Diabetes Drugs Flashcards
Insulin secretagogues
Sulfonylureas Meglitinides Phenylalanine derivatives Biguanides Thiazollidinediones (TZDs) DPP-IV Inhibitors Bile acid sesquestrants Dopamine Agonist GLP-1 Agonist Amylin Agonist
Sulfonylureas
Target fasting glucose
First gen:
Tolbutamide (Orinase)
Tolazamide (Tolinase)
Chlorpropamide ( Diabinese)
Sec Gen:
Glyburide (DiaBeta, Glynase)
Glipizide (Glucotrol)
Glimepride (Amaryl)
Meglitinides
Repagli nide (Prandin)
Phenylalanine Derivatives
Nateglinide
Starlix
Thia zolidine diones
TZDs
Pio glitazone. (Actos) Rosi glitazone (Avandia)
a Glucosidase Inhibitors
Acarbose (Precose)
Miglitol (Glyset)
DPP-IV Inhibitors
Sitagliptin (Januvia)
Saxagliptin (Onglyza)
Linagliptin (Tradenta)
Bile Acid Sesquestrants
Colesevelam (Welchol)
Dopamine Agonist
Bromocriptine (Cycloset)
GLP-1 Agonist
Exenatide (Byetta)
Liraglutide (Victoza)
Amylin Agonist
Pramlintide (Symlin)
Sulfonylureas adverse effects 1st gen
Thrombocytopenia
Agranulocytosis
Hemolytic anemia
Hyponatremia
SIADH (Syndrome of Inappropriate Antidiuretic Hormone Secretion)
Disulfiram like reaction (adverse reaction to alcohol causing nausea vomiting, throbbing headache, chest and abdominal pain hangover feeling)
Secretagogues mech
Stimulates enhanced secretion of insulin from B cells
Reduces hepatic glucose output
Secretagogues indication and contra
Indication:
T2DM only
Contraindications:
Severe renal or hepatic dysfunction
Elderly caution
Biguanides
Metformin
( Glucophage, Glucophage XR, Fortamet, Glumetza, Riomet)
Glycemic management of T1DM & T2DM
Metformin contraindication
Renal disease (potential for accumulation and causing Lactic Acidosis) Discontinued in Scr > 1.4 mg/dL for female Scr > 1.5 mg/dL males
Hepatic impairment
Heart fail
Intravascular iodinated contrast media
Metformin mech
Inhibits hepatic glucose output
Promote Glucose uptake by fat and muscles
Decreasing intestinal absorption of glucose (minor)
Side effects Metformin
30% GI effects self limiting over 1 to 2 weeks
Minimal weight loss
Reduces B12 levels
Sweating and metallic taste
TZDs indication
Contraindications
T2DM
Contra:
Hepatic dysfunction
Class III / IV HF
Anemia (plasma volume expansion , so decrease in haemoglobin and hematocrit)
Fracture risk (distal upper limbs female)
Rosi glitazone increased risk if CVS effects
Pio glitazone bladder Cancer risk
TZDs mech of action
Promotes glucose uptake by fat & muscles & inhibit hepatic glucose output by stimulation of peroxisome - proliferator-activated receptor gamma (PPAR-y)
TZDs side effects
Weight Gain Fluid retention Fat accumulation Shortness of breath Swelling of lower extremities Max effectiveness not seen until 6 to 12 weeks of use.
a Glucosidase Inhibitors
Contraindications
Inflammatory Bowel disease Colonic ulceration Obstructive Bowel disorders Serum > 2.0 mg/dL Hepatic impairment
a Glucosidase Inhibitors
Mech
Competitive inhibition of alpha Glucosidases, in intestinal brush border , slower Absorption of complex carbs
a Glucosidase side effects
Flatulence
Should be taken with meal
Hypoglycemia
GI effects (lessen over time)
Dipeptidyl peptidase - IV (DPP-IV) Inhibitors
T2 DM
Contra:
Pancreatitis
T1DM (glucose dependant insulin secretion)
DPP-IV Inhibitors mech
Prevent inactivation of incretin hormones (GLP-I) by enzyme DPP-IV.
GLP-I works to stimulate insulin secretion and decrease glucagon Secretion from pancreas during hyperglycemia.
Bile acid sesquestrants detail
Cholesevelam
Adjunctive therapy for T2DM
Contra: in patients with History of bowel obstruction Hpertriglyceridemia-induced pancreatitis Serum triglycerides above > 500 mg/dL Gastroperesis
Oral meds should be taken 1 hr before or 4hr after cholesevelam
Constipation can occur
Dopamine agonist detail
Bromocriptine
Adjunct therapy for T2DM
Contra in patients with CVS issues Dementia Psychosis Peptic ulcer
May cause fatigue, GI discomfort
Available oral combos
Metformin/glyburide (Glucovance) M/glipizide (metagliptin) M/Rosiglitazone (avandament) M/pioglitazone (Actoplus Met) M/Repaglinide (PrandiMet) M/Saxagliptin (Kombiglyze) M/Sitagliptin (Janumet) Rosi/ glimepride (Avandaryl) Pio/ gilmepride (Duetact)
Incretin Mimetics detail
Exenatide (Byetta)
Liraglutide (Victoza)
T2DM
Contra in patients with Gastroperesis Pancreatitis Renal hepatic impairment Medullary thyroid carcinoma MTC Multiple Endocrine Neoplasia Syndrome type 2 (MEN2)
Incretin Mimetics mech
Increase glucose dependant insulin secretion Decrease hepatic glucose output Increase B cell growth & replication Slow gastric emptying Enhance satiety
Amylin Agonist detail
T1DM T2DM
Contra in patients with:
Gastroperesis
Mech: slow gastric emptying
Emergency treatment options
Once weekly exenatide (Bydureon)
Sodium Glucose Transporter 2 (SGLT2)
Exenatide emergency treatment
Dose once weekly as a 2mg subcutaneous injection
Targets all over Blood glucose rather than just post parendial
6 weeks to hit steady state
Sodium Glucose Transporter 2 Inhibitor
SGLT2 is a transporter in kidney
Responsible for 90% renal glucose reabsorption
Inhibits transporter thus increase kidney excretion of Glucose
Insulin independent mechanism
No hypoglycemia
Dapa gliflozin
Ser gliflozin
Remo gliflozin
