite (anorectic effect)
MOA: DAPAGLIFLOZIN, EMPAGLIFLOZIN
inhibits SGLT2 transporter
|»_space; inhibits reabsorption of glucose in the kidneys»_space; increased excretion
Anti DM drug with possible risk of Thyroid CA
Liraglutide
Increases incidence of UTI
SGLT 2 INHIBITORS
Bile Acid Sequestrant that can lower glucose levels
Colesevelam
DRUGS FOR OBESITY
Orlistat
Sibutramine
Rimonabant
MOA: ORLISTAT
inhibits gastric and pancreatic lipases
reduces absorption of fats
MOA: SIBUTRAMINE
inhibits NEP and sertonin reuptake
reduces appetite
MOA: RIMONABANT
Selectively blocks cannabinoid-1 receptors
reduces appetite
Which of the following drugs for obesity increases risk for suicide and depression?
RIMONABANT
Which of the following drugs for obesity increases risk for cardiovascular events?
SIBUTRAMINE
Which of the following drugs for obesity increases risk for malabsoption of fat soluble vitamins?
Orlistat
Orlistat is contraindicated in
pregnancy, hepatobiliary function and malabsorption states
Which of the following drugs for obesity increases risk for rebound weight gain upon discontinuation?
Orlistat
Glucagon can be used in?
Severe hypoglycemia, Beta Blocker overdose
